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首页> 美国卫生研究院文献>Springer Open Choice >Niacin Alternatives for Dyslipidemia: Fool’s Gold or Gold Mine? Part II: Novel Niacin Mimetics
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Niacin Alternatives for Dyslipidemia: Fool’s Gold or Gold Mine? Part II: Novel Niacin Mimetics

机译：烟酸替代血脂异常的方法：傻瓜的金矿还是金矿？第二部分：新型烟酸模拟物

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摘要

Two cardiovascular outcome trials established niacin 3 g daily prevents hard cardiac events. However, as detailed in part I of this series, an extended-release (ER) alternative at only 2 g nightly demonstrated no comparable benefits in two outcome trials, implying the alternative is not equivalent to the established cardioprotective regimen. Since statins leave a significant treatment gap, this presents a major opportunity for developers. Importantly, the established regimen is cardioprotective, so the pathway is likely beneficial. Moreover, though effective, the established cardioprotective regimen is cumbersome, limiting clinical use. At the same time, the ER alternative has been thoroughly discredited as a viable substitute for the established cardioprotective regimen. Therefore, by exploiting the pathway and skillfully avoiding the problems with the established cardioprotective regimen and the ER alternative, developers could validate cardioprotective variations facing little meaningful competition from their predecessors. Thus, shrewd developers could effectively tap into a gold mine at the grave of the ER alternative. The GPR109A receptor was discovered a decade ago, leading to a large body of evidence commending the niacin pathway to a lower cardiovascular risk beyond statins. While mediating niacin’s most prominent adverse effects, GPR109A also seems to mediate anti-lipolytic, anti-inflammatory, and anti-atherogenic effects of niacin. Several developers are investing heavily in novel strategies to exploit niacin’s therapeutic pathways. These include selective GPR109A receptor agonists, niacin prodrugs, and a niacin metabolite, with encouraging early phase human data. In part II of this review, we summarize the accumulated results of these early phase studies of emerging niacin mimetics.
机译：两项心血管结果试验确定每天烟酸3克可预防硬性心脏事件。但是，正如本系列第一部分中详细介绍的那样，每晚两次仅2 g的缓释（ER）替代品在两项结果试验中均未显示出可比的益处，这意味着该替代品不等同于既定的心脏保护方案。由于他汀类药物存在重大的治疗缺口，因此为开发人员提供了重大机遇。重要的是，已建立的方案对心脏有保护作用，因此该途径可能是有益的。而且，尽管有效，但是建立的心脏保护方案繁琐，限制了临床使用。同时，ER替代品已被完全公认为替代已确立的心脏保护方案的可行替代品。因此，通过开发途径并熟练地避免已建立的心脏保护方案和ER替代方案所带来的问题，开发人员可以验证几乎没有来自其前辈的有意义竞争的心脏保护变异。因此，精明的开发人员可以有效地利用ER替代方案的坟墓开采金矿。 GPR109A受体是在十年前发现的，导致大量证据表明烟酸途径可降低他汀类药物的心血管风险。 GPR109A在介导烟酸最主要的不利影响的同时，也似乎在介导烟酸的抗脂解，抗炎和抗动脉粥样硬化作用。一些开发商正在大力投资开发烟酸治疗途径的新策略。这些药物包括选择性的GPR109A受体激动剂，烟酸前药和烟酸代谢物，可提供早期人类数据。在这篇综述的第二部分中，我们总结了新兴的烟酸模拟物这些早期研究的累积结果。

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