Roche's BTK Inhibitor Fenebrutinib Achieves Primary Endpoint in First Pivotal Phase III Study for Multiple Sclerosis
Roche
Oncology Drug Research, Development, and Manufacturing
Today, Roche officially announced the development of its BTK inhibitorfenebrutinibThe first study in the pivotal Phase III program met its primary endpoint. FenebrutinibIs aOral, Reversible, Non-covalentBruton's tyrosine kinase (BTK) inhibitor,Expected to become the first and onlyBTK Inhibitor。
Fenebrutinib is a dual inhibitor of B cell and microglial activation, and this dual inhibition may reduce disease activity and disability progression in multiple sclerosis. Its mechanism of action involves targeting B cells and microglia in the immune system. This design enables it to act systemically and cross the blood-brain barrier into the central nervous system, targeting chronic inflammation.
As a new generation of BTK inhibitor, its core advantage lies in the ability to penetrate the blood-brain barrier, showing potential for the treatment of multiple sclerosis (MS). This drug is also regarded by Wall Street analysts as a potential blockbuster.
Main Features and Mechanisms:
High Selectivity: 130-fold selectivity for BTK over other kinases.
Dual Inhibition: It can not only suppress B-cell activation but also inhibit microglial activation, which may help reduce MS disease activity and disability progression.
Crossing the Blood-Brain Barrier: Biomarker testing shows that fenebrutinib can reach effective concentrations in the central nervous system, thereby inhibiting brain inflammation.
Clinical Trial Progress:
The first of two pivotal RMS studies (FENhance 2) met its primary endpoint, showing investigationalfenebrutinibSignificantly reduced relapse rate compared to teriflunomide,
In a pivotal PPMS study (FENtrepid),fenebrutinibThe effect of delaying disability progression is at least non-inferior to Ocrevus®, the only currently approved therapy for PPMS.
The full data from the study will be presented at upcoming medical conferences; results from the second RMS study (FENhance 1) are expected in the first half of 2026.
About FENhance 1 and 2 and FENtrepid Studies
FENhance 1 and 2 are similarly designed Phase III multicenter, randomized, double-blind, double-dummy, parallel-group studies aimed at evaluating the efficacy and safety of investigational fenebrutinib compared to teriflunomide in enrolled adult patients with RMS, with a treatment period of at least 96 weeks. The primary endpoint is the annualized relapse rate. Key secondary endpoints include the time to onset of confirmed disability progression sustained for 24 weeks, 12 weeks, and 24 weeks. After the double-blind treatment period, patients have the option to enter an open-label extension phase, during which all patients receive fenebrutinib treatment.
FENtrepid is a Phase III multicenter, randomized, double-blind, double-dummy, parallel-group study designed to evaluate the efficacy and safety of fenebrutinib compared to Ocrevus® in adult patients with PPMS. Eligible participants are randomized 1:1 to receive once-daily oralfenebrutinib(Intravenous infusion of Ocrevus® matched with placebo) or (intravenous infusion of Ocrevus® plus daily oral fenebrutinib matched with placebo) treatment, with a treatment period of at least 120 weeks.
About Ocrevus Injection:
Ocrelizumab (Orelizumab Injection) developed by Roche, trade name: OCREVUS. Ocrelizumab is the first and only therapy approved for RMS and PPMS, with more than 300,000 patients treated worldwide. The phase III study results of the subcutaneous injection formulation of this drug have also been released.
Relevant Links:
MS Information Station | Roche's Ocrelizumab (Ocrevus) Approved for Marketing in China
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