Arvinas Presents Data On Oral Estrogen Receptor PROTAC Degrader At 2016 San Antonio Breast Cancer Symposium
NEW HAVEN, Conn., Dec. 9, 2016 /PRNewswire/ -- Arvinas LLC, a private biotechnology company creating a new class of drugs known as PROTACs, which function via targeted protein degradation, today announced that data were presented during an oral presentation at the 2016 San Antonio Breast Cancer Symposium highlighting the potential of its oral estrogen receptor alpha (ERa) PROTAC in reducing ERa levels in preclinical breast cancer models. The ERa protein is a key driver in hormone receptor-positive breast cancers.
"Orally administered PROTACs are an important evolution in the development of our technology, and through this study we were able to demonstrate the successful targeting and degradation of ERa by an oral PROTAC in a preclinical model of breast cancer," said Manuel Litchman, M.D., president and CEO of Arvinas. "Estrogen receptor-driven breast cancer remains a key unmet need in women's health, and we believe selective degradation of the estrogen receptor protein to be an attractive potential treatment option for patients. We will continue to evaluate our oral estrogen receptor PROTACs in a variety of anti-endocrine resistant breast cancer models."
The data were highlighted by Dr. John Flanagan, senior research investigator for Arvinas, during an oral presentation titled, "Targeted and selective degradation of estrogen receptor (ER) alpha by PROTACs,"as part of the General Session 4.
Highlights from the data presentation show:
- Oral administration of an ERa PROTAC reduces ERa levels in MCF7 xenografts and in immature rat uteri.
- Robust and selective degradation of ERa in several human breast cancer cell lines
- Significant tumor growth inhibition and ERa degradation by an ER alpha PROTAC in an MCF7 xenograft model
Additional data demonstrating preclinical efficacy improvements and clear differential biology of PROTACs compared to traditional inhibitors in other cancers were recently presented at the 28th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium and the 2016 American Society of Hematology Annual Meeting.
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. Based on groundbreaking research conducted at Yale University by Founder and Chief Scientific Advisor, Dr. Craig Crews, the company is translating innovative protein degradation approaches into novel drugs for the treatment of cancer and other diseases. The company's new PROTAC-based drug paradigm induces protein degradation, rather than protein inhibition, 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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