ライフサイエンスコーパス: ZD1839

1 ree of inhibition of EGFR phosphorylation by ZD1839.

2 ion of cells in G(1) phase after exposure to ZD1839.

3 fied the mechanism of apoptosis induction by ZD1839.

4 acy, tolerability, and optimal daily dose of ZD1839.

5 essing tumors were particularly sensitive to ZD1839.

6 from BT-474 cells was unaffected by 1 microM ZD1839.

7 escalation safety/tolerability trial of oral ZD1839 (150 to 1,000 mg/d), administered once daily for

8 ad objective partial responses observed from ZD1839 300 to 700 mg/d.

9 c disease and were treated with single-agent ZD1839 500 mg/d.

10 Exposure to 0.5 micromol/L ZD1839, a HER1-specific inhibitor, caused a 40% to 50% r

11 The specificity of ZD1839 against EGFR was confirmed in Rat1 fibroblasts tr

12 er cell lines (except MDA-453) with 1 microM ZD1839 almost completely eliminated HER2 phosphorylation

13 her demonstrated that treatment of SCCs with ZD1839 amplified radiation-induced apoptosis.

14 rved in mice treated with the combination of ZD1839 and radiation.

15 Half the cohort received ZD1839 as second-line therapy.

16 New York, NY) with either gefitinib (Iressa, ZD1839; AstraZeneca, Macclesfield, UK) or erlotinib (Tar

17 cal studies indicate that gefitinib (Iressa, ZD1839; AstraZeneca, Wilmington, DE), an orally active e

18 IGF transactivates the EGF receptor and that ZD1839 blocks IGF-mediated phosphorylation of MAPK and B

19 Finally, ZD1839 completely prevented growth of BT-474 xenografts

20 Low doses of ZD1839 delayed cell cycle progression and induced apopto

21 In both cell lines, 0.1 microM ZD1839 eliminated EGFR phosphorylation.

22 In SKBR-3 cells, ZD1839 exhibited a greater growth-inhibitory effect than

23 ion than the EGFR-selective kinase inhibitor ZD1839 (gefitinib), consistent with the HER-2 kinase pla

24 ZD1839 has single-agent activity and is well tolerated i

25 ics that correlate with tumor sensitivity to ZD1839 have been studied.

26 A431 cell growth was markedly inhibited by ZD1839 (IC(50)< or =0.1 microM) whereas the MDA-468 cell

27 sults suggest that the antitumor activity of ZD1839 in combination with radiation appears to derive f

28 We evaluated the antitumor activity of ZD1839 in combination with radiation in human squamous c

29 activity, toxicity, and pharmacodynamics of ZD1839 in SCCHN.

30 inhibitor geldanamycin or the ErbB inhibitor ZD1839 in SKBR3 cells, a human breast cancer cell line o

31 ZD1839 induced a greater degree of apoptosis and cell cy

32 Even at 0.01 micromol/L, ZD1839 inhibited autophosphorylation of HER1 by EGF.

33 N but not in vector controls, treatment with ZD1839 inhibited P-Akt levels, induced relocalization of

34 factor receptor kinase inhibitor, gefitinib (ZD1839) inhibited growth of LTLT-Ca cells (IC(50) approx

35 ZD1839 (Iressa) is a small-molecular-weight, ATP-mimetic

36 ZD1839 (Iressa) is an ATP-mimetic that inhibits the puri

37 glioma model with the EGFR kinase inhibitors ZD1839 (Iressa) or PD153035, synthetic anilinoquinazolin

38 ng preclinical and clinical investigation is ZD1839 (Iressa), a synthetic anilinoquinazoline capable

39 eptor (EGFR) kinase inhibitors, PD153035 and ZD1839 (Iressa), abolished PPARalpha and gamma agonist-d

40 dy IMC-225 and the tyrosine kinase inhibitor ZD1839 (Iressa), from the laboratory to clinical trials.

41 ZD1839 ("Iressa") is an orally-active, selective epiderm

42 ZD1839 ("Iressa"), a quinazoline tyrosine kinase inhibit

43 factor receptor (EGFR) inhibitor gefitinib (ZD1839, Iressa) blocked cell proliferation at biological

44 ation approved the EGFR inhibitor gefitinib (ZD1839, Iressa) for the treatment of patients with advan

45 Our results also indicate that ZD1839 is a potent inhibitor of neuroblastoma cell proli

46 ZD1839 is an orally active, selective EGFR tyrosine kina

47 Our findings demonstrate that in vitro, ZD1839 is as effective or more effective against MPM cel

48 Furthermore, treatment with ZD1839 led to a significant dose-dependent reduction of

49 earing mice with vehicle, the EGFR inhibitor ZD1839, LY294002, or ZD1839 plus LY294002.

50 st the NSCLC cell line A549 and suggest that ZD1839 may be an effective therapeutic option for patien

51 61 but not by MDA-453 cells, suggesting that ZD1839-mediated inhibition of the EGFR kinase explained

52 angiogenic effects, we studied the impact of ZD1839 on human umbilical vascular endothelial cells (HU

53 tudies confirmed that oral administration of ZD1839, or focal radiation, resulted in partial and tran

54 both SKBR-3 and BT-474 cells, treatment with ZD1839 plus Herceptin induced a greater apoptotic effect

55 cle, the EGFR inhibitor ZD1839, LY294002, or ZD1839 plus LY294002.

56 rug in phase III clinical trails for cancer, ZD1839, potently induces apoptosis in mammary epithelial

57 ZD1839 produced a dose-dependent inhibition of cellular

58 sis demonstrated that treatment of SCCs with ZD1839 reduced cell survival after radiation exposure.

59 Treatment with ZD1839 reduced the cell-to-cell interaction of HUVECs, r

60 treatment with the tyrosine kinase inhibitor ZD1839 revealed increased sensitivity in both transcript

61 gent the ERBB1 inhibitor, gefitinib (Iressa; ZD1839) showed minimal activity against a panel of 10 pe

62 ZD1839 significantly inhibited epidermal growth factor-d

63 Systemic treatment with ZD1839 significantly inhibited tumor-induced neovascular

64 ensitive to the growth-inhibitory effects of ZD1839 than was the NSCLC cell line A549, whereas H2591

65 cant change in EGFR or p-ERK expression with ZD1839 therapy.

66 Fourteen patients received ZD1839 through a feeding tube.

67 hich show 89% growth inhibition at 10 microM ZD1839, undergo a dose-dependent arrest at the G(1)-S ph

68 hich show 41% growth inhibition at 10 microM ZD1839, undergo no significant cell cycle changes or cha

69 ZD1839 was administered once daily for 14 consecutive da

70 Exposure to ZD1839 was dose proportional, and the mean terminal half

71 The effect of ZD1839 was further examined using an in vivo tumor xenog

72 Pharmacokinetic analysis confirmed that ZD1839 was suitable for administration as a once-daily o

73 ZD1839 was well tolerated, with DLT observed at a dose w

74 yrosine kinase inhibitor (Gefitinib, Iressa, ZD1839) with respect to its inhibitory effects on three