Imatis

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Medically reviewed

Rosario Oropesa

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 Imatis

Understanding Imatis

Imatis is a medication classified as a tyrosine kinase inhibitor (TKI). It is used primarily in the treatment of specific types of blood cancers and gastrointestinal tumors. The medication works by targeting and blocking the action of abnormal proteins that signal cancer cells to multiply, thereby helping to slow or stop the progression of the disease.

Mechanism of Action

In many cases where Imatis is prescribed, the body produces an abnormal enzyme known as Bcr-Abl. This enzyme is the result of a genetic translocation—often referred to as the Philadelphia chromosome—which causes certain white blood cells to grow uncontrollably. Imatis binds to the site of this enzyme and prevents it from sending the chemical signals required for cell division.

By focusing on these specific molecular markers, the treatment falls under the category of targeted therapy. Unlike traditional treatments that may affect all rapidly dividing cells, targeted therapies are designed to interfere with specific molecules involved in the growth and survival of cancer cells.

Primary Uses

Imatis is commonly utilized in the management of several conditions, including:

  • Chronic Myeloid Leukemia (CML): A type of cancer that begins in the bone marrow and affects the white blood cells.
  • Acute Lymphoblastic Leukemia (ALL): A fast-growing blood cancer involving specific subtypes that express the Philadelphia chromosome.
  • Gastrointestinal Stromal Tumors (GIST): A rare form of cancer that originates in the walls of the digestive tract.
  • Myelodysplastic or Myeloproliferative Diseases: A group of conditions where the bone marrow produces an excess of certain white blood cells.
  • Hypereosinophilic Syndrome (HES): A condition characterized by a persistently high number of eosinophils (a type of white blood cell) in the blood.

What side effects are possible with Imatis?

Possible Side Effects and Safety Information

The safety profile of Imatis (Imatinib mesilate) is defined by official regulatory documentation, classifying potential adverse reactions by frequency and the body system affected. These classifications distinguish between common physical manifestations and documented serious events.


Frequency and System-Organ Classes

The most frequently reported (Very Common, affecting more than 1 in 10 patients) adverse reactions include fluid retention (edema), gastrointestinal disturbances (nausea, vomiting, diarrhea, abdominal pain), fatigue, musculoskeletal pain, headache, and certain hematological changes (neutropenia, thrombocytopenia, and anemia). These events generally occur most often during the initial stages of therapy.

Reactions are classified into System-Organ Classes such as Blood and Lymphatic System Disorders, Gastrointestinal Disorders, Musculoskeletal and Connective Tissue Disorders, and Metabolism and Nutrition Disorders.


Serious Adverse Reactions

The official label documents the potential for serious adverse reactions, which include severe congestive heart failure and left ventricular dysfunction, severe hepatotoxicity (liver damage that can be fatal), and severe gastrointestinal perforations and hemorrhage. Severe bullous dermatologic reactions are also documented safety concerns.


Population-Specific and Time-Related Safety

Safety constraints apply to specific populations. The label notes reports of growth retardation in children and adolescents. Patients with pre-existing hepatic or renal impairment require close monitoring, and the use during pregnancy is associated with documented potential fetal harm. Regarding duration, while most acute events appear early, regulatory documents highlight specific safety concerns related to long-term exposure, primarily involving cardiac, hepatic, and renal function. Certain situations, such as the risk of Hypereosinophilic Cardiac Toxicity, are also noted as specific constraints.

Overdose and Emergency Response

Overdose and When to Seek Help

Documented Overdose Manifestations Official prescribing information documents that overdose of Imatinib has been associated with severe manifestations across multiple physiological systems. Documented clinical signs include prominent gastrointestinal symptoms (nausea, vomiting, diarrhea, abdominal pain), systemic effects (fever, edema, rash, fatigue, headache), and hematological toxicities such as myelosuppression. Case reports in the pediatric population show manifestations consistent with those observed in adults.

Severe and Life-Threatening Outcomes Regulatory authorities specifically list the potential for severe, life-threatening outcomes, particularly following prolonged high-dose exposure. These include severe hepatic failure (liver damage with elevated transaminases), acute renal failure (kidney damage), and dose-related cardiac effects, such as decreased left ventricular function. Gastrointestinal hemorrhage has also been documented.

Required Emergency Actions and Management Due to the risk of severe complications, the official mandate is to seek immediate medical attention or contact a Poison Control Center right away upon any suspected overdose. The regulatory profile confirms that no specific antidote is known for Imatinib. Management is strictly symptomatic and supportive, and hospitalization with close monitoring of the patient's condition is required. Monitoring must include regular checks of hematological parameters and liver function tests.

Therapeutic Uses of Imatis

Quick Facts About Imatis

  • Chronic Myelogenous Leukemia (CML): Used in the management of this condition.
  • Gastrointestinal Stromal Tumors (GIST): Employed in the treatment of specific GIST cases.
  • Acute Lymphoblastic Leukemia (ALL): Included in regimens to manage this type of leukemia.
  • Other Conditions: The medication is also utilized for certain other rare malignancies and myelodysplastic/myeloproliferative diseases.

Imatis is a medication indicated for the management of specific types of cancer. Its therapeutic domain primarily covers Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) in different phases. The drug may support the process of achieving hematologic and cytogenetic responses in adult and pediatric patients with newly diagnosed or advanced CML.

This medication is also employed in the treatment plan for specific forms of gastrointestinal stromal tumors (GIST) that are Kit-positive (CD117+). It is used following the surgical removal of the tumor in an adjuvant setting and for cases that are unresectable or have metastasized.

Additionally, Imatis is included in combination regimens for the management of Philadelphia chromosome-positive acute lymphoblastic leukemia (ALL) and for certain forms of myelodysplastic/myeloproliferative diseases and hypereosinophilic syndrome. Patients should follow the guidance of their oncology specialist to determine the appropriate use and therapeutic goal for their condition.

Eligibility and Restrictions for Use

This section outlines the official population eligibility and non-eligibility for Imatis (Imatinib), based strictly on regulatory documents.

Contraindicated Populations

Imatis is contraindicated for patients with a known hypersensitivity to the active substance, imatinib, or to any of the drug's excipients.


Conditional Use and Restrictions

Use is restricted or requires special caution and monitoring for specific groups, often necessitating dose adjustments:

  • Hepatic Impairment: Patients with pre-existing mild, moderate, or severe liver impairment require a dose reduction as per the regulatory label, and liver function must be closely monitored.
  • Renal Impairment: Patients with moderate kidney impairment are typically started at a mathbf50% reduced dose. Doses above a certain limit (e.g., 400 mg/day) are generally not recommended for this group.
  • Cardiac Risk: Patients with a history of cardiac disease or risk factors for heart failure should be carefully monitored.

Age and Reproductive Status

  • Pediatric Use: Use is established for certain indications in children and adolescents, typically 1 year of age and older. Safety and efficacy are not established in children younger than 1 year of age.
  • Pregnancy: Imatis can cause fetal harm; therefore, it is not recommended during pregnancy, and females of reproductive potential must use effective contraception.
  • Lactation (Breastfeeding): Breastfeeding is not recommended during treatment.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile of Imatis (Imatinib mesilate) is primarily defined by its effects on drug metabolism and transport, as documented in official regulatory labeling. Imatinib is mainly metabolized by the CYP3A4 enzyme and is a potent inhibitor of both CYP3A4 and the drug transporter P-glycoprotein (P-gp).

Pharmacokinetic Interaction Patterns

Substance Category Imatinib Exposure Effect Mechanism & Outcome
Strong CYP3A4 Inhibitors (e.g., Ketoconazole) Increased Imatinib plasma concentration (up to 40% in AUC) Imatinib metabolism is reduced, requiring caution.
Strong CYP3A4 Inducers (e.g., Rifampicin, St. John's Wort) Decreased Imatinib plasma concentration (up to 74% in AUC) Imatinib metabolism is accelerated, leading to loss of efficacy and is contraindicated.
CYP3A4/P-gp Substrates (e.g., Simvastatin, Cyclosporine) Increased Co-drug plasma concentration Imatinib inhibits the clearance of the co-administered drug, necessitating restrictions.

Regulatory Restrictions and Conditions

Certain combinations are formally contraindicated by regulatory authorities, specifically with strong CYP3A4 inducers like rifampicin and with the substrate Simvastatin. Additionally, Imatinib is officially required to be administered with a meal and a large glass of water to mitigate documented gastrointestinal irritation. For patients with hepatic impairment, Imatinib systemic exposure is noted to be increased by approximately 50%, elevating the clinical significance of co-administration with other interacting agents.

Mechanism of Action

Selective Kinase Inhibition: The Core Mechanism

Imatis is a tyrosine kinase inhibitor (TKI). Its primary action is to bind competitively to the adenosine triphosphate (ATP) binding pocket of specific kinases, including the aberrant BCR-ABL fusion protein, c-Kit (CD117), and PDGFR (Platelet-Derived Growth Factor Receptor). This binding stabilizes the enzyme in an inactive conformation, halting the transfer of phosphate groups and thereby immediately suppressing pro-growth signaling activity dependent on these specific enzymes.


Modulating Signaling Cascades and Apoptosis

This molecular action halts the propagation of downstream signaling pathways, such as the PI3K/AKT and RAS/MAPK cascades, which typically promote cell survival and division. This suppression triggers programmed cell death (apoptosis) and cell cycle arrest in cells reliant on these dysregulated signals.


Physiological Regulation of Proliferation and Matrix Deposition

The inhibition of PDGFR and c-Kit addresses receptor-mediated signals that drive certain physiological processes. By blocking these signals, Imatis restricts the excessive proliferation of fibroblasts and associated matrix protein production, and also modulates the function of specific inflammatory cells.

Dosage and Administration Information

How to Use Imatis — Administration Guidelines

Imatis is an oral medicine that must be taken strictly according to the prescribed procedures.

Administration and Timing

Imatis must be taken once or twice daily at around the same time(s) every day. All doses must be taken with a meal and a large glass of water to help prevent stomach irritation. Common adult daily doses are 400 mg or 600 mg. A total daily dose of 800 mg must be administered as 400 mg twice a day (morning and evening). Pediatric dosing is based on body surface area, typically 340 mg/m^2/day, which may be given once daily or in two divided doses.

Preparation Requirements

Tablets must be swallowed whole and should not be crushed, chewed, or split. If a patient is unable to swallow the tablets whole, they may be dispersed in a glass of still water or apple juice.

Tablet Strength Minimum Liquid Volume
100 mg tablet 50 mL (a little less than 2 ounces)
400 mg tablet 200 mL (a little less than 7 ounces)

The mixture must be stirred until the tablet is completely disintegrated and drunk immediately. Oral solution, if used, must be measured with an accurate measuring device provided with the medication.

Missed Dose and Continuation

If a dose is forgotten, the missed dose should be taken as soon as it is remembered. If it is almost time for the next scheduled dose, the missed dose should be skipped, and the patient should continue the regular dosing schedule. A double dose must not be taken to make up for a missed one. Treatment should be continued for the prescribed duration and never stopped without explicit instruction from the treating physician.

Recent Clinical Evidence

Research Evidence: Overview of Studies for Imatis

This section summarizes the official clinical research and regulatory findings that supported the applications for Imatis, focusing on the types of studies conducted and the outcomes measured by researchers. Findings describe group patterns, not personal outcomes.


Evidence for Use in Chronic Myelogenous Leukemia (CML)

The clinical evaluation for Imatis in Philadelphia chromosome-positive (Ph^+) CML involved many studies, including large, international Randomized Controlled Trials (RCTs). These trials were primarily designed to compare Imatis with the standard treatments used before its introduction, such as interferon-alpha ( IFN-alpha).

Researchers examined outcomes related to molecular and cellular changes, including measurements of complete cytogenetic response (CCyR) and major molecular response (MMR). Long-term observational studies followed patients to monitor Overall Survival (OS) and Progression-Free Survival (PFS), where researchers tracked the time interval patients remained alive without their disease advancing to more severe phases.

Evidence for Use in Gastrointestinal Stromal Tumors (GIST)

The clinical evidence for Imatis in Gastrointestinal Stromal Tumors (GIST) is supported by several major Phase II and III Clinical Trials. These studies focused on two main patient groups: advanced GIST and those receiving treatment after surgery (adjuvant therapy).

In studies of advanced GIST, researchers examined the Objective Response Rate (ORR) and monitored PFS and OS. In the adjuvant setting, randomized trials focused on Recurrence-Free Survival (RFS), where researchers tracked the time interval patients remained without the disease returning. Trials documented RFS and OS measurements that differed when comparing a three-year duration to a one-year duration of treatment in high-risk GIST patients.

What Remains Under Research and Uncertain

One consistently noted limitation across both CML and GIST evidence is the eventual development of acquired resistance (secondary mutations) in a subset of patients over time, which may lead to a need to explore other treatment options. Research is still exploring the optimal protocols for patients in deep response to safely attempt Treatment-Free Remission (TFR) in CML. For rare conditions, sample sizes were modest, meaning there is limited information to characterize long-term, single-agent outcomes. The study results reflect the specific conditions under which they were conducted and research does not determine whether an individual will respond similarly.

Key Studies & References Imatinib: Mechanism of Action, Efficacy, and Clinical Use in CML and GIST (StatPearls)

Frequently Asked Questions (FAQ)

Common questions about Imatis (FAQ)


Q: Is Imatis considered a traditional chemotherapy medicine?

Imatis is categorized as a targeted therapy and a protein-tyrosine kinase inhibitor. This classification indicates that the medicine works by selectively blocking specific enzymes that promote cancer cell growth. Unlike traditional cytotoxic chemotherapy, which affects rapidly dividing cells generally, Imatis targets these particular enzymes.


Q: Is Imatis the same drug as the brand name Gleevec or Glivec?

The active ingredient in Imatis is Imatinib mesilate. This is the same active compound found in the original brand name product, which is known internationally by names like Gleevec or Glivec. Imatis is often a generic version of the originator brand.


Q: Is Imatis treatment generally for a short period or long-term?

According to official product information, Imatis treatment for most approved uses is generally considered a long-term therapy. It is typically continued until there are signs of disease progression or until a person experiences side effects that require treatment to stop.


Q: Is a skin rash or other skin reactions a common side effect of Imatis?

Yes, certain skin reactions are frequently reported. Official documents indicate that a maculopapular rash, which is a type of flat, red area covered with small bumps, is a very common side effect. This means it has been reported in more than 1 in 10 patients in clinical experience.


Q: Can Imatis interact with over-the-counter pain relievers or supplements?

Imatis is known to interact with the CYP3A4 enzyme system, which metabolizes many other drugs and supplements. Official regulatory information mentions that strong inducers like St. John's Wort are contraindicated. An interaction with common pain relievers like acetaminophen is also noted as possible, suggesting that drug-drug interactions may be of clinical significance.


Q: Why are patients required to have regular blood tests while taking Imatis?

The requirement for regular blood tests is related to the possibility of certain adverse reactions documented in the official label. Imatis has been associated with changes in blood cell counts (hematologic toxicity) and potential liver damage (hepatotoxicity). These monitoring tests are conducted to evaluate a person's blood counts and liver function throughout treatment.


Q: What is the difference in action between Imatis and traditional cytotoxic drugs?

Imatis is a targeted therapy that works by selectively blocking the activity of specific enzymes (tyrosine kinases), like Bcr-Abl, that signal cells to grow and divide. Traditional cytotoxic drugs typically act more broadly by killing any rapidly dividing cells, including healthy ones, which is the main difference in their mechanism of action.


Q: Are there different doses or strengths of Imatis tablets used for different conditions?

Yes, the official regulatory labeling provides different recommended daily doses of Imatis based on the specific condition being treated. For instance, the starting dose for Chronic Phase CML may differ from the dose used for Accelerated Phase CML.


Q: Is Imatis treatment necessary even after disease symptoms have lessened?

Regulatory information notes that treatment is intended to be continued for the prescribed duration, and discontinuation should only occur under the guidance of a physician. This is based on maintaining control over the disease process.


Q: What type of research is currently being done on Imatis?

Official documents reference ongoing research focused on various aspects of Imatis use. These themes include monitoring long-term survival data and studying the feasibility of Treatment-Free Remission (TFR) protocols for patients who have achieved a deep molecular response. Studies are also conducted to evaluate outcomes in specific groups, such as children.


Q: Does Imatis have any effect on blood clotting or bruising?

Imatis has been associated with certain effects on the blood system. Regulatory documents report thrombocytopenia (low platelet count), which plays a role in clotting. In addition, serious hemorrhage (bleeding) events have also been documented in the official safety profile.


Q: Why is Imatis used to treat both blood cancers and some solid tumors?

The reason for this dual use lies in the drug's mechanism of action. Imatis is designed to block several key enzymes, including the BCR-ABL fusion protein found in some leukemias and the c-Kit or PDGFR receptors found in certain solid tumors like GIST. By inhibiting these specific targets, the drug can address different diseases driven by the same signaling pathways.


Q: Are there specific food or drink products known to interact with Imatis?

Official patient advice often states that grapefruit and grapefruit juice should be avoided while on treatment. This is because grapefruit can interfere with the way Imatis is metabolized, potentially leading to increased drug levels in the bloodstream.


Q: Can men or women on Imatis treatment still have children?

Regulatory information specifies that females of reproductive potential should use highly effective contraception during treatment due to the risk of fetal harm. Regarding men, while the regulatory label is primarily focused on women, animal data on reproductive toxicology are noted as being complex regarding male fertility.


Q: Are changes in hair or skin color a reported side effect of Imatis?

Yes, official post-marketing reports have documented pigmentary changes associated with Imatis. These changes may involve either hyperpigmentation (darkening) or hypopigmentation (lightening) of the skin or hair.


Q: Is it safe to consume alcohol while undergoing treatment with Imatis?

The official label for Imatis documents a risk of hepatotoxicity or liver damage. Given that alcohol consumption can also place stress on the liver, the official documents imply an area of clinical significance. Questions about alcohol should be directed to a healthcare provider.


Q: How long does it typically take to see the first signs of Imatis working?

Imatis is rapidly absorbed, with drug levels typically peaking in the blood within 2 to 4 hours of taking a dose. However, the signs of the medicine working are measured by changes in blood counts or molecular markers, known as hematologic response. This clinical response is usually evaluated by a physician over an interval of weeks or months.


Q: What is the general protocol for adjusting the Imatis dose if side effects occur?

Official regulatory labeling provides specific guidelines for managing certain side effects, such as low blood counts (hematologic toxicity). The protocol typically involves either a dose reduction or the temporary cessation of treatment until the adverse reaction improves.


Q: Can Imatis affect a person's ability to drive or operate machinery?

The regulatory label notes that Imatis has been associated with adverse reactions that may impair focus. Because documented reactions include dizziness, somnolence (drowsiness), and blurred vision, regulatory bodies recommend caution when performing complex tasks like driving or operating machinery.


Q: Does Imatis interact with common prescription medications for high blood pressure?

Imatis is a strong inhibitor of the CYP3A4 enzyme, which can affect the way many other prescription drugs are processed by the body. For example, some common calcium channel blockers used for high blood pressure are affected, which may lead to an increase in the concentration of that blood pressure medicine.


Q: Is depression or insomnia a reported side effect of Imatis?

Yes, official documents for adverse reactions list both insomnia (difficulty sleeping) and depression among the documented side effects that have been reported with Imatis.


Q: Why is Imatis sometimes used in combination with other chemotherapy drugs?

For certain specific conditions, the official regulatory label approves Imatis to be used in combination with chemotherapy. This is particularly noted for treating conditions like newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) in pediatric patients.


Q: Do patients with myelodysplastic syndrome (MDS) use Imatis?

Yes, Imatis is an approved treatment for adult patients who have myelodysplastic/myeloproliferative diseases (MDS/MPD) that are associated with specific gene rearrangements. This is based on regulatory approval for its use in these select groups.

How should Imatis be stored and disposed of?

Storage and Disposal of Imatis

Imatis (imatinib) must be stored under specific regulatory conditions to maintain its quality. The medication requires storage at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F).

Storage Requirements

The product must be kept in its original, tightly closed container to ensure protection from moisture and excess heat. The regulatory labeling strictly mandates that Imatis is stored out of the sight and reach of children and kept in a secure, locked area.

Disposal Instructions

For disposal of expired or unused Imatis, the drug take-back program is the officially recommended method. If a take-back option is unavailable, the product should be mixed with an undesirable substance (such as used coffee grounds) and placed in a sealed container before being thrown in the household trash. The medication must not be flushed down a toilet or drain.

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

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