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
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
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