A recent study entitled “Ezetimibe ameliorates atherogenic lipids profiles, insulin resistance and hepatocyte growth factor in obese patients with hypercholesterolemia”, showed the effects of the drug ezetimibe on specific biomarkers in obese Japanese patients. Ezetimibe is a drug that lowers cholesterol levels by inhibiting the intestinal absorption of cholesterol. This drug can be used alone or in combination with other drugs to treat hypercholesterolemia.
The study, published in the journal Lipids in Health and Disease, aimed to determine the level of specific biomarkers in Japanese obese subjects upon treatment with ezetimibe either in monotherapy or in combined therapy.
The study was named ERASE METS (Effects on Regression of AtheroSclerotic risks by Ezetimibe for the patients with METabolic Syndrome) and included 91 patients (39 males and 52 females) registered at the Kurume University Hospital, or nearby clinics, in Japan in 2011-2012. All patients were over 20 years old, obese (body mass index ≥ 25 kg/m2) and with hypercholesterolemia [low-density lipoprotein (LDL) cholesterol ≥ 120 mg/dL]. The patients were treated with 10 mg ezetimibe once a day for 24 weeks and then assessed at 12 and 24 weeks. The patients on ezetimibe monotherapy (n = 71) were not given any other drug, while the patients on combined therapy (n = 20) were given a statin (also a cholesterol-lowering drug). Blood was collected for determination of several parameters: lipid profiles [total cholesterol, LDL cholesterol, triglycerides, high-density lipoprotein (HDL) cholesterol, non-HDL cholesterol and remnant-like particle (RLP) cholesterol], free fatty acid (FFA), fasting immune-reactive insulin (IRI), aldosterone, hepatocyte growth factor (HGF), among others.
The results showed that after 12 weeks of ezetimibe therapy, the body mass index (BMI), waist circumference, total cholesterol, LDL cholesterol, non HDL cholesterol, triglycerides and RLP cholesterol were significantly decreased. After 24 weeks, the same parameters were still significantly decreased, in addition to a decrease in the levels of insulin and HGF. The authors suggest that this is the first study showing that ezetimibe treatment reduces HGF levels in obese patients with hypercholesterolemia. High HGF levels have been reported before to be strongly associated with metabolic syndrome. Regarding monotherapy vs combine therapy, the authors of the study did not find major differences, except on the reduction of insulin levels, where ezetimibe monotherapy was more effective than the combined therapy.
In contrast to this decrease in several of the parameters tested, HDL cholesterol showed a significant increase 24 weeks after ezetimibe therapy. It is important to highlight that cholesterol is an essential fat in our body and that HDL cholesterol is generally known as the “good cholesterol” as its high levels are associated with a reduced risk for heart disease.
Based on their observations, and although with some limitations, the researchers concluded that ezetimibe improves lipid profiles, thus minimizing the risk of formation of fatty deposits in the arteries. Furthermore, ezetimibe also seems to improve anthropometric factors (such as BMI and waist circumference), insulin resistance and biomarkers like HGF. The authors believe that ezetimibe may have several effects on obese patients with hypercholesterolemia and that this is a subject that deserves further investigation.