Korean J Obes.  2016 Dec;25(4):233-239. 10.7570/kjo.2016.25.4.233.

Treatment with Gefitinib, an Epidermal Growth Factor Receptor Inhibitor, Decreases Serum Cholesterol in Patients with Lung Cancer

• Kang YE
• Kim JM
• Joung KH
• Kim HJ
• Ku BJ

• KMID: 2368803
• DOI: http://doi.org/10.7570/kjo.2016.25.4.233

Abstract

BACKGROUND
Statins are used to treat hypercholesterolemia; however, major cardiovascular events are decreased only 30% by statin treatment. Treatment with an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor has been reported to decrease serum glucose levels and improved insulin sensitivity in mice and humans, but there was no study in serum cholesterol levels. This study examined the effect of gefitinib, an EGFR tyrosine kinase inhibitor, on cholesterol metabolism in humans.
METHODS
We retrospectively reviewed the medical records of 299 patients with primary lung cancer treated with gefitinib for ≥1 month and 72 patients with other treatments. Serum cholesterol, serum triglycerides, and body mass index were measured before and after treatment. The changes in serum cholesterol, serum triglycerides, and body mass index were compared between the gefitinib treatment group and the control group and were also analyzed according to the presence or absence of EGFR mutations.
RESULTS
Serum cholesterol levels decreased significantly from 178.9 to 164.4 mg/dL after 1-month of gefitinib treatment. A total of 54 of the 299 patients underwent examination for the presence of the EGFR mutations. Serum cholesterol was significantly decreased in the group with the activating EGFR mutation (Δ=21.3 mg/dL) compared to that of those without the EGFR mutation (Δ=-3.1 mg/dL) after treatment with gefitinib. In contrast, there was no significantly difference between the two groups in control patients.
CONCLUSION
Treatment with gefitinib decreased serum cholesterol in lung cancer patients, particularly in those with activating mutations in EGFR. These data suggest that EGFR tyrosine kinase inhibitors provide a novel and attractive strategy for the treatment of hypercholesterolemia.

Keyword

Gefitinib; Cholesterol; Lung neoplasm

MeSH Terms

Animals
Blood Glucose
Body Mass Index
Cholesterol*
Epidermal Growth Factor*
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors
Hypercholesterolemia
Insulin Resistance
Lung Neoplasms*
Lung*
Medical Records
Metabolism
Mice
Protein-Tyrosine Kinases
Receptor, Epidermal Growth Factor*
Retrospective Studies
Triglycerides
Cholesterol
Epidermal Growth Factor
Protein-Tyrosine Kinases
Receptor, Epidermal Growth Factor
Triglycerides