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DRUG:

HLD-0915

i
Other names: HLD-0915, H001, AR RIPTAC, HLD0915, HLD 0915
Associations
Trials
Company:
Halda Therap
Drug class:
Androgen receptor modulator, Essential cellular protein inhibitor
Associations
Trials
over1year
Prostate cancer RIPTAC™ therapeutics demonstrate activity in preclinical models of Enzalutamide-resistant prostate cancer (AACR 2023)
RIPTACs were optimized for oral bioavailability, and tumor ternary complex formation in prostate cancer cell line-derived xenograft models. RIPTAC therapeutics display nanomolar in vitro potency in AR:RIPTAC:EP ternary complex formation, which results in abrogation of the EP function and antiproliferative activity in prostate cancer cell lines, but not in AR-knockout control cells. Taken together, our in vitro mechanistic data and in vivo PD/efficacy observations in multiple prostate cancer models support further investigation of prostate cancer RIPTAC therapeutics as a novel heterobifunctional therapeutic modality in mCRPC.
Preclinical
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AR (Androgen receptor) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
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AR mutation • AR amplification
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Xtandi (enzalutamide capsule) • HLD-0915