Naismith, Robert T.; Wundes, Annette; Ziemssen, Tjalf; Jasinska, Elzbieta; Freedman, Mark S.; Lembo, Anthony J.; Selmaj, Krzysztof; Bidollari, Ilda; Chen, Hailu; Hanna, Jerome; Leigh-Pemberton, Richard; Lopez-Bresnahan, Maria; Lyons, Jennifer; Miller, Catherine; Rezendes, David; Wolinsky, Jerry S.; The EVOLVE-MS-2 Study Group published the artcile< Diroximel Fumarate Demonstrates an Improved Gastrointestinal Tolerability Profile Compared with Dimethyl Fumarate in Patients with Relapsing-Remitting Multiple Sclerosis: Results from the Randomized, Double-Blind, Phase III EVOLVE-MS-2 Study>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is diroximel fumarate gastrointestinal tolerability prole human.
Abstract: Background: Diroximel fumarate (DRF) is a novel oral fumarate approved in the USA for relapsing forms of multiple sclerosis. DRF is converted to monomethyl fumarate, the pharmacol. active metabolite of di-Me fumarate (DMF). DRF 462 mg and DMF 240 mg produce bioequivalent exposure of monomethyl fumarate and are therefore expected to have similar efficacy/safety profiles; the distinct chem. structure of DRF may contribute to its tolerability profile. Objectives: The objective of this study was to compare the gastrointestinal tolerability of DRF and DMF over 5 wk in patients with relapsing-remitting multiple sclerosis. Methods: EVOLVE-MS-2 was a phase III, randomized, double-blind, head-to-head, 5-wk study evaluating the gastrointestinal tolerability of DRF 462 mg vs DMF 240 mg, administered twice daily in patients with relapsing-remitting multiple sclerosis, using two self-administered gastrointestinal symptom scales: Individual Gastrointestinal Symptom and Impact Scale (IGISIS) and Global Gastrointestinal Symptom and Impact Scale (GGISIS). The primary endpoint was the number of days with an IGISIS intensity score ≥ 2 relative to exposure. Other endpoints included the degree of gastrointestinal symptom severity measured by IGISIS/GGISIS and assessment of safety/tolerability. Results: DRF-treated patients experienced a statistically significant reduction (46%) in the number of days with an IGISIS symptom intensity score ≥ 2 compared with DMF-treated patients (rate ratio [95% confidence interval]: 0.54 [0.39-0.75]; p = 0.0003). Lower rates of gastrointestinal adverse events (including diarrhea, nausea, vomiting, and abdominal pain) were observed with DRF than DMF (34.8% vs 49.0%). Fewer patients discontinued DRF than DMF because of adverse events (1.6% vs 5.6%) and gastrointestinal adverse events (0.8% vs 4.8%). Conclusions: DRF demonstrated an improved gastrointestinal tolerability profile compared with DMF, with less severe gastrointestinal events and fewer days of self-assessed gastrointestinal symptoms, fewer gastrointestinal adverse events, and lower discontinuation rates because of gastrointestinal adverse events. Clin. Trials Registration: ClinicalTrials.gov (NCT03093324).
CNS Drugs published new progress about Abdominal pain. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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