平特五不中

Invention 15041

Development of pan-inhibitors for castration-resistant prostate cancer treatment

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A group of inhibitors that target a unique domain for advanced prostate cancer treatment has been identified at 平特五不中.

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Market Need

For advanced stages of prostate cancer, the current treatment strategy is to suppress the level of androgens by castration and antiandrogens. This often leads to an initial positive response, but in some cases androgen receptor (AR) reactivation results in lethal castration-resistant prostate cancer (CRPC). There are two FDA approved drugs for CRPC, but drug resistance to these agents has already developed in the clinics. As reported in a series of studies, the loss of the ligand-binding domain (LBD) is a major mechanism responsible for the development of resistance to AR-focused therapies. As the antiandrogens currently used in clinics target the LBD, these mutations are therefore resistant to all treatments that are in use.

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Technology Summary

This technology is a group of novel androgen receptor inhibitors that target a different domain than current methods. Specifically, these compounds target the N-terminal domain of androgen receptors instead of the ligand binding domain. In vivo, these inhibitors have demonstrated excellent efficacy in TRAMP-C1 and 22Rv1 prostate tumor models in mice. As all of the known mechanisms that reactivate androgen receptors in CRPC depend on the N-terminal domain, these drugs provide an alternative mechanism of treatment for patients who have acquired resistance to LBD domain therapies.

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Advantages

• Acts as a pan-inhibitor of all clinically relevant mutants of androgen receptors
• In vivo experiments revealed the compounds suppressed tumor growth in mouse models
• Targets a unique domain compared to other prostate cancer treatments

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Patent Status

Filed EP, US, CA

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