Imatinib mesylate acts in metastatic or unresectable gastrointestinal stromal tumor by targeting KIT receptors--a review.
Gastrointestinal stromal tumor (GIST) is the most common mesenchymal malignancy of the gastrointestinal tract. This tumor is resistant to conventional chemotherapy and radiotherapy. Although surgery has been the only effective treatment for GIST to date, it is not enough to manage metastatic GIST. Imatinib mesylate, a KIT tyrosine kinase inhibitor, is an oral agent that has been found to have a dramatic antitumor effect on metastatic GIST with either wild-type or mutant KIT. Although imatinib mesylate has been used in GIST treatment for several years, its use marks a new era of molecular targeting therapy. While several issues remain, they should be clarified by the current clinical trials and associated laboratory studies.
Sawaki
Akira
A
Department of Gastroenterology, Aichi Cancer Center Hospital, 1-1 Kanokoden, Chikusa-ku, 464-0021 Nagoya, Japan. asawaki@aichi-cc.jp
Yamao
Kenji
K
D001549:Benzamides; D016503:Drug Delivery Systems; D005770:Gastrointestinal Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D006801:Humans; D000068877:Imatinib Mesylate; D009362:Neoplasm Metastasis; D010879:Piperazines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D019009:Proto-Oncogene Proteins c-kit / Q000187:drug effects*; D011743:Pyrimidines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases; D019009:Proto-Oncogene Proteins c-kit