|
| Primary information |
|---|
| ID | 10389 |
| Therapeutic ID | Th1062 |
| Protein Name | Rituximab |
| Sequence | >Th1062_Rituximab
QVQLQQPGAELVKPGASVKMSCKASGYTFTSYNMHWVKQTPGRGLEWIGAIYPGNGDTSYNQKFKGKATLTADKSSSTAYMQLSSLTSEDSAVYYCARSTYYGGDWYFNVWGAGTTVTVSAASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
|
| Molecular Weight | 143859.7 |
| Chemical Formula | C6416H9874N1688O1987S44 |
| Isoelectric Point | 8.68 |
| Hydrophobicity | -0.414 |
| Melting point | 61 (FAB f |
| Half-life | 22 days: , Non-Hodgkin's Lymphoma |
| Description | Rituxan is a genetically engineered chimeric murine/human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The antibody is an IgG1 kappa immunoglobulin containing murine light- and heavy-chain variable region sequences and human constant region sequences. Rituximab is composed of two heavy chains of 451 amino acids and two light chains of 213 amino acids. |
| Indication/Disease | For treatment of CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis. |
| Pharmacodynamics | Rituximab binds to the CD20 antigen, which is predominantly expressed on mature B cells and 90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells. |
| Mechanism of Action | The Fab regions of rituximab binds to the CD20 antigen on B lymphocytes, while the Fc domain recruits antibodies and complements to mediate cell lysis. |
| Toxicity | NA |
| Metabolism | Most likely removed by opsonization via the reticuloendothelial system. |
| Absorption | Following the administration of 2 doses of rituximab in patients with rheumatoid arthritis (RA), the mean (± S.D.; % CV) concentrations after the first infusion (Cmax first) and second infusion (Cmax second) were : 157 ( ± 46; 29%) and 183 ( ± 55; 30%) mcg/mL, and 318 ( ± 86; 27%) and 381 ( ± 98; 26%) mcg/mL for the 2 × 500 mg and 2 × 1000 mg doses, respectively |
| 3.1 L |
| Clearance | 0.34 L/day [RA patients] |
| Categories | Amino Acids, Peptides, and Proteins, Antibodies, Antibodies, Monoclonal, Antibodies, Monoclonal, Murine-Derived, Antineoplastic Agents, Antineoplastic Agents, Immunological, Antirheumatic Agents, Biologics for Rheumatoid Arthritis Treatment, Blood Proteins, Cancer immunotherapy, CD20-directed Antibody Interactions, CD20-directed Cytolytic Antibody, Globulins, Immunoglobulins, Immunologic Factors, Immunoproteins, Immunosuppressive Agents, Immunotherapy, Myelosuppressive Agents, Narrow Therapeutic Index Drugs, Proteins, Serum Globulins |
| Patents Number | CA2149329 |
| Date of Issue | 15-Jul-2008 |
| Date of Expiry | 12-Nov-2013 |
| Drug Interaction | Azilsartan medoxomil used in combination with rituximab may lead to hypotension |
| Target | NA |
| Brand Name | Rituxan |
| Company | Biogen Idec Inc., and Genentech USA, Inc |
| Brand Description | Biogen Idec Inc., and Genentech USA, Inc |
| Prescribed For | used in Non–Hodgkin's Lymphoma (NHL), Chronic Lymphocytic Leukemia (CLL), Rheumatoid Arthritis (RA), Granulomatosis with Polyangiitis (GPA) (Wegener's Granulomatosis) and Microscopic Polyangiitis (MPA) |
| Chemical Name | NA |
| Formulation | Rituxan is supplied at a concentration of 10 mg/mL in either 100 mg/10 mL or 500 mg/50 mL single-use vials. The product is formulated in polysorbate 80 (0.7 mg/mL), sodium citrate dihydrate (7.35 mg/mL), sodium chloride (9 mg/mL) and Water for Injection. The pH is 6.5. |
| Physical Appearance | Rituxan is a Sterile, clear, colorless, preservative-free liquid concentrate |
| Route of Administration |  Intravenous administration |
| Recommended Dosage | Initiate infusion at a rate of 50 mg/hr. In the absence of infusion toxicity, increase infusion rate by 50 mg/hr increments every 30 minutes, to a maximum of 400 mg/hr. In NHL the recommended dose is 375 mg/m2 as an Intravenous infusion. In CLL 375 mg/m2 the day prior to the initiation of FC chemotherapy, then 500 mg/m2 on Day 1 of cycles 2–6 (every 28 days). Administer Rituxan as two-1000 mg Intravenous infusions separated by 2 weeks. Administer Rituxan as a 375 mg/m2 Intravenous infusion once weekly for 4 weeks. |
| Contraindication | none |
| Side Effects | Infusion reactions, Mucocutaneous reactions, Hepatitis B reactivation with fulminant hepatitis, Progressive multifocal leukoencephalopathy , Tumor lysis syndrome , Infections, Cardiac arrhythmias, Renal toxicity, Bowel obstruction and perforation |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |