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Synthesized Methods Developed for Anti-Coagulant Drugs

Robert Linhardt (RPI)

Robert Linhardt (RPI)

Researchers at Rensselaer Polytechnic Institute in Troy, New York and University of North Carolina, Chapel Hill have developed a new method for producing the anti-coagulant drug fondaparinux that is purer, faster, and less expensive. Their findings, which the authors say offer a template for the discovery of other drugs, appear in the 28 October issue of the journal Science (paid subscription required).

Fondaparinux, marketed under the brand-name Arixta, is one of a class of anti-coagulants called heparins made of cells of organs from cattle or pigs. The brand-name version has annual sales of more than $300 million, although a generic version of the drug was approved by the FDA earlier this year.

Because heparins are derived from animal sources, they carry a risk of outside contamination. In 2008, the FDA recalled some heparin drugs for this reason. While fondaparinux is chemically synthesized and not derived from animals, the process for producing the drug is complex and detailed, requiring some 50 steps.

RPI bio-chemical engineer Robert Linhardt (pictured left) and Chapel Hill bio-chemist Jian Liu discovered a new process to make fondaparinux that uses sugars and enzymes identical to those found in the human body to build the drug piece by piece. The backbone of the material is first built by assembling the sugars. Enzymes then enhance the drug core with sulfate groups to control its structure and function in the body.

Linhardt and Liu’s process reduces the number of production steps for fondaparinux from 50 to no more than 12. The process also increases the yield 500-fold compared to the current process, according to Linhardt, with the potential at least for reducing the cost of manufacture by a similar amount. Linhardt and Liu say they have have already begun testing the drug in animal models with successful results.

This research is part of a larger effort at RPI and elsewhere to replace heparin-based and other glycoprotein-based (carbohydrate and protein) drugs with safer, low-cost, synthetic versions that do not rely on potentially contaminated animal sources.

“During this study, we were able to quickly build multiple doses in a simple laboratory setting,” says Linhardt, “and feel that this is something than can be quickly and easy commercialized to reduce the cost of this drug and help to shift how pharmaceutical companies approach the synthesis of carbohydrate-containing drugs.”

Read more: FDA Approves Anti-Coagulant Drug

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