An oral human drug absorption study to assess the impact of site of delivery on the bioavailability of bevirimat.

Bevirimat is a first in class, orally active, potent and selective inhibitor of HIV-1. It may have utility for the treatment of HIV-1-infected patients who are failing current regimens because of the development of drug resistance. In earlier studies in HIV-1-infected patients, an immediate-release tablet formulation exhibited a relative bioavailability (F(rel)) of 50% or greater and a higher intersubject variability than an oral solution.

Pharmacokinetic properties and tolerability of bevirimat and atazanavir in healthy volunteers: an open-label, parallel-group study.

Background: Bevirimat, an inhibitor of HIV-1 maturation, is currently in clinical development for the treatment of HIV-1 infection. It undergoes glucuronidation via uridine diphosphate glucuronosyltransferases (UGTs). The protease inhibitor atazanavir is a potent inhibitor of UGT1A1.

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.

Bevirimat [3-O-(3',3'-dimethylsuccinyl)betulinic acid] is the first in a new class of anti-human immunodeficiency virus (HIV) drugs that inhibit viral maturation by specifically blocking cleavage of the Gag capsid (CA) precursor, CA-SP1, to mature CA protein, resulting in defective core condensation and release of immature noninfectious virions. Four cohorts of six HIV-infected adults, with CD4 counts of >200 and plasma viral loads of 5,000 to 250,000 transcripts/ml and not currently receiving antiretroviral therapy, were randomized to receive a single oral dose of placebo, 75, 150, or 250 mg of bevirimat. Thirty blood samples for drug concentrations and 20 HIV RNA measures were collected from each subject over a 20-day period.

Multiple-dose pharmacokinetics and safety of bevirimat, a novel inhibitor of HIV maturation, in healthy volunteers.

Background And Objective: Bevirimat [3-O-(3',3'-dimethylsuccinyl)-betulinic acid] is a novel inhibitor of HIV-1 maturation. This study was performed to investigate the pharmacokinetics and safety of bevirimat during repeated dosing in healthy volunteers.

Subjects And Methods: The study was a 10-day, randomised, double-blind, placebo-controlled, dose escalation study.

Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers.

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.