Cortexolone 17 alpha-propionate
Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist, displays a strong local antiandrogenic activity in hamster's flank organ test, does not exhibit antiandrogenic activity after subcutaneous injection in vivo.
Phase 3 Clinical
Enobosarm (GTx-024, MK-2866, Ostarine) is a selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and osteoporosis.
Phase 2 Clinical
VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression; effectively blocks transcriptional activity of full-length and splice variant AR forms at low to sub-micromolar concentrations; reduces tumor volume and abolishes PSA production in LNCaP xenograft model.
EPI-001 is a small molecule that blocks transactivation of the androgen Receptor (AR) NTD (IC50=6 uM) and specificly inhibits AR without attenuating transcriptional activities of related steroid receptors; targets the transactivation unit 5 of AR and interacts with AF-1 in the NTD to prevent protein-protein interactions; inhibits endogenous expression of androgen-regulated genes, inhibits both androgen-dependent and androgen-independent (OCM-induced) proliferation of LNCaP cells; reduces the growth of CRPC xenografts; also is a selective PPAR-gamma modulator.
BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM; displays high selectivity over the glucocorticoid and progesterone receptors; displayed 3-7-fold increased antagonist activity of AR transactivation compared with bicalutamide; strongly inhibits androgen-dependent growth of the ventral prostate and seminal vesicles in rats, and is efficacious in CWR-22-BMSLD1 tumors initially refractory to treatment with bicalutamide.
Phase 1 Clinical
GLPG-0492 R enantiomer
The R enantiomer of GLPG-0492, a non-steroidal selective androgen receptor modulator (SARM) for treatment for Duchenne muscular dystrophy (DMD); shows weak potency (1.25 uM) compared with GLPG-0492.
ODM-201 (BAY-1841788, Darolutamide) is a potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM; inhibits wtAR/AR(F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR(W741L) and AR(T877A); inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay; reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model.
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