Metabolism and excretion of (<i>S</i>)-6-(3-cyclopentyl-2-(4-trifluoromethyl)-1<i>H</i>-imidazol-1-yl)propanamido)nicotinic acid (PF-04991532), a hepatoselective glucokinase activator, in humans: confirmation of the MIST potential noted in first-in-Human metabolite scouting studies.

Sharma, Raman; Bergman, Arthur; Litchfield, John; Atkinson, Karen; Kazierad, David J; Kalgutkar, Amit S

Metabolism and excretion of (S)-6-(3-cyclopentyl-2-(4-trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid (PF-04991532), a hepatoselective glucokinase activator, in humans: confirmation of the MIST potential noted in first-in-Human metabolite scouting studies.

Sharma, Raman; Bergman, Arthur; Litchfield, John; Atkinson, Karen; Kazierad, David J; Kalgutkar, Amit S.

Afiliación

Sharma R; Medicine Design Pfizer Worldwide Research and Development , Groton , CT , USA.
Bergman A; Clinical Pharmacology/Pharmacometrics Pfizer Worldwide Research and Development , Groton , CT , USA.
Litchfield J; Medicine Design Pfizer Worldwide Research and Development , Cambridge , MA , USA.
Atkinson K; Medicine Design Pfizer Worldwide Research and Development , Groton , CT , USA.
Kazierad DJ; Clinical Sciences Pfizer Worldwide Research and Development , Cambridge , MA , USA.
Kalgutkar AS; Medicine Design Pfizer Worldwide Research and Development , Cambridge , MA , USA.

Xenobiotica ; 49(12): 1447-1457, 2019 Dec.

Article en En | MEDLINE | ID: mdl-30747552

Asunto(s)

Imidazoles/farmacocinética; Ácidos Nicotínicos/farmacocinética; Adolescente; Adulto; Animales; Radioisótopos de Carbono/administración & dosificación; Radioisótopos de Carbono/farmacocinética; Sistema Enzimático del Citocromo P-450/genética; Sistema Enzimático del Citocromo P-450/metabolismo; Heces/química; Humanos; Imidazoles/metabolismo; Inactivación Metabólica; Macaca fascicularis; Masculino; Persona de Mediana Edad; Ácidos Nicotínicos/metabolismo; Proteínas Recombinantes/genética; Proteínas Recombinantes/metabolismo; Adulto Joven

Palabras clave

CYP; Glucokinase; MIST; activator; disproportionate; human; mass balance; metabolite; monkey; radiolabel; safety

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Imidazoles / Ácidos Nicotínicos Límite: Adolescent / Adult / Animals / Humans / Male / Middle aged Idioma: En Revista: Xenobiotica Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos

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