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AZD9291
AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to mutant EGFR while sparing wild-type EGFR, overcoming resistance from the T790M mutation.
AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to mutant EGFR while sparing wild-type EGFR, overcoming resistance from the T790M mutation. Used for Non-small cell lung cancer with EGFR T790M mutation (acquired resistance), Non-small cell lung cancer with activating EGFR mutations (first-line treatment).
At a glance
| Generic name | AZD9291 |
|---|---|
| Also known as | TAGRISSO, Tagrisso, Osimertinib |
| Sponsor | Soroka University Medical Center |
| Drug class | Third-generation EGFR tyrosine kinase inhibitor |
| Target | EGFR (Epidermal Growth Factor Receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
AZD9291 (osimertinib) covalently binds to cysteine-797 in the ATP-binding pocket of mutant EGFR, providing sustained inhibition of EGFR signaling in tumors harboring activating EGFR mutations or the acquired T790M resistance mutation. This mechanism allows it to achieve tumor regression in patients who have developed resistance to first- and second-generation EGFR inhibitors while maintaining a more favorable tolerability profile due to reduced wild-type EGFR inhibition.
Approved indications
- Non-small cell lung cancer with EGFR T790M mutation (acquired resistance)
- Non-small cell lung cancer with activating EGFR mutations (first-line treatment)
Common side effects
- Diarrhea
- Rash
- Nausea
- Vomiting
- Stomatitis
- Fatigue
- Decreased appetite
- Interstitial lung disease
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)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- AZD9291 CI brief — competitive landscape report
- AZD9291 updates RSS · CI watch RSS
- Soroka University Medical Center portfolio CI