Phase 1 Studies Show Promise of QuatRx's Novel Compound, Sobetirome, for Lowering LDL Cholesterol Levels

Thursday, January 31, 2008 General News
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ANN ARBOR, Mich., Jan. 29 QuatRx Pharmaceuticals, aprivately-held biopharmaceutical company developing compounds for thetreatment of major endocrine, metabolic and cardiovascular diseases, todayannounced results from two Phase 1 clinical studies with its novel lipidlowering compound, sobetirome (formerly QRX-431), in development for thetreatment of elevated LDL cholesterol (also known as "bad cholesterol")levels. The results of the studies indicated LDL lowering with both singleand multiple doses of sobetirome in a healthy volunteer population notenriched for elevated LDL levels. Sobetirome was generally well tolerated inboth studies. Sobetirome is a new selective thyroid hormone receptor betaagonist that may activate reverse cholesterol transport.

"We are excited and extremely encouraged by these Phase 1 resultsindicating that sobetirome was generally well tolerated and showed lowering ofLDL levels. We look forward to replicating these results in larger Phase 2and 3 trials. We believe this new compound has potential as monotherapy or incombination with statins for the many patients who are unable to toleratecurrent therapies or who fail to achieve lipid treatment goals with statinsalone," said Robert L. Zerbe, M.D., chief executive officer and president ofQuatRx.

Study Results

Lipid-lowering effects in both single and multiple doses were seen in therandomized, double-blind, placebo-controlled Phase 1 studies of sobetirome. Inthe single dose study of 32 subjects, low-density lipoprotein (LDL)cholesterol levels decreased by up to 22% in subjects receiving up to 450micrograms of sobetirome, compared to 2% in subjects who received placebo. Thegreatest reductions were observed 72 hours after dosing. In the multiple dosestudy of 24 subjects over two weeks, reductions in LDL cholesterol levelsdecreased up to 41% at doses up to 100 micrograms once a day, compared to anoverall 5% reduction for placebo. Subjects, who were not enriched for LDLlevels, followed a low-cholesterol diet starting one week prior torandomization and then received sobetirome or placebo. Sobetirome wasgenerally well tolerated in both studies.

In published preclinical studies in primates, sobetirome has been shown tolower LDL cholesterol and Lp(a) and to promote weight loss. Lp(a) is alipoprotein that is associated with an increased risk of stroke and coronaryheart disease. In preclinical studies in mice, sobetirome also stimulatedsteps of reverse cholesterol transport. This process involves the transportof cholesterol from peripheral tissues to the liver for conversion into bileacids and then excretion from the body.

LDL Cholesterol, Cardiovascular Disease and Current Treatments

High LDL cholesterol levels have been shown to increase the risk ofcardiovascular disease including coronary heart disease and stroke.Approximately 70 million Americans have some form of cardiovascular disease,according to the American Heart Association. Lowering LDL cholesterol toreduce cardiovascular risk is a primary focus of currently available lipidregulating therapies, of which statins are the most frequently prescribedclass. While statins have been shown to lower LDL levels in many people withhigh LDL cholesterol, some patients are unable to tolerate statins due to sideeffects and many others fail to reach their LDL treatment targets in treatmentinvolving statins alone. In addition, a substantial number of patients withelevated LDL levels also have other cardiovascular risk factors such asobesity, high Lp(a) and high triglycerides, which are not adequately addressedby statin therapy. In all of these sizable patient sub-populations, there isa need for new treatment options beyond statins.

About QuatRx

QuatRx Pharmaceuticals is focused on the discovery, licensing, developmentand commercialization of compounds in the endocrine, metabolic andcardiovascul

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