AR antagonist 9

AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC₅₀ value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC₅₀ = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against AR_F876L/T877A and AR_W741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance.

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