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Colesevelam

In Pediatric Patients with Heterozygous Familial Hypercholesterolemia

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Abstract

Colesevelam hydrochloride (colesevelam), a non-absorbed, synthetic, lipid-lowering polymer, is a bile acid sequestrant. Colesevelam binds with high affinity to bile acids within the gastrointestinal tract, thereby inhibiting the reabsorption of bile acids, resulting in decreases in serum low-density lipoprotein cholesterol (LDL-C) levels.

Colesevelam is available as tablets and as powder for oral suspension. At dosages of 3.75 g once daily or 1.875 g twice daily, colesevelam is approved in the US for the treatment of pediatric patients aged 10–17 years with heterozygous familial hypercholesterolemia. Colesevelam may be administered as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin).

A 32-week trial was conducted and consisted of a stablilization period (≈4 weeks), a randomized period (8 weeks), an open-label period (18 weeks), and a 2-week follow-up period. In the 8-week, randomized, double-blind, placebo-controlled period of the trial, colesevelam (tablets), as monotherapy or with a statin, was an effective treatment for pediatric patients with heterozygous familial hypercholesterolemia. At week 8, recipients of colesevelam 3.75 g/day had significant percentage reductions from baseline in mean LDL-C levels (primary endpoint) compared with placebo recipients.

Significant beneficial treatment effects for colesevelam 3.75 g/day versus placebo were also reported for several other lipid/lipoprotein parameters at week 8 of the study. The reported treatment effects on lipid/lipoprotein parameters were maintained over a subsequent 18-week, open-label, noncomparative period, when all patients received colesevelam 3.75 g/day.

Colesevelam 3.75 g/day was generally well tolerated for up to 26 weeks by pediatric patients with heterozygous familial hypercholesterolemia.

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Acknowledgments and Disclosures

The manuscript was reviewed by: A.S. Wierzbicki, Department of Chemical Pathology, Guy’s and St Thomas’ Hospitals, London, England.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand

    Caroline M. Perry

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  1. Caroline M. Perry
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Correspondence to Caroline M. Perry.

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Perry, C.M. Colesevelam. Pediatr-Drugs 12, 133–140 (2010). https://doi.org/10.2165/11204890-000000000-00000

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