Healthy Volunteers
Conditions
Brief summary
This is a single-dose and multiple doses study to assess the Pharmacokinetics (PK) of rilzabrutinib as well as to evaluate the tolerability of rilzabrutinib in Japanese and Caucasian Healthy Male and Female subjects.
Interventions
DRUGRilzabrutinib
Rilzabrutinib tablet(s) administered orally
Sponsors
Principia Biopharma, a Sanofi Company
Study design
Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 75 Years
Healthy volunteers
Yes
Inclusion criteria
* Japanese subjects must have both biological parents and all four grandparents of Japanese ancestry and born in a Japanese country of origin. * Caucasian subjects must have four Caucasian grandparents (Hispanics of white race can be considered Caucasian). * Healthy adult male or non-pregnant non-lactating females, 18 to 75 years of age (inclusive) at the time of screening. * Body mass index (BMI) ≥18 and ≤35 (kg/m2), inclusive, and a minimum body weight of 45 kg. Additional inclusion criteria might apply.
Exclusion criteria
* Symptoms consistent with COVID-19 such as fever, cough, and shortness of breath within 14 days before Day 1. * Positive test for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at screening or check-in (Day -1). * Known previous COVID-19 infection. * Use of any prescription or over-the-counter (OTC) medication, herbal products, or dietary supplements within the 7 days or 5 half-lives, whichever is longer, prior to the first study drug administration. Use of hormonal contraception is allowed prior to and during the study. Additional
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Accumulation ratio (Rac) | Up to 48 hours after the last rilzabrutinib dose |
| Maximum measured concentration of total rilzabrutinib in plasma (Cmax) | Up to 48 hours after the last rilzabrutinib dose |
| Time from dosing to maximum measured concentration of total rilzabrutinib in plasma (tmax) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the concentration-time curve of total rilzabrutinib in plasma from 0 to the last measurable concentration (AUC0-last) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the concentration-time curve of total rilzabrutinib in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the plasma concentration-time curve of total rilzabrutinib from zero during the dosage interval (AUC0-tau) | Up to 48 hours after the last rilzabrutinib dose |
| Terminal Half-Life of total rilzabrutinib in Plasma (t1/2) | Up to 48 hours after the last rilzabrutinib dose |
| Apparent Total Clearance of rilzabrutinib in the plasma after oral administration (CL/F) | Up to 48 hours after the last rilzabrutinib dose |
| Apparent volume of distribution after oral administration (Vd/F) | Up to 48 hours after the last rilzabrutinib dose |
| Dose proportionality of rilzabrutinib | Up to 48 hours after the last rilzabrutinib dose |
Secondary
| Measure | Time frame |
|---|---|
| Number of Adverse Events (AE) / Serious Adverse Events (SAE) | From date of signed ICF, up to 47 days |
| Bruton's Tyrosine Kinase (BTK) Occupancy characterization | Up to 48 hours after the last rilzabrutinib dose |
| Maximum measured concentration of rilzabrutinib metabolites in plasma (Cmax) | Up to 48 hours after the last rilzabrutinib dose |
| Time from dosing to maximum measured concentration of rilzabrutinib metabolites in plasma (tmax) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the concentration-time curve of rilzabrutinib metabolites in plasma from 0 to the last measurable concentration (AUC0-last) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the concentration-time curve of rilzabrutinib metabolites in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) | Up to 48 hours after the last rilzabrutinib dose |
| Area under the plasma concentration-time curve of rilzabrutinib metabolites from zero during the dosage interval (AUC0-tau) | Up to 48 hours after the last rilzabrutinib dose |
| Terminal Half-Life of rilzabrutinib metabolites in Plasma (t1/2) | Up to 48 hours after the last rilzabrutinib dose |
| Incidence of potentially clinically significant laboratory test, vital signs, and electrocardiogram (ECGs) abnormalities | Up to 14 days after rilzabrutinib dosing |
Countries
United States
Outcome results
None listed