-5%
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.
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.
