ライフサイエンスコーパス: aprepitant

1 the synthesis of the potent antiemetic drug Aprepitant.

2 s, including potential additional trials for aprepitant.

3 P = .0036) within 120 hours was increased by aprepitant.

4 273 received dexamethasone, and 278 received aprepitant.

5 CYP3A4 inhibition and induction compared to aprepitant.

6 nausea, but it was numerically superior with aprepitant.

7 A streamlined and high-yielding synthesis of aprepitant (1), a potent substance P (SP) receptor antag

8 setron 0.25 mg, dexamethasone 8 mg, and oral aprepitant 125 mg.

9 ge-based and weight-based blinded regimen of aprepitant (125 mg for ages 12-17 years; 3.0 mg/kg up to

10 gned at a one-to-one ratio to receive either aprepitant (125 mg orally on day 1 and 80 mg orally on d

11 were randomly assigned to groups given oral aprepitant (125 mg/day, n = 63) or placebo (n = 63).

12 s of 20 and 40 mg/kg b.w. On the other hand, aprepitant (16 mg/kg), domperidone (6 mg/kg), diphenhydr

13 itis was seen with fosaprepitant relative to aprepitant (2.7% v 0.3%, respectively).

14 erate in severity grade, were more common in aprepitant (22 of 63 patients, 35% vs 11 of 63, 17% in t

15 ved oral dexamethasone 4 mg twice per day or aprepitant 80 mg once per day.

16 ears) plus ondansetron on day 1, followed by aprepitant (80 mg for ages 12-17 years; 2.0 mg/kg up to

17 ib (cyclo-oxygenase inhibitors), pyrilamine, aprepitant (a neurokinin 1 receptor antagonist), or indo

18 Aprepitant, a 5-HT3 receptor antagonist (5HT3-RA), and d

19 A combination of aprepitant, a 5-HT3 receptor antagonist, and dexamethaso

20 -IR for quantitation of polymorphic forms of Aprepitant, a calibration plot was constructed with know

21 Addition of aprepitant, a neurokinin-1 receptor antagonist (NK1RA),

22 Oral aprepitant, a neurokinin-1 receptor antagonist, is recom

23 cation and quantitation of two polymorphs of Aprepitant, a substance P antagonist for chemotherapy-in

24 neuro-cancer axis with the TACR1 antagonist aprepitant, an approved anti-nausea drug, suppressed bre

25 nM, which is about 10-fold more potent than aprepitant, an NK(1) antagonist marketed for the prevent

26 (+/- standard deviation) was 114 +/- 18 for aprepitant and 106 +/- 26 for placebo (P < .001).

27 e patients were randomly assigned to receive aprepitant and 34 to receive placebo for the first cours

28 plus ondansetron and dexamethasone on day 1; aprepitant and dexamethasone on days 2 to 3; dexamethaso

29 Antiemetic protection with aprepitant and fosaprepitant was equivalent within prede

30 ed after preincubation with NK1R antagonists aprepitant and L-73060.

31 two small-molecule antagonist therapeutics - aprepitant and netupitant and the progenitor antagonist

32 ne in adults and intravenous formulations of aprepitant and netupitant-palonosetron.

33 particularly favorable are the novel NK1-RA aprepitant and the next generation 5HT3-RA palonosetron.

34 to characterize a fluorinated drug molecule, aprepitant, and its commercial nanoparticulate formulati

35 tients were randomized 1:1 to dexamethasone, aprepitant, and palonosetron with olanzapine (experiment

36 antiemetics such as transdermal scopolamine, aprepitant, and/or palonosetron.

37 Preliminary data suggested that single-dose aprepitant before chemotherapy could provide CINV protec

38 ed with the neurokinin 1 receptor antagonist aprepitant before SP stimulation.

39 te emesis, dexamethasone was not superior to aprepitant but instead had similar efficacy and toxicity

40 as a significant improvement in CR rate with aprepitant combined with a 5HT3-RA and dexamethasone.

41 Forty-two percent achieved CR with aprepitant compared with 13% with placebo (P < .001).

42 There was no toxicity with aprepitant compared with placebo.

43 ) had at least one emetic episode during the aprepitant cycle versus 32 patients (47.1%) with placebo

44 Thirty-eight patients preferred the aprepitant cycle whereas 11 preferred placebo (P < .001)

45 Patient preference strongly favored the aprepitant cycle.

46 + palonosetron + dexamethasone on day 1 with aprepitant + dexamethasone on days 2 and 3; and group 4:

47 Aprepitant did not reduce symptoms of nausea, based on t

48 astroparesis or gastroparesis-like syndrome, aprepitant did not reduce the severity of nausea when re

49 , a single-day intravenous formulation, with aprepitant; either therapy is appropriate.

50 The NK-1R antagonist aprepitant (Emend, Merck) inhibited both the SP-induced

51 ted macaques with the SP receptor antagonist aprepitant (Emend; Merck, Whitehouse Station, NJ) comple

52 The beneficial effect of adding aprepitant for control of DN was the same as adding proc

53 ed at 49 sites in 24 countries to either the aprepitant group (155 patients) or to the control group

54 days 1 to 5 was significantly higher in the aprepitant group (72.7% [n = 260] v 52.3% in the standar

55 77 (51%) of 152 patients in the aprepitant group and 39 (26%) of 150 in the control grou

56 Three patients in the aprepitant group and two in the control group did not re

57 However, patients in the aprepitant group had significant changes in secondary ou

58 febrile neutropenia (23 [15%] of 152 in the aprepitant group vs 21 [14%] of 150 in the control group

59 ebrile neutropenia (23 [15%] patients in the aprepitant group vs 22 [15%] in the control group).

60 asure (46% reduction in the VAS score in the aprepitant group vs 40% reduction in the placebo group;

61 However, aprepitant had varying effects on secondary outcomes of

62 ervous systems, and NK1R antagonists such as aprepitant have been approved for treating chemotherapy-

63 To evaluate the effect of aprepitant in addition to a standard regimen, we conduct

64 atic characterisation of the binding mode of aprepitant in complexes with human NK1R variants.

65 so implicated in cough.Objectives: To assess aprepitant in patients with lung cancer with cough and e

66 0 mg) was noninferior to standard 3-day oral aprepitant in preventing CINV during OP and DP.

67 verify whether dexamethasone is superior to aprepitant in preventing delayed emesis in patients rece

68 Whereas the FDA-approved NK(1)R antagonist aprepitant induced a transient disruption of endosomal s

69 ontaining the FDA-approved NK(1)R antagonist aprepitant, inhibit SP-induced activation of spinal neur

70 SP receptor antagonists, such as aprepitant inhibited both hapten-induced cutaneous infla

71 Aprepitant is a licensed treatment for nausea and vomiti

72 the orally active NK(1) receptor antagonist Aprepitant is described.

73 onin receptor antagonist, dexamethasone, and aprepitant is recommended before chemotherapy of high em

74 tor serotonin antagonist, dexamethasone, and aprepitant is recommended for patients receiving an anth

75 he two-drug combination of dexamethasone and aprepitant is recommended for the prevention of delayed

76 gainst the use of domperidone, prucalopride, aprepitant, nortriptyline, buspirone, and cannabidiol as

77 d a slow off-rate in the binding site, where aprepitant occupies multiple substates that exchange wit

78 ough the effects of pyrilamine, cromolyn, or aprepitant on ET-induced vascular leakage suggest a poss

79 All participants received aprepitant, ondansetron, and dexamethasone during and 2

80 rmed using data from five clinical trials of aprepitant or fosaprepitant in pediatric patients receiv

81 Receipt of ondansetron plus aprepitant or fosaprepitant was associated with a higher

82 placebo, in combination with dexamethasone, aprepitant or fosaprepitant, and a 5-hydroxytryptamine t

83 CI, 1.06 to 1.34) and in those who received aprepitant or fosaprepitant.

84 They received 3 days of aprepitant or matched placebo; after a 3-day washout, pa

85 milar: 87.6% for dexamethasone and 84.9% for aprepitant (P < .39).

86 h prochlorperazine on days 2 and 3; group 3: aprepitant + palonosetron + dexamethasone on day 1 with

87 ne on days 2 to 4) or an aprepitant regimen (aprepitant plus ondansetron and dexamethasone on day 1;

88 retreatment with the NK1R antagonist, EMEND (aprepitant) prevented these NK1R-mediated effects.

89 Significantly more patients receiving aprepitant reached the primary end point (58% v 41%; odd

90 Cough frequency improved with aprepitant, reducing by 22.2% (95% confidence interval [

91 ndansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80

92 n day 1; dexamethasone on days 2 to 4) or an aprepitant regimen (aprepitant plus ondansetron and dexa

93 stablish definitively the superiority of the aprepitant regimen versus standard therapy in the preven

94 The addition of aprepitant resulted in significantly less CINV and had a

95 This study compared a 3-day oral aprepitant schedule to a regimen containing a single dos

96 enic chemotherapy, the neurokinin antagonist aprepitant significantly enhanced the efficacy of a stan

97 Aprepitant significantly inhibited substance P-induced d

98 In fact, aprepitant - the first neurokinin-1 antagonist approved

99 Second, NK1-RAs, including aprepitant, the first approved member of this family, ar

100 Addition of aprepitant to ondansetron with or without dexamethasone

101 led phase III cross-over study that compared aprepitant to placebo combined with standard antiemetic

102 lity of the neurokinin-1 receptor antagonist aprepitant to reduce symptoms in patients with chronic n

103 ons in knockin mice expressing human NK(1)R, aprepitant transiently inhibited nociceptive responses t

104 A randomized double-blind study comparing aprepitant versus dexamethasone was completed in chemoth

105 ys 2 and 3 (group 1 v group 4); and by using aprepitant versus prochlorperazine (group 3 v group 4).

106 (95% CI, -0.02 to 0.41; P = .01); and using aprepitant versus prochlorperazine: -0.03 (95% CI, -0.24

107 ared with standard dual therapy, addition of aprepitant was generally well tolerated and provided con

108 nist, while those at high risk also received aprepitant with or without olanzapine, based on their ri

109 r (1)H-(19)F correlations of the crystalline aprepitant without interferences from other pharmaceutic