Preferred Label : Vorbipiprant;
NCIt synonyms : Prostaglandin E2 Receptor Antagonist CR6086; EP4 Receptor Antagonist CR6086; PGE2 Receptor Antagonist CR6086; EP4 Antagonist CR6086;
NCIt definition : A small molecule, orally bioavailable antagonist of the prostaglandin E2 receptor
subtype 4 (PTGER4; EP4), with potential immunomodulating and antineoplastic activities.
Upon oral administration, vorbipiprant selectively targets and binds to EP4, thereby
inhibiting the binding of the immunosuppressive prostaglandin E2 (PGE2) to EP4 and
preventing the activation of EP4. This inhibits PGE2-EP4-mediated signaling and inhibits
the proliferation of tumor cells in which the PGE2-EP4 signaling pathway is overactivated.
In addition, EP4 inhibition prevents the activity of tumor-associated myeloid cells
(TAMCs) in the tumor microenvironment (TME) by inhibiting interleukin-23 (IL-23) production
and the IL-23-mediated expansion of T helper 17 (Th17) cells. EP4, a prostanoid receptor,
is a G protein-coupled receptor that is expressed in certain types of cancers; it
promotes tumor cell proliferation and invasion.;
UNII : SS2LQQ8094;
CAS number : 1417742-86-9;
Molecule name : CR-6086; CR 6086;
NCI Metathesaurus CUI : CL1779160;
Origin ID : C186659;
UMLS CUI : C5908098;
Semantic type(s)
- concept_is_in_subset
- has_target
