VEGFR multikinase inhibitors
Oral anti-angiogenic drugs that block VEGF receptors and other kinases; used in kidney, liver, thyroid and other cancers. Hypertension is the rule.
What they are
Sunitinib, pazopanib, axitinib, cabozantinib, lenvatinib, regorafenib (and sorafenib, tivozanib, vandetanib) inhibit the kinase of VEGFR1-3 and, to different degrees, PDGFR, KIT, FGFR, RET and MET. They cut the tumour's blood supply and, through KIT, RET or MET, also hit the tumour cell itself.
Mechanism of action
VEGF binding to VEGFR2 on endothelial cells switches on its intracellular kinase and drives the growth of new vessels and their leakiness. These drugs occupy the ATP site of the receptor kinase, so tumour angiogenesis stops. The same block in normal vessels explains the shared toxicity: hypertension, proteinuria, bleeding, arterial thrombosis, gastrointestinal perforation and poor wound healing.
Target: VEGFR1-3 and other angiogenic kinases (PDGFR, KIT, FGFR, RET, MET)
Drugs in this class
- SunitinibAn oral multikinase inhibitor (VEGFR, KIT, PDGFR) for kidney cancer, GIST after imatinib and pancreatic NETs. Boxed…VEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinases
- PazopanibAn oral VEGFR multikinase inhibitor for advanced kidney cancer and soft-tissue sarcoma. Boxed warning: liver damage…VEGFR1-3, PDGFR, FGFR and KIT tyrosine kinases
- AxitinibA selective VEGFR1-3 inhibitor for advanced kidney cancer, first line with an immune checkpoint inhibitor or alone…VEGFR1, VEGFR2 (KDR) and VEGFR3 tyrosine kinases
- CabozantinibA multikinase inhibitor of VEGFR2, MET and RET for kidney, liver and thyroid cancers and NETs. Not used with recent…MET, VEGFR2, RET and KIT tyrosine kinases
- LenvatinibA broad multikinase inhibitor (VEGFR, FGFR, PDGFR, KIT, RET) for thyroid, liver, kidney and endometrial cancer. Watch…VEGFR1-3, FGFR, PDGFR, KIT and RET tyrosine kinases
- RegorafenibA later-line multikinase inhibitor for colorectal cancer, GIST and liver cancer after earlier drugs. Boxed warning…VEGFR1-3, TIE2, PDGFR, KIT, RET, RAF1 and other kinases
Others in the class
- sorafenib
- tivozanib
- vandetanib
Test yourself
Think of the answer, then tap the question to see it.
Which receptor on endothelial cells is the main target of these drugs?
VEGFR2 (KDR).
Which vital sign must be followed with every VEGFR inhibitor?
Blood pressure, because hypertension is a class effect.
Why are these drugs stopped before elective surgery?
Blocking VEGF signalling impairs wound healing.
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Sunitinib Malate - NCI (National Cancer Institute, 2025).
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Representative model, for educational purposes only.