Treatment of male mammals

US4489061A · kind A · utility

Assignee

• Salk Institute for Biological Studies · US

Inventors

• Catherine L. Rivier · Village of La Jolla, US
• Jean E. F. Rivier · Village of La Jolla, US
• Wylie W. Vale, Jr. · Village of La Jolla, US

Key dates

• Filing date: Sep 27, 1982
• Grant date: Dec 18, 1984
• Expiry date: Sep 27, 2002

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/13
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Peptides which are LRF analogs that inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads can be effective to suppress androgen-dependent behavior when administered to male mammals. The peptides are LRF antagonists having a binding affinity at least about 15 times that exhibited by LRF and having an ICR.sub.50 of less than 1/1. Examples of peptides which may be used are those having the structure: R.sub.1 -R.sub.2 -R.sub.3 -D-Trp-Ser-Tyr-R.sub.4 -Leu-Arg-Pro-Gly-NH.sub.2 wherein R.sub.1 is selected from the group consisting of hydrogen, formyl, acetyl, acrylyl, benzoyl and allyl; R.sub.2 is selected from the group consisting of dehydro Pro, dehydro D-Pro, Thz and D-Thz; R.sub.3 is selected from the group consisting of pCl-D-Phe, pF-D-Phe, pNO.sub.2 -D-Phe and 3,4 Cl-D-Phe; R.sub.4 is selected from the group consisting of D-Trp and (imBzl) D-His; and Leu may be substituted by N.alpha.MeLeu. Effective suppression of androgen-dependent behavior is achieved at a daily dosage level of not more than about 3 mg. per Kg. of body weight.