2022
Ovarian and uterine carcinosarcomas are sensitive in vitro and in vivo to elimusertib, a novel ataxia-telangiectasia and Rad3-related (ATR) kinase inhibitor
Manavella D, McNamara B, Harold J, Bellone S, Hartwich T, Yang-Hartwich Y, Mutlu L, Zipponi M, Demirkiran C, Verzosa M, Altwerger G, Ratner E, Huang G, Clark M, Andikyan V, Azodi M, Schwartz P, Dottino P, Choi J, Alexandrov L, Buza N, Hui P, Santin A. Ovarian and uterine carcinosarcomas are sensitive in vitro and in vivo to elimusertib, a novel ataxia-telangiectasia and Rad3-related (ATR) kinase inhibitor. Gynecologic Oncology 2022, 169: 98-105. PMID: 36525930, PMCID: PMC9925406, DOI: 10.1016/j.ygyno.2022.12.003.Peer-Reviewed Original ResearchConceptsHomologous recombination deficiencyCS cell linesCell linesWestern blotKinase inhibitorsOverall animal survivalProtein expressionDose-dependent increaseDose-dependent inhibitionCarcinosarcoma cell lineTumor growth inhibitionCaspase-3 expressionEndometrioid histologyAggressive malignancyUterine carcinosarcomaCS patientsPreclinical activityClinical trialsEpithelial componentAnimal survivalXenograftsApoptosis markersRecombination deficiencyP-ATRP-Chk1Elimusertib (BAY1895344), a novel ATR inhibitor, demonstrates in vivo activity in ATRX mutated models of uterine leiomyosarcoma
Harold J, Bellone S, Manavella D, Mutlu L, McNamara B, Hartwich T, Zipponi M, Yang-Hartwich Y, Demirkiran C, Verzosa M, Choi J, Dong W, Buza N, Hui P, Altwerger G, Huang G, Andikyan V, Clark M, Ratner E, Azodi M, Schwartz P, Santin A. Elimusertib (BAY1895344), a novel ATR inhibitor, demonstrates in vivo activity in ATRX mutated models of uterine leiomyosarcoma. Gynecologic Oncology 2022, 168: 157-165. PMID: 36442427, PMCID: PMC9797429, DOI: 10.1016/j.ygyno.2022.11.014.Peer-Reviewed Original ResearchConceptsPatient-derived xenograftsUterine leiomyosarcomaVivo activityVehicle control treatmentMedian overall survivalTumor volume differencesOral scheduleWestern blot analysisOverall survivalOral gavageAggressive malignancyPDX modelsClinical trialsSCID miceTumor measurementsULMS patientsSignificant growth inhibitionNovel ATR inhibitorTumor samplesSignificant toxicityWestern blotKinase inhibitorsATRX mutationsGene mutationsControl vehicle
2015
HER2 as Biomarker for Endometrial Cancer
English D, Roque D, Buza N, Santin A. HER2 as Biomarker for Endometrial Cancer. Biomarkers In Disease: Methods, Discoveries And Applications 2015, 507-526. DOI: 10.1007/978-94-007-7681-4_26.ChaptersEndometrial cancerEpidermal growth factor (EGF) familyGrowth factor familyC-erbB2 geneFactor familyCell survivalErbB pathwayNovel tyrosine kinase inhibitorOverall poor survivalOverexpression of HER2Tyrosine kinase inhibitorsKinase inhibitorsEndometrial neoplasmsPoor survivalPathwayTumor typesHER2Monoclonal antibodiesCancerGenesBiomarkersOverexpressionSurvivalWide varietyErbB2
2014
HER2 as Biomarker for Endometrial Cancer
English D, Roque D, Buza N, Santin A. HER2 as Biomarker for Endometrial Cancer. 2014, 1-16. DOI: 10.1007/978-94-007-7744-6_26-1.ChaptersEndometrial cancerEpidermal growth factor (EGF) familyGrowth factor familyC-erbB2 geneFactor familyCell survivalErbB pathwayNovel tyrosine kinase inhibitorOverall poor survivalOverexpression of HER2Tyrosine kinase inhibitorsKinase inhibitorsEndometrial neoplasmsPoor survivalPathwayTumor typesHER2Monoclonal antibodiesCancerGenesBiomarkersOverexpressionSurvivalWide varietyErbB2