While DTG PK parameters were within "no-effect" limits (90%CI of 0.80-1.25), there was a 23-29% reduction in CVC exposure when co-administered with DTG. Therefore, concomitant use of CVC and DTG should be undertaken with caution as this may result in decreased CVC exposure and loss of efficacy. If concomitant use is required, close monitoring is warranted for reduced virologic response and development of viral resistance.
Cenicriviroc vs dolutegravir
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Study Design
This is multiple-dose, open-label, crossover study in 2 groups of healthy subjects (n=20/group). In Group 1, cenicriviroc (CVC) 150 mg once daily was administered for 10 days (Days 1-10; Period 1), followed by CVC 150mg and dolutegravir (DTG) 50 mg once daily for 10 days (Days 11-20; Period 2). Plasma CVC profile was evaluated on Days 10 and 20 for calculation of AUC, Cmax and Cmin.In Group 2, DTG 50 mg once daily was administered for 10 days (Days 1-10; Period 1), followed by CVC 150 mg and DTG 50 mg once daily for 10 days (Days 11-20; Period 2). Plasma DTG profile was evaluated on Days 10 and 20 for calculation of AUC, Cmax and Cmin.
Study Results
Coadministration of CVC and DTG resulted in significant decrease of CVC exposure; geometric mean ratios (GMRs; DTG + CVC / CVC) [90% CI] of AUC and Cmax were 0.71 [0.63, 0.81] and 0.72 [0.62, 0.82], respectively. However, there was no significant increase in DTG exposure; GMR (CVC+DTG / DTG) [90%CI] of AUC and Cmax were 1.14 [1.09, 1.20] and 1.10 [1.03, 1.16], respectively.
References
E Lefebvre, J Enejosa, W Chang, et al. Pharmacokinetic interactions between cenicriviroc and dolutegravir. abstract pe10/8. 14th European Aids Conference. Brussels, Belgium. ; 2013.
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