Ridinilazole (SMT19969)
(Synonyms: SMT19969) 目录号 : GC32684
Ridinilazole (SMT19969) 是一种新型抗菌剂，对 C.
Cas No.:308362-25-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ridinilazole is a novel antibacterial with MICs range of 0.06-0.25 µg/mL (MIC90=8 µg/mL) against C. difficile.
Ridinilazole is a novel antibacterial that does not appear to act through the classical pathways associated with antibiotics, such as inhibition of cell wall, protein, lipid, RNA or DNA synthesis. Ridinilazole may impair cell division. Ridinilazole is bactericidal against C. difficile and exhibits a prolonged post-antibiotic effect. In susceptibility testing of 82 clinical isolates of C. difficile (including ribotype 027), Ridinilazole displays potent growth inhibition and has lower MICs [MIC range, 0.06-0.25 µg/mL; MIC for 90% of the organisms (MIC90), 0.125 µg/mL] than Metronidazole (MIC range, 0.125-8 µg/mL; MIC90, 8 µg/mL) or Vancomycin (MIC range, 0.5-4 µg/mL; MIC90, 2 µg/mL). Similarly, Ridinilazole is found to be more potent than Metronidazole or Vancomycin at inhibiting the growth of 50 ribotype-defined C. difficile strains. The activity of Ridinilazole against specific C. difficile ribotypes (including ribotypes 001, 002, 005, 014, 027, 054 and 106) is similar, with an MIC range of 0.06-0.5 µg/mL and an MIC90 of 0.125 µg/mL. In addition, Ridinilazole is more active against 11 ribotype 027 strains than either Metronidazole or Vancomycin[1].
In a hamster model of CDI with a once-daily dosing regimen, Ridinilazole displays greater efficacy than Vancomycin both against non-epidemic and epidemic strains of C. difficile. Similar to the twice-daily dosing study, plasma levels of Ridinilazole are below the level of detection, whereas caecal Ridinilazole concentrations are well above the MIC, thus demonstrating the non-absorbable nature of Ridinilazole and minimal systemic exposure[1].
[1]. Vickers RJ, et al. Ridinilazole: a novel therapy for Clostridium difficile infection. Int J Antimicrob Agents. 2016 Aug;48(2):137-43.
| Cas No. | 308362-25-6 | SDF | |
| 别名 | SMT19969 | ||
| Canonical SMILES | C1(C2=CC=NC=C2)=NC3=CC(C4=CC=C5C(N=C(C6=CC=NC=C6)N5)=C4)=CC=C3N1 | ||
| 分子式 | C24H16N6 | 分子量 | 388.42 |
| 溶解度 | DMSO : ≥ 60 mg/mL (154.47 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5745 mL | 12.8727 mL | 25.7453 mL |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Advances in the diagnosis and treatment of Clostridium difficile infections
Emerg Microbes Infect 2018 Feb 7;7(1):15.PMID:29434201DOI:10.1038/s41426-017-0019-4.
Clostridium difficile is a leading cause of antibiotic-associated diarrhea worldwide. The diagnosis of C. difficile infection (CDI) requires both clinical manifestations and a positive laboratory test for C. difficile and/or its toxins. While antibiotic therapy is the treatment of choice for CDI, there are relatively few classes of effective antibiotics currently available. Therefore, the development of novel antibiotics and/or alternative treatment strategies for CDI has received a great deal of attention in recent years. A number of emerging agents such as cadazolid, surotomycin, Ridinilazole, and bezlotoxumab have demonstrated activity against C. difficile; some of these have been approved for limited clinical use and some are in clinical trials. In addition, other approaches such as early and accurate diagnosis of CDI as well as disease prevention are important for clinical management. While the toxigenic culture and the cell cytotoxicity neutralization assay are still recognized as the gold standard for the diagnosis of CDI, new diagnostic approaches such as nucleic acid amplification methods have become available. In this review, we will discuss both current and emerging diagnostic and therapeutic modalities for CDI.
Update of treatment algorithms for Clostridium difficile infection
Clin Microbiol Infect 2018 May;24(5):452-462.PMID:29309934DOI:10.1016/j.cmi.2017.12.022.
Background: Clostridium difficile is the leading cause of antibiotic-associated diarrhoea, both in healthcare facilities and in the community. The recurrence rate of C. difficile infection (CDI) remains high, up to 20%. Since the publication of the European Society of Clinical Microbiology and Infectious Diseases (ESCMID) guidance document on CDI treatment in 2014, new therapeutic approaches have been developed and tested to achieve higher sustained clinical cure in CDI. Aim: To review novel treatments and approaches for CDI, except probiotics and vaccines. We focused on new antibiotics, antibiotic inactivators, monoclonal antibodies and gut microbiota modulating therapies. Sources: A literature review was performed for clinical trials published in PubMed, Embase or Cochrane Library between January 2013 and November 2017. Content: We analysed 28 clinical trials and identified 14 novel agents. Completed phase 2 studies were found for cadazolid, LFF571, Ridinilazole and nontoxigenic C. difficile strains. Four phase 3 active comparator studies comparing vancomycin with bezlotoxumab, surotomycin (n = 2) and rifaximin have been published. Seven clinical trials for treatment of multiple recurrent CDI with faecal microbiota transplantation were analysed, describing faecal microbiota transplantation by upper or lower gastrointestinal route (n = 5) or by capsules (n = 2). Implications: Metronidazole is mentioned in the ESCMID guideline as first-line therapy, but we propose that oral vancomycin will become the first choice when antibiotic treatment for CDI is necessary. Fidaxomicin is a good alternative, especially in patients at risk of relapse. Vancomycin combined with faecal microbiota transplantation remains the primary therapy for multiple recurrent CDI. We anticipate that new medication that protects the gut microbiota will be further developed and tested to prevent CDI during antibiotic therapy.
Ridinilazole: a novel antimicrobial for Clostridium difficile infection
Ann Gastroenterol 2019 Mar-Apr;32(2):134-140.PMID:30837785DOI:10.20524/aog.2018.0336.
Clostridium difficile (C. difficile) infection remains a global healthcare threat worldwide and the limited options available for its treatment are of particular concern. Ridinilazole is one potential future agent, as it demonstrates rapid bactericidal activity against C. difficile. Current studies show that Ridinilazole has a lower propensity for collateral damage to the gut microbiome and appears to diminish the production of C. difficile toxins. Results from phase II studies demonstrate that patients receiving Ridinilazole had a higher sustained clinical response compared with patients receiving vancomycin (66.7% vs. 42.4%; P=0.0004). Adverse reactions were similar between Ridinilazole and vancomycin (40% vs. 56%, respectively), with most being gastrointestinal-related. Nausea (20%) and abdominal pain (12%) were the most commonly reported adverse reactions associated with Ridinilazole. Phase II study results are promising and future availability of phase III trial results will help further delineate the role and value of Ridinilazole.
Ridinilazole for the treatment of Clostridioides difficile infection
Expert Opin Investig Drugs 2019 Apr;28(4):303-310.PMID:30767587DOI:10.1080/13543784.2019.1582640.
Ridinilazole is a novel antibiotic being developed for the treatment of Clostridioides difficile infection (CDI). Ridinilazole has completed two phase II trials and phase III trials which are denoted Ri-CoDIFy 1 and 2, are planned (ClinicalTrials.gov identifiers: NCT03595553 and NCT03595566). Areas covered: This article covers the chemistry, mechanism of action, in vitro microbiology versus C. difficile and host microbiota, pre-clinical and clinical efficacy, pharmacokinetics, pharmacodynamics and safety and tolerability of Ridinilazole. Expert opinion: Ridinilazole is a novel antibiotic with ideal properties for the treatment of CDI. Given the promising results from the phase II clinical trial, Ridinilazole may have the capability to lower the risk for CDI recurrence thus improving sustained clinical response rates - a current unmet medical need. Assuming a positive phase III trial, Ridinilazole will enter a market with heightened awareness on the importance of prevention of CDI. This along with further research into the economic consequences and decreased patient quality of life associated with recurrent CDI, should provide clinicians with further evidence for the need for therapy that limits CDI recurrence and improves sustained clinical cure.
Ridinilazole: a novel therapy for Clostridium difficile infection
Int J Antimicrob Agents 2016 Aug;48(2):137-43.PMID:27283730DOI:10.1016/j.ijantimicag.2016.04.026.
Clostridium difficile infection (CDI) is the leading cause of infectious healthcare-associated diarrhoea. Recurrent CDI increases disease morbidity and mortality, posing a high burden to patients and a growing economic burden to the healthcare system. Thus, there exists a significant unmet and increasing medical need for new therapies for CDI. This review aims to provide a concise summary of CDI in general and a specific update on Ridinilazole (formerly SMT19969), a novel antibacterial currently under development for the treatment of CDI. Owing to its highly targeted spectrum of activity and ability to spare the normal gut microbiota, Ridinilazole provides significant advantages over metronidazole and vancomycin, the mainstay antibiotics for CDI. Ridinilazole is bactericidal against C. difficile and exhibits a prolonged post-antibiotic effect. Furthermore, treatment with Ridinilazole results in decreased toxin production. A phase 1 trial demonstrated that oral Ridinilazole is well tolerated and specifically targets clostridia whilst sparing other faecal bacteria. Phase 2 and 3 trials will hopefully further our understanding of the clinical utility of Ridinilazole for the treatment of CDI.