Osimertinib: First Global Approval.

Area of Science:

• Oncology
• Pharmacology
• Medical Chemistry

Background:

• Non-small cell lung cancer (NSCLC) is a leading cause of cancer death.
• Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) is a significant challenge in NSCLC treatment.
• The EGFR T790M mutation is a common mechanism of acquired resistance.

Purpose of the Study:

• To summarize the development milestones of osimertinib.
• To highlight the approval of osimertinib for EGFR T790M-positive NSCLC.
• To discuss the potential of osimertinib in NSCLC treatment.

Main Methods:

• Osimertinib is a third-generation EGFR TKI.
• It selectively targets the EGFR T790M mutation.
• It spares wild-type EGFR.

Main Results:

• Osimertinib received accelerated approval in the USA in November 2015.
• It is indicated for metastatic EGFR T790M mutation-positive NSCLC patients with disease progression on EGFR TKI therapy.
• Osimertinib has demonstrated efficacy in clinical trials.

Conclusions:

• Osimertinib represents a significant advancement in targeted therapy for NSCLC.
• Its development addresses a critical unmet need in patients with acquired resistance.
• Further clinical development is ongoing for various treatment settings.