Integrase inhibitor

Integrase inhibitor
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Integrase_inhibitor".

Integrase inhibitors are a class of antiretroviral drug developed for the treatment of HIV infection, although they are not necessarily limited to HIV treatment. They block the action of integrase, an enzyme that integrates genetic material from the virus into its target cell.

The US FDA approved the first, Raltegravir, brand name Isentress, on October 12, 2007.

Integrase Inhibitors may be taken in combination with other types of HIV drugs to minimize adaptation by the virus. They are also necessary for people whose virus has become immune to current treatments, called salvage therapy.

Drugs under development

GS 9137 or JTK-303, licensed by Gilead Sciences from Japan Tobacco.

This drug is the only other one in development. It is currently undergoing Phase 2 trials. GS 9137 (Elvitegravir) is a low-molecular-weight, highly selective integrase inhibitor that shares the core structure of quinolone antibiotics.^[1]

References

^ AIDSinfo - HIV/AIDS Drug Information - GS 9137 (elvitegravir)

External links

MK-0518, the first Integrase Inhibitor for HIV
HIV Antiretroviral Agents in Development
GS 9137 (elvitegravir) factsheet from NIH
Savarino A. A historical sketch of the discovery and development of HIV-1 integrase inhibitors. Expert Opin Investig Drugs. 2006 Dec;15(12):1507-22. [1][2]

MeSH integrase+inhibitors

content

v • d • e Pharmacology: enzyme inhibition

Class	Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition

Substrate	Oxidoreductase (EC 1): Aromatase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors Transferase (EC 2): Integrase inhibitor - Protein kinase inhibitors - Reverse transcriptase inhibitors - COMT inhibitors Hydrolase (EC 3): Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors (ACE inhibitor, Trypsin inhibitor) - Histone deacetylase inhibitor Lyase (EC 4): Carbonic anhydrase inhibitors

v • d • e Antivirals used against HIV (HAART) (primarily J05)

Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI)	Abacavir (ABC)° • Dexelvucitabine^§ • Emtricitabine° • Lamivudine (3TC)° • Tenofovir° • Didanosine • Zidovudine (AZT) • Apricitabine^† • Stampidine^† • Elvucitabine^† • Racivir^† • Amdoxovir^† • Stavudine^‡ • Zalcitabine^‡

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)	Ateviridine^§ • Capravirine^§ • Efavirenz° • Emivirine^§ • Lodenosine^§ • Nevirapine • Etravirine • Rilpivirine^† • Loviride^‡ • Delavirdine^‡ • Quinotaline^§

Protease Inhibitors (PI)	Atazanavir° • Brecanavir^§ • Fosamprenavir° • Lopinavir° • Darunavir • Nelfinavir • Ritonavir • Saquinavir • Tipranavir • Amprenavir^‡ • Indinavir^‡

Entry/fusion inhibitors	Aplaviroc^§ • Enfuvirtide • Maraviroc • Vicriviroc^† • PRO 140^† • Ibalizumab^†

Integrase inhibitors	Raltegravir • Elvitegravir^†

Maturation inhibitors	Bevirimat^† • Vivecon™^†

Combined formulations	Combivir • Atripla • Trizivir • Truvada • Kaletra • Epzicom

Other & experimental agents	Foscarnet • Hydroxyurea • Synergistic enhancers • Epigallocatechin gallate • Portmanteau inhibitors • Globoidnan A • Griffithsin • Diarylpyrimidines • Calanolide A • Cyanovirin-N • Miltefosine • R-roscovitine^†

°DHHS preferred first-line agent. ^†Undergoing clinical trials, not FDA approved. ^‡Formerly or rarely used agent. ^§Development terminated.

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