sco-101

SCO-101 is a novel oral small molecule developed as an add-on therapy to potentiate the effects of established anti-cancer agents. It acts primarily by inhibiting the ATP binding cassette transporter subfamily G member 2 (ABCG2), a drug efflux pump and cancer stem-cell marker. By blocking ABCG2, SCO-101 increases intracellular concentrations of cytotoxic chemotherapy drugs in cancer cells—especially those with high ABCG2 expression—thereby enhancing their efficacy. Additionally, SCO-101 inhibits the liver enzyme UGT1A1 (UDP-glucuronosyltransferase 1A1), which metabolizes several drugs including SN-38 (the active metabolite of irinotecan). This inhibition leads to increased plasma exposure and half-life of SN-38 when combined with irinotecan. SCO-101 is also described as a chloride channel antagonist and has been investigated for its ability to overcome resistance in metastatic colorectal cancer and other solid tumors[1][4][7][9].

Brand names

Endovion

Other names

N-[4-bromo-2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]-N'-[3,5-bis(trifluoromethyl)phenyl]urea