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Start Over Author "Parrett CJ" Topic androgen receptor antagonists

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1. 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.

Author

Branch JR, Bush TL, Pande V, Connolly PJ, Zhang Z, Hickson I, Ondrus J, Jaensch S, Bischoff JR, Habineza G, Van Hecke G, Meerpoel L, Packman K, Parrett CJ, Chong YT, Gottardis MM, and Bignan G

Subjects
Androgen Receptor Antagonists pharmacology, Animals, Cell Line, Tumor, Humans, Ligands, Male, Mice, Models, Molecular, Mutation, Rats, Xenograft Model Antitumor Assays, Androgen Receptor Antagonists therapeutic use, Prostatic Neoplasms, Castration-Resistant drug therapy, Protein Domains genetics
Abstract

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 next-generation AR pathway inhibitor that potently abrogates AR signaling in models of human prostate adenocarcinoma. JNJ-63576253 is advancing as a clinical candidate with potential effectiveness in the subset of patients who do not respond to or are progressing while on second-generation AR-targeted therapeutics., (©2021 American Association for Cancer Research.)

Published
2021
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