2012
Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors
Markman B, Tabernero J, Krop I, Shapiro G, Siu L, Chen L, Mita M, Cuero M, Stutvoet S, Birle D, Anak Ö, Hackl W, Baselga J. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Annals Of Oncology 2012, 23: 2399-2408. PMID: 22357447, DOI: 10.1093/annonc/mds011.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAged, 80 and overAntineoplastic AgentsBreast NeoplasmsColonic NeoplasmsDiarrheaFemaleFluorodeoxyglucose F18HumansImidazolesMaleMaximum Tolerated DoseMiddle AgedNauseaPhosphoinositide-3 Kinase InhibitorsProstatic NeoplasmsQuinolinesRadionuclide ImagingRadiopharmaceuticalsTOR Serine-Threonine KinasesTreatment OutcomeYoung AdultConceptsAdvanced solid tumorsPreliminary antitumor activityStable diseaseSystemic exposureAdaptive Bayesian logistic regression modelSolid tumorsPhase I dose-escalation studyI dose-escalation studyFluorodeoxyglucose positron emission tomographyStable metabolic diseaseVariable systemic exposureAntitumor activityDose-escalation studyLow systemic exposurePI3K pathway inhibitionDay three timesLogistic regression modelsAdverse eventsDose escalationFluorodeoxyglucose uptakeRapamycin inhibitorsTumor shrinkagePharmacodynamic studiesComputed tomographyMTOR inhibitors
2010
Advances in Targeting Src in the Treatment of Breast Cancer and Other Solid Malignancies
Mayer EL, Krop IE. Advances in Targeting Src in the Treatment of Breast Cancer and Other Solid Malignancies. Clinical Cancer Research 2010, 16: 3526-3532. PMID: 20634194, DOI: 10.1158/1078-0432.ccr-09-1834.Peer-Reviewed Original ResearchConceptsMultiple solid tumor typesVascular endothelial growth factor receptorEndothelial growth factor receptorEarly phase trialsSolid tumor typesMultiple human malignanciesTargeting SrcEndocrine therapyGrowth factor receptorCombination regimensOngoing trialsFuture trialsSolid malignanciesProstate cancerBreast cancerEstrogen receptorPreclinical studiesAntitumor effectsTumor typesAngiogenesis inhibitorsCell-signaling pathwaysInhibitor dasatinibInvestigation of combinationsHuman malignanciesModest activity
2004
Frequent HIN-1 promoter methylation and lack of expression in multiple human tumor types.
Krop I, Player A, Tablante A, Taylor-Parker M, Lahti-Domenici J, Fukuoka J, Batra SK, Papadopoulos N, Richards WG, Sugarbaker DJ, Wright RL, Shim J, Stamey TA, Sellers WR, Loda M, Meyerson M, Hruban R, Jen J, Polyak K. Frequent HIN-1 promoter methylation and lack of expression in multiple human tumor types. Molecular Cancer Research 2004, 2: 489-94. PMID: 15383627, DOI: 10.1158/1541-7786.489.2.9.Peer-Reviewed Original ResearchConceptsHIN-1 expressionHIN-1 methylationHIN-1Breast carcinomaPancreatic carcinomaSmall cell lung cancerNormal tissuesMajority of lungCell lung cancerSquamous cell carcinomaMultiple human cancer typesPromoter methylationMultiple human tumor typesBronchial epithelial cellsHuman cancer typesHuman tumor typesNoncancer patientsCell carcinomaPromoter methylation statusLung cancerBronchial lavagePremalignant changesLack of expressionLung carcinomaProstate tumors