Pharmacokinetics (PK) of Rilzabrutinib (PRN1008) in Healthy Japanese and Caucasian Subjects

Principia Biopharma, a Sanofi Company23 enrolled

Overview

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.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

TREATMENT

Masking

NONE

Enrollment

Conditions

Healthy Volunteers

Interventions

RilzabrutinibDRUG

Rilzabrutinib tablet(s) administered orally

Eligibility

Sex: ALLMin age: 18 YearsMax age: 75 YearsHealthy volunteers:

Medical Language ↔ Plain English

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 exclusion criteria might apply.

Locations (1)

Investigational Site Number: 0001

Glendale, California, United States

Outcomes

Primary Outcomes

Maximum measured concentration of total rilzabrutinib in plasma (Cmax)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Time from dosing to maximum measured concentration of total rilzabrutinib in plasma (tmax)

Time frame: 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)

Time frame: 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)

Time frame: 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)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Terminal Half-Life of total rilzabrutinib in Plasma (t1/2)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Apparent Total Clearance of rilzabrutinib in the plasma after oral administration (CL/F)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Apparent volume of distribution after oral administration (Vd/F)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Dose proportionality of rilzabrutinib

Time frame: Up to 48 hours after the last rilzabrutinib dose

Accumulation ratio (Rac)

Data from ClinicalTrials.gov

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Secondary Outcomes

Incidence of potentially clinically significant laboratory test, vital signs, and electrocardiogram (ECGs) abnormalities

Time frame: Up to 14 days after rilzabrutinib dosing

Number of Adverse Events (AE) / Serious Adverse Events (SAE)

Time frame: From date of signed ICF, up to 47 days

Bruton's Tyrosine Kinase (BTK) Occupancy characterization

Time frame: Up to 48 hours after the last rilzabrutinib dose

Maximum measured concentration of rilzabrutinib metabolites in plasma (Cmax)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Time from dosing to maximum measured concentration of rilzabrutinib metabolites in plasma (tmax)

Time frame: 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)

Time frame: 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)

Time frame: 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)

Time frame: Up to 48 hours after the last rilzabrutinib dose

Terminal Half-Life of rilzabrutinib metabolites in Plasma (t1/2)

Time frame: Up to 48 hours after the last rilzabrutinib dose