In this study investigating doravirine pharmacokinetics when switching from efavirenz 600 mg to doravirine 100 mg, doravirine exposure was significantly decreased when doravirine was initiated immediately after cessation of efavirenz. Investigators plan to evaluate the clinical relevance of this interaction further.
Doravirine vs efavirenz
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Study Design
In an open-label, fixed-sequence study, healthy subjects (n=20) received doravirine (formerly known as MK-1439) 100 mg once daily for 5 days (period 1). Following a 7-day washout, subjects received efavirenz 600 mg once daily for 14 days (period 2), followed by administration of doravirine 100 mg once daily for 14 days (period 3). This study was conducted to evaluate the impact of switching treatment from efavirenz to doravirine.
Study Results
Administration of doravirine immediately after cessation of efavirenz resulted in significant decrease of AUC, Cmax, C24h for doravirine. Geometric mean ratios (GMRs; single-dose of doravirine + efavirenza / single-dose of doravirine) [90% CI] of AUC, Cmax, and C24h were 0.38 [0.33, 0.45], 0.65 [0.58, 0.73], and 0.15 [0.10, 0.23], respectively. GMRs (multiple-doses of doravirine + efavirenzb / multiple-doses of doravirine) [90% CI] of AUC, Cmax, and C24h were 0.68 [0.58, 0.80], 0.86 [0.77, 0.97], and 0.50 [0.39, 0.64], respectively.a single dose of doravirine after pre-treatment with efavirenz (efavirenz 600 mg daily for 14 days) b multiple doses of doravirine 100 mg daily for 14 days after pre-treatment with efavirenz (efavirenz 600 mg daily for 14 days)
References
K L Yee, R I Sanchez, P Auger, et al. An evaluation of doravirine pharmacokinetics when switching from efavirenz to doravirine treatment. 16th International Workshop On Clinical Pharmacology Of Hiv And Hepatitis Therapy. Washington, DC. ; 2015.
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