| Name | Fidaxomicin |
| Description | Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (1.89 mM), Sonication is recommended.
DMSO : 250 mg/mL (236.29 mM), Sonication is recommended.
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| Keywords | RNASynthesis | RNA Synthesis | RNA polymerase | PAR101 | PAR 101 | orally active | OPT80 | OPT 80 | Inhibitor | inhibit | Fidaxomicin | DNASynthesis | DNA/RNA Synthesis | DNA Synthesis | difimicin | Clostridium difficile | CDI | CDAD | Bacterial | Apoptosis | Antibiotic |
| Inhibitors Related | Neomycin sulfate | Aceglutamide | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Sulfamethoxazole sodium | Terbinafine hydrochloride | Formamide | Thymidine | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate |
| Related Compound Libraries | Polyphenolic Natural Product Library | Failed Clinical Trials Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Microbial Natural Product Library | FDA-Approved Drug Library | Natural Product Library for HTS | Immunology/Inflammation Compound Library | Anti-infective Natural Product Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
