Preclinical Incorporation Dosimetry of [18F]FACH—A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET
Abstract
:1. Introduction
2. Results
3. Discussion
4. Materials and Methods
4.1. Synthesis of [18F]FACH
4.2. Preclinical Dosimetry Studies—In Vivo PET/CT Imaging in Pigs
4.3. Image Analysis
4.4. Incorporation Dosimetry
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Sample Availability: Samples of the compounds are available from the authors. |
Target Organ | OD | ED Contr. | ED Contr. | SD |
---|---|---|---|---|
in mSv/MBq | in ± mSv/MBq | in mSv/MBq | in ± mSv/MBq | |
Adrenals | 1.42 × 10−2 | 5.69 × 10−4 | 1.31 × 10−4 | 4.73 × 10−6 |
Brain | 4.69 × 10−3 | 8.09 × 10−4 | 4.69 × 10−5 | 8.09 × 10−6 |
Esophagus | 9.03 × 10−3 | 1.21 × 10−3 | 3.61 × 10−4 | 4.86 × 10−5 |
Eyes | 6.91 × 10−3 | 1.68 × 10−3 | 0.00 | 0.00 |
Gall Bladder Wall | 5.04 × 10−2 | 3.75 × 10−2 | 4.65 × 10−4 | 3.47 × 10−4 |
Left Colon | 1.37 × 10−2 | 2.91 × 10−3 | 6.63 × 10−4 | 1.41 × 10−4 |
Small Intestine | 1.84 × 10−2 | 8.44 × 10−3 | 1.71 × 10−4 | 7.81 × 10−5 |
Stomach Wall | 1.09 × 10−2 | 3.07 × 10−3 | 1.31 × 10−3 | 3.64 × 10−4 |
Right Colon | 2.40 × 10−2 | 7.40 × 10−3 | 1.16 × 10−3 | 3.62 × 10−4 |
Rectum | 1.38 × 10−2 | 1.15 × 10−3 | 3.18 × 10−4 | 2.60 × 10−5 |
Heart Wall | 9.46× 10−3 | 7.51 × 10−4 | 8.72 × 10−5 | 6.72 × 10−6 |
Kidneys | 2.62 × 10−2 | 2.19 × 10−3 | 2.42 × 10−4 | 2.00 × 10−5 |
Liver | 2.33 × 10−2 | 1.36 × 10−2 | 9.34 × 10−4 | 5.46 × 10−4 |
Lungs | 7.88 × 10−3 | 2.27 × 10−4 | 9.46 × 10−4 | 2.72 × 10−5 |
Pancreas | 3.05 × 10−2 | 2.73 × 10−2 | 2.81 × 10−4 | 2.52 × 10−4 |
Prostate | 1.30 × 10−2 | 2.85 × 10−3 | 6.01 × 10−5 | 1.32 × 10−5 |
Salivary Glands | 7.90 × 10−3 | 2.11 × 10−3 | 7.90 × 10−5 | 2.11 × 10−5 |
Red Marrow | 1.39 × 10−2 | 2.19 × 10−3 | 1.67 × 10−3 | 2.63 × 10−4 |
Osteogenic Cells | 2.12 × 10−2 | 1.88 × 10−3 | 2.12 × 10−4 | 1.88 × 10−5 |
Spleen | 9.08 × 10−3 | 1.14 × 10−3 | 8.37 × 10−5 | 1.04 × 10−5 |
Testes | 8.45 × 10−3 | 2.21 × 10−3 | 3.38 × 10−4 | 8.87 × 10−5 |
Thymus | 8.33 × 10−3 | 1.73 × 10−3 | 7.69 × 10−5 | 1.59 × 10−5 |
Thyroid | 7.08 × 10−3 | 8.70 × 10−4 | 2.83 × 10−4 | 3.49 × 10−5 |
Urinary Bladder Wall | 6.26 × 10−2 | 2.89 × 10−2 | 2.50 × 10−3 | 1.15 × 10−3 |
Total Body | 9.76 × 10−3 | 1.53 × 10−3 | 0.00 | 0.00 |
ED | 12.4 × 10−2 |
Tracer | Target/Organ | Preclinical (μSv/MBq) | Reference |
---|---|---|---|
[18F]FACH | MCT1/4/brain tumor | 12.4 | this study |
[18F]DBT10 | α7 receptor/brain tumor | 13.7 | [22] |
(S)-(−)-[18F]fluspidine (R)-(+)-[18F]fluspidine | σ receptor/brain | 12.9 14.0 | [15] |
(−)-[18F]flubatine (+)-[18F]flubatine | α4β2 receptor/brain | 14.7 14.3 | [16] [14] |
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Sattler, B.; Kranz, M.; Wenzel, B.; Jain, N.T.; Moldovan, R.-P.; Toussaint, M.; Deuther-Conrad, W.; Ludwig, F.-A.; Teodoro, R.; Sattler, T.; et al. Preclinical Incorporation Dosimetry of [18F]FACH—A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET. Molecules 2020, 25, 2024. https://doi.org/10.3390/molecules25092024
Sattler B, Kranz M, Wenzel B, Jain NT, Moldovan R-P, Toussaint M, Deuther-Conrad W, Ludwig F-A, Teodoro R, Sattler T, et al. Preclinical Incorporation Dosimetry of [18F]FACH—A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET. Molecules. 2020; 25(9):2024. https://doi.org/10.3390/molecules25092024
Chicago/Turabian StyleSattler, Bernhard, Mathias Kranz, Barbara Wenzel, Nalin T. Jain, Rareş-Petru Moldovan, Magali Toussaint, Winnie Deuther-Conrad, Friedrich-Alexander Ludwig, Rodrigo Teodoro, Tatjana Sattler, and et al. 2020. "Preclinical Incorporation Dosimetry of [18F]FACH—A Novel 18F-Labeled MCT1/MCT4 Lactate Transporter Inhibitor for Imaging Cancer Metabolism with PET" Molecules 25, no. 9: 2024. https://doi.org/10.3390/molecules25092024