How is Caprelsa (vandetanib) administered?

300 mg orally once daily Take with or without food Dose reductions: 200 mg, then 100 mg Renal impairment (CrCl Start at 200 mg QTc monitoring: ECG at baseline, at 2-4 weeks, at 8-12 weeks, then every 3 months. Monitor after dose reductions.

Caprelsa (vandetanib) — Package Insert Navigator

1. Indications and Usage

Symptomatic or progressive medullary thyroid cancer (MTC) in patients with unresectable, locally advanced, or metastatic disease. Use is restricted to patients with MTC who are symptomatic or progressive and for whom no locally curative surgical options exist.

2. Dosage and Administration

300 mg orally once daily
Take with or without food
Dose reductions: 200 mg, then 100 mg
Renal impairment (CrCl <50 mL/min): Start at 200 mg
QTc monitoring: ECG at baseline, at 2-4 weeks, at 8-12 weeks, then every 3 months. Monitor after dose reductions.

3. Dosage Forms and Strengths

Tablets: 100 mg, 300 mg

4. Contraindications

Congenital long QT syndrome. Do not use if QTc >500 ms.

5. Warnings and Precautions

⚠ Boxed Warning

QT PROLONGATION, TORSADES DE POINTES, AND SUDDEN DEATH: Caprelsa can prolong the QT interval. Torsades de pointes and sudden death have occurred. Do not use in patients with hypocalcemia, hypokalemia, hypomagnesemia, or long QT syndrome. Available only through the Caprelsa REMS program.

QT Prolongation: Reported in 36% of patients. Requires REMS restricted distribution. Monitor ECGs and electrolytes.
Skin Reactions: Including Stevens-Johnson syndrome and erythema multiforme. Rash in 53%, acne 35%, dermatitis 15%, photosensitivity 13%. Use sun protection.
Interstitial Lung Disease (ILD): Reported in 2%. Can be fatal. Withhold and evaluate for new respiratory symptoms.
Ischemic Cerebrovascular Events: Reported in 1.3%.
Hemorrhage: Serious including fatal hemorrhagic events.
Diarrhea: Grade 3+ in 11%. Manage aggressively.
Hypertension: Reported in 33%. Monitor and treat.
Reversible Posterior Leukoencephalopathy Syndrome

6. Adverse Reactions

Most Common Adverse Reactions

Diarrhea (57%), rash (53%), acne (35%), nausea (33%), hypertension (33%), headache (26%), fatigue (24%), decreased appetite (21%), abdominal pain (21%), QTc prolongation (36%)

Diarrhea

57%

Rash

53%

QTc prolongation

36%

Acne

35%

Nausea

33%

Hypertension

33%

Headache

26%

Fatigue

24%

Decreased Appetite

21%

Abdominal Pain

21%

7. Drug Interactions

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

8. Use in Specific Populations

Pregnancy

Consult the full prescribing information for pregnancy-related considerations.

Lactation

Refer to prescribing information for lactation guidance.

Pediatric Use

Pediatric safety and efficacy information is detailed in the full label.

Hepatic/Renal Impairment

Dose modifications for organ impairment are specified in the complete prescribing information.

12. Clinical Pharmacology

Mechanism of Action

Vandetanib is an inhibitor of multiple receptor tyrosine kinases including VEGFR-2 (KDR), EGFR (HER1), RET, BRK, TIE2, members of the EPH receptor family, and Src kinase family members. RET kinase inhibition is particularly relevant for medullary thyroid cancer, which frequently harbors activating RET mutations. The combined anti-VEGFR and anti-EGFR activity provides both anti-angiogenic and direct anti-tumor effects.

Pharmacokinetics

Tmax: median 6 hours (range 4-10). Half-life: 19 days. Protein binding: ~90%. Metabolized by CYP3A4. Steady-state at ~3 months. Excreted in feces (44%) and urine (25%).

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials

ZETA — Vandetanib vs. placebo in advanced medullary thyroid cancer. Phase III, n=331.
🔬 NCT00410761 ↗ 📄 Primary Publication ↗

Additional Resources

📋 All Vandetanib Trials on ClinicalTrials.gov ↗ 📚 PubMed: Vandetanib Clinical Trials ↗

FDA-Approved Tumor Types

Caprelsa has FDA-approved indications across the following cancer types covered on PipelineEvidence:

Thyroid Cancer

External Resources

📋 DailyMed Label ↗ 🏛️ FDA Drugs@FDA ↗ 🔬 ClinicalTrials.gov ↗ 📚 PubMed Pivotal Trials ↗

Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Caprelsa. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.