Phase 1 Studies Show Promise of QuatRx's Novel Compound,Sobetirome, for Lowering LDL Cholesterol LevelsResults from two separate Phase 1 studies show sobetirome, a selective thyroid hormone receptor beta agonist, reduced levels of low-density lipoprotein versus placebo
ANN ARBOR, Mich., January 29, 2008 /PRNewswire/ -- QuatRx Pharmaceuticals, a privately-held biopharmaceutical company developing compounds for the treatment of major endocrine, metabolic and cardiovascular diseases, today announced results from two Phase 1 clinical studies with its novel lipid lowering compound, sobetirome (formerly QRX-431), in development for the treatment of elevated LDL cholesterol (also known as "bad cholesterol") levels. The results of the studies indicated LDL lowering with both single and multiple doses of sobetirome in a healthy volunteer population not enriched for elevated LDL levels. Sobetirome was generally well tolerated in both studies. Sobetirome is a new selective thyroid hormone receptor beta agonist that may activate reverse cholesterol transport.
"We are excited and extremely encouraged by these Phase 1 results indicating that sobetirome was generally well tolerated and showed lowering of LDL levels. We look forward to replicating these results in larger Phase 2 and 3 trials. We believe this new compound has potential as monotherapy or in combination with statins for the many patients who are unable to tolerate current therapies or who fail to achieve lipid treatment goals with statins alone," said Robert L. Zerbe, M.D., chief executive officer and president of QuatRx.
Lipid-lowering effects in both single and multiple doses were seen in the randomized, double-blind, placebo-controlled Phase 1 studies of sobetirome. In the single dose study of 32 subjects, low-density lipoprotein (LDL) cholesterol levels decreased by up to 22% in subjects receiving up to 450 micrograms of sobetirome, compared to 2% in subjects who received placebo. The greatest reductions were observed 72 hours after dosing. In the multiple dose study of 24 subjects over two weeks, reductions in LDL cholesterol levels decreased up to 41% at doses up to 100 micrograms once a day, compared to an overall 5% reduction for placebo. Subjects, who were not enriched for LDL levels, followed a low-cholesterol diet starting one week prior to randomization and then received sobetirome or placebo. Sobetirome was generally well tolerated in both studies.
In published preclinical studies in primates, sobetirome has been shown to lower LDL cholesterol and Lp(a) and to promote weight loss. Lp(a) is a lipoprotein that is associated with an increased risk of stroke and coronary heart disease. In preclinical studies in mice, sobetirome also stimulated steps of reverse cholesterol transport. This process involves the transport of cholesterol from peripheral tissues to the liver for conversion into bile acids and then excretion from the body.
LDL Cholesterol, Cardiovascular Disease and Current Treatments
High LDL cholesterol levels have been shown to increase the risk of cardiovascular 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 to reduce cardiovascular risk is a primary focus of currently available lipid regulating therapies, of which statins are the most frequently prescribed class. While statins have been shown to lower LDL levels in many people with high LDL cholesterol, some patients are unable to tolerate statins due to side effects and many others fail to reach their LDL treatment targets in treatment involving statins alone. In addition, a substantial number of patients with elevated LDL levels also have other cardiovascular risk factors such as obesity, high Lp(a) and high triglycerides, which are not adequately addressed by statin therapy. In all of these sizable patient sub-populations, there is a need for new treatment options beyond statins.
QuatRx Pharmaceuticals is focused on the discovery, licensing, development and commercialization of compounds in the endocrine, metabolic and cardiovascular therapeutic areas. In addition to sobetirome, QuatRx has three other product candidates in active clinical development and two preclinical development programs. Ophena(TM) which recently met all co-primary endpoints in a large, pivotal Phase 3 clinical trial, is a potential estrogen-free therapy for post-menopausal vaginal syndrome, a common problem that results from thinning of vaginal tissues associated with estrogen deficiency of menopause. Fispemifene is a new, selective estrogen receptor antagonist that is in Phase 2 studies as an oral treatment for testosterone deficiency and associated disorders in men. Becocalcidiol, a patented Vitamin D analogue, is in Phase 2 clinical trials for the treatment of psoriasis through QuatRx's licensee, CollaGenex Pharmaceuticals, Inc. QuatRx's two preclinical small molecule programs are designed to address common endocrine disorders in women.
Posted: January 2008
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