Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H14F3N3O2S |
Molecular Weight | 369.361 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C[S@@+]([O-])C2=NC3=C(N2)C=CC=C3)N=CC=C1OCC(F)(F)F
InChI
InChIKey=MJIHNNLFOKEZEW-RUZDIDTESA-N
InChI=1S/C16H14F3N3O2S/c1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22)/t25-/m1/s1
Molecular Formula | C16H14F3N3O2S |
Molecular Weight | 369.361 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22950496
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22950496
Lansoprazole is a proton pump inhibitor, which prevents the stomach from producing acid. Lansoprazole has been marketed for many years and is one of several proton-pump inhibitors (PPI's). It was used for the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastrointestinal bleeds with NSAID use. Lansoprazole belongs to a class of ant secretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but that suppress gastric acid secretion by specific inhibition of the (H+, K+ )-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. Lansoprazole is extensively metabolized in the liver. Two metabolites have been identified in measurable quantities in plasma (the hydroxylated sulfinyl and sulfone derivatives of lansoprazole). These metabolites have very little or no antisecretory activity. Lansoprazole is thought to be transformed into two active species which inhibit acid secretion by (H+, K+ )-ATPase within the parietal cell canaliculus, but are not present in the systemic circulation. The plasma elimination half-life of lansoprazole does not reflect its duration of suppression of gastric acid secretion. Thus, the plasma elimination half-life is less than two hours, while the acid inhibitory effect lasts more than 24 hours.
CNS Activity
Originator
Sources: http://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihubhttp://www.takeda.com/company/history/1985.html
Curator's Comment: # Takeda
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11693467 |
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Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20974316 |
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Target ID: CHEMBL2095173 |
5.2 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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Primary | PREVACID Approved UseUse •treats frequent heartburn (occurs 2 or more days a week) •not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect Launch Date1.0306656E12 |
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Primary | DEXILANT Approved UseDEXILANT is a proton pump inhibitor (PPI) indicated for: •Healing of all grades of erosive esophagitis (EE). (1.1) •Maintaining healing of EE and relief of heartburn. (1.2) •Treating heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD). (1.3) 1.1 Healing of Erosive Esophagitis DEXILANT is indicated for healing of all grades of erosive esophagitis (EE) for up to eight weeks. 1.2 Maintenance of Healed Erosive Esophagitis DEXILANT is indicated to maintain healing of EE and relief of heartburn for up to six months. 1.3 Symptomatic Non-Erosive Gastroesophageal Reflux Disease DEXILANT is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) for four weeks. Launch Date1.23327362E12 |
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Curative | DEXILANT Approved UseDEXILANT is a proton pump inhibitor (PPI) indicated for: •Healing of all grades of erosive esophagitis (EE). (1.1) •Maintaining healing of EE and relief of heartburn. (1.2) •Treating heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD). (1.3) 1.1 Healing of Erosive Esophagitis DEXILANT is indicated for healing of all grades of erosive esophagitis (EE) for up to eight weeks. 1.2 Maintenance of Healed Erosive Esophagitis DEXILANT is indicated to maintain healing of EE and relief of heartburn for up to six months. 1.3 Symptomatic Non-Erosive Gastroesophageal Reflux Disease DEXILANT is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) for four weeks. Launch Date1.23327362E12 |
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Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
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Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
|||
Primary | PREVACID Approved UseINDICATIONS AND USAGE. Short-Term Treatment of Active Duodenal Ulcer PREVACID is indicated for short-term treatment (up to 4 weeks) for healing and symptom relief of active duodenal ulcer.
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence.
Triple Therapy: PREVACID/amoxicillin/clarithromycin. PREVACID in combination with amoxicillin plus clarithromycin as triple therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Dual Therapy: PREVACID/amoxicillin. PREVACID in combination with amoxicillin as dual therapy, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or one-year history of a duodenal ulcer) who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
Maintenance of Healed Duodenal Ulcers PREVACID is indicated to maintain healing of duodenal ulcers. Controlled studies do not extend beyond 12 months.
Short-Term Treatment of Active Benign Gastric Ulcer PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of active benign gastric ulcer
Healing of NSAID-Associated Gastric Ulcer PREVACID IS INDICATED FOR THE TREATMENT OF NSAID-ASSOCIATED GASTRIC ULCER IN PATIENTS WHO CONTINUE NSAID USE. CONTROLLED STUDIES DID NOT EXTEND BEYOND 8 WEEKS.
Risk Reduction of NSAID-Associated Gastric Ulcer PREVACID is indicated for reducing the risk of NSAID-associated gastric ulcers in patients with a history of a documented gastric ulcer who require the use of an NSAID. Controlled studies did not extend beyond 12 weeks.
Gastroesophageal Reflux Disease (GERD) Short-Term Treatment of Symptomatic GERD PREVACID is indicated for the treatment of heartburn and other symptoms associated with GERD. Short-Term Treatment of Erosive Esophagitis PREVACID is indicated for short-term treatment (up to 8 weeks) for healing and symptom relief of all grades of erosive esophagitis. For patients who do not heal with PREVACID for 8 weeks (5-10%), it may be helpful to give an additional 8 weeks of treatment. If there is a recurrence of erosive esophagitis an additional 8-week course of PREVACID may be considered.
Maintenance of Healing of Erosive Esophagitis PREVACID is indicated to maintain healing of erosive esophagitis. Controlled studies did not extend beyond 12 months.
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome PREVACID is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome. Launch Date1.03057922E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1705 ng/mL |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1136 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
691 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
16.1 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
33.5 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
37.3 (ng/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
1005 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
559 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
964 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
658 ng/mL |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1397 ng/mL |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3192 ng × h/mL |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
143.2 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
55.5 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
87.6 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2149 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2628 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3330 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
128 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
62 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
96 (ng*h/mL)/mg Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
1914 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
15 mg 1 times / day multiple, oral dose: 15 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
2892 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3747 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01045096 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Children sex: food status: |
|
3275 ng × h/mL |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
6529 ng × h/mL |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.3 h |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANSOPRAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.59 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
|
1.66 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00847210 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: oral experiment type: multiple co-administered: |
DEXLANSOPRAZOLE plasma | Homo sapiens population: unhealthy age: Adolescents sex: food status: |
Doses
Dose | Population | Adverse events |
---|---|---|
30 mg 2 times / day multiple, intravenous Dose: 30 mg, 2 times / day Route: intravenous Route: multiple Dose: 30 mg, 2 times / day Sources: |
healthy, 18-29 years n = 18 Health Status: healthy Age Group: 18-29 years Sex: M+F Population Size: 18 Sources: |
|
90 mg single, intravenous Dose: 90 mg Route: intravenous Route: single Dose: 90 mg Sources: |
healthy, 18-29 years n = 8 Health Status: healthy Age Group: 18-29 years Sex: M+F Population Size: 8 Sources: |
|
300 mg single, oral Highest studied dose |
healthy, 35 years (range: 18 - 50 years) n = 36 Health Status: healthy Age Group: 35 years (range: 18 - 50 years) Sex: M+F Population Size: 36 Sources: |
|
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: Page: p. 35 |
Disc. AE: Abdominal pain... AEs leading to discontinuation/dose reduction: Abdominal pain (0.5%) Sources: Page: p. 35 |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 455 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 455 Sources: Page: p. 35 |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.2%) Sources: Page: p. 35 |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
Disc. AE: Diarrhea, Abdominal pain... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: Page: p. 35Abdominal pain (0.6%) |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (3 patients) Sources: Page: p. 36Eructation (2 patients) Nausea (6 patients) Vomiting (6 patients) Erosive esophagitis (1 patient) |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (1 patient) Sources: Page: p. 36Eructation (1 patient) Nausea (9 patients) Vomiting (6 patients) |
60 mg 2 times / day steady, oral Overdose Dose: 60 mg, 2 times / day Route: oral Route: steady Dose: 60 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Hypertension... Other AEs: Hypertension (serious) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Diarrhea | 0.7% Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: |
Abdominal pain | 0.5% Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 2218 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 2218 Sources: Page: p. 35 |
Diarrhea | 0.2% Disc. AE |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 455 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 455 Sources: Page: p. 35 |
Abdominal pain | 0.6% Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
Diarrhea | 0.7% Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 35 |
unhealthy, 48 years (range: 18-90 years) n = 1754 Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Population Size: 1754 Sources: Page: p. 35 |
Erosive esophagitis | 1 patient Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Eructation | 2 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Dyspepsia | 3 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Nausea | 6 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Vomiting | 6 patients Disc. AE |
60 mg 1 times / day steady, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2311 Health Status: unhealthy Age Group: adult Population Size: 2311 Sources: Page: p. 36 |
Dyspepsia | 1 patient Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Eructation | 1 patient Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Vomiting | 6 patients Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Nausea | 9 patients Disc. AE |
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: Page: p. 36 |
unhealthy, adult n = 2142 Health Status: unhealthy Age Group: adult Population Size: 2142 Sources: Page: p. 36 |
Hypertension | serious | 60 mg 2 times / day steady, oral Overdose Dose: 60 mg, 2 times / day Route: oral Route: steady Dose: 60 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | |||
Page: 11.0 |
unlikely | no (co-administration study) Comment: in vivo studies showed that DEXILANT did not have an impact on the pharmacokinetics of coadministered theophylline (CYP1A2 substrate) Page: 11.0 |
||
Page: 11.0 |
unlikely | no (co-administration study) Comment: in vivo studies showed that DEXILANT did not have an impact on the pharmacokinetics of coadministered phenytoin (CYP2C9 substrate) Page: 11.0 |
||
weak | unknown (co-administration study) Comment: The mean AUC of the active metabolite of clopidogrel was reduced by approximately 9% (mean AUC ratio was 91%, with 90% CI of 86- 97%) |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 10.0 |
yes | |||
Page: 10,12 |
yes | yes (pharmacogenomic study) Comment: mean dexlansoprazole Cmax and AUC values were up to 2 times higher in intermediate compared to extensive metabolizers; in poor metabolizers, mean Cmax was up to 4 times higher and mean AUC was up to 12 times higher compared to extensive metabolizers Page: 10,12 |
PubMed
Title | Date | PubMed |
---|---|---|
The treatment of gastroesophageal reflux disease with proton-pump inhibitors and its implications on managed care--pharmacoeconomics and its application to antisecretory drugs: a case study. | 2001 |
|
Advantage of expressing the variations in some digestive parameters as a function of gastric emptying instead of time. | 2001 |
|
Resolution of Ménétrier's disease after Helicobacter pylori eradicating therapy. | 2001 |
|
A randomized trial of lansoprazole, amoxycillin, and clarithromycin versus lansoprazole, bismuth, metronidazole and tetracycline in the retreatment of patients failing initial Helicobacter pylori therapy. | 2001 |
|
Efficacy of Helicobacter pylori eradication therapies: a single centre observational study. | 2001 |
|
[The effectiveness of 7-day combined Helicobacter eradication therapy in patients with peptic ulcer and chronic gastritis]. | 2001 |
|
Effects of lansoprazole on human gastric lipase secretion and intragastric lipolysis in healthy human volunteers. | 2001 |
|
[Administration of proton pump inhibitor caused esophageal stenosis in two patients with severe reflux esophagitis]. | 2001 Aug |
|
Helicobacter pylori eradication treatment does not benefit patients with nonulcer dyspepsia. | 2001 Aug |
|
High-dose proton-pump inhibitors as a diagnostic test of gastro-oesophageal reflux disease in endoscopic-negative patients. | 2001 Aug |
|
Efficacy of ecabet sodium for Helicobacter pylori eradication triple therapy in comparison with a lansoprazole-based regimen. | 2001 Aug |
|
Comparative pharmacokinetics and pharmacodynamics of lansoprazole oral capsules and suspension in healthy subjects. | 2001 Aug 15 |
|
Healing and relapse rates in gastroesophageal reflux disease treated with the newer proton-pump inhibitors lansoprazole, rabeprazole, and pantoprazole compared with omeprazole, ranitidine, and placebo: evidence from randomized clinical trials. | 2001 Jul |
|
Pseudomembranous colitis without diarrhoea following Helicobacter pylori eradication therapy. | 2001 Jul |
|
Impact of a formulary change in proton pump inhibitors on health care costs and patients' symptoms. | 2001 Jul |
|
Effects on 24-hour intragastric pH: a comparison of lansoprazole administered nasogastrically in apple juice and pantoprazole administered intravenously. | 2001 Jul |
|
Cost-effectiveness of proton-pump inhibitors for maintenance therapy of erosive reflux esophagitis. | 2001 Jul 15 |
|
Follow-up of Helicobacter pylori status by using 13C-urea breath test in nonulcer dyspeptic patients after eradication therapy. | 2001 Jun |
|
[Bifid median nerve in the carpal tunnel: integrated imaging]. | 2001 Jun |
|
CYP2C19 genotype and pharmacokinetics of three proton pump inhibitors in healthy subjects. | 2001 Jun |
|
Factors associated with non-response in proton pump inhibitor users: a study of lansoprazole therapy. | 2001 Jun |
|
Inhibition of hyphal growth of Candida albicans by activated lansoprazole, a novel benzimidazole proton pump inhibitor. | 2001 Jun |
|
New-generation proton pump inhibitors: overcoming the limitations of early-generation agents. | 2001 May |
|
Proton pump inhibitor resistance in the treatment of laryngopharyngeal reflux. | 2001 Oct |
|
Are children with cystic fibrosis who are treated with a proton-pump inhibitor at risk for vitamin B(12) deficiency? | 2001 Sep |
|
Effects of therapy with lansoprazole on intestinal permeability and inflammation in young cystic fibrosis patients. | 2001 Sep |
|
Review article: managing the dyspeptic patient--an interactive discussion. | 2001 Sep |
|
Review article: tackling the "dyspeptic problem". | 2001 Sep |
|
Review article: long-term use of proton pump inhibitors in GORD--help or hindrance? | 2001 Sep |
|
Lansoprazole in children: pharmacokinetics and efficacy in reflux oesophagitis. | 2001 Sep |
|
Bedtime H2 blockers improve nocturnal gastric acid control in GERD patients on proton pump inhibitors. | 2001 Sep |
|
Drug treatments in upper gastrointestinal bleeding: value of endoscopic findings as surrogate end points. | 2001 Sep |
|
Does short-term treatment with proton pump inhibitors cause rebound aggravation of symptoms? | 2001 Sep |
|
Clinical and ethical concerns about switching patient treatment to "therapeutically interchangeable" medications. | 2001 Sep 24 |
|
Noninvasive Helicobacter pylori testing for the "test-and-treat" strategy: a decision analysis to assess the effect of past infection on test choice. | 2001 Sep 24 |
|
Gastroesophageal reflux disease presenting as xerophthalmia. | 2001 Sep-Oct |
|
Enantioselective disposition of lansoprazole in extensive and poor metabolizers of CYP2C19. | 2002 Jul |
|
Pharmacokinetic differences between the enantiomers of lansoprazole and its metabolite, 5-hydroxylansoprazole, in relation to CYP2C19 genotypes. | 2004 Nov |
|
Lansoprazole enantiomer activates human liver microsomal CYP2C9 catalytic activity in a stereospecific and substrate-specific manner. | 2005 Feb |
|
Stereoselective inhibition of cytochrome P450 forms by lansoprazole and omeprazole in vitro. | 2005 Jan |
|
Enantioselective disposition of lansoprazole in relation to CYP2C19 genotypes in the presence of fluvoxamine. | 2005 Jul |
|
Effect of clarithromycin on the enantioselective disposition of lansoprazole in relation to CYP2C19 genotypes. | 2005 Jun |
|
Comparison of enantioselective disposition of rabeprazole versus lansoprazole in renal-transplant recipients who are CYP2C19 extensive metabolizers. | 2005 May |
|
Influence of ABCB1 C3435T polymorphism on the pharmacokinetics of lansoprazole and gastroesophageal symptoms in Japanese renal transplant recipients classified as CYP2C19 extensive metabolizers and treated with tacrolimus. | 2006 Dec |
|
Intestinal CYP3A4 is not involved in the enantioselective disposition of lansoprazole. | 2006 Jan |
|
Enantioselective disposition of lansoprazole and rabeprazole in human plasma. | 2006 Jun |
|
Estimation of the area under the concentration-time curve of racemic lansoprazole by using limited plasma concentration of lansoprazole enantiomers. | 2008 May |
|
Delayed release dexlansoprazole in the treatment of GERD and erosive esophagitis. | 2009 |
|
Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. | 2009 |
|
New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part II. | 2009 Dec |
Patents
Sample Use Guides
For erosive esophagitis: One 60 mg capsule once daily for up to 8 weeks
Relief of Heartburn: One 30 mg capsule once daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24887303
A stably transfected gene reporter cell line AZ-AHR, derived from human hepatoma HepG2 cells transfected with a construct containing several AhR binding sites upstream of a luciferase reporter gene, was used for assessment of AhR transcriptional activity. Cells were incubated for 24 h with DEXLANSOPRAZOLE and/or vehicle (DMSO; 0.1% v/v), in the presence or absence of TCDD (10 nM; AZ-AHR cells) or DEX (100 nM; AZ-GR cells). After the treatments, cells were lysed and luciferase activity was measured. In parallel, cell viability was determined by conventional MTT test.
Substance Class |
Chemical
Created
by
admin
on
Edited
Thu Jul 06 00:01:57 UTC 2023
by
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on
Thu Jul 06 00:01:57 UTC 2023
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Record UNII |
UYE4T5I70X
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Validated (UNII)
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NDF-RT |
N0000000147
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WHO-VATC |
QA02BC06
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NCI_THESAURUS |
C29723
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WHO-ATC |
A02BC06
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N0000175525
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LIVERTOX |
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816346
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SUB31929
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Dexlansoprazole
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DEXLANSOPRAZOLE
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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BINDER->LIGAND |
BINDING
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RACEMATE -> ENANTIOMER |
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|
SOLVATE->ANHYDROUS |
|
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|
SALT/SOLVATE -> PARENT |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
MINOR
FECAL
|
||
|
METABOLITE ACTIVE -> PRODRUG |
|
||
|
METABOLITE -> PARENT |
MINOR
FECAL
|
||
|
METABOLITE -> PARENT |
In poor metabolizer; mediator: CYP3A
MAJOR
PLASMA
|
||
|
METABOLITE -> PARENT |
Minor in plasma
MAJOR
FECAL
|
||
|
METABOLITE -> PARENT |
EM sujects
MAJOR
PLASMA; URINE
|
||
|
METABOLITE -> PARENT |
EM Subjects
MAJOR
PLASMA; URINE
|
||
|
METABOLITE -> PARENT |
PM sujects
MAJOR
URINE
|
||
|
METABOLITE -> PARENT |
Extensive metabolizers
MINOR
URINE
|
||
|
METABOLITE -> PARENT |
EM Subjects
MAJOR
PLASMA
|
||
|
METABOLITE ACTIVE -> PRODRUG |
|
||
|
METABOLITE -> PARENT |
MINOR
FECAL; PLASMA
|
||
|
METABOLITE -> PARENT |
MINOR
PLASMA; URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
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