rituximab   

GtoPdb Ligand ID: 6780

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.

Biosimilars:
NameTrade nameCompanyClinical PhaseIndications
CT-P10; rituximab-abbsBlitzima; Truxima; Tuxella (renamed Rituenza); RitemviaCelltrionApproved (EMA 2017, FDA 2018)Non-Hodgkin lymphoma (NHL), chronic lymphocytic leukaemia (CLL), granulomatosis with polyangiitis (GPA), microscopic polyangiitis (MPA) and severe rheumatoid arthritis (Truxima only). Rituenza's marketing authorisation withdrawn in EU in 2017 at Celltrion's request.
PF-05280586; rituximab-pvvrRuxience PfizerApproved (FDA 2019)NHL, CLL, GPA, MPA
BCD-020AcellBiaBiocadApproved in 2014 by the Ministry of Health of the Russian Federation; Ph 3 trials elsewhere- see NCT02744196 and NCT01759030 as examplesRheumatoid arthritis
GP2013Rixathon; RiximyoSandozApproved (EMA 2017) NHL, CLL
SAIT101 Archigen BiotechPh 3 comparision clinical trial with MabThera® for follicular lymphoma (NCT02809053), and Ph 1 NCT02819726 for rheumatoid arthritisRheumatoid arthritis, follicular lymphoma
ABP 798 AmgenPh 3 (NCT02747043; NCT02792699)Rheumatoid arthritis, NHL
BI 695500 Boehringer IngelheimDevelopment halted at Ph 3 (NCT02417129)NHL
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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.
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