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Thursday, 10/27/2022 1:54:01 AM

Thursday, October 27, 2022 1:54:01 AM

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ESSA PHARMA INC - EPI-8207 SHOWS ROBUST POTENCY DEGRADING AR, INCLUDING AR SPLICE VARIANTS AND CLINICALLY RELEVANT AR MUTANTS

About ANITAC™ Degraders Androgen receptor signaling is the main driver of prostate cancer progression and remains a crucial target for therapeutic intervention in late stages of the disease. While current antiandrogen therapies that directly or indirectly target the AR ligand-binding domain (LBD) are initially effective, resistance ultimately develops and new methods of inhibiting the AR pathway are needed.

ESSA's novel approach of targeting the N-terminal domain of the AR represents a new method of blocking AR signaling. Leveraging ESSA's scientific foundation in successfully targeting the NTD of the AR with a new class of small molecules called anitens, ESSA is developing the first generation of ANITen bAsed Chimera degraders targeting the AR NTD. In preclinical models, the orally bioavailable ANITAC degraders can eliminate forms of AR protein found in castration-resistant prostate cancer that can potentially drive disease progression including LBD mutants and LBD truncated splice variants.
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