Catalog No.S1256 Synonyms: CGP 33101
Molecular Weight(MW): 238.19
Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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|Description||Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.|
Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Rufinamide’s mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects.  Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM. 
|In vivo||Rufinamide given orally at 20 mg/kg every 12 h in healthy dogs should result in a plasma concentration and half-life sufficient to achieve the therapeutic level extrapolated from humans without short-term adverse effects in adult dogs.  Rufinamide alleviates injury-induced mechanical allodynia for 4 hours. Rufinamide reduces peak current and stabilizes the inactivated state of voltage-gated sodium channel Nav1.7, with similar effects in dorsal root ganglion neurons in the Spared Nerve Injury neuropathic pain model in mice.  Rufinamide suppresses pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and is active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg). Rufinamide suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). Rufinamide is partially effective in the mouse strychnine test. |
-  Cheng-Hakimian A, et al. Int J Clin Pract,?006, 60(11), 1497-1501.
-  Williams ET, et al. Drug Metab Lett,?011, 5(4), 280-289.
-  Wright HM, et al. J Vet Pharmacol Ther,?012, 35(6), 529-533.
|In vitro||DMSO||18 mg/mL warmed (75.56 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02095899||Withdrawn||Peripheral Nerve Injuries|Pain||University of Zurich||March 2014||Phase 2|
|NCT02332174||Completed||Seizures||Wuhan Union Hospital, China||March 2014||Phase 1|
|NCT02175173||Active, not recruiting||Lennox-Gastaut Syndrome||Eisai Co., Ltd.|Eisai Inc.||June 2013||--|
|NCT01405053||Completed||Lennox-Gastaut Syndrome||Eisai Inc.||June 2011||Phase 3|
|NCT01146951||Completed||Lennox-Gastaut Syndrome||Eisai Limited|Eisai Inc.||June 2010||Phase 3|
|NCT00448539||Completed||Refractory Partial Onset Seizures||Eisai Inc.||March 2007||Phase 3|
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