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Version: 17.06d (Release date: 2017-06-26)
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Imatinib Mesylate (Code C1687)

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Terms & Properties

Preferred Name: Imatinib Mesylate

Definition: The mesylate salt of imatinib, a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).

NCI-GLOSS Definition: A drug used to treat different types of leukemia and other cancers of the blood, gastrointestinal stromal tumors, skin tumors called dermatofibrosarcoma protuberans, and a rare condition called systemic mastocytosis. It is also being studied in the treatment of other types of cancer. Imatinib mesylate blocks the protein made by the bcr/abl oncogene. It is a type of tyrosine kinase inhibitor.

Display Name: Imatinib Mesylate

Label: Imatinib Mesylate

NCI Thesaurus Code: C1687 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C0939537  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide Monomethanesulfonate
CGP 57148
Imatinib Mesylate
imatinib mesylate
STI 571

External Source Codes: 
CAS Registry Number 220127-57-1 (see NLM ChemIDplus info)
FDA UNII Code 8A1O1M485B
ChEBI ID CHEBI:31690 (see ChEBI info)
NSC Code 716051 (see NCI DTP info)
PDQ Closed Trial Search ID 37862
PDQ Open Trial Search ID 37862 (check for NCI PDQ open clinical trial info)
UMLS CUI C0939537

Other Properties:
     Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For Philadelphia chromosome-positive chronic myelogenous leukemia and acute lymphocytic leukemia, gastrointestinal stromal tumor, hypereosinophillic syndrome, dermatofibrosarcoma protuberans, mutated-PDGFR myelodysplastic/myeloproliferative diseases.
Chemical_Formula C29H31N7O.CH4O3S
code C1687
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Imatinib
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: Yes  


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