Dalcetrapib
Probenecid raises exposure to the active thiol form of dalcetrapib by up to 21 percent (Int J Clin Pharmacol Ther 2013)
Original title: In vivo evaluation of drug-drug interactions linked to UGT inhibition: the effect of probenecid on dalcetrapib pharmacokinetics
This two-way crossover study in 20 healthy subjects assessed the effect of the UGT inhibitor probenecid on the pharmacokinetics of dalcetrapib, whose pharmacologically active thiol form undergoes glucuronidation. Subjects received a single 600 mg dose of dalcetrapib with or without probenecid, dosed at 500 mg four times daily for 6 days. Co-administration of probenecid increased the area under the curve and maximum concentration of dalcetrapib thiol by 14% and 21%, respectively. The findings illustrate the difficulty of predicting clinically relevant drug-drug interactions for UGT substrates based only on the fraction metabolized by glucuronidation.
Original abstract
Objective: To assess the effect of the UGT inhibitor probenecid on the pharmacokinetics of dalcetrapib, an investigational drug whose pharmacologically active thiol form undergoes glucuronidation (fm UGT ≥ 0.25).
Materials And Methods: A two-way crossover study in 20 healthy subjects. Subjects received a single 600 mg dose of dalcetrapib with or without probenecid (500 mg 4 times daily for 6 days).
Results: AUC∞ and Cmax of dalcetrapib thiol were increased by 14% and 21%, respectively, by co-administration of probenecid.
Conclusions: This case study illustrates the difficulty in predicting clinically relevant drug-drug interactions for UGT substrates based only on the fraction metabolized by glucuronidation.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.