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Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127

Covalent Modifiers

Covalent and noncovalent inhibitors of BTK have revolutionized the treatment of these cancers. We therefore set out to understand the nonenzymatic functions of BTK and explored targeted protein degradation to overcome the oncogenic scaffold function of mutant BTK.

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ARVINAS AND PFIZER ANNOUNCE GLOBAL COLLABORATION TO DEVELOP AND COMMERCIALIZE PROTAC® PROTEIN DEGRADER ARV-471

The Pharma Data

NYSE: PFE) today announced a global collaboration to develop and commercialize ARV-471, an investigational oral PROTAC® (PROteolysis TArgeting Chimera) estrogen receptor protein degrader. Despite advancements in oncology in recent years, considerable unmet need persists in the treatment of HR+ breast cancer.

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Arvinas, Inc. Announces Pricing of $400 Million Public Offering of Common Stock

The Pharma Data

Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation using its PROTAC ® Discovery Engine, today announced the pricing of an underwritten public offering of 5,714,286 shares of its common stock at a price of $70.00 NEW HAVEN, Conn., Forward-Looking Statements.

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How to Get Drugs Into the Brain

Drug Hunter

Overall, only a few prodrugs for CNS disorders have even reached clinical trials , so for the most part traditional property-based drug design remains the best bet for the vast majority of programs. Figure 19: Compound 7 is highly effective in a mouse model of HAT infection, leading to cures after six days of treatment. Figure 18.

Drugs 206