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