PB1087 - An Enoxaparin Obtained From Bovine Heparin is Equivalent to the Original Drug From Porcine Origin

Background: Enoxaparin and other low-molecular-weight heparins are obtained exclusively from porcine heparin. This assures the similarity of these drugs in their structure, physio-chemical properties, biological effect, and therapeutic action. Heparin from bovine intestine has a distinct por disaccharide composition and differs from the same drug from porcine origin especially due to the high content of 6-desulfated glucosamine. Therefore, bovine heparin is not used as a substrate for preparation of enoxaparin. We recently demonstrated that pharmaceutical preparation bovine heparin is a mixture of different types of glycosaminoglycans.

Aims: After a single step of purification, we obtained a preparation of bovine heparin like porcine one, denominated as high-anticoagulant bovine heparin (HABH). This observation opens the possibility to obtain low-molecular heparin starting from bovine heparin. We now employed HABH as a substrate for preparation of enoxaparin using the standard β-elimination reaction.

Methods: The product obtained was analyzed by a variety of methodologies, including: 1) molecular mass distribution, 2) anti-FXa and antifactor IIa activity, 2) structure analysis using one- and two-dimensional NRM spectroscopy, 3) analysis of the digestion products formed by heparitinases digestion, 4) test in assays of experimental thrombosis, etc.

Results: These variety of methods assured that enoxaparin obtained from HABH is equivalent in structure, physiochemical and biological properties to the original product obtained from porcine origin. We are now facing shortages of heparin and low-molecular-weight heparin due to the increased use of these drug and limited source for their heparin.

Conclusion(s): Our results indicating that similar enoxaparins are obtained from porcine and bovine heparins. This new source of enoxaparin, which we propose to denominate as “bovine enoxaparin”, can supply the marked with this drug saving drug, which depend presently on the porcine heparin for its preparation.