Development of selective androgen receptor modulators (SARMs).

Area of Science:

• Endocrinology
• Pharmacology
• Molecular Biology

Background:

• The Androgen Receptor (AR) is crucial in various physiological and pathological processes.
• Steroidal androgens face limitations in therapeutic use due to widespread expression and cross-reactivity.
• Selective androgen receptor modulators (SARMs) offer tissue-specific activation, minimizing side effects.

Purpose of the Study:

• To review the evolution of SARMs from early concepts to near-therapeutic application.
• To discuss the mechanisms of action and therapeutic potential of SARMs.
• To highlight SARMs as potential treatments for conditions including muscle-wasting, breast cancer, and osteoporosis.

Main Methods:

• Literature review of scientific publications and research on Androgen Receptor modulators.
• Analysis of the development and biological characterization of SARMs over the past two decades.
• Synthesis of contemporary views on SARM mechanisms and therapeutic benefits.

Main Results:

• SARMs have progressed significantly, moving from proof-of-concept to potential clinical use.
• SARMs demonstrate tissue-selective modulation of the Androgen Receptor.
• The development of SARMs presents a promising therapeutic avenue with reduced adverse effects compared to traditional androgens.

Conclusions:

• SARMs represent a significant advancement in targeting the Androgen Receptor pathway.
• Their tissue-selective action holds promise for treating various diseases with improved safety profiles.
• Continued research into SARMs is crucial for realizing their full therapeutic potential.