On June 25, 2019 Arvinas, Inc. (Nasdaq: ARVN), a biotechnology company creating a new class of drugs based on targeted protein degradation, reported that the U.S. Food and Drug Administration (FDA) has cleared the company’s Investigational New Drug application (IND) for ARV-471, an oral estrogen receptor (ER) PROTAC protein degrader, designed to selectively target ER for the treatment of patients with locally advanced or metastatic ER positive / HER2 negative breast cancer (Press release, Arvinas, JUN 25, 2019, View Source [SID1234537248]). Arvinas expects to initiate a Phase 1 clinical trial for ARV-471 in the third quarter of 2019.
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"ARV-471 is our second program in six months to receive IND clearance, and we are pleased to be advancing it into the clinic and progressing Arvinas’ portfolio of PROTAC protein degraders for the treatment of patients with cancer and other life-threatening diseases," said John Houston, Ph.D., President and CEO of Arvinas. "We hope the activity ARV-471 demonstrated preclinically will translate into a new, beneficial treatment for patients with locally advanced or metastatic ER positive/HER2 negative breast cancer."
In the United States, breast cancer is the second most common cancer and the second leading cause of cancer death in women. The American Cancer Society estimates that in 2019, there will be approximately 268,000 women diagnosed with invasive breast cancer in the United States. Metastatic breast cancer accounts for approximately 6% of newly diagnosed cases. Approximately 80% of newly diagnosed breast cancers are ER positive, with many patients developing resistance to current treatment options over time.
ARV-471 is a PROTAC protein degrader specifically designed to target and degrade ER. The Phase 1 trial will assess the safety, tolerability, and pharmacokinetics of ARV-471, and will also include measures of anti-tumor activity and pharmacodynamic readouts as secondary endpoints.
In preclinical studies, ARV-471 demonstrated near-complete ER degradation in tumor cells, induced robust tumor shrinkage when dosed as a single agent in multiple ER-driven xenograft models, and showed superior anti-tumor activity as a single agent and in combination with a CDK4/6 inhibitor when compared to a standard of care agent, fulvestrant, dosed as single agent or in combination with a CDK4/6 inhibitor. Arvinas believes the differentiated pharmacology of ARV-471, including its iterative degradation activity, has the potential to translate into meaningful clinical benefit for patients.