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1297538-32-9

1297538-32-9 Structure

1297538-32-9 Structure
IdentificationBack Directory
[Name]

ODM-201
[CAS]

1297538-32-9
[Synonyms]

ODM-201
BAY-1841788
Darolutamide
Darolutamide (ODM-201)
N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
N-[(1S)-2-[3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
[Molecular Formula]

C19H19ClN6O2
Questions and Answers (Q&A)Back Directory
[Description]

ODM-201 is a novel androgen receptor (AR) inhibit designed to inhibit the growth of prostate cancer cells through binding to the AR to inhibit the  testosterone-induced AR nuclear translocation. It is particularly used in patients with progressive metastatic castration-resistant prostate cancer. It is effective in inhibiting the activity of some mutant ARs emerging during antiandrogen therapies, including the F876L mutation version which is resistant to enzalutamide and ARN-509 (the second-generation antiandrogens).Therefore, it has potential to overcome the resistance issue occurring upon AR-targeted therapies.
[References]

Moilanen, Anu Maarit, et al. "Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies." Sci Rep 5.2(2015):12007. Fizazi, Karim, et al. "ODM-201, a new generation androgen receptor inhibitor for castration-resistant prostate cancer: Preclinical and phase I data." Genitourinary Cancers Symposium of the Conquer-Cancer-Foundation of 2013. Fizazi, K, et al. "Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial." Lancet Oncology 5.9(2014):975-85.
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