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 strategiesA report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]‐THK‐5351
Neelamegam R, Yokell D, Rice P, Furumoto S, Kudo Y, Okamura N, Fakhri G. A report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]‐THK‐5351. Journal Of Labelled Compounds And Radiopharmaceuticals 2017, 60: 140-146. PMID: 27859483, DOI: 10.1002/jlcr.3482.Peer-Reviewed Original ResearchConceptsO-THPNucleophilic fluorination reactionsHydrochloric acidFluorination reactionDilute hydrochloric acidSemi-preparative high-performance liquid chromatographyTosylate precursorHigh-performance liquid chromatographyUncorrected radiochemical yieldDimethyl sulfoxideRadiochemical yieldRadiosynthesis moduleMulti-center trialLiquid chromatographyAutomated radiosynthesisRadiosynthesisPositron emission tomography radiopharmaceuticalsPET imaging agentUnited States Pharmacopeia