title: The effect of ravuconazole on the pharmacokinetics of nelfinavir in healthy male volunteers.
abstract: An open-label, nonrandomized study was conducted to assess the effect of ravuconazole on the pharmacokinetics of concomitantly administered nelfinavir. Healthy volunteers received 750 mg nelfinavir on day 1, 750 mg nelfinavir and 400 mg ravuconazole on day 2, 400 mg ravuconazole on days 3 to 28, and 750 mg nelfinavir and 400 mg ravuconazole on day 29. The geometric means of C(max) and area under the curve of nelfinavir coadministered with ravuconazole were 30.7% and 31.9% higher on day 2 and 7.9% and 16.2% lower on day 29, respectively, compared to the corresponding values on day 1. These findings are consistent with the potential for ravuconazole to both inhibit and induce CYP3A isozymes. The alterations in the systemic exposure to nelfinavir were within the range defined by the 90% confidence interval. The study data indicate that coadministration of ravuconazole did not result in a clinically significant change in the plasma levels of nelfinavir.
authors.affiliation: Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08542-4000, USA.
authors.forename: Jing-He
authors.initials: JH
authors.lastname: Yan
authors.forename: Maria R
authors.initials: MR
authors.lastname: Marino
authors.forename: Robert A
authors.initials: RA
authors.lastname: Smith
authors.forename: Vanaja
authors.initials: V
authors.lastname: Kanamaluru
authors.forename: Edward M
authors.initials: EM
authors.lastname: O'Mara
authors.forename: Dennis M
authors.initials: DM
authors.lastname: Grasela
mesh_terms: D000293:Adolescent; D000328:Adult; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D004347:Drug Interactions; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D019888:Nelfinavir / Q000009:adverse effects / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000009:adverse effects / Q000494:pharmacology*; D014230:Triazoles / Q000009:adverse effects / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D013844:Thiazoles; D014230:Triazoles; C104066:ER 30346; D051544:Cytochrome P-450 CYP3A; D019888:Nelfinavir