Food Effect and Relative Bioavailability Study of Rilzabrutinib in Healthy Participants

NCT04748926 | Completed Phase 1

• 3 other identifiers: PKM17098U1111-1260-4526PRN1008-25
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

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

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (10)

• 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 Outcomes (1)

• Treatment-emergent AE and treatment-emergent SAE

  Until Day 15

Study Arms (2)

Group 1

EXPERIMENTAL

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

Group 2

EXPERIMENTAL

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

Interventions

rilzabrutinib SAR444671 DRUG

Pharmaceutical form: caplet Route of administration: oral

Group 1; Group 2

Eligibility Criteria

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

You may qualify if:

• \- 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

You may not qualify if:

• 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.

Sponsors & Collaborators

• Principia Biopharma, a Sanofi Company: lead

Study Sites (1)

Investigational Site

Adelaide, 5000, Australia

Location

Related Links

• PKM17098 Plain Language Results Summary

Study Officials

• Clinical Sciences & Operations

  Sanofi

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 3, 2021
• First Posted: February 10, 2021
• Study Start: April 7, 2021
• Primary Completion: May 21, 2021
• Study Completion: May 21, 2021
• Last Updated: September 23, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will share

Locations

AU (1)