GTx-027

GTx-027 is a selective androgen receptor modulator (SARM) which was under development for or of potential interest in the treatment of breast cancer and stress urinary incontinence (SUI) but was never marketed.^{[2][3][1][4][5]} It is taken by mouth.^[1]

GTx-027

Clinical data
Other names	GTx027
Routes of administration	Oral[1]
Drug class	Selective androgen receptor modulator[1]
Identifiers
IUPAC name (2S)-N-(3-chloro-4-cyanophenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide
CAS Number	928122-40-1 Y
PubChem CID	23653581
Chemical and physical data
Formula	C18H14ClN3O3
Molar mass	355.78 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@](COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)Cl)O
InChI InChI=1S/C18H14ClN3O3/c1-18(24,11-25-15-6-2-12(9-20)3-7-15)17(23)22-14-5-4-13(10-21)16(19)8-14/h2-8,24H,11H2,1H3,(H,22,23)/t18-/m0/s1 Key:IEGVUEFEHAFTNS-SFHVURJKSA-N

Description

The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic (androgenic) and antagonistic (antiandrogenic) effects.^[1][5] It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells in vitro.^[6][7] In addition, it has been found to increase pelvic floor muscle weight in ovariectomized female rodents.^[1][8][4] The drug has been found to increase body weight, lean body mass, and muscle strength in animals as well.^[9][10] In terms of chemical structure, GTx-027 is a nonsteroidal arylpropionamide SARM and is an analogue of enobosarm (ostarine; GTx-024).^[1][4]

GTx-027 was first described in the scientific literature by 2013.^[5][11] It is said to have either not passed preclinical research^[1] or to have reached phase 1 clinical trials prior to the discontinuation of its development.^[3] The drug was developed by GTx.^[2][3]