Last reviewed 2026-04-20 · How we verify

Tagrisso (osimertinib)

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR) that binds irreversibly to mutant forms of EGFR.

Tagrisso is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor used to treat non-small-cell lung carcinomas with specific mutations. AstraZeneca developed this medication. It works by inhibiting the activity of EGFR, a protein that promotes cancer cell growth. Tagrisso is indicated for patients with EGFR exon 19 deletions or exon 21 L858R mutations. This medication has shown clinical differentiation in treating NSCLC patients with these specific mutations. Tagrisso has significant commercial value due to its effectiveness and market demand. AstraZeneca continues to develop its pipeline, including potential new indications for Tagrisso.

At a glance

Mechanism of action

Osimertinib is a medication that targets the epidermal growth factor receptor (EGFR), a protein that promotes cancer cell growth. By inhibiting EGFR, osimertinib prevents cancer cells from growing and dividing. This mechanism of action is specific to mutant forms of EGFR, making it an effective treatment for non-small-cell lung carcinomas with these specific mutations.

Approved indications

• Adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations
• Treatment of adult patients with locally advanced, unresectable (stage III) NSCLC whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations
• First-line treatment of adult patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations
• First-line treatment of adult patients with locally advanced or metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, in combination with pemetrexed and platinum-based chemotherapy
• Treatment of adult patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, whose disease has progressed on or after EGFR TKI therapy

Common side effects

• Diarrhea
• Rash
• Musculoskeletal pain
• Nail toxicity
• Dry skin
• Stomatitis
• Fatigue
• Leukopenia
• Lymphopenia
• Thrombocytopenia
• Anemia
• Neutropenia

Drug interactions

• Strong CYP3A Inducers
• Strong CYP3A Inducers
• Moderate and/or weak CYP3A inducers
• BCRP or P-gp substrate
• Drugs that prolong the QTc interval

Key clinical trials

• Osimertinib Combined With Intracranial SRT for EGFR-Mutant NSCLC With Symptomatic Brain Metastases
• Testing Osimertinib as a Treatment for Lung Cancers With an EGFR Exon 20 Change (PHASE2)
• Osimertinib With or Without Bevacizumab as Initial Treatment for Patients With EGFR-Mutant Lung Cancer (PHASE3)
• Testing AZD9291 as Potentially Targeted Treatment in Cancers With EGFR Genetic Changes (MATCH-Subprotocol E) (PHASE2)
• Testing the Combination of MLN0128 (TAK-228) and AZD9291 in Advanced EGFR (Epidermal Growth Factor Receptor) Mutation Positive Non-small Cell Lung Cancer (PHASE1)
• Osimertinib and Necitumumab in Treating Patients With EGFR-Mutant Stage IV or Recurrent Non-small Cell Lung Cancer Who Have Progressed on a Previous EGFR Tyrosine Kinase Inhibitor (PHASE1)
• Prospective Non-Interventional Study Comparing Osimertinib +/- Chemotherapy for EGFR-Mutated NSCLC Patients
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (PHASE2)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Tagrisso CI brief — competitive landscape report
• Tagrisso updates RSS · CI watch RSS
• AstraZeneca portfolio CI