Drug intelligence / Profile preview

ibudilast

Development stage
Phase 3
Lead developer
MediciNova
Modality
Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Ibudilast is a small molecule drug with bronchodilator, vasodilator, anti-inflammatory, and neuroprotective effects. It is primarily used in Japan for the treatment of asthma and dizziness secondary to chronic cerebral circulation impairment following cerebral infarction. Ibudilast is also approved as an ophthalmic solution for allergic conjunctivitis and hay fever in Japan. Its mechanism of action includes nonselective inhibition of phosphodiesterases (mainly PDE4 but also PDE3, PDE10A, and PDE11A), antagonism at toll-like receptor 4 (TLR4), leukotriene D4 antagonist activity, platelet aggregation inhibition, suppression of glial cell activation in the CNS, and enhancement of autophagy via mTORC1-TFEB signaling. Ibudilast has shown potential benefits in multiple sclerosis (MS), particularly progressive forms by slowing brain volume loss; it may also be useful for neuropathic pain management and reducing opioid tolerance or withdrawal symptoms. The drug is under investigation for several neurological conditions including MS outside Japan[1][2][3][5][6][7].

Brand names
Ketas
Other names
ibudilast3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine
02

Targets

PDE10A (cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A)PDE3PDE5 (Phosphodiesterase 5A)CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)PDE2 (Phosphodiesterase 2)TLR4 (Toll-like receptor 4)PDE11A (Phosphodiesterase 11A)PDE4 (Phosphodiesterase 4A1)

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