Asset Details
Do you wish to reserve the book?
Safety and Pharmacokinetics of Single-Dose Novel Oral Androgen 11beta-Methyl-19-Nortestosterone-17beta-Dodecylcarbonate in Men
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Safety and Pharmacokinetics of Single-Dose Novel Oral Androgen 11beta-Methyl-19-Nortestosterone-17beta-Dodecylcarbonate in Men
Do you wish to request the book?
Safety and Pharmacokinetics of Single-Dose Novel Oral Androgen 11beta-Methyl-19-Nortestosterone-17beta-Dodecylcarbonate in Men
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Safety and Pharmacokinetics of Single-Dose Novel Oral Androgen 11beta-Methyl-19-Nortestosterone-17beta-Dodecylcarbonate in Men
2019
Overview
Context: 11[beta]-Methyl-19-nortestosterone-17[beta]-dodecylcarbonate (11[beta]-MNTDC) is an orally bioavailable prodrug of 11[beta]-methyl-19-nortestosterone (11[beta]-MNT) with androgenic and progestational activity. Objectives: (i) Quantify 11[beta]-MNT binding to androgen and progesterone receptors. (ii) Evaluate safety, tolerability, and serum gonadotropin and testosterone suppression by 11[beta]-MNTDC in men. Design and Setting: (i) In vitro receptor binding and transactivation studies and (ii) randomized, double-blind, placebo-controlled single-dose, dose-escalating phase I study at two academic medical centers. Participants and Intervention: Twelve healthy male volunteers were randomized (five active, one placebo) to escalating single oral doses (100, 200, 400, and 800 mg) of 11[beta]-MNTDC or placebo given with or without food. Main Outcome Measures: (i) In vitro 11[beta]-MNT/11[beta]-MNTDC human receptor binding and trans-activation and (ii) safety and tolerability, pharmacokinetics, and quantification of serum gonadotropin and testosterone concentrations for 24 hours following dosing. Results: 11[beta]-MNT avidly binds and activates human androgen and progesterone receptors, but 11[beta]-MNTDC has minimal activity. Single oral doses of 11[beta]-MNTDC were well tolerated without serious adverse events. Administration of 11[beta]-MNTDC with food markedly increased average 11[beta]-MNTDC and 11[beta]-MNT serum concentrations (P < 0.001 for all doses) compared with fasting with a significant dose-related effect on average serum drug concentrations (P < 0.0001). The 200-, 400-, and 800-mg doses significantly suppressed average serum testosterone concentrations (P < 0.05). Conclusions: A single, oral dose of 1133-MNTDC up to 800 mg administered with food is safe and well tolerated in healthy men. The active drug 11[beta]-MNT has androgenic and progestational activity, rapidly suppresses serum testosterone, and is a promising candidate for an effective once-daily oral male hormonal contraceptive. (J Clin Endocrinol Metab 104: 629-638, 2019)
Publisher
Oxford University Press
Subject
