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Radiation dose of the P-glycoprotein tracer 11C-laniquidar
Andrey Postnov1, Femke E Froklage, Arthur van Lingen
1Departments of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands.
Unlabelled:
Resistance to current drug therapy is an important issue in the treatment of epilepsy. Inadequate access of central nervous system drugs to their targets in the brain may be caused by overexpression or overactivity of multidrug transporters, such as P-glycoprotein (P-gp), at the blood-brain barrier. Laniquidar, an inhibitor of P-gp, has been labeled with (11)C for use in PET studies of P-gp expression in humans. Given potential interspecies differences in biodistribution, the purpose of this study was to ensure safe use of (11)C-laniquidar by determining the dosimetry of (11)C-laniquidar using whole-body PET studies.
Methods:
Six healthy volunteers were subjected to a series of 10 whole-body PET scans within approximately 70 min. Five blood samples were taken during the series.
Results:
High uptake of (11)C-laniquidar was seen in liver, spleen, kidneys, and lung, whereas brain uptake was low. The effective dose for (11)C-laniquidar was 4.76 ± 0.13 and 3.69 ± 0.01 μSv·MBq(-1) for women and men, respectively.
Conclusion:
Biodistribution and measured effective dose indicate that (11)C-laniquidar is a safe tracer for PET imaging, with a total dose of about 2 mSv for a brain PET/CT protocol.
Insights
This study found (11)C-laniquidar, a P-glycoprotein (P-gp) inhibitor tracer, has a low effective dose. Biodistribution indicates (11)C-laniquidar is safe for PET imaging in epilepsy drug resistance research.
Area of Science:
- Radiopharmaceutical dosimetry
- Neuroscience
- Pharmacology
Background:
- Epilepsy treatment faces challenges due to drug resistance.
- Overexpression of P-glycoprotein (P-gp) at the blood-brain barrier can limit CNS drug efficacy.
- Laniquidar is a P-gp inhibitor labeled with (11)C for PET imaging.
Purpose of the Study:
- To determine the dosimetry of (11)C-laniquidar in humans.
- To ensure the safe use of (11)C-laniquidar for Positron Emission Tomography (PET) studies.
- To assess potential interspecies differences in biodistribution.
Main Methods:
- Six healthy volunteers underwent whole-body PET scans.
- (11)C-laniquidar biodistribution was assessed over approximately 70 minutes.
- Blood samples were collected to measure tracer levels.
Main Results:
- High uptake of (11)C-laniquidar was observed in the liver, spleen, kidneys, and lungs.
- Low uptake was noted in the brain.
- The effective dose was calculated as 4.76 ± 0.13 μSv·MBq⁻¹ for women and 3.69 ± 0.01 μSv·MBq⁻¹ for men.
Conclusions:
- The biodistribution and effective dose of (11)C-laniquidar support its safety as a PET imaging tracer.
- A typical brain PET/CT protocol using (11)C-laniquidar results in a total radiation dose of approximately 2 mSv.
- (11)C-laniquidar is suitable for PET studies investigating P-gp expression in humans.
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