Effect of posaconazole on the pharmacokinetics of fosamprenavir and vice versa in healthy volunteers

J Antimicrob Chemother. 2010 Oct;65(10):2188-94. doi: 10.1093/jac/dkq280. Epub 2010 Jul 28.

Abstract

Objectives: To manage the interaction between fosamprenavir/ritonavir and posaconazole, we hypothesized that ritonavir can be replaced by posaconazole as an alternative booster of fosamprenavir with no significant influence on posaconazole pharmacokinetics.

Methods: This was an open-label, randomized, three period, cross-over, single-centre trial in 24 healthy volunteers. All subjects received the following three treatments for 10 days, separated by washout periods of 17 days: posaconazole 400 mg twice daily; fosamprenavir/ritonavir 700/100 mg twice daily; posaconazole 400 mg twice daily with fosamprenavir 700 mg twice daily.

Results: Twenty subjects completed the trial. Geometric mean ratios (GMR; +90% confidence interval) of posaconazole AUC and C(max) when taken with fosamprenavir versus posaconazole alone were 0.77 (0.68-0.87) and 0.79 (0.71-0.89), respectively. The GMRs of amprenavir AUC and C(max) when taken as fosamprenavir and posaconazole versus fosamprenavir/ritonavir were 0.35 (0.32-0.39) and 0.64 (0.55-0.76), respectively. No serious adverse events were reported during the trial.

Conclusion: Unboosted fosamprenavir should not be used concomitantly with posaconazole.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacokinetics*
  • Antifungal Agents / administration & dosage
  • Antifungal Agents / pharmacokinetics*
  • Carbamates / administration & dosage
  • Carbamates / pharmacokinetics*
  • Cross-Over Studies
  • Drug Interactions
  • Female
  • Furans
  • Healthy Volunteers
  • Humans
  • Male
  • Middle Aged
  • Organophosphates / administration & dosage
  • Organophosphates / pharmacokinetics*
  • Sulfonamides / administration & dosage
  • Sulfonamides / pharmacokinetics*
  • Triazoles / administration & dosage
  • Triazoles / pharmacokinetics*
  • Young Adult

Substances

  • Anti-HIV Agents
  • Antifungal Agents
  • Carbamates
  • Furans
  • Organophosphates
  • Sulfonamides
  • Triazoles
  • posaconazole
  • fosamprenavir