Lenacapavir

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Lenacapavir
Lenacapavir.svg
Clinical data
Other namesGS-6207
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
  • N-[(1R)-1-[3-[4-Chloro-3-(cyclopropylsulfonylamino)-1-(2,2-difluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonylbut-1-ynyl)pyridin-2-yl]-2-(3,5-difluorophenyl)ethyl]-2-[(2R,4S)-9-(difluoromethyl)-5,5-difluoro-7,8-diazatricyclo[4.3.0.02,4]nona-1(6),8-dien-7-yl]acetamide
CAS Number
  • 2189684-45-3
PubChem CID
Chemical and physical data
FormulaC41H36ClF8N7O5S2
Molar mass958.34 g·mol−1
3D model (JSmol)
  • CC(C)(C#CC1=NC(=C(C=C1)C2=C3C(=C(C=C2)Cl)C(=NN3CC(F)F)NS(=O)(=O)C4CC4)[C@@H](CC5=CC(=CC(=C5)F)F)NC(=O)CN6C7=C([C@@H]8C[C@@H]8C7(F)F)C(=N6)C(F)F)S(=O)(=O)C
  • InChI=1S/C41H36ClF8N7O5S2/c1-40(2,63(3,59)60)11-10-22-4-7-24(25-8-9-28(42)33-36(25)56(17-30(45)46)54-39(33)55-64(61,62)23-5-6-23)34(51-22)29(14-19-12-20(43)15-21(44)13-19)52-31(58)18-57-37-32(35(53-57)38(47)48)26-16-27(26)41(37,49)50/h4,7-9,12-13,15,23,26-27,29-30,38H,5-6,14,16-18H2,1-3H3,(H,52,58)(H,54,55)/t26-,27+,29-/m1/s1
  • Key:CPCUUUACFKQOHY-IUAQSZDVSA-N

Lenacapavir (development code GS-6207) is an experimental drug for the treatment of HIV being developed by Gilead Sciences.[1] As of 2021, it is in Phase 2/3 clinical trials.[2] 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).[2][3]

If successful in clinical trials, it would become a first-in-class HIV capsid inhibitor for the treatment of HIV.[4]

References

  1. ^ 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.
  2. ^ a b Boerner H (11 March 2021). "Lenacapavir Effective in Multidrug Resistant HIV". Medscape.
  3. ^ Highleyman L (15 March 2021). "Lenacapavir Shows Promise for Long-Acting HIV Treatment and Prevention". POZ.
  4. ^ Gallagher GM (12 March 2020). "Trial Data Released for Investigational HIV-1 Capsid Inhibitor". Contagion Live.