Tag Archive for: protac

UPDATE: Bavdegalutamide Shows Stronger Activity in Prostate Cancers With Specific AR Mutations

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New phase 1/2 results published in the Journal of Clinical Oncology provide further evidence of the clinical activity of bavdegalutamide (ARV-110), an experimental androgen receptor (AR) degrader, in patients with metastatic castration-resistant prostate cancer (mCRPC). The findings suggest that specific AR mutations may help identify patients most likely to benefit from this treatment. Unlike conventional […]

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GX-BP1: Targeting SOX2 to Prevent Resistance in mCRPC

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GX-BP1, a bioPROTAC-based SOX2 degrader, selectively targets SOX2, an undruggable protein, for ubiquitin-proteasome elimination, overcoming limitations of prior inhibition strategies. In preclinical models, GX-BP1 monotherapy delivered approximately 70% tumor growth inhibition, while combinations with agents like carboplatin/paclitaxel achieved 87-96% inhibition and near-complete tumor suppression at optimal doses. Notably, GX-BP1 paired with osimertinib eradicated cancer stem […]

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A nano-PROTAC on the horizon: combining targeted protein degradation and ferroptosis for advanced prostate cancer

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A new study from Wuhan University and the Renmin Hospital of Wuhan University has reported a promising preclinical strategy for advanced prostate cancer, especially castration-resistant prostate cancer (CRPC). The work was published online in Angewandte Chemie International Edition, one of the leading international journals in chemistry. The study describes a new nano-PROTAC platform designed to […]

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GLR2037: A First‑in‑Human AR‑Targeted PROTAC Enters Phase 1 Trials in Advanced Prostate Cancer

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A new investigational agent code‑named GLR2037 has entered early clinical development as a first‑in‑human phase 1 study in patients with advanced prostate cancer, representing a significant step in the evolution of androgen receptor–directed therapies. GLR2037 is an androgen receptor (AR)–targeting proteolysis‑targeting chimera (PROTAC), designed not merely to inhibit the AR but to promote its ubiquitin‑proteasome–mediated […]

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ANDROMEDA: Phase 1/2 Trial of AZD9750 AR Degrader in Metastatic Prostate Cancer

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The ANDROMEDA trial, a first-in-human Phase 1/2 study, is evaluating AZD9750, a novel androgen receptor (AR) PROTAC, in men with metastatic castration-resistant prostate cancer (mCRPC). PROTACs represent a paradigm shift in targeted therapy: unlike traditional AR inhibitors that merely block the receptor’s activity, AZD9750 recruits cellular machinery to completely degrade the AR protein, potentially overcoming […]

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Self-Assembled Nano-PROTAC to Improve Targeted Therapy in Castration-Resistant Prostate Cancer

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A new study published in Nature Signal Transduction and Targeted Therapy reports a major leap in the design of targeted cancer therapies through the development of an in vivo self-assembled nano-PROTAC (proteolysis targeting chimera) system capable of delivering dual-targeted degradation in castration-resistant prostate cancer (CRPC).​ PROTACs have reshaped the drug discovery landscape by inducing selective […]

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Update: HLD-0915 Advances with FDA Fast Track Designation for Metastatic Castration-Resistant Prostate Cancer

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