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Dimethandrolone

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https://www.readbyqxmd.com/read/27907978/comparison-of-the-single-dose-pharmacokinetics-pharmacodynamics-and-safety-of-two-novel-oral-formulations-of-dimethandrolone-undecanoate-dmau-a-potential-oral-male-contraceptive
#1
RANDOMIZED CONTROLLED TRIAL
R Ayoub, S T Page, R S Swerdloff, P Y Liu, J K Amory, A Leung, L Hull, D Blithe, A Christy, J H Chao, W J Bremner, C Wang
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...
March 2017: Andrology
https://www.readbyqxmd.com/read/24789057/single-escalating-dose-pharmacokinetics-safety-and-food-effects-of-a-new-oral-androgen-dimethandrolone-undecanoate-in-man-a-prototype-oral-male-hormonal-contraceptive
#2
RANDOMIZED CONTROLLED TRIAL
Prasanth Surampudi, Stephanie T Page, Ronald S Swerdloff, Jean Jacques Nya-Ngatchou, Peter Y Liu, John K Amory, Andrew Leung, Laura Hull, Diana L Blithe, Jason Woo, William J Bremner, Christina Wang
The novel androgen, dimethandrolone (DMA) has both androgenic and progestational activities, properties that may maximize gonadotropin suppression. We assessed the pharmacokinetics of dimethandrolone undecanoate (DMAU), an orally bioavailable, longer acting ester of DMA, for male contraceptive development. Our objective was to examine the safety and pharmacokinetics of single, escalating doses of DMAU (powder in capsule formulation) administered orally with or without food in healthy men. We conducted a randomized, double-blind Phase 1 study...
July 2014: Andrology
https://www.readbyqxmd.com/read/21164142/development-of-dimethandrolone-17beta-undecanoate-dmau-as-an-oral-male-hormonal-contraceptive-induction-of-infertility-and-recovery-of-fertility-in-adult-male-rabbits
#3
Barbara J Attardi, Jean A Engbring, David Gropp, Sheri Ann Hild
Dimethandrolone undecanoate (DMAU: 7α,11β-dimethyl-19-nortestosterone 17β-undecanoate) is a potent orally active androgen with progestational activity that is in development for therapeutic uses in men. We hypothesized that because of its dual activity, DMAU might have potential as a single-agent oral hormonal contraceptive. To test this possibility, adult male rabbits (5/group) of proven fertility were treated orally with vehicle or DMAU at 1.0, 2.5, 5.0, or 10.0 mg/kg/d for 12 or 13 weeks. Semen and blood samples were collected every other week through week 30...
September 2011: Journal of Andrology
https://www.readbyqxmd.com/read/20798389/long-term-effects-of-dimethandrolone-17%C3%AE-undecanoate-and-11%C3%AE-methyl-19-nortestosterone-17%C3%AE-dodecylcarbonate-on-body-composition-bone-mineral-density-serum-gonadotropins-and-androgenic-anabolic-activity-in-castrated-male-rats
#4
Barbara J Attardi, Brett T Marck, Alvin M Matsumoto, Sailaja Koduri, Sheri A Hild
The potent androgens dimethandrolone 17β-undecanoate (DMAU) and 11β-methyl-19-nortestosterone 17β-dodecylcarbonate (11β-MNTDC) are in development for androgen replacement therapy and hormonal contraception in men. They can be delivered either orally or as long-acting injectables. In the current study, their long-term effects on body composition (percentage lean and fat mass); bone mineral density (BMD); serum gonadotropin levels; and weights of the prostate, seminal vesicles, and levator ani muscle were assessed...
March 2011: Journal of Andrology
https://www.readbyqxmd.com/read/20599615/the-potent-synthetic-androgens-dimethandrolone-7%C3%AE-11%C3%AE-dimethyl-19-nortestosterone-and-11%C3%AE-methyl-19-nortestosterone-do-not-require-5%C3%AE-reduction-to-exert-their-maximal-androgenic-effects
#5
Barbara J Attardi, Sheri A Hild, Sailaja Koduri, Trung Pham, Laurent Pessaint, Jean Engbring, Bruce Till, David Gropp, Anne Semon, Jerry R Reel
Dimethandrolone (DMA: 7α,11β-dimethyl-19-nortestosterone) and 11β-methyl-19-nortestosterone (MNT) are potent androgens in development for hormonal therapy in men. As 5α-reduced androgens, such as 5α-dihydrotestosterone (DHT), may raise the risk of benign prostate hyperplasia, accelerate the development of prostate carcinoma, and increase male pattern baldness and acne, we investigated the role of 5α-reduction in the androgenic activity of DMA and MNT. The authentic 5α-reduced metabolites, 5α-dihydroDMA (5α-DHDMA) and 5α-dihydroMNT (5α-DHMNT), were prepared by chemical synthesis and compared in vitro and in vivo to the parent compounds...
October 2010: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/20378929/effects-of-synthetic-androgens-on-liver-function-using-the-rabbit-as-a-model
#6
Sheri Ann Hild, Barbara J Attardi, Sailaja Koduri, Bruce A Till, Jerry R Reel
The objective of this study was to determine whether the rabbit was a suitable model to test new synthetic androgens for potential liver toxicity within a short dosing interval. Adult male rabbits were dosed orally daily on days 0-13 with 17α-methyltestosterone (MT) as a positive control and testosterone (T) as a negative control to validate this model. Synthetic androgens tested were: 7α-methyl-19-nortestosterone (MENT), dimethandrolone-undecanoate (DMAU), and 11β-methyl-19-nortestosterone-17β-dodecylcarbonate (11β-MNTDC)...
September 2010: Journal of Andrology
https://www.readbyqxmd.com/read/18555683/dimethandrolone-7alpha-11beta-dimethyl-19-nortestosterone-and-11beta-methyl-19-nortestosterone-are-not-converted-to-aromatic-a-ring-products-in-the-presence-of-recombinant-human-aromatase
#7
Barbara J Attardi, Trung C Pham, Lisa C Radler, Janet Burgenson, Sheri A Hild, Jerry R Reel
Dimethandrolone undecanoate (DMAU: 7alpha,11beta-dimethyl-19-nortestosterone 17beta-undecanoate) is a potent orally active androgen in development for hormonal therapy in men. Cleavage of the 17beta-ester bond by esterases in vivo leads to liberation of the biologically active androgen, dimethandrolone (DMA), a 19-norandrogen. For hormone replacement in men, administration of C19 androgens such as testosterone (T) may lead to elevations in circulating levels of estrogens due to aromatization. As several reports have suggested that certain 19-norandrogens may serve as substrates for the aromatase enzyme and are converted to the corresponding aromatic A-ring products, it was important to investigate whether DMA, the related compound, 11beta-methyl-19-nortestosterone (11beta-MNT), also being tested for hormonal therapy in men, and other 19-norandrogens can be converted to aromatic A-ring products by human aromatase...
June 2008: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/16497801/dimethandrolone-undecanoate-a-new-potent-orally-active-androgen-with-progestational-activity
#8
Barbara J Attardi, Sheri A Hild, Jerry R Reel
Dimethandrolone (DMA), the 17beta-undecanoic acid ester of dimethandrolone (DMAU; 7alpha,11beta-dimethyl-19-nortestosterone) is a potent androgen currently in development for therapeutic uses in men. Cleavage of the 17beta-ester bond liberates the biologically active DMA. In this study we investigated the activity of DMAU and DMA both in vivo and in vitro. DMAU was active orally in castrate rat bioassays, and when administered sc, a single dose produced prolonged androgenic activity and suppression of LH with sustained circulating levels of DMA...
June 2006: Endocrinology
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