Co-administration of ketoconazole (400 mg once daily) and doravirine (100 mg single dose) increased doravirine AUC, Cmax and C24 by 206%, 25% and 175%, respectively. No dose adjustment is required.

No clinically significant change in doravirine concentration was observed when ketoconazole was co-administered with doravirine. Co-administration of doravirine (100 mg single dose) with ketoconazole (400 mg once daily) was studied in 10 subjects. Doravirine AUC, Cmax and C24 increased by 206%, 25% and 175% respectively. These changes are not clinically relevant.

Co-administration of doravirine (100 mg, single dose) and ketoconazole (400 mg, once daily) was studied in 10 healthy subjects. Doravirine AUC, Cmax and C24 increased by 206%, 25% and 175%, respectively. This effect was primarily caused by inhibition of CYP3A by ketoconazole. As safety has been demonstrated with a doravirine dose of up to 200 mg, the authors conclude that these pharmacokinetic changes are not clinically relevant.