ARV-378 is an orally bioavailable small molecule PROTAC designed to target and induce the degradation of the estrogen receptor protein, which plays a prominent role in the development of ER positive breast cancer.
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| [20-December-2017] |
| NEW HAVEN, Conn., Dec. 20, 2017 /PRNewswire/ -- Arvinas, a private biotechnology company creating a new class of small molecule drugs based on protein degradation, today announced the selection of its second candidate for clinical development as a novel treatment for metastatic breast cancer. ARV-378 is an orally bioavailable small molecule PROTAC (PROteolysis TArgeting Chimera) designed to target and induce the degradation of the estrogen receptor (ER) protein, which plays a prominent role in the development of ER positive breast cancer. In November, Arvinas nominated its first clinical candidate, ARV-110, designed to target and induce degradation of the androgen receptor protein. “Approximately 75% of all breast cancers are driven by overexpression of the estrogen receptor protein, making it an attractive target for degradation using our novel therapeutic modality. ARV-378 is an oral, potent selective estrogen receptor degrader that demonstrated superior efficacy in preclinical models as a stand-alone agent and in combination with standard of care,” said John Houston, Ph.D., President and Chief Executive Officer of Arvinas. “With the first two clinical candidates nominated from our protein degradation platform, we will now focus on moving both into the clinic while continuing to expand our discovery pipeline.” ARV-378 works by hijacking the cancer cell’s natural and selective process for controlling protein levels to efficiently target estrogen receptor proteins for degradation and elimination. In contrast to the traditional competitive process of target inhibition, degradation by PROTACs is iterative and can overcome increases in endogenous ligand and target expression, or mutations in the target. About Arvinas Arvinas is a pharmaceutical company focused on developing new small molecules ? known as PROTACs (PROteolysis TArgeting Chimeras) ? aimed at degrading disease-causing cellular proteins via proteolysis. Based on innovative research conducted at Yale University by Dr. Craig Crews, Founder and Chief Scientific Advisor, the company is translating natural protein degradation approaches into novel drugs for the treatment of cancer and other diseases. The proprietary PROTAC-based drug paradigm induces protein degradation, rather than protein inhibition, facilitating the ubiquitin proteasome system and offers the advantage of potentially targeting “undruggable” as well as “druggable” elements of the proteome. This greatly expands the ability to create drugs for many new, previously unapproachable targets. For more information, visit www.arvinas.com.
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