💊 DESCRIPTION
Imatinib (Imatinib mesylate) is an oral tyrosine kinase inhibitor (TKI) used primarily in the treatment of Philadelphia chromosome–positive (Ph+) cancers and tumors with specific genetic mutations.
- Form: Film-coated tablet
- Strength: 400 mg
- Route: Oral
- Indications:
- Chronic Myeloid Leukemia (CML) – all phases (chronic, accelerated, blast crisis)
- Acute Lymphoblastic Leukemia (ALL) – Ph+
- Gastrointestinal Stromal Tumors (GIST) – c-KIT (CD117) positive
- Myelodysplastic/Myeloproliferative disorders (MDS/MPD)
- Hypereosinophilic syndrome / Chronic eosinophilic leukemia
- Dermatofibrosarcoma protuberans (DFSP)
✅ ADVANTAGES
- Targeted therapy – selectively inhibits abnormal cancer-causing proteins
- Highly effective in CML and GIST
- Oral once-daily dosing is convenient
- Generally well-tolerated with fewer systemic side effects than traditional chemotherapy
- Has significantly improved survival rates in patients with CML
🌿 NATURE
- Drug Class: Tyrosine kinase inhibitor
- Mechanism of Action:
- Blocks the BCR-ABL tyrosine kinase (Philadelphia chromosome fusion gene)
- Inhibits c-KIT (GIST) and PDGFR tyrosine kinases
- Prevents phosphorylation of proteins required for cancer cell proliferation and survival
- Leads to apoptosis of malignant cells
⚠️ PRECAUTIONS
- Hematologic toxicity: Risk of neutropenia, anemia, thrombocytopenia – regular CBC monitoring needed
- Hepatotoxicity: Monitor liver function tests (LFTs)
- Edema/Fluid retention: May cause swelling, weight gain, or pleural effusion
- Gastrointestinal effects: Nausea, vomiting, diarrhea may occur
- Dermatologic reactions: Rash, itching, skin pigmentation
- Cardiac effects: Caution in patients with cardiac disease or risk factors
- Pregnancy & Lactation: Contraindicated – teratogenic
- CYP3A4 Interactions: Many drug interactions – avoid grapefruit juice, some antifungals, antiepileptics
🧊 STORAGE
- Store at 20–25°C (68–77°F)
- Protect from moisture and direct light
- Keep in original container, tightly closed
- Keep out of reach of children
👨⚕️ PATIENT ADVICE
- Take once daily with a large glass of water and food to minimize gastric irritation
- Do not crush, split, or chew the tablet
- Take at the same time each day
- Avoid grapefruit juice – it may affect drug metabolism
- Inform doctor about all medications, including over-the-counter and herbal
- Report any signs of:
- Bleeding or bruising
- Fever or signs of infection
- Jaundice (yellowing of eyes/skin)
- Sudden weight gain or swelling
- Use contraception – avoid pregnancy during and for at least 1 month after stopping treatment
- Regular blood and organ function tests are essential
📦 PACKAGING
- Primary Packaging:
- HDPE bottles or blister strips containing 400 mg film-coated tablets
- Tablet usually marked/imprinted (e.g., “400”)
- Secondary Packaging:
- Outer carton with patient information leaflet
- Labeled with:
- Strength (400 mg)
- Batch number, manufacturing & expiry dates
- Storage instructions
- Manufacturer’s details
- “Cytotoxic – handle with care” marking in some cases