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1389 details
Primary information
ThPP IDTh1062
Therapeutic Peptide/Protein NameRituximab
SequenceHeavy Chain: QVQLQQPGAELVKPGASVKMSCKASGYTFTSYNMHWV view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight143859.7
Chemical FormulaC6416H9874N1688O1987S44
Isoelectric Point8.68
Hydrophobicity-0.414
Melting Point (℃)61 (FAB f
Half Life0.8 hours (mammalian reticulocytes, in vitro)
DescriptionRituxan 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/DiseaseFor treatment of CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis.
PharmacodynamicsRituximab 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 ActionThe Fab regions of rituximab binds to the CD20 antigen on B lymphocytes, while the Fc domain recruits antibodies and complements to mediate cell lysis.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system.
AbsorptionN.A.
Volume of Distribution3.1 L
Clearance0.34 L/day [RA patients]
CategoriesAntineoplastic Agents, Immunologic Factors and Antirheumatic Agents
Patents NumberCA2149329
Date of Issue16/07/12
Date of Expiry13/11/17
Drug InteractionAzilsartan medoxomil used in combination with rituximab may lead to hypotension
TargetN.A.
Information of corresponding available drug in the market
Brand NameRituxan
CompanyBiogen Idec Inc., and Genentech USA, Inc
Brand DiscriptionRituxan (rituximab) is a genetically engineered chimeric murine/humanmonoclonal IgG1 kappa antibody directed against the CD20 antigen. Rituximab has an approximate molecular weight of 145 kD. Rituximab has a binding affinity for the CD20 antigen of approximately 8.0 nM. Rituximab is produced by mammalian cell (Chinese Hamster Ovary) suspension culture in a nutrient medium containing the antibiotic gentamicin. Gentamicin is not detectable in the final product.
Prescribed forused 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 NameN.A.
FormulationRituxan 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.
Physcial AppearnceRituxan is a Sterile, clear, colorless, preservative-free liquid concentrate
Route of Administration Intravenous administration
Recommended DosageInitiate 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.
Contraindicationnone
Side EffectsInfusion 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 Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b172773b-3905-4a1c-ad95-bab4b6126563 http://www.rxlist.com/rituxan-drug.htm
PubMed ID21813259, 16705086, 15795920, 15201414, 12826649, 9704735, 25609919, 25573987, 25586272
3-D StructureTh1062 (View) or (Download)