Phase 1
Completed N=35
A Study of LY2140023 in Healthy Males and Females
Healthy Volunteers
Source: ClinicalTrials.gov NCT01591330 ↗
Enrolled (actual)
35
Serious AEs
0.0%
Results posted
Sep 2021
Primary outcomePrimary: Pharmacokinetics: Maximum Concentration (Cmax) of LY2140023 — 277; 290; 304; 284 nanograms per milliliter (ng/mL)
Summary
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics: Maximum Concentration (Cmax) of LY2140023 |
277; 290; 304; 284 | — |
| PRIMARY Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Last Time Point of Measurable Concentration (AUC[0-tlast]) of LY2140023 |
1200; 1190; 1210; 1210 | — |
| PRIMARY Pharmacokinetics: Maximum Concentration (Cmax) of LY404039 (Active Moiety) |
476; 485; 494; 490 | — |
| 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) |
2640; 2640; 2710; 2700 | — |
| SECONDARY Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of LY2140023 |
3.00; 3.00; 3.00; 3.00 | — |
| SECONDARY Pharmacokinetics: Terminal Half Life (t1/2) of LY2140023 |
2.13; 1.93; 2.02; 2.13 | — |
| SECONDARY Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY2140023 |
66.8; 67.0; 65.9; 66.2 | — |
| SECONDARY Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY2140023 |
205; 187; 192; 204 | — |
| SECONDARY Pharmacokinetics: Time of Maximum Observed Drug Concentrations (Tmax) of LY404039 (Active Moiety) |
4.00; 4.00; 4.00; 4.00 | — |
| SECONDARY Pharmacokinetics: Terminal Half Life (t1/2) of LY404039 (Active Moiety) |
3.10; 3.05; 2.95; 3.07 | — |
| SECONDARY Pharmacokinetics: Apparent Total Body Clearance (CL/F) of LY404039 (Active Moiety) |
19.3; 19.3; 18.9; 18.9 | — |
| SECONDARY Pharmacokinetics: Volume of Distribution During the Terminal Phase (Vz/F) of LY404039 (Active Moiety) |
86.3; 85.0; 80.4; 83.6 | — |
Eligibility Criteria
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:
- female participants of child-bearing potential who test negative for pregnancy at screening and agree to use a reliable method of birth control for the duration of the study and for at least 3 months after the last dose of LY2140023
- female participants who are of non-childbearing potential (that is, postmenopausal or permanently sterile following hysterectomy, bilateral salpingectomy, or confirmed tubal occlusion [not tubal ligation]). Postmenopausal is defined as no menses for at least 1 year, or a plasma follicle stimulating hormone (FSH) value of >40 milli-international units per liter (mIU/mL), unless the participant is taking hormone replacement therapy
- 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:
- one or more seizures (except for a single simple febrile seizure [lacking focality and lasting less than 15 minutes, not associated with a central nervous system (CNS) infection or severe metabolic disturbance] as a child between ages 6 months to 5 years)
- head trauma with loss of consciousness or a post-concussive syndrome within 1 year or lifetime history of head trauma with persistent neurological deficit (focal or diffuse)
- uncontrolled migraine or transient ischemic attack (TIA) within 1 year and/or stroke with persistent neurological deficit (focal or diffuse); uncontrolled migraine is defined as migraine attacks that produce headache lasting up to 72 hours and are often accompanied by associated symptoms (nausea, photophobia, and phonophobia) that impair well-being and disrupt social functioning; TIA is defined as "mini-stroke" caused by temporary disturbance of blood supply to an area of the brain, which results in a sudden, brief decrease in brain function
- CNS infection with persistent
Data sourced from ClinicalTrials.gov (NCT01591330). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.