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Published on: March 6, 2018
Selective androgen receptor modulators in preclinical and clinical development
Ramesh Narayanan1, Michael L Mohler, Casey E Bohl
1Preclinical Research and Development, GTx, Inc., Memphis, Tennessee, USA.
Selective androgen receptor modulators (SARMs) offer anabolic benefits for muscle and bone with fewer side effects than steroids. This review covers SARM research, mechanisms, and therapeutic potential for various conditions.
Area of Science:
- Endocrinology
- Pharmacology
- Molecular Biology
Background:
- The androgen receptor (AR) is crucial for various organ functions, including muscle and bone.
- Selective androgen receptor modulators (SARMs) are nonsteroidal agents targeting AR with anabolic effects.
- SARMs show potential for treating conditions like osteoporosis and muscle wasting.
Purpose of the Study:
- To review the current research and development of SARMs.
- To discuss the crystallography of AR with SARMs.
- To explore the mechanisms of action and therapeutic indications for SARMs.
Main Methods:
- Literature review of current research on SARMs.
- Analysis of crystallographic data for AR-SARM complexes.
- Discussion of proposed mechanisms of action and clinical applications.
Main Results:
- SARMs exhibit osteo- and myo-anabolic activity.
- Compared to testosterone, SARMs have reduced effects on prostate growth.
- SARMs present therapeutic opportunities for muscle wasting, osteoporosis, frailty, and hypogonadism.
Conclusions:
- SARMs represent a promising class of drugs with significant therapeutic potential.
- Further research into SARM mechanisms and clinical applications is warranted.
- SARMs offer a potential alternative to traditional anabolic steroids with an improved safety profile.
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