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| ID | Type | Description | Link |
|---|---|---|---|
| 2020-006052-40 | EudraCT Number |
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The main objective of this trial is to investigate the relative bioavailability of a single dose of bupropion when given alone (Reference) compared with co-administration (Test) with BI 1358894 in healthy volunteers.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| bupropion alone (Reference (R)) then BI 1358894 + bupropion (Test (T)) | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Elontril | Drug | Tablet |
|
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-time Curve of Bupropion in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) | Area under the concentration-time curve of bupropion in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) is presented. Time Frame: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". | Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
| Maximum Measured Concentration of Bupropion in Plasma (Cmax) | Maximum measured concentration of bupropion in plasma (Cmax) is presented. Timeframe: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". | Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-time Curve of Bupropion in Plasma Over the Time Interval From 0 to Infinity (AUC0-∞) | Area under the concentration-time curve of bupropion in plasma over the time interval from 0 to infinity (AUC0-∞) is presented. Time Frame: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". |
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Inclusion Criteria:
Healthy male or female subjects according to the assessment of the investigator, as based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), and clinical laboratory tests
Age of 18 to 55 years (inclusive)
Body mass index (BMI) of 18.5 to 29.9 kg/m2 (inclusive)
Signed and dated written informed consent prior to admission to the study, in accordance with Good Clinical Practice (GCP) and local legislation
Male subjects, or female subjects who meet any of the following criteria from at least 30 days before the first administration of trial medication until 30 days after trial completion:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| CRS Clinical Research Services Mannheim GmbH | Mannheim | 68167 | Germany |
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| Label | URL |
|---|---|
| Related Info | View source |
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Clinical studies sponsored by Boehringer Ingelheim, phases I to IV, interventional and non-interventional, are in scope for sharing of the raw clinical study data and clinical study documents, except for the following exclusions:
For more details refer to: https://www.mystudywindow.com/msw/datasharing
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All subjects were screened for eligibility prior to participation in the trial. Subjects attended a specialist site which ensured that they (the subjects) strictly met all inclusion and none of the exclusion criteria. Subjects were not to be allocated to a treatment group if any of the entry criteria were violated.
This was a phase I, open-label, two-period fixed sequence trial to evaluate the effect of multiple doses of BI 1358894 on the pharmacokinetics of bupropion in healthy volunteers.
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| ID | Title | Description |
|---|---|---|
| FG000 | Bupropion Alone (Reference (R)) Then BI 1358894 + Bupropion (Test (T)) | Reference (R): Participants were administered on Day 1 of Visit 2 (Period: Reference) orally a single dose of 150 milligram (mg) of bupropion sustained release (SR) tablet (Elontril®) under fed conditions with 240 milliliter (mL) of water. Test (T): From Day -14 to Day 5 of Visit 3 (Period: Test) participants were administered orally once daily 2 film coated tablets of 50 mg of BI 1358894 (total dosage 100 mg/day) under fed conditions with 240 mL of water. On the 15th day of BI 1358894 administration (i.e. Day 1 of Visit 3 (Period: Test)) a single dose of 150 mg of bupropion was co-administered. The single-dose administrations of bupropion in Periods Reference and Test were to be separated by an interval of 21 days. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Reference |
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| Test |
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Treated set (TS): The TS included all subjects who were randomised and treated with at least 1 dose of trial drug.
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| ID | Title | Description |
|---|---|---|
| BG000 | Bupropion Alone (Reference (R)) Then BI 1358894 + Bupropion (Test (T)) | Reference (R): Participants were administered on Day 1 of Visit 2 (Period: Reference) orally a single dose of 150 milligram (mg) of bupropion sustained release (SR) tablet (Elontril®) under fed conditions with 240 milliliter (mL) of water. Test (T): From Day -14 to Day 5 of Visit 3 (Period: Test) participants were administered orally once daily 2 film coated tablets of 50 mg of BI 1358894 (total dosage 100 mg/day) under fed conditions with 240 mL of water. On the 15th day of BI 1358894 administration (i.e. Day 1 of Visit 3 (Period: Test)) a single dose of 150 mg of bupropion was co-administered. The single-dose administrations of bupropion in Periods Reference and Test were to be separated by an interval of 21 days. |
| Units | Counts |
|---|---|
| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Area Under the Concentration-time Curve of Bupropion in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) | Area under the concentration-time curve of bupropion in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) is presented. Time Frame: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". | Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects in the treated set (TS) who provided at least 1 PK endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. | Posted | Geometric Least Squares Mean | Standard Error | hours * nanomole/Liter | Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
Bupropion (BP): From administration (ad.) of BP+5 days of residual effect period (REP), up to 5 days(d). BI 1358894 + Bupropion: From ad. of BP on Day 1 of Visit 3 + 5 days of REP, up to 5 d. "BI 1358894 (BI) alone: From ad. of BI until ad. of BP or until last ad. prior to BP ad. + 14 d" "BI alone (continued): and from ad. of BP + 5 d of REP until last ad. of BI + 14 d of REP, up to 28d.
Treated set (TS): The TS included all subjects who were randomised and treated with at least 1 dose of trial drug.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Bupropion | Participants were administered on Day 1 of Visit 2 (Period: Reference) orally a single dose of 150 milligram (mg) of bupropion sustained release (SR) tablet (Elontril®) under fed conditions with 240 milliliter (mL) of water. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Headache | Nervous system disorders | MedDRA 24.1 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Boehringer Ingelheim, Call Center | Boehringer Ingelheim | 1-800-243-0127 | clintriage.rdg@boehringer-ingelheim.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Jul 29, 2021 | Feb 4, 2025 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Oct 13, 2021 | Feb 4, 2025 | SAP_001.pdf |
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| ID | Term |
|---|---|
| D016642 | Bupropion |
| C000730434 | TRPC inhibitor BI 1358894 |
| ID | Term |
|---|---|
| D011427 | Propiophenones |
| D007659 | Ketones |
| D009930 | Organic Chemicals |
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| BI 1358894 | Drug | Film coated tablet |
|
| Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
| COMPLETED |
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| NOT COMPLETED |
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| Years |
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| Sex: Female, Male | Count of Participants | Participants |
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| Ethnicity (NIH/OMB) | Count of Participants | Participants |
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| Race (NIH/OMB) | Count of Participants | Participants |
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| ID |
|---|
| Title |
|---|
| Description |
|---|
| OG000 | Bupropion Alone (Reference (R)) | Reference (R): Participants were administered on Day 1 of Visit 2 (Period: Reference) orally a single dose of 150 milligram (mg) of bupropion sustained release (SR) tablet (Elontril®) under fed conditions with 240 milliliter (mL) of water. |
| OG001 | BI 1358894 + Bupropion (Test (T)) | Test (T): Participants were administered from Day -14 to Day 5 of Visit 3 (Period: Test) orally once daily 2 film coated tablets of 50 mg of BI 1358894 (total dosage 100 mg/day) under fed conditions with 240 mL of water. On the 15th day of BI 1358894 administration (i.e. Day 1 of Visit 3 (Period: Test)) a single dose of 150 mg of bupropion was co-administered. |
|
|
|
| Primary | Maximum Measured Concentration of Bupropion in Plasma (Cmax) | Maximum measured concentration of bupropion in plasma (Cmax) is presented. Timeframe: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". | Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects in the treated set (TS) who provided at least 1 PK endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. | Posted | Geometric Least Squares Mean | Standard Error | nanomole/Liter | Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
|
|
|
|
| Secondary | Area Under the Concentration-time Curve of Bupropion in Plasma Over the Time Interval From 0 to Infinity (AUC0-∞) | Area under the concentration-time curve of bupropion in plasma over the time interval from 0 to infinity (AUC0-∞) is presented. Time Frame: Within 3 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "bupropion alone (Reference (R))". Within 0.5 hours (h) before and 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 10 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h after bupropion administration for the arm "BI 1358894 + bupropion (Test (T))". | Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects in the treated set (TS) who provided at least 1 PK endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. | Posted | Geometric Least Squares Mean | Standard Error | hours * nanomole/Liter | Up to 120 hours (h) after administration of bupropion (for detailed timeframe please see description). |
|
|
|
|
| 0 |
| 18 |
| 0 |
| 18 |
| 4 |
| 18 |
| EG001 | BI 1358894 | Participants were administered from Day -14 to Day 5 (included) of Visit 3 (Period: Test) orally once daily 2 film coated tablets of 50 mg of BI 1358894 (total dosage 100 mg/day) under fed conditions with 240 mL of water. | 0 | 18 | 0 | 18 | 9 | 18 |
| EG002 | BI 1358894 + Bupropion | Participants were administered from Day 1 to Day 5 of Visit 3 (Period: Test) orally once daily 2 film coated tablets of 50 mg of BI 1358894 (total dosage 100 mg/day) under fed conditions with 240 mL of water. On Day 1 participants were co-administered a single dose of 150 mg of bupropion sustained release (SR) tablet (Elontril®) under fed conditions with 240 mL of water. | 0 | 17 | 0 | 17 | 3 | 17 |
| Dizziness | Nervous system disorders | MedDRA 24.1 | Systematic Assessment |
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| Coordination abnormal | Nervous system disorders | MedDRA 24.1 | Systematic Assessment |
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| Nausea | Gastrointestinal disorders | MedDRA 24.1 | Systematic Assessment |
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| Diarrhoea | Gastrointestinal disorders | MedDRA 24.1 | Systematic Assessment |
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| Flatulence | Gastrointestinal disorders | MedDRA 24.1 | Systematic Assessment |
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| Vomiting | Gastrointestinal disorders | MedDRA 24.1 | Systematic Assessment |
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| Fatigue | General disorders | MedDRA 24.1 | Systematic Assessment |
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| Lymphopenia | Blood and lymphatic system disorders | MedDRA 24.1 | Systematic Assessment |
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| Pharyngitis | Infections and infestations | MedDRA 24.1 | Systematic Assessment |
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| Body temperature increased | Investigations | MedDRA 24.1 | Systematic Assessment |
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| C-reactive protein increased | Investigations | MedDRA 24.1 | Systematic Assessment |
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| Sleep disorder | Psychiatric disorders | MedDRA 24.1 | Systematic Assessment |
|
| Cough | Respiratory, thoracic and mediastinal disorders | MedDRA 24.1 | Systematic Assessment |
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| Hyperhidrosis | Skin and subcutaneous tissue disorders | MedDRA 24.1 | Systematic Assessment |
|
Boehringer Ingelheim (BI) acknowledges that investigators have the right to publish the study results. Investigators shall provide BI with a copy of any publication or presentation for review prior to any submission. Such review will be done with regard to proprietary information, information related to patentable inventions, medical, scientific, and statistical accuracy within 60 days. BI may request a delay of the publication in order to protect BI's intellectual property rights.