Effect of BI 201335 Mediated UGT1A1 (Uridine-diphosphate-glucuronosyltransferases) Inhibition in Healthy Volunteers

NCT02182375 | Completed Phase 1

• 1 other identifier: 1220.9
• Study Type: interventional
• Target: 24
• Locations: 0 countries
• Sites: N/A

Brief Summary

Study to investigate the effect of UGT1A1 inhibition by single and multiple oral doses of BI 201335 on the single and multiple oral dose pharmacokinetics of raltegravir and to investigate safety and tolerability.

Conditions

Healthy

Outcome Measures

Primary Outcomes (3)

• Steady-state Cmax,ss (maximum measured concentration) of raltegravir and raltegravir glucuronide

  Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15

• Steady-state AUC0-12h,ss (Area under the concentration-time curve) of raltegravir and raltegravir glucuronide

  Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15

• C12h,ss of raltegravir and raltegravir glucuronide

  Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15

Secondary Outcomes (19)

• Number of patients with abnormal findings in physical examination

  Baseline and within 7-14 days after last treatment

• Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)

  Baseline and days 1, 5, 6, 7, 15 and within 7-14 days after last treatment

• Number of patients with adverse events

  up to 7 - 14 days after last treatment

• Number of patients with abnormal findings in 12-lead ECG (electrocardiogram)

  Baseline, days 1, 5, 6, 7, 15 and within 7-14 days after last treatment

• Number of patients with abnormal changes in laboratory tests (hematology, clinical chemistry, urine analysis)

  Baseline, days 1, 2, 5, 6, 7, 8, 10, 12, 14, 15, 16 and within 7-14 days after last treatment

Study Arms (1)

BI 201335 NA

EXPERIMENTAL

400 mg raltegravir (bid) from day 1-14 and once on day 15; 240 mg BI 201335 NA (bid) from day 7-14 with a loading dose of 480 mg in the morning of day 6 and once on day 15

Drug: BI 201335 NA; Drug: Raltegravir

Interventions

BI 201335 NA DRUG

BI 201335 NA

Raltegravir DRUG

BI 201335 NA

Eligibility Criteria

• Age: 21 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy males and females
• Age ranging ≥ 21 and ≤ 50 years
• Body mass index (BMI) ≥ 18.5 and ≤ 29.9 kg/m2
• Willing to complete all study-related activities including genotyping
• Volunteers give their written informed consent prior to admission to the study

You may not qualify if:

• Any finding of the medical examination (including blood pressure, pulse rate and ECG (Electrocardiogram)) deviating from normal and of clinical relevance
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders, clinically relevant electrolyte disturbances
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• History of photosensitivity or recurrent rash
• History of orthostatic hypotension, fainting spells or blackouts
• Chronic or clinically relevant acute infections
• History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
• Intake of drugs with a long half-life (\> 24:00 hours) within at least one month or less than ten half-lives of the respective drug before enrolment in the study or during the study (with the exception of hormonal contraceptives)
• Use of any drugs which might influence the results of the trial up to 7 days prior to enrolment in the trial or during the trial
• Participation in another trial with an investigational drug (within two months prior to administration or during the trial)
• Smoker (\> 10 cigarettes or \> 3 cigars of \> 3 pipes/day)
• Inability to refrain from smoking on trial days
• Alcohol abuse (\> 60 g/day)
• Drug abuse
• Blood donation (\> 100 mL within four weeks prior to administration or during the trial)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Raltegravir Potassium

Intervention Hierarchy (Ancestors)

Pyrrolidinones; Pyrrolidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 2, 2014
• First Posted: July 8, 2014
• Study Start: January 1, 2010
• Primary Completion: March 1, 2010
• Last Updated: July 18, 2014

Record last verified: 2014-07