NEW HAVEN, Conn., Dec. 8, 2017 /PRNewswire/ -- Arvinas LLC, a private biotechnology company creating a new class of small molecule drugs based on protein degradation, today announced the presentation of new preclinical data for its novel oral estrogen receptor (ER) alpha PROTAC program during a poster session at the 2017 San Antonio Breast Cancer Symposium (SABCS), taking place from December 5-9 in San Antonio, Texas.
"The data presented today continues to support our confidence in PROTACs as a new class of therapeutic modalities. Our orally administered estrogen receptor PROTACs demonstrate superior efficacy in preclinical models compared to standard of care fulvestrant as a single agent and in combination with a CDK4/6 inhibitor," said John Houston, Ph.D., President and Chief Executive Officer of Arvinas. "We believe selective, PROTAC-mediated degradation of the estrogen receptor protein to be an attractive potential treatment option for patients with breast cancer, and will continue to advance this program to determine its full potential."
Details of the Poster Presentation:
Title: Identification of oral estrogen receptor PROTAC degraders for breast cancer
Date & Time: Friday, December 8, 2017 from 7:00 – 9:00 a.m. CT
Presenter: John J. Flanagan,PhD
Poster Number: P4-04-04
The poster contains data from in vitro and in vivo studies using model breast cancer cell lines showing robust degradation of estrogen receptor alpha and significant tumor growth inhibition with ER PROTACs.
Highlights from the poster presentation include:
- Orally bioavailable ER PROTACs demonstrate nanomolar ERa degradation potency and growth inhibition in a variety of wild-type ERa-expressing cell lines
- ER PROTACs degrade and inhibit growth of cells expressing clinically-relevant ERa variants, suggesting that ER PROTACs will be active in that resistance setting
- Oral administration of ER PROTACs provides more robust tumor growth inhibition and ERa degradation compared to fulvestrant in an orthotopic MCF7 xenograft model
- Combination of ER PROTACs and a CDK4/6 inhibitor demonstrated superior tumor growth inhibition when compared to the combination of fulvestrant and a CDK4/6 inhibitor
All recent presentations are available on the Arvinas website under Publications at www.arvinas.com.
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, via 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.