CelaSYS Customized PEGylation Solutions

Transcription

1 CelaSYS Customized PEGylation Solutions

2 Neue Ära der Wirkstoffoptimierung - New Era of Drug Optimization Die celares GmbH verfügt über exzellentes fachliches Know-how in den Bereichen Synthesechemie, Biotechnologie und Bioanalytik, das durch besondere Kompetenz und langjährige Erfahrung auf den Gebieten Polymermaterialien, modifizierte Proteinwirkstoffe und PEGylierung ergänzt wird. celares GmbH has outstanding technical know-how in the fields of synthetic chemistry, biotechnology and bioanalytics which is complemented by a high level of expertise and many years of experience in the areas of polymer materials, modified protein drugs and PEGylation. Technologische Basis des von der celares GmbH entwickelten, zum Patent angemeldeten Produktes CelaSYS bildet die sogenannte PEGylierung, bei der biopharmazeutische Wirkstoffe mit Polyethylenglykol (PEG) gekoppelt werden. Während bei der klassischen PEGylierung kettenförmige Strukturen an den Wirkstoff angehängt werden, verwendet die celares GmbH verzweigte PEG-Strukturen, die den Wirkstoff nahezu vollständig umhüllen und ihn somit zuverlässig gegen den vorzeitigen Abbau durch Antikörper und körpereigene Enzyme schützen. Mit Hilfe dieser Maskierungsreagenzien kann der Wirkstoff Angriffen durch das Immunsystem sowie enzymatischen Abbauprozessen standhalten, ungehindert an seinen Bestimmungsort gelangen und seine therapeutische Wirkung effizient entfalten. The technological basis of the CelaSYS product line developed by celares GmbH (patent pending) is the so-called PEGylation method, in which the biopharmaceutical drug is coupled with polyethylene glycol (PEG). Whereas in traditional PEGylation chain-like structures are attached to the drug molecule, celares GmbH uses branched PEG structures which cover the drug molecule almost completely, thus shielding it effectively against premature degradation by antibodies and endogenous enzymes. With the help of these masking reagents, the drug can withstand attacks by the immune system and enzymatic degradation processes, reach its destination unimpeded and exert its therapeutic effect efficiently Biopharmazeutische Wirkstoffe werden von Antikörpern inaktiviert und von Proteasen abgebaut. Dadurch wird das Medikament unwirksam. Kettenförmige PEG-Strukturen umgeben den Wirkstoff und schützen ihn begrenzt gegen Antikörper und körpereigene Enzyme. Die CelaSYS-PEGylierung umhüllt den Wirkstoff wie ein Regenschirm und schützt ihn zuverlässig gegen vorzeitigen Abbau. Antikörper Antibody Protease Proteolytic enzyme Biopharmaceutical drugs are inactivated by antibodies and degraded by proteases. Thus the drug looses its effect. Linear PEG-structures envelope the drug molecule resulting in a limited protection against antibodies and endogenous enzymes. CelaSYS PEGylation envelopes the drug molecule like an umbrella and thus shields it absolutely reliable against premature degradation.

3 Biopharmaceuticals Gaining Ground Rapidly Biopharmaceuticals are regarded as the great hope of the pharmaceutical sector. Unlike synthetic drugs, biopharmaceuticals can be tailored specifically to a particular application. Thus, diseases which have gone beyond the limitations of conventional medicine up to now will be treatable in the future. New Treatment Possibilities Genetic engineering is paving the way in the growing importance of biotechnologically based forms of therapy. It provides the scientific basis for the development of completely new generations of drugs, which are characterized by their specific mode of action and good tolerance. Biotechnologically produced drugs offer new treatment possibilities for patients whose diseases were previously untreatable or insufficiently treatable. Due to the efficiency of biopharmaceutical therapeutic approaches, experts anticipate substantial cost savings resulting in a considerable reduction of the burden on the health care system. Excellent Growth Prospects The pharmaceutical industry in particular is pinning great hopes on biotechnology. For industry experts, biotechnologically produced drugs are among the fastest-growing products on the pharmaceutical market. Development is equally rapid already today, 35 percent of all newly approved drugs are of biotechnological origin. According to estimates by the German Pharmaceutical Industry Association, this share will increase to over 50 percent by Worldwide sales of biopharmaceuticals currently amount to approximately 16 billion US dollars per year. At an average growth rate of 18 percent, this share is likely to more than double in a few years. Technological Challenge Despite all legitimate hopes, biotechnologically produced drugs have one serious flaw: due to their molecular structure, they are recognized as foreign bodies by the immune system and destroyed by endogenous defense mechanisms. In order to delay the resulting premature loss of effect through antibodies or proteases, the drug molecules are coupled with substances which are not identified as foreign by the immune system. One well-established method for achieving this is PEGylation, in which chain-like polyethylene glycol (PEG) molecules are attached to the drug molecules. Innovative Masking System Using an innovative PEGylation reagent developed by celares GmbH, for the first time it is now possible to suppress the immune response of the body almost completely, thus substantially improving the efficiency and tolerability of biotechnologically produced drugs. Rather than chain-like PEG molecules, celares GmbH uses branched structures characterized by consistently high quality which is reproducible at all times. The branched PEG structures cover the drug like an umbrella and thus shield it effectively against degradation by immune cells and endogenous enzymes. c e l a r e s GmbH Telephone [email protected]

4 CelaSYS New Standards for PEGylation PEGylation is an effective method for optimizing biopharmaceutical drugs. Coupling with PEG molecules results in considerably greater protease stability, a significant decrease in immunogenicity and a perceptible delaying of renal excretion. The CelaSYS product line developed by celares GmbH is a completely new generation of PEG-based masking reagents which are characterized by outstanding surface shielding and consistently high quality that is reproducible at any time. CelaSYS: Superior quality through monodispersity CelaSYS can be customized for almost any drug and thus tailored specifically to the individual needs of the customer. Customer-specific adaptation is made possible by an innovative synthesis in which specific properties of the masking reagent can be varied. celares GmbH has filed a patent application for CelaSYS. Intensity ELS CelaSYS, monodispers Polydispers Retention time HPLC analysis of CelaSYS and the product of a competitor: (A) CelaSYS is monodispers resulting in one single signal (B) Polydispers PEG reagents are inhomogeneous Traditional PEGylation chain-like structure polydisperse cross-links possible structurally determined fluctuations in quality at any time limited optimization possibilities CelaSYS branched structure monodisperse cross-links impossible consistently high, reproducible quality various drug-specific optimization possibilities c e l a r e s GmbH Telephone [email protected]

5 Customized PEGylation Solutions In addition to its own CelaSYS product line, celares GmbH offers numerous PEGylation services, ranging from the development of customer-specific masking reagents to the conception and implementation of individual PEGylation solutions to the production of masking reagents at pilot scale. Laboratory facilities equipped to the latest technical standards enable us to provide the entire range of modern bioanalytics, biochemistry and synthetic chemistry. Thus, in vitro assays to test protease stability and immunogenicity are just as much a part of our service palette as HPLC-MS-based quality control of masking reagents. Through our close collaboration with university and industry partners, current research findings and the latest development trends are incorporated directly into our projects and thus into your products as well. We would be happy to develop a PEGylation tailored to your drug. Take advantage of our know-how and our technical infrastructure for the optimization of your drugs. Significant increase of stability by CelaSYS Residual activity (%) with CelaSYS control without CelaSYS 50 Time (min) 100 The stability of L-Asparaginase towards Chymotrypsin is significantly increased by PEGylation with CelaSYS. As a control for enzyme activity native L-Asparaginase was incubated without Chymotrypsin. biochemical workstation HPLC system c e l a r e s GmbH Telephone [email protected]

6 c e l a r e s GmbH Robert-Rössle-Str. 10, Geb. D79 D Berlin Telefon Telefax [email protected]