Oliceridine, a G protein-selective ligand at the μ-opioid receptor, for the management of moderate to severe acute pain
Oliceridine, a G protein-selective ligand at the μ-opioid receptor, for the management of moderate to severe acute pain
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DOI：
10.1358/dot.2020.56.4.3107707
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发表时间：
2020-04-01
期刊：
影响因子：
1.8
通讯作者：
Wase, L.
中科院分区：
文献类型：
--
作者：
Gan, T. J.;Wase, L.
胆碱是一种新一代静脉注射阿片药物，是一种G蛋白选择性阿片受体激动剂。该化合物的G蛋白选择性导致有效的镇痛，并大大减少β -抑制素的募集，β -抑制素是与阿片类药物相关不良事件相关的信号通路。在随机、安慰剂对照和主动对照的临床研究中，使用奥利匹啶治疗中度至重度急性疼痛提供了比安慰剂更好的有效镇痛效果，与吗啡相比，不良事件的发生率更低，包括呼吸事件和恶心呕吐的胃肠道事件。在这里，我们回顾了静脉注射奥利胆碱的临床前和临床数据，这是一种选择性激动剂，有可能提供比传统阿片类药物更宽的治疗窗口。
Oliceridine is a next-generation investigational intravenous opioid that is a G protein-selective agonist at the mu-opioid receptor. The G protein selectivity of this compound results in potent analgesia with substantially reduced recruitment of beta-arrestin, a signaling pathway associated with opioid-related adverse events. In randomized, placebo- and active-controlled clinical studies, use of oliceridine for the management of moderate to severe acute pain provided potent analgesic effect superior to that observed with placebo, with lower incidence of adverse events, including respiratory events and gastrointestinal events of nausea and vomiting, compared with morphine. Here, we provide a review of the preclinical and clinical data of intravenous oliceridine, a selective agonist, which has the potential to offer a wider therapeutic window than conventional opioids.