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A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men

Show simple item record Amory, John K. en_US Page, Stephanie T. en_US Bremner, William J. en_US Anawalt, Bradley D. en_US Herbst, Karen L. en_US Coviello, Andrea D. en_US 2008-10-17T20:40:52Z 2008-10-17T20:40:52Z 2004-12 en_US
dc.identifier.citation J Clin Endocrinol Metab. 2004 Dec;89(12):5959-65 en_US
dc.description.abstract 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 microg/kg. In this study we examined gonadotropin and T levels in 28 healthy young men administered acyline as single doses of 150 or 300 microg/kg or serial injections of 75 microg/kg. A single 300 microg/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 microg/kg acyline to a maximum concentration of 112.4 +/- 18 ng/ml (n = 7; t(1/2) = 4.9 d). Injections of 75 microg/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. en_US
dc.language.iso en_US en_US
dc.publisher Endocrine Society en_US
dc.subject male contraception en_US
dc.subject 5-alpha reductase inhibitors en_US
dc.subject andrology en_US
dc.subject gonadotropins en_US
dc.subject testosterone en_US
dc.subject.mesh Injections, Subcutaneous en_US
dc.subject.mesh Humans en_US
dc.subject.mesh Middle Aged en_US
dc.subject.mesh Pruritus, chemically induced en_US
dc.subject.mesh Male en_US
dc.subject.mesh Drug Administration Schedule en_US
dc.subject.mesh Time Factors en_US
dc.subject.mesh Reference Values en_US
dc.subject.mesh Research Support, U.S. Gov't, P.H.S. en_US
dc.subject.mesh Oligopeptides, administration & dosage, adverse effects, blood, pharmacokinetics, pharmacology en_US
dc.subject.mesh Gonadorelin, antagonists & inhibitors en_US
dc.subject.mesh Gonadotropins, antagonists & inhibitors, blood en_US
dc.subject.mesh Erythema, chemically induced en_US
dc.subject.mesh Testosterone, antagonists & inhibitors, blood en_US
dc.subject.mesh Adult en_US
dc.title A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men en_US
dc.type Article en_US

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