Axitinib (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- AXITINIB
- INLYTA
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are discussed elsewhere in the labeling [see Warnings and Precautions (5)]: •Hypertension [see Warnings and Precautions (5.1)] •Arterial thromboembolic events [see Warnings and Precautions (5.2)] •Venous thromboembolic events [see Warnings and Precautions (5.3)] •Hemorrhage [see Warnings and Precautions (5.4)] •Cardiac failure [see Warnings and Precautions (5.5)] •Gastrointestinal perforation and fistula formation [see Warnings and Precautions (5.6)] •Thyroid dysfunction [see Warnings and Precautions (5.7)] •Reversible posterior leukoencephalopathy syndrome [see Warnings and Precautions (5.9)] •Proteinuria [see Warnings and Precautions (5.10)] •Hepatotoxicity [see Warnings and Precautions (5.11)] •Hepatic impairment [see Warnings and Precautions (5.12)]
Mechanism of Action
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. Axitinib was shown to inhibit tumor growth and phosphorylation of VEGFR-2 in tumor xenograft mouse models.
Overdosage
There is no specific treatment for INLYTA overdose. In a controlled clinical study with INLYTA for the treatment of patients with RCC, 1 patient inadvertently received a dose of 20 mg twice daily for 4 days and experienced dizziness (Grade 1). In a clinical dose finding study with INLYTA, subjects who received starting doses of 10 mg twice daily or 20 mg twice daily experienced adverse reactions which included hypertension, seizures associated with hypertension, and fatal hemoptysis. In cases of suspected overdose, INLYTA should be withheld and supportive care instituted.