For a more detailed description, please refer to our white paper, The Case for Allosteramers - Peptides as Drug Candidates.

The oral delivery of peptides is an area that has been poorly explored despite the existence of peptide-based drugs for 30 years. Allostera’s technology allows the development of short peptides (<12 amino acids) made from D-amino acids which prevents them from being degraded by stomach proteases or by any known enzymes in the human body. Allostera’s research has suggested that small peptides with certain special characteristics exhibit oral bioavailability which large proteins cannot easily attain. This because of the phenomenon of “paracellular transport” in the digestive tract.

Paracellular Transport in the Gut

Allosteramers™ are hydrophilic (water-seeking) molecules protected from degradation and therefore are ideally suited for absorption in the gut via paracellular transport.

While most drug development focuses on absorption of hydrophobic (water-avoiding) drugs in the gut directly through cells of the gut wall (transcellular transport), paracellular transport takes advantage of the concept that the gut is designed to be “leaky”. The cells of the gut wall are connected together with specific proteins that form narrow passageways that allow solutes to diffuse through this barrier. While the connections between these cells were historically named “tight junctions” they are anything but tight for certain molecules – the passageways allow many hydrophilic molecules that are small and flexible enough to permeate the barrier.

Allosteramers™ take Advantage of Paracellular Transport

We have shown that certain Allosteramers™ have the inherent properties that enable them to diffuse through these tight junctions. Given that Allosteramers™ are highly potent, we don’t need much drug to reach the system in order to achieve adequate dosing by oral administration. Thus, Allosteramers™ represent a new class of drugs that is both potent and specific like monoclonal antibodies, but also orally bioavailable like small molecules.

Additionally, Allostera’s Module X platform is the first technology that can allow screening of multiple, active, small D-peptides active against the same target for their inherent oral bioavailability.