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Acyline: the first study in humans of a potent, new gonadotropin-releasing hormone antagonist

Show simple item record Bremner, William J. en_US Amory, John K. en_US Herbst, Karen L. en_US Anawalt, Bradley D. en_US 2008-10-17T20:42:04Z 2008-10-17T20:42:04Z 2002-07 en_US
dc.identifier.citation J Clin Endocrinol Metab. 2002 Jul;87(7):3215-20 en_US
dc.description.abstract Acyline is a novel GnRH antagonist found in animal studies to be a potent suppressor of circulating gonadotropin and testosterone (T) levels. We conducted the first study of acyline administration to humans. Eight healthy, eugonadal young men were administered a series of acyline injections (0, 2.5, 7.5, 25, and 75 microg/kg), each injection separated by at least 10 d. Serum FSH, LH, and T levels were measured for 7 d after injections. Acyline suppressed FSH, LH, and T levels in a dose-dependent fashion. Maximal suppression occurred after injection of 75 microg/kg acyline, which suppressed FSH to 46.9 +/- 2.5%, LH to 12.4 +/- 2.2%, and T to 13.4 +/- 1.4% of baseline levels, maintaining suppression for over 48 h. Serum acyline levels peaked at 1 h at 18.9 +/- 0.9 ng/ml, remained significantly elevated above background 7 d after injection, and returned to background levels by 14-17 d after injection. Side-effects at the site of injection were limited to infrequent blush and pruritus that resolved within 90 min of injection. Higher doses of acyline might be effective as depot injections for long-lasting gonadotropin suppression in hormone-dependent diseases and for use in male hormonal contraception regimens. en_US
dc.language.iso en_US en_US
dc.publisher Endocrine Society en_US
dc.subject male contraception en_US
dc.subject andrology en_US
dc.subject 5-alpha reductase inhibitors en_US
dc.subject testosterone en_US
dc.subject gonadotropins en_US
dc.subject.mesh Safety en_US
dc.subject.mesh Research Support, U.S. Gov't, P.H.S. en_US
dc.subject.mesh Testosterone, blood en_US
dc.subject.mesh Skin, drug effects en_US
dc.subject.mesh Humans en_US
dc.subject.mesh Adult en_US
dc.subject.mesh Oligopeptides, adverse effects, blood, pharmacology en_US
dc.subject.mesh Pruritus, chemically induced en_US
dc.subject.mesh Male en_US
dc.subject.mesh Gonadorelin, antagonists & inhibitors en_US
dc.subject.mesh Gonadotropins, blood en_US
dc.title Acyline: the first study in humans of a potent, new gonadotropin-releasing hormone antagonist en_US
dc.type Article en_US

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