Imatib

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What Is Imatib?

Imatib is an oral tablet from Cipla containing imatinib mesylate 100 mg and 400 mg. Imatinib was the first selective BCR-ABL tyrosine kinase inhibitor approved (Novartis, brand name Gleevec / Glivec, 2001) and revolutionised the treatment of chronic myeloid leukaemia (CML) — transforming a previously fatal disease into a chronic condition with near-normal life expectancy when treated. It also blocks the related KIT and PDGFRA receptor kinases, making it active in gastrointestinal stromal tumour (GIST) and several other rare cancers.

How Does Imatib Work?

The Philadelphia chromosome (a t(9;22) translocation) creates the constitutively-active BCR-ABL fusion kinase that drives chronic myeloid leukaemia. Imatinib binds the ATP-binding site of BCR-ABL and locks it in an inactive conformation, halting the proliferative signalling. The same compound also inhibits the related KIT receptor (overactive in GIST and mast cell disease) and PDGFRA receptor (overactive in some sarcomas).

Användningsområden och indikationer

• Chronic-phase Philadelphia-chromosome-positive CML (first-line; 400 mg/day)
• Accelerated-phase or blast-crisis CML (600–800 mg/day, often as bridge to allogeneic transplant)
• Philadelphia-chromosome-positive acute lymphoblastic leukaemia (ALL), in combination with chemotherapy
• Unresectable, recurrent or metastatic gastrointestinal stromal tumour (GIST)
• Adjuvant therapy after GIST resection (3 years, KIT-positive disease)
• Hypereosinophilic syndrome with FIP1L1-PDGFRA fusion
• Dermatofibrosarcoma protuberans (PDGFRB-driven)
• Aggressive systemic mastocytosis (KIT D816V negative)

Imatib Dosage and How to Take

Standard dosing by indication:

• Chronic-phase CML: 400 mg/day (1 × 400 mg tablet)
• Accelerated/blast CML, Ph+ ALL: 600–800 mg/day (in 1–2 divided doses)
• GIST: 400 mg/day; increase to 800 mg/day if progression

1. Take with food and a large glass of water — minimises nausea and oesophageal irritation.
2. Same time each day.
3. Swallow whole. Tablets can be dispersed in water or apple juice (not grapefruit juice) if swallowing is difficult.
4. Mandatory monitoring: FBC + LFTs every 2 weeks for first 2–3 months, then monthly. BCR-ABL transcript level (PCR) every 3 months in CML — key measure of treatment response. Annual ECG / echo for cardiac function.
5. Bone marrow + cytogenetic response: baseline and at 3, 6, 12 months in CML — defines treatment success or need for switch to second-line TKI (dasatinib, nilotinib, bosutinib, ponatinib).
6. Do not stop without oncologist instruction — treatment-free remission is possible only after sustained deep molecular response (MR4 or better) for at least 2 years, under specialist supervision.

Side Effects of Imatib

Common (often mild, settle): nausea, diarrhoea, fluid retention (periorbital oedema, peripheral oedema), muscle cramps, rash, fatigue, weight gain.

Important — mandate monitoring:

• Myelosuppression — neutropenia, thrombocytopenia, anaemia (very common); dose reduction or hold for severe
• Hepatotoxicity — LFT rises common; severe hepatitis can occur
• Cardiac dysfunction — congestive heart failure (rare but documented)
• Hypothyroidism in patients post-thyroidectomy on levothyroxine
• Hypophosphataemia, hypocalcaemia
• Renal dysfunction

Rare but serious: Stevens-Johnson syndrome / TEN, hepatic failure, severe fluid retention, GI haemorrhage, tumour lysis syndrome (high tumour burden), cerebral oedema in patients with brain metastases.

Varningar och försiktighetsåtgärder

• Pregnancy: teratogenic in animal studies; case reports of human malformations. Strong contraception throughout treatment and for 14 days after the last dose. Discuss with oncologist if pregnancy planned.
• Breastfeeding: avoid — imatinib excreted in breast milk.
• Cardiac dysfunction history: baseline + ongoing echo / BNP monitoring.
• Liver disease: cautious dosing; monitor LFTs weekly initially.
• Hypothyroidism on levothyroxine: imatinib increases levothyroxine clearance; check TSH and increase levothyroxine dose as needed.
• Surgery: increased risk of bleeding from impaired wound healing; hold imatinib peri-operatively under specialist guidance.

Läkemedelsinteraktioner

Storage

• Store at room temperature, 15–30°C, in original blister.
• Keep out of reach of children, women of childbearing potential, and pets.

Relaterade alternativ på MedsBase

Other oncology medications stocked alongside this product:

• Imat (imatinib 400 mg)
• Veenat (imatinib 100 mg)
• Votrient (pazopanib 400 mg)

Browse all anti-cancer medications →

Vanliga frågor

How well does Imatib work for chronic myeloid leukaemia?

Imatinib is one of the most successful targeted cancer therapies ever developed. 10-year overall survival in chronic-phase CML on imatinib is approximately 85%, compared with median survival of 4–6 years before TKI therapy. About 90% of patients achieve a complete cytogenetic response within 12–18 months. A significant minority (~50% with sustained deep molecular response) can eventually attempt treatment-free remission under specialist supervision.

Why must I take Imatib with food?

Two reasons: (1) food significantly reduces nausea and the risk of oesophageal irritation; (2) imatinib has good oral absorption either way, but consistent food-with-dose timing reduces day-to-day variability. Take with the largest meal of the day and a full glass of water. Avoid taking on an empty stomach or with grapefruit juice (which raises levels and toxicity risk).

What blood tests do I need?

Mandatory: FBC and LFTs every 2 weeks for the first 2–3 months, then monthly. BCR-ABL transcript level by PCR every 3 months in CML — this is the key measure of treatment response and decides whether to continue imatinib or switch to a second-generation TKI (dasatinib, nilotinib). Annual cardiac assessment (ECG, echo or BNP) is reasonable in patients with cardiac risk factors.

Can I have children while on Imatib?

Imatinib is teratogenic in animal studies and case reports of human malformations exist. Strong contraception is mandatory throughout treatment and for at least 14 days after the last dose, in both male and female patients. Discuss family planning with the oncologist before starting — in some cases, a planned treatment-free remission attempt can create a window for conception.

What is “treatment-free remission” in CML?

About 50% of CML patients who achieve sustained deep molecular response (MR4 or better) for at least 2–3 years can attempt to stop imatinib under close monitoring. Around half of those who stop maintain remission off-treatment indefinitely. The other half relapse molecularly and restart imatinib (which usually re-induces remission). This is a specialist decision — never stop imatinib unilaterally.

Imatib vs newer TKIs (dasatinib, nilotinib, bosutinib)?

Imatinib is first-line for most newly-diagnosed chronic-phase CML — long safety record, lower cost, established treatment-free remission data. Dasatinib and nilotinib are second-generation TKIs with faster and deeper molecular responses; preferred first-line in higher-risk disease or younger patients prioritising treatment-free remission. Bosutinib, ponatinib are reserved for resistance or intolerance. The choice is highly individual — specialist haematology decision.

Will Imatib work for my GIST tumour?

For GIST, imatinib response depends on the underlying KIT or PDGFRA mutation. KIT exon 11 mutations have ~85% partial response rate at 400 mg/day. KIT exon 9 mutations need 800 mg/day. KIT/PDGFRA wild-type GIST and PDGFRA D842V mutation respond poorly — alternative TKIs (avapritinib for D842V) needed. Mutational testing is mandatory before starting imatinib for GIST.

Why am I retaining fluid on Imatib?

Fluid retention — periorbital puffiness, ankle swelling, weight gain — is one of the most distinctive imatinib side effects, affecting up to 60% of patients. Mechanism involves PDGFR inhibition and mild renal sodium retention. Manage with low-salt diet and modest diuretic if needed. Severe fluid retention (pulmonary oedema, pleural effusion) requires dose reduction or hold.

Can I drink alcohol while on Imatib?

Limit alcohol — both alcohol and imatinib are processed by the liver, and the combination raises hepatotoxicity risk. Occasional small amounts are usually tolerable; daily or heavy drinking should be avoided. Tell your oncologist if your LFTs rise.

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Related Anti-Cancer Medications

Other oncology medications stocked alongside this product:

• Imat (imatinib 100/400 mg)
• Veenat (imatinib 100/400 mg)
• Votrient (pazopanib 200/400 mg)
• Hydrosar (hydroxyurea 500 mg)
• Riborea (ribociclib 200 mg)

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