Roche’s BTK inhibitor fenebrutinib significantly reduced brain lesions in people with relapsing forms of multiple sclerosis

• Fenebrutinib is an investigational, potent and highly selective oral Bruton’s tyrosine kinase (BTK) inhibitor, the only reversible BTK inhibitor currently in Phase III multiple sclerosis (MS) trials
• Phase II study met its primary and secondary endpoints by reducing the total number of new gadolinium-enhancing T1 brain lesions and significantly reducing the total number of new or enlarging T2 brain lesions compared to placebo
• The safety profile of fenebrutinib was consistent with previous and ongoing clinical trials across more than 2,400 people to date
  
  

Basel, 17 May 2023 - Roche (SIX: RO, ROG; OTCQX: RHHBY) announced today positive results from the Phase II FENopta study evaluating investigational oral fenebrutinib in adults with relapsing forms of multiple sclerosis (RMS). The study met its primary and secondary endpoints, showing oral fenebrutinib significantly reduced magnetic resonance imaging (MRI) markers of MS disease activity in the brain compared to placebo. Additionally, pre-clinical data have shown fenebrutinib to be potent and highly selective, and it is the only reversible inhibitor currently in Phase III trials for MS.

“I am encouraged by this clinical data for fenebrutinib, which is important news for people living with MS,” said Levi Garraway, M.D., Ph.D., Roche’s Chief Medical Officer and Head of Global Product Development. “Fenebrutinib’s mechanism of action which can inhibit both B cells and microglia, has the potential to both reduce MS disease activity, such as relapses, and also impact disease progression.’’

Fenebrutinib significantly reduced the total number of new gadolinium-enhancing T1 brain lesions compared to placebo, the primary endpoint of the trial (p=0.0022). Additionally, fenebrutinib significantly reduced the total number of new or enlarging T2 brain lesions compared to placebo, a secondary endpoint. Furthermore, a higher proportion of patients treated with fenebrutinib were free from any new gadolinium-enhancing T1 brain lesions and new or enlarging T2-weighted brain lesions compared to placebo. T1 lesions, as measured by MRI, are a marker of active inflammation and T2 lesions represent the amount of disease burden or lesion load.