evofosfamide + sunitinib

Evofosfamide (formerly known as TH-302) is a hypoxia-activated prodrug designed to target tumor cells in low oxygen environments. Upon activation in hypoxic regions of tumors, it releases bromo-isophosphoramide mustard, a DNA alkylator that induces selective tumor cell death. Sunitinib is an oral small molecule inhibitor of multiple receptor tyrosine kinases (RTKs), including those for platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR), leading to reduced tumor vascularization and increased cancer cell apoptosis. The combination has been investigated for synergistic anti-tumor effects, particularly in renal cell carcinoma and pancreatic neuroendocrine tumors (panNETs). Preclinical studies suggest that sunitinib-induced hypoxia may enhance the activation of evofosfamide within tumors[1][2][3][4][5][6].

Brand names

Sutent

Other names

TH-302 + sunitinibevofosfamide + sunitinib