伊他司琼(Itasetron) - 药物靶点：5-HT3 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Itasetron (USAN/INN)

+ [3]

靶点

5-HT3 receptor

作用机制

5-HT3 receptor拮抗剂(5-羟色胺受体3拮抗剂)

治疗领域

其他疾病

在研适应症-

非在研适应症

焦虑症认知障碍恶心+ [2]

原研机构

C.H. Boehringer Sohn AG & Co. KG

在研机构-

非在研机构

C.H. Boehringer Sohn AG & Co. KG

Boehringer Ingelheim GmbH

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C16H20N4O2

InChIKeyRWXRJSRJIITQAK-ZSBIGDGJSA-N

CAS号123258-84-4

关联

1

项与伊他司琼相关的临床试验

NCT02259985 / Completed临床1期

Investigation of the Effects of Food on the Bioavailability and Pharmacokinetic Profile of Itasetron After a Single Oral Dose of 1 mg in Healthy Male Subjects (3-way Cross-over)

food interaction, pharmacokinetics, safety and tolerability

开始日期1998-03-01

申办/合作机构

Boehringer Ingelheim GmbH

100 项与伊他司琼相关的临床结果

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100 项与伊他司琼相关的转化医学

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100 项与伊他司琼相关的专利（医药）

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25

项与伊他司琼相关的文献（医药）

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

DAU 6215, a novel 5-HT3-receptor antagonist, selectively antagonizes scopolamine-induced deficit in a passive-avoidance task, but not scopolamine-induced hypermotility in rats

3区 · 医学

Article

作者: Borsini, Franco ; Brambilla, Alessandro ; Ghiorzi, Aldo ; Pitsikas, Nikolaos

AbstractThis study examined the effects of DAU 6215, a selective 5-HT3-receptor antagonist, on either impairment of a passive-avoidance task or hypermotility, both caused by scopolamine in rats. In the first experiment, scopolamine (0·75 mg kg−1, i.p.) disrupted acquisition of a one-trial ‘step through’ passive-avoidance response. Pretreatment with DAU 6215 (1, 10, 30 and 100 μg kg−1, i.p.) antagonized this deficit induced by scopolamine, with a bell-shaped dose-response curve. Scopolamine (0·75 mg kg−1, i.p.) produced a significant increase in locomotor activity which was unaffected by pretreatment with DAU 6215 (10 and 30 μg kg−1, i.p.). The present results further support the suggestion that 5-HT3-receptor antagonists may prevent the memory disturbance caused by a reduction in central cholinergic function in the rat. The inefficacy shown by DAU 6215 on hyperactivity induced by scopolamine appears to rule out the possibility of a pharmacokinetic interference between DAU 6215 and scopolamine.

1999-04-01·Clinical Oncology2区 · 医学

Intravenous Itasetron: Establishing the Effective Dose Range for the Prophylactic Control of Acute Emesis in Cancer Patients Undergoing High-Dose Cisplatin Chemotherapy

2区 · 医学

Article

作者: L. Patoia ; A. Giglietti ; M.A. Palladino ; D. Donati ; P. Malacarne ; A. Del Favero ; P. Cigarini ; T. Voigt ; R. Kempe ; M. Indelli ; G. Bensi

Nausea and vomiting induced by chemotherapy are a major cause of distress to patients and reduce compliance with potentially beneficial treatment. Itasetron hydrochloride is a new 5-hydroxytryptamine3 (5-HT3) antagonist with potent antiemetic properties. It is more potent than ondansetron in animal models and in early clinical studies it demonstrates a long half-life and does not undergo hepatic biotransformation before elimination. The aim of this open, uncontrolled study was to establish the effective dose range of itasetron hydrochloride given intravenously (i.v.) to patients due to receive high-dose cisplatin chemotherapy (50-120 mg/m2) for the first time. Thirty-nine patients were enrolled in the trial and received a single i.v. infusion of itasetron hydrochloride at a dose of 17-280 microg/kg body weight before commencing the cisplatin infusion (median dose 90-110 mg/m2). Antiemetic protection was demonstrated by doses in the range of 35-280 microg/kg. The 17 microg/kg dose was not effective. Treatment failure (>5 emetic episodes/24 hours) was reported in only six (16%) of the 38 evaluable patients over all treatment groups. Adverse events were generally mild or moderate and of a similar type and incidence to those of current 5-HT3 antagonists. Physicians' and patients' assessments of efficacy and tolerability of itasetron hydrochloride were similar, the majority rating the treatment as 'good' or 'very good'. In conclusion, itasetron hydrochloride is effective in the dose range 35-280 microg/kg in preventing cisplatin-induced emesis. Taken together with results from a larger dose-finding study, a dose corresponding to 35 microg/kg (equivalent to 2.5 mg itasetron, calculated as free base) has been pursued in Phase III studies with the i.v. formulation.

1999-02-01·Drugs in R & D4区 · 医学

DAU 6215, U 98079

4区 · 医学

ArticleOA

作者: &NA;

1

项与伊他司琼相关的新闻（医药）

2022-10-20

·国家药品监督管理局政务服务门户

2022年10月20日药品通知件待领取信息发布

序号受理号药品名称申请人签发日期1CYHB2201687国维D2磷酸氢钙片通化友康药业有限公司2022年10月18日2CYHS1700466鄂复方氨基酸（15）双肽（2）注射液天津金耀集团湖北天药药业股份有限公司2022年10月18日3CYHS2101027国注射用培美曲塞二钠健进制药有限公司2022年10月18日4CYHS2101028国注射用培美曲塞二钠健进制药有限公司2022年10月18日5CYHS2102157国坎地沙坦酯氢氯噻嗪片重庆圣华曦药业股份有限公司2022年10月18日6CYHS2102158国坎地沙坦酯氢氯噻嗪片重庆圣华曦药业股份有限公司2022年10月18日7CYHS2102309国洛索洛芬钠凝胶江苏福邦药业有限公司2022年10月18日8CYHS2200056国来那度胺胶囊石药集团欧意药业有限公司2022年10月18日9CYHS2200057国来那度胺胶囊石药集团欧意药业有限公司2022年10月18日10JYHB2100132国盐酸昂丹司琼注射液Novartis Pharma Schweiz AG，北京诺华制药有限公司2022年10月14日11JYHB2101155国盐酸昂丹司琼注射液Novartis Pharma Schweiz AG，北京诺华制药有限公司2022年10月14日

100 项与伊他司琼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D04642	-	-	-

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
焦虑症	临床3期	欧洲	-	-
焦虑症	临床3期	美国	-	-
认知障碍	临床3期	意大利	-	-
恶心	临床3期	-	C.H. Boehringer Sohn AG & Co. KG	-
恶心和呕吐	临床3期	欧洲	-	-
恶心和呕吐	临床3期	日本	-	-
恶心和呕吐	临床3期	美国	-	-
精神障碍	临床3期	意大利	-	-