US-based biopharmaceutical firm Esperion Therapeutics has dosed the first patient in its Phase II clinical trial of ETC-1002 to treat patients with hypercholesterolemia and hypertension, ETC-1002-014.
ETC-1002 is an orally available, once-daily small molecule designed to lower levels of LDL-cholesterol and to avoid side-effects associated with existing LDL-cholesterol lowering therapies.
Around 144 patients are expected to be enrolled in the randomised, double-blind, parallel group, multicentre trial, which is evaluating parallel doses of ETC-1002 in these patients.
Top-line results from the Phase III trial are expected to be reported in the second quarter of 2015.
Esperion president and chief executive officer Tim Mayleben said: "Many patients with high LDL-cholesterol levels also have hypertension.
"This clinical study will help to further elucidate the LDL-cholesterol lowering efficacy, safety and tolerability profile of ETC-1002 in patients with both hypercholesterolemia and hypertension."
The primary objective of the trial is to evaluate the LDL-cholesterol lowering efficacy of ETC-1002 monotherapy versus placebo in patients with both hypercholesterolemia and hypertension who are treated for six weeks.
The trial’s secondary objectives include evaluating the effect of ETC-1002 on blood pressure, other lipid and cardiometabolic biomarkers and characterising the tolerability and safety of ETC-1002.
The dual mechanism of action in ETC-1002 helps in regulating both lipid and carbohydrate metabolism.
ETC-1002 works by inhibiting ATP citrate lyase (ACL), a key enzyme in the cholesterol biosynthetic pathway as well as activates a complementary enzyme, 5′-adenosine monophosphate-activated protein kinase (AMPK).
Both enzymes are said to play major roles in the synthesis of cholesterol and glucose in the liver.
According to the company, ETC-1002 inhibits cholesterol synthesis in the liver and causes the liver to take up LDL particles from the blood, which reduces LDL-cholesterol levels.
In seven completed Phase I and II clinical trials carried out in more than 300 patients, ETC-1002 had shown consistent and clinically meaningful reductions in LDL-cholesterol, as well as reductions in levels of high sensitivity C-reactive protein (hsCRP), a key marker of inflammation associated with cardiovascular disease.
The company is focused on developing and commercialising first-in-class, oral, low-density lipoprotein cholesterol (LDL-cholesterol) lowering therapies for the treatment of patients with hypercholesterolemia and other cardiometabolic risk markers.