Terms & Properties

Preferred Name:  Selpercatinib

Definition:  An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, selpercatinib selectively binds to and targets wild-type RET as well as various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. In addition, selpercatinib targets, binds to and inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and 3 (VEGFR3), and fibroblast growth factor receptor 1 (FGFR1), 2 (FGFR2), and 3 (FGFR3). RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.

Display Name:  Selpercatinib

Label:  Selpercatinib

NCI Thesaurus Code:  C134987 (Search for linked caDSR metadata)   (search value sets)

NCI Metathesaurus Link:  CL522497  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)

6-(2-Hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo(3.1.1)heptan-3-yl)pyridin-3-yl)pyrazolo(1,5-a)pyridine-3-carbonitrile

LOXO 292

LOXO-292

LOXO292

RET Inhibitor LOXO-292

RET Kinase Inhibitor LOXO-292

Retevmo

Retsevmo

Selpercatinib

SELPERCATINIB

WHO 10967

External Source Codes: 

CAS Registry Number	2152628-33-4 (see NLM ChemIDplus info)
NCI Drug Dictionary ID	789226 (see NCI Drug Dictionary info)
FDA UNII Code	CEGM9YBNGD
PDQ Closed Trial Search ID	789226
PDQ Open Trial Search ID	789226
NCI META CUI	CL522497

Other Properties:

Name	Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For	Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC); • Adult and pediatric patients >=12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy; • Adult and pediatric patients >=12 years of age with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).
code	C134987
Contributing_Source	CTRP
Contributing_Source	FDA
Contributing_Source	GDC
Contributing_Source	HemOnc
Maps_To	Selpercatinib
	Target_Terminology: GDC       Relationship_to_Target: Has Synonym       Target_Term_Type: PT       Target_Code: therapeutic_agents
Semantic_Type	Pharmacologic Substance

Additional Concept Data: 

Defined Fully by Roles: No

URL:https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=ncit&code=C134987