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1406 details
Primary information
ThPP IDTh1066
Therapeutic Peptide/Protein NameIbritumomab
SequenceHeavy Chain: QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWV view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight143375.5
Chemical FormulaC6382H9830N1672O1979S54
Isoelectric Point7.91
Hydrophobicity-0.359
Melting Point (℃)61 (FAB f
Half Life0.8 hours (mammalian reticulocytes, in vitro)
DescriptionIndium conjugated murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes. Ibritumomab is produced in Chinese hamster ovary cells and is composed of two murine gamma 1 heavy chains of 445 amino acids each and two kappa light chains of 213 amino acids each.
Indication/DiseaseFor treatment of non-Hodgkin's lymphoma
PharmacodynamicsIbritumomab is a murine monoclonal antibody against CD20 that has been radiolabeled with yttrium-90.
Mechanism of ActionThe Fab segment of the antibody targets the CD20 epitope on B-cells, allowing the radioactive yttrium to destroy the cell via production of beta particles.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system when bound to B cells, or by human antimurine antibody production
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberCA2149329
Date of Issue16/07/12
Date of Expiry13/11/17
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 NameZevalin
CompanySpectrum Pharmaceuticals
Brand DiscriptionZevalin (ibritumomab tiuxetan) is the immunoconjugate resulting from a stable thiourea covalent bond between the monoclonal antibody ibritumomab and the linker-chelator tiuxetan [N-[2-bis(carboxymethyl)amino]-3-(p-isothiocyanatophenyl)-propyl]-[N-[2-bis(carboxymethyl)amino]-2-(methyl)-ethyl]glycine. This linker-chelator provides a high affinity, conformationally restricted chelation site for Yttrium-90. The approximate molecular weight of ibritumomab tiuxetan is 148 kD. The antibody moiety of Zevalin is ibritumomab, a murine IgGi kappa monoclonal antibody directed against the CD20 antigen.
Prescribed forZevalin is indicated for the treatment of relapsed or refractory, low-grade or follicular B-cell non-Hodgkin's lymphoma (NHL). Zevalin is indicated for the treatment of previously untreated follicular NHL in patients who achieve a partial or complete response to first-line chemotherapy.
Chemical NameN.A.
Formulation Each single-use vial includes 3.2 mg of ibritumomab tiuxetan in 2 mL of 0.9% Sodium Chloride.
Physcial AppearnceIbritumomab tiuxetan is a clear, colorless, sterile, pyrogen-free, preservative-free solution that may contain translucent particles.
Route of AdministrationIntravenous infusion
Recommended DosageDay 1: Administer rituximab 250 mg/m2 intravenous ; Day 7,8, or 9: Administer rituximab 250 mg/m2 Intravenous infusion If platelets ≥ 150,000/mm3: Within 4 hours after rituximab infusion, administer 0.4 mCi/kg (14.8 MBq per kg) Y-90 Zevalin intravenous. If platelets ≥ 100,000 but ≤ 149,000/mm3 in relapsed or refractory patients: Within 4 hours after rituximab infusion, administer 0.3 mCi/kg (11.1 MBq per kg) Y-90 Zevalin intravenous.
ContraindicationNone.
Side EffectsSerious Infusion Reactions, prolonged and Severe Cytopenias, Severe Cutaneous and Mucocutaneous Reactions, Leukemia and Myelodysplastic Syndrome, Cytopenias, fatigue, nasopharyngitis, nausea, abdominal pain, asthenia, cough, diarrhea, and pyrexia.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ccf29429-bf8e-4cce-bd12-1de56853fc5b http://www.rxlist.com/zevalin-drug.htm
PubMed ID16810345, 20383346, 28269762, 26758269, 22045523, 21355777, 21225019, 21225012, 20094643
3-D StructureTh1066 (View) or (Download)