Introduction to cabozantinib capsule instructions

1. Name: Cabozantinib,Cabozantinib

Product name:COMETRIQ

2. Indications:

Cabozantinib (Cabozantinib) is indicated for the treatment of patients with progressive metastatic medullary thyroid carcinoma (MTC).

3. Usage and dosage:

1. Recommended dose: Cabozantinib is in the form of capsules. The recommended daily dose is 140 mg once a day without food until the disease worsens or unacceptable toxicity occurs. Instruct patients not to eat for at least 2 hours before and for at least 1 hour after taking. Do not replace cabozantinib capsules with cabozantinib tablets. Swallow the capsule whole and do not open the capsule. Also do not take a missed dose within 12 hours of your next dose. Do not consume foods known to inhibit cytochrome P450 (such as grapefruit, grapefruit juice) or nutritional supplements while taking cabozantinib capsules.

2. Dosage adjustment: If intolerable adverse reactions occur after taking cabozantinib capsules, the doctor will adjust the dose. If previously received a daily dose of 140 mg, resume treatment at a daily dose of 100 mg; if previously received a daily dose of 100 mg, resume treatment at 60 mg daily; if previously received a 60 mg daily dose, resume 60 mg if tolerated, otherwise, discontinue cabozantinib capsules.

(1) Patients with hepatic impairment: For patients with mild to moderate hepatic impairment, the recommended starting dose of cabozantinib capsules is 80 mg.

3. Combined medication:

(1) Reduce the daily dose of cabozantinib by 40 mg (e.g., from 140 mg to 100 mg daily, or from 100 mg to 60 mg daily) when coadministered with a strong CYP3A4 inhibitor. Resume the same dose as before starting the CYP3A4 inhibitor 2 to 3 days after discontinuing the strong inhibitor.

(2) When coadministered with a strong CYP3A4 inducer, increase the daily dose of cabozantinib by 40 mg as tolerated (e.g., from 140 mg to 180 mg daily, or from 100 mg to 140 mg daily). After 2 to 3 days of discontinuing the strong inducer, resume the dose used before starting the CYP3A4 inducer. The daily dose should not exceed 180mg.

4. Adverse reactions:

In clinical studies of cabozantinib capsules, the most common adverse reactions, in order of frequency, were: diarrhea, stomatitis, palmoplantar red blood cell paresthesia (PPE), weight loss, decreased appetite, nausea, fatigue, oral pain, hair color change, dysgeusia, hypertension, abdominal pain and constipation. The most common laboratory abnormalities are elevated aspartate aminotransferase (AST), elevated alanine aminotransferase (ALT), lymphopenia, elevated alkaline phosphatase (ALP), hypocalcemia, neutropenia, thrombocytopenia, hypophosphatemia, and hyperbilirubinemia. Adverse events such as nosebleeds, pain in extremities, aneurysms, dissections, and ruptures of arteries (including the aorta) have also occurred after marketing.

5. Storage:

Caboozantinib is available in hard gelatin capsules that can be stored at 20°C to 25°C (68°F to 77°F); excursions allowed within the range of 15°C to 30°C (59°F to 86°F).

6. Special groups:

Based on animal studies, cabozantinib may impair fertility in both female and male animals of reproductive potential; therefore, it is recommended that females of reproductive potential use effective contraception during treatment and for 4 months after the last dose; lactating women are advised not to breastfeed during treatment and for 4 months after the last dose.

7. Mechanism of action:

In vitro biochemistry and/or cellular assays show that cabozantinib inhibits the tyrosine kinase activities of RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, ROS1, TYRO3, MER and TIE-2. These receptor tyrosine kinases are involved in normal cellular functions and pathological processes, such as tumorigenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment.

8. Overdose:

One patient was reported to have accidentally overdosed on twice the intended dose (200 mg daily) over nine days. The patient experienced grade 3 memory impairment, grade 3 altered mental status, grade 3 cognitive impairment, grade 2 weight loss, and grade 1 elevated urea nitrogen. The extent of recovery was not recorded.