Ibudilast is an anti-inflammatory and neuroprotective oral agent which shows an excellent safety profile at 60 mg/day and provides significantly prolonged time-to-first relapse and attenuated brain volume shrinkage in patients with relapsing-remitting (RR) and/or secondary progressive (SP) multiple sclerosis (MS). Ibudilast is currently in development in the U.S. (codes: AV-411 or MN-166), but is approved for use as an antiinflammatory in Japan. |
Categories | Vasodilator Agents Platelet Aggregation Inhibitors Phosphodiesterase Inhibitors Bronchodilator Agents
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Synonyms | 2-Isopropyl-3-isobutyrylpyrazolo(1,5-a)pyridine 3-isobutyryl-2-isopropylpyrazolo(1,5-a)pyridine 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine AV-411 Eyevinal I0157_SIGMA Ibudilast (jan/inn) Ibudilast [inn:jan] Ibudilastum Ibudilastum [latin] Ke tas Ketas Ketas (TN) Lopac-I-0157 MN-166 Pyrazolo(1,5-a)pyridine, 3-isobutyryl-2-isopropyl- Tocris-1694 UNII-M0TTH61XC5
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indication
For the treatment of multiple sclerosis, asthma, and cerebrovascular disease.
mechanism of action
Ibudilast has mechanisms that include anti-inflammatory effects, such as phosphodiesterase inhibition, and neuroprotective effects, such as inhibition of [nitric oxide] synthesis and reduction in reactive oxygen species.
toxicity
Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia
half life
19 hours