A database of FDA approved therapeutic peptides and proteins
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1843 details |
| Primary information | |
|---|---|
| ThPP ID | Th1231 |
| Therapeutic Peptide/Protein Name | Ibritumomab tiuxetan |
| Sequence | Heavy chainQAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMHWVKQ view full sequnce in fasta |
| Functional Classification | IIIc |
| Molecular Weight | 143375.5 |
| Chemical Formula | C6382H9830N1672O1979S54 |
| Isoelectric Point | 7.91 |
| Hydrophobicity | -0.359 |
| Melting Point (℃) | 61 °C |
| Half Life | 0.8 hours |
| Description | Indium or yttrium 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 | NA |
| Metabolism | Most likely removed by opsonization via the reticuloendothelial system when bound to B cells, or by human antimurine antibody production |
| Absorption | NA |
| Volume of Distribution | Binding observed on lymphoid cells of the bone marrow, lymph node, thymus, red and white pulp of the spleen, lymphoid follicles of the tonsil, and lymphoid nodules of other organs (e.g., large and small intestines) |
| Clearance | Approximately 7.2% of injected dose of yttrium Y 90 ibritumomab tiuxetan is excreted in urine within 7 days. |
| Categories | Antibody, Immunosuppressive Agents |
| Patents Number | CA2149329 |
| Date of Issue | 15/07/08 |
| Date of Expiry | 12/11/13 |
| Drug Interaction | The risk or severity of adverse effects can be increased while combining Ibritumomab tiuxetan with Abciximab, Acenocoumarol, Acetylsalicylic acid, Alprostadil, Anagrelide, Ancrod, Antithrombin III human, Apixaban, Ardeparin, Argatroban. |
| Target | B-lymphocyte antigen CD20, Low affinity immunoglobulin gamma Fc region receptor III-B, Complement C1r subcomponent, Complement C1q subcomponent subunit A, Complement C1q subcomponent subunit B, Complement C1q subcomponent subunit C, Low affinity immunoglobulin gamma Fc region receptor III-A, Complement C1s subcomponent, High affinity immunoglobulin gamma Fc receptor I, Low affinity immunoglobulin gamma Fc region receptor II-a,Low affinity immunoglobulin gamma Fc region receptor II-b, Low affinity immunoglobulin gamma Fc region receptor II-c |
| Information of corresponding available drug in the market | |
| Brand Name | Zevalin |
| Company | Spectrum Pharmaceuticals B.V. |
| 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-(pisothiocyanatophenyl)- 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 IgG1 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). |
| Chemical Name | NA |
| Formulation | 3.2 mg ibritumomab tiuxetan per 2 mL in a single-use vial. The contents of all vials are sterile, pyrogenfree, contain no preservatives, and are not radioactive. |
| Physcial Appearnce | Colourless Solution |
| Route of Administration | Intravenous |
| Recommended Dosage | nitiate the Zevalin therapeutic regimen following recovery of platelet counts to ≥ 150,000/mm³ at least 6 weeks, but no more than 12 weeks, following the last dose of first-line chemotherapy |
| Contraindication | None. |
| Side Effects | Serious Infusion Reactions, Severe Cutaneous and Mucocutaneous Reactions, Prolonged and Severe Cytopeniasmight occur |
| Useful Link | https://www.drugbank.ca/drugs/DB00078, http://www.rxlist.com/zevalin-drug.htm |
| PubMed ID | 10541376, 11879282, 15045033, 11752352, 17139284, 17016423 |
| 3-D Structure | Th1231 (View) or (Download) |