Repurposing Disulfiram

There is a global drive towards the repurposing of known drugs for cancer treatment due to high failure rate and cost of new drugs. Our company’s underpinning research is based on original idea to repurpose an FDA approved anti-alcoholism drug – disulfiram, into cancer treatment. Disulfiram possesses excellent anticancer activity with low toxicity to normal cells. Disulfiram’s anticancer activity is highly dependent on chelation with divalent metal ions such as copper or zinc. The anticancer activity of disulfiram is known for many years but there has been no success in clinical trials using disulfiram and copper combination in cancer patients. This is mainly due to the very short half-life of the currently available oral version of disulfiram in the bloodstream.

We first reported the importance of protecting the thiol group in the chemical structure of disulfiram, which is essential for its chelation with copper and its anticancer activity. After taking oral tablets, disulfiram is rapidly degraded to its derivative diethyldithiocarbamate (less than 2 mins) in the liver and the reactive thiol group is blocked by metabolic conversion, losing its anticancer profile. If the thiol groups in disulfiram are protected from protein binding or degradation by bypassing the portal circulation/liver metabolism, intact disulfiram can be delivered to cancer tissues, where it will react with high copper concentrations present, to form a complex that target the cancer cells.

We have used cutting-edge nano-drug-delivery technologies to extend the half-life of disulfiram in the bloodstream, and our innovative formulations manifests strong anticancer efficacy in animal models of a wide range of cancers.

One such proprietary formulations of Disulfican Ltd is an injectable version of PLGA polymer-encapsulated disulfiram microparticles, that has extended half-life in bloodstream and controlled slow-release profile. Our PLGA encapsulated disulfiram microparticles are suitable for local injection and hence used to target cancers via the local delivery/injection.