Chapter title |
Imatinib Mesylate
|
---|---|
Chapter number | 1 |
Book title |
Small Molecules in Hematology
|
Published in |
Recent results in cancer research Fortschritte der Krebsforschung Progrès dans les recherches sur le cancer, January 2018
|
DOI | 10.1007/978-3-319-91439-8_1 |
Pubmed ID | |
Book ISBNs |
978-3-31-991438-1, 978-3-31-991439-8
|
Authors |
Cornelius F. Waller, Waller, Cornelius F. |
Abstract |
Imatinib mesylate (Gleevec, Glivec [Novartis, Basel, Switzerland], formerly referred to as STI571 or CGP57148B) represents the paradigm of a new class of anticancer agents, so-called small molecules. They have a high selectivity against a specific molecular target known to be the cause for the establishment and maintenance of the malignant phenotype. Imatinib is a rationally designed oral signal transduction inhibitor that specifically targets several protein tyrosine kinases, Abl, Arg (Abl-related gene), the stem cell factor receptor (c-KIT), platelet-derived growth factor receptor (PDGF-R), and their oncogenic forms, most notably BCR-ABL. Imatinib has been shown to have remarkable clinical activity in patients with chronic myeloid leukemia (CML) and malignant gastrointestinal stroma tumors (GIST) leading to its approval for treatment of these diseases. Treatment with imatinib is generally well tolerated with a low incidence of severe side effects. The most common adverse events include mild to moderate edema, muscle cramps, diarrhea, nausea, skin rashes, and myelosuppression. Several mechanisms of resistance have been identified. Clonal evolution, amplification, or overexpression of BCR-ABL as well as mutations in the catalytic domain, P-loop, and other mutations have been demonstrated to play a role in primary and secondary resistance to imatinib, respectively. Understanding of the underlying mechanisms of resistance has led to the development of new second- and third-generation tyrosine kinase inhibitors (see chapters on dasatinib, nilotinib, bosutinib, and ponatinib). |
X Demographics
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Unknown | 1 | 100% |
Demographic breakdown
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Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
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Egypt | 1 | <1% |
Unknown | 135 | 99% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Master | 20 | 15% |
Researcher | 18 | 13% |
Student > Bachelor | 15 | 11% |
Student > Doctoral Student | 12 | 9% |
Student > Ph. D. Student | 10 | 7% |
Other | 19 | 14% |
Unknown | 42 | 31% |
Readers by discipline | Count | As % |
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Medicine and Dentistry | 32 | 24% |
Pharmacology, Toxicology and Pharmaceutical Science | 18 | 13% |
Biochemistry, Genetics and Molecular Biology | 14 | 10% |
Agricultural and Biological Sciences | 13 | 10% |
Chemistry | 7 | 5% |
Other | 8 | 6% |
Unknown | 44 | 32% |