Small molecule
PubChem CID 71496458
Osimertinib
Tagrisso
- Mechanism of action
- EGFR tyrosine kinase inhibitor (mutant-selective: exon 19 deletion, L858R, and T790M)
- In plain language
- Selectively shuts down a mutated growth-signal receptor that is driving the lung cancer's growth, while mostly sparing the normal, non-mutated version of that receptor.
- How it works
- Osimertinib is an irreversible, third-generation EGFR tyrosine kinase inhibitor that covalently binds mutant EGFR forms — exon 19 deletions, L858R, and the T790M resistance mutation — at substantially lower concentrations than wild-type EGFR. By occupying the ATP-binding site of the kinase domain, it blocks downstream signaling that drives tumor cell proliferation and survival. The drug also achieves meaningful central nervous system penetration, supporting activity against brain metastases common in EGFR-mutant NSCLC.
- Therapeutic applications
- Indicated, in EGFR exon 19 deletion- or exon 21 L858R-mutated NSCLC, as adjuvant therapy after tumor resection, for locally advanced unresectable disease that has not progressed after chemoradiation, and as first-line monotherapy or combination therapy for metastatic disease. Also indicated for metastatic EGFR T790M mutation-positive NSCLC that has progressed on or after prior EGFR TKI therapy.
- Class
- Small molecule
- Therapeutic area
- Oncology
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