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

NCT07855250 — Phase 1, Active not recruiting, 14 participants, Sanofi

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A Phase-1, Open-label, One-sequence, Two-treatment Period, Cross-over, Drug-drug Interaction Study to Evaluate the Effect of Oral Rilzabrutinib on P-gp, BCRP, OATP1B1 and OATP1B3 Substrates in Healthy Participants

Registry	NCT07855250
Status	Active not recruiting
Phase	Phase 1
Study type	Interventional; na, single group, masking: none, basic science
Enrollment	14 (Estimated)
Sponsor	Sanofi (Industry)
Conditions	Healthy Volunteer
Interventions	Rilzabrutinib, Rosuvastatin, Digoxin (Drug)
Dates	start 2026-10-01, primary completion 2026-11-03 (estimated), completion 2026-11-03 (estimated), first posted 2026-10-02, last updated 2026-10-21
Locations	1 site in Canada

-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.

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+Arms and interventions

Arm	Type	Interventions	Description
Treatment A then Treatment B	Experimental	Drug: Rilzabrutinib; Drug: Rosuvastatin; Drug: Digoxin	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

Rilzabrutinib (Drug), also known as SAR444671: From Day 1 to Day 12 of Period 2
Rosuvastatin (Drug), also known as Crestor: Single dose on Day 1 of Period 1 and on Day 8 of Period 2
Digoxin (Drug), also known as Lanicor: Single dose on Day 1 of Period 1 and on Day 8 of Period 2

+Outcome measures

Primary outcomes

AUC for digoxin and rosuvastatin [Up to Day 13 in Period 2]: area under curve
AUClast for digoxin and rosuvastatin [Up to Day 13 in Period 2]: area under the curve from time zero to the last measurable concentration
Cmax for digoxin and rosuvastatin [Up to Day 13 in Period 2]: maximum (peak) plasma concentration

Secondary outcomes

tmax for digoxin and for rosuvastatin [Up to Day 13 in Period 2]: time to reach maximum plasma concentration
tmax for rilzabrutinib [Up to Day 11 in Period 2]: time to reach maximum plasma concentration
Cmax for rilzabrutinib [Up to Day 11 in Period 2]: maximum (peak) plasma concentration
AUC0-tau for rilzabrutinib [Up to Day 11 in Period 2]: area under the plasma concentration-time curve from time 0 to tau
Assessment of AEs and TEAEs [Up to Day 21 in Period 2]: including clinical laboratory evaluation, vital signs, and electrocardiogram (ECG).

+Eligibility

Sex: All, ages: 18 Years to 55 Years, accepts healthy volunteers

Inclusion Criteria

* 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

Exclusion Criteria

* History of serious infections requiring intravenous therapy.
* Frequent headaches, migraine, nausea or vomiting.
* Blood donation within 1 month before inclusion.
* 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.

+Locations (1)

Facility	City	Country	Status
Investigational Site Number : 1240001	Québec, Quebec	Canada