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
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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