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Osimertinib (Osi)
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, blocking downstream signaling in cancer cells.
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, blocking downstream signaling in cancer cells. Used for Metastatic non-small cell lung cancer with EGFR exon 19 deletions or exon 21 L858R mutations (first-line), Metastatic non-small cell lung cancer with EGFR T790M mutation (second-line, after progression on first- or second-generation EGFR inhibitors), Adjuvant treatment of stage IB-IIIA EGFR-mutant non-small cell lung cancer after resection.
At a glance
| Generic name | Osimertinib (Osi) |
|---|---|
| Sponsor | AbbVie |
| Drug class | EGFR tyrosine kinase inhibitor (third-generation) |
| Target | EGFR (Epidermal Growth Factor Receptor) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Osimertinib selectively targets activating EGFR mutations (exon 19 deletions and L858R) and the T790M resistance mutation that emerges during first- or second-generation EGFR inhibitor treatment. 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. This mechanism makes it effective in both treatment-naïve and resistant EGFR-mutant non-small cell lung cancers.
Approved indications
- Metastatic non-small cell lung cancer with EGFR exon 19 deletions or exon 21 L858R mutations (first-line)
- Metastatic non-small cell lung cancer with EGFR T790M mutation (second-line, after progression on first- or second-generation EGFR inhibitors)
- Adjuvant treatment of stage IB-IIIA EGFR-mutant non-small cell lung cancer after resection
Common side effects
- Diarrhea
- Rash
- Dry skin
- Nausea
- Stomatitis
- Paronychia
- QTc prolongation
- Interstitial lung disease
Key clinical trials
- A Study to Assess Adverse Events, Change in Disease Activity of Intravenous Telisotuzumab Adizutecan in Combination With Osimertinib as First-Line Treatment in Adult Participants With Locally Advanced Unresectable or Metastatic EGFR-Mutated Non-Squamous Non-Small Cell Lung Cancer (PHASE2, PHASE3)
- Safety and Efficacy of Combination Osimertinib and Ipilimumab in Patients w EGFR Mutated NSCLC (PHASE1)
- Combination of Osimertinib and Aspirin to Treat 1st Generation EGFR-TKI Resistance in NSCLC (PHASE2)
- Osimertinib Combined With Aspirin Neoadjuvant Therapy for Resectable EGFR Mutated NSCLC Patients. (PHASE2)
- Dose-Esc/Exp RMC4630 & Cobi in Relapsed/Refractory Solid Tumors & RMC4630& Osi in EGFR+ Locally Adv/Meta NSCLC (PHASE1, PHASE2)
- Combination of Osimertinib and Aspirin to Treat Osimertinib Resistance Non-small Cell Lung Cancer ( NSCLC)
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:
- Osimertinib (Osi) CI brief — competitive landscape report
- Osimertinib (Osi) updates RSS · CI watch RSS
- AbbVie portfolio CI