DIPEPTIDE LINKED MEDICINAL AGENTS

摘要

PROBLEM TO BE SOLVED: To provide formulations that extend the half life of existing pharmaceuticals and improve their therapeutic index.SOLUTION: A non-enzymatic self-cleaving moiety covalently bonded to a medicinal agent is a dipeptide comprising an amino acid or hydroxyl acid and an N-alkylated amino acid. The self-cleaving moiety is linked to the medicinal agent through formation of an amide bond between the N-alkylated amino acid and an amine of the medicinal agent. The chemical cleavage half life of the dipeptide from the medicinal agent is at least about 1 hour to about 1 week in a standard PBS solution under physiological conditions.SELECTED DRAWING: None