AI Article Synopsis
- Heparin and low molecular weight heparins (LMWHs) are key drugs used for treating and preventing thromboembolic diseases.
- Enoxaparin, a clinically approved LMWH, is created through a method called alkaline depolymerization and has a specific molecule at its end-site.
- The study highlights a new conjugate, EnoxaTD, which combines enoxaparin with deoxycholic acid and shows potential as an orally active treatment for deep vein thrombosis without causing bleeding, suggesting it could be a promising drug for future oral heparin therapies.
Article Abstract
Heparin and low molecular weight heparins (LMWHs) have been the drug of choice for the treatment or the prevention of thromboembolic disease. Different methods are employed to prepare the LMWHs that are clinically approved for the market currently. In particular, enoxaparin, which has a reducing sugar moiety at the end-site of polysaccharide, is prepared by alkaline depolymerization. Focusing on this end-site-specific activity of LMWHs, we conjugated the tetraoligomer of deoxycholic acid (TetraDOCA; TD) at the end-site of enoxaparin via nonenzymatic glycosylation reaction. The end-site-specific conjugation is important for polysaccharide drug development because of the heterogeneity of polysaccharides. This study also showed that orally active enoxaparin and tetraDOCA conjugate (EnoxaTD) had therapeutic effect on deep vein thrombosis (DVT) without bleeding in animal models. Considering the importance of end-specific conjugation, these results suggest that EnoxaTD could be a drug candidate for oral heparin development.
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| http://dx.doi.org/10.1021/acs.jmedchem.6b00936 | DOI Listing |
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End-Site-Specific Conjugation of Enoxaparin and Tetradeoxycholic Acid Using Nonenzymatic Glycosylation for Oral Delivery.
J Med Chem
December 2016
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, South Korea.
Article Synopsis
- Heparin and low molecular weight heparins (LMWHs) are key drugs used for treating and preventing thromboembolic diseases.
- Enoxaparin, a clinically approved LMWH, is created through a method called alkaline depolymerization and has a specific molecule at its end-site.
- The study highlights a new conjugate, EnoxaTD, which combines enoxaparin with deoxycholic acid and shows potential as an orally active treatment for deep vein thrombosis without causing bleeding, suggesting it could be a promising drug for future oral heparin therapies.
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