BMS-564,929

BMS-564,929 is an investigational selective androgen receptor modulator (SARM) which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men ("andropause"). These symptoms may include depression, loss of muscle mass and strength, reduction in libido and osteoporosis. Treatment with exogenous testosterone is effective in counteracting these symptoms but is associated with a range of side effects, the most serious of which is enlargement of the prostate gland, which can lead to benign prostatic hyperplasia and even prostate cancer. This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in the prostate.^[1]

BMS-564,929

Clinical data
Other names	PS-178990
Legal status
Legal status	US: Investigational New Drug
Identifiers
IUPAC name 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-hexahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile
CAS Number	627530-84-1 N
PubChem CID	9882972
DrugBank	DB07286 N
ChemSpider	8058647 N
UNII	9BLW27W4X7
ChEMBL	ChEMBL229264 N
CompTox Dashboard (EPA)	DTXSID50432357
ECHA InfoCard	100.233.303
Chemical and physical data
Formula	C14H12ClN3O3
Molar mass	305.72 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(C=CC(=C1Cl)C#N)N2C(=O)[C@@H]3[C@@H](CCN3C2=O)O
InChI InChI=1S/C14H12ClN3O3/c1-7-9(3-2-8(6-16)11(7)15)18-13(20)12-10(19)4-5-17(12)14(18)21/h2-3,10,12,19H,4-5H2,1H3/t10-,12+/m1/s1 N Key:KEJORAMIZFOODM-PWSUYJOCSA-N N
NY (what is this?)  (verify)

BMS-564,929 is one such compound currently in early human clinical trials, which is an orally active, potent, and selective agonist for androgen receptors (Ki 2.1nM, 20x functional selectivity for muscle tissue over prostate) and in studies on castrated rats it was shown to counteract the decrease in muscle mass over time, and at higher doses even increased muscle mass, without significantly affecting prostate tissue.^[2] It does however vastly reduce luteinizing hormone levels, it being an astonishing 33× more suppressive compound than testosterone, which may be a problem in human clinical use.^[3]

Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and fitness, potentially producing effects similar to anabolic steroids but with significantly fewer side effects. For this reason, SARMs have already been banned by the World Anti-Doping Agency since January 2008 despite no drugs from this class yet being in clinical use, and blood tests for all known SARMs are currently being developed.^[4][5]