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The Journal of Clinical Endocrinology & Metabolism Vol. 89, No. 12 5959-5965
Copyright © 2004 by The Endocrine Society

A Single Dose of the Potent Gonadotropin-Releasing Hormone Antagonist Acyline Suppresses Gonadotropins and Testosterone for 2 Weeks in Healthy Young Men

Karen L. Herbst, Andrea D. Coviello, Stephanie Page, John K. Amory, Bradley D. Anawalt and William J. Bremner

Department of Medicine, Division of Endocrinology, Charles R. Drew University (K.L.H.), Los Angeles, California 90059; Center for Research in Reproduction and Contraception, Department of Medicine, University of Washington (A.D.C., S.P., J.K.A., B.D.A., W.J.B.), and Medical Service, Department of Veteran Affairs, Puget Sound Health Care System (B.D.A.), Seattle, Washington 98195

Address all correspondence and requests for reprints to: Dr. Karen L. Herbst, Department of Medicine, Division of Endocrinology, Metabolism, and Molecular Medicine, Charles R. Drew University, Room 3069 Third Floor, 1731 East 120th Street, Los Angeles, California 90059. E-mail: kaherbst{at}cdrewu.edu.

Acyline is a novel GnRH antagonist that reliably inhibits gonadotropins and testosterone (T) levels in men for 48 h after a single dose up to 75 µg/kg. In this study we examined gonadotropin and T levels in 28 healthy young men administered acyline as single doses of 150 or 300 µg/kg or serial injections of 75 µg/kg. A single 300 µg/kg dose of acyline suppressed gonadotropins and T to castrate levels for 15 d (baseline, 21.1 ± 3.1; nadir, 1.95 ± 0.4 nmol/liter; mean ± SEM; P < 0.05). Serum acyline levels peaked 90 min after the injection of 300 µg/kg acyline to a maximum concentration of 112.4 ± 18 ng/ml (n = 7; t1/2 = 4.9 d). Injections of 75 µg/kg acyline every 2 d for five doses suppressed gonadotropins for more than 20 d (nadir T, 1.06 ± 0.17 nmol/liter; P < 0.05 compared with baseline). Adverse events were mild and included erythema and pruritus at the injection site. Acyline, therefore, is one of the most potent peptide GnRH antagonists studied to date with minimal adverse events. A twice monthly injection of acyline could be used as a potent suppressor of the GnRH axis to advance the development of a hormonal male contraceptive or for treatment of hormonally dependent disease.




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