Daily Oral Administration of the Novel Androgen 11β-MNTDC Markedly Suppresses Serum Gonadotropins in Healthy Men

Daily Oral Administration of the Novel Androgen 11β-MNTDC Markedly Suppresses Serum Gonadotropins in Healthy Men / Fiona Yuen, Arthi Thirumalai, Cindy Pham, Ronald S. Swerdloff, Bradley D. Anawalt, Peter Y. Liu, John K. Amory, William J. Bremner, Clint Dart, Hongsheng Wu, Laura Hull, Diana L. Blithe, Jill Long, Christina Wang, Stephanie T. Page. - (The Journal of Clinical Endocrinology & Metabolism 105 (2020) 3 (March); p. 835–847).
- PMID: 31976519.
- PMCID: PMC7049261.
- DOI: 10.1210/clinem/dgaa032


Abstract

Background: 11β-methyl-19-nortestosterone (11β-MNT) is a modified testosterone (T) with androgenic and progestational activity. A single oral dose of the prodrug, 11β-MNT dodecylcarbonate (11β-MNTDC), was well tolerated in healthy men.

Methods: We conducted a randomized, double-blind study at 2 academic medical centers. 42 healthy men (18-50 years) were randomized to receive oral placebo or 11β-MNTDC, 200 or 400 mg daily, for 28 consecutive days. Primary outcome (safety and tolerability) measures were assessed twice per week. Subjects underwent serial blood sampling over 24 hours on days 1 and 28 to assess secondary outcomes: pharmacokinetics (serum drug concentrations); pharmacodynamics of 11β-MNTDC (serum sex steroids and gonadotropins); and mood and sexual function (via validated questionnaires).

Results: There were no serious adverse events. No participants discontinued because of an adverse event or laboratory test abnormality. 11β-MNTDC resulted in a dose-related increase in serum 11β-MNTDC and 11β-MNT concentrations sustained over 24 hours. Administration of 11β-MNTDC resulted in a marked suppression of serum gonadotropins, T, calculated free T, estradiol, and SHBG over the treatment period (P < 0.01). Adverse effects that may be related to 11β-MNTDC included weight gain, acne, headaches, fatigue, and mild mood changes, with 5 men reporting decreased libido and 3 decreased erectile/ejaculatory function. Serum low-density lipoprotein cholesterol, weight (~2 kg), hematocrit, and hemoglobin increased and serum high-density lipoprotein cholesterol decreased in both 11β-MNTDC groups.

Conclusion: Daily oral 11β-MNTDC for 28 days in healthy men markedly suppressed serum gonadotropin and T concentrations without serious adverse effects. These results warrant further evaluation of 11β-MNTDC as a potential male oral contraceptive.

Original document

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Study
Date
24 January 2020
People
Amory, John K.
Anawalt, Bradley D.
Blithe, Diana L.
Bremner, William J.
Dart, Clint
Hull, Laura
Liu, Peter Y.
Long, Jill
Page, Stephanie T.
Pham, Cindy
Swerdloff, Ronald S.
Thirumalai, Arthi
Wang, Christina
Wu, Hongsheng
Yuen, Fiona
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United States of America
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English
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Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
University of California, Los Angeles (UCLA)
University of Washington (UW)
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30 March 2020
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8 April 2020
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