Radiation Dose of the P-Glycoprotein Tracer 11C-Laniquidar

Journal of Nuclear Medicine

Marc C. Huisman¹  Jonas Eriksson¹  Robert C. Schuit¹  Albert D. Windhorst¹  Arthur van Lingen¹  Femke E. Froklage¹  Adriaan A. Lammertsma¹  Andrey Postnov¹  N. Harry Hendrikse¹  Jaap C. Reijneveld¹ 

关键词: P-glycoprotein;    PET;    ¹¹C-laniquidar;    dosimetry;    multidrug transporter;   

DOI  :  10.2967/jnumed.113.120857

学科分类：医学（综合）

来源: Society of Nuclear Medicine

【 摘 要 】

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 11C 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 11C-laniquidar by determining the dosimetry of 11C-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 11C-laniquidar was seen in liver, spleen, kidneys, and lung, whereas brain uptake was low. The effective dose for 11C-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 11C-laniquidar is a safe tracer for PET imaging, with a total dose of about 2 mSv for a brain PET/CT protocol.

【 授权许可】

Unknown