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].

The study used 26 male C57BL/6 mice (8 weeks old, 20-30 g). They were randomly divided into four groups. The Erdosteine group (n=6) received Erdosteine orally by gavage at a dose of 10 mg/kg daily for 7 days. The MTX + Erdosteine group (n=7) received a single intraperitoneal injection of methotrexate (10 mg/kg) on the first day, followed by oral administration of Erdosteine (10 mg/kg) daily for 7 days, starting on the same day. At the end of the experiment, animals were sacrificed by cervical dislocation, and testes were removed for biochemical and histological analysis. [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 an N-acyl amino acid. Erdosteine is a mucus-dissolving drug, also known as a mucolytic. It is a thiol derivative used to treat chronic obstructive bronchitis and its infectious acute exacerbations. The drug contains a sulfhydryl group, released after first-pass metabolism in the liver. The metabolites are three active metabolites that, in addition to their mucolytic activity, also possess free radical scavenging activity. Erdosteine works by controlling mucus production and viscosity while enhancing mucociliary clearance. It also combats free radicals generated by cigarette smoke. Clinical trials have shown that erdosteine is safe and well-tolerated. Taking 300 mg of erdosteine twice daily reduces cough (including cough frequency and severity) and reduces sputum viscosity faster and more effectively than placebo, and is more effective at reducing sputum adhesion than taking 30 mg of ambroxol twice daily. In patients with acute exacerbations of chronic bronchitis, the combination of erdosteine and amoxicillin resulted in higher antibiotic concentrations in sputum and faster, more significant improvement in clinical symptoms compared to placebo. Erdosteine has a low incidence of adverse reactions, most of which are gastrointestinal and usually mild. Erdosteine is a homocysteine-derived thiol derivative with mucolytic and free radical scavenging properties. Erdosteine and its metabolites improve sputum expectoration by regulating mucus production and viscosity, promoting mucociliary clearance. The drug also inhibits chemically induced cough reflexes and protects lung tissue from smoking-induced damage by scavenging free radicals. Indications: For the treatment of chronic bronchitis in adults. Mechanism of Action: Erdosteine is an oral mucolytic. It belongs to the thiol derivative class and is used to treat symptoms of chronic obstructive bronchitis. Erdosteine contains thiol groups, which are released after first-pass metabolism in the liver. Its three active metabolites possess mucolytic and free radical scavenging activities. Erdosteine increases sputum expectoration by regulating airway mucus production and viscosity, while enhancing mucociliary clearance. Erdosteine also inhibits the effects of free radicals in cigarette smoke. Clinical studies in patients with chronic obstructive pulmonary disease (COPD) have shown that the drug is generally safe and well-tolerated. Twice-daily administration of 300 mg erdosteine, compared to placebo, provides faster and more effective relief of cough (including cough frequency and severity) and reduces sputum viscosity; compared to twice-daily administration of 30 mg ambroxol, it is more effective in reducing sputum adhesion. In patients with acute exacerbations of chronic bronchitis, erdosteine in combination with amoxicillin increases the concentration of antibiotics in sputum, resulting in faster and more significant symptom relief compared to placebo. Erdosteine has a low incidence of adverse reactions, most of which are gastrointestinal and usually 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.)