Catalog No.S7559 Synonyms: BAY-1841788
Molecular Weight(MW): 398.85
Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
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Choose Selective Androgen Receptor Inhibitors
|Description||Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.|
In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. 
|In vivo||In mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. |
AR binding affinity:AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1 nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100 μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100 μL of supernatant fraction in 200 μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4 °C.
|In vitro||DMSO||80 mg/mL (200.57 mM)|
|Ethanol||38 mg/mL warmed (95.27 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02972060||Not yet recruiting||Prostate Cancer||European Organisation for Research and Treatment of Cancer - EORTC|Bayer||March 2017||Phase 2|
|NCT03004534||Not yet recruiting||Breast Cancer Female||Translational Research in Oncology|Bayer||February 2017||Early Phase 1|
|NCT03048110||Not yet recruiting||Biological Availability||Bayer|Orion Corporation, Orion Pharma||February 2017||Phase 1|
|NCT02933801||Not yet recruiting||Prostate Cancer Metastatic|Prostate Cancer||Swiss Group for Clinical Cancer Research||January 2017||Phase 2|
|NCT02799602||Recruiting||Prostatic Neoplasms||Bayer|Orion Corporation, Orion Pharma||November 2016||Phase 3|
|NCT02671097||Completed||Healthy Volunteers|Pharmacokinetics|Drug Interaction||Bayer||February 2016||Phase 1|
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