伊利诺伊州芝加哥美国心脏协会年会11月8日海报：抗血小板新药Evategrel在中国与美国受试者中药代与药效相近，进食只延缓吸收
美国伊利诺伊州芝加哥市，美国心脏协会（AHA）2026 科学年会 11 月 8 日展示的一项海报研究（编号 Su4001，展示时间为上午 11 时 30 分至下午 12 时 30 分）公布了在研抗血小板药物 Evategrel（CG-0255）的两项临床药理学研究结果。研发企业 CureGene 在新闻稿中介绍，这两项研究均在健康志愿者中开展，一项比较口服 Evategrel 在中国与美国受试者中的药代动力学与药效动力学，另一项考察进食如何影响口服剂型的暴露量与抗血小板效应。本届年会于 11 月 6 日至 9 日在芝加哥麦考密克会展中心举行。
公司称，两项研究采用相同设计，分别在美国与中国开展：在匹配剂量下，两个人群的血药浓度与血小板抑制过程走势相同，抑制程度随剂量上升而增强，而非因族群不同而不同。口服 Evategrel 吸收快、清除也快。
进食研究的结果是：空腹服药时吸收更快、达峰更早；餐后服药时峰值来得更晚、更低，但总暴露量与血小板抑制程度两种情况下大致相同。公司解释称，其活性代谢物 H4 与 P2Y12 受体不可逆地结合，因此起决定作用的是 H4 随时间的累积量，而非某一时刻的浓度峰值。公司称，口服 Evategrel 约 30 分钟内即产生明确的血小板抑制；静脉剂型则面向缺血性卒中急性期，意在为无法吞咽的患者提供另一条给药途径。公司称，约 40% 的卒中患者到院时无法吞咽。
公司介绍，Evategrel 是一种 P2Y12 受体拮抗剂，采用硫醇前药设计，经一步羧酸酯酶水解即释放出与氯吡格雷相同的活性代谢物 H4，不经过 CYP450 氧化，因此起效不依赖 CYP2C19。公司同时声明，该药尚未获任何监管机构批准，其安全性与有效性仍在研究中；美国注册试验正在进行，中国的注册试验将于近期启动。
At the AHA Sessions in Chicago, Illinois, a November 8 Poster on Evategrel: Chinese and U.S. Participants Showed Comparable Pharmacokinetics and Pharmacodynamics, and Food Slowed Absorption but Not Total Exposure
Results from two clinical pharmacology studies of Evategrel (CG-0255), an investigational P2Y12 receptor antagonist, were presented as a poster (Su4001, November 8, 11:30 a.m.–12:30 p.m.) at the American Heart Association Scientific Sessions 2026 in Chicago, Illinois, according to a release from its developer, CureGene. One study compared the pharmacokinetics and pharmacodynamics of oral Evategrel in Chinese and U.S. healthy volunteers; the other examined how food affects exposure to the oral formulation and its antiplatelet effect. The sessions run November 6–9 at McCormick Place in Chicago.
Both studies used the same design, one run in the United States and one in China, the company said. Oral Evategrel was absorbed quickly and cleared quickly, and at matched dose levels, plasma concentrations and platelet inhibition traced the same course in the two populations, with inhibition rising with dose rather than differing by ethnicity.
On food, the company said Evategrel taken on an empty stomach was absorbed faster and peaked sooner, while after a meal the peak came later and lower — but total exposure and the degree of platelet inhibition came out about the same either way, because the active metabolite H4 binds covalently and irreversibly to the P2Y12 receptor, so what matters is how much H4 accumulates over time. Taken orally, Evategrel produces clear platelet inhibition within about 30 minutes, the company said; the intravenous form is intended for the acute phase of ischaemic stroke, for patients who cannot swallow — a group the company put at roughly 40% of stroke patients on arrival.
Evategrel is a thiol prodrug: a single carboxylesterase-mediated hydrolysis step releases H4, the same active metabolite that clopidogrel produces, with no CYP450 oxidation involved, so onset does not depend on CYP2C19, according to the company. The company stated that the drug has not been approved by any regulatory authority and that its safety and efficacy are still being studied; a registration trial is running in the United States, and registration trials in China are due to begin shortly.
来源：CureGene
发布：GSM·美国（发布链接）
图片来源：图：芝加哥麦考密克会展中心。User:TonyTheTiger 摄，CC BY-SA 3.0，经 Wikimedia Commons。 / Photo: McCormick Place, Chicago. Photo by User:TonyTheTiger, CC BY-SA 3.0, via Wikimedia Commons.
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