Inlyta Axitinib Tablets

1. Indications and Usage
Advanced Renal Cell Carcinoma (RCC):
Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy.
First-Line Treatment:
Indicated in combination with avelumab or pembrolizumab for the first-line treatment of adult patients with advanced renal cell carcinoma.
2. Dosage and Administration
Recommended Dosage:
Starting Dose: 5 mg administered orally twice daily, approximately 12 hours apart.
Dose Titration: If blood pressure is controlled and no Grade >2 adverse reactions occur for at least 2 consecutive weeks, the dose may be increased to 7 mg, and then to 10 mg twice daily.
Dose Reduction: If dose reduction is required, reduce to 3 mg, and then to 2 mg twice daily.
Administration Instructions:
Administer with water. Swallow tablets whole.
Can be administered with or without food.
Avoid grapefruit and grapefruit juice.
3. Mechanism of Action
Tyrosine Kinase Inhibitor (TKI):
Axitinib is a potent inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3.
Physiological Effect:
It binds to the intracellular domain of these receptors, inhibiting VEGF-mediated signaling. This blocks endothelial cell proliferation and survival, leading to the inhibition of tumor angiogenesis (blood vessel formation) and tumor growth.
4. Safety and Warnings
Hypertension:
Axitinib can cause hypertension. Blood pressure should be controlled before starting treatment and monitored regularly. Dose reductions or interruptions may be necessary for uncontrolled hypertension.
Hemorrhage:
Serious and sometimes fatal hemorrhagic events have been reported. Do not use in patients with untreated brain metastases or recent active gastrointestinal bleeding.
Gastrointestinal Perforation and Fistula Formation:
Monitor patients for signs of perforation or fistula.
Reversible Posterior Leukoencephalopathy Syndrome (RPLS):
If RPLS occurs, permanently discontinue axitinib.
Wound Healing Complications:
Interrupt axitinib at least 24 hours prior to elective surgery. Do not administer for at least 2 weeks following major surgery.
5. Adverse Reactions
Most Common:
Diarrhea, hypertension, fatigue, decreased appetite, nausea, hoarseness, palmar-plantar erythrodysesthesia syndrome (hand-foot syndrome), weight decreased, vomiting, asthenia, and constipation.
6. Drug Interactions
Strong CYP3A4/5 Inhibitors:
Avoid co-administration with strong CYP3A4/5 inhibitors (e.g., ketoconazole, ritonavir). If unavoidable, reduce the axitinib dose by approximately 50%.
Strong CYP3A4/5 Inducers:
Avoid co-administration with strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin) as they may significantly decrease axitinib exposure.
7. Pharmaceutical Information
Chemical Description:
Axitinib is a small molecule tyrosine kinase inhibitor.
Storage:
Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F). Protect from moisture.