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Pieris Reports Preclinical Development Progress of its Next Generation VEGF Antagonist
Date:10/9/2009

re engineered binding proteins derived from the scaffold of natural human lipocalins. Anticalins are selected to have prescribed binding properties with selectivity and affinity fundamentally similar to that of monoclonal antibodies. Being human in origin, Anticalins are predicted to have minimal immunogenicity in man. Furthermore, compared to conventional antibodies Anticalins benefit from their small size (20 kDa), robust physicochemical properties and simple composition that together allow highly soluble and stable products to be manufactured from bacteria. Anticalins are amenable to further engineering to balance their favorable tissue penetration with adjustable serum half-life. Moreover, Anticalins have been developed as Duocalins, whose dual targeting format allows multiple targets to be bound and modulated through a single molecule.

Pieris exclusively owns the Anticalin patent estate, which offers complete freedom to operate outside the patent boundaries defined by conventional antibody products. Key patents have already been granted in the US, Asia and Europe.

About PRS-050

PRS-050 Anticalin has been designed to specifically bind and block the signaling activity of vascular endothelial growth factor (VEGF) in cancer. Optimised for extended serum half-life, PRS-050 exhibits comparable binding and functional in vitro activity to approved VEGF antagonists. Potent inhibition of VEGF-induced enhanced vascular permeability and angiogenesis, as well as anti-tumour activity, have already been demonstrated for PRS-050 in various well-validated in vivo preclinical studies.

As a next generation VEGF antagonist, PRS-050 exploits several favourable characteristics of Anticalins, including compact protein structure, high intrinsic stability, broad formulation flexibility and small molecular size with the potential to penetrate neovascularized tumour tissue more effectively. PRS-050 is being developed for a P
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