盐酸洛美利嗪(Lomerizine Hydrochloride) - 药物靶点：calcium channel_在研适应症：偏头痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Lomerazine、Lomerizine、Lomerizine hydrochloride (JAN)

+ [7]

靶点

calcium channel

作用机制

calcium channel抑制剂(钙通道抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Pfizer Japan, Inc.MSD KK

非在研机构

Merck & Co., Inc.

Santen Pharmaceutical Co., Ltd.

最高研发阶段批准上市

首次获批日期

日本 (1999-03-12),

偏头痛

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C27H30F2N2O3

InChIKeyJQSAYKKFZOSZGJ-UHFFFAOYSA-N

CAS号101477-55-8

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关联

4

项与盐酸洛美利嗪相关的临床试验

JPRN-jRCTs051220072 / Not yet recruitingN/A

Effect of Lomerizine Hydrochloride on Preventing Recurrence of Cerebral Ischemic Events in Cerebral Autosomal Dominant Arteriopathy with Subcortical Infarcts and Leukoencephalopathy - LOMCAD

开始日期2022-11-28

申办/合作机构-

JPRN-JapicCTI-183865 / Unknown statusN/A

Administration study of lomerizine to healthy adult males

开始日期2018-02-14

申办/合作机构

LSI Medience Corp.

JPRN-jRCT1080223809 / Unknown statusN/A

Administration study of lomerizine to healthy adult males

开始日期2018-02-14

申办/合作机构

LSI Medience Corp.

100 项与盐酸洛美利嗪相关的临床结果

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100 项与盐酸洛美利嗪相关的转化医学

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100 项与盐酸洛美利嗪相关的专利（医药）

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123

项与盐酸洛美利嗪相关的文献（医药）

2024-12-01·Journal of Stroke and Cerebrovascular Diseases

Study protocol for LOMCAD Trial: Effect of lomerizine hydrochloride to prevent recurrence of cerebral ischemic events in CADASIL patients

Article

作者: Teramukai, Satoshi ; Fukunaga, Daiki ; Naito, Akari ; Watanabe-Hosomi, Akiko ; Nakata, Mitsuko ; Mizuno, Toshiki ; Mizuta, Ikuko ; Ohara, Tomoyuki ; Uno-Kadowaki, Aoi ; Iwami, Yayoi ; Matsuura, Hiraku ; Ito-Ihara, Toshiko

OBJECTIVESCerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL) is one of the most common monogenic cerebral small vessel diseases. Our previous observational study suggested that lomerizine hydrochloride, a calcium channel blocker approved in Japan in 1999 for the prevention of migraine headaches, is also effective for preventing recurrent ischemic stroke in CADASIL patients. The aim of this study (LOMCAD trial) is to verify the efficacy of lomerizine hydrochloride.MATERIALS AND METHODSThis is a multicenter, prospective, single-arm trial, using a historical control for comparison. CADASIL patients with a history of two or more cerebral ischemic events within the last two years will be administered lomerizine hydrochloride (5-mg tablet twice daily) for 24 months. The primary endpoint is symptomatic cerebral ischemic events during the 24-month period. Using our historical data and Bayesian sample size calculation based on a prior predictive distribution, the planned sample size was determined as 20 subjects.CONCLUSIONWe have planned a clinical trial to verify the effectiveness of lomerizine hydrochloride as prophylaxis to prevent recurrent cerebral ischemic events in CADASIL patients.REGISTRATIONThe LOMCAD trial has been registered in the Japan Registry of Clinical Trials (jRCTs051220072, https://jrct.niph.go.jp/latest-detail/jRCTs051220072).

2024-09-01·Rapid Communications in Mass Spectrometry

Characterizing Lomerizine metabolites in camel urine: High‐resolution mass spectrometry method development and validation for enhanced doping control

Article

作者: Nagarajan, Erumaipatty Rajagounder ; Hebel, Christiana ; Nalakath, Jahfar ; Waseem, Ibrahim ; Thacholil, Rasik Puzhithinipra ; Kadry, Ahmed ; OK, Praseen ; Selvapalam, Narayanan ; Babu, Ansar

RationaleLomerizine (LMZ) is an antimigraine drug that works as a calcium channel blocker and has selective effects on the central nervous system. It is metabolized into trimetazidine (TMZ), which is a prohibited substance owing to its performance‐enhancing effects in both human and animal sports. Effective doping control measures are imperative to distinguish the source of TMZ in samples to ensure integrity and fairness of the sport, therefore a comprehensive analysis of LMZ metabolites is essential to identify potential biomarkers in camel urine for effective doping control.MethodsCamel urine samples were collected from four healthy animals following a single oral administration of LMZ at a dosage of 1 mg/kg body weight. In vitro studies were conducted using homogenized camel liver samples. Lomerizine and its metabolites were extracted using solid‐phase extraction and analyzed with a Thermo Fisher Orbitrap Exploris liquid chromatography mass spectrometry system. The acquired data was processed with the Compound Discoverer software.ResultsThe study conducted a comprehensive analysis of LMZ metabolites in camels and identified 10 phase I and one phase II metabolites. The primary pathway for the formation of phase I metabolites was de‐alkylation, while phase II metabolite was formed through alkylation of the parent drug. The study provided valuable insights into the unique metabolic pathways of LMZ in camels under specific experimental conditions.ConclusionThe developed method enables the detection and characterization of LMZ and its metabolites in camels. The identified metabolites has the potential to act as marker metabolites for the distinctive detection of LMZ in camel urine to ensure efficient analytical strategies for routine doping control applications.

2024-08-01·Drug Testing and Analysis

Doping control analysis of trimetazidine in dried blood spot

Article

作者: Kageyama, Shinji ; Okano, Masato ; Sato, Mitsuhiko ; Miyamoto, Asami ; Ota, Masanori

AbstractDried blood spot (DBS) analysis has been an inherent part of sports drug testing through the technological advancements of the past decade. Trimetazidine, a non‐threshold banned substance, is excreted into urine after a dose of the permitted drug lomerizine. Therefore, a lomerizine‐specific metabolite (M6) is analyzed to confirm the origin of trimetazidine in traditional urine analysis. Application studies were conducted to develop an analytical method for trimetazidine applicable to DBS. These studies comprise (1) the effect of different sampling sites on the detection of trimetazidine, (2) the determination of the appropriate trimetazidine level required for DBS analysis, and (3) differentiating between trimetazidine and lomerizine use. A high‐resolution mass spectrometric method for detecting trimetazidine in DBS was validated. After oral administration of trimetazidine (n = 7), venous and capillary blood (fingertip and upper arm) were spotted on cellulose paper. Trimetazidine could be identified in DBS in all subjects up to 60 h after administration. The limit of detection was 0.05 ng/ml, and the limit of identification was 0.06 ng/ml, suggesting the minimum required performance level of 0.2 ng/ml. In the fingertip capillary blood, biases of 9.7% (vs. upper arm) and 13.0% (vs. vein) were observed in the trimetazidine intensity; however, there were no concerns in the qualitative analysis. After administering lomerizine (n = 10), the intact lomerizine has a strong peak intensity in blood compared to trimetazidine. Contrary to urine analysis, the M6 was less detectable in blood. Laboratories should confirm intact lomerizine whenever trimetazidine is identified in DBS.

100 项与盐酸洛美利嗪相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02633	盐酸洛美利嗪	N02C	DB14065

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
偏头痛	日本	Pfizer Japan, Inc.	1999-03-12

未上市

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适应症	最高研发状态	国家/地区	公司	日期
青光眼	临床1期	日本	-	2003-08-24
脑梗塞	临床前	日本	-	-

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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


ARVO2014	N/A	开角型青光眼 \| 青光眼	120	Lomerizine 10 mg	夢夢襯糧顧顧鏇製選願(積艱顧觸鏇觸繭醖壓齋) = 艱顧壓齋積構遞膚遞簾艱壓獵膚糧餘衊顧醖窪 (夢築廠齋鹽築鏇製衊鹽 )	积极	2014-04-01
				Methylcobalamin 1500 μg	夢夢襯糧顧顧鏇製選願(積艱顧觸鏇觸繭醖壓齋) = 鹹醖遞觸膚壓觸蓋製衊艱壓獵膚糧餘衊顧醖窪 (夢築廠齋鹽築鏇製衊鹽 )
ARVO2010	N/A	-	9	Nilvadipine	鏇製遞襯廠壓顧鹹艱窪(鹽膚艱獵蓋築鹹遞窪鬱) = 齋鏇範憲製糧膚構糧積艱蓋壓襯憲鑰襯製壓衊 (鬱壓範鏇鹹糧網糧窪窪 )	-	2010-04-01
				Lomerizine	鏇製遞襯廠壓顧鹹艱窪(鹽膚艱獵蓋築鹹遞窪鬱) = 範衊鹽鏇顧繭顧獵選積艱蓋壓襯憲鑰襯製壓衊 (鬱壓範鏇鹹糧網糧窪窪 )
ARVO2003	N/A	视神经损伤	-	Vehicle-treated group	餘壓簾糧夢鏇鹽遞願襯(淵艱製願餘獵醖繭醖構) = 範築襯鑰繭憲醖顧衊構製鏇繭艱憲糧蓋鑰齋鏇 (廠繭製願壓窪觸觸夢壓 )	积极	2003-05-01
				Lomerizine 10 mg/kg	餘壓簾糧夢鏇鹽遞願襯(淵艱製願餘獵醖繭醖構) = 築觸窪鏇憲醖艱鏇膚鏇製鏇繭艱憲糧蓋鑰齋鏇 (廠繭製願壓窪觸觸夢壓 )