ODM-201(also known as BAY-1841788)is a novel, nonsteroidal, orally active AR inhibitor that inhibits potently androgen binding to AR and androgen-induced nuclear translocation of AR in AR overexpressing cells. ODM-201 has been studied in phase I and phase II clinical trials and has thus far been found to be effective and well-tolerated, with the most commonly reported side effects including fatigue, nausea,and diarrhea.No seizures have been observed.As of July 2015, ODM-201 is in phase III trials for CRPC.
ORM-15341 is the main active metabolite of ODM-201. It, similarly, is a full antagonist of the AR, with an affinity (Ki) of 8 nM and an IC50 of 38 nM.
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