Article
Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer.
Molecular cancer therapeutics - 1 May 2021
Branch Jonathan R, Bush Tammy L, Pande Vineet, Connolly Peter J, Zhang Zhuming, Hickson Ian, Ondrus Janine, Jaensch Steffen, Bischoff James R, Habineza Georges, Van Hecke Geert, Meerpoel Lieven, Packman Kathryn, Parrett Christopher J, Chong Yolanda T, Gottardis Marco M, Bignan Gilles
Abstract excerpt
Numerous mechanisms of resistance arise in response to treatment with second-generation androgen receptor (AR) pathway inhibitors in metastatic castration-resistant prostate cancer (mCRPC). Among these, point mutations in the ligand binding domain can transform antagonists into agonists, driving the disease through activation of AR signaling. To address this unmet need, we report the discovery of JNJ-63576253, a...
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