p; Hypomagnesemia 31 7 4 <1
Hyponatremia 30 8 26 6
GGT increased 27 5 43 9
Hematology
White blood cells decreased 35 <1 31 <1
Absolute neutrophil count decreased 31 2 17 <1
Hemoglobin decreased 31 4 71 17
Lymphocytes decreased 25 7 39 12
Platlets decreased 25 <1 27 <1
ALP, alkaline phosphatase; ALT, alanine aminotransferase; AST, aspartate aminotransferase; GGT, gamma glutamyl transferase.
National Cancer Institute Common Terminology Criteria for Adverse Events, Version 4.0CLOSE
7 DRUG INTERACTIONS
Table 3. Clinically Significant Drug Interactions Involving Drugs that Affect Cabozantinib
Strong CYP3A4 Inhibitors
* The effect of grapefruit juice varies widely among brands and is concentration-, dose-, and preparation dependent. Studies have shown that it can be classified as a "strong CYP3A inhibitor" when a certain preparation was used (e.g., high dose, double strength) or as a "moderate CYP3A inhibitor" when another preparation was used (e.g., low dose, single strength). † The effect of St. John’s Wort varies widely and is preparation-dependent
Clinical Implications:
Concomitant use of CABOMETYX with a strong CYP3A4 inhibitor increased the exposure of cabozantinib compared to the use of CABOMETYX alone [see CLINICAL PHARMACOLOGY (12.3)].
Increased cabozantinib exposure may increase the risk of exposure-related toxicity.
Prevention or Management:
Reduce the dosage of CABOMETYX if concomitant use with strong CYP3A4 inhibitors cannot be avoided [see DOSAGE AND ADMINISTRATION (2.2)].
Examples:
Boceprevir, clarithromycin, conivaptan, grapefruit juice*, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telithromycin, and voriconazole
Strong CYP3A4 Inducers
Clinical Implications:
Concomitant use of CABOMETYX with a strong CYP3A4 inducer decreased the exposure of cabozantinib compared to the use of CABOMETYX alone [see CLINICAL PHARMACOLOGY (12.3)].
Decreased cabozantinib exposure may lead to reduced efficacy.
Prevention or Management:
Increase the dosage of CABOMETYX if concomitant use with strong CYP3A4 inducers cannot be avoided [see DOSAGE AND ADMINISTRATION (2.2)].
Examples:
Rifampin, phenytoin, carbamazepine, phenobarbital, rifabutin, rifapentine, and St. John’s Wort†CLOSE
8 USE IN SPECIFIC POPULATIONS
8.1 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 [see CLINICAL PHARMACOLOGY (12.1)]. There are no available data in pregnant women to inform the drug-associated risk. In animal developmental and reproductive toxicol |
