Gleevec

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Gleevec

Gleevec: The Essentials of Imatinib Mesylate

Property Description
Active Ingredient Imatinib mesylate (INN)
Brand Originator Novartis (Original Manufacturer)
Form Oral Film-Coated Tablets
Pharmacological Class Tyrosine Kinase Inhibitor (TKI)
Common Use Targeted therapy for specific cancers
Origin Synthetic (Chemically manufactured)

Gleevec is the trade name for the prescription drug with the active ingredient imatinib mesylate, a synthetic, small-molecule medication. It is typically supplied as an oral, film-coated tablet for administration by mouth, representing a major therapeutic advancement in oncology.

The original branded formulation, Gleevec, is clinically recognized for its quality and was the first of its class to change the prognosis for patients with Chronic Myeloid Leukemia (CML), transforming it from a rapidly fatal condition into a manageable chronic disease.


What Type of Drug Is Imatinib (Gleevec)?

Imatinib (Gleevec) belongs to the pharmacological class known as tyrosine kinase inhibitors (TKIs). It is considered a form of targeted therapy because it is designed to selectively interfere with specific molecular pathways in cancer cells, minimizing damage to healthy tissue.

This classification is based on its ability to block the activity of several enzymes, including the BCR-ABL fusion protein, which are overactive in certain diseases. Imatinib functions as a kinase inhibitor targeting ABL, KIT, or PDGFR proteins.


What is Gleevec Used For? (General Therapeutic Purpose)

Gleevec is primarily prescribed for cancers driven by specific genetic defects that rely on the kinase activity it blocks. Its main therapeutic uses include managing specific forms of leukemia, such as Chronic Myeloid Leukemia (CML), and Gastrointestinal Stromal Tumors (GIST).

It is a disease-modifying medicine intended for long-term therapeutic management, providing a highly focused approach for patients whose cancers are dependent on the molecular pathway that Imatinib targets.

What side effects are possible with Gleevec?

Possible Side Effects and Safety Information

The safety profile of imatinib mesylate (Gleevec) is officially documented by government regulatory authorities, detailing potential adverse reactions and special safety considerations. The most frequently observed reactions are classified as Very Common or Common in regulatory contexts, establishing them as the expected pattern of side effects.

Frequency-Classified Adverse Reactions

The most common adverse reactions center on fluid accumulation and general systemic effects, primarily edema (fluid retention), nausea, vomiting, diarrhea, musculoskeletal pain, muscle cramps, and fatigue. Hematological toxicities, specifically neutropenia and thrombocytopenia, are also recognized as common, often occurring most frequently during the initial months of therapy.


Serious Organ-System Adverse Reactions

Official labeling documents less frequent but clinically significant adverse reactions across key physiological systems:

  • Hepatobiliary: The potential for severe hepatotoxicity, including cases leading to fatalities, is documented.
  • Cardiac: Serious events, such as congestive heart failure and left ventricular dysfunction, are reported, especially at treatment initiation in certain patient groups.
  • Gastrointestinal: The risk of gastrointestinal perforations and clinically significant hemorrhage is noted in regulatory texts.

Population-Specific and Duration-Related Safety

Specific safety considerations exist for certain populations and duration of use. Severe fluid retention is noted as being more common in older adults. For pediatric patients, the regulatory label documents reports of growth retardation. Furthermore, the safety profile highlights that potential toxicities affecting the liver, kidney, and heart must be considered during long-term exposure to the medicine.

Overdose and Emergency Response

Overdose and When to Seek Help

Imatinib mesylate overdose is associated with severe, potentially life-threatening systemic toxicities, and immediate medical intervention is required for any suspected high-dose exposure. Overdose manifestations have been documented following ingestions ranging from 1,200 mg up to 16,000 mg, or with chronic use of high daily doses.

Documented Overdose Presentations

The official regulatory documents describe manifestations across key physiological systems:

  • Gastrointestinal: Nausea, vomiting, diarrhea, and abdominal pain.
  • Hematological: Myelosuppression, which may present as neutropenia or leukopenia.
  • Organ Function: Evidence of hepatotoxicity (elevated liver aminotransferases, bilirubin) and the risk of renal failure.
  • Severe Complications: Cases of cardiac toxicity have been cited, along with the potential for severe myelosuppression and associated conditions.

Official Emergency Action

Immediate medical attention is required for a suspected overdose. Due to the lack of a specific antidote, management is officially documented as symptomatic and supportive. Regulatory procedures mandate close monitoring in a hospital setting, including observation of vital signs, hematological (blood counts), renal, and hepatic function. Supportive measures such as gastric lavage or administration of activated charcoal may be considered, depending on the ingestion time. These mandated procedures reflect the structured regulatory approach to managing acute toxicity.

Therapeutic Uses of Gleevec

Targeted Management of Cancers and Proliferative Disorders


The therapeutic use of Imatinib is relevant across several conditions characterized by periods of heightened symptoms.

Cancers Driven by Abnormal Cell Proliferation

Gleevec is commonly used to help with Philadelphia chromosome-positive (Ph+) Chronic Myeloid Leukemia (CML), applied in situations where symptoms are related to systemic imbalance and heightened physiological activity. The medication may assist with managing symptoms that create noticeable physiological strain, supporting patients in managing a difficult chronic condition. It is also relevant for managing Ph+ Acute Lymphoblastic Leukemia (ALL) and specific rare disorders, such as certain forms of Hypereosinophilic Syndrome (HES), applied in contexts where additional symptomatic support is needed to address systemic imbalance.

Advanced Solid Tumors and Risk of Recurrence

The medication is commonly used to help with unresectable, recurrent, or metastatic Gastrointestinal Stromal Tumors (GIST) and advanced Dermatofibrosarcoma Protuberans (DFSP). In these settings, Gleevec is relevant for easing symptoms that interfere with daily functioning by helping to manage manifestations related to tumor size or may assist in managing the progression of symptoms. Furthermore, it is applied in the adjuvant context following surgery, where it contributes to easing the overall symptom load by supporting management in the post-treatment clinical scenario.


Quick Fact: Relief for Systemic Imbalance The medication is considered relevant for easing symptoms that interfere with daily comfort and create noticeable physiological strain, particularly in conditions involving persistent, abnormal cell overgrowth.

Regulatory References

  1. U.S. National Institutes of Health (NIH) DailyMed Drug Label

Eligibility and Restrictions for Use

Who Can and Cannot Use Gleevec?

Eligibility for Imatinib (Gleevec) is strictly defined by regulatory bodies and focuses on patient population, specific health status, and reproductive capacity.


Absolute Contraindication

Gleevec is formally contraindicated in patients with a known history of hypersensitivity to Imatinib or any component of the tablet formulation.


Restricted Use Populations

  • Age: While approved for adults and certain pediatric indications, no clinical experience is established for the use of Imatinib in children less than two years of age.
  • Organ Function: Patients with severe hepatic impairment or moderate renal impairment are designated as a population requiring conditional use, which includes regulatory-mandated dose adjustments. Caution is advised for those with severe renal impairment due to limited clinical data.
  • Reproductive Status: Use during pregnancy is restricted, as Imatinib carries the risk of fetal harm, and women of reproductive potential must be advised to avoid pregnancy. Additionally, Imatinib is not recommended for women who are breastfeeding.
  • Comorbidities: Patients with pre-existing cardiac disease or risk factors for congestive heart failure must be carefully monitored and managed as a precaution against complications, as outlined in official labeling. Caution is also advised for populations with conditions linked to high eosinophil levels.

What should I know about interactions with other medicines?

Interactions with other medicines and products: Official Regulatory Information for Imatinib

Regulatory documentation defines the interaction profile of Imatinib mesylate (Gleevec) based on its roles as a substrate for the CYP3A4 metabolic enzyme and an inhibitor of both CYP3A4 and the P-glycoprotein (P-gp) transporter. This involvement leads to specific restrictions and administration conditions.

Contraindicated Combinations

The co-administration of Imatinib is contraindicated with specific substances. This includes the herbal product St. John’s Wort (Hypericum perforatum) because it acts as a potent CYP3A4 inducer, which significantly decreases Imatinib plasma exposure, risking reduced efficacy. Similarly, co-administration with Pimozide is contraindicated because Imatinib increases its concentration, which can pose a risk of QT-interval prolongation.

Documented Exposure Modification

Imatinib’s inhibitory effect on CYP3A4 causes it to increase the plasma concentrations of co-administered CYP3A4 substrates, such as Simvastatin. Conversely, strong CYP3A4 inhibitors (e.g., Ketoconazole) increase Imatinib's own exposure. The medicine must be administered with a meal and a large glass of water, which is a required administration-timing rule designed to minimize gastrointestinal issues and optimize absorption.

Population and Anticoagulant Notes

Patients with severe hepatic impairment are documented to have increased Imatinib exposure, which suggests a greater risk of accumulation. A specific pharmacodynamic interaction is noted for the anticoagulant Warfarin, where co-administration may lead to elevated Prothrombin Time/INR.

Mechanism of Action

Molecular Blockade of Key Tyrosine Kinases

Imatinib functions as a highly targeted Type-2 kinase inhibitor by binding specifically to the ATP-binding pocket of several key enzymes, including the BCR-ABL fusion protein, c-Kit, and PDGFR receptors. This binding stabilizes the enzyme in an inactive conformation, competitively blocking the transfer of a phosphate group required for downstream signaling.


Cascade of Cellular Growth Arrest

By successfully inhibiting the kinase activity, Imatinib stops the continuous, aberrant tyrosine phosphorylation that drives pro-survival and proliferative signaling. The removal of these pro-survival signals triggers programmed cell death (apoptosis) and the cessation of proliferation in kinase-dependent cells. This selective cellular elimination and growth arrest results in the core physiological change produced by the mechanism.


Pharmacodynamic Limitations and Structural Resistance

However, the mechanism's inhibitory function is structurally constrained by the precise shape of the enzyme's binding site. Specific genetic alterations, such as the T315I mutation, structurally prevent Imatinib from stabilizing the inactive state of the kinase. This structural limitation results in the reactivation of the aberrant signaling cascade, leading to the resumption of continuous cellular proliferation and survival signaling.

Dosage and Administration Information

How Gleevec is Used: Official Administration Guidelines

Imatinib mesylate (Gleevec) is administered through the oral route, available as film-coated tablets in 100 mg and 400 mg strengths. Specific protocols are established for the amount, timing, and administration of the medicine.


Administration Details and Dosing Protocol

Parameter Instruction
Timing in Relation to Meals Must be taken with a meal and a large glass of water.
Standard Adult Frequency Generally administered once daily for doses up to 600 mg. The 800 mg/day dose is split and taken as 400 mg twice daily (morning and evening).
Missed Dose Rule If a dose is missed, the patient should take the next dose at the regular scheduled time and not take an extra dose to compensate.
Long-Term Duration Treatment follows a continuous, long-term pattern, though specific durations are defined for certain uses, such as 3 years for adjuvant GIST.

Dosage and Population-Specific Adjustments

Standard starting doses are typically 400 mg/day for Chronic Myeloid Leukemia (CML) in the chronic phase and unresectable GIST, and 600 mg/day for the accelerated phase or Ph+ Acute Lymphoblastic Leukemia (ALL). The dose may be adjusted—escalated or reduced—based on established protocol and patient response. For pediatric patients, dosing is calculated based on Body Surface Area (BSA) at 340 mg/m^2/ day, not to exceed 600 mg daily. Furthermore, patients with severe hepatic impairment require a 25% dose reduction from the standard initial dose to ensure appropriate administration.

Alternative Administration

For patients unable to swallow the tablets whole, they may be dispersed in water or apple juice and stirred immediately before administration.

Recent Clinical Evidence

Research evidence / Overview of studies for Gleevec

Evidence for use in Chronic Myeloid Leukemia (CML)

The research foundation for Imatinib in Chronic Myeloid Leukemia (CML), particularly in the newly diagnosed chronic phase, includes large-scale Randomized Controlled Trials (RCTs). These pivotal studies were designed to evaluate the drug by comparing it against the prior standard treatment, examining important outcomes like the achievement of Cytogenetic Response and specific Molecular Responses. Studies focusing on these same trial populations have provided descriptions of long-term overall survival patterns, with follow-up extending over extended periods in some cohorts. These findings describe patterns of how patients' disease activity evolved over time in the controlled settings of the studies.

Evidence for use in Gastrointestinal Stromal Tumors (GIST)

Research exploring Imatinib for Gastrointestinal Stromal Tumors (GIST) has been conducted using different study designs. For patients with advanced, unresectable, or metastatic GIST, studies used single-arm trials to observe disease activity. For patients treated with surgery, Randomized Controlled Trials were applied to explore the use of the drug afterwards (the adjuvant setting). Advanced disease studies reported measurements of tumor shrinkage, or Objective Response Rate (ORR), in the observed populations. Research documented that the observed outcomes were studied in conjunction with the specific gene mutation examined in the GIST tumor studies.

Evidence for use in Rare Cancers and Disorders

Research has also explored the use of Imatinib in several rare conditions, including Philadelphia chromosome-positive Acute Lymphoblastic Leukemia (Ph+ ALL) and a specific type of Hypereosinophilic Syndrome (HES). For Ph+ ALL, research primarily involved single-arm trials where the drug was used alongside standard combination chemotherapy, monitoring the achievement of Complete Remission (CR). For HES, research focused primarily on patients carrying the specific FIP1L1-PDGFRα fusion kinase, monitoring the rapid normalization of white blood cell counts (Hematologic Response).

Evidence Gaps and Areas of Uncertainty

While a substantial research base exists for Imatinib, particularly for CML, several areas of uncertainty and limitation have been identified in the evidence landscape. Sample sizes were modest in trials for rare conditions, meaning the results apply only to the specific small populations studied. Comparative evidence is lacking for many settings, such as DFSP and HES, where the research is based on single-arm studies. Additionally, research is ongoing to address complex treatment questions, such as which CML patients may safely discontinue treatment after achieving deep remission.

Key Studies & References

  1. Imatinib mesylate for the treatment of unresectable or metastatic gastrointestinal stromal tumors: a retrospective study (early phase data)

Frequently Asked Questions (FAQ)

Common questions about Gleevec (FAQ)


Q: What should a patient do if they miss a scheduled dose of Gleevec?

Official guidance indicates that if a dose of Gleevec is missed, the next scheduled dose is taken at the usual time. The official product information states that an extra dose should not be taken to make up for the one that was missed.


Q: Can Gleevec tablets be safely split, crushed, or dissolved if swallowing is difficult?

Regulatory information describes that for patients who have trouble swallowing the tablets whole, the medication may be dispersed in water or apple juice. The mixture should be stirred immediately prior to administration.


Q: What are the most commonly reported side effects of taking Gleevec?

According to official regulatory sources, the most frequently reported side effects include fluid retention (edema), muscle pain and cramps, nausea, vomiting, diarrhea, a rash, and general fatigue. Blood tests may also commonly show low levels of certain blood cells.


Q: Are there any strict food or drink restrictions while taking Gleevec?

Official administration guidelines state that Gleevec must be taken with a meal and a large glass of water. Additionally, official documents describe that patients should avoid grapefruit or grapefruit juice, as well as herbal products containing St. John’s Wort.


Q: Why is grapefruit or grapefruit juice often mentioned as an interaction risk with Gleevec?

Official information indicates that Gleevec is processed by a liver enzyme called CYP3A4. Grapefruit and its juice are known to inhibit this enzyme, which can cause the level of Gleevec in the blood to increase. This elevated concentration potentially raises the risk of side effects.


Q: Does Gleevec affect the immune system and increase the risk of infection?

Yes, official labeling states that Gleevec commonly causes low white blood cell counts (neutropenia). This reduction in infection-fighting cells is linked to an increased risk of developing an infection.


Q: What effective birth control measures are recommended while on Gleevec treatment?

Official product information advises female patients of reproductive potential to use adequate contraception throughout the entire course of therapy. This precaution is also required for at least 14 days after the final dose of the medication is administered.


Q: Is Gleevec always taken for the rest of a patient’s life?

The required duration of Gleevec treatment is typically long-term and often continuous for many conditions. However, the regulatory documentation specifies fixed treatment durations for certain uses, such as three years for adjuvant Gastrointestinal Stromal Tumors (GIST) treatment.


Q: Are there research studies on stopping Gleevec and remaining disease-free (treatment-free remission)?

Research continues to explore the question of whether certain patients with Chronic Myeloid Leukemia who have achieved a deep, stable remission can safely discontinue treatment. This topic is still under active investigation.


Q: What are the signs of a severe or life-threatening skin reaction related to Gleevec?

Official labeling states that a rash accompanied by symptoms like fever, mouth sores, blistering, peeling skin, or extreme fatigue is a sign that requires immediate medical review, as the label warns against severe dermatologic reactions.


Q: What specific symptoms of infection should a person watch for while taking Gleevec?

Due to the potential for low white blood cell counts, symptoms such as fever, chills, or a persistent sore throat are listed in official documents as signs that require immediate medical review for possible infection.


Q: What symptoms of heart issues or breathing difficulty should be reported immediately?

The official label notes a risk of severe congestive heart failure. Symptoms noted on the official label that require prompt medical review include sudden weight gain, unusual swelling of the hands or feet, or unexplained shortness of breath.


Q: Can Gleevec cause changes in a patient's sense of taste or smell?

Changes in taste, sometimes referred to as dysgeusia or taste disturbance, have been reported as a possible side effect of the medication. This is listed in some regulatory documents as an uncommon adverse event.


Q: Is hair thinning or hair loss a common side effect of Gleevec?

Hair loss or thinning (alopecia) has been reported in regulatory documents. While noted as a side effect, it is not listed among the most frequent adverse events.


Q: Are there any reports of Gleevec causing changes in hair color?

Official regulatory documents acknowledge pigmentation changes as a possible side effect. These reported changes can include the lightening or darkening of both skin and hair color.


Q: Is a metallic or strange taste in the mouth common when starting Gleevec?

Alterations to taste, which some patients might describe as a strange or metallic sensation, have been reported as an adverse event. This side effect is typically classified as uncommon.


Q: Does Gleevec typically cause patients to gain or lose weight?

Weight gain is listed in regulatory texts as a common adverse reaction. This is frequently attributed to the fluid retention (edema) that many patients experience while taking the medication.


Q: Are there any serious digestive tract problems, like bleeding or holes, linked to Gleevec?

Official labeling documents a risk of severe gastrointestinal issues, including clinically significant bleeding and the potential for a gastrointestinal perforation (a hole). Unusual abdominal pain or dark stools are symptoms that official documents state require prompt medical review.


Q: Can a patient safely consume alcohol while undergoing treatment with Gleevec?

While there is no explicit contraindication against alcohol, Gleevec carries a risk of severe liver problems. Because Gleevec carries a risk of severe liver problems, concurrent consumption of alcohol may increase the overall risk of liver toxicity.


Q: How does Gleevec affect thyroid function, particularly in patients who have had a thyroidectomy?

Low thyroid function (hypothyroidism) has been reported in patients taking Gleevec, especially in those who have previously had a thyroidectomy. Regulatory documents advise that thyroid function be monitored in these patients.


Q: Can Gleevec cause or contribute to kidney problems?

Caution is advised for patients with existing kidney issues. Reports of new or worsening renal impairment and, in some cases, kidney failure have been documented, particularly with long-term use of the medicine.


Q: What happens if Gleevec is taken with an over-the-counter medication like Tylenol (acetaminophen)?

Caution is advised when using Gleevec alongside over-the-counter medications such as acetaminophen (Tylenol). Regulatory warnings highlight that high doses of both medications have been associated with an increased risk of severe liver toxicity.


Q: Is hair thinning or hair loss a common side effect of Gleevec?

Hair loss or thinning (alopecia) has been reported in regulatory documents. While noted as a side effect, it is not listed among the most frequent adverse events.


Q: Are there any reports of Gleevec causing changes in hair color?

Official regulatory documents acknowledge pigmentation changes as a possible side effect. These reported changes can include the lightening or darkening of both skin and hair color.

How should Gleevec be stored and disposed of?

How to Store and Dispose of Gleevec (Imatinib Mesylate)

Storage Requirements

Gleevec tablets must be stored at controlled room temperature, specifically between 20 C and 25 C (68 F and 77 F); excursions are permitted up to 30 C (86 F). The medication must be kept in its original container, which should remain tightly closed to ensure protection. It is essential to store Gleevec out of the reach of children.

Disposal Instructions

Unused or expired Gleevec should be disposed of properly, preferably through a medicine take-back program. If a program is unavailable, mix the tablets with an undesirable substance, such as dirt or used coffee grounds, place the mixture in a sealed plastic bag, and then discard it in the household trash. Do not flush Gleevec down the toilet or pour it into a drain.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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