Study to Determine How BCX4161 is Metabolized and Eliminated by the Body

Study Overview
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Brief Summary
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The purpose of the study is to assess the extent that radioactive dose of BCX4161 taken by mouth ends up in the urine, feces and expired air. If there are metabolites of BCX4161 made by the body, the chemical composition of these metabolites and their profile over time in blood and urine will be determined.

Official Title
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A Phase 1 Study to Evaluate the Absorption, Metabolism and Excretion of BCX4161 Following Administration of a Single, Oral Dose of [14C]-Radiolabelled BCX4161 to Healthy Male Subjects

Conditions
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Hereditary Angioedema

Intervention / Treatment
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* Drug: BCX4161


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy males Age 30 to 65 years of age (inclusive) Body mass index of 18.0 to 32.0 kg/m2 Must be willing and able to communicate and participate in the whole study Must provide written informed consent A history of regular bowel movements Must agree to use an adequate method of contraception Key Exclusion Criteria: Participation in a clinical research study within the previous 3 months Current or history of any drug or alcohol abuse in the past 2 years or positive drugs of abuse screen Current smokers Radiation exposure, including that from the present study, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years Clinically significant medical history, current medical or psychiatric condition, ECG finding, or laboratory/urinalysis abnormality Activated partial thromboplastin time or PT outside of normal laboratory limits

Ages Eligible for Study
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Minimum Age: 30 Years
Maximum Age: 65 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Intervention Model: Single Group Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: [14C] BCX4161<br>Includes a radiolabelled dose of [14C] BCX4161 and unlabelled BCX4161 | Drug: BCX4161<br> <br> |

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Mass balance of BCX4161 after a single oral dose of [14C] BCX4161 based upon radioactivity excreted in urine, expired air and feces |  | Determined from samples drawn up to 14 days post-dose | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Chemical structure elucidation of major metabolites of [14C] BCX4161 in urine, plasma, feces, urine |  | Determined from samples drawn up to 4 days post-dose | 
| Plasma pharmacokinetics (Cmax, Tmax, Tlag, AUC(0-last), AUC(0-inf), CL/F, Vz/F, AUC%extrapolated,t1/2, as applicable for each analyte) of total radioactivity, BCX4161, [14C] BCX4161 and major metabolites of [14C] BCX4161 |  | Data generated from samples drawn up to 7 days post-dose | 
| Urinary pharmacokinetics (CLr, Ae, and % dose excreted) of BCX4161 |  | Data generated from samples drawn up to 7 days post-dose | 
| Safety and tolerability evaluated through assessments of adverse events, laboratory analyses, vital signs, ECGs, and physical examinations |  | Over the duration of the study, approximately 6 weeks from screening through follow-up | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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BCX4161, BioCryst, hereditary angioedema, mass balance, kallikrein inhibitor, ADME