Axitinib

Renal Cell Carcinoma

Drug Status

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Government Approvals

US(FDA), UK(BNF)

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WHO Essential Medicine

NO

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Known Teratogen

Definite

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Pharmaceutical Class

Kinase Inhibitor

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Controlled Drug Substance

NO

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Drug Ingredient

Axitinib

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Summary

  • Axitinib is used to treat advanced renal cell carcinoma (RCC), a type of kidney cancer, in adults. It is typically used when the disease has progressed after other treatments.

  • Axitinib works by blocking certain proteins called receptor tyrosine kinases, which are involved in the growth of blood vessels that supply tumors. By inhibiting these proteins, Axitinib reduces blood supply to the tumor, slowing its growth and spread.

  • The usual starting dose of Axitinib for adults is 5 mg taken orally twice daily, approximately 12 hours apart. The tablets should be swallowed whole with water and can be taken with or without food. The dose may be adjusted based on individual tolerance and response.

  • Common side effects of Axitinib include diarrhea, high blood pressure, fatigue, decreased appetite, and nausea. More serious side effects can include severe hypertension, arterial and venous thromboembolic events, hemorrhage, and cardiac failure.

  • Axitinib may cause serious conditions like high blood pressure, arterial and venous thromboembolic events, hemorrhage, cardiac failure, gastrointestinal perforation, and impaired wound healing. It is not recommended for patients with severe hepatic impairment or a history of cardiovascular events.

Indications and Purpose

What is Axitinib used for?

Axitinib is indicated for the treatment of advanced renal cell carcinoma (RCC), a type of kidney cancer, in adults. It is used when the disease has progressed after treatment with one prior systemic therapy, such as sunitinib or a cytokine. Axitinib can be used alone or in combination with other medications like avelumab or pembrolizumab.

How does Axitinib work?

Axitinib works by inhibiting receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3. These receptors are involved in the growth of blood vessels that supply tumors. By blocking these receptors, Axitinib reduces blood supply to the tumor, slowing its growth and spread.

Is Axitinib effective?

Axitinib has been shown to be effective in treating advanced renal cell carcinoma (RCC) in clinical trials. It works by inhibiting certain proteins that promote cancer cell growth. In studies, Axitinib improved progression-free survival compared to other treatments, demonstrating its effectiveness in slowing the progression of RCC.

How does one know if Axitinib is working?

The benefit of Axitinib is evaluated through regular medical check-ups and laboratory tests ordered by your doctor. These tests monitor the cancer's response to treatment and check for any side effects. Your doctor will also assess your overall health and any symptoms you experience to determine the effectiveness of the medication.

Directions for Use

What is the usual dose of Axitinib?

The usual starting dose of Axitinib for adults is 5 mg taken orally twice daily, approximately 12 hours apart, with or without food. The dose may be adjusted based on individual tolerance and response, with possible increases to 7 mg or 10 mg twice daily. Axitinib is not approved for use in children, and its safety and effectiveness in pediatric patients have not been established.

How do I take Axitinib?

Axitinib should be taken orally twice daily, approximately 12 hours apart, with or without food. Patients should swallow the tablets whole with a glass of water and avoid splitting, chewing, or crushing them. It is important to avoid grapefruit and grapefruit juice while taking Axitinib, as they can affect how the medication works.

For how long do I take Axitinib?

Axitinib is typically used as long as it continues to provide clinical benefit or until unacceptable toxicity occurs. The duration of treatment varies depending on individual response and tolerance to the medication.

How long does it take for Axitinib to start working?

Axitinib begins to work within a few days, as blood pressure increases have been observed as early as 4 days after starting treatment. However, the full therapeutic effect, such as tumor response, may take several weeks to become evident. Regular monitoring by a healthcare provider is essential to assess its effectiveness.

How should I store Axitinib?

Axitinib should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). It should be kept in its original container, tightly closed, and away from excess heat and moisture. Ensure it is stored out of reach of children and pets to prevent accidental ingestion.

Warnings and Precautions

Who should avoid taking Axitinib?

Important warnings for Axitinib include the risk of hypertension, arterial and venous thromboembolic events, hemorrhage, cardiac failure, gastrointestinal perforation, and impaired wound healing. Patients should be monitored for these conditions. Axitinib is contraindicated in patients with severe hepatic impairment and should be used with caution in those with a history of cardiovascular events.

Can I take Axitinib with other prescription drugs?

Axitinib interacts with strong CYP3A4/5 inhibitors, which can increase its plasma concentration, and strong CYP3A4/5 inducers, which can decrease its effectiveness. Patients should avoid medications like ketoconazole, rifampin, and St. John's wort. Always inform your healthcare provider about all medications you are taking to manage potential interactions.

Can I take Axitinib with vitamins or supplements?

Axitinib may interact with St. John's wort, an herbal supplement that can decrease its effectiveness. Patients should inform their healthcare provider about all vitamins and supplements they are taking to avoid potential interactions. It is important to consult with a healthcare professional before starting any new supplements while on Axitinib.

Can Axitinib be taken safely while pregnant?

Axitinib can cause fetal harm when administered to a pregnant woman, based on its mechanism of action and animal studies. Women of reproductive potential should use effective contraception during treatment and for 1 week after the last dose. If pregnancy occurs, patients should inform their healthcare provider immediately. There is no strong evidence from human studies, but the potential risk is significant.

Can Axitinib be taken safely while breastfeeding?

It is not known if Axitinib is excreted in human milk, but due to the potential for serious adverse reactions in a breastfed child, breastfeeding is not recommended during treatment and for 2 weeks after the last dose. Mothers should discuss with their healthcare provider whether to discontinue breastfeeding or the medication.

Is Axitinib safe for the elderly?

In clinical studies, no overall differences in safety or effectiveness were observed between elderly patients (65 years and older) and younger patients. However, greater sensitivity in some older individuals cannot be ruled out. Elderly patients should be monitored closely for side effects, and dose adjustments may be necessary based on individual tolerance and response.

Is it safe to exercise while taking Axitinib?

Axitinib may cause fatigue, which could limit the ability to exercise. If you experience fatigue or any other symptoms that affect your ability to exercise, discuss this with your healthcare provider. They can provide guidance on managing these side effects and advise on safe levels of physical activity.

Is it safe to drink alcohol while taking Axitinib?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.