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
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.

Mechanism of action

VEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinasesSunitinib

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

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 →
Gastrointestinal stromal tumour after progression on, or intolerance to, imatinib. Gastrointestinal stromal tumour (GIST) →
Progressive pancreatic neuroendocrine tumours that are unresectable or metastatic. Pancreatic neuroendocrine tumours (VIPoma, glucagonoma, somatostatinoma, non-functioning) →

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

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.

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)

Connections

← Back to the class: 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 (MedlinePlus (U.S. National Library of Medicine), 2022); Sunitinib Malate - NCI (National Cancer Institute, 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.