Axitinib, an oral tyrosine kinase inhibitor (TKI) marketed under the name Inlyta, is primarily used to treat advanced renal cell carcinoma (RCC). This Pfizer-developed targeted therapy specifically inhibits the vascular endothelial growth factor receptors VEGFR-1, VEGFR-2, and VEGFR-3. This procedure successfully reduces tumor angiogenesis and stops the spread of malignancy.

Composition & Formulation

The active ingredient in each Inlyta 5 mg tablet is 5 milligrams of axitinib. In addition, the formulation contains inert excipients that aid in stabilizing the medication and guaranteeing appropriate absorption, such as lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate.

Mechanism of Action

Axitinib functions by specifically blocking VEGF receptors, which are essential for angiogenesis—the process by which new blood vessels are formed—and are required for tumor growth. Axitinib efficiently lowers the blood supply to cancer cells by inhibiting these receptors, which causes the cells to starve and ultimately die. The medication is useful in treating kidney cancer because of its high degree of specificity.

Indications

Patients with advanced renal cell carcinoma (RCC) who have not responded to at least one previous systemic treatment are the main target of axitinib 5 mg. It is frequently used after cytokine-based or sunitinib-based therapy. Axitinib and immune checkpoint inhibitors such as pembrolizumab may occasionally be used together.

Dosage & Administration

Inlyta is typically started at a dose of 5 mg twice a day, spaced about 12 hours apart. It should be taken with or without food, and with a full glass of water. Depending on each patient’s response and tolerance, the dosage may be changed. In cases of toxicity, it may be lowered to 3 mg or 2 mg twice daily, or it may be increased to 7 mg or 10 mg twice daily.

Pharmacokinetics

Absorption: Quickly absorbed; peak plasma concentration is reached two to four hours after the dose.

Metabolism: CYP3A4 is primarily responsible for this process in the liver, with CYP1A2 and CYP2C19 playing a minor role.

Elimination: Mainly eliminated by urine (23%) and feces (41%).

Dosing must be done twice day because to the half-life, which is roughly 2.5 to 6.1 hours.

Side Effects

Common side effects of axitinib 5 mg include:

• Hypertension
• Fatigue
• Diarrhea
• Nausea and vomiting
• Hand-foot syndrome (palmar-plantar erythrodysesthesia)
• Weight loss
• Loss of appetite
• Hoarseness
• Stomatitis (mouth ulcers and inflammation)

Serious adverse reactions may include:

• Hepatotoxicity
• Cardiovascular issues (heart failure, blood clots, hemorrhage)
• Proteinuria
• Thyroid dysfunction

Contraindications & Precautions

Pregnancy & Lactation: Axitinib should not be used during pregnancy or lactation due to the possibility of fetal damage.

Hypertension: Individuals should have their blood pressure checked and treated appropriately.

Liver Impairment: In patients with moderate to severe hepatic impairment, dose modifications may be required.

Drug Interactions: Axitinib’s plasma levels may change as a result of interactions with CYP3A4 inducers and inhibitors (such as rifampin and ketoconazole).

Bleeding Risks: Patients with a history of coagulopathies or gastrointestinal bleeding should exercise caution.

Storage & Handling

Store between 20°C and 25°C (68°F and 77°F) at a regulated room temperature.

To keep it dry, keep it in its original container.

Keep out of reach of children.

Conclusion

For patients with advanced renal cell carcinoma, axitinib 5 mg (Inlyta) is a very successful targeted therapy, especially for those whose prior treatments have failed. Because it disrupts angiogenesis, its specific inhibition of VEGF receptors is crucial in restricting the growth of tumors. Although it has many advantages, there are also some drawbacks, and blood pressure, liver function, and cardiovascular health must be closely monitored. Optimizing axitinib therapy results requires careful patient selection and management.

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To order from MDX Pharma BD, visit their website at https://mdxpharmabd.com, where you can browse products and place orders online. For inquiries or orders via email, contact emedicarepharma@gmail.com. Alternatively, call (+88) 01929123476. Their address is 29, Abdullahpur, Uttara, Dhaka-1230, Bangladesh.

Q. How long is the half-life of axitinib?
As long as axitinib is effective for you, you typically continue taking it. Axitinib should never be stopped without first seeing your doctor. A nurse or phlebotomist, who is trained to draw blood, will draw samples from you while you are on axitinib.

Q. What is the duration of immunotherapy?
The type of immunotherapy you are receiving will determine the frequency of your treatments. For instance, pembrolizumab is administered every three weeks, but nivolumab is administered every two weeks. The duration of each treatment session is roughly 90 minutes.