Evaluation of the relationship between [18F]FDG and P-glycoprotein expression: an experimental study

Influence of P-Glycoprotein Inhibition or Deficiency at the Blood–Brain Barrier on 18F-2-Fluoro-2-Deoxy-d-glucose (18F-FDG) Brain Kinetics

“…1). This time-dependent shift was also found in cancer cells (17,25). Interestingly, CsA was previously shown to abolish the difference in 18 F-FDG uptake between MDRpositive and MDR-negative cell lines (23).…”

“…Numerous in vitro studies, performed using different cancer cell lines, have revealed that MDR or P-gp-overexpressing cells incorporate 18 F-FDG at lower levels (14,15). This inverse relationship between P-gp function and 18 F-FDG uptake was also reported in vivo with selected cancer cells implanted as xenografts: P-gp-overexpressing tumors showed reduced 18 F-FDG uptake (16,17), which was restored using pharmacological P-gp inhibition (17). In patients, an inverse relationship was found between 18 F-FDG uptake and the level of P-gp expression examined in tumor resection (lung cancer, hepatocellular carcinoma, and intrahepatic cholangiocarcinoma) (18)(19)(20)(21)(22).…”

18FDG a PET tumor diagnostic tracer is not a substrate of the ABC transporter P-glycoprotein

“…Several authors reported strong positive correlation between the GLUT transporter expression, the 18 FDG uptake and the malignancy of tumors, while others found only weak correlations (Lorke et al, 2001;Zhao et al, 2005;Smith et al, 2007;Vallabhajosula, 2007;Ong et al, 2008;Paudyal et al, 2008;Seo et al, 2009;Smith, 2010;). Zaho et al (2005) and Yu et al (2012) demonstrated that the intratumoral 18 FDG distribution correlates well with the expression levels of GLUT-1, GLUT-3, and Hexokinase-II. In line with the above Southworth et al (2003) suggested tissue specific differences in the phosphorylation rate of 18 FDG to 18 FDG -6-phosphate.…”

“…A number of them accounted decreased accumulation of 18 FDG in cancer cells and tumors expressing Pgp at high level (Lorke et al, 2001;Higashi et al, 2004;Yamada et al, 2005;Seo et al, 2009;Smith, 2010, Yu et al, 2012. The most obvious interpretation of this observation would be that 18 FDG is a substrate of Pgp.…”

“…Positron emission tomography (PET) and single-photon emission tomography (SPECT) seems to be the most useful methods to study multidrug resistance in tumour tissues in vivo (Mairinger et al, 2011 (Lorke et al, 2001;Higashi et al, 2004;Yamada et al, 2005;Seo et al, 2009;Smith, 2010;Yu et al, 2012). It was also reported that certain Pgp modulators e.g.…”