Antagonists of alpha-melanocyte stimulating hormone and methods based thereon

• US 6,602,856 B1
• Filed: 01/17/1995
• Issued: 08/05/2003
• Est. Priority Date: 01/17/1995
• Status: Expired due to Fees

• Current Assignee: Lerner Pharmaceuticals, Inc.
• Original Assignee: Lerner Pharmaceuticals, Inc.
• Inventors: Lerner, Michael R., Quillan, J. Mark, Jayawickreme, Channa K.
• Primary Examiner(s): BORIN, MICHAEL L
• Application Number:
  US08/373,151
• Time in Patent Office: 3,122 Days
• Field of Search: 530/331, 514/18
• US Class Current: 514/10.7
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: C07K 14/68 Melanocyte-stimulating hormone [MSH]
• CPC Class Codes: C07K 5/0812 and aromatic or cycloaliphatic
• CPC Class Codes: C07K 5/0821 with the first amino acid being heterocyclic, e.g. His, Pro, Trp

Abstract

Peptide antagonists of α-melanocyte stimulating hormone are disclosed, together with methods of inhibiting the effects of α-melanocyte stimulating hormone on cells or tissues sensitive to that hormone. In particular, methods for lightening the pigmentation of skin and for treating malignant melanoma, as well as kits for practicing the invention are also disclosed.

Claims

1. A peptide antagonist of α

-melanocyte stimulating hormone comprising the amino acid sequence D-Trp-Arg-Leu or D-Trp-Arg-Leu-NH₂.

3. The peptide antagonist of α

-melanocyte stimulating hormone according to claim 1 or 2 which is purified.

4. The peptide antagonist according to claim 1 which consists of no more than 8 amino acid residues.

5. The peptide antagonist according to claim 1 which consists of no more than 12 amino acid residues.

2. A peptide antagonist of α

-melanocyte stimulating hormone, that is D-Trp-Arg-Leu or D-Trp-Arg-Leu-NH₂.

6. A pharmaceutical composition comprising (a) a peptide, said peptide comprising the amino acid sequence D-Trp-Arg-Leu or D-Trp-Arg-Leu-NH₂, and (b) a pharmaceutically acceptable carrier.

7. A pharmaceutical composition according to claim 6 wherein said pharmaceutically acceptable carrier is selected from the group consisting of a solution, cream or lotion suitable for topical application, a physiological salt or buffer suitable for systemic injection, a slow release carrier and a composition suitable for oral administration.

9. The pharmaceutical composition according to claim 6 in which the peptide consists of no more than 8 amino acid residues.

10. The pharmaceutical composition according to claim 6 in which the peptide consists of no more than 12 amino acid residues.

8. A pharmaceutical composition comprising (a) a tripeptide, said tripeptide being D-Trp-Arg-Leu or D-Trp-Arg-Leu-NH₂, and (b) a pharmaceutically acceptable carrier.