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Critical Outcome Technologies Inc. Discovers Novel Scaffolds For Inhibiting HIV Integrase
The significance of these results is 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 novel 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. On the basis of these results, COTI has filed composition of matter patents and intends to proceed with the next phase of this project that consists of optimizing a small series of potential lead candidates based on these scaffolds.
"These encouraging results provide further validation of our CHEMSAS® technology and its ability to rapidly identify innovative small molecules for difficult drug targets. The discovery of new HIV integrase inhibiting scaffolds having an entirely novel mode of interacting with the enzyme has been challenging for HIV researchers, which makes these early results quite gratifying," said Dr Wayne Danter, COTI's President and CSO.
As previously announced, these novel scaffolds are part of a codevelopment program with a major pharmaceutical partner. The codevelopment partner is now conducting and funding agreed upon in vitro experiments in their evaluation of the compounds. Once these experiments have been completed and the results have been received by COTI, the codevelopment partner will have an exclusive time period to negotiate a licensing agreement with COTI for the compounds.
Notice to Readers
Information contained in this press release may contain certain statements which constitute "forward- looking statements" within the meaning of the Securities Act (Ontario) and applicable securities laws. For example, the statement "intends to proceed with the next phase of this project" is a forwardlooking statement. Forwardlooking statements, by their nature, are not guarantees of future performance and are based upon management's current expectations, estimates, projections and assumptions. COTI operates in a highly competitive environment that involves significant risks and uncertainties which could cause actual results to differ materially from those anticipated in these forwardlooking statements. Management of COTI considers the assumptions on which these forwardlooking statements are based to be reasonable, but as a result of the many risk factors, cautions the reader that actual results could differ materially from those expressed or implied in these forwardlooking statements. Information in this press release should be considered accurate only as of the date of the release and may be superseded by more recent information disclosed in later press releases, filings with the securities regulatory authorities or otherwise.
According to the UNAIDS 2008 Report on the Global AIDS Epidemic, there are 33 million people living with HIV around the globe. The annual number of new infections is approximately 2.7 million worldwide. In 2008, the HIV market was worth $11 billion across the seven major markets of France, Germany, Italy, Japan, Spain, the UK and the US and it is expected to grow to $16 billion by 2018. This growth is driven by the growing prevalence of HIV worldwide as well as the increasing life expectancy of those receiving treatment.
About Integrase Inhibitors
The development of HIV integrase inhibitors marks an important frontier in HIV research as integrase is one of the only enzymes that researchers have had difficulty targeting. Data from large efficacy trials suggests that drug combinations containing an integrase inhibitor achieved substantial levels of viral suppression in patients with drugresistant HIV. The response seen in patients was equivalent to that seen when highly active antiretroviral therapy became available.
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