Ensitrelvir Fumaric Acid in Health care workers with SARS-CoV-2 Retrospective Chart Review - Tokyo Rinkai Hospital - - Ensitrelvir Fumaric Acid in Health care workers with SARS-CoV-2 Retrospective Chart Review - Tokyo Rinkai Hospital -

开始日期2024-04-12

申办/合作机构

Shionogi & Co., Ltd.

NCT06161688 / Recruiting临床2期IIT

Placebo-Controlled, Randomized Trial of Ensitrelvir (S-217622) for Viral Persistence and Inflammation in People Experiencing Long COVID (PREVAIL-LC)

Persistent viral infection with viral reservoirs and detection of circulating spike protein after the initial acute illness is one potential pathogenic mechanism for Long COVID. This mechanism may be susceptible to antiviral therapy that blocks viral replication, which has the potential to alleviate long COVID symptoms. This trial will study the safety and efficacy of Ensitrelvir (S-217622), an antiviral, to treat individuals with Long COVID in an adult population.

开始日期2024-04-09

申办/合作机构

The University of California, San Francisco

[+1]

CTR20240600 / CompletedN/A

富马酸恩昔特韦片人体生物等效性试验

采用单中心、随机、开放、两制剂、两周期交叉、单剂量给药设计比较空腹和餐后给药条件下，远大医药（中国）有限公司提供的富马酸恩昔特韦片（规格：125 mg）与盐野义制药株式会社持证的富马酸恩昔特韦片（规格：125 mg，XOCOVA® Tablets）在中国健康人群中吸收程度和吸收速度的差异，并评价远大医药（中国）有限公司提供的富马酸恩昔特韦片的安全性

开始日期2024-03-21

申办/合作机构

远大医药（中国）有限公司

100 项与恩赛特韦相关的临床结果

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100 项与恩赛特韦相关的转化医学

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100 项与恩赛特韦相关的专利（医药）

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项与恩赛特韦相关的文献（医药）

2024-11-01·ANTIVIRAL RESEARCH

Highly specific SARS-CoV-2 main protease (Mpro) mutations against the clinical antiviral ensitrelvir selected in a safe, VSV-based system

Article

作者: Schöppe, Helge ; Bante, David ; He, Xi ; Heilmann, Emmanuel ; Dunzendorfer-Matt, Theresia ; Costacurta, Francesco ; Moghadasi, Seyed Arad ; Sauerwein, Anna ; Sprenger, Bernhard ; Rabensteiner, Toni ; Erisoez, Ela Emilie ; Krismer, Laura ; Heberle, Anne ; Rauch, Stefanie ; von Laer, Dorothee ; Naschberger, Andreas ; Kaserer, Teresa ; Peng, Ju-Yi ; Wang, Dai

In the SARS-CoV-2 pandemic, the so far two most effective approved antivirals are the protease inhibitors nirmatrelvir, in combination with ritonavir (Paxlovid) and ensitrelvir (Xocova). However, antivirals and indeed all antimicrobial drugs are sooner or later challenged by resistance mutations. Studying such mutations is essential for treatment decisions and pandemic preparedness. At the same time, generating resistant viruses to assess mutants is controversial, especially with pathogens of pandemic potential like SARS-CoV-2. To circumvent gain-of-function research with non-attenuated SARS-CoV-2, a previously developed safe system based on a chimeric vesicular stomatitis virus dependent on the SARS-CoV-2 main protease (VSV-M^pro) was used to select mutations against ensitrelvir. Ensitrelvir is clinically especially relevant due to its single-substance formulation, avoiding drug-drug interactions by the co-formulated CYP3A4 inhibitor ritonavir in Paxlovid. By treating VSV-M^pro with ensitrelvir, highly-specific resistant mutants against this inhibitor were selected, while being still fully or largely susceptible to nirmatrelvir. We then confirmed several ensitrelvir-specific mutants in gold standard enzymatic assays and SARS-CoV-2 replicons. These findings indicate that the two inhibitors can have distinct viral resistance profiles, which could determine treatment decisions.

2024-11-01·Infectious Diseases and Therapy

Letter to the Editor: “Real-World Effectiveness of Ensitrelvir in Reducing Severe Outcomes in Outpatients at High Risk for COVID-19”

Letter

作者: Hagiya, Hideharu

2024-11-01·ANTIVIRAL RESEARCH

Replication capacity and susceptibility of nirmatrelvir-resistant mutants to next-generation Mpro inhibitors in a SARS-CoV-2 replicon system

Article

作者: Lin, Michael Z. ; Einav, Shirit ; Gammeltoft, Karen Anbro ; Gottwein, Judith ; Lo, Chieh-Wen ; Hao, Chenzhou ; Bukh, Jens ; Westberg, Michael ; Kariv, Omri ; Lin, Michael Z

There is an ongoing need to expand the anti-SARS-CoV-2 armamentarium to include agents capable of suppressing replication of drug-resistant mutants emerging during monotherapy with approved direct-acting antivirals. Using a subgenomic SARS-CoV-2 replicon system, we studied the RNA replication capacity of nirmatrelvir (NTV)-resistant mutants and their susceptibility to next-generation Mpro inhibitors, including ibuzatrelvir (ITV), ensitrelvir (ETV), and ML2006a4. Our findings revealed that E166V Mpro mutants reduced viral RNA replication, whereas other Mpro mutations retained or increased the replication capacity, suggesting the potential of the latter to dominate under NTV selective pressure. Except for having an advantage against E166A mutants, ITV largely showed the same mutational sensitivity as NTV. ETV was more effective than NTV against E166V mutants but less effective against S144A, E166A, and L167F mutants. ML2006a4 demonstrated the most effective suppression across most mutants (S144A, E166V, S144A + L50F, E166 A/V + L50F, L167F + L50F, and E166A + L167F + L50F). Thus, ML2006a4 represents an attractive investigational candidate against clinically relevant NTV-resistant SARS-CoV-2 mutants.

152

项与恩赛特韦相关的新闻（医药）

2024-10-29

·EndPoints

Shionogi touts topline data for Covid-19 antiviral for post-exposure treatment

Shionogi’s once-daily 3CL protease inhibitor hit on a primary endpoint in a late-stage trial as a post-exposure prophylaxis treatment for Covid-19 after failing a Phase 3 study in May. The oral antiviral, ensitrelvir, showed a statistically significant decrease in the proportion of patients with a symptomatic infection through 10 days after being exposed to household members with Covid-19 when compared to placebo. The company described the drug as well-tolerated with no new safety signals. Shionogi’s senior VP and head of clinical development Simon Portsmouth said in a statement that “there are currently no oral antiviral medications approved for post-exposure prophylactic use,” adding that “there is a need for convenient, preventive approaches to protect ourselves and those close to us from contracting SARS-CoV-2.” Ensitrelvir, marketed as Xocova and developed in a joint research collaboration with Hokkaido University, scored an emergency regulatory approval in Japan in 2022 before garnering a full approval in March for the treatment of Covid-19. But the drug failed in the NIH-partnered SCORPIO-HR study when it didn’t show a statistically significant reduction in patients being completely clear of symptoms for at least two days when the drug was given within three days of symptoms starting. However, a separate analysis showed that patients had no sign of six different symptoms for at least one day, earning a p-value of 0.05 compared to placebo. The trial showed other positives, according to the company, including a reduction from baseline in viral RNA levels and no symptomatic viral rebounds in patients.

临床结果临床3期上市批准

2024-10-29

·echemi

Shionogi’s COVID-19 Oral Medication Shows Significant Efficacy, but Faces a Crisis with 2 Million Treatment Courses Being Destroyed!

Shionogi & Co., one of Japan's leading drugmakers, said in a statement Tuesday that the results of an ongoing late-stage global clinical trial showed that its oral pill treatment for COVID-19 was significantly effective in reducing the spread of the virus. The drug, Ensitrelvir, which is commercially known as Xocova, showed a statistically significant reduction in patients who developed symptoms after home contact with COVID-19, Shionoi said in its statement. The Phase 3 trial, known as SCORPIO-PEP, involved about 2,400 participants in several countries in the U.S., South America, Africa and Asia. The trial results showed that Ensitrelvir was significantly effective in preventing COVID-19 transmission, especially among participants who developed symptoms after close contact with an infected person. It is worth noting, however, that in May this year, Shionogi Pharma had commented that Ensitrelvir had failed to show a significant effect in reducing common COVID-19 disease symptoms compared to a placebo. The results of this study, known as the SCORPIO-HR trial, are in stark contrast to the SCORPIO-PEP trial. Still, in March, the Japanese government fully approved the use of Ensitrelvir. However, while the government bought two million courses of treatment during the pandemic, most of the drugs went unused and will eventually be destroyed, according to media reports. This situation has led to public questioning and discussion about government decision-making and resource allocation.

临床3期临床结果紧急使用授权

2024-07-23

·药通社

立无可立，盯上新冠药？

仿制药要如何突破内卷重围？改良型新药要如何抓住风口时机？立项是企业统领全局的关键步骤，是企业打造竞争力的第一步。清晰科学的立项战略不仅能让企业在市场拼杀中发挥最强战斗力，而且能帮企业节约成本与资源。基于此，2024年8月15-16日，2024 CMC博览会同期举办仿制药和改良新药立项“稳准狠”论坛，邀请行业专家，凝聚智慧、出谋划策，一同规划仿制药和改良新药未来！一键报名 · 见证合作！距离2022年底的新冠疫情全国大爆发已经过去一年半，此时政府在为经济复苏绞尽脑汁，老百姓在为生活忙碌奔波时，身边虽偶有亲朋好友“羊”了，但症状较之前轻了许多，慢慢的大家已忽视新冠病毒的存在。从中国疾控预防控制中心2024年7月10日发布的最新全国新型冠状病毒感染疫情情况看，其实新型冠状病毒SARS-CoV-2从未离开过我们。这一年多来，流感和新冠此起彼伏，老百姓纷纷囤积奥司他韦和玛巴洛沙韦于家中常备，而屯新冠药的却在少数。目前国内已批准的小分子新冠药物主要是“2+5”，即辉瑞进口的奈玛特韦片/利托那韦片组合包装和默沙东进口的莫诺拉韦胶囊，国产新势力有河南真实生物科技有限公司阿兹夫定片、先声药业的先诺特韦片/利托那韦片组合包装、君实生物的氢溴酸氘瑞米德韦片、广东众生睿创的来瑞特韦片和广生堂的阿泰特韦片／利托那韦片组合包装。除了先声药业已转常规批准，其他均是附条件批准。此次不讨论那些治疗新冠中国特色的中药注射剂和中药汤剂。辉瑞和默沙东早已赚的盆满钵满，辉瑞2023年报披露Paxlovid全球销售 12.79 亿美元，默沙东2023年报披露莫诺拉韦胶囊全球销售 14.28 亿美元，国内四小强也是勉强抓住了新冠大爆发的尾巴完成了三期临床试验，真正商业化时，新冠流行病显著下降，可谓时运不济，先声研发不低于5亿，广东众生研发不低于6亿元，君实研发不低于8.8亿，广生堂研发不低于3.5亿，数亿的投入相信离回本还要看天吃饭。目前的销量先声＞君实＞众生＞广生堂，阿兹夫定主要是在2022年上述药物均未获批时踩上了红利。也因为新冠疫情已趋于局部流感化，多数企业纷纷终止了新冠药物的研发，包括疫苗、抗体和小分子药物，但仍有一批企业仍默默前行，实属不易！其实在新冠疫情的那些年，很多企业都立项或者引进过新冠项目，比如石药的SYH2055、翰森的HS-10517、中国生物制药的TDI01、歌礼的ASC10、前沿生物的FB2001、英矽智能的ISM3312、远大医药的GS221和STC3141，远大医药甚至还披露：在持续研发第二代小分子3CLpro抑制剂，在研产品有望实现对 COVID-19 患者的轻、中、重症治疗的全覆盖。笔者研究了远大医药披露信息的措辞后发现，GS221和STC3141对新冠有疗效的趋势；不出意外，远大医药已在去年的年报里找不到新冠项目的身影。但笔者却在CDE登记平台发现一个陌生的名字：富马酸恩昔特韦片正在做生物等效性试验，原来是远大医药改变策略，与其投入数亿元去研发新药，不如直接做个BE来的快，但比较的激进的是选择了日本上市的盐野义品种。富马酸恩昔特韦片目前未纳入参比制剂目录，无中国患者数据，甚至当年CDE都未批准盐野义附条件进口，这样的情况下去仿制是不是太冒险？BE总结报告版本日期是2024-06-18，理论上近期应该会申报，敬请期待！其实仿制进口新冠药的不仅仅是远大，早在2022年，当时原研默沙东的莫诺拉韦胶囊还没有批准附条件进口，安徽贝克已经于2022年8月完成莫诺拉韦胶囊生物等效性试验，按照化药3类申请注册了，2023年中披露的信息显示：“目前该项目处于国家药审中心审评阶段，具体为“特别审批”窗口待受理状态”，2023年底终止IPO至今再无该项目的信息，笔者分析：首先原研仅为附条件批准进口，尚未转为常规批准，附条件批准上市的药品尚未满足常规注册要求，安全性和有效性数据尚不充分。 2023年底广生堂的阿泰特韦片／利托那韦片组合包装都是附条件批准，那时的新冠阳性率还不及现在，笔者猜测CDE目前仍认为新冠药是公共卫生事件急需用药，及时是仿制药也会优先批准，所以认为安徽贝克莫诺拉韦仿制药批准的可能性已不大。当下立项难困扰很多企业，各自都在寻求差异化，有转型改良新药，有转型高端制剂，有转型上下游一体化，有转型细分（儿童、透皮、眼科）领域，有转型非药品（医美兽药）赛道，有坚定走集采的，有转型出海的，大家各显神通，都能杀出一条血路。而以上莫诺拉韦和恩昔特韦两个品种无中国人群数据，专利情况尚不明朗，加上新冠病毒亚型仍在不断变异，即使可能亚洲人和白人没有明显的种族差异，冒然做BE，还是值得商榷的！仿制药立项思路和产品布局如今有何变化？仿制药要如何突破内卷重围？改良型新药要如何抓住风口时机？ 2024年8月15-16日，2024 CMC博览会同期举办仿制药和改良新药立项“稳准狠”论坛，邀请行业专家，凝聚智慧、出谋划策，一同规划仿制药和改良新药未来！一键报名 · 见证合作！ 08/15 AM 入门篇—B证企业法规政策 ▷9:30-10:10 从仿制走向改良：在细分领域挖掘机会王立峰慧药咨询创始人 ▷10:10-10:50 缓释制剂的改良立项及临床开发策略夏燕百花村医药集团轮值总经理，礼华生物董事长 ▷10:50-11:30 基于临床需求的改良型新药立项策略与实施案例吴涛北京汇诚瑞祥医药生物科技有限公司首席科学家 ▷11:30-12:10 成功上市的505(b)(2)案例对改良新药立项启示陈洪外专局特聘专家 08/15 PM ▷14:00-14:40 以透皮给药技术平台为导向的产品立项及案例分享孙亚洲长沙晶易医药科技股份有限公司联合创始人、董事、高级工程师、NMPA高级研修学院特聘讲师 ▷14:40-15:20 以渗透泵技术平台为导向的产品立项及案例分享石劲敏汉都医药副总经理 ▷15:20-16:00 以眼部给药技术平台为导向的产品立项及案例分享 ▷16:00-16:40 以儿科药物掩味技术平台为导向的产品立项及案例分享 08/16 AM ▷9:30-10:20 独一无二——以特色、差异化布局选品思路郭新峰南京循证生物科技有限公司创始人 ▷10:20-11:30 成本优势——以集采品种选品思路张廷杰风云药谈创始人 ▷11:30-12:10 技术领先—高技术壁垒改良型新药立项及成功案例分享魏世峰北京罗诺强施医药技术研发中心有限公司董事长兼CEO 08/16 PM ▷13:30-14:30 产品为王—高度内卷之下，仿制药的立项思路与产品布局魏利军北京药眼信息咨询有限公司创始人兼CEO ▷14:30-15:00 顺势而为——以市场消费趋势为导向选品立即扫码报名推荐阅读

临床3期疫苗

100 项与恩赛特韦相关的药物交易

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研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
新型冠状病毒感染	日本	Shionogi & Co., Ltd.	2022-11-22

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
炎症	临床2期	美国	Shionogi, Inc.	2024-04-09
新冠肺炎后遗症	临床2期	美国	Shionogi, Inc.	2024-04-09
肝病	临床1期	美国	Shionogi, Inc.	2022-09-13

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


Corporate Publications 人工标引	临床2/3期	新型冠状病毒感染	-	S-217622	築鑰築夢遞淵膚鬱齋衊(遞鏇衊廠鑰衊鏇積憲構) = On day four of treatment (following the third dose), the proportion of patients with positive viral titer decreased by approximately 90% versus placebo. 築鏇獵鹹餘築獵膚繭艱 (鏇夢獵鏇築襯簾製製夢 ) 更多	积极	2022-04-24
				Placebo