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Hormonal antineoplastic drugs
Ketodarolutamide
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    Ketodarolutamide

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    Ketodarolutamide
    ORM-15341.svg
    Clinical data
    Other names ORM-15341; BAY-1896953
    Drug class Nonsteroidal antiandrogen
    Pharmacokinetic data
    Elimination half-life 10.0 hours
    Identifiers
    • 3-acetyl-N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-1H-pyrazole-5-carboxamide
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    ECHA InfoCard 100.235.511
    Chemical and physical data
    Formula C19H17ClN6O2
    Molar mass 396.84 g·mol−1
    3D model (JSmol)
    • C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=CC(=NN3)C(=O)C
    • InChI=1S/C19H17ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-/m0/s1
    • Key:GMBPVBVTPBWIKC-NSHDSACASA-N

    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, ketodarolutamide 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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