Literature DB >> 28621446

The long and winding road for selective androgen receptor modulators.

James T Dalton1.   

Abstract

Numerous selective androgen receptor modulators (SARMs) with differing chemical structures and nearly ideal pharmacological and pharmacokinetic properties have been developed that are well tolerated and selectively increase lean body mass in humans. However, definitive demonstration of the linkage between lean body mass and physical function in a relevant, large patient population has remained elusive for a SARM. The clinical endpoints serving as their basis of approval have shifted with time and clinical indication and are likely to continue to do so as the field matures with additional safety and efficacy data pertaining to the relationship between lean body mass and physical function, regulatory decisions with SARMs and other agents, and yet unexplored clinical indications.
© 2017 The British Pharmacological Society.

Entities:  

Keywords:  clinical trials; drug development; lung cancer; oncology; phase I; statistics and study design

Mesh:

Substances:

Year:  2017        PMID: 28621446      PMCID: PMC5595949          DOI: 10.1111/bcp.13345

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  18 in total

1.  Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators.

Authors:  Casey E Bohl; Zengru Wu; Jiyun Chen; Michael L Mohler; Jun Yang; Dong Jin Hwang; Suni Mustafa; Duane D Miller; Charles E Bell; James T Dalton
Journal:  Bioorg Med Chem Lett       Date:  2008-09-05       Impact factor: 2.823

2.  Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways.

Authors:  Ramesh Narayanan; Christopher C Coss; Muralimohan Yepuru; Jeffrey D Kearbey; Duane D Miller; James T Dalton
Journal:  Mol Endocrinol       Date:  2008-09-18

3.  Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women.

Authors:  Richard V Clark; Ann C Walker; Susan Andrews; Philip Turnbull; Jeffrey A Wald; Mindy H Magee
Journal:  Br J Clin Pharmacol       Date:  2017-06-10       Impact factor: 4.335

4.  The long and winding road for selective androgen receptor modulators.

Authors:  James T Dalton
Journal:  Br J Clin Pharmacol       Date:  2017-07-17       Impact factor: 4.335

5.  The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial.

Authors:  James T Dalton; Kester G Barnette; Casey E Bohl; Michael L Hancock; Domingo Rodriguez; Shontelle T Dodson; Ronald A Morton; Mitchell S Steiner
Journal:  J Cachexia Sarcopenia Muscle       Date:  2011-08-02       Impact factor: 12.910

6.  The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men.

Authors:  Shehzad Basaria; Lauren Collins; E Lichar Dillon; Katie Orwoll; Thomas W Storer; Renee Miciek; Jagadish Ulloor; Anqi Zhang; Richard Eder; Heather Zientek; Gilad Gordon; Syed Kazmi; Melinda Sheffield-Moore; Shalender Bhasin
Journal:  J Gerontol A Biol Sci Med Sci       Date:  2012-03-28       Impact factor: 6.053

7.  Mechanism of the tissue-specific action of the selective androgen receptor modulator S-101479.

Authors:  Kazuyuki Furuya; Noriko Yamamoto; Yuki Ohyabu; Teruyuki Morikyu; Hirohide Ishige; Michael Albers; Yasuhisa Endo
Journal:  Biol Pharm Bull       Date:  2013       Impact factor: 2.233

8.  Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia.

Authors:  Wenqing Gao; Jeffrey D Kearbey; Vipin A Nair; Kiwon Chung; A F Parlow; Duane D Miller; James T Dalton
Journal:  Endocrinology       Date:  2004-08-12       Impact factor: 4.736

9.  The Concise Guide to PHARMACOLOGY 2015/16: Nuclear hormone receptors.

Authors:  Stephen Ph Alexander; John A Cidlowski; Eamonn Kelly; Neil Marrion; John A Peters; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Christopher Southan; Jamie A Davies
Journal:  Br J Pharmacol       Date:  2015-12       Impact factor: 8.739

Review 10.  Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials).

Authors:  Jeffrey Crawford; Carla M M Prado; Mary Ann Johnston; Richard J Gralla; Ryan P Taylor; Michael L Hancock; James T Dalton
Journal:  Curr Oncol Rep       Date:  2016-06       Impact factor: 5.075

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  5 in total

1.  The long and winding road for selective androgen receptor modulators.

Authors:  James T Dalton
Journal:  Br J Clin Pharmacol       Date:  2017-07-17       Impact factor: 4.335

2.  Selective androgen receptor modulators (SARMs) have specific impacts on the mouse uterus.

Authors:  Ioannis Simitsidellis; Arantza Esnal-Zuffiaure; Olympia Kelepouri; Elisabeth O'Flaherty; Douglas A Gibson; Philippa T K Saunders
Journal:  J Endocrinol       Date:  2019-09       Impact factor: 4.286

Review 3.  Selective androgen receptor modulators: the future of androgen therapy?

Authors:  Andrew R Christiansen; Larry I Lipshultz; James M Hotaling; Alexander W Pastuszak
Journal:  Transl Androl Urol       Date:  2020-03

Review 4.  Inactivity and Skeletal Muscle Metabolism: A Vicious Cycle in Old Age.

Authors:  Elena Rezuş; Alexandra Burlui; Anca Cardoneanu; Ciprian Rezuş; Cătălin Codreanu; Mirela Pârvu; Gabriela Rusu Zota; Bogdan Ionel Tamba
Journal:  Int J Mol Sci       Date:  2020-01-16       Impact factor: 5.923

5.  Effect of Selective Androgen Receptor Modulator Enobosarm on Bone Healing in a Rat Model for Aged Male Osteoporosis.

Authors:  Marina Komrakova; Janek Nagel; Daniel Bernd Hoffmann; Wolfgang Lehmann; Arndt Friedrich Schilling; Stephan Sehmisch
Journal:  Calcif Tissue Int       Date:  2020-09-02       Impact factor: 4.333

  5 in total

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