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Gabapentin enacarbil

Catalog No. T15366 CAS 478296-72-9

Synonyms: XP-13512

Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. Gabapentin enacarbil provides sustained dose-proportional exposure to gabapentin and predictable bioavailability.

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Gabapentin enacarbil, CAS 478296-72-9

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Storage & Solubility Information

Description	Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. Gabapentin enacarbil provides sustained dose-proportional exposure to gabapentin and predictable bioavailability.
In vitro	Gabapentin enacarbil demonstrated active apical to basolateral transport across Caco-2 cell monolayers and pH-dependent passive permeability across artificial membranes. XP13512 inhibited uptake of (14)C-lactate by human embryonic kidney cells expressing monocarboxylate transporter type-1, and direct uptake of prodrug by these cells was confirmed using liquid chromatography-tandem mass spectrometry. XP13512 inhibited uptake of (3)H-biotin into Chinese hamster ovary cells overexpressing human sodium-dependent multivitamin transporter (SMVT) [1].
In vivo	In 4 studies of healthy volunteers (136 subjects total), the pharmacokinetics of Gabapentin enacarbil immediate- and extended-release formulations were compared with those of oral gabapentin. Gabapentin enacarbil immediate-release (up to 2800 mg single dose and 2100 mg twice daily) was well absorbed (>68%, based on urinary recovery of gabapentin), converted rapidly to gabapentin, and provided dose-proportional exposure, whereas absorption of oral gabapentin declined with increasing doses to <27% at 1200 mg. Compared with 600 mg gabapentin, an equimolar Gabapentin enacarbil extended-release dose provided extended gabapentin exposure (time to maximum concentration, 8.4 vs 2.7 hours) and superior bioavailability (74.5% vs 36.6%) [2].

Synonyms	XP-13512
Molecular Weight	329.39
Formula	C16H27NO6
CAS No.	478296-72-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 95 mg/mL (288.41 mM), Sonication is recommended.

DMSO: 95 mg/mL (288.41 mM)

H2O: 0.6 mg/mL (1.82 mM), Sonication is recommended.

References and Literature

1. Cundy KC, et al. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pha 2. Cundy KC, et al. Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin. J Clin Pharmacol. 2008 Dec;48(12):1378-88.

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Keywords

Gabapentin enacarbil 478296-72-9 Membrane transporter/Ion channel Metabolism Others Calcium Channel XP-13512 inhibit XP 13512 Inhibitor Ca channels XP13512 Ca2+ channels inhibitor

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