Imatinib
Chemical compound / From Wikipedia, the free encyclopedia
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Imatinib, sold under the brand names Gleevec and Glivec (both marketed worldwide by Novartis) among others, is an oral targeted therapy medication used to treat cancer.[2] Imatinib is a small molecule inhibitor targeting multiple tyrosine kinases such as CSF1R, ABL, c-KIT, FLT3, and PDGFR-β.[4][5] Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome–positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelodysplastic syndrome.[2]
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Trade names | Gleevec, Glivec, others |
Other names | STI-571 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a606018 |
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Routes of administration | By mouth |
Drug class | Tyrosine kinase inhibitor[2] |
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Bioavailability | 98% |
Protein binding | 95% |
Metabolism | Liver (mainly CYP3A4-mediated) |
Elimination half-life | 18 h (imatinib) 40 h (active metabolite) |
Excretion | Fecal (68%) and kidney (13%) |
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ECHA InfoCard | 100.122.739 |
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Formula | C29H31N7O |
Molar mass | 493.615 g·mol−1 |
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Common side effects include vomiting, diarrhea, muscle pain, headache, and rash.[2] Severe side effects may include fluid retention, gastrointestinal bleeding, bone marrow suppression, liver problems, and heart failure.[2] Use during pregnancy may result in harm to the baby.[2] Imatinib works by stopping the Bcr-Abl tyrosine-kinase.[2] This can slow growth or result in programmed cell death of certain types of cancer cells.[2]
Imatinib was approved for medical use in the United States in 2001.[2] It is on the World Health Organization's List of Essential Medicines.[6] A generic version became available in the UK as of 2017.[7]