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Th1052 details
Primary information
ID10363
Therapeutic IDTh1052
Protein NameEptifibatide
Sequence>Th1052_Eptifibatide CXGDWPC
Molecular Weight831.962
Chemical FormulaC35H49N11O9S2
Isoelectric PointNA
Hydrophobicity-2.3
Melting pointNA
Half-lifeApproximately 2.5 hours
DescriptionSynthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Indication/DiseaseFor treatment of myocardial infarction and acute coronary syndrome.
PharmacodynamicsEptifibatide 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.
Mechanism of ActionEptifibatide 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.
ToxicityEptifibatide 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).
MetabolismNo major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
AbsorptionThe mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%.
NA
Clearance55 mL/kg/h [patients with coronary artery disease]
CategoriesAmino Acids, Peptides, and Proteins, Antiplatelet agents, Blood and Blood Forming Organs, Decreased Platelet Aggregation, Hematologic Agents, Peptides, Peptides, Cyclic, Platelet Aggregation Inhibitors Excl. Heparin
Patents NumberUS6706681
Date of Issue16-Mar-2004
Date of Expiry16-Mar-2021
Drug InteractionNA
TargetLutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor, Integrin beta-3, Voltage-dependent N-type calcium channel (Protein Group)
Brand NameINTEGRILIN
CompanySchering-Plough/Essex
Brand DescriptionSchering-Plough/Essex
Prescribed ForAcute Coronary Syndrome (ACS), Percutaneous Coronary Intervention (PCI)
Chemical NameN6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-Llysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic (1→6)-disulfide.
FormulationEach 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.
Physical Appearance INTEGRILIN Injection is a clear, colorless, Sterile, non-pyrogenic solution of Eptifibatide
Route of AdministrationInjection Solution for Intravenous Use
Recommended DosageDosage 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).
Contraindication1. 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).
Side EffectsBleeding, Intracranial Hemorrhage and Stroke, Immunogenicity/Thrombocytopenia.
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10364
Therapeutic IDTh1052
Protein NameEptifibatide
Sequence>Th1052_Eptifibatide CXGDWPC
Molecular Weight831.962
Chemical FormulaC35H49N11O9S2
Isoelectric PointNA
Hydrophobicity-2.3
Melting pointNA
Half-lifeApproximately 2.5 hours
DescriptionSynthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Indication/DiseaseFor treatment of myocardial infarction and acute coronary syndrome.
PharmacodynamicsEptifibatide 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.
Mechanism of ActionEptifibatide 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.
ToxicityEptifibatide 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).
MetabolismNo major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
AbsorptionThe mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%.
NA
Clearance56 mL/kg/h [patients with coronary artery disease]
CategoriesAmino Acids, Peptides, and Proteins, Antiplatelet agents, Blood and Blood Forming Organs, Decreased Platelet Aggregation, Hematologic Agents, Peptides, Peptides, Cyclic, Platelet Aggregation Inhibitors Excl. Heparin
Patents NumberUS5767251
Date of Issue16-Jun-1998
Date of Expiry16-Jun-2015
Drug InteractionNA
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1NA
Useful Link 2NA
RemarksNA