Vexinib 100

Vexinib 100



Vexxa Lifesciences


VE Pharma
Concise Prescribing Info
Imatinib mesilate
Treatment of adult & childn w/ newly diagnosed Philadelphia chromosome (Bcr-Abl) +ve (Ph+) chronic myeloid leukaemia (CML) for whom bone marrow transplantation is not considered as the 1st line of treatment; Ph+ CML in chronic phase after failure of interferon-α therapy or in accelerated phase or blast crisis. Adults w/ newly diagnosed Philadelphia chromosome +ve acute lymphoblastic leukaemia (Ph+ ALL) integrated w/ chemotherapy; relapsed or refractory Ph+ ALL as monotherapy; myelodysplastic/myeloproliferative diseases (MDS/MPD) associated w/ platelet-derived growth factor receptor (PDGFR) gene re-arrangements; advanced hypereosinophilic syndrome (HES) &/or chronic eosinophilic leukaemia (CEL) w/ FIP1L1-PDGFRα rearrangement. Treatment of adults w/ Kit (CD117) +ve unresectable &/or metastatic malignant GI stromal tumours (GIST). Adjuvant treatment of adults who are at significant risk of relapse following resection of Kit (CD117) +ve GIST. Adults w/ unresectable dermatofibrosarcoma protuberans (DFSP) & recurrent &/or metastatic DFSP who are not eligible for surgery.
Dosage/Direction for Use
Haematological malignancies & malignant sarcoma 400-600 mg once daily or 400 mg bid (800 mg/day). Adult CML Chronic phase 400 mg/day, may increase to 600-800 mg/day. Accelerated phase 600 mg/day. Max: 800 mg/day (as 400 mg bid). Blast crisis 600 mg/day. Ph+ ALL 600 mg/day. MDS/MPD 400 mg/day. Treatment duration: Median of 47 mth. HES/CEL 100 mg/day, may increase to 400 mg/day. Unresectable &/or metastatic malignant GIST 400 mg/day. Treatment duration: Median of 7 mth. Following resection of GIST 400 mg/day for 36 mth. DFSP 800 mg/day. Childn CML Chronic & advance phase 340 mg/m2 daily as once daily or bid. May be given as once daily or alternatively daily dose may be split into 2 administrations (1 in the morning & 1 in the evening). May increase dose from 340 mg/m2 daily to 570 mg/m2 daily. Max: 800 mg/day. Ph+ ALL Childn 340 mg/m2 daily. Max: 600 mg/day.
Should be taken with food: Take w/ meals & a large glass of water to minimize GI irritation. For patients w/ swallowing difficulties, open cap & dilute contents in a glass of water/apple juice.
Special Precautions
Concomitant use w/ PIs, or other strong CYP3A4 inhibitors, CYP3A4 substrates w/ narrow therapeutic window (eg, cyclosporin or pimozide) or CYP2C9 substrates w/ narrow therapeutic window (eg, warfarin & other coumarin derivatives). Avoid use w/ CYP3A4 inhibitors (eg, dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarb or Hypericum perforatum). Hypothyroidism in thyroidectomy. Severe fluid retention in elderly & those w/ prior history of cardiac disease. Cardiac dysfunction. Patients w/ history of cardiac disease, risk factors for cardiac failure or history of renal failure & w/ signs or symptoms consistent w/ cardiac or renal failure. GI hemorrhage. Tumor lysis syndrome. Correct clinically significant dehydration & treatment of high uric acid levels are recommended prior to initiation of therapy. Perform regular complete blood counts & liver function (transaminases, bilirubin, alkaline phosphatase). Evaluation of performance of an echocardiogram & determination of serum troponin should be considered in patients w/ HES/CEL, & in patients w/ MDS/MPD associated w/ high eosinophil levels. Caution when driving a car or operating machinery. Hepatic dysfunction. Impaired renal function. Pregnancy & lactation. Monitor growth in childn.
Adverse Reactions
Neutropenia, thrombocytopenia, anaemia; headache; nausea, diarrhoea, vomiting, dyspepsia, abdominal pain; periorbital oedema, dermatitis, eczema, rash; muscle spasm, cramps, musculoskeletal pain including myalgia, arthralgia, bone pain; fluid retention, oedema, fatigue; increased wt. Pancytopenia, febrile neutropenia; anorexia; insomnia; dizziness, paraesthesia, taste disturbance, hypoaesthesia; eyelid oedema, increased lacrimation, conjunctival haemorrhage, conjunctivitis, dry eye, blurred vision; flushing, haemorrhage; dyspnoea, epistaxis, cough; flatulence, abdominal distension, gastro-oesophageal reflux, constipation, dry mouth, gastritis; increased hepatic enzymes; pruritus, face oedema, dry skin, erythema, alopecia, night sweats, photosensitivity reaction; joint swelling; weakness, pyrexia, anasarca, chills, rigors; decreased wt.
Drug Interactions
May decrease metabolism & increase conc w/ CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, clarithromycin). Reduced exposure & increased risk of therapeutic failure w/ CYP3A4 inducers (eg, dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarb, fosphenytoin, primidone or St. John's wort). Decreased plasma AUC w/ enzyme-inducing antiepileptic drugs eg, carbamazepine, oxcarbazepine & phenytoin. Increased mean C & AUC of simvastatin. Caution when in concomitant w/ CYP3A4 substrates w/ narrow therapeutic window (eg, cyclosporin or pimozide). May increase plasma conc of other CYP3A4 metabolised drugs (eg, triazolo-benzodiazepines, dihydropyridine Ca channel blockers, statins). Increased Cmax & AUC of CYP2D6 substrates eg, metoprolol. Caution when in concomitant w/ paracetamol. May decrease plasma exposure of levothyroxine. Increased adverse events ie, hepatotoxicity/myelosuppression w/ L-asparaginase.
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.
Vexinib 100 cap 100 mg
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