[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/) › Sunitinib

# Sunitinib

## 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…

An oral multikinase inhibitor (VEGFR, KIT, PDGFR) for kidney cancer, GIST after imatinib and pancreatic NETs. Boxed warning: liver damage.

Updated Nov 1, 2026

Also called: sunitinib malate, SU11248

## Quick facts

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

**Target**
VEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinases

**Used for**
Advanced renal cell carcinoma

**Key effects**
Fatigue · Hypertension · Diarrhoea

**Monitor**
Liver tests before and during treatment

**ATC**
L01EX01

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

✂**VEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinases**Sunitinib

ⓘ The figure shows sunitinib (SU11248) in the ATP pocket of the human VEGFR2 kinase domain.

**Target in 3D:** VEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinases. PDB structure 4AGD (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/4AGD) · Drag to rotate · pinch to zoom

Sunitinib blocks the ATP site of several receptor tyrosine kinases, including VEGFR2 and KIT. Inhibiting VEGFR cuts tumour angiogenesis, which is why it works in highly vascular kidney cancer; inhibiting KIT explains its activity in gastrointestinal stromal tumours that have become resistant to imatinib.

- Blocks the ATP site of VEGFR2, KIT, PDGFR and others
- VEGFR block: tumour angiogenesis stops
- KIT block: active in imatinib-resistant GIST

## Indications

- Advanced renal cell carcinoma, and adjuvant treatment after nephrectomy at high risk of recurrence. [Renal cell carcinoma →](https://durgical.com/en/conditions/renal-cell-carcinoma/)
- Gastrointestinal stromal tumour after progression on, or intolerance to, imatinib. [Gastrointestinal stromal tumour (GIST) →](https://durgical.com/en/conditions/gastrointestinal-stromal-tumour/)
- Progressive pancreatic neuroendocrine tumours that are unresectable or metastatic. [Pancreatic neuroendocrine tumours (VIPoma, glucagonoma, somatostatinoma, non-functioning) →](https://durgical.com/en/conditions/pancreatic-neuroendocrine-tumours/)

## Adverse effects

### Common

- Fatigue, often marked
- Hypertension
- Diarrhoea, nausea, mouth irritation, taste changes
- Hand-foot skin reaction (red, painful, peeling palms and soles)
- Yellow skin and lightening of the hair; hypothyroidism

### Serious (rare, important)

- Severe hepatotoxicity (boxed warning)
- Heart failure and reduced ejection fraction
- Arterial thrombosis (heart attack, stroke) and bleeding
- Gastrointestinal perforation
- Impaired wound healing; osteonecrosis of the jaw
- Bone marrow suppression

## Contraindications

- Used with great caution in liver disease

## Key interactions

**Strong CYP3A4 inhibitors (clarithromycin, itraconazole, ketoconazole, ritonavir) and grapefruit**
Raise its levels and its toxicity.

**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

- Liver tests before and during treatment
- Blood pressure regularly
- Thyroid function and complete blood count
- Echocardiogram, ECG and urine protein as ordered

## Administration and safety

- Oral; swallowed whole, never split, crushed, chewed or opened.
- For some cancers it is given in cycles with weeks off, for others every day: check the schedule on 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 jaundice, dark urine, itching or right upper abdominal pain.
- Explain that yellow skin and paler hair can occur; teach skin care of the palms and soles.
- 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 capsules, with or without food (food does not change its absorption).

**Metabolism**
Liver, CYP3A4, to an active metabolite.

**Half-life**
Active metabolite about 80 to 110 hours, so steady state takes about two weeks.

## Memory aid

«SUNitinib, a touch of sun»: yellow skin and pale hair; also tired, hypothyroid and hypertensive.

## Test yourself

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

## Why does sunitinib work in GIST that has become resistant to imatinib?

Because it also inhibits the KIT kinase that drives these tumours.

## Which endocrine disorder is common on sunitinib?

Hypothyroidism; thyroid function is checked regularly.

## What is sunitinib's boxed warning?

Severe, possibly fatal hepatotoxicity.

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

[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

- [Pazopanib](https://durgical.com/en/pharmacology/pazopanib/)
- [Axitinib](https://durgical.com/en/pharmacology/axitinib/)
- [Imatinib](https://durgical.com/en/pharmacology/imatinib/)

## Related conditions 3

- [Renal cell carcinoma](https://durgical.com/en/conditions/renal-cell-carcinoma/)
- [Gastrointestinal stromal tumour (GIST)](https://durgical.com/en/conditions/gastrointestinal-stromal-tumour/)
- [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: [Sunitinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a607052.html) (MedlinePlus (U.S. National Library of Medicine), 2022); [Sunitinib Malate - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/sunitinibmalate) (National Cancer Institute, 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EX01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

---
Source: https://durgical.com/en/pharmacology/sunitinib/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/sunitinib/