Androgen Receptor-targeting Regulated Induced Proximity Targeting Chimera HLD-0915

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable bifunctional small molecule composed of an androgen receptor (AR)-binding moiety that is conjugated, via a linker, to a bromodomain-containing protein 4 (BRD4)-binding moiety, with potential antineoplastic activity. Upon oral administration of AR-targeting regulated induced proximity targeting chimera (RIPTAC) HLD-0915, the AR-binding moiety targets and binds to the AR expressed on tumor cells, and the BRD4-binding moiety targets and binds to BRD4. This inhibits BRD4 activity and cell growth in AR-expressing tumor cells. AR is overexpressed in prostate cancers and is involved in the proliferation, survival and chemoresistance of tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation.

**Synonyms:** - AR-targeting RIPTAC HLD-0915 - HLD 0915 - HLD-0915 - HLD0915