Axitinib — Drug Monograph
Brand names: Inlyta
Drug class: Tyrosine Kinase Inhibitor
Mechanism of Action
Axitinib is a potent and selective second-generation inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3). By inhibiting these receptors, it blocks VEGF-mediated endothelial cell proliferation and survival, thereby inhibiting angiogenesis and tumor growth. Axitinib is designed to have high affinity for the kinase domain in its active conformation. It also shows activity against other targets such as KIT and PDGFR at higher concentrations.
FDA Indications
- Treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy
- In combination with pembrolizumab, for the first-line treatment of patients with advanced renal cell carcinoma (RCC)
- In combination with avelumab, for the first-line treatment of patients with advanced renal cell carcinoma (RCC)
Common Side Effects
- Diarrhea
- Hypertension
- Fatigue
- Decreased appetite
- Nausea
- Dysphonia
- Palmar-plantar erythrodysesthesia (hand-foot syndrome)
- Weight loss
- Vomiting
- Asthenia
- Constipation
Clinical Pearl
Axitinib has a very short half-life (approx. 2.5-6 hours), allowing for rapid management of toxicities through dose interruption. Hypertension is a common and pharmacodynamic biomarker of VEGF inhibition; aggressive blood pressure management is often necessary to continue therapy. Titration is a unique feature of axitinib, where doses can be increased if the patient has no Grade 2 or higher hypertension or other significant toxicities. In the first-line setting, it is now frequently used in…
Related Therapies & Mechanisms
- Cabozantinib (Cabometyx) — Tyrosine Kinase Inhibitor · RCC
- Lenvatinib (Lenvima) — Tyrosine Kinase Inhibitor · RCC
- Pazopanib (Votrient) — Tyrosine Kinase Inhibitor · RCC
- Sorafenib (Nexavar) — Tyrosine Kinase Inhibitor · RCC