Relative Bioavailability of Zanubrutinib Tablets Compared to Capsules and Effects of Food on the Pharmacokinetics of the Tablet in Healthy Adults

A Single-dose, Open-label, Randomized, Crossover Study in Healthy Adult Subjects to Assess the Relative Bioavailability of a Zanubrutinib Tablet Compared to Zanubrutinib Capsules and to Evaluate the Effects of Food on the Pharmacokinetics of the Zanubrutinib Tablet

Study to assess the relative bioavailability of zanubrutinib tablets compared to capsules and to evaluate the effects of food on the pharmacokinetics (PK) of the zanubrutinib tablet.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: Zanubrutinib

• Study Type: Interventional
• Enrollment (Actual): 43
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • Dallas, Texas, United States, 75247
      • Fortrea Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Body mass index between 18.0 and 32.0 kg/m^2, inclusive
• In good health, determined by no clinically significant findings from medical history, 12-lead ECGs, vital signs measurements, and clinical laboratory evaluations as assessed by the investigator or designee
• Female participants of non-childbearing potential only

Exclusion Criteria:

• Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, or psychiatric disorder, as determined by the investigator or designee
• Evidence of any infections (bacterial, viral, fungal, parasitic) within 4 weeks prior to the first dose of study drug, as determined by the investigator or designee
• History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the investigator or designee
• History or presence of an abnormal ECG prior to the first dose of the study drug that, in the opinion of the investigator or designee, is clinically significant
• Use or intent to use prescription medications within 14 days prior to dosing or nonprescription medications/products/supplements within 7 days prior to check-in
• Use of tobacco or nicotine containing products within 3 months prior to check-in

Note: Other protocol defined Inclusion/Exclusion criteria may apply

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Low Dose Cohort; Zanubrutinib will be administered as a single low dose of treatment (tablet) or reference (capsule) on separate occasions across several treatment sequences	Drug: Zanubrutinib; Administered orally as a tablet or capsule; Other Names: Brukinsa; BGB-3111
Experimental: High Dose Cohort; Zanubrutinib will be administered as a single high dose of treatment (tablet) or reference (capsule) on separate occasions across several treatment sequences	Drug: Zanubrutinib; Administered orally as a tablet or capsule; Other Names: Brukinsa; BGB-3111

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the plasma concentration-time curve from time 0 extrapolated to infinity (AUC0-inf)	Predose and up to 48 hours postdose up to Day 7
Area under the plasma concentration-time curve from time 0 to the time of the last quantifiable concentration (AUC0-t)	Predose and up to 48 hours postdose up to Day 7
Maximum observed plasma concentration (Cmax)	Predose and up to 48 hours postdose up to Day 7
Time of the maximum observed plasma concentration (Tmax)	Predose and up to 48 hours postdose up to Day 7
Apparent terminal elimination half-life (t1/2)	Predose and up to 48 hours postdose up to Day 7
Apparent volume of distribution (Vz/F)	Predose and up to 48 hours postdose up to Day 7
Rate of decrease of concentration in the terminal phase (λz)	Predose and up to 48 hours postdose up to Day 7
Apparent oral clearance (CL/F)	Predose and up to 48 hours postdose up to Day 7

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of participants with adverse events (AEs)		Up to approximately 6 months
Number of participants with clinically significant laboratory values	Laboratory values are based on hematology, clinical chemistry, and urinalysis test results	Up to approximately 6 months
Number of participants with clinically significant electrocardiogram (ECG) results		Up to approximately 6 months
Number of participants with clinically significant vital sign measurements	Vital sign measurements include supine blood pressure, supine pulse rate, respiratory rate, and oral body temperature	Up to approximately 6 months

Collaborators and Investigators

• Sponsor: BeiGene
• Investigators: Study Director: Study Director, BeiGene

Study record dates

Study Major Dates

• Study Start (Actual): June 7, 2022
• Primary Completion (Actual): December 7, 2022
• Study Completion (Actual): December 7, 2022

Study Registration Dates

• First Submitted: September 16, 2022
• First Submitted That Met QC Criteria: September 16, 2022
• First Posted (Actual): September 21, 2022

Study Record Updates

• Last Update Posted (Actual): October 26, 2024
• Last Update Submitted That Met QC Criteria: October 23, 2024
• Last Verified: October 1, 2024

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Tyrosine Kinase Inhibitors; Antineoplastic Agents; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Kinase Inhibitors; Zanubrutinib
• Other Study ID Numbers: BGB-3111-115

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No