Title : Radiation dosimetry of the alpha4beta2 nicotinic receptor ligand (+)-[18F]flubatine, comparing preclinical PET\/MRI and PET\/CT to first-in-human PET\/CT results - Kranz_2016_EJNMMI.Phys_3_25 |
Author(s) : Kranz M , Sattler B , Tiepolt S , Wilke S , Deuther-Conrad W , Donat CK , Fischer S , Patt M , Schildan A , Patt J , Smits R , Hoepping A , Steinbach J , Sabri O , Brust P |
Ref : EJNMMI Phys , 3 :25 , 2016 |
Abstract :
BACKGROUND: Both enantiomers of [18F]flubatine are new radioligands for neuroimaging of alpha4beta2 nicotinic acetylcholine receptors with positron emission tomography (PET) exhibiting promising pharmacokinetics which makes them attractive for different clinical questions. In a previous preclinical study, the main advantage of (+)-[18F]flubatine compared to (-)-[18F]flubatine was its higher binding affinity suggesting that (+)-[18F]flubatine might be able to detect also slight reductions of alpha4beta2 nAChRs and could be more sensitive than (-)-[18F]flubatine in early stages of Alzheimer's disease. To support the clinical translation, we investigated a fully image-based internal dosimetry approach for (+)-[18F]flubatine, comparing mouse data collected on a preclinical PET/MRI system to piglet and first-in-human data acquired on a clinical PET/CT system. Time-activity curves (TACs) were obtained from the three species, the animal data extrapolated to human scale, exponentially fitted and the organ doses (OD), and effective dose (ED) calculated with OLINDA. |
PubMedSearch : Kranz_2016_EJNMMI.Phys_3_25 |
PubMedID: 27770429 |
Kranz M, Sattler B, Tiepolt S, Wilke S, Deuther-Conrad W, Donat CK, Fischer S, Patt M, Schildan A, Patt J, Smits R, Hoepping A, Steinbach J, Sabri O, Brust P (2016)
Radiation dosimetry of the alpha4beta2 nicotinic receptor ligand (+)-[18F]flubatine, comparing preclinical PET\/MRI and PET\/CT to first-in-human PET\/CT results
EJNMMI Phys
3 :25
Kranz M, Sattler B, Tiepolt S, Wilke S, Deuther-Conrad W, Donat CK, Fischer S, Patt M, Schildan A, Patt J, Smits R, Hoepping A, Steinbach J, Sabri O, Brust P (2016)
EJNMMI Phys
3 :25