Cabozantinib -malate)

What it is and how it works

Mechanism of Action In vitro biochemical and/or cellular assays have shown that cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment.

Indications

is a kinase inhibitor indicated for the treatment of patients with advanced renal cell carcinoma (RCC). patients with advanced renal cell carcinoma, as a first-line treatment in combination with nivolumab patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib adult and pediatric patients 12 years of age and older with locally advanced or metastatic differentiated thyroid cancer (DTC) that has progressed following prior VEGFR-targeted therapy and who are radioactive iodine-refractory or ineligible adult and pediatric patients 12 years of age and older with previously treated, unresectable, locally advanced or metastatic, well-differentiated pancreatic neuroendocrine tumors (pNET). adult and pediatric patients 12 years of age and older with previously treated, unresectable, locally advanced or metastatic, well-differentiated extra-pancreatic neuroendocrine tumors (epNET). Renal Cell Carcinoma CABOMETYX is indicated for the treatment of patients with advanced renal cell carcinoma (RCC).

Dosage and administration (summary)

Do NOT substitute CABOMETYX tablets with cabozantinib capsules. Administer on an empty stomach at least 1 hour before or at least 2 hours after eating. Stop treatment with CABOMETYX at least 3 weeks prior to scheduled surgery, including dental surgery. Recommended Dose: RCC (Single Agent): 60 mg orally, once daily. RCC (Combination Therapy): 40 mg orally, once daily with: 240 mg nivolumab every 2 weeks by intravenous infusion; -OR- 480 mg nivolumab every 4 weeks by intravenous infusion; -OR- 600 mg nivolumab and 10,000 units hyaluronidase every 2 weeks administered subcutaneously; -OR- 1,200 mg nivolumab and 20,000 units hyaluronidase every 4 weeks administered subcutaneously.

Contraindications

None. None

Warnings and precautions

Hemorrhage: Do not administer CABOMETYX if recent history of hemorrhage. Perforations and Fistulas: Monitor for symptoms. Discontinue CABOMETYX for Grade 4 fistula or perforation. Thromboembolic Events: Discontinue CABOMETYX for myocardial infarction or serious venous or arterial thromboembolic events. Hypertension and Hypertensive Crisis: Monitor blood pressure regularly. Interrupt for hypertension that is not adequately controlled with anti-hypertensive therapy. Discontinue CABOMETYX for hypertensive crisis or severe hypertension that cannot be controlled with anti-hypertensive therapy.

Pregnancy

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

Storage and supply

tablets are supplied as follows: 60 mg tables are yellow film-coated, oval shaped with no score, debossed with "XL" on one side and "60" on the other side of the tablet; available in: bottle of 30 tablets: NDC 42388-023-26 bottle of 30 tablets packaged in a carton: NDC 42388-023-46 40 mg tablets are yellow film-coated, triangle shaped with no score…

Source: Cabozantinib (Cabometyx) — US FDA prescribing information, 2025-10-19, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.