An Open-label DDI Study to Investigate the Effect of Rilzabrutinib on P-gp, BCRP, OATP1B1 and OATP1B3 Inhibition

NCT07855250 | Recruiting Phase 1 FDA Drug

• 2 other identifiers: INT22851U1111-1334-2206
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

The study is a single-center, Phase-1, open-label, one-sequence, two-treatment period, cross-over, DDI study designed to investigate the effects of rilzabrutinib on the PK of digoxin (as P-gp substrate) and of rosuvastatin (as substrate of BCRP, OATP1B1, and OATP1B3) in healthy male and female participants. For this study a cocktail of digoxin and rosuvastatin will be used.

Conditions

Healthy Volunteer

Outcome Measures

Primary Outcomes (3)

• AUC for digoxin and rosuvastatin

  area under curve

  Up to Day 13 in Period 2

• AUClast for digoxin and rosuvastatin

  area under the curve from time zero to the last measurable concentration

  Up to Day 13 in Period 2

• Cmax for digoxin and rosuvastatin

  maximum (peak) plasma concentration

  Up to Day 13 in Period 2

Secondary Outcomes (5)

• tmax for digoxin and for rosuvastatin

  Up to Day 13 in Period 2

• tmax for rilzabrutinib

  Up to Day 11 in Period 2

• Cmax for rilzabrutinib

  Up to Day 11 in Period 2

• AUC0-tau for rilzabrutinib

  Up to Day 11 in Period 2

• Assessment of AEs and TEAEs

  Up to Day 21 in Period 2

Study Arms (1)

Treatment A then Treatment B

EXPERIMENTAL

Treatment A in Period 1: digoxin + rosuvastatin cocktail alone on Day 1 of Period 1 Treatment B in Period 2: rilzabrutinib (SAR444671) BID from Day 1 to Day 12 of Period 2, plus digoxin + rosuvastatin cocktail on Day 8 of Period 2

Drug: Rilzabrutinib; Drug: Rosuvastatin; Drug: Digoxin

Interventions

Rilzabrutinib DRUG

From Day 1 to Day 12 of Period 2

Also known as: SAR444671

Treatment A then Treatment B

Rosuvastatin DRUG

Single dose on Day 1 of Period 1 and on Day 8 of Period 2

Also known as: Crestor

Treatment A then Treatment B

Digoxin DRUG

Single dose on Day 1 of Period 1 and on Day 8 of Period 2

Also known as: Lanicor

Treatment A then Treatment B

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participant must be 18 to 55 years of age inclusive.
• Body weight between 50.0 and 100.0 kg for males, 40.0 and 90.0 kg for females.
• Contraceptive use by male and female participants should be consistent with local regulations

You may not qualify if:

• History of serious infections requiring intravenous therapy.
• Frequent headaches, migraine, nausea or vomiting.
• History of drug hypersensitivity or allergic disease.
• History of drug or alcohol abuse.
• Smoking regularly more than 5 cigarettes or equivalent in nicotine per week
• Excessive consumption of beverages containing xanthine bases.
• Pregnancy or breastfeeding.
• Recent vaccinations.
• The above information is not intended to contain all considerations relevant to a participant's potential participation in a clinical trial.

Sponsors & Collaborators

• Sanofi: lead

Study Sites (1)

Investigational Site Number : 1240001

Québec, Quebec, G1P 0A2, Canada

RECRUITING

MeSH Terms

Interventions

Rosuvastatin Calcium; Digoxin

Intervention Hierarchy (Ancestors)

Sulfonamides; Amides; Organic Chemicals; Fluorobenzenes; Hydrocarbons, Fluorinated; Hydrocarbons, Halogenated; Hydrocarbons; Sulfones; Sulfur Compounds; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Digitalis Glycosides; Cardenolides; Cardiac Glycosides; Cardanolides; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Glycosides; Carbohydrates

Central Study Contacts

Trial Transparency email recommended (Toll free for US & Canada)

CONTACT

800-633-1610; Contact-US@sanofi.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 21, 2026
• First Posted: October 2, 2026
• Study Start: October 1, 2026
• Primary Completion (Estimated): November 3, 2026
• Study Completion (Estimated): November 3, 2026
• Last Updated: October 2, 2026

Record last verified: 2026-09

Data Sharing

• IPD Sharing: Will share

Locations

CA (1)