Basiliximab

Basiliximab, sold under the brand name Simulect, is a monoclonal antibody used to prevent rejection in kidney transplants.^[2][3] It is a chimeric mouse-human monoclonal antibody to the α chain (CD25) of the IL-2 receptor of T cells.^[2] It is used in combination with other medicines used to prevent organ rejection.^[2][3]

Basiliximab

Monoclonal antibody
Type	Whole antibody
Source	Chimeric (mouse/human)
Target	CD25
Clinical data
Trade names	Simulect
AHFS/Drugs.com	Monograph
MedlinePlus	a612013
License data	EU EMA: by INN US DailyMed: Basiliximab
Pregnancy category	AU: D
Routes of administration	Intravenous
Drug class	Immunosuppressants
ATC code	L04AC02 (WHO)
Legal status
Legal status	US: WARNING[1]Rx-only[2] EU: Rx-only[3] In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life	7.2 days
Identifiers
CAS Number	179045-86-4 N
DrugBank	DB00074 Y
ChemSpider	none
UNII	9927MT646M
KEGG	D03058
ChEMBL	ChEMBL1201439 N
Chemical and physical data
Formula	C6378H9844N1698O1997S48
Molar mass	143801.68 g·mol−1
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The most common side effects (seen in more than 20% of patients) include constipation, urinary tract infections (infection of the structures that carry urine), pain, nausea (feeling sick), peripheral oedema (swelling), hypertension (high blood pressure), anemia (low red blood cell counts), headache, hyperkalaemia (high blood potassium levels), hypercholesterolaemia (high blood cholesterol levels), surgical wound complication, weight increase, increased serum creatinine (a marker of kidney problems), hypophosphataemia (low blood phosphate levels), diarrhea and upper respiratory tract infection (colds).^[3]

Basiliximab was approved for medical use in the United States and in the European Union in 1998.^[2][3][4]

Medical uses

Basiliximab is indicated for the prophylaxis of acute organ rejection in de-novo allogeneic renal transplantation.^[3] It is to be used concomitantly with ciclosporin for microemulsion- and corticosteroid-based immunosuppression, in people with panel reactive antibodies less than 80%, or in a triple maintenance immunosuppressive regimen containing ciclosporin for microemulsion, corticosteroids and either azathioprine or mycophenolate mofetil.^[3]

Basiliximab is an immunosuppressant agent used to prevent immediate transplant rejection in people who are receiving kidney transplants, in combination with other agents.^[5] It has been reported that some cases of lichen planus have been successfully treated with basiliximab as an alternative therapy to cyclosporin. No short-term side effects have been reported.^[6]

Mechanism of action

Basiliximab competes with IL-2 to bind to the alpha chain subunit of the IL2 receptor on the surface of the activated T lymphocytes and thus prevents the receptor from signaling. This prevents T cells from replicating and also from activating B cells, which are responsible for the production of antibodies, which would bind to the transplanted organ and stimulate an immune response against the transplant.^[7][8]

Chemistry

It is a chimeric CD25 monoclonal antibody of the IgG1 isotype.^[7][8]

History

It is a Novartis product and was approved by the Food and Drug Administration (FDA) in 1998.^[9]

References

1. "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.
2. "Simulect- basiliximab injection, powder, for solution". DailyMed. 6 October 2022. Archived from the original on 6 October 2022. Retrieved 27 February 2023.
3. "Simulect EPAR". European Medicines Agency. Archived from the original on 11 January 2022. Retrieved 27 February 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
4. "Basiliximab Product Approval Information - Licensing Action". U.S. Food and Drug Administration (FDA). 20 February 2009. Archived from the original on 13 January 2017. Retrieved 27 February 2023.
5. MedlinePlus. Last Revised - 15 June 2012 Basiliximab Injection Archived 5 July 2016 at the Wayback Machine
6. Katsambas AD, Lotti TM (2003). European handbook of dermatological treatments (2nd ed.). p. 291. ISBN 3-540-00878-0.
7. Hardinger KL, Brennan DC, Klein CL (July 2013). "Selection of induction therapy in kidney transplantation". Transplant International. 26 (7): 662–72. doi:10.1111/tri.12043. PMID 23279211. S2CID 3296555.
8. "Basiliximab label" (PDF). Food and Drug Administration. Archived (PDF) from the original on 22 February 2017. Retrieved 16 December 2019.
9. Waldmann TA (March 2003). "Immunotherapy: past, present and future". Nature Medicine. 9 (3): 269–77. doi:10.1038/nm0303-269. PMID 12612576. S2CID 9745527. Archived from the original on 13 April 2021. Retrieved 5 June 2020.