gs 9674

Taminadenant, also known as PBF-509 and NIR-178, is a potent and orally active adenosine A2A receptor antagonist with potential antineoplastic activity. PBF-509 selectively binds to and inhibits A2AR expressed on T lymphocytes. This abrogates the adenosine A2AR-mediated inhibition of T-lymphocytes and activates a T-cell-mediated immune response against tumor cells, thereby reducing proliferation of susceptible tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of T-cells and, upon activation by adenosine, inhibits their proliferation and activation. Adenosine is often produced in excess by cancer cells.

Cilofexor, also known as GS-9674, is a farnesoid X receptor (FXR) agonist. The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC. In clinical study, cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with PSC.

Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.