Comparison of the single dose pharmacokinetics, pharmacodynamics, and safety of two novel oral formulations of dimethandrolone undecanoate (DMAU): a potential oral, male contraceptive
| Autor: | Jing H. Chao, A. Christy, Peter Liu, R. Ayoub, Diana L. Blithe, William J. Bremner, Stephanie T. Page, John K. Amory, Christina Wang, Andrew Leung, Ronald S. Swerdloff, Laura Hull |
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| Rok vydání: | 2016 |
| Předmět: |
Adult
Male medicine.medical_specialty Urology Endocrinology Diabetes and Metabolism Population Administration Oral Male contraceptive Pharmacology Placebo Article 03 medical and health sciences Drug Delivery Systems 0302 clinical medicine Endocrinology Double-Blind Method Pharmacokinetics Internal medicine medicine Humans Nandrolone Testosterone 030212 general & internal medicine education education.field_of_study 030219 obstetrics & reproductive medicine Estradiol business.industry Contraceptive Agents Male Dihydrotestosterone Dimethandrolone Luteinizing Hormone Reproductive Medicine Pharmacodynamics Dimethandrolone-undecanoate Follicle Stimulating Hormone business medicine.drug |
| Zdroj: | Andrology. 5:278-285 |
| ISSN: | 2047-2919 |
| DOI: | 10.1111/andr.12303 |
| Popis: | Dimethandrolone (DMA, 7α,11β-dimethyl-19-nortestosterone) has both androgenic and progestational activities, ideal properties for a male hormonal contraceptive. In vivo, dimethandrolone undecanoate (DMAU) is hydrolyzed to DMA. We showed previously that single oral doses of DMAU powder in capsule taken with food are well tolerated and effective at suppressing both LH and testosterone (T), but absorption was low. We compared the pharmacokinetics and pharmacodynamics of two new formulations of DMAU, in castor oil and in self-emulsifying drug delivery systems (SEDDS), with the previously tested powder formulation. DMAU was dosed orally in healthy adult male volunteers at two academic medical centers. For each formulation tested in this double-blind, placebo-controlled study, 10 men received single, escalating, oral doses of DMAU (100, 200, and 400 mg) and two subjects received placebo. All doses were evaluated for both fasting and with a high fat meal. All three formulations were well tolerated without clinically significant changes in vital signs, blood counts, or serum chemistries. For all formulations, DMA and DMAU showed higher maximum (p |
| Databáze: | OpenAIRE |
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