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Updated: Aug 15, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Interaction between saquinavir soft-gel and rifabutin in patients infected with HIV
G J Moyle1, N E Buss, T Goggin
1Kobler Clinic, Chelsea and Westminster Hospital, 369 Fulham Rd, London SW10 9NH, UK. gm@moyleg.demon.co.uk
Aims:
To evaluate the potential pharmacokinetic interaction between the HIV protease inhibitor saquinavir and rifabutin.
Methods:
Fourteen HIV-infected patients provided full steady-state pharmacokinetic profiles following administration of rifabutin alone (300 mg once daily) or saquinavir soft-gel formulation (1200 mg three times daily) plus rifabutin (300 mg once daily) in this open label, partially randomized study.
Results:
Coadministration of saquinavir and rifabutin resulted in a reduction in saquinavir AUC(0,8 h) and C(max)(0,8 h) of 47% (95% CI 30, 60%) and 39% (95% CI 11, 59%), respectively. Rifabutin AUC(0,24 h) and C(max)(0,24 h) was increased by an average of 44% (95% CI 17, 78%) and 45% (95% CI 14, 85%), respectively. Saquinavir in combination with rifabutin was well tolerated. Gastrointestinal intolerance and asymptomatic increases in liver enzymes were the only adverse events of note.
Conclusions:
Administration of rifabutin with saquinavir may decrease the efficacy of this HIV protease inhibitor.
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