Drug intelligence / Profile preview

FP187-GC

Development stage
Discontinued
Lead developer
Forward Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

FP187-GC is a delayed- and slow-release erosion matrix oral tablet formulation of dimethyl fumarate (DMF) developed by Forward Pharma. Dimethyl fumarate is a small molecule immunomodulator that is rapidly metabolized in vivo to its active metabolite, monomethyl fumarate (MMF). MMF acts as an agonist of the hydroxycarboxylic acid receptor 2 (HCAR2) and covalently binds to Kelch-like ECH-associated protein 1 (KEAP1), thereby activating the cytoprotective Nrf2 antioxidant pathway. Additionally, DMF/MMF can covalently modify glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and interleukin-1 receptor-associated kinase 4 (IRAK4) to suppress glycolysis and innate immune signaling. FP187-GC was designed to optimize the release profile of DMF, aiming to maintain therapeutic efficacy in relapsing-remitting multiple sclerosis (RRMS) and psoriasis while reducing common side effects such as flushing and gastrointestinal irritation associated with standard formulations like Tecfidera. Following a major patent settlement and license agreement with Biogen in 2017, and subsequent unfavorable patent rulings, Forward Pharma permanently discontinued the clinical development of FP187-GC.

Other names
dimethyl fumarate slow-release formulationdelayed- and slow-release dimethyl fumarate formulation
02

Targets

KEAP1 (Kelch-like ECH-associated protein 1)IRAK4 (Interleukin-1 receptor associated kinase 4)HCAR2 (Hydroxycarboxylic acid receptor 2)GAPDH (Glyceraldehyde-3-phosphate dehydrogenase)

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