Inlyta

Advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy; Advanced RCC in combination with avelumab (first-line); Advanced RCC in combination with pembrolizumab (first-line)

Monotherapy: 5 mg orally twice daily, approximately 12 hours apart
With avelumab or pembrolizumab: 5 mg twice daily
Dose increase: May increase to 7 mg BID, then 10 mg BID if tolerated (no AEs > Grade 2, normotensive, not on antihypertensives)
Take with or without food

Tablets: 1 mg, 5 mg

None listed.

• Hypertension: 40% incidence. Monitor BP before initiation and regularly. Treat with standard antihypertensive therapy.
• Arterial Thromboembolic Events: MI, CVA, TIA reported. Use with caution in at-risk patients.
• Venous Thromboembolic Events: PE, DVT, retinal vein occlusion/thrombosis.
• Hemorrhage: Including fatal cerebral, GI, and pulmonary hemorrhage.
• Cardiac Failure: Monitor for signs/symptoms.
• GI Perforation and Fistula: Permanently discontinue.
• Thyroid Dysfunction: Hypothyroidism in 19%. Monitor thyroid function before and during treatment.
• Wound Healing: Stop at least 2 days before surgery.
• RPLS: Discontinue if confirmed.
• Proteinuria: Monitor before and during treatment.
• Hepatotoxicity: ALT elevation in 22%. Monitor LFTs before and during.
• Embryo-Fetal Toxicity

Diarrhea (55%), hypertension (40%), fatigue (39%), decreased appetite (34%), nausea (32%), dysphonia (31%), hand-foot syndrome (27%), weight decreased (25%), vomiting (24%), asthenia (21%), hypothyroidism (19%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Axitinib is a potent and selective inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3) at sub-nanomolar concentrations. These receptors mediate angiogenesis, vascular permeability, and lymphatic vessel formation. By blocking VEGFR signaling, axitinib inhibits tumor angiogenesis and growth.

Tmax: 2.5-4.1 hours. Half-life: 2.5-6.1 hours. Protein binding: >99%. Metabolized primarily by CYP3A4/5 and to a lesser extent CYP1A2, CYP2C19, UGT1A1. Fecal excretion (41%), urinary excretion (23%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• AXIS — Axitinib vs. sorafenib in previously treated advanced RCC. Phase III, n=723.
  🔬 NCT00678392 ↗ 📄 Primary Publication ↗

Inlyta has FDA-approved indications across the following cancer types covered on PipelineEvidence: