Delving into the Latest Updates on Carbocysteine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(L)-2-Amino-3-(carboxymethylthio)propionic acid, (R)-S-(carboxymethyl)cysteine, Carbecisteine

+ [23]

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious DiseasesMouth and Tooth DiseasesOtorhinolaryngologic Diseases+ [1]

Active Indication

Chronic sinusitisOtitis MediaSputum excretion difficulty+ [9]

Inactive Indication-

Originator Organization

KYORIN Pharmaceutical Co., Ltd.

Active Organization

KYORIN Pharmaceutical Co., Ltd.

Consiglio Nazionale delle Ricerche

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

Inactive Organization

Dompé Pharmaceutici Spa

Drug Highest PhaseApproved

First Approval Date

Japan (25 Oct 1980),

Acute BronchitisAcute upper respiratory tract inflammationBronchiectasis+ [4]

Regulation-

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Structure/Sequence

Molecular FormulaC5H9NO4S

InChIKeyGBFLZEXEOZUWRN-VKHMYHEASA-N

CAS Registry638-23-3

Nonalcoholic fatty liver disease (NAFLD) is a global public health concern, and the leading cause of chronic liver disease, especially in developed countries. NAFLD is characterized by lipid accumulation in the liver not attributed to other causes. Lifestyle interventions, including dietary modification and exercise, remain the cornerstone of NAFLD treatment. Pharmacological treatments aimed primarily at improving liver disease should generally be limited to those with biopsy-proven NASH and fibrosis.

Start Date01 Mar 2025

Sponsor / Collaborator

Tanta University

ChiCTR2400089858

/ SuspendedPhase 4IIT

Carbocysteine in Pre-Chronic Obstructive Pulmonary Disease Patients in China (CP-COPD): A Randomized, Double-blind, Placebo-controlled, Parallel-group, Multicenter clinical Trial

Start Date23 Sep 2024

Sponsor / Collaborator-

CTR20233108

/ CompletedNot Applicable

羧甲司坦颗粒在健康受试者中随机、开放、单次给药、两制剂、两周期、双交叉空腹和餐后状态下的生物等效性研究

[Translation] A randomized, open-label, single-dose, two-formulation, two-period, double-crossover bioequivalence study of carbocisteine granules in healthy subjects under fasting and fed conditions

主要目的：研究空腹和餐后状态下单次口服受试制剂羧甲司坦颗粒（规格：0.5g，康芝药业股份有限公司生产）与参比制剂羧甲司坦干糖浆（MUCODYNE DS 50%，规格：0.5g，由杏林制药株式会社生产，康芝药业股份有限公司提供）的药代动力学参数及相对生物利用度，评价两制剂是否具有生物等效性。次要目的：评价中国健康受试者空腹和餐后状态下单次口服受试制剂羧甲司坦颗粒和参比制剂羧甲司坦干糖浆后的安全性。

[Translation]

Primary objective: To study the pharmacokinetic parameters and relative bioavailability of the test preparation carbocysteine granules (specification: 0.5g, produced by Kangzhi Pharmaceutical Co., Ltd.) and the reference preparation carbocysteine dry syrup (MUCODYNE DS 50%, specification: 0.5g, produced by Xinglin Pharmaceutical Co., Ltd., provided by Kangzhi Pharmaceutical Co., Ltd.) after a single oral administration in the fasting and postprandial states, and to evaluate whether the two preparations are bioequivalent. Secondary objective: To evaluate the safety of the test preparation carbocysteine granules and the reference preparation carbocysteine dry syrup after a single oral administration in Chinese healthy subjects in the fasting and postprandial states.

Start Date09 Oct 2023

Sponsor / Collaborator

Honz Pharmaceutical Co., Ltd.

100 Clinical Results associated with Carbocysteine

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100 Translational Medicine associated with Carbocysteine

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100 Patents (Medical) associated with Carbocysteine

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1,121

Literatures (Medical) associated with Carbocysteine

01 Mar 2025·Neuropharmacology

Functional evidence that S-nitroso-L-cysteine may be a candidate carotid body neurotransmitter

Article

Author: Lewis, Stephen J. ; Coffee, Gregory A. ; Baby, Santhosh M. ; Seckler, James M. ; Coffee, Gregory A ; Palmer, Lisa A. ; Lewis, Stephen J ; Baby, Santhosh M ; Palmer, Lisa A ; Getsy, Paulina M ; Bates, James N ; Bates, James N. ; Getsy, Paulina M. ; Seckler, James M

The primary objective of the present study is to provide further evidence that the endogenous S-nitrosothiol, S-nitroso-L-cysteine (L-CSNO), plays an essential role in signaling the hypoxic ventilatory response (HVR) in rodents. Key findings were that (1) injection of L-CSNO (50 nmol/kg, IV) caused a pronounced increase in frequency of breathing (Freq), tidal volume (TV) and minute ventilation (MV) in naïve C57BL/6 mice, whereas injection of D-CSNO (50 nmol/kg, IV) elicited minimal responses; (2) L-CSNO elicited minor responses in (a) C57BL/6 mice with bilateral carotid sinus nerve transection (CSNX), (b) C57BL/6 mice treated neonatally with capsaicin (CAP) to eliminate small-diameter C-fibers, and (c) C57BL/6 mice receiving continuous infusion of L-CSNO receptor antagonists, S-methyl-L-cysteine and S-ethyl-L-cysteine (L-SMC + L-SEC, both at 5 μmol/kg/min, IV); and (3) injection of S-nitroso-L-glutathione (L-GSNO, 50 nmol/kg, IV) elicited pronounced ventilatory responses that were not inhibited by L-SMC + L-SEC. Subsequent exposure of naïve C57BL/6 mice to a hypoxic gas challenge (HXC; 10% O₂, 90% N₂) elicited pronounced increases in Freq, TV and MV that were subject to roll-off. These HXC responses were markedly reduced in CSNX, CAP, and L-SMC + L-SEC-infused C57BL/6 mice. Subsequent exposure of all C57BL/6 mice (naïve, CSNX, CAP, and L-SMC + L-SEC) to a hypercapnic gas challenge (5% CO₂, 21% O₂, 74% N₂) elicited similar robust increases in Freq, TV and MV. Taken together, these findings provide evidence that an endogenous factor with pharmacodynamic properties similar to those of L-CSNO, rather than L-GSNO, mediates the HVR in male C57BL/6 mice.

01 Mar 2025·Food Control

Metabolomics based on GC-MS combined with chemometrics for geographical discrimination of garlic (Allium sativum L.)

Author: Macedo, Willian R. ; Silva, Geraldo H. ; Ikehara, Brena R. M. ; Leite, Victor dos S. A. ; Pinto, Frederico G. ; Ikehara, Brena.R.M. ; Almeida, Natalia R.

Ensuring the geog. origin of products helps protect consumers against fraud and mislabeling.This study investigates the metabolomic profiles of garlic (Allium sativum L.) samples from Brazil and China using gas chromatog.-mass spectrometry (GC-MS).Multivariate anal. Partial Least Squares Discriminant Anal. (PLS-DA) and Orthogonal PLS-DA (Ortho PLS-DA) revealed clear metabolic distinctions between the two sample groups with high classification accuracy.Brazilian garlic samples showed higher levels of sulfur compounds, such as allyl Pr sulfide, cysteine sulfonic acid, and S-carboxymethyl-L-cysteine, which contribute to its pungency and potential health benefits.Amino acids L-arginine, L-glutamic acid, and L-cysteine were also significantly increased in garlic from Brazil.In contrast, Chinese garlic exhibited higher intensities of sugars (e.g., D-fructose, D-mannose) and essential amino acids (L-tryptophan, L-valine, and L-leucine).These differences in metabolism are the result of distinct metabolic profiles.GC-MS-based untargeted metabolomic and chemometric anal. were able to differentiate the geog. origin of Brazilian and Chinese garlics and remain valuable to food authentication and quality control.Further studies are needed to confirm the biomarkers for origin verification here stated.

01 Jan 2025·Archivos de Bronconeumología

Effect of Carbocysteine on Exacerbations and Lung Function in Patients With Mild-to-Moderate Chronic Obstructive Pulmonary Disease: A Multicentre, Double-Blind, Randomized, Placebo-Controlled Trial

Article

Author: Lin, Li ; Huang, Peiyu ; Tian, Heshen ; Deng, Zhishan ; Yang, Huajing ; Wang, Yiran ; Cai, Shan ; Ying, Yinghua ; Zhao, Haiyan ; Wang, Qiuyue ; Lu, Lifei ; He, Zhiyi ; Wen, Xiang ; Huang, Hong ; Wu, Fan ; Wang, Lingwei ; Cheng, Qijian ; Zhen, Youlan ; Xiao, Shan ; Zhou, Yumin ; Ran, Pixin ; Li, Haiqing ; Peng, Jieqi ; Zhao, Ningning ; Wang, Zihui ; Xu, Jianwu

OBJECTIVESCarbocysteine can reduce the frequency of acute exacerbations and improve respiratory symptoms to a certain extent in severe to very severe chronic obstructive pulmonary disease (COPD) patients. The objective of the study was to evaluate the efficacy of carbocysteine on the rate of exacerbations and pulmonary function for mild-to-moderate COPD patients.METHODSIn this phase 4, multicenter, double-blind, randomized, placebo-controlled, parallel-group trial, we randomly assigned mild-to-moderate COPD patients in a 2:1 ratio to treatment with carbocysteine (500mg, thrice daily) or matched placebo for 12 months. Eligible participants were 40-80 years of age. The coprimary outcomes were the annual rate of exacerbations of COPD (mild, moderate or severe) during the 12-month trial period or the difference in the FEV₁ before bronchodilator use at 12-month from baseline.RESULTSOwing to slower-than-anticipated recruitment caused by the COVID-19 pandemic, recruitment of an estimated sample size of 732 patients stopped after 539 patients. The sample size was indeed reached for the annual rate of exacerbations but not for pulmonary function. Among 539 patients, 362 were randomized to receive carbocysteine and 177 to receive matched placebo. There was no significant difference in the annual rate of exacerbations of COPD between carbocysteine group and placebo group (0.39 vs. 0.46 per patient year; relative risk [RR], 0.85; 95% confidence interval [CI], 0.64-1.13; P=0.273). Based on the available sample size, the difference in the change of FEV₁ before bronchodilator use at 12 months between carbocysteine group and placebo group has not been observed (46±12 vs. 50±17ml; mean difference, 6 ml; 95% CI, -24 to 36; adjusted P=0.700).CONCLUSIONSOur findings suggested that carbocysteine might not significantly reduce the annual rate of total exacerbations in patients with mild-to-moderate COPD. The findings may have been compromised by an overestimation of the efficacy of carbocysteine on reducing exacerbations in mild-to-moderate COPD and potential confounding by baseline imbalances. The efficacy on lung function could not be adequately evaluated. Clinical trial registered with Chictr.org.cn (ChiCTR1800016712).

100 Deals associated with Carbocysteine

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External Link

KEGG	Wiki	ATC	Drug Bank
D06393	Carbocysteine	R05CB03	DB04339

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Chronic sinusitis	Japan	KYORIN Pharmaceutical Co., Ltd.	30 Nov 1988
Otitis Media	Japan	KYORIN Pharmaceutical Co., Ltd.	30 Nov 1988
Sputum excretion difficulty	China	Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.	01 Jan 1986
Acute Bronchitis	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Acute upper respiratory tract inflammation	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Bronchiectasis	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Bronchitis, Chronic	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Laryngitis	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Pharyngitis	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Pulmonary Tuberculosis	Japan	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Cough	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pulmonary Disease, Chronic Obstructive	Preclinical	Italy	Consiglio Nazionale delle Ricerche	01 Sep 2013
Bronchitis	Discovery	Switzerland	Dompé Pharmaceutici Spa	04 Jul 2016

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


GAIA (ERS2012)	Not Applicable	Status Asthmaticus	286	Carbocysteine 1500mg/day	pfqyaairxa(jjhbbariqx) = qrwchzlrwh uuakrjjmhi (kgafanmcrm )	Positive	01 Sep 2012
				Placebo	pfqyaairxa(jjhbbariqx) = mhkbjxgnzs uuakrjjmhi (kgafanmcrm )