A Study of Nociceptin/Orphanin FQ Peptide Receptor Occupancy in Healthy Subjects

NCT01404091 | Completed Phase 1

• 2 other identifiers: 14333I5J-MC-NOAB
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this trial is to conduct an assessment of brain nociceptin/orphanin FQ peptide (NOP) receptor occupancy (RO) in healthy subjects.

Conditions

Depression

Outcome Measures

Primary Outcomes (1)

• Change from Baseline in Nociceptin/Orphanin FQ Peptide (NOP) Receptor Occupancy at Day 2

  Baseline, Day 2 (occurs 1-4 weeks after baseline)

Secondary Outcomes (2)

• Pharmacokinetics: maximal plasma concentration (Cmax) of LY2940094

  Predose, up to 29 hours post dose

• Pharmacokinetics: area under the concentration- time curve (AUC) of LY2940094

  Predose, up to 29 hours post dose

Study Arms (4)

Cohort 1: 40 milligram (mg) LY2940094

EXPERIMENTAL

40 mg LY2940094 was administered orally, one time only (it was originally expected that 100 mg LY2940094 would be administered). If the receptor occupancy (RO) for a given dose is lower than 50%, (time to maximum concentration \[tmax\] or an optimal time window) then a higher dose will be administered to the next cohort whereas if the RO for a given dose is higher than 50%, then a lower dose will be administered to the next cohorts.

Drug: LY2940094

Cohort 2: 10 mg LY2940094

EXPERIMENTAL

The dose levels for subjects in Cohort 2 will be defined based on the results of the receptor occupancy (RO) data of previous cohort and the ongoing review of safety data. This dose was determined to be 10 mg, and was administered orally, one time only. If the RO for a given dose is lower than 50%, (tmax or an optimal time window) then a higher dose will be administered to the next cohort whereas if the RO for a given dose is higher than 50%, then a lower dose will be administered to the next cohorts.

Drug: LY2940094

Cohort 3: 4 mg LY2940094

EXPERIMENTAL

The dose levels for subjects in Cohort 3 will be defined based on the results of the receptor occupancy (RO) data of previous cohort(s) and the ongoing review of safety data. This dose was determined to be 4 mg, and was administered orally, one time only. If the RO for a given dose is lower than 50%, (tmax or an optimal time window) then a higher dose will be administered to the next cohort whereas if the RO for a given dose is higher than 50%, then a lower dose will be administered to the next cohorts.

Drug: LY2940094

Cohort 4: 20 mg LY2940094

EXPERIMENTAL

The dose levels for subjects in Cohort 4 will be defined based on the results of the receptor occupancy (RO) data of previous cohort(s) and the ongoing review of safety data. This dose was determined to be 20 mg, and was administered orally, one time only. If the RO for a given dose is lower than 50%, (tmax or an optimal time window) then a higher dose will be administered to the next cohort whereas if the RO for a given dose is higher than 50%, then a lower dose will be administered to the next cohorts.

Drug: LY2940094

Interventions

LY2940094 DRUG

Administered orally

Cohort 1: 40 milligram (mg) LY2940094; Cohort 2: 10 mg LY2940094; Cohort 3: 4 mg LY2940094; Cohort 4: 20 mg LY2940094

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Have a body mass index between 19.0 and 30.0 kilogram square meter (kg/m²), inclusive, weight less than 125.0 kilogram (kg), and physical dimensions which appear small enough to fit into the magnetic resonance imaging (MRI) and positron emission tomography scanners (PET)
• Must be in good health, as determined by a medical history, vital signs, physical examination, 12-lead electrocardiogram (ECG) and clinical laboratory evaluations
• Have venous and arterial access sufficient to allow blood sampling
• Are nonsmokers for at least 3 months prior to Screening, according to self report (meaning zero cigarettes smoked)
• Have a calculated creatinine clearance of greater than (\>)70 milliliters per minute (mL/min) at Screening
• Are reliable and willing to make themselves available for the duration of the study and are willing to follow study procedures
• Will have given their written informed consent to participate in the study and to abide by the study restrictions

You may not qualify if:

• Male subjects who are not, or whose partners are not willing to use appropriate contraception (condom with spermicidal foam/gel/film/cream/suppository) from the time of the first dose until 3 months after dosing
• Have received any prescribed systemic or topical medication within 14 days of the first dose administration, unless in the opinion of the Investigator the medication will not interfere with the study procedures or compromise safety
• Have used any nonprescribed systemic or topical medication (including herbal remedies) within 7 days of the first dose administration (with the exception of vitamin/mineral supplements) unless in the opinion of the Investigator the medication will not interfere with the study procedures or compromise safety
• Have received any medications, including St. John's Wort, known to chronically alter drug absorption or elimination processes within 30 days of the first dose administration unless in the opinion of the Investigator the medication will not interfere with the study procedures or compromise safety
• Currently enrolled in, have completed, or discontinued within the last 30 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 donated or lost 50 to 499 mL of whole blood within 30 days, or more than 499 mL whole blood within 56 days preceding first dose administration
• Have a significant history of drug allergy as determined by the Investigator
• Have any clinically significant allergic disease (excluding nonactive hay fever), or any known allergy to LY2940094 as determined by the Investigator
• Have a semi-reclined blood pressure and pulse rate higher than 130/90 millimeters of mercury (mmHg) and 100 beats per minute, respectively, or lower than 90/50 mmHg and 40 beats per minute, respectively
• Consume more than 14 units of alcohol per week or who have a significant history of alcoholism or drug/chemical abuse/dependence as determined by the Investigator (one unit of alcohol equals ½ pint \[285 mL\] of beer or lager, one glass \[125 mL\] of wine, or 1/6 gill \[25 mL\] of spirits)
• Have a positive urine drug screen or alcohol breath test result that indicates substance abuse at screening or at admission to any treatment period
• With, or with a history of, any clinically significant neurological, gastrointestinal, renal, hepatic, cardiovascular, respiratory, metabolic, endocrine, hematological or other major disorders as determined by the Investigator
• With, or with a history of, any psychiatric illness as assessed with the Symptom Checklist (SCL-90R)
• Have had a clinically significant illness within 4 weeks of the start of dose administration as determined by the Investigator
• Have serum hepatitis (B or C), or who are carriers of the hepatitis B surface antigen or hepatitis C antibody, or who have a positive result to the test for human immunodeficiency virus (HIV) antibodies

Sponsors & Collaborators

• BlackThorn Therapeutics, Inc.: lead

Study Sites (1)

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.

Toronto, Ontario, Canada

Location

MeSH Terms

Conditions

Depression

Interventions

LY2940094

Condition Hierarchy (Ancestors)

Behavioral Symptoms; Behavior

Study Officials

• 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

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 26, 2011
• First Posted: July 27, 2011
• Study Start: July 1, 2011
• Primary Completion: November 1, 2011
• Study Completion: November 1, 2011
• Last Updated: February 3, 2017

Record last verified: 2017-02

Locations

CA (1)