On the evening of February 26, Innocare Biologics announced that the Phase II clinical data of Orelabrutinib, a new BTK inhibitor independently developed by the company, for the treatment of relapsing-remitting multiple sclerosis (RRMS) was released at the 10th Annual Forum of the American Committee for Treatment and Research in Multiple Sclerosis (ACTRIMS) in 2025, and a live poster presentation will be held on February 27, Eastern Time.

The announcement shows that Orelabrutinib has shown extremely high effectiveness in the treatment of patients with relapsing-remitting multiple sclerosis (RRMS). A dose of 80 mg of Orelabrutinib once a day showed the best efficacy and safety, so it will be used as the dose for the Phase III clinical trial of Orelabrutinib for the treatment of progressive multiple sclerosis (PMS).

In a double-blind Phase II clinical trial, 158 eligible relapsing-remitting multiple sclerosis subjects were randomly assigned to four treatment groups in a 1:1:1:1 ratio: placebo, 50 mg of obeticholic acid once a day, 80 mg of obeticholic acid once a day, and 50 mg of obeticholic acid twice a day. Placebo subjects were switched from placebo to 50 mg of obeticholic acid once a day at week 13. The primary endpoint was the cumulative number of new lesions in the brain on gadolinium-enhanced (Gd+) T1 magnetic resonance imaging (MRI) at week 12 (based on Gd+ T1 new lesions at weeks 4, 8, and 12) compared with the placebo group.

At week 12, the cumulative number of new Gd+T1 brain lesions and new/enlarged T2 brain lesions were significantly reduced in all three dose groups of orelabrutinib compared with the placebo group (p<0.05), and the cumulative number of these lesions was also significantly reduced in the 80 mg once daily dose group and the 50 mg twice daily dose group compared with the placebo group at week 24 (p<0.05). The cumulative number of new Gd+T1 brain lesions in the 80 mg once daily dose group was reduced by 90.4% at week 12 and 92.3% at week 24 compared with the placebo group. Each orelabrutinib dose group achieved control of new lesions at the earliest evaluation time point of week 4, and the efficacy lasted until week 24.

BTK plays an important role in regulating the function of B cells and myeloid cells, which is also related to the pathogenesis of MS. Obtunib is a highly selective, brain-penetrating BTK inhibitor that inhibits not only the activation of peripheral B cells and macrophages, but also the activation of B cells, microglia and macrophages in the central nervous system.