Magazine article Drug Topics

New Drug Approval May Awaken Older Antihyperlipidemic Class

Magazine article Drug Topics

New Drug Approval May Awaken Older Antihyperlipidemic Class

Article excerpt

Irom the looks of what just 1 emerged from the pipeline, an old-time antihyperlipidemic class could be making a comeback. WelChol (colesevelam HCl), a bile acid binding agent, has been approved as adjunctive therapy to diet and exercise for reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia.

Bile acid resins generally carry the appeal of a strong safety record and a mechanism of action that is synergistic with other therapies. The class is known to bind bile acids in the intestinal lumen, disrupting their enterohepatic recirculation. As the bile acid pool becomes depleted, the liver is stimulated to convert hepatocellular cholesterol into bile acids.

This process causes an increased demand of cholesterol in the liver cells, which prompts the synthesis of LDL receptors. These effects result in increased clearance of LDL cholesterol in the blood, resulting in decreased serum LDL levels. Since resins are not absorbed from the gastrointestinal tract, they lack systemic toxicity, but they are chock full of other types of side effects. The class is known for its frequent GI symptoms, such as constipation, bloating, epigastric fullness, nausea, and flatulence.

Michael Davidson, M.D., said that "colesevelam has a higher affinity for bile acids and, therefore, may have greater potency and fewer GI side effects, compared with other bile and resins." Davidson, an assistant professor in the department of Medicine at Rush Presbyterian-St. Luke's Medical Center, claims that colesevelam's incidence of GI side effects is similar to that of placebo. …

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