US-based clinical-stage biopharmaceutical company Viking Therapeutics has initiated its Phase II clinical trial of VK2809 to treat primary hypercholesterolemia and non-alcoholic fatty liver disease (NAFLD).

VK2809 is an orally administered, tissue and receptor-subtype selective agonist of the thyroid beta receptor, as well as a type of pro-drug cleaved in vivo to generate potent thyromimetics.

It selectively activates the TRß receptor in liver tissue that is instrumental in favourably affecting cholesterol and lipoprotein levels via multiple mechanisms, including increasing the expression of low-density lipoprotein (LDL) receptors and increasing mitochondrial fatty acid oxidation.

The randomised, double-blind, placebo-controlled, parallel group Phase II trial is designed to evaluate the safety, efficacy and tolerability of VK2809 while treating approximately 80 patients with elevated LDL cholesterol (LDL-C) and NAFLD.

The patients will be randomised to be administered with oral doses of VK2809 or placebo for 12 weeks on a once-daily basis, which will be followed by a four-week off-drug phase.

The trial is primarily focused on testing the efficacy of VK2809 in treating LDL-C after 12 weeks compared to placebo.

"The trial is primarily focused on testing the efficacy of VK2809 in treating LDL-C after 12 weeks compared to placebo."

The secondary and exploratory goals will be to assess changes in liver fat content, triglycerides, and inflammatory markers.

Viking CEO Brian Lian said: "This study will be critical in validating VK2809's unique liver-targeted mechanism of action, which we believe provides differentiated benefits by simultaneously reducing hepatic steatosis, an important driver of non-alcoholic steatohepatitis (NASH), and improving plasma lipid levels.

"Prior data has shown that treatment with VK2809 can lead to rapid histologic improvement in animal models of hepatic steatosis, as well as significant reductions in LDL-C, triglycerides, and atherogenic proteins in humans.”

VK2809 demonstrated efficacy in reducing triglycerides, as well as the atherogenic proteins lipoprotein-a and apolipoprotein B in patients with mild hypercholesterolemia during a Phase Ib study.

Image: Hypercholesterolemic patient with yellowish patches containing cholesterol deposits. Photo: courtesy of Bobtheowl2.