Masofaniten targets CRPCa using a novel targeting strategy binding to the AR N-terminus. Hopefully this will get around some mechanisms of castration resistance, since hormonal agents (Enza, Appa, Daro) target the AR LBD (Ligand Binding Domain) and eventually AR mutations bypass the LBD for activation rendering the hormonal agents ineffective.
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Another Drug to watch that targets the N-terminus is ARV-766, an AR degrader, that causes the complete breakdown of the AR.
Novel AR-Targeted Therapies for mHSPC: Which One to Choose
Second generation androgen receptor antagonists and challenges in prostate cancer treatment
New randomized clinical trial of Lu-177-PSMA-617 for men who are still hormone sensitive
