GILOTRIF (afatinib dimaleate)
Gilotrif helps patients with metastatic non-small cell lung cancer (NSCLC) that features specific, non-resistant EGFR mutations. It is used as a first-line option for these patients once an approved test confirms the mutation type. Additionally, it treats metastatic squamous NSCLC in patients whose disease has progressed following platinum-based chemotherapy.
How GILOTRIF Works
This medication works by covalently binding to the kinase domains of EGFR, HER2, and HER4, which irreversibly blocks the signaling pathways that drive tumor growth. By inhibiting the autophosphorylation of these receptors, the drug prevents the uncontrolled cell proliferation often caused by specific genetic mutations. This process effectively downregulates ErbB signaling to help slow or stop the progression of the cancer.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2013-07-12
- Patent Cliff
- 2031
- Routes
- ORAL
- Dosage Forms
- TABLET
GILOTRIF Approval History
What GILOTRIF Treats
1 indicationsGILOTRIF is approved for 1 conditions since its original approval in 2013. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Non-Small Cell Lung Cancer
GILOTRIF 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.
GILOTRIF 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 GILOTRIF's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications GILOTRIF treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to GILOTRIF
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
8 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT02465060 | NCI-2015-00054 NCI-2015-00054, EAY131 | Ph 2 | active not recruiting | Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) |
| NCT04439136 results posted | NCI-2020-03140 NCI-2020-03140, EAY131-B | Ph 2 | active not recruiting | Testing Afatinib as a Potential Targeted Treatment in Cancers With HER2 Genetic Changes (MATCH-Subprotocol B) |
| NCT02438722 results posted | S1403 NCI-2014-02405, BI 1200.124 | Ph 2, Ph 3 | completed | S1403, Afatinib Dimaleate With or Without Cetuximab in Treating Patients With Newly Diagnosed Stage IV or Recurrent, EGFR Mutation Positive Non-small Cell Lung Cancer |
| NCT02122172 results posted | 13-0540 NCI-2014-00859, IRB13-0540 | Ph 2 | terminated | Afatinib in Advanced Refractory Urothelial Cancer |
| NCT02364609 results posted | 704874 UCDCC#250, 1200.237 | Ph 1 | completed | Pembrolizumab and Afatinib in Patients With Non-small Cell Lung Cancer With Resistance to Erlotinib |
| NCT02451553 | 9078 NCI-2015-00684, 9078 | Ph 1 | completed | Afatinib Dimaleate and Capecitabine in Treating Patients With Advanced Refractory Solid Tumors, Pancreatic Cancer or Biliary Cancer |
| NCT02747953 | 2011-09-011 | Ph 2 | completed | Gilotrif (Afatinib) in Advanced Non-Small Cell Lung Cancer Patients Pre-treated With Erlotinib or Gefitinib |
| NCT02541903 results posted | F150330009 (UAB 14113) | Ph 2 | terminated | Trial Using Gilotrif for Advanced Penile Squamous Cell Carcinoma |
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.
GILOTRIF FDA Label Details
Indications & Usage
FDA Label (PDF)GILOTRIF is indicated for the treatment of Non-Small Cell Lung Cancer.
GILOTRIF Patents & Exclusivity
Patents (10 active)
Pro Intelligence Preview
Deep insights for GILOTRIF
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2031
- • 90 active patents
Trial Analysis
- • 8 total trials
- • Stage: Stable
Competitive Landscape
- • 20 similar drugs
- • 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.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment