M-02(M-02) - _专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点-

作用机制-

治疗领域

消化系统疾病

在研适应症-

非在研适应症

阿片类药物引起的便秘

原研机构

上海瀚迈生物医药科技有限公司

在研机构-

非在研机构

上海瀚迈生物医药科技有限公司

最高研发阶段无进展临床1期

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

登录后查看时间轴

关联

3

项与 M-02 相关的临床试验

NCT05259371 / RecruitingN/A

A 16-Week, Multi-Center, Open-Label, Exploratory Study to Evaluate the Safety and Efficacy of the Application of Pulse Electrical Stimulation Around the Eye in Early to Moderate Dry Age-Related Macular Degeneration

This study aims to evaluate the safety and efficacy of applying pulse electrical stimulation around eyes of age-related macular patients.

开始日期2022-10-05

申办/合作机构

Nu Eyne Co. Ltd.初创企业

CTR20212557 / Completed临床1期

M-02胶囊在健康受试者中多次给药的安全性、耐受性及药动学研究

主要目的：评价M-02胶囊在健康受试者中多次口服给药的安全性与耐受性。次要目的：评价M-02胶囊在健康受试者中多次给药的药代动力学（PK）特征。

开始日期2021-11-01

申办/合作机构

上海瀚迈生物医药科技有限公司

CTR20210655 / Completed临床1期

M-02胶囊在健康受试者中单次给药的安全性、耐受性及药动学研究

主要目的：评价M-02胶囊在健康受试者中单次口服给药的安全性与耐受性。次要目的：评价M-02胶囊在健康受试者中单次给药的药代动力学（PK）特征。

开始日期2021-04-15

申办/合作机构

上海瀚迈生物医药科技有限公司

100 项与 M-02 相关的临床结果

登录后查看更多信息

100 项与 M-02 相关的转化医学

登录后查看更多信息

100 项与 M-02 相关的专利（医药）

登录后查看更多信息

10

项与 M-02 相关的文献（医药）

2024-10-01·Pharmacological Reports

Pharmacokinetic interaction between regorafenib and atorvastatin in rats

Article

作者: Grześkowiak, Edmund ; Karbownik, Agnieszka ; Wolc, Anna ; Czyrski, Andrzej ; Szałek, Edyta ; Karaźniewicz-Łada, Marta ; Szkutnik-Fiedler, Danuta ; Otto, Filip ; Lewandowski, Konrad

AbstractBackgroundRegorafenib is used in the treatment of colorectal cancer and hepatocellular carcinoma. Due to the co-morbidity of hyperlipidemia in these conditions, statins, including atorvastatin, are used as potential adjuvant therapy agents. Both regorafenib and atorvastatin are metabolized by CYP3A4. In addition, atorvastatin is a P-gp and BCRP substrate, whereas regorafenib and its active metabolites M-2 and M-5 are inhibitors of these transporters. Hence, the concomitant use of both drugs may increase the risk of a clinically significant drug–drug interaction. Therefore, the present study aimed to assess the pharmacokinetic interactions of atorvastatin and regorafenib and their active metabolites.MethodsMale Wistar rats were assigned to three groups (eight animals in each) and were orally administered: regorafenib and atorvastatin (IREG+ATO), a carrier with regorafenib (IIREG), and atorvastatin with a carrier (IIIATO). Blood samples were collected for 72 h. UPLC-MS/MS was the method of measurement of regorafenib and atorvastatin concentrations. The pharmacokinetic parameters were calculated with a non-compartmental model.ResultsA single administration of atorvastatin increased the exposure to regorafenib and its active metabolites. In the IREG+ATO group, the Cmax, AUC0–t, and AUC0–∞ of regorafenib increased 2.7, 3.2, and 3.2-fold, respectively. Atorvastatin also significantly increased the Cmax, AUC0–t, and AUC0–∞ of both regorafenib metabolites. Regorafenib, in turn, decreased the AUC0–t and AUC0–∞ of 2-OH atorvastatin by 86.9% and 67.3%, and the same parameters of 4-OH atorvastatin by 45.0% and 46.8%, respectively.ConclusionsThis animal model study showed a significant pharmacokinetic interaction between regorafenib and atorvastatin. While this interaction may be clinically significant, this needs to be confirmed in clinical trials involving cancer patients.Graphical abstract

2020-07-01·Future Medicinal Chemistry4区 · 医学

Structure-based Virtual screening, Biological Evaluation and Biophysical Study of Novel Mcl-1 Inhibitors

4区 · 医学

Article

作者: Liu, Bo ; Du, Jintong ; Hou, Xuben ; Fang, Hao ; Liu, Lulu ; Yang, Jing ; Yu, Jinming

Aim: Targeting the protein–protein interactions (PPIs) associated with Mcl-1 has become a promising therapeutic approach for cancer. Herein, we reported the discovery of novel Mcl-1 inhibitors using an integrated computational approach. Results: Among 30 virtual screening hits, five compounds show inhibitory activities against Mcl-1. The most potent inhibitors M02 ( K i = 5.4 μM) and M08 ( Ki = 0.53 μM) exhibit good selectivity against Bcl-2 and Bcl-xL. Compound M08 exhibits anti-proliferation activity and induces caspase-3 activation in Jurkat cancer cells. Moreover, 1H⁄15N HSQC NMR experiments suggested that compound M08 likely binds in the P2 pocket of Mcl-1 and engages R263 in a salt bridge. Conclusion: Our study provides a good starting point for future discovery of more potent Mcl-1 selective inhibitors.

2020-01-01·Bioorganic Chemistry2区 · 化学

First triclosan-based macrocyclic inhibitors of InhA enzyme

2区 · 化学

Article

作者: Saffon, Nathalie ; Pasca, Maria Rosalia ; Sammartino, José Camilla ; Lherbet, Christian ; Degiacomi, Giulia ; Rodriguez, Frédéric

Two macrocyclic derivatives based on the triclosan frame were designed and synthesized as inhibitors of Mycobacterium tuberculosis InhA enzyme. One of the two molecules M02 displayed promising inhibitory activity against InhA enzyme with an IC₅₀ of 4.7 μM. Molecular docking studies of these two compounds were performed and confirmed that M02 was more efficient as inhibitor of InhA activity. These molecules are the first macrocyclic direct inhibitors of InhA enzyme able to bind into the substrate pocket. Furthermore, these biaryl ether compounds exhibited antitubercular activities comparable to that of triclosan against M. tuberculosis H37Rv strain.

100 项与 M-02 相关的药物交易

登录后查看更多信息