Viking Therapeutics Inc (VKTX)

[XenaLives]

VK2809
Selective Thyroid Receptor-ß Agonist
Liver Disorders


Overview & Profile
We are developing a unique series of selective thyroid hormone receptor beta (TRß) agonists for metabolic disorders. Our lead candidate, VK2809, is a novel, orally available small molecule thyroid hormone receptor agonist that possesses selectivity for liver tissue, as well as the beta receptor subtype, suggesting promise for the treatment of metabolic disorders, including non-alcoholic steatohepatitis (NASH). The liver-targeting properties of our TRß agonists are designed to reduce or eliminate the deleterious effects of extra-hepatic thyroid receptor activation. In particular, high tissue and TRß selectivity may lead to reduced activity at the TRa receptor, which can be associated with increased respiration and cardiac tissue hypertrophy.

Thyroid hormones are known to reduce body mass, affect growth, modulate lipid metabolism and impact the functions of multiple organs in humans. Their physiologic activity is derived from binding to hormonal receptors located in the nuclei of cells (nuclear hormone receptors). Characteristics of thyroid hormone activity that are of importance to drug development include the ability to reduce atherogenic lipids associated with cardiovascular disease and induce an increase in metabolism, resulting in weight loss. Patients with abnormally high or low thyroid hormone levels demonstrate clinical profiles consistent with these characteristics. Numerous animal models have provided further support of these physiologic effects.

thyroid-receptor-overview
Graphic: Harrison’s Principles of Internal Medicine, 17th Edition, Chapter 335, Fig 335-4, copyright McGraw-Hill, 2008.
Thyroid Receptor Subtypes

https://www.vikingtherapeutics.com/pipeline/metabolic-disease-program/