CAZAR

Cabozantinib is a kinase inhibitor indicated for the treatment of-

1. Patients with advanced renal cell carcinoma (RCC)
2. Patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib

Cytotoxic Chemotherapy

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.

Recommended Dosage for Renal Cell Carcinoma: The recommended dosage of Cabozantinib is 60 mg once daily without food until the patient no longer experiences clinical benefit or experiences unacceptable toxicity.

Recommended Dosage for Hepatocellular Carcinoma: The recommended dosage of Cabozantinib is 60 mg once daily without food until disease progression or unacceptable toxicity.

1. Strong CYP3A4 inhibitors: Reduce the Cabozantinib dosage if coadministration cannot be avoided.
2. Strong CYP3A4 inducers: Increase the Cabozantinib dosage if coadministration cannot be avoided.

1. Stop treatment with Cabozantinib at least 28 days prior to scheduled surgery, including dental surgery
2. Do not substitute Cabozantinib tablets with cabozantinib capsules.
3. Do not administer Cabozantinib with food. Administer at least 1 hour before or at least 2 hours after eating
4. Swallow Cabozantinib tablets whole. Do not crush Cabozantinib tablets.
5. Do not take a missed dose within 12 hours of the next dose.
6. Modify the dose for certain patients with hepatic impairment and for patients taking drugs known to strongly induce or inhibit CYP450

Hemorrhage Perforations and Fistulas Thrombotic Events Hypertension and Hypertensive Crisis Diarrhea Palmar-plantar Erythrodysesthesia Proteinuria Osteonecrosis of the Jaw Wound Complications Reversible Posterior Leukoencephalopathy Syndrome

Based on findings from animal studies and its mechanism of action, Cabozantinib can cause fetal harm when administered to a pregnant woman. There is no information regarding the presence of Cabozantinib or its metabolites in human milk, or their effects on the breastfed child or milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with Cabozantinib and for 4 months after the final dose.

One case of overdosage was reported following administration of another formulation of cabozantinib; a patient inadvertently took twice the intended dose for 9 days. The patient suffered Grade 3 memory impairment, Grade 3 mental status changes, Grade 3 cognitive disturbance, Grade 2 weight loss, and Grade 1 increase in BUN. The extent of recovery was not documented.

Store Cabozantinib at room temperature 20°C to 25°C

Safe

Cabozantinib (20 mg, 80mg)