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A few days ago, Arvinas and Pfizer jointly announced that the latest phase 1 clinical results of the jointly developed PROTAC protein degradation therapy ARV-471 will be presented at the San Antonio Breast Cancer Symposium (SABCS) in early December
One end of the PROTAC molecule can bind to the target protein, and the other end can recruit E3 ubiquitin ligase to label the target protein with a ubiquitin "tag" and promote their degradation by the proteasome
ARV-471 is a potential "best-in-class" protein degrader
As of June 6 this year, 50 previously treated breast cancer patients were treated with different doses of ARV-471, up to 700 mg, according to the SABCS abstract
Tissue biopsy analysis showed that ARV-471 reduced ER levels by up to 90% regardless of whether tumors expressed wild-type ER or mutant ER
Among 34 patients who could be assessed for clinical benefit (including confirmed complete response, partial response, or stable disease for more than 24 weeks), the clinical benefit rate was 41%
Of the 28 patients with measurable disease at baseline, two had confirmed partial responses
ARV-471 is currently being tested in Phase 2 clinical trials at doses of 200 mg or 500 mg daily
References:
[1] Arvinas and Pfizer Announce Updated Phase 1 Dose Escalation Data for ARV-471 to be Presented in Spotlight November Poster Session at 2021 San Antonio Breast Cancer Symposium.
