National Cancer Institute Thesaurus

Last uploaded: February 23, 2024
Preferred Name

Osimertinib

Synonyms

OSIMERTINIB

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

Mereletinib

Osimertinib

AZD-9291

AZD9291

Definitions

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#C116377

Accepted_Therapeutic_Use_For

metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC)

CAS_Registry

1421373-65-0

code

C116377

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712

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

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C201600

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

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784

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

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C177537

Contributing_Source

CTRP

FDA

GDC

HemOnc

DEFINITION

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

FDA_UNII_Code

3C06JJ0Z2O

FULL_SYN

OSIMERTINIB

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

Mereletinib

Osimertinib

AZD-9291

AZD9291

Has_Salt_Form

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

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

Is_Value_For_GDC_Property

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1909

label

Osimertinib

Maps_To

Osimertinib

NCI_Drug_Dictionary_ID

747632

PDQ_Closed_Trial_Search_ID

747632

PDQ_Open_Trial_Search_ID

747632

Preferred_Name

Osimertinib

prefixIRI

Thesaurus:C116377

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C3896906

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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