Gleevec (imatinib)
GLEEVEC (imatinib mesylate) – a kinase inhibitor drug commonly used to treat certain types of leukemia, myeloproliferative diseases, and certain other malignancies.
FDA approved uses: Gleevec is indicated for:
Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase; Patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in blast crisis (BC), accelerated phase (AP), or in chronic phase (CP) after failure of interferon-alpha therapy; Adult patients with relapsed or refractory Philadelphia chromosome positive
acute lymphoblastic leukemia (Ph+ ALL); Adult patients with myelodysplastic/ myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements; Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown; Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown; Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP); Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST); Adjuvant treatment of adult patients following resection of Kit (CD117) positive GIST.
Available dosage forms: Tablets (scored) – 100 and 400 mg.
Usual dosage: Dose varies by condition being treated and degree of hepatic impairment, if any. Depending on condition dose may range from 300 mg/day to 800 mg/day.
Contraindications: The manufacturer states that there are no contraindications to Gleevec.
Special Warnings: The following events have occurred and warrant special consideration during initial prescribing and ongoing monitoring of treatment with Gleevec: Edema and severe fluid restrictions, cytopenias (particularly anemias, neutropenia, and thrombocytopenia, severe congestive heart failure and left ventricular dysfunction, severe hepatotoxicity including fatalities, grade 3/grade 4 hemorrhage, GI perforations (some fatal), cardiogenic shock, bullous dermatologic reactions, fetal harm, and growth retardation in children .
Adverse reactions (side effects) of these medications: The most common side effects of Gleevec include edema, nauseam vomiting, muscle cramps, musculoskeletal pain, rash, fatigue, abdominal pain, and diarrhea. Other adverse reactions seen in clinical trials or post-marketing include: headache, joint pain, nasopharyngitis, GI hemorrhage, CNS hemorrhage, myalgia, dyspepsia, pharyngolaryngeal pain, upper respiratory tract infection, dizziness, pyrexia, weight gain, insomnia, depression bone pain, constipation, cough, dyspnea, night sweats,
hypokalemia, pneumonia, anxiety and liver toxicity.
Common drug interactions: Gleevec has been found to have significant drug interaction with agents inducing CYP3A metabolism (rifampin, St. John’s Wort); agents inhibiting CYP3A metabolism (ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, and voriconazol); drugs metabolized by CYP3A4 (alfentanil, cyclosporine, diergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus or tacrolimus, DHP calcium channel blockers, certain “statins”). Caution is recommended when administering Gleevec with CYP2D6 substrates that have a narrow therapeutic window.
Special instructions for patients: Take Gleevec exactly as directed by physician, do not change dose or stop unless told to do so by the doctor. Inform doctor if you are pregnant or think you may be pregnant. Inform doctor if you experience side effects, including fever, shortness of breath, blood in the stool, jaundice, sudden weight gain, symptoms of heart failure, or if you have a history of cardiac disease of risk factors for cardiac failure.
Full prescribing information may be found at the manufacturer‘s official website Gleevec.com or at the U.S. Food and Drug Administration’s website at Gleevec Info at Drugs@FDA
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