The poster titled, "An oral androgen receptor PROTAC degrader for prostate cancer" (abstract 179448) presents data from in vitro and in vivo studies of prostate cancer cell lines treated with a small molecule AR PROTAC that simultaneously binds E3-ubiquitin ligase and AR. The results show robust and durable degradation of all clinically relevant mutant AR proteins, including 92-98% degradation of total AR across all cell lines, suppression of prostate-specific antigen gene expression, inhibition of cell proliferation and the inducing of apoptosis of prostate cancer cell lines.
Regulating the androgen receptor signaling is an important factor in controlling progression in prostate cancer, but currently, standard of care androgen receptor inhibitors like enzalumtamide (Xtandi®) have shown limited efficacy because increased androgen production, increased expression of the androgen receptor and specific mutations of the receptor can overcome inhibition. Arvinas' approach focuses on degrading the androgen receptor, resulting in its elimination. In contrast to traditional target inhibition, which is a competitive process, degradation is progressive and therefore less susceptible to increases in endogenous ligand, target expression, or mutations in the target.
Abstracts 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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