E7046 is a specific, orally bioavailable EP4 antagonist (IC50: 13.5 nM, Ki: 23.14 nM), exhibiting anti-tumor activities.

EP4:13.5 nM, EP4:23.14 nM (Ki)

Through selective EP4 antagonism, E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells [1].

E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. The blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells [1]. In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significantly better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors [2].