> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/tolebrutinib-b5990158-f7fd-4e57-bbf2-d7588c1fff05
> Record changed: 2026-10-13

# Tolebrutinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

**Drug name**

Tolebrutinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

**Molecular weight**

455.52

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

**Structure (SMILES)**

C=CC(=O)N1CCC\[C@@H\](n2c(=O)n(-c3ccc(Oc4ccccc4)cc3)c3c(N)nccc32)C1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

### Other names (19)

- prn 2246
- PRN-2246
- prn2246
- PRN2246
- sar 442168
- SAR-442168
- sar442168
- Sar442168
- SAR442168
- tolebrutinib
- Tolebrutinib
- tolebrutinib \[INN\]
- TOLEBRUTINIB \[USAN\]
- Tolebrutinib \[WHO-DD\]
- tolebrutinib 120mg
- tolebrutinib 60mg
- tolebrutinib inn
- tolebrutinib usan
- tolebrutinib who dd

## Identifiers

**ATC classification codes**

- L04AA62

**CAS registry numbers**

- 1971920-73-6

**ChEMBL ID**

CHEMBL4650323

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

**InChIKey**

KOEUOFPEZFUWRF-LJQANCHMSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650323)

**PubChem compound IDs**

- 124111565

**FDA ingredient codes (UNII)**

- 8CZ82ZYY9X

## Regulatory information

### European Union

**Status**

Authorised

**Status date**

19 Jun 2026

**Authorisation date**

19 Jun 2026

**Approved indications**

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

**Product number**

EMEA/H/C/006386

**Authorisation holder**

Sanofi Winthrop Industrie

**Priority medicines scheme**

No

**Generic**

No

**Biosimilar**

No

**Generic medicines**

0

**Biosimilar medicines**

0

**Advanced therapy**

No

**Conditional approval**

No

**Additional monitoring**

Yes

**Accelerated assessment**

No

**Exceptional circumstances**

No

#### Therapeutic areas

- Multiple Sclerosis, Chronic Progressive

European medicines record

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/cenrifki)

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

tolebrutinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
Bruton tyrosine kinase

**Gene symbol**  
BTK

**Protein identifier**  
Q06187

**Median affinity**

7.67

**Affinity units**  
pIC50
- **Mechanism**  
Tyrosine-protein kinase BTK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase BTK

**Protein identifier**  
Q06187

### Open Targets mechanisms

- **Mechanism**  
Tyrosine-protein kinase BTK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase BTK

### Investigated indications (4)

- **Condition**  
Kidney Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003086

**Subject identifier**  
D007674
- **Condition**  
Multiple Sclerosis, Chronic Progressive

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0008520

**Subject identifier**  
D020528
- **Condition**  
Multiple Sclerosis, Chronic Progressive

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0008522

**Subject identifier**  
D020528
- **Condition**  
Multiple Sclerosis

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0005301

**Subject identifier**  
D009103

### Open Targets indications (5)

- **Condition identifier**  
EFO\_0003086

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0008520

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005284

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005301

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0009688

**Highest recorded phase**  
3

### Trial references (12)

- NCT03889639  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03889639)
- NCT03996291  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03996291)
- NCT04171310  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04171310)
- NCT04410978  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04410978)
- NCT04410991  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04410991)
- NCT04742400  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04742400)
- NCT06064539  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06064539)
- NCT06106074  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06106074)
- NCT04411641  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04411641)
- NCT06372145  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06372145)
- NCT04458051  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04458051)
- NCT05282030  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05282030)

## Chemical properties

**Hydrogen bond acceptors**

7

**Hydrogen bond donors**

1

**Polar surface area**

95.38

**Calculated partition coefficient (ALogP)**

3.91

**Calculated partition coefficient (XLogP)**

3.2

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

5

**Heavy atoms**

34

**Molecular formula**

C26H25N5O3

**Monoisotopic mass**

455.19573968

**Natural product**

No

## Evidence counts

**Recorded assays**

31

**Active assays**

9

### Active assay types

- Confirmatory

## Related records

### Trials (13)

- [A Study to Investigate Long-term Safety and Tolerability of Tolebrutinib in Participants With Multiple Sclerosis.](https://trialight.com/data/trial/a-study-to-investigate-long-term-safety-and-tolerability-of-cdd4fe6f-9a19-4ce7-924a-3df50888513c.md)
- Dose-finding Study for SAR442168 in Relapsing Multiple Sclerosis
- Long Term Safety and Efficacy Study of Tolebrutinib (SAR442168) in Participants With Relapsing Multiple Sclerosis
- Nonrelapsing Secondary Progressive Multiple Sclerosis (NRSPMS) Study of Bruton's Tyrosine Kinase (BTK) Inhibitor Tolebrutinib (SAR442168) (HERCULES)
- Primary Progressive Multiple Sclerosis (PPMS) Study of Bruton's Tyrosine Kinase (BTK) Inhibitor Tolebrutinib (SAR442168) (PERSEUS)
- Relapsing Forms of Multiple Sclerosis (RMS) Study of Bruton's Tyrosine Kinase (BTK) Inhibitor Tolebrutinib (SAR442168) (GEMINI 1)
- Relapsing Forms of Multiple Sclerosis (RMS) Study of Bruton's Tyrosine Kinase (BTK) Inhibitor Tolebrutinib (SAR442168) (GEMINI 2)
- Study of Drug-drug Interaction of the Effects of Gemfibrozil and Rifampicin on SAR442168 in Healthy Adult Subjects
- Study of Excretion Balance and Pharmacokinetics of \[14C\]-SAR442168 in Healthy Male Subjects
- Study of the Tolerability and Pharmacokinetics of Oral Doses of SAR442168 With a Food Effect Investigation in Healthy Adult Participants
- Study to Assess the Plasma Concentration of Tolebrutinib Given as a Tablet to Adult Participants With Mild Hepatic Impairment Compared to Participants With Normal Hepatic Function
- Study to Assess the Plasma Concentration of Tolebrutinib Given as a Tablet to Adult Participants With Renal Impairment Compared to Healthy Participants.
- Tolebrutinib, a Brain-penetrant Bruton's Tyrosine Kinase Inhibitor, for the Modulation of Chronically Inflamed White Matter Lesions in Multiple Sclerosis

### In development for (4)

- [Kidney disorder](https://trialight.com/data/condition/kidney-disorder-e50371fe-f1a7-53fe-9cfb-9d6da9130e3c.md) Phase 1
- [Multiple sclerosis](https://trialight.com/data/condition/multiple-sclerosis-62806c95-fe1b-529e-bd16-95cb92d15375.md) Phase 3
- Primary progressive multiple sclerosis Phase 3
- [Secondary progressive multiple sclerosis](https://trialight.com/data/condition/secondary-progressive-multiple-sclerosis-c559b49a-e39f-545b-aab5-dd41263dd2f6.md) Phase 3

### Targets (1)

- [BTK](https://trialight.com/data/target/btk-0715d96c-6e26-5c6e-a6e0-2a745512051d.md) Tyrosine-protein kinase BTK inhibitor

---

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