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Cometriq (CABOZANTINIB)
Cometriq works by blocking the activity of vascular endothelial growth factor receptor 2, a protein involved in tumor growth and angiogenesis.
Cabozantinib (Cometriq), developed by Exelixis Inc., is a marketed drug primarily indicated for progressive, metastatic medullary thyroid cancer, with a key composition patent expiring in 2028. Its mechanism of action, which blocks vascular endothelial growth factor receptor 2, provides a strong therapeutic profile against tumor growth and angiogenesis, distinguishing it from off-patent competitors like sunitinib and pazopanib. The primary risk to Cometriq's market position is the upcoming patent expiry of sorafenib and vandetanib in 2028, and regorafenib in 2030, which could intensify competition from patent-protected and generic alternatives.
At a glance
| Generic name | CABOZANTINIB |
|---|---|
| Sponsor | Exelixis Inc |
| Drug class | Kinase Inhibitor |
| Target | Vascular endothelial growth factor receptor 2 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2012 |
Mechanism of action
In vitro biochemical and/or cellular assays have shown that cabozantinib inhibits the tyrosine kinase activity of RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, ROS1, TYRO3, MER, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment.
Approved indications
- Progressive, Metastatic Medullary Thyroid Cancer
Common side effects
- Diarrhea
- Stomatitis
- Nausea
- Oral pain
- Constipation
- Abdominal pain
- Decreased weight
- Decreased appetite
- Fatigue
- Hypertension
- Hair color changes
- Dysgeusia
Drug interactions
- P-glycoprotein Substrates
- boceprevir
- carbamazepine
- clarithromycin
- dexamethasone
- enzalutamide
- fosphenytoin
- indinavir
- itraconazole
- ketoconazole
- mibefradil
- nefazodone
Key clinical trials
- Cabozantinib S-malate in Treating Patients With Relapsed Osteosarcoma or Ewing Sarcoma (PHASE2)
- Comparing Retreatment of 177Lu-DOTATATE PRRT Versus the Usual Treatment in Patients With Metastatic Unresectable Gastroenteropancreatic Neuroendocrine Tumors, NET RETREAT Trial (PHASE2)
- Cabozantinib S-malate and Nivolumab With or Without Ipilimumab in Treating Patients With Metastatic Genitourinary Tumors (PHASE1)
- BiCaZO: A Study Combining Two Immunotherapies (Cabozantinib and Nivolumab) to Treat Patients With Advanced Melanoma or Squamous Cell Head and Neck Cancer, an immunoMATCH Pilot Study (PHASE2)
- Testing Cabozantinib in Patients With Advanced Pancreatic Neuroendocrine and Carcinoid Tumors (PHASE3)
- A Study to Test the Addition of the Drug Cabozantinib to Chemotherapy in Patients With Newly Diagnosed Osteosarcoma (PHASE2,PHASE3)
- Testing the Addition of an Anti-cancer Drug, Sapanisertib, to the Usual Chemotherapy Treatment (Cabozantinib) in Metastatic Liver Cell Cancer With a Change in Genes for the Protein β-Catenin, The SAPHIRE Trial (PHASE1,PHASE2)
- Immunotherapy With Nivolumab and Ipilimumab Followed by Nivolumab or Nivolumab With Cabozantinib for Patients With Advanced Kidney Cancer, The PDIGREE Study (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Cometriq CI brief — competitive landscape report
- Cometriq updates RSS · CI watch RSS
- Exelixis Inc portfolio CI