molecules of the month


oral AR-degrading PROTAC

Ph. II for adv. prostate cancer

from CRBN-based E3 recruiter + AR ligand

AACR, April 2023

Arvinas, New Haven, CT

ARV-776, AR, oral AR-degrading PROTAC, Ph. II for adv. prostate cancer, from CRBN-based E3 recruiter + AR ligand, AACR, April 2023, ARVINAS, NEW HAVEN, CT
6 mins read

A second-generation AR bifunctional degrader for drug-resistant prostate cancer. ARV-766 is Arvinas’ second bifunctional CRL4CRBN E3 ligase-based androgen receptor (AR) degrader to enter the clinic for the treatment of prostate cancer (PCa), after ARV-110 (bavdegalutamide). The glutarimide recruiting element is notable as it is simpler than other phthalidomide-based E3 ligands, and the aryloxy tetramethylcyclobutane moiety appears to be derived from a Pfizer ligand and engages the AR ligand binding domain (LBD), leading to proteasome-dependent AR degradation via the ubiquitin-proteosome system. On Jun. 8th, 2023, Arvinas released interim data from its Ph. I/II trial showing that the drug was well-tolerated, with 42% of patients with ligand-binding domain (LBD) mutations showing a significant response as measured by PSA50. The androgen receptor in…

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