The objective of this study was to compare the week 48 antiviral efficacy of cabotegravir plus rilpivirine long-acting dosed every 8 weeks with that of every 4 weeks dosing.
Emergent resistance to LEN was uncommon in treatment-naïve participants receiving SC or oral LEN (0.6%, 1/157). These interim resistance findings support the ongoing evaluation of LEN for treatment and prevention of HIV.
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.
Structural and mechanistic bases for a potent HIV-1 capsid inhibitor Read More »
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.
Promising Early Results for Potent, Long-Acting HIV Injection Read More »
A 5-step enantioselective synthesis of the potent anti-HIV nucleoside islatravir is reported. The highly efficient route was enabled by a novel enantioselective alkynylation of an α,β-unsaturated ketone, a unique ozonolysis-dealkylation cascade in water, and an enzymatic aldol-glycosylation cascade.
We report the practical synthesis of a key fragment of islatravir (MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently under investigation for treatment and pre-exposure prophylaxis (PrEP) against HIV infection. The fragment, the unnatural nucleobase 2-fluoroadenine, is incorporated into MK-8591 via a biocatalytic aldol-glycosylation cascade, which imposes stringent requirements for its synthesis and
An update on HPTN 083, the study that established that PrEP given as an injection every two months had superior efficacy to a daily pill in gay and bisexual men and transgender women, was presented this week at the Conference on Retroviruses and Opportunistic Infections (CROI 2022).
Injected PrEP: cabotegravir maintains its advantage over four years Read More »
Through 48 weeks of a phase 2 dose-ranging study, the novel antiretroviral islatravir had a good safety profile when combined with the nonnucleoside doravirine [1]. The two-drug regimen had modest effects on metabolic variables and body weight.
Islatravir Safety Through 48 Weeks With Doravirine in Phase 2 Trial Read More »
Presentation from 23rd Interantional 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,
Lenacapavir Sustained Delivery Formulation Supports 6-Month Dosing Interval Read More »
