HIV/AIDS still remains one of the biggest health challenges worldwide. With more than 37 million people living with HIV globally, developing new and effective treatment options continues to be a priority. Integrase inhibitors are an important new class of antiretroviral drugs that work by blocking the enzyme HIV integrase.

How do Integrase Inhibitors Work?

To understand how integrase inhibitors are effective against HIV, it's important to first know how the HIV life cycle works. After HIV enters and infects a host cell, it begins replicating by generating DNA from its RNA genetic material. This process of reverse transcription produces double-stranded HIV DNA. A key viral enzyme called integrase is then needed to insert this HIV DNA into the host cell's genome, where it can continue replicating and producing new virus particles.

Integrase Inhibitors work by blocking the integrase enzyme from performing its function of integrating the HIV DNA into the host cell's chromosomes. Without integration, the virus is unable to establish a persistent infection or replicate itself. The isolated HIV DNA is eventually degraded by the cell’s natural DNA repair processes. This mechanism of action makes integrase inhibitors a unique and important tool in suppressing and controlling HIV viral loads in infected individuals.

Approved Integrase Inhibitors Drugs

There are currently three integrase inhibitor drugs that have been approved by regulatory agencies like the FDA for clinical use:

Raltegravir (Isentress) - Developed by Merck, raltegravir was the first in class integrase inhibitor approved in 2007. It demonstrated good efficacy and tolerability in clinical trials.

Elvitegravir (Vitekta) - Developed jointly by Gilead Sciences and Janssen, elvitegravir was approved in 2012. It is primarily used as part of fixed-dose combination therapies.

Bictegravir (Biktarvy) - Developed by Gilead Sciences, bictegravir was approved in 2018. Clinical trials demonstrated it to be as effective as existing drugs with a higher resistance barrier and fewer side effects.

All three drugs have demonstrated highly significant reductions in viral loads when used as part of combination antiretroviral therapy (cART). They have become important components of preferred first-line and switch HIV treatment regimens.