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Dasatinib

(duh-sat-uh-nib)

Trade/other name(s): Sprycel

Why would this drug be used?

This drug is used to treat certain kinds of leukemia, especially chronic myelogenous leukemia (CML) and some forms of acute lymphocytic leukemia (ALL). It is also being studied for use against a number of other cancers and non-cancerous conditions.

How does this drug work?

Dasatinib is a targeted therapy called a tyrosine kinase inhibitor. Tyrosine kinases are proteins at the surface of a cell that signal the cell's control center to grow and divide. Dasatinib blocks the signals from these proteins, which helps stop the leukemia cells from growing.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. Reduced liver function may result in more drug than expected staying in the body, which could lead to unwanted side effects. Your doctor may need to adjust your dose accordingly.
  • If you have any type of heart problem (including long QT syndrome), if you have had chemotherapy that affects the heart, or if you are taking medicines to help your heart rhythm. This drug may affect the rhythm of the heart or have other effects.
  • If you have congestive heart failure. This drug may contribute to heart failure or make existing conditions worse.
  • If you are lactose intolerant. This drug contains lactose.
  • If you have ever had blood clots or are taking any "blood-thinning" medicines (see next section). Dasatinib may increase your risk of serious bleeding problems, and your doctor may have to watch you more closely.
  • If you have any other medical conditions such as kidney disease, high blood pressure, 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. 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. Although 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 and the options that may preserve your ability to have children.
  • About any other prescription or over-the-counter medicines 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

The following drugs can also cause dasatinib to build up in the body, raising the risk of serious side effects:

  • the antidepressant nefazodone (Serzone)
  • the antibiotics erythromycin (EES), clarithromycin (Biaxin), telithromycin (Ketek), and similar drugs
  • anti-fungal antibiotics such as ketoconazole (Nizoral), itraconazole (Sporanox), voriconazole (Vfend)
  • HIV drugs such as indinavir, ritonavir, fosamprenavir, nelfinavir, atazanavir, and others

Do not start or stop taking these medicines while on dasatinib without talking with the prescribing doctor(s) about all of the medicines you take, including dasatinib.

These drugs and supplements can lower the levels of dasatinib in the blood and make it less effective:

  • anti-seizure drugs carbamazepine (Tegretol), phenobarbital (Luminal), and phenytoin (Dilantin)
  • TB drugs rifampin (Rifadin, Rimactane; also in Rifamate and Rifater), and rifabutin (Mycobutin)
  • the steroid drug dexamethasone (Decadron)
  • St. John's wort (herbal dietary supplement)

If you need to take these drugs, your doctor may need to adjust your dose of dasatinib.

Drugs commonly used to treat heartburn, reflux, or ulcers reduce the acid levels in the stomach, which affects the amount of dasatinib your body can absorb. Tell your doctor if you are taking:

  • any H2 blocker such as cimetidine (Tagamet), ranitidine (Zantac), famotidine (Pepcid), or nizatidine (Axid)
  • any proton pump inhibitor such as omeprazole (Prilosec), esomeprazole (Nexium), pantoprazole (Protonix), rabeprazole (Aciphex), or lansoprazole (Prevacid).

Antacids (Maalox, Mylanta, Tums, etc.) may affect the body's ability to absorb dasatinib. If you are taking antacids, they should be taken at least 2 hours before or after you take dasatinib.

Dasatinib may raise your risk of heart rhythm problems even more if you are taking other drugs that affect the body's mineral (electrolyte) balance or that affect the heart rhythm, such as these:

  • diuretics (water pills)
  • antibiotics such as ciprofloxacin (Cipro), levofloxacin Levaquin), sparfloxacin (Zagam), moxifloxacin (Avelox), erythromycin (E.E.S., E-Mycin, Erythrocin), clarithromycin (Biaxin), or pentamidine (Pentam, NebuPent)
  • anti-fungal drugs (amphotericin B)
  • heart rhythm drugs such as amiodorone (Cordarone, Pacerone), disopyrmide (Norpace), ibutilide (Corvert), procainamide (Procan, Pronestyl), quinidine (Quinidex, Cardioquin), sotalol (Betapace), dofetilide (Tikosyn)
  • mental health drugs such as haloperidol (Haldol), thioridazine (Mellaril), pimozide (Orap), mesoridazine (Serentil), chlorpromazine (Thorazine)
  • methadone (Dolophine, Methadose)
  • the anti-nausea drug droperidol (Inapsine)
  • anti-malaria drugs halofantrine (Halfan) and chloroquine (Aralen)
  • bepridil (Vascor), a drug for angina or heart pain

Dasatinib may change the blood levels of other drugs you are taking, including cyclosporine (Sandimmune), alfentanil (Alfenta), fentanyl (Duragesic, Actiq, Fentora, Onsolis), pimozide (Orap), sirolimus (Rapamune), tacrolimus (Prograf), and ergotamine (Ergomar). Tell your doctor if you are taking any of these drugs.

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

  • vitamin E
  • non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), and many others
  • warfarin (Coumadin)
  • ticlopidine (Ticlid)
  • clopidogrel (Plavix)

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.

There may be more drugs that interact with dasatinib. Check with your doctor, nurse, or pharmacist about other medicines, vitamins, herbs, and supplements, and whether alcohol can cause problems with this medicine.

Interactions with foods

Avoid grapefruit, grapefruit juice, or grapefruit extract. Grapefruit may change the level of dasatinib in your blood. Check with your doctor, nurse, or pharmacist about whether some other 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?

Dasatinib is a pill taken by mouth. The usual starting dose depends on what kind of cancer is being treated. Swallow tablets whole, with water. Do not crush, cut, chew, or break tablets. The tablets may be taken with or without food, but avoid grapefruit or grapefruit juice. Do not take antacids within 2 hours of this drug.

The dose or schedule may need to be adjusted if you have side effects, are taking certain other drugs that may interact with dasatinib, if you have liver problems, or if it appears that the starting dose is not having the desired effect.

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. Store the medicine in a tightly closed container away from heat and moisture and away from children and pets.

Precautions

Your doctor will probably test your blood throughout your treatment, and look for possible effects of the drug on blood counts or on blood chemistry levels. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to lower or delay your next dose of this drug, or even stop it altogether. Be sure to keep all your appointments for lab tests and doctor visits.

Dasatinib may lower your blood platelet count in the weeks after it is given, which can raise your risk of bleeding. Some people taking dasatinib have had serious bleeding in the stomach, intestine, or brain, which in some cases has been life-threatening. Talk with your doctor before taking any drugs or supplements that could affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), or vitamin E. Tell your doctor right away if you notice unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, or black, tarry stools.

This drug may lower your red blood cell count. If this happens, it will usually happen a few weeks after starting treatment. A low red blood cell count (known as anemia) can cause shortness of breath, or make you feel weak or tired all the time. Your doctor may give you medicines to help prevent or treat this condition, or you may need to have blood transfusions.

This drug can lower your white blood cell count, especially in the weeks after the drug is given. This can increase your chance of getting an infection. Be sure to tell your doctor or nurse right away if you have any signs of infection, such as fever (100.5° or higher), chills, pain when urinating, new onset of cough, or bringing up sputum.

Do not get any immunizations (vaccines), either during or after treatment with dasatinib, without your doctor's OK. Dasatinib may affect your immune system. This could keep vaccinations from working, or even lead to serious infections if you get a live virus vaccine during or soon after treatment. Try to avoid contact with people who have recently received a vaccine that uses live virus, such as the oral polio vaccine or smallpox vaccine. Check with your doctor about this.

Dasatinib may cause fluid to build up around your heart or lungs or in your belly, and may cause swelling around your eyes or in your hands or feet (edema). Tell your doctor or nurse right away if you have rapid weight gain, swelling around your eyes or in your hands or feet, swelling in your abdomen, or trouble breathing (shortness of breath).

Some patients taking this drug have developed heart problems such as a heart attack or a decrease in heart function. In some, the heart function problems led to congestive heart failure, a condition where the heart is unable to pump enough blood to meet the needs of the body. Symptoms include shortness of breath and swelling in your feet and legs. Let your doctor know right away if you have problems with chest pain or pressure or symptoms of congestive heart failure.

This drug can cause a change in heart rhythm called long QT syndrome, which can be serious or even lead to death. Your doctor may check your heart with an EKG before you start this drug and check it again after you have been on it for a time. Certain drugs that may also affect heart rhythm should be avoided while on this drug (see “Interactions with other drugs”). Report any episodes of fast or irregular heartbeat, chest pain, lightheadedness, dizziness, or shortness of breath to your doctor right away.

Your liver may be affected by this drug, which could increase liver enzyme levels in your blood. Your doctor will probably check your liver function with blood tests regularly. Dasatinib may need to be stopped or the dose changed if the effects are severe. If you have liver problems before starting treatment, the doctor may need to watch you more carefully.

This drug can rarely lead to an increase in the blood pressure of the arteries in the lungs, called pulmonary arterial hypertension. This causes the heart to work harder than normal, and can lead to not having enough oxygen in the blood and symptoms like shortness of breath, fatigue (tiredness), and swelling in the hands and feet. This problem may improve if the drug is stopped.

Women should avoid pregnancy while taking this drug and for some time afterward. The drug may harm the fetus. Men taking the drug should use condoms with their female partners to avoid causing pregnancy. 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

  • swelling around the eyes or in the hands or feet (edema)*
  • nausea
  • diarrhea (usually mild)
  • feeling tired
  • headache
  • fever
  • muscle or bone pain
  • skin rash
  • shortness of breath
  • low white blood cell count (with increased risk of infection)*
  • low blood platelet count (with increased risk for bleeding)*

Less common

  • fluid buildup in the lining of the lungs (pleural effusion), heart (pericardial effusion), or abdomen (ascites)*
  • bleeding problems*
  • change in heart rhythm*
  • feeling dizzy
  • infections
  • cough
  • vomiting
  • abdominal pain
  • chest pain
  • loss of appetite
  • weight loss
  • weight gain*
  • constipation
  • weakness
  • joint pain
  • swelling or sores in the mouth
  • low red blood cell counts (anemia)*
  • low blood calcium or phosphate levels (Your doctor will discuss the importance of this finding, if any.)

Rare

  • abnormal blood tests suggesting drug may be affecting the liver. (Your doctor will discuss the importance of this finding, if any.)*
  • congestive heart failure (can cause shortness of breath or swelling in hands or feet)*
  • heart attack*
  • pulmonary arterial hypertension (can cause shortness of breath or swelling in hands or feet)*
  • pneumonia
  • infection
  • bleeding in the brain
  • death due to bleeding in the brain or other problems

*See "Precautions" section for more detailed information.

There are other side effects not listed above that 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 2006.

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: 02/26/2010
Last Revised: 10/12/2011