[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/) › Axitinib # Axitinib ## 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 selective VEGFR1-3 inhibitor for advanced kidney cancer, first line with an immune checkpoint inhibitor or alone after one prior therapy. Updated Nov 1, 2026 Also called: AG-013736 ## Quick facts **Group** [VEGFR multikinase inhibitors](https://durgical.com/en/pharmacology/classes/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. 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 ✂**VEGFR1, VEGFR2 (KDR) and VEGFR3 tyrosine kinases**Axitinib ⓘ The figure shows axitinib in the ATP pocket of the human VEGFR2 kinase domain. **Target in 3D:** VEGFR1, VEGFR2 (KDR) and VEGFR3 tyrosine kinases. PDB structure 4AG8 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/4AG8) · Drag to rotate · pinch to zoom 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 →](https://durgical.com/en/conditions/renal-cell-carcinoma/) - Advanced renal cell carcinoma, alone after failure of one prior systemic therapy. [Renal cell carcinoma →](https://durgical.com/en/conditions/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) ### Serious (rare, important) - Arterial thrombosis (heart attack, stroke) and bleeding - Gastrointestinal perforation - Wounds that do not heal - Hepatotoxicity ## 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. ## Memory aid «AXItinib, the precise AXE»: it cuts only the VEGF receptors and partners immunotherapy in kidney cancer. ## 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. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/axitinib/) [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 2 - [Sunitinib](https://durgical.com/en/pharmacology/sunitinib/) - [Pembrolizumab](https://durgical.com/en/pharmacology/pembrolizumab/) ## Related conditions 1 - [Renal cell carcinoma](https://durgical.com/en/conditions/renal-cell-carcinoma/) [← 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: [Axitinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a612017.html) (MedlinePlus (U.S. National Library of Medicine), 2024); [Axitinib - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/axitinib) (National Cancer Institute, 2022); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EK01) (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/axitinib/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/axitinib/