Glivec Medicines Fight against Cancer

In this factsheet:
• How does Gleevec work? What will it do for me?
• How should I use Gleevec?
• What form(s) does Gleevec come in?
• Who should NOT take Gleevec?
• What side effects are possible with Gleevec?
• Are there any other precautions or warnings for Gleevec?
• What other drugs could interact with Gleevec?

DIN (Drug Identification Number)

What is GLEEVEC^®?

GLEEVEC is a first-line Ph+ CML treatment, a potent and specific inhibitor of the BCR-ABL tyrosine kinase, the cause of Ph+ CML. It is a revolutionary drug that attacks only the cells that cause Ph+ CML, without harming healthy cells.

How GLEEVEC works: GLEEVEC focuses on and works to "turn off" specific proteins in cancer cells that cause the cancer cells to grow and multiply. GLEEVEC may block the signal from the cancer protein that causes Ph+ CML—the BCR-ABL protein.

How effective is GLEEVEC?: In a multicenter, international study of 1106 newly diagnosed Ph+ CML patients, GLEEVEC was compared with interferon-alpha therapy. The study was designed so that if after a designated period of time a patient did not achieve a predefined response, a change in therapy was permitted. After 7 years, only 2% of patients remained on interferon-alpha therapy. Of the patients taking GLEEVEC, 92.5% had not progressed to either the accelerated phase or blast phase. The overall survival rate was 86% for those taking GLEEVEC and 83% for those taking interferon alpha.

Side effects: Almost all patients treated with GLEEVEC in clinical trials experienced side effects at some time. In general, side effects vary with each person. It is important to discuss any side effects with your healthcare team.

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:

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.

How to take it: For most patients, GLEEVEC is available as a once-a-day medication. Unlike many cancer medicines, GLEEVEC comes in a tablet form that you take by mouth with water, instead of by injection. You should take GLEEVEC exactly as your doctor tells you.

GLEEVEC is available by prescription only and is supplied as 100-mg and 400-mg tablets. For patients having difficulty swallowing, GLEEVEC can be dissolved in water or apple juice.

How does Gleevec work? What will it do for me?

Imatinib belongs to a family of medications called protein tyrosine kinase inhibitors. It is used to treat adults and children who have been newly diagnosed with chronic myeloid leukemia (CML). It works by affecting enzymes that play a role in certain cancer cells.

It is also used to treat adults with chronic myeloid leukemia (CML) in blast crisis (sudden attack), accelerated phase (fast growth), or in chronic phase (long-term illness) after the failure of interferon-alpha therapy. Imatinib is also used to treat adults with cancerous gastrointestinal stromal tumours (GIST) that cannot be removed by surgery or that are spreading to other parts of the body.

It is used to treat adults who have been newly diagnosed with certain types of acute lymphoblastic leukemia (Ph+ALL) and Ph+ALL that has not responded (is refractory) to other medications. Imatinib is also used to treat dermatofibrosarcoma protuberans (DFSP), a cancer where tissue under the skin grows out of control when it cannot be removed by surgery or it is spreading to other parts of the body.

Other types of cancers can also be treated with imatinib. Imatinib may also be used to treat some types of myelodysplastic/myeloproliferative diseases (MDS/MPD), aggressive sytstemic mastocytosis (ASM), hypereosinophilic syndrome (HES), and chronic eosinophilic leukemia (CEL). In these conditions, different types of blood cells start growing out of control.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. As well, some forms of this medication may not be used for all of the conditions discussed here. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

How should I use Gleevec?

Treatment with imatinib should be started under the direct supervision of a physician experienced in the treatment of the conditions for which this medication is being used.

For newly diagnosed chronic myeloid leukemia (CML) or chronic phase CML, the usual adult dose of imatinib is 400 mg daily. The usual adult dose in accelerated phase or blast crisis CML is 600 mg daily. The dose for children is based on the child's height and weight and will be calculated by your doctor.

For cancerous gastrointestinal stromal tumours (GIST), the usual adult dose ranges from 400 mg to 600 mg daily. Dose adjustments may be required depending on your response and on the side effects you experience.

For Ph+ALL, the usual adult dose is 600 mg daily.

For MDS/MPD in adult patients, the starting dose is 400 mg daily.

For some types of ASM, HES, or CEL, the starting dose is 100 mg daily. Depending on how you respond to the treatment and on the side effects you experience, you doctor may increase your dose to 400 mg daily.

For DFSP in adult patients, imatinib is taken as 800 mg daily. Doses of 800 mg should be taken as 400 mg twice a day, in the morning and evening.

Imatinib should be taken by mouth, with a meal and a large glass of water. Avoid drinking grapefruit juice while you are taking imatinib. Swallow the tablets whole.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

What form(s) does Gleevec come in?

100 mg
Each scored tablet contains imatinib 100 mg. Nonmedicinal ingredients: cellulose (microcrystalline), colloidal silicon dioxide, crospovidone, hydroxypropyl methylcellulose, magnesium stearate, ferric oxide (red), ferric oxide (yellow), hydroxypropyl methylcellulose, polyethylene glycol, and talc.

400 mg
Each scored tablet contains imatinib 400 mg. Nonmedicinal ingredients: cellulose (microcrystalline), colloidal silicon dioxide, crospovidone, hydroxypropyl methylcellulose, magnesium stearate, ferric oxide (red), ferric oxide (yellow), hydroxypropyl methylcellulose, polyethylene glycol, and talc.

Who should NOT take Gleevec?

Imatinib should not be taken by anyone who is allergic to imatinib or to any of the ingredients of the medication.

This medication should not be used except under direct supervision by an experienced physician.