Biological Activity
ODM-201 is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in AR-HEK293 cells.
In Vitro
In competitive AR binding assays, the inhibition constant (Ki) values of 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 ODM-201 and ORM-15341 vs. 410 and 420 nM for enzalutamide and ARN-509. ODM-201 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 ODM-201 and ORM-15341 are specific to AR-dependent PC cells[1].
In Vivo
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 ODM-201 twice daily do not decrease significantly during the treatment[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.