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Esomeprazole

Alias: Esomeprazole (–) Omeprazole(–)-Omeprazole (S) Omeprazole (S)-Omeprazole
Cat No.:V9010 Purity: ≥98%
Esomeprazole,the S-isomer of omeprazole, is a proton pump inhibitor (PPI) used forthe treatment for frequent heartburn/gastroesophageal reflux disease-GERD
Esomeprazole
Esomeprazole Chemical Structure CAS No.: 119141-88-7
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
Other Sizes

Other Forms of Esomeprazole:

  • Esomeprazole Magnesium trihydrate
  • Esomeprazole-d6 sodium (Esomeprazole sodium-d6; (S)-Omeprazole-d6 sodium; (-)-Omeprazole-d6 sodium)
  • Esomeprazole sodium (S-Omeprazole sodium)
  • Esomeprazole magnesium (S-Omeprazole magnesium)
  • Esomeprazole magnesium
  • Esomeprazole potassium salt
  • Esomeprazole hemistrontium-Omeprazole hemistrontium
  • Esomeprazole-d3
  • Esomeprazole-d3 potassium
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description

Esomeprazole, the S-isomer of omeprazole, is a proton pump inhibitor (PPI) used for the treatment for frequent heartburn/gastroesophageal reflux disease-GERD

Biological Activity I Assay Protocols (From Reference)
ln Vitro
By increasing intracellular acidity, esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) therapy suppresses triple-negative breast cancer cells' in vitro proliferation in a dose-dependent manner [1].
ln Vivo
The C57BL/6J mice treated with esomeprazole (30–300 mg/kg; oral gavage; daily; for 19 or 11 days) showed a significant reduction in the animals' lung fibrosis progression. Additionally, esomeprazole lowers circulating fibrosis and inflammatory markers [2].
Cell Assay
Cell Viability Assay[1]
Cell Types: MDA-MB-468 Cell
Tested Concentrations: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Duration: 20 hrs (hours)
Experimental Results: Inhibition of triple negative breast cancer cells in a dose-dependent manner in vitro.
Animal Protocol
Animal/Disease Models: C57BL/6J mice (8 weeks old, 25-30 g) cotton smoke-induced lung injury [2]
Doses: 30 mg/kg, 300 mg/kg
Route of Administration: po (oral gavage); daily; continued for 19 Or 11-day
Experimental Results: Dramatically inhibited the progression of lung fibrosis in animals.
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
Omeprazole delayed-release capsules contain an enteric-coated granule formulation of omeprazole (because omeprazole is acid-labile), so that absorption of omeprazole begins only after the granules exit the stomach. Absorption of omeprazole occurs rapidly, with peak plasma concentrations of omeprazole achieved within 0.5-3.5 hours. Absolute bioavailability (compared with intravenous administration) is approximately 30-40% at doses of 20-40 mg, largely due to pre-systemic metabolism. The bioavailability of omeprazole increases slightly upon repeated administration of omeprazole delayed-release capsules.
After a single dose oral dose of a buffered solution of omeprazole, negligible (if any) amounts of unchanged drug were excreted in urine. Most of the dose (about 77%) was eliminated in urine as at least six different metabolites. Two metabolites were identified as _hydroxyomeprazole_ and the corresponding _carboxylic acid_. The remainder of the dose was found in the feces. This suggests significant biliary excretion of omeprazole metabolites. Three metabolites have been identified in the plasma, the _sulfide_ and _sulfone_ derivatives of omeprazole, and _hydroxyomeprazole_. These metabolites possess minimal or no antisecretory activity.
Approximately 0.3 L/kg, corresponding to the volume of extracellular water.
Healthy subject (delayed release capsule), total body clearance 500 - 600 mL/min Geriatric plasma clearance: 250 mL/min Hepatic impairment plasma clearance: 70 mL/min
Absorption: rapid. Distribution: Distributed in tissue, particularly gastric parietal cells.
Elimination: Renal 72 to 80%. Fecal 18 to 23%. In dialysis - Not readily dialyzable, because of extensive protein binding.
To clarify the in vivo first-pass metabolism of omeprazole, the pharmacokinetics were examined after oral, intraduodenal, intraportal venous, and intravenous administration at various doses to rats. Extraction ratios in the liver and intestinal tract were determined from the areas under the concentration-time curve (AUC) for intraportal venous and intravenous administration and from those for intraduodenal and intraportal venous administration, respectively. Assuming that the drug was absorbed from the gastrointestinal tract completely, the hepatic and intestinal extraction ratios were 0.80, 0.63, and 0.59 at doses of 2.5, 5, and 10 mg/kg and 0.70 and 0.73 at doses of 5 and 10 mg/kg, respectively. The bioavailability of orally administered omeprazole was 6.4, 9.6, and 12.6% at the doses of l0, 20, and 40 mg/kg, respectively. There were no differences in the distribution volume of steady state, total clearance, or elimination half-life at any doses. In addition, the AUC value after oral administration (20 mg/kg) in rats acutely intoxicated with CC(14) was 2.4 times larger than that in the control. These findings suggest that omeprazole undergoes a first-pass metabolism in the intestinal mucosa and/or lumen, as well as in the liver, and that the major contribution to the dose-dependent increase in bioavailability is a saturation of the first-pass metabolism in the liver.
Omeprazole is distributed into human milk; following oral administration of omeprazole 20 mg in one lactating women, concentrations of the drug were measured in breast milk.
For more Absorption, Distribution and Excretion (Complete) data for OMEPRAZOLE (6 total), please visit the HSDB record page.
The plasma elimination half-life of esomeprazole is approximately 1 to 1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the feces.
Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 to 20 umol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.
NEXIUM Delayed-Release Capsules and NEXIUM For Delayed-Release Oral Suspension contain a bioequivalent enteric-coated granule formulation of esomeprazole magnesium. Bioequivalency is based on a single dose (40 mg) study in 94 healthy male and female volunteers under fasting condition. After oral administration peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 90% compared to 64% after a single dose of 40 mg. The mean exposure (AUC) to esomeprazole increases from 4.32 umol*hr/L on Day 1 to 11.2 umol*hr/L on Day 5 after 40 mg once daily dosing.
Metabolism / Metabolites
Omeprazole is heavily metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The main part of its metabolism depends on the polymorphically expressed CYP2C19, which is responsible for the formation of _hydroxyomeprazole_, the major metabolite found in plasma. The remaining part depends on CYP3A4, responsible for the formation of _omeprazole sulphone_.
The in vitro metabolism of omeprazole was studied in human liver microsomes in order to define the metabolic pathways and identify the cytochrome P450 (CYP) isoforms responsible for the formation of the major omeprazole metabolites. 2 The four major metabolites identified in vitro, in tentative order of importance, were hydroxyomeprazole, omeprazole sulphone, 5-O-desmethylomeprazole, and an unidentified compound termed metabolite X. Omeprazole pyridone was also detected but could not be quantitated. Incubation of hydroxyomeprazole and omeprazole sulphone with human microsomes resulted in both cases in formation of the hydroxysulphone. The kinetics of formation of the four primary metabolites studied were biphasic suggesting the involvement of multiple CYP isoforms in each case. Further studies used substrate concentrations at which the high affinity activities predominated. 3 Formation of the major metabolite, hydroxyomeprazole, was significantly correlated with S-mephenytoin hydroxylase and with benzo[a]pyrene metabolism and CYP3A content. Inhibition studies with isoform selective inhibitors also indicated a dominant role of S-mephenytoin hydroxylase with some CYP3A contribution in the formation of hydroxyomeprazole. Correlation and inhibition data for the sulphone and metabolite X were consistent with a predominant role of the CYP3A subfamily in formation of these metabolites. Formation of 5-O-desmethylomeprazole was inhibited by both R, S-mephenytoin and quinidine, indicating that both S-mephenytoin hydroxylase and CYP2D6 may mediate this reaction in human liver microsomes and in vivo. The Vmax/Km (indicator of intrinsic clearance in vivo) for hydroxyomeprazole was four times greater than that for omeprazole sulphone. Consistent with findings in vivo, the results predict that omeprazole clearance in vivo would be reduced in poor metabolisers of mephenytoin due to reduction in the dominant partial metabolic clearance to hydroxyomeprazole.
Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack antisecretory activity. The major part of esomeprazole's metabolism is dependent upon the CYP 2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP 3A4 which forms the sulphone metabolite. CYP 2C19 isoenzyme exhibits polymorphism in the metabolism of esomeprazole, since some 3% of Caucasians and 15 to 20% of Asians lack CYP 2C19 and are termed Poor Metabolizers. At steady state, the ratio of AUC in Poor Metabolizers to AUC in the rest of the population (Extensive Metabolizers) is approximately 2. Following administration of equimolar doses, the S- and R-isomers are metabolized differently by the liver, resulting in higher plasma levels of the S- than of the R-isomer.
Omeprazole has known human metabolites that include 3-Hydroxyomeprazole, 5-Hydroxyomeprazole, Omeprazole sulfone, and 5'-O-Desmethyl omeprazole.
Hepatic. Omeprazole is extensively metabolized by the cytochrome P450 (CYP) enzyme system. The two primary CYP isozymes involved are CYP2C19 and CYP3A4. Metabolism is stereoselective in which the S-isomer is converted to 5'O-desmethylomeprazole via CYP2C19. CYP3A4 converts the S-isomer to 3-hydroxyomeprazole. The R-isomer is converted to 5-hydroxyomeprazole by CYP2C19. CYP3A4 converts the R-isomer to any four different metabolites: 5-hydroxyomeprazole (5-OH OME), omeprazole sulfone (OME sulfone), 5'-O-desmethylomeprazole (5'-desmethyl OME), and 3-hydroxyomeprazole (3-OH OME).
Route of Elimination: Urinary excretion is a primary route of excretion of omeprazole metabolites. Little, if any unchanged drug was excreted in the urine. The majority of the dose (about 77%) was eliminated in urine as at least six metabolites. Two were identified as hydroxyomeprazole and the corresponding carboxylic acid. The remainder of the dose was recovered in the feces.
Half Life: 0.5-1 hour (healthy subjects, delayed-release capsule);
3 hours (hepatic impairment)
Biological Half-Life
0.5-1 hour (healthy subjects, delayed-release capsule) Approximately 3 hours (hepatic impairment)
Plasma - Normal hepatic function - 30 minutes to 1 hour. Chronic hepatic disease - 3 hours.
Toxicity/Toxicokinetics
Toxicity Summary
Omeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, omeprazole blocks the final step in acid production, thus reducing gastric acidity.
Interactions
Inhibition of the cytochrome p450 enzyme system by omeprazole, especially in high dose, may cause a decrease in the hepatic metabolism of /coumarin- or indandione-derivative anticoagulants, diazepam or phenytoin/ which may result in delayed elimination and increased blood concentrations, when these medications are used concurrently with omeprazole.
Omeprazole may increase gastrointestinal pH; concurrent use /of ampicillin esters, iron salts, or ketoconazole/ with omeprazole may result in a reduction in absorption of ampicillin esters, iron salts, or ketoconazole.
Concurrent use of omeprazole with /bone marrow depressants/ may increase the leukopenic and/or thrombocytopenic effects of both these medications; if concurrent use is required, close observation for toxic effects should be considered.
The effect of omeprazole on drug metabolism was studied using the model drugs antipyrine and (14)C-aminopyrine. Elimination of both model drugs was assessed before and after 15 days of therapy in male subjects. It was concluded that metabolic inhibition of the model drugs would not occur with normal clinical doses of omeprazole.
For more Interactions (Complete) data for OMEPRAZOLE (9 total), please visit the HSDB record page.
In a single-dose study, concomitant administration of omeprazole 20 mg and sucralfate 1 g resulted in delayed absorption of omeprazole and decreased omeprazole bioavailability by 16%. Proton-pump inhibitors should be administered at least 30 minutes before sucralfate.
Pharmacokinetic interaction with omeprazole (decreased plasma concentrations and AUC of rilpivirine).32 343 Concomitant use of other proton-pump inhibitors also may result in decreased plasma concentration of rilpivirine.343 Concomitant use of rilpivirine and proton-pump inhibitors is contraindicated.
Concomitant use of omeprazole 40 mg once daily and atazanavir (with or without low-dose ritonavir) results in a substantial decrease in plasma concentrations of atazanavir and possible loss of the therapeutic effect of the antiretroviral agent or development of drug resistance. Concomitant use of omeprazole 40 mg once daily (administered 2 hours before atazanavir) and atazanavir 400 mg once daily decreased the AUC and peak plasma concentration of atazanavir by 94 and 96%, respectively. The manufacturer of esomeprazole states that concomitant administration with atazanavir is not recommended. If atazanavir is administered in an antiretroviral treatment-naive patient receiving a proton-pump inhibitor, a ritonavir-boosted regimen of 300 mg of atazanavir once daily with ritonavir 100 mg once daily with food is recommended. The dose of the proton-pump inhibitor should be administered approximately 12 hours before ritonavir-boosted atazanavir; the dose of the proton-pump inhibitor should not exceed omeprazole 20 mg daily (or equivalent). Concomitant use of proton-pump inhibitors with atazanavir is not recommended in antiretroviral treatment-experienced patients.
Concomitant use of omeprazole 20 mg once daily and digoxin in healthy individuals increased digoxin bioavailability by 10% (up to 30% in some individuals). Because esomeprazole is an enantiomer of omeprazole, concomitant use of esomeprazole with digoxin is expected to increase systemic exposure to digoxin; therefore, monitoring for manifestations of digoxin toxicity may be required during such concomitant use.
For more Interactions (Complete) data for Esomeprazole (7 total), please visit the HSDB record page.
Non-Human Toxicity Values
LD50 Mouse iv 0.08 g/kg
LD50 Mouse oral >4 g/kg
LD50 Rat iv >0.05 g/kg
LD50 Rat oral >4 g/kg
References

[1]. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

[2]. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

[3]. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

Additional Infomation
Therapeutic Uses
Anti-Ulcer Agents; Enzyme Inhibitors
Omeprazole is indicated for the treatment of a complex of symptoms which may be caused by any of the conditions where a reduction of gastric acid secretion is required (e.g., duodenal ulcer, gastric ulcer, nonsteroidal anti-inflammatory drugs associated gastric and duodenal ulcer, reflux esophagitis, gastroesophageal reflex disease) or when no identifiable organic cause is found (i.e., functional dyspepsia). /Included in US product labeling/
Omeprazole is indicated for the treatment of heartburn and other symptoms associated with gastroesophageal reflux disease. Omeprazole is indicated for the short-term treatment of erosive esophagitis (associated with gastroesophageal reflux disease) that has been diagnosed by endoscopy. Omeprazole also is indicated to maintain healing of erosive esophagitis. /Included in US product labeling/
Omeprazole is indicated for the long-term treatment of pathologic gastric hypersecretion associated with Zollinger-Ellison syndrome (alone or as part of multiple endocrine neoplasia Type-1), systemic mastocytosis, and multiple endocrine adenoma. /Included in US product labeling/
For more Therapeutic Uses (Complete) data for OMEPRAZOLE (8 total), please visit the HSDB record page.
Anti-Ulcer Agents; Proton Pump Inhibitors
Although evidence currently is limited, proton-pump inhibitors have been used for gastric acid-suppressive therapy as an adjunct in the symptomatic treatment of upper GI Crohn's disease, including esophageal, gastroduodenal, and jejunoileal disease.22 23 24 25 26 27 28 Most evidence of efficacy to date has been from case studies in patients with Crohn's-associated peptic ulcer disease unresponsive to other therapies (e.g., H2-receptor antagonists, cytoprotective agents, antacids, and/or sucralfate). /Not included in product label/
Esomeprazole magnesium is used for the long-term treatment of pathologic GI hypersecretory conditions. Efficacy for this indication was established in an open-label study in a limited number of patients with previously diagnosed pathologic GI hypersecretory conditions (e.g., Zollinger-Ellison syndrome, idiopathic gastric acid hypersecretion); patients received total daily dosages of esomeprazole ranging from 80 mg-240 mg. The drug generally was well tolerated at these dosages for the duration of the study (12 months). At 12 months of therapy, 90% of patients treated with esomeprazole had controlled basal acid output (BAO) levels, defined as BAO of less than 5 or 10 mEq/hour in patients who had or had not previously undergone gastric acid-reducing surgery, respectively.
Esomeprazole magnesium is used for reducing the occurrence of gastric ulcers associated with chronic nonsteroidal anti-inflammatory agent (NSAIA) therapy in patients at risk for developing these ulcers, including individuals 60 years of age or older and/or those with a documented history of gastric ulcers. Efficacy for this indication was established in two 6-month randomized, controlled studies in patients receiving chronic therapy with either a prototypical NSAIA or a selective cyclooxygenase-2 (COX-2) inhibitor; individuals enrolled in these studies were considered to be at risk for developing NSAIA-associated ulcers because of their age (60 years or older) and/or a history of documented gastric or duodenal ulcer within the previous 5 years, but they had no evidence of gastric or duodenal ulcers on endoscopic examination at the start of the studies. Results of the studies indicated that esomeprazole 20 or 40 mg daily was more effective than placebo in preventing gastric ulcer occurrence during 6 months of treatment; however, no additional benefit was observed with the 40-mg daily dosage compared with the 20-mg daily dosage. In these studies, 94.7-95.4% of patients receiving esomeprazole 20 mg daily, 95.3-96.7% of those receiving esomeprazole 40 mg daily, and 83.3-88.2% of those receiving placebo remained free of gastric ulcers, as determined by serial endoscopic examinations, throughout the 6-month study.1 The occurrence rate of duodenal ulcers was too low to determine the effect of esomeprazole therapy on duodenal ulcer occurrence.
For more Therapeutic Uses (Complete) data for Esomeprazole (6 total), please visit the HSDB record page.
Drug Warnings
Pregnancy risk category: C /RISK CANNOT BE RULED OUT. Adequate, well controlled human studies are lacking, and animal studies have shown risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy; but the potential benefits may outweigh the potential risk./
No information is available on the relationship of age to the effects of omeprazole in geriatric patients. However, a somewhat decreased rate of elimination and increased bioavailability are more likely to occur in geriatric patients taking omeprazole.
Omeprazole generally is well tolerated. The most frequent adverse effects associated with omeprazole therapy involve the GI tract (e.g., diarrhea, nausea, constipation, abdominal pain, vomiting) and the CNS (e.g., headache, dizziness).
Diarrhea, abdominal pain, nausea, vomiting, constipation, flatulence, and acid regurgitation are the most frequent adverse GI effects of omeprazole, occurring in about 1-5% of patients. Dysphagia, abdominal swelling, anorexia, irritable colon, fecal discoloration, pancreatitis (sometimes fatal), esophageal candidiasis, mucosal atrophy of the tongue, taste perversion, and dry mouth have been reported occasionally but in many cases were not directly attributed to the drug. Benign gastric fundic polyps have been reported rarely and appear to resolve upon discontinuation of omeprazole therapy.
For more Drug Warnings (Complete) data for OMEPRAZOLE (15 total), please visit the HSDB record page.
It is unknown whether esomeprazole is distributed into milk. However, omeprazole is distributed into human milk; discontinue nursing or drug because of potential risk in nursing infants.
FDA Pregnancy Category: B /NO EVIDENCE OF RISK IN HUMANS. Adequate, well controlled studies in pregnant women have not shown increased risk of fetal abnormalities despite adverse findings in animals, or, in the absents of adequate human studies, animal studies show no fetal risk. The chance of fetal harm is remote but remains a possibility./
When esomeprazole is used in fixed combination with naproxen, the usual cautions, precautions, and contraindications associated with naproxen must be considered in addition to those associated with esomeprazole.
Administration of proton-pump inhibitors has been associated with an increased risk for developing certain infections (e.g., community-acquired pneumonia).
For more Drug Warnings (Complete) data for Esomeprazole (12 total), please visit the HSDB record page.
Pharmacodynamics
**Effects on gastric acid secretion** This drug decreases gastric acid secretion. After oral administration, the onset of the antisecretory effect of omeprazole is usually achieved within one hour, with the maximum effect occurring by 2 hours after administration. The inhibitory effect of omeprazole on acid secretion increases with repeated once-daily dosing, reaching a plateau after four days. **Effects on serum gastrin** In studies of 200 or more patients, serum gastrin levels increased during the first 1-2 weeks of daily administration of therapeutic doses of omeprazole. This occurred in a parallel fashion with the inhibition of acid secretion. No further increase in serum gastrin occurred with continued omeprazole administration. Increased gastrin causes enterochromaffin-like cell hyperplasia and increased serum Chromogranin A (CgA) levels. The increased CgA levels may lead to false positive results in diagnostic studies for neuroendocrine tumors. **Enterochromaffin-like (ECL) cell effects** Human gastric biopsy samples have been obtained from more than 3000 pediatric and adult patients treated with omeprazole in long-term clinical studies. The incidence of enterochromaffin-like cell hyperplasia in these studies increased with time; however, no case of ECL cell carcinoids, dysplasia, or neoplasia have been identified in these patients. These studies, however, are of insufficient in power and duration to draw conclusions on the possible influence of long-term administration of omeprazole in the development of any premalignant or malignant conditions. **Other effects** Systemic effects of omeprazole in the central nervous system, cardiovascular and respiratory systems have not been found to date. Omeprazole, given in oral doses of 30 or 40 mg for 2-4 weeks, showed no effect on thyroid function, carbohydrate metabolism, or circulating levels of parathyroid hormone, cortisol, estradiol, testosterone, prolactin, cholecystokinin or secretin.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H19N3O3S
Molecular Weight
345.417
Exact Mass
345.114
CAS #
119141-88-7
Related CAS #
Esomeprazole magnesium trihydrate;217087-09-7;Esomeprazole sodium;161796-78-7;Esomeprazole magnesium;161973-10-0;Esomeprazole magnesium salt;1198768-91-0;Esomeprazole potassium salt;161796-84-5;Esomeprazole hemistrontium;914613-86-8;Esomeprazole-d3 sodium;Esomeprazole-d3
PubChem CID
4594
Appearance
Crystals from acetonitrile
White to off-white crystalline powder
Density
1.4±0.1 g/cm3
Boiling Point
600.0±60.0 °C at 760 mmHg
Flash Point
316.7±32.9 °C
Vapour Pressure
0.0±1.7 mmHg at 25°C
Index of Refraction
1.669
LogP
2.17
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
5
Heavy Atom Count
24
Complexity
453
Defined Atom Stereocenter Count
0
SMILES
O=[S@](C1=NC2=CC=C(OC)C=C2N1)CC3=NC=C(C)C(OC)=C3C
InChi Key
SUBDBMMJDZJVOS-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H19N3O3S/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17/h5-8H,9H2,1-4H3,(H,19,20)
Chemical Name
1H-Benzimidazole, 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2- pyridinyl)methyl)sulfinyl)-
Synonyms
Esomeprazole (–) Omeprazole(–)-Omeprazole (S) Omeprazole (S)-Omeprazole
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~361.88 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8950 mL 14.4751 mL 28.9503 mL
5 mM 0.5790 mL 2.8950 mL 5.7901 mL
10 mM 0.2895 mL 1.4475 mL 2.8950 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-1971 in Combination With Atezolizumab in Participants With Locally Advanced or Metastatic Solid Tumors
CTID: NCT05487235
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Voxelotor CYP and Transporter Cocktail Interaction Study
CTID: NCT05981365
Phase: Phase 1    Status: Completed
Date: 2024-11-22
Study of GS-4571 in Healthy Participants, Nondiabetic Obese Participants, and Nonobese Participants With Type 2 Diabetes Mellitus (T2DM)
CTID: NCT06562907
Phase: Phase 1    Status: Recruiting
Date: 2024-11-21
A Study to Compare How Different Substances (Caffeine, Warfarin, Omeprazole, Metoprolol, and Midazolam) Are Handled by the Body of Healthy People and People With Liver Cirrhosis
CTID: NCT05741385
Phase: N/A    Status: Recruiting
Date: 2024-11-18
Study on the Effect of Atorvastatin Co-administered With Omeprazole on Statin Lactone
CTID: NCT06690164
Phase: Phase 4    Status: Not yet recruiting
Date: 2024-11-15
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An Open-label, DDI Study to Investigate the Effects of Amlitelimab on the PK of Selected Cytochrome P450 Substrates
CTID: NCT06686628
Phase: Phase 1    Status: Recruiting
Date: 2024-11-13


A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body
CTID: NCT06494761
Phase: Phase 1    Status: Completed
Date: 2024-11-13
Study to Investigate the Effect of Rocatinlimab (AMG 451) on the Pharmacokinetics of Multiple Cytochrome P450 (CYP450) Substrates in Participants With Moderate to Severe Atopic Dermatitis
CTID: NCT05891119
PhaseEarly Phase 1    Status: Active, not recruiting
Date: 2024-11-07
A Study to Assess the Safety, Tolerability and Pharmacokinetics (PK) of Xanomeline With Trospium Chloride Versus KarXT in Healthy Adult and Elderly Participants of Japanese Ethnicity and to Assess the Effect of Omeprazole on the PK of Xanomeline With Trospium Chloride in Healthy Adult Participants
CTID: NCT06605950
Phase: Phase 1    Status: Recruiting
Date: 2024-10-31
Study of H2 Antagonist and a Proton Pump Inhibitor of Selpercatinib in Healthy Participants
CTID: NCT05338502
Phase: Phase 1    Status: Completed
Date: 2024-10-30
Drug-drug Interaction Trial With Tralokinumab in Moderate to Severe Atopic Dermatitis - ECZTRA 4
CTID: NCT03556592
Phase: Phase 1    Status: Completed
Date: 2024-10-26
IRX-2 Regimen in Treating Women With Cervical Squamous Intraepithelial Neoplasia 3 or Squamous Vulvar Intraepithelial Neoplasia 3
CTID: NCT03267680
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-10-10
A Trial of Omeprazole and Low Dose Aspirin to Identify Colorectal Biomarkers of Preventive Efficacy
CTID: NCT06378398
PhaseEarly Phase 1    Status: Recruiting
Date: 2024-10-09
GERD Infant Feeding Therapeutics Trial (GIFT Trial)
CTID: NCT06114836
Phase: N/A    Status: Recruiting
Date: 2024-10-04
Pharmacokinetic Drug-drug Interaction Study of Encorafenib and Binimetinib on Probe Drugs in Patients With BRAF V600-mutant Melanoma or Other Advanced Solid Tumors
CTID: NCT03864042
Phase: Phase 1    Status: Completed
Date: 2024-09-27
Interaction of BI 425809 With Midazolam, Warfarin, Omeprazole and Digoxin
CTID: NCT02783040
Phase: Phase 1    Status: Completed
Date: 2024-09-20
A Study Investigating the Change in Metabolism Phenotype in Paediatric, Adolescent & Young Adults With Hodgkin or Non-Hodgkin Lymphoma.
CTID: NCT06383338
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-09-19
A Study to Learn How Different Amounts of PF-06954522 Are Tolerated and Act in Adults With Type 2 Diabetes Mellitus
CTID: NCT06279234
Phase: Phase 1    Status: Recruiting
Date: 2024-09-19
KF2022#4-trial: Effects of a Beta Blocker and NSAID on CYP Mediated Drug Metabolism
CTID: NCT06566794
Phase: N/A    Status: Not yet recruiting
Date: 2024-08-22
Pre-operative IRX-2 in Early Stage Breast Cancer (ESBC)
CTID: NCT02950259
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-08-21
High Dose Omeprazole in Patients With Pancreatic Cancer
CTID: NCT04930991
PhaseEarly Phase 1    Status: Recruiting
Date: 2024-08-16
Study in Subjects With Rheumatoid Arthritis to Evaluate the Effect of a Single Dose of Olokizumab on the Pharmacokinetics of Substrates for CYP1A2, CYP2C9, CYP2C19 and CYP3A4
CTID: NCT04246762
Phase: Phase 1    Status: Completed
Date: 2024-08-15
Assessment of Gastric pH Changes Induced by Ascorbic Acid Tablets
CTID: NCT04199624
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-08-15
Luminal Fructose Kinetics (MARTINI Study)
CTID: NCT06539494
Phase: Phase 2    Status: Recruiting
Date: 2024-08-06
A Study to Evaluate the Effect of Ustekinumab on Cytochrome P450 Enzyme Activities Following Induction and Maintenance Dosing in Participants With Active Crohn's Disease or Ulcerative Colitis
CTID: NCT03358706
Phase: Phase 1    Status: Suspended
Date: 2024-06-21
A Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects
CTID: NCT06162169
Phase: Phase 1    Status: Completed
Date: 2024-06-13
A Study to Estimate the Effect of Multiple Dose Abrocitinib on Caffeine, Efavirenz, and Omeprazole in Healthy Participants
CTID: NCT05067439
Phase: Phase 1    Status: Completed
Date: 2024-05-31
Reducing Gastrointestinal Bleeding With Proton Pump Inhibitor Therapy in Acute Venous Thromboembolism
CTID: NCT06393868
Phase: Phase 3    Status: Not yet recruiting
Date: 2024-05-01
Proton Pump Inhibitors (PPI) and Fat Absorption in Cystic Fibrosis (CF) and Exocrine Pancreatic Insufficiency (EPI)
CTID: NCT03551691
Phase: Phase 2    Status: Completed
Date: 2024-04-30
EFFICACY OF ORAL AROEIRA (Schinus Terebinthifolia Raddi) COMPARED TO OMEPRAZOLE IN DYSPEPPSIA
CTID: NCT04069286
Phase: Phase 3    Status: Not yet recruiting
Date: 2024-04-29
A Study to Evaluate the Impact of Lactobacillus Rhamnosus GG on Proton Pump Inhibitor-Induced Gut Dysbiosis
CTID: NCT05517928
Phase: N/A    Status: Recruiting
Date: 2024-04-23
Drug-durg Interaction of Leritrelvir(RAY1216) With Midazolam, Omeprazole, Rosuvastatin, Verapamil, and Rifampin
CTID: NCT06031454
Phase: Phase 1    Status: Completed
Date: 2024-04-16
Biomarkers for Prediction of Analgesic Efficacy in Knee OA.
CTID: NCT05256342
Phase: N/A    Status: Completed
Date: 2024-04-12
A Clinical Trial to Evaluate a High-Fat Meal and Omeprazole Enteric-coated Tablets on ASBK021
CTID: NCT06322706
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-03-21
Evaluation of the Effects of Omeprazole and Rifampin on the Pharmacokinetics of VX-548 in Healthy Participants
CTID: NCT05635110
Phase: Phase 1    Status: Completed
Date: 2024-03-20
Safety and Efficacy of Triple and Quadruple Regimens as First Line Therapy for Management of Helicobacter Pylori Infection in Egyptians
CTID: NCT06315478
Phase: Phase 4    Status: Completed
Date: 2024-03-18
IRX-2 Regimen in Patients With Newly Diagnosed Stage II, III, or IVA Squamous Cell Carcinoma of the Oral Cavity
CTID: NCT02609386
Phase: Phase 2    Status: Completed
Date: 2024-01-30
A Study of Effect of Multiple Doses of LOXO-305 on the Pharmacokinetics of Single Oral Doses of CYP1A2, CYP2C9, CYP2C19 Substrates in Healthy Participants
CTID: NCT06215430
Phase: Phase 1    Status: Completed
Date: 2024-01-22
A Study to Evaluate the Impact of Omeprazole on the Pharmacokinetics of Sotorasib Co-administered With an Acidic Beverage in Healthy Volunteers
CTID: NCT05497557
Phase: Phase 1    Status: Completed
Date: 2024-01-19
Evaluation of Pharmacokinetic Interaction Between GSK3640254 and Caffeine, Metoprolol, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin in Healthy Adults
CTID: NCT04425902
Phase: Phase 1    Status: Completed
Date: 2024-01-05
Effect of Acid Suppression Medication on Pediatric Microbiome
CTID: NCT02016820
Phase: N/A    Status: Terminated
Date: 2023-12-26
Effectiveness of Vonoprazan vs Omeprazole as Empiric Therapy for Gastroesophageal Reflux Disease (GERD) Patients Without Alarm Features
CTID: NCT04028466
Phase: Phase 4    Status: Terminated
Date: 2023-11-22
A Study to Assess the Effect of BMS-986419 on the Single Dose Drug Levels of Probe Substrates in Healthy Participants
CTID: NCT05932277
Phase: Phase 1    Status: Completed
Date: 2023-10-30
A Study to Evaluate the Drug-drug Interaction Potential of BMS-986196 in Healthy Participants
CTID: NCT05852769
Phase: Phase 1    Status: Completed
Date: 2023-09-26
A Study of ALXN1840 (Coated and Non-coated) Administered With And Without Omeprazole In Healthy Adults
CTID: NCT05319912
Phase: Phase 1    Status: Completed
Date: 2023-08-02
A Study of ALXN1840 (Non-coated) Administered With And Without Omeprazole In Healthy Adults
CTID: NCT05319899
Phase: Phase 1    Status: Completed
Date: 2023-08-01
Effect of a Proton Pump Inhibitor on the PK of Tepotinib
CTID: NCT03531762
Phase: Phase 1    Status: Completed
Date: 2023-07-28
Open-Label, Multicenter, Two-Part, Phase 1 Study to Characterize Effects of a Moderate CYP3A Inhibitor on PK of Tazemetostat, Effects of Tazemetostat on PK of CYP2C8 and CYP2C19 Substrates, and Effect of Increased Gastric pH on PK of Tazemetostat in B-cell Lymphoma or Advanced Solid Tumor Patients
CTID: NCT03028103
Phase: Phase 1    Status: Completed
Date: 2023-06-26
PROUD Study - Preventing Opioid Use Disorders
CTID: NCT04766996
Phase: Phase 4    Status: Terminated
Date: 2023-06-22
Pharmacokinetic Drug-Drug Interaction Study of Rucaparib
CTID: NCT02740712
Phase: Phase 1    Status: Completed
Date: 2023-06-09
Bioequivalence Study of 20 mg Omeprazole Capsules in Indonesia Healthy Subject
CTID: NCT05849883
Phase: N/A    Status: Completed
Date: 2023-05-09
Efficacy and Safety of Houtou Jianweiling Tablet in the Treatment of Chronic Non-Atrophic Gastritis
CTID: NCT04672018
Phase: Phase 2    Status: Completed
Date: 2023-04-18
Bioavailability and Bioequivalence of Two Risdiplam Tablets in Healthy Participants
CTID: NCT04718181
Phase: Phase 1    Status: Completed
Date: 2023-03-13
Placebo In Chronic Back Pain - Double-Blind Randomized Control Trial
CTID: NCT02013427
Phase: Phase 4    Status: Completed
Date: 2023-03-03
High Dose Dual Therapy vs Clarithromycin Triple Therapy for Treatment Naive H Pylori Infection in an Urban Population
CTID: NCT05342532
Phase: Phase 4    Status: Completed
Date: 2023-02-01
Preventing Cardiac Complication of COVID-19 Disease With Early Acute Coronary Syndrome Therapy: A Randomised Controlled Trial.
CTID: NCT04333407
Phase: N/A    Status: Terminated
Date: 2023-01-18
Study to Assess the Effect of Co-Administration of AZD9833 on the Pharmacokinetics of Midazolam, of Omeprazole, of Celecoxib and of Dabigatran Etexilate in Healthy Postmenopausal Female Volunteers
CTID: NCT05438303
Phase: Phase 1    Status: Completed
Date: 2023-01-12
The Possible Protective Role of Omeprazole Against Oxaliplatin Induced Neuropathy in Cancer Patients
CTID: NCT05680870
Phase: Phase 3    Status: Not yet recruiting
Date: 2023-01-11
A Study of Imlunestrant (LY3484356) in Female Healthy Participants
CTID: NCT05444556
Phase: Phase 1    Status: Completed
Date: 2022-11-25
Efficacy and Safety Evaluation of Neobianacid® in GERD and EPS
CTID: NCT03238534
Phase: Phase 4    Status: Completed
Date: 2022-11-21
Placebo In Chronic Back Pain (Phase 2)
CTID: NCT02986334
Phase: Phase 4    Status: Completed
Date: 2022-11-07
Risk of CYP2C19 Phenoconversion in Healthy Volunteers With Rapid, Normal, and Intermediate Predicted Metabolizers' Status
CTID: NCT05264142
Phase: Phase 1    Status: Unknown status
Date: 2022-11-03
A Study to Evaluate the Impact of Acid-reducing Agents on the Pharmacokinetics (PK) of AMG 510 in Healthy Participants
CTID: NCT05599828
Phase: Phase 1    Status: Completed
Date: 2022-10-31
Study to Evaluate the Drug-drug Interaction Effect of Omeprazole on the Pharmacokinetics (PK) of AMG 510 in Healthy Participants
CTID: NCT05581992
Phase: Phase 1    Status: Completed
Date: 2022-10-17
A Study to Assess the Effects of Itraconazole, Rifampicin, and Omeprazole on Pharmacokinetics of Adavosertib
CTID: NCT04959266
Phase: Phase 1    Status: Terminated
Date: 2022-09-16
High Dose Oral Omeprazole in High Risk UGIB
CTID: NCT04394663
Phase: N/A    Status: Recruiting
Date: 2022-08-26
Effect of Omeprazole on PK of Fluzoparib in Healthy Male Subjects
CTID: NCT04108676
Phase: Phase 1    Status: Completed
Date: 2022-07-29
A Multiple-Dose Pharmacokinetics Study of Two Gefapixant (AF-219/MK-7264) Formulations
CTID: NCT02492776
Phase: Phase 1    Status: Completed
Date: 2022-07-22
A Study to Assess the Effect of Intragastric pH and Fasting on the Pharmacokinetics of Gefapixant (AF-219/MK-7264)
CTID: NCT02229877
Phase: Phase 1    Status: Completed
Date: 2022-07-22
A Study of Effect of Food and a Proton Pump Inhibitor on Selpercatinib (LY3527723) in Healthy Participants
CTID: NCT05468164
Phase: Phase 1    Status: Completed
Date: 2022-07-21
Evaluating the Effects of Omeprazole on the Pharmacokinetics of XS004 (Dasatinib) Tablets in Healthy Adult Subjects Under Fasting Conditions
CTID: NCT05433896
Phase: Phase 1    Status: Completed
Date: 2022-06-27
Metformin's Effect on Drug Metabolism in Patients With Type 2 Diabetes
CTID: NCT04504045
Phase: Phase 1    Status: Terminated
Date: 2022-06-16
Drug-drug Interaction Between Belumosudil, Itraconazole, Rifampicin, Rabeprazole, and Omeprazole in Healthy Volunteers
CTID: NCT03530995
Phase: Phase 1    Status: Completed
Date: 2022-05-25
A Study to Investigate the Effect of Single and Repeated Oral Doses of ACT-539313 on What the Body Does to Flurbiprofen, Omeprazole, Midazolam in Healthy Subjects
CTID: NCT05254548
Phase: Phase 1    Status: Completed
Date: 2022-05-04
---------------------
OPEN, COMPARATIVE STUDY TO EVALUATE THE PERFORMANCE AND SAFETY OF THE MEDICAL DEVICE MARIAL® IN ASSOCIATION WITH PROTON-PUMP INHIBITORS VERSUS PPI ALONE IN PATIENTS AFFECTED BY GASTROESOPHAGEAL REFLUX DISEASE
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2020-12-03
Intestinal disposition of budesonide in healthy volunteers
CTID: null
Phase: Phase 2    Status: Completed
Date: 2019-12-20
Potential effect of proton-pump inhibitor on angiogenic markers in preeclampsia: a pilot study
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2018-09-05
Proton pump inhibitors (PPI) as a new strategy for therapy in sepsis: clinical trial to reduce severity of organ failure and in vitro experiments to search specific hallmarks in monocytes from septic patients and to characterize the mechanism of action of PPI (PPI-SEPSIS)
CTID: null
Phase: Phase 4    Status: Completed
Date: 2018-07-12
Evaluation of the effect of Gerdoff administered in combination to a treatment with protonic pump inhibitors vs the only treatment with protonic pump inhibitors, administered for 6 weeks, on higher symptoms associated to gerd, in patients with first diagnosis of gastroesophageal reflux disease. An open, multicentre, prospective, randomized, double parallel treatment arms study.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2017-03-14
Effect of omeprazole intake on faecal calprotectin
CTID: null
Phase: Phase 3    Status: Completed
Date: 2017-01-23
Multicentre controlled, randomized clinical trial to compare the efficacy and safety of ambulatory treatment of mild acute diverticulitis without antibiotics with the standard treatment with antibiotics
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2016-10-27
A Randomized Phase 2 Trial of Neoadjuvant and Adjuvant Therapy with the IRX-2 Regimen in Patients with Newly Diagnosed Stage II, III or IVA Squamous Cell Carcinoma of the Oral Cavity
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2016-10-27
Relief of heartburn and epigastric pain comparing Neobianacid® with omeprazole: a randomized, double blind, double dummy, reference product controlled, parallel group, non-inferiority clinical study
CTID: null
Phase: Phase 4    Status: Completed
Date: 2016-07-06
The impact of proton-pump inhibitors (antacids) on threshold dose distributions
CTID: null
Phase: Phase 3    Status: Completed
Date: 2015-09-24
A PHASE 2B/3, MULTICENTER, RANDOMIZED, OPEN-LABEL TRIAL TO EVALUATE THE COMBINATION OF CYCLOSPORINE AND OMEPRAZOLE AND OMEPRAZOLE ALONE IN PARTICIPANTS WITH NEW ONSET TYPE 1 DIABETES
CTID: null
Phase: Phase 2, Phase 3    Status: Prematurely Ended
Date: 2015-09-08
A randomized controlled multicenter trial of a five day course of oral colistin and neomycin followed by restoration of the gut microbiota using fecal transplantation to eradicate intestinal carriage of extended spectrum beta-lactamase or carbapenemase-producing Enterobacteriaceae in high-risk patients
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2015-05-26
The effect of on demand versus continuous use of proton pump inhibitors on reflux symptoms, quality of life and self-rated health in patients with gastro-oesophageal reflux disease
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2015-03-10
Supersaturation and precipitation of indinavir in the stomach of healthy human volunteers
CTID: null
Phase: Phase 4    Status: Completed
Date: 2014-12-24
Rectal and oral omeprazole treatment of gastroesophageal reflux in infants with esophageal atresia or congenital diaphragmatic hernia.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2013-10-24
A randomised placebo-controlled pilot trial of omeprazole in idiopathic pulmonary fibrosis (IPF)
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-09-20
A large, international, randomized, placebo-controlled trial to assess the impact of dabigatran (a direct thrombin inhibitor) and omeprazole (a proton-pump inhibitor) in patients suffering myocardial injury after noncardiac surgery
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2013-09-05
COAST - Cisplatin Ototoxicity attenuated by Aspirin Trial
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-09-25
A prospective, multicenter, open-label, patients with non-erosive gastroesophageal reflux disease (NERD) non-responders to therapy with PPIs
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2012-04-17
FIRST-LINE ERADICATOR THERAPY OF HELICOBACTER PYLORI INFECTION: OPEN CLINICAL TRIAL, RANDOMIZED, MULTICENTRE, THREE-ARMED, COMPARING THE CLASSICAL TRIPLE THERAPY VERSUS A MODIFIED SEQUENTIAL THERAPY AND A CURRENT THERAPY
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2012-04-02
Eficacia y seguridad de PYLERA (subcitrato potásico de bismuto, metronidazol y clorhidrato de tetraciclina) con omeprazol, administrados 10 días en sujetos con fracaso del tratamiento de erradicación de Helicobacter pylori
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-07-17
A Phase II trial of broad spectrum antibiotic therapy for early stage chronic lymphocytic leukaemia.
CTID: null
Phase: Phase 4    Status: Completed
Date: 2011-03-24
A double-blind, double-dummy, randomised, study to assess the superiority of Zegerid® 20 mg vs. Losec® 20 mg in the rapid relief of heartburn associated with GERD as on demand therapy.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-02-09
ESTUDIO FASE IV, PROSPECTIVO, ALEATORIZADO Y COMPARATIVO ENTRE LA TERAPIA “SECUENCIAL” Y “CONCOMITANTE” PARA LA ERRADICACIÓN DE Helicobacter pylori EN LA PRÁCTICA CLÍNICA HABITUAL
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2010-09-22
Etude de non-infériorité de l’efficacité de Gaviscon suspension buvable en flacon versus Oméprazole 20mg sur le pyrosis chez des patients ayant un RGO dont l’épisode actuel n’est pas traité.
CTID: null
Phase: Phase 4    Status: Completed
Date: 2010-06-01
Comparaison de l’effet antisécrétoire d’une dose unique de rabeprazole 20 mg et d’omeprazole 20 mg chez des sujets obèses
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2010-04-06
Farmacocinética en la obesidad mórbida: estudio de la influencia de dos técnicas de cirugía bariátrica (bypass Gástrico y Sleeve Gastrectomy) en el metabolismo de fármacos.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2009-10-06
Farmakologisk behandling af CNDI – Et ”proof-of-concept” studie.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2009-08-28
Assessment of platelet inhibitory response to clopidogrel when coadministered with a proton pump inhibitor
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2009-07-09
A trial of position control therapy (PCT) for treatment of infantile gastro-oesophageal reflux
CTID: null
Phase:    Status: Ongoing
Date: 2008-10-23
Ensayo clínico unicéntrico, simple ciego y aleatorizado de comparación de la eficacia erradicadora de primera línea frente al Helicobacter pylori entre la triple terapia convencional oral con claritromicina, amoxicilina y omeprazol (CAO) durante 10 días frente a triple terapia alternativa oral con levofloxacino, amoxicilina y omeprazol (LAO) durante 10 días
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2008-09-29
Estudio piloto comparativo del lansoprazol en formulación bucodispersable frente al omeprazol intravenoso en la evaluación del dolor torácico agudo de origen esofágico.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2008-09-20
An open label, exploratory study on the effect of rhBSSL on the fat absorption in patients with cystic fibrosis and pancreatic insufficiency.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-07-24
Efficacy and Safety of Quadruple Therapy by Bismuth Subcitrate Potassium, Metronidazole, and Tetracycline Given x 10 days With Omeprazole in Eradication of Helicobacter pylori: A Comparison to Omeprazole, Amoxicillin and Clarithromycin Given x 7 days
CTID: null
Phase: Phase 3    Status: Completed
Date: 2008-03-28
Tratamiento con omeprazol para la profilaxis de la hemorragia digestiva y el reflujo gastroesofágico en niños críticos
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2008-02-25
Effect of domperidone and omeprazole in gastro-oesophageal reflux disease in infants between 0 and 2 years.
CTID: null
Phase:    Status: Ongoing
Date: 2007-10-03
Helicobacter pylori Eradication vs Aspirin Toxicity Trial
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2007-09-21
Helicobacter eradication therapy in Chronic Obstructive Pulmonary Disease: A pilot,randomised, double blinded, placebo controlled trial
CTID: null
Phase: Phase 4    Status: Completed
Date: 2007-06-22
A Phase I, Randomized, Open-Label, Multi-National Study to Evaluate the Pharmacokinetics of Repeated Once-Daily Intravenous Doses of Esomeprazole in Paediatric Patients 0 to 17 Years Old, Inclusive
CTID: null
Phase: Phase 1    Status: Completed
Date: 2007-05-14
A phase III, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group, Treatment-withdrawal Study to Evaluate the Efficacy and Safety of Esomeprazole for the Treatment of Gastroesophageal Reflux Disease (GERD) in Infants Aged 1 to 11 months, Inclusive
CTID: null
Phase: Phase 3    Status: Completed
Date: 2007-05-03
An open-label randomised observer-blind study to evaluate 24-hour intragastric pH profile at day 1 and day 14 during treatment with a fixed combination of a histamine type 2 receptor antagonist and a proton pump inhibitor
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-03-05
Omeprazole and reflux disease - improvement of clinical outcome by genotype-adjusted dosing
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2007-03-02
OMEPRAZOLE 1 - Recherche de dose et Pharmacocinétique de population de l'Oméprazole chez le nouveau-né en traitement du reflux gastro-oesophagien.
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2007-02-16
Farmacokinetische evaluatie van enteraal toegediende omeprazole-suspensie bij patiënten met cerebral palsy.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-02-13
Endoscopic healing and tolerability of Soraprazan 20 mg qd compared to Soraprazan 10 mg qd and to Esomeprazole 40 mg qd in patients suffering from GERD Grade A-D (LA classification)
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2006-11-07
Symptom relief and tolerability of Soraprazan 20 mg qd and Soraprazan 10 mg qd compared to Esomeprazole 20 mg qd in patients with non-erosive gastroesophageal reflux disease (NERD)
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2006-11-06
A randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of esomeprazole once daily for the treatment of gastroesophageal reflux disease (GERD) in neonatal patients, including premature and up to 1 month corrected age
CTID: null
Phase: Phase 2, Phase 3    Status: Completed
Date: 2006-10-27
An 8 week, non-selected, cohort, study to investigate whether the treatment of reflux induced cough alters associated bronchial hyperresponsiveness.
CTID: null
Phase: Phase 4    Status: Prematurely Ended
Date: 2006-10-16
Stereoselective pharmacokinetics and CYP2C19-genotyping as outcome predictors of an omeprazole therapy in patients with GERD -- a pilot study (phase IV-study)
CTID: null
Phase: Phase 4    Status: Completed
Date: 2006-08-21
A study to assess the effectiveness of esomeprazole 40 mg once daily in subjects with continuing gastroesophageal reflux disease (GORD) symptoms following treatment with a previous full dose proton pump inhibitor (PPI). An 8 week, open label, multicentre study.
CTID: null
Phase: Phase 4    Status: Completed
Date: 2006-07-03
Double-blind, triple dummy, parallel-group, randomized, six-month study to compare celecoxib (200 mg BID) with diclofenac SR (75 mg BID) plus omeprazole (20 mg QD) for gastrointestinal events in subjects with osteoarthritis and rheumatoid arthritis at high-risk of gastrointestinal adverse events
CTID: null
Phase: Phase 4    Status: Suspended by CA, Completed
Date: 2006-06-15
A 16-day, randomized, double-blind, double-dummy, placebo-controlled, parallel-group trial comparing lumiracoxib 100mg o.d. with naproxen 500 mg b.i.d. plus omeprazole 20mg o.d. and placebo in healthy volunteers to confirm the safety and tolerability of lumiracoxib in the small bowel.
CTID: null
Phase: Phase 4    Status: Completed
Date: 2006-05-05
Treatment of extraesophageal manifestations of laryngopharyngeal reflux with Nexium (esomeprazole) 20mg bid, a doubleblind placebo controlled study
CTID: null
Phase: Phase 4    Status: Completed
Date: 2006-02-07
EFECTO DEL ÁCIDO ACETILSALICÍLICO EN LA PROLIFERACIÓN Y APOPTOSIS CELULAR DEL EPITELIO METAPLÁSICO DEL ESÓFAGO DE BARRETT
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2005-11-24
A randomised, double-blind, parallel-group, placebo controlled study of
CTID: null
Phase: Phase 3    Status: Completed
Date: 2005-11-07
Förekomst av syrarelaterade besvär efter utsättning av protonpumpshämmare hos friska frivilliga.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2005-07-01
Phänotypisierung und Genotypisierung von Cytochrom P450-Enzymen
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2004-12-06
PPI as an adjunct to endoscopic hemostasis for bleeding peptic ulcer a randomized clinical trial of a high vs a standard regimen for the i.v. drug infusion
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2004-10-01
An Open-label, Randomised, Multicentrlse if(down_display === 'none' || down_display === '') { icon_angle_up.style.display = 'none'; icon_angle_down.styl

Biological Data
  • Measurement of plasma ADMA and NO concentration at necropsy in sham (clean air), vehicle, and esomeprazole treated mice. Exposure to smoke increased ADMA (sham vs. vehicle) and NO while esomeprazole treatment further spiked the concentration of ADMA (*p < 0.05 vs. sham group) to modulate NO (*p < 0.05 vehicle vs. sham group; #p < 0.05 vehicle vs. Eso-L/Eso-H groups). Data is mean ± SEM from at least 5 animals per group run in replicates. Eso-L, low dose of esomeprazole (i.e. 30 mg/kg); Eso-H, high dose of esomeprazole (i.e., 300 mg/kg).[2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.
  • ELISA-based measurement of circulating TNFα, IL1β, and MMP7 concentration in the plasma of sham, vehicle, and esomeprazole treated animals. Smoke exposure increased levels of the proinflammatory cytokines (TNFα and IL1β), and the profibrotic protein MMP7 [sham (clean air) vs. vehicle]. However, therapeutic dose of esomeprazole reduced their concentration (*p < 0.05 vs. vehicle control). Data is mean ± SEM from at least 5 animals per group run in duplicates. Eso-L, low dose of esomeprazole; Eso-H, high dose of esomeprazole.[2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.
  • Fibrosis score based on scanning of multiple non-overlapping fields of Masson's Trichrome stained sections of lung tissue harvested from animals exposed to clean air (sham) or cotton smoke. The clean air exposed animals in the sham group show no fibrotic changes. However, the animals in the vehicle treated control group show higher fibrotic changes (indicated by red pie) while the animals in the therapeutic esomeprazole (Esomeprazole-L) group show normalized levels of collagen (indicated by blue pie) compared to vehicle or high-dose (Esomeprazole-H) group. Two or three slides per group were scanned and the total number of non-overlapping fields counted is shown below each pie. The averaged fibrotic score is shown as bar graph in the lower panel (*p < 0.05 vs. sham group).[2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.
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