TAGRISSO (osimertinib mesylate)
TAGRISSO is indicated for the treatment of Adjuvant therapy after tumor resection in adult patients with EGFR exon 19 deletions or exon 21 L858R mutation-positive non-small cell lung cancer (NSCLC); Locally advanced, unresectable (stage III) EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC that has not progressed during or following platinum-based chemoradiation therapy; First-line treatment of adult patients with metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC; First-line treatment of adult patients with locally advanced or metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC, in combination with pemetrexed and platinum-based chemotherapy; Metastatic EGFR T790M mutation-positive NSCLC in patients whose disease has progressed on or after EGFR tyrosine kinase inhibitor therapy.
How TAGRISSO Works
Osimertinib is a kinase inhibitor that binds irreversibly to mutant forms of the epidermal growth factor receptor (EGFR), such as exon 19 deletions and L858R mutations. By targeting these mutations at lower concentrations than wild-type EGFR, the drug inhibits the signaling pathways that drive tumor growth. The medication and its active metabolites also inhibit other kinases, including HER2 and HER4, and have demonstrated the ability to distribute to the brain in animal models.
Details
- Status
- Prescription
- First Approved
- 2015-11-13
- Patent Cliff
- 2042
- Revenue
- $1.9B (Q4-2025)
- Routes
- ORAL
- Dosage Forms
- TABLET
TAGRISSO Approval History
What TAGRISSO Treats
5 indicationsTAGRISSO is approved for 5 conditions since its original approval in 2015. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Adjuvant therapy after tumor resection in adult patients with EGFR exon 19 deletions or exon 21 L858R mutation-positive non-small cell lung cancer (NSCLC)
- Locally advanced, unresectable (stage III) EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC that has not progressed during or following platinum-based chemoradiation therapy
- First-line treatment of adult patients with metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC
- First-line treatment of adult patients with locally advanced or metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC, in combination with pemetrexed and platinum-based chemotherapy
- Metastatic EGFR T790M mutation-positive NSCLC in patients whose disease has progressed on or after EGFR tyrosine kinase inhibitor therapy
TAGRISSO Target & Pathway
ProTarget
A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.
Pathway Context
HER2 forms dimers with other HER family members to activate growth signaling
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
TAGRISSO Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TAGRISSO's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TAGRISSO treats. First-in-class if their pivotal trials read out positive.
Clinical Trial Registry
5 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06525246 | ONO-7475-03 jRCT2051210045 | Ph 1 | completed | Study of ONO-7475 in Combination With Osimertinib in EGFR Gene Mutation-positive Non-small Cell Lung Cancer |
| NCT07229729 | SHR-A2102-212 | Ph 2 | recruiting | A Study of SHR-A2102 in Combination With Other Anti-tumor Therapies for Resectable Non-small Cell Lung Cancer |
| NCT06829459 | SYH2065-002 | Ph 3 | recruiting | A Study to Evaluate the Efficacy and Safety of Glumetinib Combined With Osimertinib Mesylate Versus Platinum-based Doublet Chemotherapy in Non-Small Cell Lung Cancer Patients After Resistance to EGFR-TKIs |
| NCT06530719 | IRB-2024-701 | Ph 2 | not yet recruiting | A Study to Evaluate the Efficacy of Osimertinib in Patients With EGFR-sensitive Mutated Non-small Cell Lung Cancer Progression After Receiving Adjuvant Targeted Therapy Following Radical Surgery |
| NCT06306456 | GH21C201 | Ph 1, Ph 2 | recruiting | A Phase Ib/II Clinical Study of GH21 Capsules Combined With Osimertinib Mesylate Tablets in Patients With NSCLC |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TAGRISSO FDA Label Details
Indications & Usage
FDA Label (PDF)TAGRISSO is indicated for the treatment of Adjuvant therapy after tumor resection in adult patients with EGFR exon 19 deletions or exon 21 L858R mutation-positive non-small cell lung cancer (NSCLC); Locally advanced, unresectable (stage III) EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC that has not progressed during or following platinum-based chemoradiation therapy; First-line treatment of adult patients with metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC; First-line treatment of adult patients with locally advanced or metastatic EGFR exon 19 deletions or exon 21 L858R mutation-positive NSCLC, in combination with pemetrexed and platinum-based chemotherapy; Metastatic EGFR T790M mutation-positive NSCLC in patients whose disease has progressed on or after EGFR tyrosine kinase inhibitor therapy.
TAGRISSO Patents & Exclusivity
Patents (5 active)
Exclusivity
Pro Intelligence Preview
Deep insights for TAGRISSO
Revenue Insights
- • Q4-2025: $1.9B
- • Historical trend analysis
Patent Timeline
- • Cliff: 2042
- • 68 active patents
Trial Analysis
- • Clinical trial tracking
- • Development stage analysis
Competitive Landscape
- • Competitor tracking
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.