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imatinib

Pronunciation

Generic Name: imatinib (im MA ta nib)
Brand Name: Gleevec

What is imatinib?

Imatinib interferes with the growth of some cancer cells.

Imatinib is used to treat certain types of leukemia (blood cancer), bone marrow disorders, and skin cancer, or certain tumors of the stomach and digestive system.

Imatinib may also be used for purposes not listed in this medication guide.

What is the most important information I should know about imatinib?

Imatinib can lower blood cells that help your body fight infections and help your blood to clot. You may get an infection or bleed more easily. Call your doctor if you have unusual bruising or bleeding, or signs of infection (fever, chills, body aches).

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Imatinib may increase the risk of liver problems. Tell your doctor if you have upper stomach pain, loss of appetite, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).

Imatinib may increase the risk of fluid retention or heart problems. Tell your doctor if you have swelling or rapid weight gain, shortness of breath, fast or slow heart rate, weak pulse, or fainting.

What should I discuss with my healthcare provider before taking imatinib?

You should not use this medication if you are allergic to imatinib.

To make sure imatinib is safe for you, tell your doctor if you have:

  • liver disease;

  • kidney disease;

  • underactive thyroid, recent or upcoming thyroid surgery;

  • heart disease, congestive heart failure;

  • history of stomach ulcer or bleeding; or

  • if you are receiving chemotherapy.

FDA pregnancy category D. Do not use imatinib if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment.

It is not known whether imatinib passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

Do not give this medication to anyone under 1 year old without medical advice.

Imatinib can affect growth in children. Talk with your doctor if you think your child is not growing at a normal rate while using this medicine.

How should I take imatinib?

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Take this medicine with a large glass of water.

You may dissolve the imatinib tablet in water or apple juice to make swallowing easier.

Imatinib should be taken with a meal. Do not take imatinib on an empty stomach.

Imatinib can lower blood cells that help your body fight infections and help your blood to clot. Your blood will need to be tested often. Your cancer treatments may be delayed based on the results of these tests.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember, making sure you also eat a meal and drink a large glass of water. Skip the missed dose if it is almost time for your next dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking imatinib?

Avoid being near people who are sick or have infections. Tell your doctor at once if you develop signs of infection.

Avoid activities that may increase your risk of bleeding or injury. Use extra care to prevent bleeding while shaving or brushing your teeth.

This medicine can pass into body fluids (including urine, feces, vomit, semen, vaginal fluid). For at least 48 hours after you receive a dose, avoid allowing your body fluids to come into contact with your hands or other surfaces. Patients and caregivers should wear rubber gloves while cleaning up body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Body fluids should not be handled by a woman who is pregnant or who may become pregnant. Use condoms during sexual activity to avoid exposure to body fluids.

Grapefruit and grapefruit juice may interact with imatinib and lead to potentially dangerous effects. Avoid the use of grapefruit products while taking imatinib.

Imatinib side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • fever, chills, body aches, flu symptoms;

  • easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin;

  • swelling, rapid weight gain, feeling short of breath (even with mild exertion);

  • nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);

  • bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;

  • lower back pain, blood in your urine, little or no urinating;

  • numbness or tingly feeling around your mouth;

  • muscle weakness, tightness, or contraction, overactive reflexes;

  • fast or slow heart rate, weak pulse, confusion, fainting; or

  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Common side effects may include:

  • mild nausea or stomach pain, vomiting, diarrhea;

  • joint or muscle pain; or

  • headache, feeling tired.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Imatinib dosing information

Usual Adult Dose for Chronic Myelogenous Leukemia:

Chronic phase: 400 mg orally once a day.
Accelerated phase: 600 mg orally once a day.

Disease progression chronic phase: 600 mg orally once a day.
Disease progression accelerated phase: 400 mg orally twice a day.

A dose increase from 400 mg to 600 mg in adult patients with chronic phase disease, or from 600 mg to 800 mg (given as 400 mg twice daily) in adult patients in accelerated phase or blast crisis may be considered in the absence of severe adverse drug reaction and severe non-leukemia related neutropenia or thrombocytopenia in the following circumstances: disease progression (at any time), failure to achieve a satisfactory hematologic response after at least three months of treatment, failure to achieve a cytogenetic response after six to twelve months of treatment, or loss of a previously achieved hematologic or cytogenetic response.

Dose adjustments for Chronic Phase CML (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

Dose adjustments for Ph+ CML: Accelerated Phase and Blast Crisis (starting dose 600 mg)
ANC less than 0.5 x 10(9)/L and/or Platelets less than 10 x 10(9)/L:
1. Check if cytopenia is related to leukemia (marrow aspirate or biopsy).
2. If cytopenia is unrelated to leukemia, reduce dose of imatinib to 400 mg.
3. If cytopenia persists 2 weeks, reduce further to 300 mg.
4. If cytopenia persists 4 weeks and is still unrelated to leukemia, stop imatinib until ANC greater than or equal to 1 x 10(9)/L and platelets greater than or equal to 20 x 109/L and then resume treatment at 300 mg.

Usual Adult Dose for Gastrointestinal Stromal Tumor:

For adult patients with unresectable and/or metastatic, malignant GIST:
Recommended dose: 400 mg/day
A dose increase up to 800 mg daily (given as 400 mg twice daily) may be considered, as clinically indicated, in patients showing clear signs or symptoms of disease progression at a lower dose and in the absence of severe adverse drug reactions.

For the adjuvant treatment of adult patients following complete gross resection of GIST:
Recommended dose: 400 mg/day
In the clinical study, imatinib was administered for one year. The optimal treatment duration with imatinib is not known.

Dose adjustments for GIST (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose of 300 mg.

Usual Adult Dose for Acute Lymphoblastic Leukemia:

For use in the treatment of Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL):

Recommended dose: 600 mg/day for adult patients with relapsed/refractory Ph+ ALL

Dose adjustments for ALL (starting dose 600 mg)
ANC less than 0.5 x 10(9)/L and/or Platelets less than 10 x 10(9)/L:
1. Check if cytopenia is related to leukemia (marrow aspirate or biopsy).
2. If cytopenia is unrelated to leukemia, reduce dose of imatinib to 400 mg.
3. If cytopenia persists 2 weeks, reduce further to 300 mg.
4. If cytopenia persists 4 weeks and is still unrelated to leukemia, stop imatinib until ANC greater than or equal to 1 x 10(9)/L and platelets greater than or equal to 20 x 109/L and then resume treatment at 300 mg.

Usual Adult Dose for Systemic Mastocytosis:

Recommended dose: 400 mg/day for patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation. If c-Kit mutational status is not known or unavailable, treatment with imatinib 400 mg/day may be considered for patients with ASM not responding satisfactorily to other therapies.

Dose adjustments for ASM (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

For patients with ASM associated with eosinophilia (a clonal hematological disease related to the fusion kinase FIP1L1-PDGFRalpha):
Recommended starting dose: 100 mg/day
A dose increase from 100 mg to 400 mg for these patients may be considered in the absence of adverse drug reactions if assessments demonstrate an insufficient response to therapy.

Dose adjustments for ASM associated with eosinophilia (starting dose 100 mg)
ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at previous dose (i.e. before severe adverse reaction).

Usual Adult Dose for Hypereosinophilic Syndrome:

For patients with hypereosinophilic syndrome/chronic eosinophilic leukemia (HES/CEL):
Recommended dose: 400 mg/day

Dose adjustments for HES/CEL (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

For patients with HES/CEL patients with demonstrated FIP1L1-PDGFRalpha fusion kinase:
Recommended starting dose: 100 mg/day
Dose increase from 100 mg to 400 mg for these patients may be considered in the absence of adverse drug reactions if assessments demonstrate an insufficient response to therapy.

Dose adjustments for HES/CEL with FIP1L1-PDGFRalpha fusion kinase (starting dose 100 mg)
ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at previous dose (i.e. before severe adverse reaction).

Usual Adult Dose for Chronic Eosinophilic Leukemia:

For patients with hypereosinophilic syndrome/chronic eosinophilic leukemia (HES/CEL):
Recommended dose: 400 mg/day

Dose adjustments for HES/CEL (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

For patients with HES/CEL patients with demonstrated FIP1L1-PDGFRalpha fusion kinase:
Recommended starting dose: 100 mg/day
Dose increase from 100 mg to 400 mg for these patients may be considered in the absence of adverse drug reactions if assessments demonstrate an insufficient response to therapy.

Dose adjustments for HES/CEL with FIP1L1-PDGFRalpha fusion kinase (starting dose 100 mg)
ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at previous dose (i.e. before severe adverse reaction).

Usual Adult Dose for Dermatofibrosarcoma Protuberans:

Recommended dose: 800 mg/day for patients with dermatofibrosarcoma protuberans (DFSP)

Dose adjustments for DFSP (starting dose 800 mg)
ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 X 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at 600 mg.
3. In the event of recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at reduced dose of 400 mg.

Usual Adult Dose for Myeloproliferative Disorders:

Recommended dose: 400 mg/day for patients with myelodysplastic/myeloproliferative diseases (MDS/MPD)

MDS/MPD (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

Usual Adult Dose for Myelodysplastic Diseases:

Recommended dose: 400 mg/day for patients with myelodysplastic/myeloproliferative diseases (MDS/MPD)

MDS/MPD (starting dose 400 mg)
ANC less than 1.0 x 10(9)/L and/or Platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at the original starting dose of 400 mg or 600 mg.
3. If recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at a reduced dose (300 mg if starting dose was 400 mg, 400 mg if starting dose was 600 mg).

Usual Pediatric Dose for Chronic Myelogenous Leukemia:

Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in chronic phase:

340 mg/m2 orally once a day or 170 mg/m2 orally twice a day

Maximum Dose: 600 mg daily

Duration of therapy: Treatment may be continued as long as there is no evidence of progressive disease or unacceptable toxicity.

Comments: There is no experience with imatinib treatment in children under 1 year of age.

Dose adjustments for newly diagnosed pediatric chronic phase CML (starting dose 340 mg/m2):

ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L:
1. Stop imatinib until ANC greater than or equal to 1.5 x 10(9)/L and platelets greater than or equal to 75 x 10(9)/L.
2. Resume treatment with imatinib at previous dose (i.e. before severe adverse reaction).
3. In the event of recurrence of ANC less than 1.0 x 10(9)/L and/or platelets less than 50 x 10(9)/L, repeat step 1 and resume imatinib at reduced dose of 260 mg/m2.

Usual Pediatric Dose for Acute Lymphoblastic Leukemia:

Newly diagnosed Ph+ ALL in combination with chemotherapy:

340 mg/m2 orally once a day

Maximum Dose: 600 mg once a day

Duration of therapy: Treatment may be continued as long as there is no evidence of progressive disease or unacceptable toxicity.

Comments: There is no experience with imatinib treatment in children under 1 year of age.

What other drugs will affect imatinib?

Many drugs can interact with imatinib. Not all possible interactions are listed here. Tell your doctor about all your medications and any you start or stop using during treatment with imatinib, especially:

  • acetaminophen (Tylenol);

  • aprepitant;

  • bosentan;

  • cimetidine;

  • cyclosporine;

  • haloperidol;

  • St. John's wort;

  • an antibiotic--clarithromycin, ciprofloxacin, doxycycline, erythromycin, metronidazole, nafcillin, norfloxacin, rifabutin, rifampin, rifapentine, tetracycline;

  • antifungal medication--clotrimazole, fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole;

  • an antidepressant--desipramine, nefazodone, sertraline;

  • a blood thinner such as warfarin, Coumadin;

  • heart or blood pressure medication--amiodarone, diltiazem, dronedarone, lidocaine, nicardipine, quinidine, verapamil;

  • hepatitis C medications--boceprevir, telaprevir;

  • HIV/AIDS medication--atazanavir, delavirdine, darunavir when given with ritonavir, efavirenz, fosamprenavir, indinavir, nelfinavir, nevirapine, ritonavir, saquinavir; or

  • seizure medication--carbamazepine, fosphenytoin, oxcarbazepine, phenobarbital, phenytoin, primidone.

This list is not complete and many other drugs can interact with imatinib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Give a list of all your medicines to any healthcare provider who treats you.

Where can I get more information?

  • Your pharmacist can provide more information about imatinib.
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 11.03. Revision Date: 2013-07-08, 2:32:27 PM.

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