ライフサイエンスコーパス: eribulin

1 approval include pazopanib, trabectedin, and eribulin.

2 ts were more common in patients who received eribulin (152 [67%]) than in those who received dacarbaz

3 randomly allocated to treatment groups (508 eribulin, 254 TPC).

4 d the microtubule targeting anti-cancer drug Eribulin [5-7] to explore the consequences of stalled pr

5 and washout/retention studies show that [3H]eribulin accumulates to lower intracellular levels than

6 In the per-protocol population (n = 87), eribulin achieved an independently reviewed objective re

7 Eribulin also binds microtubules with a maximum stoichio

8 in the absence of any drugs, we propose that Eribulin amplifies a natural pathway toward catastrophe

9 Objective response rates were 11.0% for eribulin and 11.5% for capecitabine.

10 ed in 224 (99%) of 226 patients who received eribulin and 218 (97%) of 224 who received dacarbazine.

11 nd neutropenia (260 [52%] patients receiving eribulin and 73 [30%] of those on TPC at all grades).

12 nia or fatigue (270 [54%] of 503 patients on eribulin and 98 [40%] of 247 patients on TPC at all grad

13 Median PFS times for eribulin and capecitabine were 4.1 and 4.2 months, respe

14 Bcl-2 phosphorylation patterns parallel eribulin and ER-076349 mitotic block reversibility patte

15 iral formation is strongly inhibited by both eribulin and ER-076349.

16 y of mitochondria in neuronal cells, whereas eribulin and vincristine inhibited transport only at sig

17 ng the lengths of microtubules and the drugs eribulin and vincristine that bind at microtubule ends,

18 whereas the microtubule-destabilizing drugs, eribulin and vincristine, which bind preferentially to m

19 ents (5-fluoruracil, carboplatin, cisplatin, eribulin, and paclitaxel), based on their continued viab

20 a permuted block scheme by region, previous eribulin, and receptor status.

21 improvement in overall survival (OS) for the eribulin arm, with a manageable toxicity profile.

22 inblastine induced additional lower-affinity eribulin binding sites, most likely at splayed microtubu

23 Using [(3)H]eribulin, we found that eribulin binds soluble tubulin at a single site; however

24 -ray crystallography, we first revealed that Eribulin binds to a site on beta-tubulin that is require

25 Overall, our results indicate that eribulin binds with high affinity to microtubule plus en

26 bservations that mitotic blockade induced by eribulin, but not ER-076349, is irreversible as measured

27 group analysis of the efficacy and safety of eribulin compared with dacarbazine in patients with LPS,

28 urvival was improved in patients assigned to eribulin compared with those assigned to an active contr

29 gnificantly improved in patients assigned to eribulin compared with those assigned to dacarbazine (me

30 signed to an active control, suggesting that eribulin could be a treatment option for advanced soft-t

31 Eribulin demonstrated activity with manageable tolerabil

32 ibited anterograde axonal transport, whereas eribulin did not.

33 Eribulin does not suppress dynamic instability at microt

34 Eribulin (E7389), a mechanistically unique microtubule i

35 Notably, although eribulin exhibited greater DRG and SN penetration than p

36 eaths (10 [4%] vs 3 [1%]); one death (in the eribulin group) was considered treatment-related by the

37 A new convergent synthesis of eribulin has been achieved, using (1) catalytic asymmetr

38 s, ketone 4sc, containing all the carbons of Eribulin, has been synthesized from 1s and 3c.

39 2 study showed activity and tolerability of eribulin in advanced or metastatic soft-tissue sarcoma.

40 studies are justified to explore the role of eribulin in earlier lines of therapy as well as in combi

41 study evaluated efficacy and tolerability of eribulin in heavily pretreated patients with metastatic

42 Interestingly, we found that Eribulin increases the frequency of EB3 comet "splitting

43 Eribulin inhibits this oligomer formation 4-6-fold, whil

44 These results suggest that eribulin is a global inhibitor of tubulin polymer format

45 growth by 50%, we found that one molecule of eribulin is bound per two microtubules, indicating that

46 Eribulin is currently undergoing phase III clinical tria

47 mice exposed to the antitubulin cancer drugs eribulin, ixabepilone, paclitaxel, or vinorelbine at MTD

48 significantly improved in women assigned to eribulin (median 13.1 months, 95% CI 11.8-14.3) compared

49 east cancer were randomly allocated (2:1) to eribulin mesilate (1.4 mg/m(2) administered intravenousl

50 randomly assigned (1:1) patients to receive eribulin mesilate (1.4 mg/m(2) intravenously on days 1 a

51 Eribulin mesilate is a non-taxane microtubule dynamics i

52 cline, were randomly assigned 1:1 to receive eribulin mesylate (1.4 mg/m(2) intravenously on days 1 a

53 with an anthracycline and a taxane received eribulin mesylate (1.4 mg/m(2)) as a 2- to 5-minute intr

54 Eribulin mesylate (E7389), a nontaxane microtubule dynam

55 Eribulin mesylate (E7389), a synthetic analogue of the m

56 Overall, our findings indicate that eribulin mesylate induces less neuropathy in mice than p

57 In contrast, eribulin mesylate produced no significant deleterious ef

58 Eribulin mesylate, a novel microtubule-targeting analogu

59 e more severe neuropathy in mice relative to eribulin mesylate, paralleling their toxicity profiles i

60 of three drugs: paclitaxel, ixabepilone, and eribulin mesylate.

61 les, indicating that the binding of a single eribulin molecule at a microtubule end can potently inhi

62 ral information, we engineered a fluorescent Eribulin molecule.

63 We demonstrate that single Eribulin molecules specifically interact with microtubul

64 Median OS times for eribulin (n = 554) and capecitabine (n = 548) were 15.9

65 y 22, 2013, we randomly assigned patients to eribulin (n=228) or dacarbazine (n=224).

66 dverse event leading to discontinuation from eribulin, occurring in 24 (5%) of 503 patients.

67 penia (at day 15), an alternative regimen of eribulin on days 1 and 8 of a 21-day cycle was administe

68 omer formation or the inhibitory activity of eribulin on this process.

69 ed therapy were randomly assigned to receive eribulin or capecitabine as their first-, second-, or th

70 the binding of two halichondrin B analogues, eribulin (previously, ER-086526, E7389) and ER-076349, t

71 Eribulin represents an important treatment option for pa

72 Our results suggest that eribulin's in vivo superiority derives from its ability

73 butes to long-term cell-viability loss after eribulin's irreversible blockade.

74 Eribulin showed a significant and clinically meaningful

75 Eribulin strongly inhibits formation of the 1:2 stathmin

76 Eribulin targets microtubules, suppressing dynamic insta

77 ted in ligated sciatic nerves of control and eribulin-treated mice, but not in paclitaxel-treated mic

78 val of heavily pretreated patients receiving eribulin versus currently available treatments.

79 PFS was also improved with eribulin versus dacarbazine (2.9 v 1.7 months, respectiv

80 , 0.51; 95% CI, 0.35 to 0.75; P < .001) with eribulin versus dacarbazine, respectively.

81 ble after 3-6 months after administration of eribulin, vinorelbine, and ixabepilone, we observed dela

82 ion In patients with previously treated LPS, eribulin was associated with significantly superior OS a

83 In this phase III study, eribulin was not shown to be superior to capecitabine wi

84 Longer OS with eribulin was observed in all LPS histologic subtypes and

85 Using [(3)H]eribulin, we found that eribulin binds soluble tubulin a

86 Focusing on paclitaxel and eribulin, we performed a 2-week MTD-dosing regimen, foll

87 This phase III randomized trial compared eribulin with capecitabine in patients with locally adva

88 Purpose A phase III study comparing eribulin with dacarbazine in patients with advanced lipo

89 metastatic soft-tissue sarcoma who received eribulin with that in patients who received dacarbazine