ライフサイエンスコーパス: EFV

17 re obtained over a period of 40 days, from 9 EFV-naive men (i.e., men about to receive EFV for the fi

18 1 RNA in SP was undetectable in 8 (89%) of 9 EFV-naive men and remained undetectable in 10 (83%) of 1

19 However, all EFV concentrations in SP were >/=40-fold higher than the

20 The US EFV package insert recommends an EFV dose increase for patients on RIF weighing >/=50 kg.

21 , VAF from 190+/-83 cm2 to 107+/-44 cm2, and EFV from 137+/-37 ml to 98+/-25 ml (all p<0.0001).

22 tions conferring resistance to NVP, DLV, and EFV and several HIV-1 clades A in PBMC.

23 ed 20 weeks of tenofovir, emtricitabine, and EFV.

24 ATV+DDI+FTC and EFV+FTC-TDF were hypothesized to be non-inferior to EFV+

25 assay, it was remarkably superior to NVP and EFV and comparable to ETV.

26 e relationship between the degree of NVP and EFV resistance and the impairment of viral replication i

27 s) were markedly less susceptible to NVP and EFV.

28 The effects of ATV/r and EFV upon safety and tolerability risk did not differ sig

29 the TC/HDL-C ratio were similar with RPV and EFV.

30 ray absorptiometry) of rilpivirine (RPV) and EFV plus 2 nucleoside/nucleotide reverse transcriptase i

31 participants with virologic failure assigned EFV had more RT changes, including and excluding known r

32 The other principal differences between EFV and l-Glu in CYP46A1 activation include an apparent

33 g the dosing interval, no single SPrcolon;BP EFV-concentration ratio was significantly predictive of

34 We propose a model for CYP46A1 activation by EFV and show that EFV enhanced CYP46A1 activity and cere

35 in the ABC/3TC and TDF/FTC groups (combining EFV and ATV/r arms; median change, -341 [interquartile r

36 Comparing EFV+FTC-TDF to EFV+3TC-ZDV, during a median 184 wk of fo

37 be adequate in patients receiving concurrent EFV.

38 atment-naive patients on regimens containing EFV versus NVP from randomised trials and observational

39 oxil fumarate (DF)-emtricitabine once daily (EFV-TDF-FTC group).

40 citabine-tenofovir-disoproxil fumarate (DF) (EFV+FTC-TDF).

41 At such small doses, EFV may be devoid of adverse effects elicited by high dr

42 ral decay rate was also faster in the 3-drug EFV group than in the triple-nucleoside group (P=.09).

43 ntly faster in subjects receiving the 3-drug EFV regimen (0.67/day), compared with those receiving th

44 men), zidovudine/lamivudine plus EFV (3-drug EFV regimen) or zidovudine/lamivudine/abacavir plus EFV

45 ral decay in subjects randomized to a 3-drug EFV-based regimen corresponded to the overall superior e

46 Decay rates in the 4-drug EFV group were intermediate.

47 ovudine/lamivudine/abacavir plus EFV (4-drug EFV regimen).

48 Efavirenz (EFV) is a nonnucleoside reverse transcriptase inhibitor

49 tabine (FTC)/NVP (n = 9), TDF/3TC/efavirenz (EFV) (n = 6), and TDF/FTC/EFV (n = 19).

50 and M184V with failure of d4T/3TC/efavirenz (EFV; P < .01).

51 ), including nevirapine (NVP) and efavirenz (EFV), has been associated with severe hepatic injury.

52 , especially nevirapine (NVP) and efavirenz (EFV).

53 Compared with no ART, efavirenz (EFV) reduced exposure to all antimalarial components by

54 nges compared with those assigned efavirenz (EFV) (P >/= .13).

55 immunodeficiency virus (HIV) drug efavirenz (EFV) alters mitochondrial function in cultured neurons a

56 , we found that the anti-HIV drug efavirenz (EFV) can pharmacologically activate CYP46A1 in mice.

57 ith lamivudine or emtricitabine): efavirenz (EFV) plus zidovudine (AZT) (n = 524); EFV plus tenofovir

58 pared to historical estimates for efavirenz (EFV)- and ritonavir/lopinavir (LPV/r)-based regimens.

59 th standard of care-co-formulated efavirenz (EFV)/FTC/TDF-as initial treatment for HIV infection.

60 udy was conducted to determine if efavirenz (EFV) or atazanavir/ritonavir (ATV/r)-based combination a

61 isoenzymes, potentially lowering efavirenz (EFV) exposure.

62 transcriptase inhibitors (NNRTI) efavirenz (EFV) and nevirapine (NVP) in first-line antiretroviral t

63 e transcriptase inhibitor (NNRTI) efavirenz (EFV) showed subunit-specific perturbation in the rate of

64 acodynamic, and dose responses of efavirenz (EFV) in SP versus those in blood plasma (BP).

65 nimals received a short course of efavirenz (EFV) monotherapy before combination ART was started.

66 were exposed to a short course of efavirenz (EFV) monotherapy.

67 The distribution of efavirenz (EFV) was then monitored in a series of hair strands coll

68 In the presence of efavirenz (EFV), a virus carrying RT-K103N together with IN-G140S a

69 zanavir plus ritonavir (ATV/r) or efavirenz (EFV) in initial antiretroviral regimens among women and

70 found that four pharmaceuticals (efavirenz (EFV), acetaminophen, mirtazapine, and galantamine) presc

71 compared the effect of switching efavirenz (EFV) to raltegravir (RAL) on hepatic steatosis among HIV

72 01E+G190S are highly resistant to efavirenz (EFV) and can develop during failure of EFV-containing re

73 and delavirdine (DLV), but not to efavirenz (EFV) and etravirine (ETR), consistent with their increas

74 he noninferiority of switching to efavirenz (EFV) versus remaining on ritonavir-boosted lopinavir (LP

75 ng triple-nucleoside-based versus efavirenz (EFV)-based regimens.

76 rom the excitotoxic insult, while efavirenz (EFV) did not contrast the neurotoxic effect of glutamate

77 ir (TDF)-emtricitabine (FTC) with efavirenz (EFV) or atazanavir plus ritonavir (ATV/r), on bone miner

78 r DF-emtricitabine (TDF/FTC) with efavirenz (EFV) or atazanavir-ritonavir (ATV/r).

79 r DF/emtricitabine (TDF/FTC) with efavirenz (EFV) or atazanavir/ritonavir (ATV/r) in human immunodefi

80 lamivudine [3TC]/zidovudine [ZDV]/efavirenz [EFV], 3TC/ZDV/nelfinavir [NFV], or other regimens) and s

81 /3TC than for TDF/FTC when given with either EFV or ATV/r.

82 onducted a pharmacokinetic study to evaluate EFV trough concentrations (Cmin) and human immunodeficie

83 occurred more frequently among those failing EFV, the clinical relevance of which warrants further in

84 reduced susceptibility to NVP (8.9-13-fold), EFV (4-56-fold), etravirine (ETV; 1.9-4.7-fold) and decr

85 Virologic failure following EFV-containing treatment was associated with more HIV-1

86 and -4.0% (P = .024), respectively; and for EFV versus ATV/r were -1.7% and -3.1% (P = .035) and -3.

87 0.610/day), significantly slower than d1 for EFV-based regimens [P < .001]).

88 the mechanisms responsible for the frequent EFV-associated neurotoxicity.

89 ith NAFLD were randomized 1:1 to switch from EFV to RAL (400 mg twice daily), maintaining nucleoside

90 ants exposed to ART from conception, TDF-FTC-EFV was associated with a lower risk for adverse birth o

91 arate, emtricitabine, and efavirenz (TDF-FTC-EFV) (901 of 2472 [36.4%]) compared with TDF-FTC and nev

92 Compared with TDF-FTC-EFV, all other regimens were associated with higher risk

93 TDF/3TC/efavirenz (EFV) (n = 6), and TDF/FTC/EFV (n = 19).

94 TDF/FTC/EFV was equivalent or superior to its comparator arms.

95 emtricitabine/tenofovir disoproxil fumarate (EFV/FTC/TDF).

96 aecalibacterium prausnitzii were depleted in EFV and PI compared to HIV SN and negatively correlated

97 The loss in EFV was limited (-27+/-11%) compared to VAF diminution (

98 o cART and 10 each taking cART that included EFV or ATV/r.

99 (NRTI) regimen versus regimens that included EFV plus an NRTI.

100 Nucleoside Reverse Transcriptase Inhibitors (EFV) or ritonavir-boosted Protease Inhibitors (PI) with

101 Six years after treatment initiation, EFV plus AZT showed the highest cumulative resistance in

102 o receive ABC-3TC or TDF-FTC with open-label EFV or ATV/r.

103 ted Cox regression confirmed that first-line EFV plus AZT (reference) was associated with a higher me

104 ompared to <60 kg, was associated with lower EFV Cmin (1.68 vs 2.02, P = .021).

105 iated with a trend toward higher, not lower, EFV Cmin compared to EFV alone.

106 Patients weighing >/=60 kg had lower median EFV Cmin versus those <60 kg, but there was no associati

107 Overall, median EFV exposure in SP was 3.4% (range, 2.0%-5.0%) of that i

108 We then evaluated the anti-HIV medication EFV for the mode of interaction with CYP46A1 and the eff

109 Moreover, EFV and l-Glu synergistically activated CYP46A1.

110 infection and reduces susceptibility to NVP, EFV, ETV, and AZT.

111 escribed EFV, but only 32% of NVP and 50% of EFV-associated episodes were detected during the first 1

112 gs include the greater antiviral activity of EFV versus NVP and longer intracellular half-life of FTC

113 After three doses over 4 days of EFV monotherapy, 103N mutations (AAC and AAT) rapidly em

114 The doses of EFV administered to mice and required for the stimulatio

115 e data do not support weight-based dosing of EFV with RIF.

116 V-1-infected women, and once-daily dosing of EFV+FTC-TDF are advantageous for use of this regimen for

117 renz (EFV) and can develop during failure of EFV-containing regimens in patients.

118 es in 50% inhibitory concentration (IC50) of EFV than viruses carrying a single NNRTI mutation.

119 rations with cholesterol, in the presence of EFV or l-Glu, suggest that water displacement from the h

120 eplicate more efficiently in the presence of EFV than in its absence.

121 Similarly, in the presence of EFV, the RT-E138K plus IN-G140S/Q148H mutant virus was f

122 This finding supports the use of EFV as the preferred NNRTI in first-line treatment regim

123 The ratio of %EFV to %VAF loss decreased with sleep apnea syndrome (1.

124 mefantrine were 10-fold lower in children on EFV vs LPV/r-based ART, changes that were associated wit

125 he IN-G140S/Q148H mutations had no effect on EFV or RPV susceptibility.

126 ) patients on RAL and 3 (15%) individuals on EFV (P = .029).

127 s (HIV) virologic suppression in patients on EFV (600 mg) and RIF-based tuberculosis treatment in the

128 HIV-infected patients on EFV plus tenofovir/emtricitabine or abacavir/lamivudine

129 s of recurrent malaria by day 28 in those on EFV vs LPV/r-based ART.

130 For those on EFV, close clinical follow-up for recurrent malaria foll

131 95% confidence interval [CI] 0.76, 2.05) or EFV (HR 1.23, 95% CI 0.77, 1.96), with significantly sho

132 receiving failing regimens containing NVP or EFV, respectively.

133 ed a randomized trial of open-label ATV/r or EFV combined with abacavir/lamivudine (ABC/3TC) or tenof

134 n a 1:1 ratio to receive EVG/COBI/FTC/TDF or EFV/FTC/TDF, once daily, plus matching placebo.

135 d protease inhibitors are often favored over EFV in women of childbearing potential.

136 proximately 2.5 microM for both p66- and p51-EFV complexes, 250 nM for the p66/p66-EFV complex, and 7

137 66/p66-EFV complex, and 7 nM for the p51/p51-EFV complex.

138 ssociation constant of 92 nM for the p66/p51-EFV complex was calculated from the thermodynamic linkag

139 In the crystal structure of the p66/p51-EFV complex, the drug is bound to the p66 subunit.

140 nd p51-EFV complexes, 250 nM for the p66/p66-EFV complex, and 7 nM for the p51/p51-EFV complex.

141 imen) or zidovudine/lamivudine/abacavir plus EFV (4-drug EFV regimen).

142 leoside regimen), zidovudine/lamivudine plus EFV (3-drug EFV regimen) or zidovudine/lamivudine/abacav

143 EFV Cmin was measured 20-28 hours post-EFV dose at weeks 4, 8, 16, 24 on-RIF and weeks 4, 8 off

144 y, including 312 and 256 patients prescribed EFV and NVP, respectively.

145 prescribed NVP and 8.0% of those prescribed EFV, but only 32% of NVP and 50% of EFV-associated episo

146 9 EFV-naive men (i.e., men about to receive EFV for the first time) and from 12 EFV-experienced men

147 Seven hundred eighty patients received EFV; 543 provided >/=1 EFV Cmin.

148 experienced men (i.e., men already receiving EFV as part of an antiretroviral regimen).

149 oholic fatty liver disease (NAFLD) receiving EFV plus 2 nucleoside analogues.

150 at TE in HIV-infected patients not receiving EFV.

151 eiving ATV/r, and 2 of 10 subjects receiving EFV in combination with atovaquone 750 mg BID achieved a

152 Subjects receiving EFV-based cART had 47% and 44% lower atovaquone AUCtau t

153 Only 5 of 10 subjects receiving EFV-based cART plus atovaquone 750 mg BID had an atovaqu

154 Compared with RPV, EFV significantly (P < .001) increased lipid levels.

155 with previously published results and the RT-EFV cocrystal structure.

156 In SP, EFV reaches concentrations above the HIV-1 IC(90)(WT) th

157 48 weeks, HIV-infected individuals switching EFV to RAL showed decreases in the degree of hepatic ste

158 d parameters and fewer dyslipidemia AEs than EFV-based treatment.

159 icant losses in spine, but not hip, BMD than EFV.

160 Fewer (P < .001) RPV-treated patients than EFV-treated patients had TC, LDL-C, and triglyceride lev

161 More RPV- than EFV-treated patients had HDL-C values below these cutoff

162 We determined that EFV stimulates K101E+G190S virus during early infection

163 for CYP46A1 activation by EFV and show that EFV enhanced CYP46A1 activity and cerebral cholesterol t

164 We show that EFV promotes inducible nitric oxide synthase (iNOS) expr

165 We also showed that EFV stimulates K101E+Y188L and K101E+V106I virus, but no

166 The EFV variation was not correlated with percentage of body

167 edian time to viral suppression than did the EFV-TDF-FTC group (28 vs. 84 days, P<0.001), as well as

168 L arm and 30 (Q1-Q3, -17 to 49) dB/m for the EFV group (P = .011).

169 the CYP46A1 surface, which differs from the EFV-binding site.

170 ies/mL by 48 months was 0.07 and 0.12 in the EFV and LPV/r groups, respectively (P = .21).

171 pies/mL were less frequently observed in the EFV group than the LPV/r group (odds ratio [OR] 0.67, 95

172 s lower in the DTG-ABC-3TC group than in the EFV-TDF-FTC group (2% vs. 10%); rash and neuropsychiatri

173 higher in the DTG-ABC-3TC group than in the EFV-TDF-FTC group (88% vs. 81%, P=0.003), thus meeting t

174 lence) were significantly more common in the EFV-TDF-FTC group, whereas insomnia was reported more fr

175 n participants with virologic failure in the EFV-TDF-FTC group.

176 48 in the EVG/COBI/FTC/TDF group than in the EFV/FTC/TDF group (median 13 mumol/L, IQR 5 to 20 vs 1 m

177 the EVG/COBI/FTC/TDF group vs 18/352 in the EFV/FTC/TDF group).

178 to EFV+FTC-TDF versus 313 (60%) assigned to EFV+3TC-ZDV (HR 0.64, CI 0.54-0.76; p<0.001) and there w

179 76 (15%) among 519 participants assigned to EFV+3TC-ZDV (HR 1.51, CI 1.12-2.04; p = 0.007).

180 curred in 243 (46%) participants assigned to EFV+FTC-TDF versus 313 (60%) assigned to EFV+3TC-ZDV (HR

181 se inhibitor backbone than women assigned to EFV, or men assigned to ATV/r.

182 ward higher, not lower, EFV Cmin compared to EFV alone.

183 TC-TDF had similar high efficacy compared to EFV+3TC-ZDV in this trial population, recruited in diver

184 Comparing ATV+DDI+FTC to EFV+3TC-ZDV, during a median follow-up of 81 wk there we

185 -TDF were hypothesized to be non-inferior to EFV+3TC-ZDV if the upper one-sided 95% confidence bound

186 EVG/COBI/FTC/TDF was non-inferior to EFV/FTC/TDF; 305/348 (87.6%) versus 296/352 (84.1%) of p

187 in 2 of 2 RT-SHIV-infected macaques prior to EFV exposure.

188 , indicating that they were present prior to EFV exposure.

189 ted children >/=3 years of age from LPV/r to EFV are sustained long-term.

190 Children randomized to EFV had a reduced risk of elevated total cholesterol (OR

191 zed to ATV/r compared to women randomized to EFV.

192 ring the early steps of infection similar to EFV, but that the newest NNRTI, etravirine (ETR), did no

193 =3 years of age were randomized to switch to EFV or remain on LPV/r in Johannesburg, South Africa.

194 Comparing EFV+FTC-TDF to EFV+3TC-ZDV, during a median 184 wk of follow-up there w

195 e emergence, compared with other treatments: EFV plus TDF (hazard ratio [HR], 0.57; range, 0.42-0.76)

196 The US EFV package insert recommends an EFV dose increase for p

197 nce imaging to assess epicardial fat volume (EFV), cardiac function, and computed tomography visceral

198 g a single-cycle cell culture assay in which EFV was added either during the infection or the virus p

199 With EFV, lipid levels increased in each N[t]RTI subgroup (ex

200 similar extent (by 12% with RPV and 11% with EFV).

201 rease in limb fat (16% with RPV and 17% with EFV).

202 treated (348 with EVG/COBI/FTC/TDF, 352 with EFV/FTC/TDF).

203 ic failure rates were seen with ABC/3TC with EFV (HR 2.46, 95% CI 1.20, 5.05) or ATV/r (HR 2.22, 95%

204 mes to regimen modification for ABC/3TC with EFV or ATV/r and to safety events with EFV.

205 14, hsCRP, and Lp-PLA2 levels, compared with EFV/FTC/TDF.

206 ide analogues unchanged, or to continue with EFV plus 2 nucleoside analogues.

207 by CAP, compared with those continuing with EFV.

208 r ABC/3TC or TDF/FTC were not different with EFV or ATV/r.

209 with EFV or ATV/r and to safety events with EFV.

210 domized to 4 arms of ABC-3TC or TDF-FTC with EFV or ATV/r.

211 emia AEs were less common with RPV than with EFV.

212 transition at lower viremia levels than with EFV.

213 more common with EVG/COBI/FTC/TDF than with EFV/FTC/TDF (72/348 vs 48/352) and dizziness (23/348 vs

214 Individuals who received 3TC/ZDV/EFV had a more rapid phase 1 viral decay rate than those

215 Our findings indicate that the 3TC/ZDV/EFV regimen may be more potent than 3TC/ZDV/NFV or other

216 y with efavirenz plus lamivudine-zidovudine (EFV+3TC-ZDV), atazanavir plus didanosine-EC plus emtrici