Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib
Collier T, Normandin M, Stephenson N, Livni E, Liang S, Wooten D, Esfahani S, Stabin M, Mahmood U, Chen J, Wang W, Maresca K, Waterhouse R, El Fakhri G, Richardson P, Vasdev N. Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib. Nature Communications 2017, 8: 15761. PMID: 28594000, PMCID: PMC5472746, DOI: 10.1038/ncomms15761.Peer-Reviewed Original ResearchMeSH KeywordsAminopyridinesAnaplastic Lymphoma KinaseAnimalsCarbon RadioisotopesChemistry Techniques, SyntheticContrast MediaFluorine RadioisotopesHumansIsotope LabelingLactamsLactams, MacrocyclicMacaca mulattaMaleMicePositron-Emission TomographyProtein-Tyrosine KinasesProto-Oncogene ProteinsPyrazolesTissue DistributionXenograft Model Antitumor AssaysConceptsAnaplastic lymphoma kinasePositron emission tomographyPositron emission tomography imagingC-ros oncogene 1Non-small cell lung cancerCell lung cancerBrain tumor lesionsOptimal therapeutic outcomesLung cancer patientsBlood-brain barrierPF-06463922Clinical trial investigatorsTumor uptakeLung cancerSmall molecule inhibitorsCancer patientsTherapeutic outcomesLorlatinibEmission tomographyDosimetry assessmentNon-human primatesTrial investigatorsBrain permeabilityEarly goalRadiolabeling strategiesBrain Penetration of the ROS1/ALK Inhibitor Lorlatinib Confirmed by PET
Collier T, Maresca K, Normandin M, Richardson P, McCarthy T, Liang S, Waterhouse R, Vasdev N. Brain Penetration of the ROS1/ALK Inhibitor Lorlatinib Confirmed by PET. Molecular Imaging 2017, 16: 1536012117736669. PMID: 29067878, PMCID: PMC5661750, DOI: 10.1177/1536012117736669.Peer-Reviewed Original ResearchConceptsPositron emission tomographyLung cancerTreatment of non-small-cell lung cancerBrain metastases of patientsNon-small-cell lung cancerPositron emission tomography evaluationNonhuman primatesRodent tumor modelsGoal of clinical translationOptimal therapeutic outcomesMetastasis of patientsBlood-brain barrierBrain metastasesPF-06463922Preclinical modelsClinical trial investigatorsTumor modelMolecular alterationsLorlatinibTherapeutic outcomesCancer therapeuticsBrain penetrationClinical translationEmission tomographyTrial investigators