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Contezolid free base

编号: 20653
Cas号: 1112968-42-9
纯度: 98% Min.

Contezolid (Youxitai ®), an orally administered oxazolidinone antibacterial agent, is being developed by Shanghai MicuRx Pharmaceutical Co., Ltd. for the treatment of multidrug-resistant (MDR) Gram-positive bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci. In June 2021, it was approved by the National Medical Products Administration of China for the treatment of complicated skin and soft tissue infections (cSSTI), including, but not limited to, methicillin-susceptible S. aureus, MRSA, Streptococcus pyogenes and Streptococcus agalactiae. The recommended dosage of contezolid is 800 mg (i.e. two 400 mg tablets) every 12 h for 7-14 days. Contezolid is also undergoing clinical development for acute bacterial skin and skin structure infections (ABSSSI) in the USA, and for diabetic foot infections.

仅供研究使用。 我们不向患者出售。

化学信息

名称Contezolid free base
Iupac 化学名称4(1H)-Pyridinone, 2,3-dihydro-1-(2,3,6-trifluoro-4-((5S)-5-((3-isoxazolylamino)methyl)-2-oxo-3-oxazolidinyl)phenyl)-
同义词Contezolid Free Base; MRX1; MRX 1; MRX-1
英文同义词Contezolid Free Base; MRX1; MRX 1; MRX-1
分子式C18H15F3N4O4
分子量408.33
SmileO=C1CCN(C2=C(F)C=C(N3C(O[C@@H](CNC4=NOC=C4)C3)=O)C(F)=C2F)C=C1
InChiKeySULYVXZZUMRQAX-NSHDSACASA-N
InChiInChI=1S/C18H15F3N4O4/c19-12-7-13(15(20)16(21)17(12)24-4-1-10(26)2-5-24)25-9-11(29-18(25)27)8-22-14-3-6-28-23-14/h1,3-4,6-7,11H,2,5,8-9H2,(H,22,23)/t11-/m0/s1
Cas号1112968-42-9
相关CAS号

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外观性状固体粉末
纯度98% Min.
存储短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度
可溶性溶于DMSO
处理方式
运输条件作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

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4: Yuan H, Wu H, Zhang Y, Huang H, Li Y, Wu J, Cao G, Yu J, Guo B, Wu J, Yuan Z, Chen Y, Yang W, Wu X, Zhang J. Clinical Pharmacology and Utility of Contezolid in Chinese Patients with Complicated Skin and Soft-Tissue Infections. Antimicrob Agents Chemother. 2022 Jun 21;66(6):e0243021. doi: 10.1128/aac.02430-21. Epub 2022 May 16. PMID: 35575579; PMCID: PMC9217102.


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6: Yang M, Zhan S, Fu L, Wang Y, Zhang P, Deng G. Prospects of contezolid (MRX-I) against multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis. Drug Discov Ther. 2022 May 17;16(2):99-101. doi: 10.5582/ddt.2022.01025. Epub 2022 Apr 12. PMID: 35418550.


7: Li B, Liu Y, Luo J, Cai Y, Chen M, Wang T. Contezolid, a novel oxazolidinone antibiotic, may improve drug-related thrombocytopenia in clinical antibacterial treatment. Front Pharmacol. 2023 Apr 24;14:1157437. doi: 10.3389/fphar.2023.1157437. PMID: 37168994; PMCID: PMC10165100.


8: Wu X, Meng J, Yuan H, Zhong D, Yu J, Cao G, Liu X, Guo B, Chen Y, Li Y, Shi Y, Gordeev MF, Wu J, Zhang J. Pharmacokinetics and Disposition of Contezolid in Humans: Resolution of a Disproportionate Human Metabolite for Clinical Development. Antimicrob Agents Chemother. 2021 Oct 18;65(11):e0040921. doi: 10.1128/AAC.00409-21. Epub 2021 Aug 16. PMID: 34398672; PMCID: PMC8522743.


9: Wang S, Cai C, Shen Y, Sun C, Shi Q, Wu N, Zheng S, Qian J, Zhang R, Zhou H. In vitro Activity of Contezolid Against Methicillin-Resistant Staphylococcus aureus, Vancomycin-Resistant Enterococcus, and Strains With Linezolid Resistance Genes From China. Front Microbiol. 2021 Aug 19;12:729900. doi: 10.3389/fmicb.2021.729900. PMID: 34489919; PMCID: PMC8417360.


10: Pi R, Chen X, Meng J, Liu Q, Chen Y, Bei C, Wang C, Gao Q. Drug Degradation Caused by mce3R Mutations Confers Contezolid (MRX-I) Resistance in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2022 Oct 18;66(10):e0103422. doi: 10.1128/aac.01034-22. Epub 2022 Oct 3. PMID: 36190243; PMCID: PMC9578412.


11: Wang W, Voss KM, Liu J, Gordeev MF. Nonclinical Evaluation of Antibacterial Oxazolidinones Contezolid and Contezolid Acefosamil with Low Serotonergic Neurotoxicity. Chem Res Toxicol. 2021 May 17;34(5):1348-1354. doi: 10.1021/acs.chemrestox.0c00524. Epub 2021 Apr 29. PMID: 33913699.


12: Guo W, Hu M, Xu N, Shangguan Y, Xia J, Hu W, Li X, Zhao Q, Xu K. Concentration of contezolid in cerebrospinal fluid and serum in a patient with tuberculous meningoencephalitis: A case report. Int J Antimicrob Agents. 2023 Aug;62(2):106875. doi: 10.1016/j.ijantimicag.2023.106875. Epub 2023 Jun 3. PMID: 37276894.


13: Wu J, Cao G, Wu H, Chen Y, Guo B, Wu X, Yu J, Ni K, Qian J, Wang L, Wu J, Wang Y, Yuan H, Zhang J, Xi Y. Evaluation of the Effect of Contezolid (MRX-I) on the Corrected QT Interval in a Randomized, Double-Blind, Placebo- and Positive- Controlled Crossover Study in Healthy Chinese Volunteers. Antimicrob Agents Chemother. 2020 May 21;64(6):e02158-19. doi: 10.1128/AAC.02158-19. PMID: 32229495; PMCID: PMC7269508.


14: Liu J, Wang W, Wang C, Zhang L, Zhang X, Liu S, Xu Y, Wang H, Dai Q, Liu C, Wang X, Yuan Z, Gordeev MF. Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies. ACS Med Chem Lett. 2022 Jun 29;13(7):1030-1035. doi: 10.1021/acsmedchemlett.2c00191. PMID: 35859881; PMCID: PMC9290071.


15: Wu J, Yang X, Wu J, Wang J, Wu H, Wang Y, Yuan H, Yang H, Wang H, Zhang J. Dose adjustment not required for contezolid in patients with moderate hepatic impairment based on pharmacokinetic/pharmacodynamic analysis. Front Pharmacol. 2023 Mar 13;14:1135007. doi: 10.3389/fphar.2023.1135007. PMID: 36992830; PMCID: PMC10040594.


16: Wang XK, Yu J, Xie CY, Hu XX, Nie TY, Li X, Wang PH, Li GQ, Yuan H, Yang XY, Li CR, You XF. In vivo pharmacodynamic study of contezolid acefosamil, a prodrug of contezolid for oral and intravenous administration. J Antimicrob Chemother. 2023 Jul 5;78(7):1632-1636. doi: 10.1093/jac/dkad138. PMID: 37202829.


17: Rodgers MP, Wertheim HFL. Comment on: A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections. J Antimicrob Chemother. 2022 Oct 28;77(11):3209-3210. doi: 10.1093/jac/dkac222. PMID: 35791752.


18: Zhao S, Zhang W, Zhang L, Zhang J, Li J, Si L, Ding Y, Li M, Song Y. Use of Contezolid for the Treatment of Refractory Infective Endocarditis in a Patient with Chronic Renal Failure: Case Report. Infect Drug Resist. 2023 Jun 13;16:3761-3765. doi: 10.2147/IDR.S413452. PMID: 37333679; PMCID: PMC10276592.


19: Wang Y, Wu H, Wu J, Fan Y, Liu X, Li Y, Hu J, Zhang J, Guo B. Development and validation of ultra-performance liquid chromatography-tandem mass spectrometric methods for simultaneous and rapid determination of contezolid and its major metabolite M2 in plasma and urine samples and its application to a study in subjects with moderate liver impairment. J Chromatogr B Analyt Technol Biomed Life Sci. 2022 Feb 15;1191:123129. doi: 10.1016/j.jchromb.2022.123129. Epub 2022 Jan 15. PMID: 35066246.


20: Zhao X, Huang H, Yuan H, Yuan Z, Zhang Y. A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections. J Antimicrob Chemother. 2022 May 29;77(6):1762-1769. doi: 10.1093/jac/dkac073. PMID: 35265985.

化学结构

20653 - Contezolid free base | CAS 1112968-42-9

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