AKR1C3 Enzyme Prodrug
OBI-3424 is a first-in-class novel small-molecule prodrug that selectively targets cancers overexpressing the enzyme aldo-keto reductase 1c3 (AKR1C3), selectively releases a potent DNA alkylating agent in the presence of the AKR1C3 enzyme. This selective mode of activation distinguishes OBI-3424 from traditional alkylating agents such as cyclophosphamide and ifosfamide which are non-selective.
AKR1C3 overexpression has been documented in a number of treatment-resistant and difficult to treat cancers including: hepatocellular carcinomas (HCC), castrate-resistant prostate cancer (CRPC) and T-cell acute lymphoblastic leukemia (T-ALL).
Furthermore, individualized patient selection by staining for AKR1C3 overexpression by immunohistochemistry can be performed to identify patients with other tumor types most likely to respond to treatment with OBI-3424, and thus offering the possibility for a streamlined clinical development strategy.
OBI Pharma plans an Investigational New Drug (IND) application filing with the U.S. Food and Drug Administration (FDA) in early 2018 and Phase 1 clinical testing during 1H, 2018.
OBI Pharma has OBI 3424 worldwide rights for the exception of the following countries, which Ascenta Pharma has rights: China, Hong Kong, Macao, Taiwan, Japan, South Korea, Singapore, Malaysia, Thailand, Turkey and India.
AACR-NCI-EORTC 2017 International Conference on Molecular Targets and Cancer Therapeutics, Philadelphia, PA.(USA), Oct. 26-30, 2017
“The AKR1C3-Activated Prodrug OBI-3424 Exerts Profound In Vivo Efficacy Against Preclinical Models of T-Cell Acute Lymphoblastic Leukemia (T-ALL); a Pediatric Preclinical Testing Consortium Study”, presented by Prof. Richard B. Lock, PhD.
AACR 2016 Annual Meeting, New Orleans, LA (USA), April 16-20, 2016
“Broad In Vitro and In Vivo Antitumor Activity of TH-3424: Preclinical Rationale for a Highly Selective AKR1C3 Prodrug for Treating Cancer”, presented by Dr. Jianxin Duan, PhD.