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| ID | Type | Description | Link |
|---|---|---|---|
| H8Y-MC-HBCY | Other Identifier | Eli Lilly and Company |
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The study will evaluate the effect of different particle size of LY2140023. The study involves 4 single doses of 80 milligrams (mg) LY2140023 taken as 1 tablet by mouth with a washout period of at least 3 days between doses. This study will last approximately 60 days not including screening. Screening is required within 30 days prior to study entry.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| LY2140023 Reference Form | Experimental | LY2140023: 80 mg, administered once, orally. There is a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
|
| LY2140023 Test-Low | Experimental | LY2140023: 80 mg, low particle size, administered once, orally. There is a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
|
| LY2140023 Test-Medium | Experimental | LY2140023: 80 mg, medium particle size, administered once, orally. There is a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
|
| LY2140023 Test-High | Experimental | LY2140023: 80 mg, high particle size, administered once, orally. There is a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| LY2140023 Reference form | Drug | 80-mg tablet administered orally |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics: Maximum Concentration (Cmax) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose | |
| Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose | |
| Pharmacokinetics: Maximum Concentration (Cmax) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose | |
| Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose | |
| Pharmacokinetics: Terminal Half Life (t1/2) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
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Inclusion Criteria:
are overtly 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 a body mass index (BMI) of 19 to 32 kilograms per meter squared (kg/m^2), inclusive, at the time of screening
have clinical laboratory test results within normal reference ranges for the population or investigator site or results with acceptable deviations that are judged to be not clinically significant by the investigator
have venous access sufficient to allow for blood sampling as per the protocol
are reliable and willing to make themselves available for the duration of the study and are willing to follow study procedures
have given written informed consent approved by Lilly and the chosen ethical review board (ERB)
Exclusion Criteria:
are currently enrolled in or have completed or discontinued within the last 90 days from a clinical trial involving an investigational product, 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, LY404039, related compounds, or any components of the formulation
are persons who have previously completed or withdrawn from this study or any other study investigating LY2140023 and have previously received the investigational product
have an abnormality in the 12-lead electrocardiogram (ECG) that, in the opinion of the investigator, increases the risks associated with participating in the study
have an abnormal blood pressure or pulse rate as determined by the investigator
have a history or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the study medication; or of interfering with the interpretation of data
have evidence or any history of significant active neuropsychiatric disease
have increased risk of seizures based on a history of:
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
show evidence of human immunodeficiency (HIV) virus infection and/or positive human HIV antibodies
show evidence of hepatitis C and/or positive hepatitis C antibody
show evidence of hepatitis B and/or positive hepatitis B surface antigen
are women with a positive pregnancy test or women who are lactating
intend to use over-the-counter (OTC) or prescription medication within 14 days prior to dosing of LY2140023
have donated blood of more than 500 milliliters (mL) within the 3 months prior to screening, or plan to donate blood within the 3 months after the last dose
have an average weekly alcohol intake that exceeds 28 units per week (males) and 21 units per week (females), or are unwilling to stop alcohol consumption for 48 hours prior to check-in for each treatment period until discharge in each period (1 unit = 12 ounces [oz] or 360 mL of beer; 5 oz or 150 mL of wine; 1.5 oz or 45 mL of distilled spirits)
have a clinically significant abnormality in the neurological examination
participants judged prior to randomization to be at suicidal risk by the investigator
participants who are unwilling to refrain from tobacco- or nicotine-containing products while in the Clinical Research Unit (CRU) or are unable to abide by CRU restrictions
show evidence of pruritus or skin exfoliation
have an eosinophil count > 1.5 x 10^9 per liter (L)
show evidence of active renal disease or creatinine clearance (CrCl) less than 90 milliliters per minute (mL/min) (as calculated by the Cockcroft-Gault equation)
in the opinion of the investigator or sponsor, are unsuitable for inclusion in the study
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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 |
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| ID | Title | Description |
|---|---|---|
| FG000 | Sequence 1 | LY2140023 80 milligrams (mg) reference form (RF) in Period 1, LY2140023 80 mg Test-low in Period 2, LY2140023 80 mg Test-medium in Period 3, LY2140023 80 mg Test-high in Period 4. Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
| FG001 | Sequence 2 | LY2140023 80 mg Test-low in Period 1, LY2140023 80 mg Test-high in Period 2, LY2140023 80 mg RF Period 3, LY2140023 80 mg Test-medium in Period 4. Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
| FG002 | Sequence 3 | LY2140023 80 mg Test-high in Period 1, LY2140023 80 mg Test-medium in Period 2, LY2140023 80 mg Test-low in Period 3, LY2140023 80 mg RF in Period 4. Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
| FG003 | Sequence 4 | LY2140023 80 mg Test-medium in Period 1, LY2140023 80 mg RF in Period 2, LY2140023 80 mg Test-high in Period 3, LY2140023 80 mg Test-low in Period 4. Each LY2140023 dose was administered once, orally. There was a minimum 3-day washout period between dosing in one period and dosing in the next dosing period. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Period 1 |
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| Washout of at Least 3 Days |
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| Period 2 |
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| Washout of at Least 3 Days |
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| Period 3 |
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| Washout of at Least 3 Days |
| ||||||||||||||||||||||
| Period 4 |
|
All participants who received at least 1 dose of study drug
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| ID | Title | Description |
|---|---|---|
| BG000 | Overall Study | All participants |
| 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 Concentration (Cmax) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms per milliliter (ng/mL) | Predose and at 0.5, 1, 2, 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 | LY2140023 Reference Form | LY2140023: 80 mg, administered once, orally. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Abdominal pain upper | 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 |
|---|---|
| C000626254 | pomaglumetad methionil |
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| LY2140023 Test-Low | Drug | 80-mg tablet administered orally |
|
|
| LY2140023 Test-Medium | Drug | 80-mg tablet administered orally |
|
|
| LY2140023 Test-High | Drug | 80-mg tablet administered orally |
|
|
| Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY2140023 | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Time of Maximum Observed Drug Concentrations (Tmax) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Terminal Half Life (t1/2) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY404039 (Active Moiety) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
| United Kingdom |
| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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| COMPLETED |
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| NOT COMPLETED |
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| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Race/Ethnicity, Customized | Number | participants |
|
| Region of Enrollment | Number | participants |
|
| Weight | Mean | Standard Deviation | kilograms (kg) |
|
| Body Mass Index (BMI) | BMI is an estimate of body fat based on body weight divided by height squared. | Mean | Standard Deviation | kilograms per meter squared (kg/m^2) |
|
| LY2140023 Test-Medium |
LY2140023: 80 mg, medium particle size, administered once, orally. |
| OG003 | LY2140023 Test-High | LY2140023: 80 mg, high particle size, administered once, orally. |
|
|
| Primary | Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanograms*hours per milliliter (ng*h/mL) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Primary | Pharmacokinetics: Maximum Concentration (Cmax) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng/mL | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Primary | Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Geometric Mean | Geometric Coefficient of Variation | ng*h/mL | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Median | Full Range | hours (h) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Terminal Half Life (t1/2) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Geometric Mean | Full Range | h | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
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| Secondary | Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Geometric Mean | Geometric Coefficient of Variation | liters per hour (L/h) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY2140023 | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY2140023 plasma concentration data. | Posted | Geometric Mean | Geometric Coefficient of Variation | Liters (L) | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Time of Maximum Observed Drug Concentrations (Tmax) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Median | Full Range | h | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Terminal Half Life (t1/2) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Geometric Mean | Full Range | h | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| Secondary | Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Geometric Mean | Geometric Coefficient of Variation | L/h | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
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| Secondary | Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY404039 (Active Moiety) | All participants who received at least 1 dose of study drug, did not vomit within 5 hours postdose, and have evaluable LY404039 (active moiety) plasma concentration data following administration of LY2140023. | Posted | Geometric Mean | Geometric Coefficient of Variation | L | Predose and at 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 12, 16, and 24 hours postdose |
|
|
|
| 0 |
| 35 |
| 17 |
| 35 |
| EG001 | LY2140023 Test-Low | LY2140023: 80 mg, low particle size, administered once, orally. | 0 | 33 | 15 | 33 |
| EG002 | LY2140023 Test-Medium | LY2140023: 80 mg, medium particle size, administered once, orally. | 0 | 32 | 12 | 32 |
| EG003 | LY2140023 Test-High | LY2140023: 80 mg, high particle size, administered once, orally. | 0 | 32 | 16 | 32 |
| Diarrhoea | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Vomiting | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Feeling hot | General disorders | MedDRA 14.1 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Presyncope | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Somnolence | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
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