| Identification | Back Directory | [Name]
GS-6207 | [CAS]
2189684-44-2 | [Synonyms]
GS-6207
Lenacapavir
1H-Cyclopropa[3,4]cyclopenta[1,2]pyrazole-1-acetamide, N-[(1S)-1-[3-[4-chloro-3-[(methylsulfonyl)amino]-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl]-6-[3-methyl-3-(methylsulfonyl)-1-butyn-1-yl]-2-pyridinyl]-2-(3,5-difluorophenyl)ethyl]-5,5-difluoro-3b,4,4a,5-tetrahydro-3-(trifluoromethyl)-, (3bS,4aR)- | [Molecular Formula]
C39H32ClF10N7O5S2 | [MDL Number]
MFCD32701907 | [MOL File]
2189684-44-2.mol | [Molecular Weight]
968.28 |
| Chemical Properties | Back Directory | [density ]
1.62±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 250 mg/mL (258.19 mM) | [form ]
Solid | [pka]
4.63±0.30(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Description]
HIV-1 capsid inhibitor GS-6207 (lenacapavir) is a drug being developed by Gilead Sciences, Inc. It is a first-in-class, oral HIV-1 capsid inhibitor. | [Uses]
Lenacapavir can be useful in capsid inhibition in multidrug-resistant HIV-1 infection. | [Application]
Lenacapasvir was first approved in the European Union in 2022 for use in combination with other antiretroviral drugs to treat multidrug-resistant adults with HIV and those who are unable to establish a suppressive antiviral regimen. Subsequently, the drug also received similar approvals in Canada and the United States. Lenacapasvir is available as an oral and injectable therapy and is a long-acting, extended-release drug for the treatment of HIV-1. When used in combination with other antiretroviral drugs, it may only need to be administered once every 6 months, aiming to improve patient compliance and medication adherence. | [Mechanism of action]
GS-6207 disrupts HIV capsid, a multimeric shell that is essential to viral replication, at multiple stages throughout the viral life cycle.
| [Synthesis]
Lenacapavir sodium (GS-6207-02) is a first-in-class HIV capsid inhibitor. Process development of the four-step final assembly of lenacapavir sodium from four synthetic intermediates was reported by Anna M. Wagner and colleagues in 2024. A bis-bromopyridine core is sequentially subjected to an alkynylation, an amide coupling with a chiral pyrazole carboxylic acid, and a Suzuki cross-coupling with an indazole boronic ester. The final step is a telescoped bis-methanesulfonylation and hydrolysis to yield the API.
 | [IC 50]
HIV-1 | [storage]
Store at -20°C |
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