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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.
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accuracy and the completeness of the information that provided and
here information is for informational purposes only.
The information contained herein should NOT be used as a substitute
for the advice of a qualified physician. This may not cover
everything about particular health conditions,
lab tests, medicines, all possible side effects, drug interactions,
warnings, alerts, etc. Please consult your healthcare professional
and discuss all your queries related to any disease or medicine. We
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