Technology Overview
Mechanism of proteolysis targeting chimera (PROTAC) technology.
Castration-resistant prostate cancer (CRPC) is an advanced and incurable stage of prostate cancer. Although anti-androgen therapies are the mainstay of treatment for CRPC, around 60% of patients develop drug resistance. ITRI-148, a novel AR-NTD protein degrader, is developed to overcome anti-androgen drug resistance issue through efficient degradation of AR and AR-V7. It shows superior efficacy compared to current drug Enzalutamide and competitor compound ARV-110 in preclinical models of CRPC.
Features & Specifications
- Orally bioavailable AR/AR-V7 PROTAC overcome CRPC drug-resistant, high potent and well-tolerated.
- Superior to current drug Enzalutamide (FDA approved) and competitor EPI-7386.
- Potential to address unmet need.
Applications & Benefits
Current drug development in CRPC, AR-PROTAC drug is targeting to AR-LBD domain not for AR-V7 resistance target, expected that limited efficacy for advanced CRPC. ITRI-PROTAC drug (AR/AR-V7) with a decent oral availability and a strong antitumor efficacy in a therapy-resistant prostate cancer model. Without hormone ablation, single use of ITRI PROTAC is sufficient to greatly impair tumor growth. Compensatory hormone synthesis in the tumor niche occurs after standard hormone therapy and restrains the efficacy of androgen antagonist drugs. The patent application process has been completed. Meanwhile, we collaborate with pharmaceutical companies and startups to accelerate protein degradation research and enhance Taiwan’s international visibility in the rug development field.
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