Vandetanib

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.

• CAPRELSA is indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Use CAPRELSA in patients with indolent, asymptomatic or slowly progressing disease only after careful consideration of the treatment related risks of CAPRELSA.

• Do not use in patients with congenital long QT syndrome [see Boxed Warning ] . Do not use in patients with congenital long QT syndrome.contraindicated

The recommended dose of CAPRELSA is 300 mg taken orally once daily until disease progression or unacceptable toxicity occurs. CAPRELSA may be taken with or without food. Do not take a missed dose within 12 hours of the next dose. Do not crush CAPRELSA tablets. The tablets can be dispersed in 2 ounces of water by stirring for approximately 10 minutes (will not completely dissolve). Do not use other liquids for dispersion. Swallow immediately after dispersion. Mix any remaining residue with 4 additional ounces of water and swallow. The dispersion can also be administered through nasogastric or gastrostomy tubes. 300 mg once daily. ( 2 ) CAPRELSA may be taken with or without food. ( 2 ) Dosage reduction may be necessary in the event of severe toxicities or QTc interval prolongation. ( 2.1 ) The starting dose is 200 mg in patients with moderate renal impairment. ( 2.1 ) 2.1 Dosage Adjustment For Adverse Reactions The 300 mg daily dose can be reduced to 200 mg (two 100 mg tablets) and then to 100 mg for Common Terminology Criteria for Adverse Events (CTCAE) Grade 3 or greater toxicities. Interrupt CAPRELSA for the following: Corrected QT interval, Fridericia (QTcF) greater than 500 ms: Resume at a reduced dose when the QTcF returns to less than 450 ms. CTCAE Grade 3 or greater toxicity: Resume at a reduced dose when the toxicity resolves or improves to CTCAE Grade 1. For recurrent toxicities, reduce the dose of CAPRELSA to 100 mg after resolution or improvement to CTCAE Grade 1 severity, if continued treatment is warranted.

Prolonged QT interval, torsades de pointes, and sudden death: Monitor electrocardiograms and levels of serum potassium, calcium, magnesium and TSH. Reduce CAPRELSA dose as appropriate. ( 2.1 , 5.1 ) Severe skin reactions, including toxic epidermal necrolysis and Stevens-Johnson syndrome, some fatal. Discontinue CAPRELSA for severe skin reactions. ( 2.1 , 5.2 ) Interstitial lung disease (ILD), including fatalities: investigate unexplained non-specific respiratory signs and symptoms. Discontinue CAPRELSA for confirmed ILD. ( 2.1 , 5.3 ) Ischemic cerebrovascular events, hemorrhage, heart failure, diarrhea, hypertension, and reversible posterior leukoencephalopathy syndrome: Discontinue or interrupt CAPRELSA. ( 2.1 , 5.4 , 5.5 , 5.6 , 5.7 , 5.9 , 5.10 ) Impaired wound healing: Withhold for at least 1 month prior to elective surgery. Do not administer CAPRELSA for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of treatment with CAPRELSA after resolution of wound healing complications has not been established. ( 5.14 ) Embryo-fetal toxicity: Can cause fetal harm. Advise women of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.15 , 8.1 ) Osteonecrosis, including osteonecrosis of the jaw: Withhold CAPRELSA for 1 month prior to scheduled dental surgery and permanently discontinue if osteonecrosis occurs ( 5.16 , 6.2 ). 5.1 QT Prolongation and Torsades de Pointes CAPRELSA can prolong the QT interval in a concentration-dependent manner [see Clinical Pharmacology (12.2) ] .

The following serious adverse reactions are discussed elsewhere in the label: QT Prolongation and Torsades de Pointes [see Boxed Warning , Warnings and Precautions (5.1) ] Severe Skin Reactions [see Warnings and Precautions (5.2) ] Interstitial Lung Disease [see Warnings and Precautions (5.3) ] Ischemic Cerebrovascular Events [see Warnings and Precautions (5.4) ] Hemorrhage [see Warnings and Precautions (5.5) ] Heart Failure [see Warnings and Precautions (5.6) ] Diarrhea [see Warnings and Precautions (5.7) ] Hypothyroidism [see Warnings and Precautions (5.8) ] Hypertension [see Warnings and Precautions (5.9) ] Reversible Posterior Leukoencephalopathy Syndrome [see Warnings and Precautions (5.10) ] Renal Failure [see Warnings and Precautions (5.12) ] Embryo-Fetal Toxicity [see Warnings and Precautions (5.15) ] Osteonecrosis [see Warnings and Precautions (5.16) ] The most common adverse drug reactions (>20%) seen with CAPRELSA and with a between-arm difference of ≥5 % have been diarrhea/colitis, rash, acneiform dermatitis, hypertension, nausea, headache, upper respiratory tract infections, decreased appetite and abdominal pain. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, Contact Sanofi Genzyme at 1-800-633-1610 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

8.1 Pregnancy Risk Summary Based on its mechanism of action and findings in animals, CAPRELSA can cause fetal harm when administered to a pregnant woman. There are no available human data on CAPRELSA use in pregnant women to inform a drug-associated risk. Vandetanib is embryotoxic, fetotoxic, and induced fetal malformations in rats at exposures less than or equal to those expected at the recommended human dose of 300 mg/day. Advise patients of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal data In reproductive toxicity studies, administration of vandetanib to female rats prior to mating and through the first week of pregnancy at a dose of 25 mg/kg/day (approximately equal to the human exposure at the 300 mg clinical dose based on C max ), there were increases in pre-implantation loss and post-implantation loss resulting in a reduction in the number of live embryos. During organogenesis, vandetanib caused an increase in post-implantation loss, including occasional total litter loss at a dose of 25 mg/kg/day.

Metabolism

A population pharmacokinetic analysis of CAPRELSA was conducted in 231 patients with MTC following oral administration of 300 mg daily doses. The pharmacokinetics of CAPRELSA at the 300 mg dose in MTC patients are characterized by a mean clearance of approximately 13.2 L/h, a mean volume of distribution of approximately 7450 L, and a median plasma half-life of 19 days.

In the event of an overdose, monitor patients closely for QTc prolongation. Adverse events including QT interval prolongation should be monitored closely as they may not resolve fully until approximately three plasma half-lives of the drug.

• Apr 6, 2011NDANDA022405Genzyme Corp

1. 1Diarrhoea32318%
2. 2Fatigue1709.6%
3. 3Rash1709.6%
4. 4Electrocardiogram Qt Prolonged1418.0%
5. 5Hypertension1116.3%
6. 6Nausea1076.0%
7. 7Acne955.4%
8. 8Disease Progression804.5%
9. 9Blood Pressure Increased774.3%
10. 10Asthenia754.2%
11. 11Dyspnoea754.2%
12. 12Death724.1%
13. 13Headache703.9%
14. 14Decreased Appetite613.4%
15. 15Off Label Use583.3%

The 10 most recently updated of 114 ClinicalTrials.gov registrations naming Vandetanib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• 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
  Completed · Phase 3 · Interventional · 205 enrolled · Sanofi
  NCT01298323updated 2026-04-17
• A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer
  Active not recruiting · Phase 3 · Interventional · 291 enrolled · Loxo Oncology, Inc.
  NCT04211337updated 2026-03-19
• Vandetanib and Everolimus in Treating Patients With Advanced or Metastatic Cancer
  Completed · Phase 1 · Interventional · 151 enrolled · M.D. Anderson Cancer Center
  NCT01582191updated 2025-10-27
• To Compare The Effects Of Two Doses Of Vandetanib In Patients With Advanced Medullary Thyroid Cancer
  Completed · Phase 4 · Interventional · 81 enrolled · Sanofi
  NCT01496313updated 2025-10-03
• An Efficacy Study Comparing ZD6474 to Placebo in Medullary Thyroid Cancer
  Completed · Phase 3 · Interventional · 331 enrolled · Genzyme, a Sanofi Company
  NCT00410761updated 2025-09-24
• Clinical Trial Comparing Gemcitabine and Vandetanib Therapy With Gemcitabine Alone in Pancreatic Carcinoma
  Completed · Phase 2 · Interventional · 142 enrolled · University of Liverpool
  NCT01601808updated 2025-03-13
• SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer
  Active not recruiting · Phase 2 · Interventional · 1,460 enrolled · UNICANCER
  NCT02299999updated 2025-01-15
• Efficacy Study Comparing ZD6474 in Combination With Pemetrexed and Pemetrexed Alone in 2nd Line NSCLC Patients
  Completed · Phase 3 · Interventional · 698 enrolled · Genzyme, a Sanofi Company
  NCT00418886updated 2024-12-31
• Observational Study to Evaluate Vandetanib in RET -/+ Patients With Metastatic Medullary Thyroid Cancer
  Completed · Observational · 31 enrolled · Genzyme, a Sanofi Company
  NCT01945762updated 2024-12-18
• Efficacy of Organoid-Based Drug Screening to Guide Treatment for Locally Advanced Thyroid Cancer
  Recruiting · Phase 2 · Interventional · 75 enrolled · West China Hospital
  NCT06482086updated 2024-12-05

Frequently asked questions

How does Vandetanib work?

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.

What is Vandetanib used for?

According to FDA labeling, Vandetanib carries indications including: CAPRELSA is indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Use CAPRELSA in patients with indolent, asymptomatic or slowly progressing disease only after careful consideration of the treatment related risks of CAPRELSA.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Vandetanib?

Vandetanib is classified as Other protein kinase inhibitors, Kinase Inhibitor, Organic Cation Transporter 2 Inhibitors, P-Glycoprotein Inhibitors, Protein Kinase Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration, Vascular Growth Decrease.

What are the brand names for Vandetanib?

Vandetanib is marketed under brand names including Caprelsa.

What are the contraindications for Vandetanib?

Vandetanib labeling lists contraindications including: Do not use in patients with congenital long QT syndrome [see Boxed Warning ] . Do not use in patients with congenital long QT syndrome.. Always consult the full prescribing information and a clinician.