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E. O'Mara*, V. Mummaneni, M. Bifano, D. Randall, H. Uderman, L. Knox, and M. Geraldes.
Bristol-Myers Squibb Pharmaceutical Res. Inst., Princeton, NJ.
Background:BMS-232632 (BMS) is a new protease inhibitor (PI) that has shown excellent anti-HIV activity. Ritonavir (RTV) is a potent inhibitor of cytochrome P450 (CYP) 3A4, and BMS is a CYP3A4 substrate. Therefore, the effect of ritonavir on the pharmacokinetics of BMS was ascertained.
Methods:Thirty-two healthy subjects were randomized to receive open-label drugs coadministered with a light meal once daily (QD). Two groups of sixteen received BMS alone for six days at 200 mg and 400 mg QD, respectively. All had a BMS PK profile drawn on day 6. On day 7, each BMS group was subdivided to receive RTV, at 100 or 200 mg QD. PK profile of BMS was drawn on day 16.
Results:Summary of BMS pharmacokinetic parameters:
No serious laboratory or clinical adverse events were observed during review of preliminary safety data.
Conclusion:Co-administration of BMS-232632 and RTV increased exposure of BMS several-fold at each BMS dose level versus BMS alone.
© 8th Conference on Retroviruses and Opportunistic Infections