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Cabozantinib

Tyrosine Kinase Inhibitor · Antineoplastic agent

Tyrosine Kinase InhibitorAntineoplastic agent
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
D
FDA category + note
Top interactionssee all 12
  • AbarelixSevereDatabaseDDInter
  • AbciximabSevereDatabaseDDInter
  • AbirateroneSevereDatabaseDDInter
  • AcalabrutinibSevereDatabaseDDInter

Mechanism

Cabozantinib is an inhibitor of several protein kinases. It functions as a multikinase inhibitor, targeting pathways involved in cancer cell growth and progression.

Indications

Treatment of progressive, unresectable locally advanced or metastatic medullary thyroid carcinomaAdvanced renal cell carcinomaHepatocellular cancer (HCC) in the second-line setting (for patients with good performance status and intact liver function)systemic therapy of medullary thyroid cancer without regard to driver mutation statusadvanced RCC (as monotherapy and in combination with nivolumab)HCC who have been previously treated with sorafenibprogressive, metastatic medullary thyroid cancer

Dosing

Adult
For medullary thyroid carcinoma: 140 mg once daily by mouth using capsules. For advanced renal cell carcinoma: 60 mg once daily by mouth using tablets. For dose adjustment or treatment interruption due to side-effects, consult product literature (closely monitor for first 8 weeks of therapy). Note: Cabozantinib tablets and capsules are not bioequivalent.
Hepatic adjustment
The dose of cabozantinib should be reduced in patients with mild-to-moderate hepatic impairment.

Pharmacokinetics

Half-life
about 99 h (elimination)
Metabolism
CYP3A4 (substrate)

Contraindications

  • patients with a recent history of bleeding
  • patients with thromboembolic events

Side effects

Common
Palmar-plantar erythrodysaesthesia syndromediarrhea (≥25%)fatigue (≥25%)nausea (≥25%)PPES (≥25%)hypertension (≥25%)vomiting (≥25%)weight loss (≥25%)constipation (≥25%)
Serious
  • Reversible posterior leucoencephalopathy syndrome
  • Hypertension (discontinue treatment if uncontrolled)
  • Increased risk of fistulas
  • Increased risk of gastro-intestinal perforation
  • Increased risk of intra-abdominal abscess
  • GI perforations
  • fistulas

Pregnancy & lactation

Pregnancy

D

Drug interactions

Abarelix
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Abciximab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Abiraterone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Acalabrutinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adenosine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfuzosin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alimemazine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alteplase
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Tyrosine Kinase Inhibitor drugs

Ask House about Cabozantinib

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Sources: Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-10 · House clinical team