Active metabolite of the antimicrobial nitazoxanide (NTZ) with antiparasitic, antiviral and broad-spectrum bacterial pyruvate-ferredoxin oxidoreductase (PFOR) inhibitory efficacy.
Tizoxanide (TIZ) is the active metabolite of the broad-spectrum parasiticidal drug nitazoxanide (NTZ), a noncompetitive inhibitor against bacterial pyruvate-ferredoxin oxidoreductase (PFOR Ki 2 to 10 μM). NTZ deacetylates rapidly to TIZ in plasma (t1/2 ~6 min at 37°C in human plasma) and in the presence of liver microsomes. NTZ is also reported to exhibit antiviral activity against Hepatitis C, Norovirus, Paramyxovirus, Influenza, Vaccinia, and Zika.
Nitazoxanide (NTZ) and its metabolite tizoxanide (TIZ) were studied as antimycobacterial agents in vitro (in mycobacterial growth indicator tube [MGIT] cultures) and in a whole blood bactericidal assay. Both NTZ and TIZ show high protein binding. In MGIT cultures (albumin concentration = 78 μM)
The Journal of antimicrobial chemotherapy, 46(1), 57-60 (2000-07-07)
The effects of nitazoxanide and its metabolites, tizoxanide and tizoxanide glucuronide, on the development of the asexual and sexual stages of Cryptosporidium parvum in differentiated human enterocytic HCT-8 cells were evaluated in a quantitative alkaline phosphatase immunoassay. Nitazoxanide, tizoxanide and
Nitazoxanide (NTZ) is a broad-spectrum antimicrobial agent. Tizoxanide (T) and tizoxanide glucuronide (TG) are the major circulating metabolites after oral administration of NTZ. A rapid and specific LC-MS/MS method for the simultaneous quantification of T and TG in mouse plasma
Antimicrobial agents and chemotherapy, 51(3), 868-876 (2006-12-13)
Nitazoxanide (NTZ) exhibits broad-spectrum activity against anaerobic bacteria and parasites and the ulcer-causing pathogen Helicobacter pylori. Here we show that NTZ is a noncompetitive inhibitor (K(i), 2 to 10 microM) of the pyruvate:ferredoxin/flavodoxin oxidoreductases (PFORs) of Trichomonas vaginalis, Entamoeba histolytica
International journal of clinical pharmacology and therapeutics, 40(5), 213-220 (2002-06-08)
Nitazoxanide (N) is a new broad-spectrum intestinal antiparasitic agent. Deacetyl-N or tizoxanide (T) and its glucuronide (TG) are the major circulating species metabolites after oral administration of N. Bioavailability is substantially increased by food. The objectives of this phase IA
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