Background: Hyperlipidemia is a worldwide problem related to cardiovascular disease (CVD) and sudden death. Low-density lipoprotein cholesterol (LDL-C) has been treated well by the use of statins, but hypertriglyceridemia was not the case. Previous fibrates have been shown a certain effect of preventing CVD events, but some remain not enough or even could cause adverse events. Pemafibrate is a selective peroxisome proliferator-activated receptor α modulator (SPPARMα) with the potential to reduce high triglycerides. To evaluate the clinical effectiveness and safety profile of Pemafibrate, we have started with half dose once-daily administration.

Methods: Thirty-three patients with hypertriglyceridemia, triglyceride (TG) levels > 150 mg/dL, were treated with Pemafibrate (0.1 mg, once daily) from July 2018 to February 2019. Changes in TG (non-fasting) and LDL-C, high-density lipoprotein cholesterol (HDL-C), aspartate aminotransferase (AST), alanine aminotransferase (ALT), creatine kinase (CK), creatinine (Cre), blood glucose (PBG) (postprandial), hemoglobin A1c (HbA1c), and body weight (BW) levels were investigated, compared to the baseline levels of the previous visit.

Results: Of the 33 patients, 11 were using other fibrates before. Nine were given statins along with. Baseline TG was 285.0 (210.5 - 423.0) mg/dL, LDL-C 116.4 ± 33.4 mg/dL, and HDL-C 46.5 ± 12.5 mg/dL. TG changes were statistically significant (-20.8 ± 47.6%; P < 0.01). Patients with TG > 200 mg/dL, who used fibrates for the first time, experienced the most significant changes in TG levels (-34.5 ± 37.2%; P < 0.01). In patients using statins already, TG reduction was relatively less, compared to those not using statins (-25.4 ± 36.1%; P < 0.01). HDL-C increased by 3.9 ± 10.2 mg/dL (P < 0.05). LDL-C increased by 16.6 ± 23.7 mg/dL (P < 0.001) in patients not using statins, while patients using statins did not show such significant change. AST, ALT, CK, Cre, PBG, HbA1c and BW did not significantly change.

Conclusions: A selective PPARα modulator, Pemafibrate, effectively improved hypertriglyceridemia without major adverse events in real practice, with half dose once-daily administration. Combined use of statins might be a potent therapeutic maneuver for dyslipidemia.