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[4]
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,[6] is a medication used to treat non-small-cell lung carcinomas with specific mutations.[7][8] 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.[9]

Osimertinib was approved for medical use in the United States in November 2015,[10] and in the European Union in February 2016.[5]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  2. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  3. ^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
  4. ^ a b "Tagrisso- osimertinib tablet, film coated". DailyMed. 5 June 2020. Retrieved 16 October 2020.
  5. ^ a b Cite error: The named reference Tagrisso EPAR was invoked but never defined (see the help page).
  6. ^ "Proposed INN: List 113" (PDF). International Nonproprietary Names for Pharmaceutical Substances (INN). 29 (2): 285. 2015. Archived (PDF) from the original on 28 April 2017. Retrieved 16 November 2015.
  7. ^ Ayeni D, Politi K, Goldberg SB (September 2015). "Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer". Clinical Cancer Research. 21 (17): 3818–20. doi:10.1158/1078-0432.CCR-15-1211. PMC 4720502. PMID 26169963.
  8. ^ Tan CS, Gilligan D, Pacey S (September 2015). "Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer". The Lancet. Oncology. 16 (9): e447–e459. doi:10.1016/S1470-2045(15)00246-6. PMID 26370354.
  9. ^ "FDA Approves First Adjuvant Therapy for Most Common Type of Lung Cancer". U.S. Food and Drug Administration (FDA) (Press release). 18 December 2020. Retrieved 20 December 2020.
  10. ^ Cite error: The named reference FDA approval package was invoked but never defined (see the help page).