Drug-carrier conjugates

US4587046A · kind A · utility

Assignee

• The Regents of the University of California · US

Inventors

• Murray Goodman · Village of La Jolla, US
• Neal Castagnoli · San Rafael, US
• Kenneth A. Jacobson · Silver Spring, US
• Kenneth L. Melmon · Woodside, US
• Roberto P. Rosenkranz · Menlo Park, US
• Michael S. Verlander · Del Mar, US

Key dates

• Filing date: May 18, 1982
• Grant date: May 6, 1986
• Expiry date: May 18, 2002

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/29
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Biologically active drugs, e.g. catecholamine hormones, are coupled to carrier molecules, e.g. monodisperse peptides to produce conjugate molecules. The conjugate molecules retain biological activity, but the pharmacokinetic, pharmacodynamic and/or potency properties of the drug is modified. The drug is coupled to the carrier via a spacer moiety which not only serves to covalently link the drug to the carrier, but also insulates the biologically active portion of the drug, i.e., the pharmacophore, from degradation during the coupling process. The carrier preferably consists of a monodisperse peptide in which the sequence of amino acid residues is carefully preselected and controlled.