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| ID | Type | Description | Link |
|---|---|---|---|
| B1Y-JE-HCLX | Other Identifier | Eli Lilly and Company |
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The purposes of this study are to look at safety, how well the study drug (LY110140) is tolerated, and how much of the study drug gets into the blood stream when given as single dose (SD) and multiple doses (MD) to healthy Japanese male participants. Participants will participate in SD portion for approximately 6 weeks and in MD portion for approximately 10 weeks.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 5 milligrams (mg) LY110140 (SD) | Experimental | 5 mg administered once in the fasted state on Day 1 |
|
| 20 mg LY110140 (SD) | Experimental | 20 mg administered once in the fasted state on Day 1 |
|
| 40 mg LY110140 (SD) | Experimental | 40 mg administered once in the fasted state on Day 1 |
|
| Placebo (MD) | Placebo Comparator | Placebo once daily oral dosing for 28 consecutive days |
|
| 20 mg LY110140 (MD) | Experimental | 20 mg once daily oral dosing for 28 consecutive days |
|
| 40 mg LY110140 (MD) | Experimental | 40 mg once daily oral dosing for 28 consecutive days |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| LY110140 | Drug | Administered orally as capsules |
|
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With One or More Drug-Related Adverse Events (AEs) or Any Serious AEs During the Single-Dose (SD) Period | A drug-related AE was an AE that occurred postdose or was present predose and became more severe postdose and was considered to be related to study treatment. A summary of AEs, regardless of causality, is located in the Reported Adverse Events module. | Baseline up to Day 43 |
| Number of Participants With One or More Drug-Related Adverse Events (AEs) or Any Serious AEs During the Multiple-Dose (MD) Period | A drug-related AE was an AE that occurred postdose or was present predose and became more severe postdose and was considered to be related to study treatment. A summary of AEs, regardless of causality, is located in the Reported Adverse Events module. | Baseline up to Day 70 |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The Cmax of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Predose up to Day 43 |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST) | Eli Lilly and Company | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. | Osaka | 532-0003 |
The study consisted of 2 parts: the open-label, single-dose (SD) period which included 3 cohorts (Cohorts 1 to 3) and the placebo-controlled, multiple-dose (MD) period which included 2 cohorts (Cohorts 4 and 5).
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| ID | Title | Description |
|---|---|---|
| FG000 | 5 mg LY110140 (SD) | Cohort 1: 5-milligram (mg) LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. |
| FG001 | 20 mg LY110140 (SD) | Cohort 2: 20-mg LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. |
| FG002 | 40 mg LY110140 (SD) | Cohort 3: 40-mg LY110140 (fluoxetine hydrochloride) dose (two 20-mg LY110140 capsules) orally administered once, in a fasted state, during the SD period. |
| FG003 | Placebo (MD) | Participants, in Cohorts 4 and 5, who received a placebo capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28 participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| FG004 | 20 mg LY110140 (MD) | Participants, in Cohort 4, who received 20-mg LY110140 (fluoxetine hydrochloride) capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28, participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| FG005 | 40 mg LY110140 (MD) | Participants, in Cohort 5, who received two 20-mg LY110140 (fluoxetine hydrochloride) capsules, orally administered once daily for 28 days, during the MD period. On Days 1 and 28, participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
All randomized participants.
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| ID | Title | Description |
|---|---|---|
| BG000 | 5 mg LY110140 (SD) | Cohort 1: 5-milligram (mg) LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. |
| BG001 | 20 mg LY110140 (SD) |
| Units | Counts |
|---|---|
| Participants |
|
| 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 | Number of Participants With One or More Drug-Related Adverse Events (AEs) or Any Serious AEs During the Single-Dose (SD) Period | A drug-related AE was an AE that occurred postdose or was present predose and became more severe postdose and was considered to be related to study treatment. A summary of AEs, regardless of causality, is located in the Reported Adverse Events module. | Randomized participants, in Cohorts 1, 2, and 3, who received at least 1 dose of study drug and had at least 1 postdose safety assessment. | Posted | Number | participants | Baseline up to Day 43 |
|
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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 | 5 mg LY110140 (SD) | Cohort 1: 5-milligram (mg) LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Atrioventricular block first degree | Cardiac disorders | MedDRA 14.1 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Chief Medical Officer | Eli Lilly and Company | 800-545-5979 |
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| ID | Term |
|---|---|
| D005473 | Fluoxetine |
| ID | Term |
|---|---|
| D011437 | Propylamines |
| D000588 | Amines |
| D009930 | Organic Chemicals |
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|
| Placebo | Drug | Administered orally as capsules in the placebo arm and to maintain the blind in the 20 mg LY110140 (MD) arm |
|
| Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to Last Time Point [AUC(0-tlast)] of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-tlast) of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Predose up to Day 43 |
| Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-infinity)] of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-infinity) of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Predose up to Day 43 |
| Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The Cmax of plasma total fluoxetine and norfluoxetine on Day 1 and Day 28 of the MD period is reported. | Days 1 and 28 |
| Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to 24 Hours [AUC(0-24)] of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-24) of plasma total fluoxetine and norfluoxetine on Day 1 of the MD period is reported. | Day 1 |
| Pharmacokinetics: Area Under the Concentration-Time Curve for Dosing Interval (Tau) at Steady State [AUC(Tau,Steady State)] of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(tau,steady state) of plasma total fluoxetine and norfluoxetine during the MD period is reported. | Predose up to Day 28 |
| Change From Baseline in Bazett's and Fridericia's Corrected QT (QTcB and QTcF) Intervals | The number of participants with a maximum increase from baseline in 12-lead electrocardiogram (ECG) QTcB and QTcF intervals >30 milliseconds (ms) and >60 ms for the single-dose (SD) and multiple-dose (MD) periods is reported. | Baseline, up to Day 43 (SD period) and Baseline, up to Day 70 (MD period) |
| Japan |
Cohort 2: 20-mg LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period.
| BG002 | 40 mg LY110140 (SD) | Cohort 3: 40-mg LY110140 (fluoxetine hydrochloride) dose (two 20-mg LY110140 capsules) orally administered once, in a fasted state, during the SD period. |
| BG003 | Placebo (MD) | Participants, in Cohorts 4 and 5, who received a placebo capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28 participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| BG004 | 20 mg LY110140 (MD) | Participants, in Cohort 4, who received 20-mg LY110140 (fluoxetine hydrochloride) capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28, participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| BG005 | 40 mg LY110140 (MD) | Participants, in Cohort 5, who received two 20-mg LY110140 (fluoxetine hydrochloride) capsules, orally administered once daily for 28 days, during the MD period. On Days 1 and 28, participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. |
| BG006 | Total | Total of all reporting groups |
| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race/Ethnicity, Customized | Number | participants |
|
| Region of Enrollment | Number | participants |
|
| Cytochrome P450 2D6 (CYP2D6) intermediate and extensive metabolizers | Based upon a laboratory deoxyribonucleic acid (DNA) screening test, participants were identified as having either the CYP2D6 intermediate metabolizer genotype or the CYP2D6 extensive metabolizer genotype. Intermediate metabolizers were individuals who carry 1 functional (normal or decreased allele) and a null or decreased allele. Extensive metabolizers were individuals with 2 fully active enzyme alleles. | Number | participants |
|
| 20 mg LY110140 (SD) |
Cohort 2: 20-mg LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. |
| OG002 | 40 mg LY110140 (SD) | Cohort 3: 40-mg LY110140 (fluoxetine hydrochloride) dose (two 20-mg LY110140 capsules) orally administered once, in a fasted state, during the SD period. |
|
|
| Primary | Number of Participants With One or More Drug-Related Adverse Events (AEs) or Any Serious AEs During the Multiple-Dose (MD) Period | A drug-related AE was an AE that occurred postdose or was present predose and became more severe postdose and was considered to be related to study treatment. A summary of AEs, regardless of causality, is located in the Reported Adverse Events module. | Randomized participants, in Cohorts 4 and 5, who received at least 1 dose of study drug or placebo and had at least 1 postdose safety assessment. | Posted | Number | participants | Baseline up to Day 70 |
|
|
|
| Secondary | Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The Cmax of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Randomized participants, in Cohorts 1, 2, and 3, who received at least 1 dose of study drug and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | Predose up to Day 43 |
|
|
|
| Secondary | Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to Last Time Point [AUC(0-tlast)] of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-tlast) of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Randomized participants, in Cohorts 1, 2, and 3, who received at least 1 dose of study drug and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms*hour per milliliter (ng*hr/mL) | Predose up to Day 43 |
|
|
|
| Secondary | Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-infinity)] of Single Dose (SD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-infinity) of plasma total fluoxetine and norfluoxetine during the SD period is reported. | Randomized participants, in Cohorts 1, 2, and 3, who received at least 1 dose of study drug and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms*hour per milliliter (ng*hr/mL) | Predose up to Day 43 |
|
|
|
| Secondary | Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The Cmax of plasma total fluoxetine and norfluoxetine on Day 1 and Day 28 of the MD period is reported. | Randomized participants, in Cohorts 4 and 5, who received at least 1 dose of study drug (excluding placebo) and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | Days 1 and 28 |
|
|
|
| Secondary | Pharmacokinetics: Area Under the Concentration-Time Curve From Zero to 24 Hours [AUC(0-24)] of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(0-24) of plasma total fluoxetine and norfluoxetine on Day 1 of the MD period is reported. | Randomized participants, in Cohorts 4 and 5, who received at least 1 dose of study drug (excluding placebo) and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms*hour per milliliter (ng*hr/mL) | Day 1 |
|
|
|
| Secondary | Pharmacokinetics: Area Under the Concentration-Time Curve for Dosing Interval (Tau) at Steady State [AUC(Tau,Steady State)] of Multiple Doses (MD) of LY110140 | Study drug was administered as LY110140 (fluoxetine hydrochloride) and its active portion, fluoxetine, was metabolized to norfluoxetine in the body. The AUC(tau,steady state) of plasma total fluoxetine and norfluoxetine during the MD period is reported. | Randomized participants, in Cohorts 4 and 5, who received at least 1 dose of study drug (excluding placebo) and had evaluable pharmacokinetic data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms*hour per milliliter (ng*hr/mL) | Predose up to Day 28 |
|
|
|
| Secondary | Change From Baseline in Bazett's and Fridericia's Corrected QT (QTcB and QTcF) Intervals | The number of participants with a maximum increase from baseline in 12-lead electrocardiogram (ECG) QTcB and QTcF intervals >30 milliseconds (ms) and >60 ms for the single-dose (SD) and multiple-dose (MD) periods is reported. | Randomized participants, in Cohorts 1, 2, and 3, who received at least 1 dose of study drug and had at least 1 postdose safety assessment. | Posted | Number | participants | Baseline, up to Day 43 (SD period) and Baseline, up to Day 70 (MD period) |
|
|
|
|
| 0 |
| 8 |
| 3 |
| 8 |
| EG001 | 20 mg LY110140 (SD) | Cohort 2: 20-mg LY110140 (fluoxetine hydrochloride) capsule orally administered once, in a fasted state, during the SD period. | 0 | 8 | 1 | 8 |
| EG002 | 40 mg LY110140 (SD) | Cohort 3: 40-mg LY110140 (fluoxetine hydrochloride) dose (two 20-mg LY110140 capsules) orally administered once, in a fasted state, during the SD period. | 0 | 8 | 2 | 8 |
| EG003 | Placebo (MD) | Participants, in Cohorts 4 and 5, who received a placebo capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28 participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. | 0 | 8 | 3 | 8 |
| EG004 | 20 mg LY110140 (MD) | Participants, in Cohort 4, who received 20-mg LY110140 (fluoxetine hydrochloride) capsule, orally administered once daily for 28 days, during the MD period. On Days 1 and 28 participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. | 0 | 12 | 3 | 12 |
| EG005 | 40 mg LY110140 (MD) | Participants, in Cohort 5, who received two 20-mg LY110140 (fluoxetine hydrochloride) capsules, orally administered once daily for 28 days, during the MD period. On Days 1 and 28 participants were required to fast at least 8 hours prior to dosing and 4 hours postdose. | 0 | 12 | 6 | 12 |
| Conjunctivitis allergic | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Eye discharge | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Ocular hyperaemia | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
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| Haemorrhoids | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Proctalgia | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Stomatitis | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Chills | General disorders | MedDRA 14.1 | Systematic Assessment |
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| Pyrexia | General disorders | MedDRA 14.1 | Systematic Assessment |
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| Tonsillitis | Infections and infestations | MedDRA 14.1 | Systematic Assessment |
|
| Excoriation | Injury, poisoning and procedural complications | MedDRA 14.1 | Systematic Assessment |
|
| Alanine aminotransferase increased | Investigations | MedDRA 14.1 | Systematic Assessment |
|
| Aspartate aminotransferase increased | Investigations | MedDRA 14.1 | Systematic Assessment |
|
| Blood triglycerides increased | Investigations | MedDRA 14.1 | Systematic Assessment |
|
| White blood cell count decreased | Investigations | MedDRA 14.1 | Systematic Assessment |
|
| White blood cell count increased | Investigations | MedDRA 14.1 | Systematic Assessment |
|
| Arthralgia | Musculoskeletal and connective tissue disorders | MedDRA 14.1 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
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| Anxiety | Psychiatric disorders | MedDRA 14.1 | Systematic Assessment |
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| Cough | Respiratory, thoracic and mediastinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Oropharyngeal pain | Respiratory, thoracic and mediastinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Rhinorrhoea | Respiratory, thoracic and mediastinal disorders | MedDRA 14.1 | Systematic Assessment |
|
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| Title | Measurements |
|---|---|
|
| Norfluoxetine |
|
| Norfluoxetine |
|
| Norfluoxetine |
|
| Day 1, Norfluoxetine |
|
| Day 28, Norfluoxetine |
|
| QTcF >30 ms |
|
| QTcB >60 ms |
|
| QTcF >60 ms |
|