Important note: Information in this article was accurate in August 1999. The state of the art may have changed since the publication date.AIDSWEEKLY Plus; Monday, August 30, 1999
Daniel J. DeNoon, Senior Editor
CW HENDERSON PUBLISHER -- The protease inhibitor next in line for approval has favorable single-dose pharmacokinetics (PK).
Glaxo Wellcome researchers Brian M. Sadler and colleagues studied the PK of amprenavir (formerly known as VX-478 or 141W94) in patients with HIV infection.
"Amprenavir appears to be safe and well tolerated over the dose range of 150 to 1,200 mg," they reported. "On the basis of the present single-dose studies, amprenavir is an HIV protease inhibitor with favorable absorption and clearance pharmacokinetics that are only minimally affected by food."
Sadler et al. reported their findings in the journal Antimicrobial Agents and Chemotherapy ("Safety and Pharmacokinetics of Amprenavir (141W94), a Human Immunodeficiency Virus (HIV) Type 1 Protease Inhibitor, Following Oral Administration of Single Doses to HIV Infected Adults," Antimic Ag Chem, 1999;43(7):1686-92).
Three of the four currently approved protease inhibitors (PI) require attention to meal times. Indinavir absorption is reduced with a standard meal, while nelfinavir and saquinavir absorption significantly increase when taken with a meal.
The studies show that amprenavir absorption is not significantly affected even by a high-fat meal. The drug has a half-life of eight hours, suggesting twice-daily dosing.
One serious problem with the drug has been solved: the early hard-gel formulation was unstable at room temperature, requiring that the drug be constantly refrigerated until use. A new soft-gel formulation has comparable PK and is completely stable at room temperature.
The corresponding author for this study is Brian M. Sadler, Division of Clinical Pharmacology, Glaxo Wellcome Inc., Research Triangle Park, NC 27709. Phone: (919) 483- 1449. Fax: (919) 483-6380. Email: <bms44974@glaxowellcome.com>.
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