Results 41 to 50 of about 1,701 (184)

Lenacapavir at the Spatiotemporal Limit: Tissue Pharmacokinetics, Pharmacokinetic Tail Dynamics, and the Emergence of Capsid Resistance in Long-Acting HIV Prevention. [PDF]

open access: yesClin Pharmacol
Background: Lenacapavir (LEN), a first-in-class HIV-1 capsid inhibitor administered subcutaneously twice yearly, has demonstrated near-perfect efficacy in Phase 3 trials, generating justified enthusiasm for its potential to reconfigure HIV prevention ...
Chris-Uchendu HC   +8 more
europepmc   +2 more sources

Supplemental Material - Cross-resistance to entry inhibitors and lenacapavir resistance through Week 52 in study CAPELLA

open access: yes, 2023
Supplemental Material for Cross-resistance to entry inhibitors and lenacapavir resistance through Week 52 in study CAPELLA by Nicolas Margot, Nina Pennetzdorfer, Vidula Naik, Martin Rhee, and Christian Callebaut in Journal of Antiviral Therapy.
Nicolas Margot (420403)   +4 more
core   +1 more source

Breakthrough Design of Highly Potent Antivirals Against Wild‐Type HIV‐1 and Lenacapavir‐Resistant M66I Variant

open access: yesAngewandte Chemie, Volume 138, Issue 46, 9 November 2026.
Lenacapavir, the first‐in‐class drug targeting HIV‐1 capsid, is a breakthrough drug in HIV‐1 treatment and prophylaxis. However, a single M66I mutation confers complete viral resistance to lenacapavir. We report herein the design and synthesis of innovative R2 analogs demonstrating low nM potency against HIV‐1 M66I and excellent pharmacokinetics in ...
Nicolas Jamey   +13 more
wiley   +2 more sources

Genetic diversity of capsid protein (p24) in human immunodeficiency virus type-1 (HIV-1) variants circulating in the Russian Federation

open access: yesВопросы вирусологии, 2023
Introduction. The human immunodeficiency virus (HIV) protein p24 plays an important role in the life cycle of the virus, and also is a target for diagnostic tests and for new antiretroviral drugs and therapeutic vaccines.
A. I. Kuznetsova   +10 more
doaj   +1 more source

Efficacy and safety of long-acting lenacapavir for HIV treatment and prevention: A systematic review of randomized trials

open access: yesInternational Journal of Infectious Diseases
Background: Lenacapavir is a first-in-class, long-acting HIV-1 capsid inhibitor enabling treatment and prevention with reduced reliance on daily oral adherence. Evidence from randomized trials across indications remains fragmented.
Blessed Takunda Mukuhlani   +1 more
doaj   +1 more source

Impact of HIV-1 capsid polymorphisms on viral infectivity and susceptibility to lenacapavir

open access: yesmBio
Lenacapavir (LEN) is a first-in-class capsid (CA) inhibitor for the treatment and prevention of HIV-1 infection. While LEN has shown potent antiviral activity across all major HIV-1 subtypes, the impact of existing HIV-1 CA sequence diversity on the ...
Derek Hansen   +8 more
doaj   +1 more source

Preparation of a key intermediate en route to the anti-HIV drug lenacapavir [PDF]

open access: yes, 2023
A very efficient 4-step synthesis of the main fragment of Gilead’s anti-HIV drug lenacapavir is described. The route showcases a 1,2-addition to an intermediate aldehyde using an organozinc halide derived from a commercially available difluorobenzyl ...
Yuting, Hu   +4 more
core   +2 more sources

Genetic Diversity in the Capsid Protein-Coding Region of HIV-1 Circulating in Benguela, Angola: Implications for Primary Resistance to the Novel Capsid Inhibitor Lenacapavir

open access: yesViruses
In 2023, the HIV-1 pandemic claimed around 630,000 lives worldwide due to AIDS-related complications. Its burden is significantly heavier in Sub-Saharan Africa, where an increased HIV-1 genetic diversity is common, which increases the risk of resistance ...
Gonçalo Queirós   +3 more
doaj   +1 more source

Operationalization of the African Medicines Agency: Retrospective evaluation of the continental centralized pilot procedure timelines to recommendation and national registrations

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Aims Regulatory inconsistency across Africa causes duplicative assessments, prolonged approvals, and delayed medical access. To inform the African Medicines Agency (AMA), the African Medicines Regulatory Harmonisation (AMRH) piloted Africa's first continental scientific evaluation of human medicinal products.
Alex Juma Ismail   +4 more
wiley   +1 more source

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