Researchers have developed a new anticoagulant with anti-clotting activity that can be quickly reversed to minimise the risk of serious bleeding in hospitals.
The therapy combines a lab-made peptide with one from a blood-feeding insect, the tsetse fly (genus Glossina), an insect which is linked to the serious and debilitating illness known as sleeping sickness.
The anticoagulant activity can be switched off on demand by applying an antidote that breaks the relatively weak bonds holding the 2 peptides together.
The researchers hope their work will lead to new treatments that minimise the risk of serious bleeding in hospital emergency admissions. It’s estimated that anticoagulant-related bleeding is responsible for 15% of all emergency hospital admissions due to adverse drug effects.
The new findings are published in Nature Biotechnology.
“What’s exciting here is that we have applied a completely novel approach to drug discovery,” says coauthor Rich Payne, a professor at the school of chemistry at the University of Sydney.
“The anticoagulant we have developed uses what we call supramolecular chemistry. This allows the two active molecules needed to suppress coagulation, to self-assemble.
“The architecture also means we can apply an antidote that can quickly disassemble the joined molecules, triggering a rapid cessation of the active combination and the anticoagulant effect.
“This has never been done before in drug discovery.”
The tsetse-fly-derived peptides block the action of the clotting enzyme thrombin.
This new approach could offer a more reliable option for surgical and post-operative drugs and for managing a range of conditions, such as heart disease, stroke, and venous thrombosis.
