Classifications: antineoplastic; monoclonal antibody; tyrosine kinase inhibitor (tki); signal transductor inhibitor (sti); Therapeutic: antineoplastic; monoclonal antibody; tki
Pregnancy Category: D
100 mg capsule
Tyrosine kinase inhibitor and signal transductor inhibitor (STI); STIs interfere with intracellular signaling pathways that
are involved in the development of malignancies. Imatinib inhibits abnormal Bcr-Abl tyrosine kinase created by the Philadelphia
chromosome abnormality in chronic myeloid leukemia (CLM). Tyrosine kinase is required for activation of a wide variety of
intracellular activities vital to cell functioning and intracellular metabolic pathways.
Inhibits WBC cell proliferation and induces cell death in Bcr-Abl tyrosine kinase positive cells as well as in newly formed
leukemic cells. Thus, it interferes with progression of chronic myeloid leukemia (CML).
Treatment of CML in blast crisis, or in chronic phase after failure of interferon-alpha therapy; unresectable and/or metastatic
malignant gastrointestinal stromal tumors (GISTs).
Acute lymphocytic leukemia (ALL), soft tissue sarcoma.
Hypersensitivity to imatinib or any of its components; viral infections, including herpes and chickenpox; intramuscular
injections with concurrent thrombocytopenia; pregnancy (category D), lactation; children <3 y.
History of hypersensitivity to other monoclonal antibodies; hepatic or renal impairment; bleeding, bone marrow suppression;
cardiac disease; dental disease, dental work; older adults, females of childbearing age; fungal infections; GI bleeding;
heart failure; hepatic disease; herpes infection, immunosuppression, infection; jaundice; neutropenia; peripheral edema,
renal disease; thrombocytopenia, vaccination, varicella, viral infection; concurrent administration of drugs which are CYP3A4
inhibitors (i.e., ketoconazole, itraconazole, erythromycin, clarithromycin).
Route & Dosage
|CML Chronic Phase
Adult: PO 400800 mg q.d. with a meal and large glass of water
Child (>3 y): PO 260 mg/m2/d in 1 or 2 divided dose(s) (max: 340 mg/m2/d)
CML Accelerated Phase or Blast Crisis
Adult: PO 600 mg q.d. with a meal and large glass of water
Adult: PO 400600 mg q.d. times up to 24 mo
Reduce dose to 300 mg q.d. (chronic) or 400 mg q.d. (accelerated, blast crisis).
- Give with meal and large glass of water (at least 8 oz).
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole: Fluid retention, edema, fatigue,
weight gain, fever,
night sweats, weakness. CNS: CNS hemorrhage, headache. GI: Nausea, vomiting, diarrhea, GI hemorrhage,
dyspepsia, abdominal pain, constipation, anorexia,
increased AST, ALT, and bilirubin
. Hematologic: Hemorrhage, neutropenia, thrombocytopenia,
petechiae, epistaxis, pancytopenia
Hypokalemia. Musculoskeletal: Muscle cramps, pain, arthralgia,
myalgia. Respiratory: Cough, dyspnea,
. Skin: Rash,
InteractionsDrug: Clarithromycin, erythromycin, ketoconazole, itraconazole
may increase imatinib levels and toxicity
; carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin
may decrease imatinib levels; may increase levels of benzodiazepines
, dihydropyridine, calcium channel blockers
), warfarin. Herbal: St. John's wort
may decrease imatinib levels.
Well absorbed, 98% reaches systemic circulation. Peak:
24 h. Metabolism:
Primarily by CYP3A4 in liver. Elimination:
Primarily in feces. Half-Life:
18 h imatinib, 40 h active metabolite
Assessment & Drug Effects
- Monitor for S&S of fluid retention. Weigh daily and report rapid weight gain immediately.
- Lab tests: CBC with platelet count and differential weekly times 1 mo, biweekly for the 2nd mo, periodically thereafter as
clinically indicated; baseline and monthly AST, ALT, alkaline phosphatase, bilirubin; periodic serum creatinine and electrolytes.
- Withhold drug and notify physician for any of the following: bilirubin >3 times ULN, AST/ALT >5 times ULN; treatment may
be reinstituted when bilirubin <1.5 times ULN and AST/ALT <2.5 times ULN.
- Review concurrent medications. Consult physician about switching patients taking warfarin to low-molecular weight or standard
heparin. Patients taking ketoconazole and other CYP3A4 inhibitors may experience increased adverse drug reactions.
Patient & Family Education
- Do not take any OTC drugs (e.g., acetaminophen, St. John's wort) without consulting physician.
- Report any S&S of bleeding immediately to physician (e.g., black tarry stool, bright red or coke colored urine, bleeding
- Report immediately to physician any unexplained change in mental status.
- Use effective means of contraception while taking this drug. Women of childbearing age should avoid becoming pregnant.