Table 1

Clinical trials designed to investigate PROTAC AR degraders for the treatment of advanced prostate cancer

Drug nameClinical trial identifierLocationDisease settingPhaseStatusEfficacy resultsa
Bavdegalutamide (ARV-110)NCT03888612USmCRPCPhase 1/2Primary stage completed; study ongoing
  • 46% PSA50 rate and RECIST responses occurred in patients with tumors harboring AR T878X or H875Y mutations.

  • A ≥ 50% decrease in PSA occurred in patients without AR T878X/H875Y mutations6.

ARV-766NCT05067140USmPCPhase 1/2Ongoing50% PSA50 rate in patients with AR LBD mutations7.
HP518NCT06155084ChinamCRPCPhase 1Ongoing
NCT05252364AustraliamCRPCPhase 1Complete
AC176NCT05673109ChinamCRPCPhase 1Terminated
NCT05241613USmCRPCPhase 1Terminated
  • aListed for phase ≥2 trials for which data are available. AR, androgen receptor; LBD, ligand-binding domain; mCRPC, metastatic castration-resistant prostate cancer; PROTAC, PROteolysis TArgeting Chimera; RECIST, response evaluation criteria in solid tumors; PSA, prostate-specific antigen.