Food Effect and Relative Bioavailability Study of Rilzabrutinib in Healthy Participants

A Randomized, Open-label, Phase I Study to Assess the Effects of Food and Formulation on the Pharmacokinetics of a Single Dose of Rilzabrutinib (SAR444671 [Formerly PRN1008]) in Healthy Male and Female Participants

Primary Objective:

• To evaluate the impact of food on the pharmacokinetics (PK) of rilzabrutinib following single oral doses to healthy subjects.
• To evaluate the impact of formulation on the PK of rilzabrutinib following single oral doses to healthy subjects

Secondary Objective:

- To assess the safety and tolerability of single oral doses of rilzabrutinib administered under fasted and fed conditions

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: rilzabrutinib SAR444671; Drug: rilzabrutinib SAR444671; Drug: rilzabrutinib SAR444671

Detailed Description

The total study duration is approximately 43 days for each participant, including a screening period of 2 to 28 days, treatment period of 12 days, and follow-up of 3 days

• Study Type: Interventional
• Enrollment (Actual): 24
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • Adelaide, Australia, 5000
    • Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion criteria :

- Participants who are overtly healthy as determined by medical evaluation

• Body mass index (BMI) within the range ≥18 and ≤31 kg/m2 (inclusive) and a minimum body weight of 45 kg.
• Female participant is eligible to participate if she is not pregnant or breastfeeding
• Male participants are eligible to participate if they agree to refrain from donating sperm and use contraception/barrier or be abstinent from intercourse

Exclusion criteria:

• COVID-19 infection, positive test result for human immunodeficiency virus (HIV), hepatitis B virus or hepatitis C virus antibody
• Use of any prescription or over-the-counter (OTC) medication, herbal products, or dietary supplements within 7 days
• Participation in another clinical trial of a drug or device whereby the last investigational drug/device administration is within 30 days or 5 half-lives, whichever is longer, prior to the first dose of study drug.
• Clinically significant abnormal in vital signs. - Any specific situation during study implementation/course that may rise ethics considerations.

The above information is not intended to contain all considerations relevant to a subject's potential participation in a clinical trial.

Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Group 1; Participants will receive caplets after fast (treatment A) on Day 1 and caplets after meal (treatment B) on day 6, and then receive either oral formulation 1 tablets after fast (treatment C) or oral formulation 2 tablets after fast (treatment D) on day 11.	Drug: rilzabrutinib SAR444671; Pharmaceutical form: caplet Route of administration: oral; Drug: rilzabrutinib SAR444671; Pharmaceutical form: Oral Formulation 1 tablets Route of administration: oral; Drug: rilzabrutinib SAR444671; Pharmaceutical form: Oral Formulation 2 tablets Route of administration: oral
Experimental: Group 2; Participants will receive caplets after meal (treatment B) on Day 1 and caplets after fast (treatment A) on day 6, and then receive either oral formulation 1 tablets after fast (treatment C) or oral formulation 2 tablets after fast (treatment D) on day 11.	Drug: rilzabrutinib SAR444671; Pharmaceutical form: caplet Route of administration: oral; Drug: rilzabrutinib SAR444671; Pharmaceutical form: Oral Formulation 1 tablets Route of administration: oral; Drug: rilzabrutinib SAR444671; Pharmaceutical form: Oral Formulation 2 tablets Route of administration: oral

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Rilzabrutinib plasma PK parameters following administration of the reference formulation in the fed and fasted states: Cmax	maximun plasma concentration	From Day 1 to Day 7
Rilzabrutinib plasma PK parameters following administration of the reference formulation in the fed and fasted states: Tmax	time to maximum plasma concentration	From Day 1 to Day 7
Rilzabrutinib plasma PK parameters following administration of the reference formulation in the fed and fasted states: AUC0-last	area under the plasma concentration-time curve from zero to the last measurable concentration	From Day 1 to Day 7
Rilzabrutinib plasma PK parameters following administration of the reference formulation in the fed and fasted states: AUC0-inf	area under the plasma concentration-time curve from zero to infinity	From Day 1 to Day 7
Rilzabrutinib plasma PK parameters following administration of the reference formulation in the fed and fasted states: half-life	terminal elimination phase half-life	From Day 1 to Day 7
Rilzabrutinib plasma PK parameters following administration of two test formulations in the fasted state: Cmax	maximun plasma concentration	From Day 11 to Day 12
Rilzabrutinib plasma PK parameters following administration of two test formulations in the fasted state: Tmax	time to maximum plasma concentration	From Day 11 to Day 12
Rilzabrutinib plasma PK parameters following administration of two test formulations in the fasted state: AUC0-last	area under the plasma concentration-time curve from zero to the last measurable concentration	From Day 11 to Day 12
Rilzabrutinib plasma PK parameters following administration of two test formulations in the fasted state: AUC0-inf	area under the plasma concentration-time curve from zero to infinity	From Day 11 to Day 12
Rilzabrutinib plasma PK parameters following administration of two test formulations in the fasted state: half-life	terminal elimination phase half-life	From Day 11 to Day 12

Secondary Outcome Measures

Outcome Measure	Time Frame
Treatment-emergent AE and treatment-emergent SAE	Until Day 15

Collaborators and Investigators

• Sponsor: Principia Biopharma, a Sanofi Company

Study record dates

Study Major Dates

• Study Start (Actual): April 7, 2021
• Primary Completion (Actual): May 21, 2021
• Study Completion (Actual): May 21, 2021

Study Registration Dates

• First Submitted: February 3, 2021
• First Submitted That Met QC Criteria: February 8, 2021
• First Posted (Actual): February 10, 2021

Study Record Updates

• Last Update Posted (Actual): April 25, 2022
• Last Update Submitted That Met QC Criteria: April 21, 2022
• Last Verified: April 1, 2022

More Information

Terms related to this study

• Other Study ID Numbers: PKM17098; U1111-1260-4526 (Other Identifier: UTN); PRN1008-25 (Other Identifier: Principia Biopharma)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: Yes
• IPD Plan Description: Qualified researchers may request access to patient level data and related study documents including the clinical study report, study protocol with any amendments, blank case report form, statistical analysis plan, and dataset specifications. Patient level data will be anonymized and study documents will be redacted to protect the privacy of trial participants. Further details on Sanofi's data sharing criteria, eligible studies, and process for requesting access can be found at: https://vivli.org

Drug and device information, study documents

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