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Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: scarfe gb. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
CYP-Mediated Sulfoximine Deimination of AZD6738.
Jones BC, Markandu R, Gu C, Scarfe G. Jones BC, et al. Drug Metab Dispos. 2017 Nov;45(11):1133-1138. doi: 10.1124/dmd.117.077776. Epub 2017 Aug 23. Drug Metab Dispos. 2017. PMID: 28835442
Phase I study of orally administered 14Carbon-isotope labelled-vistusertib (AZD2014), a dual TORC1/2 kinase inhibitor, to assess the absorption, metabolism, excretion, and pharmacokinetics in patients with advanced solid malignancies.
MacDonald A, Scarfe G, Magirr D, Sarvotham T, Charlton J, Brugger W, Dean E. MacDonald A, et al. Cancer Chemother Pharmacol. 2019 Apr;83(4):787-795. doi: 10.1007/s00280-019-03781-x. Epub 2019 Feb 13. Cancer Chemother Pharmacol. 2019. PMID: 30758651 Clinical Trial.
21 results