Drugs in R & D

, Volume 8, Issue 3, pp 155–168 | Cite as

HIV-1 Integrase Inhibitors

An Emerging Clinical Reality
  • Raveendra Dayam
  • Laith Q. Al-Mawsawi
  • Nouri Neamati
Review Article

Abstract

From the discovery of HIV-1 integrase (IN) inhibitors using enzyme-based assays in 1992, it has taken 15 years to achieve success in human clinical trials. Currently available antiretroviral drugs set high clinical standards in efficacy and long-term safety for upcoming novel HIV/AIDS therapeutic agents. The results from advanced stages of human clinical trials with IN inhibitors indicate a promising future for these compounds as a novel class of antiretroviral drugs. Success and failure of previously discovered antiretroviral drugs have taught us that there are no magic bullets in eradicating HIV. However, approval of drugs selectively targeting IN has long been awaited. There is once again a surge of interest in the field focusing on clinical development of IN inhibitors. Here, we summarise the current status of IN inhibitors under clinical development. These agents include S-1360, GSK-364735, L-870,810, L-870,812, MK-0518, GS-9137, L-900564, GS-9224, and BMS-707035. Promising antiviral activity has already been achieved with MK-0518 and GS-9137 in late-stage clinical studies.

Keywords

Strand Transfer Potent Antiviral Activity Catalytic Core Domain Optimise Background Therapy Quinolone Carboxylic Acid 

Notes

Acknowledgements

This work was supported by grants from The Campbell Foundation and the Universitywide AIDS Research Program to Nouri Neamati. The authors have no conflicts of interest that are directly relevant to the content of this review.

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Copyright information

© Adis Data Information BV 2007

Authors and Affiliations

  • Raveendra Dayam
    • 1
  • Laith Q. Al-Mawsawi
    • 1
  • Nouri Neamati
    • 1
  1. 1.Department of Pharmacology and Pharmaceutical Sciences, School of PharmacyUniversity of Southern CaliforniaLos AngelesUSA

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