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TMC435 & Drug Interactions: Evaluation of metabolic interactions for TMC435 via cytochrome P450 (CYP) enzymes in healthy volunteers
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Reported by Jules Levin
EASL Apr 14-18 2010 Vienna Austria
V.Sekar1, R.Verloes2, P. Meyvisch2, K. Spittaels2, S.H. Akuma2, G. De Smedt2
1Tibotec Inc, USA; 2Tibotec BVBA, Belgium
*0.025 mg/kg midazolam (i.v. given slowly over a 1-minute period), dextromethorphan (30 mg p.o.), caffeine (150 mg p.o.), omeprazole (40 mg p.o.) and warfarin (10 mg p.o.) supplemented with vitamin K (10 mg p.o.)
QD, once daily
a n=10 for t1/2term
b Accurate determination not possible
AUC24h, area under the concentration-time curve from administration up to 24 hours post-dose; BID, twice daily; CI, conJdence interval; C0h, pre-dose plasma concentration;
Cmax, maximum plasma concentration; Cmin, minimum plasma concentration; QD, once daily; t1/2term, terminal elimination half-life; tmax, time to reach maximum concentration
Compared with TMC435 alone, concomitant TMC435 and ritonavir administration resulted in:
- higher mean plasma concentrations of TMC435
- a 14.3-, 4.7- and 7.2-fold increase in TMC435 Cmin, Cmax and AUC24h, respectively.
a n=17 for Day 1
b n=19 for Day 1 and 2, n=18 for Day 4
AUC24h, area under the concentration-time curve from administration up to 24 hours post-dose; CI, conJdence interval; C0h, pre-dose plasma concentration; Cmin, minimum plasma concentration; Cmax, maximum plasma concentration; NQ, not quantiJable; LS, least squares; QD, once daily; tmax, time to reach maximum concentration
References
1. Lin TI et al. Antimicrob Agents Chemother 2009; 53: 1377-1385.
2. Reesink HW et al. Gastroenterology 2010; 138: 913-921.
3. Reesink HW et al. Poster presented at the 60th AASLD meeting, Boston, MA, USA,
30 October-3 November, 2009.
4. Marcellin P et al. Poster presented at the 44th Annual Meeting of European Association for the Study of the Liver (EASL), Copenhagen, Denmark, 22-26 April, 2009.
5. Manns M et al. Presented at the 44th Annual Meeting of European Association for the Study of the Liver (EASL), Copenhagen, Denmark, 22-26 April, 2009.
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