Table 1: Drug inhibitors of CES1 and/or CES2.


Drug inhibitor CES1 inhibition CES2 inhibition Mechanism of action
Carvedilol Irinotecan: K i : 1.60 (Comp) [ 36 ] Adrenergic antagonist
Diltiazem Trandolapril: K i : 9 μM (comp) [ 37 ] Irinotecan: K i : 0.25 (Noncomp) [ 38 ] Calcium channel blocker
Fenofibrate Irinotecan: Ki: 0.04 (Comp) [ 39 ] PPAR- α Activator
Loperamide MLA: K i : 1.50 [Comp) [ 40 ] μ-opioid receptor agonist
Nitrendipine Imidapril: K i : 1.24 μM (mix) [ 3 ] Calcium channel blocker
Physostigmine Irinotecan: Ki: 0.3 (Mix) [ 36 ] Acetylcholinesterase inhibitor
Simvastatin Imidapril: K i : 0.11 μM (comp) [ 39 ] Irinotecan: K i : 0.67 (noncomp) [ 39 ] HMG-CoA Reductase inhibitor
Telmisartan Imidapri: K i : 1.69 μM (comp) [ 38 ] Angiotensin II receptor blocker
Troglitazone Imidapri: K i : 0.62 μM (Mix) [ 39 ] PPAR agonist

MLA: Methylumbelliferyl acetate; Comp: competitive; Noncomp: noncompetitive; Mix: competitive and noncompetitive; PPAR: activating peroxisome proliferator-activated receptor; HMG-CoA: 3-hydroxy-3-methylglutaryl coenzyme A.