Anacetrapib
Anacetrapib does not meaningfully inhibit P-glycoprotein, leaving digoxin exposure essentially unchanged (Biopharm Drug Dispos 2011)
Original title: Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects
To assess whether anacetrapib interacts with orally administered digoxin, a P-glycoprotein substrate with a narrow therapeutic window, this study co-administered the two drugs in healthy subjects. Anacetrapib was generally well tolerated with digoxin. The geometric mean ratios (digoxin plus anacetrapib versus digoxin alone) and 90% CIs for digoxin AUC0-last and AUC0-infinity were 1.05 (0.96, 1.15) and 1.07 (0.98, 1.17), both within the bioequivalence interval of (0.80, 1.25), supporting the primary study hypothesis; the ratio and 90% CI for digoxin Cmax was 1.23 (1.14, 1.32), and median Tmax and mean apparent terminal half-life of digoxin were comparable between treatments. These results show single-dose digoxin pharmacokinetics were not meaningfully altered by multiple-dose anacetrapib, indicating anacetrapib does not meaningfully inhibit P-glycoprotein and that no digoxin dosage adjustment is needed during co-administration.
Original abstract
Anacetrapib is currently being developed for the oral treatment of dyslipidemia. A clinical study was conducted in healthy subjects to assess the potential for an interaction with orally administered digoxin. Anacetrapib was generally well tolerated when co-administered with digoxin in the healthy subjects in this study. The geometric mean ratios (GMR) for (digoxin + anacetrapib/digoxin alone) and 90% confidence intervals (CIs) for digoxin AUC(0-last) and AUC(0-∞) were 1.05 (0.96, 1.15) and 1.07 (0.98, 1.17), respectively, both being contained in the accepted interval of bioequivalence (0.80, 1.25), the primary hypothesis of the study. The GMR (digoxin + anacetrapib /digoxin alone) and 90% CIs for digoxin C(max) were 1.23 (1.14, 1.32). Median T(max) and mean apparent terminal t(½) of digoxin were comparable between the two treatments. The single-dose pharmacokinetics of orally administered digoxin were not meaningfully affected by multiple-dose administration of anacetrapib, indicating that anacetrapib does not meaningfully inhibit P-glycoprotein. Thus, no dosage adjustment for digoxin is necessary when co-administered with anacetrapib.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.