Browse result page of ThPDB2


This is the result page of the browse module of ThPDB2. This page gives the information about the query submitted by the user as per the browse category. Further details of the entries can be seen by clicking on the ID or THPP_ID. Further the user can sort the entries on the basis of various fields by clicking on the respective headers. The user can also download the results in various formats.




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IDTHPP_IDTherapeutic NameSequenceMolecular WeightChemical FormulaIsoelectric PointHydrophobicityMelting PointHalf LifeDescriptionDisease/IndicationPharmacodynamicsMechanism of ActionToxicityMetabolismAbsorptionVolume of DistributionClearanceCategoriesPatent NumberDate of IssueDate of ExpiryDrug InteractionTargetBrand NameCompanyBrand DescriptionPrescribed forChemical NameFormulationPhysical AppearanceRoute of AdministationRecommended DosageContraindicationSide EffectsUseful Links 1Useful Links 2Remarks
10032Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NANormal renal function: 0.42 hours (in normal conditions)Bivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kg3.4 mL/min/kg [Normal renal function]Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsUS75827271-Sep-200927-Jul-2028Deferasirox, Anticoagulants increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.ProthrombinAngiomaxSandoz Canada Incorporated, The Medicines Company,Cardinal Health, Sandoz IncSandoz Canada Incorporated, The Medicines Company,Cardinal Health, Sandoz IncIt is used for thinning the blood in patients with unstable angina who are undergoing percutaneous transluminal coronary angioplasty (PTCA) and in patients undergoing percutaneous coronary intervention (PCI).D-phenylalanyl-L-prolyl-L-arginyl-L-prolyl-glycylglycyl-glycyl-glycyl-L-asparagyl-glycyl-L-aspartyl-L-phenylalanyl-L-glutamyl-L-glutamyl-L-isoleucyl-L-prolyl-L-glutamyl-L-glutamyl-L-tyrosyl-L-leucine trifluoroacetate (salt) hydrateEach vial contains 250 mg bivalirudin, 125 mg mannitol, and sodium hydroxide to adjust the pH to 5-6 (equivalent of approximately 12.5 mg sodium). When reconstituted with Sterile Water for Injection, the product yields a clear to opalescent, colorless toSupplied in single-use vials as a white lyophilized cakeIntravenous infusionIntravenous (IV) bolus dose of 0.75 mg/kg, followed by an infusion of 1.75 mg/kg/h for the duration of the PCI/PTCA procedure.Allergic and have major active bleedingAnxiety; back, stomach, or pelvic pain; headache; nausea; nervousness; pain at the injection site; trouble sleeping; upset stomach; vomiting. And severe side effect may include Severe allergic reactions (rash; hives; itching; difficulty breathing.LinkNANA
10033Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NACreatinine clearance 10-29mL/min: 0.95 hoursBivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kg3.4 mL/min/kg [mild renal function]Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsUS519640423-Mar-199315-Dec-2014Gemcitabine, Gemcitabine may enhance the adverse/toxic effect of Bleomycin. The risk of pulmonary toxicity may be increased. Use extreme caution if using gemcitabine and bleomycin in combination. Monitor for the development of pulmonary toxicityNAAngioxThe Medicines Company UK LtdThe Medicines Company UK LtdUsed as an anticoagulant in adult patients undergoing percutaneous coronary intervention (PCI), including patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary PCI. Angiox is also indicated for the treatment of adult patientsNAEach vial contains 250 mg bivalirudin.Powder for concentrated solutionInjection0.75 mg/kg IV bolus, initially, followed by continuous infusion at rate of 1.75 mg/kg/hr for duration of procedureHypersensitivity, active bleeding or increased risk of bleeding because of haemostasis disorder or irreversible coagulation disorder, uncontrolled hypertension, subacute bacterial endocarditis, severe renal impairment and in dialysis dependent pateints,NALinkNANA
10034Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NADialysis-dependant patients: 3.5 hoursBivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kg2.7 mL/min/kg [moderate renal function]Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsCA206515014-Dec-199917-Aug-2010Ginkgo biloba, Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.NANANANANANANANANANANANALinkNANA
10035Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NANABivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kg2.8 mL/min/kg [severe renal function]Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsNANANARivaroxaban, Anticoagulants may enhance the anticoagulant effect of rivaroxaban. Avoid concurrent use of rivaroxaban with other anticoagulants whenever possible, other than during transition periods, due to the possible increased for bleeding.NANANANANANANANANANANANALinkNANA
10036Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NANABivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kg1 mL/min/kg [Dialysis-dependent patients]Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsNANANATreprostinil, The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.NANANANANANANANANANANANALinkNANA
10037Th1006Bivalirudin>Th1006_Bivalirudin FPRPGGGGNGDFEEIPEEYL 2180.285C98H138N24O333.91-0.985NANABivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.Bivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.Inhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.Based on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.80% proteolytic cleavageBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.0.2L/kgNAAmino Acids, Peptides, and Proteins, Anticoagulants, Antithrombins, Blood and Blood Forming Organs, Enzyme Inhibitors, Hematologic Agents, Peptides, Protease Inhibitors, Serine Protease Inhibitors, Thrombin InhibitorsNANANANANANANANANANANANANANANANANANANA
10038Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature puberty.Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANAGonadotropin-releasing hormone receptorEligardAtrix Labs/QLT InAtrix Labs/QLT InEligard is used to treat the symptoms of prostate cancer in men.5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-arginyl-N-ethyl-L-prolinamide acetateELIGARD is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the ATRIGEL DeSuspensionSubcutaneous Injection7.5mg-1 injection/month, 22.5mg-1 injection per 3 month, 30mg-1 injection per 4 month, 45 mg- 1 injection every 6 month.Hypersensitivity and pregnancyRare pain or unusual sensations in your back; numbness, weakness, or tingly feeling in your legs or feet; muscle weakness or loss of use; loss of bowel or bladder control; or liver problems - nausea, upper stomach pain, itching, tired feeling, loss of apetite.LinkNANA
10039Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANAEnantoneTakedaTakedaNANANASolutionInjectionOne3.75 mg DPS mnthly or one 11.25 mg DPS every 3 month as a single SC/IM injection.Hypersensitivity, undiagnosed abnormal vag bleeding, pregnancy, lactationWeightloss, Parosmia (distortion of the sense of smell, as in smelling odours that are not present), Nausea (feeling of having an urge to vomit), Musculoskeletal Stiffness (stiffness of the body's muscles, joints, tendons, ligaments and nerves), Mood Swinng.LinkNANA
10040Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANALeuplinCardinal HealthCardinal HealthNANANANAInjectionNANANALinkNANA
10041Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANALeuProMaxxBaxter/TevaBaxter/TevaNANANANANANANANALinkNANA
10042Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANALeupromerOso Biopharmaceuticals Manufacturing LLCOso Biopharmaceuticals Manufacturing LLCNANANANAInjectionNANANALinkNANA
10043Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANALupronAbbott/TAP PharmaceuticalsAbbott/TAP PharmaceuticalsNANANANAInjection7.5 mg for 1-month, 22.5 mg for 3-month, 30 mg for 4-month, and 45 mg for 6-month administration are prescribed for the palliative treatment of advanced prostate cancer, 3.75 mg for 1-month and 11.25 mg for 3-month administration are used for the manageme.Allergic, pregnancy, lactationNALinkNANA
10044Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANALutrateHospira Inc.Hospira Inc.NANANANANANANANALinkNANA
10045Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANAMemryteCuraxisCuraxisNANANANANANANANALinkNANA
10046Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANAProstap 3Sanofi-Aventis Inc. , Sun Pharmaceutical Industries Ltd. , Takeda Pharmaceutical Co. Ltd. , Teva Pharmaceutical Industries Ltd. , Tolmar Inc.Sanofi-Aventis Inc. , Sun Pharmaceutical Industries Ltd. , Takeda Pharmaceutical Co. Ltd. , Teva Pharmaceutical Industries Ltd. , Tolmar Inc.NANANANANANANANALinkNANA
10047Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANAProstap SR, Camcevi, Fensolvi, Lupaneta Pack 1-month, Lupron, Lupron Depot-ped, Zeulide DepotTakeda UK Limited, Eon Labs, Physicians Total Care Inc.Takeda UK Limited, Eon Labs, Physicians Total Care Inc.NANANANANANANANALinkNANA
10048Th1007Leuprolide>Th1007_Leuprolide PHWSYLLR 1209.398C59H84N16O12NA0.1NAApproximately 3 hoursLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).To treat prostate cancer, endometriosis, uterine fibroids and premature pubertyLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.Subcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is aPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).Bioavailability by subcutaneous administration is comparable to that by intravenous administration.27 L [intravenous bolus administration to healthy male volunteers]Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]Adrenal Cortex Hormones, Agents Causing Muscle Toxicity, Amino Acids, Peptides, and Proteins, Antineoplastic Agents, Antineoplastic Agents, Hormonal, Antineoplastic and Immunomodulating Agents, Drugs causing inadvertant photosensitivity, Drugs that are Mainly Renally Excreted, Endocrine Therapy, Fertility Agents, Fertility Agents, Female, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Gonadotropin-releasing hormone agonist, Gonadotropins, Hormones and Related Agents, Hyperglycemia-Associated Agents, Hypothalamic Hormones, Moderate Risk QTc-Prolonging Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptides, Photosensitizing Agents, Pituitary Hormone-Releasing Hormones, Proteins, QTc Prolonging Agents, Reproductive Control AgentsNANANANANAViadurBayer AGBayer AGNA5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-Lleucyl-L-arginyl-N-ethyl-L-prolinamide acetateNANANANANANALinkNANA
10187Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANANeosporinPfizerPfizerNeosporin ointment is an antibiotic combination which works by killing sensitive bacteria on the skin or in wounds.Thus, treating and preventing infection due to minor cuts, scrapes, and burns.NAEach gram contains: neomycin sulfate equivalent to 3.5 mg neomycin base, polymyxin B sulfate equivalent to 10,000 polymyxin B units, bacitracin zinc equivalent to 400 bacitracin units, and white petrolatum, q.s.OintmentExternal use onlyApply the ointment every 3 or 4 hours for 7 to 10 days depending on the severity of the infection.Individuals who have shown hypersensitivity to any of its componentsRash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; skin irritation, pain, burning, cracking, redness, or peeling not present before using Neosporin ointment; worsening or recurrence of wound symptoms.LinkNANA
10188Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANANANANANANANANANANANANALinkNANA
10189Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANANANANANANANANANANANANALinkNANA
10190Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANASofradexSanofiSanofiUsed in the eye(s) to treat Inflammation in the eye when prevention of bacterial infection is also needed. Signs include sore, red or swollen eyes. It is used in the ear(s) to treat Inflammation of the ear canal (otitis externa)NAEach bottle contains 0.5% w/v of Framycetin Sulphate, Dexamethasone Sodium Metasulphobenzoate (equivalent to 0.050% w/v of Dexamethasone) and 0.005% w/v of Gramicidin. The other ingredients are citric acid, sodium citrate, lithium chloride, phenylethyl alSterile, clear, bright, colourless, aqueous solutionAuricular and Ocular use.One or two drops applied to each affected eye up to six times daily or more frequently if required. Two or three drops instilled into the ear three or four times daily.If glaucoma is present or herpetic keratitis (e.g. dendritic ulcer) is considered a possibility. Otitis Externa should not be treated when the eardrum is perforated because of the risk of ototoxicity. Hypersensitivity to framycetin sulphate, dexamethasone sodium metasulphobenzoate, gramicidin or to any of the excipients.Stop using Sofradex if: You get any kind of skin problem, such as a rash or itching around your eyes or irritation burning, stinging, itching or swelling, your eyes have problems focussing or develop a blind spot. You may have increased pressure in the eye, you have difficulty seeing at night or notice that your eyesight is cloudy and fuzzy, or you see halos around lights. These could be signs of cataracts. This may occur after using the medicine for a long timeLinkNANA
10191Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANANANANANANANANANANANANALinkNANA
10192Th1024Gramicidin D>Th1024_Gramicidin_D VGALAVVVWLWLWLWX 1811.253C96H135N19O16NANA229NAGramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form an alpha helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution.For treatment of skin lesions, surface wounds and eye infectionsGramicidin is particularly effective against gram-positive bacteria because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solutionGramicidin D binds and inserts itself into bacterial membranes (preference to gram-positive cell membranes) resulting in membrane disruption and permeabilization (it acts as a channel). This leads to loss of intracellular solutes (e.g., K+ and amino acids); dissipation of the transmembrane potential; inhibition of respiration; a reduction in ATP pools; and inhibition of DNA, RNA, and protein synthesis, which leads to cell death.NANANANANAAmino Acids, Peptides, and Proteins, Anti-Bacterial Agents, Anti-Infective Agents, Anti-Infective Agents, Local, Membrane Proteins, P-glycoprotein inhibitors, P-glycoprotein substrates, Peptides, Peptides, Cyclic, Pore Forming Cytotoxic Proteins, Proteins, Throat PreparationsNANANANANANANANANANANANANANANANALinkNANA
10363Th1052Eptifibatide>Th1052_Eptifibatide CXGDWPC831.962C35H49N11O9S2NA-2.3NAApproximately 2.5 hoursSynthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.For treatment of myocardial infarction and acute coronary syndrome.Eptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets.Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous Intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis).No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%.NA55 mL/kg/h [patients with coronary artery disease]Amino Acids, Peptides, and Proteins, Antiplatelet agents, Blood and Blood Forming Organs, Decreased Platelet Aggregation, Hematologic Agents, Peptides, Peptides, Cyclic, Platelet Aggregation Inhibitors Excl. HeparinUS670668116-Mar-200416-Mar-2021NALutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor, Integrin beta-3, Voltage-dependent N-type calcium channel (Protein Group)INTEGRILINSchering-Plough/EssexSchering-Plough/EssexAcute Coronary Syndrome (ACS), Percutaneous Coronary Intervention (PCI)N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-Llysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic (1→6)-disulfide.Each 10-mL vial contains 2 mg/mL of INTEGRILIN and each 100-mL vial contains either 0.75 mg/mL of INTEGRILIN or 2 mg/mL of INTEGRILIN. Each vial of either size also contains 5.25 mg/mL citric acid and sodium hydroxide to adjust the pH to 5.35.INTEGRILIN Injection is a clear, colorless, Sterile, non-pyrogenic solution of EptifibatideInjection Solution for Intravenous UseDosage in Acute Coronary Syndrome (ACS): 180 mcg/kg intravenous (IV) bolus as soon as possible after diagnosis, followed by continuous infusion of 2 mcg/kg/min Dosage in 180 mcg/kg IV bolus immediately before PCI followed by continuous infusion of 2 mcg/kg/min and a second bolus of 180 mcg/kg (given 10 minutes after the first bolus).1. Severe hypertension (systolic blood pressure > 200 mm Hg or diastolic blood pressure > 110 mm Hg) not adequately controlled onantihypertensive therapy. 2. History of stroke within 30 days or any history of hemorrhagic stroke. 3. Current or planned administration of another parenteral GP IIb/IIIa inhibitor. 4.Hypersensitivity to INTEGRILIN or any component of the product (hypersensitivity reactions that occurred included anaphylaxis and urticaria).Bleeding, Intracranial Hemorrhage and Stroke, Immunogenicity/Thrombocytopenia.LinkNANA
10364Th1052Eptifibatide>Th1052_Eptifibatide CXGDWPC831.962C35H49N11O9S2NA-2.3NAApproximately 2.5 hoursSynthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.For treatment of myocardial infarction and acute coronary syndrome.Eptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets.Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous Intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis).No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%.NA56 mL/kg/h [patients with coronary artery disease]Amino Acids, Peptides, and Proteins, Antiplatelet agents, Blood and Blood Forming Organs, Decreased Platelet Aggregation, Hematologic Agents, Peptides, Peptides, Cyclic, Platelet Aggregation Inhibitors Excl. HeparinUS576725116-Jun-199816-Jun-2015NANANANANANANANANANANANANANANANA
10375Th1056Vasopressin>Th1056_Vasopressin CYFQNCPRG 2140.46C92H130N28O24S4NA-4.9NA10-20 minutesAntidiuretic hormone, also known as vasopressin, is a nine amino acid peptide secreted from the posterior pituitary. Antidiuretic hormone binds to receptors in the distal or collecting tubules of the kidney and promotes reabsorbtion of water back into the circulation.For the treatment of enuresis, polyuria, diabetes insipidus, polydipsia and oesophageal varices with bleedingVasopressin is an antidiuretic hormone indicated for the prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows, and in diabetes insipidus. Vasopressin can cause contraction of smooth muscle of the gastrointestinal tract and of all parts of the vascular bed, especially the capillaries, small arterioles and venules. It has less effect on the smooth musculature of the large veins. Vasopressin may also be used to control bleeding in some forms of von Willebrand disease and to treat extreme cases of bed wetting in children. It may also play a role in memory formation although the mechanism is unknown.Vasopressin acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of vasopressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.Vasopressin overdose is expected to present with consequences related to excessive vasoconstriction of peripheral, mesenteric, coronary vascular beds, hyponatremia, and possibly with ventricular tachyarrhythmias, rhabdomyolysis, and gastrointestinal symptoms. As vasopressin is rapidly metabolized and cleared, symptoms will resolve with cessation of vasopressin administration.The majority of a dose of vasopressin is metabolized and rapidly destroyed in the liver and kidneys.NANAVasopressin has a clearance of 9-25 mL/min/kg in patients with vasodilatory shock receiving 0.01-0.1 U/min of vasopressin.Amino Acids, Peptides, and Proteins, Antidiuretic Agents, Arginine Vasopressin, Arginine Vasopressin, analogs & derivatives, Cardiovascular Agents, Coagulants, Decreased Diuresis, Hematologic Agents, Hemostatics, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Natriuretic Agents, Nerve Tissue Proteins, Neuropeptides, Oligopeptides, Peptide Hormones, Peptides, Pituitary, Pituitary Hormones, Pituitary Hormones, Posterior, Proteins, Vasoconstriction, Vasoconstrictor Agents, Vasopressin and Analogues, VasopressinsNANANANAVasopressin V2 receptor,Vasopressin V1a receptor,Vasopressin V1b receptor, Oxytocin receptorPitressinJHP PharmaceuticalsJHP PharmaceuticalsVasopressin is indicated for prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows, and in diabetes insipidus.NAVasopressin 20 units, Sodium Chloride 9 mg, Chlorobutanol 0.5% (as a preservative), Water for Injection q.s. pH (range 2.5 - 4.5) adjusted with Acetic Acid.Vasopressin Injection, USP is a Sterile, aqueous solution of synthetic vasopressin (8-L-arginine vasopressin) of the posterior pituitary glandintramuSubcutaneousular or Subcutaneous useFor Abdominal Distention, Abdominal Roentgenography, Diabetes Insipidus: Ten units of vassopressin (0.5mL) will usually elicit full physiologic response in adult patients.Anaphylaxis or hypersensitivity to the drug or its components.anaphylaxia (cardiac arrest), circumoral pallor, arrhythmias, decreased cardiac output, angina, myocardial ischemia, peripheral vasoconstruction and gangrene, nausea, vomiting, tremor, vertigo, bronchial constrictionLinkNANA
10476Th1087Oxytocin>Th1087_Oxytocin CYIQNCPLG 1007.187C43H66N12O12S25.51-2.7192-194 ℃1-6 min9-residue cyclic peptide, synthetically prepared to avert possible contamination with vasopressin and small polypeptidesTo assist in labor, elective labor induction, uterine contraction inductionUsed to induce labor or to enhance uterine contractions during labor. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+-dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+, which in turn activates myosins light chain kinase.. Oxytocin has specific receptors in the muscle llining of the uterus and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term.Binds the oxytocin receptor which leads to an increase in intracellular calcium levels. The oxytocin-oxytocin receptor system plays an important role as an inducer of uterine contractions during parturition and of milk ejection.Administration of supratherapeutic doses of exogenous oxytocin can lead to myocardial ischemia, tachycardia, and arrhythmias. High doses can also lead to uterine spasms, hypertonicity, or rupture. Oxytocin has antidiuretic properties, thus, high daily doses (as a single dose or administered slowly over 24 hours) may lead to extreme water intoxication resulting in maternal seizures, coma, and even death. The risk of antidiuresis and water intoxication in the mother appears to be greater when fluids are given orallyOxytocin is rapidly removed from the plasma by the liver and kidney. The enzyme oxytocinase is largely responsible for the metabolism and regulation of oxytocin levels in pregnancy and only a small percentage of the neurohormone is excreted in the urine unchanged.Oxytocinase activity increases throughout pregnancy and peaks in the plasma, placenta and uterus near term. The placenta is a key source of oxytocinase during gestation and produces increasing amounts of the enzyme in response to increasing levels of oxytocin produced by the mother. Oxytocinase activity is also expressed in mammary glands, heart, kidney, and the small intestine.Lower levels of activity can be found in the brain, spleen, liver, skeletal muscle, testes, and colon. The level of oxytocin degradation is negligible in non-pregnant women, men, and cord bloodOxytocin is administered parenterally and is fully bioavailable. It takes approximately 40 minutes for oxytocin to reach steady-state concentrations in the plasma after parenteral administration.NAIn a study that observed 10 women who were given oxytocin to induce labor, the mean metabolic clearance rate was 7.87 mL/min.Oxytocics, Anti-tocolytic Agents and Labor Induction AgentsNANANANAOxytocin receptorPitocinJHP PharmaceuticalsJHP PharmaceuticalsInduction or Stimulation of Labor, Control of Postpartum Uterine Bleeding, Treatment of Incomplete, Inevitable, or Elective AbortionNANAPitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for Intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to contain 10 units of oxytocic hormone/mL and containsIntravenous infusioninitial dose should be 0.5–1 mU/min (equal to 3–6 mL of the dilute oxytocin solution per hour). At 30–60 minute intervals the dose should be gradually increased in increments of 1–2 mU/min until the desired contraction pattern has been established.Do NOT use Pitocin if: you are allergic to any ingredient in Pitocin; your birth canal is too small compared with the fetus's head; you have other complications that require medical intervention for birth; you have bacteria in the blood; you cannot have a child through vaginal delivery because of certain conditions (eg, genital herpes, cervical cancer)Symptoms of overdose: Restlessness, shakiness, sleepiness, slow to respond, slurred speech, unconsciousness.LinkNANA
10477Th1087Oxytocin>Th1087_Oxytocin CYIQNCPLG 1007.187C43H66N12O12S25.51-2.7192-194 ℃1-6 min9-residue cyclic peptide, synthetically prepared to avert possible contamination with vasopressin and small polypeptidesTo assist in labor, elective labor induction, uterine contraction inductionUsed to induce labor or to enhance uterine contractions during labor. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+-dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+, which in turn activates myosins light chain kinase.. Oxytocin has specific receptors in the muscle llining of the uterus and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term.Binds the oxytocin receptor which leads to an increase in intracellular calcium levels. The oxytocin-oxytocin receptor system plays an important role as an inducer of uterine contractions during parturition and of milk ejection.Administration of supratherapeutic doses of exogenous oxytocin can lead to myocardial ischemia, tachycardia, and arrhythmias. High doses can also lead to uterine spasms, hypertonicity, or rupture. Oxytocin has antidiuretic properties, thus, high daily doses (as a single dose or administered slowly over 24 hours) may lead to extreme water intoxication resulting in maternal seizures, coma, and even death. The risk of antidiuresis and water intoxication in the mother appears to be greater when fluids are given orallyOxytocin is rapidly removed from the plasma by the liver and kidney. The enzyme oxytocinase is largely responsible for the metabolism and regulation of oxytocin levels in pregnancy and only a small percentage of the neurohormone is excreted in the urine unchanged.Oxytocinase activity increases throughout pregnancy and peaks in the plasma, placenta and uterus near term. The placenta is a key source of oxytocinase during gestation and produces increasing amounts of the enzyme in response to increasing levels of oxytocin produced by the mother. Oxytocinase activity is also expressed in mammary glands, heart, kidney, and the small intestine.Lower levels of activity can be found in the brain, spleen, liver, skeletal muscle, testes, and colon. The level of oxytocin degradation is negligible in non-pregnant women, men, and cord bloodOxytocin is administered parenterally and is fully bioavailable. It takes approximately 40 minutes for oxytocin to reach steady-state concentrations in the plasma after parenteral administration.NAIn a study that observed 10 women who were given oxytocin to induce labor, the mean metabolic clearance rate was 7.87 mL/min.Oxytocics, Anti-tocolytic Agents and Labor Induction AgentsNANANANAOxytocin receptorSyntocinonNANANANANANANANANANANANANA
10559Th1111Defibrotide>Th1111_Defibrotide NA NANANANANAt1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hoursSodium salt of a mixture of single-stranded oligodeoxyribonucleotides, derived from porcine mucosal DNA. It has been shown to possess antithrombotic, anti-inflammatory and anti-ischemic properties and without the associated disadvantages of significant systemic anticoagulant effects. It is marketed under the brand names Dasovas (FM), Noravid, and Prociclide in a variety of countries, but is currently not approved in the USA. The manufacturer is Gentium.Defibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many othersDefibrotide is a deoxyribonucleic acid derivative extracted from mammalian organs, which has been developed for the treatment of a number of vascular disorders. It appears to increase fibrinolysis and may possess antithrombotic, antiatherosclerotic and anti-ischaemic actions, probably due to its ability to selectively increase prostaglandin I2 and E2 levels and to increase tissue plasminogen activator and decrease plasminogen activator inhibitor function. Defibrotide is available as an intravenous and intramuscular preparation, and also as an oral formulation for long term use.The drug appears to prevent the formation of blood clots and to help dissolve blood clots by increasing levels of prostaglandin I2, E2, and prostacyclin, altering platelet activity, increasing tissue plasminogen activator function, and decreasing activity of tissue plasminogen activator inhibitor. Prostaglandin I2 relaxes the smooth muscle of blood vessels and prevents platelets from adhering to each other. Prostaglandin E2 at certain concentrations also inhibits platelet aggregation. Moreover, the drug provides additional beneficial anti-inflammatory and antiischemic activities as recent sudies have shown. It is yet unclear, if the latter effects can be utilized clinically (e.g., treatment of ischemic stroke).NANABioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%).NANAAntithrombinsNANANANAAdenosine receptor A1,Adenosine receptor A2a,Adenosine receptor A2bNoravidsanofi-aventissanofi-aventisDefibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many others.Polydeoxyribonucleotides of bovine lungN. A.N. A.NA6.25mg/kg body weight every 6 hours (25mg/kg/day)NANALinkNANA
10560Th1111Defibrotide>Th1111_Defibrotide NA NANANANANAt1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hoursSodium salt of a mixture of single-stranded oligodeoxyribonucleotides, derived from porcine mucosal DNA. It has been shown to possess antithrombotic, anti-inflammatory and anti-ischemic properties and without the associated disadvantages of significant systemic anticoagulant effects. It is marketed under the brand names Dasovas (FM), Noravid, and Prociclide in a variety of countries, but is currently not approved in the USA. The manufacturer is Gentium.Defibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many othersDefibrotide is a deoxyribonucleic acid derivative extracted from mammalian organs, which has been developed for the treatment of a number of vascular disorders. It appears to increase fibrinolysis and may possess antithrombotic, antiatherosclerotic and anti-ischaemic actions, probably due to its ability to selectively increase prostaglandin I2 and E2 levels and to increase tissue plasminogen activator and decrease plasminogen activator inhibitor function. Defibrotide is available as an intravenous and intramuscular preparation, and also as an oral formulation for long term use.The drug appears to prevent the formation of blood clots and to help dissolve blood clots by increasing levels of prostaglandin I2, E2, and prostacyclin, altering platelet activity, increasing tissue plasminogen activator function, and decreasing activity of tissue plasminogen activator inhibitor. Prostaglandin I2 relaxes the smooth muscle of blood vessels and prevents platelets from adhering to each other. Prostaglandin E2 at certain concentrations also inhibits platelet aggregation. Moreover, the drug provides additional beneficial anti-inflammatory and antiischemic activities as recent sudies have shown. It is yet unclear, if the latter effects can be utilized clinically (e.g., treatment of ischemic stroke).NANABioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%).NANAAntithrombinsNANANANAAdenosine receptor A1,Adenosine receptor A2a,Adenosine receptor A2bDefitelioNANANANANANANANANANANANANA
10628Th1127Buserelin>Th1127_Buserelin XHWSYXLRP 1239.447C60H86N16O13NANANA50-80 minutes by IV dose, 80 mins. By SC dose, 1-2 hrs by Intranasal doseBuserelin is a luteinizing hormone-releasing hormone (LHRH) agonist. It is a synthetic hormone which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR) and is used in prostate cancer treatment.Buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.NABuserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of LH and testosterone. However, there is a concomitant surge in LH and testosterone levels with the decrease in androgens, so antiandrogens must administered.NANANANANANANANANANALutropin-choriogonadotropic hormone receptor,Gonadotropin-releasing hormone receptorSuprecur (Nasal Spray Solution)Sanofi-AventisSanofi-AventisTreatment of endometriosis – an illness where some of the tissues that line the womb are found elsewhere in the body. As part of a treatment for infertility – it works by stopping the natural production of hormones that control ovulation. Synthetic hormones are then used to artificially stimulate ovulation. Your doctor should give you more information about how your treatment worksNAEach spray dose contains 150 micrograms of the active substance, buserelin as buserelin acetate. The other ingredients are citric acid, sodium citrate, sodium chloride and benzalkonium chloride in aqueous solution150 micrograms Nasal Spray SolutionNasal sprayTreatment of endometriosis: The usual dose is one spray in each nostril three times each day. This is to make a total daily dose of 900 micrograms; Use the spray in the morning, at mid-day and in the evening; Treatment will be for a maximum of 6 months;Treatment should be started on the first or second day of your menstrual period.This is to lower the chances you may be pregnant. Your doctor may perform a pregnancy test if there is any doubt; You may get a menstrual period after the first few weeks of using this medicine. You may also carry on getting breakthrough bleeding or spotting As part of treatment for infertility.Do not use this medicine and tell your doctor if: You are allergic (hypersensitive) to buserelin or goserelin, benzalkonium chloride or other ingredients of Suprecur Nasal Spray. Signs of an allergic reaction include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue; You have abnormal menstrual bleeding where the cause is not endometriosis; You have a tumour that is not affected by hormones; You are pregnant or breast-feeding.This medicine is for use in women only. If you are not sure, talk to your doctor or pharmacist before using Suprecur Nasal Spray.Allergic reaction, diarrhoea, pain, swelling or a feeling of tension in stomach, weight gain, difficulty in breathing, decreased urination. These could be signs of a serious side effect called ’Ovarian Hyperstimulation Syndrome’. This is more likely if you are taking other hormones as well as Suprecur Nasal Spray (buserelin) as part of a treatment for infertility.LinkNANA
10629Th1127Buserelin>Th1127_Buserelin XHWSYXLRP 1239.447C60H86N16O13NANANA50-80 minutes by IV dose, 80 mins. By SC dose, 1-2 hrs by Intranasal doseBuserelin is a luteinizing hormone-releasing hormone (LHRH) agonist. It is a synthetic hormone which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR) and is used in prostate cancer treatment.Buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.NABuserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of LH and testosterone. However, there is a concomitant surge in LH and testosterone levels with the decrease in androgens, so antiandrogens must administered.NANANANANANANANANANALutropin-choriogonadotropic hormone receptor,Gonadotropin-releasing hormone receptorSuprecur (injection)Sanofi-AventisSanofi-AventisinfertilityNAEach 1ml of solution contains 1 milligram of the active substance, buserelin as buserelin acetate. The other ingredients are, sodium chloride, sodium dihydrogen phosphate, sodium hydroxide, benzyl alcohol and water for injections1mg/ml InjectionSubcutaneousTreatment starts on day 1 or day 21 of menstrual cycle. Daily dose is: 200 to 500 micrograms given as a single daily injection or 500 micrograms twice a day; Daily injections until blood tests show that levels of sex hormones are lowered. This usually takes one to three weeks; After this other hormones along with Suprecur Injection;Doctor determines the treatment timeDo not have this medicine and tell your doctor if: Allergy (hypersensitive) to buserelin or other similar medicines such as goserelin, or any of the other ingredients of Suprecur Injection. Abnormal menstrual bleeding Pregnancy or breast-feeding A tumour that is not affected by changes in hormone levels. This medicine is for use in women only. However there is another form of this medicine that can be used in men. Men should not use either form of this medicine if they have had their testicles removed.NALinkNANA
10650Th1135Ocriplasmin>Th1135_Ocriplasmin APSFDCGKPQVEPKKCPGR 27250C1214H1890N338O348S14NANANANAOcriplasmin is a recombinant (derived from Pichia pastoris) truncated form of human plasmin with a molecular weight of 27.2 kDa. It is a 249 amino acid protein that is made up of two peptide chains. Agent for pharmacologic vitreolysis; thrombolytic agent. FDA approved on October 17, 2012.Ocriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion.NAOcriplasmin has proteolytic activity against protein components of the vitreous body and the vitreoretinal interface (VRI) (e.g. laminin, fibronectin and collagen), thereby dissolving the protein matrix responsible for the vitreomacular adhesion (VMA).The most commonly reported reactions (= 5%) in patients treated with ocriplasmin were vitreous floaters, conjunctival hemorrhage, eye pain, photopsia, blurred vision, macular hole, reduced visual acuity, visual impairment, and retinal edema.Ocriplasmin is quickly inactivated by protease inhibitor a2-antiplasmin or a2-macroglobulin.Because of the small dose administered (0.125 mg), ocriplasmin is not expected to be in the systemic circulation following injection. Within 30 minutes after injection, levels of ocriplasmin in the vitreous are 12 mcg/mL. 24 hours after injection, levels in the virtreous are 0.5 mcg/mLNANAOphthalmicsNANANANAFibronectin,Alpha-2-macroglobulin,Alpha-2-antiplasminJetreaThromboGenics NVThromboGenics NVsymptomatic vitreomacular adhesion.NAEach vial contains 0.5 mg ocriplasmin (active) and 0.21 mg citric acid, 0.75 mg mannitol, sodium hydroxide (for pH adjustment) and water for injection. The pH of the solution is 3.1.JETREA is a Sterile, clear and colorless solution with no preservativesIntravitreal Injection0.125 mg (0.1 mL of the diluted solution)NADecreased Vision, Intravitreal Injection Procedure Associated Effects, Potential for Lens Subluxation, Retinal BreaksLinkNANA
10668Th1145Romiplostim>Th1145_Romiplostim IEGPTLRQWLAARA 59000C2634H4086N722O790S18NANANAImmunen thrombocytopenia patients, subQ = 3.5 days (median) (range 1-34 days)Romiplostim is a thrombopoiesis stimulating dimer Fc-peptide fusion protein (peptibody) to increase platelet production through activation of the thrombopoietin receptor. The peptibody molecule has two identical single-chain subunits, each one is made up of 269 amino acid residues. Each subunit consists of an IgG1 Fc carrier domain that is covalently attached to a polypeptide sequence that contains two binding domains to interact with thrombopoietin receptor c-Mpl. Each domain consists of 14 amino acids. Interestingly, romiplostim's amino acid sequence is not similar to that of endogenous thrombopoietin. Romiplostim is produced by recombinant DNA technology in Escherichia coli. FDA approved on August 22, 2008.Treatment of chronic immune thrombocytopenic purpura.Responses to platelet increase varies between patients thus indicating a need for individualization of dose. However, a dose dependent-increase in platelet counts have been observed in clinical trials. Does not affect platelet destruction.Romiplostim is a thrombopoietin receptor agonist that activates intracellular transcriptional pathways via c-Mpl to increase production of platelets. It also works similarly to thrombopoietin (TPO), an endogenous glycoprotein hormone that regulates the production of platelets in the bone marrow.The most common adverse reactions (= 5% higher patient incidence in Nplate versus placebo) are arthralgia, dizziness, insomnia, myalgia, pain in extremity, abdominal pain, shoulder pain, dyspepsia, and paresthesia. Headache was the most commonly reported adverse reaction that did not occur at = 5% higher patient incidence in Nplate versus placebo. LD50 = 980 mg/kg.NACmax, healthy volunteers, subQ = 24-36 hours; Cmax, immune thrombocytopenia patients, subQ = 7-50 hours (median = 14 hours). Not affected by age, weight, or gender. Accumulation does not occur after six weekly doses of 3 mcg/kg romiplostim.In healthy volunteers, non-linear decrease in Vd with increase IV dose of romiplostim which indicates saturation of c-Mpl receptors. Vd, 0.3 µg/kg = 122 mL/kg Vd, 10 µg/kg = 48.2 mL/kgNAAmino Acids, Peptides, and Proteins,Biological Factors,Blood and Blood Forming Organs,Carbohydrates,Colony-Stimulating Factors,Cytokines,Glycoconjugates,Glycoproteins,Hematinics,Hematopoietic Cell Growth Factors,Hemostatics,Increased Megakaryocyte Maturation,Increased Platelet Production,Intercellular Signaling Peptides and Proteins,Membrane Proteins,Peptides,Proteins,Receptors, Thrombopoietin, agonists,Recombinant Proteins,Thrombopoietin Receptor Agonist,Thrombopoietin Receptor AgonistsNANANANAThrombopoietin receptorNplateAmgenAmgenNplate is indicated for the treatment of thrombocytopenia in patients with chronic immune thrombocytopenia (ITP) who have had an insufficient response to corticosteroids, immunoglobulins or splenectomy.NATwo vial presentations are available, which contain a sufficient amount of active ingredient to provide either 250 mcg or 500 mcg of deliverable romiplostim, respectively. Each single-use 250 mcg vial of Nplate contains the following: 375 mcg romiplostim, 30 mg mannitol, 15 mg sucrose, 1.2 mg L-histidine, 0.03 mg polysorbate 20, and sufficient HCl to adjust the pH to a target of 5.0. Each single-use 500 mcg vial of Nplate contains the following: 625 mcg romiplostim, 50 mg mannitol, 25 mg sucrose, 1.9 mg L-histidine, 0.05 mg polysorbate 20, and sufficient HCl to adjust the pH to a target of 5.0Sterile, preservative-free, lyophilized, solid white powderSubcutaneous InjectionUse the lowest dose of Nplate to achieve and maintain a platelet count ≥ 50 x 109/L as necessary to reduce the risk for bleeding. Administer Nplate as a weekly subcutaneous injection with dose adjustments based upon the platelet count response. The prescribed Nplate dose may consist of a very small volume (eg, 0.15 mL). Administer Nplate only with a syringe that contains 0.01 mL graduations. The initial dose for Nplate is 1 mcg/kg based on actual body weight. Dose AdjustmentsUse the actual body weight at initiation of therapy, then adjust the weekly dose of Nplate by increments of 1 mcg/kg until the patient achieves a platelet count ≥ 50 x 109/L as necessary to reduce the risk for bleeding; do not exceed a maximum weekly dose of 10 mcg/kg. In clinical studies, most patients who responded to Nplate achieved and maintained platelet counts ≥ 50 x 109/L with a median dose of 2 mcg/kg. During Nplate therapy, assess CBCs, including platelet counts, weekly until a stable platelet count ( ≥ 50 x 109/L for at least 4 weeks without dose adjustment) has been achieved. Obtain CBCs, including platelet counts, monthly thereafter.NAThe following serious adverse reactions: Progression of Myelodysplastic Syndromes, Thrombotic/Thromboembolic Complications, Loss of Response to Nplate, Overdoses due to medication errors have been reported in patients receiving Nplate. In the event of overdose, platelet counts may increase excessively and result in thrombotic/thromboembolic complications. In this case, discontinue Nplate and monitor platelet counts. Reinitiate treatment with Nplate in accordance with dosing and administration recommendations.LinkNANA
10692Th1156Abarelix>Th1156_Abarelix XXXSYNLXPA 1416.063C72H95ClN14O14NANANA13.2 ± 3.2 daysSynthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market.For palliative treatment of advanced prostate cancer.Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesisAbarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretionNANANANANAAnti-Testosterone AgentsUS596889519-10-199912-Nov-2016Tacrolimus, Thiothixene, Toremifene, Trimipramine, Voriconazole, Vorinostat, Ziprasidone, Zuclopenthixol- All above drugs cause Additive QTc Prolongation and increases the risk of severe ventricular arrythmiasGonadotropin-releasing hormone receptorPlenaxisSpeciality european pharmaSpeciality european pharmaPlenaxis is indicated for the palliative treatment of men with advanced symptomatic prostate cancer, in whom LHRH agonist therapy is not appropriate and who refuse surgical castration, and have one or more of the following: (1) risk of neurological compromise due to metastases, (2) ureteral or bladder outlet obstruction due to local encroachment or metastatic disease, or (3) severe bone pain from skeletal metastases persisting on narcotic analgesia.Abarelix is chemically described as acetyl-D-β-naphthylalanyl-D-4-chlorophenylalanyl- D-3-pyridylalanyl-L-seryl-L-N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(ε)-isopropyllysyl- L-prolyl-D-alanyl-amide.The single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injectionAbarelix for injectable suspension is supplied as a white to off-white sterile dry powderIntramuscular InjectionThe recommended dose of Plenaxis is 100 mg administered intramuscularly to the buttock on Day 1, 15, 29 (week 4) and every 4 weeks thereafter.Plenaxis is not indicated in women or pediatric patients. In addition, Plenaxis may cause fetal harm if administered to a pregnant woman.Diarrhea, Dizziness, Flushing of Skin, Headache, Constipation, Sleep DisturbanceLinkNANA
10693Th1156Abarelix>Th1156_Abarelix XXXSYNLXPA NANANANANA13.2 ± 3.2 daysNANANANANANANANANAAnti-Testosterone AgentsUS642368623-07-20026-Jul-2015NAGonadotropin-releasing hormone receptorNANANANANANANANANANANANANANA
11841Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANAAmino Acids, Peptides, and ProteinsNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11842Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANAMembrane ProteinsNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11843Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANAMyelin ProteinsNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11844Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANANerve Tissue ProteinsNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11845Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANAPeptidesNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11846Th1261Dirucotide>Th1261_Dirucotide DENPVVHFFKNIVTPRT NANANANANANADirucotide is a synthetically prepared peptide. In particular, the sequence prepared is a 17 amino acid chain that is identical to a section of myelin basic protein (MBP) that is found in humans. Dirucotide has been developed for the treatment of multiple sclerosis (MS). Developed at the University of Alberta, dirucotide is being investigated by BioMS Medical Corp.For the treatment of multiple sclerosis (MS).MS is generally considered an autoimmune disease, caused by immune attack against normal components of the central nervous system. The specificity of the immune attack at the molecular level is determined in each case by the HLA type of the individual patient, and HLA type is known to be one factor that contributes to susceptibility to MS. The MBP8298 synthetic peptide is a molecular replicate of the site of attack that is dominant in MS patients with HLA haplotypes DR-2 or DR-4. These HLA types are found in 65-75% of all MS patients.The apparent mechanism of action of MBP8298 is the induction or restoration of immunological tolerance with respect to ongoing immune attack at this molecular site. High doses of antigen delivered periodically by the intravenous route are expected to suppress immune responses to the administered substance. The potential benefit of MBP8298 for any individual patient is therefore expected to be related to the extent to which his or her disease process is dominated by autoimmune attack at the site represented by this synthetic peptide.NANANANANAProteinsNANANANANANANANANANANANANANA(4S)-5-[[(2S)-4-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-oxopentanoic acidNALinkNANA
11953Th1272Tigapotide>Th1272_Tigapotide PGDSTRKCMDLKGNK NANANANANA0.35 hours to 1.45 hoursTigapotide is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid.For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.PCK3145 is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is down regulated in patients with advanced prostate cancer, and believed to be a survival mechanism for the cancer cells. Results from an earlier trial conducted in the U.K. showed PCK3145 to be safe and well tolerated at all doses tested and further suggest that it also plays a role in preventing the metastatic process as measured by its effect on MMP-9 levels, a Gelatinase B enzyme involved in angiogenesis, tumor invasion and metastasis.The mechanism of action and receptor for PCK3145 suggests PCK3145 to be a signal transduction inhibitor with multiple ways (apoptosis, anti-angiogenesis and anti-metastasis) to restrict disease development.Non-clinical toxicology studies in mice and primates indicated that a treatment for 28 consecutive days by intravenous administration of PCK3145 up to 450 mg/kg/day in mice and 25 mg/kg/day in primates resulted in no clear evidence of toxicity.NANANANAAmino Acids, Peptides, and ProteinsNANANANA40S ribosomal protein SANANANANANANANANANANANALinkNANA
11954Th1272Tigapotide>Th1272_Tigapotide PGDSTRKCMDLKGNK NANANANANA0.35 hours to 1.45 hoursTigapotide is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid.For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.PCK3145 is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is down regulated in patients with advanced prostate cancer, and believed to be a survival mechanism for the cancer cells. Results from an earlier trial conducted in the U.K. showed PCK3145 to be safe and well tolerated at all doses tested and further suggest that it also plays a role in preventing the metastatic process as measured by its effect on MMP-9 levels, a Gelatinase B enzyme involved in angiogenesis, tumor invasion and metastasis.The mechanism of action and receptor for PCK3145 suggests PCK3145 to be a signal transduction inhibitor with multiple ways (apoptosis, anti-angiogenesis and anti-metastasis) to restrict disease development.Non-clinical toxicology studies in mice and primates indicated that a treatment for 28 consecutive days by intravenous administration of PCK3145 up to 450 mg/kg/day in mice and 25 mg/kg/day in primates resulted in no clear evidence of toxicity.NANANANAPeptidesNANANANA40S ribosomal protein SANANANANANANANANANANANALinkNANA
11955Th1272Tigapotide>Th1272_Tigapotide PGDSTRKCMDLKGNK NANANANANA0.35 hours to 1.45 hoursTigapotide is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid.For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.PCK3145 is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is down regulated in patients with advanced prostate cancer, and believed to be a survival mechanism for the cancer cells. Results from an earlier trial conducted in the U.K. showed PCK3145 to be safe and well tolerated at all doses tested and further suggest that it also plays a role in preventing the metastatic process as measured by its effect on MMP-9 levels, a Gelatinase B enzyme involved in angiogenesis, tumor invasion and metastasis.The mechanism of action and receptor for PCK3145 suggests PCK3145 to be a signal transduction inhibitor with multiple ways (apoptosis, anti-angiogenesis and anti-metastasis) to restrict disease development.Non-clinical toxicology studies in mice and primates indicated that a treatment for 28 consecutive days by intravenous administration of PCK3145 up to 450 mg/kg/day in mice and 25 mg/kg/day in primates resulted in no clear evidence of toxicity.NANANANAProteinsNANANANA40S ribosomal protein SANANANANANANANANANANANALinkNANA
11956Th1272Tigapotide>Th1272_Tigapotide PGDSTRKCMDLKGNK NANANANANA0.35 hours to 1.45 hoursTigapotide is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid.For the treatment of late stage Hormone Refractory Prostate Cancer (HRPC) for which no effective therapy currently exists.PCK3145 is a synthetic 15-mer peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is down regulated in patients with advanced prostate cancer, and believed to be a survival mechanism for the cancer cells. Results from an earlier trial conducted in the U.K. showed PCK3145 to be safe and well tolerated at all doses tested and further suggest that it also plays a role in preventing the metastatic process as measured by its effect on MMP-9 levels, a Gelatinase B enzyme involved in angiogenesis, tumor invasion and metastasis.The mechanism of action and receptor for PCK3145 suggests PCK3145 to be a signal transduction inhibitor with multiple ways (apoptosis, anti-angiogenesis and anti-metastasis) to restrict disease development.Non-clinical toxicology studies in mice and primates indicated that a treatment for 28 consecutive days by intravenous administration of PCK3145 up to 450 mg/kg/day in mice and 25 mg/kg/day in primates resulted in no clear evidence of toxicity.NANANANASeminal Plasma ProteinsNANANANA40S ribosomal protein SANANANANANANANANANANANALinkNANA