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www.fdanews.com/articles/88610-metabasis-begins-trial-of-investigational-cholesterol-drug

METABASIS BEGINS TRIAL OF INVESTIGATIONAL CHOLESTEROL DRUG

November 3, 2006

Metabasis Therapeutics has initiated a Phase I clinical trial of MB07811, a novel, orally active product candidate for the management of hyperlipidemia, or elevated cholesterol. MB07811 uses the company's proprietary HepDirect prodrug technology to target a beta-subtype-selective thyroid hormone receptor (TRB) agonist to the liver to reduce serum cholesterol (LDL) and triglycerides (TGs). The company believes that this drug class has the potential to be additive to the statins class of hyperlipidemia drugs, and preclinical data suggests that MB07811 could be as effective at lowering serum cholesterol as statins.

The study will evaluate the safety and tolerability of MB07811 in a rising single dose study in healthy volunteers. Assuming the successful completion of additional preclinical trials and the Phase I single dose trial, the company expects to pursue further clinical studies, including a multiple-dose Phase I study in healthy volunteers.

Thyroid hormone receptor agonists are known to reduce cholesterol in animal models, but typically at doses similar to those associated with potential safety concerns, including cardiac and other non-hepatic toxicities. MB07811 is a HepDirect prodrug of a novel TRB receptor agonist discovered at Metabasis that is designed to deliver the agonist to the site where cholesterol is produced, the liver, while reducing the exposure of the agonist to other tissues.