GLEEVEC FAQs—KIT+ GIST Dosing

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    How do I take GLEEVEC?

    • GLEEVEC® should be taken with a meal and a full glass of water and should be taken approximately at the same time each day.
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    Can GLEEVEC be taken with or without food?

    • GLEEVEC should be taken with food and a large glass of water to minimize GI upset.  GLEEVEC should not be taken with grapefruit juice.
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    How is GLEEVEC supplied?

    • GLEEVEC comes as 100-mg and 400-mg scored tablets. Your doctor will prescribe your dose based on the specifics of your disease.
    • GLEEVEC 100 mg: Very dark yellow to brownish orange, film-coated tablets, round, biconvex with beveled edges, debossed with "NVR" on one side, and "SA" with score on the other side.
    • GLEEVEC 400 mg: Very dark yellow to brownish orange, film-coated tablets, ovaloid, biconvex with beveled edges, debossed with "400" on one side with score on the other side, and "SL" on each side of the score.
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    How should GLEEVEC be stored?

    • GLEEVEC should be stored at room temperature.  Do not store medicine in hot, damp, or humid places. Keep all medications away from the reach of children.
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    What should I do if I miss a dose?

    • If a dose of this medicine is missed, contact your physician or pharmacist.  DO NOT double dose.
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    Can I take an extra dose?

    • No. Continue with therapy as directed by your physician.
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    Can I stop taking GLEEVEC if I feel better?

    • It is very important for you to continue taking GLEEVEC unless the physician has told you to stop treatment.
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    How soon can I expect to see improvement?

    • It is important to remember that people respond differently to therapy.  How you respond to treatment with GLEEVEC will depend on many factors, but your physician has prescribed GLEEVEC because he or she believes you might benefit from it.
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    How does GLEEVEC work in treating metastatic/unresectable KIT+ GIST?

    • GLEEVEC targets several different tumor proteins, including KIT that is the suspected cause of most gastrointestinal stromal tumors (GISTs). In KIT–positive (KIT+) GISTs, an abnormal KIT protein sends out a constant signal that tells the cells to keep growing resulting in tumor formation; GLEEVEC may work by blocking, or turning off, the signal from the KIT protein, so the cancerous cells stop growing.
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    How does GLEEVEC work as adjuvant treatment after resection of KIT+ GIST?

    • Even when an operation has gone well and the tumor has been removed completely, there is still a chance that the GIST will grow back. The results of a clinical trial have shown that patients with KIT+ GIST who took a targeted therapy called GLEEVEC after their operation (as adjuvant treatment) were much less likely to have their tumor grow back compared with patients who did not take GLEEVEC.
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    How long do I have to take GLEEVEC after surgery?

    • In the adjuvant clinical study, GLEEVEC was administered for 1 year in patients with tumor size ≥3cm. The optimal duration of GLEEVEC therapy is unknown.
    • Treatment length will vary from patient to patient.  Speak with your physician for information about your specific condition.
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    Can I take other medications while on GLEEVEC?

    • Do not take any other medications without talking to your doctor or pharmacist first, including over-the-counter medications such as Tylenol® (acetaminophen); herbal products (St. John's wort, Hypericum perforatum); Coumadin® (warfarin sodium); rifampin; erythromycin; metoprolol; ketoconazole; and Dilantin® (phenytoin). Taking these with GLEEVEC may affect how they work, or affect how GLEEVEC works.
    • You should also tell your doctor if you are taking or plan to take iron supplements.  Patients should also avoid grapefruit juice and other foods that may affect how GLEEVEC works.
    • Tylenol (acetaminophen) is a registered trademark of McNeil Consumer & Specialty Pharmaceuticals, a division of McNeil PPC, Inc. Coumadin (warfarin sodium) is a registered trademark of Bristol-Myers Squibb Company. Dilantin (phenytoin) is a registered trademark of Parke-Davis, a division of Pfizer Inc.
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    What are the possible side effects of GLEEVEC?

    • The following serious side effects have been reported by patients taking GLEEVEC:
      • Severe fluid retention (holding water) and swelling
      • Cytopenias (reduction of certain elements in blood circulation)
      • Severe congestive heart failure (impaired ability of the heart to pump blood) and left ventricular dysfunction (impaired functioning of the left side of the heart)
      • Severe liver problems (hepatotoxicity)
      • Hemorrhage (abnormal bleeding)
      • GI perforation (holes in the stomach or intestine)
      • Hypereosinophilic (a condition with increased eosinophils, which are a type of white blood cell) heart disease
      • Skin reactions (such as fluid-filled blisters)
      • Hypothyroidism (reduction in thyroid hormones)
      • Potential toxicities from long-term use, specifically liver, kidney, and/or heart toxicities
      • Potential harm to an unborn child
      • Growth retardation (slowing of growth)
      • Tumor lysis syndrome (electrolyte disturbance)
      • Dizziness, blurred vision, and somnolence
    • Your doctor will check you closely for any side effects to stop more serious complications from occurring. Patients with heart disease or risk factors for heart failure should also be monitored carefully.
    • GLEEVEC is sometimes associated with stomach or intestinal irritation. GLEEVEC should be taken with food and a large glass of water to minimize this problem. There have been rare reports, including deaths, of stomach or intestinal perforation (a small hole or tear).
    • If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.
    • Some common side effects of GLEEVEC

    • Almost all patients treated with GLEEVEC experience side effects at some time. Most side effects are mild to moderate in severity. Some common side effects that you may experience include:
      • Fluid retention (holding water)
      • Muscle cramps, pain, or bone pain
      • Abdominal pain
      • Anorexia (loss of appetite)
      • Vomiting
      • Diarrhea
      • Decreased hemoglobin (decrease in blood cells which carry oxygen)
      • Hemorrhage (abnormal bleeding)
      • Nausea
      • Fatigue
      • Rash
    • If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.
    • The severity of some side effects may be reduced with the help of other medicines and advice from your doctor, while others may require stopping GLEEVEC therapy for a while or changing the dose. However, in some cases, GLEEVEC therapy may need to be discontinued.
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Side effects

Almost all people taking GLEEVEC experience side effects. Be sure to talk to your oncologist and/or healthcare professional about any GLEEVEC side effects you are experiencing.

Some serious side effects include:

  • Severe fluid retention (holding water), which can cause swelling around the eyes or swelling of the lower legs, lungs, and heart (reported in 9%-13.1% of patients); fatal in rare cases
  • Increased pressure in the heart or brain; fatal in rare cases
  • Low levels of certain blood cells
  • Heart failure
  • Liver problems
  • Hemorrhage (abnormal bleeding); reported in 5%-12.9% of patients in clinical trials
  • Skin blistering
  • Low levels of thyroid hormone

Some common side effects are:

  • Fluid retention (holding water)
  • Muscle cramps or pain and bone pain
  • Abdominal pain
  • Vomiting
  • Diarrhea
  • Decreased hemoglobin (decrease in blood cells which carry oxygen)
  • Nausea
  • Fatigue
  • Skin reactions, some severe
  • Anorexia (loss of appetite)

Supportive care may help reduce the severity of some side effects, whereas others require discontinuation or dosage adjustment. Don't stop taking your medication or change your dose without talking to your oncologist.

GLEEVEC can cause harm to the unborn child when administered to a pregnant woman. Women should be aware of the potential harm to the fetus. Be sure to inform your doctor if you are or think you may be pregnant. You should not breastfeed while taking GLEEVEC.

Side effects

What it feels like

How your doctor may manage it

Swelling and fluid retention

Swollen legs or feet and swelling around the eyes. Fluid retention can appear as quick weight gain or swelling in your lower legs or other parts of your body. Fluid retention can be serious or even life threatening

  • Regular checkups to monitor your weight
  • Prescribe a topical steroid cream to reduce the swelling around your eyes
  • Tell you to limit your salt intake
  • Prescribe a diuretic (a medicine to help your body get rid of extra fluids)
  • Decrease dose of GLEEVEC

Skin reactions, some severe (including erythema muliforme and Stevens-Johnson syndrome)

Scaly skin; red itchy bumps on skin. Flu-like symptoms followed by painful red or purplish rash

  • Recommend an over-the-counter (OTC) antihistamine
  • Prescribe a corticosteroid or stronger antihistamine
  • Painkillers, sedatives, antibiotics for secondary infections
  • May interrupt therapy and resume at a lower dose

Nausea and vomiting

Feeling queasy or like you have to throw up.You may also feel like you have indigestion

  • Recommend taking GLEEVEC with a meal and a large glass of water. (If you have been instructed not to take GLEEVEC with meals, contact your doctor before changing your dose to mealtimes.)
  • Recommend OTC medications
  • If you are taking your GLEEVEC once a day, talk to your doctor about possibly dividing the dose in half and taking it twice a day

Muscle cramps

Pain or spasms in the legs, feet, or calves

  • Recommend an OTC pain reliever like ibuprofen
  • Recommend a prescription pain reliever
  • Recommend calcium and magnesium supplements

Muscle and bone pain

Whole-body ache; twitching or burning muscles

  • Recommend an OTC pain reliever like ibuprofen
  • Recommend a prescription pain reliever

Diarrhea

More bowel movements; loose stools

  • Recommend an OTC medication

Important information about GLEEVEC® (imatinib mesylate)

GLEEVEC® (imatinib mesylate) is available only by prescription.

GLEEVEC® Indications

GLEEVEC® (imatinib mesylate) tablets are indicated for:

  • Newly diagnosed adult and pediatric patients with Philadelphia chromosome–positive chronic myeloid leukemia (Ph+ CML) in the chronic phase
  • Patients with Ph+ CML in blast crisis (BC), accelerated phase (AP), or in the chronic phase (CP) after failure of interferon-alpha therapy
  • Adult patients with relapsed or refractory Ph+ acute lymphoblastic leukemia (Ph+ ALL)
  • Pediatric patients with newly diagnosed Philadelphia chromosome–positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy
  • Adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene rearrangements
  • Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-KIT mutation or with c-KIT mutational status unknown
  • Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown
  • Adult patients with unresectable, recurrent, and/or metastatic dermatofibrosarcoma protuberans (DFSP)
  • Patients with KIT (CD117)-positive gastrointestinal stromal tumors (GISTs) that are cancerous, cannot be surgically removed, and/or have spread to other parts of the body
  • Adult patients after surgery who have had their KIT (CD117)-positive GISTs completely removed

SAFETY: Important product information (Please see accompanying full Prescribing Information)

Who should NOT take GLEEVEC

  • Women who are or could be pregnant. Harm to the unborn child can occur when administered to pregnant women. Therefore, women should not become pregnant and should be advised of the potential risk to the unborn child if GLEEVEC is used during pregnancy
  • Women who are breastfeeding because of the potential for serious adverse reactions in nursing infants

Sexually active females should use highly effective birth control while taking GLEEVEC.

Be sure to talk to your doctor and/or healthcare professional about these issues before taking GLEEVEC.

Warnings and precautions

  • GLEEVEC is often associated with edema (swelling) and serious fluid retention (holding water). It is important that patients be weighed and monitored regularly for signs and symptoms of serious fluid retention or unexpected weight gain. Patients experiencing unexpected, rapid weight gain should speak to their doctor about appropriate supportive care treatment. Studies have shown that edema tended to occur more often among patients who are 65 and older or those taking higher doses of GLEEVEC. If you experience severe fluid retention, your doctor may treat you with diuretics and may stop your GLEEVEC treatment until the fluid retention has been managed. Treatment can be returned as appropriate depending on the initial severity of the event
  • Cytopenias (reduction or lack of certain cell elements in blood circulation) have occurred. Your doctor will test your blood weekly for the first month, biweekly for the second month, and periodically thereafter. In most cases, your doctor will reduce or interrupt your GLEEVEC therapy; in rare cases, if the cytopenia is severe, your doctor may discontinue treatment
  • Severe congestive heart failure (impaired ability of the heart to pump blood) and left ventricular dysfunction (impaired functioning of the left side of the heart) have been reported, particularly in patients with other health issues and risk factors. Patients with heart disease or risk factors for heart disease or history of renal failure will be monitored and treated for the condition
  • Severe liver problems (hepatotoxicity) may occur. Cases of fatal liver failure and severe liver injury requiring liver transplants have been reported with both short-term and long-term use of GLEEVEC. Your doctor will check your liver function before beginning treatment and continue to monitor liver function as needed. If you experience severe liver problems, your doctor may stop your treatment with GLEEVEC until the liver problem has been managed
  • Bleeding may occur. Severe gastrointestinal (GI) bleeding has been reported in patients with Ph+ CML and KIT+ GIST. GI tumor sites may be the cause of this bleeding; therefore, GI symptoms should be monitored at the start of treatment
  • GI perforation (small holes or tears in the wall of the stomach or intestine), in some cases fatal, has been reported
  • In patients with hypereosinophilic syndrome (a condition with increased eosinophils, which are a type of white blood cell), e.g., HES, MDS/MPD, or ASM and heart involvement, cases of heart disease have been associated with the initiation of GLEEVEC therapy. Speak to your doctor regarding appropriate supportive care or discontinuing GLEEVEC
  • Skin reactions, such as fluid-filled blisters, have been reported with the use of GLEEVEC
  • Clinical cases of hypothyroidism (reduction in thyroid hormones) have been reported in patients taking levothyroxine replacement during treatment with GLEEVEC. Your doctor should closely monitor your thyroid hormone levels
  • Long-term use may result in potential liver, kidney, and/or heart toxicities. Immune system suppression may also result from long-term use
  • GLEEVEC can cause harm to the unborn child when administered to a pregnant woman. Women should be aware of the potential harm to the fetus. Be sure to inform your doctor if you are or think you may be pregnant. You should not breastfeed while taking GLEEVEC
  • Growth retardation (slowing of growth) has been reported in children taking GLEEVEC. The long-term effects of extended treatment with GLEEVEC on growth in children are unknown. Growth retardation may be monitored in children receiving treatment
  • Cases of tumor lysis syndrome (TLS), which refers to an electrolyte disturbance caused by the breakdown of tumor cells, have been reported and can be life threatening in some cases. The patients at risk of TLS are those who have a higher number of tumor cells and whose tumors are fast growing before beginning therapy. Your doctor should monitor you closely and take appropriate precautions. Correction of clinically significant dehydration and treatment of high uric acid levels are recommended prior to initiation of GLEEVEC
  • Motor vehicle accidents involving patients receiving GLEEVEC have been reported. Patients should be advised that they may experience undesirable effects such as dizziness, blurred vision, or drowsiness during treatment with GLEEVEC. Caution should be recommended when driving a car or operating machinery

Additional important safety information

The following serious side effects have been reported by patients taking GLEEVEC:

  • Severe fluid retention (holding water), which can cause swelling around the eyes or swelling of the lower legs, lungs, and heart; fatal in rare cases
  • Increased pressure in the heart or brain; fatal in rare cases
  • Low levels of certain blood cells
  • Heart failure
  • Liver problems
  • Hemorrhage (abnormal bleeding)
  • Skin blistering
  • Low levels of thyroid hormone

Your doctor will check you closely for any side effects to stop more serious complications from occurring. Patients with heart disease or risk factors for heart failure should also be monitored carefully.

GLEEVEC is sometimes associated with stomach or intestinal irritation. GLEEVEC should be taken with food and a large glass of water to minimize this problem. There have been rare reports, including deaths, of stomach or intestinal perforation (a small hole or tear).

If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.

Common side effects of GLEEVEC

Almost all patients treated with GLEEVEC experience side effects at some time. Most side effects are mild to moderate in severity. Some common side effects that you may experience include:

  • Fluid retention (holding water)
  • Muscle cramps, pain, or bone pain
  • Abdominal pain
  • Anorexia (loss of appetite)
  • Vomiting
  • Diarrhea
  • Decreased hemoglobin (decrease in blood cells which carry oxygen)
  • Hemorrhage (abnormal bleeding)
  • Nausea
  • Fatigue
  • Rash

If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.

The severity of some side effects may be reduced with the help of other medicines and advice from your doctor, while others may require stopping GLEEVEC therapy for a while or changing the dose. However, in some cases, GLEEVEC therapy may need to be discontinued.

Tell your doctor if you have a history of heart disease or risk factors for heart disease or if you experience side effects, including fever, shortness of breath, blood in your stools, jaundice (yellowing of the skin and/or eyes), sudden weight gain, or symptoms of heart failure during therapy with GLEEVEC.

After the approval of GLEEVEC, the following adverse events have been reported in patients treated with GLEEVEC: compression of the heart due to increased fluid, swelling of the brain, GI perforation (holes in the stomach or intestine), and sudden lung failure. These events, including some fatalities, may or may not have been drug related.

Take GLEEVEC exactly as prescribed. Do not change your dose or stop taking GLEEVEC unless you are told to do so by your doctor. If you miss a dose, take your dose as soon as possible, unless it is almost time for your next dose. In this case, your missed dose should not be taken. A double dose should not be taken to make up for any missed dose. You should take GLEEVEC with a meal and a large glass of water.

Do not take any other medications without talking to your doctor or pharmacist first, including over-the-counter medications such as Tylenol® (acetaminophen); herbal products (St. John's wort, Hypericum perforatum); or prescription medications including Coumadin® (warfarin sodium); rifampin; erythromycin; metoprolol; ketoconazole; and Dilantin® (phenytoin). Taking these with GLEEVEC may affect how they work, or affect how GLEEVEC works.

You should also tell your doctor if you are taking or plan to take iron supplements. Patients should also avoid grapefruit juice and other foods that may affect how GLEEVEC works.

Tylenol (acetaminophen) is a registered trademark of McNeil Consumer & Specialty Pharmaceuticals, a division of McNeil PPC, Inc. Coumadin (warfarin sodium) is a registered trademark of Bristol-Myers Squibb Company. Dilantin (phenytoin) is a registered trademark of Parke-Davis, a division of Pfizer Inc.

Please see accompanying full Prescribing Information, which includes a more complete discussion of the risks associated with GLEEVEC.

You are encouraged to report negative side effects of prescription drugs to the FDA.  Visit www.fda.gov/medwatch, or call 1-800-FDA-1088.