Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia

Table 1 Summary efficacy data from published Phase II trials with pemafibrate

Citation no.	Patients	N	Dose (mg/day)	Weeks	Mean ∆ in TG (%)	Mean ∆ in HDL-C (%)
Monotherapy
[56]	Japanese patients with atherogenic dyslipidaemia^a	224	Pemafibrate	12
			0.05		↓30.9 ± 6.9***	↑11.9 ± 2.8***
			0.1		↓36.4 ± 6.6***	↑16.5 ± 2.7***
			0.2		↓42.6 ± 6.7***	↑16.3 ± 2.8***
			0.4		↓42.7 ± 6.7***	↑21.0 ± 2.8***
			Fenofibrate
			100		↓29.7 ± 6.7	↑14.3 ± 2.8
			Placebo		↑28.5 ± 6.8	↓2.3 ± 2.8
[63]	Japanese patients with atherogenic dyslipidaemia^a	526	Pemafibrate	12		↑20.3–24.7
			0.1		↓46.3***
			0.2		↓46.7***
			0.4		↓51.8***
			Fenofibrate			↑17.2–26.5
			100		↓38.3***
			200		↓51.5***
			Placebo		↓2.7
Add-on to statin
[60]	Japanese patients with TG ≥ 2.3 mmol/L	423	Pemafibrate	24
			0.2		↓46.8 ± 2.6***	↑17.6 ± 17.2***
			0.2/0.4^c		↓50.8 ± 2.5***	↑16.3 ± 14.6***
			Placebo		↓0.8 ± 3.0	↑4.4 ± 12.7
[60]	Add-on to pitavastatin Japanese patients with TG ≥ 2.3 mmol/L, non-HDL-C ≥ 3.9 mmol/L	188	Pemafibrate	12
			0.1		↓46.1 ± 3.9***	↑13.6 ± 15.4**
			0.2		↓53.4 ± 3.8***	↑19.7 ± 19.4***
			0.4		↓52.0 ± 3.9***	↑12.7 ± 19.3*
			Placebo		↓6.9 ± 4.0	↑3.4 ± 12.5
[59]	T2DM and dyslipidemia Japanese patients with TG ≥ 1.7 and < 11.3 mmol/L	167	Pemafibrate	24
			0.2		↓44.3***
			0.4		↓45.1***
			Placebo		↓10.8***
[61]	Caucasian patients, controlled LDL-C and atherogenic dyslipidaemia^b	408	Pemafibrate	12	↓34.0–54.4***	↑7.4–12.9***
[61]		408	0.1, 0.2 or 0.4	12
[62]	Caucasian type 2 diabetes patients with controlled LDL-C and atherogenic dyslipidaemia^b	161^d	Pemafibrate	12	↓44.7–67.4***	NR
[62]		161^d	0.1, 0.2 or 0.4	12

HDL-C high-density lipoprotein cholesterol, LDL-C low-density lipoprotein cholesterol, TG triglycerides, T2DM type 2 diabetes mellitus
** p < 0.01, *** p < 0.001 versus control
^aTG ≥ 2.3 mmol/L (200 mg/dL) and low HDL-C
^bTG 1.9–5.7 mmol/L (175–500 mg/dL) and low HDL-C
For both a and b, low HDL-C was defined as < 1.3 mmol/L (50 mg/dL) in men or < 1.4 mmol/L (55 mg/dL) in women
^cPatients with TG ≥ 1.7 mmol/L (150 mg/dL) at week 8 were uptitrated to 0.4 mg/day from week 12
^dSubgroup analysis of Kastelein et al. [61]

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