Safety, Tolerability and Pharmacokinetics of BI 653048 H3PO4 Oral Drinking Solution in Healthy Male Volunteers

NCT02217644 | Completed Phase 1

• 1 other identifier: 1262.1
• Study Type: interventional
• Target: 80
• Locations: 0 countries
• Sites: N/A

Brief Summary

• Investigation of safety and tolerability of BI 653048 H3PO4 following the administration of single rising doses of an aqueous solution in healthy male subjects
• Pharmacokinetic and pharmacodynamic characteristics of BI 653048, including the investigation of dose proportionality
• Investigation of relative bioavailability of capsules versus aqueous solution

Conditions

Healthy

Outcome Measures

Primary Outcomes (5)

• Number of patients with clinically significant findings in vital signs

  blood pressure (BP), pulse rate (PR) respiratory rate (RR), oral body temperature (T), orthostatic test

  up to 10 days after drug administration

• Number of patients with clinically significant findings in ECG

  up to 10 days after drug administration

• Number of patients with clinically significant findings in laboratory tests

  up to 10 days after drug administration

• Number of patients with adverse events

  up to 10 days after drug administration

• Assessment of tolerability performed by the investigator on a four-point scale

  up to 10 days after drug administration

Secondary Outcomes (24)

• Cmax (maximum measured concentration of the analyte in plasma)

  up to 72 hours after drug administration

• tmax (time from dosing to maximum measured concentration)

  up to 72 hours after drug administration

• AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)

  up to 72 hours after drug administration

• %AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation)

  up to 72 hours after drug administration

• AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)

  up to 72 hours after drug administration

Study Arms (4)

BI 653048 H3PO4 solution

EXPERIMENTAL

single rising doses

Drug: BI 653048 H3PO4 solution

BI 653048 H3PO4 low dose capsule

EXPERIMENTAL

Drug: BI 653048 H3PO4 low dose capsule

BI 653048 H3PO4 high dose capsule

EXPERIMENTAL

Drug: BI 653048 H3PO4 high dose capsule

Placebo

PLACEBO COMPARATOR

Drug: Placebo

Interventions

BI 653048 H3PO4 solution DRUG

BI 653048 H3PO4 solution

BI 653048 H3PO4 low dose capsule DRUG

BI 653048 H3PO4 low dose capsule

BI 653048 H3PO4 high dose capsule DRUG

BI 653048 H3PO4 high dose capsule

Placebo DRUG

Placebo

Eligibility Criteria

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

You may qualify if:

• Healthy males according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), clinical laboratory tests
• Age ≥21 years and ≤50 years
• Body Mass Index (BMI) ≥18.5 kg/m2 and BMI ≤29.9 kg/m2
• Signed and dated written informed consent prior to admission to the trial in accordance with Good Clinical Practice (GCP) and the local legislation

You may not qualify if:

• Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
• Any evidence of a clinically relevant concomitant disease
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of the gastrointestinal tract (except appendectomy)
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• History of relevant orthostatic hypotension, fainting spells or blackouts
• Chronic or relevant acute infections
• History of relevant allergy/hypersensitivity (including allergy to drug or its excipients)
• Intake of drugs with a long half-life (\>24 h) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
• Use of drugs which might reasonably influence the results of the trial or that prolong the QT/QTc interval based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial
• Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
• Smoker (\>10 cigarettes or \>3 cigars or \>3 pipes/day)
• Inability to refrain from smoking on trial days
• Alcohol abuse (more than 60 g/day)
• Drug abuse

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Related Publications (1)

• Harcken C, Scholl P, Nabozny G, Thomson D, Bianchi D. Clinical profile of the functionally selective glucocorticoid receptor agonist BI 653048 in healthy male subjects. Expert Opin Investig Drugs. 2019 May;28(5):489-496. doi: 10.1080/13543784.2019.1599859. Epub 2019 Apr 9.

  PMID: 30908082 DERIVED

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 14, 2014
• First Posted: August 15, 2014
• Study Start: November 1, 2008
• Primary Completion: June 1, 2009
• Last Updated: August 15, 2014

Record last verified: 2014-08