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AC0176 is an investigational, orally bioavailable small molecule chimeric degrader of the androgen receptor (AR), developed for the potential treatment of prostate cancers, particularly metastatic castration-resistant prostate cancer (mCRPC). It functions as a proteolysis-targeting chimera (PROTAC), selectively binding to and degrading both wildtype and mutant forms of AR—including mutations such as L702H, T878A, H875Y, and W742C—that are implicated in resistance to current AR-targeted therapies. By promoting degradation of AR protein rather than merely inhibiting its activity, AC0176 aims to block AR-mediated signaling pathways critical for tumor cell proliferation. Preclinical studies have demonstrated potent and selective AR degradation with promising anti-tumor activity. The drug is currently in Phase 1 clinical trials and has received Fast Track designation from the FDA for mCRPC patients who have progressed on or after androgen receptor signaling inhibitors[2][3][4][5][6][7][8].
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