Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

Chris P Miller; Maysoun Shomali; C Richard Lyttle; Louis St L O'Dea; Hillary Herendeen; Kyla Gallacher; Dottie Paquin; Dennis R Compton; Bishwabhusan Sahoo; Sean A Kerrigan; Matthew S Burge; Michael Nickels; Jennifer L Green; John A Katzenellenbogen; Alexei Tchesnokov; Gary Hattersley

doi:10.1021/ml1002508

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

ACS Med Chem Lett. 2010 Dec 2;2(2):124-9. doi: 10.1021/ml1002508. eCollection 2011 Feb 10.

Authors

Chris P Miller¹, Maysoun Shomali¹, C Richard Lyttle¹, Louis St L O'Dea¹, Hillary Herendeen¹, Kyla Gallacher¹, Dottie Paquin¹, Dennis R Compton², Bishwabhusan Sahoo², Sean A Kerrigan², Matthew S Burge², Michael Nickels², Jennifer L Green², John A Katzenellenbogen³, Alexei Tchesnokov⁴, Gary Hattersley¹

Affiliations

¹ Radius Health, Inc., 300 Technology Square, Cambridge, Massachusetts 02139, United States.
² Obiter Research, 2809 Gemini Court, Champaign, Illinois 61822-9647, United States.
³ Department of Chemistry, University of Illinois at Urbana-Champaign, 600 South Mathews Avenue, Urbana, Illinois 61801, United States.
⁴ Cambridge Major Laboratories, Inc., W130 N10497 Washington Drive, Germantown, Wisconsin 53022, United States.

Abstract

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.

Keywords: Androgen; Herschberger assay; SARM; cachexia; oxadiazole; primate.