Study to Determine the Absorption, Metabolism, and Excretion of [14C]LX4211 in Healthy Male Subjects (AME)

A Phase 1, Open-label, Nonrandomized, Single Dose Study to Evaluate the Absorption, Metabolism, and Excretion of [14C]-LX4211, Following Oral Administration, in Healthy Male Subjects

This phase 1 study is to evaluate the pharmacokinetics (PK), metabolism, routes and extent of elimination of a single oral dose of 400 mg [14C]LX4211 to healthy male subjects

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: [14C]-LX4211

• Study Type: Interventional
• Enrollment (Actual): 8
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • Lexicon Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Adults ≥18 to ≤55 years of age
• Vital signs at Screening in the following ranges: systolic blood pressure, 90-140 mm Hg; diastolic blood pressure, 50-90 mm Hg; heart rate, 50-100 bpm
• Body mass index (BMI) ≥18 and ≤35 kg/sq m
• Historically able to produce a minimum of 1 bowel movement per day
• Willing and able to provide written informed consent

Exclusion Criteria:

• Female
• Receipt of any investigational drug within 30 days prior to Dosing, or investigational protein or antibody-based therapeutic agents within 3 months prior to Screening
• Prior exposure to LX4211
• Use any tobacco product within 2 months prior to Screening and while participating in the study (Day -1 through Discharge)
• History of bariatric surgery or any other GI surgery that may induce malabsorption
• History of any major surgery within 6 months prior to Screening
• History of renal or hepatic disease, or significantly abnormal kidney or liver function tests at Screening
• History of any clinically relevant psychiatric, renal, hepatic, pancreatic, cardiovascular, neurological, hematological, or GI abnormality
• History of any active infection within 14 days prior to Dosing
• History of alcohol or substance abuse within 2 years prior to Dosing
• History of human immunodeficiency virus (HIV), hepatitis B, or hepatitis C
• Donation or loss of >400 mL of blood or blood product within 3 months of Dosing
• Positive urine glucose at Screening
• Positive urine screen for drugs of abuse at Screening or Day -1
• Positive breath test for alcohol at Screening or Day -1
• Participation in >1 other radiolabeled investigational study drug trial within 12 months prior to Day -1
• Exposure to significant radiation within 12 months prior to Day -1

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: [14C]-LX4211; 400 mg LX4211 administered orally	Drug: [14C]-LX4211

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area Under Curve (AUC)	Day 1: predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of subjects experiencing an adverse event	Day 1 through discharge
Urinary recovery of radioactivity	predose through 24 hours
Fecal recovery of radioactivity	predose through 24 hours
Whole blood and plasma concentration of total radioactivity	predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose

Collaborators and Investigators

• Sponsor: Lexicon Pharmaceuticals
• Investigators: Study Director: Ikenna Ogbaa, M.D., Lexicon Pharmaceuticals, Inc.

Study record dates

Study Major Dates

• Study Start: March 1, 2013
• Primary Completion (Actual): May 1, 2013
• Study Completion (Actual): May 1, 2013

Study Registration Dates

• First Submitted: March 21, 2013
• First Submitted That Met QC Criteria: March 21, 2013
• First Posted (Estimate): March 26, 2013

Study Record Updates

• Last Update Posted (Estimate): June 18, 2013
• Last Update Submitted That Met QC Criteria: June 17, 2013
• Last Verified: June 1, 2013

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Hypoglycemic Agents; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Sodium-Glucose Transporter 2 Inhibitors; (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol
• Other Study ID Numbers: LX4211.1-108-NRM; LX4211.108