rituximab   Click here for help

GtoPdb Ligand ID: 6780

Synonyms: HSDB 7455 | IDEC-C2B8 | MabThera® | Rituxan®
Approved drug Immunopharmacology Ligand
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 Rituenza's marketing authorisation withdrawn in EU in 2017 at Celltrion's request.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
rituximab-arrx; ABP 798RiabniAmgenApproved (FDA 2020)NHL, CLL, GPA (Wegener's granulomatosis), and MPA
rituximab; RTXM83-MB01; RTXM-83Novex; RigetuxermAbxienceApproved (Brazil 2019; and other Latin American countries)NHL
BI 695500 Boehringer IngelheimDevelopment halted at Ph 3 (NCT02417129)NHL
Click here for help

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 interactive charts of activity data across species

IUPHAR Pharmacology Education Project (PEP) logo

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) [11].
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) Primary target of this compound Hs Antibody Binding 8.5 pKd - 11
⤷ pKd 8.5 (Kd 3.1x10-9 M) [11]
Targets where the ligand is described in the comment field
Target Comment
C5a1 receptor C5a1 receptor is currently referred to as C5aR1 in the literature. C5a1 has been an attractive target for pharmacological inhibition to treat a myriad of inflammatory and neurodegenerative diseases. Several C5a1 antagonists have been reported that have progressed to various stages of clinical development [7-8,10], although none are yet approved for use in humans. The non-peptide C5aR1 inhibitor CCX168 (Avacopan®), developed by ChemoCentryx, is currently the most clinically advanced C5aR1 inhibitor [4]. The drug has recently completed a Phase III clinical trial for ANCA-associated vasculitis under a concomitant treatment scheme with rituximab or cyclophosphamide/azathioprine (NCT02994927). Considering the potential benefits of blocking the C5a-C5aR1 axis to limit myeloid infiltration and prevent excessive lung inflammation in Coronavirus disease 2019 (COVID-19) [5], the two anti-C5a/C5aR1 blocking antibodies, avdoralimab (IPH5401) and vilobelimab (IFX-1), are currently being studied in patients with COVID-19 severe pneumonia (NCT04371367 and NCT04333420 for IPH5401 and IFX-1, respectively) [13].