Imanix 100 mg (Tablet)

Indications

• Treatment for chronic myeloid leukemia in chronic phase
• Treatment for chronic myeloid leukemia in blast crisis or accelerated phase
• Treatment for acute lymphoblastic leukemia
• Treatment for platelet-derived growth factor receptor gene rearrangements
• Treatment for systemic mastocytosis without D816V c-Kit mutation
• Treatment for hypereosinophilic syndrome
• Treatment for chronic eosinophilic leukemia
• Treatment for dermatofibrosarcoma protuberans
• Treatment for unresectable and/or metastatic gastrointestinal stromal tumors
• Adjuvant treatment following complete gross resection of gastrointestinal stromal tumors

Pharmacology

• Small molecule protein-tyrosine kinase inhibitor
• Inhibits Bcr-Abl tyrosine kinase activity
• Inhibits receptor tyrosine kinases including Kit, platelet-derived growth factor receptors alpha and beta
• Well absorbed after oral administration
• Mean absolute bioavailability of 98%
• Metabolized by CYP3A4
• Major active metabolite N-demethylated piperazine derivative
• Predominant elimination in feces
• Elimination half-lives of approximately 18 and 40 hours

Dosage & Administration

• 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
• Doses to be taken with a meal and a large glass of water

Interaction

• Concomitant administration with CYP3A4 inducers may reduce total exposure
• Concomitant administration with CYP3A4 inhibitors may result in significant imatinib exposure increase
• Grapefruit juice may increase plasma concentrations
• Interactions with drugs metabolized by CYP3A4 and CYP2D6
• Use caution with CYP3A4 substrates that have a narrow therapeutic window

Side Effects

• Fluid retention and edema
• Hematologic toxicity
• Congestive heart failure and left ventricular dysfunction
• Hepatotoxicity
• Hemorrhage
• Gastrointestinal disorders
• Dermatologic toxicities
• Hypothyroidism
• Growth retardation in children and adolescents
• Tumor lysis syndrome
• Impairments related to driving and using machinery
• Renal toxicity

Pregnancy & Lactation

• Women of childbearing potential must use effective contraception
• Limited data on use in pregnant women
• Potential reproductive toxicity
• Imatinib can be distributed into human milk
• Effects of low-dose exposure to infant unknown
• Fertility effects on male and female rats observed

Precautions & Warnings

• Edema and severe fluid retention
• Cytopenias, particularly anemia, neutropenia, and thrombocytopenia
• Severe congestive heart failure and left ventricular dysfunction
• Severe hepatotoxicity, including fatalities
• Grade 3/4 hemorrhage
• Cardiogenic shock/left ventricular dysfunction
• Bullous dermatologic reactions
• Hypothyroidism
• Fetal harm
• Growth retardation in children and pre-adolescents
• Tumor lysis syndrome
• Reports of motor vehicle accidents
• Renal toxicity

Overdose Effects

• Experience with higher than recommended therapeutic dose is limited
• Events reported include nausea, vomiting, diarrhea, rash, edema, thrombocytopenia, and abdominal pain

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

Related Brands

• Enliven 100 mg (Capsule) - orion-pharma-ltd