Darolutamide

1297538-32-9

C19H19ClN6O2

DMSO : >= 44 mg/mL (110.32 mM)

Others

Darolutamide (ODM-201; BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC₅₀ of 26 nM in in vitro assay. IC50 & Target: IC50: 26 nM (AR-HEK293 cells, AR)^[1] In Vitro: In competitive AR binding assays, the inhibition constant (Ki) values of Darolutamide (ODM-201) are 11 nM. ODM-201and ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than enzalutamide or ARN-509, IC50 values being 230 and 170 nM for Darolutamide and ORM-15341 vs. 410 and 420 nM for enzalutamide and ARN-509. Darolutamide has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells confirming that the antiproliferative properties of Darolutamide and ORM-15341 are specific to AR-dependent PC cells^[1]. In Vivo: Darolutamide (ODM-201) showes a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p<0.001) or Enzalutamide (p=0.0245), which also showes inhibition of tumor growth (p<0.05) vs. castrated, untreated mice. Further, there is no sign of treatment-related toxicities; the body weights of mice treated with Darolutamide twice daily do not decrease significantly during the treatment^[1].