About
Imatinib is a potent and selective tyrosine kinase inhibitor that targets the Bcr-Abl tyrosine kinase, which is the hallmark of chronic myeloid leukemia (CML). It also inhibits other receptor tyrosine kinases, including KIT (stem cell factor receptor) and PDGFR (platelet-derived growth factor receptor), which are implicated in the pathogenesis of gastrointestinal stromal tumors (GIST) and other proliferative disorders. By binding to the ATP-binding site of these kinases, imatinib prevents the phosphorylation of downstream proteins, thereby blocking cell proliferation and inducing apoptosis in cancer cells that rely on these activated kinases for survival.
This targeted approach has revolutionized the treatment of CML, transforming it from a fatal disease into a manageable chronic condition for many patients. Its efficacy in GIST is also significant, providing a crucial therapeutic option for patients with unresectable or metastatic disease. The specificity of imatinib for these oncogenic kinases minimizes damage to healthy cells, contributing to a more favorable side effect profile compared to traditional chemotherapy.
Uses
- Chronic myeloid leukemia (CML) in chronic, accelerated, or blast crisis phases.
- Gastrointestinal stromal tumors (GIST) that are unresectable or metastatic.
- Acute lymphoblastic leukemia (ALL) with Philadelphia chromosome positivity.
- Myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR gene rearrangements.
Directions For Use
Take orally with a meal and a large glass of water to minimize gastrointestinal irritation. Do not crush or chew tablets.
Benefits
- Highly effective in treating chronic myeloid leukemia.
- Significantly improves survival rates in CML patients.
- Provides a targeted therapy for gastrointestinal stromal tumors.
- Reduces tumor burden and prevents disease progression.
- Generally well-tolerated compared to conventional chemotherapy.
- Available in oral form for convenient long-term management.
Side Effects
- Fluid retention (edema, especially periorbital)
- Nausea and vomiting
- Diarrhea
- Muscle cramps and musculoskeletal pain
- Fatigue
- Skin rash
- Abdominal pain
- Headache
- Neutropenia (low white blood cell count)
- Thrombocytopenia (low platelet count)
- Anemia
- Hepatotoxicity (liver damage)
Safety Measures
- Alcohol - Avoid or limit alcohol consumption as it can increase the risk of liver toxicity, a known side effect of imatinib.
- Pregnancy - Contraindicated in pregnancy due to potential for severe fetal harm. Women of childbearing potential must use highly effective contraception.
- Breastfeeding - Not recommended during breastfeeding as imatinib is excreted in human milk and could cause serious adverse effects in the infant.
- Liver - Use with caution in patients with hepatic impairment; dose adjustment may be necessary. Monitor liver function tests regularly.
- Kidney - Use with caution in patients with renal impairment; dose adjustment may be necessary. Monitor renal function parameters.
- Lung - Rare cases of interstitial lung disease or pulmonary hypertension have been reported. Monitor for new or worsening respiratory symptoms.
Disclaimer
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