Axitinib

What it is and how it works

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.

Mechanism class: Receptor Tyrosine Kinase Inhibitors

Indications

is a kinase inhibitor indicated: • in combination with avelumab, for the first-line treatment of patients with advanced renal cell carcinoma (RCC). • in combination with pembrolizumab, for the first-line treatment of patients with advanced RCC. • as a single agent, for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy. First-Line Advanced Renal Cell Carcinoma INLYTA in combination with avelumab is indicated for the first-line treatment of patients with advanced renal cell carcinoma (RCC). INLYTA in combination with pembrolizumab is indicated for the first-line treatment of patients with advanced RCC. Second-Line Advanced Renal Cell Carcinoma INLYTA as a single agent is indicated for the treatment of advanced RCC after failure of one prior systemic therapy.

Dosage and administration (summary)

• INLYTA 5 mg orally twice daily with avelumab 800 mg every 2 weeks. • INLYTA 5 mg orally twice daily with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks. • INLYTA as a single agent the starting dose is 5 mg orally twice daily. • Dose adjustments can be made based on individual safety and tolerability. • Administer INLYTA dose approximately 12 hours apart with or without food. • INLYTA should be swallowed whole with a glass of water. • See Full Prescribing Information for dosage modifications for adverse reactions. • If a strong CYP3A4/5 inhibitor is required, decrease the INLYTA dose by approximately half.

Contraindications

None. None.

Warnings and precautions

• Hypertension: Hypertension including hypertensive crisis has been observed. Blood pressure should be well-controlled prior to initiating INLYTA. Monitor for hypertension and treat as needed. Withhold and then dose reduce INLYTA or permanently discontinue based on severity of hypertension. • Arterial and Venous Thromboembolic Events: Arterial and venous thrombotic events have been observed and can be fatal. Use with caution in patients who are at increased risk for these events. Permanently discontinue INLYTA if an arterial thromboembolic event occurs during treatment.

Pregnancy

Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action, INLYTA can cause fetal harm when administered to a pregnant woman. There are no available human data to inform the drug-associated risk.

Storage and supply

tablets are supplied as follows: • 1 mg tablets are red film-coated, oval tablets debossed with "Pfizer" on one side and "1 XNB" on the other; available in bottles of 180: NDC 0069-0145-01. • 5 mg tablets are red film-coated, triangular tablets debossed with "Pfizer" on one side and "5 XNB" on the other.

Source: Axitinib (Inlyta) — US FDA prescribing information, 2025-02-19, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.