# Development of a New Carbohydrate-based Anticoagulant Drug

> **NIH NIH R44** · GLYCAN THERAPEUTICS CORPORATION · 2020 · $1,248,861

## Abstract

Low molecular weight heparins (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 chemical 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 phase I STTR studies, we have
identitifed a heparin dodecasaccharide (12-mer) as a candidate to substitute animal-sourced
LMWH. We also demonstrated the ability to synthesize this 12-mer at the scale of 20 g in four
batches. In the presently proposed Phase II SBIR studies, we will assess the feasibility of a
larger scale synthesis (200 grams) to conduct IND-enabling studies. Aim 1 will develop a
process to prepare 50 g of the 12-mer via a series of efforts for improving enzyme production,
reaction efficacy and simplifying purifications. Aim 2 will examine the immunogenicity of the 12-
mer in a murine model. We will also conduct 14-day toxicity studies in rat and dog as well as
related IND-enabling studies. The completion of this project will modernize this century-old drug
with improved safety and anticoagulant properties.

## Key facts

- **NIH application ID:** 9971554
- **Project number:** 5R44HL139187-03
- **Recipient organization:** GLYCAN THERAPEUTICS CORPORATION
- **Principal Investigator:** Vijayakanth Pagadala
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $1,248,861
- **Award type:** 5
- **Project period:** 2017-08-01 → 2022-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9971554

## Citation

> US National Institutes of Health, RePORTER application 9971554, Development of a New Carbohydrate-based Anticoagulant Drug (5R44HL139187-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9971554. Licensed CC0.

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