National Cancer Institute Thesaurus

Last uploaded: February 23, 2024
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Preferred Name

Osimertinib Mesylate
Synonyms

OSIMERTINIB MESYLATE

Osimertinib Mesylate

AZD9291 Mesylate

2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-, Methanesulfonate (1:1)

Tagrisso

Tagrix
Definitions

The mesylate salt form of osimertinib, a third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib covalently binds to and inhibits the activity of numerous mutant forms of EGFR, including the secondarily-acquired resistance mutation T790M, L858R, and exon 19 deletions, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.
ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C170266
CAS_Registry

1421373-66-1
code

C170266
Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923
Contributing_Source

CTRP

FDA
DEFINITION

The mesylate salt form of osimertinib, a third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib covalently binds to and inhibits the activity of numerous mutant forms of EGFR, including the secondarily-acquired resistance mutation T790M, L858R, and exon 19 deletions, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.
Display_Name

Osimertinib Mesylate
FDA_UNII_Code

RDL94R2A16
FULL_SYN

OSIMERTINIB MESYLATE

Osimertinib Mesylate

AZD9291 Mesylate

2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-, Methanesulfonate (1:1)

Tagrisso

Tagrix
Has_Free_Acid_Or_Base_Form

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116377
Has_Target

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C98503

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C126892

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C98515
label

Osimertinib Mesylate
NCI_META_CUI

CL1382757
Preferred_Name

Osimertinib Mesylate
prefixIRI

Thesaurus:C170266
Semantic_Type

Pharmacologic Substance
subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C2167

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C129825
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