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Research ArticleArticle

Metabolic Disposition of Osimertinib in Rat, Dog, and Man: insights into a drug designed to bind covalently to a cysteine residue of EGFR

Paul A Dickinson, Mireille V Cantarini, Jo Collier, Paul Frewer, Scott Martin, Kathryn Pickup and Peter Ballard
Drug Metabolism and Disposition May 25, 2016, dmd.115.069203; DOI: https://doi.org/10.1124/dmd.115.069203
Paul A Dickinson
1 AstraZeneca;
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Mireille V Cantarini
1 AstraZeneca;
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Jo Collier
2 Quotient Clinical Ltd.
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Paul Frewer
1 AstraZeneca;
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Scott Martin
1 AstraZeneca;
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Kathryn Pickup
1 AstraZeneca;
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Peter Ballard
1 AstraZeneca;
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  • For correspondence: peter.ballard@astrazeneca.com

Data Supplement

Files in this Data Supplement:

  • Supplemental Data -

    Supplemental Figure 1 - Structure of 14C-osimertinib and 3H-osimertinib

    Supplemental Table 1 - Extent of formation of AZ5104 and AZ7550 in heterologously expressed human CYP isozymes (results shown as a percentage of formation by cytochrome P450 CYP 3A4)

    Supplemental Table 2 - Mean rate of formation of AZ5104, AZ7550, and M1 after incubation of osimertinib in human hepatocytes with and without cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) inhibitors (results shown as pmol/min/million cells)

    Supplemental Table 3 - Cumulative recovery of radioactivity in urine and feces in healthy male volunteers after a single oral dose of 14C-osimertinib 20 mg

    Supplemental Table 4 - Cumulative percentage dose excreted in urine as osimertinib, AZ5104, and AZ7550 and renal clearance in healthy male volunteers after a single oral dose of 14C-osimertinib 20 mg

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