Fig. 1: Reduction of OBI-3424 by AKR1C3 in the presence of NADPH to produce the cytotoxic agent OBI-2660. | British Journal of Cancer

Fig. 1: Reduction of OBI-3424 by AKR1C3 in the presence of NADPH to produce the cytotoxic agent OBI-2660.

From: Phase 1 dose-escalation study evaluating the safety, pharmacokinetics, and clinical activity of OBI-3424 in patients with advanced or metastatic solid tumors

Fig. 1

In the presence of NADPH, reduction of OBI-3424 is mediated by AKR1C3 to release the cytotoxic moiety OBI-2660, which is an aziridine bis-alkylating agent, leading to crosslinking of DNA at the N7 (or O6) position of guanine and subsequent cell death. AKR1C3 aldo-keto reductase family 1 member C3.

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