Delving into the Latest Updates on Cibenzoline Succinate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cibenzoline, Cifenline, コハク酸シベンゾリン

+ [10]

Target

SCNA

Action

blockers

Mechanism

SCNA blockers(Sodium voltage-gated channel alpha subunits blockers)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Tachycardia

Inactive Indication-

Originator Organization

UPSA SAS

Active Organization

Choseido Pharmaceutical Co., Ltd.

TOA Eiyo Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (28 Sep 1990),

Tachycardia

Regulation-

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Structure/Sequence

Molecular FormulaC22H24N2O4

InChIKeyXFUIOIWYMHEPIE-UHFFFAOYSA-N

CAS Registry100678-32-8

Author: Takamisawa, Itaru ; Kitaoka, Hiroaki ; Nomura, Akihiro ; Ikeda, Shuntaro ; Shirotani, Shota ; Takayama, Morimasa ; Miyamoto, Yuya ; Okamoto, Ryuji ; Maejima, Yasuhiro ; Kubo, Toru ; Takashio, Seiji ; Tokita, Yukichi ; Fujino, Noboru ; Takei, Yasuyoshi ; Dohi, Kaoru ; Inomata, Takayuki ; Sugiura, Kenta ; Doi, Hirosato ; Izumiya, Yasuhiro ; Ogimoto, Akiyoshi ; Minami, Yuichiro ; Doi, Yoshinori L ; Shibata, Atsushi ; Chikamori, Taishiro ; Akasaki, Yuichi ; Higuchi, Koji ; Akita, Keitaro ; Tsujita, Kenichi ; Ieda, Masaki ; Furugen, Azusa ; Watanabe, Eiichi ; Maekawa, Yuichiro ; Tsujiuchi, Miki ; Yamaguchi, Osamu ; Shiraishi, Yasuyuki ; Tada, Norio ; Ebato, Mio ; Kato, Takao ; Nabeta, Takeru ; Yokota, Takashi ; Fujita, Shuichi ; Hoshiga, Masaaki ; Takano, Hitoshi

Background:

The Japanese Hypertrophic Cardiomyopathy Registry Study was designed to provide comprehensive, real-world insights into the clinical characteristics and management of hypertrophic cardiomyopathy (HCM) in Japan.

Methods:

This multicentre, prospective study enrolled consecutive patients with HCM from 24 referral hospitals across Japan starting in 2016. The baseline characteristics of 1485 patients enrolled by December 2019 are presented in this analysis.

Results:

The median ages at registration and diagnosis were 69 and 60 years, respectively, with men accounting for 54% of the cohort. Familial HCM was confirmed in 18% of cases. Of the cohort, 36% had hypertrophic obstructive cardiomyopathy (HOCM), while 8% had mid-ventricular obstruction, 14% had apical HCM and 4% were in the end-stage phase. Atrial fibrillation was observed in 27% of patients, though the majority were asymptomatic or had mild symptoms at registration. Adverse outcomes included prior sustained ventricular tachycardia or fibrillation (6%), heart failure requiring hospitalisation (11%) and embolic events (5%). Defibrillator implantation was performed in 11% of patients. Differences in the defibrillator indications for primary prevention in the current three guidelines and status of defibrillator deployment at registration were clarified: the percentages of class IIa recommendation in the whole cohort and of patients with defibrillator implantation in class IIa were 22% and 19% in the Japanese guidelines, 4% and 39% in the European guidelines and 28% and 22% in the American guidelines, respectively. Beta blockers were prescribed to 90% of patients with HOCM, while 51% received cibenzoline. Septal reduction therapies were performed in 22% of patients with HOCM, with 6% undergoing surgical myectomy.

Conclusions:

As the first large-scale, prospective HCM registry in Japan, this study provides valuable baseline data on the clinical characteristics and management of HCM. These findings will help address gaps between current practice and guideline recommendations, improving the care of patients with HCM.

25 Jun 2025·CIRCULATION JOURNAL

Impact of Chronic Cibenzoline Therapy on Left Ventricular Remodeling in Patients With Hypertrophic Non-Obstructive Cardiomyopathy

Article

Author: Otani, Takashi ; Hamada, Mareomi ; Shigematsu, Yuji ; Ogimoto, Akiyoshi ; Ikeda, Shuntaro

BACKGROUND:

Changes in left ventricular (LV) remodeling, especially in relation to the duration of therapy, are poorly understood in patients with hypertrophic non-obstructive cardiomyopathy (HNCM).

METHODS AND RESULTS:

This study included 254 consecutive patients with HNCM. Patients were divided into 3 groups according to the length of chronic cibenzoline therapy (CCT): Group I (n=104), CCT ≥10 years; Group II (n=85), 5 years≤CCT<10 years; and Group III (n=65), 1 year ≤CCT<5 years. SV1+RV5 and the maximum depth of precordial negative T waves were measured on electrocardiograms (ECG). In addition to routine echocardiographic indices, we measured the distance between the mitral valve and the apex (i.e., the "LV long distance" [LVLD]). After CCT, ECG indices and LV wall thicknesses were decreased in all 3 groups. LV dimensions and LV fractional shortening were preserved, and did not differ significantly among the groups. Left atrial dimension and the E/A ratio also did not differ among the groups, whereas the E/early diastolic annular velocity (Ea) ratio was decreased in Groups I and II. After CCT, LVLD was increased in all groups (all P<0.0001). These improvements were greater in Group I than in Groups II and III.

CONCLUSIONS:

CCT preserved LV systolic function and reduced LV hypertrophy in patients with HNCM. The E/Ea ratio was improved in Groups I and II. Thus, CCT aids in treating patients with HNCM.

21 Feb 2025·BIOLOGICAL & PHARMACEUTICAL BULLETIN

<i>α</i><sub>1</sub>-Adrenoceptor Blockade by Class I Antiarrhythmic Drugs in Guinea Pig Thoracic Aorta as Revealed by Mechanical and Fluorescence Displacement Analysis

Article

Author: Kawazoe, Ayaka ; Shirai, Kuniaki ; Tanaka, Hikaru ; Seki, Maika ; Tsukada, Kohei ; Igarashi, Hiro ; Namekata, Iyuki ; Miyahara, Marina ; Hamaguchi, Shogo

The effects of thirteen Vaughn Williams class I antiarrhythmic drugs on the α₁-adrenergic receptor-mediated contraction were examined in thoracic aorta tissue preparations isolated from the guinea pig. Cibenzoline, quinidine, aprindine, and ranolazine, as well as prazosin, inhibited the phenylephrine-induced contraction with pA₂ values of 5.64, 5.59, 5.61, 5.08, and 8.50, respectively, but not prostaglandin F_2α-induced. These drugs reduced the staining of the smooth muscle layer by fluorescent prazosin. Propafenone inhibited the phenylephrine-induced contraction with an apparent pA₂ value of 5.31 and reduced the staining by fluorescent prazosin, but also inhibited the prostaglandin F_2α-induced contraction. Other class I antiarrhythmic drugs, disopyramide, pirmenol, procainamide, lidocaine, mexiletine, flecainide, pilsicainide, and GS-458967, affected neither the contraction by phenylephrine nor the fluorescent staining by prazosin. These results indicate that among the class I antiarrhythmic drugs, cibenzoline, aprindine, and propafenone, as well as quinidine and ranolazine, have α₁-adrenoceptor-blocking activity at therapeutically relevant concentrations.

100 Deals associated with Cibenzoline Succinate

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