Hereditary Angioedema
Conditions
Keywords
BCX4161, BioCryst, hereditary angioedema, mass balance, kallikrein inhibitor, ADME
Brief summary
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.
Interventions
DRUGBCX4161
Sponsors
BioCryst Pharmaceuticals
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
30 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy males 2. Age 30 to 65 years of age (inclusive) 3. Body mass index of 18.0 to 32.0 kg/m2 4. Must be willing and able to communicate and participate in the whole study 5. Must provide written informed consent 6. A history of regular bowel movements 7. Must agree to use an adequate method of contraception Key
Exclusion criteria
1. Participation in a clinical research study within the previous 3 months 2. Current or history of any drug or alcohol abuse in the past 2 years or positive drugs of abuse screen 3. Current smokers 4. Radiation exposure, including that from the present study, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years 5. Clinically significant medical history, current medical or psychiatric condition, ECG finding, or laboratory/urinalysis abnormality 6. Activated partial thromboplastin time or PT outside of normal laboratory limits
Design outcomes
Primary
| Measure | 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
| Measure | 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 |
Countries
United Kingdom
Outcome results
None listed