Scientists from EPFL have increased the bioavailability of special drugs for stroke prevention ninefold. The study, which will lead to the development of the first oral drugs for many diseases, was published in the journal Nature Chemical Biology.
There are many diseases for which the target molecules are known. Blocking these molecules with drugs can cure patients, relieve symptoms or slow progression. But most drugs are small, flat molecules that cannot bind effectively to large targets. This problem can be solved with the help of protein drugs, but their requirement for injection makes their use difficult.
In a new study, scientists show that special molecules, cyclic peptides, can bind to complex targets when taken orally. These small, circular molecules are made of the same building blocks as larger proteins. Previously, they were difficult to use as oral medications because they were quickly digested or poorly absorbed in the gastrointestinal tract. To make cyclic peptides more stable, researchers added thioester bonds to their structures.
The resulting drugs were tested on animals. When tested, the peptides showed oral bioavailability of up to 18%; that is, 18% of the drug successfully entered the bloodstream and had a therapeutic effect. Considering that orally administered cyclic peptides typically exhibit bioavailability below 2%, increasing this rate to 18% is a significant advance.
Experimental cyclic peptides targeted thrombin, a protein molecule that plays a central role in the blood clotting process. Targeting this is key to preventing and treating thrombotic diseases, including stroke and heart attack.
The scientists noted that their method is universal: It can be adapted to target a wide range of proteins, potentially leading to breakthroughs in the treatment of many diseases.
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Source: Gazeta
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