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| Targets |
Ridinilazole targets the bacterial cell division machinery in C. difficile. By disrupting cell division, it leads to bacterial cell death. Its narrow-spectrum activity is a key feature that minimizes disruption to the normal gut microbiota.
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| ln Vitro |
Ridinilodium is a novel family of antibacterial medications that doesn't seem to work via the traditional antibiotic action channels, like blocking the creation of proteins, lipids, cell walls, RNA, or DNA. Cell division may be hampered by rediprazole. Ridinilodium has long-lasting post-antibiotic effects and is bactericidal against Clostridium difficile. When 82 clinical isolates of C. difficile, including ribotype 027, were subjected to susceptibility testing, rindinilmaze showed strong growth inhibition with a low minimum inhibitory concentration (MIC) of 0.06-0.25 µg/mL. This is lower than the MICs of metronidazole (MIC range: 0.125-8 µg/mL; MIC90, 8 µg/mL) and vancomycin (MIC range: 0.5-4 µg/mL; MIC90, 2 μg/ml) combined. Similarly, it was discovered that rindinilmaze was superior to vancomycin or metronidazole in terms of stopping the growth of 50 C. difficile strains that were identified by ribotype. With a MIC range of 0.06–0.5 µg/mL and a MIC90 of 0.125 µg/mL, rindinilodium is similarly active against particular C. difficile ribotypes, including ribotypes 001, 002, 005, 014, 027, 054, and 106. Furthermore, Ridinilodium has greater efficacy against 11 ribotype 027 bacteria when compared to metronidazole or vancomycin [1].
In vitro, Ridinilazole demonstrates potent activity against C. difficile, with MICs ranging from 0.06 to 0.25 µg/mL (MIC90 = 8 µg/mL). |
| ln Vivo |
Vancomycin was less successful than ridinilmaze for treating C strains that were either epidemic or non-epidemic. difficile in a once-daily dosage schedule for CDI in hamsters. As with the twice-daily dosage study, cecal and plasma concentrations of ridinilmaze were significantly above the minimum inhibitory concentration (MIC) and below detection levels, respectively, indicating that the drug is nonabsorbable and causes little systemic exposure [1].
In vivo, Ridinilazole is an orally administered antibiotic. It is poorly absorbed, allowing it to achieve high concentrations in the gastrointestinal tract where C. difficile resides. It has been evaluated in clinical trials for CDI. |
| Enzyme Assay |
The standard assay for antibacterial activity is the broth microdilution method. C. difficile is cultured in a liquid medium under anaerobic conditions in a 96-well plate. Various concentrations of Ridinilazole are added. The MIC is determined as the lowest concentration that inhibits visible growth.
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| Cell Assay |
Cells (C. difficile) are cultured in appropriate anaerobic media. The compound is added at various concentrations, and growth inhibition is assessed by measuring optical density. The MIC is determined after a defined incubation period.
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| Animal Protocol |
In vivo, Ridinilazole is administered orally. Its efficacy is assessed in animal models of CDI or in clinical trials, where it is compared to standard-of-care antibiotics like vancomycin.
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| ADME/Pharmacokinetics |
Ridinilazole has a molecular weight of 388.43 g/mol and a molecular formula of C24H16N6. It is a non-absorbable compound.
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| Toxicity/Toxicokinetics |
In clinical trials, Ridinilazole was well-tolerated. Its narrow-spectrum activity and poor absorption limit systemic exposure, which may contribute to a favorable safety profile.
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| References |
[1]. Vickers RJ, et al. Ridinilazole: a novel therapy for Clostridium difficile infection. Int J Antimicrob Agents. 2016 Aug;48(2):137-43.
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| Additional Infomation |
Ridinilazole is being investigated in the clinical trial NCT02092935 (a comparative study of SMT19969 and vancomycin in the treatment of Clostridium difficile-associated diarrhea (CDAD)). Ridinilazole is a narrow-spectrum antibiotic with potential activity against Clostridium difficile infection (CDI). After oral administration, Ridinilazole exerts its bactericidal effect against Clostridium difficile by inhibiting cell division. This inhibits the production of bacterial toxins and suppresses the associated inflammatory response. Compared to other antibiotics used to treat Clostridium difficile infection, Ridinilazole does not disrupt the gut microbiota and maintains the activity of the gut microbiota and the associated bile acid metabolome.
Ridinilazole is a promising novel antibiotic in development for C. difficile infection. Its unique mechanism of action and narrow-spectrum profile make it a valuable candidate for addressing this serious infection. |
| Molecular Formula |
C24H16N6
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|---|---|
| Molecular Weight |
388.434
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| Exact Mass |
388.143
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| CAS # |
308362-25-6
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| PubChem CID |
16659285
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
774.9±70.0 °C at 760 mmHg
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| Flash Point |
352.4±28.6 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.764
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| LogP |
3.51
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
524
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1([H])C(C2C([H])=C([H])N=C([H])C=2[H])=NC2C([H])=C([H])C(=C([H])C1=2)C1C([H])=C([H])C2=C(C=1[H])N([H])C(C1C([H])=C([H])N=C([H])C=1[H])=N2
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| InChi Key |
UHQFBTAJFNVZIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H16N6/c1-3-19-21(29-23(27-19)15-5-9-25-10-6-15)13-17(1)18-2-4-20-22(14-18)30-24(28-20)16-7-11-26-12-8-16/h1-14H,(H,27,29)(H,28,30)
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| Chemical Name |
2-pyridin-4-yl-6-(2-pyridin-4-yl-3H-benzimidazol-5-yl)-1H-benzimidazole
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| Synonyms |
SMT19969; SMT 19969; SMT-19969
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~64.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5745 mL | 12.8723 mL | 25.7447 mL | |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1489 mL | |
| 10 mM | 0.2574 mL | 1.2872 mL | 2.5745 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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