An AKR1C3-specific prodrug with potent anti-tumor activities against T-ALL

Abstract

AKR1C3 overexpression has been reported in various types of cancers, including T-ALL. AST-006 (TH-3424), an AKR1C3-specific prodrug, was reported recently to have potent cytotoxicity against liver cancer cells overexpressing AKR1C3 and T-ALL. In this study, AST-006 demonstrated potent anti-tumor activity against different T-ALL cell lines in vitro and in vivo, including patient-derived xenograft (PDX) model. AST-006 also exhibited minimal cytotoxicity against primary human T-cells in vitro and lymphocytes in cynomolgus monkeys in vivo, indicating that AST-006 is a promising therapeutic for T-ALL.

Keywords:

• T-ALL
• AKR1C3
• prodrug
• biomarker
• AST-006
• B-ALL

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This project was financially supported by Department of Science and Technology of Guangdong Province (PR China) [2016A050503028].