imatinib mesylate


Summary: A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.

Top Publications

  1. Dahlin J, Ekoff M, Grootens J, Löf L, Amini R, Hagberg H, et al. KIT signaling is dispensable for human mast cell progenitor development. Blood. 2017;130:1785-1794 pubmed publisher
    ..Contrary to the prevailing consensus, our results show that SCF and KIT signaling are dispensable for early mast cell development. ..
  2. Jeon J, Sparreboom A, Baker S. Kinase Inhibitors: The Reality Behind the Success. Clin Pharmacol Ther. 2017;102:726-730 pubmed publisher
    ..The future fate of kinase inhibitors, however, is bright, as evidenced from ongoing efforts to increase their efficacy while remediating their weaknesses in order to provide the best quality of care to patients. ..
  3. Lengline E, Beldjord K, Dombret H, Soulier J, Boissel N, Clappier E. Successful tyrosine kinase inhibitor therapy in a refractory B-cell precursor acute lymphoblastic leukemia with EBF1-PDGFRB fusion. Haematologica. 2013;98:e146-8 pubmed publisher
  4. Liang S, Yu H, Chen X, Shen T, Cui Z, Si G, et al. PDGF-BB/KLF4/VEGF Signaling Axis in Pulmonary Artery Endothelial Cell Angiogenesis. Cell Physiol Biochem. 2017;41:2333-2349 pubmed publisher
    ..Overall, our study contributes to a better understanding of PAH pathogenesis. ..
  5. Burwick R, Kuo K, Brewer D, Druker B. Maternal, Fetal, and Neonatal Imatinib Levels With Treatment of Chronic Myeloid Leukemia in Pregnancy. Obstet Gynecol. 2017;129:831-834 pubmed publisher
    ..Imatinib is effective for CML in pregnancy, but caution is warranted in light of potentially unrecognized fetal and neonatal effects. ..
  6. Hochhaus A, Larson R, Guilhot F, Radich J, Branford S, Hughes T, et al. Long-Term Outcomes of Imatinib Treatment for Chronic Myeloid Leukemia. N Engl J Med. 2017;376:917-927 pubmed publisher
    ..Funded by Novartis Pharmaceuticals; IRIS numbers, NCT00006343 and NCT00333840 .). ..
  7. Chen Q, Wang S, Lin C, Chen S, Zhao X, Li Y. [ABIN1 is not involved in imatinib upregulating A20 to inhibit the activation of NF-?B pathway in Jurkat T cells]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2017;33:577-580 pubmed
    ..Conclusion IM could upregulate A20 protein to inhibit the activation of NF-?B pathway in Jurkat T cells, which was independent of the ABIN1 protein. ..
  8. Kaneko M, Nozawa H, Emoto S, Murono K, Sasaki K, Otani K, et al. Neoadjuvant Imatinib Therapy Followed by Intersphincteric Resection for Low Rectal Gastrointestinal Stromal Tumors. Anticancer Res. 2017;37:5155-5160 pubmed
    ..Neoadjuvant imatinib therapy and ISR for low rectal GISTs is a challenging, but promising, alternative to achieve complete resection margins and preserve anal function. ..
  9. Leoni V, Biondi A. Tyrosine kinase inhibitors in BCR-ABL positive acute lymphoblastic leukemia. Haematologica. 2015;100:295-9 pubmed publisher

More Information


  1. Georgiou G, Efthymiou A, Vardounioti I, Boutsikas G, Angelopoulou M, Vassilakopoulos T, et al. Development of acute myeloid leukemia with NPM1 mutation, in Ph-negative clone, during treatment of CML with imatinib. Leukemia. 2012;26:824-6 pubmed publisher
  2. de Lima L, Bueno C, Vivona D, Hirata R, Hirata M, Hungria V, et al. Relationship between SLCO1B3 and ABCA3 polymorphisms and imatinib response in chronic myeloid leukemia patients. Hematology. 2015;20:137-42 pubmed publisher
    Genetic variations in membrane transporters may contribute to imatinib mesylate (IM) resistance in chronic myeloid leukemia (CML)...
  3. Penn M, Kamath M. Novel mechanisms for maintaining endothelial barrier function in sepsis. Circulation. 2012;126:2677-9 pubmed publisher
  4. Kim I, Rhee C, Yeo C, Kang H, Lee D, Lee S, et al. Effect of tyrosine kinase inhibitors, imatinib and nilotinib, in murine lipopolysaccharide-induced acute lung injury during neutropenia recovery. Crit Care. 2013;17:R114 pubmed publisher
    ..Our data indicated that imatinib or nilotinib effectively attenuated LPS-induced ALI during neutropenia recovery. These results provide evidence for the therapeutic potential of imatinib and nilotinib in ALI during neutropenia recovery. ..
  5. Hong F, Mitchell C, Zantomio D. Gelatinous transformation of the bone marrow as a late morphological change in imatinib mesylate treated chronic myeloid leukaemia. Pathology. 2010;42:84-5 pubmed publisher
  6. Lu Y, Mao F, Li X, Zheng X, Wang M, Xu Q, et al. Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFR?) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2017;60:5099-5119 pubmed publisher
    ..It was worth noting that 31 inhibited GIST-T1 tumor growth (TGI = 81.5%) and even the BaF3-TEL-cKIT-T670I tumor progression (TGI = 41.9%, 1-resistant GISTs) at a dosage of 100 mg/kg/day without exhibiting apparent toxicity. ..
  7. Kurokawa Y, Yang H, Cho H, Ryu M, Masuzawa T, Park S, et al. Phase II study of neoadjuvant imatinib in large gastrointestinal stromal tumours of the stomach. Br J Cancer. 2017;117:25-32 pubmed publisher
    ..Neoadjuvant imatinib treatment for 6-9 months is a promising treatment for large gastric GISTs, allowing a high R0 resection rate with acceptable toxicity. ..
  8. Janssen J, Berendse H, Schuurhuis G, Merle P, Ossenkoppele G. A 51-year-old male CML patient with progressive hearing loss, confusion, ataxia, and aphasia during imatinib treatment. Am J Hematol. 2009;84:679-82 pubmed publisher
  9. Wu B, Liu M, Li T, Lin H, Zhong H. An economic analysis of high-dose imatinib, dasatinib, and nilotinib for imatinib-resistant chronic phase chronic myeloid leukemia in China: A CHEERS-compliant article. Medicine (Baltimore). 2017;96:e7445 pubmed publisher
    ..The results should be carefully explained due to the assumptions and limitations used in the study. ..
  10. Rókusz A, Veres D, Szücs A, Bugyik E, Mózes M, Paku S, et al. Ductular reaction correlates with fibrogenesis but does not contribute to liver regeneration in experimental fibrosis models. PLoS ONE. 2017;12:e0176518 pubmed publisher
    ..No evidences support the persistent antifibrotic property of imatinib or erlotinib. ..
  11. Jiao Y, Li G, Li Q, Ali R, Qin L, Li W, et al. mTOR (Mechanistic Target of Rapamycin) Inhibition Decreases Mechanosignaling, Collagen Accumulation, and Stiffening of the Thoracic Aorta in Elastin-Deficient Mice. Arterioscler Thromb Vasc Biol. 2017;37:1657-1666 pubmed publisher
    ..Our findings suggest that mTOR-sensitive perturbation of smooth muscle cell mechanosensing contributes to elastin aortopathy. ..
  12. Bazeos A, Marin D, Reid A, Gerrard G, Milojkovic D, May P, et al. hOCT1 transcript levels and single nucleotide polymorphisms as predictive factors for response to imatinib in chronic myeloid leukemia. Leukemia. 2010;24:1243-5 pubmed publisher
  13. O Connell E, Kamenyeva O, Lustigman S, Bell A, Nutman T. Defining the target and the effect of imatinib on the filarial c-Abl homologue. PLoS Negl Trop Dis. 2017;11:e0005690 pubmed publisher
    ..loa microfilariae before they are treated within the context of conventional mass drug administration. ..
  14. Druker B. Perspectives on the development of imatinib and the future of cancer research. Nat Med. 2009;15:1149-52 pubmed publisher
  15. Speight R, Nicolle A, Needham S, Verrill M, Bryon J, Panter S. Rare, germline mutation of KIT with imatinib-resistant multiple GI stromal tumors and mastocytosis. J Clin Oncol. 2013;31:e245-7 pubmed publisher
  16. Liu Q, Zhong G, Zhou W, Lin G. Initial application of transanal endoscopic microsurgery for high-risk lower rectal gastrointestinal stromal tumor after imatinib mesylate neoadjuvant chemotherapy: A case report. Medicine (Baltimore). 2017;96:e7538 pubmed publisher
    ..Neoadjuvant therapy with imatinib mesylate (IM) has achieved great success in GIST, which potentially extends the applications of function-preserving ..
  17. Lee K, Ouwehand I, Giannini A, Thomas N, Dibb N, Bijlmakers M. Lck is a key target of imatinib and dasatinib in T-cell activation. Leukemia. 2010;24:896-900 pubmed publisher
  18. Schork N. Personalized medicine: Time for one-person trials. Nature. 2015;520:609-11 pubmed publisher
  19. Yang F, Jin C, Fu D, Ni Q. Extra-gastrointestinal stromal tumor of the pancreas: clinical characteristics, diagnosis, treatment, and outcome. J Surg Oncol. 2011;103:739-40 pubmed publisher
  20. Maharsy W, Aries A, Mansour O, Komati H, Nemer M. Ageing is a risk factor in imatinib mesylate cardiotoxicity. Eur J Heart Fail. 2014;16:367-76 pubmed
    ..Chemotherapy-induced heart failure is increasingly recognized as a major clinical challenge. Cardiotoxicity of imatinib mesylate, a highly selective and effective anticancer drug belonging to the new class of tyrosine kinase inhibitors, ..
  21. Grant H, Jiang X, Stebbing J, Foroni L, Craddock C, Griffiths M, et al. Analysis of BCR-ABL1 tyrosine kinase domain mutational spectra in primitive chronic myeloid leukemia cells suggests a unique mutator phenotype. Leukemia. 2010;24:1817-21 pubmed publisher
  22. Perna F, Abdel Wahab O, Levine R, Jhanwar S, Imada K, Nimer S. ETV6-ABL1-positive "chronic myeloid leukemia": clinical and molecular response to tyrosine kinase inhibition. Haematologica. 2011;96:342-3 pubmed publisher
  23. Sharifnia T, Hong A, Painter C, Boehm J. Emerging Opportunities for Target Discovery in Rare Cancers. Cell Chem Biol. 2017;24:1075-1091 pubmed publisher
    ..Together, these advances motivate consideration of new research frameworks to accelerate rare cancer target discovery. ..
  24. Golub T. Counterpoint: Data first. Nature. 2010;464:679 pubmed publisher
  25. Joensuu H, Blay J, Comandone A, Martín Broto J, Fumagalli E, Grignani G, et al. Dovitinib in patients with gastrointestinal stromal tumour refractory and/or intolerant to imatinib. Br J Cancer. 2017;117:1278-1285 pubmed publisher
    ..Dovitinib is an active treatment for patients with GIST who are intolerant to imatinib or whose GIST progresses on imatinib. ..
  26. Fischer J, Dalhoff C, Schrey A, Graebner O, Michaelis S, Andrich K, et al. Dasatinib, imatinib and staurosporine capture compounds - Complementary tools for the profiling of kinases by Capture Compound Mass Spectrometry (CCMS). J Proteomics. 2011;75:160-8 pubmed publisher
    ..Besides sets of expected kinases we identified additional specific interactors; these off-targets may be of relevance in the view of the pharmacological profile of dasatinib and imatinib. ..
  27. Onaka T, Takahashi N, Miura M, Yonezawa A, Imada K, Sawada K. Pharmacokinetics of nilotinib in imatinib-resistant/intolerant chronic myeloid leukemia patients on hemodialysis for chronic renal failure. Am J Hematol. 2012;87:451 pubmed publisher
  28. Revheim M, Hole K, Bruland O, Reitan E, Bjerkehagen B, Julsrud L, et al. Multimodal functional imaging for early response assessment in GIST patients treated with imatinib. Acta Oncol. 2014;53:143-8 pubmed publisher
  29. Nieborowska Skorska M, Hoser G, Hochhaus A, Stoklosa T, Skorski T. Anti-oxidant vitamin E prevents accumulation of imatinib-resistant BCR-ABL1 kinase mutations in CML-CP xenografts in NSG mice. Leukemia. 2013;27:2253-4 pubmed publisher
  30. Horwitz R, Cullen M, Abell J, Christian J. Medicine. (De)personalized medicine. Science. 2013;339:1155-6 pubmed publisher
  31. Tzvetkov M, Seitz T, Bokelmann K, Mueller T, Brockmoller J, Koepsell H. Does the haplotype Met408-Del420, which was apparently predictive for imatinib efficacy, really exist and how strongly may it affect OCT1 activity?. Blood. 2014;123:1427-9 pubmed publisher
  32. Sotiropoulos G, Stamopoulos P, Kykalos S, Machairas N. Conventional transanal excision for a very low gastrointestinal stromal tumour. BMJ Case Rep. 2017;2017: pubmed publisher
    ..We herein report on a young patient with a >5?cm rectal GIST localised at 1?cm from the anorectal junction. ..
  33. Egan J. Targeting Stem Cells in Chronic Myeloid Leukemia with a PPAR-? Agonist. N Engl J Med. 2015;373:1973-5 pubmed publisher
    ..Combining a tyrosine kinase inhibitor (imatinib) and a thiazolidinedione (pioglitazone) is proposed for the treatment of chronic myeloid leukemia. ..
  34. Lin H, Roberts D, Kay J, Stankovic K. Sensorineural hearing loss following imatinib (Gleevec) administration. Otolaryngol Head Neck Surg. 2012;146:335-7 pubmed publisher
  35. Nishida T, Doi T. Rechallenge of drugs in the era of targeted therapy. Lancet Oncol. 2013;14:1143-5 pubmed publisher
  36. de Masson A, Bouaziz J, Peffault De Latour R, Wittnebel S, Ribaud P, Rubio M, et al. Limited efficacy and tolerance of imatinib mesylate in steroid-refractory sclerodermatous chronic GVHD. Blood. 2012;120:5089-90 pubmed publisher
  37. Louis A, Singh S, Gupta S, Sharma A. Primary GIST of the liver masquerading as primary intra-abdominal tumour: a rare extra-gastrointestinal stromal tumour (EGIST) of the liver. J Gastrointest Cancer. 2014;45:392-4 pubmed publisher
  38. Bixby D, Talpaz M. Mechanisms of resistance to tyrosine kinase inhibitors in chronic myeloid leukemia and recent therapeutic strategies to overcome resistance. Hematology Am Soc Hematol Educ Program. 2009;:461-76 pubmed publisher
    ..This review will describe the efforts at understanding the pathogenesis of imatinib resistance and the molecular rationale for the development of second- and now third-generation therapies for patients with CML. ..
  39. Papageorgiou S, Pappa V, Economopoulou C, Tsirigotis P, Konsioti F, Ionnidou E, et al. Dasatinib induces long-term remission in imatinib-resistant Philadelphia chromosome-positive acute megakaryoblastic leukemia but fails to prevent development of central nervous system progression. Leuk Res. 2010;34:e254-6 pubmed publisher
  40. Thakral B, Higa B, Venkataraman G, Velankar M. Bone marrow with gelatinous transformation associated with residual disease in imatinib mesylate-treated chronic myelogenous leukaemia (CML). Pathology. 2012;44:59 pubmed publisher
  41. Chen W, Kuang Y, Qiu H, Cao Z, Tu Y, Sheng Q, et al. Dual Targeting of Insulin Receptor and KIT in Imatinib-Resistant Gastrointestinal Stromal Tumors. Cancer Res. 2017;77:5107-5117 pubmed publisher
    ..Our findings suggest that combinatorial inhibition of IR and KIT warrants clinical evaluation as a novel therapeutic strategy in imatinib-resistant GISTs. Cancer Res; 77(18); 5107-17. ©2017 AACR. ..
  42. Bellora F, Dondero A, Corrias M, Casu B, Regis S, Caliendo F, et al. Imatinib and Nilotinib Off-Target Effects on Human NK Cells, Monocytes, and M2 Macrophages. J Immunol. 2017;199:1516-1525 pubmed publisher
    ..Our results contribute to better interpreting the off-target efficacy of TKIs in tumors and to envisaging strategies aimed at facilitating antitumor immune responses. ..
  43. Yap E, Norziha Z, Simbun A, Tumian N, Cheong S, Leong C, et al. MicroRNAs that affect the Fanconi Anemia/BRCA pathway are downregulated in imatinib-resistant chronic myeloid leukemia patients without detectable BCR-ABL kinase domain mutations. Leuk Res. 2017;59:32-40 pubmed publisher
    Chronic myeloid leukemia (CML) patients who do not achieve landmark responses following treatment with imatinib mesylate (IM) are considered IM-resistant...
  44. Xie Q, Lin Q, Li D, Chen J. Imatinib induces autophagy via upregulating XIAP in GIST882 cells. Biochem Biophys Res Commun. 2017;488:584-589 pubmed publisher
    ..The main effective treatment for GISTs is tyrosine kinase inhibitors, such as imatinib mesylate. However, GISTs respond to imatinib treatment eventually develop acquired resistance, which is a main ..
  45. Ubink I, Bloemendal H, Elias S, Brink M, Schwartz M, Holierhoek Y, et al. Imatinib treatment of poor prognosis mesenchymal-type primary colon cancer: a proof-of-concept study in the preoperative window period (ImPACCT). BMC Cancer. 2017;17:282 pubmed publisher NCT02685046 . Registration date: February 9, 2016. ..
  46. Vasconcelos A, Azevedo I, Melo F, Neves W, Azevedo A, Melo R. BCR-ABL1 transcript types showed distinct laboratory characteristics in patients with chronic myeloid leukemia. Genet Mol Res. 2017;16: pubmed publisher
    ..In agreement with published data, our results showed association of the BCR-ABL1 transcript e14a2 with thrombocytosis and the BCR-ABL1 transcript e13a2 with higher leukocytosis in patients with chronic myeloid leukemia. ..
  47. Silveira R, Fachel A, Moreira Y, de Souza C, Costa F, Verjovski Almeida S, et al. Protein-coding genes and long noncoding RNAs are differentially expressed in dasatinib-treated chronic myeloid leukemia patients with resistance to imatinib. Hematology. 2014;19:31-41 pubmed publisher
    ..In addition to protein-coding genes, lncRNAs have been recently implicated in pathways leading to tumorigenesis. Our data point to new possible regulatory elements involved in dasatinib resistance in CML. ..
  48. Zhang J, He Y, Zhu R, Du W, Xiao J. Deregulated expression of Cdc6 as BCR/ABL-dependent survival factor in chronic myeloid leukemia cells. Tumour Biol. 2017;39:1010428317713394 pubmed publisher
  49. Redaelli S, Piazza R, Rostagno R, Magistroni V, Perini P, Marega M, et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol. 2009;27:469-71 pubmed publisher
  50. Tefferi A, Levitt R, Lasho T, Knudson R, Ketterling R. Postimatinib therapy emergence of a new JAK2V617F clone and subsequent development of overt polycythemia vera in a patient with chronic myelogenous leukaemia. Eur J Haematol. 2010;85:86-7 pubmed publisher
  51. Breccia M, Finsinger P, Loglisci G, Latagliata R, Mancini M, Salaroli A, et al. The EUTOS score identifies chronic myeloid leukeamia patients with poor prognosis treated with imatinib first or second line. Leuk Res. 2012;36:e209-10 pubmed publisher
  52. Zhao Y, Wang J, Luo Y, Shi J, Zheng W, Tan Y, et al. Reduced-intensity allogeneic hematopoietic stem cell transplantation combined with imatinib has comparable event-free survival and overall survival to long-term imatinib treatment in young patients with chronic myeloid leukemia. Ann Hematol. 2017;96:1353-1360 pubmed publisher
    ..However, RIST + IM was more affordable than IM alone in a 10-year scale. Thus, RIST + IM could be considered as an alternative treatment option, especially when the patients have low EBMT risk scores and demand a definite cure for CML. ..
  53. Reber L, Starkl P, Balbino B, Sibilano R, Gaudenzio N, Rogalla S, et al. The tyrosine kinase inhibitor imatinib mesylate suppresses uric acid crystal-induced acute gouty arthritis in mice. PLoS ONE. 2017;12:e0185704 pubmed publisher
    ..Here we demonstrate that treatment with the tyrosine kinase inhibitor imatinib mesylate (imatinib) can suppress inflammation induced by injection of MSU crystals into subcutaneous air pouches or ..