Pharmaceutical agents, compositions containing the same and methods for their use for enhancing the
bioavailability and pharmacological
efficacy of therapeutic peptides. The pharmaceutical agents have the formulaCarrier-
Linker-PeptideWherein
Peptide is a therapeutically active
peptide species having the formula aan wherein n is the number of
amino acid residues in the
peptide and n is 2 to 40, Carrier is benzoyl, phenylacetyl, cinnamoyl, 3-OH-cinnamoyl, 3,4-OH-cinnamoyl, 3,4-dimethoxycinnamoyl, 3,4-methylenedioxycinnamoyl, 3-methoxycinnamoyl, 3,4-diethoxy-cinnamoyl, 3,4,5-trimethoxy-cinnamoyl, t-butoxycarbonyl, benzyloxycarbonyl, pivaloyl, N-9-fluorenylmethoxycarbonyl, fumaroyl and derivatives thereof and
Linker is a C6 to C16 lipidic chain or a derivative thereof, an 8-amino-3,6-dioxaoctanoic acid or polymeric derivative thereof, pseudo
peptide, or peptide mimic. Methods of use of compositions having the formula Carrier-
Peptide wherein Carrier and
Peptide are as just defined are also disclosed.