Potential of testosterone buciclate for male contraception: endocrine differences between responders and nonresponders

The Journal of Clinical Endocrinology and Metabolism
H M BehreE Nieschlag

Abstract

Suppression of serum LH and FSH, by testosterone (T) alone or in combination with other agents, has proved to be the most promising approach to male contraception. T enanthate, the only androgen preparation tested in male contraceptive efficacy trials so far, must be injected every week due to its short terminal elimination half-life of 4.5 days and leads to supraphysiological T serum levels. A new T ester synthesized under WHO and NIH auspices, testosterone buciclate (TB), showed a favorable pharmacokinetic profile, with a terminal half-life of 29.5 days when tested in hypogonadal men. Here we describe the results of the first clinical trial with TB for male contraception. After two control examinations, normal healthy male volunteers were given a single im injection of 600 mg TB (group I; n = 4) and 1200 mg TB (group II; n = 8) on day 0. Follow-up examinations were performed every 2 weeks up to week 32. In both groups mean serum T levels remained in the normal physiological range throughout the study course. Serum levels of dihydrotestosterone (DHT) showed a dose- and time-dependent increase, with serum levels slightly above the normal range in group II for several weeks and a maximal concentration of 3.8 +/- 0.5 nmol/L (mean...Continue Reading

Citations

Jul 5, 2005·Molecular Interventions·Jiyun ChenJames T Dalton
Aug 2, 2001·APMIS : Acta Pathologica, Microbiologica, Et Immunologica Scandinavica·J L SpearowM Barkley
Jun 15, 2011·Biological Trace Element Research·Chung Soo ChangSat Byul Park
Oct 12, 2010·Contraception·Eberhard Nieschlag
Dec 24, 2005·Contraception·Jennifer P BarfieldTrevor G Cooper
Jul 21, 2006·The European Journal of Contraception & Reproductive Health Care : the Official Journal of the European Society of Contraception·Melanie Wenk, Eberhard Nieschlag
Jul 18, 2016·Molecular and Cellular Endocrinology·Mohammed Akli AyoubEric Reiter
Feb 25, 2000·Human Reproduction·D J HandelsmanA J Conway
Dec 6, 2002·Endocrine Reviews·R A Anderson, D T Baird
Apr 9, 2019·European Journal of Endocrinology·Eberhard Nieschlag, Susan Nieschlag
Sep 28, 2017·International Journal of Reproductive Medicine·Olufunmilade Akinfolarin OmisanjoKhadijah Adebisi Shittu
Sep 1, 1999·Clinical Endocrinology·E NieschlagG F Weinbauer

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