Disease relevance of LOSIGAMONE

• 1 Losigamone is a novel anticonvulsant undergoing phase III clinical trials in patients with partial and secondary generalized seizures [1].

Psychiatry related information on LOSIGAMONE

• Isobolographic analysis of interactions between losigamone and conventional antiepileptic drugs in the mouse maximal electroshock model [2].

High impact information on LOSIGAMONE

• Effects of the anticonvulsant losigamone and its isomers on the GABAA receptor system [3].
• Both isomers of losigamone likewise stimulated 36Cl influx into spinal cord neurons, and these effects were similarly antagonized by BIC and PIC [3].
• Losigamone induced a decrease in amplitude of I(NaP) at depolarized membrane potentials which was reversible in cultured neurons [4].
• Stereoselective metabolism of a new anticonvulsant drug candidate, losigamone, by human liver microsomes [5].
• Losigamone reversibly reduced the number of action potentials elicited by 1 s long depolarising current injections [6].

Chemical compound and disease context of LOSIGAMONE

• The aim of this study was the isobolographic evaluation of interactions between losigamone (LSG), valproate (VPA), carbamazepine (CBZ), phenytoin (PHT), and phenobarbital (PB) in the maximal electroshock (MES) test in mice [2].

Biological context of LOSIGAMONE

• Effects of losigamone on synaptic potentials and spike frequency habituation in rat entorhinal cortex and hippocampal CA1 neurones [6].
• Pharmacokinetics of losigamone, a new antiepileptic drug, in healthy male volunteers [7].
• The single- and multiple-dose kinetics of 200 mg losigamone and its enantiomeres did not differ from each other in a significant way [8].

Gene context of LOSIGAMONE

• Cytochrome CYP2A6 appears to be the main isoenzyme responsible for the metabolism of losigamone [9].
• Comparison of the effects of losigamone and its isomers on maximal electroshock induced convulsions in mice and on three different patterns of low magnesium induced epileptiform activity in slices of the rat temporal cortex [10].
• Losigamone add-on therapy in partial epilepsy: a placebo-controlled study [11].

Analytical, diagnostic and therapeutic context of LOSIGAMONE

• Efficacy and safety of Losigamone in partial seizures: a randomized double-blind study [12].
• In a crossover study, 200 mg [14C]-labelled Losigamone, as well as 100 mg of each of the unlabelled enantiomers, was administered to 5 healthy volunteers as an oral suspension [13].
• Pharmacokinetics of [14C]-labelled Losigamone and enantiomers after oral administration to healthy subjects [13].

References