Rituximab

Rituximab
Monoclonal antibody
TypeWhole antibody
SourceChimeric (mouse/human)
TargetCD20
Clinical data
Trade namesRituxan, Mabthera, others
Biosimilarsrituximab-abbs,[1] rituximab-pvvr,[2] rituximab-arrx,[3] Blitzima[4] Ituxredi,[5][6] Riabni,[3] Rixathon,[7] Riximyo,[8] Ruxience,[2] Truxima[1]
AHFS/Drugs.comMonograph
MedlinePlusa607038
License data
Pregnancy
category
Routes of
administration		Intravenous
Drug classMonoclonal antibody
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability100% (IV)
Elimination half-life30 to 400 hours (varies by dose and length of treatment)
ExcretionUncertain: may undergo phagocytosis and catabolism in RES
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.224.382 Edit this at Wikidata
Chemical and physical data
FormulaC6416H9874N1688O1987S44
Molar mass143860.04 g·mol−1
 ☒NcheckY (what is this?)  (verify)

Rituximab, sold under the brand name Rituxan among others, is a monoclonal antibody medication used to treat certain autoimmune diseases and types of cancer.[18] It is used for non-Hodgkin lymphoma, chronic lymphocytic leukemia (in children and adults, but not recommended in elderly patients), rheumatoid arthritis, granulomatosis with polyangiitis, idiopathic thrombocytopenic purpura, pemphigus vulgaris, myasthenia gravis and Epstein–Barr virus-positive mucocutaneous ulcers.[18][19][20][21] It is given by slow intravenous infusion (injected slowly through an IV line).[18]

The most common side effects with intravenous infusions are reactions related to the infusion (such as fever, chills and shivering) while most common serious side effects are infusion reactions, infections and heart-related problems.[16] Similar side effects are seen when it is injected under the skin, with the exception of reactions around the injections site (pain, swelling and rash), which occur more frequently with the skin injections.[16]

Severe side effects include reactivation of hepatitis B in those previously infected, progressive multifocal leukoencephalopathy, toxic epidermal necrolysis, and death.[18][22] It is unclear if use during pregnancy is safe for the developing fetus or newborn baby.[9][18]

Rituximab is a chimeric monoclonal antibody against the protein CD20, which is primarily found on the surface of immune system B cells.[23] When it binds to this protein it triggers cell death.[18]

Rituximab was approved for medical use in 1997.[23] It is on the World Health Organization's List of Essential Medicines.[24] Rituxan is co-marketed by Biogen and Genentech in the US, by Roche elsewhere except Japan, and co-marketed by Chugai Pharmaceuticals and Zenyaku Kogyo in Japan.[25][26]

  1. ^ a b c "Truxima- rituximab-abbs injection solution". DailyMed. Archived from the original on 25 March 2021. Retrieved 26 March 2021.
  2. ^ a b c "Ruxience- rituximab-pvvr injection solution". DailyMed. Retrieved 26 March 2021.
  3. ^ a b c "Riabni- rituximab-arrx injection solution". DailyMed. Archived from the original on 25 March 2021. Retrieved 26 March 2021.
  4. ^ "Blitzima EPAR". European Medicines Agency. 13 July 2017. Archived from the original on 9 September 2021. Retrieved 1 July 2024.
  5. ^ Cite error: The named reference Ituxredi EPAR was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference Ituxredi PI was invoked but never defined (see the help page).
  7. ^ "Rixathon EPAR". European Medicines Agency. 15 June 2017. Archived from the original on 9 September 2021. Retrieved 7 January 2024.
  8. ^ "Summary Basis of Decision (SBD) for Riximyo". Health Canada. 23 October 2014. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
  9. ^ a b "Rituximab Use During Pregnancy". Drugs.com. 16 December 2019. Archived from the original on 30 August 2019. Retrieved 2 February 2020.
  10. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  11. ^ Rituximab (rch) (CAS registry number: 174722-31-7) Archived 30 November 2015 at the Wayback Machine
  12. ^ "Health product highlights 2021: Annexes of products approved in 2021". Health Canada. 3 August 2022. Archived from the original on 25 March 2024. Retrieved 25 March 2024.
  13. ^ "Mabthera 100 mg Concentrate for Solution for Infusion - Summary of Product Characteristics (SmPC)". (emc). 13 March 2021. Archived from the original on 21 January 2022. Retrieved 26 March 2021.
  14. ^ "Mabthera 1400 mg Solution for Subcutaneous Injection - Summary of Product Characteristics (SmPC)". (emc). 13 March 2021. Retrieved 26 March 2021.
  15. ^ Cite error: The named reference Rituxan FDA label was invoked but never defined (see the help page).
  16. ^ a b c "Mabthera EPAR". European Medicines Agency. 17 September 2018. Archived from the original on 9 September 2021. Retrieved 8 September 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  17. ^ "Mabthera PI". Union Register of medicinal products. 3 June 1998. Retrieved 5 July 2024.
  18. ^ a b c d e f "Rituximab". The American Society of Health-System Pharmacists. Archived from the original on 27 March 2016. Retrieved 8 December 2016.
  19. ^ Tandan R, Hehir MK, Waheed W, Howard DB (August 2017). "Rituximab treatment of myasthenia gravis: A systematic review". Muscle & Nerve. 56 (2): 185–196. doi:10.1002/mus.25597. PMID 28164324. S2CID 19504332.
  20. ^ Singer O, McCune WJ (May 2017). "Update on maintenance therapy for granulomatosis with polyangiitis and microscopic polyangiitis". Current Opinion in Rheumatology. 29 (3): 248–253. doi:10.1097/BOR.0000000000000382. PMID 28306595. S2CID 35805200.
  21. ^ Dojcinov SD, Fend F, Quintanilla-Martinez L (March 2018). "EBV-Positive Lymphoproliferations of B- T- and NK-Cell Derivation in Non-Immunocompromised Hosts". Pathogens. 7 (1): 28. doi:10.3390/pathogens7010028. PMC 5874754. PMID 29518976.
  22. ^ "FDA Drug Safety Communication: Boxed Warning and new recommendations to decrease risk of hepatitis B reactivation with the immune-suppressing and anti-cancer drugs Arzerra (ofatumumab) and Rituxan (rituximab)". U.S. Food and Drug Administration (FDA). 29 February 2016. Archived from the original on 28 April 2020. Retrieved 2 February 2020.
  23. ^ a b Bosch X, Ramos-Casals M, Khamashta MA (2013). Drugs Targeting B-Cells in Autoimmune Diseases. Springer Science & Business Media. pp. 1–4. ISBN 9783034807067. Archived from the original on 5 November 2017.
  24. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
  25. ^ "FDA Approves Rituxan Plus Chemotherapy for the Most Common Type of Adult Leukemia" (Press release). Biogen. 18 February 2010. Archived from the original on 9 July 2021. Retrieved 30 June 2021.
  26. ^ "FDA Approves Genentech's Rituxan (rituximab) in Children With Two Rare Blood Vessel Disorders" (Press release). Genentech. 27 September 2019. Retrieved 27 August 2024 – via Business Wire.