Molecules, Vol. 25, Pages 2024: Preclinical Incorporation Dosimetry of [18F]FACH —A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET

Molecules, Vol. 25, Pages 2024: Preclinical Incorporation Dosimetry of [18F]FACH—A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET Molecules doi: 10.3390/molecules25092024 Authors: Bernhard Sattler Mathias Kranz Barbara Wenzel Nalin T. Jain Rareş-Petru Moldovan Magali Toussaint Winnie Deuther-Conrad Friedrich-Alexander Ludwig Rodrigo Teodoro Tatjana Sattler Masoud Sadeghzadeh Osama Sabri Peter Brust Overexpression of monocarboxylate transporters (MCTs) has been shown for a variety of human cancers (e.g., colon, brain, breast, and kidney) and inhibition resulted in intracellular lactate accumulation, acidosis, and cell death. Thus, MCTs are promising targets to investigate tumor cancer metabolism with positron emission tomography (PET). Here, the organ doses (ODs) and the effective dose (ED) of the first 18F-labeled MCT1/MCT4 inhibitor were estimated in juvenile pigs. Whole-body dosimetry was performed in three piglets (age: ~6 weeks, weight: ~13–15 kg). The animals were anesthetized and subjected to sequential hybrid Positron Emission Tomography and Computed Tomography (PET/CT) up to 5 h after an intravenous (iv) injection of 156 ± 54 MBq [18F]FACH. All relevant organs were defined by volumes of interest. Exponential curves were fitted to the time–activity data. Time and mass scales were adapted to the human order of magnitude and the ODs calculated u...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research