Metabolism Xagena

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Xagena Newsletter

Management of hypercholesterolemia: Mipomersen is a promising therapy

By inhibiting apolipoprotein B ( ApoB ) synthesis, Mipomersen ( Kynamro ) can significantly reduce ApoB-containing lipoproteins in hypercholesterolemic patients.

The purpose of a study was to ascertain both the extent to which Mipomersen can decrease ApoB-containing lipoproteins and the safety of Mipomersen therapy.

Studies were identified through literature search.

The efficacy endpoints were the changes in low-density lipoprotein cholesterol ( LDL-C ), non-high-density lipoprotein cholesterol ( non-HDL-C ), ApoB, and lipoprotein (a) [ Lp(a) ].
The safety endpoints were the incidence of injection-site reactions, flu-like symptoms, and elevated transaminases.

Six randomized controlled trials with 444 patients were included in the analysis. Compared with the placebo group, patients who received Mipomersen therapy had a significant reduction in LDL-C ( 33.13 % ), as well as a reduction in non-HDL-C ( 31.70% ), ApoB ( 33.27% ), and LP(a) ( 26.34% ).

Mipomersen therapy was also associated with an obvious increase in injection-site reactions with an odds ratio ( OR ) of 14.15, flu-like symptoms with an OR of 2.07, and alanine aminotransferase levels greater than or equal to 3 × the upper limit of normal with an OR of 11.21.

In conclusion, Mipomersen therapy is effective for lowering ApoB-containing lipoproteins in patients with severe hypercholesterolemia.
Future studies exploring how to minimize side effects of Mipomersen therapy are needed. ( Xagena )

Li N et al, Am J Cardiovasc Drugs 2014;14:367-376