2024
ARV-766, a proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC): Initial results of a phase 1/2 study.
Petrylak D, McKean M, Lang J, Gao X, Dreicer R, Geynisman D, Stewart T, Gandhi M, Appleman L, Dorff T, Chatta G, Tutrone R, De La Cerda J, Berghorn E, Gong J, Yu T, Dominy E, Chan E, Shore N. ARV-766, a proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC): Initial results of a phase 1/2 study. Journal Of Clinical Oncology 2024, 42: 5011-5011. DOI: 10.1200/jco.2024.42.16_suppl.5011.Peer-Reviewed Original ResearchMetastatic castration-resistant prostate cancerTreatment-related adverse eventsAR-LBD mutationsPhase 1/2 studyClinical activityProstate cancerAndrogen receptorAdverse eventsMetastatic castration-resistant prostate cancer treatmentProgressive metastatic castration-resistant prostate cancerPhase 1 dose-escalation portionDisease progressionTreatment-emergent adverse eventsCastration-resistant prostate cancerResistant to available therapiesAssociated with poor outcomesDose-limiting toxicityAndrogen deprivation therapyAdvanced prostate cancerIncreased blood creatinineWild-type ARSubgroup of patientsDose-dependent increaseDeprivation therapyPretreated patients
2023
A phase 2 expansion study of ARV-766, a PROTAC androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC).
Petrylak D, Stewart T, Gao X, Berghorn E, Lu H, Chan E, Gedrich R, Lang J, McKean M. A phase 2 expansion study of ARV-766, a PROTAC androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC). Journal Of Clinical Oncology 2023, 41: tps290-tps290. DOI: 10.1200/jco.2023.41.6_suppl.tps290.Peer-Reviewed Original ResearchMetastatic castration-resistant prostate cancerNovel hormonal agentsCohort expansionDisease progressionEastern Cooperative Oncology Group performance status scoreOngoing androgen deprivation therapyProstate-specific antigen (PSA) declineCastration-resistant prostate cancerGonadotropin-releasing hormone analogueCohort expansion studyAndrogen deprivation therapyPerformance status scoreOverall response ratePhase 1 portionWild-type ARDeprivation therapyPrior chemotherapyCurative optionDose escalationAvailable therapiesHormonal agentsStatus scoreCurrent therapiesLigand-binding domainClinical trials
2022
Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC).
Gao X, Burris H, Vuky J, Dreicer R, Sartor A, Sternberg C, Percent I, Hussain M, Kalebasty A, Shen J, Heath E, Abesada-Terk G, Gandhi S, McKean M, Lu H, Berghorn E, Gedrich R, Chirnomas S, Vogelzang N, Petrylak D. Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC). Journal Of Clinical Oncology 2022, 40: 17-17. DOI: 10.1200/jco.2022.40.6_suppl.017.Peer-Reviewed Original ResearchMetastatic castration-resistant prostate cancerNovel hormonal agentsProstate-specific antigenClinical activityBetter prostate-specific antigenOngoing phase 1/2 studyCastration-resistant prostate cancerBiomarker-defined subgroupsPhase 2 dosePhase 1/2 studyWild-type ARFourth subgroupPhase 1AR alterationsRECIST responseSpecific molecular profilePrior therapyAdverse eventsAR-V7Tumor shrinkageHormonal agentsTreatment optionsClinical historyDisease progressionProstate cancer