ERDOSTEINE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C8H11NO4S2
Molecular Weight	249.307
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

OC(=O)CSCC(=O)NC1CCSC1=O

InChI

InChIKey=QGFORSXNKQLDNO-UHFFFAOYSA-N

InChI=1S/C8H11NO4S2/c10-6(3-14-4-7(11)12)9-5-1-2-15-8(5)13/h5H,1-4H2,(H,9,10)(H,11,12)

HIDE SMILES / InChI

Description

Erdosteine is an antioxidant compound developed by Edmond Pharma and approved in Europe for the treatment of chronic bronchitis and COPD. Erdosteine has two thiol groups and is believed to act as a free radicals scavenger (through the formation of the active metabolite I, N-thiodiglycolylhomocysteine). Also the drug effect may be due to the inhibition of the activity of elastase enzyme and its interaction with mucosa. The drug got Orphan Drug designation by FDA for the treatment of bronchiectasis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
mucus secretion	Modulator
Neutrophil elastase	Inhibitor
reactive oxygen species biosynthetic process	Antagonist

Conditions

Condition	Modality	Targets	Highest Phase	Product
Chronic bronchitis	Primary		Approved	ERDOTIN
Chronic obstructive pulmonary disease	Primary		Approved	ERDOTIN

C_max

Value	Dose	Co-administered	Analyte	Population
1.419 μg/mL	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
1.594 μg/mL	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
1.34 μg/mL	900 mg single, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
1.15 μg/mL	300 mg 3 times / day multiple, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
3.45 μg/mL	900 mg single, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens
3.17 μg/mL	300 mg 3 times / day multiple, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
3.492 μg × h/mL	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
3.523 μg × h/mL	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
3.71 μg × h/mL	900 mg single, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
3.55 μg × h/mL	300 mg 3 times / day multiple, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
12.32 μg × h/mL	900 mg single, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens
12.23 μg × h/mL	300 mg 3 times / day multiple, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.478 h	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
2.603 h	600 mg single, oral		ERDOSTEINE plasma	Homo sapiens
1.29 h	900 mg single, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
1.36 h	300 mg 3 times / day multiple, oral	THEOPHYLLINE	ERDOSTEINE plasma	Homo sapiens
1.68 h	900 mg single, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens
1.49 h	300 mg 3 times / day multiple, oral	THEOPHYLLINE	HOMOCYSTEINE,N-[[(CARBOXYMETHYL)THIO]ACETYL]- plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
300 mg 3 times / day multiple, oral Recommended	unhealthy, ADULT

Showing 1 to 1 of 1 entries

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PubMed

Show entries

Title	Date	PubMed
The SH-metabolite I of erdosteine, a mucolytic drug, enhances the inhibitory effect of salbutamol on the respiratory burst of neutrophils.	2002	12512232
Effects of erdosteine treatment against doxorubicin-induced toxicity through erythrocyte and plasma oxidant/antioxidant status in rats.	2003 Apr	12644389
Sensitive determination of erdosteine in human plasma by use of automated 96-well solid-phase extraction and LC-MS/MS.	2004 Feb 18	15127822
Inhibitory effects of metabolite I of erdosteine on the generation of nitric oxide and peroxynitrite chemiluminescence by human neutrophils.	2004 Jul	15161993
Cisplatin-induced acute renal failure is ameliorated by erdosteine in a dose-dependent manner.	2004 Jul-Aug	15300714

Showing 1 to 5 of 47 entries

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Patents

Sample Use Guides

In Vivo Use Guide

1 capsule (300 mg) 2-3 times a day

Route of Administration: Oral

In Vitro Use Guide

Unknown

Show entries

Name

Type

Language

ERDOSTEINE

Official Name

English

RV144

Code

English

RV-144

Code

English

Erdosteine [WHO-DD]

Common Name

English

ERDOSTEINE [MART.]

Common Name

English

Showing 1 to 5 of 9 entries

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Show entries

Classification Tree

Code System

Code

Designated

FDA ORPHAN DRUG

417413

Mucolytics

WHO-ATC

R05CB15

Mucolytics

WHO-VATC

QR05CB15

Agent Affecting Respiratory System

NCI_THESAURUS

C74536

Positive

EU-Orphan Drug

EU/3/12/1084

Showing 1 to 5 of 5 entries

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Show entries

Code System

Code

Type

Description

NCI_THESAURUS

C61750

PRIMARY

MESH

C048498

PRIMARY

EVMPD

SUB06595MIG

PRIMARY

ChEMBL

CHEMBL1697744

PRIMARY

RXCUI

24305

PRIMARY

RxNorm

Showing 1 to 5 of 15 entries

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ACTIVE MOIETY


					PQ4H3CJ9NU

Erdosteine Metabolite 1

SUBSTANCE RECORD


					76J0853EKA

ERDOSTEINE

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Doses

PubMed

Patents

Sample Use Guides

C_max

T_1/2