Tolebrutinib: First Approval

Trojano M, Paolicelli D. Targeting smouldering neuroinflammation in multiple sclerosis: insights from tolebrutinib clinical trials. Lancet Reg Health Eur. 2025;54(101359):1–2.

Google Scholar 

Emirates News Agency-WAM. Emirates Drug Establishment grants global first approval for ‘Tolebrutinib’ [media release]. 26 Aug 2025. http://www.wam.ae.

Sanofi. CENRIFKI® (tolebrutinib) film coated tablets, for oral use: UAE package leaflet. 2025.

Sanofi. Update on the US regulatory review of tolebrutinib in non-relapsing, secondary progressive multiple sclerosis [media release]. 22 Sep 2025. http://www.sanofi.com.

Sanofi. Sanofi, Principia agree to develop multiple sclerosis drug candidate [media release]. 9 Nov 2017. http://en.sanofi.com.

Sanofi. Sanofi to acquire Principia Biopharma [media release]. 17 Aug 2020. http://www.sanofi.com.

Sanofi. Sanofi completes Principia Biopharma Inc. acquisition [media release]. 28 Sep 2020. http://www.sanofi.com.

Owens TD, Smith PF, Redfern A, Xing Y, Shu J, Karr DE, et al. Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168). Clin Transl Sci. 2022;15(2):442–50. https://doi.org/10.1111/cts.13162.

Article  PubMed  CAS  Google Scholar 

Fox RJ, Bar-Or A, Traboulsee A, et al. Tolebrutinib in nonrelapsing secondary progressive multiple sclerosis. N Engl J Med. 2025;392(19):1883–92.

Article  PubMed  CAS  Google Scholar 

Turner TJ, Brun P, Gruber RC, et al. Comparative CNS pharmacology of the Bruton’s tyrosine kinase (BTK) inhibitor tolebrutinib versus other BTK inhibitor candidates for treating multiple sclerosis. Drugs R D. 2024;24(2):263–74.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Cabanis M-J, Nicolas O, Vitse O, Cabanis M-J, Jan C, Brun P, et al. A phase I trial assessing the safety, pharmacokinetics, cerebrospinal fluid penetrance, and food effect of BTK inhibitor tolebrutinib in healthy volunteers. Clin Transl Sci. 2024;17(2):e13693. https://doi.org/10.1111/cts.13693.

Article  PubMed Central  CAS  Google Scholar 

Gaitan MI, Raza S, Donnay C, et al. Primary outcome of a phase 2 clinical trial of tolebrutinib, a brain-penetrant BTK inhibitor, for the modulation of chronically inflamed white matter lesions in MS [abstract no. LB1.2]. Mult Scler J. 2024;30(Suppl 1):11.

Google Scholar 

Nicolas O, Moliner P, Soubayrol P, et al. Absorption, metabolism, and excretion of [14C]-tolebrutinib after oral administration in humans, contribution of the metabolites to pharmacological activity. Clin Drug Investig. 2023;43(8):653–65.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Oh J, Arnold DL, Cree BAC, et al. Tolebrutinib versus teriflunomide in relapsing multiple sclerosis. N Engl J Med. 2025;392(19):1893–904.

Article  PubMed  CAS  Google Scholar 

Reich DS, Arnold DL, Vermersch P, et al. Safety and efficacy of tolebrutinib, an oral brain-penetrant BTK inhibitor, in relapsing multiple sclerosis: a phase 2b, randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2021;20(9):729–38.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Oh J, Fox RJ, Arnold DL, Syed S, Dukovic D, Vargas WS, et al. Tolebrutinib phase 2b long-term extension study: two-year safety, MRI, and clinical efficacy outcomes in patients with relapsing multiple sclerosis. Neurol Open Access. 2025;1(3):e000028. https://doi.org/10.1212/WN9.0000000000000028.

Article  Google Scholar 

Oh J, Reich D, Traboulsee A, et al. Safety and clinical efficacy outcomes from the long-term extension study of tolebrutinib in participants with relapsing multiple sclerosis: 3-year results [abstract no. P278/1470 plus poster]. Mult Scler J. 2023;29(Suppl 3):334–5.

Google Scholar 

Fox R, Reich D, Traboulsee A, et al. Baseline characteristics in the tolebrutinib phase 3 primary progressive multiple sclerosis PERSEUS clinical trial [abstract no. EPV-626 plus poster]. Eur J Neurol. 2025;32(Suppl 1):63.

Google Scholar 

Comments (0)

No login
gif