tolebrutinib

Tolebrutinib is an orally bioavailable, brain-penetrant, selective small molecule inhibitor of Bruton's tyrosine kinase (BTK). It is designed to cross the blood-brain barrier and inhibit BTK activity both in the periphery and central nervous system. By inhibiting BTK, tolebrutinib modulates B-cell receptor signaling and suppresses immune cell activation—including B cells, macrophages, and microglia—thereby reducing neuroinflammation implicated in multiple sclerosis (MS) progression. Tolebrutinib is under development primarily for non-relapsing secondary progressive multiple sclerosis (nrSPMS), with additional studies ongoing for primary progressive MS. Developed by Sanofi, it has received FDA Breakthrough Therapy designation based on phase 3 data showing significant delay in disability progression in nrSPMS[1][3][4][5].

Other names

tolebrutinib