New Era in Drug Development - Oral Peptides.


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  • Mar 29, 2017
    One of the biggest bottlenecks in therapeutic development is that a large proportion of the proteins can currently not be targeted by classical small molecules administered orally.
    For decades, a substantial number of proteins, vital for treating various diseases, have remained elusive to oral drug therapy. Traditional small molecules often struggle to bind to proteins with flat surfaces or require specificity for particular protein homologs. Typically, larger biologics that can target these proteins demand injection, limiting patient convenience and accessibility.

    A potential solution could be offered by cyclic peptides due to their ability to bind challenging targets with high affinity while being relatively small and, thus, in reach of being orally available.
    Cyclic peptides, which are versatile molecules known for their high affinity and specificity in binding challenging disease targets. At the same time, developing cyclic peptides as oral drugs has proven difficult because they are rapidly digested or poorly absorbed by the gastrointestinal tract.

    Now a team of scientists at The École polytechnique fédérale de Lausanne (EPFL) has succeeded in generating cyclic peptides that bind to a disease target of choice and can also be administered orally. This finding opens the door to a new class of orally available drugs, addressing a long-standing challenge in the pharmaceutical industry.

    Prof Christian Heinis comments -
    "There are many diseases for which the targets were identified but drugs binding and reaching them could not be developed. Most of them are types of cancer, and many targets in these cancers are protein-protein interactions that are important for the tumor growth but cannot be inhibited."