| 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 在Caco-2细胞单层中展现了从顶向基底的主动转运能力，以及在人造膜上的pH依赖性被动渗透性。XP13512抑制了表达单羧酸运输蛋白1型的人类胚胎肾细胞对(14)C-乳酸的摄取，并且通过液相色谱-串联质谱分析确认了这些细胞对前药物的直接摄取。XP13512还抑制了过表达人类依赖钠的多维生素转运器（SMVT）的中国仓鼠卵巢细胞对(3)H-生物素的摄取[1]。 |
| In vivo | 在对健康志愿者（共136名受试者）进行的4项研究中，比较了Gabapentin enacarbil即释放和缓释配方与口服Gabapentin的药代动力学。Gabapentin enacarbil即释放（最高单剂量2800mg及每日两次2100mg）的吸收良好（基于Gabapentin尿液回收率>68%），迅速转化为Gabapentin，并提供了剂量比例暴露。相比之下，口服Gabapentin的吸收随剂量增加而减少，至1200mg时<27%。与600mg Gabapentin相比，等摩尔的Gabapentin enacarbil缓释剂量提供了更长时间的Gabapentin暴露（达到最高浓度时间，8.4比2.7小时）和更高的生物利用度（74.5%比36.6%）[2]。 |
| Synonyms | XP-13512, 加巴喷丁酯 |
| molecular weight | 329.39 |
| Molecular formula | C16H27NO6 |
| CAS | 478296-72-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | 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 | 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. |