Perfline |  |
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Synthetic heparin becomes a reality.
The pursuit of a synthetic version of heparin, free of animal materials and made with stricter quality controls, is gaining more attention as awareness grows that the anticoagulant can be easily contaminated during the process of biological extraction.
Researchers at Rensselaer Polytechnic Institute and University of North Carolina at Chapel Hill have discovered an alternative way to produce heparin. Their findings could enable the current supply of heparin, now extracted from porcine tissues, to be replaced or supplemented by the synthetic version.
Heparin, as we know, is a complex carbohydrate used to prevent blood coagulation during medical procedures and treatments such as hemodyalisis, cardiopulmonary bypass coronary artery stenting, and many others.
The researchers reported that they have synthetically prepared heparin in quantities large enough for use in human medical treatments by engineering recently discovered heparin biosynthetic enzymes. These discoveries will enable the researchers to effectively replace a variable raw material - heparin derived from processed animal organs -- with a synthetic material -- synthetic heparin -- and have the same therapeutic result.
After determining the molecular structure of complex carbohydrates such as heparin, the researchers established a structure-activity relationship that may reveal lead compounds for new drug development. The research team has developed a large-scale process involving the engineered enzymes and co-factor recycling that can be applied to synthesize the heparin and other heparin-based structures that regulate cell growth and may have applications in wound healing or cancer treatment.
A provisional patent request was filed and the whole work was supported by the National Institutes of Health and the American Heart Association.
March 26, 2008 10:37 am - Rio de Janeiro, Brazil |
Perfline | |
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A few more details on the creation of a synthetic heparin: Researchers at the University of North Carolina School of Pharmacy have patented a synthetic version of heparin, called Recomparin, that is less complex chemically and should be easier to produce than previous forms. Led by Jian Liu, PhD, scientists in the UNC School of Pharmacy discovered that they could remove a complex element from the heparin molecule without altering the drug’s function. The component, a single sugar called iduronic acid, is difficult to replicate and was long thought to be an important contributor to heparin’s function as an anticoagulant. Their findings were published in the September 24, 2007, issue of the journal Chemistry & Biology. The study was supported by a grant from the National Institutes of Health. The other authors of the study are Jinghua Chen, PhD, and Courtney Jones, a doctoral student, both with the School of Pharmacy.
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.
March 27, 2008 10:29 am - Rio de Janeiro, Brazil |
Joel Krieger | |
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As a cationic peptide derived from fish milt (spermatic cells) and used in medical applications as a carrier for injectable insulin and as a heparin antagonist, protamine can also suffer contamination during the biological extraction process. This has not been described yet, at least to my knowledge. However globalization is moving excellence centers and replacing manufacturing plants so quickly that it may create the appropriate environment to reduce safety to the benefit of increasing profits.
There is a private company in the USA that has synthesized a product called "Heptagonist" which in preliminary studies in vitro is able to neutralize heparin. Animal studies will demonstrate the existence, the range, and the severity of side effects.
Let us all hope that we will have another heparin antagonist out of laboratories without the side effects of the biological protamine. March 31, 2008 11:21 am - Cebu, Phillipines |
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Hanna Tsui |
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The search for a synthetic heparin formulation, free of animal materials and made with absolute quality controls gains more attention. Jian Liu, associate professor of medicinal chemistry and natural products at the University of North Carolina School of Pharmacy, who is developing a synthetic heparin says that for the time being, we are stuck with the porcine heparin.
FDA officials said as much as 50 percent of Baxter's heparin tested from suspect lots recalled showed that the raw ingredient used to make the drug contained oversulfated chondroitin sulfate, an unapproved dietary supplement taken orally to treat joint pain.
Synthetic heparin has its own drawbacks, however. It is complex to make and development costs could push the price up between five and 40 times the $1 per-vial cost of the decades-old heparin, researchers and analysts said. It's been inexpensive to derive heparin from animal sources so that there has been little incentive to consider a synthetic version of this particular heparin, said FDA spokeswoman Karen Riley.
Meanwhile we should all be strictly careful with systemic anticoagulation for cardiopulmonary bypass. Pehaps time has come to become more familiar with alternative drugs while systhetic heparin is still under development and in vitro experimentation. April 4, 2008 10:44 am - Singapore |
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