Lenacapavir

Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat HIV/AIDS.[8] It is taken by mouth or by subcutaneous injection.[8]

Lenacapavir
Clinical data
Trade namesSunlenca
Other namesGS-CA1, GS-6207
License data
Pregnancy
category
Routes of
administration		By mouth, subcutaneous
Drug classCapsid inhibitors
ATC code
Legal status
Legal status
Identifiers
  • N-[(1S)-1-{3-[4-chloro-3-(methanesulfonamido)-1-(2,2,2- trifluoroethyl)-1H-indazol-7-yl]-6-[3-(methanesulfonyl)-3- methylbut-1-yn-1-yl]pyridin-2-yl}-2-(3,5-difluorophenyl)ethyl]-2- [(3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro- 1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl]acetamide
CAS Number
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
Chemical and physical data
FormulaC39H32ClF10N7O5S2
Molar mass968.28 g·mol−1
3D model (JSmol)
  • CC(C)(C#Cc1ccc(-c2ccc(Cl)c3c(NS(C)(=O)=O)nn(CC(F)(F)F)c23)c([C@H](Cc2cc(F)cc(F)c2)NC(=O)Cn2nc(C(F)(F)F)c3c2C(F)(F)[C@@H]2C[C@H]32)n1)S(C)(=O)=O
  • InChI=1S/C39H32ClF10N7O5S2/c1-36(2,63(3,59)60)10-9-21-5-6-22(23-7-8-26(40)30-32(23)57(17-37(43,44)45)54-35(30)55-64(4,61)62)31(51-21)27(13-18-11-19(41)14-20(42)12-18)52-28(58)16-56-34-29(33(53-56)39(48,49)50)24-15-25(24)38(34,46)47/h5-8,11-12,14,24-25,27H,13,15-17H2,1-4H3,(H,52,58)(H,54,55)/t24-,25+,27-/m0/s1
  • Key:BRYXUCLEHAUSDY-WEWMWRJBSA-N

The most common side effects include reactions at the injection site and nausea.[8][9]

Lenacapavir was approved for medical use in the European Union in August 2022,[8][10] in Canada in November 2022,[4][5] and in the United States in December 2022.[9][11]

Lenacapavir is the first of a new class of drugs called capsid inhibitors to be FDA-approved for treating HIV/AIDS.[9] Lenacapavir works by blocking the HIV-1 viral capsid, interfering with essential steps of the virus's lifecycle.[9] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[12]

Medical uses

Lenacapavir, in combination with other antiretrovirals, is indicated for the treatment of HIV/AIDS. It is used in heavily treatment-experienced adults with multiple drug resistance in whom current antiretroviral therapy is ineffective due to resistance, intolerance or safety considerations.[7][9]

History

Lenacapavir is being developed by Gilead Sciences.[13]

As of 2021, it is in phase II/III clinical trials.[14] It is being investigated as a treatment for HIV patients infected with multidrug-resistant virus and as a twice-yearly injectable for pre-exposure prophylaxis (PrEP).[14][15]

The safety and efficacy of lenacapavir were established through a multicenter clinical trial with 72 participants whose HIV infections were resistant to multiple classes of HIV medications.[9] These participants had to have high levels of virus in their blood despite being on antiretroviral drugs.[9] Participants were enrolled into one of two study groups.[9] One group was randomized to receive either lenacapavir or placebo in a double-blind fashion, and the other group received open-label lenacapavir.[9] The primary measure of efficacy was the proportion of participants in the randomized study group who achieved a certain level of reduction in virus during the initial 14 days compared to baseline.[9]

The U.S. Food and Drug Administration (FDA) granted the application for lenacapavir priority review, fast track, and breakthrough therapy designations.[9] The FDA granted the approval of Sunlenca to Gilead Sciences.[9]

Society and culture

On 23 June 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Sunlenca, intended for the treatment of adults with multidrug‑resistant human immunodeficiency virus type 1 (HIV‑1) infection.[16] The applicant for this medicinal product is Gilead Sciences Ireland UC.[16]

Lenacapavir was approved for medical use in the European Union in August 2022,[8][17] in Canada in November 2022,[4][5] and in the United States in December 2022.[9]

References
  1. "Sunlenca". Therapeutic Goods Administration (TGA). 6 April 2023. Retrieved 7 April 2023.
  2. "Sunlenca lenacapavir (as sodium) 300 mg film coated tablet blister pack (392350)". Therapeutic Goods Administration (TGA). 28 March 2023. Retrieved 7 April 2023.
  3. "Sunlenca lenacapavir (as sodium) 463.5 mg/1.5 mL solution for injection vial (386895)". Therapeutic Goods Administration (TGA). 28 March 2023. Retrieved 7 April 2023.
  4. "Sunlenca Product information". Health Canada. 25 April 2012. Retrieved 23 December 2022.
  5. "Sunlenca Product information". Health Canada. 25 April 2012. Retrieved 23 December 2022.
  6. "Summary Basis of Decision - Sunlenca". Health Canada. 10 March 2023. Retrieved 24 April 2023.
  7. "Sunlenca- lenacapavir sodium tablet, film coated Sunlenca- lenacapavir sodium kit". DailyMed. 21 December 2022. Retrieved 21 January 2023.
  8. "Sunlenca EPAR". European Medicines Agency (EMA). 22 June 2022. Archived from the original on 26 August 2022. Retrieved 25 August 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9. "FDA Approves New HIV Drug for Adults with Limited Treatment Options" (Press release). U.S. Food and Drug Administration (FDA). 22 December 2022. Retrieved 23 December 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  10. "Gilead Announces First Global Regulatory Approval of Sunlenca (Lenacapavir), the Only Twice-Yearly HIV Treatment Option". Gilead Sciences, Inc. (Press release). 22 August 2022. Retrieved 23 December 2022.
  11. "Sunlenca (lenacapavir) Receives FDA Approval as a First-in-Class, Twice-Yearly Treatment Option for People Living With Multi-Drug Resistant HIV". Gilead Sciences, Inc. (Press release). 22 December 2022. Retrieved 23 December 2022.
  12. "Advancing Health Through Innovation: New Drug Therapy Approvals 2022". U.S. Food and Drug Administration (FDA). 10 January 2023. Retrieved 22 January 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  13. Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, et al. (August 2020). "Clinical targeting of HIV capsid protein with a long-acting small molecule". Nature. 584 (7822): 614–618. Bibcode:2020Natur.584..614L. doi:10.1038/s41586-020-2443-1. PMC 8188729. PMID 32612233. S2CID 220293679.
  14. Boerner H (11 March 2021). "Lenacapavir Effective in Multidrug Resistant HIV". Medscape. Archived from the original on 16 March 2021. Retrieved 15 March 2021.
  15. Highleyman L (15 March 2021). "Lenacapavir Shows Promise for Long-Acting HIV Treatment and Prevention". POZ. Archived from the original on 19 July 2021. Retrieved 15 March 2021.
  16. "Sunlenca: Pending EC decision". European Medicines Agency. 23 June 2022. Archived from the original on 26 June 2022. Retrieved 26 June 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  17. "Sunlenca Product information". Union Register of medicinal products. Retrieved 3 March 2023.
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