Autoimmune DisorderPhase 1NCT06342700
A Food Effect and Relative Bioavailability Study of Rilzabrutinib in Healthy Participants
A Phase 1 study testing Rilzabrutinib crystalline form and Rilzabrutinib amorphous form in people with Autoimmune Disorder and Healthy Volunteers, run by Sanofi at 1 site in United States.
Trial summary
This is a cross-over, Phase 1, 4-arm study. The purpose of this study is to measure the relative bioavailability and food effect of crystalline formulation rilzabrutinib and amorphous formulation rilzabrutinib in healthy male and female participants aged 18 to 55 years of age. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Autoimmune Disorder, Healthy Volunteers
- What is being tested?
- Rilzabrutinib crystalline form and Rilzabrutinib amorphous form
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 28 participants
- Where
- 1 siteUnited States
- Study dates
- 25 Mar 2024to 23 Apr 2024
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Body weight between 50.0 and 100.0 kg, inclusive, if male, and between 40.0 and 90.0 kg, inclusive, if female, body mass index (BMI) between 18.0 and 32.0 kg/m2, inclusive
- Laboratory parameters within the normal range, unless the Investigator considers an abnormality to be clinically irrelevant for healthy participant. Hepatic transaminases (aspartate aminotransferase, alanine aminotransferase) should not exceed 1.25 × the upper laboratory norm (ULN); total bilirubin should not exceed 1 × ULN
- Willing to abstain from using tobacco or nicotine-containing products or consuming alcohol from check-in (Day -1) until discharge at end-of-study visit
- Willing to abstain from taking any prescription drugs, dietary supplements, or non-prescription drugs within 14 days or 5 half-lives, whichever, is longer, prior to the first dose of study drug through the follow-up phone call. Use of hormonal contraception and aspirin (at doses of ≤2000 mg/day) or ibuprofen (at doses of ≤1200 mg/day) are allowed prior to and during the study
- Negative urine drug/alcohol testing at screening and check-in (Day -1). Screening urine drug/alcohol testing may be repeated once if deemed appropriate by the site Investigator
- Willing to abstain from consuming grapefruit, star fruit, or Seville orange-containing products from 14 days prior to first dose of study drug until discharge from the clinical study unit
Who cannot join
- Any history or presence of clinically relevant cardiovascular, pulmonary, gastrointestinal, hepatic, renal, metabolic, hematological, neurological, osteomuscular, articular, psychiatric, systemic, ocular, gynecologic (if female), infectious disease, or signs of acute illness
- Participant has clinical signs and symptoms consistent with COVID-19, eg, fever, dry cough, dyspnea, loss of taste and smell, sore throat, fatigue or confirmed infection by appropriate laboratory test within the last 4 weeks prior to Screening. Participant who had severe course of COVID-19 (ie, hospitalization, extracorporeal membrane oxygenation [ECMO], mechanically ventilated)
- Participant has a positive test result for SARS-CoV-2 (measured via Real-time Reverse Transcriptase Polymerase Chain Reaction [RT-PCR] or Rapid Antigen Test [RAT])
- Frequent headaches and/or migraine, recurrent nausea and/or vomiting (for vomiting only: more than twice a month)
- Blood donation, any volume, within 1 month before inclusion
- Symptomatic postural hypotension, irrespective of the decrease in blood pressure, or asymptomatic postural hypotension defined as a decrease in systolic blood pressure <30 mmHg within 3 minutes when changing from supine to standing position
Show all 21Show fewer
- Presence or history of drug hypersensitivity, or allergic disease diagnosed and treated by a physician. Participants with known hypersensitivity to any component of the IMP formulation or allergic disease diagnosed and treated by a physician
- History or presence of drug or alcohol abuse (alcohol consumption more than 40 g per day on a regular basis)
- Regular intake of nicotine (via patch, smoking, vaping or other forms) more than 10 mg per day (based on the average nicotine content of 10-12 mg of nicotine per cigarette and inhalation of up to 2 mg of nicotine per cigarette), and unable to stop smoking during the study (occasional smoker can be enrolled)
- Excessive consumption of beverages containing xanthine bases (more than 4 cups or glasses per day)
- If female, pregnancy (defined as positive β-HCG blood test), or breast-feeding
- Any medication (including St John's Wort or ginseng) within 14 days before inclusion or within 5 times the elimination half-life or pharmacodynamic half-life of the medication, with the exception of aspirin/ibuprofen, hormonal contraception, and menopausal hormone replacement therapy
- Any vaccination within the last 28 days and any biologics (antibody or its derivatives) given within 4 months before inclusion:
- Non-live vaccines, including COVID-19: last administration of a vaccine within 4 weeks before randomization
- Live vaccines: last administration of a vaccine within 3 months before randomization
- Positive result on any of the following tests: hepatitis B surface antigen (HBs Ag), anti-hepatitis C virus (anti-HCV) antibodies, anti-human immunodeficiency virus 1 and 2 antibodies (anti-HIV1 and anti HIV2 Ab)
- Positive result on urine drug screen (amphetamines/methamphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine, opiates)
- Positive alcohol breath or alcohol urine test
- Positive pregnancy test
- Gilbert's Syndrome
- The above information is not intended to contain all considerations relevant to a participant's potential participation in a clinical trial.
Trial locations and contacts
1 site in 1 country.
United States1 site
Nucleus Network Site Number : 8400001
Saint Paul, Minnesota, 55114
About this study
Official title: A Randomized, Open-label, Single-dose, 4-period, 4--sequence, Crossover Phase I Relative Bioavailability Study Comparing Crystalline Formulation Tablet Versus Reference Amorphous Formulation Tablet of Rilzabrutinib (SAR444671) in Fasted and Fed Conditions in Healthy Male and Female Participants
This is a cross-over, Phase 1, 4-arm study. The purpose of this study is to measure the relative bioavailability and food effect of crystalline formulation rilzabrutinib and amorphous formulation rilzabrutinib in healthy male and female participants aged 18 to 55 years of age.
The total study duration per participant is expected to be up to 36 days, including:
- Screening: up to 4 weeks
- Treatment periods: once successfully screened, enrolled participants will be randomized to 1 of 4 treatment sequences with 4 single dose treatment periods.
- Washout: One day washout is planned after each treatment period hence providing 2 days between doses.
- Safety follow-up: participants will be asked to participate in an end-of-study safety assessment upon discharge from the clinical study unit, ie, on Day 8 of the study.
- Conditions
- Autoimmune Disorder, Healthy Volunteers
- Being tested
- Rilzabrutinib crystalline form, Rilzabrutinib amorphous form
- Medical subject headings
- Autoimmune Diseases
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Rilzabrutinib crystalline formDrug
Also called SAR444671
Pharmaceutical form:Film coated tablet Route of administration:Oral
Rilzabrutinib amorphous formDrug
Also called SAR444671
Pharmaceutical form:Film coated tablet Route of administration:Oral
| Study group | Role | What they receive |
|---|---|---|
| Treatment A: SAR444671 amorphous fasted | Active comparator | Participants will receive single oral dose of amorphous tablet formulation rilzabrutinib (SAR444671) under fasted conditions on Day 1 for one period Receives: Drug: Rilzabrutinib amorphous form |
| Treatment B: SAR444671 crystalline fasted | Experimental | Participants will receive single oral dose of crystalline tablet formulation rilzabrutinib (SAR444671) under fasted conditions on Day 1 for one period Receives: Drug: Rilzabrutinib crystalline form |
| Treatment C: SAR444671 amorphous fed | Active comparator | Participants will receive single oral dose of amorphous tablet formulation rilzabrutinib (SAR444671) under fed conditions on Day 1 for one period Receives: Drug: Rilzabrutinib amorphous form |
| Treatment D: SAR444671 crystalline fed | Experimental | Participants will receive single oral dose of crystalline tablet formulation rilzabrutinib (SAR444671) under fed conditions on Day 1 for one period Receives: Drug: Rilzabrutinib crystalline form |
What is being measured
The primary outcome is the main question the study is designed to answer.
Relative bioavailability as assessed by rilzabrutinib Cmax following administration of the test and reference formulations in the fasted state
Cmax: maximum plasma concentration
Measured: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUClast following administration of the test and reference formulations in the fasted state
AUClast: area under the plasma concentration versus time curve from time zero to the last measurable concentration
Measured: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUC following administration of the test and reference formulations in the fasted state
AUC: area under the plasma concentration versus time curve extrapolated to infinity
Measured: Day 1 to Day 8
Secondary outcomes (7)
Relative bioavailability as assessed by rilzabrutinib Cmax following administration of the test and reference formulations in the fed state
Cmax: maximum plasma concentration
Measured: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUClast following administration of the test and reference formulations in the fed state
AUClast: area under the plasma concentration versus time curve from time zero to the last measurable concentration
Measured: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUC following administration of the test and reference formulations in the fed state
AUC: area under the plasma concentration versus time curve extrapolated to infinity
Measured: Day 1 to Day 8
Food effects as assessed by rilzabrutinib Cmax following administration of the test and reference formulations under the fed versus fasted state
Cmax: maximum plasma concentration
Measured: Day 1 to Day 8
Food effects as assessed by rilzabrutinib AUClast following administration of the test and reference formulations under the fed versus fasted state
AUClast: area under the plasma concentration versus time curve from time zero to the last measurable concentration
Measured: Day 1 to Day 8
Food effects as assessed by rilzabrutinib AUC following administration of the test and reference formulations under the fed versus fasted state
AUC: area under the plasma concentration versus time curve extrapolated to infinity
Measured: Day 1 to Day 8
Number of participants with adverse events, treatment-emergent adverse events, serious adverse events and adverse events of special interest
Measured: Day 1 to Day 8
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted2 Apr 2024
- Study start25 Mar 2024
- Primary completion23 Apr 2024
- Study completion23 Apr 2024
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Autoimmune DisorderStudies of the same condition, open and under way.
- More trials run by SanofiThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 28 participants (actual)
Sponsor and investigators
- Lead sponsor
- Sanofi
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT06342700
- Sponsor's protocol ID
- PKM18138
- Other IDs
- U1111-1299-1906
- Status last verified
- Aug 2025
- First submitted
- 18 Mar 2024
- Last updated
- 3 Sep 2025
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- Yes: 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
Study at a glance
From the registry record, last updated by the sponsor on 3 Sep 2025. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Randomized, Open-label, Single-dose, 4-period, 4--sequence, Crossover Phase I Relative Bioavailability Study Comparing Crystalline Formulation Tablet Versus Reference Amorphous Formulation Tablet of Rilzabrutinib (SAR444671) in Fasted and Fed Conditions in Healthy Male and Female Participants
- ClinicalTrials.gov ID
- NCT06342700
- Acronym / sponsor ID
- PKM18138
- Conditions
- Autoimmune Disorder, Healthy Volunteers
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 28 participants (actual)
- Lead sponsor
- SanofiIndustry (pharma, biotech, devices)
- Study start
- 25 Mar 2024 (actual)
- Primary completion
- 23 Apr 2024 (actual)
- Study completion
- 23 Apr 2024 (actual)
- First posted
- 2 Apr 2024 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is a cross-over, Phase 1, 4-arm study. The purpose of this study is to measure the relative bioavailability and food effect of crystalline formulation rilzabrutinib and amorphous formulation rilzabrutinib in healthy male and female participants aged 18 to 55 years of age.
The total study duration per participant is expected to be up to 36 days, including:
- Screening: up to 4 weeks
- Treatment periods: once successfully screened, enrolled participants will be randomized to 1 of 4 treatment sequences with 4 single dose treatment periods.
- Washout: One day washout is planned after each treatment period hence providing 2 days between doses.
- Safety follow-up: participants will be asked to participate in an end-of-study safety assessment upon discharge from the clinical study unit, ie, on Day 8 of the study.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 4
| Arm | Type | Receives |
|---|---|---|
| Treatment A: SAR444671 amorphous fasted | Active comparator | Drug: Rilzabrutinib amorphous formParticipants will receive single oral dose of amorphous tablet formulation rilzabrutinib (SAR444671) under fasted conditions on Day 1 for one period |
| Treatment B: SAR444671 crystalline fasted | Experimental | Drug: Rilzabrutinib crystalline formParticipants will receive single oral dose of crystalline tablet formulation rilzabrutinib (SAR444671) under fasted conditions on Day 1 for one period |
| Treatment C: SAR444671 amorphous fed | Active comparator | Drug: Rilzabrutinib amorphous formParticipants will receive single oral dose of amorphous tablet formulation rilzabrutinib (SAR444671) under fed conditions on Day 1 for one period |
| Treatment D: SAR444671 crystalline fed | Experimental | Drug: Rilzabrutinib crystalline formParticipants will receive single oral dose of crystalline tablet formulation rilzabrutinib (SAR444671) under fed conditions on Day 1 for one period |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (6 listed)
- Body weight between 50.0 and 100.0 kg, inclusive, if male, and between 40.0 and 90.0 kg, inclusive, if female, body mass index (BMI) between 18.0 and 32.0 kg/m2, inclusive
- Laboratory parameters within the normal range, unless the Investigator considers an abnormality to be clinically irrelevant for healthy participant. Hepatic transaminases (aspartate aminotransferase, alanine aminotransferase) should not exceed 1.25 × the upper laboratory norm (ULN); total bilirubin should not exceed 1 × ULN
- Willing to abstain from using tobacco or nicotine-containing products or consuming alcohol from check-in (Day -1) until discharge at end-of-study visit
- Willing to abstain from taking any prescription drugs, dietary supplements, or non-prescription drugs within 14 days or 5 half-lives, whichever, is longer, prior to the first dose of study drug through the follow-up phone call. Use of hormonal contraception and aspirin (at doses of ≤2000 mg/day) or ibuprofen (at doses of ≤1200 mg/day) are allowed prior to and during the study
- Negative urine drug/alcohol testing at screening and check-in (Day -1). Screening urine drug/alcohol testing may be repeated once if deemed appropriate by the site Investigator
Key exclusion criteria (21 listed)
- Any history or presence of clinically relevant cardiovascular, pulmonary, gastrointestinal, hepatic, renal, metabolic, hematological, neurological, osteomuscular, articular, psychiatric, systemic, ocular, gynecologic (if female), infectious disease, or signs of acute illness
- Participant has clinical signs and symptoms consistent with COVID-19, eg, fever, dry cough, dyspnea, loss of taste and smell, sore throat, fatigue or confirmed infection by appropriate laboratory test within the last 4 weeks prior to Screening. Participant who had severe course of COVID-19 (ie, hospitalization, extracorporeal membrane oxygenation [ECMO], mechanically ventilated)
- Participant has a positive test result for SARS-CoV-2 (measured via Real-time Reverse Transcriptase Polymerase Chain Reaction [RT-PCR] or Rapid Antigen Test [RAT])
- Frequent headaches and/or migraine, recurrent nausea and/or vomiting (for vomiting only: more than twice a month)
- Blood donation, any volume, within 1 month before inclusion
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Rilzabrutinib crystalline formAlso: SAR444671Pharmaceutical form:Film coated tablet Route of administration:Oral | Drug | Treatment B: SAR444671 crystalline fasted, Treatment D: SAR444671 crystalline fed |
| Rilzabrutinib amorphous formAlso: SAR444671Pharmaceutical form:Film coated tablet Route of administration:Oral | Drug | Treatment A: SAR444671 amorphous fasted, Treatment C: SAR444671 amorphous fed |
Primary outcome
Relative bioavailability as assessed by rilzabrutinib Cmax following administration of the test and reference formulations in the fasted state
Time frame: Day 1 to Day 8
Cmax: maximum plasma concentration
Relative bioavailability as assessed by rilzabrutinib AUClast following administration of the test and reference formulations in the fasted state
Time frame: Day 1 to Day 8
AUClast: area under the plasma concentration versus time curve from time zero to the last measurable concentration
Relative bioavailability as assessed by rilzabrutinib AUC following administration of the test and reference formulations in the fasted state
Time frame: Day 1 to Day 8
AUC: area under the plasma concentration versus time curve extrapolated to infinity
7 secondary outcomes
Relative bioavailability as assessed by rilzabrutinib Cmax following administration of the test and reference formulations in the fed state
Time frame: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUClast following administration of the test and reference formulations in the fed state
Time frame: Day 1 to Day 8
Relative bioavailability as assessed by rilzabrutinib AUC following administration of the test and reference formulations in the fed state
Time frame: Day 1 to Day 8
Food effects as assessed by rilzabrutinib Cmax following administration of the test and reference formulations under the fed versus fasted state
Time frame: Day 1 to Day 8
Food effects as assessed by rilzabrutinib AUClast following administration of the test and reference formulations under the fed versus fasted state
Time frame: Day 1 to Day 8
Food effects as assessed by rilzabrutinib AUC following administration of the test and reference formulations under the fed versus fasted state
Time frame: Day 1 to Day 8
Number of participants with adverse events, treatment-emergent adverse events, serious adverse events and adverse events of special interest
Time frame: Day 1 to Day 8
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 3 Sep 2025.
- PKM18138 Plain Language Results SummaryLink provided by the sponsor.
- Individual participant dataSharing planned: Yes. 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
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
The record lists no contact. Use the official record to reach the sponsor.
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Rilzabrutinib crystalline form and Rilzabrutinib amorphous form in people with Autoimmune Disorder and Healthy Volunteers, run by Sanofi at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 6 inclusion and 21 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 3 Sep 2025. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Relative bioavailability as assessed by rilzabrutinib Cmax following administration of the test and reference formulations in the fasted state (time frame: Day 1 to Day 8). The study lists 3 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 3 Sep 2025.