Bioequivalence Trial of 2 Dose Strengths of BI 201335 NA Soft Gelatine Capsules

Assessment of Bioequivalence Between Two Different Formulations of BI 201335 NA Soft Gelatine Capsules in Healthy Male Volunteers. (an Open-label, Randomised, Single-dose, Four-period Replicated Crossover Study)

The objective is to investigate the bioequivalence of 2 dose strengths of 40 mg and 120 mg BI 201335 NA soft gelatine capsules.

Study Overview

• Status: Completed
• Conditions: Hepatitis C
• Intervention / Treatment: Drug: BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 40 mg capsule

• Study Type: Interventional
• Enrollment (Actual): 60
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Sumida-ku,Tokyo, Japan
    • 1220.53.08101 Boehringer Ingelheim Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion criteria:

1. Healthy male volunteers without any clinical significant findings and complications
2. Age: 20 - 45 years
3. BMI: 18.5 - 25.0 kg/m2
4. Signed informed consent

Exclusion criteria:

1. Any finding of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance.
2. Any evidence of a clinically relevant concomitant disease according to investigator's clinical judgement.
3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders.
4. History of jaundice
5. Surgery of the gastrointestinal tract (except appendectomy).
6. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders.
7. History of relevant orthostatic hypotension, fainting spells or blackouts.
8. Chronic or relevant acute infections.
9. History of relevant allergy/hypersensitivity (including allergy to drug or its excipients) according to investigator's clinical judgement.
10. Intake of drugs with a long half-life (>24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
11. Use of drugs which might reasonably influence the results (pharmacokinetic) of the trial within at least 10 days prior to administration or during the trial.
12. Participation in another trial with an investigational drug within two months prior to administration or during the trial.
13. Smoking (>10 cigarettes or >3 cigars or >3 pipes/day).
14. Inability to refrain from smoking during the trial.
15. Alcohol abuse (more than 60 g/day: e.g., 3 middle-sized bottles of beer, 3 gous [equivalent to 540 mL] of sake).
16. Drug abuse.
17. Blood donation (more than 100 mL within four weeks prior to administration).
18. Excessive physical activities (within one week prior to administration).
19. Any laboratory value outside the reference range that is of clinical relevance according to investigator's clinical judgement.
20. Any history of relevant liver diseases (for instance, disturbances of liver function, Dubin-Johnson syndrome, Rotor syndrome, or previous liver tumours).

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

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Treatment sequence 1; Test - Reference - Reference - Test	Drug: BI 201335 NA 120 mg capsule; 1capsule of BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 120 mg capsule; 1 capsule of BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 40 mg capsule; 3 capsules of BI 201335 NA 40 mg capsule
Experimental: Treatment sequence 2; Reference - Test - Test - Reference	Drug: BI 201335 NA 120 mg capsule; 1capsule of BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 120 mg capsule; 1 capsule of BI 201335 NA 120 mg capsule; Drug: BI 201335 NA 40 mg capsule; 3 capsules of BI 201335 NA 40 mg capsule

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Curve of the Analyte From Time 0 to the Last Quantifiable Data Point (AUC0-tz)	Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 to the time of the last quantifiable data point. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration
Maximum Measured Concentration (Cmax)	Maximum measured concentration of faldaprevir in plasma. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Curve Over the Time Interval From 0 Extrapolated to Infinity (AUC0-inf)	Area under the concentration-time curve of faldaprevir in plasma over the time interval from 0 extrapolated to infinity. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration
Time From Dosing to the Maximum Measured Concentration (Tmax)	Time from dosing to the maximum measured concentration of the analyte in plasma. Means presented are adjusted means and the standard deviation is actually the intra-individual coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration
Terminal Rate Constant (λz)	Terminal rate constant of the analyte in plasma. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration
Terminal Half-life (t1/2)	Terminal half-life of faldaprevir in plasma. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration
Mean Residence Time (MRTpo)	Mean residence time of the analyte in the body after oral administration. Geometric means presented are adjusted means and the coefficient of variation is the intra-individual geometric coefficient of variation.	3 hours (h) before drug administration and 1h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h, 48h, 72h and 96h after drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: October 1, 2012
• Primary Completion (Actual): January 1, 2013
• Study Completion (Actual): January 1, 2013

Study Registration Dates

• First Submitted: October 9, 2012
• First Submitted That Met QC Criteria: October 9, 2012
• First Posted (Estimate): October 12, 2012

Study Record Updates

• Last Update Posted (Estimate): July 31, 2015
• Last Update Submitted That Met QC Criteria: July 3, 2015
• Last Verified: July 1, 2015

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Digestive System Diseases; RNA Virus Infections; Virus Diseases; Infections; Blood-Borne Infections; Communicable Diseases; Liver Diseases; Flaviviridae Infections; Hepatitis, Viral, Human; Hepatitis; Hepatitis C
• Other Study ID Numbers: 1220.53