Integrase inhibitor

Source: Wikipedia, the free encyclopedia.

Integrase inhibitors (INIs) 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 have been applied to other retroviruses. The class of integrase inhibitors called integrase strand transfer inhibitors (INSTIs) are in established medical use. Other classes, such as allosteric integrase inhibitors (ALLINIs) or integrase binding inhibitors (INBIs), are still experimental.

The

Isentress).[1] Research published at the time supported the conclusion that "[for people living with HIV,] raltegravir plus optimized background therapy provided better viral suppression than optimized background therapy alone for at least 48 weeks."[2]

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.[3] They are also useful in salvage therapy for patients whose virus has mutated and acquired resistance to other drugs.[citation needed]

Drugs in use and under development

In use

  • Raltegravir (Isentress), developed by Merck & Co., was the first INSTI approved by the FDA in October 2007.
  • Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
    ).
  • Dolutegravir (Tivicay), licensed by ViiV Healthcare, was approved for use in the US in 2013, and in the EU in January 2014.
  • The combination drug
    better source needed
    ]
  • Cabotegravir, developed by ViiV Healthcare, was approved in conjunction with rilpivirine by the FDA in January 2021 (cabotegravir/rilpivirine).

Under development

  • Pirmitegravir (STP0404)
  • MK-2048, a second generation integrase inhibitor, that appears to have a duration of action up to four times longer than raltegravir.[citation needed]

See also

References

  1. U.S. Food and Drug Administration. October 12, 2007. Archived from the original
    on January 12, 2017. Retrieved October 8, 2019.
  2. S2CID 17257548
    .
  3. PMID 25151562
    .
  4. ^ "Elvitegravir". AIDSinfo. National Institutes of Health. Archived from the original on 2011-09-27. Retrieved 2007-10-13.
  5. ^ "U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection" (Press release). Gilead. February 7, 2018.

Further reading

  • Savarino A (December 2006). "A historical sketch of the discovery and development of HIV-1 integrase inhibitors". Expert Opin Investig Drugs. 15 (12): 1507–22.
    S2CID 207475472
    .

External links
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