Pro-Drug

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
Substrate Main targeted enzyme families Type Structure
Unecritinib Not A\/B H target Pro-Drug Drug Piperidine Pyrazole Pyridine
Ramipril Carb_B_Chordata Not A\/B H target Pro-Drug Drug
NT-0796 Carboxylesterase Carb_B_Chordata Not A\/B H target Pro-Drug Drug Indacen Pyrimidine
Candesartan-cilexetil Carb_B_Chordata Not A\/B H target Drug Pro-Drug Pyrrolidine Angiotensin-receptor blocker Benzimidazole
Fosinopril Plasmodium_subtelomeric_PST-A Carb_B_Chordata Not A\/B H target Drug Pro-Drug Pyrrolidine Angiotensin-converting enzyme inhibitor Organophosphate
Fenofibrate Carb_B_Chordata Pro-Drug Drug Propionate
Sirpiglenastat Carb_B_Chordata Pro-Drug Drug Peptide
QA-Cbl BCHE Pro-Drug Drug Choline ester Trimethylammonium
Anordrin Carb_B_Chordata Pro-Drug Drug Propionate
Phospho-Ibuprofen Carb_B_Chordata phospho-NSAID Drug Pro-Drug
Dimethyl-fumarate Carb_B_Chordata Drug Pro-Drug Not A\/B H target
Beclomethasone-dipropionate Arylacetamide_deacetylase Drug Pro-Drug Not A\/B H target Steroid Propionate Phenanthrene
S-bromobenzylglutathione-dicyclopentyl-ester Carb_B_Chordata Not A\/B H target Pro-Drug Drug Sulfur Compound Peptide
MGS0274 Carb_B_Chordata Not A\/B H target Pro-Drug Drug
Tenofovir-alafenamide Carboxypeptidase_S10 Carb_B_Chordata Drug Pro-Drug Aminopurin Propionate
Ethyl-Zaltoprofen Hormone-sensitive_lipase_like Bacterial_lip_FamI.3 Not A\/B H target Drug Pro-Drug Propionate Alkyl ester
Ethyl-Carprofen Hormone-sensitive_lipase_like Not A\/B H target Drug Pro-Drug Carbazol Propionate Alkyl ester
Ethyl-Flurbiprofen Hormone-sensitive_lipase_like Bacterial_lip_FamI.3 Canar_LipB Not A\/B H target Drug Pro-Drug Propionate Alkyl ester
Imidapril Carb_B_Chordata Pro-Drug Drug Not A\/B H target Imidazole
Indiplon Arylacetamide_deacetylase Pro-Drug Drug Not A\/B H target Sulfur Compound Pyrimidine Pyrazole
Rifapentine Arylacetamide_deacetylase Pro-Drug Drug Not A\/B H target Piperazine Antibiotic
Rifabutin Arylacetamide_deacetylase Pro-Drug Drug Not A\/B H target Piperidine Antibiotic
Baloxavir-marboxil Arylacetamide_deacetylase Pro-Drug Drug Not A\/B H target Sulfur Compound
Abiraterone-acetate Arylacetamide_deacetylase Pro-Drug Drug Pyridine Not A\/B H target Phenanthrene
Ketoconazole Arylacetamide_deacetylase Pro-Drug Drug Not A\/B H target Piperazine Imidazole Dioxolane
Flupirtine Carb_B_Chordata Pro-Drug Drug Not A\/B H target Carbamate
Acebutolol Carb_B_Chordata Pro-Drug Drug Not A\/B H target
Mycophenolate-mofetil Carb_B_Chordata Pro-Drug Drug Not A\/B H target Morpholine Benzofuran
Nintedanib Carb_B_Chordata Pro-Drug Drug Not A\/B H target Piperazine
Vixotrigine Carb_B_Chordata Pro-Drug Drug Not A\/B H target Pyrrolidine Carboxamide
Clofibrate Carb_B_Chordata Pro-Drug Drug Not A\/B H target Propionate
Bemnifosbuvir Carboxypeptidase_S10 Carb_B_Chordata Pro-Drug Drug Not A\/B H target Propionate Purine
Remdesivir Carb_B_Chordata Carboxypeptidase_S10 Pro-Drug Drug Not A\/B H target Propionate Triazine
Molnupiravir Carb_B_Chordata BCHE Pro-Drug Drug Not A\/B H target Propionate Nucleoside
Idalopirdine-rivastigmine BCHE Drug Pro-Drug Indole Carbamate Derivative of Rivastigmine Multitarget 5-HT-receptor-ligand
CHEMBL1784957 ACHE Drug Pro-Drug Carbamate Derivative of Rivastigmine
CurDD BCHE CMBL Carb_B_Chordata Drug Pro-Drug Natural_modified
Eslicarbazepine-acetate Carb_B_Chordata Arylacetamide_deacetylase Drug Pro-Drug Benzazepin Carbamate Acetate Carboxamide Azepane
Trandolapril Carb_B_Chordata Not A\/B H target Drug Pro-Drug Pyrrolidine Angiotensin-converting enzyme inhibitor
Selexipag Carb_B_Chordata Sulfonyl Sulfur Compound Not A\/B H target Pro-Drug Drug
Ciclesonide Carb_B_Chordata BCHE Not A\/B H target Pro-Drug Butyrate Drug
Clevidipine Not A\/B H target Pro-Drug Butyrate Drug
2-oxo-clopidogrel Carb_B_Chordata Not A\/B H target Drug Pro-Drug Pyridine Acetate
Dipivefrin Carb_B_Chordata ACHE BCHE Drug Not A\/B H target Pro-Drug Propionate
W22-methyl-ester Bacterial_esterase Canar_LipB Benzodiazepin Not A\/B H target Drug Pro-Drug Azepane
Enalapril Carb_B_Chordata Not A\/B H target Drug Pro-Drug Pyrrolidine Angiotensin-converting enzyme inhibitor
Quinapril Carb_B_Chordata Isoquinoline Not A\/B H target Drug Pro-Drug Angiotensin-converting enzyme inhibitor
Sacubitril Carb_B_Chordata Pro-Drug Not A\/B H target Drug Oxobutanoate
Dabigatran-etexilate Carb_B_Chordata Pro-Drug Not A\/B H target Drug Pyridine Propionate Benzimidazole
Temocapril Carb_B_Chordata Not A\/B H target Pro-Drug Drug Angiotensin-converting enzyme inhibitor Azepane
Oseltamivir Carb_B_Chordata BCHE Pro-Drug Drug Not A\/B H target
Isosorbide-2-aspirinate BCHE Isosorbide Salicylic Acetate Benzoate Pro-Drug Drug
Isosorbide-2,5-diaspirinate BCHE Isosorbide Salicylic Acetate Benzoate Pro-Drug Drug
Nitroaspirin BCHE Salicylic Pro-Drug
Isosorbide-2-aspirinate-5-mononitrate BCHE Isosorbide Salicylic Pro-Drug
Isosorbide-2-aspirinate-5-salicylate BCHE Carb_B_Chordata Isosorbide Salicylic Acetate Benzoate Pro-Drug
Bambuterol BCHE Pro-Drug Drug Carbamate tert-Butyl Adrenergic-Receptor-ligand
Naproxen-Ethyl-Ester Canar_LipB 6_AlphaBeta_hydrolase Hormone-sensitive_lipase_like Profen prodrug Pro-Drug Drug Naphthalen Propionate
Naproxen-Methyl-Ester 6_AlphaBeta_hydrolase Hormone-sensitive_lipase_like Profen prodrug Pro-Drug Drug Naphthalen Propionate
Ibuprofen-Ethyl-Ester Hormone-sensitive_lipase_like Profen prodrug Pro-Drug Drug Propionate
Ketoprofen-Glycerol-Ester Canar_LipB Profen prodrug Pro-Drug Drug Propionate
Ketoprofen-Vinyl-Ester Canar_LipB Profen prodrug Pro-Drug Drug Aryl ester Propionate
Ketoprofen-Butyl-Ester Canar_LipB Profen prodrug Pro-Drug Drug Aryl ester Propionate
Ketoprofen-Ethyl-Ester CarbLipBact_1 Hormone-sensitive_lipase_like Bacterial_lip_FamI.3 Lipase_2 Canar_LipB Profen prodrug Pro-Drug Drug Alkyl ester Propionate
Capecitabine Carboxylesterase Carb_B_Chordata Drug Carbamate Pyrimidine Pro-Drug