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HLD-0915 is an orally bioavailable, heterobifunctional small molecule developed using the Regulated Induced Proximity Targeting Chimera (RIPTAC™) platform. It is designed to treat metastatic castration-resistant prostate cancer (mCRPC) by leveraging the expression of the full-length Androgen Receptor (AR) in tumor cells. The molecule functions via a "hold and kill" mechanism, where it induces the formation of a stable trimeric complex between the AR and an essential protein (EP) required for cell survival. This interaction leads to the loss of function of the essential protein specifically within AR-expressing cancer cells, resulting in selective apoptosis and tumor regression. HLD-0915 is intended to overcome resistance to traditional androgen receptor pathway inhibitors (ARPIs) and other standard-of-care therapies, as its activity depends on the presence of the AR protein rather than its signaling activity.
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