Hsyu PH, Lewis R, Tran J, Lillibridge J, Schultz-Smith M, Kerr B; International Conference on AIDS.
Int Conf AIDS. 2000 Jul 9-14; 13: 44 (abstract no. LbPeB7049).
Agouron Pharm. Inc., San Diego, CA 92121. Fax: +1 858-678-8248, E-mail: poe.hsyu@agouron.com.
Introduction: Combination of mini-doses (100-200 mg/day) of RTV with saquinavir and indinavir has been used to increase the levels of the two protease inhibitors. In this study, various investigational combinations of once daily (QD) of NFV and RTV were studied to assess the effect of RTV on PK of NFV. Methods: This was an open-label, 7 parallel-arm study. Ten healthy subjects were enrolled in each arm. Concentrations of NFV and its active metabolite M8 were measured on Day 14 for 24 hours. Fasting metabolic labs were monitored before and after treatment. Results: Three arms of the study had similar or superior PK compared to the NFV 12500 mg BID control arm. The preliminary results (geometric mean and 95% CI) are presented as follows: (Table: see text) No serious AEs were observed in this study. NFV 1250mg BID alone did not significantly alter triglycerides, whereas 5 of the 6 arms with RTV significantly increased triglycerides. Other metabolic laboratory values were not significantly changed. Conclusion: These data suggest that once-daily dosing of NFV with minidoses of RTV produced NFV and M8 exposures over a 24hr dosing interval that approximated 1250mg NFV BID dosing without RTV. However, mini-doses of RTV also significantly increased fasting serum trigycerides within 2 weeks. Additional clinical studies are planned to determine the safety and efficacy of once daily NFV/RTV.
Publication Types:
Keywords:
- HIV Protease Inhibitors
- Indinavir
- Nelfinavir
- Protease Inhibitors
- Ritonavir
- Saquinavir
- Triglycerides
- pharmacokinetics
Other ID:
UI: 102242566
From Meeting Abstracts