Fidaxomicin

Catalog No.S4227 Synonyms: OPT-80, PAR-101

Fidaxomicin Chemical Structure

Molecular Weight(MW): 1058.04

Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.

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Biological Activity

Description Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
Targets
RNA polymerase [1]
In vitro

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. [1]

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. [1]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (94.51 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1058.04
Formula

C52H74Cl2O18

CAS No. 873857-62-6
Storage powder
in solvent
Synonyms OPT-80, PAR-101

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT02179658 Completed Drug: OPT-80|Drug: vancomycin Clostridium Difficile Astellas Pharma Inc June 23 2014 Phase 3

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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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DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID