Enliven 100 mg (Capsule)
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Medicine Details
Category | Details |
---|---|
Generic | Imatinib mesylate |
Company | Orion pharma ltd |
Title
- Imatinib Tablets
Categories
- Cancer Treatment
- Medication
Description
- Imatinib is a targeted cancer therapy used to treat various types of cancers, including leukemia and gastrointestinal stromal tumors.
Dosage
- Adults with Ph+ CML CP: 400 mg/day
- Adults with Ph+ CML AP or BC: 600 mg/day
- Pediatrics with Ph+ CML CP: 340 mg/m2/day
- Adults with Ph+ ALL: 600 mg/day
- Pediatrics with Ph+ ALL: 340 mg/m2/day
- Adults with MDS/MPD: 400 mg/day
- Adults with ASM: 100 mg/day or 400 mg/day
- Adults with HES/CEL: 100 mg/day or 400 mg/day
- Adults with DFSP: 800 mg/day
- Adults with metastatic and/or unresectable GIST: 400 mg/day
- Adjuvant treatment of adults with GIST: 400 mg/day
- Patients with mild to moderate hepatic impairment: 400 mg/day
- Patients with severe hepatic impairment: 300 mg/day
- Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day.
Indications
- Treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+CML) in different phases
- Treatment of Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in adults and pediatrics
- Treatment of myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor (PDGFR) gene rearrangements
- Treatment of aggressive systemic mastocytosis, hypereosinophilic syndrome, chronic eosinophilic leukemia, dermatofibrosarcoma protuberans, and gastrointestinal stromal tumors
Pharmacology
- Imatinib is a small molecule protein-tyrosine kinase inhibitor that targets Bcr-Abl tyrosine kinase, Kit receptor, discoidin domain receptors, colony stimulating factor receptor, and platelet-derived growth factor receptors. It inhibits cellular events mediated by activation of these receptor kinases.
Absorption and distribution
- Imatinib is well absorbed after oral administration with Cmax achieved within 2-4 hours post-dose. Mean absolute bioavailability is 98%. At clinically relevant concentrations of Imatinib, binding to plasma proteins in in vitro experiments is approximately 95%.
Metabolism
- CYP3A4 is the major enzyme responsible for the metabolism of Imatinib. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4.
Excretion
- Imatinib elimination is predominately in the feces, mostly as metabolites. Approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose).
Interaction
- Concomitant administration of strong CYP3A4 inducers may reduce total exposure of imatinib; consider alternative agents. Concomitant administration of strong CYP3A4 inhibitors may result in a significant imatinib exposure increase. Imatinib will increase the plasma concentration of CYP3A4 metabolized drugs.
Side effects
- Fluid retention and edema
- Hematologic toxicity
- Congestive heart failure and left ventricular dysfunction
- Hepatotoxicity
- Hemorrhage
- Gastrointestinal disorders
- Hypothyroidism
- Tumor lysis syndrome
- Impairments related to driving and using machinery
- Renal toxicity
Pregnancy and lactation
- Women of childbearing potential must use effective contraception during treatment and for at least 15 days after stopping treatment with Imatinib. Imatinib should not be used during pregnancy unless clearly necessary. Women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib.
Precautions and warnings
- Edema and severe fluid retention
- Cytopenias
- Severe congestive heart failure and left ventricular dysfunction
- Severe hepatotoxicity
- Grade 3/4 hemorrhage
- Cardiogenic shock/left ventricular dysfunction
- Bullous dermatologic reactions
- Hypothyroidism
- Fetal harm
- Growth retardation in children and adolescents
- Tumor lysis syndrome
- Renal toxicity
Overdose effects
- Experience with doses higher than the recommended therapeutic dose is limited. Reported symptoms include nausea, vomiting, diarrhea, rash, edema, pancytopenia, and abdominal pain. The outcome in these cases was generally 'improved' or 'recovered'.
Therapeutic class
- Targeted Cancer Therapy
- Tyrosine Kinase Inhibitor
Storage conditions
- Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.