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

Start Date01 Mar 1998

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with Itasetron

100 Translational Medicine associated with Itasetron

100 Patents (Medical) associated with Itasetron

Literatures (Medical) associated with Itasetron

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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.

01 Apr 1999·Clinical OncologyQ2 · MEDICINE

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

Q2 · MEDICINE

Article

Author: 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.

01 Feb 1999·Drugs in R & DQ4 · MEDICINE

DAU 6215, U 98079

Q4 · MEDICINE

ArticleOA

Author: &NA;

100 Deals associated with Itasetron

External Link

KEGG	Wiki	ATC	Drug Bank
D04642	-	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anxiety Disorders	Phase 3	US	-	-
Anxiety Disorders	Phase 3	-	-	-
Cognition Disorders	Phase 3	IT	-	-
Nausea	Phase 3	-	C.H. Boehringer Sohn AG & Co. KG	-
Nausea and vomiting	Phase 3	-	-	-
Nausea and vomiting	Phase 3	JP	-	-
Nausea and vomiting	Phase 3	US	-	-
Psychotic Disorders	Phase 3	IT	-	-

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