Osimertinib
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor used to treat certain types of non-small cell lung cancer (NSCLC). It irreversibly binds to and inhibits mutant forms of the EGFR protein, including T790M mutations and common activating mutations like L858R and exon 19 deletions. This targeted therapy is typically prescribed for patients whose tumors have progressed after first-line EGFR inhibitor therapy.
A targeted therapy for EGFR-mutated non-small cell lung cancer that works by irreversibly inhibiting mutant EGFR proteins.
Key facts at a glance
- ATC
- L01EB04
- RxNorm
- 1721560
- Generic
- Osimertinib
- Class
- atc-l01
- Brands
- Tagrisso
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
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Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Treatment of non-small cell lung cancer (NSCLC) with EGFR mutations, including T790M-positive NSCLC after prior EGFR inhibitor therapy, and as first-line treatment for patients with EGFR-mutated advanced NSCLC.
Osimertinib is an irreversible EGFR tyrosine kinase inhibitor that selectively binds to and inhibits mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at lower concentrations than wild-type EGFR, blocking tumor cell proliferation and promoting cell death.
May cause serious side effects including interstitial lung disease, QT prolongation, and cardiomyopathy. Regular monitoring of cardiac function and liver enzymes may be required. Discuss all current medications with a healthcare provider due to potential drug interactions.
Official drug label
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This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy