Minted: - / 5000

2969 Ketodarolutamide
e81e204dfa53a74a4797cf03199384b146f57b4efa41b28d0e10daeb9731af38

Properties

Background

Orange
Bottle

Light blue
Cap

Gray
Syringe

Orange
Bubbles
No
Drops
Yes
Label
Cross

Chemistry

Formula
C19H17ClN6O2
Carbon
19
Polarity
Neutral

Ketodarolutamide (developmental code names ORM-15341, BAY-1896953) is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of darolutamide (ODM-201, BAY-1841788), an NSAA which is used in the treatment of prostate cancer in men. Similarly to its parent compound, darolutamide acts as a highly selective, high-affinity, competitive silent antagonist of the androgen receptor (AR). Both agents show much higher affinity and more potent inhibition of the AR relative to the other NSAAs enzalutamide and apalutamide, although they also possess much shorter and comparatively less favorable elimination half-lives. They have also been found not to activate certain mutant AR variants that enzalutamide and apalutamide do activate. Both darolutamide and ketodarolutamide show limited central nervous system distribution, indicating peripheral selectivity, and little or no inhibition or induction of cytochrome P450 enzymes such as CYP3A4, unlike enzalutamide and apalutamide.

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