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Pro-Drug

General

A prodrug is a medication or compound that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug. For example, salicin is a beta-D-glucopyranoside that is cleaved by esterases to release salicylic acid. Aspirin, acetylsalicylic acid, first made by Felix Hoffmann at Bayer in 1897, is a synthetic prodrug of salicylic acid. Many prodrugs are synthetized to slow down the delivery of the active compound. Esterases often hydrolyze prodrugs and are targeted for that role. Genetic variants of these esterases may act differently and explain variation of response in patients bearing these variant
Inhibitor Main targeted enzyme familyes Type Structure
Retagliptin DPP4N_Peptidase_S9 Drug Gliptin Triazol Trifluoro Pro-Drug Imidazole
Sofosbuvir Carb_B_Chordata Pro-Drug Drug Not A\/B H target
Remdesivir Carb_B_Chordata Pro-Drug Drug Not A\/B H target Propionate Triazine
Idalopirdine-rivastigmine BCHE Drug Pro-Drug Carbamate Derivative of Rivastigmine Multitarget 5-HT-receptor-ligand
CHEMBL1784957 ACHE Drug Pro-Drug Carbamate Derivative of Rivastigmine
Pyridophen-10 ACHE Muscarinic antagonist Propionate Carbamate Pro-Drug Multitarget Not A\/B H target PET probe
Dimethylhydroxycarbaphen BCHE Muscarinic antagonist Propionate Carbamate Pro-Drug Multitarget Not A\/B H target
Terbutaline-monocarbamate BCHE Derivative of Bambuterol Carbamate Drug tert-Butyl Not A\/B H target Pro-Drug
Bambuterol BCHE Derivative of Bambuterol Carbamate Drug tert-Butyl Not A\/B H target Pro-Drug
SN-38 Carb_B_Bacteria Carb_B_Chordata Drug Derivative of Irinotecan Not A\/B H target Pro-Drug