ARV-110 Demonstrates Efficacy and Plasma PSA Reduction in an Enzalutamide-Insensitive PDX Model ARV-110 is showing early clinical benefit in highly refractory patients

2019年2月26日 · Methods: Here we report an orally bioavailable small molecule AR PROTAC degrader, ARV-110, that promotes ubiquitination and degradation of AR. This molecule has been characterized in in vitro degradation and functional assays, and DMPK, toxicology and preclinical efficacy studies.

Conclusions: ARV-110, a novel AR protein degrader, demonstrates clinical activity in a post-NHA, heavily pretreated mCRPC pt population, with greatest PSA 50 activity and RECIST responses in pts with AR T878 and/or H875 mutations, likely representing a particularly ARV …

About Bavdegalutamide (ARV-110) Bavdegalutamide is an investigational orally bioavailable PROTAC® protein degrader designed to selectively target and degrade the androgen receptor (AR). Bavdegalutamide is being developed as a potential treatment for men with metastatic castration-resistant prostate cancer.

2025年1月14日 · Bavdegalutamide (ARV-110) is a PROteolysis TArgeting Chimera (PROTAC) protein degrader that recruits the cereblon-containing E3 ubiquitin ligase to direct the polyubiquitination and subsequent proteasomal degradation of AR.

2025年1月1日 · ARV-110 has shown its ability to induce degradation of the AR in prostate cancer−associated cell lines such as LNCaP and VCaP cells, with a half-maximal degradation concentration (DC 50) of 1 nM. Proteomic screening analysis revealed that treatment with ARV-110 at a concentration of 10 nM selectively degraded up to 85% of AR in VCaP cells.

2020年5月25日 · ARV-110 is an orally bioavailable PROTAC that specifically degrades AR ≥ 95% and achieves anti-tumor activity in ENZ-naïve and -resistant prostate cancer xenograft models.

ARV-110 is a first-in-class, oral PROteolysis TArgeting Chimera (PROTAC) protein degrader that selectively targets the androgen receptor and, in phase 1 trials, has demonstrated clinical activity in patients with mCRPC who have been heavily pre-treated.

2018年7月1日 · Here we report an orally bioavailable small molecule ARV-110 that leads to ubiquitination and degradation of AR. ARV-110 completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC 50) < 1 nM.