Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme: Translation from rat to human
Shcherbinin S, Kielbasa W, Dubois S, Lowe S, Phipps K, Tseng J, Kevin D, Natanegara F, Warner S, Dreyfus N, Lindsay‐Scott P, Hawk M, McDonald N, Zhang X, Gilmore J, Biglan K, Mergott D, Russell D, Gunn R, Constantinescu C, Nuthall H, Collins E. Brain target occupancy of LY3372689, an inhibitor of the O‐GlcNAcase (OGA) enzyme: Translation from rat to human. Alzheimer's & Dementia 2020, 16 DOI: 10.1002/alz.040558.Peer-Reviewed Original ResearchPET scansEnzyme occupancyHealthy volunteersPlasma concentration-dependent increaseSingle oral dose studyOral dose studyBaseline PET scanSingle oral doseTau-related diseasesDose-dependent changesConcentration-dependent increaseHuman PET studiesDose cohortsOral doseSingle dosesDose studyClinical studiesEfficacy trialsPharmacokinetic samplesFrontal cortexInitial cohortDose selectionHigh doseNumber of subjectsEnzyme inhibitors