Less complex synthetic heparin created

Washington, Sept 22 : Researchers have patented a synthetic version of the drug heparin, called Recomparin, that is less complex chemically and easier to produce than previous forms.

Heparin has loads of advantages such as it helps in preventing clots from forming and restricting the flow of blood during and after procedures such as kidney dialysis, heart-bypass surgery, stent implantation and knee and hip replacement. The annual worldwide sales of the drug are estimated at 3 billion dollars.

The findings are published in the Sept. 24, 2007; issue of the journal Chemistry & Biology.

The study was conducted by a team of researchers led by Jian Liu, Ph.D, an associate professor, at the University of North Carolina.

Liu said that a single sugar component called iduronic acid is difficult to replicate and was long thought to be an important contributor to heparin’s function but scientists recently discovered that they could remove the complex element from the heparin molecule without altering the drug’s function.

“We proved we don’t really need that structure for the anticoagulant effect. By eliminating the iduronic acid unit, we were able to reduce the structural complexity of the heparin molecule by approximately 50 percent,” Liu said.

Heparin is a natural substance that is extracted from animal tissue, chiefly from cows and pigs. Outbreaks of diseases among livestock can interfere with production of the drug, driving up prices and tightening supplies.

“Synthesizing heparin, rather than extracting it from animals, gives us more control over its anticoagulant properties and creates a purer, safer, more reliable drug,” Liu said.

Liu said that currently, synthetic forms of heparin are difficult to produce in large quantities because of the drug’s complexity, resulting in expensive therapies that are not widely used.

Liu also said that the simpler structure of Recomparin is likely to be easier to produce than other forms of synthetic heparin. It is also expected to reduce dangerous side effects, such as uncontrolled bleeding, while providing the same benefits as naturally derived heparin.

The next step for Recomparin will be to find a company to license the drug and begin the process of getting Food and Drug Administration approval.

The study was supported by a grant from the National Institutes of Health.
(With inputs from ANI)

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