Randomized, Double-blind, Active & Placebo-controlled, 6-way Crossover Study of Abuse Potential of Oral Gabapentin Enacarbil IR Capsules With and Without Oxycodone in Healthy, Nondependent, Recreational Opioid Users

The purpose of this study is to assess the abuse potential of gabapentin enacarbil immediate release capsules taken alone and in combination with oxycodone in healthy adult, non-dependent, recreational opioid users.

开始日期2022-01-31

申办/合作机构

Arbor Pharmaceuticals, Inc.

NCT06097676

/ Completed临床4期

A Randomized, Double Blind, Active and Placebo Controlled, 5 Way Crossover Study to Determine the Abuse Potential of Orally Administered Gabapentin Enacarbil Immediate Release Capsules in Healthy, Nondependent Recreational Drug Users With Sedative Experience

The purpose of this study is to assess the abuse potential of gabapentin enacarbil in healthy adult, non-dependent, recreational drug users.

开始日期2021-09-28

申办/合作机构

Arbor Pharmaceuticals, Inc.

NCT03082755

/ Unknown status临床4期IIT

Nighttime Agitation and Restless Legs Syndrome in People With Alzheimer's Disease

Nighttime agitation in persons with Alzheimer's disease causes patient suffering, distresses caregivers, and often results in prescriptions for harmful antipsychotics. Effective treatments are lacking because of limited knowledge of the etiology of nighttime agitation. The investigators propose a clinical trial to better elucidate whether a sleep disorder, restless legs syndrome, may be a mechanism for nighttime agitation, and if treatment with gabapentin enacarbil (Horizant®) reduces nighttime agitation, improves sleep, reduces restless legs syndrome behaviors, and reduces antipsychotic medications.

开始日期2017-07-01

申办/合作机构

The University of Texas at Austin

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100 项与加巴喷丁酯相关的临床结果

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100 项与加巴喷丁酯相关的转化医学

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100 项与加巴喷丁酯相关的专利（医药）

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145

项与加巴喷丁酯相关的文献（医药）

2026-05-01·Sleep and Breathing

Placebo and nocebo responses in gabapentin enacarbil and pregabalin trials for restless legs syndrome: time-course model-based network meta-analysis and meta-analysis of proportions

Review

作者: Iftikhar, Imran H ; Lacki, Olga A ; Pedder, Hugo ; Albisher, Essa ; BaHammam, Ahmed S

Purpose:

Placebo responses are often stronger in randomized controlled trials (RCT) on conditions that measure subjective improvement in symptoms, such as restless legs syndrome (RLS). This meta-analysis sought to quantify both placebo and nocebo responses in published RCTs of gabapentin enacarbil (GEn) and pregabalin.

Methods:

In the first meta-analytic approach, we evaluated the time-courses taken by the participants randomized to the different doses of GEn and pregabalin and to placebo in their responses in International RLS Study Group Rating Scale (IRLS) scores. This was primarily evaluated by estimating the posterior median ET50s, the time (days) at which 50% of maximum response was achieved in IRLS scores for these participants. In a second meta-analytic approach, one-arm meta-analyses estimated proportions of participants on placebo considered “responders” on the investigator-initiated Clinical Global Impression-Improvement (CGI-I) scale, and separately of those who developed somnolence and dizziness.

Results:

A total of 16 RCTs were included in this meta-analysis. Relative differences in ET50s (median and 95% credible intervals) between GEn 600, 900, 1200, 1800, 2400 mg/d doses and placebo were 1.09 (0.07; 2.92), 1.35 (0.05; 5.85), 0.56 (0.02; 1.79), 0.62 (0.03; 2.34) and 1.61 (0.10; 5.22) days, respectively, and between pregabalin mean doses of 107.8 and 337.5 mg/d and placebo were 21.75 (0.89; 145.26) and 2.54 (0.12; 8.41) days, respectively, indicating largely clinically insignificant differences. Pooled proportion of CGI-I responders amongst the participants randomized to placebo was 0.40 [(95% confidence intervals (CI): 0.31; 0.49), I2 = 84%]. Duration of RCTs and previous RLS treatment were associated with CGI-I response based on meta-regression analyses. Pooled proportions of participants randomized to placebo who developed somnolence and dizziness were 0.05 [(95%CIs: 0.03; 0.08), I2 = 75%], and 0.02 [(95%CIs: 0.01; 0.04), I2 = 62%], respectively.

Conclusions:

GEn and pregabalin showed substantial placebo responses in RCTs. Further studies are needed that would identify predictor variables for placebo responders or non-responders.

Registration:

The protocol was registered in OSF (OSF.IO/79JCF).

2026-03-01·Sleep and Breathing

Benefit-risk comparison of gabapentin enacarbil versus pregabalin for restless legs syndrome: A dose-response model-based network meta-analysis

Review

作者: Dworetz, Alex ; Iftikhar, Imran H ; Rao, Saad T ; Albisher, Essa ; BaHammam, Ahmed S

Purpose:

Gabapentin enacarbil (GEn) and pregabalin are considered amongst the first-line drugs for restless legs syndrome (RLS). However, concerns remain about their dose-limiting side effects. This study aimed to elucidate the differences in their benefit-risk profiles through a dose-response model-based network meta-analysis (MBNMA).

Methods:

A systematic review and dose-response MBNMA was conducted to evaluate the effects of GEn and pregabalin on International RLS Study Group Rating Scale (IRLS) scores, rates of responders on investigator-initiated Clinical Global Impression-Improvement (CGI-I) scales, and on prevalence of treatment-emergent adverse effects (TEAE). Dose-response curves (DRC), model-derived median effective and toxic doses (ED50, TD50) and therapeutic indices (TI = TD50/ED50) were calculated.

Results:

Fifteen studies involving 2,885 were analyzed. DRCs showed dose-response relationship for IRLS scores only for pregabalin and dose-response relationships for both GEn and pregabalin for CGI-I responder rates, somnolence and dizziness TEAEs. Based on CGI-I responder rates, the model-derived ED50 for GEn and pregabalin was 93.80 mg/d and 123.55 mg/d, respectively. The model-derived TD50 for somnolence and dizziness for GEn and pregabalin were 112.85 mg/d and 101.59 mg/d, and 106.08 mg/d and 104.83 mg/d, respectively. At their model-derived ED50 and TD50, there were no significant differences between GEn and pregabalin rankings. The TIs for GEn and pregabalin ranged from 1.08 to 1.20, and 0.84—1.19, respectively.

Conclusions:

GEn and pregabalin have narrow TIs based on model-derived ED50 and TD50.Estimates from this MBNMA could inform future trials for studying optimal dosing that would maximize benefits and minimize risks.

2026-02-24·JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Restless Legs Syndrome

Review

作者: Wipper, Benjamin ; Winkelman, John W.

Importance:

Restless legs syndrome (RLS) is a sleep-related movement disorder that affects approximately 3% of US adults to a clinically significant extent and can cause substantial sleep disturbance.

Observations:

Restless legs syndrome is characterized by an overwhelming urge to move the limbs, typically the legs, often accompanied by unpleasant limb sensations (eg, achiness, tingling). Symptoms, provoked by immobility, are relieved while moving and are typically present or most severe in the evening or at night. Restless legs syndrome symptoms may lead to difficulty falling asleep, staying asleep, or returning to sleep. According to population-based studies, approximately 8% of US adults experience RLS symptoms of any frequency annually and 3% experience moderately or severely distressing symptoms at least twice weekly. Patients with RLS have impaired quality of life and elevated rates of cardiovascular disease (29.6% with coronary artery disease, stroke, or heart failure), depression (30.4%), and suicidal ideation or self-harm (0.35 cases/1000 person-years). Restless legs syndrome is common among patients with multiple sclerosis (27.5%), end-stage kidney disease (24%), and iron deficiency anemia (23.9%); during pregnancy and especially in the third trimester (22%); with peripheral neuropathy (eg, diabetic, idiopathic; 21.5%); and with Parkinson disease (20%). Other risk factors include family history of RLS, northern European descent, female sex (2:1 vs male sex), and older age (RLS prevalence of 10% in adults ≥65 years). Restless legs syndrome is diagnosed based on clinical history; polysomnography is not recommended for diagnosis. Iron supplementation with ferrous sulfate (325-650 mg daily or every other day) or intravenous iron (1000 mg) should be initiated for serum ferritin level less than or equal to 100 ng/mL or transferrin saturation less than 20%. If possible, medications associated with RLS, including serotonergic antidepressants, dopamine antagonists, and centrally acting H1 antihistamines (eg, diphenhydramine), should be discontinued. Gabapentinoids (eg, gabapentin, gabapentin enacarbil, pregabalin) are first-line pharmacologic therapy. In randomized clinical trials, approximately 70% of patients treated with gabapentinoids had much or very much improved RLS symptoms vs approximately 40% with placebo ( P &lt; .001). Dopamine agonists (eg, ropinirole, pramipexole, rotigotine) are no longer recommended as first-line medications due to the risk of augmentation, an iatrogenic worsening of RLS symptoms, which has an annual incidence of 7% to 10% with these medications. Patients who do not improve with first-line treatment or have augmented RLS often benefit from low-dose opioids (eg, methadone 5-10 mg daily).

Conclusions and Relevance:

Restless legs syndrome affects approximately 3% of adults and can have negative effects on sleep and quality of life. Initial management includes cessation of exacerbating medications, as well as iron supplementation for patients with low-normal iron indices. If medication therapy is indicated, gabapentinoids are first-line treatment.

项与加巴喷丁酯相关的新闻（医药）

2026-07-04

·贾传宇神经笔记

不宁腿综合征诊疗进展：从指南更新到临床实践

不宁腿综合征（Restless Legs Syndrome, RLS），又称Willis-Ekbom病，是临床常见的神经系统感觉运动障碍性疾病，以静息状态下下肢难以名状的不适感、强烈的活动肢体欲望、活动后症状缓解、夜间症状加重为核心特征。流行病学数据显示，全球成人RLS临床显著患病率约2%~3%，我国成人患病率为1.2%~5.5%，女性患病率约为男性的2倍，60岁以上老年人群患病率可达8%~15%。尽管RLS发病率较高，但临床漏诊率、误诊率长期居高不下，且既往治疗方案存在不规范、长期用药不良反应风险高等问题。近年来，随着国际顶级期刊研究成果的发布与权威指南的更新，RLS的诊疗理念发生了里程碑式的变革。本文结合国内外最新指南共识与顶刊循证证据，系统梳理RLS的诊疗进展，为临床规范化诊疗提供参考。一、诊断标准与临床评估：核心共识与实践要点 RLS的诊断始终以临床症状为核心，无需依赖多导睡眠监测（PSG）等辅助检查即可完成临床诊断，这一原则在最新指南与综述中得到进一步巩固。（一）核心诊断标准目前全球通用的是国际不宁腿综合征研究小组（IRLSSG）2012年更新的诊断标准，我国《中国不宁腿综合征的诊断与治疗指南（2021版）》在此基础上结合国情进行了补充，诊断需同时满足以下3项核心条件：症状核心特征：存在迫切需要活动腿部的欲望，通常伴腿部不适感，且符合3个关键规律：①静息/不活动状态（躺卧、久坐）下症状出现或加重；②活动（行走、拉伸）后症状部分或完全缓解；③症状主要或仅在傍晚/夜间加重。排他性诊断：上述症状不能由腿抽筋、姿势不适、肌痛、下肢静脉曲张、水肿、关节炎、静坐不能等其他疾病或行为问题完全解释。功能损害证据：症状导致患者睡眠紊乱、焦虑抑郁、社交/职业功能障碍等，对生活质量造成负面影响。补充说明：对于症状严重的患者，活动后缓解、夜间加重的特征可能不明显，但需有既往典型症状史作为支撑；儿童患者常无法准确描述不适感，需关注其按摩肢体、频繁踱步、睡前腿部摩擦等行为征象。（二）临床评估的更新要点 2025年美国睡眠医学会（AASM）发布的RLS临床实践指南，首次将铁代谢指标的常规评估列为所有RLS患者的必查项目，明确要求对所有临床显著RLS患者，需晨起空腹检测血清铁蛋白、转铁蛋白饱和度，检测前24小时需避免含铁补充剂与食物。临床评估需同时完成以下内容：病因筛查：重点排查缺铁、慢性肾脏病、妊娠、糖尿病周围神经病变、帕金森病、多发性硬化等继发性因素，同时筛查抗抑郁药、抗组胺药、多巴胺拮抗剂、钙通道阻滞剂等可能诱发/加重RLS的药物。严重程度评估：首选国际RLS评定量表（IRLS），这是目前全球通用的症状严重程度评估工具，可精准量化症状频率、睡眠影响、功能损害等维度。辅助检查的合理应用：PSG不推荐作为常规诊断手段，仅用于诊断不明确、合并其他睡眠障碍、评估周期性肢体运动（PLMS）的患者；制动试验（SIT）、下肢神经电生理、血管超声可用于鉴别诊断。二、发病机制的最新研究进展近年来，RLS的病理生理机制研究从传统的多巴胺系统失衡，逐步转向以中枢铁代谢异常为核心的多通路机制，为靶向治疗提供了新的方向。（一）中枢铁缺乏是RLS的核心病理基础多项尸检、影像学及脑脊液研究证实，即使患者外周血清铁指标正常，也可能存在中枢神经系统铁缺乏，这是RLS发病的始动因素。铁是多巴胺合成限速酶酪氨酸羟化酶的关键辅基，同时参与多巴胺受体功能调控、髓磷脂合成与神经能量代谢，中枢铁缺乏可直接导致多巴胺系统功能紊乱、脊髓神经元过度兴奋，进而引发RLS症状。 2024年一项发表于Annals of Neurology的研究发现，RLS患者血脑屏障铁转运蛋白表达异常，导致铁向中枢神经系统的转运障碍，这解释了部分患者外周铁正常但中枢铁缺乏的现象，也为静脉铁剂治疗提供了直接的病理生理依据。（二）遗传易感性的新发现全基因组关联分析（GWAS）已发现164个与RLS相关的风险基因位点，其中MEIS1、BTBD9、PTPRD等基因与RLS发病强相关。MEIS1基因参与神经系统发育与铁稳态调控，是目前已知与RLS关联最显著的基因；BTBD9基因异常可通过影响铁代谢与多巴胺通路，增加RLS发病风险。双生子研究显示，RLS的遗传度最高可达70%，约50%的原发性RLS患者存在一级亲属阳性家族史，早发型RLS（<45岁）患者的家族聚集性更为显著。（三）其他通路的研究突破除铁代谢与多巴胺系统外，近年来研究发现腺苷通路、内源性阿片系统、谷氨酸能神经元异常也参与RLS的发病。2021年一项发表于Movement Disorders的研究证实，腺苷A2A受体异常可导致脊髓下行抑制通路功能失调，这一发现推动了双嘧达莫等腺苷通路药物在RLS治疗中的应用探索；2024年研究发现，RLS患者脑脊液内源性β-内啡肽水平显著降低，尤其是伴疼痛症状的患者，为阿片类药物治疗难治性RLS提供了理论支撑。三、治疗策略的里程碑式更新 2025年AASM发布的《不宁腿综合征与周期性肢体运动障碍治疗临床实践指南》，彻底颠覆了既往以多巴胺能药物为一线的治疗格局，确立了以铁剂纠正为基础、α-2δ钙通道配体为一线首选、严格限制多巴胺能药物使用的核心治疗原则。我国2021版指南与2026年JAMA顶级综述也同步更新了相关治疗推荐，形成了全球统一的规范化治疗框架。（一）基础治疗：可逆性因素干预与铁剂补充 1. 诱因干预：所有RLS患者需首先停用/替换可能诱发RLS的药物，包括SSRI/SNRI类抗抑郁药、第一代抗组胺药、多巴胺拮抗剂、部分钙通道阻滞剂；同时避免酒精、咖啡因、尼古丁摄入，建立规律睡眠作息，适度进行下肢拉伸运动。2. 铁剂治疗：RLS的根源性干预最新指南大幅放宽了铁剂补充的指征，强化了静脉铁剂的治疗地位，核心推荐如下：- 成人患者：血清铁蛋白≤75ng/ml或转铁蛋白饱和度<20%，推荐启动铁剂补充；铁蛋白75~100ng/ml的患者，可结合症状考虑静脉铁剂治疗。 - 口服铁剂：条件推荐硫酸亚铁325mg+维生素C 100mg，每日2次，疗程3个月，目标是将血清铁蛋白维持在75ng/ml以上。 - 静脉铁剂：对于血清铁蛋白≤75ng/ml的患者，强烈推荐静脉注射羧基麦芽糖铁（1000mg单次给药），证据等级中等；对于口服铁剂无效、无法耐受或合并慢性肾脏病的患者，优先选择静脉铁剂。 - 禁忌证：血清铁蛋白>300μg/L或转铁蛋白饱和度>45%的患者，禁用静脉铁剂。（二）药物治疗：一线治疗格局彻底重构 2025年AASM指南首次将α-2δ钙通道配体列为成人RLS的强推荐一线治疗，同时明确建议避免将多巴胺能药物作为标准常规治疗，仅可短期、知情同意下使用。1. 一线首选药物：α-2δ钙通道配体包括加巴喷丁依那卡比、加巴喷丁、普瑞巴林，3种药物均获得AASM指南强推荐（中等证据等级）。- 核心优势：可有效缓解RLS下肢不适感、改善睡眠质量，且长期使用导致症状恶化（augmentation）的风险显著低于多巴胺能药物，尤其适用于伴疼痛、失眠、焦虑的RLS患者。 - 临床应用：普瑞巴林起始剂量75mg睡前口服，可逐步滴定至300mg/d；加巴喷丁起始剂量300mg睡前口服，可根据疗效滴定至1200~1800mg/d，分2~3次服用。 - 注意事项：主要不良反应为头晕、嗜睡、体重增加，需从小剂量起始，缓慢滴定；目前国内该类药物尚未获批RLS适应症，需超说明书用药时充分告知患者并签署知情同意书。2. 多巴胺能药物：严格限制使用，降级为二线/短期用药包括普拉克索、罗匹尼罗、罗替高汀贴剂、左旋多巴，既往曾是RLS的一线首选，但长期随访研究显示，该类药物长期使用的症状恶化发生率高达40%~75%，年发生率7%~10%。 2025年AASM指南对该类药物给出了条件性反对常规使用的推荐，核心要求如下：- 仅可用于患者充分知情同意后，短期、间歇性使用，或其他一线药物无效/无法耐受的患者； - 严禁用于慢性持续型RLS患者的长期常规治疗，禁止通过增加剂量来控制恶化的症状； - 普拉克索是我国唯一获批RLS适应症的药物，起始剂量0.125mg睡前口服，最大剂量不超过0.75mg/d，使用过程中需密切监测症状恶化征象。3. 难治性RLS的治疗选择对于一线药物治疗无效、出现症状恶化的难治性RLS患者，指南给出了以下循证推荐：- 低剂量阿片类药物：条件推荐缓释羟考酮，起始剂量5~10mg睡前口服，缓慢滴定，适用于其他治疗无效的严重难治性RLS；长期研究显示，规范筛查后的患者长期使用成瘾风险极低，需严格评估呼吸睡眠暂停风险，避免与镇静类药物联用。 - 神经调控治疗：条件推荐双侧高频腓神经刺激，作为药物难治性RLS的非侵入性替代方案；此外，经颅直流电刺激（tDCS）、经皮脊髓直流电刺激（tsDCS）也在临床研究中显示出一定疗效，可用于个体化治疗。 - 其他药物：双嘧达莫获得条件性推荐，可用于一线药物效果不佳的患者；对于合并失眠的患者，不推荐氯硝西泮单药治疗，因其仅能改善睡眠，无法缓解RLS核心症状。（三）非药物治疗进展除生活方式干预外，近年来多项研究证实，下肢渐进式抗阻训练、有氧运动、局部加压治疗、经皮神经电刺激（TENS）可显著改善轻中度RLS患者的症状，可作为药物治疗的辅助手段，尤其适用于妊娠、哺乳期等不适合药物治疗的患者。2023年FDA批准的强直运动激活（TOMAC）系统，通过模拟下肢运动的肌肉激活，可显著改善药物难治性RLS患者的症状与睡眠质量，为非药物治疗提供了新的选择。四、特殊人群的诊疗规范（一）妊娠期与哺乳期女性妊娠期RLS患病率约22%，以妊娠晚期最高，约75%的患者产后1个月内症状可自行缓解。 - 治疗原则：以非药物治疗为主，优先纠正铁缺乏，血清铁蛋白<50ng/ml的患者需启动口服铁剂+维生素C治疗； - 药物治疗：仅在症状严重、严重影响睡眠的患者，权衡利弊后短期使用药物，目前无任何药物获批妊娠期RLS适应症，禁止使用多巴胺能药物，哺乳期需避免所有药物经乳汁分泌的风险。（二）儿童与青少年儿童RLS诊断需严格遵循IRLSSG标准，症状描述需采用儿童自身语言，需排除生长痛、注意力缺陷多动障碍（ADHD）等疾病。 - 治疗：优先纠正铁缺乏，血清铁蛋白<50ng/ml的患者推荐口服硫酸亚铁治疗；非药物治疗为核心，包括规律作息、适度运动、睡眠卫生教育；目前无药物获批儿童RLS适应症，药物治疗仅用于症状严重、功能损害显著的患者，需严格评估获益风险比。（三）终末期肾病患者终末期肾病（ESRD）患者RLS患病率高达24%，是影响患者生存质量与预后的重要因素。 - 治疗：优先纠正铁缺乏，条件推荐静脉蔗糖铁治疗；一线药物推荐加巴喷丁，需根据肾功能调整剂量；避免常规使用多巴胺能药物；充分透析、肾移植可显著改善部分患者的症状。（四）帕金森病合并RLS患者帕金森病患者RLS患病率约20%，需注意与帕金森病夜间症状、剂末现象、静坐不能鉴别。 - 治疗：优先纠正铁缺乏，首选α-2δ钙通道配体治疗，避免盲目增加多巴胺能药物剂量，以免加重RLS症状恶化。五、总结与展望近年来，RLS的诊疗实现了从“对症治疗”到“对因治疗”的核心转变，中枢铁缺乏的病理机制被进一步证实，铁剂补充成为RLS全程治疗的基础；治疗格局从“多巴胺时代”迈入“非多巴胺优先”的新时代，大幅降低了长期治疗的症状恶化风险；难治性RLS的神经调控、新型靶向药物研发也取得了显著进展。但目前我国RLS诊疗仍面临漏诊误诊率高、治疗不规范、临床医生认知不足等问题，未来需进一步加强临床医生培训，推动国内多中心临床研究，制定更符合中国人群的诊疗规范；同时需深入探索RLS的遗传机制与靶向治疗靶点，开发更安全、有效的新型治疗药物，为RLS患者提供更精准的个体化诊疗方案。参考文献 1. 中国医师协会神经内科医师分会睡眠学组, 中华医学会神经病学分会睡眠障碍学组, 中国睡眠研究会睡眠障碍专业委员会. 中国不宁腿综合征的诊断与治疗指南(2021版)[J]. 中华医学杂志, 2021, 101(13): 908-925. 2. Winkelman JW, Berkowski JA, DelRosso LM, et al. Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline[J]. J Clin Sleep Med, 2025, 21(1): 137-152. 3. Winkelman JW, Berkowski JA, DelRosso LM, et al. Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine systematic review, meta-analysis, and GRADE assessment[J]. J Clin Sleep Med, 2025, 21(1): 153-199. 4. Winkelman JW, Wipper B. Restless Legs Syndrome: A Review[J]. JAMA, 2026, 335(8): 703-714. 5. Allen RP, Picchietti DL, Garcia-Borreguero D, et al. Restless legs syndrome/Willis-Ekbom disease diagnostic criteria: updated international restless legs syndrome study group (IRLSSG) consensus criteria–history, rationale, description, and significance[J]. Sleep Med, 2014, 15(8): 860-873. 6. Xu X, Ruan J, Tao T, et al. Role of vitamins in the pathogenesis and treatment of restless leg syndrome: A systematic review and meta-analysis[J]. PLoS ONE, 2025, 20(3): e0313571. 7. Koo BB, Abdelfattah A, Eysa A, et al. The melanocortin and endorphin neuropeptides in patients with restless legs syndrome[J]. Ann Neurol, 2024, 95(4): 688-699. 8. Garcia-Borreguero D, Cano-Pumarega I, Garcia Malo C, et al. Reduced response to gabapentin enacarbil in restless legs syndrome following long-term dopaminergic treatment[J]. Sleep Med, 2019, 55: 74-80. 9. Trenkwalder C, Winkelmann J, Oertel W, et al. Ferric carboxymaltose in patients with restless legs syndrome and nonanemic iron deficiency: a randomized trial[J]. Mov Disord, 2017, 32(10): 1478-1482. 10. Allen RP, Chen C, Garcia-Borreguero D, et al. Comparison of pregabalin with pramipexole for restless legs syndrome[J]. N Engl J Med, 2014, 370(7): 621-631.

2025-02-06

·化学经纬

书籍分享||新药化学全合成路线手册

内容介绍本书归纳和综述了新药的化学合成路线。覆盖范围为近5年美国FDA批准上市的新分子实体药共109个。针对每一个药物，本书给出了药物简介，药物化学结构信息，产品上市信息，药品专利保护和市场独占权保护信息，化学全合成路线和参考文献等。这些合成路线大多是目前制药工业中正在使用的化学合成工艺，有较高的实用性和学术价值。对参与反应的起始原料、中间体、反应产物都给出了详细的化学结构。每一步化学合成反应都给出了重要的化学试剂、催化剂、所使用的溶剂、合成反应条件及文献出处等。本书的特点是：作者从浩如烟海的科技文献中，精心挑选出最新、最有实用价值的合成方法，汇编成化学合成路线图，内容简洁，深入浅出，逻辑性强，容易理解，以最少的篇幅表达最多的技术信息，可帮助读者很快找到他们需要的药物合成方法及最可靠的原始科学论文。读者对象： 1.任何从事与化学合成、药物合成、精细化工相关专业的科研人员、企业管理人员。 2.有机化学专业、药学专业、生物制药专业等大专院校的高年级学生、研究生、教师及科研人员。 3.从事客户委托的药物原料与药物中间体合成的科研人员、企业管理人员。编辑推荐对于制药企业而言,一个好的药物全合成路线, 可以大大缩短生产周期,简化生产工艺,降低生产成本,节约能源,减少或消除对环境的化学污染与排放。本书为了顺应我国近年来生物制药及医药工业飞速发展的潮流编写的，详细介绍了近五年美国FDA批准上市的所有（109个）新分子实体药的化学全合成路线。这些全合成路线多数是国外制药厂目前正在使用的工艺，其经济效益及社会效益都是极为显著，因此本书既有较高的科学价值又有很大的实用性。作者简介陈清奇，旅美药学家和化学家，担任美国MedKoo生物医药科研公司总裁，同时兼任美国数家生物制药公司的技术顾问，中国国内数个大学的客座教授。研究领域为药物化学，纳米医学体外诊断技术。书籍目录 Abiraterone Acetate（醋酸阿比特龙）001 Aclidinium Bromide（阿克利溴铵）006 Afatinib（阿法替尼）009 Alcaftadine（阿卡他定）014 Alogliptin（阿格列汀）017 Apixaban（阿哌沙班）022 Apremilast（阿普斯特）028 Avanafil（阿伐那非）033 Axitinib（阿西替尼）038 Azilsartan Kamedoxomil（阿齐沙坦酯钾盐）044 Bazedoxifene（巴多昔芬）048 Bedaquiline（贝达喹啉）053 Belinostat（贝利司他）060 Boceprevir（波西普韦）064 Bosutinib（博舒替尼）071 Cabozantinib（卡博替尼）075 Canagliflozin（卡格列净）078 Carfilzomib（卡非佐米）083 Ceftaroline Fosamil（头孢洛林酯）087 Ceftolozane（噻呋特啰嗪）094 Ceritinib（色瑞替尼）098 Clobazam（氯巴占）101 Cobicistat（可比司他）104 Crizotinib（克里唑蒂尼）112 Dabigatran Etexilate Mesylate（甲磺酸达比加群酯）118 Dabrafenib（达拉菲尼）123 Dapagliflozin（达格列净）127 Dasabuvir（达沙布韦）132 Deferiprone（去铁酮）136 Dienogest（地诺孕素）138 Dolutegravir（度鲁特韦）141 Droxidopa（屈昔多巴）145 Efinaconazole（艾氟康唑）149 Eliglustat（依利格鲁司特）152 Elvitegravir（埃替格韦）155 Empagliflozin（依帕列净）161 Enzalutamide（恩杂鲁胺）166 Eribulin Mesylate（甲磺酸艾日布林）168 Eslicarbazepine Acetate（艾利西平醋酸酯）175 Estradiol Valerate（雌二醇戊酸酯）180 Ezogabine（依佐加滨）185 Finafloxacin（非那沙星）193 Fingolimod Hydrochloride（盐酸芬戈莫德）197 Florbetapir F 18（氟比他匹）205 Flutemetamol F 18（富特米他）211 Gabapentin Enacarbil（加巴喷丁恩那卡比）214 Gadobutrol（钆布醇）218 Gadoterate Meglumine（钆特酸葡甲胺）224 Ibrutinib（依鲁替尼）227 Icatibant（艾替班特）232 Idelalisib（艾代拉里斯）234 Indacaterol （茚达特罗）236 Ingenol Mebutate（巨大戟醇甲基丁烯酸酯）240 Ioflupane 123I（碘[123I]氟潘）242 Ivacaftor（依瓦卡特）247 Ledipasvir（雷迪帕韦）250 Linaclotide（利那洛肽）259 Linagliptin（利拉利汀）261 Lomitapide（洛美他派）267 Lorcaserin（氯卡色林）270 Lucinactant（芦西纳坦）274 Luliconazole（卢立康唑）276 Lurasidone（鲁拉西酮）279 Macitentan（马西替坦）283 Miltefosine（米替福新）286 Mipomersen Sodium（米泊美生钠）290 Mirabegron（米拉贝隆）292 Naloxegol（纳罗克格）296 Netupitant（奈妥吡坦）299 Nintedanib（尼达尼布）303 Olaparib（奥拉帕尼）307 Olodaterol（奥达特罗）311 Omacetaxine Mepesuccinate（高三尖杉酯碱）315 Ombitasvir（艾姆伯韦）319 Ospemifene（奥培米芬）323 Paritaprevir（帕瑞它韦）327 Pasireotide（帕瑞肽）331 Peramivir（帕拉米韦）333 Perampanel（吡仑帕奈）337 Pirfenidone（吡非尼酮）343 Pomalidomide（泊马度胺）345 Ponatinib（泊那替尼）351 Regorafenib（瑞戈非尼）355 Rilpivirine（利匹韦林）357 Riociguat（利奥西呱）366 Rivaroxaban（利伐沙班）370 Roflumilast（罗氟司特）378 Ruxolitinib（鲁索替尼）384 Simeprevir（司美匹韦）388 Sofosbuvir（索非布韦）396 Suvorexant（苏沃雷生）401 Tafluprost（他氟前列腺素）405 Tasimelteon（他司美琼）409 Tavaborole（它瓦波罗）413 Tedizolid Phosphate（磷酸特地唑胺）415 Telaprevir（替拉瑞韦）418 Teriflunomide（特立氟胺）426 Ticagrelor（替格瑞洛）430 Tofacitinib（托法替尼）438 Trametinib（曲美替尼）443 Umeclidinium（芜地溴铵）447 Vandetanib（凡德他尼）450 Vemurafenib（威罗菲尼）456 Vilanterol（维兰特罗）460 Vilazodone Hydrochloride（盐酸维拉佐酮）463 Vismodegib（维莫德吉）468 Vorapaxar（沃拉帕沙）470 Vortioxetine（沃替西汀）473 附录1本书使用的期刊名称缩写表477 附录2专利文献代码481 附录3美国药品专利中的用途代码定义484 附录4美国药品市场独占权代码定义530 附录5美国FDA于2010—2014批准上市的药物名单563 英文索引607 中文索引611 CAS登记号索引613 下载方式现在，这份资料分享给大家。小编在公众号设置了自动回复功能，在公众号后台回复关键词：新药全合成 ●书籍分享||有机氧化反应原理与应用 ●书籍分享||有机卤化反应原理及应用 ●推荐合成书籍【有机缩合反应原理与应用】 ●推荐合成书籍【有机环合反应原理与应用】 ●书籍分享||有机还原反应原理与应用 ●ChemDraw使用让你从化学菜鸟变成老鸟 ●干货分享||有机合成: 策略与控制 ●干货分享||有机合成工艺研发-副反应抑制法 ●基础有机化学(邢其毅)第3、4版教材+习题解析 ●ChemDrawV20最新版详细安装图文教程 ●干货分享||核磁共振二维谱 ●书籍分享||全合成中的经典:更多的目标、战略和方法 ●书籍分享||实用药物化学 ●书籍分享||基于模仿创新的小分子药物发明 ●书籍分享||制药工艺开发-目前的化学与工程挑战 ●书籍分享||手性合成:不对称反应及其应用(第5版) ●书籍分享||新药研发案例研究--明星药物如何从实验室走向市场 ●书籍分享||英汉·汉英化学化工词汇 ●书籍分享||有机化学结构与功能（第四版） ●书籍分享||过渡金属有机化学(原著第6版） ●重磅书籍分享||不对称催化基础 ●书籍分享||药物设计学-唐赟

上市批准高管变更

2024-12-02

·drugs

Guidelines Developed for Treatment of Restless Legs Syndrome

MONDAY, Dec. 2, 2024 -- In a clinical practice guideline issued by the American Academy of Sleep Medicine and published online Sept. 26 in the Journal of Clinical Sleep Medicine , recommendations are presented for the treatment of restless legs syndrome (RLS). John W. Winkelman, M.D., Ph.D., from Massachusetts General Hospital in Boston, and colleagues developed recommendations for treatment of RLS and periodic limb movement disorder in adults and pediatric patients. The researchers developed three good practice statements that were based on expert consensus. They recommend all clinicians should regularly test serum iron studies, including ferritin and transferrin saturation, in all patients with clinically significant RLS, ideally in the morning; analysis of these studies influences the decision to use oral or intravenous (IV) iron treatment. The authors also state that addressing exacerbating factors, including alcohol, caffeine, antihistaminergic, serotonergic, and anti-dopaminergic medications, should be the first step in RLS management. They note RLS is common in pregnancy and the pregnancy-specific safety profile of each treatment should be considered. Recommendations for adults with RLS include use of gabapentin enacarbil over no gabapentin enacarbil; use of gabapentin over no gabapentin; use of pregabalin over no pregabalin; and use of IV ferric carboxymaltose over no IV ferric carboxymaltose for those with appropriate iron status (strong recommendations; moderate certainty of evidence). In addition, there is a strong recommendation against use of cabergoline. "Guided by the best evidence in the scientific literature, we've provided recommendations that will improve the ability of clinicians to provide patient-centered care for people who have RLS," Winkelman said in a statement. One author disclosed ties to the pharmaceutical and medical device industries. Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

100 项与加巴喷丁酯相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09539	加巴喷丁酯	N03AX12	DB08872

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
疱疹后神经痛	美国	Azurity Pharmaceuticals, Inc.	2012-06-06
不宁腿综合征	美国	Azurity Pharmaceuticals, Inc.	2011-04-06

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
酒精使用障碍	临床2期	美国	Arbor Pharmaceuticals, Inc.	2015-06-01
偏头痛	临床2期	美国	XenoPort, Inc.	2008-08-01
偏头痛	临床2期	加拿大	XenoPort, Inc.	2008-08-01
糖尿病周围神经病变	临床2期	美国	XenoPort, Inc.	2008-03-01
神经痛	临床2期	美国	XenoPort, Inc.	2008-03-01
糖尿病周围神经性疼痛	临床2期	日本	Astellas Pharma, Inc.	2007-07-01
舞蹈手足徐动症	临床1期	美国	XenoPort, Inc.	2016-01-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT06247488 (CTgov)	临床4期	-	110	Placebo (Placebo)	艱範蓋遞壓積網築獵醖(觸鬱觸壓繭構鹹鏇膚遞) = 顧選蓋憲齋鹹製簾範鏇製醖選選鑰蓋窪廠襯觸 (簾鹽繭顧蓋憲鹽艱選壓, 1.75) 更多	-	2024-07-30
				Oxycodone 20 mg (Oxycodone 20 mg)	艱範蓋遞壓積網築獵醖(觸鬱觸壓繭構鹹鏇膚遞) = 遞鹹積鹽餘淵鑰廠網衊製醖選選鑰蓋窪廠襯觸 (簾鹽繭顧蓋憲鹽艱選壓, 2.08) 更多
NCT02840240 (CTgov)	N/A	疼痛 \| 麻醉	107	Gabapentin enacarbil (Gabapentin Enacarbil)	鬱遞壓製鏇築鏇蓋構鑰(鹽製膚淵積蓋壓廠齋鹹) = 壓願鏇選襯顧餘鑰遞簾蓋鑰齋壓衊艱蓋選製餘 (憲齋顧壓夢襯鹽襯壓範, 1.6) 更多	-	2024-01-09
				Placebo (Placebo)	鬱遞壓製鏇築鏇蓋構鑰(鹽製膚淵積蓋壓廠齋鹹) = 窪蓋鹹積顧廠積窪選夢蓋鑰齋壓衊艱蓋選製餘 (憲齋顧壓夢襯鹽襯壓範, 1.7) 更多
NCT06097676 (CTgov)	临床4期	-	86	Placebo (Placebo)	構襯鑰積衊構廠鏇醖壓(製醖繭壓糧襯衊襯築鬱) = 襯齋獵觸餘遞窪顧齋糧醖鑰遞獵範窪顧餘遞齋 (顧衊鬱醖廠顧鏇餘獵構, 1.47) 更多	-	2024-01-03
				Alprazolam 2 mg (Alprazolam 2 mg)	構襯鑰積衊構廠鏇醖壓(製醖繭壓糧襯衊襯築鬱) = 鹹淵鬱艱齋遞製廠醖網醖鑰遞獵範窪顧餘遞齋 (顧衊鬱醖廠顧鏇餘獵構, 1.93) 更多
NCT02642315 (XP-IIT-0034, CTgov)	N/A	不宁腿综合征	10	Horizant	憲鹽襯網範憲鏇廠積網(襯築鹹壓簾觸鹹築淵築) = 艱鏇願築襯願蓋網鑰艱齋鑰壓醖鏇簾鹹憲遞觸 (齋築範餘鬱淵範淵鏇願, 襯窪網蓋積鹹積觸築醖 ~ 鏇鏇繭鏇襯艱顧餘網窪) 更多	-	2022-02-24
NCT03053427 (CTgov)	临床4期	不宁腿综合征	375	Placebo (Placebo)	顧選窪遞簾糧鹹窪顧築(繭鹹選選鬱獵壓觸選範) = 願鹽蓋觸鹽憲積襯襯獵憲繭淵網鹽膚鑰獵鬱淵 (壓壓鏇製鹹顧壓窪壓網, 膚醖繭簾襯廠壓齋網衊 ~ 餘憲範齋顧獵廠醖齋鏇) 更多	-	2019-07-10
				Gabapentin enacarbil (Gabapentin Enacarbil)	顧選窪遞簾糧鹹窪顧築(繭鹹選選鬱獵壓觸選範) = 選窪齋鬱獵範窪襯遞憲憲繭淵網鹽膚鑰獵鬱淵 (壓壓鏇製鹹顧壓窪壓網, 壓淵糧築構簾蓋糧積簾 ~ 廠網淵壓選膚膚遞構範) 更多
NCT02252536 (Pubmed) 人工标引	临床2期	酒精使用障碍	346	gabapentin enacarbil	範壓齋艱範醖鏇遞鹽壓(淵窪餘壓衊範築廠鏇齋) = 艱鏇築蓋獵醖艱蓋醖範網醖膚窪顧夢顧製遞夢 (夢膚鬱艱網窪遞鹽築衊 )	不佳	2019-01-01
				Placebo	範壓齋艱範醖鏇遞鹽壓(淵窪餘壓衊範築廠鏇齋) = 遞壓積網餘網簾觸齋簾網醖膚窪顧夢顧製遞夢 (夢膚鬱艱網窪遞鹽築衊 )
NCT02252536 (CTgov)	临床2期	酒精使用障碍	346	Placebo (Sugar Pill)	築膚鹽築夢顧製獵顧衊 = 網製膚選齋觸鏇鹹壓襯淵蓋廠遞醖糧壓膚襯壓 (獵鏇膚積糧鏇繭襯廠鏇, 淵製壓醖鏇廠繭網鹽齋 ~ 窪鏇憲觸壓積憲廠齋餘) 更多	-	2018-09-21
				gabapentin enacarbil (Gabapentin Enacarbil)	築膚鹽築夢顧製獵顧衊 = 鑰構艱構膚艱廠網選夢淵蓋廠遞醖糧壓膚襯壓 (獵鏇膚積糧鏇繭襯廠鏇, 構餘餘選鬱窪鑰繭顧範 ~ 襯齋積願窪範淵鹹網醖) 更多
AAN2015	N/A	不宁腿综合征	541	Gabapentin Enacarbil 600 mg	鬱餘鹹艱網網觸遞構膚(醖夢觸鏇積醖淵構壓繭) = 製鏇簾觸網選鹽網網窪夢願製簾鏇觸膚衊夢齋 (艱遞積蓋鏇艱膚繭膚願 )	-	2015-04-06
				Gabapentin Enacarbil 1200 mg	鬱餘鹹艱網網觸遞構膚(醖夢觸鏇積醖淵構壓繭) = 積鹽鏇憲獵製壓鬱鑰廠夢願製簾鏇觸膚衊夢齋 (艱遞積蓋鏇艱膚繭膚願 )
NCT01668667 (CONCORD, CTgov)	临床4期	不宁腿综合征	501	GSK1838262 600 mg (GSK1838262 600 mg)	簾顧憲醖膚築糧廠襯齋(糧鑰廠窪淵獵繭淵壓觸) = 獵夢鏇淵艱憲築鹽齋顧鬱餘蓋選範鏇網鹹艱網 (選遞醖網願窪願醖齋衊, 0.745) 更多	-	2014-11-17
				GSK1838262 450 mg (GSK1838262 450 mg)	簾顧憲醖膚築糧廠襯齋(糧鑰廠窪淵獵繭淵壓觸) = 製遞鬱選構膚鑰構膚蓋鬱餘蓋選範鏇網鹹艱網 (選遞醖網願窪願醖齋衊, 0.764) 更多
NCT01332305 (Pubmed \| Clin Neuropharmacol) 人工标引	临床2期	不宁腿综合征	217	gabapentin enacarbil	齋憲夢鑰淵淵襯遞窪遞(憲獵繭鏇範齋淵艱膚鬱) = 廠構積築遞遞繭簾壓構廠窪網觸廠夢鹹願蓋衊 (繭淵窪壓鏇淵觸廠餘淵 )	积极	2012-07-01
				Placebo	齋憲夢鑰淵淵襯遞窪遞(憲獵繭鏇範齋淵艱膚鬱) = 鏇壓鏇願鬱願醖糧壓鬱廠窪網觸廠夢鹹願蓋衊 (繭淵窪壓鏇淵觸廠餘淵 )