生物活性

• 描述Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture^[3]. Efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI) with IC50 of 60 nM^[4]. Efavirenz inhibits synthesis using an RNA PPT-primed substrate with an IC50 of 17 nM^[5]. Efavirenz is administered once-daily and its simple dosing schedule improves adherence to therapy allowing for durability of the virologic and clinical responses^[6]. Efavirenz exerts a lysergide (LSD)-like effect on brain serotonergic pathways and affects CNS metabolic pathways, including mitochondrial function^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01837277	Severely Immunocompromised HIV... more >> Patients Collapse <<	Phase 2 Phase 3	Unknown	March 2016	Brazil ... more >> Fundação Bahiana de Infectologia/SEI Not yet recruiting Salvador, Bahia, Brazil, 40010-160 Contact: Estela Luz, RN, MSci    32838123    eluz5@yahoo.com.br    Principal Investigator: Carlos Brites, MD, PhD          Sub-Investigator: Fabianna Bahia, MD, PhD          Universidade Federal do Rio de Janeiro Not yet recruiting Rio de Janeiro, RJ, Brazil Contact: Monica Ponze, RN    5521222739073       Principal Investigator: Mauro Schechter, MD, PhD          Hospital de Clinicas de Porto Alegre Not yet recruiting Porto Alegre, RS, Brazil Contact: Priscila Pelaez, MD          Principal Investigator: Eduardo Sprinz, MD, PhD Collapse <<
  NCT00002227	HIV Infections	Phase 2	Completed	-	United States, District of Col... more >>umbia Richard Elion Washington, District of Columbia, United States, 20009 The Whitman Walker Clinic Washington, District of Columbia, United States, 20009 United States, Massachusetts Community Research Initiative of New England Brookline, Massachusetts, United States, 02445 United States, Ohio Remington Davis Inc Columbus, Ohio, United States, 43215 United States, Pennsylvania The Milton S Hersey Med Ctr / Div of Hematology Hershey, Pennsylvania, United States, 170330850 United States, South Carolina Coastal Carolina Research Ctr Mount Pleasant, South Carolina, United States, 29464 United States, Texas Montrose Clinic Houston, Texas, United States, 77006 United States, Virginia Hampton Roads Med Specialists Hampton, Virginia, United States, 23666 Collapse <<
  NCT00002225	HIV Infections	Phase 2	Completed	-	United States, District of Col... more >>umbia The Whitman Walker Clinic Washington, District of Columbia, United States, 20009 United States, Illinois AIDS Research Alliance - Chicago Chicago, Illinois, United States, 60657 United States, New York North Shore AIDS Hosp / Division of Infectious Disease Manhassett, New York, United States, 11030 Univ of Rochester Med Ctr Rochester, New York, United States, 14642 United States, North Carolina Carolinas Research Associates Charlotte, North Carolina, United States, 28207 Collapse <<

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• 参考文献

• [1] Held DM, Kissel JD, et al. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22.

  [2] Young SD, Britcher SF, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5.

  [3] Young SD, Britcher SF, Tran LO, Payne LS, Lumma WC, Lyle TA, Huff JR, Anderson PS, Olsen DB, Carroll SS, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5

  [4] Held DM, Kissel JD, Saran D, Michalowski D, Burke DH. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22

  [5] Grobler JA, Dornadula G, Rice MR, Simcoe AL, Hazuda DJ, Miller MD. HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem. 2007 Mar 16;282(11):8005-10

  [6] Maggiolo F. Efavirenz. Expert Opin Pharmacother. 2007 Jun;8(8):1137-45

  [7] Van de Wijer L, Schellekens AFA, Burger DM, Homberg JR, de Mast Q, van der Ven AJAM. Rethinking the risk-benefit ratio of efavirenz in HIV-infected children. Lancet Infect Dis. 2016 May;16(5):e76-e81

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