Imatero-400

Imatero-400

imatinib

Manufacturer:

Camber

Distributor:

Camber
Concise Prescribing Info
Contents
Imatinib mesylate
Indications/Uses
Relapsed or refractory Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). Aggressive systemic mastocytosis w/o the D816V c-Kit mutation or w/ c-Kit mutational status unknown. Unresectable, recurrent &/or metastatic dermatofibrosarcoma protuberans. Kit (CD117)-positive unresectable &/or metastatic malignant GI stromal tumors; adjuvant treatment of adults following complete gross resection of Kit (CD117)-positive GI stromal tumors. Hypereosinophilic syndrome &/or chronic eosinophilic leukemia who have FIP1L1-platelet-derived growth factor (PDGF) receptor α fusion kinase & for patients w/ hypereosinophilic syndrome &/or chronic eosinophilic leukemia who are FIP1L1-PDGF receptor α fusion kinase negative or unknown. Myelodysplastic/myeloproliferative diseases associated w/ PDGF receptor gene rearrangements. Newly diagnosed adult & ped patients w/ Ph+ chronic myeloid leukemia (CML) in chronic phase. Patients w/ Ph+ CML in blast crisis, accelerated phase, or in chronic phase after failure of interferon-α therapy.
Dosage/Direction for Use
Adult Acute lymphoblastic leukemia 600 mg/day. Aggressive systemic mastocytosis 400 mg/day w/o D816V c-Kit mutation. Aggressive systemic mastocytosis associated w/ eosinophilia Initially 100 mg/day. Consider dose increase from 100-400 mg in the absence of adverse reactions if assessments demonstrate an insufficient response to therapy. Chronic eosinophilic leukemia 400 mg/day. Chronic eosinophilic leukemia w/ demonstrated FIP1L1-PDGF receptor α fusion kinase Initially 100 mg/day. Consider dose increase from 100-400 mg in the absence of adverse reactions. Chronic myeloid leukemia Accelerated phase or blast crisis: 600 mg/day. Consider dose increase from 600-800 mg in the absence of severe adverse reactions & severe non-leukemia-related neutropenia or thrombocytopenia. Chronic phase: 400 mg/day. Consider dose increase from 400-600 mg in the absence of severe adverse reactions & severe non-leukemia-related neutropenia or thrombocytopenia. Dermatofibrosarcoma protuberans 800 mg/day. Adjuvant GI stromal tumors 400 mg/day. Unresectable &/or metastatic, malignant GI stromal tumors 400 mg/day. Consider dose increase up to 800 mg daily (given as 400 mg bid) in the absence of severe adverse reactions. Hypereosinophilic syndrome 400 mg/day. Hypereosinophilic syndrome w/ demonstrated FIP1L1-PDGF receptor α fusion kinase Initially 100 mg/day. Consider dose increase from 100-400 mg in the absence of adverse reactions. Myelodysplastic/myeloproliferative diseases 400 mg/day. Childn ≥2 yr Newly diagnosed Ph+ CML chronic phase 340 mg/m2/day. Max dose: 600 mg/day. Patients w/ mild renal impairment (CrCl 40-59 mL/min) Max dose: 600 mg, moderate renal impairment (CrCl 20-39 mL/min) Initially decreased by 50% of recommended starting dose. Max dose: 400 mg. Severe hepatic impairment Decreased recommended doe by 25%.
Administration
Should be taken with food: Take w/ meals & a full glass of water to minimise GI discomfort. For patients w/ swallowing difficulties, tab may be dispersed in water/apple juice. Disperse each 100-mg tab in 50 mL of water & each 400-mg tab in 200 mL of water. Stir & administer after complete disintegration of tab.
Special Precautions
Severe fluid retention may occur. Carefully investigate unexpected rapid wt gain & provide appropriate treatment. Perform CBCs wkly for the 1st mth, bi-wkly for the 2nd mth, & periodically thereafter as clinically indicated (eg, every 2-3 mth). Carefully monitor patients w/ cardiac disease or risk factors for cardiac failure & evaluate, & treat any patient w/ signs & symptoms consistent w/ cardiac failure; liver function (transaminases, bilirubin & alkaline phosphatase) before initiation of treatment & mthly thereafter; hepatic impairment. Hemorrhage, GI irritation. Perform ECG & determining serum troponin in patients w/ hypereosinophilic syndrome/chronic eosinophilic leukemia & in patients w/ myelodysplastic/myeloproliferative diseases or aggressive systemic mastocytosis associated w/ high eosinophilic levels; if either is abnormal, consider prophylactic use of systemic steroids for 1-2 wk. Bullous dermatologic reactions including erythema multiforme & Stevens-Johnson syndrome. Closely monitor TSH levels in thyroidectomy patients undergoing levothyroxine replacement; patients at risk of tumor lysis syndrome. Severe renal & hepatic impairment. Pregnancy & lactation. Childn <2 yr; closely monitor growth during therapy. Elderly ≥65 yr.
Adverse Reactions
Edema/fluid retention (includes aggravated edema, anasarca, ascites, pericardial effusion, peripheral edema, pleural effusion, pulmonary edema & superficial edema), facial edema, chest pain; fatigue, pain, fever, headache, dizziness, insomnia, depression, anxiety, chills; rash, dermatitis, pruritus, alopecia; increased LDH, hypoproteinemia, decreased albumin, hypokalemia; nausea, diarrhea, vomiting, abdominal pain & distention, anorexia, wt gain, dyspepsia, flatulence, constipation, taste disturbance; anemia, leukopenia, hemorrhage, neutropenia, thrombocytopenia; increased AST/ALT, alkaline phosphatase, bilirubin; muscle cramps, arthralgia, joint pain, myalgia, weakness, musculoskeletal pain, rigors, paresthesia, bone pain; periorbital edema, increased lacrimation, blurred vision; increased serum creatinine; nasopharyngitis, cough, dyspnea, upper resp tract infection, pharyngolaryngeal pain, rhinitis, pharyngitis, pneumonia, sinusitis; infection, night sweats, influenza, diaphoresis.
Drug Interactions
Increased risk of hepatotoxicity w/ ginseng & acetaminophen. Decreased plasma conc & increased metabolism w/ CYP3A4 inducers (eg, carbamazepine, dexamethasone, fosphenytoin, oxcarbazepine, phenobarb, phenytoin, primidone, rifabutin, rifampin, St. John's wort). Increased plasma conc & may decrease metabolism w/ CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole). Increase mean Cmax & AUC of CYP2D6 substrates (eg, metoprolol). May increase plasma conc of CYP3A4 substrates [eg, alfentanil, cyclosporine, dihydropyridine, Ca channel blockers, ergot alkaloids, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, triazolobenzodiazepines (eg, midazolam, triazolam)]. May increase levothyroxine hepatic clearance. Warfarin.
MIMS Class
Targeted Cancer Therapy
ATC Classification
L01EA01 - imatinib ; Belongs to the class of BCR-ABL tyrosine kinase inhibitors. Used in the treatment of cancer.
Presentation/Packing
Form
Imatero-400 FC tab 400 mg
Packing/Price
30's
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