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

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