Clinical data
Trade names Tagrisso, Tagrix
AHFS/Drugs.com tagrisso
Routes of
Oral tablets
Legal status
Legal status
Pharmacokinetic data
Protein binding Probably high[1]
Metabolism Oxidation (CYP3A)
Biological half-life 48 hours
Excretion Feces (68%), urine (14%)
Synonyms AZD9291
CAS Number 1421373-65-0
PubChem (CID) 71496458
DrugBank DB09330
ChemSpider 31042598
KEGG D10766
ChEBI CHEBI:90943 YesY
Chemical and physical data
Formula C28H33N7O2
Molar mass 499.62 g·mol−1
3D model (Jmol) Interactive image

Osimertinib (previously known as mereletinib or AZD9291;[2] trade name Tagrisso) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug[3][4] developed by AstraZeneca Pharmaceuticals – for mutated EGFR cancers.

Approvals and indications

In November 2015, after a Priority Review, the US FDA granted accelerated approval to osimertinib for the treatment of metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA-approved test, which has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.[5][6]

The FDA approval made reference to two clinical trials, in which an EGFR T790M mutation was confirmed by a Cobas EGFR mutation test; osimertinib was given as 80 mg once daily.[1][7]

The EU gave a similar approval in Feb 2016[8] after two Phase II studies (AURA extension and AURA2).

Clinical trials

First-line use

Osimertinib has also given encouraging results in early trials as a first-line therapy.[9]


  1. 1 2 "Tagrisso (osimertinib) Tablet, for Oral Use. Full Prescribing Information" (PDF). AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850. Retrieved 16 November 2015.
  2. "Proposed INN: List 113" (PDF). International Nonproprietary Names for Pharmaceutical Substances (INN). 29 (2): 285. 2015. Retrieved 16 November 2015.
  3. Ayeni D, Politi K, Goldberg SB (2015). "Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer". Clin. Cancer Res. 21 (17): 3818–20. doi:10.1158/1078-0432.CCR-15-1211. PMID 26169963.
  4. Tan CS, Gilligan D, Pacey S (2015). "Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer". Lancet Oncol. 16 (9): e447–59. doi:10.1016/S1470-2045(15)00246-6. PMID 26370354.
  5. U.S. Food and Drug Administration. Hematology/Oncology (Cancer) Approvals & Safety Notifications.
  6. Xu M, Xie Y, Ni S, Liu H (2015). "The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC)". Ann Transl Med. 3 (7): 96. doi:10.3978/j.issn.2305-5839.2015.03.60. PMC 4430733Freely accessible. PMID 26015938.
  7. U.S. Food and Drug Administration. "Osimertinib".
  8. Tagrisso (osimertinib) approved in EU as first-in-class treatment for patients with EGFR T790M mutation-positive metastatic non-small cell lung cancer
  9. First-Line Osimertinib Yields Nearly 80% Response in Advanced Lung Cancer. April 2016

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