Imatinib (Gleevec)

Generic Name: Imatinib

Imatinib is a small molecule kinase inhibitor. Gleevec film-coated tablets contain imatinib mesylate equivalent to 100 mg or 400 mg of imatinib free base. Imatinib mesylate is designated chemically as 4-[(4-Methyl1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate and its structural formula is:


GLEEVEC® (imatinib mesylate) - Structural Formula Illustration

Imatinib mesylate is a white to off-white to brownish or yellowish tinged crystalline powder. Its molecular formula is C29H31N7O • CH4SO3 and its molecular weight is 589.7. Imatinib mesylate is soluble in aqueous buffers less than or equal to pH 5.5 but is very slightly soluble to insoluble in neutral/alkaline aqueous buffers. In non-aqueous solvents, the drug substance is freely soluble to very slightly soluble in dimethyl sulfoxide, methanol, and ethanol, but is insoluble in n-octanol, acetone, and acetonitrile.

Inactive Ingredients: colloidal silicon dioxide (NF); crospovidone (NF); hydroxypropyl methylcellulose (USP); magnesium stearate (NF); and microcrystalline cellulose (NF). Tablet coating: ferric oxide, red (NF); ferric oxide, yellow (NF); hydroxypropyl methylcellulose (USP); polyethylene glycol (NF) and talc (USP).

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Dr. Anirban Deep Banerjee

Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the Bcr-Abl tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML). It inhibits proliferation and induces apoptosis in Bcr-Abl positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib also inhibits the receptor tyrosine kinases for platelet derived growth factor (PDGF) and stem cell factor (SCF) - called c-kit. Imatinib was identified in the late 1990s by Dr Brian J. Druker. Its development is an excellent example of rational drug design. Soon after identification of the bcr-abl target, the search for an inhibitor began. Chemists used a high-throughput screen of chemical libraries to identify the molecule 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib.

Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.

Chronic myelogenous leukemia

The U.S. Food and Drug Administration (FDA) has approved imatinib as first-line treatment for Philadelphia chromosome-positive CML, both in adults and children. The drug is approved in multiple contexts of Philadelphia chromosome-positive CML, including after stem cell transplant, in blast crisis, and newly diagnosed.

Due in part to the development of imatinib and related drugs, the five year survival rate for people with chronic myeloid leukemia increased from 31% in 1993 to 59% in 2003 to 2009.

Gastrointestinal stromal tumors

The FDA first granted approval for advanced GIST patients in 2002. On 1 February 2012, imatinib was approved for use after the surgical removal of KIT-positive tumors to help prevent recurrence. The drug is also approved in unresectable KIT-positive GISTs.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

  • Abdominal or stomach pain, cramping, burning, or tenderness
  • bleeding from wound after surgery
  • bleeding gums
  • bleeding problems
  • bloating or swelling of the face, hands, lower legs, or feet
  • blood in the urine
  • bloody eye
  • bloody nose
  • blue lips and fingernails
  • blurred vision
  • body aches or pain
  • chest pain or discomfort
  • chills
  • clay-colored stools
  • cough
  • coughing that sometimes produces a pink frothy sputum
  • coughing up blood
  • decrease in the amount of urine
  • decreased appetite
  • decreased urination
  • diarrhea
  • difficult or labored breathing
  • difficulty with swallowing
  • dizziness
  • dry mouth
  • ear congestion
  • fever
  • general feeling of discomfort or illness
  • headache
  • inability to speak
  • increased menstrual flow or vaginal bleeding
  • increased thirst
  • irregular heartbeat
  • itching or skin rash
  • joint pain
  • large, flat, blue, or purplish patches on the skin
  • loss of appetite
  • loss of voice
  • mood changes
  • muscle aches and pain
  • muscle cramps
  • nausea and vomiting
  • noisy, rattling breathing
  • nosebleed
  • numbness or tingling in the hands, feet, or lips
  • pain or tenderness around the eyes and cheekbones
  • painful or difficult urination
  • pale skin
  • prolonged bleeding from cuts
  • rapid weight gain
  • red, black, bloody, or tarry stools
  • red or dark brown urine
  • redness of the eye
  • seizures
  • shivering
  • slurred speech
  • small red or purple spots on the skin
  • sneezing
  • sore throat
  • sores, ulcers, or white spots on the lips or in the mouth
  • stuffy or runny nose
  • sweating
  • swelling in the legs and ankles
  • swollen glands
  • temporary blindness
  • tightness in the chest
  • trouble sleeping
  • troubled breathing at rest
  • troubled breathing when moving or walking
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • vomiting of blood or material that looks like coffee grounds
  • weakness in the arm or leg on one side of the body, sudden and severe
  • yellow eyes or skin

Incidence not known

  • Anxiety
  • blistering, peeling, or loosening of the skin
  • change in vision not present before treatment
  • chest pain, possibly moving to the left arm, neck, or shoulder
  • confusion
  • delayed or slow growth in children
  • irregular, fast or slow, or shallow breathing
  • nausea, heartburn, or indigestion, severe and continuing
  • pain in the bones
  • red, irritated eyes
  • red skin lesions, often with a purple center
  • seeing floaters, veil, or curtain appearing across part of vision
  • severe abdominal or stomach pain, cramping, or burning
  • severe constipation
  • severe vomiting
  • tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Acid or sour stomach
  • belching
  • difficulty having a bowel movement (stool)
  • difficulty with moving
  • discouragement
  • excess air or gas in the stomach or intestines
  • fear or nervousness
  • feeling sad or empty
  • feeling unusually cold
  • full or bloated feeling
  • increased bowel movements
  • irritability
  • lack or loss of strength
  • loose stools
  • loss of interest or pleasure
  • muscle stiffness
  • night sweats
  • passing gas
  • stomach discomfort, upset, or pain
  • swollen joints
  • trouble concentrating
  • weight loss

Less common

  • Back pain
  • bad, unusual, or unpleasant (after) taste
  • change in taste
  • watering of the eyes

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For the treatment of aggressive systemic mastocytosis (ASM):
      • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For the treatment of chronic eosinophilic leukemia (CEL) or hypereosinophilic syndrome (HES):
      • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For the treatment of dermatofibrosarcoma protuberans (DFSP):
      • Adults—800 milligrams (mg) per day as a single dose or divided and given as 400 mg 2 times per day.
      • Children—Use and dose must be determined by your doctor.
    • For the treatment of gastrointestinal stromal tumors (GIST):
      • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 800 mg per day.
      • Children—Use and dose must be determined by your doctor.
    • For the treatment of myelodysplastic syndrome (MDS) or myeloproliferative diseases (MPD):
      • Adults—400 milligrams (mg) once a day.
      • Children—Use and dose must be determined by your doctor.
    • For the treatment of Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL):
      • Adults—600 milligrams (mg) once a day.
      • Children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The dose is usually 340 milligrams per square meter (mg/m[2]) per day. The dose may be taken once a day or the dose may be divided into two small doses (once in the morning and once in the evening). However, the dose is usually not more than 600 mg per day.
      • Children younger than 1 year of age—Use and dose must be determined by your doctor.
    • For the treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML):
      • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 800 mg per day.
      • Children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The dose is usually 340 milligrams per square meter (mg/m[2]) per day. The dose may be taken once a day or divided into 2 small doses (once in the morning and once in the evening). However, the dose is usually not more than 600 mg per day.
      • Children younger than 1 year of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Eliglustat
  • Flibanserin
  • Lomitapide
  • Measles Virus Vaccine, Live
  • Mumps Virus Vaccine, Live
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Varicella Virus Vaccine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acetaminophen
  • Adenovirus Vaccine
  • Aprepitant
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Bosutinib
  • Brexpiprazole
  • Carbamazepine
  • Cholera Vaccine, Live
  • Cilostazol
  • Clozapine
  • Cobimetinib
  • Dihydroergotamine
  • Domperidone
  • Doxorubicin
  • Doxorubicin Hydrochloride Liposome
  • Enzalutamide
  • Eplerenone
  • Ergotamine
  • Fentanyl
  • Fosaprepitant
  • Fosphenytoin
  • Gemfibrozil
  • Ginseng
  • Hydrocodone
  • Ibrutinib
  • Idelalisib
  • Ifosfamide
  • Influenza Virus Vaccine, Live
  • Ivabradine
  • Ivacaftor
  • Ketoconazole
  • Lumacaftor
  • Lurasidone
  • Mitotane
  • Naloxegol
  • Olaparib
  • Phenobarbital
  • Phenytoin
  • Pimozide
  • Piperaquine
  • Poliovirus Vaccine, Live
  • Rifampin
  • Simeprevir
  • Smallpox Vaccine
  • Sonidegib
  • St John's Wort
  • Tacrolimus
  • Tolvaptan
  • Typhoid Vaccine
  • Venetoclax
  • Warfarin
  • Yellow Fever Vaccine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Levothyroxine
  • Suvorexant

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Grapefruit Juice

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. Taking too much may increase the chance of side effects, while taking too little may not improve your condition.

This medicine should be taken with a tall glass of water and a meal to help prevent stomach irritation.

Swallow the tablet whole. Do not break or crush it.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of imatinib to treat Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase and acute lymphoblastic leukemia (Ph+ ALL) in children younger than 1 year of age. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of imatinib in the elderly. However, serious side effects (eg, swelling of the face, hands, fingers, feet, and/or lower legs, and unusual weight gain) may be more likely to occur in elderly patients, who may be more sensitive than younger adults to the effects of imatinib.

Breastfeeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

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