The versatile peptides penetrating deep into tissue

Bicycles^® are synthetic bicyclic peptides rotationally limited by symmetrical small molecule scaffolds that constrain the molecule into rigid two-loop structures. They can be optimised to have high affinity and exquisite selectivity to difficult-to-drug targets. Bicycles are made stable through optimisation and their low molecular weight delivers favourable pharmacokinetics, enabling deep tissue penetration, high solubility and flexibility in the areas of manufacturing, route of administration and formulation.

Bicycles are being investigated in a number of ways and disease areas, including as cytotoxic targeting agents (Bicycle^® Toxin Conjugates, or BTCs) where a tumor-targeting Bicycle is linked to a toxin payload to form a drug conjugate.¹ The tumor-targeted Bicycle directs the payload to the specific cell or tissue for release and targeted therapeutic response.

Bicycles can also be joined with each other to form higher order structures such as tandems, trimers, and tetramers, allowing them to engage targets and target classes inaccessible to traditional small molecules or to engage multiple drug targets or cell types simultaneously.

Bicycles are a new modality that have the potential to become part of the next generation of therapeutics, combining specificity, potency, and attractive drug-like properties. In collaboration with Bicycle Therapeutics, we are developing Bicycle-based molecules against a wide range of drug targets in two of our therapy areas, Respiratory & Immunology and Cardiovascular, Renal and Metabolism. 

References

1. http://www.bicycletherapeutics.com/programs/#bicycle-conjugates