ライフサイエンスコーパス: lopinavir

1 is conserved across two drugs (ritonavir and lopinavir).

2 evirapine and 120 received ritonavir-boosted lopinavir).

3 , except for small effects of amprenavir and lopinavir.

4 1-6.95 nM for atazanvir and 0.64-8.54 nM for lopinavir.

5 avir, saquinavir, ritonavir, amprenavir, and lopinavir.

6 1.13-1.26], p<0.0001), and ritonavir-boosted lopinavir (1.11 [1.06-1.16], p<0.0001), but not other ri

7 gned (1:1) to receive oral ritonavir-boosted lopinavir (100 mg ritonavir, 400 mg lopinavir) plus 400

8 itro, but they did inhibit ZMPSTE24 (IC(50): lopinavir, 18.4 +/- 4.6 microM; tipranavir, 1.2 +/- 0.4

9 Dual therapy consisted of lopinavir 400 mg and ritonavir 100 mg plus lamivudine 15

10 Triple therapy consisted of lopinavir 400 mg and ritonavir 100 mg twice daily and la

11 eive a ritonavir-boosted protease inhibitor (lopinavir 400 mg with ritonavir 100 mg, twice per day) p

12 mg) once daily or ritonavir (100 mg)-boosted lopinavir (400 mg) twice daily, with prompt return to co

13 tipranavir, whereas 47% showed resistance to lopinavir, 58% showed resistance to atazanavir, and >60%

14 pharmacokinetics, and antiviral activity of lopinavir, a human immunodeficiency virus (HIV) protease

15 es high ethanol concentrations to solubilize lopinavir, a poorly soluble antiretroviral.

16 assessed included atazanavir, darunavir, and lopinavir (administered with ritonavir).

17 an 50% inhibitory concentrations (IC(50)) of lopinavir against isolates with 0 to 3, 4 or 5, 6 or 7,

18 the 50% inhibitory concentration (IC(50)) of lopinavir against seven mutant clones decreased by up to

19 utcomes were superior with ritonavir-boosted lopinavir among young children with no prior exposure to

20 avir-boosted atazanavir or ritonavir-boosted lopinavir and a nucleoside reverse transcriptase inhibit

21 The MDR 769 protease crystal complexes with lopinavir and DMP450 reveal completely different binding

22 hat NtRTI-sparing ART with ritonavir-boosted lopinavir and raltegravir (raltegravir-group) provided n

23 dovudine plus enteric-coated didanosine plus lopinavir and ritonavir for 7 days, (B) zidovudine plus

24 We investigated whether dual therapy with lopinavir and ritonavir plus lamivudine is non-inferior

25 Dual therapy with lopinavir and ritonavir plus lamivudine regimen warrants

26 Treatment with lopinavir and ritonavir, but not amprenavir, induced ER

27 rodrugs of the HIV protease inhibitors (PIs) lopinavir and ritonavir.

28 d decreased mucosal injury after exposure to lopinavir and ritonavir.

29 Our data indicated that the HIV PIs lopinavir and saquinavir affect preerythrocytic-stage pa

30 Lopinavir and saquinavir have gametocytocidal and transm

31 The HIV PIs lopinavir and saquinavir, the nonnucleoside reverse-tran

32 d non-inferior efficacy to ritonavir-boosted lopinavir and two or three NtRTIs (NtRTI-group) in parti

33 gating at high-concentrations of atazanavir, lopinavir, and amprenavir (APV).

34 dinavir, nelfinavir, amprenavir, saquinavir, lopinavir, and atazanavir revealed that the natural poly

35 PIs (ritonavir, lopinavir, and atazanavir) but not nucleoside reverse tr

36 level resistance to multiple PIs, but not to lopinavir, and grew to 30% of that of the wild type.

37 l cross-resistance to darunavir, atazanavir, lopinavir, and saquinavir, but not other PIs, and contai

38 efavirenz and rilpivirine, ritonavir-boosted lopinavir, and the integrase inhibitors raltegravir and

39 cing by specific small hairpin RNA prevented lopinavir- and ritonavir-induced barrier dysfunction in

40 rapy (n = 150) or continue ritonavir-boosted lopinavir-based therapy (n = 148).

41 y compared with continuing ritonavir-boosted lopinavir-based therapy did not result in significantly

42 ial viral suppression with ritonavir-boosted lopinavir-based therapy, switching to efavirenz-based th

43 s than 50 copies/mL during ritonavir-boosted lopinavir-based therapy; 298 were randomized and 292 (98

44 s nevirapine or tenofovir-emtricitabine plus lopinavir boosted by a low dose of ritonavir.

45 ion capacity was observed for atazanavir and lopinavir but not darunavir.

46 ART regimens were based on ritonavir-boosted lopinavir, combined with zidovudine or tenofovir plus la

47 ing clinically useful susceptibility only to lopinavir, darunavir, and saquinavir.

48 n amino acid residues in Gag correlated with lopinavir EC50 (p < 0.01), of which 380 K and 389I showe

49 The evolution of incremental resistance to lopinavir (emergence of new mutation[s] and/or at least

50 f 48 weeks, median predose concentrations of lopinavir exceeded the protein-binding corrected concent

51 s (OR = 1.66; 95% CI, 1.10-2.49), >/= 1 year lopinavir exposure (OR = 1.36; 95% CI, 1.06-1.73), and c

52 erculosis, preservation of ritonavir-boosted lopinavir for second-line treatment, and harmonization o

53 (14%) and 36 of 251 in the ritonavir-boosted lopinavir group (14%) had virologic failure or died.

54 mary end point than in the ritonavir-boosted lopinavir group (26% vs. 8%) (adjusted P=0.001).

55 virapine group than in the ritonavir-boosted lopinavir group (40.8% vs. 19.3%; P<0.001).

56 virapine group than in the ritonavir-boosted lopinavir group reached a primary end point (39.6% vs. 2

57 irapine group and 9 in the ritonavir-boosted lopinavir group), and 5 died without prior virologic fai

58 irapine group and 1 in the ritonavir-boosted lopinavir group).

59 and 0.284 (n = 42) in the ritonavir-boosted lopinavir group.

60 p and 0.020 (n = 3) in the ritonavir-boosted lopinavir group.

61 favirenz group than in the ritonavir-boosted lopinavir group.

62 , and either nevirapine or ritonavir-boosted lopinavir in HIV-infected children 2 to 36 months of age

63 plus either nevirapine or ritonavir-boosted lopinavir in HIV-infected children 6 to 36 months of age

64 with the regimen based on ritonavir-boosted lopinavir in Johannesburg, South Africa.

65 d to the recommendation of ritonavir-boosted lopinavir in such settings.

66 mance of nevirapine versus ritonavir-boosted lopinavir in young children has not been rigorously esta

67 navir, indinavir, ritonavir, saquinavir, and lopinavir, including amino acid substitutions D30N, I50V

68 On average, the IC(50) of lopinavir increased by 1.74-fold per mutation in isolate

69 Ritonavir, like lopinavir, inhibits ZMPSTE24 and leads to an accumulatio

70 ly demonstrated that a commonly used HIV-PI, lopinavir, inhibits ZMPSTE24, thereby blocking lamin A b

71 show, with metabolic labeling studies, that lopinavir leads to the accumulation of the farnesylated

72 alcohol and the HIV PIs ritonavir (RIT) and lopinavir (LOP).

73 follows: atazanavir (ATV) 300 mg once daily, lopinavir (LPV) 400 mg twice daily, or darunavir (DRV) 6

74 In contrast, lopinavir (LPV) and amprenavir did not increase osteocla

75 Rs were sensitive to the HIV-1 PR inhibitors lopinavir (LPV) and darunavir (DRV), as well as to the b

76 The crystal structures of lopinavir (LPV) and two new inhibitors containing phenyl

77 udy, antiretroviral drug granules, including lopinavir (LPV) ISNP granules and a fixed-dose combinati

78 = 524); EFV plus tenofovir (TDF) (n = 615); lopinavir (LPV) plus AZT (n = 573); LPV plus TDF (n = 30

79 issolution of an ASD containing RTV, ATV and lopinavir (LPV) was also investigated.

80 The safety and antiviral activity of lopinavir (Lpv), a protease inhibitor (PI) coformulated

81 election in culture against the PR inhibitor lopinavir (LPV), darunavir (DRV), or TL-3.

82 itors darunavir (DRV), saquinavir (SQV), and lopinavir (LPV), relative to that of PR.

83 (EFV) versus remaining on ritonavir-boosted lopinavir (LPV/r) for virologic control in children infe

84 in utero to ZDV/lamivudine/ritonavir-boosted lopinavir (LPV/r) had a higher left ventricular shorteni

85 estimates for efavirenz (EFV)- and ritonavir/lopinavir (LPV/r)-based regimens.

86 rom the 11 identified in these analyses (the lopinavir mutation score) may be useful for the interpre

87 HERG) potassium channels, and we showed that lopinavir, nelfinavir, ritonavir, and saquinavir caused

88 We also recorded block by lopinavir of repolarising potassium current (I(Kr)) chan

89 s were followed from the time they started a lopinavir or an atazanavir regimen.

90 ive confounders, currently receiving boosted lopinavir or darunavir as monotherapy (n = 67) or triple

91 onavir-boosted atazanavir, ritonavir-boosted lopinavir, other ritonavir-boosted protease inhibitors,

92 t efavirenz is inferior to ritonavir-boosted lopinavir (P < .001) for both end points.

93 t WHO's recommendation for ritonavir-boosted lopinavir plus NRTI for second-line antiretroviral thera

94 raltegravir would be non-inferior to boosted lopinavir plus NRTIs for virological suppression in reso

95 Ritonavir-boosted lopinavir plus raltegravir is an appropriate alternative

96 We aimed to assess whether boosted lopinavir plus raltegravir would be non-inferior to boos

97 oses below the approved dose (eg, efavirenz, lopinavir plus ritonavir, atazanavir, and darunavir).

98 e without prior exposure), ritonavir-boosted lopinavir plus tenofovir-emtricitabine was superior to n

99 (raltegravir group) or to ritonavir-boosted lopinavir plus two or three NRTIs selected from an algor

100 -boosted lopinavir (100 mg ritonavir, 400 mg lopinavir) plus 400 mg raltegravir twice a day (raltegra

101 Ritonavir and lopinavir precipitated acute, decompensated heart failur

102 susceptibility to the new protease inhibitor lopinavir (previously ABT-378) was explored using a pane

103 displayed >60-fold-reduced susceptibility to lopinavir, providing insight into suitable upper genotyp

104 y (Global AntiRetroviral Design Encompassing Lopinavir/r and Lamivudine vs LPV/r based standard thera

105 A total of 6668 individuals started a lopinavir regimen (213 deaths, 457 AIDS-defining illness

106 intention-to-treat' effect for atazanavir vs lopinavir regimens on each of the outcomes.

107 ion-to-treat hazard ratios for atazanavir vs lopinavir regimens were 0.70 (95% confidence interval [C

108 re at 12 months for atazanavir compared with lopinavir regimens.

109 ined eight or more mutations associated with lopinavir resistance and/or displayed >60-fold-reduced s

110 No lopinavir resistance was observed.

111 mong the subjects demonstrating evolution of lopinavir resistance, mutations at positions 82, 54, and

112 vudine and lamivudine plus ritonavir-boosted lopinavir resulted in better outcomes than did treatment

113 The most commonly used HIV PIs (lopinavir, ritonavir, and amprenavir) were used; their e

114 on-inferiority of fosamprenavir-ritonavir to lopinavir-ritonavir (95% CI around the treatment differe

115 genotypic resistance testing with respect to lopinavir-ritonavir (Kaletra) regimens and may provide i

116 with zidovudine (ZDV), lamivudine (3TC), and lopinavir-ritonavir (LPV/r), were followed up longitudin

117 ; ARR, 1.15; 95% CI, 1.04-1.27); TDF-FTC and lopinavir-ritonavir (TDF-FTC-LPV-R) (112 of 231 [48.5%];

118 based ART); or tenofovir, emtricitabine, and lopinavir-ritonavir (tenofovir-based ART).

119 (400 mg twice daily; n=353) or to remain on lopinavir-ritonavir (two 200 mg/50 mg tablets twice dail

120 dovudine alone); zidovudine, lamivudine, and lopinavir-ritonavir (zidovudine-based ART); or tenofovir

121 navir-ritonavir 700 mg/100 mg twice daily or lopinavir-ritonavir 400 mg/100 mg twice daily, each with

122 ent groups (fosamprenavir-ritonavir 53, 12%; lopinavir-ritonavir 43, 10%).

123 ohort of subjects, short-term treatment with lopinavir-ritonavir does not appear to directly promote

124 us-infected human subjects were treated with lopinavir-ritonavir for 1 month and, on the basis of for

125 itor-based antiretroviral therapy (ART) with lopinavir-ritonavir for human immunodeficiency virus (HI

126 rhoea, which occurred in ten patients in the lopinavir-ritonavir group (3%) and no patients in the ra

127 as longer in the efavirenz group than in the lopinavir-ritonavir group (P=0.006) but was not signific

128 19 (90.6%, 87.1-93.5) of 352 patients in the lopinavir-ritonavir group (treatment difference -6.2%, -

129 -ritonavir group and 317 of 444 (71%) in the lopinavir-ritonavir group achieving HIV-1 RNA less than

130 0.0001) in the raltegravir group than in the lopinavir-ritonavir group in each study, yielding combin

131 er of serious adverse events occurred in the lopinavir-ritonavir group than in the NNRTI group (5.6%

132 for malaria was significantly higher in the lopinavir-ritonavir group than in the NNRTI group.

133 group), lopinavir-ritonavir plus two NRTIs (lopinavir-ritonavir group), and lopinavir-ritonavir plus

134 mparison between the efavirenz group and the lopinavir-ritonavir group).

135 r was 89% in the efavirenz group, 77% in the lopinavir-ritonavir group, and 83% in the NRTI-sparing g

136 ccurred significantly more frequently in the lopinavir-ritonavir group, and elevated alanine aminotra

137 In the lopinavir-ritonavir group, lumefantrine levels exceeding

138 y in the raltegravir group compared with the lopinavir-ritonavir group.

139 ss likely in the efavirenz group than in the lopinavir-ritonavir group.

140 ht into the genetic barrier to resistance to lopinavir-ritonavir in both antiretroviral therapy-naive

141 for lopinavir-ritonavir with continuation of lopinavir-ritonavir in HIV-infected patients with stable

142 to initial response while on treatment with lopinavir-ritonavir in Phase II and III studies.

143 Lopinavir-ritonavir is a preferred protease inhibitor co

144 s two NRTIs (lopinavir-ritonavir group), and lopinavir-ritonavir plus efavirenz (NRTI-sparing group).

145 The alternative regimen of lopinavir-ritonavir plus efavirenz may prevent toxic eff

146 efavirenz plus two NRTIs (efavirenz group), lopinavir-ritonavir plus two NRTIs (lopinavir-ritonavir

147 The use of either efavirenz or lopinavir-ritonavir plus two nucleoside reverse-transcri

148 rse-transcriptase inhibitor [NRTI] group) or lopinavir-ritonavir plus zidovudine-lamivudine (the prot

149 ence of resistance observed after initiating lopinavir-ritonavir therapy in antiretroviral-naive pati

150 esponse system in a 1:1 ratio to switch from lopinavir-ritonavir to raltegravir (400 mg twice daily;

151 vir has shown similar efficacy and safety to lopinavir-ritonavir when each is combined with two nucle

152 We compared substitution of raltegravir for lopinavir-ritonavir with continuation of lopinavir-riton

153 eive a ritonavir-boosted protease inhibitor (lopinavir-ritonavir) plus clinician-selected NRTIs (NRTI

154 Surprisingly, after exposure to lopinavir-ritonavir, absolute forearm blood-flow respons

155 tolerability, and emergence of resistance as lopinavir-ritonavir, each in combination with abacavir-l

156 ipid concentrations than was continuation of lopinavir-ritonavir, efficacy results did not establish

157 for the combined trials (raltegravir, n=350; lopinavir-ritonavir, n=352).

158 ated with antiretroviral regimens containing lopinavir-ritonavir, patients might want to switch one o

159 dren would be lower among children receiving lopinavir-ritonavir-based antiretroviral therapy (ART) t

160 Lopinavir-ritonavir-based ART as compared with NNRTI-bas

161 I-based ART were randomly assigned to either lopinavir-ritonavir-based ART or NNRTI-based ART and wer

162 Lopinavir-ritonavir-based ART was accompanied by an incr

163 regimen: 86 received NNRTI-based ART, and 84 lopinavir-ritonavir-based ART.

164 fants from the IMPAACT P1030 trial receiving lopinavir-ritonavir-based cART.

165 ed patients with stable viral suppression on lopinavir-ritonavir-based combination therapy.

166 laria was lower among children receiving the lopinavir-ritonavir-based regimen than among those recei

167 ntification for at least 3 months while on a lopinavir-ritonavir-based regimen.

168 establish non-inferiority of raltegravir to lopinavir-ritonavir.

169 susceptibility to fosamprenavir-ritonavir or lopinavir-ritonavir.

170 per genotypic and phenotypic breakpoints for lopinavir-ritonavir.

171 promise the genetic barrier to resistance to lopinavir-ritonavir.

172 runavir/ritonavir (800/100 mg once daily) or lopinavir/ritonavir (400/100 mg twice daily) monotherapy

173 ART included lopinavir/ritonavir (400/100 mg) twice daily and emtrici

174 azanavir (300 mg) plus ritonavir (100 mg) or lopinavir/ritonavir (800/200 mg) with the 3D regimen is

175 trials evaluating the safety and efficacy of lopinavir/ritonavir (LPV/r) capsules administered twice

176 antimalarial components by 2.1- to 3.4-fold; lopinavir/ritonavir (LPV/r) increased lumefantrine expos

177 l Group (ACTG) A5230 study entry, a study of lopinavir/ritonavir (LPV/r) monotherapy after first-line

178 al Trials Group (ACTG) A5230 study evaluated lopinavir/ritonavir (LPV/r) monotherapy following virolo

179 This multicenter trial evaluated whether lopinavir/ritonavir (LPV/r) monotherapy in HIV type 1-in

180 children <6 years of age were randomized to lopinavir/ritonavir (LPV/r) or nonnucleoside reverse tra

181 study demonstrated short-term superiority of lopinavir/ritonavir (LPV/r) over nevirapine (NVP) in ant

182 Three randomized trials compared lopinavir/ritonavir (LPV/r) to nevirapine (NVP) for anti

183 to compare the efficacy of NVP-based versus lopinavir/ritonavir (LPV/r)-based initial ART.

184 reverse transcriptase inhibitor (NNRTI)- or lopinavir/ritonavir (LPV/r)-based regimen were enrolled.

185 er, open-label, phase 1/2 treatment trial of lopinavir/ritonavir (Pediatric AIDS Clinical Trials Grou

186 ction of HIV protease inhibitors (ritonavir, lopinavir/ritonavir 4:1, atazanavir, atazanavir/ritonavi

187 10]; P<.001) and nelfinavir use (OR, 2.4 vs. lopinavir/ritonavir [95% CI, 1.6-3.6]; P<.001).

188 TDF-based regimens (TDF+emtricitabine [FTC]+lopinavir/ritonavir [LPV/r], 71.1%; 95% CI, 43.6%-98.6%;

189 at 5 y when starting unboosted atazanavir or lopinavir/ritonavir among those with a low risk score wa

190 atients randomized 1:1 to receive open-label lopinavir/ritonavir at a dose of 800/200 mg once daily o

191 ther triple ARV (zidovudine, lamivudine, and lopinavir/ritonavir during pregnancy and breastfeeding)

192 dine/zidovudine, emtricitabine/tenofovir, or lopinavir/ritonavir for 7 or 21 days.

193 ine (3TC), tenofovir/emtricitabine (FTC), or lopinavir/ritonavir for either 7 or 21 days.

194 We found that lopinavir/ritonavir had a dose-dependent effect on liver

195 ata suggest that the HIV protease inhibitors lopinavir/ritonavir may have potent antimalarial activit

196 tiretroviral therapy-naive patients received lopinavir/ritonavir or nelfinavir, plus stavudine and la

197 wever, evening atazanavir plus ritonavir and lopinavir/ritonavir regimens are not recommended in comb

198 as similar between groups, infants receiving lopinavir/ritonavir suppressed EBV more rapidly.

199 n compared with those who were switched from lopinavir/ritonavir to atazanavir/ritonavir.

200 ouble-blind, randomized, controlled study of lopinavir/ritonavir versus nelfinavir, each administered

201 mass index and random assignment to receive lopinavir/ritonavir were associated with more rapid nevi

202 renavir, indinavir, indinavir/ritonavir, and lopinavir/ritonavir were associated with suboptimal adhe

203 ind, randomized, phase 3 study that compared lopinavir/ritonavir with nelfinavir, each coadministered

204 77); saquinavir/ritonavir, 1.12 (0.48-2.61); lopinavir/ritonavir, 1.23 (0.58-2.59); nevirapine, 1.53

205 nce of genotypic or phenotypic resistance to lopinavir/ritonavir, defined as any active site or prima

206 the administration of a novel combination of lopinavir/ritonavir, efavirenz, tenofovir disoproxil fum

207 riptase inhibitor-sparing regimen of NRTIs + lopinavir/ritonavir, or a NRTI-sparing regimen of efavir

208 3 different antiretroviral drugs (efavirenz, lopinavir/ritonavir, or atazanavir/ritonavir).

209 tenofovir, atazanavir, atazanavir/ritonavir, lopinavir/ritonavir, other boosted protease inhibitors b

210 All patients were on therapy (lopinavir/ritonavir, stavudine, and lamivudine) with pla

211 by thick smear or PCR findings, between the lopinavir/ritonavir-based and efavirenz-based ART arms (

212 nfected infants starting nevirapine-based vs lopinavir/ritonavir-based antiretroviral regimens.

213 We sought to evaluate whether lopinavir/ritonavir-based antiretroviral therapy (ART) r

214 Lopinavir/ritonavir-based ART did not reduce the risk of

215 s 12 and 28 and randomly assigned to receive lopinavir/ritonavir-based or efavirenz-based ART.

216 deficiency virus-infected patients receiving lopinavir/ritonavir-based regimens with hypercholesterol

217 women in the NVP arm vs. 3 (9%) of 32 in the lopinavir/ritonavir-containing arm (hazard ratio = 3.84)

218 the NVP-containing treatment arm than in the lopinavir/ritonavir-containing treatment arm.

219 her for nelfinavir-treated patients than for lopinavir/ritonavir-treated patients (Cox model hazard r

220 For nelfinavir-treated patients, but not for lopinavir/ritonavir-treated patients, higher baseline HI

221 igher in nelfinavir-treated patients than in lopinavir/ritonavir-treated patients.

222 ease, was detected in virus isolates from 51 lopinavir/ritonavir-treated subjects with available geno

223 ficantly higher in nelfinavir-treated versus lopinavir/ritonavir-treated subjects.

224 ir, or a NRTI-sparing regimen of efavirenz + lopinavir/ritonavir.

225 elfinavir and of 15% at 80%-85% adherence to lopinavir/ritonavir.

226 ed, 56% received darunavir/ritonavir and 44% lopinavir/ritonavir.

227 were zidovudine/lamivudine and nelfinavir or lopinavir/ritonavir.

228 domized between 26 and 34 weeks gestation to lopinavir/ritonavir/zidovudine/lamivudine (PI group) or

229 tudies indicated that HIV PIs (ritonavir and lopinavir) significantly increased hepatic lipid accumul

230 vir-boosted atazanavir, or ritonavir-boosted lopinavir therapy.

231 protease-inhibitor-based (ritonavir-boosted lopinavir) treatment in children who had achieved suppre

232 predictors of CKD whereas ritonavir-boosted lopinavir use was a significant predictor for both end p

233 ir-boosted atazanavir, and ritonavir-boosted lopinavir use were independent predictors of chronic ren

234 The selection of in vivo resistance to lopinavir was characterized by analyzing the longitudina

235 tion in susceptibility to PIs atazanavir and lopinavir was observed across 20 viruses, with EC50s ran

236 Predose concentrations of lopinavir were more variable in the once-daily group (me

237 inhibitor (standardised to ritonavir-boosted lopinavir) with two to three NRTIs (clinician-selected,

238 ith eight HAART drugs [ritonavir, indinavir, lopinavir, zidovudine (AZT), abacavir, stavudine, didano