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Caprelsa (VANDETANIB)
Caprelsa works by blocking a specific protein that helps cancer cells grow and spread.
At a glance
| Generic name | VANDETANIB |
|---|---|
| Sponsor | Sanofi |
| Drug class | Kinase Inhibitor [EPC] |
| Target | Receptor-interacting serine/threonine-protein kinase 2 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2011 |
Mechanism of action
In vitro studies have shown that vandetanib inhibits the tyrosine kinase activity of the EGFR and VEGFR families, RET, BRK, TIE2, and members of the EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. In addition, the N-desmethyl metabolite of the drug, representing to 17.1% of vandetanib exposure, has similar inhibitory activity to the parent compound for VEGF receptors (KDR and Flt-1) and EGFR. In vitro, vandetanib inhibited epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. In vivo, vandetanib administration reduced tumor cell-induced angiogenesis, tumor vessel permeability, and inhibited tumor growth and metastasis in mouse models
Approved indications
- Carcinoma of thyroid
- Medullary thyroid carcinoma
Boxed warnings
- WARNING: QT PROLONGATION, TORSADES DE POINTES, AND SUDDEN DEATH CAPRELSA can prolong the QT interval. Torsades de pointes and sudden death have occurred in patients receiving CAPRELSA. Do not use CAPRELSA in patients with hypocalcemia, hypokalemia, hypomagnesemia, or long QT syndrome. Correct hypocalcemia, hypokalemia and/or hypomagnesemia prior to CAPRELSA administration. Monitor electrolytes periodically. Avoid drugs known to prolong the QT interval [see Warnings and Precautions (5.1) ] . WARNING: QT PROLONGATION, TORSADES DE POINTES, AND SUDDEN DEATH See full prescribing information for complete boxed warning. CAPRELSA can prolong the QT interval. Torsades de pointes and sudden death have occurred in patients receiving CAPRELSA. Do not use CAPRELSA in patients with hypocalcemia, hypokalemia, hypomagnesemia, or long QT syndrome. Correct hypocalcemia, hypokalemia and/or hypomagnesemia prior to CAPRELSA administration. Monitor electrolytes periodically. Avoid drugs known to prolong the QT interval ( 5.1 ).
Common side effects
- Diarrhea/Colitis
- Rash
- Acneiform Dermatitis
- Hypertension
- Nausea
- Headache
- Upper Respiratory Tract Infections
- Decreased Appetite
- Abdominal Pain
- Fatigue
- Dyspepsia
- Vomiting
Drug interactions
- High Risk QT Prolonging Agents
- P-glycoprotein Substrates
- abarelix
- apomorphine
- arsenic trioxide
- astemizole
- carbamazepine
- chloroquine
- chlorpromazine
- clarithromycin
- dasatinib
- dexamethasone
Key clinical trials
- A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer (PHASE3)
- Vandetanib and Everolimus in Treating Patients With Advanced or Metastatic Cancer (PHASE1)
- To Compare The Effects Of Two Doses Of Vandetanib In Patients With Advanced Medullary Thyroid Cancer (PHASE4)
- An Efficacy Study Comparing ZD6474 to Placebo in Medullary Thyroid Cancer (PHASE3)
- Study to Determine if Contacting Patients With MTC More Frequently Results in Earlier Detection and Treatment of Signs and Symptoms of AEs and Thus a Decrease in the Percentage of Time Patients Experience AEs During First 12 Months on Vandetanib Treatment (PHASE3)
- Clinical Trial Comparing Gemcitabine and Vandetanib Therapy With Gemcitabine Alone in Pancreatic Carcinoma (PHASE2)
- SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (PHASE2)
- Efficacy Study Comparing ZD6474 in Combination With Pemetrexed and Pemetrexed Alone in 2nd Line NSCLC Patients (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:
- Caprelsa CI brief — competitive landscape report
- Caprelsa updates RSS · CI watch RSS
- Sanofi portfolio CI