ライフサイエンスコーパス: mefloquine

1 er malaria treatments currently approved for mefloquine.

2 few alternatives, which include quinine and mefloquine.

3 overall predictor of treatment failure with mefloquine.

4 to the known antimalarials, chloroquine and mefloquine.

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

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

7 ermeability across MDCK cell monolayers than mefloquine.

8 egarding the absolute stereochemistry of the mefloquines.

9 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

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

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

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

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

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

15 Mefloquine, a close derivative of quinine and quinidine

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

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

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

19 Mefloquine also blocked channels formed by the lens gap

20 Mefloquine also down-regulated several important functio

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

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

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

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

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

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

27 Mefloquine and doxycycline are the two drugs recommended

28 Mefloquine and doxycycline were both highly efficacious

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

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

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

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

33 Mefloquine, another important antimalarial quinoline, as

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

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

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

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

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

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

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

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

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

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

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

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

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

47 Mefloquine, at 25 microM, blocked gap junctional couplin

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

49 Mutagenesis of mefloquine-binding residues generates parasites with inc

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

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

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

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

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

55 Mefloquine could be successfully differentiated from oth

56 Mefloquine-currently evaluated as a potential alternativ

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

72 426 days per 1000 patients in the artesunate-mefloquine group versus 2828 days per 1000 patients in t

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

93 ng the popular trioxane drug artemether plus mefloquine hydrochloride.

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

95 (4 h), artemisinin derivatives, quinine and mefloquine impacted H2O2 levels in mitochondria, whereas

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

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

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

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

100 ) 6 weeks after the second administration of mefloquine IPTp.

101 ial comparing sulfadoxine-pyrimethamine with mefloquine IPTp.

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

103 Mefloquine is a widely used antimalarial without a known

104 Mefloquine is associated with adverse neurological effec

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

106 Artesunate-mefloquine is highly efficacious for treatment of uncomp

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

108 Mefloquine is the drug of choice for chemoprophylaxis fo

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

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

111 Mefloquine is well tolerated at prophylactic dosages, bu

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

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

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

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

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

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

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

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

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

121 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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

140 Two patients receiving mefloquine plus artesunate had seizures.

141 0.4 to 85.6) and that in the group receiving mefloquine plus artesunate was 83.9% (355 of 423 patient

142 8.3 to 99.7) and that in the group receiving mefloquine plus artesunate was 97.8% (360 of 368 patient

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

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

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

146 12 corresponding to local discontinuation of mefloquine regimens.

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

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

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

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

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

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

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

154 inoline methanols were designed based on the mefloquine scaffold.

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

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

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

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

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

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

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

162 (3-21G level) calculations were performed on mefloquine, the lead compound in this series, to check t

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

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

165 The mefloquine transcriptome was found to be enriched for im

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

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

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

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

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

171 In 1984 mefloquine was introduced as treatment for uncomplicated

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

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

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

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

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

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