Axitinib

What is Axitinib?

• Axitinib (Inlyta) is a kinase inhibitor used in the therapy of advanced renal cell carcinoma.

What are the uses of this medicine?

This medicine is used to treat kidney cancer that has spread or cannot be removed by surgery (advanced renal cell carcinoma or RCC):

• in combination with avelumab or pembrolizumab as your first treatment.
• alone when 1 prior drug treatment regimen for your RCC has not worked.

How does this medicine work?

• Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations.
• These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression.
• VEGF-mediated endothelial cell proliferation and survival were inhibited by axitinib in vitro and in mouse models.
• Axitinib was shown to inhibit tumor growth and phosphorylation of VEGFR-2 in tumor xenograft mouse models.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Co-administration of Inlyta with strong CYP3A4/5 inhibitors should be avoided.
• Grapefruit or grapefruit juice may also increase axitinib plasma concentrations and should be avoided.
• Co-administration of Inlyta with strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarbital, and St. John's wort) should be avoided.
• Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, and nafcillin) may also reduce the plasma exposure of axitinib and should be avoided if possible.

Is this medicine FDA approved?

• Axitinib received approval for use in the United States in 2012 for therapy of advanced renal cell carcinoma.

How should this medicine be used?

Recommended dosage: First-Line Advanced RCC:

• The recommended dose of Inlyta is 5 mg orally taken twice daily (12 hours apart) with or without food in combination with avelumab 800 mg administered as an intravenous infusion over 60 minutes every 2 weeks until disease progression or unacceptable toxicity.
• The recommended dose of Inlyta is 5 mg orally twice daily (12 hours apart) with or without food in combination with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks administered as an intravenous infusion over 30 minutes until disease progression or unacceptable toxicity.

Second-Line Advanced RCC: When Inlyta is used as a single agent, the recommended starting oral dose is 5 mg twice daily. Administer Inlyta doses approximately 12 hours apart with or without food.

• If a strong CYP3A4/5 inhibitor is required, decrease the Inlyta dose by approximately half.
• For patients with moderate hepatic impairment, decrease the starting dose by approximately half.

Administration:

• Take Inlyta exactly as prescribed by your healthcare provider.
• Your healthcare provider may change your dose if needed.
• Inlyta can be taken with or without food.
• Take Inlyta 2 times a day about 12 hours apart.
• Swallow Inlyta tablets whole with a glass of water.
• Your healthcare provider should check your blood pressure regularly during treatment with Inlyta.
• If you vomit or miss a dose of Inlyta, take your next dose at your regular time. Do not take two doses at the same time.
• If you take too much Inlyta, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 1 mg and 5 mg tablets

This medicine is available in fallowing brand namesː

• Inlyta

What side effects can this medication cause?

The most common side effects of Inlyta with avelumab include:

• diarrhea
• feeling tired
• muscle and bone pain
• nausea
• mouth sores
• rash, redness, itching, or peeling of your skin on your hands and feet
• hoarseness
• decreased appetite
• low levels of thyroid hormone
• rash
• liver problems
• cough
• shortness of breath
• stomach-area (abdomen) pain
• headache

The most common side effects of Inlyta with pembrolizumab include:

• diarrhea
• feeling tired or weak
• liver problems
• low levels of thyroid hormone
• decreased appetite
• rash, redness, itching or peeling of your skin on your hands and feet
• nausea
• mouth sores or swelling of the lining of the mouth, nose, eyes, throat, intestines, or vagina
• hoarseness
• rash
• cough
• constipation

The most common side effects of Inlyta when used alone include:

• diarrhea
• feeling tired or weak
• decreased appetite
• nausea
• hoarseness
• rash, redness, itching or peeling of your skin on your hands and feet
• decreased weight
• vomiting
• constipation

Inlyta may cause serious side effects, including:

• High blood pressure (hypertension)
• Blood clots in your veins or arteries
• Bleeding
• Heart failure
• Tear in your stomach or intestinal wall (perforation)
• Risk of wound healing problems
• Reversible Posterior Leukoencephalopathy Syndrome (RPLS)
• Protein in your urine
• Liver problems
• Heart problems

What special precautions should I follow?

• Hypertension including hypertensive crisis has been observed. Blood pressure should be well-controlled prior to initiating Inlyta. Monitor for hypertension and treat as needed. For persistent hypertension despite use of anti-hypertensive medications, reduce the Inlyta dose.
• Arterial and venous thrombotic events have been observed and can be fatal. Use with caution in patients who are at increased risk for these events.
• Hemorrhagic events, including fatal events, have been reported. Inlyta has not been studied in patients with evidence of untreated brain metastasis or recent active gastrointestinal bleeding and should not be used in those patients.
• Cardiac failure has been observed and can be fatal. Monitor for signs or symptoms of cardiac failure throughout treatment with Inlyta.
• Gastrointestinal perforation and fistula, including death, have occurred. Use with caution in patients at risk for gastrointestinal perforation or fistula.
• Hypothyroidism requiring thyroid hormone replacement has been reported. Monitor thyroid function before initiation of, and periodically throughout, treatment with Inlyta.
• Impaired wound healing can occur in patients who receive drugs that inhibit the vascular endothelial growth factor (VEGF) signaling pathway. Withhold Inlyta for at least 2 days prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of Inlyta after resolution of wound healing complications has not been established.
• RPLS has been observed. Permanently discontinue Inlyta if signs or symptoms of RPLS occur.
• In a controlled clinical study with Inlyta for the treatment of patients with RCC, proteinuria was reported. Monitor for proteinuria before initiation of, and periodically throughout, treatment with Inlyta. For moderate to severe proteinuria, reduce the dose or temporarily interrupt treatment with Inlyta.
• Liver enzyme elevation has occurred during treatment with Inlyta as a single agent. Monitor ALT, AST and bilirubin before initiation of, and periodically throughout, treatment with Inlyta. When used in combination with avelumab or pembrolizumab, higher frequencies of Grade 3 and 4 ALT and AST elevation may occur. Consider more frequent monitoring of liver enzymes. Consider withholding Inlyta and/or avelumab or pembrolizumab, initiating corticosteroid therapy, and/or permanently discontinuing the combination for severe or life-threatening hepatotoxicity.
• The systemic exposure to axitinib was higher in subjects with moderate hepatic impairment (Child-Pugh class B) compared to subjects with normal hepatic function. Decrease the starting dose of Inlyta if used in patients with moderate hepatic impairment. Inlyta has not been studied in patients with severe hepatic impairment.
• Inlyta in combination with avelumab can cause severe and fatal cardiovascular events. Optimize management of cardiovascular risk factors. Discontinue Inlyta in combination with avelumab for Grade 3–4 events.
• Based on its mechanism of action and findings from animal studies, Inlyta can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risk to the fetus and to use effective contraception.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypertension
• seizures associated with hypertension
• fatal hemoptysis

Management of overdosage:

• There is no specific treatment for Inlyta overdose.
• In cases of suspected overdose, Inlyta should be withheld and supportive care instituted.

Can this medicine be used in pregnancy?

• Based on findings in animal studies and its mechanism of action, Inlyta can cause fetal harm when administered to a pregnant woman.
• There are no available human data to inform the drug-associated risk.

Can this medicine be used in children?

• The safety and efficacy of Inlyta in pediatric patients have not been studied.

What are the active and inactive ingredients in this medicine?

• Active ingredient: axitinib
• Inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, and Opadry® II red 32K15441. The Opadry II red 32K15441 film coating contains: lactose monohydrate, HPMC 2910/Hypromellose 15cP, titanium dioxide, triacetin (glycerol triacetate), and red iron oxide.

Who manufactures and distributes this medicine?

• Packager: Pfizer Laboratories Div Pfizer Inc

What should I know about storage and disposal of this medication?

• Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

• Dailymed label info on Axitinib
• FDA Axitinib

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