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Imatinib
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==Side effects== [[File:Bcr abl STI 1IEP.png|right|thumb|bcr-abl kinase (green), which causes [[Chronic myelogenous leukemia|CML]], inhibited by imatinib (red; small molecule).]] The most common side effects include nausea, vomiting, diarrhea, headaches, leg aches/cramps, fluid retention, visual disturbances, itchy rash, lowered resistance to infection, bruising or bleeding, loss of appetite,<ref>{{cite web|title=Imatinib|url=http://www.macmillan.org.uk/Cancerinformation/Cancertreatment/Treatmenttypes/Biologicaltherapies/Cancergrowthinhibitors/Imatinib.aspx#DynamicJumpMenuManager_6_Anchor_3|work=Macmillan Cancer Support|access-date=26 December 2012|url-status=live|archive-url=https://web.archive.org/web/20121122103401/http://www.macmillan.org.uk/Cancerinformation/Cancertreatment/Treatmenttypes/Biologicaltherapies/Cancergrowthinhibitors/Imatinib.aspx#DynamicJumpMenuManager_6_Anchor_3|archive-date=22 November 2012}}</ref> weight gain, reduced number of blood cells ([[neutropenia]], [[thrombocytopenia]], [[anemia]]), and [[edema]].<ref name="AustriaCodex">{{cite book|title=Austria-Codex| veditors = Haberfeld H |publisher=Österreichischer Apothekerverlag|location=Vienna|year=2009|edition=2009/2010|isbn=978-3-85200-196-8|language=German}}</ref> === Cardiotoxicity === In some individuals, imatinib use was reported to be associated with [[left ventricular dysfunction]] which sometimes progressed to [[congestive cardiac failure]] despite an absence of prior heart disease. Clinical trials of imatinib did not report cardiac adverse effects, but had reported a notably high incidence of peripheral oedema, with some cases classified as severe.<ref name="pmid16862153" /> Patient biopsies as well as mice treated with large doses of imatinib exhibited cellular signs of [[cardiotoxicity]]. Cardiotoxic effects appeared to mediated by inhibition of cytoplasmic [[Abl1|ABL1 tyrosine kinase]].<ref name="pmid16862153">{{cite journal | vauthors = Kerkelä R, Grazette L, Yacobi R, Iliescu C, Patten R, Beahm C, Walters B, Shevtsov S, Pesant S, Clubb FJ, Rosenzweig A, Salomon RN, Van Etten RA, Alroy J, Durand JB, Force T | title = Cardiotoxicity of the cancer therapeutic agent imatinib mesylate | journal = Nat. Med. | volume = 12 | issue = 8 | pages = 908–16 | date = August 2006 | pmid = 16862153 | doi = 10.1038/nm1446 | s2cid = 9385835 |url=http://www.escholarship.org/uc/item/34r245fh | access-date = 16 August 2019 | archive-date = 21 June 2020 | archive-url=https://web.archive.org/web/20200621012322/https://escholarship.org/uc/item/34r245fh | url-status = live }}</ref> === Childhood growth inhibition === Multiple human and animal studies suggest that if imatinib is used in prepubescent children, it may delay normal growth (more specifically bone elongation), although some may experience at least partial catch-up growth during [[puberty]].<ref name="pmid21592517" /> The reason for this side effect is unclear; interference with a [[Growth hormone|growth hormone (GH)]]-related pathway may be involved (prepubertal growth is GH-dependent, whereas pubertal growth is [[Synergy|synergystically]] promoted by both GH and sex hormones).<ref name="pmid21592517">{{cite journal |vauthors=Shima H, Tokuyama M, Tanizawa A, Tono C, Hamamoto K, Muramatsu H, Watanabe A, Hotta N, Ito M, Kurosawa H, Kato K, Tsurusawa M, Horibe K, Shimada H | title = Distinct impact of imatinib on growth at prepubertal and pubertal ages of children with chronic myeloid leukemia | journal = J. Pediatr. | volume = 159 | issue = 4 | pages = 676–81 |date=October 2011 | pmid = 21592517 | doi = 10.1016/j.jpeds.2011.03.046 }}</ref> ===Pigmentation changes=== Imatinib use may cause lightening/depigmentation or darkening/repigmentation of hair (as is the case with some other tyrosine kinase inhibitors) and/or skin as well as hyperpigmentation of the [[gingiva]]. The median onset of hair color change is 4 weeks after initiation of therapy (but may occur over a year after initiation), is dose-dependent, and is reversible upon treatment discontinuation or dose reduction.<ref name=":0">{{cite journal | vauthors = Ricci F, De Simone C, Del Regno L, Peris K | title = Drug-induced hair colour changes | journal = European Journal of Dermatology | volume = 26 | issue = 6 | pages = 531–536 | date = December 2016 | pmid = 27545142 | doi = 10.1684/ejd.2016.2844 }}</ref> [[C-kit]] receptors - one of the [[biological target]] of imatinib - are expressed by melanocytes.<ref name=":0" />
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