2016
Preclinical and first‐in‐human phase I studies of KW‐2450, an oral tyrosine kinase inhibitor with insulin‐like growth factor receptor‐1/insulin receptor selectivity
Schwartz GK, Dickson MA, LoRusso P, Sausville EA, Maekawa Y, Watanabe Y, Kashima N, Nakashima D, Akinaga S. Preclinical and first‐in‐human phase I studies of KW‐2450, an oral tyrosine kinase inhibitor with insulin‐like growth factor receptor‐1/insulin receptor selectivity. Cancer Science 2016, 107: 499-506. PMID: 26850678, PMCID: PMC4832855, DOI: 10.1111/cas.12906.Peer-Reviewed Original ResearchConceptsOral tyrosine kinase inhibitorTyrosine kinase inhibitorsIGF-1RSolid tumorsHuman Phase I StudyInsulin-like growth factor receptor 1Colon carcinoma xenograft modelKinase inhibitorsHuman epidermal growth factor receptorPhase I clinical trialDose of KWModest antitumor activityAdvanced solid tumorsMetastatic breast cancerPhase I studiesGrowth factor receptor 1Human IGF-1RHuman malignant cell linesEpidermal growth factor receptorFactor receptor 1Inhibitory activityEvaluable patientsGrowth factor receptorMalignant cell linesStable disease
2012
Phase I study of humanized monoclonal antibody AVE1642 directed against the type 1 insulin-like growth factor receptor (IGF-1R), administered in combination with anticancer therapies to patients with advanced solid tumors
Macaulay V, Middleton M, Protheroe A, Tolcher A, Dieras V, Sessa C, Bahleda R, Blay J, LoRusso P, Mery-Mignard D, Soria J. Phase I study of humanized monoclonal antibody AVE1642 directed against the type 1 insulin-like growth factor receptor (IGF-1R), administered in combination with anticancer therapies to patients with advanced solid tumors. Annals Of Oncology 2012, 24: 784-791. PMID: 23104723, PMCID: PMC3574548, DOI: 10.1093/annonc/mds511.Peer-Reviewed Original ResearchMeSH KeywordsAdultAgedAntibodies, Monoclonal, HumanizedAntineoplastic Combined Chemotherapy ProtocolsDeoxycytidineDiarrheaDocetaxelDoxorubicinErlotinib HydrochlorideFemaleGemcitabineHumansLeiomyosarcomaMaleMelanomaMiddle AgedQuinazolinesReceptor, IGF Type 1Skin NeoplasmsSoft Tissue NeoplasmsTaxoidsTreatment OutcomeConceptsAdvanced solid tumorsInsulin-like growth factor receptorType 1 insulin-like growth factor receptorGrowth factor receptorIGF-IISolid tumorsDisease controlCommon adverse eventsFactor receptorIGF-1R antibodyDurable disease controlCohort C2Adverse eventsPartial responseCohort BDocetaxel administrationSteroid premedicationControl ratePK interactionsGrade 3IGF-BP3Blood samplesCohort C1PatientsAVE1642