AFINITOR
Afinitor (everolimus) is a kinase inhibitor indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer **in combination with exemestane** after failure of letrozole or anastrozole. It is also indicated for adults with progressive neuroendocrine tumors (NET) of pancreatic origin, as well as progressive, **well-differentiated**, non-functional NET of gastrointestinal or lung origin that are unresectable, locally advanced, or metastatic. (Note: It is not indicated for functional carcinoid tumors). Additionally, it is used for advanced renal cell carcinoma (RCC) following failure of sunitinib or sorafenib. In the context of Tuberous Sclerosis Complex (TSC), Afinitor is indicated for renal angiomyolipoma not requiring immediate surgery and for subependymal giant cell astrocytoma (SEGA) requiring therapeutic intervention. **Afinitor Disperz** is specifically indicated as **adjunctive** treatment for adult and pediatric patients (aged 2 years and older) with TSC-associated partial-onset seizures.
How AFINITOR Works
Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR), a serine-threonine kinase downstream of the PI3K/AKT pathway. By binding to the intracellular protein FKBP-12, everolimus forms a complex that inhibits mTOR Complex 1 (mTORC1). This inhibition reduces the activity of downstream effectors **S6 ribosomal protein kinase (S6K1) and eukaryotic initiation factor 4E-binding protein (4E-BP1)**, which are critical for protein synthesis. These molecular effects lead to decreased cell proliferation, reduced angiogenesis (via suppression of HIF-1 and vascular endothelial growth factor [VEGF] expression), and diminished glucose uptake
Details
- Status
- Prescription
- First Approved
- 2009-03-30
- Routes
- ORAL
- Dosage Forms
- TABLET
AFINITOR Approval History
What AFINITOR Treats
7 indicationsAFINITOR is approved for 7 conditions since its original approval in 2009. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Breast Cancer
- Neuroendocrine Tumors
- Renal Cell Carcinoma
- Renal Angiomyolipoma
- Tuberous Sclerosis Complex
- Subependymal Giant Cell Astrocytoma
- Seizures
AFINITOR Competitors
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Competitors share the same molecular target (HER2). Earlier expiry dates signal biosimilar/generic opportunities.
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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.
AFINITOR FDA Label Details
ProIndications & Usage
FDA Label (PDF)AFINITOR is a kinase inhibitor indicated for the treatment of: Postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole. Adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic. Limitations of Use: AFINITOR is not indicated for the treatment of patients with functional carc...
AFINITOR Patents & Exclusivity
Patents (48 active)
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.