Integrase inhibitor

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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.

[edit] 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]

[edit] References

1. ^ http://aidsinfo.nih.gov/DrugsNew/DrugDetailT.aspx?int_id=421

[edit] 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

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 - Kinase inhibitors - Reverse transcriptase inhibitors Hydrolase (EC 3): Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors (ACE inhibitor, Trypsin 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)° • Emtricitabine° • Lamivudine (3TC)° • Tenofovir° • Didanosine • Zidovudine (AZT) • Apricitabine† • Stampidine† • Elvucitabine† • Racivir† • Amdoxovir† • Stavudine‡ • Zalcitabine‡ Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) Efavirenz° • Nevirapine • Etravirine • Rilpivirine† • Loviride‡ • Delavirdine‡ Protease Inhibitors (PI) Atazanavir° • Fosamprenavir° • Lopinavir° • Darunavir • Nelfinavir • Ritonavir • Saquinavir • Tipranavir • Amprenavir‡ • Indinavir‡ Entry/fusion inhibitors 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.