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Drug Names(s): GSK1838262, gabapentin enacarbil, XP13512, ASP8825, Solzira, Regnite (Japan)
Description: XP13512 is a Transported Prodrug of gabapentin (Neurontin; Pfizer). XP13512 is designed to rapidly convert to gabapentin once absorbed from the GI tract, resulting in limited systemic exposure to the intact Transported Prodrug. In preclinical studies, oral dosing of XP13512 produced blood levels of gabapentin that are proportional to the oral dose. Substantially higher blood levels of gabapentin were achieved after oral dosing of XP13512 compared to equivalent oral doses of gabapentin itself.
While the exact mechanism of action of gabapentin is unknown, its therapeutic action on neuropathic pain is thought to involve voltage-gated N-type calcium ion channels. It is thought to bind to the alpha2delta subunit of the voltage-dependent calcium channel in the central nervous system.
XenoPort and Astellas
In November 2005, XenoPort and Astellas Pharma (Astellas) entered into a license agreement for exclusive rights in Japan and several other Asian countries to develop and commercialize XP13512. Under the terms of the agreement, Astellas has obtained exclusive rights to develop and commercialize XP13512 in Japan, Korea, the Philippines, Indonesia, Thailand and Taiwan. XenoPort will receive an initial license payment of $25 million. In addition, XenoPort is eligible to receive clinical and regulatory milestone payments totaling up to $60 million. XenoPort will receive royalties on any sales of XP13512 in the Astellas territory at a royalty rate in the mid-teens on a percentage basis.
XenoPort and GSK
In February 2007, GlaxoSmithKline (GSK) and XenoPort announced an exclusive agreement to co-develop and commercialize XP13512, in the US and other countries worldwide, excluding certain Asian countries. Under the terms of the...See full deal structure in Biomedtracker
Partners: Astellas Pharma, Inc.
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