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    Fenebrutinib (RG7845)

    Modality: Bruton’s tyrosine kinase inhibitor (BTKi)

    Disease State: Multiple Sclerosis (MS)

    Summary

    Fenebrutinib is an investigational, potent, non-covalent, reversible Bruton’s tyrosine kinase inhibitor (BTKi) in Phase III studies for Relapsing Multiple Sclerosis (RMS) and Primary Progressive Multiple Sclerosis (PPMS).1

    Clinical Trials

    Multiple Sclerosis
    Phase Enrollment Status Title
    Phase II ENROLLING A Pharmacokinetics (PK), Pharmacodynamics (PD), Safety and Tolerability Study of Fenebrutinib in Children and Adolescents With Relapsing Multiple Sclerosis (RMS) (FENerations1) View Details
    Phase II ACTIVE, NOT ENROLLING A Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Efficacy of Fenebrutinib in Relapsing Multiple Sclerosis (FENopta) View Details
    Phase III ACTIVE, NOT ENROLLING A Phase III Multicenter, Randomized, Double-Blind, Double-Dummy, Parallel-Group Study to Evaluate the Efficacy and Safety of Fenebrutinib Compared With Ocrelizumab in Adult Patients With Primary Progressive Multiple Sclerosis (FENtrepid) View Details
    Phase III ACTIVE, NOT ENROLLING A Phase III Multicenter Randomized, Double-Blind, Double-Dummy, Parallel-Group Study to Evaluate the Efficacy and Safety of Fenebrutinib Compared With Teriflunomide in Adult Patients With Relapsing Multiple Sclerosis (FENhance 1) View Details
    Phase III ACTIVE, NOT ENROLLING A Phase III Multicenter Randomized, Double-Blind, Double-Dummy, Parallel-Group Study to Evaluate the Efficacy and Safety of Fenebrutinib Compared With Teriflunomide in Adult Patients With Relapsing Multiple Sclerosis (FENhance 2) View Details

    Proposed Mechanism of Action

    Bruton’s tyrosine kinase (BTK) plays a central role in the activation of B cells and myeloid cells (macrophages, microglia).2,3

    Bruton’s tyrosine kinase is an enzyme that plays a key role in B cell receptor-mediated signaling and activation of B cells, and fragment crystallizable (Fc) receptor signaling in myeloid lineage cells such as macrophages, monocytes and neutrophils.4,5

    Fenebrutinib is designed as a BTK inhibitor to inhibit B cell and microglia activation.1,3

    Understanding of BTK function(s) and effect(s) of BTKis in microglia is less advanced compared to B cells.
    1. Whang JA, Chang BY. Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis. Drug Discov Today. 2014;19(8):1200-1204. doi:10.1016/​j.drudis.2014.03.028. 2. Crawford JJ, Johnson AR, Misner DL, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018;61(6):2227-2245. doi:10.1021/​acs.jmedchem.7b01712. 3. Weber MS, Harp C, Bremer M, et al. Compared with evobrutinib and tolebrutinib, fenebrutinib displays highest in vitro potency on both B cells and myeloid progenitor lineage cells. Poster presented at: American Academy of Neurology (AAN) 2021 Virtual Annual Meeting; April 17-22, 2021. Poster P15.091. 4. Bar-Or A, Oh J, Dufek M, et al. Fenebrutinib maintains low disease activity in relapsing multiple sclerosis: clinical, safety and biomarker results from the FENopta open-label extension. Poster presented at: ACTRIMS 2025; February 27–March 1, 2025; West Palm Beach, FL. Presentation P091. 5. Johnson A, Wittwer A, Pufahl R, et al. How does fenebrutinib work? exploring kinetic and mechanistic features that influence BTK potency, selectivity and pharmacology. Poster presented at: ACTRIMS 2025; February 27–March 1, 2025; West Palm Beach, FL. Poster P146.

    1. Johnson A, Wittwer A, Pufahl R, et al. How does fenebrutinib work? exploring kinetic and mechanistic features that influence BTK potency, selectivity and pharmacology. Poster presented at: ACTRIMS 2025; February 27–March 1, 2025; West Palm Beach, FL. Poster P146.
    2. Airas L, Bermel RA, Chitnis T, et al. A review of Bruton's tyrosine kinase inhibitors in multiple sclerosis. Ther Adv Neurol Disord. 2024;17:17562864241233041. Published 2024 Apr 17. doi:10.1177/​17562864241233041
    3. Bar-Or A, Oh J, Dufek M, et al. Fenebrutinib maintains low disease activity in relapsing multiple sclerosis: clinical, safety and biomarker results from the FENopta open-label extension. Poster presented at: ACTRIMS 2025; February 27–March 1, 2025; West Palm Beach, FL. Presentation P091.
    4. Whang JA, Chang BY. Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis. Drug Discov Today. 2014;19(8):1200-1204. doi:10.1016/​j.drudis.2014.03.028.
    5. Crawford JJ, Johnson AR, Misner DL, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018;61(6):2227-2245. doi:10.1021/​acs.jmedchem.7b01712

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    TOP

    • BTK
      Bruton’s tyrosine kinase

    • BTKi
      Bruton’s tyrosine kinase inhibitor

    • CNS
      Central nervous system

    • Fc
      Fragment crystallizable

    • MOA
      Mechanism of action

    • MS
      Multiple sclerosis

    • PD
      Pharmacodynamics

    • PK
      Pharmacokinetics

    • PPMS
      Primary progressive multiple sclerosis

    • RMS
      Relapsing multiple sclerosis