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Prodrug Bioconversion

Meaning

The metabolic process within the body where an initially inactive or less active precursor molecule, known as a prodrug, undergoes a chemical transformation to yield its final, therapeutically active form. This essential conversion is typically catalyzed by specific endogenous enzymes located in the liver, gastrointestinal tract, or, importantly for non-oral delivery, within the layers of the skin. This strategy is primarily utilized to enhance the drug’s physicochemical properties, such as its stability or ability to penetrate biological barriers.