Imatinib

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Imatinib
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Revision Date: 01/03/2008 1:49:15 PM.

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

What is imatinib?

Imatinib interferes with the growth of some cancer cells.

Imatinib is used to treat a type of blood cancer called Philadelphia chromosome positive chronic myeloid leukemia (CML). It is also used to treat certain tumors of the stomach and digestive system.

Imatinib may also be used for other purposes not listed in this medication guide.
What is the most important information I should know about imatinib?
Do not use this medication without telling your doctor if you are pregnant. It could cause harm to the unborn baby. Use an effective form of birth control, and tell your doctor if you become pregnant during treatment.

Before using this medication, tell your doctor if you are allergic to any drugs, or if you have liver disease, kidney disease, congestive heart failure, or a history of stomach ulcer or bleeding.
Take this medicine with a large glass of water. Imatinib should be taken with a meal. Do not take the medicine on an empty stomach.

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

To be sure this medication is not causing harmful effects, your blood will need to be tested on a regular basis. Your liver function may also need to be tested. Do not miss any scheduled appointments.
What should I discuss with my healthcare provider before taking imatinib?
Do not use this medication if you are allergic to imatinib.

Before using this medication, tell your doctor if you are allergic to any drugs, or if you have:

* liver disease;
* kidney disease;
* congestive heart failure; or
* a history of stomach ulcer or bleeding.

If you have any of these conditions, you may need a dose adjustment or special tests to safely take this medication.
FDA pregnancy category D. This medication can cause harm to an unborn baby. Do not use imatinib without telling your doctor if you are pregnant. Tell your doctor if you become pregnant during treatment. Use an effective form of birth control while you are using this medication. It is not known whether imatinib passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medication to anyone younger than 18 years old without a doctor's advice.

How should I take imatinib?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take this medicine with a large glass of water. Imatinib should be taken with a meal.

To be sure this medication is not causing harmful effects, your blood will need to be tested on a regular basis. Your liver function may also need to be tested. Do not miss any scheduled appointments.
Store imatinib 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. If it is almost time for your next meal, skip the missed dose and take the medicine when you eat your next meal. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include severe muscle cramps.
What should I avoid while taking imatinib?

Do not take imatinib on an empty stomach.

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 any of these serious side effects:

*

fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;
*

nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
*

fever, chills, body aches, flu symptoms;
*

black, bloody, or tarry stools;
*

coughing up blood or vomit that looks like coffee grounds;
*

pale skin, easy bruising or bleeding, unusual weakness;
*

feeling short of breath, even with mild exertion;
*

swelling, rapid weight gain; or
*

sudden, severe headache or pain behind the eyes.

Less serious side effects may include:

*

mild nausea, diarrhea, upset stomach, gas;
*

muscle or joint pain;
*

skin rash;
*

headache, dizziness;
*

stuffy nose, cough, sore throat;
*

depression, sleep problems (insomnia); or
*

tired feeling.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect.
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:

Greater than 3 years: Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in chronic phase: 260 mg/m2 orally once a day or 130 mg/m2 twice a day (morning and evening)

Dose adjustments for pediatric patients with chronic phase CML recurring after transplant or resistant to interferon (starting dose 260 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 200 mg/m2.

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.
What other drugs will affect imatinib?

Many drugs can interact with imatinib. Below is just a partial list. Tell your doctor if you are using:

* cyclosporine (Gengraf, Neoral, Sandimmune);
* dexamethasone (Decadron, Hexadrol);
* fentanyl (Actiq, Duragesic, Ionsys);
* sirolimus (Rapamune), tacrolimus (Prograf);
* St. John's wort;
* a blood thinner such as warfarin (Coumadin);
* an antibiotic such as azithromycin (Zithromax), ciprofloxacin (Cipro), clarithromycin (Biaxin), erythromycin (E-Mycin, E.E.S., Ery-Tab, Erythrocin), griseofulvin (Fulvicin, Grifulvin, Grisactin), itraconazole (Sporanox), ketoconazole (Nizoral), metronidazole (Flagyl, Protostat), rifampin (Rifadin, Rimactane, Rifater);
* antidepressants such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), or sertraline (Zoloft);
* a barbiturate such as amobarbital (Amytal) or phenobarbital (Luminal, Solfoton);
* a calcium channel blocker such as diltiazem (Tiazac, Cartia, Cardizem), nifedipine (Procardia, Adalat), verapamil (Calan, Covera, Isoptin, Verelan), and others;
* cholesterol-lowering medicines such as lovastatin (Mevacor), simvastatin (Zocor), pravastatin (Pravachol), fluvastatin (Lescol), atorvastatin (Lipitor), or cerivastatin (Baycol).
* ergot medicine such as ergotamine (Ergomar, Cafergot) or dihydroergotamine (D.H.E. 45, Migranal Nasal Spray);
* HIV medication such as nevirapine (Viramune), delavirdine (Rescriptor), efavirenz (Sustiva), indinavir (Crixivan), ritonavir (Norvir), saquinavir (Invirase), or nelfinavir (Viracept);
* sedatives such as alprazolam (Xanax) or triazolam (Halcion); or
* seizure medication such as carbamazepine (Carbatrol, Tegretol) or phenytoin (Dilantin).

This list is not complete and there may be other drugs that can interact imatinib. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

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