Toxicokinetic profile of fusarenon-X and its metabolite nivalenol in the goat (Capra hircus).

Abstract The main aim of this research was to evaluate the toxicokinetic characteristics of fusarenon-X (FX) and its metabolite, nivalenol (NIV), in goats. The amounts of FX and NIV in post-mitochondrial (S-9), microsomal and cytosolic fractions of diverse tissues of the goat were also investigated. FX was intravenously (iv) or orally (po) administered to goats at dosages of 0.25 and 1 mg/kg bw, respectively. The concentrations of FX and NIV in plasma, feces and urine were quantified by liquid chromatography tandem-mass spectrometry (LC-ESI-MS/MS). The concentrations of FX in plasma were quantified up to 8 h with both routes of administration. A large amount of NIV (metabolite) was quantifiable in plasma, urine and feces after both administrations. The C max value of FX was 413.39 ± 206.84 ng/ml after po administration. The elimination half-life values were 1.64 ± 0.32 h and 4.69 ± 1.25 h after iv and po administration, respectively. In vitro experiments showed that the conversion FX-to-NIV mainly occurs in the liver microsomal fraction. This is the first study that evaluates the fate and metabolism of FX in ruminant species. Highlights • This is the first study that evaluates the fate and metabolism of FX in ruminant species. • FX is absorbed from the gastrointestinal tract with a relatively low bioavailability in goats. • The liver is the organ responsible for the FX-to-NIV biotransformation in goats. • FX is excreted mainly as NIV in the feces of goats after p.o. administration of FX. [ABSTRACT FROM AUTHOR]