Effects of Food on the Bioavailability and Pharmacokinetic Profile of Itasetron After a Single Oral Dose in Healthy Male Subjects

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Other: high fat breakfast; Drug: Itasetron tablet; Drug: Itasetron infusion

• Study Type: Interventional
• Enrollment (Actual): 15
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 21 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• all participants in the study will range from 21 to 50 years of age and be within +- 20% of their normal weight (Broca-index)
• written informed consent in accordance with Good Clinical Practica and local legislation

Exclusion Criteria:

• Subjects will be excluded from the study if the results of the medical examination or laboratory tests are judged by the investigator to differ significantly from normal clinical values
• Subjects with known gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Subjects with diseases of the central nervous system (such as epilepsy) or with psychiatric disorders
• Subjects with known history of orthostatic hypotension, fainting spells or blackouts
• Subjects with chronic or relevant acute infections
• Subjects with history of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
• Subjects who have taken a drug with a long half-life (>= 24 hours) within one month before enrolment in the study
• Subjects who received any other drugs which might influence the results of the trial during the week previous the start of the study
• Subjects who have participated in another study with an investigational drug within the last 2 months preceding this study
• Subjects who are unable to refrain from smoking on study days
• Subjects who smoke more than 10 cigarettes (or 3 cigars or pipes) per day
• Subjects who drink more than 60 g of alcohol per day
• Subjects who are dependent on drugs
• Subjects who have donated blood (>= 100 ml) within the last 4 weeks
• Subjects who participated in excessive physical activities (e.g. competitive sports) within the last week before the study

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Itasetron tablet fed	Other: high fat breakfast; Drug: Itasetron tablet
Active Comparator: Itasetron tablet fasted	Drug: Itasetron tablet
Active Comparator: Itasetron infusion fasted	Drug: Itasetron infusion

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the concentration time curve from zero to infinity (AUC0-inf)	up to 48 hours after drug administration
Maximum concentration of drug in plasma	up to 48 hours after drug administration
Time to maximum concentration (tmax)	up to 48 hours after drug administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Elimination half-life (t1/2)		up to 48 hours after drug administration
Area under the concentration time curve from zero to to the time of last data point above limit of quantitation (AUC0-tlast)		up to 48 hours after drug administration
Cmax/AUC ratio		up to 48 hours after drug administration
Mean residence time in the body (MRTtot)		up to 48 hours after drug administration
Apparent volume of distribution during the terminal phase λz (Vz)		up to 48 hours after drug administration
Total clearance from plasma (CLtot)		up to 48 hours after drug administration
Apparent volume of distribution after intravascular dose at steady state (Vss)		up to 48 hours after drug administration
Number of participants with clinically significant findings in vital signs	blood pressure, pulse rate	up to 8 days after last drug administration
Number of participants with clinically significant findings in ECG		up to 8 days after last drug administration
Number of participants with clinically significant findings in laboratory tests		up to 8 days after last drug administration
Number of participants with adverse events		up to 8 days after last drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: March 1, 1998
• Primary Completion (Actual): May 1, 1998

Study Registration Dates

• First Submitted: October 7, 2014
• First Submitted That Met QC Criteria: October 7, 2014
• First Posted (Estimate): October 9, 2014

Study Record Updates

• Last Update Posted (Estimate): October 9, 2014
• Last Update Submitted That Met QC Criteria: October 7, 2014
• Last Verified: October 1, 2014

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Autonomic Agents; Peripheral Nervous System Agents; Antiemetics; Gastrointestinal Agents; Serotonin Agents; Serotonin Antagonists; Serotonin 5-HT3 Receptor Antagonists; Itasetron
• Other Study ID Numbers: 208.629