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efavirenz (Sustiva)

HIV-1 reverse transcriptase inhibitor; RN given for (+-)-isomer; L-743,726 is the (S)-isomer; structure in first source

Also Known As:

Sustiva; 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; Bristol-Myers Squibb brand of efavirenz; DMP 266; DMP-266; Du Pont brand of efavirenz; L 743,726; L 743726; L-743,726; L-743726; Merck Sharp & Dohme brand of efavirenz; Stocrin; United Drug brand of efavirenz; efavirenz, (R)-isomer; efavirenz, (S)-isomer

Networked: 642 relevant articles (33 outcomes, 136 trials/studies)

Relationship Network

Drug Context: Research Results

Heterocyclic Compounds: 60
- 1-Ring Heterocyclic Compounds
  - Oxazines: 2
    - Benzoxazines: 7
      - efavirenz: 642
- 2-Ring Heterocyclic Compounds
  - Benzoxazines: 7
    - efavirenz: 642

Experts

1.	Haas, David W: 17 articles (12/2015 - 12/2004)
2.	Gulick, Roy M: 17 articles (02/2015 - 04/2004)
3.	Ribaudo, Heather J: 15 articles (02/2015 - 04/2004)
4.	Morse, Gene D: 10 articles (08/2014 - 06/2003)
5.	Daar, Eric S: 9 articles (02/2015 - 12/2007)
6.	Acosta, Edward P: 9 articles (08/2014 - 04/2004)
7.	Sax, Paul E: 9 articles (07/2014 - 12/2009)
8.	Kuritzkes, Daniel R: 9 articles (03/2010 - 04/2004)
9.	Grinsztejn, Beatriz: 8 articles (01/2016 - 08/2004)
10.	Havlir, Diane V: 8 articles (04/2015 - 10/2003)

Related Diseases

1.	Infection 07/01/2014 - "Association between efavirenz as initial therapy for HIV-1 infection and increased risk for suicidal ideation or attempted or completed suicide: an analysis of trial data." 07/01/2015 - "In 2010-12, the proportion of fully active efavirenz-based ART was lower in cases of subtype B versus non-B infection (P = 0.021). " 03/01/2015 - "CAP-EFV-NPs showed significantly higher prophylactic activity (P < 0.01) against HIV-1 infection to TZM-bl cells as compared to efavirenz solution and blank CAP nanoparticles. " 03/01/2015 - "CAP-EFV-NPs, CAP-EFV-NP-Gel and efavirenz solution were evaluated for cytotoxicity to HeLa cells and for in vitro short-term (1-day) and long-term (3-day) prophylaxis against HIV-1 infection in TZM-bl cells. " 08/01/2014 - "Efavirenz is widely prescribed for HIV-1 infection. "
2.	HIV Infections (HIV Infection) 11/01/2012 - "First-line treatment of HIV infection: efavirenz is better documented." 06/01/2008 - "This case report provides evidence that reduced efavirenz doses may be effective in the treatment of HIV infection. " 01/01/2001 - "In conclusion, current treatment guidelines for HIV infection recognise efavirenz-based combination regimens as a first-line treatment option. " 01/01/2015 - "Electronic databases (Pubmed, Embase, the Cochrane Library, Trip Database) were searched up till 23 December 2013 for randomized controlled clinical trials published as a peer-reviewed papers, and concerning efavirenz-based regimens used as initial treatment for HIV infection. " 08/04/2009 - "Stepped-dose versus full-dose efavirenz for HIV infection and neuropsychiatric adverse events: a randomized trial."
3.	Tuberculosis (Tuberculoses) 02/01/2014 - "We investigated the population pharmacokinetics and pharmacogenetics of efavirenz in 307 patients coinfected with human immunodeficiency virus and tuberculosis and included in the Cambodian Early vs Late Initiation of Antiretrovirals trial (CAMELIA) in Cambodia. " 01/01/2014 - "Plasma concentrations, efficacy and safety of efavirenz in HIV-infected adults treated for tuberculosis in Cambodia (ANRS 1295-CIPRA KH001 CAMELIA trial)." 01/15/2015 - "Pregnancy and tuberculosis treatment or prophylaxis can affect efavirenz pharmacokinetics, maternal human immunodeficiency virus type 1 (HIV-1) treatment outcomes, and mother-to-child transmission (MTCT) risk. " 01/15/2015 - "Pharmacokinetics of efavirenz and treatment of HIV-1 among pregnant women with and without tuberculosis coinfection." 01/01/2015 - "Efavirenz dosing: influence of drug metabolizing enzyme polymorphisms and concurrent tuberculosis treatment."
4.	Acquired Immunodeficiency Syndrome (AIDS) 08/01/2014 - "This study aimed to develop a reverse phase high-performance liquid chromatographic (RP-HPLC) method for the determination of efavirenz in human plasma and to use it for determining the concentrations of efavirenz in Chinese AIDS patient. " 07/01/2014 - "Adverse experiences were measured at 1 and 6 months using the efavirenz checklist, a 35-item instrument developed by the AIDS Clinical Trials Group. " 08/01/2013 - "The aim of this study was therefore to evaluate the effects of 14 single-nucleotide polymorphisms (SNPs) in five drug-metabolizing enzyme genes on steady-state plasma efavirenz levels in South African HIV/AIDS patients as well as their clinical validity. " 12/01/2012 - "Antiretroviral therapy-naive AIDS Clinical Trials Group studies A5202, A5095, and ACTG 384 included plasma sampling for efavirenz pharmacokinetics. " 01/01/2012 - "This study investigated variation in NR1I2 and NR1I3 and its effect on plasma efavirenz levels in HIV/AIDS patients. "
5.	Body Weight (Weight, Body) 10/01/2009 - "We aimed in this study to describe efavirenz concentration-time courses in treatment-naïve children after once-daily administration to study the effects of age and body weight on efavirenz pharmacokinetics and to test relationships between doses, plasma concentrations, and efficacy. " 01/14/2015 - "Impact of body weight on virological and immunological responses to efavirenz-containing regimens in HIV-infected, treatment-naive adults." 01/01/2014 - "A low efavirenz concentration was independently associated with 18492T→C (β=-0.937, P=0.004) and high body weight (β=-0.032, P=0.046). " 02/01/2013 - "As shown by multivariate analysis, low efavirenz concentrations were significantly associated with the 1/1 haplotype (beta = -1.084, P = 0.027) and high body weight (beta = -0.076, P = 0.002). " 01/01/2013 - "However, the proportion of patients with efavirenz concentrations below 1,000 ng/ml was not different between those weighing less than or more than 50 kg (6% and 10%, respectively; P=0.13) and a body weight above 50 kg was not associated with a higher risk of plasma efavirenz concentrations below 1,000 ng/ml. When plasma efavirenz concentrations below 1,000 ng/ml were present, they were not associated with virological failure. "

Related Drugs and Biologics

1.	emtricitabine (Emtriva)
2.	tenofovir
3.	Nevirapine (Viramune)
4.	Carbon Monoxide
5.	Ritonavir (Norvir)
6.	lopinavir (Kaletra)
7.	Protease Inhibitors (Protease Inhibitor)
8.	Rifampin (Rifampicin)
9.	MK 0518
10.	Lamivudine (3TC)

Related Therapies and Procedures

1.	Highly Active Antiretroviral Therapy (HAART)
2.	Castration
3.	Directly Observed Therapy
4.	Art Therapy
5.	Aftercare (After-Treatment)