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Comparison of the circulating metabolite profile of PF-04991532, a hepatoselective glucokinase activator, across preclinical species and humans: potential implications in metabolites in safety testing assessment.
Sharma R, Litchfield J, Bergman A, Atkinson K, Kazierad D, Gustavson SM, Di L, Pfefferkorn JA, Kalgutkar AS. Sharma R, et al. Among authors: litchfield j. Drug Metab Dispos. 2015 Feb;43(2):190-8. doi: 10.1124/dmd.114.061218. Epub 2014 Nov 10. Drug Metab Dispos. 2015. PMID: 25384899 Clinical Trial.
Transporter-Enzyme Interplay in the Pharmacokinetics of PF-06835919, A First-in-class Ketohexokinase Inhibitor for Metabolic Disorders and Non-alcoholic Fatty Liver Disease.
Weng Y, Fonseca KR, Bi YA, Mathialagan S, Riccardi K, Tseng E, Bessire AJ, Cerny MA, Tess DA, Rodrigues AD, Kalgutkar AS, Litchfield JE, Di L, Varma MVS. Weng Y, et al. Among authors: litchfield je. Drug Metab Dispos. 2022 Jul 2:DMD-AR-2022-000953. doi: 10.1124/dmd.122.000953. Online ahead of print. Drug Metab Dispos. 2022. PMID: 35779864 Free article.
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats.
Litchfield J, Sharma R, Atkinson K, Filipski KJ, Wright SW, Pfefferkorn JA, Tan B, Kosa RE, Stevens B, Tu M, Kalgutkar AS. Litchfield J, et al. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6262-7. doi: 10.1016/j.bmcl.2010.08.095. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20829042
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: litchfield j. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
Stevens BD, Litchfield J, Pfefferkorn JA, Atkinson K, Perreault C, Amor P, Bahnck K, Berliner MA, Calloway J, Carlo A, Derksen DR, Filipski KJ, Gumkowski M, Jassal C, MacDougall M, Murphy B, Nkansah P, Pettersen J, Rotter C, Zhang Y. Stevens BD, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6588-92. doi: 10.1016/j.bmcl.2013.10.057. Epub 2013 Nov 4. Bioorg Med Chem Lett. 2013. PMID: 24239482
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 R, Bergman A, Litchfield J, Atkinson K, Kazierad DJ, Kalgutkar AS. Sharma R, et al. Among authors: litchfield j. Xenobiotica. 2019 Dec;49(12):1447-1457. doi: 10.1080/00498254.2019.1581960. Epub 2019 Mar 7. Xenobiotica. 2019. PMID: 30747552 Clinical Trial.
134 results