For: Renal Cell Carcinoma, Hepatocellular Carcinoma
Cabometyx (cabozantinib) is a tyrosine kinase inhibitor indicated for the treatment of patients with advanced renal cell carcinoma (RCC), and patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
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CABOMETYX- cabozantinib s-malate tablet
1 INDICATIONS AND USAGE
CABOMETYX is indicated for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior anti-angiogenic therapy.
2 DOSAGE AND ADMINISTRATION
2.1 Recommended Dose
Do not substitute CABOMETYX tablets with cabozantinib capsules.
The recommended daily dose of CABOMETYX is 60 mg. Do not administer CABOMETYX with food. Instruct patients not to eat for at least 2 hours before and at least 1 hour after taking CABOMETYX. Continue treatment until patient no longer experiences clinical benefit or experiences unacceptable toxicity.
Swallow CABOMETYX tablets whole. Do not crush CABOMETYX tablets.
Do not take a missed dose within 12 hours of the next dose.
Do not ingest foods (e.g., grapefruit, grapefruit juice) or nutritional supplements that are known to inhibit cytochrome P450 during CABOMETYX treatment.
DOSAGE FORMS AND STRENGTHS
60 mg CABOMETYX tablets are yellow film-coated, oval shaped with no score, and debossed with "XL" on one side and "60″ on the other side.
40 mg CABOMETYX tablets are yellow film-coated, triangle shaped with no score, and debossed with "XL" on one side and "40″ on the other side.
20 mg CABOMETYX tablets are yellow film-coated, round with no score, and debossed with "XL" on one side and "20″ on the other side.
5 WARNINGS AND PRECAUTIONS
Severe hemorrhage occurred with CABOMETYX. The incidence of Grade ≥ 3 hemorrhagic events was 2.1% in CABOMETYX-treated patients and 1.6% in everolimus-treated patients. Fatal hemorrhages also occurred in the cabozantinib clinical program.
Do not administer CABOMETYX to patients that have or are at risk for severe hemorrhage.
COMETRIQ is the (S)-malate salt of cabozantinib, a kinase inhibitor. Cabozantinib (S)-malate is described chemically as N -(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N" -(4-fluorophenyl)cyclopropane- 1,1-dicarboxamide, (2S)-hydroxybutanedioate. The molecular formula is C28 H24 FN3 O5 �C4 H6 O5 and the molecular weight is 635.6 Daltons as malate salt. The chemical structure of cabozantinib (S)-malate salt is:
image of chemical structure of CABOMETYX
(click image for full-size original)
Cabozantinib (S)-malate salt is a white to off-white solid that is practically insoluble in aqueous media.
CABOMETYX (cabozantinib) tablets are supplied as film-coated tablets containing 20 mg, 40 mg, or 60 mg of cabozantinib, which is equivalent to 25 mg, 51 mg, or 76 mg of cabozantinib (S)-malate, respectively. CABOMETYX also contains the following inactive ingredients: microcrystalline cellulose, lactose anhydrous, hydroxypropyl cellulose, croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate.
The film coating contains hypromellose, titanium dioxide, triacetin, and iron oxide yellow.
12 CLINICAL PHARMACOLOGY
12.1 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