COTI Phase 1 results showed that the majority of currently marketed and developmental stage HIV Integrase inhibitors have a very similar way of interacting with and inhibiting the enzyme through a diketo acid type moiety.
COTI has used its proprietary technology, Chemsas, to discover several new small molecule scaffolds that have an entirely new binding mode and interaction with the active site of the viral enzyme.
COTI has completed the synthesis and initial confirmatory in-vitro testing of the first three novel scaffolds from this program. All three scaffolds demonstrated good inhibitory activity in a biochemical HIV integrase assay at nanomolar concentrations.
Based on these results, COTI has filed composition of matter patents and intends to proceed with the next phase of this project that consists of optimising a small series of potential lead candidates based on these scaffolds.
Wayne Danter, president and CSO of COTI, said: “The discovery of new HIV integrase inhibiting scaffolds having an entirely new mode of interacting with the enzyme has been challenging for HIV researchers.”