Prodrug The term prodrug, which was used initially by Albert Hl, is a pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation a prodrug also can be activated by a nonenzymatic process such as hydrolysis but in this case the compounds generally are inherently unstable and may cause stability problemsProdrug • The term prodrug, which was used initially by Albert HI, is a pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation. • A prodrug also can be activated by a nonenzymatic process such as hydrolysis, but in this case the compounds generally are inherently unstable and may cause stability problems