Clinical trial NCT02218294: Study to Determine How BCX4161 is Metabolized and Eliminated by the Body
Official title: 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Hereditary Angioedema
Keywords: BCX4161
BioCryst
hereditary angioedema
mass balance
kallikrein inhibitor
ADME
Lead sponsor: BioCryst Pharmaceuticals
Sponsor class: INDUSTRY
First posted: 2014-08-18
Enrollment: 7
Sex: MALE
Minimum age (years): 30
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

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.


Eligibility criteria: 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

Primary outcomes:
measure: Mass balance of BCX4161 after a single oral dose of [14C] BCX4161 based upon radioactivity excreted in urine, expired air and feces
timeFrame: Determined from samples drawn up to 14 days post-dose
Secondary outcomes:
measure: Chemical structure elucidation of major metabolites of [14C] BCX4161 in urine, plasma, feces, urine
timeFrame: Determined from samples drawn up to 4 days post-dose
measure: 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
timeFrame: Data generated from samples drawn up to 7 days post-dose
measure: Urinary pharmacokinetics (CLr, Ae, and % dose excreted) of BCX4161
timeFrame: Data generated from samples drawn up to 7 days post-dose
measure: Safety and tolerability evaluated through assessments of adverse events, laboratory analyses, vital signs, ECGs, and physical examinations
timeFrame: Over the duration of the study, approximately 6 weeks from screening through follow-up
Other outcomes:
Locations:
city: Ruddington
country: United Kingdom
facility: Quotient Clinical Ltd
state: Nottingham
Study officials:
affiliation: Quotient Clinical Ltd
name: Joanne Collier, MBChB, FFPM, Dip Stats (OU)
role: PRINCIPAL_INVESTIGATOR
References: