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

+ [24]

Target-

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.

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

Consiglio Nazionale delle Ricerche

Inactive Organization

Dompé Pharmaceutici Spa

Drug Highest PhaseApproved

First Approval Date

JP (25 Oct 1980),

Acute BronchitisAcute upper respiratory tract inflammationBronchiectasis+ [4]

Regulation-

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Structure

Molecular FormulaC5H9NO4S

InChIKeyGBFLZEXEOZUWRN-VKHMYHEASA-N

CAS Registry638-23-3

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.

CTR20220884 / CompletedNot Applicable

羧甲司坦片在健康成年受试者中单中心、随机、开放、空腹/餐后条件下、单次给药、两周期、两序列、自身交叉对照的人体生物等效性试验

[Translation] A single-center, randomized, open-label, fasting/postprandial, single-dose, two-cycle, two-sequence, self-crossover controlled human bioequivalence study of carbocisteine tablets in healthy adult subjects

主要研究目的：以广州欧化药业有限公司持证、广东华南药业集团有限公司生产的羧甲司坦片（规格：0.25g）为受试制剂，以杏林製薬株式会社生产的羧甲司坦片（商品名：ムコダイン，规格：250mg）为参比制剂，研究受试制剂与参比制剂的吸收速度和吸收程度，评价两制剂在空腹/餐后条件下单次给药时的生物等效性。次要研究目的：观察在空腹/餐后条件下单次口服两制剂在健康受试者中的安全性。

[Translation]

Main research purpose: Carbocysteine tablets (specification: 0.25g) produced by Guangzhou Ouhua Pharmaceutical Co., Ltd. and produced by Guangdong Huanan Pharmaceutical Group Co., Ltd. were used as the test preparation. Carbocysteine tablets produced by Xinglin Pharmaceutical Co., Ltd. Tan tablets (trade name: Mokuno, specification: 250mg) are reference preparations. The absorption speed and degree of absorption of the test preparation and the reference preparation are studied, and the bioequivalence of the two preparations when single administration under fasting/postprandial conditions is evaluated. effectiveness. Secondary study objectives: To observe the safety of a single oral administration of two formulations in healthy subjects under fasting/postprandial conditions.

Start Date19 Apr 2022

Sponsor / Collaborator

Zengcheng Guangzhou Ouhua 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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584

Literatures (Medical) associated with Carbocysteine

16 Nov 2024·Natural Product Research

Naturally occurring organosulfur compounds effectively inhibits PCSK-9 activity and restrict PCSK-9-LDL-receptor interaction via in-silico and in-vitro approach

Article

Author: Khan, Mohd Shahnawaz ; Waiz, Mohd ; Alvi, Sahir S. ; Ahmad, Saheem ; Khan, M. Salman ; Ahmad, Parvej

The present study intended to divulge the potential role of garlic-derived organosulfur compounds (OSCs) in targeting PCSK-9 and averting its interaction with the EGF-A portion of LDL-R via in-vitro and in-silico analysis. Our in-silico screening data showed that 3-(Propylsulfinyl)-L-alanine (PSA), S-Ethyl-L-cysteine (SEC), alliin, and S-Allyl-L-cysteine (SAC) exhibited higher binding energy (-7.05, -7.00, -6.65, and -6.31 Kcal/mol, respectively) against PCSK-9, among other selected OSCs. Further, the protein-protein interaction study of PCSK-9-OSCs-complex with EGF-A demonstrated a similar binding pattern with E-total values ranging from -430.01 to -405.6 Kcal/mol. These results were further validated via in-vitro analysis which showed that SEC, SAC, and diallyl trisulphide (DAT) exhibited the lowest IC₅₀ values of 4.70, 5.26, and 5.29 µg/mL, respectively. In conclusion, the presented data illustrated that SEC, SAC, and DAT were the best inhibitors of PCSK-9 activity and may have the potential to improve the LDL-R function and lower the circulatory LDL-C level.

01 Nov 2024·Plant Physiology and Biochemistry

Inhibition of sulfur assimilation by S-benzyl-L-cysteine: Impacts on growth, photosynthesis, and leaf proteome of maize plants

Article

Author: Grizza, Luiz Henryque Escher ; Wagner, Ana Luiza Santos ; Seixas, Flavio Augusto Vicente ; dos Santos, Wanderley Dantas ; Abrahão, Josielle ; de Carvalho Contesoto, Isabela ; Dos Santos, Wanderley Dantas ; de Paiva Foletto-Felipe, Marcela ; Menezes, Paulo Vinícius Moreira da Costa ; Santos Wagner, Ana Luiza ; Foletto-Felipe, Marcela de Paiva ; Ferro, Ana Paula ; de Oliveira, Marco Aurélio Schüler ; Constantin, Rodrigo Polimeni ; Contesoto, Isabela de Carvalho ; Marchiosi, Rogério ; da Costa Menezes, Paulo Vinícius Moreira ; Tomazini, Larissa Fonseca ; Ferrarese-Filho, Osvaldo

Sulfur is an essential nutrient for various physiological processes, including protein synthesis and enzyme activation. We aimed to evaluate how S-benzyl-L-cysteine (SBC), an inhibitor of the sulfur assimilation pathway, affects maize plants' growth, photosynthesis, and leaf proteomic profile. Thus, maize plants were grown for 14 days in vermiculite supplemented with SBC. Photosynthesis was assessed using light and CO₂ response curves and chlorophyll a fluorescence. Leaf proteome analysis was conducted to evaluate photosynthetic protein biosynthesis, and ROS content was quantified to assess oxidative stress. Applying SBC resulted in a significant decrease in the growth of maize plants. The gas exchange analysis revealed that maize plants exhibited a diminished rate of CO₂ assimilation attributable to both stomatal and non-stomatal limitations. Furthermore, SBC suppressed the activity of important elements involved in the photosynthetic electron transport chain (including photosystems I and II, cytochrome b₆f, and ATP synthase) and enzymes responsible for the Calvin cycle, some of which have sulfur-containing prosthetic groups. Consequently, the diminished electron flow rate resulted in a substantial increase in the levels of ROS within the leaves. Our research highlights the crucial role of SBC in disrupting maize photosynthesis by limiting L-cysteine and assimilated sulfur availability, which are essential for the synthesis of protein and prosthetic groups and photosynthetic processes, emphasizing the potential of OAS-TL as a new herbicide site of action.

12 Aug 2024·Chemistry – A European Journal

Crystal to Hydrogel Transformation in S‐Benzyl‐L‐Cysteine‐Containing Cyclic Dipeptides ‐ Nanostructure Elucidation and Applications

Article

Author: Sepay, Nayim ; Ghosh, Saswati ; Banerji, Biswadip

AbstractCyclic dipeptides (CDPs) are crucial building blocks for a range of functional nanomaterials due to their simple chemical structure and high molecular stability. In this investigation, we synthesized a set of S‐benzyl‐L‐cysteine‐based CDPs (designated as P1‐P6) and thoroughly examined their self‐assembly behavior in a methanol‐water solvent to elucidate the relationship between their structure and gelation properties. The hydrophobicity of the amino acids within the CDPs was gradually increased. The present study employed a comprehensive array of analytical techniques, including NMR, FT‐IR, AFM, thioflavin‐T, congo‐red CD, X‐ray crystallography, and biophysical calculations like Hirshfield Surface analysis and DFT analysis. These methods revealed that in addition to hydrogen bonding, the hydrophobic nature of the amino acid side chain significantly influences the propensity of CDPs to form hydrogels. Each CDP yielded distinct nanofibrillar networks rich in β‐sheet structures, showcasing unique morphological features. Moreover, we explored the practical application of these CDP‐based hydrogels in water purification by utilizing them to remove harmful organic dyes from contaminated water. This application underscores the potential of CDPs in addressing environmental challenges, offering a promising avenue for the future development of these materials in water treatment technologies.

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	JP	KYORIN Pharmaceutical Co., Ltd.	30 Nov 1988
Otitis Media	JP	KYORIN Pharmaceutical Co., Ltd.	30 Nov 1988
Sputum excretion difficulty	CN	Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.	01 Jan 1986
Acute Bronchitis	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Acute upper respiratory tract inflammation	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Bronchiectasis	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Bronchitis, Chronic	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Laryngitis	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Pharyngitis	JP	KYORIN Pharmaceutical Co., Ltd.	25 Oct 1980
Pulmonary Tuberculosis	JP	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
Bronchitis	Phase 2	CH	Dompé Pharmaceutici Spa	04 Jul 2016
Pulmonary Disease, Chronic Obstructive	Preclinical	IT	Consiglio Nazionale delle Ricerche	01 Sep 2013

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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	cyvskgqkvi(csqglusqxl) = kznswcpjwo sefygqtwff (iplnxlmuli )	Positive	01 Sep 2012
				Placebo	cyvskgqkvi(csqglusqxl) = kgmdqcmjuh sefygqtwff (iplnxlmuli )