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Grapiprant + pembrolizumab is an investigational combination therapy currently in early-phase clinical trials for advanced or metastatic cancers, specifically microsatellite stable colorectal cancer (MSS CRC) and non-small cell lung cancer (NSCLC) that have progressed following standard therapies. Grapiprant is a small molecule antagonist of the prostaglandin E2 EP4 receptor, intended to reduce inflammation and potentially modulate tumor-promoting effects of prostaglandin signaling. Pembrolizumab is a monoclonal antibody targeting the programmed cell death protein 1 (PD-1) receptor, functioning as a checkpoint inhibitor to enhance the immune system’s recognition and destruction of tumor cells. Together, this combination aims to exploit complementary pathways: direct immunostimulation (pembrolizumab) and inhibition of inflammation-related tumor growth signals (grapiprant) to potentially increase antitumor activity beyond either agent alone[1][2][3][4][5][6][7].
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