Ensitrelvir Fumaric Acid

6月1日，日本盐野义（Shionogi）宣布，其口服抗病毒药物 XOCOVA® (ensitrelvir)已获得美国FDA 批准，用于 12 岁及以上青少年和成人患者的新冠肺炎（COVID-19）暴露后预防（PEP）。 此次获批比原定的《处方药用户付费法案》（PDUFA）目标日期（6月16日）提前了超过两周。这一进展标志着目前美国医疗市场上，首个且唯一获批用于新冠暴露后预防的口服抗病毒药物正式登场，为临床提供了关键的预防手段。 临床核心数据：阻断率达67% XOCOVA的获批基于其关键的III 期临床研究 SCORPIO-PEP的积极结果。该研究是目前唯一一项达到“预防暴露后出现症状性新冠感染”这一主要终点的口服抗病毒药物III 期试验。 关键疗效指标：发病风险降低： 在接触新冠确诊病例的未感染人群中，与安慰剂组相比，使用XOCOVA 组在接触后至第10 天出现症状性新冠感染的风险显著降低了 67%（研究涉及受试者：XOCOVA 组n=1,030；安慰剂组n=1,011）。用药方案： 该药物采用五天口服疗法，第一天服用3 片，第二天至第五天每天服用1 片。 安全性特征：在临床试验中，XOCOVA 表现出良好的耐受性。两组的不良事件发生率相近，分别为XOCOVA 组15.1% 与安慰剂组15.5%。常见不良事件（发生率≥1% 且高于安慰剂组）主要为头痛、腹泻及咳嗽。值得注意的是，试验中未发现由该药物引起的味觉障碍（dysgeusia）报告。 填补“感染后-发病前”的防控缺口 虽然目前已有针对新冠的疫苗（如Pfizer-BioNTech, Moderna, Novavax）以及用于确诊后的治疗药物（如Paxlovid, Veklury, Lagevrio），但在“接触病毒后、尚未发病前”这一关键窗口期，一直缺乏有效的口服药物干预。 弗吉尼亚大学医学院临床病毒学名誉教授Frederick Hayden 博士指出：“XOCOVA 的获批提供了一种全新的预防策略。除了家庭内部接触外，它在养老院、慢病/急症护理机构的聚集性疫情中，以及高风险的旅行接触后场景中，均具备巨大的应用潜力。” 为什么需要暴露后预防？ 尽管Omicron 及其亚变异株的致病性有所演变，但新冠病毒的传染性依然极强。数据显示，与感染者共同生活的个体中，感染率高达 47%。 美国疾控中心（CDC）的监测数据进一步揭示了持续的健康威胁： ·病例基数大：仅在2025年10月至2026年5月期间，美国就出现了380万至1240万例新发新冠病例。 ·医疗负担重：同期导致的门诊就诊人次高达80万至230万，住院治疗12万至24万例，死亡病例达1.3万至4.2万例。 ·长远影响：新冠感染后，患者出现神经、心血管、呼吸及肾脏相关疾病的风险在感染后一年内持续升高。 创新机制：精准阻断病毒复制 XOCOVA是一种 SARS-CoV-2 主蛋白酶（main protease）抑制剂。该蛋白酶对于病毒的复制至关重要，XOCOVA 通过选择性抑制该酶的活性，从而阻断病毒的复制过程。 盐野义制药执行总裁Nathan McCutcheon表示：“无论受试者的疫苗接种状态或既往免疫水平如何，Xocova都被临床证明能够有效预防有症状新冠感染。这为面临暴露风险的人群提供了一个早期干预、主动保护的全新选择。” 该药此前已于2022 年11 月在日本获得紧急审批，并于2024 年3 月在日本获得全面批准用于新冠肺炎的治疗。此次FDA 的批准，标志着盐野义在该病毒传染病领域的全球战略布局又迈出了实质性的一步。 --- 以上正文 --- 往期好文 《新药价值评估模型 3.0》提示词 MASH 新药竞争格局-2026年3月 口服GLP-1竞争格局 JPM值得关注的CNS领域进展：Kv7 钾离子通道 诺和诺德：中国最高法院对司美格鲁肽化合物专利作出了积极的裁决 报告：肿瘤浸润淋巴细胞（TIL）疗法综述 - 2025年12月 Treg：调节性T细胞（Treg）疗法演进过程、竞争格局（含附件） 体内CAR-T：竞争格局全析，交易、管线、主流递送平台 TSLP竞争格局：SHR-1905启动特应性皮炎2期临床 报告：FGF21的研究进展-2025年10月 报告：T细胞衔接器（TCE）在自身免疫性疾病的研究进展 2026年的创新药，需要关注的重点 药番茄追踪新药情报，分享AI在制药领域落地应用，欢迎感兴趣的朋友加群交流。 若如上二维码添加失败，也可以添加助理微信进群。 声明：本文内容供业内同行交流学习，不代表药番茄表平台立场，不构成任何投资意见和建议。药番茄不对任何主体因使用本文内容而导致的任何损失承担责任。内容如有疏漏，欢迎沟通指出！

The FDA delivered its green light more than two weeks early, with the agency originally slated to weigh in on Shionogi’s Xocova application by June 16. After a prior misfire in demonstrating its protease inhibitor ensitrelvir’s potential as a COVID-19 treatment for U.S. patients, Shionogi has secured an FDA green light for the medicine in the prevention setting.Sold under the Xocova moniker—and available in Japan since 2022—Shionogi’s oral drug has been cleared for post-exposure prophylaxis (PEP) of COVID-19 in U.S. adults and adolescents ages 12 and older following contact with someone who has COVID.With the FDA's sign-off, Xocova has earned the distinction of becoming the first oral drug approved in the U.S. to protect against COVID after exposure, Shionogi noted in a June 1 press release.  The drug is taken over five days, beginning with three tablets on day one and just one tablet on the following four. The FDA delivered its green light more than two weeks early, with the agency originally slated to weigh in on Shionogi’s Xocova application by June 16. Beyond currently approved COVID-19 vaccines from Pfizer-BioNTech, Moderna and Novavax, the U.S. has also cleared antiviral treatments in Pfizer’s Paxlovid, Gilead’s Veklury and Merck & Co.’s Lagevrio, all for treatment after symptom onset. Shionogi’s drug, meanwhile, “has the potential to benefit anyone who does not want to get COVID-19,” Frederick Hayden, M.D., professor emeritus of clinical virology at the University of Virginia School of Medicine, said in the company’s release. Aside from use among households, Xocova could offer an appealing prophylactic option in other exposure incidents, including outbreaks in nursing homes and care facilities, and after travel-related contact, Hayden added.  The FDA’s approval hinges on Shionogi’s SCORPIO-PEP trial, in which Xocova curbed the risk of symptomatic COVID-19 by 67% in uninfected people following exposure to someone infected, through 10 days, as weighted against placebo. Shionogi’s trial enrolled 2,387 participants who had a negative local screening test for the SARS-CoV-2 virus and no symptoms at enrollment after being exposed to an infected person in their household. The company’s primary analysis relied on 2,041 household contact participants with a lab-confirmed negative test at baseline. The Osaka-headquartered company noted that its antiviral was generally well tolerated, with headache, diarrhea and cough the most common side effects among patients on Xocova. “Xoxova is the first and only oral option clinically proven to help prevent symptomatic COVID-19 after exposure among study participants regardless of vaccination status or baseline immunity from prior infection,” Nathan McCutcheon, president and CEO of Shionogi’s U.S. arm, said in a statement. With the drug, “people who are exposed to COVID-19 can act early to help protect themselves,” he added. While the heyday of COVID-19 vaccine and drug sales has long waned—as evinced by Pfizer and Moderna’s ongoing earnings pressures—Shionogi feels Xocova still has an important niche to fill as the disease remains highly transmissible. Up to 47% of people who live with someone infected with COVID risk developing it themselves, Shionogi reckons, pointing to CDC estimates that there were some 3.8 million to 12.4 million new COVID cases in the U.S. from the beginning of last October to May 23, 2026. These infections led to hundreds of thousands of outpatient visits, some 240,000 hospitalizations and between 13,000 and 42,000 deaths, according to the data. In Shionogi’s home country of Japan, Xocova also holds a post-exposure prophylaxis approval. The antiviral was originally greenlit under an emergency nod there as a COVID-19 treatment in November 2022 before securing a full approval in that setting in early 2024. The medication is also available in Singapore. With its protection nod, Shionogi has found a new niche in the U.S. market for Xocova, which disappointed in the late-stage SCORPIO-HR trial back in May 2024. In the study, the antiviral failed to chart a statistically significant reduction in time to sustained resolution of 15 common COVID symptoms. That performance caused the study to miss its primary endpoint. Shionogi leadership admitted at the time that the data were mixed, but they stood behind their asset’s potential and pledged to continue working with regulators to make ensitrelvir more broadly available. Shionogi clarified in its approval announcement Monday that Xocova is cleared as a preventative and not on offer as a COVID treatment in the U.S.