Unlocking PARP inhibitor efficacy for HRD-negative cancers using the alphalex tumor targeting platform inhibitor efficacy for HRD-negative cancers using the alphalex tumor targeting platform.
Bindra R, Sundaram R, Aiello R, Marshall D, Bourassa P, Csengery J, Zhang Q, Robinson B, lopresti-Morrow L, Bechtold J, Tylaska L, Paradis T, Paralkar V, Hellsund P, Glazer P. Unlocking PARP inhibitor efficacy for HRD-negative cancers using the alphalex tumor targeting platform inhibitor efficacy for HRD-negative cancers using the alphalex tumor targeting platform. Journal Of Clinical Oncology 2019, 37: e14664-e14664. DOI: 10.1200/jco.2019.37.15_suppl.e14664.Peer-Reviewed Original ResearchHomologous recombination deficiencyHRD statusAnti-cancer agentsClinical trialsSignificant bone marrow toxicityTumor cellsInhibitor efficacyPhase I clinical trialIND-enabling studiesDose-limiting toxicityBone marrow toxicitySignificant tumor cell killingSmall molecule anti-cancer agentNormal tissue toxicityTumor cell killingTumor-targeting approachesPARP inhibitor efficacyRelevant chemotherapyVivo tumor modelsMarrow toxicityBRCA1/2 mutationsComplete sparingBone marrowSolid tumorsChemotherapyARV-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
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