the future of P ePtides interview with dr. daniel erne, cto · grounds. Nor is it possible to...
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20 Bachem Annual Report 2013 Peptides have been in use as active pharmaceutical ingredients for as long as 50 years now. Do peptide- based drugs still have a future these days? Peptides are in demand as active pharmaceutical ingredients now more than ever. Generally speaking, these are highly active, highly specific and metabolically favorable substances. As you might expect from the diverse physiological functions they perform, peptides are suitable for a wide range of very different therapeutic indica- tions. In addition to the large areas of oncology and diabetology, peptides are also useful therapeutic options in renal failure, cardiovascular disease, palliative care and neurodegenerative disorders such as multiple sclerosis and autoimmune disorders like Crohn’s disease, to give just a few examples. Numerous peptides are in clinical de- velopment as vaccines or antibiotics and for the treatment of orphan dis- eases. How are new peptide-based drugs discovered? Nature has an unbelievable reservoir of biologically active peptides in store. Many of the peptide-based drugs we know of today were originally discov- ered in animal organisms, and thou- sands await discovery and character- ization. Targeted alterations of natural structures and subsequent structure- activity relationship studies give rise to new peptide-based drugs. Advanc- es in proteomics research promote the development of new peptides as po- tential drugs on the basis of insights into the function of proteins in healthy and diseased organisms. Peptides are protein-like sub- stances. Proteins are made by bio- technology today. Does this pose a threat for suppliers of chemically synthetized peptides? Chemical synthesis and recombinant technology both have their justifica- tion. With chemical synthesis, there are limits to the length of the peptide chains you can produce, while recom- binant technology is unsuitable for producing shorter proteins on cost grounds. Nor is it possible to produce peptides by recombinant technology if they contain unnatural amino acids or have undergone any other struc- tural modifications. Having said that, Bachem succeeded last year in push- ing the generally accepted limit of about 100 amino acids per peptide. In collaboration with Japanese re- searchers, an industrial process was developed for the first time that enables the synthetic production of interferon -1a, a glycosylated protein 166 amino acids long. Until then, pro- duction of such proteins was the ex- clusive preserve of recombinant tech- nology. What trends do you see for peptide development going forward? We’re seeing a trend toward more complex structures for peptidic drugs. Targeted structural alterations are be- ing used to optimize biophysical prop- erties to enhance activity and bioavail- ability. In the area of vaccines, epitope mimetics are being used to create complex cocktails. We can also expect further advances in drug delivery sys- tems that are likely to give peptides an additional boost as a drug class. THE FUTURE OF PEPTIDES INTERVIEW WITH DR. DANIEL ERNE, CTO Daniel Erne is a chemistry PhD with 29 years of experience in peptide chemistry. 26 of those years were spent with Bachem Group. Dr. Erne headed the Quality Control depart- ment of Bachem Feinchemikalien AG, as it was then known, established the Quality Assurance and Regulatory Affairs unit and has been a member of the Bachem Group’s Corporate Executive Committee since 1997.
Transcript of the future of P ePtides interview with dr. daniel erne, cto · grounds. Nor is it possible to...
20 Bachem Annual Report 2013
Peptides have been in use as active pharmaceutical ingredients for as long as 50 years now. Do peptide-based drugs still have a future these days?Peptides are in demand as active pharmaceutical ingredients now more than ever. Generally speaking, these are highly active, highly specific and metabolically favorable substances. As you might expect from the diverse physiological functions they perform, peptides are suitable for a wide range of very different therapeutic indications. In addition to the large areas of oncology and diabetology, peptides are also useful therapeutic options in renal failure, cardiovascular disease, palliative care and neurodegenerative disorders such as multiple sclerosis and autoimmune disorders like Crohn’s disease, to give just a few examples. Numerous peptides are in clinical development as vaccines or antibiotics and for the treatment of orphan diseases.
How are new peptide-based drugs discovered?Nature has an unbelievable reservoir of biologically active peptides in store. Many of the peptidebased drugs we know of today were originally discovered in animal organisms, and thousands await discovery and characterization. Targeted alterations of natural structures and subsequent structureactivity relationship studies give rise to new peptidebased drugs. Advances in proteomics research promote the development of new peptides as potential drugs on the basis of insights into the function of proteins in healthy and diseased organisms.
Peptides are protein-like sub-stances. Proteins are made by bio - technology today. Does this pose a threat for suppliers of chemically synthetized peptides?Chemical synthesis and recombinant technology both have their justification. With chemical synthesis, there are limits to the length of the peptide chains you can produce, while recombinant technology is unsuitable for producing shorter proteins on cost grounds. Nor is it possible to produce peptides by recombinant technology if they contain unnatural amino acids or have undergone any other structural modifications. Having said that, Bachem succeeded last year in pushing the generally accepted limit of about 100 amino acids per peptide. In collaboration with Japanese researchers, an industrial process was developed for the first time that enables the synthetic production of interferon 1a, a glycosylated protein 166 amino acids long. Until then, production of such proteins was the exclusive preserve of recombinant technology.
What trends do you see for peptide development going forward?We’re seeing a trend toward more complex structures for peptidic drugs. Targeted structural alterations are being used to optimize biophysical properties to enhance activity and bioavailability. In the area of vaccines, epitope mimetics are being used to create complex cocktails. We can also expect further advances in drug delivery systems that are likely to give peptides an additional boost as a drug class.
the future of PePtidesinterview with dr. daniel erne, cto
Daniel Erne is a chemistry PhD with 29 years of experience in peptide chemistry. 26 of those years were spent with Bachem Group. Dr. Erne headed the Quality Control depart-ment of Bachem Feinchemikalien AG, as it was then known, established the Quality Assurance and Regulatory Affairs unit and has been a member of the Bachem Group’s Corporate Executive Committee since 1997.
21 Bachem Annual Report 2013
What are the new trends in peptide therapeutics that you observe in the United States?Recently we have observed a striking increase in the complexity of the molecules we are requested to develop. There is a significant demand for longer peptidebased active pharmaceutical ingredients. Furthermore, modifications to the peptide basic structure are often requested. We are frequently asked to produce peptides conjugated with other chemical entities such as PEG or lipids. The development of industrially viable synthetic strategies for these types of peptidic molecules represents a significant challenge. Fortunately, Bachem has always invested in recruiting topnotch scientists with strong backgrounds in both peptide and organic chemistry. This allows us to integrate our available expertise in different fields and to design robust manufacturing processes.
What are the specific challenges you face today?Devising new synthetic strategies to make such complex molecules in industrial quantities also calls for stateoftheart analytical capabilities. The characterization of these molecules requires specialized equipment and a significant effort in analytical method development. In the R&D department of Bachem Americas, Inc. we recently expanded our analytical capabilities to address the specific requirements of the process development approach.
What excited you last year?Still on the subject of peptide complexity, we have seen a significant interest in dyeconjugated peptides for tumordiagnostic applications. Dyes, specifically fluorescent dyes, are extremely sensitive molecules. We had the opportunity last year to develop dyeconjugated peptides for human application. We were rewarded with great success and were excited both to be able to produce these complex molecules and to be actively supporting the battle against cancer.
What is your outlook for the next years?We are really excited about the future. The complexity of the molecules described requires exactly the type of expertise we have developed in the Bachem Group. We have the background knowledge necessary to successfully produce these molecules at large scale and in consistent quality. Bachem is well positioned to further expand its worldwide leadership in peptide manufacturing, true to the claim to be a Pioneering Partner for Peptides to both the biotech and pharmaceutical industry.
the future of PePtidesinterview with dr. matteo villain
Pioneering Partner for PePtides
Dr. Matteo Villain joined Bachem Americas, Inc. in 2004 and is VP of Research and Development. He has 20 years of experience in peptide chemistry and collaborated with different universities and research organizations in both the USA and Switzerland. His main focus was the development of peptide therapeutics and solid-phase peptide synthesis strategies. He is a contributor to more than 20 peer reviewed scientific publications, and is an inventor in multiple approved patents.
