Axitinib
VEGFR multikinase inhibitors
VEGFR multikinase inhibitorsHigh 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 selective VEGFR1-3 inhibitor for advanced kidney cancer, first line with an immune checkpoint inhibitor or alone after one prior therapy.
Also called: AG-013736
Quick facts
- Group
- VEGFR multikinase inhibitors
- Target
- VEGFR1, VEGFR2 (KDR) and VEGFR3 tyrosine kinases
- Used for
- Advanced renal cell carcinoma
- Key effects
- Diarrhoea · Hypertension · Fatigue and weakness
- Monitor
- Blood pressure regularly · Laboratory tests
- ATC
- L01EK01
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows axitinib in the ATP pocket of the human VEGFR2 kinase domain.
Axitinib is a more selective inhibitor that blocks the kinase of VEGFR1, 2 and 3, the receptors that drive tumour angiogenesis. With pembrolizumab or avelumab it adds an anti-angiogenic effect to immune checkpoint blockade in kidney cancer.
- Selectively blocks the VEGFR1-3 kinases
- Tumour angiogenesis stops
- Combined with pembrolizumab or avelumab in kidney cancer
Indications
- Advanced renal cell carcinoma, first line with pembrolizumab or avelumab. Renal cell carcinoma →
- Advanced renal cell carcinoma, alone after failure of one prior systemic therapy. Renal cell carcinoma →
Adverse effects
Common
- Diarrhoea, nausea, decreased appetite, weight loss
- Hypertension
- Fatigue and weakness
- Voice changes (hoarseness)
- Hand-foot skin reaction (red, painful, peeling palms and soles)
Contraindications
- No absolute contraindications in the label apart from hypersensitivity; see the warnings
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
- Blood pressure regularly
- Laboratory tests, including liver tests
- Signs of bleeding and wound healing
Administration and safety
- Oral tablets twice daily at evenly spaced times, swallowed whole with a glass of water.
- Grapefruit, its juice and St John's wort are avoided because they change its levels.
- If the patient vomits after a dose, the dose is not repeated; the next one is taken at the usual time.
- 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.
- Ask about wounds that are not healing and planned surgery or dental work.
- Confirm a negative pregnancy test before the first dose and teach contraception during treatment and afterwards.
Pharmacokinetics
- Absorption
- Oral tablets, twice daily, with or without food.
- Metabolism
- Liver, mainly CYP3A4/5.
- Half-life
- Short and variable: about 2.5 to 6 hours.
Test yourself
Think of the answer, then tap the question to see it.
Which receptors does axitinib block selectively?
VEGFR1, VEGFR2 and VEGFR3.
With which immunotherapies is axitinib combined in kidney cancer?
Pembrolizumab or avelumab.
What happens to axitinib before planned surgery?
It is stopped beforehand and restarted when the wound has healed, because it impairs healing.
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: Axitinib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2024); Axitinib - NCI (National Cancer Institute, 2022); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.