2019
First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in patients with advanced solid tumors
Shimomura A, Yamamoto N, Kondo S, Fujiwara Y, Suzuki S, Yanagitani N, Horiike A, Kitazono S, Ohyanagi F, Doi T, Kuboki Y, Kawazoe A, Shitara K, Ohno I, Banerji U, Sundar R, Ohkubo S, Calleja E, Nishio M. First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in patients with advanced solid tumors. Molecular Cancer Therapeutics 2019, 18: molcanther.0831.2018. PMID: 30679388, DOI: 10.1158/1535-7163.mct-18-0831.Peer-Reviewed Original ResearchConceptsGastrointestinal stromal tumorsPreliminary antitumor efficacyDose-escalation phaseAdvanced solid tumorsSolid tumorsTAS-116Eye disordersEscalation phaseFirst-in-human phase I studyPretreated gastrointestinal stromal tumoursHsp90 inhibitorsTreatment-related adverse eventsNon-small cell lung cancerFirst-in-human studyOral HSP90 inhibitorPhase I studyCell lung cancerPartial responseStromal tumorsDose proportionalityAntitumor efficacySafety profileSystemic exposureAdverse eventsLung cancer
2017
First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in advanced solid tumors.
Yanagitani N, Horiike A, Kitazono S, Ohyanagi F, Kondo S, Shimomura A, Fujiwara Y, Doi T, Kuboki Y, Kawazoe A, Shitara K, Ohno I, Banerji U, Sundar R, Ohkubo S, Huang J, Nishio M, Yamamoto N. First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in advanced solid tumors. Journal Of Clinical Oncology 2017, 35: 2546-2546. DOI: 10.1200/jco.2017.35.15_suppl.2546.Peer-Reviewed Original ResearchTAS-116Solid tumorsFirst-in-human phase I studyAntitumor activityOral HSP90 inhibitorAccelerated titration designPhase 2 studyPhase I studyPreliminary antitumor activityPhase 1 studyEvidence of target engagementDose expansionFlat doseEscalating dosesDose proportionalityRepeated administrationQD scheduleSafety profileEye disordersIncreased creatinineAdverse eventsTitration designDays administrationNon-purinePatients