Drug intelligence / Profile preview

AC0176

Development stage
Discontinued
Lead developer
Accutar Biotechnology
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

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].

Other names
androgen receptor degrader ac176
02

Targets

AR (Adrenergic receptors)E3 ligase (E3 ubiquitin ligases)

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