Drug intelligence / Profile preview

islatravir + lenacapavir

Development stage
Phase 3
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

A once-weekly oral combination therapy of **islatravir** (a first-in-class nucleoside reverse transcriptase translocation inhibitor developed by Merck) and **lenacapavir** (a first-in-class HIV-1 capsid inhibitor developed by Gilead Sciences) is under investigation for the treatment of HIV-1 infection in virologically suppressed adults. Islatravir inhibits HIV-1 reverse transcription through multiple mechanisms as a deoxyadenosine analog, while lenacapavir interferes with several stages of the HIV lifecycle by binding to the viral capsid protein, blocking processes including nuclear import, assembly, and proper core formation. The combination demonstrated a high rate of sustained viral suppression (94.2% at 48 weeks) in Phase II trials and presents potential as the first once-weekly oral HIV regimen, offering an alternative to daily therapies[1][3][4][5][7][9].

Other names
islatravir and lenacapavir combinationoral weekly islatravir and lenacapavir
02

Targets

p24 (HIV-1 capsid protein p24)Human immunodeficiency virus type 1 reverse transcriptase

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