Adult: As cap: Initially, 140 mg once daily. Adjust dose in decrements of 40 mg daily, if necessary. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline). This indication and dosage is specific for cap formulation. Do not use interchangeably with the tab formulation due to different bioequivalence.
Adult: As tab: Initially, 60 mg once daily. Adjust dose in decrements of 20 mg daily, if necessary. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline). This indication and dosage is specific for tab formulation. Do not use interchangeably with the cap formulation due to different bioequivalence.
Special Patient Group
Patient taking strong CYP3A4 inhibitor (e.g. ketoconazole, itraconazole):
As tab: Reduce daily dose by 20 mg. As cap: Reduce daily dose by 40 mg. Resume normal dosing 2-3 days after discontinuation of the strong CYP3A4 inhibitor.
Patient taking strong CYP3A4 inducer (e.g. rifampin, phenobarbital, phenytoin, carbamazepine):
As tab: Increase daily dose by 20 mg. Max 80 mg daily. As cap: Increase daily dose by 40 mg. Max: 180 mg daily. Resume normal dosing 2-3 days after discontinuation of strong CYP3A4 inhibitor.
Unresectable locally advanced medullary thyroid carcinoma; Metastatic medullary thyroid carcinoma:
Mild to moderate impairment: As cap: Initially, 60 mg. Severe: Not recommended.
Monitor blood pressure prior to therapy and regularly thereafter; platelet count, and urine protein regularly. Perform oral examinations prior to and periodically throughout the therapy. Monitor for signs and symptoms of RPLS (e.g. seizures, headache); thromboembolic events (e.g. acute MI).
May increase serum concentration with grapefruit or grapefruit juice. May decrease serum concentration with St. John’s wort.
Description: Cabozantinib is a proinvasive receptor tyrokinases (RTKs) inhibitor. It acts by inducing apoptosis of cancer cells and suppresses tumour growth, metastasis, and angiogenesis. Pharmacokinetics: Absorption: Food, particularly high fat meal, increases rate and extent of absorption. Bioavailability: Tab formulation has a 19% increase in Max concentration compared to cap following a single 140 mg dose, and therefore are not bioequivalent. Time to peak plasma concentration: 2-5 hours (cap); 3-4 hours (tab). Distribution: Volume of distribution: 349 L (cap); 319 L (tab). Plasma protein binding: >99.7%. Metabolism: Metabolised in the liver by CYP3A4, and by CYP2C9 (minimal). Excretion: Via faeces (approx 54%, 43% as unchanged drug); urine (approx 27%). Terminal half-life: 55 hours (cap); 99 hours (tab).
Store between 20-25°C. Protect from moisture.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01XE26 - cabozantinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
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