Oral ARV-110 Shows Promise in Heavily Treated mCRPC Patients

Oral ARV-110 Shows Promise in Heavily Treated mCRPC Patients
ARV-110, an investigational oral therapy that degrades the androgen receptor, has a favorable safety profile and showed promising anti-tumor activity in heavily pretreated men with metastatic castration-resistant prostate cancer (mCRPC), updated Phase 1 data suggests. The approach worked particularly well in a population with specific mutations in the androgen receptor, the researchers said. But it also was found to have promising efficacy in a group of patients without genetic alterations in the receptor. Arvinas, its maker, is therefore advancing the development of ARV-110 for these two indications. “It is exciting to see that ARV-110 continues to be active and well tolerated in what we believe is the most heavily pretreated patient population that has ever been studied with an [androgen receptor]-directed therapy,” Ron Peck, PhD, chief medical officer at Arvinas, said in a press release. While medicines that target the androgen receptor — such as  Zytiga and Xtandi — are a mainstay for the treatment of advanced prostate cancer, tumors often develop a resistance to such treatments and continue to grow. One of the mechanisms linked with resistance is the production of a variant of the androgen receptor, called AR-V7, that is able to escape the action of androgen receptor inhibitors. In other cases, cancer cells overproduce the androgen receptor. ARV-110 is a potential oral candidate that targets the androgen receptor — a nuclear receptor that regulates the development and growth of the prostate — for degradation. The medicine, developed using Arvinas' PROTAC protein degradation platform, delivers small tags to the androgen receptor, triggering its destruction by the cells’ natural protein degrading system. An ongoing Phase 1 tria
Subscribe or to access all post and page content.