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]
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]
^"Imatinib (Gleevec) Use During Pregnancy". Drugs.com. 27 August 2018. Archived from the original on 17 February 2020. Retrieved 16 February 2020.
^ abcdefghi"Imatinib Mesylate". The American Society of Health-System Pharmacists. Archived from the original on 16 January 2017. Retrieved 8 January 2017.
^"Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 6 July 2023. Retrieved 30 March 2024.
^Green KN, Crapser JD, Hohsfield LA (September 2020). "To Kill a Microglia: A Case for CSF1R Inhibitors". Trends in Immunology. 41 (9): 771–784. doi:10.1016/j.it.2020.07.001. PMC 7484341. PMID 32792173.
^Mun SH, Park PS, Park-Min KH (August 2020). "The M-CSF receptor in osteoclasts and beyond". Experimental & Molecular Medicine. 52 (8): 1239–1254. doi:10.1038/s12276-020-0484-z. PMC 8080670. PMID 32801364.
^World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
^"Oxford Pharmacy Store Generic Imatinib". oxfordpharmacystore.co.uk. Archived from the original on 2 April 2017. Retrieved 1 April 2017.
Imatinib, sold under the brand names Gleevec and Glivec (both marketed worldwide by Novartis) among others, is an oral targeted therapy medication used...
action as a tyrosine kinase, targeted therapies (the first of which was imatinib) that specifically inhibit the activity of the BCR-ABL protein have been...
the years. However, French scientists treating leukemia patients with imatinib, a drug used in treating cancer, noted an unexpected side effect: some...
step for the development of cancer. Therefore, kinase inhibitors, such as imatinib and osimertinib, are often effective cancer treatments. Most tyrosine kinases...
anion, the spelling used is sometimes mesilate (as in imatinib mesilate, the mesylate salt of imatinib). Mesylate esters are a group of organic compounds...
exon 17 are responsible for resistance to targeted therapy drugs like imatinib mesylate, a tyrosine kinase inhibitor. KIT-p.D419del (exon 8) — A subset...
CML CP) or Ph+ CML CP resistant or intolerant to prior therapy including imatinib. newly diagnosed Ph+ acute lymphoblastic leukaemia (ALL) in combination...
tissue. One of the most successful molecular targeted therapeutics is imatinib, marketed as Gleevec, which is a kinase inhibitor with exceptional affinity...
kinase inhibitors specific to such domains as CC, Y177, and Rho (such as imatinib and sunitinib) are important drugs against a variety of cancers including...
well as in accelerated and chronic phase CML that has not responded to imatinib. It is taken by mouth. Common side effects may include low platelets, low...
small number of children also develop this disease. It is treated with imatinib (Gleevec in United States, Glivec in Europe) or other drugs. The five-year...
approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) in January 2006. Sunitinib...
cancer's cell division. The classic example of targeted development is imatinib mesylate (Gleevec), a small molecule which inhibits a signaling molecule...
reactions with phenelzine, and a potential interaction has been reported with imatinib, resulting in hepatotoxicity, and with lamotrigine. The common ginsengs...
γ-secretase. Imatinib itself does not get into the brain so imatinib could not be used as an AD therapeutic. However it may be possible to identify imatinib-like...
return for a large sum of money. Due to patent protection, the Swiss drug imatinib is very expensive and cannot be afforded by most leukemia patients in China...
pensions crisis; Osiris Therapeutics; apoptosis and Ian Judson, and trials of imatinib for gastrointestinal stromal tumors (GIST); the Geron Corporation and the...
rituximab, sirolimus, alefacept, and the tyrosine kinase inhibitors, imatinib, nilotinib, and dasatinib. Experimental therapies under investigation include...
Systemic mastocytosis Chronic myelogenous leukemia (largely replaced by imatinib, but still in use for its cost-effectiveness) Reported side effects are:...
eosinophils through ADCC antagonists of leukotriene synthesis or receptors imatinib (STI571) – inhibits PDGF-BB in hypereosinophilic leukemia Monoclonal antibodies...
factor and vascular endothelial growth factor. Bosutinib inhibited 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines, but...