ENB-003

ENB-003 is a first-in-class, selective and potent small molecule inhibitor of the endothelin B receptor (ETBR), a G-protein-coupled receptor overexpressed in various solid tumors. ETBR plays a key role in tumor cell proliferation, invasion, epithelial-mesenchymal transition (EMT), angiogenesis, and immune evasion by blocking T-cell trafficking. By antagonizing ETBR, ENB-003 aims to overcome resistance to immunotherapies such as anti-PD-1 (e.g., pembrolizumab) and CAR-T therapies. Preclinical studies have shown that ENB-003 enhances the efficacy of these immunotherapies across multiple cancer types. Clinically, it is being investigated primarily for platinum-resistant/refractory ovarian cancer, pancreatic cancer, malignant melanoma, and other advanced solid tumors—often in combination with pembrolizumab—with promising early results including disease control and objective responses in heavily pre-treated patients[1][3][4][5][6][7][8][9].

Other names

sodium bispiperidine-carboxamido-dimethylpenatnamido-methoxycarbonyl-indol-propanamidohexanoate