Feb 26, 2019 · ARV-110 treatment leads to highly selective AR degradation, as demonstrated by proteomic studies. In VCaP cells, PROTAC-mediated AR degradation suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.

Apr 2, 2025 · 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.

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 …

May 25, 2020 · 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, a novel proteolysis-targeting chimera (PROTAC), has been reported to show satisfactory safety and tolerability for prostate cancer therapy in phase I clinical trials. However, there is a lack of bioanalytical assays for ARV-110 determination in biological samples.

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

Bavdegalutamide, also called ARV-110, is a drug that is being evaluated as a treatment for metastatic prostate cancer. It is a PROteolysis TArgeting Chimera (PROTAC) androgen receptor degrader • PROTAC protein degraders are designed to …

Jul 1, 2021 · ARV-110 potently downregulates androgen responsive genes, inhibits proliferation and induces apoptosis in AR dependent prostate cancer cells. In vivo, ARV-110 is orally bioavailable and robustly degrades AR with a >90% observed maximum degradation (Dmax) at efficacious doses.

Jul 1, 2018 · 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.

Jan 1, 2025 · 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. Compared with enzalutamide, ARV-110 demonstrated stronger inhibitory effects …