Osimertinib

Osimertinib
Clinical data
Trade namesTagrisso, others
Other namesAZD9291, mereletinib, osimertinib mesilate (JAN JP), osimertinib mesylate (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa616005
License data
Pregnancy
category
  • AU: D
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein bindingProbably high
MetabolismOxidation (CYP3A)
Elimination half-life48 hours
ExcretionFeces (68%), urine (14%)
Identifiers
  • N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H33N7O2
Molar mass499.619 g·mol−1
3D model (JSmol)
  • C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C
  • InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
  • Key:DUYJMQONPNNFPI-UHFFFAOYSA-N

Osimertinib, sold under the brand name Tagrisso, is a medication used to treat non-small-cell lung carcinomas with specific mutations. It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.

The most common side effects include diarrhea, rash, musculoskeletal pain, dry skin, skin inflammation around nails, sore mouth, fatigue, and cough.

Osimertinib was approved for medical use in the United States in November 2015, and in the European Union in February 2016.