更新于：2024-05-07
Leritrelvir
来瑞特韦
更新于：2024-05-07
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2023-03-21), |
最高研发阶段(中国)批准上市 |
特殊审评附条件批准 (中国)、特殊审批 (中国) |
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关联
9
项与 来瑞特韦 相关的临床试验A Phase I Single Dose, Non-Randomised, Open-Label, Parallel Group Study to Investigate the Effect of Severe Kidney Impairment on the Pharmacokinetics, Safety and Tolerability of Leritrelvir(RAY1216)
Single-center, Open-label, Non-randomized and Single-dose Clinical Trial to Explore the Mass Balance of Oral Suspension of 400mg [14C]RAY1216
A Phase I Single Dose, Non-Randomised, Open-Label, Parallel Group Study to Investigate the Effect of Hepatic Impairment on the Pharmacokinetics, Safety and Tolerability of Leritrelvir(RAY1216)
100 项与 来瑞特韦 相关的临床结果
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100 项与 来瑞特韦 相关的转化医学
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100 项与 来瑞特韦 相关的专利（医药）
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5
项与 来瑞特韦 相关的文献（医药）2024-03-01International Journal of Antimicrobial Agents
Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis
Review
作者: Xin, Chuanwei ; Yang, Wenjuan ; Zheng, Bei ; Han, Bing ; Ying, Yin ; Zhu, Jun ; Yang, Bo ; Zhang, Meiling ; Zhao, Qinqin ; Feng, Pinpin ; Li, Gonghua
OBJECTIVE:
This study aimed to explore the efficacy and safety of small-molecule antivirals for treating coronavirus disease 2019 (COVID-19).
METHODS:
Seven databases were searched from their inception to 01 June 2023. The risk of bias in randomised controlled trials and retrospective studies was evaluated individually using the Cochrane risk-of-bias tool and Newcastle Ottawa Scale.
RESULTS:
In total, 160 studies involving 933 409 COVID-19 patients were evaluated. Compared with placebo or standard of care, proxalutamide demonstrated remarkable efficacy in reducing mortality rates, hospitalisation rates, serious adverse events, and the need for mechanical ventilation. Furthermore, it significantly enhanced both the rate of clinical improvement and expedited the duration of clinical recovery when compared with control groups. In patients with mild-to-moderate COVID-19, proxalutamide exhibited the above advantages, except for mortality reduction. Triazavirin was the most effective treatment for reducing the time required for viral clearance and improving the discharge rate. Leritrelvir and VV116 were ranked first in terms of enhancing the viral clearance rate on days 7 and 14, respectively. Molnupiravir was the most effective treatment for reducing the need for oxygen support. Overall, these findings remained consistent across the various subgroups.
CONCLUSIONS:
A thorough evaluation of effectiveness, applicable to both mild-to-moderate and unstratified populations, highlights the specific advantages of proxalutamide, nirmatrelvir/ritonavir, triazavirin, azvudine, molnupiravir, and VV116 in combating COVID-19. Additional clinical data are required to confirm the efficacy and safety of simnotrelvir/ritonavir and leritrelvir. The safety profiles of these antivirals were deemed acceptable.
2024-01-01eClinicalMedicine
Leritrelvir for the treatment of mild or moderate COVID-19 without co-administered ritonavir: a multicentre randomised, double-blind, placebo-controlled phase 3 trial
Article
作者: Tong, Jianlin ; Zhong, Nanshan ; Liang, Shiwei ; Xiang, Tianxin ; Li, Haijun ; Chen, Ruifeng ; Lu, Hongzhou ; Zheng, Jingping ; Deng, Ying ; Liang, Jingyi ; Zhang, Ping ; Wang, Xifu ; Wang, Furong ; Pan, Hongqiu ; Guo, Xiaoyun ; Ge, Fangqi ; Ou, Shuqiang ; Zhang, Yu ; Lin, Zhengshi ; Song, Yudi ; Li, Weiyang ; Zhan, Yangqing ; Jiang, Mei ; Zheng, Zhigang ; Fang, Zhonghao ; Li, Yueping ; Chen, Dexiong ; Yang, Zifeng ; Luo, Jincan ; Yao, Herui ; Lin, Ling ; Lin, Bingliang ; Su, Liang ; Meng, Qingwei ; Yu, Tao ; Huang, Chaolin ; Xu, Ruhong ; Sun, Ruilin ; Kang, Changyuan
Background:
Leritrelvir is a novel α-ketoamide based peptidomimetic inhibitor of SARS-CoV-2 main protease. A preclinical study has demonstrated leritrelvir poses similar antiviral activities towards different SARS-CoV-2 variants compared with nirmatrelvir. A phase 2 clinical trial has shown a comparable antiviral efficacy and safety between leritrelvir with and without ritonavir co-administration. This trial aims to test efficacy and safety of leritrelvir monotherapy in adults with mild-to-moderate COVID-19.
Methods:
This was a randomised, double-blind, placebo-controlled, multicentre phase 3 trial at 29 clinical sites in China. Enrolled patients were from 18 to 75 years old, diagnosed with mild or moderate COVID-19 and not requiring hospitalization. Patients had a positive SARS-CoV-2 nucleic acid test (NAT) and at least one of the COVID-19 symptoms within 48 h before randomization, and the interval between the first positive SARS-CoV-2 NAT and randomization was ≤120 h (5 days). Patients were randomly assigned in a 1:1 ratio to receive a 5-day course of either oral leritrelvir 400 mg TID or placebo. The primary efficacy endpoint was the time from the first dose to sustained clinical recovery of all 11 symptoms (stuffy or runny nose, sore throat, shortness of breath or dyspnea, cough, muscle or body aches, headache, chills, fever ≥37 °C, nausea, vomiting, and diarrhea). The safety endpoint was the incidence of adverse events (AE). Primary and safety analyses were performed in the intention-to-treat (ITT) population. This study is registered with ClinicalTrials.gov, NCT05620160.
Findings:
Between Nov 12 and Dec 30, 2022 when the zero COVID policy was abolished nationwide, a total of 1359 patients underwent randomization, 680 were assigned to leritrelvir group and 679 to placebo group. The median time to sustained clinical recovery in leritrelvir group was significantly shorter (251.02 h [IQR 188.95-428.68 h]) than that of Placebo (271.33 h [IQR 219.00-529.63 h], P = 0.0022, hazard ratio [HR] 1.20, 95% confidence interval [CI], 1.07-1.35). Further analysis of subgroups for the median time to sustained clinical recovery revealed that (1) subgroup with positive viral nucleic acid tested ≤72 h had a 33.9 h difference in leritrelvir group than that of placebo; (2) the subgroup with baseline viral load >8 log 10 Copies/mL in leritrelvir group had 51.3 h difference than that of placebo. Leritrelvir reduced viral load by 0.82 log10 on day 4 compared to placebo. No participants in either group progressed to severe COVID-19 by day 29. Adverse events were reported in two groups: leritrelvir 315 (46.46%) compared with placebo 292 (43.52%). Treatment-relevant AEs were similar 218 (32.15%) in the leritrelvir group and 186 (27.72%) in placebo. Two cases of COVID-19 pneumonia were reported in placebo group, and one case in leritrelvir group, none of them were considered by the investigators to be leritrelvir related. The most frequently reported AEs (occurring in ≥5% of participants in at least one group) were laboratory finding: hypertriglyceridemia (leritrelvir 79 [11.7%] vs. placebo 70 [10.4%]) and hyperlipidemia (60 [8.8%] vs. 52 [7.7%]); all of them were nonserious.
Interpretation:
Leritrelvir monotherapy has good efficacy for mild-to-moderate COVID-19 and without serious safety concerns.
Funding:
This study was funded by the National Multidisciplinary Innovation Team Project of Traditional Chinese Medicine, Guangdong Science and Technology Foundation, Guangzhou Science and Technology Planning Project and R&D Program of Guangzhou Laboratory.
2023-09-01eClinicalMedicine
Antiviral efficacy of RAY1216 monotherapy and combination therapy with ritonavir in patients with COVID-19: a phase 2, single centre, randomised, double-blind, placebo-controlled trial
Article
作者: Zhu, Ya-Min ; Yang, Zi-Feng ; Li, Hai-Jun ; Lin, Ling ; Zhong, Nan-Shan ; Cai, Rui-Huan ; Wei, Ying-Na ; Yang, Fei ; Cai, Mi-Mi ; Lin, Zhao-Xin ; Wang, Bei ; Wu, Shu-Hua ; Ou, Xia-Fei
Background:
This study aimed to evaluate the efficacy and safety of RAY1216, a novel inhibitor of 3-chymotrypsin-like cysteine protease (3CLpro), in adults with coronavirus disease 2019 (COVID-19).
Methods:
This phase 2, single centre, randomised, double-blind, placebo-controlled trial included hospitalised patients between August 14, 2022, and September 26, 2022, in Sanya Central Hospital (The Third People's Hospital of Hainan Province) in China with no severe symptoms if they had laboratory-confirmed severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection for not more than 120 h (5 days) and a real-time quantitative polymerase chain reaction (qPCR) cycle threshold (Ct) value of ≤30 for both the open reading frames 1 ab (ORF1ab) and nucleocapsid (N) genes within 72 h before randomisation. Half of the participants (n = 30) were randomly assigned (2:1) to receive either RAY1216 or a matched placebo three times a day (TID) for 5 days (15 doses in total), while the other half received RAY1216 plus ritonavir (RAY1216 plus RTV) or a matched placebo every 12 h for 5 days (10 doses in total). The primary endpoint was the time of viral clearance. Secondary outcomes included the changes of the SARS-CoV-2 RNA viral load, the positivity rate of the nucleic acid test, and the recovery time of clinical symptoms. A safety evaluation was performed to record and analyse all adverse events that occurred during and after drug administration as well as any cases in which dosing was halted because of these events. Clinicaltrials.gov identifier: ChiCTR2200062889.
Findings:
The viral shedding times in the RAY1216 and RAY1216 plus RTV groups were 166 h (95% confidence interval (CI): 140-252) and 155 h (95%CI: 131-203), respectively, which were 100 h (4.2 days) and 112 h (4.6 days) shorter than that of the placebo group, respectively (RAY1216 group vs. Placebo p = 0.0060, RAY1216 plus RTV group vs. Placebo p = 0.0001). At 24 h, 72 h, and 120 h after administration, the viral RNA loads in the RAY1216 and RAY1216 plus RTV groups were significantly less than those of the placebo groups. At 280 h (11.5 days) after administration, the nucleic acid test results in the RAY1216 and RAY1216 plus RTV groups were both negative. The common adverse events related to the investigational drugs were mild and self-limiting laboratory examination abnormalities.
Interpretation:
Our findings suggest that RAY1216 monotherapy and RAY1216 plus ritonavir both demonstrated significant antiviral activity and reduced the duration of COVID-19 while maintaining a satisfactory safety profile. Considering the limited clinical application of RTV, it is recommended to use RAY1216 alone to further verify its efficacy and safety.
Funding:
This study was sponsored by the Key Research and Development Program of China (2022YFC0868700).
100 项与 来瑞特韦 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 新型冠状病毒感染 | 批准上市 | 中国 更多 | |
| 肾脏疾病 | 临床1期 | 中国 更多 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 1,359 | 窪鏇憲蓋鑰衊蓋壓鹽餘(壓鏇鑰壓鹽鹽夢窪鹹網) = 淵壓獵鏇膚築餘淵繭範 鏇糧遞餘糧鏇鏇艱壓齋 (蓋鏇糧願壓鹽壓鹹醖築, 188.95 ~ 428.68) 更多 | 积极 | 2023-12-14 | |||
Placebo | 窪鏇憲蓋鑰衊蓋壓鹽餘(壓鏇鑰壓鹽鹽夢窪鹹網) = 醖鏇構淵鏇蓋鏇範遞衊 鏇糧遞餘糧鏇鏇艱壓齋 (蓋鏇糧願壓鹽壓鹹醖築, 219.00 ~ 529.63) 更多 |
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