Disposition of Carbon-14-Labeled LY2886721 ([^14C]-LY2886721) Following Oral Administration in Healthy Human Participants

NCT01367262 | Completed Phase 1 Results

• 2 other identifiers: 13736I4O-MC-BACD
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

This open-label study is being conducted to determine the metabolism and physiological disposition of radiolabeled LY2886721 after a single dose in healthy male participants.

Conditions

Healthy Volunteers

Keywords

Absorption; Distribution; Metabolism; Excretion

Outcome Measures

Primary Outcomes (1)

• Percentage of Urinary and Fecal Excretion of LY2886721 Radioactivity Over Time

  Urinary and fecal excretion of LY2886721 radioactivity over time was expressed as a percentage of the total radioactive dose administered. The amount of drug-related material excreted in urine and feces (Ae) at a specific collection interval (i) was calculated as the product of radioactivity concentration and volume or weight. The Ae values for each collection interval were then summed and calculated as Total Ae=Ae(i1)+Ae(i2)+Ae(in). The percentage of the total radiolabeled dose administered that was excreted in feces or urine=\[(Total Ae)/(Total radioactive dose administered)\]\*100.

  Predose up to 7 days (168 hours) postdose

Secondary Outcomes (7)

• Plasma Pharmacokinetics (PK) of LY2886721: Area Under the Concentration-Time Curve From Time 0 to Infinity [AUC(0 to Inf)]

  Predose up to 4 days (96 hours) postdose

• PK of Radioactivity: AUC(0 to Inf)

  Predose up to 4 days (96 hours) postdose

• Plasma PK of LY2886721: Maximum Observed Concentration (Cmax)

  Predose up to 4 days (96 hours) postdose

• PK of Radioactivity: Cmax

  Predose up to 4 days (96 hours) postdose

• Relative Abundance of LY2886721 and the Metabolites of LY2886721 in Plasma

  1 to 8 hours postdose

Study Arms (1)

Radiolabeled LY2886721

EXPERIMENTAL

Single 25 milligram (mg) oral dose containing 80 microCuries of radiolabeled LY2886721

Drug: LY2886721

Interventions

LY2886721 DRUG

Administered orally

Radiolabeled LY2886721

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy males as determined by medical history and physical examination
• Males will be sterile (including vasectomy) or if the participant is not sterile and is sexually active, he will agree to use from check-in until 3 months after exit/discharge, 1 of the following approved methods of contraception: a male condom with spermicide, a sterile sexual partner, use by female sexual partner of an intrauterine device with spermicide, a female condom with spermicide, contraceptive sponge with spermicide, a diaphragm with spermicide, a cervical cap with spermicide, or oral, implantable, transdermal, intravaginal, or injectable contraceptives
• Have a body mass index of 19 to 30 kilograms per square meter (kg/m\^2)
• 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 for blood sampling
• Have normal blood pressure and heart rate (sitting)
• Experience a minimum of at least 1 bowel movement per day
• 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 institutional review board (IRB) governing the site

You may not qualify if:

• Are currently enrolled in, have completed, or discontinued within the last 30 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 LY2886721, related compounds, or any components of the formulation
• Are persons who have previously received the investigational product in this study, have completed or withdrawn from this study or any other study investigating LY2886721
• Have a Bazett's corrected QT (QTcB) interval value of \>450 milliseconds (msec) or any abnormality in the 12-lead electrocardiogram (ECG) increases the risks associated with participating in the study
• Have an abnormal blood pressure
• 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
• Regularly use known drugs of abuse and/or show positive findings on urinary drug screening
• Show evidence of human immunodeficiency virus (HIV) infection and/or positive 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
• Intend to use prescription medication, over-the-counter medication, or herbal preparations containing St. John's Wort, kava, garlic, ginger, ginko biloba, or guarana within 14 days prior to admission
• Eating of grapefruit or grapefruit-containing foods, or drinking grapefruit-containing juices within 7 days prior to dosing or any time during the study
• Have used any tobacco- or nicotine-containing products (including, but not limited to, cigarettes, pipes, cigars, chewing tobacco, nicotine patches, nicotine lozenges, or nicotine gum) within 6 months prior to dosing
• Have donated blood of more than 500 milliliters (mL) within the last month
• Have an average weekly alcohol intake that exceeds 21 units per week (males up to age 65), or are unwilling to stop alcohol consumption from 48 hours prior to check-in until end of study \[1 unit = 12 ounces (oz) or 360 mL of beer; 5 oz or 150 mL of wine; 1.5 oz or 45 mL of distilled spirits\]

Sponsors & Collaborators

• Eli Lilly and Company: 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.

Madison, Wisconsin, United States

Location

MeSH Terms

Interventions

N-(3-(2-amino-4a,5,7,7a-tetrahydro-4H-furo(3,4-d)(1,3)thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide

Limitations and Caveats

Assay sensitivity of plasma and whole blood radioactivity were not generally quantifiable after 24-hours postdose. Consequently, the AUC(0-inf) estimate for total radioactivity in plasma and whole blood should be considered underestimated.

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

800-545-5979

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

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: June 3, 2011
• First Posted: June 7, 2011
• Study Start: June 1, 2011
• Primary Completion: July 1, 2011
• Study Completion: July 1, 2011
• Last Updated: September 13, 2019
• Results First Posted: September 13, 2019

Record last verified: 2019-05

Locations

US (1)