spec sheet6 rows
Axitinib is an oral kinase inhibitor for advanced renal cell carcinoma, used after another systemic treatment has failed or alongside an immune checkpoint inhibitor.
- AXIS was the first phase 3 trial to compare two targeted agents head to head in renal cell carcinoma and showed median progression-free survival of 6.7 months with axitinib versus 4.7 months with sorafenib (HR 0.665) in 723 previously treated patients [2].
- Despite the progression-free survival gain, the final AXIS overall-survival analysis found no significant difference between axitinib and sorafenib [3]; axitinib's approval rests on progression-free survival, not survival.
- Axitinib is roughly 50 to 450 times more selective for VEGFR-1/2/3 than for PDGFR-beta, KIT or FLT3, which is why its toxicity profile is dominated by class VEGF effects rather than myelosuppression [1].
- Axitinib's modern role is as the tyrosine-kinase partner in first-line immunotherapy doublets: pembrolizumab plus axitinib (KEYNOTE-426, PMID 30779529) and avelumab plus axitinib (JAVELIN Renal 101, PMID 30779531) both beat sunitinib.
- Axitinib is cleared mainly by CYP3A4/5, so strong CYP3A inhibitors and inducers materially change exposure and require dose adjustment (Inlyta US prescribing information).
Mechanism
It potently inhibits vascular endothelial growth factor receptors 1, 2 and 3, starving a tumour of new blood vessels rather than attacking the tumour cells directly. That same VEGF blockade produces its characteristic toxicities: hypertension, proteinuria, impaired wound healing and arterial thrombotic events.
receptor fingerprint
VEGFR-2 (KDR/FLK-1 receptor tyrosine kinase)ATP-competitive inhibitor
VEGFR-1 (FLT1 receptor tyrosine kinase)ATP-competitive inhibitor
VEGFR-3 (FLT4 receptor tyrosine kinase)ATP-competitive inhibitor
PDGFR-beta (platelet-derived growth factor receptor beta)Inhibitor
KIT (CD117 receptor tyrosine kinase)Inhibitor
Safetyrisks and cautions, not medical advice
an oral antineoplastic dosed against blood pressure and proteinuria, with arterial thrombosis and impaired wound healing among its expected effects
Subjective profileweighing the evidence above
A VEGF receptor inhibitor is not a drug anyone takes unsupervised, and the reason is written into how it is managed: blood pressure and urinary protein are the feedback signals, and treatment adjusted against measurements nobody is taking is not treatment. Arterial clots and wounds that will not close are expected effects rather than rare surprises, and the disease it treats is followed with imaging by people who do that for a living. The entry exists to explain the pharmacology; where to buy it is not a question with an answer here.
Resources
No suppliers are provided for compounds like this. This entry is here for reference.
Research
- 2008first citedNonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent,…
- 2011controlled trialComparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS):…
- 2020most recentPembrolizumab plus axitinib versus sunitinib monotherapy as first-line treatment of advanced re…
- 1.Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3
- 2.Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): a randomised phase 3 trial
- 3.Axitinib versus sorafenib as second-line treatment for advanced renal cell carcinoma: overall survival analysis and updated results from a randomised phase 3 trial
- 4.Pembrolizumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma
- 5.Avelumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma
- 6.Pembrolizumab plus axitinib versus sunitinib monotherapy as first-line treatment of advanced renal cell carcinoma (KEYNOTE-426): extended follow-up from a randomised, open-label, phase 3 trial
6 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
Notes and cautions
- Axitinib carries no boxed warning, but it produces the full VEGF-inhibitor toxicity set: hypertension including hypertensive crisis (dose titration is guided by blood pressure), arterial and venous thromboembolic events, haemorrhage including fatal bleeds, and gastrointestinal perforation and fistula formation.
- Thyroid dysfunction, proteinuria, hepatotoxicity, reversible posterior leukoencephalopathy syndrome and impaired wound healing all require monitoring; treatment should be stopped at least 24 hours before elective surgery.
- Blood pressure should be controlled before starting and monitored throughout, and the drug is embryo-fetal toxic so effective contraception is required.