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Turning peptides into drugs

It is possible to overcome most of the challenges of using peptides as drugs through peptide enhancement techniques. These aims to constrain the structure of the amino acid chain to make it more rigid and stable, thereby decreasing its susceptibility to degradation, all while maintaining or improving the efficacy of the molecule.

Through Zealand’s 13 years of experience, the company has been focused on peptide drug discovery and development and built a world-leading position in the field. We have an experienced and integrated R&D organization, broadly recognized for its capabilities, and with all main functions in-house, including:

  • Identification of novel biological targets and testing of their therapeutic relevance (idea generation)
  • Innovation, design, modification and optimization of peptides
  • Solutions to the challenges of turning peptide molecules into durable, stable and cost-effective drugs
  • Preclinical and clinical development of novel drugs targeting diabetes/metabolic diseases and related disorders

Through our focused R&D process and our skills in peptide drug innovation and optimization we have created focused peptide libraries consisting of more than 3,900 peptides, filed 440 active patent applications, of which 159 have been issued, and have taken 8 new compounds into the clinic since our interception in 1998.

New peptide drug program

The outset for every new peptide drug program at Zealand is the identification of a biological target with therapeutic relevance in a given disease area. Upon selection of the disease target, we build or screen groups of peptides which have high binding affinity to this target to select peptide backbones (amino acid sequences) to form the basis for the further drug discovery process.

The subsequent process of structural modification of therapeutically relevant peptides for optimized peptide drug potency and selectivity is one of Zealand’s key competences. Furthermore, we have in-house expertise in the optimization of selected lead peptide molecules for better cost effectiveness, improved delivery and longer shelf life for the end product.

Peptide enhancement techniques applied by Zealand in the peptide innovation and optimization process include:

  • Replacement, addition and deletion of amino acids
  • Amino acid chain constraining techniques to make the peptide structure more rigid and to improve the molecular stability of the peptide
  • Addition of conjugates to decrease susceptibility to degradation.

Beside our capabilities in the process of turning peptides into drugs, we have built substantial in-house preclinical expertise, including the optimization and effective use of a range of different disease models in our therapeutic target areas.

We also have in-house competences and knowledge in effectively taking drug candidates through the early stages of clinical development through to Phase IIa proof of concept studies in humans. In the design of clinical studies, we combine our internal clinical expertise in our target therapeutic areas with close interaction with medical experts and potential partners to ensure a constant insight and understanding of medical trends and patient focus.

SIP® technology

An example of a Zealand proprietary peptide enhancing technology is the SIP® tail technology, which stands for Structure Induced Probe. The SIP® technology adds a number of specific aminoacids to the peptide, thereby strengthening or tightening its molecular structure to make it less susceptible to biological degradation. This ensures a longer life-span in the blood and thereby
permits less frequent dosing. The SIP® technology has been employed for lixisenatide, ZP1846 and elsiglutide.

More recent projects at Zealand have involved the addition of a fatty acid to the amino acid chain of a given peptide as another technique to increase its half life in the blood stream, working with dual acting peptides where one compound is able to simultaneously activate two different
peptide receptors (e.g. ZP2929), and the use of new methods to restrain the peptide structure as in the collaboration with Pepscan.