The versatile peptides penetrating deep into tissue

自行车^® 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. 自行车 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.

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

自行车 can also be joined with each other to form higher order structures such as tandems, 三聚, 和四聚体, allowing them to engage targets and target classes inaccessible to traditional small molecules or to engage multiple drug targets or cell types simultaneously.

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

参考文献

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