Lenacapavir

Current HIV treatments require drugs that must be taken daily, and care would be improved with an effective drug that is long-acting. GS-6207 (Lenacapavir) is a drug developed by Gilead Sciences that shows potential for a 6-month dosing interval and is in phase 2/3 clinical trials.

A highly potent, long-acting drug candidate with a novel mode of action showed promising anti-HIV activity in recent phase 1 trials. The slow-release compound, lenacapavir (previously GS-6207), would be used in combination with other antiretroviral agents, researchers said at the 23rd International AIDS Conference.

♦ Single LEN SC doses up to 900 mg were generally safe and well tolerated – Injection-site reactions were common, but all were mild ♦ LEN 900 mg SC maintained target concentrations for 26 wk (6 mon), supporting its use as a q6mon antiretroviral agent ♦ PK simulations support LEN regimen with oral PK loading,

This article describes the potential of GS-6207, a small molecule that disrupts the functions of HIV capsid protein, as a long-acting agent to treat or prevent infection with HIV.

In this Phase 1 study, single SC doses of LEN resulted in potent antiviral activity over 10 days ♦ Rare low-level resistance to LEN via a single mutation (Q67H) emerged only at LEN exposures below the expected exposure in Ph2/3 studies ♦ Previous in vitro characterization identified that Q67H mutation had the least impact on

Ongoing studies are evaluating long-acting dosing of lenacapavir for treating HIV-1 in combination with other antiretrovirals and preventing HIV-1 as a single agent.