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| Clinical data | |
|---|---|
| Other names | ORM-15341; BAY-1896953 |
| Drug class | Nonsteroidal antiandrogen |
| Pharmacokinetic data | |
| Eliminationhalf-life | 10.0 hours[1] |
| Identifiers | |
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| CAS Number | |
| PubChemCID | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.235.511 |
| Chemical and physical data | |
| Formula | C19H17ClN6O2 |
| Molar mass | 396.84 g·mol−1 |
| 3D model (JSmol) | |
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Ketodarolutamide (developmental code namesORM-15341,BAY-1896953) is anonsteroidal antiandrogen (NSAA) and the majoractive metabolite ofdarolutamide (ODM-201, BAY-1841788), an NSAA which is used in the treatment ofprostate cancer in men.[2][3][4][5] Similarly to itsparent compound, ketodarolutamide acts as a highlyselective, high-affinity,competitivesilent antagonist of theandrogen receptor (AR).[2][3][4][5] Both agents show much higher affinity and morepotent inhibition of the AR relative to the other NSAAsenzalutamide andapalutamide, although they also possess much shorter and comparatively less favorableelimination half-lives.[2][3][4][5] They have also been found not to activate certainmutant AR variants that enzalutamide and apalutamide do activate.[2][3][4][5] Both darolutamide and ketodarolutamide show limitedcentral nervous systemdistribution, indicatingperipheral selectivity, and little or noinhibition orinduction ofcytochrome P450enzymes such asCYP3A4, unlike enzalutamide and apalutamide.[2][3][4][5]
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