Integrase inhibitors in salvage therapy regimens for HIV-1 infection. 2009

Kersten K Koelsch, and David A Cooper
National Centre in HIV Epidemiology and Clinical Research, University of New South Wales, Sydney, Australia. k.koelsch@amr.org.au

OBJECTIVE To review current knowledge and the role of integrase inhibitors in the setting of HIV salvage therapy. We will discuss results from recent studies and literature and comment on the potential for integrase inhibitors in defined clinical settings. RESULTS Raltegravir has been studied most intensively in treatment-experienced patients and is the first integrase inhibitor that has been licensed for use in this patient group. Most studies have shown good tolerability data and very potent virus suppression. In patients with limited treatment options, switching from enfuvirtide appears to be well tolerated, whereas switching from a protease inhibitor-based regimen may increase the rates of viral failure. Elvitegravir also showed good results in early phase clinical trials and is currently undergoing phase III clinical trials. CONCLUSIONS Given that integrase inhibitors belong to a new class of antiretroviral agents with a diverse drug resistance profile, and are active against both chemokine (C-C motif) receptor 5 and chemokine (C-X-C motif) receptor 4 strains, they are exciting additions to salvage therapy regimen. Raltegravir and elvitegravir are metabolized via different pathways, which will affect their respective use. The major limitation for the use of integrase inhibitors is a potentially low threshold for viral drug resistance, so functional monotherapy must be avoided.

UI MeSH Term Description Entries
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015363 Quinolones A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID. Ketoquinoline,Ketoquinolines,Oxoquinoline,Oxoquinolines,Quinolinone,Quinolinones,Quinolone
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D015658 HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS). HTLV-III Infections,HTLV-III-LAV Infections,T-Lymphotropic Virus Type III Infections, Human,HIV Coinfection,Coinfection, HIV,Coinfections, HIV,HIV Coinfections,HIV Infection,HTLV III Infections,HTLV III LAV Infections,HTLV-III Infection,HTLV-III-LAV Infection,Infection, HIV,Infection, HTLV-III,Infection, HTLV-III-LAV,Infections, HIV,Infections, HTLV-III,Infections, HTLV-III-LAV,T Lymphotropic Virus Type III Infections, Human
D016879 Salvage Therapy A therapeutic approach, involving chemotherapy, radiation therapy, or surgery, after initial regimens have failed to lead to improvement in a patient's condition. Salvage therapy is most often used for neoplastic diseases. Salvage Treatment,Therapy, Salvage,Salvage Therapies,Salvage Treatments,Therapies, Salvage,Treatment, Salvage,Treatments, Salvage
D019428 HIV Integrase Inhibitors Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA. Integrase Inhibitors, HIV,Inhibitors, HIV Integrase

Related Publications

Kersten K Koelsch, and David A Cooper
December 2010, The Journal of antimicrobial chemotherapy,
Kersten K Koelsch, and David A Cooper
July 2010, Future medicinal chemistry,
Kersten K Koelsch, and David A Cooper
July 2006, AIDS patient care and STDs,
Kersten K Koelsch, and David A Cooper
November 2007, Medizinische Monatsschrift fur Pharmazeuten,
Kersten K Koelsch, and David A Cooper
July 2008, Current opinion in drug discovery & development,
Kersten K Koelsch, and David A Cooper
May 1999, Lancet (London, England),
Kersten K Koelsch, and David A Cooper
April 2000, Lancet (London, England),
Kersten K Koelsch, and David A Cooper
April 2005, MMW Fortschritte der Medizin,
Kersten K Koelsch, and David A Cooper
August 1999, Journal of medicinal chemistry,
Kersten K Koelsch, and David A Cooper
April 1997, Journal of medicinal chemistry,
Copied contents to your clipboard!