Patent ID: 7329507

Claim:
A method of designing a prodrug for administration to a patient, the method comprising: (1) identifying an oligopeptide of the formula (AA) n -AA 3 -AA 2 -AA 1 , wherein: each AA independently represents an amino acid, n is 0 or 1, and when n is 1, then (AA) n is AA 4 which represents any amino acid, AA 3 represents isoleucine, AA 2 represents any amino acid, and AA 1 represents any amino acid, (2) linking the oligopeptide at a first attachment site of the oligopeptide to a stabilizing group, and (3) directly or indirectly linking the oligopeptide to a therapeutic agent at a second attachment site of the oligopeptide, wherein steps (2) and (3) may be performed in any order or concurrently and further wherein a conjugate is formed by performance of steps (1) through (3), (4) testing if the conjugate is cleavable by TOP, (5) testing if the conjugate is stable in whole blood, and (6) selecting the conjugate as a prodrug if the conjugate is resistant to cleavage by TOP and stable in whole blood.