Effect of Carbidopa on 18F-FDOPA Uptake in Insulinoma: From Cell Culture to Small-Animal PET Imaging

J Nucl Med. 2017 Jan;58(1):36-41. doi: 10.2967/jnumed.116.180588. Epub 2016 Sep 8.

Abstract

Patient premedication with carbidopa seems to improve the accuracy of 6-18F-fluoro-3,4-dihydroxy-l-phenylalanine (18F-FDOPA) PET for insulinoma diagnosis. However, the risk of PET false-negative results in the presence of carbidopa is a concern. Consequently, we aimed to evaluate the effect of carbidopa on 18F-FDOPA uptake in insulinoma β-cells and an insulinoma xenograft model in mice.

Methods: 18F-FDOPA in vitro accumulation was assessed in the murine β-cell line RIN-m5F. In vivo small-animal PET experiments were performed on tumor-bearing nude mice after subcutaneous injection of RIN-m5F cells. Experiments were conducted with and without carbidopa pretreatment.

Results: Incubation of RIN-m5F cells with 80 μM carbidopa did not significantly affect the cellular accumulation of 18F-FDOPA. Tumor xenografts were clearly detectable by small-animal PET in all cases. Insulinoma xenografts in carbidopa-treated mice showed significantly higher 18F-FDOPA uptake than those in nontreated mice. Regardless of carbidopa premedication, the xenografts were characterized by an early increase in 18F-FDOPA uptake and then a progressive reduction over time.

Conclusion: Carbidopa did not influence in vitro 18F-FDOPA accumulation in RIN-m5F cells but improved insulinoma imaging in vivo. Our findings increase current knowledge about the 18F-FDOPA uptake profile of RIN-m5F cells and a related xenograft model. To our knowledge, the present work represents the first preclinical research specifically focused on insulinomas, with potential translational implications.

Keywords: 18F-FDOPA; PET; RIN-m5F; carbidopa; insulinoma; small-animal PET.

MeSH terms

  • Animals
  • Carbidopa / administration & dosage*
  • Cell Line, Tumor
  • Dihydroxyphenylalanine / analogs & derivatives*
  • Dihydroxyphenylalanine / pharmacokinetics
  • Female
  • Image Enhancement / methods
  • Insulinoma / diagnostic imaging
  • Insulinoma / metabolism*
  • Metabolic Clearance Rate / drug effects
  • Mice, Nude
  • Organ Specificity / drug effects
  • Pancreatic Neoplasms / diagnostic imaging*
  • Pancreatic Neoplasms / metabolism*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / pharmacokinetics
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Tissue Distribution / drug effects

Substances

  • Radiopharmaceuticals
  • fluorodopa F 18
  • Dihydroxyphenylalanine
  • Carbidopa