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| ID | Type | Description | Link |
|---|---|---|---|
| H8Y-MC-HBCZ | Other Identifier | Eli Lilly and Company |
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The study will evaluate the effect of activated charcoal on absorption of LY2140023. The study involves a single dose of 80 milligrams (mg) LY2140023 taken as 1 tablet by mouth 2 times during study (once with activated charcoal, once without activated charcoal). This study will last approximately 16 days, not including screening. Screening is required within 28 days prior to study entry.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 80 mg LY2140023 | Experimental | Single oral dose of 80 milligrams (mg) LY2140023 administered alone |
|
| 80 mg LY2140023 + 75 g aqueous activated charcoal | Experimental | Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 grams (g) aqueous activated charcoal. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| LY2140023 | Drug |
| ||
| Aqueous activated charcoal |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2140023 | Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal. | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2140023 | Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal. | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY404039 (Active Moiety) | Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal. | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY404039 (Active Moiety) | Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal. | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
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Inclusion Criteria:
are healthy males or females, as determined by medical history and physical examination
male participants agree to use a reliable method of birth control during the study and for 3 months following the last dose of LY2140023, and agree not to donate sperm for 3 months following the last dose of LY2140023
female participants:
have given written informed consent approved by Lilly and the chosen ethical review board (ERB)
Exclusion Criteria:
are currently enrolled in, have completed or discontinued within the last 90 days from, a clinical trial involving an investigational product other than the investigational product used in this study; or are concurrently enrolled in any other type of medical research judged not to be scientifically or medically compatible with this study
have known allergies to LY2140023 or LY404039, related compounds, activated charcoal, or any components of the formulation
are participants who have previously withdrawn from this study or any other study investigating LY2140023 after receiving at least 1 dose of LY2140023
show evidence or any history of significant active neuropsychiatric disease (for example, manic depressive illness, schizophrenia, depression)
have increased risk of seizures based on a history of:
show evidence of active renal disease (for example, diabetic renal disease, polycystic kidney disease) or creatinine clearance less than 90 milliliters per minute (mL/min) as determined by the Cockroft Gault formula
show evidence or any history of known substance dependence or abuse at any time (according to Diagnostic and Statistical Manual of Mental Disorders [DSM-IV] diagnosis), or regularly use known drugs of abuse and/or show positive findings on urinary drug screening
have a clinically significant abnormality in the neurological examination
participants judged prior to randomization to be at suicidal risk by the investigator
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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. | Leeds | West Yorkshire | LS2 9LH |
This was a 2-period crossover study. Participants received single doses of LY2140023 on 2 different occasions: 1) LY2140023 administered alone (Treatment A) and 2) LY2140023 administered and followed 1 hour later by a single dose of aqueous activated charcoal (Treatment B). Participants were randomized to Treatment Sequence AB or BA.
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| ID | Title | Description |
|---|---|---|
| FG000 | First LY2140023 Alone, Then LY2140023 + Activated Charcoal | Period 1: Single oral dose of 80 milligrams (mg) LY2140023 administered alone Period 2: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 grams (g) aqueous activated charcoal There was a washout period of at least 3 days between dosing occasions. |
| FG001 | First LY2140023 + Activated Charcoal, Then LY2140023 Alone | Period 1: Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal Period 2: Single oral dose of 80 mg LY2140023 administered alone There was a washout period of at least 3 days between dosing occasions. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Period 1 |
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| |||||||||||||||||||||||||||
| Period 2 |
|
All participants
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| ID | Title | Description |
|---|---|---|
| BG000 | All Participants | This was 2-period crossover study. Participants received single oral doses of LY2140023 on 2 different occasions: 1) 80 mg LY2140023 administered alone (Treatment A) and 2) 80 mg LY2140023 administered and followed 1 hour later by a single oral dose of 75 g aqueous activated charcoal (Treatment B). Participants were randomly assigned to treatment sequence AB or BA. |
| 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 | Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2140023 | Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal. | Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable Cmax data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 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 | 80 mg LY2140023 | Single oral dose of 80 mg LY2140023 administered alone |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Nausea | Gastrointestinal 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 |
|---|---|
| C534551 | LY 2140023 |
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| Drug |
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| United Kingdom |
| Received Activated Charcoal |
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| COMPLETED |
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| NOT COMPLETED |
|
|
| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race/Ethnicity, Customized | Number | participants |
|
| Region of Enrollment | Number | participants |
|
Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal |
|
|
| Primary | Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2140023 | Venous blood samples were collected for pharmacokinetic parameter estimates for LY2140023 alone and in the presence of aqueous activated charcoal. | Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable AUC(0-inf) data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram hours per milliliter (ng*h/mL) | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Primary | Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY404039 (Active Moiety) | Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal. | Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable Cmax data. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Primary | Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY404039 (Active Moiety) | Venous blood samples were collected for pharmacokinetic parameter estimates for LY404039 alone and in the presence of aqueous activated charcoal. | Participants who received study drug(s), did not have an incidence of vomiting following administration of LY2140023, and had evaluable AUC(0-inf) data. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | Predose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| 0 |
| 22 |
| 16 |
| 22 |
| EG001 | 80 mg LY2140023 + 75 g Aqueous Activated Charcoal | Single oral dose of 80 mg LY2140023 followed 1 hour later by single oral dose of 75 g aqueous activated charcoal | 0 | 24 | 13 | 24 |
| Vomiting | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
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| Feeling hot | General disorders | MedDRA 14.1 | Systematic Assessment |
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| Dizziness | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
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| Headache | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
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