Lenacapavir

Lenacapavir
Names
Trade namesSunlenca
Other namesGS-CA1, GS-6207
IUPAC name
  • 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
Clinical data
Drug classCapsid inhibitors[1]
Main usesHIV/AIDS[2]
Side effectsInjection site reaction, nausea[2]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		By mouth, subcutaneous
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Chemical and physical data
FormulaC39H32ClF10N7O5S2
Molar mass968.28 g·mol−1
3D model (JSmol)
SMILES
  • 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
  • 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

Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat HIV/AIDS.[2] It is used together with other medications, in those with medication resistant disease.[1] It is started by mouth and than given by injection under the skin twice per year.[2]

Common side effects include reactions at the injection site and nausea.[2] Other side effects may include immune reconstitution syndrome.[1] While there is no evidence of harm in pregnacy, such use has not been well studied.[1] It is a capsid inhibitors and works by interfering with multiple steps of the viral lifecycle.[1]

Lenacapavir was approved for medical use in Europe, Canada, and the United States in 2022.[2][1][3] In the United States it costs about 42,250 USD the first year and 39,000 USD each year thereafter as of 2022.[6]

Medical uses

Lenacapavir, in combination with other antiretrovirals, is indicated for the treatment of HIV/AIDS caused by HIV-1.[5][7]

Dosage

On day 1 and 2, 600 mg is given by mouth.[1] This is followed on day 8 by 300 mg.[1] Than on day 15, 927 mg by injection under the skin is given and this is repeated every 26 weeks.[1]

History

Lenacapavir is being developed by Gilead Sciences.[8] Lenacapavir is the first of a new class of drugs called capsid inhibitors.[7]

As of 2021, it is in phase II/III clinical trials.[9] 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).[9][10]

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.[7] These participants had to have high levels of virus in their blood despite being on antiretroviral drugs.[7] Participants were enrolled into one of two study groups.[7] One group was randomized to receive either lenacapavir or placebo in a double-blind fashion, and the other group received open-label lenacapavir.[7] 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.[7]

The U.S. Food and Drug Administration (FDA) granted the application for lenacapavir priority review, fast track, and breakthrough therapy designations.[7] The FDA granted the approval of Sunlenca to Gilead Sciences.[7]

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.[11] The applicant for this medicinal product is Gilead Sciences Ireland UC.[11]

Lenacapavir was approved for medical use in the European Union in August 2022,[2] in Canada in November 2022,[3][4] and in the United States in December 2022.[7]

References

  1. 1 2 3 4 5 6 7 8 9 "DailyMed - SUNLENCA- lenacapavir sodium tablet, film coated SUNLENCA- lenacapavir sodium kit". dailymed.nlm.nih.gov. Archived from the original on 21 January 2023. Retrieved 1 February 2023.
  2. 1 2 3 4 5 6 7 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.
  3. 1 2 3 "Sunlenca Product information". Health Canada. 25 April 2012. Archived from the original on 15 January 2023. Retrieved 23 December 2022.
  4. 1 2 "Sunlenca Product information". Health Canada. 25 April 2012. Archived from the original on 15 January 2023. Retrieved 23 December 2022.
  5. 1 2 "Archive copy" (PDF). Archived (PDF) from the original on 2023-01-15. Retrieved 2022-12-23.{{cite web}}: CS1 maint: archived copy as title (link)
  6. ↑ "FDA Approves First-in-Class Drug for HIV". Medscape. Archived from the original on 31 December 2022. Retrieved 1 February 2023.
  7. 1 2 3 4 5 6 7 8 9 10 "FDA Approves New HIV Drug for Adults with Limited Treatment Options" (Press release). U.S. Food and Drug Administration (FDA). 22 December 2022. Archived from the original on 15 January 2023. Retrieved 23 December 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  8. ↑ 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.
  9. 1 2 Boerner H (11 March 2021). "Lenacapavir Effective in Multidrug Resistant HIV". Medscape. Archived from the original on 16 March 2021. Retrieved 15 March 2021.
  10. ↑ 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.
  11. 1 2 "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.
Identifiers:
  • "Lenacapavir". Drug Information Portal. U.S. National Library of Medicine. Archived from the original on 2022-06-26. Retrieved 2022-12-23.
  • "Lenacapavir sodium". Drug Information Portal. U.S. National Library of Medicine. Archived from the original on 2023-01-15. Retrieved 2022-12-23.
  • "Lenacapavir". Clinical Info. National Institutes of Health. Archived from the original on 2023-01-15. Retrieved 2022-12-23.
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