are a class of antiretroviral drug
designed to block the action of integrase
, a viral enzyme that inserts the viral genome into the DNA
of the host cell. Since integration is a vital step in retroviral replication, blocking it can halt further spread of the virus. Integrase inhibitors were initially developed for the treatment of HIV
infection, but they could be applied to other retroviruses.
The first integrase inhibitor approved by the U.S. Food and Drug Administration
(FDA) was raltegravir
(brand name Isentress
), approved on October 12, 2007. Research results published in the New England Journal of Medicine
on July 24, 2008, concluded that "raltegravir plus optimized background therapy provided better viral suppression than optimized background therapy alone for at least 48 weeks."
Since integrase inhibitors target a distinct step in the retroviral life cycle, they may be taken in combination with other types of HIV drugs to minimize adaptation by the virus. They are also useful in salvage therapy
for patients whose virus has mutated and acquired resistance to other drugs.
Drugs under development
- Elvitegravir (GS 9137 or JTK-303), licensed by Gilead Sciences from Japan Tobacco, is currently undergoing Phase 3 clinical trials. GS 9137 is a low-molecular-weight, highly selective integrase inhibitor that shares the core structure of quinolone......