Gleevec (imatinib)

What is Gleevec?

Gleevec is a brand-name prescription medication. It’s used to treat certain types of blood cancers in adults and children. Gleevec is also used to treat a type of skin cancer and a type of gastrointestinal cancer.

Gleevec contains the drug imatinib mesylate, which belongs to a class of drugs called tyrosine kinase inhibitors.

Gleevec comes as a tablet that you take by mouth. You take the drug either once or twice a day, depending on the dosage your doctor prescribes.

What it does

The Food and Drug Administration (FDA) has approved Gleevec to treat certain types of blood cancers, including:

• Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in adults and children
• Ph+ acute lymphocytic leukemia (ALL) that’s relapsed* or refractory* in adults
• newly diagnosed Ph+ ALL in children
• myelodysplastic/myeloproliferative diseases (bone marrow cancers) in adults with platelet-derived growth factor receptor (PDGFR) gene rearrangements
• hypereosinophilic syndrome or chronic eosinophilic leukemia in adults
• aggressive systemic mastocytosis in adults without the D816v c-Kit mutation

* Relapsed cancer has returned after remission, which is a decrease in cancer signs and symptoms. Refractory cancer hasn’t responded to previous cancer treatments.

Gleevec is also approved to treat:

• a type of skin cancer called dermatofibrosarcoma protuberans (DFSP) in adults
• a type of gastrointestinal cancer called Kit-positive gastrointestinal stromal tumors (GIST) in adults

For details, see the sections for “Gleevec for CML” and “Other uses for Gleevec.”

Gleevec effectiveness

Gleevec has been found effective in treating several different types of blood cancers.

In one clinical study, adults with newly diagnosed CML in the chronic phase took Gleevec for seven years. In this group, 96.6 % of people had a complete response to the drug. This means that no cancerous cells were found in their blood, and they had no symptoms of cancer.

Complete response is one way to describe the success rate. In the group of people who received standard chemotherapy, 56.6% had a complete response.

Gleevec has also been found effective in treating gastrointestinal stromal tumors (GIST) in clinical studies. The overall survival rate was about four years. This means that half the people in the study lived for about four years after they started taking Gleevec. People who took Gleevec after having surgery lived for about five years after starting the drug.

To learn how effective Gleevec is in treating other types of cancers, see the “Other uses for Gleevec” section.

Gleevec generic

Gleevec is available as a brand-name medication and as a generic form.

Gleevec contains the active drug ingredient imatinib mesylate.

Gleevec side effects

Gleevec can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Gleevec. These lists don’t include all possible side effects.

For more information on the possible side effects of Gleevec, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome.

More common side effects

The more common side effects of Gleevec can include:

• diarrhea
• belly pain
• fatigue (lack of energy)
• edema (swelling, typically in your legs, ankles, or feet and around your eyes)
• muscle cramps or pain
• nausea
• vomiting
• rash

Many of these side effects may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk with your doctor or pharmacist.

Serious side effects

Serious side effects from Gleevec aren’t common, but they can occur. Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency.

Serious side effects and their symptoms can include the following:

• Severe fluid retention (too much fluid or water) in and around your heart, lungs (pleural effusion), and belly (ascites). Symptoms can include:
• unexpected, rapid weight gain
• chest pain
• shortness of breath
• trouble taking deep breaths
• trouble breathing when you lie down
• dry cough
• swollen belly
• Blood disorders, including anemia (low levels of red blood cells), neutropenia (low levels of white blood cells), and thrombocytopenia (low levels of platelets). Symptoms can include:
• fatigue (lack of energy)
• rapid heart rate
• shortness of breath
• frequent infections
• fevers
• bruising easily
• bleeding gums
• blood in urine or stool
• Congestive heart failure and other heart problems, such as left-sided heart failure. Symptoms can include:
• unexpected weight gain
• edema (swelling of your feet, ankles, and legs)
• abnormal heart rate or rhythm (heartbeat that’s too fast, too slow, or irregular)
• chest pain
• shortness of breath
• Liver damage or liver failure. Symptoms can include:
• nausea
• diarrhea
• loss of appetite
• itchy skin
• jaundice (yellowish color of your skin and the whites of your eyes)
• edema (swelling of your legs, ankles, and feet)
• ascites (fluid buildup in your belly)
• frequent bruising
• frequent bleeding
• Severe hemorrhage (bleeding that doesn’t stop), most often in your intestines. Symptoms can include:
• blood in stool
• black or tarry stool
• fatigue (lack of energy)
• coughing up blood
• coughing up black sludge
• nausea
• stomach cramps
• Gastrointestinal problems, including perforations (tears) in your stomach or intestines. Symptoms can include:
• nausea
• vomiting
• severe pain in your stomach
• fever
• shortness of breath
• fast heartbeat
• Severe skin problems. Symptoms can include:
• erythema multiforme (red patches or blisters, often on the soles of your feet or the palms of your hands)
• Stevens-Johnson syndrome (fever; painful sores on your mouth, throat, eyes, genitals, or entire body)
• fever
• body aches
• Hypothyroidism (low thyroid levels) in people who have had their thyroid removed and are taking thyroid replacement medication. Symptoms can include:
• Slowed growth in children. Symptoms can include:
• not growing at a normal rate
• smaller size than other children their age
• Tumor lysis syndrome (when cancer cells release harmful chemicals into your blood). Symptoms can include:
• fatigue (lack of energy)
• nausea
• vomiting
• diarrhea
• muscle cramps
• abnormal heart rhythm (heartbeat that’s too fast, too slow, or irregular)
• seizures
• Kidney damage. Symptoms can include:
• urinating less often than usual
• edema (swelling of your legs, ankles, and feet)
• fatigue (lack of energy)
• nausea
• confusion
• high blood pressure
• Side effects that can lead to motor vehicle accidents. Symptoms can include:
• dizziness
• sleepiness
• blurred vision

Side effect details

You may wonder how often certain side effects occur with this drug, or whether certain side effects pertain to it. Here’s some detail on several of the side effects this drug may or may not cause.

Allergic reaction

As with most drugs, some people can have an allergic reaction after taking Gleevec. Symptoms of a mild allergic reaction can include:

• skin rash
• itchiness
• flushing (warmth and redness in your skin)

A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:

• angioedema (swelling under your skin, typically in your eyelids, lips, hands, or feet)
• swelling of your tongue, mouth, or throat
• trouble breathing

Call your doctor right away if you have a severe allergic reaction to Gleevec. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency.

Long-term side effects

Some of the side effects seen in clinical studies can happen with long-term use of Gleevec. These include heart problems, such as congestive heart failure and left-sided heart failure.

In a clinical study, more than 500 people who took Gleevec for chronic myeloid leukemia (CML) were followed for up to 11 years. People in this long-term study had many of the same common side effects that were reported in shorter studies. However, these side effects seemed to improve over time.

Serious side effects seen with long-term use included:

• severe blood disorders (low levels of red blood cells, white blood cells, or platelets) in six people
• heart problems, including congestive heart failure, in seven people
• six cases of new cancer, including multiple myeloma in one person and colon cancer in another person

Side effects were most common during the first year of treatment with Gleevec. But the longer that people took Gleevec, the less often they had many of these side effects. For example, in the first year of the study, three people had serious blood disorders, but after the fifth year, only one person did.

In a five-year study of people with gastrointestinal stromal tumors (GIST), 16% of people stopped taking Gleevec because of side effects. The side effects were similar to those described in the CML study above. Forty percent of people in the study were prescribed lower doses of the drug to ease their side effects.

If you’re concerned about possible long-term side effects of Gleevec, talk with your doctor. They can suggest ways to reduce your risks for certain side effects.

Eye-related side effects

In clinical studies of Gleevec, some people had eye-related side effects such as swelling and blurry vision.

Eyelid swelling and swelling around the eyes were some of the most common side effects. Up to 74.2% of people who took Gleevec had periorbital edema (swelling of the eye area).

If you have this side effect, your doctor may prescribe a diuretic (often called a water pill). Diuretics help your body get rid of extra water and salt when you urinate. This eases fluid buildup. Your doctor may also lower your dose of Gleevec, if needed.

In addition, clinical studies reported that up to 11.1% of people who took Gleevec had blurry vision. If you have blurry vision, don’t drive or use heavy machinery. And be sure to tell your doctor that you can’t see clearly.

Other less common eye-related side effects included:

• dry eye
• watery eyes
• eye irritation
• conjunctivitis (often called pink eye)
• broken blood vessels in the eye
• swelling of the retina (a layer of tissue in the back of your eye)

If you’re taking Gleevec and have any eye-related side effects, talk with your doctor. They can suggest ways to ease your symptoms.

Hair loss

Hair loss (alopecia) is a possible side effect of taking Gleevec.

One study tested how Gleevec works in people with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML). Seven percent of these people had hair loss after they took the drug.

In another study, people took Gleevec to treat gastrointestinal stromal tumors (GIST). Between 11.9% and 14.8% of these people had hair loss. This side effect was seen more often in people who took higher doses of Gleevec.

Hair loss due to cancer treatment is usually temporary. If you’re concerned about this side effect, talk with your doctor. They can suggest tips to help you reduce hair loss during your treatment.

Rash and other skin side effects

Gleevec can cause mild and more serious side effects to your skin.

More common skin reactions

Rashes and other mild skin reactions are very common in people who take Gleevec.

In clinical studies, people took Gleevec to treat Ph+ chronic myeloid leukemia (CML). Up to 40.1% of these people had rashes or other skin reactions after taking the drug.

In other clinical studies, people took Gleevec for gastrointestinal stromal tumors (GIST). After taking the drug, up to 49.8% of these people had rashes or other skin reactions. These included:

• peeling of the skin
• dry skin
• skin discoloration (a bluish tint to the skin)
• infections of hair follicles (sacs under your skin that hold the roots of your hair)
• erythema (reddening of skin)
• purpura (purple-colored spots on skin)

These side effects were more common in people who took higher doses of Gleevec.

If you’re concerned about rashes or other mild skin reactions due to Gleevec, talk with your doctor. They can suggest ways to help ease your symptoms.

Serious skin reactions

In clinical studies, serious skin reactions were very rare in people who took Gleevec. Up to 1% of people who took this drug had a serious skin reaction. Examples of serious drug-related skin effects include:

• Stevens-Johnson syndrome (fever; painful sores on your mouth, throat, eyes, genitals, or entire body)
• exfoliative dermatitis (skin peeling over large parts of your body)
• vesicular rash (small blisters and a rash)

Rashes and blisters can be very painful. And if they’re not treated, they can trap bacteria and lead to serious infections. So if you’re taking Gleevec and have a rash or blisters with a fever or you don’t feel well, tell your doctor right away. Also mention any other skin reactions you have.

Side effects affecting driving

In clinical studies, some people who took Gleevec had side effects that could affect their ability to drive. These included:

• dizziness: in up to 19.4% of people
• blurry vision: in up to 11.1% of people
• fatigue: in 74.9% of people

These side effects may affect your ability to drive or use heavy machinery. There have been reports of motor vehicle accidents by people who took Gleevec. So you should use caution when driving or using machinery while taking Gleevec.

Slowed wound healing (not a side effect)

Slowed wound healing wasn’t reported in clinical studies of Gleevec.

Some types of cancer treatment, such as radiation and chemotherapy, may weaken your immune system. This can make wounds heal more slowly.

If you’re concerned about slowed wound healing, ask your doctor whether you have a higher risk for this problem based on your medical condition.

Liver cancer (may not be a side effect)

Liver cancer wasn’t reported as a side effect in clinical studies of Gleevec. However, liver damage has occurred in both short- and long-term use of Gleevec. Some cases of liver damage have led to liver failure and liver transplant.

Liver damage is often found when doctors monitor enzymes (special proteins) that are made in the liver. Enzyme levels that are higher than normal can be a sign of liver damage.

Some physical symptoms of liver damage include:

• nausea
• diarrhea
• loss of appetite
• itchy skin
• jaundice (yellowish color of your skin and the whites of the eyes)
• edema (swelling of your legs, ankles, and feet)
• ascites (fluid buildup in your belly)
• frequent bruising
• frequent bleeding

During clinical studies, up to 5% of people with chronic myeloid leukemia (CML) had severely high liver enzyme levels during Gleevec treatment. Up to 6.8% of people with gastrointestinal stromal tumors (GIST) had severely high liver enzyme levels during treatment. And up to 0.1% of people who took Gleevec had liver failure.

While you take Gleevec, your doctor will monitor how your liver is working. If you have signs of liver damage while taking Gleevec, your doctor may reduce your dose. This may prevent damage that could lead to liver failure.

Side effects in children

Children in clinical studies who took Gleevec had side effects that were very similar to those in adults. But researchers found these exceptions:

• fewer children had muscle or bone pain than adults had
• edema (swelling of the legs, ankles, feet, and area around the eyes) wasn’t reported in children

The most commonly reported side effects reported in children were nausea and vomiting. The most common serious side effects were low levels of white blood cells and platelets.

If your child has these side effects, talk with your child’s doctor about ways to manage them.

Gleevec for CML

The Food and Drug Administration (FDA) has approved Gleevec for certain people with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML). The Philadelphia chromosome is chromosome number 22 with a defect. People with Ph+ CML have a specific change in their DNA that causes too many white blood cells to form.

CML is divided into three phases:

• Chronic phase. This is the first phase of CML. Most people are diagnosed with CML during the chronic phase. Symptoms are usually mild, if there are any at all.
• Accelerated phase. In this second phase, the number of cancer cells in your blood increases. You may have more symptoms, such as fever and weight loss.
• Blast crisis phase. In this most advanced phase, cancer cells in your blood have spread to other organs and tissues. Your symptoms may be more severe.

Gleevec is approved to treat newly diagnosed Ph+ CML in the chronic phase in people of all ages.

It’s also approved to treat Ph+ CML in the chronic, accelerated, or blast crisis phase for people who have had unsuccessful treatment with interferon-alpha therapy. Interferon-alpha is a drug that was used more often in the past to treat CML. It’s been replaced by drugs such as Gleevec that have been shown to be more effective.

Effectiveness

In a seven-year clinical study, the survival rate for adults who took Gleevec for newly diagnosed Ph+ CML was 86.4%. This means that 86.4% of the adults survived for seven years after they started taking Gleevec. This was compared to 83.3% of people who took standard chemotherapy drugs.

In a clinical study, people who had previously tried interferon-alpha for CML took Gleevec. Some of these people had a complete response to Gleevec treatment. This means that no cancerous cells were found in their blood, and they had no symptoms of cancer. Here’s how many people with CML had a complete response to taking Gleevec:

• 95% of people in the chronic phase
• 38% of people in the accelerated phase
• 7% of people in the blast crisis phase

The clinical study also included children with Ph+ CML in the chronic phase. In the group that took Gleevec, 78% of children had a complete response to the drug.

Other uses for Gleevec

In addition chronic myeloid leukemia (see above), the Food and Drug Administration (FDA) has approved Gleevec to treat several other conditions.

Gleevec for acute lymphocytic leukemia (ALL)

Gleevec is FDA-approved to treat:

• Philadelphia chromosome-positive (Ph+) acute lymphocytic leukemia (ALL) that’s relapsed* or refractory* in adults
• newly diagnosed Ph+ ALL in children when used with chemotherapy

* Relapsed cancer has returned after remission, which is a decrease in cancer signs and symptoms. Refractory cancer hasn’t responded to previous cancer treatments.

In a clinical study, 19% of adults with relapsed or refractory ALL who took Gleevec had a complete response in their blood to treatment. This means that they had no symptoms of cancer.

A clinical study also looked at children with ALL who took Gleevec and had chemotherapy. For 70% of the children, their cancer didn’t get worse for four years.

Gleevec for other types of blood cancers

Gleevec is FDA-approved to treat other types of blood cancers, including:

• Myelodysplastic/myeloproliferative diseases (bone marrow cancers) in adults with platelet-derived growth factor receptor (PDGFR) gene rearrangements. In a small clinical study, 45% of people treated with Gleevec had a complete response in their blood to treatment. This means that no cancer cells were found in their blood, and they had no symptoms of cancer.
• Hypereosinophilic syndrome and/or chronic eosinophilic leukemia in adults, including people with FIP1L1-PDGFRα fusion kinase. In small clinical studies, 100% of people with the PDGFR gene mutation who took Gleevec had a complete response in their blood to treatment. Between 21% and 58% of people without the gene mutation or with an unknown mutation status who took Gleevec had a complete response in their blood.
• Aggressive systemic mastocytosis in adults without the D816v c-Kit mutation. In a small clinical study, 100% of people with the FIP1L1-PDGFRα fusion kinase mutation who were treated with Gleevec had a complete response to treatment.

Gleevec for skin cancer

Gleevec is FDA-approved to treat dermatofibrosarcoma protuberans, a rare type of skin cancer, in adults. It’s approved for people whose cancer:

• can’t be operated on
• has come back after treatment
• is metastatic (has spread to other parts of the body)

A small number of people have been treated with Gleevec for this condition in clinical studies. Of those people who took Gleevec, 39% had a complete response to treatment. This means that a skin biopsy (removing and testing a small sample of skin) showed no signs of cancer.

Gleevec for gastrointestinal cancer

Gleevec is FDA-approved to treat Kit-positive gastrointestinal stromal tumors (GIST) in adults that can’t be operated on or are metastatic (have spread to other parts of the body). Gleevec is also approved to treat GIST in adults who have had surgery to remove tumors. This form of treatment (adjuvant treatment) is used to prevent the cancer from returning after surgery.

In clinical studies, people with GIST that couldn’t be surgically removed took 400 or 800 mg of Gleevec. They survived for about four years.

Other people with GIST did have surgery. Between 14 and 70 days later, they started taking Gleevec in the study. They had about a 60% lower risk of either dying or having the cancer return over a period of 12 months. This was compared to people who took a placebo (treatment with no active medication).

Off-label uses for Gleevec

In addition to the uses listed above, Gleevec may be used off-label for other uses. Off-label drug use is when a drug that’s approved for one use is prescribed for a different one that’s not approved.

Gleevec may be used off-label for other cancers, including:

However, there isn’t much research on how Gleevec works in humans with these conditions. More studies are needed to determine whether Gleevec helps treat each condition.

Gleevec for children

Gleevec is FDA-approved as a treatment for children with the following conditions:

• newly diagnosed Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase (the first phase of the disease)
• newly diagnosed Ph+ acute lymphocytic leukemia (ALL) when used with chemotherapy

Gleevec is approved for use in children of all ages. However, there haven’t been studies on how safe or effective Gleevec is in children younger than age 1 year.

Gleevec cost

As with all medications, the cost of Gleevec can vary. To find current prices for Gleevec in your area, check out GoodRx.com:

The cost you find on GoodRx.com is what you may pay without insurance. The actual price you’ll pay depends on your insurance coverage and the pharmacy you use.

Financial and insurance assistance

If you need financial support to pay for Gleevec , or if you need help understanding your insurance coverage, help is available.

Novartis Pharmaceutical Corporation, the manufacturer of Gleevec, offers a program called Novartis Oncology Universal Co-pay Program. For more information and to find out if you’re eligible for support, call 877-577-7756 or visit the program website.

Gleevec dosage

The Gleevec dosage your doctor prescribes will depend on several factors. These include:

• the type and severity of the condition you’re using Gleevec to treat
• age
• weight (for children)
• presence of gene mutations
• other medical conditions you may have
• other medication you may take
• side effects you may have

The dose you will receive depends on your cancer. For some cancers, your doctor may start you on a low dosage. Then they’ll adjust it over time to reach the dosage that’s right for you.

The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to suit your needs.

Drug forms and strengths

Gleevec comes as a tablet that you take by mouth (you swallow it). It’s available in 100-mg tablets and 400-mg tablets.

The 100-mg and 400-mg tablets come in bottles. The 400-mg tablets also come in blister packs that are hard for children to open.

Gleevec dosages

The following doses are typical starting dosages for each condition:

• adults with Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase (the first phase of the disease): 400 mg/day
• adults with Ph+ CML in the accelerated or blast crisis phase (the second and third phases of the disease): 600 mg/day
• adults with Ph+ acute lymphocytic leukemia (ALL): 600 mg/day
• adults with myelodysplastic/myeloproliferative disease: 400 mg/day
• adults with aggressive systemic mastocytosis: 100 mg or 400 mg/day
• adults with hypereosinophilic syndrome and/or chronic eosinophilic leukemia: 100 mg/day or 400 mg/day
• adults with dermatofibrosarcoma protuberans: 800 mg/day
• adults with gastrointestinal stromal tumors (GIST): 400 mg/day

Your doctor may prescribe a different dosage for you. They’ll base it on how well your body responds to the drug, how severe your side effects are, and other factors. If you have questions about the right dosage of Gleevec for you, talk with your doctor.

Pediatric dosage

Dosages for children are the following:

• children with Ph+ CML in the chronic phase (the first phase of the disease): 340 mg/m2/day
• children with Ph+ ALL: 340 mg/m2/day to be taken with chemotherapy

Your child’s doctor will base the dosage on your child’s height and weight. (So 340 mg/m2 means 340 mg per square meter of body surface area.) For example, if your child is 4 feet tall and weighs 49 lbs., their body surface area is about 0.87 m2. So the dosage for Ph+ CML would be 300 mg.

What if I miss a dose?

If you miss a dose of Gleevec, take one as soon as you remember. If it’s almost time for your next dose, wait and take the next dose as scheduled. Don’t take two doses to make up for the missed dose. This can increase your risk for serious side effects.

Will I need to use this drug long term?

Gleevec is meant to be used as a long-term treatment. If you and your doctor determine that Gleevec is safe and effective for you, you’ll likely take it long term.

Alternatives to Gleevec

Other drugs are available that can treat your condition. Some may be better suited for you than others. If you’re interested in finding an alternative to Gleevec, talk with your doctor to learn more about other medications that may work well for you.

Note: Some of the drugs listed here are used off-label to treat these specific conditions.

Alternatives for CML

Examples of other drugs that may be used to treat Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) are:

• dasatinib (Sprycel)
• nilotinib (Tasigna)
• bosutinib (Bosulif)
• ponatinib (Iclusig)
• omacetaxine (Synribo)
• daunorubicin (Cerubidine)
• cytarabine
• interferon-alpha (Intron A)

Alternatives for GIST

Examples of other drugs that may be used to treat gastrointestinal stromal tumors (GIST) are:

• sunitinib (Sutent)
• regorafenib (Stivarga)
• sorafenib (Nexavar)
• nilotinib (Tasigna)
• dasatinib (Sprycel)
• pazopanib (Votrient)

Alternatives for other conditions Gleevec may treat are also available. Talk with your doctor about which medications can be used for your condition.

Gleevec vs. Tasigna

You may wonder how Gleevec compares to other medications that are prescribed for similar uses. Here we look at how Gleevec and Tasigna are alike and different.

Uses

The Food and Drug Administration (FDA) has approved both Gleevec and Tasigna to treat certain types of blood cancers.

Both drugs are FDA-approved to treat newly diagnosed Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase in adults and children.

Chronic myeloid leukemia (CML) is divided into three phases:

• Chronic phase. This is the first phase of CML. Most people are diagnosed with CML during the chronic phase. Symptoms are usually mild, if there are any at all.
• Accelerated phase. In this second phase, the number of cancer cells in your blood increases. You may have more symptoms, such as fever and weight loss.
• Blast crisis phase. In this most advanced phase, cancer cells in your blood have spread to other organs and tissues. Your symptoms may be more severe.

Gleevec is approved to treat Philadelphia-positive (Ph+) CML in adults who are in the chronic, accelerated, or blast crisis phase if interferon-alpha therapy hasn’t worked.

Interferon-alpha is a drug that was commonly used to treat CML in the past. It’s a man-made drug that acts like certain immune system proteins and prevents the growth of cancer cells.

Tasigna is approved in to treat Ph+ CML in the chronic or accelerated phases in adults if other treatments haven’t worked, including treatment with Gleevec. Tasigna isn’t approved for the blast crisis phase.

Tasigna is also approved to treat Ph+ CML in children ages 1 year and older if other treatments haven’t worked. Gleevec is approved to treat newly diagnosed Ph+ CML in children.

Gleevec is also approved to treat other types of cancers. See the “Other uses for Gleevec” section to learn more.

Drug forms and administration

Gleevec contains the drug imatinib. Tasigna contains the drug nilotinib.

Gleevec comes as a tablet. Tasigna comes as a capsule. Both drugs are taken by mouth.

Gleevec is taken once or twice a day, depending on your dose. Tasigna is taken twice a day.

Gleevec comes as 100-mg and 400-mg tablets. Tasigna comes as 50-mg, 150-mg, and 200-mg capsules.

Side effects and risks

Gleevec and Tasigna contain similar drugs. Therefore, both medications can cause very similar side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Gleevec, with Tasigna, or with both drugs (when taken individually).

• Can occur with Gleevec:
• edema (swelling of your legs, ankles, and feet, and around your eyes)
• muscle cramps
• muscle pain
• bone pain
• stomach pain
• Can occur with Tasigna:
• headache
• itchy skin
• cough
• constipation
• joint pain
• nasopharyngitis (common cold)
• fever
• night sweats
• Can occur with both Gleevec and Tasigna:
• nausea
• vomiting
• diarrhea
• rash
• fatigue (lack of energy)

Serious side effects

These lists contain examples of serious side effects that can occur with Gleevec, with Tasigna, or with both drugs (when taken individually).

• Can occur with Gleevec:
• congestive heart failure or heart problems such as left-sided heart failure
• gastrointestinal perforations (holes in your stomach or intestines)
• severe skin reactions, including Stevens-Johnson syndrome (fever; painful sores on your mouth, throat, eyes, genitals, or entire body)
• kidney damage
• hypothyroidism (low thyroid levels) in people who have had their thyroid removed
• Can occur with Tasigna:
• long QT interval (abnormal electrical activity in your heart), which is rare but could lead to sudden death
• blocked blood vessels in the heart
• pancreatitis
• electrolyte imbalances (high or low levels of certain minerals)
• Can occur with both Gleevec and Tasigna:
• blood disorders, including anemia (low levels of red blood cells), neutropenia (low levels of white blood cells), and thrombocytopenia (low levels of platelets)
• liver damage
• tumor lysis syndrome (cancer cells release harmful chemicals into your blood)
• hemorrhage (bleeding that doesn’t stop)
• severe fluid retention (too much fluid or water)
• slowed growth in children

Effectiveness

Gleevec and Tasigna have different FDA-approved uses. But they both treat Ph+ CML in the chronic and accelerated phases if certain other treatments haven’t worked. CML has three phases: chronic (phase 1), accelerated (phase 2), and blast crisis (phase 3).

The use of Gleevec and Tasigna in treating newly diagnosed Ph+ CML in adults has been directly compared in a clinical study. Researchers compared people who took either 400 mg of Gleevec once a day or 300 mg of Tasigna twice a day.

After 12 months of treatment, 65% of people who took Gleevec had no Ph+ cells in their bone marrow (where cancerous CML cells grow). Of people who took Tasigna, 80% had no Ph+ cells in their bone marrow.

After five years of treatment, 60% of people who took Gleevec had a significantly reduced number of cancerous genes in their blood. This was compared to 77% of people who took Tasigna.

Also after five years of treatment, 91.7% of people who took Gleevec were still alive. That’s compared to 93.7% of people who took Tasigna.

The results of this study suggest that Tasigna may be more effective than Gleevec at treating newly diagnosed Ph+ CML in the chronic phase.

Costs

Gleevec and Tasigna are both brand-name drugs. Tasigna doesn’t have a generic form, but Gleevec has a generic form called imatinib. Brand-name medications usually cost more than generics.

According to estimates on GoodRx.com, brand-name Gleevec may cost less than Tasigna. The generic form of Gleevec (imatinib) also costs less than Tasigna. The actual price you’ll pay for either drug depends on your dose, insurance plan, your location, and the pharmacy you use.

Gleevec vs. Sprycel

You may wonder how Gleevec compares to other medications that are prescribed for similar uses. Here we look at how Gleevec and Sprycel are alike and different.

Uses

The Food and Drug Administration (FDA) has approved both Gleevec and Sprycel to treat certain types of blood cancers.

Both drugs are both FDA-approved to treat newly diagnosed Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase in adults and children.

CML is divided into three phases:

• Chronic phase. This is the first phase of CML. Most people are diagnosed with CML during the chronic phase. Symptoms are usually mild, if there are any at all.
• Accelerated phase. In this second phase, the number of cancer cells in your blood increases. You may have more symptoms, such as fever and weight loss.
• Blast crisis phase. In this most advanced phase, cancer cells in your blood have spread to other organs and tissues. Your symptoms may be more severe.

Gleevec and Sprycel are used to treat Ph+ CML in adults in the chronic phase.

Gleevec is also used to treat Ph+ CML in adults in the chronic, accelerated, or blast-crisis phases if interferon-alpha therapy didn’t work. Interferon-alpha is a drug that was commonly used to treat CML in the past. It’s a man-made drug that acts like certain immune system proteins and prevents the growth of cancer cells.

Sprycel is also used to treat Ph+ CML in adults in the chronic, accelerated, or blast-crisis phases if Gleevec didn’t work.

Both Gleevec and Sprycel are approved to treat Ph+ CML in the chronic phase in children. They are both also approved to treat Ph+ acute lymphocytic leukemia (ALL) in children along with chemotherapy.

Gleevec is also approved to treat other types of cancers. See the “Other uses for Gleevec” section to learn more.

Drug forms and administration

Gleevec contains the drug imatinib. Sprycel contains the drug dasatinib.

Gleevec and Sprycel both come as tablets that you take by mouth (you swallow them).

Gleevec tablets come in two strengths: 100 mg and 400 mg. It’s taken once or twice a day, depending on your dose.

Sprycel tablets come in the following strengths: 20 mg, 50 mg, 70 mg, 80 mg, 100 mg, and 140 mg. Sprycel is taken once a day.

Side effects and risks

Gleevec and Sprycel are similar but contain different drugs. Therefore, both medications can cause very similar side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Gleevec, with Sprycel, or with both drugs (when taken individually).

• Can occur with Gleevec:
• vomiting
• muscle cramps
• belly pain
• eye-area edema (swelling around eyes)
• Can occur with Sprycel:
• trouble breathing
• headache
• bleeding
• weakened immune system (your body can’t fight infections as well)
• Can occur with both Gleevec and Sprycel:
• edema (swelling of your legs, ankles, and feet)
• nausea
• muscle pain
• bone pain
• diarrhea
• rash
• fatigue (lack of energy)

Serious side effects

These lists contain examples of serious side effects that can occur with Gleevec, with Sprycel, or with both drugs (when taken individually).

• Can occur with Gleevec:
• heart problems, such as congestive heart failure
• liver damage
• gastrointestinal perforations (holes in your stomach or intestines)
• kidney damage
• hypothyroidism (low thyroid levels) in people who have had their thyroid removed
• Can occur with Sprycel:
• pulmonary arterial hypertension (high blood pressure in blood vessels in your lungs)
• long QT interval (a type of abnormal electrical activity in your heart)
• ischemic heart attack (lack of oxygen to heart muscles)
• Can occur with both Gleevec and Sprycel:
• severe fluid retention (too much fluid or water) around your lungs, heart, and belly
• severe blood disorders (low levels of red blood cells, platelets, or white blood cells)
• severe hemorrhage (bleeding that doesn’t stop)
• severe skin reactions, including Stevens-Johnson syndrome (fever; painful sores on your mouth, throat, eyes, genitals, or entire body)
• tumor lysis syndrome (cancer cells release harmful chemicals into your blood)
• abnormal heart rate or rhythm (heartbeat that’s too fast, too slow, or irregular)
• stunted growth in children

Effectiveness

Gleevec and Sprycel have different FDA-approved uses. But they both treat newly diagnosed Ph+ CML in the chronic phase (the first phase of CML) in adults and children. Gleevec and Sprycel also both treat Ph+ ALL in children when used in combination with chemotherapy.

In addition, both Gleevec and Sprycel treat Ph+ CML in the advanced and blast phases in adults, or Ph+ ALL, if other drugs didn’t work for them.

The use of Gleevec and Sprycel in treating newly diagnosed Ph+ CML in adults has been directly compared in a clinical study. Researchers compared people who took either 400 mg of Gleevec a day or 100 mg of Sprycel a day.

Within 12 months, 66.2% of people who took Gleevec had no Ph+ cells in their bone marrow (where cancerous CML cells develop). In the group that took Sprycel, 76.8% of the people had no Ph+ cells in their bone marrow.

After five years of treatment, an estimated 89.6% of people who took Gleevec were still alive. That’s compared to an estimated 90.9% of people who took Sprycel.

The results of this study suggest that Sprycel may be slightly more effective than Gleevec at treating newly diagnosed Ph+ CML in the chronic phase.

Costs

Gleevec and Sprycel are both brand-name drugs. Sprycel doesn’t have a generic form, but Gleevec has a generic form called imatinib. Brand-name medications usually cost more than generics.

According to estimates on GoodRx.com, brand-name Gleevec may cost less than Sprycel. The generic form of Gleevec (imatinib) may also cost less than Sprycel. The actual price you’ll pay for either drug depends on your dose, your insurance plan, your location, and the pharmacy you use.

Gleevec and alcohol

It’s not known whether Gleevec and alcohol interact with each other.

However, your liver metabolizes (breaks down) both Gleevec and alcohol. So drinking too much alcohol while you’re taking Gleevec may prevent your liver from breaking down the drug. This could raise levels of Gleevec in your body and increase your risk for serious side effects, including liver damage.

Both Gleevec and alcohol can cause side effects such as:

• nausea
• diarrhea
• headache
• fatigue (lack of energy)

Drinking alcohol during your Gleevec treatment could increase your risk of having these side effects.

If you drink alcohol, talk with your doctor about how much is safe for you during your Gleevec treatment.

Gleevec interactions

Gleevec can interact with several other medications. It can also interact with certain supplements as well as certain foods.

Different interactions can cause different effects. For instance, some can interfere with how well a drug works, while others can cause increase side effects.

Gleevec and other medications

Below is a list of medications that can interact with Gleevec. This list doesn’t contain all drugs that may interact with Gleevec.

Before taking Gleevec, talk with your doctor and pharmacist. Tell them about all prescription, over-the-counter, and other drugs you take. Also tell them about any vitamins, herbs, and supplements you use. Sharing this information can help you avoid potential interactions.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Gleevec and Tylenol

Taking Gleevec with Tylenol (acetaminophen) can increase your risk for serious side effects, such as liver damage.

Enzymes (special proteins) in your liver break down both Gleevec and Tylenol. Together, the two drugs can overwhelm the enzymes and damage cells in your liver.

Ask your doctor whether it’s safe for you to take Tylenol during your Gleevec treatment.

Gleevec and certain seizure medications

Taking Gleevec with certain seizure medications can decrease Gleevec levels in your body. This can make Gleevec less effective (work less well).

Examples of seizure medications that can decrease Gleevec levels include:

• phenytoin (Dilantin, Phenytek)
• carbamazepine (Carbatrol, Tegretol)
• phenobarbital

If you’re taking Gleevec and certain seizure medications, your doctor may prescribe a different seizure drug or adjust the dosage of Gleevec.

Gleevec and certain antibiotics

Taking Gleevec with certain antibiotics (drugs that treat bacterial infections) can increase Gleevec levels in your body. Antibiotics prevent Gleevec from breaking down in your body. This increases your risk for serious side effects.

An example of an antibiotic that can increase Gleevec levels is clarithromycin (Biaxin XL).

If you’re taking Gleevec and need an antibiotic, your doctor may monitor you for side effects. They may also reduce your Gleevec dosage for a time.

Gleevec and certain antifungals

Taking Gleevec with certain antifungals (drugs that treat fungal infections) can prevent the breakdown of Gleevec in your body. This can raise Gleevec levels in your blood and increase your risk for serious side effects.

Examples of antifungals that can increase Gleevec levels are:

• itraconazole (Onmel, Sporanox, Tolsura)
• ketoconazole (Extina, Ketozole, Xolegel)
• voriconazole (Vfend)

If you’re taking Gleevec and need antifungal treatment, your doctor will monitor you for side effects. They may also reduce your Gleevec dosage for a time.

Gleevec and opioids

Taking Gleevec with certain pain medications can increase levels of the pain reliever in your body. This could make you more likely to have serious side effects such as sedation (feeling drowsy and less alert) and respiratory depression (slow breathing).

Examples of opioid pain medications that can increase Gleevec levels include:

• oxycodone (Oxycontin, Roxicodone, Xtampza ER)
• tramadol (ConZip, Ultram)
• methadone (Dolophine, Methadose)

Talk with your doctor about whether it’s safe to take pain medication during your Gleevec treatment. They may suggest other ways to ease your pain.

Gleevec and certain HIV medications

Taking Gleevec with certain HIV medications can increase your risk for serious side effects. Certain HIV drugs can prevent Gleevec from breaking down, leading to higher levels of Gleevec in your body.

Examples of HIV medications that can increase Gleevec levels include:

• atazanavir (Reyataz)
• nevirapine (Viramune)
• saquinavir (Invirase)

Another HIV medication, efavirenz (Sustiva), can decrease levels of Gleevec in your body. This can cause Gleevec to be less effective.

Many HIV medications come as combination tablets, which means they include more than one drug. So be sure to talk with your doctor about all the HIV medications you take.

If you need to take Gleevec with certain HIV medications, your doctor may change your Gleevec dosage.

Gleevec and certain blood pressure medications

Taking Gleevec with certain blood pressure medications can increase or decrease the levels of either drug in your body. This could make you more likely to have side effects or reduce how well the medications work.

Example of these drugs include verapamil (Calan, Tarka).

If you need to take Gleevec with any of these medications, your doctor will monitor you more closely for side effects. They may also adjust the dosage of either medication or recommend a different drug.

Gleevec and warfarin

Taking Gleevec with warfarin (Coumadin, Jantoven) can increase your risk for bleeding. Gleevec prevents warfarin from breaking down in your body. This increases levels of warfarin and can lead to bleeding that’s hard to control.

If you need an anticoagulant (blood thinner) while taking Gleevec, your doctor will likely prescribe a drug other than warfarin.

Gleevec and St. John’s wort

Taking Gleevec with St. John’s wort can decrease levels of Gleevec in your body. This can make Gleevec less effective (not work as well).

Ask your doctor whether St. John’s wort is safe for you to take during your Gleevec treatment. They may recommend an alternative to St. John’s Wort or increase your Gleevec dose.

Gleevec and grapefruit

Eating grapefruit or drinking grapefruit juice during your Gleevec treatment can increase your risk for serious side effects. Grapefruit contains chemicals that prevent Gleevec from breaking down in your body. This causes increased levels of Gleevec, which can lead to more severe side effects.

Be sure to avoid eating grapefruit and drinking grapefruit juice during your Gleevec treatment.

How to take Gleevec

Be sure to take Gleevec according to your doctor or healthcare provider’s instructions.

When to take

For Gleevec doses of 600 mg or less, the drug should be taken once a day. You can take it at any time.

If your doctor prescribes 800 mg of Gleevec a day, you’ll take it in two doses: 400 mg in the morning and 400 mg in the evening.

Your doctor will give you instructions on when you should take your dose.

Taking Gleevec with food

Take Gleevec with a meal and a large glass of water. This can help prevent an upset stomach.

Can Gleevec be crushed, split, or chewed?

You shouldn’t crush, split, or chew Gleevec tablets. Crushed and split tablets can be harmful to any skin or other body parts that come in contact with them.

If you have trouble swallowing Gleevec tablets, place the tablet in a large glass of water or apple juice. Stir the water with a spoon to help the tablet dissolve. Then drink the mixture right away.

How Gleevec works

Gleevec contains the drug imatinib, which belongs to a class of drugs called tyrosine kinase inhibitors (TKIs). Medications in the TKI drug class are targeted therapies. They affect very specific proteins in cancer cells.

Gleevec is approved to treat several different conditions. Here we’ll explore how Gleevec works to treat two of them.

For Ph+ CML

In Philadelphia-positive (Ph+) chronic myeloid leukemia (CML), the cells that create white blood cells have a mistake in their genetic makeup. This genetic mistake is found on a DNA strand called the Philadelphia chromosome.

The Philadelphia chromosome contains an abnormal gene (BCR-ABL1) that causes too many white blood cells to form. These white blood cells don’t mature and die like they’re supposed to. Immature white blood cells called “blasts” crowd out other types of blood cells that your blood needs to work correctly.

Gleevec works by attaching to a protein, called tyrosine kinase, in cells made by BCR-ABL1. When Gleevec binds to this protein, the drug prevents the cell from sending signals that tell the cell to grow. Without these growth signals, the cancerous blood cells die. This helps restore the number of blast cells to a healthier number.

For GIST

Gleevec also helps treat gastrointestinal stromal tumors (GIST). In many GIST tumor cells, there are a higher number of certain proteins, called Kit and platelet-derived growth factor (PDGF), than in normal cells. These proteins help cancer cells grow and divide.

Gleevec targets these proteins and prevents them from working. This slows the growth of cancer. It also causes cancer cells to die.

How long does it take to work?

It depends. The timing of when Gleevec starts to work is different for each person.

Clinical studies looked at people with CML who took Gleevec. In one month, the number of cancerous cells in the blood was reduced in about half of the people in the blast crisis stage (advanced stage of CML). In studies of people with GIST who took Gleevec, the tumors stopped growing or shrank in three months.

Your doctor will routinely monitor your blood to see if Gleevec is working for you.

Gleevec and pregnancy

You should avoid Gleevec if you’re pregnant. There have been reports of miscarriages and harm to the fetus in women who took Gleevec while pregnant. And in animal studies, pregnant females who were given Gleevec had an increased risk for birth defects.

If you’re pregnant, your doctor may advise you to wait until after you’ve given birth to start taking Gleevec. Or they will recommend a different drug.

If you’re taking Gleevec, it’s important to use effective birth control so you don’t become pregnant. After you take your last dose of Gleevec, keep using birth control for 14 days.

Gleevec and breastfeeding

Studies show that Gleevec passes into human breast milk. This can cause serious harm to a breastfeeding infant.

If you’re breastfeeding and considering taking Gleevec, your doctor may advise you to stop breastfeeding when you start treatment.

After you take your last dose of Gleevec, wait at least one month before you start breastfeeding.

Gleevec overdose

Taking too much Gleevec can increase your risk for serious side effects.

Overdose symptoms

Symptoms of an overdose can include:

• nausea
• vomiting
• diarrhea
• belly pain
• severe rash
• muscle spasms (twitches)
• headache
• lack of appetite
• muscle weakness
• fatigue (lack of energy)
• swelling
• blood disorders, such as low levels of platelets, red blood cells, or white blood cells
• fever

What to do in case of overdose

If you think you’ve taken too much of this drug, call your doctor. You can also call the American Association of Poison Control Centers at 800-222-1222 or use their online tool. But if your symptoms are severe, call 911 or go to the nearest emergency room right away.

Common questions about Gleevec

Here are answers to some frequently asked questions about Gleevec.

Is Gleevec a type of chemotherapy?

Gleevec isn’t technically a form of chemotherapy. Gleevec is a targeted therapy that affects specific molecules in cancer cells.

By singling out specific molecules, targeted therapies like Gleevec help slow the growth and spread of cancer cells. Your doctor will typically prescribe a targeted therapy for you based on the type of cancer you have.

Chemotherapy drugs are different from targeted therapies. Chemotherapy medications act on all cells in the body that are rapidly growing, not just cancer cells. Chemotherapy drugs usually kill the growing cells and affect more cells in the body than targeted therapy does.

Is the generic form of Gleevec as effective as the brand-name drug?

The Food and Drug Administration (FDA) requires the makers of generic drugs to prove that their product has:

• the same active ingredient as the brand-name drug
• the same strength and dosage form as the brand-name drug
• the same route of administration (how you take the drug)

The generic drug is also required to work in the same way and just as well as the brand-name product.

According to the FDA, the generic form of Gleevec meets these requirements. This means that the FDA guarantees that the generic form is as effective as the brand-name drug.

Can I develop resistance to treatment with Gleevec?

Yes. It’s possible for you to develop resistance to Gleevec. Resistance means that the drug stops working over time. It’s thought that this is caused by a change in the genes of cancer cells.

If you develop resistance to Gleevec, your doctor may prescribe a higher dose. They’ll see if the cancer cells respond again to the medication. Your doctor may also prescribe a different drug that you don’t have resistance to.

Are there dietary restrictions I should follow while taking Gleevec?

There are no formal dietary restrictions that you should follow while taking Gleevec. However, you should avoid eating grapefruit and drinking grapefruit juice. Grapefruit contains a chemical that can prevent your body from metabolizing (breaking down) Gleevec. This can lead to higher levels of the drug in your blood. Levels of Gleevec that are higher than normal increase your risk for serious side effects.

In addition, your doctor may give you general advice on your diet to help ease certain side effects. For example, Gleevec causes nausea and vomiting in many people. To help prevent this, your doctor may recommend that you avoid foods that can make nausea worse. These include heavy, greasy, or fatty foods, and spicy or acidic foods. Examples are most red sauces, fried foods, and many fast food items.

Finally, if you’re taking Gleevec for a gastrointestinal cancer, such as gastrointestinal stromal tumors (GIST), your doctor may recommend specific dietary restrictions. The goal is to prevent problems in your stomach or intestines. Talk with your doctor about which foods are best for you.

Will I have withdrawal symptoms if I stop using Gleevec?

You might. Some people have had withdrawal symptoms after ending their Gleevec treatment. In one small clinical study, 30% of people had muscle or bone pain after stopping Gleevec. The pain was most often in their shoulders, hips, legs, and arms. This withdrawal symptom occurred within one to six weeks of stopping treatment.

About half of the people treated their pain with over-the-counter pain relievers. The other half needed prescription medication. In most people who had these withdrawal symptoms, muscle and bone pain went away within three months to a year or longer.

Will I need to use other drugs with Gleevec for treatment?

It depends on how advanced your cancer is. For advanced stages of cancer or cancers that have spread to the brain or spine, your doctor may add chemotherapy to your Gleevec treatment. In addition, children with Philadelphia-positive (Ph+) acute lymphocytic leukemia (ALL) may receive Gleevec along with chemotherapy.

For certain types of cancers, your doctor may also prescribe a steroid. And you may need to use medications to manage side effects, such as pain relievers for muscle pain.

Gleevec expiration, storage, and disposal

When you get Gleevec from the pharmacy, the pharmacist will add an expiration date to the label on the bottle. This date is typically one year from the date they dispensed the medication.

The expiration date helps guarantee the effectiveness of the medication during this time. The current stance of the Food and Drug Administration (FDA) is to avoid using expired medications. If you have unused medication that has gone past the expiration date, talk with your pharmacist. They can tell you whether you might still be able to use it.

Storage

How long a medication remains good can depend on many factors, including how and where you store the medication.

Store your Gleevec pills at room temperature in a tightly sealed container. Be sure to protect them from moisture.

Disposal

If you no longer need to take Gleevec and have leftover medication, it’s important to dispose of it safely.

This helps prevent others, including children and pets, from taking the drug by accident. It also helps keep the drug from harming the environment.

The FDA website provides several useful tips on medication disposal. You can also ask your pharmacist for information on how to dispose of your medication.

Professional information for Gleevec

The following information is provided for clinicians and other healthcare professionals.

Indications

Gleevec (imatinib) is FDA-approved to treat the following:

• adults and children with newly diagnosed Philadelphia-positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase
• adults with Ph+ CML in any phase, following failure of interferon-alpha therapy
• adults with relapsed or refractory Ph+ acute lymphocytic leukemia (ALL)
• children with newly diagnosed Ph+ ALL in combination with chemotherapy
• adults with myelodysplastic/myeloproliferative disease associated with platelet-derived growth factor receptor gene rearrangements
• adults with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown
• adults with hypereosinophilic syndrome and/or chronic eosinophilic leukemia with FIP1L1-PDGFRα fusion kinase, negative for the FIP1L1-PDGFRα fusion kinase, or unknown status
• adults with unresectable, recurrent, or metastatic dermatofibrosarcoma protuberans (DFSP)
• adults with unresectable or metastatic malignant Kit+ gastrointestinal stromal tumors (GIST)
• adjuvant therapy for adults with Kit+ GIST following complete gross resection

Mechanism of action

Gleevec inhibits the BCR-ABL tyrosine kinase, which is the abnormal tyrosine kinase found in Ph+ CML. Inhibition of BCR-ABL tyrosine kinase prevents cellular proliferation and induces apoptosis in BCR-ABL cell lines and in leukemic cell lines. Gleevec also inhibits the tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF) as well as c-Kit, which inhibits proliferation and induces apoptosis in GIST cells.

Pharmacokinetics and metabolism

Mean absolute bioavailability is 98% following oral administration. Approximately 95% of dose is bound to plasma proteins (mostly albumin and α1-acid glycoprotein).

Metabolism occurs primarily via CYP3A4 to an active metabolite, with minor metabolism occurring via CYP1A2, CYP2D6, CYP2C9, and CYP2C19. The main circulating active metabolite is formed primarily by CYP3A4. Approximately 68% is eliminated in the feces, with 13% in the urine. Elimination half-life of unchanged drug is 18 hours and elimination half-life of major active metabolite is 40 hours.

Contraindications

There are no absolute contraindications to Gleevec use.

Storage and handling

Gleevec tablets should be stored at room temperature (77°F/25°C) in a tightly-sealed container. Protect tablets from moisture.

Gleevec tablets are considered hazardous, according to Occupational Safety and Health Administration (OSHA) standards. Tablets should not be crushed. Avoid touching crushed tablets. If skin or mucus membranes come in contact with crushed tablets, wash the affected area according to OSHA guidance.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.