Design , Synthesis , and Preclinical Characterization of the Selective Androgen Receptor Modulator ( SARM ) RAD 140

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.

[1]  F. Piu,et al.  Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. , 2009, Journal of medicinal chemistry.

[2]  S. Bhasin,et al.  Selective androgen receptor modulators as function promoting therapies , 2009, Current opinion in clinical nutrition and metabolic care.

[3]  E. Garvey,et al.  1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position. , 2009, Bioorganic & medicinal chemistry letters.

[4]  E. Garvey,et al.  The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore. , 2009, Bioorganic & medicinal chemistry letters.

[5]  P. Hodor,et al.  Gene expression analyses in cynomolgus monkeys provides mechanistic insight into high-density lipoprotein-cholesterol reduction by androgens in primates. , 2008, Endocrinology.

[6]  L. Freedman,et al.  Selective androgen receptor modulators for frailty and osteoporosis. , 2007, Current opinion in investigational drugs.

[7]  Haixia Wang,et al.  Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications. , 2007, Journal of medicinal chemistry.

[8]  J. Dalton,et al.  Ockham's razor and selective androgen receptor modulators (SARMs): are we overlooking the role of 5alpha-reductase? , 2007, Molecular interventions.

[9]  Donald P. McDonnell,et al.  International Union of Pharmacology. LXV. The Pharmacology and Classification of the Nuclear Receptor Superfamily: Glucocorticoid, Mineralocorticoid, Progesterone, and Androgen Receptors , 2006, Pharmacological Reviews.

[10]  J. Dalton,et al.  Chemistry and Structural Biology of Androgen Receptor , 2005 .

[11]  Duane D. Miller,et al.  The Para Substituent of S-3-(Phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides Is a Major Structural Determinant of in Vivo Disposition and Activity of Selective Androgen Receptor Modulators , 2005, Journal of Pharmacology and Experimental Therapeutics.

[12]  D. Christiani,et al.  Body weight, alcohol consumption and liver enzyme activity--a 4-year follow-up study. , 2001, International journal of epidemiology.

[13]  Chris P. Miller,et al.  A new synthesis of highly functionalized oxazoles , 1993 .

[14]  R. K. Meyer,et al.  Myotrophic Activity of 19-Nortestosterone and Other Steroids Determined by Modified Levator Ani Muscle Method.∗ , 1953, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine.

[15]  Duane D. Miller,et al.  Nonsteroidal Tissue‐Selective Androgen Receptor Modulators , 2008 .

[16]  Stanley R Krystek,et al.  Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. , 2007, Endocrinology.

[17]  F. Selmin,et al.  Assessment of fertility in male rats after extended chemical castration with a GnRH antagonist. , 2004, AAPS PharmSci.

[18]  Y. Nishino.  Effects of androgens and related steroids on liver functions and enzymes. , 1975, Pharmacology & therapeutics. Part B: General & systematic pharmacology.