Roche Announces Positive Phase II Results for Fenebrutinib in Relapsing Multiple Sclerosis

On May 17, Roche announced that the Phase II FENopta study of its third-generation BTK inhibitor fenebrutinib for the treatment of relapsing multiple sclerosis (RMS) had achieved positive results.

FENopta Study is a global, randomized, double-blind, placebo-controlled clinical trial that enrolled 109 patients with RMS aged 18-55, aiming to evaluate the efficacy, safety, and pharmacokinetics of fenebrutinib. The primary endpoint is the number of new gadolinium-enhancing T1 lesions detected by brain magnetic resonance imaging (MRI) at week 12. Secondary endpoints include the number of new or enlarging T2 lesions detected by brain MRI at weeks 4/8/12, the proportion of patients with new T1 lesions or new or enlarging T2 lesions at weeks 4/8/12, etc. T1 lesions are markers of active inflammation, while T2 lesions represent disease burden or lesion load.

The results showed that, compared with the placebo group, the number of new T1 lesions in the fenebrutinib group was significantly reduced (P=0.0022), and the number of new or enlarging T2 lesions was also significantly reduced. Moreover, the proportion of patients with new T1 lesions or new or enlarging T2 lesions was lower in the fenebrutinib group than in the placebo group.

BTK is an enzyme that regulates B-cell development and activation and is also involved in the activation of myeloid cells (such as macrophages and microglia) in the innate immune system. Fenebrutinib is an orally administered, reversible, non-covalent BTK inhibitor that blocks the function of BTK. Preclinical data show that fenebrutinib has strong activity and high selectivity, with a selectivity for BTK that is 130 times greater than that for other kinases.

The Structural Formula of Fenebrutinib

Roche is conducting three Phase III registrational clinical trials of fenebrutinib for the treatment of multiple sclerosis (MS), including FENhance, FENhance2, and FENtrepid. These three studies are expected to be completed in 2025 and 2026.

Registration Clinical Trials of Fenebrutinib (Source: PharmaCube NextPharma Database)

Currently, there are four BTK inhibitors globally conducting Phase III clinical trials for multiple sclerosis, and fenebrutinib is the only third-generation BTK inhibitor among them. The other three are evobrutinib (Merck), remibrutinib (Novartis), and tolebrutinib (Sanofi).

MS Phase III BTK Inhibitor Under Research (Source: Nextpharma Database by PharmaCube)

Multiple Sclerosis (MS) is a chronic disease that affects more than 2 million people worldwide. MS occurs when the immune system abnormally attacks the insulating layer and support around nerve cells (myelin) in the central nervous system (brain, spinal cord, and optic nerves), leading to inflammation and subsequent damage. This damage can cause a range of symptoms, including muscle weakness, fatigue, and vision difficulties, and may eventually lead to disability. The majority of MS patients experience their first episode between the ages of 8 and 20, making it a leading cause of non-traumatic disability in young adults.

RMS includes Relapsing-Remitting MS (RRMS) and Secondary Progressive MS (SPMS). RRMS is the most common form of MS, characterized by new or worsening signs or symptoms, followed by periods of recovery. Approximately 85% of MS patients are initially diagnosed with RRMS. Most individuals diagnosed with RRMS will eventually transition to Secondary Progressive MS (SPMS), with their disability progressively worsening over time.

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