Glivec

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Glivec

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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 Glivec

Quick Facts

Property Description
Active Ingredient Imatinib Mesylate
Form Oral Film-coated Tablets
Pharmacological Class Protein-Tyrosine Kinase Inhibitor (TKI)
Common Type Targeted Therapy / Synthetic Small Molecule
Rx Status Prescription-only Medicine

Glivec is the international brand name for the active ingredient Imatinib Mesylate, a synthetic targeted therapy medication and one of the first established small molecule inhibitors in its class. It is taken orally, typically as a film-coated tablet, and works by blocking specific molecular signals within abnormal cells to suppress their growth.


What Type of Medicine is Glivec (Imatinib Mesylate)?

Glivec is a prescription drug containing the active ingredient Imatinib Mesylate, which is derived from the 2-phenylaminopyrimidine chemical structure. It belongs to the specialized pharmacological class of Protein-Tyrosine Kinase Inhibitors (TKIs). As a selective inhibitor and a single-entity product, Imatinib is a small molecule inhibitor designed to reach molecular targets inside cells and is administered orally.


Composition, Form, and General Therapeutic Purpose

The medicine's core component is Imatinib Mesylate, which is compounded with standard pharmaceutical excipients to produce the final oral film-coated tablet form. The general therapeutic purpose of this drug is to achieve a cytostatic effect, meaning it helps to suppress abnormal cell proliferation rather than broadly causing immediate cell death. It acts as a specialized molecular blocker of specific enzymes, notably the BCR-ABL fusion protein. This inhibitory activity interferes with key disease-driving mechanisms and serves as a critical control mechanism against uncontrolled cellular proliferation.


How Does Glivec Differ from Traditional Chemotherapy?

Glivec is a targeted therapy, which distinguishes it from cytotoxic chemotherapy agents. Traditional chemotherapy broadly damages most rapidly dividing cells, often including healthy ones. In contrast, Glivec is designed to specifically target and inhibit particular faulty proteins, such as tyrosine kinases and the BCR-ABL fusion protein, responsible for driving the abnormal growth in certain diseases. This high selectivity is the core differentiating factor, allowing it to shut down the molecular fault with greater precision.

What side effects are possible with Glivec?

Possible Side Effects and Safety Information

Glivec (Imatinib Mesylate) is associated with an official safety profile categorized by adverse reaction frequency and affected body systems, as documented in regulatory labeling. The most frequently reported adverse reactions are classified as Very Common (occurring in 10% or more of patients) and typically involve fluid retention/oedema (particularly periorbital swelling), gastrointestinal effects (nausea, vomiting, diarrhea), fatigue, and musculoskeletal symptoms (muscle spasms, pain).

The adverse effects are grouped into System-Organ Classes (SOC) that include Blood and Lymphatic System Disorders (e.g., neutropenia, thrombocytopenia), Gastrointestinal Disorders, Musculoskeletal Issues, and Skin and Subcutaneous Tissue Disorders.

Serious Adverse Reactions and Safety Constraints

The regulatory label documents the potential for serious adverse reactions. These include severe fluid retention (such as pleural effusion or pulmonary oedema), severe haematological toxicities, and rare cases of severe hepatotoxicity or fatal hepatic failure. Clinically critical mucocutaneous reactions, such as Stevens-Johnson Syndrome, are also noted.

Official safety notes specify that haematological toxicities are generally observed during the initial cycles of treatment. Caution is required when the medicine is used in patients with pre-existing hepatic or cardiac impairment. Specific safety considerations are documented for older adults, who may experience a higher incidence of oedema, and for the pediatric population, where monitoring for growth retardation is advised.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory information describes specific manifestations that occur following high-dose exposures to Glivec (Imatinib Mesylate).

Classification Documented Overdose Findings
Documented Presentations Gastrointestinal effects (nausea, vomiting, diarrhea, abdominal pain), edema, fatigue, and muscle cramps [Source: MedlinePlus Drug Information].
Severe Outcomes Life-threatening events may include signs of liver failure, as reported in one case of a 10 g overdose, and congestive heart failure due to severe fluid retention [Source: EMA Scientific Discussion].
Laboratory Manifestations Documented findings include changes in blood counts, such as myelosuppression (neutropenia, thrombocytopenia, anemia), and markers of hepatotoxicity (elevated liver enzymes and bilirubin) [Source: FDA Prescribing Information].

The official profile specifies that no specific antidote is known for Imatinib Mesylate overdose, and treatment involves providing symptomatic and supportive treatment [Source: EMA Scientific Discussion]. The patient should be kept under observation [Source: FDA Prescribing Information].

When Immediate Medical Help is Required

Regulatory authorities mandate that individuals must seek immediate medical attention for any suspected ingestion beyond the prescribed amount [Source: MedlinePlus Drug Information]. Emergency services must be contacted immediately if the person has collapsed, had a seizure, has trouble breathing, or cannot be awakened [Source: MedlinePlus Drug Information].

Therapeutic Uses of Glivec

What Glivec Treats: Main Uses and Benefits

Glivec (Imatinib Mesylate) is a targeted therapeutic medicine commonly applied in clinical settings that involve acute or unstable symptom patterns. Its primary role is applied in addressing conditions characterized by periods of heightened symptoms, offering patients long-term support for their condition. The medication is used across various conditions presenting with such acute episodes.

Therapeutic Scope and Patient Benefit

This medicine is commonly used as a long-term treatment for Philadelphia chromosome positive (Ph+) Chronic Myeloid Leukemia (CML) and certain Ph+ Acute Lymphoblastic Leukemia (Ph+ ALL). It is also considered relevant for easing symptoms in specific solid tumors, most notably Gastrointestinal Stromal Tumors (GIST), in addition to rare blood disorders like certain Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) and conditions related to Hypereosinophilic Syndrome (HES). The medicine helps with managing symptoms that interfere with daily functioning and contributes to easing the overall symptom load associated with heightened physiological activity. It may assist with managing symptoms that create noticeable physiological strain in advanced GIST, supports the patient during difficult episodes by easing distress, and is commonly used as an adjuvant treatment following surgical removal of high-risk GIST to help manage the risk of the tumor returning.


Quick Fact: Relief for Uncontrolled Cellular Activity

Property Description
Primary Indication Chronic Myeloid Leukemia (Ph+)
Benefit Focus Supports management of symptoms related to systemic imbalance
Use Context Long-term disease management, post-surgical adjuvant therapy
Symptom Managed Symptoms related to heightened physiological activity

Regulatory References

  1. European Medicines Agency (EMA) product information

Eligibility and Restrictions for Use

Who can and cannot use Glivec (Imatinib)

The eligibility for Glivec is governed by official regulatory rules that define specific patient populations based on absolute contraindications, age, and pre-existing health conditions.

  • Absolute Contraindication: The medicine is strictly contraindicated in any patient with a known hypersensitivity (allergy) to the active substance, imatinib, or any of the components in the tablet.

  • Reproductive Status: Use during pregnancy is not recommended due to documented risk of fetal harm; therefore, females of reproductive potential are required to use effective contraception. Similarly, it is not recommended while breastfeeding, as the drug is known to pass into human milk.

  • Age Eligibility: Glivec is approved for adults and for pediatric patients aged 1 year and older for specific indications (Ph+ leukemias). Safety and efficacy have not been established in children under the age of one year.

  • Organ Function & Health Status: Patients with severe hepatic (liver) impairment are considered a restricted population and require initial management adjustments. Additionally, close monitoring is mandated for patients with pre-existing cardiac disease or risk factors for heart failure.

What should I know about interactions with other medicines?

Glivec (Imatinib) interacts with numerous other medicinal products by affecting certain Cytochrome P450 (CYP) enzymes and the P-glycoprotein (P-gp) transporter. Imatinib is primarily metabolized by CYP3A4, and is also an inhibitor of CYP3A4, CYP2D6, CYP2C9, and CYP2C19.

Interacting Medicines and Products

Interaction Type Examples (Specific Drugs or Classes) Regulatory Constraint/Requirement
Decreased Imatinib Levels (Avoid) Strong CYP3A4 Inducers (e.g., rifampicin, phenytoin, carbamazepine, St. John's wort) Avoid concomitant use as these decrease imatinib exposure, risking loss of effectiveness.
Increased Imatinib Levels (Use Caution) Potent CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole, erythromycin) Use with caution; may require a dose reduction for imatinib.
Increased Co-administered Drug Levels Warfarin, Cyclosporine, Pimozide, Dihydropyridine Calcium Channel Blockers, certain HMG-CoA Reductase Inhibitors (e.g., simvastatin), Digoxin Requires close monitoring and potential dose reduction for the co-administered drug. For Warfarin, INR must be frequently monitored.
Reduced Efficacy of Co-administered Drug Hormonal Contraceptives that are CYP3A4 substrates May lead to lower exposure and possible reduced effectiveness of the contraceptive; non-hormonal contraception may be required.

These documented interactions are based on Glivec's ability to inhibit these metabolic enzymes, which increases the concentration of many co-administered medicines, or on its own metabolism being accelerated by enzyme-inducing agents. This profile strictly dictates specific monitoring and dose modification rules for co-administered products, or outright avoidance of certain combinations.

Mechanism of Action

Targeted Inhibition of Oncogenic Kinases

Glivec's mechanism involves competitive inhibition of specific, constitutively active enzymes belonging to the tyrosine kinase family, primarily the BCR-ABL fusion protein and mutated c-KIT and PDGFR kinases. The active ingredient, Imatinib, binds to the ATP-binding pocket of these enzymes, locking them into an inactive conformation and directly preventing phosphorylation.

Blockade of Aberrant Signal Transduction

This molecular interaction engages the cellular machinery to interrupt the continuous, dysregulated "grow and survive" signals transmitted by the faulty kinases to the cell nucleus. By preventing the phosphorylation cascade, Imatinib essentially switches off the proliferation signal within the cell, which alters the downstream signaling profile and produces a state of functional inactivation within the target pathways.

Selective Suppression of Proliferative Activity

The ultimate physiological effect is the cessation of abnormal cell proliferation and the initiation of programmed cell death (apoptosis) in cells entirely dependent on the inhibited kinase. This core mechanism acts to dismantle the underlying molecular fault that drives the excessive cell growth, which constitutes the final cellular consequence of the kinase inhibition.

Dosage and Administration Information

How to Use Glivec (Imatinib Mesylate)

Glivec is an oral medication, administered via film-coated tablets, with use defined by specific parameters regarding dose, frequency, and administration conditions.


Official Administration Guidelines

The standard instruction for taking Glivec is that it must be taken with a meal and a large quantity of fluid, specifically a large glass of water. This requirement is part of the proper use of the medication. The tablets should generally be swallowed whole, but for patients who cannot, they may be dispersed in a glass of water or apple juice and consumed immediately.

Dosing Patterns and Frequency

Administration is typically once daily (QD) for doses up to and including 600 mg per day. Total daily doses of 800 mg are administered as a divided dose (400 mg taken twice daily, morning and evening). Starting doses vary by clinical context, ranging from 100 mg to 600 mg daily. The total course of treatment is usually continuous and long-term, but a specific duration of 36 months is defined for its use in the adjuvant setting for Gastrointestinal Stromal Tumors (GIST).

Population-Specific Instructions

Specific protocols apply to certain patient groups. For pediatric patients, dosing is calculated based on Body Surface Area (mg/m^2), not to exceed 600 mg daily. Furthermore, a 25% reduction in the initial starting dose is specified for adult patients with documented severe hepatic impairment (liver dysfunction).

In the event a dose is missed, the standard procedure is that the missed dose should not be taken, and the user should proceed with the next scheduled dose at the usual time.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Glivec

The clinical evaluation of Glivec (Imatinib Mesylate) has involved research, primarily focusing on its role in certain cancers and rare blood disorders. This overview describes the types of studies that have been conducted and the specific outcomes they were designed to measure, according to authoritative research sources.


Evidence for use in Chronic Myeloid Leukemia (CML)

The research foundation for Glivec in Philadelphia chromosome positive (Ph+) Chronic Myeloid Leukemia (CML) includes numerous studies. Initial evaluation relied on large, long-term Randomized Controlled Trials (RCTs). These studies were designed to compare Glivec against another therapeutic approach (a combination of interferon-alpha and cytarabine) in adults newly diagnosed with CML in the chronic phase.

Researchers examined key outcomes, including the disease’s characteristic measurements. The studies monitored hematologic response (how blood cell counts evolve), cytogenetic response (tracking the presence of the abnormal Philadelphia chromosome), and molecular response (monitoring the level of the BCR-ABL gene transcript).

The findings described patterns related to the presence of specific levels of molecular and cytogenetic response in the studied populations. Key trials reported on these measurements across the follow-up, with the longest studies reporting on outcomes tracked for a median of over 10 years. This evidence describes the observation of outcomes across the full duration of follow-up.


Evidence for use in Gastrointestinal Stromal Tumors (GIST)

The research for Glivec in Gastrointestinal Stromal Tumors (GIST) has been conducted across two main clinical situations: advanced, unresectable disease and following surgery for certain patients.

For advanced or metastatic GIST, the initial evidence was derived from Phase 2 single-arm trials. These studies focused on tracking tumor response, primarily measuring the reduction in tumor size (Objective Response Rate) in patients. Research explored how these outcomes varied in cohorts defined by specific tumor gene mutations, such as those involving KIT exon 11. Findings described the evolution of tumor size measurements in the observed populations.

Research for use in patients following certain types of surgery comes from Randomized Controlled Trials (RCTs). These RCTs compared the outcomes of using Glivec for different durations (such as 1 year versus 3 years) against observation alone. The studies tracked Relapse-Free Survival (RFS) and Overall Survival (OS). Studies tracked Relapse-Free Survival when comparing observed durations of Glivec use (e.g., three years) to other periods or observation.


Gaps and Areas of Ongoing Research

While Glivec is supported by extensive research, certain areas of investigation remain active and characterize the current limits of the evidence base:

  • Optimal Duration of Therapy: For GIST, research is ongoing to fully characterize the outcomes of using Glivec for periods longer than three years following surgery.
  • Stopping Treatment: For CML patients who achieve very deep molecular responses, evidence is limited regarding the observation of outcomes when discontinuing Glivec therapy.
  • Long-Term Effects: Ongoing research continues to monitor and describe all potential non-hematologic health patterns tracked in patients who have been observed for more than a decade.

Key Studies & References

  1. Imatinib in Chronic Myeloid Leukemia: an Overview (Reference to IRIS Trial and Key Outcomes)
  2. Adjuvant therapy for primary GIST: is longer really better? A narrative review (Refers to 10-year follow-up data for SSGXVIII/AIO Trial)

Frequently Asked Questions (FAQ)

Common questions about Glivec (FAQ)


Q: What is the difference between Glivec and generic imatinib?

Glivec is the brand name established internationally for the medicine. The active ingredient, which performs the therapeutic action, is called imatinib mesylate. Official documents define imatinib mesylate as the active substance found in the Glivec product.


Q: Are there different strengths of Glivec tablets available?

Yes, Glivec is available in different strengths of film-coated tablets. According to the official prescribing information, the medicine is available in 100 mg and 400 mg tablet strengths.


Q: What kind of stomach issues are associated with taking Glivec?

Official product information lists common gastrointestinal side effects such as nausea, vomiting, and diarrhea. Less common but serious adverse reactions have also been reported, including stomach bleeding (haemorrhage) or perforation of the gastrointestinal tract.


Q: Does Glivec interact with over-the-counter pain relievers like ibuprofen?

Glivec is a known inhibitor of certain liver enzymes, such as CYP2C9, which are responsible for processing other drugs. Because of this, Glivec may increase the blood levels of other medicines metabolized by these enzymes. The prescribing information describes the need for caution when used with certain drug classes.


Q: Does Glivec interact with common supplements like Vitamin D or multivitamins?

Official documentation highlights the importance of discussing supplements that affect the CYP3A4 enzyme system. For instance, the herbal product St. John's wort is strictly contraindicated because it significantly decreases the blood levels of Glivec.


Q: What are the specific risks associated with taking Glivec during pregnancy?

Based on regulatory data, Glivec can cause fetal harm if used during pregnancy. Reports in women have included instances of spontaneous abortions and congenital anomalies in infants. Due to these documented risks, the regulatory label specifies that effective contraception should be used during treatment and for a period afterward.


Q: Why are people sometimes concerned about fluid retention in the face or ankles?

Fluid retention, or oedema, is a very common side effect documented in official safety information. It frequently appears as swelling around the eyes (periorbital oedema) and can also cause swelling in the legs and ankles.


Q: What is the connection between Glivec and bleeding risk?

Glivec is associated with haematological toxicities, which are conditions affecting the blood, including a decrease in platelets (thrombocytopenia). This reduction in platelets can increase the risk of bleeding. Gastrointestinal haemorrhage is also listed as an uncommon adverse reaction in the official safety profile.


Q: Is Glivec related to drugs used for rheumatoid arthritis?

Glivec is classified as a Protein-Tyrosine Kinase Inhibitor (TKI). This is a class of targeted medicines that includes other therapies approved for the treatment of various conditions, including certain inflammatory diseases like rheumatoid arthritis.


Q: Is Glivec considered a first-line treatment for its main indication?

Glivec is approved for use in newly diagnosed adult and pediatric patients with chronic phase Philadelphia chromosome positive Chronic Myeloid Leukemia (Ph+ CML). This indicates its intended use in newly diagnosed populations.


Q: What is the scientific basis for Glivec’s targeted mechanism?

The targeted action of Glivec is based on its selective inhibition of specific faulty enzymes, such as the BCR-ABL fusion protein (in CML) and mutated c-KIT or PDGFR (in GIST). This inhibitory activity acts to dismantle the underlying molecular fault that drives the excessive cell growth.


Q: Why is the dosage sometimes different for children compared to adults?

Dosing for pediatric patients is calculated based on Body Surface Area ( mg/m^2), rather than a fixed standard dose. This is a common and established method used to determine the appropriate drug exposure for children.


Q: Does Glivec cause hair loss?

Yes, alopecia (hair loss) is listed in official product information as a common adverse reaction. It is one of the many effects documented in the drug's safety profile.


Q: Is Glivec safe for people with kidney disease?

Glivec should be used with caution in patients with existing kidney disease (renal impairment). The regulatory guidance states that close monitoring of renal function is advised during treatment, as the medicine's effects may be increased.


Q: Are there any common foods or drinks that interact with Glivec?

The official regulatory information explicitly advises that the consumption of grapefruit and grapefruit juice should be avoided during treatment. This is because these products can increase the blood levels of Glivec.


Q: Why is the drug used for certain types of gastrointestinal tumors?

Glivec is used for Gastrointestinal Stromal Tumors (GIST) because it targets and inhibits specific proteins, such as c-KIT (CD117), that are responsible for driving the growth of these tumors. This targeted approach aims to interrupt the signaling pathways that cause the cells to proliferate.


Q: Is Glivec used to treat anything other than cancer?

Yes, Glivec is approved for the treatment of certain non-cancerous diseases in adults. These indications include specific forms of Hypereosinophilic Syndrome (HES) and Chronic Eosinophilic Leukemia (CEL) that involve a fault in the PDGFR gene.


Q: What happens if Glivec treatment is stopped?

Regulatory studies and official information state that treatment with Glivec is generally continuous and long-term. Research is ongoing to better characterize the observation of outcomes for CML patients who discontinue therapy after achieving a deep response, and treatment decisions are made by healthcare professionals based on individual patient assessment.


Q: Do I need special monitoring while taking Glivec?

Yes, regular monitoring is described in regulatory guidance. This typically includes check-ups, regular blood tests (such as Complete Blood Count/CBC), weight checks, and monitoring of liver enzymes and kidney function throughout therapy.


Q: How often are blood tests usually needed when taking Glivec?

Official prescribing information states that a Complete Blood Count (CBC) is generally performed weekly during the first month of therapy. Testing is then done biweekly during the second month, and periodically thereafter.


Q: Is it true that Glivec can be used for hypereosinophilic syndrome?

Yes, Glivec is an approved treatment for adult patients with hypereosinophilic syndrome (HES) who have the FIP1L1-PDGFRalpha fusion kinase. This is a specific non-cancer indication documented in regulatory labeling.


Q: What is the risk of skin reactions while taking Glivec?

Skin reactions, including a rash, are a very common adverse reaction documented in the official safety profile. More serious, but rare, skin reactions such as Stevens-Johnson Syndrome have also been reported.


Q: What are the official restrictions for using Glivec in older patients?

While there are no absolute contraindications based on age alone, official safety notes specify that older adults may experience a higher incidence of oedema (fluid retention). Specific caution and monitoring are documented in regulatory guidance when the medicine is used in this population.


Q: Is there a chance that the body becomes resistant to Glivec over time?

Regulatory research has investigated mechanisms of resistance in CML cells. The development of resistance to tyrosine kinase inhibitors is a known factor that may affect the progression of the disease.


Q: Why are there warnings about thyroid function with Glivec?

Warnings about thyroid function are documented, specifically regarding the reporting of hypothyroidism (underactive thyroid) in certain patients. This concern is noted especially in those who have had a thyroidectomy and are receiving thyroid hormone replacement therapy.


Q: Are there any specific dietary restrictions required for people taking Glivec?

The official regulatory information only notes one specific food restriction: the avoidance of grapefruit and grapefruit juice, which can increase the blood levels of the drug. Glivec is also officially administered with a meal and a large glass of water, as described in the instructions for use.


Q: Are there specific side effects that require immediate medical attention?

Yes, specific symptoms of serious adverse reactions are noted as needing immediate medical attention. These include signs of severe liver problems (e.g., yellowing of the skin/eyes), unusual bleeding/bruising, severe abdominal pain, and rapid, unexpected weight gain (a sign of severe fluid retention).


Q: Does Glivec affect the ability to drive or use machines?

Glivec may cause side effects such as dizziness, blurred vision, or drowsiness. Patients are advised in the regulatory information to exercise caution when driving or operating machinery until they know how the medicine affects them.


Q: What are the known potential effects of Glivec on bone health?

Official safety data lists muscle and bone pain as a common side effect of Glivec. Additionally, growth retardation has been reported in children and pre-adolescents receiving treatment due to the medicine's effect on developing tissues.

How should Glivec be stored and disposed of?

Glivec (imatinib mesylate) tablets must be stored strictly according to regulatory guidelines to ensure product stability and safety. The required storage environment is controlled room temperature, specifically between 20 C and 25 C (68 F to 77 F), with excursions up to 30 C permitted. The tablets must be kept in the original container and protected from moisture.

Official Storage and Handling Requirements

Scope Item Required Condition
Temperature Controlled Room Temperature (20 C–25 C)
Protection Store in original container; protect from moisture
Child Safety Keep out of the sight and reach of children
Prepared Dose Consume solution immediately if dissolved in liquid

Disposal Requirements

Disposal must adhere to local regulations for pharmaceutical waste and cytotoxic agents. Glivec tablets should not be disposed of in household trash or flushed down the toilet, as this violates specific environmental restrictions documented in the prescribing information. Patients must contact their healthcare provider for instructions on disposing of unused medication.

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

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