[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [VEGFR multikinase inhibitors](https://durgical.com/en/pharmacology/classes/vegfr-multikinase-inhibitors/) › Cabozantinib

# Cabozantinib

## VEGFR multikinase inhibitors?

VEGFR multikinase inhibitors

## High alert?

An error with this medicine can cause serious harm: double checks and protocols are used.

## Pregnancy: avoid?

Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men…

A multikinase inhibitor of VEGFR2, MET and RET for kidney, liver and thyroid cancers and NETs. Not used with recent serious bleeding.

Updated Nov 1, 2026

Also called: cabozantinib-S-malate

## Quick facts

**Group**
[VEGFR multikinase inhibitors](https://durgical.com/en/pharmacology/classes/vegfr-multikinase-inhibitors/)

**Target**
MET, VEGFR2, RET and KIT tyrosine kinases

**Used for**
Advanced renal cell carcinoma · Previously treated

**Key effects**
Diarrhoea · Fatigue and weight loss · Hypertension

**Monitor**
Blood pressure regularly · Signs of bleeding

**ATC**
L01EX07

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**MET, VEGFR2, RET and KIT tyrosine kinases**Cabozantinib

ⓘ The figure shows cabozantinib in the ATP pocket of the human MET kinase; it also blocks VEGFR2.

**Target in 3D:** MET, VEGFR2, RET and KIT tyrosine kinases. PDB structure 9T2V (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/9T2V) · Drag to rotate · pinch to zoom

Cabozantinib inhibits several tyrosine kinases, most potently VEGFR2, then MET, RET and KIT. Blocking VEGFR2 cuts angiogenesis, blocking MET and KIT reaches growth signals of the tumour cell, and RET blockade fits its use in medullary thyroid cancer.

- Blocks VEGFR2, MET, RET and KIT kinases
- VEGFR2: angiogenesis stops; MET and KIT: tumour signals cut
- RET: activity in medullary thyroid cancer

## Indications

- Advanced renal cell carcinoma, alone or first line with nivolumab. [Renal cell carcinoma →](https://durgical.com/en/conditions/renal-cell-carcinoma/)
- Hepatocellular carcinoma previously treated with sorafenib. [Hepatocellular carcinoma →](https://durgical.com/en/conditions/hepatocellular-carcinoma/)
- Progressive metastatic medullary thyroid cancer. [Medullary thyroid carcinoma →](https://durgical.com/en/conditions/medullary-thyroid-carcinoma/)
- Differentiated thyroid cancer that no longer responds to radioactive iodine, after VEGFR-targeted therapy. [Thyroid cancer (papillary) →](https://durgical.com/en/conditions/thyroid-cancer/)
- Previously treated, metastatic well-differentiated neuroendocrine tumours of the pancreas or other organs. [Pancreatic neuroendocrine tumours (VIPoma, glucagonoma, somatostatinoma, non-functioning) →](https://durgical.com/en/conditions/pancreatic-neuroendocrine-tumours/)

## Adverse effects

### Common

- Diarrhoea, nausea, vomiting, constipation
- Fatigue and weight loss
- Hand-foot skin reaction (red, painful, peeling palms and soles)
- Hypertension
- Mouth sores, taste changes, change of hair colour

### Serious (rare, important)

- Severe bleeding
- Gastrointestinal perforation and fistulas
- Thrombotic events
- Impaired wound healing; osteonecrosis of the jaw

## Contraindications

- Recent history of serious bleeding

## Key interactions

**Strong CYP3A4 inhibitors (clarithromycin, itraconazole, ketoconazole, ritonavir) and grapefruit**
Raise cabozantinib exposure.

**Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, St John's wort)**
Lower its levels and can make it fail.

**Anticoagulants and antiplatelet drugs**
Add to its bleeding risk.

## What is monitored

- Blood pressure regularly
- Signs of bleeding, perforation or thrombosis
- Dental examination before and during treatment
- Laboratory tests as ordered

## Administration and safety

- Oral, once daily on an empty stomach, away from meals; swallowed whole, not split, crushed or opened.
- Capsule and tablet products are approved for different cancers: check that the form dispensed matches the order.
- Grapefruit, its juice and St John's wort are avoided because they change its levels.
- Stopped before planned surgery or dental surgery and restarted only when the wound has healed, as the doctor directs.

## Pregnancy and breastfeeding

Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men with partners who could conceive), and breastfeeding is avoided.

## Nursing care

- Measure blood pressure at every visit and teach home monitoring if ordered.
- Teach to report bleeding, black stools, vomiting blood, severe abdominal pain, chest pain or stroke symptoms at once.
- Advise a dental check before starting and to tell any dentist or surgeon about the drug.
- Confirm a negative pregnancy test before the first dose and teach contraception during treatment and afterwards.

## Pharmacokinetics

**Absorption**
Oral, once daily, on an empty stomach.

**Metabolism**
Liver, CYP3A4.

**Half-life**
Long: about 99 hours.

## Memory aid

«CABOzantinib carries the METals»: MET + RET + VEGFR2; think RET for medullary thyroid cancer.

## Test yourself

Think of the answer, then tap the question to see it.

## Which kinase targets of cabozantinib explain its use in medullary thyroid cancer?

RET, together with VEGFR2.

## In which liver cancer setting is cabozantinib used?

Hepatocellular carcinoma after sorafenib.

## Which history makes cabozantinib unsuitable?

A recent serious bleeding episode.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/cabozantinib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

**Pregnancy: avoid**
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men…

## Connections

## Related drugs 3

- [Lenvatinib](https://durgical.com/en/pharmacology/lenvatinib/)
- [Sorafenib](https://durgical.com/en/pharmacology/sorafenib/)
- [Nivolumab](https://durgical.com/en/pharmacology/nivolumab/)

## Related conditions 5

- [Renal cell carcinoma](https://durgical.com/en/conditions/renal-cell-carcinoma/)
- [Hepatocellular carcinoma](https://durgical.com/en/conditions/hepatocellular-carcinoma/)
- [Medullary thyroid carcinoma](https://durgical.com/en/conditions/medullary-thyroid-carcinoma/)
- [Thyroid cancer (papillary)](https://durgical.com/en/conditions/thyroid-cancer/)
- [Pancreatic neuroendocrine tumours (VIPoma, glucagonoma, somatostatinoma, non-functioning)](https://durgical.com/en/conditions/pancreatic-neuroendocrine-tumours/)

[← Back to the class: VEGFR multikinase inhibitors](https://durgical.com/en/pharmacology/classes/vegfr-multikinase-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Cabozantinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a616037.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [Cabozantinib-S-Malate - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/cabozantinib-s-malate) (National Cancer Institute, 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EX07) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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