There are three natural product classes known to potently inhibit cyclophilins: cyclosporins, peptolides, and sanglifehrins. All three compounds are off patent and can be used to generate derivatives that are new/patentable and have new property profiles that can be tailored to specific therapeutic requirements. Cypralis has assembled a collection of over 2,000 compounds that are potent cyclophilin inhibitors, are mostly non-immunosuppressive (defined as absence of calcineurin inhibition) and span a wide range of cyclophilin subtype inhibitory potency, solubility, and PK properties. The collection includes compounds that are suitable for intravenous injection/infusion, for oral and topical applications and have generally excellent drug properties. Notably, members of one chemical family have been shown to penetrate the blood-brain barrier, giving high brain levels in rodents after oral dosing.
Cypralis has established extensive IP protection around these compounds and is using them as pharmacological tools for target validation studies and as starting points for medicinal chemistry programmes.
Please contact us to explore opportunities for collaboration or investment.