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
2016
ARV-330: Androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Jin M, Crew A, Rossi A, Willard R, Dong H, Siu K, Wang J, Gordon D, Chen X, Ferraro C, Crews C, Coleman K, Winkler J. ARV-330: Androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2016, 34: 267-267. DOI: 10.1200/jco.2016.34.2_suppl.267.Peer-Reviewed Original ResearchAndrogen receptorAR mutationsProstate cancerTotal androgen receptorTreatment of miceAR protein levelsProstate cancer cellsGood pharmacokinetic propertiesPlasma PSAMetastatic diseaseNM R1881SC injectionAndrogen productionDisease progressionPSA expressionIntact miceTherapeutic effectCastrated miceVCaP cellsAnimal modelsProstate involutionTumor growthVivo efficacyPreclinical developmentPharmacokinetic properties