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Product
Anti-cancer Products (Imatib)
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Anti-cancer Products (Imatib)
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Imatib (alpha)
COMPOSITION
Each capsule contains
• Imatinib (as mesylate) ............. 100 mg
» It is the main treatment for chronic myeloid leukaemia.
» It is a type of biological treatment that targets a protein made by CML cells.
» It is a type of growth blocker, called a tyrosine kinase inhibitor (TKI).
» Tyrosine kinases are a group of proteins that cells use to signal to each other to
grow.
» This drug stops the messages from these proteins getting to cancer cells and so
interferes with their growth.
► Chronic myeloid leukemia can express BCR-ABL,
► Gastrointestinal stromal tumours (GISTs) can express c-kit
► Small cell lung cancer can express c-kit and stem cell factor
► Adenocarcinomas of the breast, colon, and prostate and glioblastomas ( most
common and most aggressive of the primary brain tumors ) can express
platelet
-derived growth factor (PDGF-1)
► 89 % overall survival at 5 yr with Imatinib exceeds
that of all other CML therapies, with < 5 % of deaths
related to CML .
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Pharmacokinetic data
» Bioavailability 98%
» Protein binding 95%
» Metabolism Hepatic (mainly CYP3A4-mediated)
» Half life 18 hours (imatinib)
» Excretion Fecal (68%)
renal (13%).
Indications and Usage
• Imatib is indicated for the treatment of patients with Philadelphia chromosome positive chronic myeloid leukemia (CML) in blast crisis ,accelerated phase or in
chronic phase after failure of interferon-alpha
therapy. (terminal phase of CML, an increase in the number of immature WBC )
• Imatib is also indicated for the treatment of patients with C-Kit gene (CD117) positive un-resectable and/or metastatic malignant GIST ( G.I stromal tumors )
Dosage & Administration
• The prescribed dose should be administered orally, with a meal and a large glass of water.
• Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day.
• Treatment may be continued as long as there is no evidence of progressive disease or unacceptable toxicity.
• -Chronic phase CML 400 mg/day
-Accelerated phase or blast crisis 600 mg/day
-Unresectable and/or metastatic 400 mg/day
malignant GIST (or) 600 mg/day
Hematologic Adverse Reactions
Dose reduction or treatment interruptions for severe neutropenia and thrombocytopenia are recommended.
Paediatric
The safety and efficacy of Imatinib mesylate in patients under the age of 18 years have not been established.
Pregnancy
• Women of childbearing potential should be advised to avoid becoming pregnant.
• If Imatinib mesylate is used during pregnancy or if the patient becomes pregnant while taking Imatinib mesylate the patient should be apprised of the
potential hazard to the fetus.
Nursing Mothers
It is not known whether Imatinib mesylate or its metabolites are excreted in human milk.
Geriatric Use
The efficacy of Imatinib mesylate was similar in older and younger patients.
Contraindications
Use of imatinib mesylate is contraindicated in patients with hypersensitivity to imatinib or to any other component of imatinib mesylate.
Side effects
•Edema, nausea, rash and musculoskeletal pain are common but mild.
•Up to 6 out of every 10 people (60%) treated
» Feel sick
» water retention
» puffy eyes
•Severe congestive cardiac failure is an uncommon but recognised side effect of imatinib .
Other less common side effects
• Being sick or diarrhoea (in 5 out of 10)
• A rash (in 4 out of 10)
• Headaches or tiredness (in 3 out of 10)
Other more serious side effects
• A drop in the number of white blood cells, increasing your risk of serious infection.
• A severe drop in platelets in the blood, causing bleeding problems.
This drug can occasionally affect the liver and you will probably have blood tests to check for this.
PRESENTATION
1 strip …….10 capsules
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