- Also called:
- STI571
- Related Topics:
- anticancer drug
imatinib
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What is imatinib?
Imatinib is an anticancer drug, approved by the FDA in 2001, primarily for treating chronic myelogenous leukemia (CML). It was later approved for advanced gastrointestinal stromal tumors (GISTs). Unlike traditional anticancer agents, Imatinib targets abnormal proteins specific to cancer cells, such as bcr-abl tyrosine kinase in CML cells and c-kit in GIST cells, which reverses the effects of these kinases by blocking the proliferation of the cells. This targeted approach has led to a five-year survival rate of nearly 90 percent for previously untreated CML patients. Imatinib is administered orally, with mild to moderate side effects including gastrointestinal upset, edema, bone pain, and fatigue.
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What type of health problem is imatinib used to treat?
Imatinib is an anticancer drug, also known as Gleevec, that doctors use mainly to treat chronic myelogenous leukemia (CML). The FDA first approved it in 2001 for CML treatment and, in 2002, for treating advanced gastrointestinal stromal tumors (GISTs). GISTs are rare cancers affecting interstitial cells, which regulate the gastrointestinal tract's autonomic nervous function. Clinical trials are testing how well imatinib works against other cancers.
Imatinib aims at abnormal proteins that encourage the growth and survival of cancer cells unique to these cells. It can reverse CML effects by blocking the proliferation of cells that possess the bcr-abl tyrosine kinase and works similarly in GIST patients with abnormal activity of a tyrosine kinase called c-kit.
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How does imatinib work in the body?
Imatinib is an anticancer drug that treats chronic myelogenous leukemia (CML) and advanced gastrointestinal stromal tumors (GISTs). Unlike traditional anticancer agents, Imatinib targets abnormal proteins that promote the growth and survival of cancer cells and are unique to these cells. Imatinib inhibits bcr-abl tyrosine kinase, an enzyme found in CML cells with the Philadelphia chromosome genetic defect. The abnormal kinase stimulates the continuous proliferation of bone marrow stem cells, increasing myelogenous cells and causing symptoms like fatigue and spleen enlargement. Imatinib blocks the proliferation of cells with bcr-abl tyrosine kinase, reversing these effects. It works similarly in GIST patients, targeting the tyrosine kinase called c-kit.
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What kinds of cancer can be treated with imatinib?
Imatinib is an anticancer drug used to treat chronic myelogenous leukemia (CML) and advanced gastrointestinal stromal tumors (GISTs). Imatinib is designed to target abnormal proteins that promote the growth of cancer cells. It inhibits an enzyme called bcr-abl tyrosine kinase, which occurs only in CML cells carrying a genetic defect known as the Philadelphia chromosome. Imatinib is typically used in patients newly diagnosed with CML and in patients experiencing CML blast crisis. It is only given to GIST patients who have tumors that cannot be removed surgically or that have metastasized.
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Are there any common side effects of taking imatinib?
Common, mild to moderate side effects of imatinib include gastrointestinal upset, edema (fluid retention), bone pain, and fatigue. Severe edema can occur in some patients, leading to swelling in the lower legs and difficulty breathing. Elderly patients may face a higher risk of side effects like edema, anemia, and heart failure. Imatinib can also interfere with liver metabolism of drugs like warfarin and phenytoin, causing toxicity or reduced drug activity.
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Why is imatinib considered an important drug in cancer treatment?
Imatinib is an important anticancer drug, primarily for treating chronic myelogenous leukemia (CML). Approved in 2001, it targets abnormal proteins that promote cancer cell growth, unlike traditional chemotherapy that affects all cells.
Imatinib's success marks a milestone, proving targeted therapies can be more effective and safer. It inhibits bcr-abl tyrosine kinase, found in CML cells with the Philadelphia chromosome, which causes an increase in myelogenous cells. By blocking this enzyme, Imatinib reverses these effects. It is also used to treat gastrointestinal stromal tumors (GISTs). Because targeted drugs attack only the molecules responsible for specific tumor cell behavior, they are less toxic to normal cells compared with traditional chemotherapeutic agents.
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imatinib, anticancer drug used primarily in the treatment of chronic myelogenous leukemia (CML). Imatinib was approved by the U.S. Food and Drug Administration in 2001 under the trade name Gleevec for the treatment of CML. The following year it was approved for the treatment of advanced gastrointestinal stromal tumours (GISTs), which are rare cancers affecting interstitial cells that regulate the autonomic nervous function of the gastrointestinal tract. Clinical trials investigating the efficacy of imatinib against other types of cancers are ongoing.
Imatinib is designed to target abnormal proteins that promote the growth and survival of cancer cells and that are unique to these cells. This differs from traditional anticancer agents, which act on general mechanisms controlling cell replication or programmed cell death (apoptosis) and which do not differentiate between cancer cells and normal cells. Imatinib is highly effective—the five-year survival rate for previously untreated CML patients is nearly 90 percent. Imatinib’s success clinically has come to represent an important milestone in the advancement of cancer treatment, since it demonstrated that targeted therapies could be more effective and safer than traditional nonselective anticancer agents. Imatinib served as a model for the subsequent development of other selective anticancer drugs, which as a group are known as targeted therapies.
Imatinib inhibits an enzyme called bcr-abl tyrosine kinase, which occurs only in CML cells carrying a genetic defect known as the Philadelphia chromosome. The abnormal kinase stimulates the continuous proliferation of bone marrow stem cells that give rise to myelogenous cells (granulocytes and macrophages). This causes an increase in the number of myelogenous cells in the body, leading to symptoms such as fatigue and enlargement of the spleen. However, imatinib can reverse these effects by blocking the proliferation of cells that possess the bcr-abl tyrosine kinase. Imatinib works similarly in patients affected by GIST, which arises from the abnormal activity of a tyrosine kinase called c-kit.
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Imatinib is administered orally and is typically used in patients who are newly diagnosed with CML and in patients who are experiencing CML blast crisis. Blast crisis occurs when mature myelogenous cells acquire the ability to replicate uncontrollably, causing a dramatic increase in the number of immature, or blast, cells circulating in the body. Imatinib is given only to GIST patients who have tumours that cannot be removed surgically or that have metastasized (spread to other parts of the body). Mild to moderate side effects of the drug include gastrointestinal upset, edema (fluid retention), bone pain, and fatigue. In some patients edema is severe and can lead to swelling in the lower legs and to difficulty breathing. Elderly patients appear to be at increased risk of certain side effects, including edema, anemia, and heart failure. Imatinib interferes with the liver’s metabolism of a variety of other agents, including warfarin and phenytoin. These interactions can lead to severe toxicity or to decreased drug activity.