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 Rituenza's marketing authorisation withdrawn in EU in 2017 at Celltrion's request.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, EMA 2020)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

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.

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View interactive charts of activity data across species

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View more information in the IUPHAR Pharmacology Education Project: rituximab

Bioactivity Comments
The patents covering rituximab do not contain any data regarding antibody-antigen affinity [2-3], but a dissociation constant is provided by Stein et al (2004) [6].
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD20 (membrane-spanning 4-domains, subfamily A, member 1) Hs Antibody Binding 8.5 pKd - 6
⤷ pKd 8.5 (Kd 3.1x10-9 M) [6]