TPST-1495 + pembrolizumab

TPST-1495 + pembrolizumab is a combination therapy under clinical investigation for the treatment of advanced solid tumors. **TPST-1495** is an orally bioavailable, first-in-class, small molecule dual antagonist of the prostaglandin E2 (PGE2) receptors EP2 and EP4. It selectively inhibits PGE2-mediated tumor-promoting and immune-suppressive pathways while sparing EP1 and EP3, which are considered antitumorigenic. **Pembrolizumab** is a monoclonal antibody that acts as an immune checkpoint inhibitor targeting the programmed cell death protein 1 (PD-1) receptor, thereby potentiating anti-tumor immune responses. The rationale for the combination is to block both PGE2-mediated immune suppression and inhibitory PD-1 signaling in the tumor microenvironment, potentially overcoming resistance to checkpoint inhibitors and enhancing anti-tumor efficacy. The combination is being tested mainly in solid tumors including colorectal cancer, non-small cell lung cancer, endometrial cancer, and others[1][3][5][7].

Other names

TPST-1495 + Keytruda