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HIV Integrase Library

According to the UNAIDS 2009 Report on the Global AIDS Epidemic, there are more than 33 million people living with HIV worldwide. The annual number of new infections is approximately 2.7 million worldwide. It has been estimated that the global HIV/AIDS market was worth $12 billion in 2009.

COTI believes that future optimal therapy for HIV infection will continue to include a combination of a Reverse Transcriptase Inhibitor, a Protease Inhibitor and an Integrase Inhibitor however, there is a need for a second generation integrase inhibitor with a with a binding mode that is different from current integrase treatments and that is active against specific mutant strains of the virus.

COTI has focused on the discovery and development of novel virocidal HIV integrase inhibitors characterized by activity against Isentress® (raltegravir) resistant mutant strains and a unique binding mode that differentiates it from current integrase treatments. This small library of small molecules is designed to be orally available and engineered so that no boosting is required.

Licensing/Co-Development Opportunity

At present, COTI has synthesized a number of scaffolds. Initial confirmatory in vitro testing of the first three novel scaffolds demonstrated good inhibitory activity in a biochemical HIV integrase assay at nanomolar concentrations. Either these compounds will be further developed or new analogs will be generated in meeting the virocidal and mutation resistance objectives.

COTI is currently looking for a licensing or co-development partner for these compounds.

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