The Sound of Evolution
Osimertinib
Mechanism of action:
Osimertinib is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor. Osimertinib mainly acts on mutant epidermal growth factor receptor (EGFR) and forms a covalent bond with the receptor's tyrosine kinase domain, thereby inhibiting receptor signaling. As a result, downstream signaling pathways including PI3K-AKT, MAPK-ERK, and JAK-STAT are blocked, which suppresses cell proliferation and triggers apoptosis.
Reference(s):
1. Xu M et al. (2015). The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC). Ann Transl Med.
2. Tan CS et al. (2015). Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer. Lancet Oncol.
3. Ayeni D et al. (2015). Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer. Clin Cancer Res.