Development of dekaparin to replace animal-sourced heparin

NIH RePORTER · NIH · R44 · $747,280 · view on reporter.nih.gov ↗

Abstract

The goal of this proposal is to develop dekaparin, a synthetic glycan, to replace animal-derived low molecular weight heparins (LMWHs). LMWHs are partially depolymerized natural products of heparin, which are isolated from porcine intestine. A worldwide distribution of contaminated heparin in 2007 was associated with 85 deaths in the US. This crisis revealed the vulnerability of the LMWH supply chain. LMWHs are complex mixtures, having average molecular masses of 3500-6000 Daltons, corresponding to 12-20 saccharide units. The efficient preparation of a synthetic LMWH could improve the safety, availability and efficacy. However, the production of homogeneous LMWHs has not been possible due to difficulties in the synthesis. Glycan Therapeutics proposes to assess an innovative chemoenzymatic approach that would provide an unprecedented efficiency in the preparation of heparin. Our product will be animal-free, structurally homogenous, safe for renal-impaired patients, and have the ability of its anticoagulant activity to be neutralized by protamine. In the presently proposed SBIR Phase IIB grant application, we will conduct the synthesis of dekaparin under the GMP conditions and complete the formulation, which will clear the IND requirements by FDA. Glycan Therapeutics will also develop a 505(b)(2) regulatory strategy to shorten the regulatory pathway. The completion of this project will modernize this century-old drug with improved safety and anticoagulant properties.

Key facts

NIH application ID
10766662
Project number
2R44HL139187-04
Recipient
GLYCAN THERAPEUTICS CORPORATION
Principal Investigator
Vijayakanth Pagadala
Activity code
R44
Funding institute
NIH
Fiscal year
2024
Award amount
$747,280
Award type
2
Project period
2017-08-01 → 2026-06-30