| Primary information |
|---|
| ThPP ID | Th1068 |
| Therapeutic Peptide/Protein Name | Tositumomab |
| Sequence | Heavy Chain 1: QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMH view full sequnce in fasta |
| Functional Classification | IIb |
| Molecular Weight | 143859.7 |
| Chemical Formula | C6416H9874N1688O1987S44 |
| Isoelectric Point | 8.68 |
| Hydrophobicity | -0.4144 |
| Melting Point (℃) | 61 (FAB f |
| Half Life | 0.8 hours (mammalian reticulocytes, in vitro) |
| Description | Murine IgG2a lambda monoclonal antibody against CD20 antigen (2 heavy chains of 451 residues, 2 lambda chains of 220 residues). It is produced in an antibiotic-free culture of mammalian cells. It can be covalently linked to Iodine 131 (a radioactive isotope of iodine). |
| Indication/Disease | For treatment of non-Hodgkin's lymphoma (CD20 positive, follicular) |
| Pharmacodynamics | Tositumomab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells. |
| Mechanism of Action | Binds to the CD20 antigen which is found on mature B lymphocytes. The antibody binding appears to induce apoptosis, complement-dependent cytotoxicity and cell death through ionizing radiation. |
| Toxicity | N.A. |
| Metabolism | Most likely removed by opsonization via the reticuloendothelial system when bound to B lymphocytes, or by human antimurine antibody production |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | 68.2 mg/hr [patients with NHL] |
| Categories | N.A. |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | Natalizumab with immunosuppressant, Tositumomab, may increase the adverse effects. Increased risk of Progressive Multifocal Leukoencephalopathy (PML) and other infections. Concurrent therapy should be avoided |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Bexxar |
| Company | Galaxo Smith Kline |
| Brand Discription | The BEXXAR therapeutic regimen is composed of the monoclonal antibody tositumomab, and the radiolabeled monoclonal antibody, I-131 tositumomab |
| Prescribed for | The BEXXAR therapeutic regimen (Tositumomab and Iodine I 131 Tositumomab) is indicated for the treatment of patients with CD20 antigen-expressing relapsed or refractory, low grade, follicular, or transformed non-Hodgkin's lymphoma, including patients with Rituximab-refractory non-Hodgkin’s lymphoma. Determination of the effectiveness of the BEXXAR therapeutic regimen is based on overall response rates in patients whose disease is refractory to chemotherapy alone or to chemotherapy and Rituximab. The effects of the BEXXAR therapeutic regimen on survival are not known. |
| Chemical Name | N.A. |
| Formulation | The formulation contains 100 mg/mL maltose, 8.5 mg/mL sodium chloride, 1 mg/mL phosphate, 1 mg/mL potassium hydroxide, and Water for Injection, USP. The pH is approximately 7.2. |
| Physcial Appearnce | Tositumomab is supplied as a Sterile, pyrogen-free, clear to opalescent, colorless to slightly yellow, preservative-free solution |
| Route of Administration | Intravenous (Intravenous) administration |
| Recommended Dosage | The BEXXAR therapeutic regimen consists of 2 separate components (tositumomab and iodine I 131 tositumomab) administered in 2 separate steps (dosimetric dose and therapeutic dose) separated by 7 to 14 days.Tositumomab 450 mg by Intravenous infusion.I-131 tositumomab (5 mCi I-131 and 35 mg protein) by Intravenous infusion |
| Contraindication | The BEXXAR therapeutic regimen is contraindicated in patients with known hypersensitivity to murine proteins or any other component of the BEXXAR therapeutic regimen. |
| Side Effects | Serious Allergic Reactions, Including Anaphylaxis, Prolonged and Severe Cytopenias, Secondary malignancies, Hypothyroidism, neutropenia, thrombocytopenia, anemia, infections (including pneumonia, bacteremia, septicemia, bronchitis, and skin infections), infusion reactions, asthenia, fever, and nausea. |
| Useful Link | http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=11680 http://www.rxlist.com/bexxar-drug.htm |
| PubMed ID | 16179960, 15071612, 27195659, 25568316, 22531442, 21355777, 21225019, 19649342, 19455266 |
| 3-D Structure | Th1068 (View) or (Download) |