预约演示

更新于：2025-09-06

Gabapentin

加巴喷丁

更新于：2025-09-06

概要

基本信息

简介Gabapentin 是辉瑞公司开发的一种小分子药物，可作为 CACNA2D2 和 Cav2.2 阻断剂发挥作用。该药物已被批准用于治疗各种疾病，包括焦虑、咳嗽、糖尿病性神经病变、癫痫、纤维肌痛、不宁腿综合征和癫痫发作。加巴喷丁的作用机制包括阻断钙离子流入神经元，从而降低其兴奋性，缓解疼痛和抽搐等症状。自 1993 年首次获得批准以来，加巴喷丁已成为治疗这些疾病的广泛处方药。但需要注意的是，加巴喷丁可能会引起某些副作用，如嗜睡、头晕、协调困难等。因此，其使用必须由医疗保健提供者密切监测，患者应遵循规定的剂量和使用指南。

药物类型

小分子化药

别名

1-(Aminomethyl)cyclohexaneacetic acid、Gabapentin (JAN/USP/INN)、CI-945

+ [16]

靶点

CACNA2D1 x CACNA2D2

作用方式

阻滞剂

作用机制

CACNA2D1阻滞剂(电压门控性钙通道α2/δ亚基-1阻滞剂)、CACNA2D2阻滞剂(电压门控性钙通道α2/δ亚基-2阻滞剂)

治疗领域

免疫系统疾病神经系统疾病内分泌与代谢疾病+ [3]

在研适应症

周围神经痛疱疹后神经痛焦虑症+ [7]

非在研适应症

肌萎缩侧索硬化腕管综合征消化不良+ [7]

原研机构

Pfizer Inc.

在研机构

Viatris Pharma GmbH

Pfizer Inc.Viatris Specialty LLC

+ [3]

非在研机构

Assertio Therapeutics, Inc.

Viatris, Inc.Gebr. Gödecke Beteiligungs- und Verwaltungsgesellschaft mbH

+ [1]

权益机构

Fuji Pharma Co., Ltd.

深圳市海普瑞药业集团股份有限公司

美时化学制药股份有限公司

+ [7]

最高研发阶段批准上市

首次获批日期

美国 (1993-12-30),

焦虑症咳嗽糖尿病性神经病变+ [5]

最高研发阶段(中国)撤市

特殊审评孤儿药 (美国)

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结构/序列

分子式C9H17NO2

InChIKeyUGJMXCAKCUNAIE-UHFFFAOYSA-N

CAS号60142-96-3

关联

694

项与加巴喷丁相关的临床试验

NCT07158476

/ Enrolling by invitation临床4期IIT

Efficacy of Methylprednisolone for Pain Control After ACL Repair: A Randomized Controlled Trial

Opioids are commonly used after orthopedic surgery for pain control but have been shown to increase complications, surgeries, readmissions, and risk for opioid use disorder. The purpose of this study is to investigate the impact of adding a methylprednisolone taper to the pain regimen after ACL repair surgery to determine if this results in decreased postoperative pain and opioid use without increasing complications.

开始日期2025-09-01

申办/合作机构

St. Louis University

NCT07047040

/ Not yet recruiting临床2/3期IIT

Analgesic Efficacy of Pre-operative Dose of Ketorolac And Gabapentin in Patients Undergoing Unilateral Total Knee Arthroplasty A Randomized Double Blinded Controlled Trial

Evaluation of the analgesic efficacy of a pre-operative dose of ketorolac and gabapentin in reducing post-operative pain scores in patients undergoing TKA

开始日期2025-08-15

申办/合作机构

Assiut University

NCT07131527

/ RecruitingN/AIIT

Comparative Study Between the Efficacy of Pre- Operative Oral Gabapentin Versus Diclofenac Sodium in Post-operative Analgesia in Adult Undergoing Laparoscopic Cholecystectomy

this study amis to compare between perioperative oral Gabapentin versus Diclofenac sodium on postoperative analgesia patients undergoing laparoscopic cholecystectomy

开始日期2025-07-14

申办/合作机构

Sohag University

100 项与加巴喷丁相关的临床结果

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100 项与加巴喷丁相关的转化医学

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100 项与加巴喷丁相关的专利（医药）

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10,873

项与加巴喷丁相关的文献（医药）

2026-03-01·Medical Gas Research

Effects of pulsed radiofrequency combined with ozone on zoster-associated pain: a systematic review and meta-analysis

Review

作者: Shen, Qiu-Song ; Kan, Hou-Ming ; Ding, Xiao-Tong ; Huang, Jin-Zhao ; Wang, Rui-Yu

Pulsed radiofrequency combined with ozone therapy has been a newly proposed treatment method for zoster-associated pain in recent years. To explore the effectiveness of a regimen of pulsed radiofrequency combined with ozone for the treatment of zoster-associated pain. We searched commonly used English databases (the Cochrane Library, PubMed, CINAHL, Embase, and Web of Science) and Chinese databases (the CNKI, WanFang, CBM, and VIP databases) for randomized controlled trials. Two researchers independently screened the literature on the basis of the set conditions and extracted data from the included literature. The meta-analysis was conducted via Review Manager 5.4 software. A meta-analysis was conducted on 18 studies, with a total of 1496 participants (742 in the experimental group and 754 in the control group). The results revealed that the pulsed radiofrequency combined with ozone presented lower unidimensional pain scores (standardized mean difference [SMD] = −1.55, 95% confidence interval [CI] = [−2.04, −1.06]; heterogeneity: P < 0.00001, I2 = 94%; test effect: Z = 6.18, P < 0.00001), a lower pain rating index (mean difference [MD] = −2.65, 95% CI = [−3.86, −1.44]; heterogeneity: P = 0.001, I2 = 85%; test effect: Z = 4.29, P < 0.0001) and presented pain intensity scores (MD = −0.58, 95% CI = [−0.62, −0.54]; heterogeneity: P = 0.61, I2 = 0%; test effect: Z = 27.91, P < 0.00001), a lower Pittsburgh sleep quality index (MD = −1.62, 95% CI = [−2.94, −0.31]; heterogeneity: P < 0.00001, I2 = 93%; test effect: Z = 2.42, P = 0.02), and lower interleukin-6 expression levels (SMD = −1.94, 95% CI = [−2.91, −0.97]; heterogeneity: P < 0.00001, I2 = 93%; test effect: Z = 3.92, P < 0.0001), lower gabapentin consumption (MD = −146.92, 95% CI = [−189.93, −103.91]; heterogeneity: P = 0.23, I2 = 30%; test effect: Z = 6.70, P < 0.00001). Pulsed radiofrequency combined with ozone is an effective treatment for zoster-associated pain that can effectively alleviate patients’ pain and improve sleep quality, providing a new treatment option for zoster-associated pain in the future.

2025-12-31·Future Science OA

Evaluating cytidine, uridine, and gabapentin combinations for pain modulation and p-CREB expression in neuropathic model

Article

作者: Alzaghari, Lujain F. ; Qnais, Esam Y. ; Al-Najjar, Mohammad A. A. ; Barakat, Muna ; Chellappan, Dinesh Kumar ; Alqudah, Abdelrahim ; Athamneh, Rabaa Y.

AIMS:

To evaluate the analgesic and neuroprotective effects of cytidine, uridine, and gabapentin-administered alone and in combination-in models of diabetic neuropathy and formalin-induced acute and inflammatory pain.

MATERIALS & METHODS:

Oral doses of cytidine, uridine, and gabapentin (100 mg/kg each) were administered to rats with streptozotocin-induced diabetic neuropathy and in a formalin test model. Behavioral responses were recorded at 30, 60, and 120 minutes following treatment after five weeks of diabetes induction. Spinal cord p-CREB expression was measured to assess molecular changes, and pretreatments with naloxone, yohimbine, and methysergide were employed to explore opioid, adrenergic, and serotonergic contributions.

RESULTS:

All treatments significantly reduced formalin-induced pain in both acute and inflammatory phases (p < 0.05; p < 0.001) and increased mechanical pain thresholds in the diabetic neuropathy model at all-time points (p < 0.05). Combination therapy proved more effective than gabapentin alone (p < 0.05) and was associated with decreased spinal p-CREB levels, indicating altered anti-nociceptive signaling.

CONCLUSIONS:

The combined use of cytidine, uridine, and gabapentin enhances analgesia and neuroprotection compared to monotherapy, supporting its potential as a novel, analgesic-free treatment strategy for diabetic neuropathy.

2025-12-01·Acta Epileptologica

Psychiatric disorders with antiseizure medications in children: an analysis of the FDA adverse event reporting system database

Article

作者: Jiang, Li ; Meng, Linxue ; Wang, Lingman ; Gui, Jianxiong ; Zhang, Xiaofang ; Ma, Jiannan

Abstract:

Background:

Epilepsy is a chronic neurological disorder marked by a persistent tendency to generate seizures, leading to substantial cognitive, behavioral, and psychosocial consequences. This study investigated psychiatric disorder-related adverse events (AEs) associated with antiseizure medications (ASMs) in children using the Food and Drug Administration Adverse Event Reporting System (FAERS) database.

Methods:

This study conducted a comprehensive analysis of FAERS data from 2004 to 2024, focusing on psychiatric AEs in children with epilepsy or seizures treated with ASMs. Signal values were computed using reporting odds ratio (ROR), proportional reporting ratio (PRR), Bayesian Confidence Propagation Neural Network (BCPNN), and Multi-item Gamma Poisson Shrinker (MGPS).

Results:

A total of 2539 preferred terms (PTs) were included, involving 25 system organ classifications (SOCs). Nervous system, skin and subcutaneous tissue, and psychiatric disorders are the three most common SOCs for ASMs in children. There were 24 ASMs, whose AEs involved psychiatric disorders, totaling 110 PTs and 214 drug-PT relationships. Psychotic symptoms (notably lorazepam and topiramate, n = 116 and 109), substance dependence and abuse (notably pregabalin and clonazepam, n = 291 and 110), and the other neuropsychiatric symptoms (notably levetiracetam and valproic acid, n = 70 and 62) were the common types of psychiatric disorder-related AEs of ASMs in children. A total of nine ASMs (brivaracetam, clonazepam, diazepam, eslicarbazepine, gabapentin, lamotrigine, lorazepam, perampanel, and tiagabine) were associated with suicidal and self-injurious behavior in children.

Conclusions:

This study highlights psychiatric AEs of ASMs in children, offering critical insights to improve clinical medication practices and enhance treatment safety. Further research with broader clinical data is needed to promote safe and rational medication use.

138

项与加巴喷丁相关的新闻（医药）

2025-08-12

·GlobeNewswire-Health Care

Grace Therapeutics Announces First Quarter 2026 Financial Results, Provides Business Update

Submission of New Drug Application (NDA) to U.S. Food and Drug Administration (FDA) for GTx-104 Seeking Approval of GTx-104 in the Treatment of Patients with aneurysmal Subarachnoid Hemorrhage (aSAH) NDA Supported by Data from Phase 3 STRIVE-ON Safety Trial, which Met Primary Endpoint and Provided Evidence of Clinical Benefit Compared to Orally Administered Nimodipine PRINCETON, N.J., Aug. 12, 2025 (GLOBE NEWSWIRE) -- Grace Therapeutics, Inc. (Nasdaq: GRCE) (Grace Therapeutics or the Company), a late-stage, biopharma company advancing GTx-104, a clinical-stage, novel, injectable formulation of nimodipine being developed for IV infusion to address significant unmet medical needs in aSAH patients, today announced the financial results and business highlights for the quarter ended June 30, 2025. “During our first quarter of 2026 we continued to execute on our clinical and corporate goals, led by the submission of our NDA to the FDA for GTx-104 for the treatment of aSAH,” said Prashant Kohli, CEO of Grace Therapeutics. “Our NDA for GTx-104 was a significant milestone for the Company and built on more than a decade of painstaking research and innovation. Our NDA is supported by a robust data package including positive results from our STRIVE-ON trial, which provided evidence of improved clinical outcomes in aSAH patients treated with GTx-104 as well as potential medical and pharmacoeconomic benefits of GTx-104 in the treatment of aSAH. The standard of care for aSAH has not seen meaningful innovation in nearly 40 years, and we believe the STRIVE-ON trial results point to a very promising role for GTx-104 as a potential breakthrough for the care of aSAH patients. We are hopeful the FDA will accept our NDA for formal review, and look forward to continued engagement with the FDA during the review process.” First Quarter 2026 Corporate Highlights Submission to the FDA of the Company’s NDA for GTx-104. The application included a comprehensive data package, including positive data obtained from the Company’s Phase 3 STRIVE-ON safety trial of GTx-104, whereby it met its primary endpoint and provided evidence of clinical benefit when compared to orally administered nimodipine. Submission of the NDA has the potential to trigger the exercise of up to $7.6 million in warrants issued as part of a private placement the Company completed in September 2023. Under the terms of the September 2023 private placement, each warrant is exercisable for one share of common stock at an exercise price of $3.003 per share. These warrants are immediately exercisable and will expire on the earlier of (i) the 60th day after the date of the acceptance by the FDA of an NDA for the Company's product candidate GTx-104 or (ii) September 25, 2028. The FDA typically has a 60-day period to determine if the Company’s NDA is complete and acceptable for filing. Grace has obtained Orphan Drug Designation from the FDA for GTx-104, which generally provides seven years of marketing exclusivity in United States upon FDA approval of the NDA. Additionally, the Company believes that its U.S. and international patent estate will provide additional marketing exclusivity for GTx-104. First Quarter 2026 Financial Results The Company reported a net loss of $3.4 million, or $0.21 per share, for the three months ended June 30, 2025, an increase of $0.8 million from the net loss of $2.6 million, or $0.24 per share, for the three months ended June 30, 2024. The increase in net loss was primarily due to a $1.9 million difference in the change in fair value of derivative warrant liabilities and a $0.7 million decrease in income tax benefit, partially offset by a $1.8 million decrease in research and development expenses and a $0.1 million decrease in general and administrative expenses. Total research and development expenses were approximately $0.9 million for the three months ended June 30, 2025, compared to $2.7 million for the three months ended June 30, 2024. The decrease of approximately $1.8 million was primarily due to a $1.9 million decrease in research activities mainly due to completion of our GTx-104 pivotal Phase 3 STRIVE-ON safety clinical trial, offset in part by a $0.1 million increase in professional fees in connection with the preparation and submission of our NDA to the FDA. General and administrative expenses were approximately $2.1 million for the three months ended June 30, 2025, a decrease of $0.1 million from $2.2 million for the three months ended June 30, 2024. The decrease was primarily a result of decreased legal, accounting, tax, audit and other professional fees related to the continuance and domestication completed in October 2024, offset in part by an increase in salaries and benefits due to merit increases, increases in other general and administrative expenses primarily due to costs for GTx-104 commercial assessment, and an increase in stock-based compensation due to the issuance of new stock option awards. Cash Runway As of June 30, 2025, cash and cash equivalents were $20.0 million, a net decrease of approximately $2.1 million compared to cash and cash equivalents of $22.1 million at March 31, 2025. The private placement the Company completed in February 2025 included common warrants exercisable for shares of common stock (or pre-funded warrants in lieu thereof) at an exercise price of $3.395 per share. Each common warrant is immediately exercisable and will expire on the earlier of (i) the 60th day after the date the FDA approves the NDA for GTx-104 and (ii) September 25, 2028. Potential gross proceeds from the exercise of the February 2025 common warrants are $15.0 million. The private placement the Company completed in September 2023 included common warrants exercisable for shares of common stock at an exercise price of $3.003 per share. Each common warrant is immediately exercisable and will expire on the earlier of (i) the 60th day after the date of the acceptance by the FDA of the NDA for GTX-104 or (ii) five years from the date of issuance. Potential gross proceeds from the exercise of the September 2023 common warrants are $7.6 million. While the Company believes that current cash and cash equivalents provide cash runway through at least the next twelve months, the runway could extend into the second quarter of calendar 2027 if all of the common warrants issued in connection with the Company’s February 2025 and September 2023 private placements are exercised at the election of the investors. About the STRIVE-ON Trial The STRIVE-ON trial (NCT05995405) was a prospective, randomized open-label trial of GTx-104 compared with oral nimodipine in patients hospitalized with aSAH. 50 patients were administered GTx-104 and 52 patients received oral nimodipine. The primary endpoint was the number of patients with at least one episode of clinically significant hypotension reasonably considered to be caused by the drug, and additional secondary endpoints included safety, clinical, and pharmacoeconomic outcomes. The trial met its primary endpoint, with patients receiving GTx-104 observed to have a 19% reduction in at least one incidence of clinically significant hypotension compared to oral nimodipine (28% versus 35%). Other measures also favored or were comparable to GTx-104, including: 54% patients had relative dose intensity (RDI) of 95% or higher compared to only 8% on oral nimodipine, and 29% more patients had favorable functional outcomes at 90 days. In addition, there were fewer intensive care unit (ICU) readmissions, ICU days, and ventilator days for patients receiving GTx-104 versus oral nimodipine. Adverse events were comparable between the two arms and no new safety issues were identified with patients receiving GTx-104. All deaths in both arms of the trial were due to severity of the patient’s underlying disease. There were eight deaths on the GTx-104 arm compared to four deaths on the oral nimodipine arm. The survival status of one patient on the oral nimodipine arm was unknown. No deaths were determined to be related to GTx-104 or oral nimodipine. About aneurysmal Subarachnoid Hemorrhage (aSAH) aSAH is bleeding over the surface of the brain in the subarachnoid space between the brain and the skull, which contains blood vessels that supply the brain. A primary cause of such bleeding is the rupture of an aneurysm in the brain. The result is aSAH, a relatively uncommon type of stroke that accounts for about 5% of all strokes and an estimated 42,500 U.S. hospital treated patients. About the Grace Therapeutics Asset Portfolio GTx-104 is a clinical stage, novel, injectable formulation of nimodipine being developed for IV infusion in aSAH patients to address significant unmet medical needs. The unique nanoparticle technology of GTx-104 facilitates aqueous formulation of insoluble nimodipine for a standard peripheral IV infusion. GTx-104 provides a convenient IV delivery of nimodipine in the Intensive Care Unit potentially eliminating the need for nasogastric tube administration in unconscious or dysphagic patients. Intravenous delivery of GTx-104 also has the potential to lower food effects, drug-to-drug interactions, and eliminate potential dosing errors. Further, GTx-104 has the potential to better manage hypotension in aSAH patients. GTx-104 has been administered in over 200 patients and healthy volunteers and was well tolerated with significantly lower inter- and intra-subject pharmacokinetic variability compared to oral nimodipine. GTx-102 is a novel, concentrated oral-mucosal spray of betamethasone intended to improve neurological symptoms of Ataxia-Telangiectasia (A-T), for which there are currently no FDA-approved therapies. GTx-102 is a stable, concentrated oral spray formulation comprised of the gluco-corticosteroid betamethasone that, together with other excipients can be sprayed conveniently over the tongue of the A-T patient and is rapidly absorbed. The Company received written responses to its End of Phase 1 meeting in GTx-102 where the FDA made recommendations on the path toward an NDA. The FDA provided guidance on the design of a single pivotal efficacy and safety trial, including the neurological assessment scale for the primary endpoint, that could, with appropriate confirmatory evidence, support an NDA. The further development of GTx-102 has been deprioritized in favor of focusing on development of GTx-104. It is also possible that the Company may license or sell GTx-102. GTx-101 is a non-narcotic, topical bio-adhesive film-forming bupivacaine spray designed to ease the symptoms of patients suffering with postherpetic neuralgia (PHN). GTx-101 is administered via a metered-dose of bupivacaine spray and forms a thin bio-adhesive topical film on the surface of the patient’s skin, which enables a touch-free, non-greasy application. It also comes in convenient, portable 30 ml plastic bottles. Unlike oral gabapentin and lidocaine patches, which are used for the treatment of PHN, the Company believes that the biphasic delivery mechanism of GTx-101 has the potential for rapid onset of action and continuous pain relief for up to eight hours. No skin sensitivity was reported in a Phase 1 trial. The further development of GTx-101 has been deprioritized in favor of focusing on development of GTx-104. It is also possible that the Company may license or sell GTx-101. About Grace Therapeutics Grace Therapeutics, Inc. (Grace Therapeutics or the Company) is a late-stage biopharma company with drug candidates addressing rare and orphan diseases. Grace Therapeutics’ novel drug delivery technologies have the potential to improve the performance of currently marketed drugs by achieving faster onset of action, enhanced efficacy, reduced side effects, and more convenient drug delivery. Grace Therapeutic’s lead clinical assets have each been granted Orphan Drug Designation by the FDA, which provides seven years of marketing exclusivity post-launch in the United States, and additional intellectual property protection with over 40 granted and pending patents. Grace Therapeutics’ lead clinical asset, GTx-104, is an IV infusion targeting aneurysmal Subarachnoid Hemorrhage (aSAH), a rare and life-threatening medical emergency in which bleeding occurs over the surface of the brain in the subarachnoid space between the brain and skull. For more information, please visit: www.gracetx.com. Forward-Looking Statements Statements in this press release that are not statements of historical or current fact constitute "forward-looking statements" within the meaning of the U.S. Private Securities Litigation Reform Act of 1995, as amended, Section 27A of the Securities Act of 1933, as amended, and Section 21E of the Securities Exchange Act of 1934, as amended, and "forward-looking information" within the meaning of Canadian securities laws (collectively, "forward-looking statements"). Such forward-looking statements involve known and unknown risks, uncertainties, and other factors that could cause the actual results of Grace Therapeutics to be materially different from historical results or from any future results expressed or implied by such forward-looking statements. In addition to statements which explicitly describe such risks and uncertainties, readers are urged to consider statements containing the terms "believes," "belief," "expects," "intends," "anticipates," "estimates," "potential," "should," "may," "will," "plans," "continue," "targeted" or other similar expressions to be uncertain and forward-looking. Readers are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date of this press release. The forward-looking statements in this press release, including statements regarding, the Company’s cash runway, the future prospects of the Company’s GTx-104 drug candidate, the timing and outcome of the Company’s NDA submission for GTx-104, the Company’s belief that the data and regulatory packages as currently structured will be sufficient for submission of such NDA, GTx-104’s potential to bring enhanced treatment options to patients suffering from aSAH, GTx-104’s potential to be administered to improve the management of hypotension in patients with aSAH, the ability of GTx-104 to achieve a pharmacokinetic and safety profile similar to the oral form of nimodipine, GTx-104’s potential to achieve medical and pharmacoeconomic benefit, GTx-104’s commercial prospects, the future prospects of the Company’s GTx-102 drug candidate, GTx-102’s potential to provide clinical benefits to decrease symptoms associated with A-T, the timing and outcomes of a Phase 3 efficacy and safety trial for GTx-102, the timing of an NDA filing for GTx-102, the future prospects of the Company’s GTX-101 drug candidate, GTX-101’s potential to be administered to PHN patients to treat the severe nerve pain associated with the disease and any future patent and other intellectual property filings made by the Company for new developments are based upon Grace Therapeutics’ current expectations and involve assumptions that may never materialize or may prove to be incorrect. Actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of various risks and uncertainties, including, without limitation: (i) the success and timing of regulatory submissions of the Phase 3 STRIVE-ON safety trial for GTx-104; (ii) regulatory requirements or developments and the outcome of the Company’s NDA application for GTx-104; (iii) changes to regulatory pathways; and (iv) legislative, regulatory, political and economic developments. The foregoing list of important factors that could cause actual events to differ from expectations should not be construed as exhaustive and should be read in conjunction with statements that are included herein and elsewhere, including the risk factors detailed in the "Special Note Regarding Forward-Looking Statements," "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" sections of the Company's Annual Report on Form 10-K for the fiscal year ended March 31, 2025, the Company’s Quarterly Report on Form 10-Q for the quarterly period ended June 30, 2025 to be filed with the Securities and Exchange Commission (“SEC”) and other documents that have been and will be filed by Grace Therapeutics from time to time with the SEC and Canadian securities regulators. All forward-looking statements contained in this press release speak only as of the date on which they were made. Grace Therapeutics undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made, except as required by applicable securities laws. For more information, please contact: Grace Therapeutics Contact: Prashant KohliChief Executive OfficerTel: 609-322-1602Email: info@gracetx.comwww.gracetx.com Investor Relations: LifeSci AdvisorsMike MoyerManaging DirectorPhone: 617-308-4306Email: mmoyer@lifesciadvisors.com ---tables to follow--- GRACE THERAPEUTICS, INC.Condensed Consolidated Balance Sheets(Unaudited) June 30,2025 March 31, 2025 (Expressed in thousands except share data) $ $ Assets Current assets: Cash and cash equivalents 20,005 22,133 Receivables 20 126 Prepaid expenses 500 453 Total current assets 20,525 22,712 Equipment, net 14 15 Intangible assets 41,128 41,128 Goodwill 8,138 8,138 Total assets 69,805 71,993 Liabilities and Stockholders’ equity Current liabilities: Trade and other payables 2,315 1,930 Total current liabilities 2,315 1,930 Derivative warrant liabilities 1,628 1,141 Deferred tax liability 2,312 2,312 Total liabilities 6,255 5,383 Commitments and contingencies Stockholders’ equity: Preferred stock, $0.0001 par value per share; 10,000,000 authorized; none issued and outstanding as of June 30, 2025 and March 31, 2025 — — Common stock, $0.0001 par value per share; 100,000,000 authorized; 13,828,562 and 13,718,106 shares issued and outstanding as of June 30, 2025 and March 31, 2025, respectively 1 1 Additional paid-in capital 293,636 293,334 Accumulated other comprehensive loss (6,038) (6,038)Accumulated deficit (224,049) (220,687)Total stockholders' equity 63,550 66,610 Total liabilities and stockholders’ equity 69,805 71,993 GRACE THERAPEUTICS, INC.Condensed Consolidated Statements of Loss and Comprehensive Loss(Unaudited) Three months ended June 30, 2025 June 30, 2024 (Expressed in thousands, except share and per share data) $ $ Operating expenses Research and development expenses (955) (2,708)General and administrative expenses (2,135) (2,255)Loss from operating activities (3,090) (4,963) Foreign exchange gain (loss) 10 (8)Change in fair value of derivative warrant liabilities (487) 1,395 Interest and other income, net 205 235 Other (expense) income, net (272) 1,622 Loss before income tax benefit (3,362) (3,341) Income tax benefit — 724 Net loss and total comprehensive loss (3,362) (2,617) Basic and diluted loss per share (0.21) (0.24) Weighted-average number of shares outstanding 15,924,522 10,928,543

临床结果申请上市财报孤儿药临床1期

2025-07-21

·药学进展

独家原创|赵雪主治医师：抗精神病药、抗抑郁药与不宁腿综合征

“点击蓝字关注我们赵雪毕业于上海交通大学医学院。上海市精神卫生中心主治医师、上海市精神心理疾病临床医学研究中心秘书。主要研究方向为精神药物遗传药理学。主持上海市精神卫生中心院级课题、上海交通大学“医工交叉”等科研项目多项。作为主要研究人员参与国家自然科学基金、上海市申康医院发展中心“促进市级医院临床技能与临床创新三年行动计划”等多项纵向科研课题。作为研究骨干参与多项国际多中心和国内多中心（牵头）临床试验。以第一（含共一）作者发表多篇中英文学术论文。抗精神病药、抗抑郁药与不宁腿综合征 PPS 郭瑛睿1，钱瑞仪1，禹顺英2，沈一峰3，赵雪3*（1.上海交通大学医学院附属精神卫生中心精神科，上海 200030；2.上海交通大学医学院附属精神卫生中心遗传室，上海 200030；3.上海交通大学医学院附属精神卫生中心临床研究中心，上海 200030）[摘要] 不宁腿综合征（restless legs syndrome,RLS）是抗精神病药和抗抑郁药的常见不良反应之一，影响患者夜间睡眠、加重精神症状、降低患者生活质量，但其在临床实践尚未受到广泛重视。针对抗精神病药和抗抑郁药的 RLS 发生风险，这两类药物导致 RLS 的可能机制及相关治疗手段进行综述，以期为 RLS 的临床治疗提供参考。不宁腿综合征（restless legs syndrome，RLS）又称不安腿综合征，是临床常见的运动感觉性神经系统疾病，主要表现为强烈、迫切想要移动肢体的冲动或欲望，常常伴随着肢体深处不舒服或难以描述的感觉，夜间睡眠或安静时出现或加重，具有昼夜节律性，按摩或活动后缓解，可导致严重睡眠障碍。在《精神障碍诊断与统计手册（第 5 版）》（the fifith edition of the diagnostic and statistical manual of mental disorders，DSM-5）中， RLS属于睡眠-觉醒障碍中异常睡眠的一类疾病。一般人群中RLS的发病率为 3%~19%，女性发病率更高[1]，其中约有2.5%的患者症状严重到需要接受医疗干预[2]。根据病因不同，RLS可分为原发性和继发性2种类型。原发性RLS通常在40岁之前发病，主要与遗传因素有关。继发性RLS伴发于各类躯体疾病，如神经系统疾病、铁缺乏症、慢性肾功能衰竭、糖尿病、自身免疫性疾病、甲状腺疾病、血管疾病、精神疾病等[1, 3-4]。RLS也是精神类药物的不良反应之一。据报道，抗精神病药、抗抑郁药和抗癫痫药是引起RLS最常见的3类药物[1]。早在1999年，1例病案报告指出奥氮平可能导致RLS[5]，此后越来越多的精神类药物被报道能够诱发RLS这一不良反应，不同药物发生RLS的风险有所不同。如上所述，引起RLS的精神类药物主要为抗精神病药及抗抑郁药，故本文主要针对抗精神病药和抗抑郁药引起RLS的发生风险，这两类药物导致RLS的可能机制及相关治疗手段进行综述。1抗精神病药、抗抑郁药与不宁腿综合征 Elrassas等[6]开展的横断面研究结果显示，200名接受抗抑郁药和抗精神病药治疗的患者中，服用第1代抗精神病药（除氟哌啶醇外）的患者发生RLS比例最高（58.7%），其次是选择性5-羟色胺再摄取抑制剂（selective serotonin reuptake inhibitors，SSRIs）类药物（52.6%）和阿立哌唑（46.4%），接受曲唑酮（24.2%）和氟哌啶醇（31%）治疗的患者发生RLS可能性最小。 1.1 抗精神病药与不宁腿综合征有研究结果显示，与对照组（9.3%）相比，接受抗精神病药治疗的精神分裂症患者发生RLS的概率（21.4%）明显更高[7]。在各类抗精神病药中，奥氮平、喹硫平和氯氮平引起RLS的报道最多[1]，利培酮、鲁拉西酮等药物引起RLS的报道相对较少（见表1[5,8-29]）。也有部分研究结果显示，喹硫平和阿立哌唑能够改善其他抗精神病药引起的RLS症状[11,30]，可能是因为相对于多巴胺D2受体，这2种药物对5-羟色胺（5-hydroxytryptamine，5-HT）受体具有更高亲和力。另有研究报道，抗精神病药与抗抑郁药联用，如喹硫平与文拉法辛[31] 或帕罗西汀[18] 联用会导致RLS，停用2种药物中的一种会改善RLS症状。1.2 抗抑郁药与不宁腿综合征在多种抗抑郁药中，SSRIs、5-HT和去甲肾上腺素再摄取抑制剂（ serotonin-norepinephrine reuptake inhibitors，SNRIs）、四环类非典型抗抑郁药米氮平导致RLS的报道较多（见表2[32-46]）。Cetin Erdem 等[47]报道，在198名接受4~8周SSRIs/SNRIs药物治疗的门诊患者中，RLS的发生率为25%。与女性相比，男性使用抗抑郁药后发生RLS的风险增加[48]。Kolla等[49]报道，在各种抗抑郁药中，米氮平可能与较高的RLS发生率有关，也会恶化患者原有的RLS症状[50]，其次是文拉法辛，而安非他酮可能会减轻RLS症状。当联合使用2种或2种以上药物时，如氟西汀与米氮平联用[51]、帕罗西汀与度洛西汀联用[52]、艾司西酞普兰与锂盐或喹硫平联用[53]，患者发生RLS的风险也会相应增加。关于新型抗抑郁药伏硫西汀是否增加RLS风险的研究结果并不一致，有研究发现其可减轻RLS症状[54-55]，但也有研究报道伏硫西汀可诱发RLS[45]。2抗精神病药、抗抑郁药引起不宁腿综合征的可能机制2.1 多巴胺功能紊乱既往神经影像学研究表明，RLS患者脑内存在多巴胺能活性低下表现[56]。RLS包括运动和感觉异常两个维度的症状表现，感觉和运动回路受脊髓投射至大脑的相关区域控制，这些区域与不同神经递质有关，包括背区（5-HT）、丘脑区（去甲肾上腺素）和下丘脑后方的A11区（多巴胺）[57]。多巴胺受体激动剂是治疗RLS的一线药物，多巴胺拮抗剂（如抗精神病药）则会诱发RLS，提示多巴胺活性在RLS中的重要作用。抗精神病药与抗抑郁药增加RLS风险的具体机制目前尚不明确，多巴胺能活性降低被认为可能是抗精神病药诱发RLS的主要原因。阿立哌唑为多巴胺（D2、D3、D4）受体部分激动剂，正电子发射断层显像（positron emission tomography，PET）研究表明在治疗剂量下阿立哌唑受体占有率为95%[58]，阿立哌唑通过激动多巴胺受体改善RLS症状，该效果与罗匹尼罗和普拉克索等多巴胺受体激动剂相似。然而，与其他非典型抗精神病药物（如利培酮）相比，氯氮平和喹硫平的D2受体占有率较低，如果多巴胺功能降低能够诱发RLS，这些药物诱发RLS的可能性应该较小，这与多数研究报道不符。另有研究者认为，喹硫平因其镇静催眠作用，常在夜间使用可改善患者睡眠，而夜间多巴胺受体敏感性较白天增加[59]；另外，喹硫平常被用来与抗抑郁药（如SSRIs、米氮平等）合用改善情感症状，而抗抑郁药能够通过增加5-HT功能减少多巴胺释放 [60]，增加RLS发生风险。此外，有研究表明泌乳素（prolactin，PRL）水平可能在抗精神病药所致 RLS中起重要作用。多巴胺受体激动剂如左旋多巴和卡麦角林能够降低泌乳素水平，这2种药物均可以治疗RLS[61]。抗精神病药（如利培酮、奥氮平）能够增加PRL水平[62]，可能是引起RLS症状的间接原因。阿立哌唑可以降低抗精神病药引起的高泌乳素血症[63]，可能是阿立哌唑能够缓解RLS症状的另一原因 [23]。2.2 铁缺乏有研究发现，RLS患者脑脊液中铁蛋白含量减少[64] 及转铁蛋白含量升高；脑影像学研究也发现，RLS患者大脑中铁含量减少[65]；RLS患者尸检脑神经胶质细胞中铁含量较低[66]。外周铁水平正常的RLS患者补充铁剂也能改善RLS症状，可能是因为血脑屏障使大脑中铁水平独立于外周铁水平[67]。此外，脑内铁水平降低也会导致多巴胺代谢和D2受体状态改变，尤其是在黑质和壳核区域[9]。目前有研究发现，抗精神病药能够影响体内铁稳态[68]和肝脏铁代谢[69]，引起低铁血症。目前仍缺乏直接证据表明使用抗精神病或抗抑郁药出现RLS的患者是否存在外周或中枢铁代谢异常，仍需更多研究证据来明确这一可能机制。 2.3 遗传因素遗传因素是RLS的重要致病因素，大部分家族性RLS呈常染色体显性遗传，少数家族则呈常染色体隐性遗传或非孟德尔遗传模式[70]。既往遗传学研究多集中于原发性 RLS，全基因组关联研究发现位于不同染色体的 RLS 风险基因，包括BTBD9基因（位于染色体6p21）、MEIS1基因（位于染色体2p14）、PTPRD 基因（位于染色体9p24.1-p23）、MAP2K5/SKOR1 基因（位于染色体15q23）和TOX3/BC034767 基因（位于染色体 16q12.1）[71]。近期有研究发现7个全新的RLS易感基因位点：RLS1（位于染色体12q12-q21）、RLS2（位于染色体 14q13-q21）、RLS3（位于染色体 9p24-p22）、RLS4（位于染色体 2q33）、RLS5（位于染色体20p13）、RLS6（位于染色体 19p13）及RLS7（位于染色体16p12.1）[72-73]。截至目前，抗精神病药或抗抑郁药所致RLS的遗传学研究仍较少。有研究发现，MAOA基因VNTR与MAOB基因A644g多态的单倍型频率与抗精神病药引起RLS严重程度有关[74]。另一项研究显示，MAP2K5基因多态性增加了抗精神病药物诱发RLS的风险[75]。3抗精神病药、抗抑郁药引起不宁腿综合征的治疗RLS的治疗分为非药物治疗和药物治疗。非药物治疗包括：消除或减少继发性因素的影响，如尽量避免使用能够诱发或加重RLS的药物（如多巴胺受体拮抗剂、抗抑郁药、抗组胺药等）；保持良好的睡眠卫生习惯；加强体育锻炼；结合物理治疗（如重复经颅磁刺激、重复经颅电刺激）等。药物治疗包括：多巴胺激动剂（如罗匹尼罗、罗替戈汀、普拉克索），α2δ钙通道配体类药物（如普瑞巴林、加巴喷汀-恩那卡比、加巴喷汀），这些药物均为治疗RLS的一线用药 [76]，也可使用苯二氮䓬类镇静药[77] 和抗癫痫药[78] 等。治疗抗精神病药或抗抑郁药引起的RLS具有一定挑战性，目前仍缺乏高水平临床研究或相关指南指导医生用药。在既往相关病例报道中，临床医生一般采取减量或停用现用药物，加用多巴胺受体激动剂或α2δ钙通道配体类药物（具体病例处理方式可参考表1和表2），上述策略均能够有效改善患者RLS症状。值得注意的是，多巴胺受体激动剂和α2δ钙通道配体类药物可能会导致患者精神症状波动或病情复发。在既往病案报道中，加用小剂量阿立哌唑也是改善 RLS症状的常用手段，阿立哌唑剂量为1~10 mg·d-1[23,30]，在临床实践中医生可根据患者具体情况探索使用阿立哌唑的剂量。铁缺乏是RLS病理生理学中重要假说之一。在患者出现RLS症状后，医生可以通过相关检测指标（包括铁蛋白、转铁蛋白、血清铁、总铁结合力、转铁蛋白饱和度等）评估患者外周铁储存情况。如果患者确实存在缺铁表现，可采用铁替代疗法，如口服硫酸亚铁，若患者不能耐受或有效吸收口服铁剂，也可考虑静脉补铁，同时补充维生素C有助于促进消化道对铁的吸收[76]。在补充铁剂后，需动态观察患者RLS症状改善和评估外周铁相关指标变化。4结语精神障碍患者常合并睡眠障碍，而RLS会进一步加重患者睡眠问题，同时伴有强烈心理不适感。此外，RLS能够增加肥胖、抑郁症、焦虑症、高血压及其他心血管疾病的发生风险，显著降低患者生活质量、延缓患者康复[79]。Cetin Erdem等[47]的研究显示，服用抗抑郁药发生RLS的患者生活质量显著下降。一项回顾性队列研究发现，自杀和自残风险与RLS呈正相关[80]。尽管在临床实践中，使用抗精神病药或抗抑郁药后出现RLS的病例并不少见，但与其他药物不良反应（如心血管不良反应、代谢综合征等）相比，RLS仍未得到有效识别和广泛重视。尤其在患者用药后出现新发睡眠问题时，不能简单地归结为疾病症状的一部分，应仔细识别是否存在RLS的可能性。目前关于精神类药物引起RLS的各方面研究仍较少，后续需要更多关注和探索，从而更好地为患者及临床服务。参考文献：[1]Patatanian E, Claborn M K. 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Is there any association between antidepressants and restless legs syndrome in a large Turkish population receiving mono or combined treatment? A cross-sectional comparative study[J]. Psychiatry Clin Psychopharmacol, 2019, 29(4): 565-569.[49] Kolla B P, Mansukhani M P, Bostwick J M. The influence of antidepressants on restless legs syndrome and periodic limb movements: a systematic review[J]. Sleep Med Rev, 2018, 38: 131- 140.[50] Teive H A G, de Quadros A, Barros F C, et al. Worsening of autosomal dominant restless legs syndrome after use of mirtazapine: case report[J]. Arq Neuropsiquiatr, 2002, 60(4): 1025-1029.[51] Prospero-Garcia K A, Torres-Ruiz A, Ramirez-Bermudez J, et al. Fluoxetine-mirtazapine interaction may induce restless legs syndrome: report of 3 cases from a clinical trial[J]. J Clin Psychiatry, 2006, 67(11): 1820.[52] Nikolaou K N, Michopoulos I, Douzenis A, et al. Restless legs syndrome associated with the combined use of duloxetine plus paroxetine[J]. 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Mechanism of new antipsychotic medications: occupancy is not just antagonism[J]. Arch Gen Psychiatry, 2003, 60(10): 974-977.[59] Garcia-Borreguero D, Larrosa O, Granizo J J, et al. Circadian variation in neuroendocrine response to L-dopa in patients with restless legs syndrome[J]. Sleep, 2004, 27(4): 669-673.[60] Zhou F M, Liang Y, Salas R, et al. Corelease of dopamine and serotonin from striatal dopamine terminals[J]. Neuron, 2005, 46(1): 65-74.[61] Trenkwalder C, Benes H, Grote L, et al. Cabergoline compared to levodopa in the treatment of patients with severe restless legs syndrome: results from a multi-center, randomized, active controlled trial[J]. Mov Disord, 2007, 22(5): 696-703.[62] Koch M T, Carlson H E, Kazimi M M, et al. Antipsychotic-related prolactin levels and sexual dysfunction in mentally ill youth: a 3-month cohort study[J]. J Am Acad Child Adolesc Psychiatry, 2023, 62(9): 1021-1050.[63] Jiang Q, Li T, Zhao L, et al. Treatment of antipsychotic-induced hyperprolactinemia: an umbrella review of systematic reviews and meta-analyses[J]. Front Psychiatry, 2024, 15: 1337274.[64] Clardy S L, Earley C J, Allen R P, et al. Ferritin subunits in CSF are decreased in restless legs syndrome[J]. J Lab Clin Med, 2006, 147(2): 67-73.[65] Allen R P, Barker P B, Wehrl F W, et al. MRI measurement of brain iron in patients with restless legs syndrome[J]. Neurology, 2001, 56(2): 263-265.[66] Connor J R, Boyer P J, Menzies S L, et al. Neuropathological examination suggests impaired brain iron acquisition in restless legs syndrome[J]. Neurology, 2003, 61(3): 304-309.[67] Yu P, Chang Y Z. Brain iron metabolism and regulation[J]. Adv Exp Med Biol, 2019, 1173: 33-44.[68] Schoretsanitis G, Nikolakopoulou A, Guinart D, et al. Iron homeostasis alterations and risk for akathisia in patients treated with antipsychotics: a systematic review and meta-analysis of crosssectional studies[J].Eur Neuropsychopharmacol, 2020, 35: 1-11.[69] May M, Barlow D, Ibrahim R, et al. Mechanisms underlying antipsychotic-induced NAFLD and iron dysregulation: a multi-omic approach[J]. Biomedicines, 2022, 10(6): 1225.[70] Jiménez-Jiménez F J, Alonso-Navarro H, García-Martín E, et al.Genetics of restless legs syndrome: an update[J]. Sleep Med Rev, 2018, 39: 108-121.[71] Akçimen F, Sarayloo F, Liao C, et al. Transcriptome-wide association study for restless legs syndrome identifies new susceptibility genes[J]. Commun Biol, 2020, 3(1): 373.[72] Estiar M A, Senkevich K, Yu E, et al. Lack of causal effects or genetic correlation between restless legs syndrome and Parkinson’s disease[J]. Mov Disord, 2021, 36(8): 1967-1972.[73] Lin W S. The conundrum of the origin of restless legs syndrome[J].Sleep, 2022, 45(5): zsac018.[74] Kang S G, Park Y M, Choi J E, et al. Association study between antipsychotic-induced restless legs syndrome and polymorphisms of monoamine oxidase genes in schizophrenia[J]. Human Psychopharmacology, 2010, 25(5): 397-403.[75] Kang S G, Lee Y J, Park Y M, et al. Haplotype association of the MAP2K5 gene with antipsychotics-induced symptoms of restless legs syndrome among patients with schizophrenia[J]. Psychiatry Investig, 2018, 15(1): 84-89.[76] Liu Z, Guan R, Pan L. Exploration of restless legs syndrome under the new concept: a review[J]. Medicine (Baltimore), 2022, 101(50): e32324.[77] Walters A S, Spruyt K, Ba D M, et al. A historical overview of the role of benzodiazepines including clonazepam in the treatment of adult restless legs syndrome and periodic limb movements in sleep[J]. Tremor Other Hyperkinet Mov (N Y), 2024, 14: 21.[78] Al-Kassmy J, Alsalmi M, Kang W, et al. Anticonvulsant agents for treatment of restless legs syndrome: a case report with lamotrigine and a review of the literature[J]. Neurologist, 2024, 29(3): 173- 178.[79] Shen Y, Liu H, Dai T, et al. Association between restless legs syndrome and hypertension: a meta-analysis of nine population-based studies[J]. Neurol Sci, 2018, 39(2): 235-242.[80] Zhuang S, Na M, Winkelman J W, et al. Association of restless legs syndrome with risk of suicide and self-harm[J]. JAMA Netw Open, 2019, 2(8): e199966.美编排版：覃冰冰感谢您阅读《药学进展》微信平台原创好文，也欢迎各位读者转载、引用。本文选自《药学进展》2025年第 6 期。《药学进展》杂志由教育部主管、中国药科大学主办，中国科技核心期刊（中国科技论文统计源期刊）。刊物以反映药学科研领域的新方法、新成果、新进展、新趋势为宗旨，以综述、评述、行业发展报告为特色，以药学学科进展、技术进展、新药研发各环节技术信息为重点，是一本专注于医药科技前沿与产业动态的专业媒体。《药学进展》注重内容策划、加强组稿约稿、深度挖掘、分析药学信息资源、在药学学科进展、科研思路方法、靶点机制探讨、新药研发报告、临床用药分析、国际医药前沿等方面初具特色；特别是医药信息内容以科学前沿与国家战略需求相合，更加突出前瞻性、权威性、时效性、新颖性、系统性、实战性。根据最新统计数据，刊物篇均下载率连续三年蝉联我国医药期刊榜首，复合影响因子1.216，具有较高的影响力。《药学进展》编委会由国家重大专项化学药总师陈凯先院士担任主编，编委由新药研发技术链政府监管部门、高校科研院所、制药企业、临床医院、CRO、金融资本及知识产权相关机构近两百位极具影响力的专家组成。联系《药学进展》↓↓↓编辑部官网：pps.cpu.edu.cn；邮箱：yxjz@163.com；电话：025-83271227。欢迎投稿、订阅！往期推荐聚焦“兴药为民·2023生物医药创新融合发展大会”“兴药为民·2023生物医药创新融合发展大会”盛大启幕！院士专家齐聚杭城，绘就生物医药前沿赛道新蓝图“兴药强刊”青年学者论坛暨《药学进展》第二届青年编委会议成功召开“兴药为民·2023生物医药创新融合发展大会”路演专场圆满收官！校企合作新旅程已启航我知道你在看哟

临床研究

2025-07-21

·摩熵医药

重磅抗“糖痛”药首仿炸场，三巨头入局，百亿赛道变天！

注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需要得到授权。7月19日，CDE官网显示，海南合瑞制药股份有限公司申报的4类化学仿制药苯磺酸美洛加巴林片的上市申请已获受理。合瑞制药由此正式加入该品种的首仿争夺战。截图来源：CDE官网美洛加巴林（mirogabalin）是第三代钙离子通道调节剂类药物，其适应症为糖尿病性周围神经病理性疼痛（DPNP），主要通过调节钙离子通道，减少钙离子的内流，从而抑制神经元的过度兴奋和神经递质的过度释放。截图来源：摩熵医药全球药物研发数据库苯磺酸美洛加巴林片由日本第一三共公司（Daiichi Sankyo）自主研发并原研上市，2019年首次在日本获批。据摩熵医药数据库显示，自上市以来，苯磺酸美洛加巴林片在全球的销售额持续飙涨，2019-2023年累计销售达1429亿日元（即时汇率换算约10亿美元），2024年全球销售额近4亿美元，同比增长达21.59%。截图来源：摩熵医药全球药物研发数据库2024年6月，苯磺酸美洛加巴林片获批进入中国市场，打破在中国长期以来糖尿病性周围神经病理性疼痛无药可用的治疗困境。同年11月，通过谈判纳入医保目录。据摩熵医药数据，2021年我国糖尿病患病人数已达1.17亿，且呈逐年增长态势。作为糖尿病最常见的慢性并发症，糖尿病周围神经病（DPN）在我国的发病率约为21.8%，其中57.2%会发展为糖尿病性周围神经病理性疼痛（DPNP）。截图来源：摩熵医药流行病学数据库依托我国庞大的糖尿病患病基数与未被满足的治疗需求，苯磺酸美洛加巴林片有望复制同类神经痛药物加巴喷丁的市场表现，成长为亿级规模的重磅品种。截图来源：摩熵医药全国医院销售（全终端）数据库作为应对治疗领域药物匮乏的突破性产品，苯磺酸美洛加巴林片登陆中国市场一年时间便引来国内企业的热切关注，止痛药细分赛道的仿制浪潮已然出现。除合瑞制药外，南京正大天晴、齐鲁制药、苑东生物3家企业申报的苯磺酸美洛加巴林片上市申请也已获受理，目前均处于审评阶段，首仿之争拉开帷幕。截图来源：摩熵医药中国药品审评数据库值得关注的是，南京正大天晴作为该产品国内首家申报仿制上市及开展生物等效性试验的药企，2023年9-11月完成试验后即进入上市申报流程，效率显著。目前，已有7家药企完成BE试验，另有13家正处于进行阶段。截图来源：摩熵医药中国临床试验数据库苯磺酸美洛加巴林核心化合物专利已在国内授权（CN101878193B），保护期至2028年9月。第一三共还在制剂组合物以及固体制剂专利进行了布局，涉及CN104334169B、CN114786653B、CN107405322B等专利。截图来源：摩熵医药全球上市药品专利数据库小结作为第三代钙离子通道调节剂，苯磺酸美洛加巴林片起效迅速、镇痛持久、耐受性良好的优势，能为DPNP患者带来多重获益。如今首仿之争已正式开启，哪家企业将率先突围、与原研企业第一三共一决高下，我们拭目以待。END本文为原创文章，转载请留言获取授权近期热门资源获取中国临床试验趋势与国际多中心临床展望-2025052024年医药企业综合实力排行榜-202505中国带状疱疹疫苗行业分析报告-2025052023H2-2024H1中国药品分析报告-202504数据透视：中药创新药、经典验方、改良型新药、同名同方的申报、获批、销售情况-2025032024年中国1类新药靶点白皮书-202503中国AI医疗健康企业创新发展百强榜单-202502解码护肤抗衰：消费偏好洞察与市场格局分析-2025022024年FDA批准上市的新药分析报告-202501小分子化药白皮书（上）-2025012024年中国医疗健康投融资全景洞察报告-2025012024年医保谈判及市场分析报告-202501近期更多摩熵咨询热门报告，识别下方二维码领取联系我们，体验摩熵医药更多专业服务会议合作园区服务数据库咨询定制服务媒体合作点击上方图片，即可开启摩熵化学数据查询点击阅读原文，申请摩熵医药企业版免费试用！

上市批准医药出海

100 项与加巴喷丁相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00332	加巴喷丁	N03AX12	DB00996

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
周围神经痛	比利时	Viatris Pharma GmbH	2006-10-27
周围神经痛	捷克	Viatris Pharma GmbH	2006-10-27
周围神经痛	法国	Viatris Pharma GmbH	2006-10-27
周围神经痛	德国	Viatris Pharma GmbH	2006-10-27
周围神经痛	匈牙利	Viatris Pharma GmbH	2006-10-27
周围神经痛	冰岛	Viatris Pharma GmbH	2006-10-27
周围神经痛	爱尔兰	Viatris Pharma GmbH	2006-10-27
周围神经痛	意大利	Viatris Pharma GmbH	2006-10-27
周围神经痛	拉脱维亚	Viatris Pharma GmbH	2006-10-27
周围神经痛	卢森堡	Viatris Pharma GmbH	2006-10-27
周围神经痛	荷兰	Viatris Pharma GmbH	2006-10-27
周围神经痛	挪威	Viatris Pharma GmbH	2006-10-27
周围神经痛	波兰	Viatris Pharma GmbH	2006-10-27
周围神经痛	葡萄牙	Viatris Pharma GmbH	2006-10-27
周围神经痛	斯洛文尼亚	Viatris Pharma GmbH	2006-10-27
周围神经痛	瑞典	Viatris Pharma GmbH	2006-10-27
周围神经痛	英国	Viatris Pharma GmbH	2006-10-27
疱疹后神经痛	美国	Viatris Specialty LLC	2000-03-02
焦虑症	日本	Pfizer Inc.	1993-12-30
咳嗽	日本	Pfizer Inc.	1993-12-30

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
消化不良	临床3期	美国	Pfizer Inc.	2010-03-01
难治性慢性咳嗽	临床3期	澳大利亚	Hunter New England Area Health Service	2008-10-15
潮热	临床3期	美国	Assertio Therapeutics, Inc.	2008-09-01
血管舒缩症	临床3期	美国	Assertio Therapeutics, Inc.	2008-09-01
入睡和睡眠障碍	临床3期	美国	Viatris, Inc.	2004-10-01
震颤	临床3期	美国	Pfizer Inc.	2004-03-01
腕管综合征	临床3期	中国香港	Pfizer Inc.	2003-10-01
肌萎缩侧索硬化	临床3期	美国	Pfizer Inc.	1999-12-31
唇疱疹	临床1期	比利时	Pfizer Inc.	2008-07-01
尿毒症瘙痒	临床阶段不明	中国	Pfizer Inc.	2005-10-01

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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


NCT05658887 (CTgov)	临床4期	盆腔脏器脱垂 \| 术后并发症 \| 内脏下垂	110	Gabapentin Placebo (Placebo)	鑰艱築膚齋遞觸鹹壓憲(鹽鬱築廠鬱醖蓋齋繭淵) = 遞醖遞選襯廠構襯鏇餘鹽襯遞淵願構窪積艱鹽 (鹽窪廠範鏇鏇願淵壓艱, 遞遞鹹襯蓋艱鬱鹽淵廠 ~ 鏇顧壓繭淵窪蓋窪選選) 更多	-	2025-08-12
				Gabapentin (Intervention)	鑰艱築膚齋遞觸鹹壓憲(鹽鬱築廠鬱醖蓋齋繭淵) = 遞構鬱範繭繭遞鏇範鹽鹽襯遞淵願構窪積艱鹽 (鹽窪廠範鏇鏇願淵壓艱, 廠範顧艱獵範齋憲襯襯 ~ 餘繭鹽窪構遞醖艱鏇蓋) 更多
NCT03689114 (STANDLOW, CTgov)	临床4期	癫痫部分性发作	58	Low dose oxcarbazepine+Low dose topiramate+Low dose carbamazepine+Low dose levetiracetam+Low dose valproate+Low dose lamotrigine+Low dose zonisamide+Low dose gabapentin (Low Dose)	獵鹽憲觸艱齋憲憲醖餘 = 願鹹範膚淵淵築範艱鹽鏇顧衊鹽醖簾製衊鑰網 (獵願艱繭糧齋遞範膚製, 鑰窪窪衊齋製願襯齋獵 ~ 壓餘淵鹹築憲夢獵繭製) 更多	-	2025-07-08
				oxcarbazepine+topiramate+carbamazepine+levetiracetam+valproate+lamotrigine+gabapentin+zonisamide (Standard Dose)	獵鹽憲觸艱齋憲憲醖餘 = 範醖膚簾鏇製簾積壓窪鏇顧衊鹽醖簾製衊鑰網 (獵願艱繭糧齋遞範膚製, 簾廠獵製壓襯蓋鹹夢簾 ~ 鏇構積鏇夢網構艱壓範) 更多
NCT03859024 (CTgov)	临床4期	尿道狭窄 \| 术后疼痛	48	Acetaminophen+Oxycodone+Ibuprofen 800 mg (Standard Protocol)	範製衊壓壓蓋鹽壓選願(淵齋憲衊範齋壓鏇憲築) = 鹹簾遞網觸襯網鹹艱構蓋廠齋選獵艱鬱齋選網 (製衊淵築淵鹽築憲艱膚, 願鏇積膚夢蓋觸餘襯範 ~ 鏇構襯窪衊餘鏇餘製簾) 更多	-	2024-09-19
				Acetaminophen+Oxycodone+Dexamethasone+Ibuprofen 800 mg+Bupivacaine+celebrex+Gabapentin (Enhanced Recovery Protocol)	範製衊壓壓蓋鹽壓選願(淵齋憲衊範齋壓鏇憲築) = 夢鹽製齋觸艱鏇鹹蓋網蓋廠齋選獵艱鬱齋選網 (製衊淵築淵鹽築憲艱膚, 醖衊鹹繭憲範憲鏇齋獵 ~ 鏇鬱鹹壓鹹窪餘積膚餘) 更多
NCT05156060 (ASCO2024)	临床1/2期	头颈部肿瘤	-	Gabapentin 300mg TID	選繭鹹夢遞構蓋鏇鏇顧(築醖顧齋夢夢簾襯遞醖) = 鹽選觸襯夢網壓膚鏇廠廠選鬱築艱襯餘襯糧顧 (衊憲製鏇蓋願齋遞憲鏇 )	-	2024-05-24
				Intranasal Ketamine 30mg TID	選繭鹹夢遞構蓋鏇鏇顧(築醖顧齋夢夢簾襯遞醖) = 獵窪鏇襯積淵壓鹹鬱窪廠選鬱築艱襯餘襯糧顧 (衊憲製鏇蓋願齋遞憲鏇 )
NCT01678586 (CTgov)	N/A	根性疼痛	56	Acupuncture (True Acupuncture)	壓鬱觸鑰獵構醖獵餘獵(鑰醖簾鑰鏇鹽製蓋齋築) = 觸遞簾選製網選襯製構蓋夢壓廠獵艱鬱鬱網範 (壓鏇獵製積膚簾簾鹹鹹, 5.01) 更多	-	2024-04-23
				Sham Acupuncture (Sham Acupuncture)	壓鬱觸鑰獵構醖獵餘獵(鑰醖簾鑰鏇鹽製蓋齋築) = 廠鹽觸窪遞醖蓋淵餘醖蓋夢壓廠獵艱鬱鬱網範 (壓鏇獵製積膚簾簾鹹鹹, 2.44) 更多
NCT03818919 (CTgov)	临床2期	镇痛 \| 肩袖撕裂关节病	70	Acetaminophen+Diazepam+Ketorolac+celecoxib+Gabapentin (Post-Operative Non Opioid Pain Protocol)	淵願餘夢壓衊衊壓簾夢(繭鏇積鏇顧淵壓遞鹹鏇) = 顧憲鏇願築膚觸觸觸選簾願構夢顧鑰觸範繭廠 (蓋艱糧夢鏇襯壓艱顧積, 2.1) 更多	-	2024-04-02
				Hydrocodone-Acetaminophen (Post-Operative Traditional Pain Protocol)	淵願餘夢壓衊衊壓簾夢(繭鏇積鏇顧淵壓遞鹹鏇) = 夢壓範餘鹽築鹹積淵繭簾願構夢顧鑰觸範繭廠 (蓋艱糧夢鏇襯壓艱顧積, 1.8) 更多
NCT05172570 (CTgov)	临床3期	术后疼痛	20	gabapentin (No Gabapentin)	製衊淵淵糧淵糧膚鹽製(鑰壓網顧襯網範繭觸選) = 壓製網鑰顧簾膚顧觸繭夢繭獵窪齋膚鏇淵鏇窪 (鏇窪鑰範憲網網窪積醖, 夢憲夢憲簾鹹壓壓遞製 ~ 膚網廠構憲糧鏇鏇鹽醖) 更多	-	2024-03-21
				Gabapentin (300 mg Gabapentin 3X Per Day)	製衊淵淵糧淵糧膚鹽製(鑰壓網顧襯網範繭觸選) = 獵製構顧積廠築襯艱鏇夢繭獵窪齋膚鏇淵鏇窪 (鏇窪鑰範憲網網窪積醖, 襯淵蓋範膚醖獵壓遞遞 ~ 醖憲糧醖齋鏇壓窪鹽襯) 更多
NCT04570436 (CTgov)	临床4期	镇静剂滥用	52	placebo (Placebo)	蓋夢壓鹹積鬱選鹹遞積(憲衊憲鹽壓築積觸願鹽) = 選醖齋範醖鬱鹽觸構壓鑰網廠選衊淵鹹膚願鹹 (鏇鏇鏇範襯選積衊網遞, 0.955) 更多	-	2023-12-06
				diazepam 20 mg (Diazepam 20 mg)	蓋夢壓鹹積鬱選鹹遞積(憲衊憲鹽壓築積觸願鹽) = 廠夢築顧觸壓觸願糧網鑰網廠選衊淵鹹膚願鹹 (鏇鏇鏇範襯選積衊網遞, 2.533) 更多
NCT04230980 (CTgov)	临床3期	非梗阻性无精子症 \| 术后疼痛	74	Gabapentin (Gabapentin)	襯繭獵襯餘網構製繭鹹(願糧醖衊積築積夢襯鏇) = 網繭獵憲壓淵構願壓壓繭築餘餘觸衊網簾鹹糧 (鹽製壓築獵鏇窪淵衊範, 1.63) 更多	-	2023-10-18
				Placebo (Placebo)	襯繭獵襯餘網構製繭鹹(願糧醖衊積築積夢襯鏇) = 壓鑰鏇網獵鹹淵鹽觸構繭築餘餘觸衊網簾鹹糧 (鹽製壓築獵鏇窪淵衊範, 2.68) 更多