Trial reportAntimicrobial agents and chemotherapy2007
Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers.
Trial report in Antimicrobial agents and chemotherapy, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
33 citing papers in PubMed.
- Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection.Antimicrobial agents and chemotherapy · 2007Trial
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- Targeting the host factor HGS-viral membrane protein interaction in coronavirus infection.The Journal of clinical investigation · 2026Article
- Betulinic Acid ω-Triphenylphosphonium Alkyl Esters: Antiproliferative Activities and In Silico Pharmacokinetic Profiles.Biomedicines · 2025Article
- Selected Plant Triterpenoids and Their Derivatives as Antiviral Agents.Molecules (Basel, Switzerland) · 2023Review
- Betulin and Its Derivatives Reduce Inflammation and COX-2 Activity in Macrophages.Inflammation · 2023Article
- Betulinic Acid Decorated with Polar Groups and Blue Emitting BODIPY Dye: Synthesis, Cytotoxicity, Cell-Cycle Analysis and Anti-HIV Profiling.Biomedicines · 2021Article
- Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors.European journal of medicinal chemistry · 2021Article
- Natural Products with Inhibitory Activity against Human Immunodeficiency Virus Type 1.Advances in virology · 2021Review
- Structure and Anti-HIV Activity of Betulinic Acid Analogues.Current medical science · 2018Review
- Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.Journal of medicinal chemistry · 2016Article
- Estrogen Receptor Signaling and the PI3K/Akt Pathway Are Involved in Betulinic Acid-Induced eNOS Activation.Molecules (Basel, Switzerland) · 2016Article
- Pharmacological intervention of HIV-1 maturation.Acta pharmaceutica Sinica. B · 2015Review
- Role of Marine Natural Products in the Genesis of Antiviral Agents.Chemical reviews · 2015Review
- HIV-1 gag: an emerging target for antiretroviral therapy.Current topics in microbiology and immunology · 2015Review
- Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors.Journal of medicinal chemistry · 2012Article
- A historical overview of natural products in drug discovery.Metabolites · 2012Article
- Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.Tetrahedron letters · 2012Article
- New betulinic acid derivatives as potent proteasome inhibitors.Bioorganic & medicinal chemistry letters · 2011Article
- New approaches for antiviral targeting of HIV assembly.Journal of molecular biology · 2011Review
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bevirimat (BVM; formerly known as PA-457) is a novel inhibitor of human immunodeficiency virus (HIV) maturation that is being developed for the treatment of HIV infection. The pharmacokinetics of this agent in healthy male volunteers were studied in a randomized, double-blind study in which the participants received single oral doses of placebo (n = 8) or escalating doses of BVM at 25, 50, 100, or 250 mg (n = 6 per dose); escalation was performed only after the pharmacokinetics and safety of the preceding dose had been evaluated. Plasma was collected over 480 h after dosing and urine was collected over 48 h after dosing for determination of the values of pharmacokinetic parameters. BVM was well absorbed after oral administration, with peak plasma concentrations being achieved 1 to 3 h after dosing. The half-life was 60 to 80 h. The exposure assessed by determination of the peak concentration and the area under the concentration-time curve was dose proportional. Single oral doses of BVM were well tolerated: there were no dose-limiting toxicities, and no serious adverse events were reported. These findings suggest that that BVM offers a favorable pharmacokinetic profile, with predictable pharmacokinetics following the oral administration of single doses. The long half-life of BVM may facilitate once-daily dosing.
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