Prodrug
An inactive or less active form of a peptide that is converted to the active form in the body through enzymatic or chemical processes. Prodrug design can improve oral bioavailability or targeting.
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Related Terms
A breakdown product formed when the body metabolizes a peptide. Some metabolites are active and contribute to therapeutic effects; others are inactive waste products cleared by the kidneys or liver.
First-pass metabolismThe metabolism of an orally administered peptide by the gut wall and liver before it reaches systemic circulation. First-pass effect dramatically reduces oral bioavailability for most peptides.
BioavailabilityThe fraction of an administered dose that reaches systemic circulation unchanged. Subcutaneous injection provides 65–95% bioavailability for most peptides; oral bioavailability is typically below 1% without absorption enhancers.