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Synonyms: HSDB 7455 | IDEC-C2B8 | MabThera® | Rituxan®
rituximab is an approved drug (FDA (1997), EMA (1998))
Compound class: Antibody
Comment: Rituximab is a type I anti-CD20 monoclonal, designed to target surface CD20 on B-lymphocytes. It is a cancer and autoimmune disease drug.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: rituximab
|No information available.|
|Summary of Clinical Use|
|Used to treat CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and several autoimmune conditions (severe active, DMARD/TNF inhibitor-refracrtory rheumatoid arthritis; severe, active granulomatosis with polyangiitis (Wegener's, GPA); microscopic polyangiitis (MPA)). Rituximab is also used to suppress antibody-mediated rejection in living-donor kidney recipients prior to an ABO-incompatible transplant [4-5].
A modified formulation containing rituximab + human hyaluronidase (Rituxan Hycela) that can be delivered subcutaneously (the original rituximab only formulation has to be administered intravenously) was FDA approved in June 2017 for the treatment of previously untreated and relapsed or refractory follicular lymphoma, previously untreated diffuse large B-cell lymphoma (DLBCL), and previously untreated and previously treated chronic lymphocytic leukemia (CLL).
In June 2018, the FDA approved the use of rituximab as a much needed treatment for the potentially life-threatening skin disease pemphigus vulgaris (PV), for use in adult patients with moderate to severe disease. EMA approval for the treatment of PV patients followed in March 2019.
|Mechanism Of Action and Pharmacodynamic Effects|
|Anti-CD20 monoclonal antibody. The Fab regions of this antibody bind to the CD20 antigen on B lymphocytes, and the Fc domain recruits antibodies and complements to mediate cell lysis.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)