2023
An oral androgen receptor RIPTAC for prostate cancer.
Raina K, Eastman K, Yu X, Forbes C, Jones K, Mousseau J, Li H, Kayser-Bricker K, Crews C. An oral androgen receptor RIPTAC for prostate cancer. Journal Of Clinical Oncology 2023, 41: 184-184. DOI: 10.1200/jco.2023.41.6_suppl.184.Peer-Reviewed Original ResearchPCa cell linesAR expressionProstate cancerAR-positive cellsCastration-resistant settingLow oral doseProstate cancer modelTumor growth inhibitionProstate cancer cellsCell linesEfficacious exposureVCaP xenograftsOral dosePreclinical dataOral dosingLow nM concentrationsTumor-specific inhibitionCancer modelPharmacokinetic propertiesNormal tissuesOral bioavailabilitySignaling InhibitorsToxicology studiesAR geneCancer cells
2019
ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Snyder L, Willard R, Vitale N, Pizzano J, Gordon D, Bookbinder M, Macaluso J, Dong H, Ferraro C, Wang G, Wang J, Crews C, Houston J, Crew A, Taylor I. ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2019, 37: 259-259. DOI: 10.1200/jco.2019.37.7_suppl.259.Peer-Reviewed Original ResearchAndrogen receptorAR degradationProstate cancerAR proteinAR target gene PSADegradation of ARCastration-resistant prostate cancerAR target gene expressionIND-enabling studiesMajority of patientsProstate cancer patientsMouse xenograft studiesPreclinical efficacy studiesProstate cancer modelMutant AR proteinAndrogen environmentMetastatic diseaseMost patientsAR signalingCancer patientsPreclinical dataAR pathwayMechanisms of resistanceLow nanomolar concentrationsFIH studies
2018
An oral androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Snyder L, Willard R, Vitale N, Raina K, Pizzano J, Gordon D, Bookbinder M, Macaluso J, Dong H, Liu Z, Ferraro C, Wang G, Wang J, Crews C, Houston J, Crew A, Taylor I. An oral androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2018, 36: 381-381. DOI: 10.1200/jco.2018.36.6_suppl.381.Peer-Reviewed Original ResearchAndrogen receptorProstate cancerAR proteinAR target gene PSADegradation of AREnzalutamide-Resistant Prostate CancerCastration-resistant prostate cancerAR degradationMajority of patientsMouse xenograft studiesPreclinical efficacy studiesMutant AR proteinNon-rodent speciesAndrogen environmentMetastatic diseaseMost patientsAR signalingPreclinical dataAR pathwayMechanisms of resistanceDrug exposureXenograft studiesVCaP cellsEfficacy studiesExploratory toxicology studies