Small molecule · Oncology

Osimertinib

Tagrisso
Small moleculeEGFR tyrosine kinase inhibitor (mutant-selective: exon 19 deletion, L858R, and T790M)

PubChem CID 71496458 · 3D model

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Selectively shuts down a mutated growth-signal that is driving the lung cancer's growth, while mostly sparing the normal, non-mutated version of that receptor.

How it works

Lung cancer cells with certain EGFR gene mutations rely on a constantly switched-on growth signal to keep multiplying. Osimertinib locks onto that mutated switch and jams it shut, while mostly leaving the normal version of the same receptor, found in healthy cells, alone — this selectivity is part of why side effects tend to be more manageable than older-generation drugs in this class. Because it can reach into brain tissue, it also helps control cancer that has spread to the brain.

What it’s used for

Approved for non-small cell lung cancer driven by specific EGFR gene mutations. Used after surgery to help prevent the cancer from returning, for cancer that hasn't spread but can't be removed by surgery, and as an initial treatment for cancer that has spread to other parts of the body. Also used for advanced lung cancer that has developed a specific resistance mutation after treatment with an earlier EGFR-targeting drug.

Mechanism
EGFR (mutant-selective: exon 19 deletion, L858R, and T790M)
Drug class
Therapeutic area
Oncology

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