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Nov 29, 2012
 |  BC Innovations  |  Targets & Mechanisms

Solving triptolide

University of Minnesota researchers have developed a water-soluble prodrug of the poorly soluble cancer therapeutic triptolide that could give a second life to the plant-derived compound.1Minneamrita Therapeutics LLC holds a license to the new molecule and plans to start a Phase I trial within six months.

Triptolide is a diterpenoid triepoxide derived from the traditional Chinese medicine plant Tripterygium wilfordii.

In early 2007, researchers at the University of Minnesota led by Ashok Saluja showed that small interfering RNA-mediated knockdown of heat shock protein 70 (Hsp70) potently killed pancreatic cancer cells,2 which prompted them to search for pharmacological agents that inhibit the protein.

Later that year, Saluja and colleagues showed that triptolide potently killed pancreatic cancer cells by downregulating Hsp70.3 However, after working with the compound and showing antiproliferative effects in two other forms of cancer,4,5 it became clear that triptolide was not suited for clinical development.

"Triptolide is not very soluble in water, so if we were to try to deliver it to a patient we would first need to dissolve it in solvents, which could be very harsh to the patient," said Saluja, professor and vice chair of research in the Department of Surgery at the University of Minnesota and a cofounder of Minneamrita. "Thus, we decided to modify the compound to make it more water soluble."

The resulting compound, called minnelide, is...

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