Treatment With WelChol(R) (Colesevelam Hydrochloride) May Lead To Increased LDL Particle Size For Patients With Moderate Hypercholesterolemia

Market Wire, 20050229

Sankyo Pharma Inc. announced today that WelChol, at the recommended starting daily dosage (3.8g), significantly increased low-density lipoprotein - cholesterol (LDL-C) particle size from baseline. The results of this analysis were presented recently at the European Atherosclerosis Society's 73rd Congress in Salzburg, Austria. In addition, investigators found that WelChol produced statistically significant reductions in LDL cholesterol (the "bad" cholesterol) and total cholesterol (2).

Analyses of published studies reported that the presence of small, dense LDL-C particles is associated with an increased risk of coronary heart disease (CHD). Patients with ischemic heart disease (heart problems caused by narrowed heart arteries) have a higher proportion of small, dense LDL-C particles than do healthy patients (3),(4).

Peter H. Jones MD, study investigator and Associate Professor of Medicine, Baylor College of Medicine, Houston, noted, "Although lowering LDL-cholesterol remains the primary goal of lipid management, small, dense LDL-C particles are a significant residual risk factor for cardiovascular disease."

For patients with moderate hypercholesterolemia, treatment with WelChol at the recommended starting dose may lead to an improved particle size distribution.

About the Study

In this multi-center, double-blind, placebo-controlled study, 149 patients with moderate hypercholesterolemia (LDL-C greater than or equal to 160 mg/dL; triglycerides less than or equal to 300 mg/dL) were randomized to WelChol (1.5-3.8 g) or placebo daily for 6 weeks. The primary endpoint was the percent change in LDL-C from baseline. Administration of WelChol resulted in a dose-dependent reduction in LDL-C (these results have been previously published).

Additionally, the effects of WelChol (colesevelam hydrochloride) on LDL-C particle size were assessed by NMR*. WelChol had negligible effects on LDL particle size at doses up to 3.0 g daily. However, at the recommended daily starting dose (3.8 g), WelChol significantly increased LDL-C particle size from baseline (1.1% increase, P less than 0.05 vs. 0.22% increase with placebo, P=NS**)(5).

About WelChol

WelChol, available by prescription only, effectively lowers LDL cholesterol by an average of 15-18% (depending on dose)(6) and is the only lipid-lowering agent that is FDA-approved for combination use with any dose of any statin. Administered alone or in combination with a statin, WelChol is indicated as adjunctive therapy to diet and exercise for the reduction of elevated cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa) when diet and exercise alone are not adequate. The effects of WelChol either alone or with a statin on cardiovascular morbidity and mortality have not been determined.

WelChol is non-systemic which means it is not absorbed into the blood stream. In addition, WelChol is well tolerated. The most common side effects (less than 5%) versus placebo (sugar pill) are gas (12% vs. 14%), constipation (11% vs. 7%), and upset stomach (8% vs. 3%). Patients who have bowel blockage should not take WelChol. Also, liver-function monitoring is not required with WelChol, and in combination with a statin, no additional liver-function monitoring is required beyond that which is required for the prescribed statin alone. As with all medications, patients should always let their healthcare provider know about the medications and supplements they are taking.

For more information on WelChol, call 877-4-SANKYO (877-472-6596), or go to the WelChol web site at www.welchol.com.

About Sankyo

Sankyo Pharma Inc. is dedicated to developing and marketing important pharmaceutical products for the U.S. market. Sankyo Pharma has offices in New York and New Jersey with a Research Institute in California.

Anational sales force of 550 representatives promotes Sankyo Pharma products, and they are supported by dedicated managed care and field-based medical personnel.

Sankyo Pharma launched WelChol(R)(colesevelam hydrochloride) in September 2000. In less than 12 months after launch, WelChol vaulted to the number one position in its class, with first full-year sales exceeding $90 million in 2001.

In addition, Sankyo Pharma developed Benicar(TM) (olmesartan medoxomil), an angiotensin II receptor blocker (ARB) indicated for the treatment of hypertension. Sankyo Pharma co-promotes Benicar, with Forest Laboratories. Benicar effectively lowers diastolic and systolic blood pressure in patients who suffer from hypertension. Benicar is not recommended for use in pregnant women. Please see full product information including boxed warning about use in pregnancy.

Sankyo Pharma also markets and distributes the GlucoWatch(R) G2(TM) Biographer (manufactured by Cygnus, Inc.), the first and only monitoring system that provides glucose readings continuously, automatically and non-invasively.

Sankyo Pharma's parent company, Sankyo Co. Ltd. of Tokyo, is Japan's second largest pharmaceutical company, with annual worldwide sales of $4.5 billion. Sankyo has a long history of discovering new classes of drugs, including the statin class of lipid-lowering drugs, with its discovery of the first statin, mevastatin, and the co-discovery of lovastatin, the first statin to be marketed. Additionally, Sankyo discovered, co-developed and manufactures pravastatin sodium. Sankyo independently markets pravastatin sodium throughout the world and through its licensee, Bristol-Myers Squibb. Pravastatin sodium is marketed as Pravachol(R) in the United States.