ArticleMolecular pharmaceutics2023
Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent.
Article in Molecular pharmaceutics, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 41 citations in OpenAlex.
- Effectiveness and Safety of Lenacapavir-Containing Regimens in Highly Experienced HIV-Infected Patients With Multidrug Resistance: Real-world Results From the French Compassionate Use ProgramOpen forum infectious diseases · 2026Trial
- Lenacapavir initiation with concomitant primidone: A case report with therapeutic drug monitoring.British journal of clinical pharmacology · 2026Article
- Review
- Review
- A French national observatory of people with HIV initiating lenacapavir-based treatment after regulatory approval.Antimicrobial agents and chemotherapy · 2026Observational
- Accelerating Subcutaneous Drug Development: A Mechanistic Absorption Model for the Open Systems Pharmacology Framework.CPT: pharmacometrics & systems pharmacology · 2026Article
- Pharmacokinetics, Pharmacodynamics, Efficacy and Drug Resistance Selection of Injectable Long-Acting Lenacapavir Pre-Exposure Prophylaxis (PrEP) Against HIV.CPT: pharmacometrics & systems pharmacology · 2026Article
- Initiation of Long-Acting Antiretroviral Combinations Achieve Sustained Virologic Remission in Early-Life SIV Infection.Research square · 2026Article
- Damaging the conical morphology of HIV-1 capsid by targeting the FG-binding pocket and disfavoring pentameric subunits needed for core closure.bioRxiv : the preprint server for biology · 2026Article
- TARDBP as a regulator of HIV-1 assembly and infection: a review of targeting the viral capsid precursor Pr55Gag and limiting viral core entry.Cell communication and signaling : CCS · 2026Review
- Evaluating Model-Based Extrapolation of Plasma Exposure for Long-Acting Injectable Products: From Single- to Multiple-Dose Trials.CPT: pharmacometrics & systems pharmacology · 2026Article
- Emerging concepts in HIV pre-exposure prophylaxis: focus on twice-yearly lenacapavir.Drugs in context · 2026Review
- Lenacapavir at the Spatiotemporal Limit: Tissue Pharmacokinetics, Pharmacokinetic Tail Dynamics, and the Emergence of Capsid Resistance in Long-Acting HIV Prevention.Clinical pharmacology : advances and applications · 2026Review
- Structural, biophysical, and virological mechanistic characterization of HIV-1 capsid-targeting antivirals.bioRxiv : the preprint server for biology · 2025Article
- Discovery of Lenacapavir: First-in-Class Twice-Yearly Capsid Inhibitor for HIV-1 Treatment and Pre-exposure Prophylaxis.Journal of medicinal chemistry · 2025Article
- Pharmacokinetics, pharmacodynamics, efficacy and drug resistance selection of injectable long-acting lenacapavir pre-exposure prophylaxis (PrEP) against HIV.medRxiv : the preprint server for health sciences · 2025Article
- Recent Advances in Heterocyclic HIV Protease Inhibitors.International journal of molecular sciences · 2025Review
- Pharmacological advances in HIV treatment: from ART to long-acting injectable therapies.Archives of virology · 2025Review
- Impact of HIV-1 capsid polymorphisms on viral infectivity and susceptibility to lenacapavir.mBio · 2025Article
- Drug interactions in people with HIV treated with antivirals for other viral illnesses.Expert opinion on drug metabolism & toxicology · 2025Review
Corrections and comments
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Authors and funding
20 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Lenacapavir (LEN) is a picomolar first-in-class capsid inhibitor of human immunodeficiency virus type 1 (HIV-1) with a multistage mechanism of action and no known cross resistance to other existing antiretroviral (ARV) drug classes. LEN exhibits a low aqueous solubility and exceptionally low systemic clearance following intravenous (IV) administration in nonclinical species and humans. LEN formulated in an aqueous suspension or a PEG/water solution formulation showed sustained plasma exposure levels with no unintended rapid drug release following subcutaneous (SC) administration to rats and dogs. A high total fraction dose release was observed with both formulations. The long-acting pharmacokinetics (PK) were recapitulated in humans following SC administration of both formulations. The SC PK profiles displayed two-phase absorption kinetics in both animals and humans with an initial fast-release absorption phase, followed by a slow-release absorption phase. Noncompartmental and compartmental analyses informed the LEN systemic input rate from the SC depot and exit rate from the body. Modeling-enabled deconvolution of the input rates from two processes: absorption of the soluble fraction (minor) from a direct fast-release process leading to the early PK phase and absorption of the precipitated fraction (major) from an indirect slow-release process leading to the later PK phase. LEN SC PK showed flip-flop kinetics due to the input rate being substantially slower than the systemic exit rate. LEN input rates via the slow-release process in humans were slower than those in both rats and dogs. Overall, the combination of high potency, exceptional stability, and optimal release rate from the injection depot make LEN well suited for a parenteral long-acting formulation that can be administered once up to every 6 months in humans for the prevention and treatment of HIV-1.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.