BACKGROUND Lenvatinib is an oral, multitargeted, tyrosine kinase inhibitor under clinical investigation in solid tumors. In vitro evidence indicates that lenvatinib metabolism may be modulated by ketoconazole, an inhibitor of CYP3A4 and p-glycoprotein. METHODS In this Phase I, single-center, randomized, open-label, two-period, crossover study, healthy adults (18-55 years; N = 18) were randomi...

The purpose of this study was to compare the kinetics of intestinal and hepatic cytochrome P-450 3A (CYP3A) inhibition by using microsomal midazolam 1'-hydroxylation as a marker of enzyme activity. The effect of two antifungal agents commonly implicated in CYP3A drug-drug interactions was examined. Inhibition type and affinities were determined for human liver and intestinal microsomes screened...

We performed a detailed investigation of the kinetics of ketoconazole activity in the setting of broth dilution testing of Candida albicans susceptibility. Turbidimetric readings reflected parallel quantitative colony counts. The method of endpoint determination markedly affected the results. Determinations of 50% inhibitory concentrations clearly separated the ketoconazole-resistant strains fr...

The article Ketoconazole in Cushing’s syndrome: a profile of its use, written by Matt Shirley, was originally published electronically SpringerLink on 07 January 2021 without open access.

Indonesia is a tropical country that has fair temperature and humidity supporting the growth of pathogenic fungi. Pathogenic fungi commonly encountered infecting humans in are species Malassezia furfur Trichophyton mentagrophytes . Nutmeg ( Myristica fragrans Houtt.) one Indonesian plants known to have potential antifungal activity. The purpose this study was examine activity nutmeg ethanol ext...

Ketoconazole has been shown in clinical trials to increase the plasma exposure of the oral anticoagulant prodrug AZD0837 [(2S)-N-{4- [(Z)-amino(methoxyimino)methyl]benzyl}-1-{(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyethanoyl}-azetidine-2-carboxamide] and its active metabolite, AR-H067637 [(2S)-N-{4-[amino(imino)methyl]benzyl}-1-{(2R)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxye...

Ketoconazole, an antifungal antibiotic, inhibits cholesterol synthesis by blocking demethylation of lanosterol. Effects of this inhibition were studied on serum cholesterol, lipoproteins and cholesterol precursors, biliary lipid composition, and fecal steroid elimination in five patients with prostate cancer treated with large doses of ketoconazole. The serum level of total cholesterol fell by ...

MICs and minimum fungicidal concentrations of amphotericin B, miconazole, itraconazole, ketoconazole, fluconazole, and flucytosine against 17 isolates of Scopulariopsis spp. were determined by a broth microdilution method. All the isolates were resistant to itraconazole, fluconazole, and flucytosine, and amphotericin B, miconazole, and ketoconazole MICs were low for only a few.

Mice were treated with ketoconazole with and without dimethyl sulfoxide. Concentrations of ketoconazole at 3 and 5 h after treatment were significantly higher in serum (P less than 0.05) and brain tissue homogenate (P less than 0.01) of mice treated with dimethyl sulfoxide than in those of mice not treated with dimethyl sulfoxide.

In a murine model of Leishmania infantum visceral leishmaniasis, metronidazole, ketoconazole, fluconazole, itraconazole, and terbinafine were less effective than antimonial agents in reducing hepatic parasite load. Ketoconazole potentiated the effect of meglumine antimoniate reference therapy through its marked activity against spleen infection.