Tolebrutinib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Tolebrutinib
- Molecular weight
- 455.52
- Structure (SMILES)
- C=CC(=O)N1CCC[C@@H](n2c(=O)n(-c3ccc(Oc4ccccc4)cc3)c3c(N)nccc32)C1
- 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
- ATC classification codes
- L04AA62
- CAS registry numbers
- 1971920-73-6
- ChEMBL ID
- CHEMBL4650323
- InChIKey
- KOEUOFPEZFUWRF-LJQANCHMSA-N
- PubChem compound IDs
- 124111565
- FDA ingredient codes (UNII)
- 8CZ82ZYY9X
- 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
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- tolebrutinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
- 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
- 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
- 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
- NCT03889639
- NCT03996291
- NCT04171310
- NCT04410978
- NCT04410991
- NCT04742400
- NCT06064539
- NCT06106074
- NCT04411641
- NCT06372145
- NCT04458051
- NCT05282030
- 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
- 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.
- 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 Phase 1
- Multiple sclerosis Phase 3
- Primary progressive multiple sclerosis Phase 3
- Secondary progressive multiple sclerosis Phase 3
Targets (1)
- BTK Tyrosine-protein kinase BTK inhibitor