Current medical therapy is not without problems. Commonly used small molecule and antibody drugs both have multiple limitations.
There are several limitations of small molecule drugs:
Small surface area exposure can limit binding affinity and specificity
Poor modulation of protein-protein Interactions; Most designs cannot incorporate avidity or allosteric modulation
Need for optimizing ADME
Meanwhile, there are also multiple limitations of antibody biologics as well:
Biophysical properties prevent cell penetration and limit tissue penetration
Many uncertainties in the drug product CMC and immunogenicity
Manufacturing process complexity and high cost
Challenges of undruggable targets and Protein-Protein Interaction:
Among the most difficult and “undruggable” targets are those which exert their biological function through engagement in intracellular protein-protein interactions.
Flat and extended contact surfaces along with intracellular localization make such target very challenging for antibodies or small molecule drugs to act.
To respond to this unmet medical need, Tavotek has created a new generation of intracellular targeting multicyclic peptides for tissue penetration and modulation of protein-protein interactions.
The design strategy for these MIP molecules are:
Multicyclic to obtain antibody-like potency and specificity
Large binding footprint for targeting protein-protein interactions
Tissue penetration with smaller molecule
Engineered targeting to the diseased cell
Direct intracellular targeting for destruction via proteasomes
Relatively easy and inexpensive to manufacture
Potential oral or pulmonary dosing
Potential advantages of Tavotek’s MIP molecules are:
More accurate homing of molecule to target tissue
More complete intra-cellular delivery for optimal protein-protein interaction intervention
Binding and targeting intracellular tumor targets for their degradation using innate proteasomal machinery
Higher stability of our multicyclic design with potentially more surface area to better modulate the target protein activity
Potentially orally available with additional features added to inhibit GI digestion