Pharmacy Times – December 2013


Drug Interactions: Insights and Observations


Carboxylesterases and Drug Interactions


John R. Horn, PharmD, FCCP and Philip D. Hansten, PharmD






1. Laizure SC et al. The role of human carboxylesterase in drug metabolism: have we overlooked their importance? Pharmacother. 2013;33:210-22.

2. Tang MJ et al. Antiplatelet agents aspirin and clopidogrel are hydrolyzed by distinct carboxylesterases, and clopidogrel is transesterificated in the presence of ethyl alcohol. J Pharmacol Experiment Ther. 2006;319:1467-76.

3. Shi D et al. Anti-influenza prodrug oseltamivir is activated by carboxylesterase human carboxylesterase 1, and the activation is inhibited by the antiplatelet agent clopidogrel. J Pharmacol. Exp Ther. 2006;319:1477-84.

4. Xiao D et al. Carboxylesterase-2 is a highly sensitive target of the antiobesity agent orlistat with profound implications in the activation of anticancer prodrugs. Biochem Pharmacol. 2013;85:439-47.

5. Lewis JP et al. The functional G143E variant of carboxylesterase 1 is associated with increased clopidogrel active metabolite levels and greater clopidogrel response. Pharmacogen and Genomics. 2013;23:1-8.