Alirocumab Reduces Cholesterol in Phase III Study
Treatment more effective than ezetimibe (October 16)
The phase III ODYSSEY MONO study of alirocumab (Sanofi/Regeneron), an investigational, fully human monoclonal antibody targeting PCSK9 (proprotein convertase subtilisin/kexin type 9), has met its primary efficacy endpoint.
The mean reduction in low-density lipoprotein cholesterol (LDL-C, or “bad” cholesterol) from baseline to week 24 — the trial’s primary efficacy endpoint — was significantly greater in patients treated with alirocumab compared with those treated with ezetimibe (Zetia, Merck) (47.2% vs. 15.6%, respectively; P < 0.0001). In the study, which included up-titration for patients who did not achieve an LDL-C level of 70 mg/dL, most of the patients continued to be treated with the initial low dose of alirocumab (75 mg).
Treatment-emergent adverse events (AEs) were reported in 69.2% of the alirocumab group and in 78.4% of the ezetimibe group. The most common type of AEs was infections (42.3% with alirocumab vs. 39.2% with ezetimibe), which included nasopharyngitis, influenza, and upper respiratory tract infections. Injection-site reactions occurred in fewer than 2% of patients in both groups. Muscle-related AEs occurred in 3.8% of patients treated with alirocumab and in 3.9% of patients treated with ezetimibe.
Alirocumab is administered via subcutaneous injection. By blocking PCSK9 — a determinant of circulating LDL-C levels in the blood — alirocumab increases the number of LDL receptors on hepatocytes, thereby lowering LDL-C levels.
Source: Regeneron; October 16, 2013.