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

NCT02218294 | Completed Phase 1

• 1 other identifier: BCX4161-103
• Study Type: interventional
• Target: 7
• Locations: 1 country
• Sites: 1

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.

Conditions

Hereditary Angioedema

Keywords

BCX4161; BioCryst; hereditary angioedema; mass balance; kallikrein inhibitor; ADME

Outcome Measures

Primary Outcomes (1)

• 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 Outcomes (4)

• 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

Study Arms (1)

[14C] BCX4161

EXPERIMENTAL

Includes a radiolabelled dose of \[14C\] BCX4161 and unlabelled BCX4161

Drug: BCX4161

Interventions

BCX4161 DRUG

[14C] BCX4161

Eligibility Criteria

• Age: 30 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• BioCryst Pharmaceuticals: lead

Study Sites (1)

Quotient Clinical Ltd

Ruddington, Nottingham, NG11 6JS, United Kingdom

Location

MeSH Terms

Conditions

Angioedemas, Hereditary

Interventions

avoralstat

Condition Hierarchy (Ancestors)

Angioedema; Vascular Diseases; Cardiovascular Diseases; Hereditary Complement Deficiency Diseases; Primary Immunodeficiency Diseases; Genetic Diseases, Inborn; Congenital, Hereditary, and Neonatal Diseases and Abnormalities; Urticaria; Skin Diseases, Vascular; Skin Diseases; Skin and Connective Tissue Diseases; Hypersensitivity, Immediate; Hypersensitivity; Immune System Diseases; Immunologic Deficiency Syndromes

Study Officials

• Joanne Collier, MBChB, FFPM, Dip Stats (OU)

  Quotient Clinical Ltd

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: August 14, 2014
• First Posted: August 18, 2014
• Study Start: August 1, 2014
• Primary Completion: September 1, 2014
• Study Completion: September 1, 2014
• Last Updated: October 29, 2014

Record last verified: 2014-10

Locations

GB (1)