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