Compound that is metabolized into a pharmacologically active drug
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug.[1][2] Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME).[3][4]
Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract.[2] A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.
Note 2: Prodrugs can thus be viewed as drugs containing specialized nontoxic protective groups used in a transient manner to alter or to eliminate undesirable properties in the parent molecule.[6]
^Rautio J, Meanwell NA, Di L, Hageman MJ (August 2018). "The expanding role of prodrugs in contemporary drug design and development". Nature Reviews. Drug Discovery. 17 (8): 559–587. doi:10.1038/nrd.2018.46. PMID29700501. S2CID19489166.
^Malhotra B, Gandelman K, Sachse R, Wood N, Michel MC (2009). "The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine". Current Medicinal Chemistry. 16 (33): 4481–4489. doi:10.2174/092986709789712835. PMID19835561.