Mk-4541

MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model[1].

Research Areas >> Cancer

Research Areas >> Endocrinology

Signaling Pathways >> Metabolic Enzyme/Protease >> 5 alpha Reductase

Signaling Pathways >> Others >> Androgen Receptor

MK-4541 (100 mg/kg; 每天1次，每周5次，持续5周) 抑制含 R-3327-G 细胞的无胸腺裸鼠前列腺肿瘤生长[1]。 MK-4541 (100 mg/kg, 200 mg/kg; 每周5次，持续5周) 对精囊具有抗雄激素作用，降低完好男性的血浆睾酮浓度，并抑制 Ki67 表达[1]。 MK-4541 (15 mg/kg, 50 mg/kg; 每周5次，持续8周) 导致成年阉割小鼠肌肉骨骼质量和功能的损失[1]。 Animal Model: R3327-G prostate tumors in xenograft mouse model[1] Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg Administration: Oral gavage; once daily, 5 times per week for 5 weeks Result: Significantly inhibited tumor growth at 100 mg/kg, as well as reducing plasma testosterone concentration and Ki67 expression.

[1]. Chisamore MJ, et al. A novel selective androgen receptor modulator (SARM) MK-4541 exerts anti-androgenic activity in the prostate cancer xenograft R-3327G and anabolic activity on skeletal muscle mass & function in castrated mice. J Steroid Biochem Mol Biol. 2016 Oct;163:88-97.