Generon successfully established a dimeric cytokine (DiKineTM) platform used to generate therapeutic recombinant human cytokines as receptor agonists while enhancing bioactivity and extending serum half-life with a robust manufacturing feasibility in comparison to its native counterpart, PEGylated recombinant proteins.

DiKineTM technology is based on the basic structure of an immunoglobulin (Ig), or an antibody (Ab). Therapeutic Abs have been widely used clinically to block the interaction of an antigen with its target or block the binding of a ligand to its receptor. Therapeutic receptor Fc fusion proteins have also been successfully developed by blocking a natural ligand binding to its receptor, thus preventing cell surface receptor activation. Generon’s ligand Fc fusion platform generates dimeric cytokines (ligands or agonists) aiming to enhance cell surface receptor activation. The addition of an Fc fragment of an Ab leads to the extended serum half-life of given cytokines. Figures below illustrate the basic structure of an antibody, a receptor-Fc fusion protein as well as the ligand-Fc fusion protein generated by Generon’s DiKineTM platform.

The DiKineTM platform has been clinically validated as we have used it to successfully develop F-627 (a rhG-CSF dimer), F-652 (a rhIL-22 dimer), and F-899 (a rhGH dimer). The clinical study results of F-627 and F-652 demonstrated the expected pharmacokinetic and pharmacodynamic (PK/PD) properties and favorable safety profiles.

        Antibody    Receptor-Fc Fusion Protein  DiKineTM Dimer