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 Rituenza's marketing authorisation withdrawn in EU in 2017 at Celltrion's request.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
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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

IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: rituximab

References
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Sjogren's syndrome: New paradigms and areas for future research.
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Therapeutic application of chimeric and radiolabeled antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma.
Patent number: US5843439. Assignee: Anderson DR, Nabil H, Leonard JE, Newman RA, Reff ME, Rastetter WH. Priority date: 13/11/1992. Publication date: 01/12/1998.
3. Anderson DR, Rastetter WH, Hanna N, Leonard JE, Newman RA, Reff ME. (1994)
Therapeutic application of chimeric and radiolabeled antibodies to human b lymphocyte restricted differentiation antigen for treatment of b cell lymphoma.
Patent number: WO1994011026. Assignee: Idec Pharma Corp. Priority date: 26/02/2015. Publication date: 26/05/1994.
4. Bekker P, Dairaghi D, Seitz L, Leleti M, Wang Y, Ertl L, Baumgart T, Shugarts S, Lohr L, Dang T et al.. (2016)
Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study.
PLoS ONE, 11 (10): e0164646. [PMID:27768695]
5. Carvelli J, Demaria O, Vély F, Batista L, Chouaki Benmansour N, Fares J, Carpentier S, Thibult ML, Morel A, Remark R et al.. (2020)
Association of COVID-19 inflammation with activation of the C5a-C5aR1 axis.
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6. Fehr T, Stussi G. (2012)
ABO-incompatible kidney transplantation.
Curr Opin Organ Transplant, 17 (4): 376-85. [PMID:22790072]
7. Hawksworth OA, Li XX, Coulthard LG, Wolvetang EJ, Woodruff TM. (2017)
New concepts on the therapeutic control of complement anaphylatoxin receptors.
Mol Immunol, 89: 36-43. [PMID:28576324]
8. Li XX, Lee JD, Massey NL, Guan C, Robertson AAB, Clark RJ, Woodruff TM. (2020)
Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function.
Biochem Pharmacol, 180: 114156. [PMID:32682759]
9. Macklin PS, Morris PJ, Knight SR. (2015)
A systematic review of the use of rituximab as induction therapy in renal transplantation.
Transplant Rev (Orlando), 29 (2): 103-8. [PMID:25555541]
10. Monk PN, Scola AM, Madala P, Fairlie DP. (2007)
Function, structure and therapeutic potential of complement C5a receptors.
Br J Pharmacol, 152 (4): 429-48. [PMID:17603557]
11. Stein R, Qu Z, Chen S, Rosario A, Shi V, Hayes M, Horak ID, Hansen HJ, Goldenberg DM. (2004)
Characterization of a new humanized anti-CD20 monoclonal antibody, IMMU-106, and Its use in combination with the humanized anti-CD22 antibody, epratuzumab, for the therapy of non-Hodgkin's lymphoma.
Clin Cancer Res, 10 (8): 2868-78. [PMID:15102696]
12. Verstappen GM, van Nimwegen JF, Vissink A, Kroese FGM, Bootsma H. (2017)
The value of rituximab treatment in primary Sjögren's syndrome.
Clin Immunol, 182: 62-71. [PMID:28478105]
13. Vlaar APJ, de Bruin S, Busch M, Timmermans SAMEG, van Zeggeren IE, Koning R, Ter Horst L, Bulle EB, van Baarle FEHP, van de Poll MCG et al.. (2020)
Anti-C5a antibody IFX-1 (vilobelimab) treatment versus best supportive care for patients with severe COVID-19 (PANAMO): an exploratory, open-label, phase 2 randomised controlled trial.
Lancet Rheumatol, 2 (12): e764-e773. DOI: 10.1016/S2665-9913(20)30341-6 [PMID:33015643]