European patent granted for XL-protein’s PASylation® technology

FREISING, GERMANY, MARCH 17th, 2011 – XL-protein GmbH, a German biotech company that specialises in the development of biopharmaceuticals with extended plasma half-life, today announced that the European Patent Office granted a core patent (EP2173890) for XL-protein’s PASylation® technology.

Beside the granted PASylation® EP patent, several other corresponding national patent applications are currently processed worldwide. The European patent covers the use of random coil polypeptide sequences comprising the natural amino acids Proline, Serine, and Alanine (PAS) to enhance the stability of biologically active proteins if attached as part of a fusion protein.

The N- or C-terminal PAS tag can be directly produced together with the therapeutic protein in microbial hosts, e.g. E. coli, or in cell culture, thus avoiding costly in vitro coupling steps that are required for other presently available approaches such as PEGylation. Furthermore, the biodegradability of the PAS polypeptide should prevent organ accumulation during chronic treatment.

PASylation® can be applied both to existing biologics, yielding ‘biobetters’, or to innovative therapeutic proteins or peptides, leading to a prolonged plasma half-life by a factor 10-100 as demonstrated in numerous animal studies. Thus, PASylation® offers a superior solution to a general problem in biological drug development, eventually allowing less frequent and lower dosing together with better tolerability for patients.

Dr. Arne Skerra, founder and CEO of XL-protein GmbH, said: “This patent is an important milestone for our company and its collaboration partners. It reinforces our competitive market position and will strengthen corporate development”.
This revolutionary principle for increasing drug stability was originally developed at the Technische Universität München (TUM). In 2009, XL-protein entered into a license agreement with TUM via Bayerische Patentallianz GmbH, the central patent and marketing agency for 28 Bavarian universities and universities of applied sciences, and acquired the exclusive worldwide rights for the PASylation® technology, which also includes the right to grant sublicenses.
Mr. Peer Biskup, CEO of the Bayerische Patentallianz GmbH, commented: “The Bayerische Patentallianz is very pleased with the timely decision of the EPO to grant the first PASylation® patent and with the positive development of XL-protein’s business, which involves both in house drug development activities and partnering with pharma and biotech companies.”

Phylogica collaborates with XL-protein on inflammation Program

XL-protein Collaborates with Phylogica on Inflammation Program

PERTH, AUSTRALIA, January 13, 2011 – Phylogica Ltd (ASX: PYC), a leading Australian-based drug discovery company, announced today an alliance with XL-protein GmbH, a German-based biotech company that specialises in extending the circulation half-life of biopharmaceuticals. Through this alliance, Phylogica gains access to a unique modification technology that strengthens the Company’s Phylomer drug discovery platform.

XL-protein’s PASylation technology was originally developed by a leading academic group at the prestigious Technical University of Munich (TUM). The technology utilises a genetic technique to fuse a polymer of natural amino acids onto the relevant peptide or protein-based therapeutic, which slows the body’s clearance of the drug and prolongs the therapeutic effect.

Phylogica and XL-protein will initially collaborate on a pilot study to validate the technology in combination with one of Phylogica’s Phylomer peptides targeting CD40 ligand from its in-house anti-inflammatory programme. Under the terms of the agreement, Phylogica has an option to obtain an exclusive license to the PASylation technology for peptide-based products in relation to CD40 ligand and has rights of negotiation for a license to the technology for Phylomers that bind other targets.

It is anticipated that the plasma half-life of PASylated Phylomers will be significantly extended, making them more suitable for less frequent administration and at lower dose. Long acting Phylomers would be ideal for treating chronic indications, such as rheumatoid arthritis, coronary artery disease and inflammatory bowel disease, in which CD40 ligand has been implicated as a potential target.

Phylogica’s Chief Executive Officer, Dr Paul Watt, commented: “Phylogica is excited to enter into this collaboration with XL-protein. This deal provides us with access to the next generation of polypeptide fusions for optimising the half-life of our Phylomers. The technology combination of XL-protein and Phylogica could also significantly facilitate the ease of manufacturing and lower the cost of goods.”

Dr Arne Skerra, founder and CEO of XL-protein GmbH, said: “XL-protein is delighted to apply its PASylation technology to Phylomers, which will serve to validate the benefit of this revolutionary half-life extension technology to a highly promising class of therapeutic peptide drugs.”

The Bavarian Patent Alliance GmbH and the biotech company XL-protein GmbH have signed an exclusive licensing agreement on a promising invention of the Technical University of Munich

München, Germany, September 17, 2009 The Bavarian Patent Alliance GmbH and the biotech company XL-protein GmbH have signed an exclusive licensing agreement on a promising invention of the Technical University of Munich.

With the so-called “PASylation technology” the plasma half-life of biological agents is extended manifold. Therapeutic proteins are directly fused on the genetic level with sequences of the amino acids proline, alanine and serine. The “PAS” polymers are stable in plasma and pharmacologically inert. They adopt a bulky random coil structure, which significantly increases the size of the protein. Thus, the typically rapid clearance of the biological via kidney filtration is retarded by 1-2 orders of magnitude. In this way the duration of drug action in the human body can be extended to several days.

Through the acquisition of the worldwide patent rights XL-protein takes, as the exclusive licensee, advantage of the PASylation technology originally developed at the Institute of Biological Chemistry at the Technical University of Munich (TUM).

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