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Cross-over to Osimertinib
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, blocking downstream signaling in EGFR-mutant lung cancers.
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, blocking downstream signaling in EGFR-mutant lung cancers. Used for First-line treatment of metastatic non-small cell lung cancer with EGFR exon 19 deletions or L858R mutations, Treatment of metastatic EGFR T790M mutation-positive non-small cell lung cancer, Adjuvant treatment of stage IB-IIIA EGFR-mutant non-small cell lung cancer after resection.
At a glance
| Generic name | Cross-over to Osimertinib |
|---|---|
| Sponsor | AstraZeneca |
| Drug class | EGFR tyrosine kinase inhibitor (third-generation) |
| Target | EGFR (Epidermal Growth Factor Receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Osimertinib selectively targets activating EGFR mutations (L858R, exon 19 deletions) and the resistant T790M mutation with high potency and specificity. By covalently binding to the ATP-binding pocket of mutant EGFR, it prevents autophosphorylation and downstream proliferation signals, while showing reduced activity against wild-type EGFR, thereby improving tolerability.
Approved indications
- First-line treatment of metastatic non-small cell lung cancer with EGFR exon 19 deletions or L858R mutations
- Treatment of metastatic EGFR T790M mutation-positive non-small cell lung cancer
- Adjuvant treatment of stage IB-IIIA EGFR-mutant non-small cell lung cancer after resection
Common side effects
- Diarrhea
- Rash
- Dry skin
- Nausea
- Fatigue
- Stomatitis
- QTc prolongation
Key clinical trials
- AZD9291 Versus Gefitinib or Erlotinib in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (PHASE3)
- A Study to Evaluate the Efficacy and Safety of Glumetinib Combined With Osimertinib Mesylate Versus Platinum-based Doublet Chemotherapy in Non-Small Cell Lung Cancer Patients After Resistance to EGFR-TKIs (PHASE3)
- AZD9291 (Osimertinib) Versus Platinum-Based Doublet-Chemotherapy in Locally Advanced or Metastatic Non-Small Cell Lung Cancer (PHASE3)
- Osimertinib in Combination With Alisertib or Sapanisertib for the Treatment of Osimertinib-Resistant EGFR Mutant Stage IIIB or IV Non-Small Cell Lung Cancer (PHASE1)
- Study Evaluating Efficacy and Safety of Capmatinib in Combination With Osimertinib in Adult Subjects With Non-small Cell Lung Cancers as Second Line Therapy (PHASE3)
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:
- Cross-over to Osimertinib CI brief — competitive landscape report
- Cross-over to Osimertinib updates RSS · CI watch RSS
- AstraZeneca portfolio CI