Development Capability

Mimetica has demonstrated the ability to successfully transfer the biological activity of peptide GPCR ligands to its proprietary scaffolds in every case attempted.

It has also demonstrated the ability to optimise those active compounds to increase activity and selectivity.

Lead Compounds

Mimetica has developed active (< 10 uM) mimetics against several receptors including:

C5a – inflammation
MC-1 – inflammation, pigmentation
MC-4 – obesity, sexual function
MC-5 – dermatology
SST-4/5 – anti-angiogenesis, cancer
urotensin II
integrin GPIIb/IIIa

The most advanced compounds are those for MC5-R which show low nanomolar activity and 100 fold selectivity.

The mimetics have several advantages over native peptides making them more likely to be useful drugs:

enhanced stability
increased lipophilicity
improved bioavailability
increased rigidity
decreased size

Representative mimetics have demonstrated good levels of caco-2 permeability, stability to plasma and cellular proteases and oral availability in rat models. No evidence of systematic stability or toxicity problems has been found.

Mimetica’s unique chemistry provides many opportunities for the optimisation of the lead compounds initially generated. The unique flexibility and control of the synthesis and the range of Mimetica’s scaffolds means that iterative optimisation can be highly effective. Mimetica has demonstrated that variation of the scaffold shape can lead to large increases in activity and selectivity.