"目錄號: HY-14740
Metabolic Enzyme/ProteaseAnti-infection-
Elvitegravir 是一種HIV integrase抑制劑饵撑，作用于 HIV-1IIIB苹支，HIV-2EHO和 HIV-2ROD，IC50分別為 0.7 nM级历，2.8 nM 和 1.4 nM互婿。
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生物活性
Description
Elvitegravir is anHIV integraseinhibitor for HIV-1IIIB, HIV-2EHOand HIV-2RODwithIC50of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
IC50& Target
IC50: 0.7 nM (HIV-1IIIB), 2.8 nM (HIV-2EHO), 1.4 nM(HIV-2ROD)[1]
In Vitro
Elvitegravir (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratory strains of HIV, with EC50values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir is evaluated against wild-type clinical isolates representing various subtypes of HIV-1. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC50ranging from 0.1 to 1.26 nM. Moreover, Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor, the compound L-870,810. The cytotoxicities of these inhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration that suppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from three independent donors are 4.6±0.5 μM and 2.7±0.6 μM, respectively. Thus, Elvitegravir can suppress various HIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated with resistance to currently approved antiretroviral drugs[1].
Clinical Trial
Gilead Sciences
HIV Infection
July 2008
Phase 3
Massachusetts General Hospital-Brigham and Women's Hospital-Gilead Sciences
HIV Disease
January 2014
St Stephens Aids Trust-ViiV Healthcare
HIV
October 2014
Phase 1
Fundacion Clinic per a la Recerca Biomédica
HIV
June 6, 2015
Phase 4
Fondation Ophtalmologique Adolphe de Rothschild
HIV
September 2016
University of Washington-Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann-Gilead Sciences
HIV-2 Infection
September 2014
Phase 4
St Stephens Aids Trust-Merck Sharp & Dohme Corp.
HIV
March 2015
Phase 4
AIDS Clinical Trials Group-National Institute of Allergy and Infectious Diseases (NIAID)
HIV-1 Infection
January 2017
Phase 2
Janssen Sciences Ireland UC
Healthy
June 2015
Phase 1
Juan A. Arnaiz-Hospital Clinic of Barcelona
Patient Compliance-Antiretroviral Therapy Intolerance
June 2015
Phase 4
Technische Universit?t München-Gilead Sciences-MUC Research GmbH
Insulin Resistance
July 2014
Phase 1
Merck Sharp & Dohme Corp.
HIV-1 Infection
June 9, 2015
Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)-Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
HIV Infections
March 2003
Phase 4
University of Zurich
HIV Infections
January 2002
Gilead Sciences
HIV Infections
February 2007
Phase 2
Gilead Sciences
Acquired Immune Deficiency Syndrome (AIDS)-HIV Infections
August 26, 2013
Phase 2-Phase 3
Gilead Sciences
Acquired Immunodeficiency Syndrome-HIV Infections
December 6, 2012
Phase 2-Phase 3
PENTA Foundation
HIV Infection
June 2016
Phase 2-Phase 3
Juan A. Arnaiz-Hospital Clinic of Barcelona
AIDS
January 2015
Phase 3
Gilead Sciences
HIV-HIV-1-Human Immunodeficiency Virus
February 2006
Phase 2
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References
