Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models

Darolutamide is a novel androgen receptor (AR) antagonist with a distinct chemical structure compared to other AR antagonists and currently in clinical Phase 3 trials for prostate cancer. Using cell‐based transactivation assays, we demonstrate that darolutamide, its diastereomers and its main metabo...

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Veröffentlicht in:	International journal of cancer 2019-09, Vol.145 (5), p.1382-1394
Hauptverfasser:	Sugawara, Tatsuo, Baumgart, Simon J., Nevedomskaya, Ekaterina, Reichert, Kristin, Steuber, Holger, Lejeune, Pascale, Mumberg, Dominik, Haendler, Bernard
Format:	Artikel
Sprache:	eng
Schlagworte:	androgen receptor Androgen Receptor Antagonists - chemistry Androgen Receptor Antagonists - pharmacology Androgen receptors Androgens Animals antagonist Antagonists Cancer Cell Line, Tumor Cell lines Cell viability Clinical trials Gene Expression - drug effects Gene regulation Humans Hydrophobicity Male Medical research Mice Mice, SCID Models, Molecular Molecular Cancer Biology Molecular modelling Mutants Prostate Prostate cancer Prostatic Neoplasms, Castration-Resistant - drug therapy Prostatic Neoplasms, Castration-Resistant - genetics Prostatic Neoplasms, Castration-Resistant - metabolism Protein Domains Pyrazoles - chemistry Pyrazoles - pharmacology Receptors, Androgen - chemistry Receptors, Androgen - genetics Receptors, Androgen - metabolism Regulatory sequences Tumor cell lines Viability Xenograft Model Antitumor Assays Xenografts
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