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European Biopharmaceutical Review

Optimised Peptide APIs

Udo Haberl, Hans-Georg Frank and Marco Emgenbroich at AplaGen GmbH analyse the pharmacokinetic and pharamacodynamic optimisation of peptide APIs

PEPTIDES AS APIS: ADVANTAGES AND DRAWBACKS

Peptides as a class of active agents are somewhere on the borderline between classical biotechnological drugs and small drugs. They resemble recombinant drugs in view of their general protein nature, but are usually produced by chemical methods in a solid phase synthesis process. Their protein nature is the strongest point for their potential use as drugs. Most of the interactions inside cells and inside the whole body are based on protein-protein interactions, at least as far as phenotypic changes – including changes in disease state – are concerned.

Many of these interactions are already characterised, and there are numerous recognised endogenous peptides which prove the general concept of peptides as drugs. Thus, there is an entry into drug design and discovery which is remarkably direct and easy, as is the case for small drugs. Usually, small drugs do not show such a close relationship to internal body processes and interactions as peptides. However, these advantageous similarities to the internal machinery of the body are combined with some less advantageous properties which are common to most peptides of possible pharmacological relevance.


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Dr Udo Haberl is Head of Drug Design at AplaGen GmbH. He obtained a PhD from the University of Bonn, specialising in theoretical organic chemistry and the development of anti-cancer drugs. He is author of molecular modeling software and worked at the University of Notre Dame (US) and at different biotech companies, where he gained 10 years of experience in the design of pharmaceutical drugs. At AplaGen, he focuses on the design and optimisation of peptide sequences, linker structures and new technologies for peptide stabilisation.

Dr Hans-Georg Frank is CSO and co-founder of AplaGen GmbH. He is a physician and obtained his PhD/MD from the Free University of Berlin. He worked scientifically at the Free University of Berlin and the University of Technology in Aachen, Germany, focusing on embryology, developmental biology and oncological topics. Besides working as an academic scientist he also managed clinical studies at Sandoz AG in Nürnberg, Germany. During his academic career he acquired significant grants from The Rockefeller Foundation and the WHO, as well as from the German Research Council, and has published more than 50 articles in peer-reviewed journals. He was also appointed as a Professor at the University of Technology in Aachen. At AplaGen, he focuses on the development of EPO-mimetic peptides.

Dr Marco Emgenbroich is currently Head of the Supportive Organic Chemistry group at AplaGen. His focus is the development of HES-based drug carrier systems. He studied chemistry in Düsseldorf, Germany. He obtained his doctorate degree in 2003 by further specialising in the area of biomimetic polymers. During his PhD studies he joined the DFG-graduate school ‘Molecular Physiology’ and managed the local exhibitions and symposia InCom and LifeCom on the area of bioanalytical chemistry. Before joining AplaGen Marco worked on bioanalytical applications of biomimetic receptors, during his postdoctorate studies in Dortmund, Germany.

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Dr Udo Haberl
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Dr Hans-Georg Frank
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Dr Marco Emgenbroich
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