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Drug

Tolebrutinib

Approved · EMA
Late-stage development

Also known as 2h-imidazo(4,5-c)pyridin-2-one, 4-amino-1,3-dihydro-1-((3r)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl)-3-(4-phenoxyphenyl)-, 4-amino-1,3-dihydro-1-((3r)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl)-3-(4-phenoxyphenyl)-2h-imidazo(4,5-c)pyridin-2-one.

RxNorm2674331ChEMBLCHEMBL4650323UNII8CZ82ZYY9X
1
Active clinical trials
1
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Approval: Cenrifki (EMA)

Regulatory2026-06-19EMA

An Interventional, Phase 3 Extension Study to Investigate Long-term Safety and Tolerability of Tolebrutinib in Participants With Relapsing Multiple Sclerosis, Primary Progressive Multiple Sclerosis, or Nonrelapsing Secondary Progressive Multiple Sclerosis

Clinical trial2026-02-13Results expected Q2 2029 · ClinicalTrials.gov

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Primary Progressive Multiple Sclerosis (PERSEUS)

Clinical trial2025-11-14Completed · ClinicalTrials.gov

Long-term Extension Safety and Efficacy Study of SAR442168 in Participants With Relapsing Multiple Sclerosis

Clinical trial2025-10-23Results posted · ClinicalTrials.gov

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

Clinical trial2025-07-02Results posted · ClinicalTrials.gov

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

Clinical trial2025-07-02Results posted · ClinicalTrials.gov

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Nonrelapsing Secondary Progressive Multiple Sclerosis

Clinical trial2025-07-02Results posted · ClinicalTrials.gov

A Phase 2 Clinical Trial of Tolebrutinib, a Brain-penetrant Bruton's Tyrosine Kinase Inhibitor, for the Modulation of Chronically Inflamed White Matter Lesions in Multiple Sclerosis

Clinical trial2024-08-13Results posted · ClinicalTrials.gov

An Open-label, Multi-center Phase 1 Pharmacokinetic and Tolerability Study of Tolebrutinib Given as a Single Oral Dose in Participants With Renal Impairment and in Matched Participants With Normal Renal Function.

Clinical trial2022-08-02Completed · ClinicalTrials.gov

An Open-label Phase 1, Pharmacokinetic and Tolerability Study of Tolebrutinib Given as a Single Dose in Adult Participants With Mild Hepatic Impairment, and in Matched Participants With Normal Hepatic Function

Clinical trial2022-05-24Completed · ClinicalTrials.gov

A Randomized, Double-blind, Placebo-controlled Study of the Tolerability and Pharmacokinetics of Ascending Single and 14-day Repeated Oral Doses of SAR442168 With a Food Effect Investigation in Healthy Adult Participants

Clinical trial2022-05-23Completed · ClinicalTrials.gov

A Phase 1, Single-center, Open-label, Two-cohort, Two-period, One-sequence, Two Treatment, Drug-drug Interaction Study of the Effects of Gemfibrozil and Rifampicin on SAR442168 in Healthy Subjects

Clinical trial2020-07-08Completed · ClinicalTrials.gov

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Tolebrutinib
Aliases & brands
2h-imidazo(4,5-c)pyridin-2-one, 4-amino-1,3-dihydro-1-((3r)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl)-3-(4-phenoxyphenyl)-4-amino-1,3-dihydro-1-((3r)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl)-3-(4-phenoxyphenyl)-2h-imidazo(4,5-c)pyridin-2-one
RxNorm CUI
2674331
ChEMBL ID
CHEMBL4650323
UNII
8CZ82ZYY9X
Regulatory jurisdictions
ema

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval
2026-06-19
Latest approval
2026-06-19
Authorities
EMA
Total events
1
emaEuropean Medicines Agency· 1 event
2026-06-19Approval
Approval: Cenrifki (EMA)

Indication: Cenrifki is indicated for the treatment of adult patients with secondary progressive multiple sclerosis (SPMS) without relapses in the last 2 years.

Evidence ↗

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

11 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
11
registered trials across all phases
LATEST COMPLETION 2025
1
Active studies
5
Late-stage (III+)
9
Completed
1
Discontinued
PHASE DISTRIBUTIONn = 11
Phase 14Phase 22Phase 35

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

An Interventional, Phase 3 Extension Study to Investigate Long-term Safety and Tolerability of Tolebrutinib in Participants With Relapsing Multiple Sclerosis, Primary Progressive Multiple Sclerosis, or Nonrelapsing Secondary Progressive Multiple Sclerosis

Active, not recruitingPH IIIKey trialSanofin=2,5002029

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Primary Progressive Multiple Sclerosis (PERSEUS)

CompletedPH IIISanofin=7672025

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Nonrelapsing Secondary Progressive Multiple Sclerosis

CompletedPH IIIKey trialSanofin=1,1312024

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

CompletedPH IIISanofin=8992024

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

CompletedPH IIISanofin=9742024

Recent completions

Trials that read out recently, adding to the completed evidence base.

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Primary Progressive Multiple Sclerosis (PERSEUS)

CompletedPH IIISanofin=7672025

Long-term Extension Safety and Efficacy Study of SAR442168 in Participants With Relapsing Multiple Sclerosis

CompletedPH IISanofin=1252024

A Phase 3, Randomized, Double-blind, Efficacy and Safety Study Comparing SAR442168 to Placebo in Participants With Nonrelapsing Secondary Progressive Multiple Sclerosis

CompletedPH IIIKey trialSanofin=1,1312024

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

CompletedPH IIISanofin=8992024

A Phase 3, Randomized, Double-blind Efficacy and Safety Study Comparing SAR442168 to Teriflunomide (Aubagio®) in Participants With Relapsing Forms of Multiple Sclerosis

CompletedPH IIISanofin=9742024

An Open-label, Multi-center Phase 1 Pharmacokinetic and Tolerability Study of Tolebrutinib Given as a Single Oral Dose in Participants With Renal Impairment and in Matched Participants With Normal Renal Function.

CompletedPH ISanofin=222022
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.