Release date: 2026-03-20 17:05:44 Recommended: 54
Cabozantinib is a small-molecule multi-targeted tyrosine kinase inhibitor developed by Exelixis, Inc. (USA). It was first approved by the FDA in November 2012 for progressive metastatic medullary thyroid cancer, with subsequent expansions of approved indications, earning it a reputation as a "broad‑spectrum targeted therapy".
Usual Doses Recommended by the FDA (Prescribing Information):
(1) Cabozantinib capsules
140 mg orally once daily until the patient no longer derives clinical benefit or until unacceptable toxicity occurs.
(2) Cabozantinib tablets
Body Surface Area (BSA) ≥ 1.2 m²: 60 mg orally once daily until disease progression or unacceptable toxicity.
Cabozantinib tablets
Monotherapy: 60 mg orally once daily until the patient no longer derives clinical benefit or until unacceptable toxicity.
Combination therapy: 40 mg once daily in combination with nivolumab, until disease progression or unacceptable toxicity.
Tablets: 60 mg orally once daily until the patient no longer derives clinical benefit or until unacceptable toxicity.
Cabozantinib tablets
BSA ≥ 1.2 m²: 60 mg once daily until disease progression or unacceptable toxicity.
BSA < 1.2 m²: 40 mg once daily until disease progression or unacceptable toxicity.
The above information is sourced from Drugs.com and reflects the dosage ranges approved in countries outside mainland China only. It does not represent the approved use in mainland China. Do not make any treatment decisions based on this information.
Cabozantinib tablets and capsules are not interchangeable.
Cabozantinib should be taken on an empty stomach, at least 2 hours before or 1 hour after a meal.
Do not open, break, crush, or chew tablets or capsules. Swallow whole with a full glass of water.
If the next dose is due in less than 12 hours, skip the missed dose; do not double the dose.
During treatment with cabozantinib, avoid foods known to inhibit or induce CYP450 activity (e.g., grapefruit) or nutritional supplements (e.g., St. John’s Wort).
Cardiovascular system: Blood pressure (baseline and periodic monitoring during treatment)
Musculoskeletal system: Oral examination (due to risk of osteonecrosis of the jaw; baseline and periodic monitoring)
Renal function: Urinary protein (periodic monitoring during treatment)
Endocrine system: Thyroid function (baseline and periodic monitoring during treatment)
Metabolism: Serum calcium (periodic monitoring during treatment)
Cabozantinib capsules/tablets
Mild to moderate renal impairment: No dose adjustment recommended.
Severe renal impairment: No data available.
(1) Cabozantinib capsules (for medullary thyroid cancer)
Mild to moderate hepatic impairment: 80 mg orally once daily.
Severe hepatic impairment: Not recommended.
(2) Cabozantinib tablets (for medullary thyroid cancer)
Mild hepatic impairment: No dose adjustment recommended.
Moderate hepatic impairment: 40 mg once daily; for pediatric patients with BSA < 1.2 m², reduce from 40 mg to 20 mg once daily.
Severe hepatic impairment: Not recommended.
(3) Cabozantinib tablets (for renal cell carcinoma)
Mild to moderate hepatic impairment: 40 mg orally once daily.
Severe hepatic impairment: Not recommended.
(1) If ALT or AST > 3 × ULN but ≤ 10 × ULN and total bilirubin < 2 × ULN:
Hold cabozantinib and nivolumab until toxicity resolves to Grade 0 or 1; consider corticosteroid therapy as appropriate. One or both agents may be resumed after recovery.
(2) If ALT or AST > 10 × ULN, or > 3 × ULN with total bilirubin ≥ 2 × ULN:
Permanently discontinue cabozantinib and nivolumab. Corticosteroid therapy may be considered if an immune‑mediated reaction is suspected.