ライフサイエンスコーパス: mefloquine

1 ermeability across MDCK cell monolayers than mefloquine.

2 er malaria treatments currently approved for mefloquine.

3 iperaquine and 5.2% (2.9-7.9) for artesunate-mefloquine.

4 few alternatives, which include quinine and mefloquine.

5 overall predictor of treatment failure with mefloquine.

6 be responsive to chloroquine or artemisinin-mefloquine.

7 cluding the drugs Captopril, Normorphine and Mefloquine.

8 to the known antimalarials, chloroquine and mefloquine.

9 reochemistry of (+)-anti- as well as (-)-syn-mefloquine.

10 or twice-daily dose for 3 days, followed by mefloquine.

11 egarding the absolute stereochemistry of the mefloquines.

12 group was 1.55 (95% CI 1.42-1.67) and in the mefloquine (10 mg/kg) group was 2.34 (2.17-2.52), corres

13 a (IBSM) and treated with DSM265 (150 mg) or mefloquine (10 mg/kg).

14 mg) plus dapsone (18.75 mg; n=317 and 285), mefloquine (125 mg; n=320 and 284), or placebo (n=320 an

15 Mefloquine (25 microM) caused no significant change in e

16 [17%]), dihydroartemisinin-piperaquine plus mefloquine (269 [24%]), artesunate-mefloquine (73 [7%]),

17 nt after dihydroartemisinin-piperaquine plus mefloquine (30 [3.8%] of 794) than after dihydroartemisi

18 e treated with oral regimen only (95 AL, 162 mefloquine, 36 atovaquone-proguanil [AP], and 17 others)

19 junction uncouplers quinine (250 microM) and mefloquine (500 nM) both disrupted 4-12 Hz oscillations

20 uine plus mefloquine (269 [24%]), artesunate-mefloquine (73 [7%]), artemether-lumefantrine (289 [26%]

21 7.0-32.0]), lumefantrine (5.1 nM [3.2-7.7]), mefloquine (9.5 nM [6.6-13.0]), dihydroartemisinin (1.5

22 99]) was non-inferior to that of artesunate-mefloquine (95% [69 of 73; 95% CI 87 to 99]) in three si

23 icacy of dihydroartemisinin-piperaquine plus mefloquine (96% [68 of 71; 95% CI 88 to 99]) was non-inf

24 Mefloquine, a close derivative of quinine and quinidine

25 During US military operations in Somalia, mefloquine, a drug for malaria chemoprophylaxis, was not

26 Triple therapy (cobimetinib + mefloquine + aCD40) achieved cytotoxic T-cell activation

27 with protease inhibitor was antagonistic to mefloquine action, as it is to chloroquine action.

28 Q, and seven compounds were more active than mefloquine against CQR strain W2.

29 Mefloquine also blocked channels formed by the lens gap

30 Mefloquine also down-regulated several important functio

31 A, 6 studies), 7,340 (47.8%) with artesunate-mefloquine (AM, 25 studies), and 4,639 (30.2%) with dihy

32 We show that mefloquine, an antimalarial drug, is one such agent.

33 apy with the highly effective combination of mefloquine and 3 days' artesunate.

34 Dihydroartemisinin-piperaquine plus mefloquine and artemether-lumefantrine plus amodiaquine

35 sitivity to the structurally unrelated drugs mefloquine and artemisinin, and to several other antimal

36 nine and sensitivity to the new alternatives mefloquine and artemisinin.

37 ed to the use of newer antimalarials such as mefloquine and artemisinin.

38 data reveal one possible mode of action for mefloquine and demonstrate the vast potential of cryo-el

39 Mefloquine and doxycycline are the two drugs recommended

40 Mefloquine and doxycycline were both highly efficacious

41 ses in signal at very high concentrations of mefloquine and related compounds were more marked with t

42 pharmacological inhibition of autophagy with mefloquine and verteporfin re-establishes cholangiocyte

43 hrenia (risperidone, belaperidone), malaria (mefloquine) and nicotine addiction (cytisine, vareniclin

44 minant of in-vitro and in-vivo resistance to mefloquine, and also to reduced artesunate sensitivity i

45 <10% with the nonartemisinin drugs quinine, mefloquine, and atovaquone-proguanil.

46 for chloroquine, decreased for lumefantrine, mefloquine, and DHA, and were unchanged for other drugs.

47 ne, piperaquine, pyronaridine, lumefantrine, mefloquine, and DHA, but higher for quinine and pyrimeth

48 bility to the partner drugs lumefantrine and mefloquine, and the active artemisinin metabolite dihydr

49 quine or dihydroartemisinin-piperaquine plus mefloquine; and in Laos, Myanmar, Bangladesh, India, and

50 Mefloquine, another important antimalarial quinoline, as

51 octanol, carbenoxolone, flufenamic acid, and mefloquine) are antagonists of the P2X7R indicate the in

52 , dihydroartemisinin-piperaquine (86.9%), or mefloquine-artesunate (73.8%).

53 Deployment of mefloquine-artesunate (MAS3) on the Thailand-Myanmar bor

54 tment (IPT) with a fixed-dose combination of mefloquine-artesunate (MQAS) or sulfadoxine-pyrimethamin

55 ccurred significantly more frequently in the mefloquine-artesunate group (50.6%) and the amodiaquine-

56 ihydroartemisinin-piperaquine group, and the mefloquine-artesunate group.

57 emisinin-piperaquine group, and 96.8% in the mefloquine-artesunate group; the PCR-adjusted cure rates

58 mether-lumefantrine, amodiaquine-artesunate, mefloquine-artesunate, or dihydroartemisinin-piperaquine

59 drugs and identified the antimalarial agent mefloquine as a compound that selectively kills AML cell

60 We also identify mefloquine as a positive modulator of PANX1 that binds n

61 ng the antimalarial fluorine-containing drug mefloquine as an example.

62 The emergence of artesunate-mefloquine (AS+MQ)-resistant Plasmodium falciparum in th

63 omized, controlled trial of CQ vs artesunate-mefloquine (AS-MQ) for uncomplicated vivax malaria was c

64 hydroartemisinin-piperaquine with or without mefloquine, as part of the TRACII trial.

65 e artemether-lumefantrine (AL) or artesunate-mefloquine (ASMQ) were screened for total immunoglobulin

66 g/kg artesunate at 0, 24, and 48 h, 15 mg/kg mefloquine at 72 h, and 10 mg/kg mefloquine at 96 h.

67 h, 15 mg/kg mefloquine at 72 h, and 10 mg/kg mefloquine at 96 h.

68 Mefloquine, at 25 microM, blocked gap junctional couplin

69 quine or dihydroartemisinin-piperaquine plus mefloquine; at three sites in Cambodia they were assigne

70 Some female soldiers inadvertently used mefloquine before becoming aware of their pregnancy.

71 Mutagenesis of mefloquine-binding residues generates parasites with inc

72 MEK (using cobimetinib) and autophagy (using mefloquine), but not either treatment alone, activates t

73 with a longacting, efficacious drug such as mefloquine can reduce episodes of malaria in infants in

74 Mefloquine caused vomiting in 141 of 1731 (8%) doses giv

75 squitoes to volunteers taking chloroquine or mefloquine (chemoprophylaxis with sporozoites).

76 he effect of blood-stage drugs (doxycycline, mefloquine, chloroquine, chloroquine-proguanil) or atova

77 ested known nonhemolytic antimalarial drugs: mefloquine, chloroquine, doxycycline, and pyrimethamine.

78 widespread reports on the adverse effects of mefloquine, controlled studies found that serious neurop

79 Mefloquine could be successfully differentiated from oth

80 Mefloquine-currently evaluated as a potential alternativ

81 These are the first X-ray structures for mefloquine derivatives that were obtained by coupling to

82 ctron microscopy to guide the development of mefloquine derivatives to inhibit parasite protein synth

83 Consistent with this, we determined that mefloquine disrupts lysosomes, directly permeabilizes th

84 Recent in vitro studies have shown that mefloquine disrupts neuronal calcium homeostasis via lib

85 Moreover, mefloquine does not appear to impair performance while d

86 provides additional postmarketing data that mefloquine does not cause gross congenital malformations

87 smodium falciparum 80S ribosome with the (+)-mefloquine enantiomer bound to the ribosome GTPase-assoc

88 A total of 2506 cases of mefloquine exposure during pregnancy or in the pre- and

89 The drug safety database analysis of mefloquine exposure in pregnancy showed that the birth d

90 days was lower in patients in the artesunate-mefloquine group (71 [62%; 95% CI 52.2-70.6]) than in th

91 Fever clearance was faster in the artesunate-mefloquine group (mean 11.5 h [95% CI 8.3-14.6]) than in

92 r clearance of ring stages in the artesunate-mefloquine group (mean time to 50% clearance of baseline

93 in 44 (86%) of 51 patients in the artesunate-mefloquine group and 41 (84%) of 49 patients in the chlo

94 (interquartile range [IQR], 70%-100%) in the mefloquine group compared to an increase of 20% (IQR, -1

95 One (<1%) patient in the artesunate-mefloquine group had a serious neuropsychiatric event re

96 426 days per 1000 patients in the artesunate-mefloquine group versus 2828 days per 1000 patients in t

97 CI 76-91]) of 115 patients in the artesunate-mefloquine group versus 61 (55% [45-64]) of 111 patients

98 n the 68 soldiers (16.9 person-years) in the mefloquine group; thus, the protective efficacy of meflo

99 fants died in the chlorproguanil-dapsone and mefloquine groups (18 and 15, respectively) than in the

100 At the moderate-transmission site, mefloquine had a protective efficacy of 38.1% (95% CI 11

101 n wild-type and in knockout animals, whereas mefloquine had no effects.

102 of hemichannels-carbenoxolone, lanthanum and mefloquine-had no significant effect on the current gene

103 found to enhance parasite susceptibility to mefloquine, halofantrine and artemisinin.

104 First, structural models of erythro-mefloquine HCl compatible with NMR-derived (3)J(HH) scal

105 h the important antimalaria drug rac-erythro-mefloquine HCl has been on the market as Lariam for deca

106 hat the assignment of 11R,12S to (-)-erythro-mefloquine HCl is correct.

107 The experimental results for (-)-erythro-mefloquine HCl matched our calculated chiroptical data f

108 ol the popular trioxane drug artemether plus mefloquine hydrochloride (average survival time of only

109 :1) total synthesis of (+)-anti- and (-)-syn-mefloquine hydrochloride from a common intermediate is d

110 r.) total synthesis of (+)-anti- and (-)-syn-mefloquine hydrochloride from a common intermediate is d

111 asymmetric (er > 99:1) synthesis of (+)-anti-mefloquine hydrochloride is also presented that uses a S

112 hemotherapy using monomeric trioxane 4b plus mefloquine hydrochloride is considerably better than the

113 omeric trioxane 4b combined with 20 mg/kg of mefloquine hydrochloride, all of the malaria-infected mi

114 y as one 6 mg/kg dose combined with 18 mg/kg mefloquine hydrochloride, only sulfide 3-arteSanilide 12

115 meric trioxane 12c combined with 18 mg/kg of mefloquine hydrochloride, Plasmodium berghei-infected mi

116 e of only 54 mg/kg combined with 13 mg/kg of mefloquine hydrochloride, this trioxane dimer 4c as well

117 ng the popular trioxane drug artemether plus mefloquine hydrochloride.

118 itory concentration (IC50) values, and lower mefloquine IC50 values; none had multiple pfmdr1 copies,

119 (4 h), artemisinin derivatives, quinine and mefloquine impacted H2O2 levels in mitochondria, whereas

120 in pfmdr1 is the main cause of resistance to mefloquine in falciparum malaria.

121 icacy of dihydroartemisinin-piperaquine plus mefloquine in the three sites in Myanmar was 91% (42 of

122 livary injection of the gap junction blocker mefloquine, indicating that excitation to the olive is c

123 expression induced in neurons in response to mefloquine-induced disruption of calcium homeostasis and

124 In this study we evaluated the efficacy of mefloquine IPTp against S. haematobium infection in preg

125 ) 6 weeks after the second administration of mefloquine IPTp.

126 ial comparing sulfadoxine-pyrimethamine with mefloquine IPTp.

127 Here, we demonstrate that mefloquine is a protein synthesis inhibitor.

128 Mefloquine is a widely used antimalarial without a known

129 Mefloquine is associated with adverse neurological effec

130 Thus, mefloquine is expected to be a useful tool to study the

131 Artesunate-mefloquine is highly efficacious for treatment of uncomp

132 nce to current drugs such as chloroquine and mefloquine is spreading at an alarming rate, and our ant

133 Mefloquine is the drug of choice for chemoprophylaxis fo

134 ysis of derivatives of (+)-anti- and (-)-syn-mefloquine is used to lay to rest a 40 year argument reg

135 modium falciparum and Plasmodium vivax where mefloquine is used to treat P. falciparum infection, dru

136 Mefloquine is well tolerated at prophylactic dosages, bu

137 ii UBP1 can mediate high-level resistance to mefloquine, lumefantrine, and piperaquine.

138 Of the total 2246 mefloquine maternal prospective exposures (95.2%), 2139

139 In Cambodia, artesunate plus mefloquine may be a viable option to treat dihydroartemi

140 r studies confirm these findings, the use of mefloquine may transform future IPTp programs into a 2-p

141 Mefloquine (MF), a quinoline antimalaria drug, was the m

142 Here, we show that mefloquine (MFQ) inhibits several mutant hemichannel for

143 rmacologic inhibition of Panx1 channels with mefloquine (MFQ) reduced severity of acute and chronic E

144 Mefloquine (MFQ), moxifloxacin (MXF), and ethambutol (EM

145 and hygromycin B) and the antimalarial drug mefloquine (MFQ), which has also been identified as a re

146 combination therapies for malaria, including mefloquine (MFQ)-artesunate and lumefantrine (LUM)-artem

147 either 18beta-glycyrrhetinic derivatives or mefloquine), modafinil restored electrotonic coupling wi

148 lure of 6.3 (95% CI 2.9-13.8, p<0.001) after mefloquine monotherapy and 5.4 (2.0-14.6, p=0.001) after

149 vitro drug resistance and in vivo failure of mefloquine monotherapy.

150 Mozambique to establish the efficacy of IPTp-mefloquine (MQ) compared with IPTp-sulphadoxine-pyrimeth

151 Mefloquine (MQ) has been used as an effective malaria pr

152 We studied the safety and efficacy of mefloquine (MQ) in women receiving CTXp and long-lasting

153 ed 252 patients to receive either artesunate-mefloquine (n=127) or chloroquine (n=125); 226 (90%) pat

154 d Nov 25, 2013 (150 mg DSM265, n=7; 10 mg/kg mefloquine, n=2).

155 urther tested in vivo, and it was found that mefloquine, nelfinavir, and extracts of Ganoderma lucidu

156 rch terms malaria, chemoprophylaxis, travel, mefloquine, neuropsychiatric adverse events, tolerabilit

157 A combination of artesunate with mefloquine now cures more than 95% of acute infections.

158 The effect of exposure to mefloquine on pregnancy and offspring outcomes was evalu

159 en connexin hemichannels were inhibited with mefloquine or 2-octanol.

160 odia they were assigned to either artesunate-mefloquine or dihydroartemisinin-piperaquine plus mefloq

161 ined by the resolution of either the initial mefloquine or one of the final products.

162 yed in patients treated with ACTs containing mefloquine or piperaquine compared with artemether-lumef

163 inically used broad-spectrum Panx1 blockers, mefloquine or probenecid, suppressed ATP release and red

164 hich case atovaquone-proguanil is best, with mefloquine or quinine plus tetracycline or doxycycline a

165 target dose 12 mg/kg artesunate and 25 mg/kg mefloquine) or chloroquine (target dose 25 mg/kg).

166 7.8] for dihydroartemisinin-piperaquine plus mefloquine; p=0.50).

167 Mefloquine (Panx1 blocker) reduced these IL-1beta respon

168 ne per day and mefloquine placebo; 250 mg of mefloquine per week (preceded by a loading dose of 250 m

169 ed whether introduction of either artesunate-mefloquine-piperaquine or artemether-lumefantrine-amodia

170 to receive 100 mg of doxycycline per day and mefloquine placebo; 250 mg of mefloquine per week (prece

171 ne and 60 mg of artesunate or with 250 mg of mefloquine plus 100 mg of artesunate.

172 igher with pyronaridine-artesunate than with mefloquine plus artesunate (10.2% [95% CI, 5.4 to 18.6]

173 Pyronaridine-artesunate was noninferior to mefloquine plus artesunate for the primary outcome: adeq

174 Two patients receiving mefloquine plus artesunate had seizures.

175 0.4 to 85.6) and that in the group receiving mefloquine plus artesunate was 83.9% (355 of 423 patient

176 8.3 to 99.7) and that in the group receiving mefloquine plus artesunate was 97.8% (360 of 368 patient

177 d significantly by multiple Panx inhibitors (mefloquine, probenecid, and (10)Panx1), ectonucleotidase

178 tibility to the clinical drugs lumefantrine, mefloquine, quinine and amodiaquine.

179 xperimentally derived IC50 concentrations of mefloquine, quinine and pyrimethamine.

180 12 corresponding to local discontinuation of mefloquine regimens.

181 evels remained high, no evidence of emerging mefloquine resistance was found.

182 e possible role of pfmdr1 in amodiaquine and mefloquine resistance, demonstrating selection on pfmdr1

183 multiple pfmdr1 copies, a genetic marker of mefloquine resistance.

184 ng activity in chloroquine-resistant than in mefloquine-resistant cell lines and were generally more

185 ug resistance 1 gene (pvmdr1) may select for mefloquine-resistant P. vivax Surveillance is not undert

186 sequently converted to (+)-anti- and (-)-syn-mefloquine, respectively.

187 quently converted into (+)-anti- and (-)-syn-mefloquine, respectively.

188 The synthetic (+)-anti- and (-)-syn-mefloquine samples were derivatized with (S)-(+)-mandeli

189 Novel 1,2-diamines based on the mefloquine scaffold prepared in enantiomerically pure fo

190 inoline methanols were designed based on the mefloquine scaffold.

191 ng a yeast genome-wide functional screen for mefloquine sensitizers, we identified genes associated w

192 used as IPTp for the prevention of malaria, mefloquine shows promising activity against concomitant

193 sms in pfmdr1 were associated with increased mefloquine susceptibility in vitro, but not in vivo.

194 ock sizes of 20), to receive oral artesunate-mefloquine (target dose 12 mg/kg artesunate and 25 mg/kg

195 ficantly faster in participants who received mefloquine than in participants who received DSM265 (p<0

196 ance was faster in patients given artesunate-mefloquine than in those given chloroquine (18.0 h [rang

197 nt in surveillance studies of drugs, such as mefloquine, that still retain efficacy in sub-Saharan Af

198 (3-21G level) calculations were performed on mefloquine, the lead compound in this series, to check t

199 PfMDR1, suggesting sustained sensitivity to mefloquine, the partner drug in the local first-line art

200 and 5.4 (2.0-14.6, p=0.001) after artesunate-mefloquine therapy.

201 D 18.6] vs 0.9 ms [16.1]; p<0.01) but adding mefloquine to dihydroartemisinin-piperaquine did not (me

202 The mefloquine transcriptome was found to be enriched for im

203 ls specifically increased 2.5-fold at 6 h in mefloquine-treated parasites and threefold in parasites

204 C2A failed to clear upon oral artesunate and mefloquine treatment alone or in combination, and ex viv

205 We show that mefloquine treatment of falciparum malaria eliminates ea

206 thapsigargin, hydrogen peroxide, or low-dose mefloquine treatment.

207 f the antimalarial compounds piperaquine and mefloquine-two slow-clearing partner drugs in current fi

208 apid selection for resistance, implying that mefloquine use in Africa should be considered only as pa

209 uine group; thus, the protective efficacy of mefloquine was 100% (CI, 96% to 100%).

210 cy after dihydroartemisinin-piperaquine plus mefloquine was 98% (149 of 152; 95% CI 94 to 100) and af

211 In 1984 mefloquine was introduced as treatment for uncomplicated

212 1) and the in-vitro and in-vivo responses to mefloquine were assessed in 618 samples from patients wi

213 important antimalaria drugs chloroquine and mefloquine were strongly enhanced utilizing deep UV and

214 ACTs, artemether-lumefantrine and artesunate-mefloquine) where the likelihood of increased artemisini

215 The antimalarial drug mefloquine, which selectively blocks Cx50 and not Cx46 G

216 We aimed to compare artesunate-mefloquine with chloroquine to define the optimum treatm

217 rs were identified that bind piperaquine and mefloquine with dissociation constants (K (d)'s) measure

218 We reviewed studies on tolerability of mefloquine with particular focus on its neuropsychiatric