The study will evaluate the safety and tolerability of MB07811. 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).
Metabasis believes that this drug class has the potential to be additive to the class of hyperlipidemia drugs known as “statins”, and preclinical data suggests that MB07811 could be as effective at lowering serum cholesterol as this important drug class. At present statins represent a drug class that is the single largest pharmaceutical market in the world, growing by over 15% per year.
MB07811 is designed to deliver the agonist to the liver, the site where cholesterol is produced, while reducing the exposure of the agonist to other tissues. The company believes that liver-targeting may avoid the safety concerns previously seen with non-liver targeted TRB agonists.
Patients with hyperlipidemia, a clinical condition characterized by an elevation of cholesterol and/or triglycerides in the bloodstream, are at greater risk of cardiovascular disease and of experiencing a heart attack or stroke.
Although effective for treating many patients with elevated LDL cholesterol, statins have little affect on TGs, and can cause side effects.
In preclinical studies, Metabasis demonstrated that MB07811 lowers LDL cholesterol with a significantly improved safety profile relative to non-liver targeted TRB agonists. Preclinical studies have also shown that MB07811 results in decreased triglycerides.
“The HepDirect technology is currently used in pradefovir and MB07133, two product candidates that are currently in clinical trials for the treatment of hepatitis B and primary liver cancer, respectively. Clinical data to date on both of these promising product candidates have provided evidence that the HepDirect technology is targeting drugs to the liver, as expected,” commented Dr Mark Erion, chief scientific officer of Metabasis.