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Gleevec

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Gleevec (imatinib) is a targeted therapy known as a tyrosine kinase inhibitor used to treat certain types of leukemia and gastrointestinal stromal tumours. It helps patients by blocking the abnormal proteins that signal cancer cells to multiply. This action assists in slowing or stopping the progression of the disease.


Ingredient
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Imatinib
Reference Brand
Glivec
Manufacturer
Novartis
Product Form
Tablet, Capsule
Regulatory Classification
Rx
Primary Category
Cancer Treatment
Product Category
Antineoplastic Agents, Protein Kinase Inhibitors
Pharmacological Class
Tyrosine Kinase Inhibitor
Manufacturer Description
A breakthrough targeted cancer therapy used to manage various types of leukaemia and digestive system tumours.
Mechanism of Action
Glivec works by blocking a specific abnormal enzyme (BCR-ABL tyrosine kinase) that signals cancer cells to multiply. By shutting down this 'switch,' it stops the growth of white blood cells in certain types of leukaemia and helps destroy tumour cells in GIST.
Route of Administration
Oral
Onset Time
Varies; several weeks for initial response
Duration
Continuous daily dosing
Contraindications
Hypersensitivity to imatinib
Severe Adverse Events
Severe neutropenia (low white cells), Liver toxicity, Gastrointestinal bleeding, Heart failure
Common Side Effects
Nausea, Muscle cramps, Eyelid swelling, Diarrhoea
Uncommon Side Effects
Fluid retention (oedema), Skin rash, Headache, Fatigue
Drug Interactions
Paracetamol, Warfarin, Ketoconazole, St John's Wort
Pregnancy Safety Warnings
Not recommended; effective contraception is mandatory.
Age Restrictions
Suitable for both adults and children.
Storage Guidelines
Store at room temperature in original packaging.
Related Products
Dasatinib, Nilotinib, Bosutinib

Gleevec FAQ

Can I travel internationally with Gleevec tablets?

Yes, you can travel with Gleevec, but keep the medication in its original labeled container, carry a copy of the prescription, and declare it at customs if required. It is advisable to bring a supply that will last at least the duration of your trip plus a few extra days.

Will Gleevec show up on a drug test for work or sports?

Imatinib is not a prohibited substance in most occupational drug-testing programs or in standard anti-doping panels. However, specific sports organisations may have their own regulations; athletes should check the latest World Anti-Doping Agency (WADA) list.

What do the imprinted numbers on the tablet mean?

The 100 mg tablets are typically imprinted with “100 IM” and the 400 mg tablets with “400 IM”. These markings help pharmacists and patients verify the strength of the medication.

Are there differences in Gleevec tablets sold in the UK versus other countries?

Formulation (imatinib mesylate) and tablet strengths are generally consistent worldwide, but packaging, excipients, and labeling may vary to meet local regulatory requirements. Always use the product supplied by UK pharmacies.

Can I take Gleevec with my herbal supplement St John’s wort?

St John’s wort induces CYP3A4 and can lower imatinib concentrations, potentially reducing its effectiveness. Discuss any herbal products with your oncologist before combining them.

How long can I store an opened bottle of Gleevec?

Tablets remain stable until the expiry date indicated on the pack, provided they are stored at room temperature in a dry place. Do not use tablets that appear discolored or have an unusual odor.

What should I do if I experience severe skin rash while on Gleevec?

A severe or spreading rash may signal a hypersensitivity reaction. Contact your healthcare provider promptly; they may pause treatment and prescribe antihistamines or corticosteroids, or consider an alternative therapy.

Is dose reduction ever needed for older adults?

Age alone does not dictate dose reduction, but older patients often have concurrent liver or kidney disease that may require a lower dose. Dose adjustments are guided by organ function and tolerability, not chronological age.

Why are there both 100 mg and 400 mg tablets if the usual dose is 400 mg?

The 100 mg tablets provide flexibility for clinicians to tailor the dose for patients who need lower amounts due to toxicity, drug interactions, or organ impairment. They also allow split dosing in rare circumstances where divided doses are preferred.

What is Gleevec?

Gleevec is a brand-name medication whose active ingredient is imatinib. It belongs to the oncology support class of drugs and is supplied as oral pill tablets in strengths of 100 mg and 400 mg. In the United Kingdom Gleevec is a prescription-only medicine (POM) regulated by the Medicines and Healthcare products Regulatory Agency (MHRA). It is used under the supervision of a qualified oncology specialist.

How Imatinib Works in the Body

Imatinib is a tyrosine-kinase inhibitor (TKI). It blocks the activity of specific enzymes that signal cells to grow and divide. The most important targets are:

  • BCR-ABL - an abnormal enzyme produced by the Philadelphia chromosome in chronic myeloid leukaemia (CML).
  • c-KIT and PDGFR - receptors that are over-active in gastrointestinal stromal tumours (GIST) and some other solid cancers.

By occupying the ATP-binding site of these enzymes, imatinib prevents them from phosphorylating downstream proteins. This halts uncontrolled cell proliferation and can trigger cancer cell death. The drug is absorbed well from the gastrointestinal tract; peak plasma concentrations are typically reached within 2-4 hours after a dose, and the half-life is about 18 hours, supporting once-daily dosing.

Conditions Treated with Gleevec

In the UK, Gleevec is approved for the following indications:

  • Chronic myeloid leukaemia (CML) in chronic or accelerated phase, and for patients who have previously received interferon-α therapy.
  • Adult gastrointestinal stromal tumours (GIST) that are unresectable, metastatic, or recurrent, provided the tumour expresses a KIT exon 11 mutation or an appropriate PDGFR mutation.

These approvals are based on large, randomised clinical trials that demonstrated improved survival and disease control compared with earlier therapies. Gleevec is prescribed by oncologists and haematologists experienced in managing these cancers.

Evidence-Based Off-Label Uses

Research studies have explored imatinib in other malignancies that involve similar tyrosine-kinase pathways, for example:

  • Philadelphia chromosome-positive acute lymphoblastic leukaemia (Ph-positive ALL) - controlled trials have shown benefit when imatinib is combined with standard chemotherapy.
  • Systemic mastocytosis - case series report symptom improvement due to inhibition of KIT.

These uses are not approved by the MHRA for Gleevec. Off-label prescribing requires a thorough risk-benefit assessment by a specialist and informed consent from the patient.

Who Should (and Should Not) Use Gleevec?

Ideal Patient Profile

  • Adults diagnosed with CML or GIST who meet the molecular or genetic criteria for imatinib therapy.
  • Patients with adequate hepatic and renal function (see dosing adjustments below).

Absolute Contraindications

  • Known hypersensitivity to imatinib or any of the tablet excipients.
  • Pregnancy (imatinib is classified as pregnancy category D in the UK; it may cause fetal harm).
  • Severe hepatic impairment (Child-Pugh Class C).

Relative Contraindications & Precautions

  • Moderate hepatic dysfunction - dose may need reduction; monitor liver enzymes.
  • Renal impairment (creatinine clearance <30 mL/min) - consider dose adjustment and close monitoring.
  • Concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) - may increase imatinib plasma levels, raising toxicity risk.
  • Concomitant use of strong CYP3A4 inducers (e.g., rifampicin, carbamazepine) - may reduce efficacy.

Special Populations

  • Breast-feeding mothers: Imatinib is excreted in milk; discontinuation of breast-feeding is advised.
  • Elderly patients: No dose reduction is required solely based on age, but comorbidities and organ function should be assessed.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Swelling of the hands, feet, or face (peripheral oedema) - often mild and self-limiting.
  • Nausea or mild gastrointestinal upset.
  • Muscle cramps or weakness.
  • Skin rash or mild itching.
  • Fatigue or low-grade fever.

These effects are usually manageable with supportive care and dose timing adjustments.

Serious Adverse Events

  • Hepatotoxicity - elevated transaminases; may progress to hepatitis. Prompt liver-function monitoring is essential.
  • Neutropenia and thrombocytopenia - increased infection risk; regular full-blood-count (FBC) checks are required.
  • Cardiac toxicity - rare cases of heart failure and QT-interval prolongation have been reported; baseline ECG may be advisable for patients with cardiac history.
  • Pancreatitis - severe abdominal pain with raised pancreatic enzymes; immediate medical attention required.

Drug Interactions

  • CYP3A4 inhibitors (e.g., azole antifungals, macrolide antibiotics) can raise imatinib levels → consider dose reduction.
  • CYP3A4 inducers (e.g., phenytoin, St John’s wort) may lower concentrations → monitor response, possibly increase dose.
  • Warfarin - imatinib may enhance anticoagulant effect; INR should be checked more frequently.
  • Quinidine - can increase plasma imatinib; watch for toxicity.

Food and Lifestyle Interactions

  • Imatinib may be taken with or without food; a high-fat meal can slightly delay absorption but does not affect overall exposure.
  • Alcohol should be limited, especially in patients with liver disease.
  • No specific restrictions on driving, but severe fatigue or dizziness warrants caution.

Safety Note: Patients should disclose all medicines, supplements, and herbal products to their treating clinician before starting Gleevec.

How to Take Gleevec

Standard Dosing

  • Chronic myeloid leukaemia (CML) - 400 mg taken once daily (one 400 mg tablet).
  • Gastrointestinal stromal tumour (GIST) - 400 mg taken once daily (one 400 mg tablet).

If a 400 mg tablet is not tolerated, the dose can be divided using the 100 mg tablets (e.g., four 100 mg tablets once daily).

Dose Adjustments

  • Mild to moderate hepatic impairment - consider reducing the daily dose to 300 mg; monitor liver function tests every 2-4 weeks.
  • Severe hepatic impairment - avoid use; if essential, start at 100 mg daily and evaluate response closely.
  • Renal impairment (CrCl < 30 mL/min) - start with 300 mg daily; monitor renal function and complete blood counts.

Administration Tips

  • Swallow the tablet whole with a glass of water.
  • Do not crush, chew, or split the tablets unless instructed by a pharmacist.
  • Take the same dose at the same time each day to maintain steady blood levels.

Missed Dose

  • If you remember the missed dose within 12 hours, take it.
  • If the next scheduled dose is due, skip the missed dose - do not double-dose.

Overdose

  • Symptoms may include severe nausea, vomiting, diarrhoea, dizziness, or low blood pressure.
  • Seek emergency medical care; activated charcoal may be considered if presentation is early. There is no specific antidote.

Discontinuation

  • For CML, abrupt cessation can lead to disease flare; a gradual taper is not usually required, but the decision must be made by the oncology team.
  • For GIST, stopping the drug may cause rapid tumour progression; discuss any change of therapy with your doctor.

Monitoring and Follow-Up

  • Baseline assessments before starting therapy: complete blood count (CBC), liver function tests (ALT, AST, bilirubin), renal profile, and, where appropriate, a baseline ECG.
  • During treatment: CBC and liver enzymes every 2-4 weeks for the first 3 months, then every 3 months if stable.
  • Molecular monitoring (BCR-ABL transcript levels) in CML is performed by specialised laboratories to gauge response.
  • Imaging (CT or MRI) for GIST disease assessment at intervals recommended by the treating oncologist.

Patients should contact their healthcare provider promptly if they experience fever, unusual bruising, persistent nausea, jaundice, or any new cardiac symptoms.

Storage and Handling

  • Store tablets at room temperature (15-25 °C) away from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use tablets after the expiry date printed on the package.
  • Unused medication should be returned to a pharmacy for safe disposal; do not flush down the toilet.

Medication-Specific Glossary

Tyrosine-Kinase Inhibitor (TKI)
A class of drugs that block enzymes (tyrosine kinases) involved in signalling pathways that promote cancer cell growth.
BCR-ABL
An abnormal fusion protein with constitutive tyrosine-kinase activity, produced by the Philadelphia chromosome translocation in CML.
c-KIT
A receptor tyrosine kinase that, when mutated, drives the development of many gastrointestinal stromal tumours.
Therapeutic Window
The range of drug concentrations in which efficacy is achieved without unacceptable toxicity; for imatinib, careful monitoring helps stay within this window.

Medical Disclaimer

This article provides educational information about Gleevec (imatinib) and is not a substitute for professional medical advice. Treatment decisions, including the use of the medication for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Gleevec is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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