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Peptide Drugs - IRBM
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Peptides represent a unique class of pharmaceutical compounds, molecularly poised between small molecules and proteins, yet biochemically and therapeutically distinct from both. As intrinsic signalling molecules for many physiological functions, peptides present an opportunity for therapeutic intervention that closely mimics natural pathways. Peptide-based therapeutics are currently experiencing a renaissance in the global market with collective sales of more than US$ 20 Billion in 2017 and more than 100 approved peptide therapeutics for various clinical indications.

The peptide chemistry group at IRBM Science Park has a world-class expertise in the development of peptide therapeutics with an excellent track record in the clinic (7 patent applications and 3 clinical candidates approved since 2010). The group is structured to deliver high-quality peptides, difficult sequences and powerful tools for drug discovery research targeting one or more of the following requirements:

  • Unique intrinsic properties
  • Excellent pharmacological profile
  • High specificity, safety, tolerability, and efficacy
  • Low complexity production
  • Affordable production cost

The team has extensive experience in different therapeutic areas with a focus on target identification/validation and lead optimization. The hit-to-lead process proceeds from peptide engineering and design, through multi-parametric optimization for activity, efficacy and selectivity. The discovery phase takes advantage of a large collection of non-natural amino acids (>500, commercial or ad hoc synthesized) and chemical constraints to stabilize the active conformation.

Peptide Discovery - Macrocyclic drugs: Synthesis of NonNatural Amino Acids
Peptide Discovery - Macrocyclic drugs: Synthesis of NonNatural Amino Acids

Pharmacokinetics profiles are optimized by modifying peptide structures to overcome rapid metabolism and disposition due to enzymatic degradation and renal clearance. Finally, potential anaphylactic effects caused by mast cell activation and histamine release can be assessed in vitro, ensuring a cost-effective way of identifying dangerous responses prior to entering in vivo trials.

Peptide Discovery – Macrocyclic Drugs: Synthesis of Building Blocks for Linkers
Peptide Discovery – Macrocyclic Drugs: Synthesis of Building Blocks for Linkers

An integrated platform of different areas of expertise expands our peptide discovery efforts with additional tools, including the use of our phage display libraries, structural studies through NMR and the bioanalysis of peptides for in vivo studies supported by state-of-the-art mass spectrometry instrumentation.

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