Axitinib is a tyrosine kinase inhibitor that selectively inhibits the activity of vascular endothelial growth factor receptors (VEGFR-1), VEGFR-2, and VEGFR-3, blocking the tumor angiogenesis signaling pathway and thereby inhibiting tumor growth and metastasis.

1、 Drug name

1. Common name: Axitinib

2. Product Name: INLYTA ®

3. Main ingredient: Axitinib

2、 Indications

Used to treat advanced renal cell carcinoma (RCC) that has previously failed a systemic treatment regimen.

3、 Specifications and characteristics

Tablet specification: 5 milligrams.

4、 Main components

1. Active ingredient: Axitinib.

2. Accessories: Microcrystalline cellulose, lactose monohydrate, cross-linked carboxymethyl cellulose sodium, magnesium stearate, and Opadry ® IIred32K15441 coating material.

5、 Usage and dosage

1. The recommended initial oral dose is 5 milligrams, administered twice daily with an interval of approximately 12 hours between doses.

2. Can be taken with food or on an empty stomach.

3. The whole piece should be swallowed with water.

6、 Dose adjustment

1. Dose adjustment based on individual safety and tolerability.

2. For patients with good tolerance and no specific adverse reactions for more than two weeks, the dose can be increased from 5 milligrams twice daily to 7 milligrams twice daily, and further to 10 milligrams twice daily.

3. If a reduction is required, the recommended doses are 3 milligrams twice daily and 2 milligrams twice daily.

4. If a potent CYP3A4/5 inhibitor is required, the dose of axitinib should be reduced by about half.

5. The starting dose for patients with moderate liver injury (Child Pugh B grade) should be reduced by about half.

7、 Medication precautions

1. Medication time: twice a day, with an interval of about 12 hours, unrelated to eating.

2. Missed dose: If one dose is missed or vomiting occurs after taking the medication, it should not be taken again. The next dose should be taken according to the original plan.

3. Surgery: Medication should be stopped at least 24 hours before planned surgery.

8、 Medication for special populations

1. Pregnant women: Due to the potential harm to the fetus caused by the mechanism of action, pregnant women should avoid using it. Women of childbearing age should use effective contraception during and after treatment.

2. Breastfeeding period: It is not clear whether it is secreted through breast milk. It is recommended to weigh the pros and cons before deciding to stop breastfeeding or medication.

3. Children: Safety and effectiveness have not yet been established.

4. Elderly: No need to adjust dosage.

5. Liver dysfunction: Mild injury does not require adjustment of starting dose; Moderate injury should reduce the initial dose; Patients with severe injuries have no experience using it.

6. Renal insufficiency: Mild to severe injury does not require adjustment of starting dose; Patients with end-stage renal disease should use it with caution.

9、 Adverse reactions

1. The most common adverse reactions (with an incidence rate of ≥ 20%) include diarrhea, hypertension, fatigue, loss of appetite, nausea, difficulty speaking, palmar swelling and tenderness syndrome, weight loss, vomiting, fatigue, and constipation.

2. Serious warnings and precautions include hypertension and hypertensive crisis, arterial and venous thrombotic events, bleeding, gastrointestinal perforation and fistula formation, thyroid dysfunction, poor wound healing, reversible posterior encephalopathy syndrome, proteinuria, elevated liver enzymes, etc.

10、 Contraindications

None.

11、 Drug interactions

1. Should avoid co administration with potent CYP3A4/5 inhibitors such as ketoconazole, itraconazole, clarithromycin, etc. If co administration is necessary, the dose of axitinib should be halved.

2. Should avoid co administration with potent CYP3A4/5 inducers such as rifampicin, dexamethasone, phenytoin, carbamazepine, St. John's wort, etc.

3. It is also advisable to avoid consuming grapefruit or drinking grapefruit juice.

12、 Storage method

Store at room temperature of 20 ° C to 25 ° C (68 ° F to 77 ° F), allowing fluctuations between 15 ° C to 30 ° C (59 ° F to 86 ° F) during short distance transportation.

Axitinibinformation