Imatinib mesylate (sold as Gleevec in the USA and Glivec elsewhere) is the first effective drug treatment for gastrointestinal stromal tumor (GIST cancer). The drug is manufactured by Novartis Pharmaceuticals of Basel, Switzerland and New Hanover, New Jersey. It was approved by the FDA in February 2002 for treatment of metastatic or unresectable (inoperable) gastrointestinal stromal tumor (GIST). In 2008 it was FDA-approved as “adjuvant treatment” for GIST, meaning Gleevec is taken after surgical removal of a high-risk primary GIST to prevent recurrence.
Imatinib (Gleevec) is the first marketed “molecularly targeted therapy” for cancer. This means that the drug affects only those cells that express highly specific targets, in contrast to conventional cancer chemotherapies that affect all fast-growing cells in the body. The targets of imatinib in GIST patients are two growth-factor receptors named KIT and PDGFRA. The drug is also used against chronic myelogenous leukemia, a disease in which affected patients have an abnormal protein called BCR-ABL that is targeted by imatinib.
Information about imatinib treatment for GIST is divided among these subpages (click to link to page):
-
Imatinib (Gleevec) Basics
-
Imatinib for Unresectable or Metastatic GIST
-
Post-Surgery Preventive Imatinib (Adjuvant Gleevec)
-
Gleevec Side Effects and Tips
-
Pregnancy and Gleevec
- Measuring Imatinib (Gleevec) Blood Plasma Levels
References and Selected Bibliography |
Altered bone and mineral metabolism in patients receiving imatinib mesylate. |
Berman E, Nicolaides M, Maki RG, Fleisher M, Chanel S, Scheu K, Wilson BA, Heller G, Sauter NP. N Engl J Med. 2006 May 11;354(19):2006-13. PMID: 16687713 |
Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. |
Kerkela 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. Nat Med. 2006 Jul 23; [Epub ahead of print] PMID 16862153 |
KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours. |
Debiec-Rychter M, Sciot R, Le Cesne A, Schlemmer M, Hohenberger P, van Oosterom AT, Blay JY, Leyvraz S, Stul M, Casali PG, Zalcberg J, Verweij J, Van Glabbeke M, Hagemeijer A, Judson I; EORTC Soft Tissue and Bone Sarcoma Group; The Italian Sarcoma Group; Australasian GastroIntestinal Trials Group. Eur J Cancer. 2006 May;42(8):1093-103. PMID: 16624552 |
Update of phase I study of imatinib (STI571) in advanced soft tissue sarcomas and gastrointestinal stromal tumors: a report of the EORTC Soft Tissue and Bone Sarcoma Group. |
van Oosterom AT, Judson IR, Verweij J, Stroobants S, Dumez H, Donato di Paola E, Sciot R, Van Glabbeke M, Dimitrijevic S, Nielsen OS; European Organisation for Research and Treatment of Cancer Soft Tissue and Bone Sarcoma Group. Eur J Cancer. 2002 Sep;38 Suppl 5:S83-7. PMID: 12528778 |
Gastrointestinal stromal tumor: 5 years later. |
van der Zwan SM, DeMatteo RP. Cancer. 2005 Nov 1;104(9):1781-8. Review. PMID: 16136600 |
New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. |
Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, Verweij J, Van Glabbeke M, van Oosterom AT, Christian MC, Gwyther SG. J Natl Cancer Inst. 2000 Feb 2;92(3):205-16. PMID: 10655437 |
Is there a role for surgery in patients with “unresectable” cKIT+ gastrointestinal stromal tumors treated with imatinib mesylate? |
Scaife CL, Hunt KK, Patel SR, Benjamin RS, Burgess MA, Chen LL, Trent J, Raymond AK, Cormier JN, Pisters PW, Pollock RE, Feig BW. Am J Surg. 2003 Dec;186(6):665-9. PMID: 14672776 |
Gastrointestinal stromal tumors and the evolution of targeted therapy. |
Sanborn RE, Blanke CD. Clin Adv Hematol Oncol. 2005 Aug;3(8):647-57. Review. PMID: 16167051 |
Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia. |
O’Brien SG, Meinhardt P, Bond E, Beck J, Peng B, Dutreix C, Mehring G, Milosavljev S, Huber C, Capdeville R, Fischer T. Br J Cancer. 2003 Nov 17;89(10):1855-9. PMID: 14612892 |
Severe hepatic injury caused by imatinib mesylate administered for the treatment of chronic myeloid leukemia and the efficacy of prednisolone for its management. |
Ikuta K, Torimoto Y, Jimbo J, Inamura J, Shindo M, Sato K, Tokusashi Y, Miyokawa N, Kohgo Y. Int J Hematol. 2005 Nov;82(4):343-6. PMID: 16298828 |
Indications for imatinib mesylate therapy and clinical management. |
Guilhot F. Oncologist. 2004;9(3):271-81. Review. PMID: 15169982 |
Nursing implications of imatinib as molecularly targeted therapy for |
Griffin JM, Amand MS, Demetri GD. Clin J Oncol Nurs. 2005 Apr;9(2):161-9. Review. PMID: 15853160 |
Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal |
Demetri GD, von Mehren M, Blanke CD, Van den Abbeele AD, Eisenberg B, Roberts PJ, Heinrich MC, Tuveson DA, Singer S, Janicek M, Fletcher JA, Silverman SG, Silberman SL, Capdeville R, Kiese B, Peng B, Dimitrijevic S, Druker BJ, Corless C, Fletcher CD, Joensuu H. N Engl J Med. 2002 Aug 15;347(7):472-80. PMID: 12181401 |
Imatinib and gastrointestinal stromal tumors: Where do we go from here? |
De Giorgi U, Verweij J. Mol Cancer Ther. 2005 Mar;4(3):495-501. Review. PMID: 15767559 |
Biology of gastrointestinal stromal tumors. |
Corless CL, Fletcher JA, Heinrich MC. J Clin Oncol. 2004 Sep 15;22(18):3813-25. PMID: 15365079 |
PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib. |
Corless CL, Schroeder A, Griffith D, Town A, McGreevey L, Harrell P, Shiraga S, Bainbridge T, Morich J, Heinrich MC. J Clin Oncol. 2005 Aug 10;23(23):5357-64. Epub 2005 May 31. Review.PMID: 15928335 |
CT evaluation of the response of gastrointestinal stromal tumors after imatinib mesylate treatment: a quantitative analysis correlated with FDG PET findings. |
Choi H, Charnsangavej C, de Castro Faria S, Tamm EP, Benjamin RS, Johnson MM, Macapinlac HA, Podoloff DA. AJR Am J Roentgenol. 2004 Dec;183(6):1619-28. PMID: 15547201 |
Consensus meeting for the management of gastrointestinal stromal tumors. Report of the GIST Consensus Conference of 20-21 March 2004, under the auspices of ESMO. |
Blay JY, Bonvalot S, Casali P, Choi H, Debiec-Richter M, Dei Tos AP, Emile JF, Gronchi A, Hogendoorn PC, Joensuu H, Le Cesne A, McClure J, Maurel J, Nupponen N, Ray-Coquard I, Reichardt P, Sciot R, Stroobants S, van Glabbeke M, van Oosterom A, Demetri GD; GIST consensus meeting panelists. Ann Oncol. 2005 Apr;16(4):566-78. Review. Erratum in: Ann Oncol. 2005 Jun;16(6):993. Mac Clure, J [corrected to McClure, J]. PMID: 15781488 |
State-of-the art therapy for gastrointestinal stromal tumors. |
Blanke CD, Corless CL. Cancer Invest. 2005;23(3):274-80. Review. PMID: 15945512 |
Low dose versus high dose imatinib for gastrointestinal stromal tumors. |
Blanke C. Nat Clin Pract Gastroenterol Hepatol. 2005 Feb;2(2):76-7. PMID: 16265122 |
Management of gastrointestinal stromal tumors in the imatinib era: selected case studies. |
Benjamin RS, Blanke CD, Blay JY, Bonvalot S, Eisenberg B. Oncologist. 2006 Jan;11(1):9-20. PMID: 16401709 |
Resection of residual disease in patients with metastatic gastrointestinal stromal tumor. |
Bauer S, Hartmann JT, de Wit M, Lang H, Grabellus F, Antoch G, Niebel W, Erhard J, Ebeling P, Zeth M, Taeger G, Seeber S, Flasshove M, Schutte J. Int J Cancer. 2005 Nov 1;117(2):316-25. PMID: 15900603 |
Ungrouped links |
Imatinib does not induce cardiac left ventricular failure in gastrointestinal stromal tumours patients: Analyis of EORTC-ISG-AGITG study 62005. |
Verweij J, Casali PG, Kotasek D, Le Cesne A, Reichard P, Judson IR, Issels R, van Oosterom AT, Van Glabbeke M, Blay JY. Eur J Cancer. 2007 Mar 1; [Epub ahead of print] PMID: 17336514 |