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Table 3 Application, mechanism and peak plasma concentrations for menadione and gemcitabine

From: Repurposing FDA approved drugs as radiosensitizers for treating hypoxic prostate cancer

 

Menadione

Gemcitabine

Approved application

Used in vitamin K deficiency and severe hypoprothrombinemia

Treatment of locally advanced or metastatic cancer

Mechanism of action

Synthetic vitamin K3. It is also an inhibitor of Siah2 (E3 ubiquitin ligase) ligase activity

Inhibition of DNA synthesis and inhibition of enzymes related to deoxynucleotide metabolism

Peak plasma concentration and equivalent in vitro dose

115–407 ng/mL

668.6 ng–2.3 µM

3–6 µg/mL

11.2–22.4 µM

Equivalent in vitro dose

668.6 ng–2.3 µM

11.2–22.4 µM

  1. Reported values for phytomenadione, doses up to 200 mg menadione are tolerated in humans