gms | German Medical Science

Soluferon^® is a 2^nd generation modified interferon-β (IFN-β) with increased bioavailability, due to enhanced hydrophilic properties. It is well known that the major shortcomings of the currently marketed interferon-ß, namely limited efficacy and tolerability, have been attributed to their high hydrophobicity causing aggregation and antigenicity.

In order to improve the pharmacokinetic properties of Soluferon^® the amino acid sequence of human interferon-β was changed. In the non-functional portion of the molecule, eight hydrophobic amino acids and one cystein were replaced by hydrophilic serine moieties. As a result hydrophobicity was reduced and bioavailability was increased up to six-fold when compared to human interferon-β. As Soluferon^® belongs to the Type-I interferon family, it was hypothesised that, among other beneficial effects, Soluferon^® has antiviral activity.

Preclinical studies support this thesis: Soluferon^® inhibits the infection of human cells with Adenovirus. This effect is dose-independent. It also blocks dose-dependent proliferation of Coxsackie Virus, EMCV and Poliovirus. Furthermore, Soluferon^® and Rebif, the positive control, induce IFN-susceptible gene expression for MxA protein in human cells, starting already at a concentration of 5 U/ml. They were also shown to activate IFN-susceptible gene factor dependent promotors with a similar efficiency. Already low doses of Soluferon showed a strong (10 to 60-fold) inhibitory effect on multiplication of influenza virus (H1N1) in human cells.

Moreover, tests in non-human primates showed promising results regarding pharmacodynamic parameters, e.g. 2'-5'-OAS.

These results state that great success can be achieved by the development and marketing of Soluferon® for antiviral therapy.