Gabapentin enacarbilCAS# 478296-72-9 |
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| Cas No. | 478296-72-9 | SDF | Download SDF |
| PubChem ID | 9883933 | Appearance | Powder |
| Formula | C16H27NO6 | M.Wt | 329.39 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (303.59 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[1-[[1-(2-methylpropanoyloxy)ethoxycarbonylamino]methyl]cyclohexyl]acetic acid | ||
| SMILES | CC(C)C(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O | ||
| Standard InChIKey | TZDUHAJSIBHXDL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H27NO6/c1-11(2)14(20)22-12(3)23-15(21)17-10-16(9-13(18)19)7-5-4-6-8-16/h11-12H,4-10H2,1-3H3,(H,17,21)(H,18,19) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Gabapentin enacarbil Dilution Calculator
Gabapentin enacarbil Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0359 mL | 15.1796 mL | 30.3591 mL | 60.7183 mL | 75.8979 mL |
| 5 mM | 0.6072 mL | 3.0359 mL | 6.0718 mL | 12.1437 mL | 15.1796 mL |
| 10 mM | 0.3036 mL | 1.518 mL | 3.0359 mL | 6.0718 mL | 7.5898 mL |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.2144 mL | 1.518 mL |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.6072 mL | 0.759 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
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Efficacy of gabapentin enacarbil in adult patients with severe primary restless legs syndrome.[Pubmed:27198947]
Sleep Med. 2016 Mar;19:50-6.
AIM: Assess efficacy and tolerability of Gabapentin enacarbil (GEn) in adults with severe primary restless legs syndrome (RLS). METHODS: We pooled data from three 12-week, double-blind, placebo-controlled, randomized trials (NCT00298623, NCT00365352, NCT01332305) across GEn 600-mg, GEn 1200-mg, and placebo treatment groups for severe primary RLS (baseline International Restless Legs Scale (IRLS) total score >/=24). Co-primary end points at week 12 were mean change from baseline in IRLS total score and proportion of responders ("much"/very much" improved) on the investigator-rated Clinical Global Impression - Improvement (CGI-I) Scale. Outcomes for individual IRLS items (eg, sleep, mood, quality of life, pain, safety) were assessed. RESULTS: A total of 309 patients had severe primary RLS (placebo, n = 110; GEn 600 mg, n = 80; GEn 1200 mg, n = 119). GEn 600 mg and 1200 mg significantly improved least-squares mean IRLS total scores versus placebo at week 12 (placebo, -12.3; GEn 600 mg, -16.3; GEn 1200 mg, -18.0; treatment difference vs. placebo, both p <0.01). Significantly more patients with severe primary RLS treated with GEn 600 mg (64%) and 1200 mg (74%) were CGI-I responders at week 12 versus placebo (42%; p <0.01 for both GEn doses). Both GEn doses led to significant improvements in the other outcomes explored versus placebo at week 12. The most frequent treatment-emergent adverse events (TEAEs) were somnolence (GEn, 21-24%; placebo, 3%) and dizziness (GEn, 14-19%; placebo, 3%). CONCLUSIONS: GEn (600 mg or 1200 mg) once daily significantly improved RLS symptoms and consequences of these symptoms in severe primary RLS. The most frequent TEAEs were somnolence and dizziness.
The Effect of Gabapentin Enacarbil on Pain Associated with Moderate-to-Severe Primary Restless Legs Syndrome in Adults: Pooled Analyses from Three Randomized Controlled Trials.[Pubmed:27095237]
CNS Drugs. 2016 May;30(5):443-54.
BACKGROUND: Adults with moderate-to-severe primary restless legs syndrome (RLS) often experience painful dysesthesias, which may lead to impaired quality of life. OBJECTIVES: The aim of this study was to assess the effects of Gabapentin enacarbil (GEn) on pain associated with moderate-to-severe primary RLS in adults. METHODS: Data were pooled from three double-blind, randomized, placebo-controlled, 12-week trials (NCT00298623, NCT00365352, NCT01332305) for adults receiving GEn or placebo once daily. Change in average daily RLS pain score and a combined International Restless Legs Scale (IRLS)-pain response were examined. RESULTS: The modified intention-to-treat population included 671 adults (placebo, n = 244; GEn 600 mg, n = 161; GEn 1200 mg, n = 266). Both GEn doses significantly improved average daily RLS pain score at week 12 (p < 0.001 for GEn 600 mg vs. placebo and GEn 1200 mg vs. placebo). The combined IRLS-pain response subanalysis included 366 patients with a baseline IRLS total score >/=15 and pain score >/=4 (placebo, n = 133; GEn 600 mg, n = 86; GEn 1200 mg, n = 147). Most patients were both IRLS and pain responders (placebo, 40 %; GEn 600 mg, 70 %; GEn 1200 mg, 67 %). Spearman rank correlations between IRLS total and pain score (change from baseline to week 12) were moderate or strong. The most frequent treatment-emergent adverse events were somnolence (placebo, 5 %; GEn 600 mg, 20 %; GEn 1200 mg, 23 %) and dizziness (placebo, 4 %; GEn 600 mg, 13 %; GEn 1200 mg, 22 %). CONCLUSIONS: This post hoc pooled analysis suggests that GEn (600 and 1200 mg) once daily significantly improved pain associated with moderate-to-severe primary RLS in adults; however, the analysis was not powered to detect statistical differences between the two GEn doses. Numerically, more GEn-treated patients had a combined IRLS-pain response than placebo-treated patients.
Effect of Gabapentin Enacarbil on Individual Items of the International Restless Legs Study Group Rating Scale and Post-sleep Questionnaire in Adults with Moderate-to-Severe Primary Restless Legs Syndrome: Pooled Analysis of 3 Randomized Trials.[Pubmed:27288210]
Clin Ther. 2016 Jul;38(7):1726-1737.e1.
PURPOSE: Few studies have investigated restless legs syndrome (RLS) treatment effects on individual International RLS Study Group Rating Scale (IRLS) items. We assessed the effects of Gabapentin enacarbil (GEn) on individual IRLS items and their correlation with sleep disturbances in adults with moderate-to-severe primary RLS. METHODS: Data were pooled from the randomized, double-blind, placebo-controlled, 12-week studies of XP052, XP053, and XP081 for adults who received GEn (600 or 1200 mg) or placebo once daily. Adults had primary RLS, IRLS total score >/=15, and RLS symptoms >15 days during the month before screening and for >/=4 of the 7 consecutive evenings at baseline. End points included mean change from baseline to week 12 in individual IRLS and post-sleep questionnaire (PSQ) items. For IRLS items, least squares mean treatment differences were calculated from a mixed model for repeated measures. For PSQ items, Cochran-Mantel-Haenszel row mean scores tests with integer scoring were used. Correlations between IRLS and PSQ items were assessed by Spearman's rank coefficients. Safety profile outcomes included treatment-emergent adverse events (TEAEs) and serious TEAEs. FINDINGS: The modified intent-to-treat population included 671 patients (GEn 600 mg = 161; GEn 1200 mg = 266; placebo = 244). GEn significantly improved mean [SE] differences versus placebo for all IRLS items at week 12, including severity of sleep disturbance (GEn 600 mg, -0.4 [0.10]; GEn 1200 mg, -0.4 [0.09]), daytime tiredness (-0.4 [0.09]; -0.4 [0.08]), RLS severity (-0.4 [0.10]; -0.3 [0.08]), impact on daily affairs (-0.3 [0.07]; -0.3 [0.07]), and mood disturbance (-0.2 [0.07]; -0.3 [0.06]); all P<0.001). For PSQ items, significant (P<0.01) improvements occurred with both GEn doses versus placebo at week 12. The correlations between IRLS and PSQ items for change from baseline to week 12 were moderate to strong, and all correlations were significant (P<0.001). The most frequent TEAEs were somnolence (GEn 600 mg, 20%; GEn 1200 mg, 23%; placebo, 5%) and dizziness (GEn 600 mg, 14%; GEn 1200 mg, 22%; placebo, 5%). IMPLICATIONS: GEn significantly improved individual IRLS items and sleep disturbance versus placebo. Correlations between IRLS and PSQ items were moderate to strong. This was not a formal meta-analysis and was not powered to compare the GEn doses. Nevertheless, our study finds that the benefits of GEn extend to individual IRLS items and supports the importance of sleep quality in RLS treatment. ClinicalTrials.gov identifiers: NCT00298623, NCT00365352, and NCT01332305.
Gabapentin Enacarbil: A Review in Restless Legs Syndrome.[Pubmed:27146056]
Drugs. 2016 May;76(8):879-87.
Gabapentin enacarbil is an extended-release prodrug of gabapentin that is approved in the USA (Horizant((R))) and Japan (Regnite((R))) for the treatment of moderate to severe primary restless legs syndrome (RLS) in adults [featured indication]. This article summarizes pharmacological, efficacy and tolerability data relevant to the use of oral Gabapentin enacarbil in this indication. In double-blind, multicentre trials, treatment with Gabapentin enacarbil 600 mg/day for 12 weeks significantly improved the symptoms of moderate to severe primary RLS in adults. Gabapentin enacarbil also significantly improved RLS pain scores and generally improved sleep and mood outcomes. These data are supported by retrospective pooled analyses of three of these trials (XP081, PIVOT RLS I and PIVOT RLS II), with Gabapentin enacarbil generally improving symptoms irrespective of disease severity, associated sleep disturbance or prior dopamine agonist use. Responses to Gabapentin enacarbil were sustained in longer-term trials, with lower relapse rates in Gabapentin enacarbil than placebo recipients in a longer-term maintenance study. Overall, in short and longer-term trials, relatively few patients discontinued treatment, adverse events were mostly mild to moderate in severity, and somnolence/sedation and dizziness were the most commonly reported adverse events. Notably, there were no reports of augmentation or QT-interval prolongation. Gabapentin enacarbil is an important agent for the treatment of adults with moderate to severe primary RLS.
