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| ID | Type | Description | Link |
|---|---|---|---|
| I4O-MC-BACD | Other Identifier | Eli Lilly and Company |
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This open-label study is being conducted to determine the metabolism and physiological disposition of radiolabeled LY2886721 after a single dose in healthy male participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Radiolabeled LY2886721 | Experimental | Single 25 milligram (mg) oral dose containing 80 microCuries of radiolabeled LY2886721 |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| LY2886721 | Drug | Administered orally |
|
| Measure | Description | Time Frame |
|---|---|---|
| Percentage of Urinary and Fecal Excretion of LY2886721 Radioactivity Over Time | Urinary and fecal excretion of LY2886721 radioactivity over time was expressed as a percentage of the total radioactive dose administered. The amount of drug-related material excreted in urine and feces (Ae) at a specific collection interval (i) was calculated as the product of radioactivity concentration and volume or weight. The Ae values for each collection interval were then summed and calculated as Total Ae=Ae(i1)+Ae(i2)+Ae(in). The percentage of the total radiolabeled dose administered that was excreted in feces or urine=[(Total Ae)/(Total radioactive dose administered)]*100. | Predose up to 7 days (168 hours) postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Plasma Pharmacokinetics (PK) of LY2886721: Area Under the Concentration-Time Curve From Time 0 to Infinity [AUC(0 to Inf)] | Predose up to 4 days (96 hours) postdose | |
| PK of Radioactivity: AUC(0 to Inf) | AUC(0 to inf) for plasma and whole blood total radioactivity is reported as hours*nanogram equivalents per milliliter (h*ng Eq/mL). |
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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. | Madison | Wisconsin |
Participants were considered to have completed the study at 9 days postdose or earlier if ≥90% of administered radioactivity recovered or 24-hour urine and fecal samples from 2 consecutive collections each had radioactivity levels <1.0% of total administered radioactivity in urine and feces combined.
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| ID | Title | Description |
|---|---|---|
| FG000 | [^14C]-LY2886721 | Single 25-milligram (mg) LY2886721 dose containing approximately 80 microCuries (μCi) of carbon-14-labeled LY2886721 ([^14C]-LY2886721), administered as an oral solution. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
All enrolled participants.
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| ID | Title | Description |
|---|---|---|
| BG000 | [^14C]-LY2886721 | Single 25-mg LY2886721 dose containing approximately 80 μCi of [^14C]-LY2886721, administered as an oral solution. |
| 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 | Percentage of Urinary and Fecal Excretion of LY2886721 Radioactivity Over Time | Urinary and fecal excretion of LY2886721 radioactivity over time was expressed as a percentage of the total radioactive dose administered. The amount of drug-related material excreted in urine and feces (Ae) at a specific collection interval (i) was calculated as the product of radioactivity concentration and volume or weight. The Ae values for each collection interval were then summed and calculated as Total Ae=Ae(i1)+Ae(i2)+Ae(in). The percentage of the total radiolabeled dose administered that was excreted in feces or urine=[(Total Ae)/(Total radioactive dose administered)]*100. | All enrolled participants. | Posted | Mean | Standard Deviation | percentage of radioactive dose | Predose up to 7 days (168 hours) postdose |
|
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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 | [^14C]-LY2886721 | Single 25-mg LY2886721 dose containing approximately 80 μCi of [^14C]-LY2886721, administered as an oral solution. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Application site erythema | General disorders | MedDRA 14.0 | Systematic Assessment |
Assay sensitivity of plasma and whole blood radioactivity were not generally quantifiable after 24-hours postdose. Consequently, the AUC(0-inf) estimate for total radioactivity in plasma and whole blood should be considered underestimated.
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Chief Medical Officer | Eli Lilly and Company | 800-545-5979 |
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| ID | Term |
|---|---|
| C000596181 | N-(3-(2-amino-4a,5,7,7a-tetrahydro-4H-furo(3,4-d)(1,3)thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide |
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| Predose up to 4 days (96 hours) postdose |
| Plasma PK of LY2886721: Maximum Observed Concentration (Cmax) | Predose up to 4 days (96 hours) postdose |
| PK of Radioactivity: Cmax | The Cmax of total radioactivity in plasma and whole blood are reported as nanogram equivalents per milliliter (ng Eq/mL). | Predose up to 4 days (96 hours) postdose |
| Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Plasma | The metabolites of LY2886721 were identified using a high performance liquid chromatography (HPLC) chromatogram. The relative abundance of LY2886721 and its metabolites in plasma were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | 1 to 8 hours postdose |
| Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Urine | The metabolites of LY2886721 were identified using an HPLC chromatogram. The relative abundance of LY2886721 and its metabolites in urine were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | 0 to 72 hours postdose |
| Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Feces | The metabolites of LY2886721 were identified using an HPLC chromatogram. The relative abundance of LY2886721 and its metabolites in feces were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | 0 to 144 hours postdose |
| United States |
| years |
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| Sex/Gender, Customized | 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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| Region of Enrollment | Count of Participants | Participants |
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| Secondary | Plasma Pharmacokinetics (PK) of LY2886721: Area Under the Concentration-Time Curve From Time 0 to Infinity [AUC(0 to Inf)] | All enrolled participants. | Posted | Geometric Mean | Geometric Coefficient of Variation | hours*nanograms per milliliter (h*ng/mL) | Predose up to 4 days (96 hours) postdose |
|
|
|
| Secondary | PK of Radioactivity: AUC(0 to Inf) | AUC(0 to inf) for plasma and whole blood total radioactivity is reported as hours*nanogram equivalents per milliliter (h*ng Eq/mL). | All enrolled participants. | Posted | Geometric Mean | Geometric Coefficient of Variation | h*ng Eq/mL | Predose up to 4 days (96 hours) postdose |
|
|
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| Secondary | Plasma PK of LY2886721: Maximum Observed Concentration (Cmax) | All enrolled participants. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | Predose up to 4 days (96 hours) postdose |
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| Secondary | PK of Radioactivity: Cmax | The Cmax of total radioactivity in plasma and whole blood are reported as nanogram equivalents per milliliter (ng Eq/mL). | All enrolled participants. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng Eq/mL | Predose up to 4 days (96 hours) postdose |
|
|
|
| Secondary | Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Plasma | The metabolites of LY2886721 were identified using a high performance liquid chromatography (HPLC) chromatogram. The relative abundance of LY2886721 and its metabolites in plasma were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | All enrolled participants. | Posted | Mean | Standard Deviation | percentage of recovered radioactivity | 1 to 8 hours postdose |
|
|
|
| Secondary | Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Urine | The metabolites of LY2886721 were identified using an HPLC chromatogram. The relative abundance of LY2886721 and its metabolites in urine were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | All enrolled participants. | Posted | Mean | Standard Deviation | percentage of recovered radioactivity | 0 to 72 hours postdose |
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|
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| Secondary | Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Feces | The metabolites of LY2886721 were identified using an HPLC chromatogram. The relative abundance of LY2886721 and its metabolites in feces were reported as a percentage of recovered radioactivity and calculated by dividing the sum of the radioactive content of fractions contributing to a particular peak by the sum of the radioactive content of all fractions in the radio chromatogram, then multiplying by 100. Radioactivity corresponds to 80 μCi [^14C]-LY2886721. | All enrolled participants. | Posted | Mean | Standard Deviation | percentage of recovered radioactivity | 0 to 144 hours postdose |
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|
| 0 |
| 6 |
| 3 |
| 6 |
| Vessel puncture site haematoma | General disorders | MedDRA 14.0 | Systematic Assessment |
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| Headache | Nervous system disorders | MedDRA 14.0 | Systematic Assessment |
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| Predominant Metabolite 2h Postdose |
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| LY2886721 (parent) 4h Postdose |
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| Predominant Metabolite 4h Postdose |
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| LY2886721 (parent) 8h Postdose |
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| Predominant Metabolite 8h Postdose |
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