2022
In Vivo Head‐To‐Head Comparison of [18F]GTP1 and [18F]PI2620 in Alzheimer’s Disease
Bohorquez S, Constantinescu C, Manser P, Gunn R, Russell D, Tonietto M, Bullich S, Stephens A, Mueller A, Klein G, Teng E, Pickthorn K. In Vivo Head‐To‐Head Comparison of [18F]GTP1 and [18F]PI2620 in Alzheimer’s Disease. Alzheimer's & Dementia 2022, 18 DOI: 10.1002/alz.063517.Peer-Reviewed Original ResearchChoroid plexusAlzheimer's diseaseTau pathology distributionModerate AD subjectsTarget cortical regionsTherapeutic trialsTau pathologyHead studiesPathology distributionCentrum semiovaleCortical greyBraak regionsAD subjectsHuman studiesInferior cerebellumSubcortical regionsHead comparisonQuantification scaleCortical regionsSubcortical structuresMinute imagesCSF spaceDiseaseUnimpaired subjectsSUVRPROGRESS IN DEVELOPING A LIGHT‐STABLE 4R TAU PET IMAGING AGENT: APN‐1701 FIH
Tempest P, Lin Y, Tai C, Ono M, Russell D, Sandiego C, Carroll V, Gunn R, Margolin R, Higuchi M, Jang M. PROGRESS IN DEVELOPING A LIGHT‐STABLE 4R TAU PET IMAGING AGENT: APN‐1701 FIH. Alzheimer's & Dementia 2022, 18 DOI: 10.1002/alz.063028.Peer-Reviewed Original ResearchAD subjectsMulticenter phase 2 clinical trialAlzheimer's diseasePhase 2 clinical trialTau PET tracersPET imaging agentSimilar brain regionsCortical uptakeTest-retest studyCN subjectsClinical trialsNormal subjectsTau tracersBrain regionsSUV valuesDiverse tauopathiesPET tracersSame rank orderSUVR imagesImaging agentImaging profileDiseaseIn Vivo Head‐To‐Head Comparison of [18F]GTP1 and [18F]PI2620 in Alzheimer’s Disease
Bohorquez S, Constantinescu C, Manser P, Gunn R, Russell D, Tonietto M, Bullich S, Stephens A, Mueller A, Klein G, Teng E, Pickthorn K. In Vivo Head‐To‐Head Comparison of [18F]GTP1 and [18F]PI2620 in Alzheimer’s Disease. Alzheimer's & Dementia 2022, 18 DOI: 10.1002/alz.063513.Peer-Reviewed Original ResearchChoroid plexusAlzheimer's diseaseTau pathology distributionModerate AD subjectsTarget cortical regionsTherapeutic trialsTau pathologyHead studiesPathology distributionCentrum semiovaleCortical greyBraak regionsAD subjectsHuman studiesInferior cerebellumSubcortical regionsHead comparisonQuantification scaleCortical regionsSubcortical structuresMinute imagesCSF spaceDiseaseUnimpaired subjectsSUVRPROGRESS IN DEVELOPING A LIGHT‐STABLE 4R TAU PET IMAGING AGENT: APN‐1701 FIH
Tempest P, Lin Y, Tai C, Ono M, Russell D, Sandiego C, Gunn R, Carroll V, Margolin R, Kao T, Higuchi M, Jang M. PROGRESS IN DEVELOPING A LIGHT‐STABLE 4R TAU PET IMAGING AGENT: APN‐1701 FIH. Alzheimer's & Dementia 2022, 18 DOI: 10.1002/alz.063025.Peer-Reviewed Original ResearchAD subjectsMulticenter phase 2 clinical trialAlzheimer's diseasePhase 2 clinical trialTau PET tracersPET imaging agentSimilar brain regionsCortical uptakeTest-retest studyCN subjectsClinical trialsNormal subjectsTau tracersBrain regionsSUV valuesDiverse tauopathiesPET tracersSame rank orderSUVR imagesImaging agentImaging profileDisease
2021
Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme, following administration of single and multiple doses to healthy volunteers
Kielbasa W, Shcherbinin S, Goldsmith P, Phipps K, Biglan K, Mancini M, Russell D, Constantinescu C, Gunn R, Nuthall H, Mergott D, Lowe S, Collins E. Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme, following administration of single and multiple doses to healthy volunteers. Alzheimer's & Dementia 2021, 17 DOI: 10.1002/alz.057774.Peer-Reviewed Original ResearchHealthy volunteersEnzyme occupancyPET scansSingle doseMultiple-dose clinical studiesPost-dose intervalPositron emission tomography radioligandBaseline PET scanLonger clinical trialsTarget occupancyTau-related diseasesMultiple dosesMultiple dosingClinical trialsPlasma pharmacokineticsClinical studiesEfficacy trialsSD studiesDose selectionTomography radioligandEnzyme inhibitorsPotential treatmentAlzheimer's diseasePET studiesTarget engagement