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
2017
An oral androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Snyder L, Bookbinder M, Chen X, Crew A, Crews C, Dong H, Gordon D, Raina K, Rossi A, Taylor I, Vitale N, Wang J, Willard R, Zimmermann K. An oral androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2017, 35: 273-273. DOI: 10.1200/jco.2017.35.6_suppl.273.Peer-Reviewed Original ResearchAndrogen receptorAR degradationProstate cancerAR proteinAR target gene PSADegradation of ARCastration-resistant prostate cancerTotal androgen receptorMajority of patientsMutant AR proteinTumor growth inhibitionVivo preclinical studiesCell linesInhibits cell proliferationVCaP xenograftsMetastatic diseaseMost patientsAR pathwayElevated androgensMechanisms of resistancePreclinical studiesXenograft studiesVCaP cellsOral bioavailabilityPotent apoptosis