Primary information |
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ThPP ID | Th1066 |
Therapeutic Peptide/Protein Name | Ibritumomab |
Sequence | Heavy Chain: QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWV view full sequnce in fasta |
Functional Classification | IIb |
Molecular Weight | 143375.5 |
Chemical Formula | C6382H9830N1672O1979S54 |
Isoelectric Point | 7.91 |
Hydrophobicity | -0.359 |
Melting Point (℃) | 61 (FAB f |
Half Life | 0.8 hours (mammalian reticulocytes, in vitro) |
Description | Indium 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/Disease | For treatment of non-Hodgkin's lymphoma |
Pharmacodynamics | Ibritumomab is a murine monoclonal antibody against CD20 that has been radiolabeled with yttrium-90. |
Mechanism of Action | The 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. |
Toxicity | N.A. |
Metabolism | Most likely removed by opsonization via the reticuloendothelial system when bound to B cells, or by human antimurine antibody production |
Absorption | N.A. |
Volume of Distribution | N.A. |
Clearance | N.A. |
Categories | N.A. |
Patents Number | CA2149329 |
Date of Issue | 16/07/12 |
Date of Expiry | 13/11/17 |
Drug Interaction | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
Target | N.A. |
Information of corresponding available drug in the market |
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Brand Name | Zevalin |
Company | Spectrum Pharmaceuticals |
Brand Discription | Zevalin (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 for | Zevalin 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 Name | N.A. |
Formulation | Â Each single-use vial includes 3.2 mg of ibritumomab tiuxetan in 2 mL of 0.9% Sodium Chloride. |
Physcial Appearnce | Ibritumomab tiuxetan is a clear, colorless, sterile, pyrogen-free, preservative-free solution that may contain translucent particles. |
Route of Administration | Intravenous infusion |
Recommended Dosage | Day 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. |
Contraindication | None. |
Side Effects | Serious 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 Link | http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ccf29429-bf8e-4cce-bd12-1de56853fc5b http://www.rxlist.com/zevalin-drug.htm |
PubMed ID | 16810345, 20383346, 28269762, 26758269, 22045523, 21355777, 21225019, 21225012, 20094643 |
3-D Structure | Th1066 (View) or (Download) |