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Version: 17.06d (Release date: 2017-06-26)
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Lorlatinib (Code C113655)

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Terms & Properties

Preferred Name: Lorlatinib

Definition: An orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. Upon administration, lorlatinib binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, PF-06463922 is able to cross the blood brain barrier. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.

Display Name: Lorlatinib

Label: Lorlatinib

NCI Thesaurus Code: C113655 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3827088  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
2H-4,8-Methenopyrazolo(4,3-H)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile, 7-amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-, (10R)-
7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile
Lorlatinib
LORLATINIB
PF-06463922

External Source Codes: 
CAS Registry Number 1454846-35-5 (see NLM ChemIDplus info)
FDA UNII Code OSP71S83EU
PDQ Closed Trial Search ID 756930
PDQ Open Trial Search ID 756930 (check for NCI PDQ open clinical trial info)
UMLS CUI C3827088

Other Properties:
     Name Value (qualifiers indented underneath)
code C113655
Contributing_Source CTRP
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C113655

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