Arvinas Presents Preclinical Data on Protein Degrader, ARV-471, at the 2018 San Antonio Breast Cancer Symposium (SABCS)
“We believe that ARV-471 has the potential to be the first oral protein degrader for the treatment of patients with metastatic ER-positive/HER2-negative breast cancer, when used either as a single-agent or in combination with other routinely used anti-cancer agents,” said
Key highlights from the poster "ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer”:
- Orally bioavailable ARV-471 demonstrated potent ERa degradation in wild-type and mutant ERa-expressing cell lines.
- Oral administration of ARV-471 caused near-complete ERa degradation and resulted in tumor shrinkage in an orthotopic MCF7/estradiol breast cancer preclinical model; ARV-471 demonstrated superior tumor growth inhibition and ERa degradation compared to standard-of-care agent, fulvestrant.
- Combination of ARV-471 and a CDK4/6 inhibitor demonstrated superior tumor growth inhibition when compared to the combination of fulvestrant and a CDK4/6 inhibitor.
- ARV-471 inhibited growth of tamoxifen-resistant and ERa gene (ESR1) mutant tumors while also reducing tumor ERa levels.
- ARV-471 displayed no ER agonist activity.
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Source: Arvinas Inc.