e7070 demonstrates potent antitumour activity

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Inpharma 1319 - 5 Jan 2002 E7070 demonstrates potent antitumour activity E7070 * has potent antitumour activity in vitro and in vivo and appears to have a novel mechanism of action, say researchers from Japan. Exposure of P388 murine leukaemia cells to E7070 in vitro appeared to cause cell cycle disturbance in the G1 phase, in a time- and dose-dependent manner. E7070 showed a unique antiproliferative spectrum against a panel of 42 human tumour cell lines. In HCT116 colon cancer cells, extending the exposure time to E7070 increased the cytotoxic effect. When administered for 4 days, E7070 supressed the growth of several human tumour xenografts in mice and also induced tumour regression in 3 of 5 colorectal and 2 of 2 lung cancers, including HCT15 colon cancer, which is resistant to various drugs. The tumour volume of HCT116 and LX-1 lung cancer xenografts was reduced by 73–85% at the maximum tolerated dosage of 50 mg/kg/day. In the HCT116 xenograft model, E7070 was superior to fluorouracil, mitomycin and irinotecan. Mitomycin and irinotecan showed only tumour suppression and fluorouracil did not show antitumour activity in this model. The activity of E7070 may be independent of the multidrug resistance phenotype, comment the researchers. * Eisai; phase II for colorectal, head and neck, and non-small-cell lung cancer Ozawa Y, et al. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. European Journal of Cancer 37: 2275-2282, Nov 2001 800886573 1 Inpharma 5 Jan 2002 No. 1319 1173-8324/10/1319-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved

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Inpharma 1319 - 5 Jan 2002

E7070 demonstrates potentantitumour activity

E7070* has potent antitumour activity in vitro and invivo and appears to have a novel mechanism of action,say researchers from Japan.

Exposure of P388 murine leukaemia cells to E7070 invitro appeared to cause cell cycle disturbance in the G1phase, in a time- and dose-dependent manner. E7070showed a unique antiproliferative spectrum against apanel of 42 human tumour cell lines. In HCT116 coloncancer cells, extending the exposure time to E7070increased the cytotoxic effect.

When administered for 4 days, E7070 supressed thegrowth of several human tumour xenografts in mice andalso induced tumour regression in 3 of 5 colorectal and2 of 2 lung cancers, including HCT15 colon cancer,which is resistant to various drugs. The tumour volumeof HCT116 and LX-1 lung cancer xenografts was reducedby 73–85% at the maximum tolerated dosage of 50mg/kg/day. In the HCT116 xenograft model, E7070 wassuperior to fluorouracil, mitomycin and irinotecan.Mitomycin and irinotecan showed only tumoursuppression and fluorouracil did not show antitumouractivity in this model.

The activity of E7070 may be independent of themultidrug resistance phenotype, comment theresearchers.* Eisai; phase II for colorectal, head and neck, and non-small-cell lungcancer

Ozawa Y, et al. E7070, a novel sulphonamide agent with potent antitumouractivity in vitro and in vivo. European Journal of Cancer 37: 2275-2282, Nov2001 800886573

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Inpharma 5 Jan 2002 No. 13191173-8324/10/1319-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved