Osimertinib · Tagrisso, AZD-9291

What is Osimertinib?

Osimertinib is an orally available, irreversible kinase inhibitor that covalently binds mutant forms of EGFR, including T790M, L858R and exon 19 deletions, at lower concentrations than wild-type EGFR. Its active metabolites AZ7550 and AZ5104 contribute similar inhibition. It is studied in EGFR-mutated non-small cell lung cancer, small cell lung cancer and breast cancer.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Tagrisso, AZD-9291

Drug type

Small molecule

Targets

epidermal growth factor receptor (EGFR), HER2 (ERBB2) (secondary target), HER3 (ERBB3) (secondary target), HER4 (ERBB4) (secondary target)

Mechanism

Inhibitor of epidermal growth factor receptor (EGFR)

Pathways

EGFR-mediated signaling, tumor cell proliferation

Therapy area

Oncology

Developer

Astrazeneca

In trials of

AAPG, ABBV, APLM, BMY, JAZZ, PBYI, SMMT

FDA status

Approved as Tagrisso (November 13, 2015), NDA208065 · FDA label

UNII

3C06JJ0Z2O

✅ FDA-approved uses

• Non-small cell lung cancer

From the indications section of the FDA label (version of Sep 25, 2024). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Breast CancerEGFR Positive Non-small Cell Lung CancerLung CancerMetastatic Non Small Cell Lung CancerNon-Small Cell Lung CancerSmall Cell Lung Cancer ( SCLC )Transformed Small Cell Lung CancerEGFR Gene MutationLung Cancer Metastatic

Other drugs acting on EGFR

Sources

• FDA label (DailyMed)
• FDA label Tagrisso (2024-09-25), indications
• NCI Thesaurus
• NCI Thesaurus
• ClinicalTrials.gov NCT04001777
• ClinicalTrials.gov NCT04085315
• ClinicalTrials.gov NCT06618287
• ClinicalTrials.gov NCT07153055

Updated Oct 11, 2026.