Eslicarbazepine Acetate - CAS 236395-14-5
Catalog number: 236395-14-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine.
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(10S)-10-(Acetyloxy)-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide; (S)-(-)-10-Acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide; BIA 2-093; Sep 0002093;
1. Voltage-gated sodium channel blockers, 2001-2006: An overview
Hedvig Bolcskei, Istvan Tarnawa, Pa l Kocsis. Med Chem Res (2008) 17:356–368
A traditional therapeutic area of VGSC blockers is epilepsy. Phenytoin derivatives (e.g., phosphenytoin) should be mentioned first. Carbamazepine and its derivatives are also widely used antiepileptics (e.g., oxcarbazepine, licarbazepine, eslicarbazepine, and eslicarbazepine acetate). Eslicarbazepine is the optically active isomer of licarbazepine (Fig. 1). Amitryptiline (Fig. 1), just like other tricyclic antidepressants, is effective against various pain syndromes, and blocks sodium channels. Various diphenylamineanalogues were prepared by Hudgens and co-workers. A structure–activityrelationship (SAR) study among them revealed that the tricyclic moiety is not essential for hNaV1.2 activity (Hudgens et al., 2006).
2. Recent and Emerging Anti-seizure Drugs: 2013
William O. Tatum, DO. Current Treatment Options in Neurology (2013) 15:505-518
Eslicarbazepine acetate (Esli) is a prodrug that was approved in the US in 2012 as Zebinix® (Exalief® in Europe). It is activated to eslicarbazepine (S-licarbazepine), an active metabolite of oxcarbazepine. It is indicated in the treatment of adults with focal seizures with/without generalization. Esli is a pro-drug that is rapidly metabolized by hydrolysis almost exclusively to S-licarbazepine. It blocks voltage-gated sodium channels. However in comparison, Esli has a lower affinity for the sodium channel in the resting state and preferentially blocks rapidly firing neurons during the inactive state. It has a bioavailability that is approximately 94 % of the parent dose and a half-life of 20–24 hours. It has linear pharmacokinetics and is metabolized without the formation of an epoxide intermediary and Esli does not undergo autoinduction. It may be reduced by enzymeinducing ASDs (EIASDs), but does not affect other ASDs and is primarily excreted by the kidney.
3. Newer Antiepileptic Drugs: Evidence Based Use
Gouri Rao Passi. Indian J Pediatr (October 2014) 81(10):1042–1051
There are many newer molecules in the pipeline with novel mechanisms of action which will need more pediatric data such as lacosamide, ezogabine, eslicarbamazepine, perampenel and brivaracetam. Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels which reduces the ability of (epileptic) neurons to sustain prolonged firing bursts and may mediate neuronal plasticity which holds the hint of inhibiting epileptogenesis. It has been known to cause suicidal ideation and conduction blocks. However, it has not yet been cleared for use below 17 y. Ezogabine has a different mechanism of action (K channel opener) and inhibits smooth muscle contractility, which has raised concerns about its effect on bladder function. Eslicarbazepine acetate displays a greater affinity for the inactive state (already fired) of the sodium channel rather than the resting state (waiting to fire), meaning that it could be more selective for rapidly firing neurons. Perampenel is approved only above 12 y of age for partial onset epilepsy. It acts as a non competitive inhibitor of the AMPA glutamate receptor. It has a boxed warning of severe neuropsychiatric side effects. Brivaracetam has 13 times higher affinity for the synaptic vesicle protein 2A than levetiracetam and also inhibits sodium channels. It has orphan drug status for symptomatic myoclonus.
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CAS 236395-14-5 Eslicarbazepine Acetate

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