ascorbate + menadione sodium bisulfite

The combination of ascorbate (vitamin C) and menadione sodium bisulfite (a water-soluble form of vitamin K3) is a small molecule drug investigated primarily for its pro-oxidant anticancer properties. This combination—often referred to by the code names VC/VK3 or M/A and marketed under the brand name Apatone—has demonstrated synergistic cytotoxic effects against various cancer cell lines while sparing normal cells. The mechanism involves induction of oxidative stress in cancer cells through mitochondrial superoxide production and disruption of mitochondrial function. This leads to decreased ATP production, loss of mitochondrial membrane potential, activation of nucleases causing DNA damage, and ultimately necrotic cell death via autoschizis. The drug also downregulates immune checkpoint protein PD-L1 in tumor cells. Preclinical studies have shown efficacy in prostate cancer xenografts and other solid tumors; clinical trials have reached Phase 2 for indications such as prostatic cancer, edema associated with joint diseases (including osteolysis and synovitis), foreign-body reaction, wounds/injuries healing enhancement, and polycystic kidney disease[1][3][5]. Menadione sodium bisulfite alone has also been studied for its ability to target PI 3-kinase VPS34 activity relevant to muscle disorders[6].

Brand names

ApatoneApatone-B

Other names

ascorbic acid + menadione sodium bisulfitevitamin C + vitamin K3 combinationVC/VK3 combination