Erdosteine is an oral mucolytic drug that is utilized in many chronic respiratory disorders as an expectorant. By preventing NF-κB activation in LPS-stimulated murine macrophages, eugenosteine reduces inflammation. Erdosteine, however, does not prevent the phosphorylation of the Akt and MAPK pathways brought on by LPS. Cell viability was assessed in order to assess the harmful effects of erdosteine on macrophages. Erdosteine at 1, 10, or 100 μg/mL did not cause any observable cytotoxicity. In RAW 264, LPS (1 μg/mL) treatment caused IκBα degradation.7 cells, RAW 264, with the highest deterioration seen after 10 minutes.Erdosteine at the specified concentrations was pretreated for 6 hours on 7 cells, and after that, LPS (1 μg/mL) was added after 10 minutes. The baseline levels of IκBα were unaffected by the ergotoxine pretreatment. Baseline levels of IκBα were unaffected by treatment with DMSO alone in a volume equivalent to that used for erdosteine administration. After 10 minutes of LPS treatment, there was a drop in the quantity of IκBα. IκBα degradation can be successfully inhibited by pretreatment with erdosteine at the prescribed concentration and time [1].

The following four groups of 26 male mice were created: Groups 1–4: control; Group 2–4: methotrexate (MTX) treatment; Group 5–6: MTX + Erdosteine treatment. On the first day of the trial, Groups 2 and 4 received a single oral dose of erdosteine every day for seven days, whereas Groups 3 and 4 received a single intraperitoneal injection of methotrexate. Upon completion of the study, the animals' testicles were extracted and weighed. Comparing the methotrexate group to the control group, there was a significant difference (p<0.05) in the total antioxidant capacity, total oxidative stress level, and myeloperoxidase activity. Between the methotrexate group and the control group, there was no difference in the levels of lipid peroxidation. In conclusion, methotrexate-induced toxicity to the testicles is effectively prevented by erdosteine. By causing spermatogenesis to develop in the seminiferous tubules, co-administration of erdosteine and methotrexate heals testicular injury [2].

[1]. Anti-inflammatory Effect of Erdosteine in Lipopolysaccharide-Stimulated RAW 264.7 Cells. Inflammation. 2016 Aug;39(4):1573-81.

[2]. Beneficial effect of erdosteine on methotrexate-induced testicular toxicity in mice. Toxicol Ind Health. 2010 Aug;26(7):433-8.

[3]. Recipharm’s proprietary molecule Erdosteine recognised as COPD treatment.

Erdosteine is a N-acyl-amino acid.
Erdosteine is a drug that causes a breakdown of mucus, also known as a mucolytic agent. It is a thiol derivative produced for the clinical management of chronic obstructive bronchitis, in addition to infective exacerbations of chronic bronchitis. This drug contains sulfhydryl groups which are released after erdosteine undergoes hepatic first pass metabolism. Three active metabolites result and possess mucolytic activity in addition to free radical scavenging activity. Erdosteine acts to control mucus production and control its viscosity while increasing mucociliary transport. It also combats the effects of free radicals resulting from cigarette smoke. Erdosteine has been shown to be safe and well tolerated in clinical trials. Erdosteine 300mg twice daily reduced cough (both frequency and severity) and sputum viscosity more quickly and more effectively than placebo and reduced the adhesivity of sputum more effectively than ambroxol 30mg twice daily. Co-administration of erdosteine and amoxicillin in patients with acute infective exacerbation of chronic bronchitis resulted in higher concentrations of the antibiotic in the sputum, leading to earlier and more pronounced amelioration of clinical symptoms compared with placebo. Erdosteine is associated with a low incidence of adverse events, most of which are gastrointestinal and generally mild.
Erdosteine is a homocysteine-derived thiol derivative with mucolytic and free radical scavenging properties. Erdosteine and its metabolites modulate mucus production and viscosity, by which facilitating mucociliary transport and improving expectoration. This agent also suppresses the chemical-induced cough reflex as well as protects lung tissues from damages caused by cigarette smoking mediated through free radicals scavenging.

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Drug Indication
Fro the treatment of chronic bronchitis in adults.

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Mechanism of Action
Erdosteine, is an orally administered mucolytic agent. It is classified as a thiol derivative and produced for the management of symptoms caused by chronic obstructive bronchitis. Erdosteine contains sulfhydryl groups which are released after hepatic first-pass metabolism in the liver. Its active metabolites (3 in number) exert both mucolytic activity and scavenging activity against free radicals. Erdosteine acts to regulate the production of mucus in the airway and regulates its viscosity while enhancing mucociliary transport. This leads to an increase in expectoration. Erdosteine shows inhibition against the effects of free radicals from cigarette smoke. Clinical studies in patients with chronic obstructive lung disease (COPD) have shown that this drug is generally safe and well tolerated. Erdosteine 300mg twice daily reduced cough (both frequency and severity) and sputum viscosity more quickly and more effectively than placebo and reduced the adhesivity of sputum more effectively than ambroxol 30mg twice daily. Co-administration of erdosteine and amoxicillin in patients with acute infective exacerbation of chronic bronchitis resulted in higher concentrations of the antibiotic in the sputum, leading to earlier and more pronounced amelioration of clinical symptoms compared with placebo. Erdosteine is associated with a low incidence of adverse events, most of which are gastrointestinal and generally mild.

249.012

84611-23-4

Erdosteine-13C4;Erdosteine-d4

65632

White to off-white solid powder

1.5±0.1 g/cm3

590.4±50.0 °C at 760 mmHg

156-160°C

310.8±30.1 °C

0.0±3.6 mmHg at 25°C

1.615

-0.32

2

6

5

15

282

0

O=C(CSCC(NC1CCSC1=O)=O)O

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)

2-[2-oxo-2-[(2-oxothiolan-3-yl)amino]ethyl]sulfanylacetic acid

Erdosteine PV144 PV 144 RV 144 RV144 PV-144

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~50 mg/mL (~200.55 mM)
H2O : ~6.67 mg/mL (~26.75 mM)

Solubility in Formulation 1: ≥ 3.25 mg/mL (13.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 3.25 mg/mL (13.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 3.25 mg/mL (13.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 6.67 mg/mL (26.75 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)