Preferred Label : Cambritaxestat;
NCIt synonyms : ATX Inhibitor IOA-289; ENPP2 Inhibitor IOA-289; Autotaxin Inhibitor IOA-289;
NCIt definition : An orally bioavailable small molecule inhibitor of autotaxin (ATX; ectonucleotide
pyrophosphatase/phosphodiesterase family member 2; ENPP2), with potential antifibrotic
and antineoplastic activities. Upon oral administration, cambritaxestat targets and
binds to both the substrate pocket and the lysophosphatidic acid (LPA) carrier channel
of ATX, thereby inhibiting the activity of ATX. This both directly inhibits the proliferation
of tumor cells and reduces fibrosis in the tumor microenvironment (TME), allowing
lymphocytes to infiltrate into the tumor and enhancing immune responses against tumor
cells. ATX, a secreted glycoprotein with lysophospholipase D activity, hydrolyzes
lysophosphatidylcholine (LPC) to LPA. LPA-mediated signaling plays an important role
in cellular migration, proliferation and survival in fibrotic response. ATX and LPA
are overexpressed in many tumors.;
UNII : LYY3P2KA27;
CAS number : 1979939-16-6;
Molecule name : IOA 289; IOA-289;
NCI Metathesaurus CUI : CL1912837;
Origin ID : C192808;
UMLS CUI : C5785431;
Semantic type(s)
- concept_is_in_subset
- has_target
