GlycoAdvance has been used successfully to improve glycosylation levels of several different recombinant glycoproteins. In the first 22 feasibility studies conducted by Neose, GlycoAdvance improved glycosylation in fusion proteins, antibodies, hormones, blood factors, cytokines, enzymes, enzyme inhibitors, and transgenically produced proteins.

In the study below the initial degree of sialylation of the recombinant protein following expression in CHO cells was 64%. After GlycoAdvance, the degree of sialylation increased to 92%.

The half-life of the remodeled glycoprotein was substantially increased.

Biogen and Eli Lilly
At the 2001 Biotechnology Industry Organization annual meeting in San Diego, CA, Biogen and Eli Lilly presented results of GlycoAdvance studies using compounds they provided to Neose.

Biogen reported that GlycoAdvance improved the in vivo half-life of a protein produced in two different cell lines by 48% and 245%.

Eli Lilly reported the results of a continuous infusion study performed in monkeys that showed that GlycoAdvance treated protein had 2.5 times the steady-state circulatory half-life of the untreated material. After the infusion was stopped the terminal half-life of the GlycoAdvance material was 3 times that of the untreated material.

AVANT Immunotherapeutics
At IBC's 2002 conference entitled, The Impact of Post-Translational and Chemical Modifications on Protein Therapeutics, AVANT presented results showing that GlycoAdvance was able to double the circulatory half-life of its TP10, a recombinant soluble complement receptor inhibitor with >18 bi-antennary glycosylation sites per molecule. TP10 produced in conventional Chinese hamster ovary (CHO) cell culture (DUKXB11 strain) was further glycosylated using Neose’s GlycoAdvance (sialic acid added using sialyltransferase and CMP–sialic acid and purified by FPLC). The resulting increase in half-life was demonstrated in a pharmacokinetic study in rats comparing GlycoAdvance improved TP10 versus the original CHO material.

A second study used GlycoAdvance to further convert the enzymatically sialylated TP10 to a second compound TP20, through the addition of fucose by fucosyltransferase and GDP-fucose and purified by FPLC. TP20 may have application in the treatment of cerebral ischemic stroke. An in vitro E-selectin binding assay compared Neose produced TP20 with TP20 produced in a conventional CHO cell culture. The GlycoAdvance produced TP20 was 10 times more active than the CHO produced material in binding the E-selectin target.