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New review of pemafibrate, novel SPPARMalpha

Selective peroxisome proliferator-activated receptor alpha modulators (SPPARM?) may offer a novel therapeutic approach to the management of atherogenic dyslipidaemia. The concept of SPPARM? is that by modulating the unique receptor–cofactor binding profile of PPARalpha, it is possible to improve potency and selectivity while at the same time avoiding unwanted side effects of the fibrates.
This review summarizes the experimental and clinical evidence for pemafibrate (K-877), a novel SPPARM?. In clinical trials, treatment with pemafibrate led to marked reduction of triglycerides, remnant cholesterol and apolipoprotein CIII, together with an increase in high-density lipoprotein cholesterol. Whether pemafibrate, against a background of intensive statin therapy, is able to reduce the residual risk of cardiovascular events in patients with type 2 diabetes and atherogenic dyslipidaemia, will be addressed by the PROMINENT (Pemafibrate to Reduce cardiovascular OutcoMes by reducing triglycerides IN diabetic patiENTs) study. PROMINENT aims to recruit 10,000 patients with type 2 diabetes mellitus, with and without cardiovascular disease, who will be randomized to treatment with pemafibrate 0.4 mg/day or placebo. The primary study outcome is a composite of nonfatal myocardial infarction, nonfatal ischaemic stroke, hospitalization for unstable angina requiring unplanned coronary revascularization, or cardiovascular death. Results are not expected until 2022.
Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia.

Fruchart JCF.