Cardiology University of Cincinnati, Sterling Research Group , 375 Glensprings Dr. 2nd Floor, Cincinnati, OH 45246 USA +1 513 671 8080 ; +1 513 671 8090
Expert Opin Pharmacother. 2015 Jan;16(1):123-33. doi: 10.1517/14656566.2015.991307. Epub 2014 Dec 5.
ω-3 carboxylic acids (ω3 CA), also called ω3 free fatty acids (ω3 FFA), with the trade name Epanova™ is a new formulation of eicosapentaenoic acid (EPA) + docosahexaenoic acid (DHA) approved for the treatment of severe hypertriglyceridemia. The FFA form of EPA and DHA is associated with higher bioavailability than other forms of ω3 fatty acids, potentially resulting in efficacy at lower doses and less dependence on meal relationship.
The efficacy and safety of ω3 CA from clinical trials as well as PK and PD data will be reviewed. The mechanism of action of ω3 fatty acids in the lowering of triglycerides (TG) will be discussed and comparison is made with ω3 ethyl ester compounds.
ω3 CA are a unique form of ω3 fatty acids that appear safe and effective in lowering serum TG and offer the possibility of better patient compliance due to lower-dose efficacy and the ability to take with or without food. ω3 CA lowered TG by 26 and 31% for the 2 and 4 g/day doses, respectively, and Apo CIII was also lowered 11 and 14%, respectively, as well.
ω-3 羧酸(ω3CA),也称为 ω3 游离脂肪酸(ω3FFA),商品名为 Epanova™,是一种新的二十碳五烯酸(EPA)+二十二碳六烯酸(DHA)配方,用于治疗严重的高甘油三酯血症。与其他形式的 ω3 脂肪酸相比,EPA 和 DHA 的 FFA 形式具有更高的生物利用度,可能导致在更低剂量下具有疗效,并且对进餐时间的依赖性更小。
将从临床试验中回顾 ω3CA 的疗效和安全性以及 PK 和 PD 数据。将讨论 ω3 脂肪酸降低甘油三酯(TG)的作用机制,并与 ω3 乙酯化合物进行比较。
ω3CA 是一种独特的 ω3 脂肪酸形式,似乎在降低血清 TG 方面既安全又有效,并由于疗效更高的低剂量和能够随餐或不随餐服用,从而有可能提高患者的依从性。ω3CA 分别使 2g/天和 4g/天剂量的 TG 降低了 26%和 31%,Apo CIII 也分别降低了 11%和 14%。