In two 12-week studies, ezetimibe monotherapy significantly decreased
plasma LDL-C levels and increased plasma HDL-C levels, with a
tolerability profile similar to that of placebo. The 10-mg dose of
ezetimibe provided greater benefit on LDL-C blood level reduction
compared with 5 mg, without affecting tolerability and without any
significant increase in adverse events. Therefore, the 10-mg dose of
ezetimibe was chosen as the only dose for phase III clinical trials.
The 10-mg dose of ezetimibe was subsequently submitted to the FDA for
approval in December 2001 and was approved for clinical use in November
HE, Moore PB, Drehobl MA, et al., for the Ezetimibe Study Group.
Effectiveness and tolerability of ezetimibe in patients with primary
hypercholesterolemia: pooled analysis of two phase II studies. Clin