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Sorafenib Activity and Disposition in Liver Cancer Does Not Depend on Organic Cation Transporter 1

Mingqing Chen1, Claudia Neul2,3, Elke Schaeffeler2,3,4

  • 1Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, The Ohio State University, Columbus, Ohio, USA.

Clinical Pharmacology and Therapeutics
|July 28, 2019
PubMed

Insights

Organic cation transporter 1 (OCT1) does not transport sorafenib, a drug used for advanced hepatocellular carcinoma (HCC). This study indicates OCT1 is not a valid biomarker for predicting sorafenib response in HCC patients.

Area of Science:

  • Pharmacology
  • Oncology
  • Molecular Biology

Background:

  • Systemic therapy for advanced hepatocellular carcinoma (HCC) using sorafenib exhibits significant interindividual pharmacokinetic variability and unpredictable side effects.
  • Organic cation transporter 1 (OCT1), encoded by the SLC22A1 gene, has been suggested as a potential clinical biomarker for predicting HCC treatment response.

Purpose of the Study:

  • To investigate the role of OCT1 in the cellular uptake and transport of sorafenib.
  • To determine if OCT1 functions as a transporter for sorafenib and assess its validity as a biomarker for sorafenib response in HCC.

Main Methods:

  • Utilized Xenopus laevis oocytes and mammalian cell lines overexpressing functional OCT1 protein to assess sorafenib transport.
  • Analyzed sorafenib accumulation in liver cancer cell lines with varying OCT1 expression levels.
  • Examined sorafenib pharmacokinetics in mice with different OCT1 genotypes.
  • Investigated SLC22A1 mRNA expression and its correlation with DNA methylation in The Cancer Genome Atlas (TCGA) HCC cohort.

Main Results:

  • Overexpression of OCT1 in oocytes and cell lines did not facilitate sorafenib transport.
  • Sorafenib accumulated in liver cancer cell lines irrespective of OCT1 mRNA and protein levels.
  • Sorafenib pharmacokinetics in mice were independent of OCT1 genotype.
  • SLC22A1 mRNA expression was significantly reduced by DNA methylation in HCC samples from the TCGA.

Conclusions:

  • Cellular uptake of sorafenib is independent of OCT1.
  • OCT1 is not a valid biomarker for predicting sorafenib response or guiding treatment decisions in advanced HCC.

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