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

License Organization-

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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1,126

Literatures (Medical) associated with Carbocysteine

01 Jul 2025·Journal of Affective Disorders

Hyperforin-induced gut microbiota metabolite carbocysteine protects against depressive-like behaviors in mice by modulating the colonic mucus barrier

Article

Author: Liu, Xuhui ; Zhang, Zheng ; Xing, Bo ; Shi, Kaixuan ; Chen, Qingjie

OBJECTIVEDepression affects millions, and current treatments have limitations, necessitating new approaches. Earlier research confirms Hyperforin's ability to reduce anhedonic behaviors in mice and modulate gut microbiota. This study aims to identify specific metabolic changes induced by Hyperforin that could illuminate its impact on gut microbiome metabolism, possibly uncovering novel metabolites for developing antidepressant therapies.METHODSFollowing the chronic stress model, untargeted metabolomic analysis of fecal samples was conducted to identify metabolic changes induced by Hyperforin. Bioinformatics tools analyzed the origins of differentially expressed metabolites and their correlation with Akkermansia muciniphila and Muribaculum intestinale. The significant metabolite Carbocysteine was further investigated for its antidepressant effects using behavioral assays in a mouse model of depression. Additionally, the response of the colonic mucus barrier was evaluated using Periodic Acid-Schiff (PAS) staining, scanning electron microscopy (SEM), and enzyme-linked immunosorbent assays (ELISA).RESULTSHyperforin significantly altered fecal metabolite profiles in stressed mice, with a notable shift in 239 metabolites mainly associated with co-metabolism pathways and microbiota-specific processes. Among these, Carbocysteine emerged as a key metabolite linked to beneficial bacteria Akkermansia muciniphila and Muribaculum intestinale, with its levels significantly elevated following Hyperforin treatment. Behavioral assessments indicated that Carbocysteine supplementation ameliorated depressive-like behaviors in the chronic restraint stress mouse model. It also enhanced colonic mucus production and integrity.CONCLUSIONOur research highlights Hyperforin's role in modulating gut microbiota metabolism and identifies Carbocysteine as a potential antidepressant. These findings advance our understanding of the gut-brain axis (GBA) in depression and pave the way for developing new therapeutics.

01 Jun 2025·Food and Chemical Toxicology

20-Week toxicity study of rotigotine behenate extended-release microspheres for intramuscular injection in sprague dawley rats

Article

Author: Zhang, Hong ; Tian, Jingwei ; Qin, Caiyi ; Cen, Xiaobo ; Lv, Wenjing ; Zhao, Xinyu ; Yu, Xin ; Wu, Mengting ; Yin, Zhicong ; Chen, Yumeng ; Guo, Wei

Based on the concept of continuous dopaminergic stimulation (CDS), Rotigotine Behenate extended-release microspheres for injection (RBEM) are currently under development. To support human clinical trials of RBEM, a 20-week repeat-dose toxicity study was conducted. SD rats intramuscularly received RBEM (60, 180, and 540 mg/kg) once every 4 weeks for 5 repeated doses followed by a 12-week recovery period, no clear sex difference was noted in the plasma exposure of rotigotine in rats, and the exposure generally increased in a dose-proportional manner. No obvious systemic toxicity occurred. Ovarian corpus luteum and breast acinar hypertrophy in rats were believed to be associated with the activation of dopamine receptors by RBEM and decreased prolactin levels. The reversible vacuolar degeneration or foamy macrophage infiltration at the injection site, adjacent tissues, and alveoli of rats were associated with local inflammation and foreign body removal reaction caused by PLGA and SCMC. In this study, the non-observed-adverse-effect-level (NOAEL) in rats was 540 mg/kg (based on rotigotine), which was equivalent to 24 times the maximum clinical recommended dose of RBEM, 448 mg/person/28 days (expressed as the dose of rotigotine behenate). In conclusion, RBEM exhibited a good safety margin and can be used in phase I clinical trials. Keywords: Parkinson's disease; RBEM; Continuous dopaminergic stimulation; Repeated dose toxicity.

01 Mar 2025·Neuropharmacology

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

Article

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

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	wsigvgxltn(bwsuxlyryv) = utrmsdnovw kutpcaipbx (jyqkdpmkqo )	Positive	01 Sep 2012
				Placebo	wsigvgxltn(bwsuxlyryv) = zsxrszlawl kutpcaipbx (jyqkdpmkqo )