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Axitinib

(ack-sit-uh-nib)

Trade/other name(s): Inlyta®

Why would this drug be used?

This drug is used to treat kidney cancer. It is also being studied for use against other types of cancer.

How does this drug work?

Axitinib is a type of targeted therapy known as a kinase inhibitor. Kinases are proteins on or near the surface of a cell that transmit important signals to the cell's control center. Axitinib inhibits some kinase proteins (VEGFR-1, VEGFR-2, and VEGFR-3) that would normally help form new blood vessels (angiogenesis) that could feed a growing tumor. By blocking these proteins, axitinib may help stop the growth of tumors.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have ever had high blood pressure. This drug may raise blood pressure. Your blood pressure should be well controlled before starting this drug, and your doctor will monitor it closely during treatment.
  • If you have a heart problems, including congestive heart failure. This drug may weaken the heart muscle and make heart problems worse (see “Precautions”).
  • If you have any type of liver disease (including hepatitis). This drug may cause liver damage in some people. Your doctor will do blood tests to check your liver function before and during treatment. The dose of this drug may need to be lowered in people whose liver is not functioning normally. (see “Precautions”)
  • If you have ever had thyroid problems. This drug may cause the thyroid gland to become underactive. Your doctor will do blood tests to check your thyroid function before and during treatment. (see “Precautions”)
  • If you’ve ever had blood clots in your veins or arteries. These can cause heart attacks, strokes, changes in vision, problems breathing, and leg swelling. This drug can cause blood clots, which in some cases may be life threatening (see “Precautions”).
  • If you’ve ever had any bleeding problems, such as coughing up blood or having blood in your urine or stools. This drug may make bleeding worse, which in some cases may be life threatening (see “Precautions”).
  • If you have a wound that is not healed or are planning to have surgery soon. This drug may affect wound healing, so it should be stopped at least 24 hours before any surgery (see “Precautions”).
  • If you have any other medical conditions such as kidney disease, congestive heart failure, diabetes, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug can cause problems with the fetus if taken at the time of conception or during pregnancy. Women who could become pregnant and men who are taking this drug should use some kind of birth control during treatment. Check with your doctor about what kinds of birth control can be used with this medicine. In pregnant women, treatment with this drug should be used only if the potential benefit to the mother outweighs the risk to the fetus.
  • If you are breast-feeding. While no studies have been done, this drug may pass into breast milk and affect the baby. Breast-feeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. This drug may affect fertility. Talk with your doctor about the possible risk with this drug.
  • About any other prescription or over-the-counter medicines or supplements you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

Axitinib can interact with a number of drugs and supplements, so it is very important to check with your health care team before taking any new medicines.

The following drugs and supplements can lower the levels of axitinib in the blood and might make it less effective:

  • Anti-seizure drugs, such as carbamazepine (Tegretol), phenobarbital (Solfoton), and phenytoin (Dilantin)
  • Drugs to treat tuberculosis (TB), such as rifampin (Rifadin, Rimactane; also in Rifamate and Rifater), rifabutin (Mycobutin), and rifapentin (Prifin)
  • The steroid drug dexamethasone (Decadron)
  • St. John's wort (an herbal dietary supplement)
  • Some antibiotics, such as nafcillin
  • Some anti-HIV drugs, such as efavirenz (Sustiva) and etravirine (Intelence)
  • Some drugs used to treat pulmonary arterial hypertension (high blood pressure in the arteries leading to the lungs), such as bosentan (Tracleer)

Some drugs and supplements could cause axitinib to build up in your blood, which might worsen side effects and other problems:

  • Some antibiotics, such as erythromycin, clarithromycin (Biaxin), telithromycin (Ketek), and similar drugs
  • Anti-fungal medicines such as ketoconazole (Nizoral), itraconazole (Sporanox), and voriconazole (Vfend)
  • Some anti-depressant drugs, such as nefazodone (Serzone)
  • Some anti-HIV drugs, such as indinavir (Crixivan), ritonavir (Kaletra), nelfinavir (Viracept), atazanavir (Reyataz), saquinavir (Invirase), and others

These drugs should be avoided while taking axitinib if possible, but if you need to take any of them, your doctor may need to adjust your dose of axitinib. Do not start or stop taking any of these medicines while on axitinib without talking with your doctor(s) about all of the medicines you take, including axitinib.

Other medicines or supplements may affect blood levels of axitinib, or levels of these drugs may be affected by taking axitinib. Make sure your doctor is aware of all drugs and supplements you are taking.

Any drugs or supplements that interfere with blood clotting can raise the risk of bleeding during treatment with axitinib. These include:

  • Vitamin E
  • Non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), and many others. Check with your pharmacist to see if any of your medicines, including non-prescription drugs, contain any of these.
  • Warfarin (Coumadin)
  • Ticlopidine (Ticlid)
  • Clopidogrel (Plavix)
  • Dabigatran (Pradaxa)
  • Rivaroxaban (Xarelto)
  • Apixaban (Eliquis)
  • Fondaparinux (Arixtra)
  • Any type of heparin including enoxaparin (Lovenox) and dalteparin (Fragmin)

Note that many cold, flu, fever, and headache remedies contain aspirin or ibuprofen. Ask your pharmacist if you aren't sure what’s in the medicines you take.

Check with your doctor, nurse, or pharmacist about any other medicines, herbs, and supplements you are taking, and if alcohol can cause problems with this medicine.

Interactions with foods

Grapefruit and grapefruit juice may affect the amount of axitinib in your body. Do not eat grapefruit or drink grapefruit juice while taking this drug. Check with your doctor, nurse, or pharmacist about whether any other specific foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Axitinib is taken by mouth as tablets. The usual starting dose is 5 mg (milligrams), twice a day. The tablets should be taken in the morning and in the evening, about 12 hours apart. They should be swallowed whole (not chewed or crushed) with a glass of water. They can be taken with or without food. Your dose may be raised after a few weeks if you are not having any problems taking it. On the other hand, the dose may need to be lowered if you have side effects.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you. Keep the medicine in a tightly closed container away from heat and moisture and out of the reach of children and pets.

Precautions

This drug may interact with a number of other drugs or supplements in the body. (See "Interactions" above.) Be sure your doctor is aware of all drugs and supplements you are taking. Do not start or stop taking any drug without talking to your doctor about all of them.

Axitinib can cause high blood pressure, which in some cases may be life threatening. Patients should have normal blood pressure before starting this drug, and blood pressure should be checked regularly while the patient is taking axitinib.

Patients taking axitinib have an increased risk of certain problems caused by blood clots, such as heart attack, stroke, transient ischemic attack (TIA), pulmonary embolism (a blood clot in the lungs), and loss of vision (caused when a blood clot blocks a blood vessel in the eye). This drug should be used with caution in patients who are already at high risk for these problems. Call your doctor right away if you have pain in the chest, neck, pain, jaw or arm, shortness of breath, headache, numbness or weakness on one side of your body, trouble talking, or vision changes.

Problems with bleeding from the stomach, intestines, lungs, and brain have been seen in some patients taking axitinib. This bleeding was fatal for a few. This drug should not be given to patients who have had recent problems with bleeding from these areas or who have cancer spread to the brain that has not been treated. Speak with your doctor before taking any drugs or supplements that might affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), any type of “blood thinner”, heparin, or vitamin E (See “Interactions with other drugs”). Tell your doctor right away if you have unusual bruising, or bleeding such as nosebleeds, bleeding gums, coughing or vomiting up blood, heavier-than-normal menstrual bleeding, blood in the urine, rectal bleeding, or black, tarry stools.

This drug can cause problems with wound healing and should be stopped at least 24 hours before any planned surgery.

This drug may cause the thyroid gland to become underactive, a condition called hypothyroidism. Your doctor will check your thyroid function before and during treatment with blood tests. Tell your doctor if you notice symptoms such as feeling more tired than normal, gaining weight, feeling cold, or being constipated. If the thyroid is underactive, it can easily be treated with medicine.

Rarely, axitinib can cause holes (perforations) in the digestive tract, or passageways that aren’t supposed to be there (fistulas). Both of these can be life-threatening. Tell your doctor or nurse right away if you have severe stomach (abdominal) pain, if you are vomiting blood, or if you have red or very dark colored stools.

This drug may cause liver damage, which may show up as abnormal blood test results. This drug should be used at a lower dose (or not at all) in patients with known liver problems. Your doctor will order blood tests and will check you for signs of liver problems before and during treatment to make sure your liver is working well. Tell your doctor or nurse right away if you have yellowing of the skin or the whites of your eyes (jaundice), dark urine, nausea or vomiting, loss of appetite, pain on the right side of your belly, or any abnormal bruising or bleeding.

Rarely, this drug may weaken the heart muscle, leading to a condition known as congestive heart failure. Let your doctor know right away if you notice symptoms of congestive heart failure, such as shortness of breath, swollen feet or ankles, or irregular heartbeat.

Axitinib can damage the kidneys, leading to a finding of protein in the urine. Your doctor will check your urine for protein before and during treatment. The dose of axitinib may need to be lowered or the drug may need to be stopped if this becomes a problem.

In rare cases, this drug may affect the brain in what is known as reversible posterior leukoencephalopathy syndrome (RPLS). Symptoms of RPLS might include seizures, high blood pressure, headache, trouble thinking, confusion, changes in vision, blindness, or other problems. Tell your doctor right away if you notice any of these symptoms. Symptoms usually go away once this medicine is stopped.

Avoid pregnancy while taking this drug. It may harm the fetus. Both men and women should use effective birth control during treatment. Talk with your doctor about this.

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • Diarrhea
  • High blood pressure*
  • Feeling tired
  • Loss of appetite
  • Nausea
  • Vomiting
  • Voice changes
  • Hand-foot syndrome (redness, pain, itching, and/or peeling palms of the hands and soles of the feet)
  • Weight loss
  • Feeling weak
  • Constipation
  • Low blood cell counts
  • Abnormal blood test results suggesting the drug may be affecting the liver (Your doctor will discuss the importance of this finding, if any.)*

Less common

  • Hypothyroidism*
  • Cough
  • Joint pain
  • Mouth sores
  • Shortness of breath
  • Abdominal pain
  • Headache
  • Rash
  • Change in how things taste
  • Protein in the urine (a sign of kidney damage)*
  • Feeling dizzy
  • Dry skin
  • Upset stomach
  • Itching
  • Muscle pain
  • Nose bleeds

Rare

  • Hair loss (may include body and facial hair)
  • Hemorrhoids
  • Severe bleeding (from the kidneys/bladder, stomach/intestine, rectum, or lungs)*
  • Ringing in the ears
  • Burning of the mouth or tongue
  • Blood clot in the lungs or legs*
  • Heart attack*
  • Stroke or transient ischemic attack (sometimes called a "mini-stroke")*
  • Vision loss*
  • Hole (perforation) in the stomach or intestines*
  • Changes in the brain that can cause headache, confusion, seizures, or blindness*
  • Congestive heart failure*
  • Death from bleeding, blood clots, or other problems

*See the "Precautions" section for more detailed information.

Other side effects not listed above can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 2012

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.


Last Medical Review: 11/06/2013
Last Revised: 08/29/2014