THRESHOLD IS EVALUATING TH-3424, FOR TUMORS THAT OVEREXPRESS AN ENZYME, AKR1C3, THAT MAKES THEM RESISTANT TO RADIATION THERAPY AND CHEMOTHERAPY.
TH-3424 is a novel small-molecule that targets cancers that overexpress high levels of the enzyme aldo-keto reductase 1C3 (AKR1C3). Tumors overexpressing AKR1C3 can be resistant to radiation therapy and chemotherapy. TH-3424 is a prodrug that selectively releases a potent DNA cross-linking agent in the presence of AKR1C3. TH-3424 is being evaluated for the potential treatment of hepatocellular (liver) cancer (HCC), castration-resistant prostate cancer (CRPC), T-cell acute lymphoblastic leukemias (T-ALL), and other cancers expressing high levels of aldo-keto reductase family 1 member C3 (AKR1C3). Preliminary nonclinical toxicology studies suggested an adequate therapeutic index that the Company believes warrants continued development. The Company is conducting Investigational New Drug (IND)-enabling toxicology studies of TH-3424 in collaboration with Ascenta Pharmaceuticals, Ltd.