HIV Integrase Inhibitors

The Need

The Human Immunodeficiency Virus (HIV) is the virus that causes Acquired Immunodeficiency Syndrome (AIDS). HIV attacks the immune system, resulting in a chronic, progressive illness and leaving infected people vulnerable to opportunistic infections and cancers. The median time from infection to AIDS diagnosis now exceeds 10 years. AIDS is often fatal. There is no cure.

According to the Joint United Nations Programme on HIV/AIDS (UNAIDS) there were 39.5 million people worldwide living with HIV. Moreover, in 2006 there were 4.3 million people newly affected with HIV. Also in 2006 there were 2.9 million deaths related to AIDS.

Our Solution

COTI believes that future optimal therapy will include a combination of a Reverse Transcriptase Inhibitor (RTI), a Protease Inhibitor (PI) and an Integrase Inhibitor (IntInh). HIV Integrase is the viral enzyme system responsible for incorporating viral DNA into host DNA resulting in chronic infection. Integrase inhibitors may also become an effective preventative therapy following accidental exposure.

A library of 10 low toxicity anti-HIV small molecules (EC50 < 1 µmol/l) which are also highly effective in silico against HIV Integrase (i.e. IC50 < 1 µmol/l) has been discovered and undergone final optimization.