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Journal of Clinical Endocrinology & Metabolism, Vol 63, 303-308, Copyright © 1986 by Endocrine Society

ARTICLES

Single subcutaneous doses of a luteinizing hormone-releasing hormone antagonist suppress serum gonadotropin and testosterone levels in normal men [published erratum appears in J Clin Endocrinol Metab 1986 Oct;63(4):940]

SN Pavlou, CR Debold, DP Island, G Wakefield, J Rivier, W Vale and D Rabin

The ability of single doses of a LHRH antagonist [Ac-delta 3Pro1, 4F-D- Phe2, D-Trp3,6]LHRH (4F-antagonist) to suppress serum gonadotropin and testosterone levels was studied in six normal men. The 4F-antagonist was given sc at four doses: 40, 80, 160, and 320 micrograms/kg body weight. Serum immunoreactive LH, FSH, and testosterone and bioactive LH were measured at intervals for the subsequent 18 h. Serum LH decreased rapidly by (mean +/- SE) 39.7 +/- 2.7%, 41.6 +/- 5.4%, 45.5 +/- 4.7%, and 45.3 +/- 5.4% after each of the four doses. The mean number of LH pulses and their amplitude decreased after each dose and remained suppressed for at least 6 h. After each of the four doses, mean serum FSH levels decreased by 20.0 +/- 4.1%, 33.8 +/- 6.8%, 25.8 +/- 3.6%, and 33.3 +/- 5.7%, and mean serum testosterone levels decreased by 47.7 +/- 7.3%, 55.6 +/- 10.5%, 58.2 +/- 10.8%, and 76.0 +/- 6.0%. Serum testosterone remained low for at least 18 h after the two higher doses. LH bioactivity and the ratio of bioactive LH to immunoreactive LH decreased in all subjects, especially after higher doses of the 4F- antagonist. No side effects or adverse reactions occurred after 4F- antagonist administration, and toxicology studies were negative. These results demonstrate that a single sc injection of this potent LHRH antagonist inhibits the pituitary-gonadal axis in normal men.


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R. S. Swerdloff, C. J. Bagatell, C. Wang, B. D. Anawalt, N. Berman, B. Steiner, and W. J. Bremner
Suppression of Spermatogenesis in Man Induced by Nal-Glu Gonadotropin Releasing Hormone Antagonist and Testosterone Enanthate (TE) Is Maintained by TE Alone
J. Clin. Endocrinol. Metab., October 1, 1998; 83(10): 3527 - 3533.
[Abstract] [Full Text]


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