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Th1063 details
Primary information
ID1398
ThPP IDTh1063
Therapeutic Peptide/Protein NameBasiliximab
SequenceHeavy Chain: QLQQSGTVLARPGASVKMSCKASGYSFTRYWMHWIKQ view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight143801.3
Chemical FormulaC6378H9844N1698O1997S48
Isoelectric Point8.68
Hydrophobicity-0.473
Melting Point (℃)61 (FAB f
Half Life7.2 ± 3.2 days (adults)
DescriptionA recombinant chimeric (murine/human) monoclonal antibody (IgG1k) that functions as an immunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor a-chain (IL-2R alpha, also known as CD25 antigen) on the surface of activated T-lymphocytes. It is a 144 kDa glycoprotein obtained from fermentation of an established mouse myeloma cell line genetically engineered to express plasmids containing the human heavy and light chain constant region genes and mouse heavy and light chain variable region genes encoding the RFT5 antibody that binds selectively to the IL-2R alpha.
Indication/DiseaseFor prophylactic treatment of kidney transplant rejection
PharmacodynamicsBasiliximab functions as an IL-2 receptor antagonist. Specifically it inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection.
Mechanism of ActionBasiliximab binds with high-affinity to the alpha-subunit (CD25) of the high-affinity IL-2 receptor. This inhibits IL-2 binding, which inhibits T-cell activation and prevents the body from mounting an immune response against the foreign kidney.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system.
AbsorptionN.A.
Volume of Distribution7.8 ± 5.1 L [Pediatric] 4.8 ± 2.1 L [Adult]
Clearance41 ± 19 mL/h [Adult patients undergoing first kidney transplantation] 17 ± 6 mL/h [pediatric patients undergoing renal transplantation] 31 ± 19 mL/h [adolescent patients undergoing renal transplantation]
CategoriesImmunosuppressive Agents
Patents NumberCA2038279
Date of Issue10/03/03
Date of Expiry12/03/15
Drug InteractionCanakinumab, Rilonacept results in increased immunosuppressive effects; increases the risk of infection
TargetN.A.
Information of corresponding available drug in the market
Brand NameSimulect
CompanyNovartis
Brand DiscriptionSimulect (basiliximab) is a chimeric (murine/human) monoclonal antibody(IgG1K), produced by recombinant DNA technology, that functions as animmunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor α-chain (IL-2Rα, also known as CD25 antigen) on the surface of activated T-lymphocytes. Based on the amino acid sequence, the calculated molecular weight of the protein is 144 kilodaltons. It is aglycoprotein obtained from fermentation of an established mouse myeloma cell line genetically engineered to express plasmids containing the human heavy and light chain constant region genes and mouse heavy and light chain variable region genes encoding the RFT5 antibody that binds selectively to the IL-2Rα.
Prescribed forSimulect (basiliximab) is indicated for the prophylaxis of acute organ rejection in patients receiving renal transplantation when used as part of an immunosuppressive regimen that includes cyclosporine, USP (MODIFIED) and corticosteroids.
Chemical NameN.A.
FormulationEach 10-mg vial contains 10 mg basiliximab, 3.61 mg monobasic potassium phosphate, 0.50 mg disodium hydrogen phosphate (anhydrous), 0.80 mg sodium chloride, 10 mg sucrose, 40 mg mannitol and 20 mg glycine, to be reconstituted in 2.5 mL of Sterile Water for Injection, USP. No preservatives are added. Each 20-mg vial contains 20 mg basiliximab, 7.21 mg monobasic potassium phosphate, 0.99 mg disodium hydrogen phosphate (anhydrous), 1.61 mg sodium chloride, 20 mg sucrose, 80 mg mannitol and 40 mg glycine, to be reconstituted in 5 mL of Sterile Water for Injection, USP. No preservatives are added.
Physcial AppearanceSimulect (basiliximab) , is a sterile lyophilisate which is available in 6 mL colorless glass vials and is available in 10 mg and 20 mg strength powder.
Route of Administrationintavenous infusion mainly or bolus (if no allerg
Recommended DosageIn adult patients, the recommended regimen is two doses of 20 mg each. The first 20-mg dose should be given within 2 hours prior to transplantation surgery. The recommended second 20-mg dose should be given 4 days after transplantation.
ContraindicationSimulect (basiliximab) is contraindicated in patients with known hypersensitivity to basiliximab or any other component of the formulation.
Side EffectsGastrointestinal System: constipation, nausea, abdominal pain, vomiting, diarrhea, dyspepsia; Body as a Whole-General: pain, peripheral edema, fever, viral infection; Metabolic and Nutritional: hyperkalemia, hypokalemia, hyperglycemia, hypercholesterolemia, hypophosphatemia, hyperuricemia; Urinary System: urinary tract infection;Respiratory System: dyspnea, upper respiratory tract infection; Skin and Appendages: surgical wound complications, acne;Cardiovascular Disorders-General: hypertension; Central and Peripheral Nervous System: headache, tremor; Psychiatric: insomnia; Red Blood Cell: anemia.
Useful Linkhttp://www.rxlist.com/simulect-drug.htm http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1af01887-b69d-444b-91ed-ebfe12784440
PubMed ID25501951, 22151353
3-D StructureTh1063 (View) or (Download)
Primary information
ID1399
ThPP IDTh1063
Therapeutic Peptide/Protein NameBasiliximab
SequenceHeavy Chain: QLQQSGTVLARPGASVKMSCKASGYSFTRYWMHWIKQ view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight143801.3
Chemical FormulaC6378H9844N1698O1997S48
Isoelectric Point8.68
Hydrophobicity-0.473
Melting Point (℃)62 (FAB f
Half Life7.2 ± 3.2 days (adults)
DescriptionA recombinant chimeric (murine/human) monoclonal antibody (IgG1k) that functions as an immunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor a-chain (IL-2R alpha, also known as CD25 antigen) on the surface of activated T-lymphocytes. It is a 144 kDa glycoprotein obtained from fermentation of an established mouse myeloma cell line genetically engineered to express plasmids containing the human heavy and light chain constant region genes and mouse heavy and light chain variable region genes encoding the RFT5 antibody that binds selectively to the IL-2R alpha.
Indication/DiseaseFor prophylactic treatment of kidney transplant rejection
PharmacodynamicsBasiliximab functions as an IL-2 receptor antagonist. Specifically it inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection.
Mechanism of ActionBasiliximab binds with high-affinity to the alpha-subunit (CD25) of the high-affinity IL-2 receptor. This inhibits IL-2 binding, which inhibits T-cell activation and prevents the body from mounting an immune response against the foreign kidney.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system.
AbsorptionN.A.
Volume of Distribution7.8 ± 5.1 L [Pediatric] 4.8 ± 2.1 L [Adult]
Clearance42 ± 19 mL/h [Adult patients undergoing first kidney transplantation] 17 ± 6 mL/h [pediatric patients undergoing renal transplantation] 31 ± 19 mL/h [adolescent patients undergoing renal transplantation]
CategoriesImmunosuppressive Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25501951, 22151353
3-D StructureTh1063 (View) or (Download)