Trodusquemine is an aminosterol (a

polyamine A polyamine is an organic compound having more than two amino groups. Alkyl polyamines occur naturally, but some are synthetic. Alkylpolyamines are colorless, hygroscopic, and water soluble. Near neutral pH, they exist as the ammonium derivatives. ...

steroid A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and a ...

) similar to

squalamine Squalamine is a steroid-polyamine conjugate compound with broad spectrum antimicrobial activity and anti-angiogenic activity. It was studied as a potential cancer drug and as a potential treatment for wet macular degeneration but as of 2018 had n ...

that is an allosteric inhibitor of protein-tyrosine phosphatase 1B (PTP1B). It was isolated from the

dogfish shark Squalidae, more commonly known as dogfish, dog sharks, or spiny dogfish, are one of several families of sharks categorized under Squaliformes, making it the second largest order of sharks, numbering 119 species across 7 families. Having earned t ...

by scientists at Magainin Pharmaceuticals (subsequently called Genaera) in 2000 and underwent some drug development as a potential treatment for diabetes or obesity, but the company ran out of money and closed in 2009. Trodusquemine and some other drug assets were sold to Ohr Pharmaceutical for $200,000 by Genaera's liquidator. In 2014 a company called Depymed was formed based on work done on PTP1B inhibitors at Cold Spring Harbor Laboratory, and it licensed rights to Trodusquemine from Ohr. Depymed wanted to develop it for HER2-positive breast cancer. As of 2017, Depymed was running a Phase I clinical trial of the drug.

Coronary heart disease

British Heart Foundation trials using mice with atherosclerosis which were conducted at the University of Aberdeen suggests a link between atherosclerosis and

insulin resistance Insulin resistance (IR) is a pathological condition in which cell (biology), cells fail to respond normally to the hormone insulin. Insulin is a hormone that facilitates the transport of glucose from blood into cells, thereby reducing blood gluco ...

due to impaired insulin receptor (IR) signalling. Inhibiting the activity of PTP1B, which is the major negative regulator of the insulin receptor appeared to inhibit atherosclerotic plaque formation. The trial mice reportedly had significantly less fatty plaques in their arteries following a single dose of trodusquemine.

References

{{reflist Experimental drugs Enzyme inhibitors Polyamines Cholestanes Secondary amines Sulfate esters