molecules of the month


oral BTK inhibitor

Ph. III for multiple sclerosis

from ATP site-directed compound libraries + optimization

Clinical data release, May 16, 2023

Genentech, South San Francisco, CA

fenebrutinib, BTK, oral BTK inhibitor, Ph. III for multiple sclerosis, from ATP site-directed compound libraries + optimization, Clinical data release, May 16, 2023 GENENTECH, SOUTH SAN FRANCISCO, CA
16 mins read

A reversible BTK inhibitor reduces brain lesions in multiple sclerosis (MS). Genentech recently announced that fenebrutinib (GDC-0853), a noncovalent Bruton’s tyrosine kinase (BTK) inhibitor, showed promise in reducing brain lesions in Ph. II clinical trials for relapsing multiple sclerosis (RMS) and would be entering Ph. III. Following the success of BTK inhibitors in oncology, BTK has been a hotly pursued target to treat chronic autoimmune diseases, with multiple companies evaluating BTK inhibitors in a range of clinically and commercially important indications. Other candidates for MS, evobrutinib, tolebrutinib, remibrutinib, and orelabrutinib, are all covalent Btk inhibitors, leaving fenebrutinib as the only noncovalent inhibitor in late clinical evaluation for MS. While evobrutinib, tolebrutinib, orelabrutinib, have all been placed on clinical hold in…

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