Generic Gleevec ( Imatinib )

Gleevec

Gleevec (imatinib mesylate) is a tyrosine kinase inhibitor indicated for the treatment of Philadelphia chromosome‑positive chronic myeloid leukemia (CML) in chronic, accelerated, or blast phase, Philadelphia chromosome‑positive acute lymphoblastic leukemia, myelodysplastic/myeloproliferative diseases associated with platelet‑derived growth factor receptor gene rearrangements, aggressive systemic mastocytosis, hypereosinophilic syndrome, unresectable or metastatic gastrointestinal stromal tumours (GIST), and dermatofibrosarcoma protuberans. Imatinib works by selectively inhibiting the BCR‑ABL tyrosine kinase, the abnormal enzyme produced by the Philadelphia chromosome, as well as c‑KIT and platelet‑derived growth factor receptors. This blocks downstream signalling pathways that drive the uncontrolled proliferation of malignant cells.

Usual adult dose: For chronic phase CML, the recommended dose is 400 mg taken orally once daily with a meal and a large glass of water. For accelerated or blast phase CML, the dose is 600 mg once daily. For GIST, the dose is 400 mg once daily; in progressive disease, 400 mg twice daily may be considered. The tablets should be swallowed whole; they may be dispersed in a glass of water or apple juice if swallowing is difficult. The 100 mg tablet is used for dose reductions, paediatric dosing, and for patients intolerant to the 400 mg strength. Treatment continues as long as clinical benefit is observed and unacceptable toxicity does not occur. Dose modifications may be required for hematologic or hepatic toxicity. If a dose is missed, the patient should take the next dose at the usual time; two doses must not be taken on the same day. No dose adjustment is required in mild‑to‑moderate renal impairment; caution is advised in severe renal impairment. In hepatic impairment, dose reduction may be necessary.

Dosage form: Film‑coated tablets: 100 mg (orange‑brown, round, imprinted with "NVR" and "SA") and 400 mg (orange‑brown, oval, imprinted with "NVR" and "400"). Available in bottles or blister packs of 30, 60, or 90 tablets.

Onset of action: Hematologic response in chronic phase CML is typically observed within 1 to 2 months, with complete hematologic response achieved in up to 95% of patients within 3 months. Cytogenetic and major molecular responses develop more gradually, usually within 6 to 12 months of continuous therapy. For GIST, tumour shrinkage or stabilization may be seen within 2 to 3 months.

Duration of action: The elimination half‑life of imatinib is approximately 18 hours, with its major active metabolite having a half‑life of about 40 hours, supporting once‑daily dosing. The therapeutic effect is maintained with continuous daily treatment. Long‑term therapy is generally required to sustain remission; discontinuation can be considered only in selected patients with deep and sustained molecular response under specialist supervision.

Alcohol recommendation: Alcohol should be avoided or strictly limited during treatment with Gleevec. Alcohol may increase the risk of hepatotoxicity and gastrointestinal irritation, and can contribute to dehydration, which may worsen renal function in patients receiving imatinib. Patients with liver impairment or those taking other hepatotoxic medications should exercise particular caution.

Most common side effects: Fluid retention (periorbital edema, peripheral edema), nausea, vomiting, diarrhea, muscle cramps, musculoskeletal pain, fatigue, rash, and headache. Myelosuppression, including neutropenia, thrombocytopenia, and anemia, is common and requires regular complete blood count monitoring, especially during the first few months of therapy. Hepatotoxicity, ranging from transaminase elevations to rare cases of severe hepatitis, necessitates periodic liver function tests. Cardiotoxicity, including congestive heart failure, has been reported; patients with pre‑existing cardiac disease should be monitored closely. Hypothyroidism can occur in patients who have undergone thyroidectomy. Gastrointestinal irritation can be reduced by taking the tablets with food and water. Serious skin reactions, including Stevens‑Johnson syndrome, have been reported; imatinib should be discontinued if severe dermatologic toxicity develops. Tumour lysis syndrome may occur in patients with high tumour burden; adequate hydration and uric acid control are important. Women of childbearing potential must use effective contraception during treatment, as imatinib may cause fetal harm. Gleevec is available only by prescription and must be prescribed and supervised by a healthcare professional experienced in oncology or hematology.

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Buy Generic Gleevec (Imatinib) without prescription in Canada

At our pharmacy, you can buy Gleevec without a prescription, with discreet and anonymous packaging delivered within 5-14 days across Canada.

What is Gleevec?

Gleevec is a targeted cancer therapy that changed the way chronic myeloid leukemia (CML) is treated. The active ingredient is imatinib, a tyrosine kinase inhibitor that blocks specific proteins inside cancer cells. It is used to treat several types of cancer and blood disorders: Philadelphia chromosome-positive chronic myeloid leukemia, a type of acute lymphoblastic leukemia (ALL) with the same genetic abnormality, gastrointestinal stromal tumors (GIST), and a few rare bone marrow disorders. Gleevec doesn't cure these diseases in most cases, but it can keep them under control for many years.

What makes Gleevec special is that it targets the exact molecular defect that drives certain cancers. In CML, a swapping of genetic material between chromosomes 9 and 22 creates a new gene called BCR-ABL. This gene produces a protein that tells white blood cells to multiply without stopping. Gleevec binds to that protein and shuts it off. The overproduction of abnormal white cells stops, and the blood counts return toward normal. The effect is usually measured within weeks to months. For most patients with chronic phase CML, Gleevec keeps the disease in remission for years. It is taken as a daily oral tablet. The standard dose is 400 mg once daily for chronic phase CML, and 600 mg once daily for accelerated phase or blast crisis. The 100 mg tablet is used for patients who need a lower dose, such as those with liver or kidney problems, or for children whose dose is calculated by body weight.

Mechanism and Pharmacology

Imatinib is a small molecule that inhibits several tyrosine kinases. Tyrosine kinases are enzymes that attach phosphate groups to proteins, which is a key step in many cellular signalling pathways. In cancer, these pathways are often stuck in the "on" position. Imatinib specifically blocks the BCR-ABL tyrosine kinase, the abnormal enzyme produced by the Philadelphia chromosome. It also inhibits two other kinases: c-KIT, which is mutated in gastrointestinal stromal tumors, and PDGFRA. By blocking these enzymes, imatinib prevents the uncontrolled growth signals from reaching the cell nucleus. The cancer cells stop dividing and undergo apoptosis, programmed cell death.

The drug is well absorbed after oral administration, with bioavailability over 90 percent. Food, especially a high-fat meal, slows absorption but does not significantly reduce the total amount absorbed. Peak plasma levels are reached in 2 to 4 hours. Imatinib is metabolized in the liver, primarily by CYP3A4, to an active metabolite that has similar potency. The half-life of imatinib is about 18 hours, and the active metabolite's half-life is about 40 hours. This allows for once-daily dosing. Steady-state levels are reached after about a week. The drug is eliminated mainly in the feces via bile. Dose adjustment is required in moderate to severe liver impairment, but kidney function does not significantly affect drug levels. However, because the drug can cause fluid retention and worsen kidney function, patients are monitored closely.

How to Use Gleevec

Take Gleevec with a meal and a large glass of water. This reduces stomach irritation and helps the drug absorb. The standard dose for chronic phase CML is 400 mg once daily. For accelerated phase or blast crisis, it is 600 mg once daily. For GIST, the dose is usually 400 mg once daily, sometimes increased to 800 mg divided into two doses if the cancer progresses. Children with CML receive a dose based on body surface area, typically 340 mg per square meter per day, not exceeding 600 mg. The 100 mg tablet is useful for dose adjustments and for children.

Swallow the tablets whole. Do not crush, chew, or break them. If you cannot swallow tablets, your doctor or pharmacist can advise you on how to dissolve the tablet in water or apple juice, but this should only be done under instruction. Take the dose at the same time each day, with food. If you miss a dose, take it as soon as you remember, but if it is almost time for the next dose, skip the missed one. Do not double up. Never stop taking Gleevec without talking to your oncologist. Stopping suddenly in a patient with a good response can sometimes allow the leukemia to return. Regular blood tests are needed to monitor your blood counts and liver function. Your dose may be adjusted based on these results. Do not change the dose yourself.

Side Effects of Gleevec

The side effects are real but often manageable, and many improve over time. Fluid retention is one of the most common and potentially serious problems. You may notice swelling around your eyes, in your ankles, or in your abdomen. This can be a sign of fluid building up, and in rare cases, it can progress to heart failure or pleural effusion, fluid around the lungs. Weigh yourself regularly. Sudden weight gain, shortness of breath, or swelling needs immediate medical attention. Gastrointestinal problems include nausea, vomiting, diarrhea, and stomach pain. Taking the tablets with food and water helps. Some patients lose their appetite or have a metallic taste in the mouth.

Muscle cramps and bone pain are common, especially in the first weeks of treatment as the leukemia cells die. This can be uncomfortable but is a sign the drug is working. Fatigue is frequent. A skin rash or itching may occur. Low blood counts are expected, because the drug suppresses the bone marrow while it clears the abnormal cells. Neutropenia, thrombocytopenia, and anemia are monitored with regular blood tests. Your doctor may hold the dose or reduce it if counts drop too low. Liver enzyme elevations are common and usually mild, but serious liver damage can occur. Yellowing of the skin or eyes, dark urine, or severe abdominal pain should be reported immediately. Heart problems, including heart failure and left ventricular dysfunction, are rare but serious, especially in elderly patients or those with pre-existing heart disease.

High-Risk Groups (Elderly, Pregnancy)

Pregnancy. Imatinib is pregnancy category D. It can cause serious birth defects and fetal loss. It should not be used during pregnancy unless the mother's life depends on it. Women of childbearing age must use effective contraception during treatment and for at least two weeks after the last dose. If pregnancy occurs, the patient must be informed of the risk. Breastfeeding is not recommended while taking Gleevec, as the drug passes into breast milk and could harm the infant.

Elderly patients can use Gleevec without dose adjustment for age alone. However, older adults are more likely to have heart, kidney, or liver problems that complicate treatment. They are also more prone to fluid retention and heart failure. Careful monitoring is essential. The starting dose may be the same, but more frequent dose adjustments may be needed. Patients with moderate to severe liver impairment require a lower dose, often 300 mg daily instead of 400 mg, because the drug is metabolized by the liver. Kidney function does not require a dose change, but the drug can worsen renal function, so serum creatinine is monitored. Patients with a history of heart disease or uncontrolled hypertension should have a cardiac evaluation before starting. The risk of fluid retention and heart failure is higher in these patients. The 100 mg tablet is often used for dose reduction in these situations.

Interaction With Activities (Driving, Alcohol)

Gleevec can cause fatigue, dizziness, and blurred vision. If you feel tired or your vision is blurry, don't drive. These effects are more common at the start of treatment and after dose increases. Most patients adapt, but be cautious. Alcohol should be limited. Alcohol can worsen liver irritation and add to the fatigue. It can also increase the risk of stomach bleeding when combined with Gleevec. Heavy drinking is strongly discouraged. If you drink, keep it light and tell your oncologist. Grapefruit juice and grapefruit should be avoided. They inhibit the enzyme CYP3A4, which breaks down imatinib, and can cause blood levels to rise to dangerous heights.

Drug Interactions

Gleevec is metabolized by CYP3A4, so drugs that affect this enzyme can change its levels. Strong CYP3A4 inhibitors, like ketoconazole, itraconazole, clarithromycin, and ritonavir, can increase imatinib levels and the risk of side effects. Strong CYP3A4 inducers, like rifampin, phenytoin, carbamazepine, and St. John's Wort, can lower imatinib levels and reduce its effectiveness. These combinations should be avoided if possible. Gleevec itself inhibits several CYP enzymes, including CYP3A4, CYP2D6, and CYP2C9. It can increase the levels of drugs metabolized by these enzymes, such as simvastatin, cyclosporine, and warfarin. The dose of these drugs may need to be adjusted. Warfarin and other anticoagulants increase the risk of bleeding, and the INR should be monitored closely. Acetaminophen (Tylenol) can interact with imatinib and increase the risk of liver damage, especially at high doses. Avoid taking more than the recommended dose of acetaminophen. Grapefruit juice must be avoided entirely. Always bring a complete list of your medications, supplements, and herbal products to your oncologist and pharmacist before starting Gleevec.

Alternative Options

For chronic myeloid leukemia, the treatment landscape has advanced significantly. Dasatinib (Sprycel), nilotinib (Tasigna), and bosutinib (Bosulif) are newer second-generation tyrosine kinase inhibitors that work faster and are effective against some imatinib-resistant mutations. They have their own side effect profiles. Ponatinib (Iclusig) is used for patients with the T315I mutation, which is resistant to imatinib and the second-generation drugs. For GIST, sunitinib (Sutent) and regorafenib (Stivarga) are used when imatinib stops working. The choice of drug depends on the specific mutation, the patient's other health conditions, and how well they tolerate the medication. Gleevec remains a first-line option because it is effective, well-studied, and available as a generic, making it more affordable. For many patients, it continues to be the right first choice.

INN, Brand Names, and Classification in Canada

INN (International Nonproprietary Name): Imatinib mesylate
Available brand names in Canada: Gleevec, and generic imatinib
ATC code: L01EA01
Forms and strengths: Tablets 100 mg and 400 mg. The 100 mg tablet is used for dose adjustments and pediatric dosing; the 400 mg tablet is the standard adult dose for chronic phase CML and GIST.
Manufacturers: Novartis Pharmaceuticals Canada Inc. (Gleevec), and diverse generic manufacturers including Apotex Inc., Teva Canada Limited, and Sandoz Canada Inc.
Registration status in Canada: Registered
Classification: Prescription (Rx)

Frequently Asked Questions

How long does it take for Gleevec to work?
Blood counts often start to normalize within a few weeks. The complete cytogenetic response, meaning the Philadelphia chromosome disappears from the bone marrow, can take several months. The goal is a deep molecular response, which may take a year or more. Patience is key.

Will I lose my hair?
Hair thinning is uncommon with Gleevec, but some patients notice it. It is usually mild and reversible. It's not the complete hair loss typically seen with chemotherapy.

Can I stop taking Gleevec once my blood counts are normal?
Stopping is possible for some patients in deep molecular remission, but only under strict medical supervision. Treatment-free remission is achievable for a minority of patients after several years of deep response. Do not stop on your own. The leukemia can return.

Why do I need to avoid grapefruit juice?
Grapefruit juice blocks the enzyme that breaks down Gleevec. This can cause blood levels of the drug to rise to dangerous levels, increasing the risk of serious side effects. Avoid grapefruit entirely during treatment.

What should I do if I notice swelling in my ankles?
Fluid retention is a common side effect. Report it to your oncologist. The dose may be adjusted, or a diuretic may be prescribed. Sudden weight gain or shortness of breath is more serious and requires immediate attention.

Delivery Information Across Canada

We ship Gleevec and generic imatinib to all provinces and territories. Delivery times vary depending on how remote your location is:

  • Ontario (Toronto, Ottawa, Mississauga): 5 to 7 days
  • Quebec (Montreal, Quebec City, Laval): 5 to 7 days
  • British Columbia (Vancouver, Victoria, Burnaby): 5 to 9 days
  • Alberta (Calgary, Edmonton, Red Deer): 5 to 9 days
  • Manitoba (Winnipeg, Brandon): 5 to 9 days
  • Saskatchewan (Saskatoon, Regina): 5 to 9 days
  • Nova Scotia (Halifax, Sydney): 5 to 9 days
  • New Brunswick (Moncton, Fredericton): 5 to 9 days
  • Newfoundland and Labrador (St. John's, Corner Brook): 7 to 14 days
  • Prince Edward Island (Charlottetown): 7 to 14 days
  • Yukon, Northwest Territories, Nunavut: 7 to 14 days

All shipments are packed discreetly with no branding or indication of contents on the outside.

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