Description: Axitinib (trade name Inlyta) is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models and has shown partial responses in clinical trials with renal cell carcinoma (RCC) and several other tumour types. Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression. VEGF-mediated endothelial cell proliferation and survival were inhibited by axitinib in vitro and in mouse models. It was approved by the U.S. Food and Drug Administration. (Source: NIH Inxight Drugs)
Clinical Indication: Axitinib is indicated for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy. (Source: ClinPGx)
Description: Axitinib is a second generation oral tyrosine kinase inhibitor targeted against vascular endothelial growth factor (VEGF) receptors VEGFR1 (coded for by FLT1, VEGFR2 (KDR) and VEGFR3 (FLT4). (Source: ClinPGx)
Drug Label Annotation: Population pharmacokinetic analyses indicate that there are no clinically relevant effects of age, gender, race, body weight, body surface area, UGT1A1 genotype, or CYP2C19 genotype on the clearance of axitinib. (Source: ClinPGx)
Description: Axitinib is a Type-1 kinase inhibitor. Axitinib inhibits several receptor tyrosine kinases including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT. (Source: IUPHAR/BPS Guide to Pharmacology)