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An open-label, 3 period, fixed-sequence study was conducted in 20 healthy adult participants. Participants received a dose of 200mg of Grazoprevir (GZR), which is equivalent to the exposure of 100mg of GZR in HCV infected patients.In Period 1, participants received GZR (200mg) + Elbasvir (EBR, 50mg) daily from days 1 to 8.In Period 2, participants received Rilpivirine (RPV, 25mg) daily on days 1 to 11.In Period 3, participants received GZR (200mg) + EBR (50mg) + RPV (25mg) daily on days 1 to 9.There was a 9 day washout period between Periods 1 and 2, but no washout between Periods 2 and 3. PK parameters were determined for RPV on day 11 of Period 2 and day 9 of Period 3. PK parameters were determined for GZR and EBR on day 8 of Period 1 and day 9 of Period 3.
DrugAUC GMR (90% CI)Cmax GMR (90% CI)GZR0.98 (0.89-1.07)0.97 (0.83-1.14)EBR1.07 (1.00-1.15)1.07 (0.99-1.16)RPV1.13 (1.07-1.20)1.07 (0.97-1.17)Results showed the co-administration of GZR/EBR + RPV had no clinically meaningful effect on the PK of RPV, GZR, or EBR. The authors state that these agents can be co-administered in HIV/HCV coinfected patients without the need for dose adjustments.
Yeh WW, Feng HP, P Auger, et al. No pharmacokinetic interaction between hcv inhibitors grazoprevir/elbasvir with rilpivirine. abstract 17. 16th International Workshop On Clinical Pharmacology Of Hiv And Hepatitis Therapy. Washington, DC. ; 2015.