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Pharmacokinetic and Toxicokinetic Studies of Potential Antifungal Compounds, KAF-200522 and KAF-200522 . HCl, in Animal Models / 한국실험동물학회지
Laboratory Animal Research ; : 399-405, 2010.
Artigo em Coreano | WPRIM | ID: wpr-65552
ABSTRACT
Recent researches on clinically used triazole antifungal reagents are focused on their pharmacokinetic disadvantage which increases the probability of inducing adverse effects in patients. For this point, in the present laboratory, Chemon Inc., has investigated new antifungal reactive compounds, KAF-200522 and its chloride form, KAF-200522 . HCl, which has a modified triazole structure. Pharmacokinetic data were measured with LC-MS/MS in male mice which were orally treated with the above compounds at 10 mg/kg. Tmax and t1/2 of KAF-200522 . HCl were comparable to KAF-200522, but AUC and Cmax were 1.4 and 1.6 times higher than those of KAF-200522, respectively. In beagle dogs, AUC and Cmax of KAF-200522 . HCl were 2.7 and 1.4 times higher than those of KAF-200522, and t1/2 was 3.5 times higher than that of KAF-200522. Moreover, in beagle dogs, the oral bioavailability value of KAF-200522 . HCl was revealed as 31.0% to contrast to 6.2% of KAF-200522. In 1-week repeated oral treatment toxicity study of KAF-200522 in male rats, inhibition of body weight gain was observed in 120 mg/kg treatment group, and loss of body weight was observed in 600 mg/kg treatment group. In the toxicokinetic study of KAF-200522, no accumulation after the systemic exposure was observed. In conclusion, as to the new antifungal drug development, KAF-200522 . HCl was considered to be advantageous in pharmacokinetic characteristics compared to KAF-200522.
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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Peso Corporal / Disponibilidade Biológica / Área Sob a Curva / Modelos Animais / Indicadores e Reagentes Tipo de estudo: Estudo prognóstico Limite: Animais / Humanos / Masculino Idioma: Coreano Revista: Laboratory Animal Research Ano de publicação: 2010 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Peso Corporal / Disponibilidade Biológica / Área Sob a Curva / Modelos Animais / Indicadores e Reagentes Tipo de estudo: Estudo prognóstico Limite: Animais / Humanos / Masculino Idioma: Coreano Revista: Laboratory Animal Research Ano de publicação: 2010 Tipo de documento: Artigo