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

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;

01 Jun 1997·Anti-Cancer DrugsQ4 · MEDICINE

Comparison of oral itasetron with oral ondansetron

Q4 · MEDICINE

Article

Author: Voigt, Thor ; Egerer, Gerlinde ; Salwender, Hans ; Kempe, Rudolf ; Goldschmidt, Hartmut

Itasetron hydrochloride is a new 5-hydroxytryptamine3 (5-HT3) antagonist. Experimental investigations show that orally it is rapidly absorbed (about 90 min), is highly bioavailable (greater than 90%), has a long half-life (about 12 h) and is more potent (about 10 times) in animal models than ondansetron, currently standard therapy for the prophylactic control of chemotherapy induced nausea and vomiting. This paper describes the results of a study designed to assess the efficacy and tolerability of five (0.5, 1, 2, 4 and 8 mg) twice-daily doses of itasetron hydrochloride, in comparison with 8 mg b.i.d. ondansetron. Assessments were made in patients (n = 104) with histologically confirmed cancer (excluding head and neck tumors) and about to receive their first course of moderately emetogenic chemotherapy. Itasetron hydrochloride demonstrated comparable efficacy to ondansetron; no statistically significant between-group differences were observed in the primary (complete response rate) or secondary (nausea and delayed emesis) efficacy criteria. Adverse events were similar in type and incidence across all treatment groups, and were those expected for this therapeutic class. The tolerability of itasetron hydrochloride was assessed as 'very good' or 'rather good' by 81% of patients and 89% of physicians. In conclusion, itasetron hydrochloride is effective and well tolerated in patients receiving moderately emetogenic chemotherapy. Oral doses of 1 mg b.i.d. or above will be used in further clinical studies.

100 Deals associated with Itasetron

External Link

KEGG	Wiki	ATC	Drug Bank
D04642	-	-	-

R&D Status

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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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