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安圭定(二乙酰氧基镰刀菌烯醇,NSC-141537)的I期评估。

Phase I evaluation of anguidine (diacetoxyscirpenol, NSC-141537).

作者信息

Goodwin W, Haas C D, Fabian C, Heller-Bettinger I, Hoogstraten B

出版信息

Cancer. 1978 Jul;42(1):23-6. doi: 10.1002/1097-0142(197807)42:1<23::aid-cncr2820420104>3.0.co;2-i.

DOI:10.1002/1097-0142(197807)42:1<23::aid-cncr2820420104>3.0.co;2-i
PMID:667795
Abstract

A toxicologic evaluation of anguidine (diacetoxyscirpenol) was completed for a 5 day schedule. At 4.5 mg/M2 and 6 mg/M2 iv push CNS symptoms and hypotension were dose limiting but only mild to moderate myelosuppression was observed. At the 6 mg/M2 dose level on a 5 day schedule given by 8 hour infusion, myelosuppression was unacceptable while other toxic manifestations were minimal. An infusion of 4.5 mg/M2 over 4-8 hours appears to be an acceptable compromise between CNS, cardiovascular, and GI toxicity and myelosuppression. For patients with liver dysfunction or prior nitrosourea therapy, the starting dose should be 3.0 mg/M2.

摘要

完成了对安圭定(二乙酰氧基雪腐镰刀菌烯醇)的5日疗程毒理学评估。静脉推注剂量为4.5mg/M²和6mg/M²时,中枢神经系统症状和低血压为剂量限制性毒性,但仅观察到轻度至中度骨髓抑制。以8小时输注方式给予5日疗程,剂量为6mg/M²时,骨髓抑制不可接受,而其他毒性表现轻微。4 - 8小时内输注4.5mg/M²似乎是中枢神经系统、心血管和胃肠道毒性与骨髓抑制之间可接受的折衷方案。对于肝功能不全或既往接受过亚硝基脲治疗的患者,起始剂量应为3.0mg/M²。

相似文献

1
Phase I evaluation of anguidine (diacetoxyscirpenol, NSC-141537).安圭定(二乙酰氧基镰刀菌烯醇,NSC-141537)的I期评估。
Cancer. 1978 Jul;42(1):23-6. doi: 10.1002/1097-0142(197807)42:1<23::aid-cncr2820420104>3.0.co;2-i.
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Cancer Treat Rep. 1979 Nov-Dec;63(11-12):2015-7.
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Phase II evaluation of anguidine (NSC-141537) for adenocarcinoma of the colon or rectum.安圭定(NSC-141537)用于结肠或直肠癌的II期评估。
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Fundam Appl Toxicol. 1985 Dec;5(6 Pt 1):1034-49. doi: 10.1016/0272-0590(85)90140-x.
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Cancer Treat Rep. 1983 Mar;67(3):285-6.

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