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Imatinib is a tyrosine kinase inhibitor targeting Bcr-Abl kinase, as well as other receptor tyrosine kinases (e.g., Kit, PDGFR-alpha/beta). It works by:
- Blocking cellular events mediated by these kinases.
- Reducing tumor proliferation and survival.
- Imatinib is absorbed well orally, with peak levels in 2–4 hours.
- Bioavailability: 98%.
- Plasma protein binding: ~95%.
- Metabolized by CYP3A4, with a minor role of CYP1A2, CYP2D6, CYP2C9, and CYP2C19.
- Main active metabolite: N-demethylated derivative.
- Predominantly eliminated in feces (~68%) and urine (~13%) as metabolites.
- Half-life: Imatinib ~18 hours; metabolite ~40 hours.
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✅ Description:
Enliven is indicated for the following conditions:
- Newly diagnosed adult and pediatric patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in the chronic phase.
- Adult patients with Ph+ CML in blast crisis, accelerated phase, or chronic phase after interferon-alpha therapy failure.
- Adults with relapsed/refractory Ph+ acute lymphoblastic leukemia (Ph+ ALL).
- Pediatric patients with newly diagnosed Ph+ ALL in combination with chemotherapy.
- Adults with myelodysplastic/myeloproliferative diseases associated with PDGFR gene rearrangements.
- Adults with aggressive systemic mastocytosis without D816V c-Kit mutation or with unknown c-Kit mutational status.
- Adults with hypereosinophilic syndrome (HES) or chronic eosinophilic leukemia (CEL) with FIP1L1-PDGFRa fusion kinase or negative/unknown status.
- Adults with unresectable, recurrent, or metastatic dermatofibrosarcoma protuberans.
- Patients with Kit (CD117)-positive unresectable/metastatic gastrointestinal stromal tumors (GIST).
- Adjuvant treatment in adult patients following complete resection of Kit (CD117)-positive GIST.
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✔️ Side Effects of Imatinib
- Common: Fluid retention, cytopenias (anemia, neutropenia), gastrointestinal symptoms (nausea, vomiting, diarrhea).
- Serious: Congestive heart failure, hepatotoxicity, hemorrhage, dermatologic reactions (e.g., Stevens-Johnson syndrome), and renal toxicity.
✔️ Overdose Effects
Symptoms may include nausea, vomiting, gastrointestinal pain, edema, cytopenias, or increased bilirubin. Symptomatic treatment and monitoring are required.
✔️ Dosage & Administration of Imatinib
- Take with food and a large glass of water. Tablets may be dissolved in water/apple juice if needed.
- Doses vary by condition, ranging from 100 mg to 800 mg daily, with some conditions requiring twice-daily dosing.
✔️ Interactions
- CYP3A4 Inducers: May reduce imatinib levels (e.g., rifampin, phenytoin).
- CYP3A4 Inhibitors: May increase imatinib levels (e.g., ketoconazole, grapefruit juice).
- CYP3A4 Substrates: Caution with narrow therapeutic index drugs (e.g., certain calcium channel blockers, statins).
- Warfarin: Prefer heparin over warfarin.
✔️ Precautions & Warnings
- Monitor for fluid retention, hepatotoxicity, and cytopenias.
- Avoid use during pregnancy unless necessary; advise effective contraception.
- Breastfeeding is not recommended.
- Monitor growth in children; potential growth retardation has been reported.
- Caution patients about operating machinery or driving.
✔️ Storage Conditions
- Store below 30°C, in a cool and dry place, away from light and moisture.
- Keep out of the reach of children.
⚠️Disclaimer:
At ePharma, we’re committed to providing accurate and accessible health information. However, all content is intended for informational purposes only and should not replace medical advice from a qualified physician. Please consult your healthcare provider for personalized guidance. We aim to support, not substitute, the doctor-patient relationship.
