A Randomized, Open, Two-sequence, Two-cycle, Double-cross Design Bioequivalence Trial of Fasting Single Oral STI-1558 Capsule in Healthy Chinese Subjects

This study is a randomized, open, single-dose, two-sequence, two-cycle, double-cross design bioequivalence study.
32 eligible subjects will be randomly assigned to TR group and RT group in a 1:1 ratio. Subjects in the TR group will take the test preparation (T) 200 mg/ pill × 1 pill on day 1 (D1) and the reference preparation (R) 200 mg/ pill × 1 pill on day 8 (D8). The sequence of medication in RT group is reversed from TR group. Wash for at least 7 days between doses.
Screening was performed within 28 days prior to initial dosing, and all eligible subjects were admitted to the clinical research Center 1 day prior to Cycle 1 dosing (D-1) and discharged on day 10 of the study (D10) after completing Cycle 2 PK blood collection, corresponding safety examination, and evaluation. On the 14th day of the study (± 1 day), the clinical research center was returned for follow-up to further evaluate the safety and tolerability of the subjects.

开始日期2023-09-28

申办/合作机构

浙江艾森药业有限公司

NCT05754411

/ Completed临床1期

[14C] Study on Mass Balance and Biotransformation of STI-1558 in Healthy Chinese Adult Male Subjects

This trial adopts a single-center, single-dose, single-period, non-randomized, open-label study design. It is planned to enroll 6
8 healthy male subjects, and each subject receives single oral administration of drug solution containing 600mg/approximately 100µCi [14C]STI-1558 under fasting conditions on trial D1. The whole blood, plasma, urine and stool samples are collected at specified time points/intervals during the trial. The pharmacokinetic parameters of the total radioactivity in plasma and whole blood, the material concentration ratios of the total radioactivity in plasma and whole blood, and the material balances are obtained by testing the total radioactivity of [14C]STI-1558 in plasma, whole blood, urine and feces. Meanwhile, using isotope tracer and mass spectrometry techniques, the main pathways and characteristics of metabolism and elimination of STI-1558 in humans are obtained through the quantification of radioactive metabolite profiles and the structure identification of the main metabolites in plasma, urine and feces of the subjects. The entire duration of trial is expected to be 5 months.

开始日期2023-05-15

申办/合作机构

浙江艾森药业有限公司

NCT05716425

/ Completed临床3期

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Phase III Clinical Study Evaluating the Efficacy and Safety of STI-1558 in Adult Subjects With Mild or Moderate (COVID-19)

This is a multicenter, randomized, double-blind, placebo-controlled phase III clinical study to evaluate the efficacy and safety of STI-1558 in adult subjects with mild/moderate COVID-19. One thousand and two hundred adult subjects with mild/moderate COVID-19 (including subjects with high risk factors for progression into severe cases) are planned to be enrolled and randomized in a ratio of 1:1 into the test group or the placebo group (600 in the test group and 600 in the placebo group).

开始日期2023-02-08

申办/合作机构

浙江艾森药业有限公司

100 项与奥格特韦钠相关的临床结果

登录后查看更多信息

100 项与奥格特韦钠相关的转化医学

登录后查看更多信息

100 项与奥格特韦钠相关的专利（医药）

登录后查看更多信息

项与奥格特韦钠相关的文献（医药）

2024-05-28·NEJM evidence

How To Measure Benefit in a Changing Pandemic — Olgotrelvir for SARS-CoV-2

Article

作者: Sherman, Amy C. ; Baden, Lindsey R.

Since January 2020, there have been over 775 million confirmed cases of Covid-19 and 7 million deaths globally.1 Vaccinations and increased virologic exposure in the population have attenuated the nature of the clinical illness and reduced the severe outcomes associated with the early pandemic stages. However, there is ongoing global transmission of SARS-CoV-2 and evolution of variant strains, with the potential to cause more serious illness. Only limited antiviral options are available to reduce symptomatic illness and disease progression.2-4 Unlike monoclonal antibodies, which target epitopes on the viral surface, small-molecule antivirals such as those targeting the SARS-CoV-2 main protease (Mpro) are under different selective pressure and have the potential to remain active against rapidly emerging viral variants.

2024-05-28·NEJM evidence

Olgotrelvir as a Single-Agent Treatment of Nonhospitalized Patients with Covid-19

Article

作者: Shao, Lei ; Ji, Henry ; Yan, Kuan ; Peng, Chunxian ; Ma, Xiaojun ; Lv, Dongqing ; Dang, Qiang ; Li, Guangming ; Wang, Lifeng ; Royal, Mike ; Tong, Zhaowei ; Zhu, Zhenhong ; Feng, Jiemei ; Jin, Can ; Lin, Bingliang ; Jiang, Rongmeng ; Wang, Shanbo ; Lin, Yuanlong ; Brunswick, Mark ; Qiu, Yunqing ; Gao, Feng ; Han, Bing ; Wang, Jinxiang ; Liu, Jia ; Han, Limei ; Shen, Wei ; Kotoi, Olivia ; Mao, Long ; Xu, Wanhong ; Wang, Kai ; Kushnareva, Yulia ; Xu, Xiao ; Peng, Jie ; Chen, Ying ; Kong, Weixiang ; Lin, Ling ; Sun, Wei ; Zhang, Xiaoying ; Lin, Zhenhao ; Fan, Lingyan ; Lu, Hongzhou ; Li, Yongxia ; Wang, Chao ; Lu, Xiaobo

BACKGROUND:

Olgotrelvir is an oral antiviral with dual mechanisms of action targeting severe acute respiratory syndrome coronavirus 2 main protease (i.e., M^pro) and human cathepsin L. It has potential to serve as a single-agent treatment of coronavirus disease 2019 (Covid-19).

METHODS:

We conducted a phase 3, double-blind, randomized, placebo-controlled trial to evaluate the efficacy and safety of olgotrelvir in 1212 nonhospitalized adult participants with mild to moderate Covid-19, irrespective of risk factors, who were randomly assigned to receive orally either 600 mg of olgotrelvir or placebo twice daily for 5 days. The primary and key secondary end points were time to sustained recovery of a panel of 11 Covid-19-related symptoms and the viral ribonucleic acid (RNA) load. The safety end point was incidence of treatment-emergent adverse events.

RESULTS:

The baseline characteristics of 1212 participants were similar in the two groups. In the modified intention-to-treat population (567 patients in the placebo group and 558 in the olgotrelvir group), the median time to symptom recovery was 205 hours in the olgotrelvir group versus 264 hours in the placebo group (hazard ratio, 1.29; 95% confidence interval [CI], 1.13 to 1.46; P<0.001). The least squares mean (95% CI) changes of viral RNA load from baseline were -2.20 (-2.59 to -1.81) log₁₀ copies/ml in olgotrelvir-treated participants and -1.40 (-1.79 to -1.01) in participants receiving placebo at day 4. Skin rash (3.3%) and nausea (1.5%) were more frequent in the olgotrelvir group than in the placebo group; there were no treatment-related serious adverse events, and no deaths were reported.

CONCLUSIONS:

Olgotrelvir as a single-agent treatment significantly improved symptom recovery. Adverse effects were not dose limiting. (Funded by Sorrento Therapeutics, a parent company of ACEA Therapeutics; ClinicalTrials.gov number, NCT05716425.).

2024-02-01·Med (New York, N.Y.)

Olgotrelvir, a dual inhibitor of SARS-CoV-2 Mpro and cathepsin L, as a standalone antiviral oral intervention candidate for COVID-19

作者: Bao, Yimei ; Kushnareva, Yulia ; Han, Qing ; Zhu, Zhenhong ; Li, Yi ; Chumakova, Ludmila ; Powers, Colin ; Shen, Wei ; Teijaro, John ; Xu, Lijun ; Yang, Haigang ; Xu, Changxu ; Zhang, Can ; Kotoi, Olivia ; Stegman, Karen ; Xie, Hui ; Argent, Christopher ; Wang, Chao ; Qian, Shengdian ; Wang, Shanbo ; Lin, Zhenhao ; Lin, Yuanlong ; Lu, Hongzhou ; Liu, Na ; Li, Tingting ; Kerwin, Lisa ; Zhang, Yuren ; Ji, Henry ; Xu, Wanhong ; Liu, Jia ; Allen, Robert ; Xu, Xiao ; Jin, Can ; Hu, Yong ; Royal, Mike ; Mao, Long ; Zhang, Xiaoying ; Brunswick, Mark ; Shao, Jianping ; Shaabani, Namir ; Shu, Dan

(Med 5, 42–61.e1–e23; January 12, 2024) In our originally published article, we inadvertently omitted a value in the table of Figure 4A. The cell in column “2000 mg” and row “Cmax (ng/mL)a” contained only the standard deviation (± 5050), while the mean value (17800) was missing. The text within the cell has been corrected online from “± 5050” to “17800 ± 5050,” and the full revised figure appears below. The authors apologize for this error and any confusion it may have caused. Olgotrelvir, a dual inhibitor of SARS-CoV-2 Mpro and cathepsin L, as a standalone antiviral oral intervention candidate for COVID-19Mao et al.MedJanuary 4, 2024In BriefMao et al. discovered and developed a next-generation antiviral, olgotrelvir, as a standalone treatment for COVID-19 without ritonavir. Olgotrelvir, with a dual mechanism of action targeting SARS-CoV-2 Mpro and human cathepsin L, significantly inhibited virus replication in an animal model and in COVID-19 patients by oral administration. Full-Text PDF Open Access

171

项与奥格特韦钠相关的新闻（医药）

2026-08-11

·深圳市生物医药产业联盟

深圳三院卢洪洲院长牵头临床研究1类创新药入选《自然》杂志年度榜单

2026年06月12日，国际顶级期刊《Nature Reviews Drug Discovery》（影响因子：91.2）发布年度全球新药靶点报告。报告指出，2025 年全球主要药品监管机构（美国 FDA、欧盟 EMA、日本 PMDA 及中国NMPA）批准了94款具有明确作用机制靶点的新药，其中11个靶点为此前从未被上市药物调控过的全新作用机制靶点，对应10款创新药物。由深圳市第三人民医院卢洪洲教授团队与浙江艾森药业联合研发的奥格特韦钠胶囊成功入选，这也是中国创新药首次荣登该权威榜单！卢洪洲教授 2025年获批的具有新型作用机制靶点的药物奥格特韦钠胶囊作为全球首个双靶点小分子抗新冠病毒药物，一方面靶向组织蛋白酶L（CTSL），阻断病毒入侵宿主细胞；另一方面抑制SARS-CoV-2主蛋白酶（3CL蛋白酶），抑制病毒复制，实现“单药双靶”双重功效！深圳三院卢洪洲教授牵头的奥格特韦钠I期临床研究于2024年01月在全球顶级科学期刊出版商Cell Press旗下《Med》杂志发表。研究结果表明：奥格特韦钠胶囊无需联用肝代谢酶抑制剂利托那韦，可单药口服。相较于需联用利托那韦的其他抗新冠病毒药品，显著降低药物-药物相互作用风险。同年5月，卢洪洲教授作为通讯作者在顶级医学期刊《NEJM Evidence》发表了奥格特韦钠胶囊Ⅲ期临床研究结果。全国总计25家中心参与，共纳入1212例新冠病毒感染患者。疗效方面，奥格特韦钠组11种目标症状（发热、咳嗽和咽痛等）相较于安慰剂组，首次达到持续恢复的中位时间缩短约2.44天（P<0.001）。同时亚组研究中，奥格特韦钠对大于60岁和进展成重症高风险因素的心血管疾病患者疗效更为显著。相较于安慰剂组，奥格特韦钠组所有目标症状的持续临床恢复时间降幅分别达到33.3%和46.0%。同时Ⅲ期临床研究纳入重复感染人群超过50%，更贴合当前新冠病毒感染的治疗现状。安全性方面，奥格特韦钠单药给药，耐受性良好，无发生率≥5%的药物相关不良事件，且不良事件均为轻中度。此次入选2025年全球新药靶点权威榜单，标志着奥格特韦钠胶囊作为全球首个双靶点抗新冠病毒药，获得了国际学术界的高度认可。该药已于2025年11月获国家药品监督管理局批准上市。深圳市第三人民医院卢洪洲教授从I期到Ⅲ期全程主导推进，为这一国产创新药的成功上市提供了坚实支撑，展现了中国临床研究者在国际新药研发中的核心力量！参考文献：[1] Avram S, Halip L, Curpan R, et al. Novel drug targets in 2025. Nat Rev Drug Discov. 2026;25(7):503.[2] Mao L, Shaabani N, Zhang X, et al. Olgotrelvir, a dual inhibitor of SARS-CoV-2 Mpro and cathepsin L, as a standalone antiviral oral intervention candidate for COVID-19. Med. 2024;5(1):42-61.e23. [3] Jiang R, Han B, Xu W, et al. Olgotrelvir as a Single-Agent Treatment of Nonhospitalized Patients with Covid-19. NEJM Evid. 2024;3(6):EVIDoa2400026. 声明：稿件内容源自联盟会员单位，联盟转载仅作宣传。 END 往期推荐关于SZBio 深圳市生物医药产业联盟是深圳市发改委落实深圳“20+8”战略性新兴产业集群布局、践行“一集群、一联盟”顶层工作体系的重要载体，于2024年3月14日正式揭牌成立。联盟在全市各产业主管部门指导支持下运营，立足深圳生物医药全产业链发展需求，面向本土上下游生态主体及意向落地深圳的域外生物医药企业，搭建垂直深耕、全域联动的综合资源对接与信息共享平台。目前联盟已集聚近300家会员单位，覆盖本土上市龙头、行业标杆、科创新锐企业，同时吸纳产业资本、产业园区、科研院所、高等院校等多元主体入驻。联盟着力打通产业信息壁垒，构建高效顺畅的全链条政企协同沟通机制，激活产业创新源头动能，聚力探索政、企、医、校、投深度融合的可持续发展模式，搭建多层次、立体化的生物医药产业创新生态体系。

2026-08-11

·学习强国

填补中国全新机制靶点药物空白 “衢州造”登上《自然》全球新靶点药物榜单

8月5日，记者从衢州市市场监管局获悉，国际顶级期刊《自然综述：药物发现》（Nature Reviews Drug Discovery）最新一期发布了2025年度全球新药靶点报告。由浙江艾森药业有限公司自主研发的奥格特韦钠胶囊入选全球11个全新机制靶点药物名单，这是中国创新药首次登上该榜单。报告中特别标注：这是中国首次迎来具备全新作用靶点的药物上市。奥格特韦钠胶囊是全球首个双靶点新冠口服新药，也是衢州市首款1类原创新药，今年1月已正式在衢州智造新城投入批量生产。2025年，全球各大主流药监机构共批准94款靶点机制清晰的新药，但其中仅有11个靶点是此前从未被任何上市药物调控过的“全新作用机制靶点”，对应药物仅10款，奥格特韦钠胶囊正是其中之一。“国内绝大多数新药研发，是基于国外已经验证的有效靶点，好比早就知道原野上有一朵花，科研人员通过不同路径去摘这朵已知的花。”艾森药业总经理徐万红解释道，“而全新机制靶点药物，是科研团队发现了一朵此前全世界都不知道的花——不仅找到全新靶点，还摸索出可行路径，研发出药物实现靶点调控，从而更优更安全地治疗疾病。”与市面上同类新冠治疗药物相比，该药采用单药设计，打破了传统联合用药的局限，可同时抑制3CL蛋白酶与组织蛋白酶L，同步完成“阻断病毒入侵人体细胞、抑制病毒体内复制”的双重功效。这能有效减少药物相互作用风险，对合并多种基础疾病的患者更为友好，临床适用人群更广。这份亮眼成绩是衢州市生物医药产业高质量发展的缩影。艾森药业2015年落地衢州，同步布局杭州、美国加州研发中心。研发出新药离不开属地全方位政策与要素支撑。“聚焦新药研发、临床、注册、审评、审批、上市全流程，我们搭建全链条指导服务体系，30余次对接国家、省级药监部门，助推新药上市。”衢州市市场监管局产业专班负责人介绍，为保障创新药对生产环境的高要求，还与衢州智造新城管委会协调保障企业厂区布局的独立性。“这几天我们正筹备相关材料，推进奥格特韦钠胶囊纳入国家医保集采的谈判工作。后续还将持续挖掘双靶点药物药理价值，启动慢性阻塞性肺疾病、骨质疏松相关临床研究。”徐万红表示，公司还有多款新药处于不同临床阶段，新一代BTK抑制剂阿比替尼即将进入三期临床试验，全球首个CD38靶点ADC新药正在中美同步开展临床试验。

抗体药物偶联物临床3期

2026-08-10

·杭州澳赛诺ALLSINO

恭喜艾森！全球创新药领域新突破，奥格特韦钠胶囊获国际认可，入选 Nature 2025全新机制靶点药物榜单

本文转载自艾森药业官方公众号原文链接：喜讯！奥格特韦钠胶囊入选 Nature 2025 年度“十大新靶点药物”榜单近日，国际顶级期刊《Nature Reviews Drug Discovery》公布了 2025 年度全新机制靶点药物报告。报告指出，2025 年，全球主要药品监管机构（美国 FDA、欧盟 EMA、日本 PMDA 及中国NMPA）首次批准了 94 款具有明确作用机制靶点的新药。其中，11 个靶点为此前从未被上市药物调控过的全新作用机制靶点，对应 10 款创新药物。奥格特韦钠胶囊成功入围该榜单。 2025年获批的具有新型作用机制靶点的药物[1] 双靶点创新性突破文章指出，奥格特韦钠胶囊的作用靶点是组织蛋白酶L（CTSL）和 3CL 蛋白酶（3CL pro）。其中 CTSL 这一靶点的独特之处在于—它并非直接攻击病毒本身，而是作用于人体细胞表面的组织蛋白酶L，通过抑制病毒入侵宿主细胞从而发挥抗病毒的作用。同时，奥格特韦钠还能抑制新冠病毒的病毒复制关键酶 -3CL 蛋白酶，起到抑制病毒复制的作用[1,2]。奥格特韦钠胶囊作用机制图[2] 单药方案破解联合用药难题奥格特韦钠胶囊另一个优势在于无需联用利托那韦的单药设计。传统抗新冠病毒药多数需联合利托那韦作为药代动力学增强剂，存在较高的药物-药物相互作用风险。奥格特韦钠单药给药[2]，无惧 DDI 风险，尤其适合老年和伴有基础疾病的新冠病毒感染患者使用。国际顶刊发表，奥格特韦钠胶囊显著缩短患者恢复时间，安全性高奥格特韦钠胶囊的Ⅲ期临床试验结果发表于《NEJM Evidence》。临床研究共纳入 1,218 例受试者。结果显示，奥格特韦钠胶囊可显著缩短新冠患者 11 种目标症状（发热、咳嗽、乏力等）的持续恢复时间，较安慰剂组提前恢复 2.44 天。更加值得关注的是，奥格特韦钠胶囊可使 60 岁以上年龄亚组目标症状的持续临床恢复时间缩短 33%，心血管疾病高风险亚组目标症状的持续临床恢复时间缩短 46%，疗效更优[3]。同时，临床研究中，奥格特韦钠胶囊药物相关AE的严重程度大多为 1 级或者 2 级，未出现发生率大于 5%的 AE；奥格特韦钠组治疗期间 3 级以上 TEAE 发生率低于安慰剂组，未发现 4 级药物相关 TEAE[3]。奥格特韦钠III期临床数据[3] 展望作为 2025 年度十大全新靶点创新药的代表之一，奥格特韦钠胶囊凭借其“安全性高、症状恢复快、无惧药物相互作用风险”的特点，为当前新冠病毒感染患者特别是老年及合并基础疾病患者提供了更佳的治疗选择，也为全球公共卫生安全贡献中国药物治疗的最新方案！参考文献:（上下滑动查看更多） [1]. Avram S, Halip L, Curpan R, et al. Novel drug targets in 2025. Nat Rev Drug Discov. 2026;25(7):503. [2]. Mao L, Shaabani N, Zhang X, et al. Olgotrelvir, a dual inhibitor of SARS-CoV-2 Mpro and cathepsin L, as a standalone antiviral oral intervention candidate for COVID-19. Med. 2024;5(1):42-61.e23. [3]. Jiang R, Han B, Xu W, et al. Olgotrelvir as a Single-Agent Treatment of Nonhospitalized Patients with Covid-19. NEJM Evid. 2024;3(6):EVIDoa2400026. 往期回顾喜报|澳赛诺助力1类口服新药奥格特韦钠获批上市！ ACEA Pharma|关于艾森艾森药业成立于2015年，是一家专注于原创新药研发与产业化的生物医药企业，聚焦感染、肿瘤、自身免疫、代谢等重大疾病领域，持续探索未满足临床需求的创新疗法。公司在美国圣地亚哥、中国杭州设有研发中心，并在浙江衢州建设符合国内外cGMP标准的生产及中试基地，构建覆盖研发、临床开发及商业化生产的创新药产业体系。艾森自主研发的双靶点抗新冠病毒创新药奥格特韦钠于2025年获批上市，多个创新药项目已进入临床研究阶段，覆盖肿瘤、自身免疫等疾病领域。 Allsino|关于澳赛诺杭州澳赛诺生物科技有限公司【诺泰生物（股票代码 688076）旗下全资子公司】，成立于2004年5月，设有一个研发中心（浙江杭州）和一个GMP商业化生产基地（浙江建德），是一家专注于小分子新药、高级中间体及多肽片段研发和生产的国际化企业。公司始终坚持以技术创新为驱动，已建立符合USFDA/EDQM/NMPA的质量管理体系，并为全球知名药企提供合规、高效的CDMO服务。

100 项与奥格特韦钠相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D12777 D12778	-	-	-

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
新型冠状病毒感染	中国	浙江艾森药业有限公司	2025-10-28

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
慢性阻塞性肺疾病	临床申请批准	中国	浙江艾森药业有限公司	2025-04-14
SARS-CoV-2 急性呼吸道疾病	药物发现	-	ACEA Therapeutics, Inc.	-

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05716425 (phase 3, Pubmed \| NEJM Evid)	临床3期	新型冠状病毒感染	1,212	Olgotrelvir 600 mg	鏇觸鑰壓鑰齋簾窪壓窪(鑰製鹽積鬱築齋獵獵遞) = 襯簾範積餘構醖壓窪簾餘夢壓衊壓願窪憲構鑰 (壓醖鹽鑰夢顧鹹鹹憲鏇, -2.59 ~ -1.81) 更多	积极	2024-06-01
NCT05716425 (phase 3, Pubmed \| NEJM Evid)	临床3期	新型冠状病毒感染	1,212	Placebo	鏇觸鑰壓鑰齋簾窪壓窪(鑰製鹽積鬱築齋獵獵遞) = 簾積襯壓襯膚範壓鏇餘餘夢壓衊壓願窪憲構鑰 (壓醖鹽鑰夢顧鹹鹹憲鏇, -1.79 ~ -1.01) 更多	积极	2024-06-01
NCT05364840 (MPR-COV-101AU, GlobeNewswire) 人工标引	临床1期	新型冠状病毒感染	58	STI-1558	糧繭觸鏇獵築餘蓋觸積(繭範窪鏇範顧糧鬱齋廠) = 艱蓋願襯夢範夢壓鬱衊壓蓋襯鹹衊餘築壓鹹遞 (糧獵構齋夢襯餘蓋簾鏇 )	积极	2022-11-29
NCT05523739 (MPR-COV-101CN, GlobeNewswire) 人工标引	临床1期	新型冠状病毒感染	78	STI-1558	鹽窪憲廠壓鹽鹹簾衊衊(襯夢衊鬱繭艱齋鬱築顧) = most subjects reporting no AEs 顧憲壓選構齋鹽網衊製 (醖鹽簾顧簾夢選網夢範 ) 更多	积极	2022-11-29