For research use only.
Catalog No.S4227 Synonyms: OPT-80, PAR-101
CAS No. 873857-62-6
Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
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|Description||Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.|
Fidaxomicin acts as a RNA polymerase inhibitor by binding to the DNA template–RNA polymerase (RNAP) complex prior to the formation of the open RNAP-DNA complex in which transcription is initiated. Therefore it will inhibit protein synthesis. As a result, apoptosis is triggered in susceptible organisms such as C. difficile. 
|In vivo||The minimum inhibitory concentration for 90% of organisms for fidaxomicin against C. difficile is 0.9978 to 2 μg/mL. Fidaxomicin is not systemically absorbed as shown by a plasma concentrations below the lower limit of quantification after single-dose or multiple-dose. In contrast, fecal concentrations of fidaxomicin are much higher and are concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; AUC = 14 ng•hr/mL. Fidaxomicin is hydrolyzed by gastric acid or intestinal microsomes into a less active metabolite (OP-1118). The cytochrome enzyme system are not involved in the metabolism of fidaxomicin. |
|In vitro||DMSO||100 mg/mL (94.51 mM)|
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In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04138706||Recruiting||Drug: Vancomycin|Drug: Placebos||Clostridium Difficile Infection||McGill University Health Centre/Research Institute of the McGill University Health Centre|Canadian Institutes of Health Research (CIHR)||November 19 2020||Phase 4|
|NCT02437591||Completed||Drug: fidaxomicin||Inflammatory Bowel Disease (IBD)|Clostridium Difficile Infection (CDI)||Astellas Pharma Europe Ltd.|Astellas Pharma Inc||August 13 2015||Phase 4|
|NCT02395848||Recruiting||Drug: Fidaxomicin||Clostridium Difficile Infection||McMaster University|Vancouver Island Health Authority||July 2015||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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