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NEW HAVEN, Conn., November 2, 2017 – Arvinas LLC, a private biotechnology company creating a new class of small molecule drugs based on protein degradation, today announced the selection of its first candidate for clinical development as a novel treatment for metastatic castration-resistant prostate cancer (mCRPC). ARV-110 is an orally bioavailable small molecule PROTAC (PROteolysis TArgeting Chimera) designed to target and induce the degradation of the androgen receptor (AR) protein, which plays a prominent role in the development of mCRPC.
“We believe that our first clinical candidate from our protein degradation platform will offer a novel therapeutic modality to patients with mCRPC. ARV-110 is an oral, potent androgen receptor degrader that demonstrated efficacy in preclinical models in settings where standard of care therapies are ineffective, specifically, when the androgen receptor is overexpressed, mutated, or in high androgen ligand concentration environments,” said John Houston, Ph.D., President and Chief Executive Officer of Arvinas. “Having met customary criteria for preclinical efficacy and safety, we are on track to initiate a clinical study of the AR PROTAC in mCRPC patients in the second half of 2018.”
ARV-110 works by hijacking the cancer cell’s natural and selective process for controlling protein levels to efficiently target androgen 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.
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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