MRI Outcomes from the Long-term Extension Study of Tolebrutinib in Patients with Relapsing Multiple Sclerosis: 2-Year Results
Daniel Reich1, Anthony Traboulsee2, Sana Syed3, Zhixing Xu3, Timothy Turner3, Douglas Arnold4
1National Institute of Neurological Disorders and Stroke, 2University of British Columbia, 3Sanofi, 4NeuroRx Research and Montréal Neurological Institute, McGill University
Objective:

To report MRI outcomes at Week (W) 96 (2 years) in LTS16004 (NCT03996291), an ongoing long-term safety (LTS) extension study of the Phase 2b trial (NCT03889639) of tolebrutinib, a brain-penetrant Bruton’s tyrosine kinase inhibitor in participants with relapsing multiple sclerosis.

Background:

In the double-blind phase (DBP) of the Phase 2b trial, tolebrutinib was well-tolerated over 12 weeks with dose-dependent reductions in new gadolinium-enhancing T1 and new/enlarging T2-lesions.

Design/Methods:

In LTS Part A, participants continued receiving their DBP tolebrutinib dose (5, 15, 30, or 60mg/day) until Phase 3 dose selection. In open-label Part B, all participants received 60mg/day. MRI outcomes included numbers of new gadolinium-enhancing T1 and new/enlarging T2-lesions, T2-lesion volume change, slowly evolving lesions (SEL), and paramagnetic rim lesions (PRL).

Results:

124/125 participants completed Part A and transitioned to Part B; 114 (90.5%) remained on study as of 18 February 2022 (W96 cut-off). Mean age±SD at DBP baseline was 37.7±9.6 years (range 19–56); 69% were women. New gadolinium-enhancing lesion counts remained low in 60/60-mg arm through W96 and were reduced in other arms W48 through W96 (W96 mean±SD: 0.85±2.5, 0.41±0.91, 0.90±2.16, 0.31±0.66 in 5/60-, 15/60-, 30/60-, 60/60-mg arms, respectively). New/enlarging T2-lesion counts remained low for 60/60-mg. T2-lesion volume change remained low for 60/60-mg (W96 vs baseline [mean±SD]: +0.38±2.11 cm3). Median (IQR) W96 SEL volume was 247.5 (84–420), 258 (66–906), 570 (133.5–1011), and 244.5 (87–939) mm3 for 5/60-, 15/60-, 30/60-, and 60/60-mg, respectively. PRL count remained unchanged in 18 participants; 2 had 1 PRL at baseline but none at W96, and 3 had 1–3 additional PRL at W96 vs baseline (none in the 60/60-mg arm).

Conclusions:
New gadolinium-enhancing lesion counts remained low for tolebrutinib 60/60-mg and were reduced in lower dose arms W48 through W96, when all participants had switched to 60mg. 
10.1212/WNL.0000000000202144