2017
A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2− Metastatic Breast Cancer
Mayer IA, Abramson VG, Formisano L, Balko JM, Estrada MV, Sanders ME, Juric D, Solit D, Berger MF, Won HH, Li Y, Cantley LC, Winer E, Arteaga CL. A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2− Metastatic Breast Cancer. Clinical Cancer Research 2017, 23: 26-34. PMID: 27126994, PMCID: PMC5085926, DOI: 10.1158/1078-0432.ccr-16-0134.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAntineoplastic Combined Chemotherapy ProtocolsAromatase InhibitorsBiomarkers, TumorBreast NeoplasmsCell Line, TumorDNA Mutational AnalysisFemaleHumansIn Situ Hybridization, FluorescenceLetrozoleMaximum Tolerated DoseMiddle AgedMutationNeoplasm MetastasisNeoplasm StagingNitrilesPhosphatidylinositol 3-KinasesPhosphoinositide-3 Kinase InhibitorsReceptor, ErbB-2Receptor, Fibroblast Growth Factor, Type 1Receptors, EstrogenThiazolesTreatment OutcomeTriazolesConceptsMaximum-tolerated doseBreast cancer cellsEndocrine therapyClinical benefitCommon drug-related adverse eventsDrug-related adverse eventsMutant breast cancer cellsBreast cancer refractoryPIK3CA mutation statusPIK3CA-mutated tumorsClinical benefit ratePhase Ib studyPI3K catalytic subunit p110αDose-limiting toxicityCancer cellsSelective oral inhibitorOverexpression of FGFR1Combination of letrozoleSynergistic antitumor activityCatalytic subunit p110αCancer refractoryFGFR1/2 amplificationMetastatic ERAdverse eventsObjective response
2014
First-in-human study of AMG 337, a highly selective oral inhibitor of MET, in adult patients (pts) with advanced solid tumors.
Hong D, LoRusso P, Hamid O, Beaupre D, Janku F, Khan R, Kittaneh M, Loberg R, Amore B, Caudillo I, Hwang Y, Tang R, Ngarmchamnanrith G, Kwak E. First-in-human study of AMG 337, a highly selective oral inhibitor of MET, in adult patients (pts) with advanced solid tumors. Journal Of Clinical Oncology 2014, 32: 2508-2508. DOI: 10.1200/jco.2014.32.15_suppl.2508.Peer-Reviewed Original ResearchAdvanced solid tumorsSelective oral inhibitorAMG 337Adult patientsOral inhibitorHuman studiesSolid tumors
2009
A first-in-human phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors
Wagner A, Von Hoff D, LoRusso P, Tibes R, Mazina K, Ware J, Yan Y, Derynck M, Demetri G. A first-in-human phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors. Journal Of Clinical Oncology 2009, 27: 3501-3501. DOI: 10.1200/jco.2009.27.15_suppl.3501.Peer-Reviewed Original ResearchDose-proportional increaseAnti-tumor activityDose levelsPK dataPan-PI3K inhibitor GDCSolid tumorsPhase ICA-125 responseDose escalation armDose-escalation cohortsDrug-related AEsGrade 1/2 nauseaPreliminary PK dataSingle-dose PKAdvanced solid tumorsTotal daily dosesFDG-PET uptakeSelective oral inhibitorSteady-state PKHuman phase IProstate cancer modelPotential signsBID armCancer ptsQD arm
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