Indian Institute of Science (IISc) researchers have demonstrated a novel method for improving the pharmacokinetic properties of macrocyclic peptides – drug molecules that are pursued heavily by pharmaceutical industries worldwide.
- The researchers have demonstrated that substituting just a single atom – oxygen with sulphur – in the backbone of a macrocyclic peptide can make it more resistant to digestive enzymes and can increase its permeability through cell membranes, boosting its bioavailability. Drug absorption is quantified in terms of bioavailability.
- Bioavailability is the extent to which absorption occurs. In other words, bioavailability is the fraction of the administered drug that reaches the systemic circulation in the unchanged form.
