Pharmacokinetics and Pharmacodynamics of LGD-3303 [9-Chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an Orally Available Nonsteroidal-Selective Androgen Receptor Modulator

@article{Vajda2009PharmacokineticsAP,
  title={Pharmacokinetics and Pharmacodynamics of LGD-3303 [9-Chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an Orally Available Nonsteroidal-Selective Androgen Receptor Modulator},
  author={Eric G. Vajda and Francisco J. L{\'o}pez and Peter J. Rix and Robert Hill and Yanling Chen and Kyoung Jin Lee and Zhihong O’Brien and William Y. Chang and Martin D. Meglasson and Yong-Hee Lee},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2009},
  volume={328},
  pages={663 - 670}
}
Selective androgen receptor modulators (SARMs) are a new class of molecules in development to treat a variety of diseases. SARMs maintain the beneficial effects of androgens, including increased muscle mass and bone density, while having reduced activity on unwanted side effects. The mechanisms responsible for the tissue-selective activity of SARMs are not fully understood, and the pharmacokinetic (PK)/pharmacodynamic (PD) relationships are poorly described. Tissue-specific compound… 
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Pharmacological characterization of an imidazolopyrazole as novel selective androgen receptor modulator

Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.

This Award Address attempts to chronicle the landmark discoveries, organize the SARM landscape into clinically relevant bins, and provide insight into the clinical prospects for SARMs.

Deciphering the selective androgen receptor modulators paradigm

The aim of the present paper is to summarize the current standing of research and development of SARMs and plausible molecular mechanisms underlying the potential for selective modulation of androgen receptor (AR) by different ligands and provides an update on SARM discovery paradigms for preclinical evaluations.

Selective androgen receptor modulator activity of a steroidal antiandrogen TSAA-291 and its cofactor recruitment profile.

Recent advances in the development of selective androgen receptor modulators

A new class of molecules targeting androgen receptors called selective androgen receptor modulators is being developed, analogous to the clinically successful and at present marketed selective estrogen receptors modulators.

A novel selective androgen receptor modulator, NEP28, is efficacious in muscle and brain without serious side effects on prostate.

Recent developments in antiandrogens and selective androgen receptor modulators

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