Imatinib

Imatinib, sold under the brand names Gleevec among others, is a medication used to treat cancer. Specifically, it is used for chronic myelogenous leukemia and acute lymphocytic leukemia.

Imatinib

Imatinib; 152459-95-5; Sti-571; STI571; Cgp 57148

Celonib, Glivec, Imalek, Lupinib, Mesylonib, Mitinab, Shantinib, Unitinib, Veenat

N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]benzamide

NA

Imatinib is an antineoplastic agent used to treat chronic myelogenous leukemia. Imatinib is a 2-phenylaminopyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes. 

PO- Dose varies from 400mg/day to 800mg/day depending on condition. 400 to 600mg/day should be administered once daily, 800mg/day should be administered twice daily.

For the treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML), Ph+ acute lymphoblastic leukaemia, myelodysplastic/myeloproliferative diseases, aggressive systemic mastocytosis, hypereosinophilic syndrome and/or chronic eosinophilic leukemia (CEL), dermatofibrosarcoma protuberans, and malignant gastrointestinal stromal tumors (GIST).

Fluid retention/oedema, nausea and vomiting, muscle cramps, musculoskeletal pain, haemorrhage, diarrhoea, rash. Fatigue, asthenia, headache, upper respiratory tract infection, dizziness, insomnia, depression, anxiety, increased wt, joint pain, arthralgia, myalgia, back pain, abdominal pain, flatulence, dyspepsia, influenza, loose stools, anorexia, constipation, taste disturbance, nasopharyngitis, cough, pharyngolaryngeal pain, pharyngitis, sinusitis, pneumonia, dyspnoea, pyrexia, night sweats, rigors, hepatotoxicity, hypokalaemia, pruritus, chest pain, increased lacrimation.

• Increased blood levels with CYP3A4 inhibitors (azole antifungals, macrolide antibiotics). Reduced blood levels with CYP3A4 inducers (carbamazepine, dexamethasone, St John's wort, phenobarbital, phenytoin, rifampicin).
• Ciclosporin, pimozide, triazolo-benzodiazepines, dihydropyridine calcium-channel blockers, certain statins (CYP3A4 substrates), warfarin (CYP2C9) and CYP2D6 increase blood levels of these drugs.

Contraindicated in lactation

Store at 25°C. 

Molecular weight

493.6027

Molecular formula

C29H31N7O

CAS number

152459-95-5

Precautions

• Cardiac disease or increased risk for CHF. Monitor for signs of severe fluid retention.
• Monitor TSH levels in thyroidectomy patients receiving levothyroxine replacement therapy.Monitor liver function (alkaline phosphatase, bilirubin, transaminases) prior to therapy, then monthly or as clinically indicated during treatment.
• Monitor CBC regularly.
• Renal and hepatic impairment.
•  Monitor LFTs.
• Pregnancy.