DTP-348

DTP-348 is an orally bioavailable small molecule inhibitor of carbonic anhydrase IX (CAIX), a hypoxia-inducible transmembrane glycoprotein highly expressed in solid tumors. By inhibiting CAIX, DTP-348 disrupts the reversible conversion of carbon dioxide and water to carbonic acid, protons, and bicarbonate ions, thereby reducing extracellular acidification in hypoxic tumor environments. This mechanism impairs tumor growth and can sensitize tumors to radiotherapy. DTP-348 belongs to the nitroimidazole class and incorporates a sulfamide moiety as a zinc-binding group for potent CAIX inhibition. It has demonstrated nanomolar-range inhibition of CAIX in vitro (Ki = 8.3 nM) and has shown efficacy in preclinical models with limited toxicity at relevant concentrations. The drug is under investigation for use as both a direct anticancer agent and as a radiosensitizer, particularly targeting advanced solid tumors[1][4][5][6].

Other names

2-(2-methyl-5-nitro-1H-imidazol-1-yl) ethylsulfamide