Effect of Activated Charcoal and Time of Dose on the Pharmacokinetics of LY2624803 in Healthy Subject

Evaluation of the Impact of Activated Charcoal and Time of Dose on the Absorption of LY2624803 in Healthy Subjects

The purpose of this study is to determine the effect of activated charcoal and dosing time on the absorption of LY2624803 in healthy subjects. In this crossover study, there are three treatments with a washout period of at least 7 days in between treatments. Each subject will participate in all three treatments with random assignment to the treatment sequence.

Study Overview

• Status: Completed
• Conditions: Insomnia
• Intervention / Treatment: Drug: LY2624803; Other: Activated Charcoal

• Study Type: Interventional
• Enrollment (Actual): 21
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • West Yorkshire
    • Leeds, West Yorkshire, United Kingdom, LS2 9LH
      • 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.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Are overtly healthy males or females, as determined by medical history and physical examination.
• Male subjects with female partners of child-bearing potential and female subjects of child-bearing potential, agree to use 2 reliable methods of contraception from the time of the first dose until 3 months after the last dose of study drug or are women not of child-bearing potential due to postmenopausal or permanently sterilized [for example, tubal occlusion, hysterectomy, bilateral salpingectomy]).
• Have a body mass index (BMI) between 18.5 and 32 kilograms per square meter (kg/m2), inclusive, and a body weight of 50 kg or above at screening.
• Have clinical laboratory test results within normal reference range 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 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 ethical review board governing the site.

Exclusion Criteria:

• Are currently enrolled in, or discontinued within the last 90 days from, a clinical trial involving an investigational drug or device or off-label use of a drug or device (other than the study drug 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 LY2624803 or related compounds.
• Are persons who have previously completed or withdrawn from this study or any other study investigating LY2624803.
• 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 as determined by the investigator.
• Have a history or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal (except appendectomy), endocrine, hematological, dermatological, venereal, 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.
• Show evidence or history of postural hypotension, loss of consciousness, explained or unexplained syncope or seizure episodes or a family history of seizures. A history of a single febrile convulsion is acceptable.
• Show evidence of significant active neuropsychiatric disease.
• Regularly use known drugs of abuse and/or show positive findings on urinary drug screening.
• Show evidence of human immunodeficiency virus (HIV) 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 or prescription medications, with the exception of vitamins and paracetamol, which cannot be safely discontinued within 7 days prior to admission.
• Have donated blood of more than 500 milliliters (mL) within the last 3 months prior to screening.
• Have an average weekly alcohol intake that exceeds 28 units per week (males) and 21 units per week (females), and are subjects unwilling to stop alcohol consumption from 48 hours prior to admission until discharge from the unit for each treatment period, and to limit alcohol intake to a maximum of 2 units/day between treatment periods.
• Have a history of breast cancer.
• Are subjects with excessive xanthine consumption.
• Exhibit any other condition, which, in the opinion of the investigator would preclude participation in the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 6 mg LY2624803 Alone Morning Dosing; Participants received 6 milligrams (mg) LY2624803 alone orally (po) at approximately 0800 hours following an overnight fast.	Drug: LY2624803; Administered orally (po), once.
Experimental: 6 mg LY2624803 Morning Dosing + Activated Charcoal; Participants received 6 mg LY2624803 po at approximately 0800 hours following an overnight fast, followed 1 hour later by a single po dose of 1 gram per kilogram (g/kg) body weight of activated charcoal, mixed with caffeine-free diet cola.	Drug: LY2624803; Administered orally (po), once.; Other: Activated Charcoal; Administered po
Experimental: 6 mg LY2624803 Alone Evening Dosing; Participants received 6 mg LY2624803 alone po at approximately 2200 hours following a 4-hour fast.	Drug: LY2624803; Administered orally (po), once.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Concentration-Time Curve (AUC) for LY2624803 and the Metabolite LSN2797276	AUC from time 0, extrapolated to infinity, estimated for both LY2624803 and the metabolite LSN2797276.	Predose and up to Day 4
Maximum Concentration (Cmax) for LY2624803 and the Metabolite, LSN2797276,	Cmax estimated for both LY2624803 and the metabolite LSN2797276.	Predose and up to Day 4

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Time to Maximum Plasma Concentration (Tmax) for LY2624803 and the Metabolite, LSN2797276	Tmax, estimated for both LY2624803 and the metabolite LSN2797276.	Predose and up to day 4

Collaborators and Investigators

• Sponsor: Eli Lilly and Company

Study record dates

Study Major Dates

• Study Start: October 1, 2010
• Primary Completion (Actual): December 1, 2010
• Study Completion (Actual): December 1, 2010

Study Registration Dates

• First Submitted: November 4, 2010
• First Submitted That Met QC Criteria: November 4, 2010
• First Posted (Estimate): November 7, 2010

Study Record Updates

• Last Update Posted (Estimate): December 22, 2011
• Last Update Submitted That Met QC Criteria: November 17, 2011
• Last Verified: November 1, 2011

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Protective Agents; Antidotes; Charcoal
• Other Study ID Numbers: 12814; I2K-MC-ZZBQ (Other Identifier: Eli Lilly and Company)