MGL-3196 (VIA-3196) photo credit The haystack http://cenblog.org/the-haystack/tag/mgl-3196/
Madrigal Pharmaceuticals, acquired from VIA Pharmaceuticals, licensed from Roche to treat high cholesterol/high triglycerides , it mimics thyroid hormone, targeted to thyroid hormone receptor beta in the liver
Specifically, MGL-3196 is a thyroid hormone analog, designed to target a thyroid hormone receptor in the liver. These receptors regulate genes involved in cholesterol regulation and metabolism.
MGL-3196 is an orally administered, small-molecule liver-directed ß-selective THR agonist designed to specifically target receptors in the liver involved in metabolism and cholesterol regulation, and avoid side effects associated with thyroid hormone receptor activation outside the liver, including those mediated by THR-α receptors. MGL-3196 has currently completed Phase I single and multiple dose trials in healthy volunteers. MGL-3196 is being developed for dyslipidemia/hypercholesterolemia to lower LDL cholesterol, triglyceride levels and Lp(a), and was inlicensed from Roche Pharmaceuticals. MGL-3196 has excellent safety in comparative studies with other THR agonists tested previously because of MGL-3196’s high liver uptake and high ß-selectivity and nearly complete lack of THR-α activity.
MGL-3196 has completed a single ascending dose study in healthy volunteers in which the compound appeared safe at all doses tested. The multiple ascending dose study in healthy volunteers with mildly elevated LDL cholesterol was completed in October 2012 and provided additional safety and pharmacodynamic information. The Phase I multiple dose, proof of concept study enrolled 48 healthy volunteers with mildly elevated LDL cholesterol to evaluate the safety, pharmacokinetics and pharmacodynamics of MGL-3196 after two weeks of daily dosing. Results showed that MGL-3196 was well tolerated and appeared safe at all doses tested. Daily doses of 50-200 mg showed highly statistically significant reductions relative to placebo of up to 30% LDL-cholesterol (p=.05-<.0001; 28%, non-HDL cholesterol (p=.027-.0001); 24% Apolipoprotein B (p=.008-.0004); and strong trends and up to 60% reduction of triglycerides (range, p=.13-.016).