Osimertinib is a tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma. Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals.
- Mechanism
- Curator reviewed · 5 references
Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs. As a third-generation tyrosine kinase inhibitor, osimertinib is specific for the gate-keeper T790M mutation which increases ATP binding activity to EGFR and results in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity. Compared to wild-type EGFR, osimertinib has 200 times higher affinity for EGFR molecules with the L858R/T790M mutation in vitro.
- Primary indication
- Osimertinib is indicated for the: Adjuvant treatment of non-small cell lung cancer (NSCLC) after tumour resection in adult patients whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations,...Curator reviewed · 14 structured indications
- Formula / weight
- C28H33N7O2 · 499.619 g/mol (avg)
- First approval
- Canada, 2016 · United States, 2015 · European Union, 2016
- Also known as
- Mereletinib
- Code names
- AZD-9291
- Brand names
Resolves to
DUYJMQONPNNFPI-UHFFFAOYSA-NSMILESCOC1=C(NC2=NC=CC(=N2)C2=CN(C)C3=C2C=CC=C3)C=C(NC(=O)C=C)C(=C1)N(C)CCN(C)CWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Osimertinib, and which of those have an active Phase 3 trial?
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