LEVOLANSOPRAZOLE

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

Structure Search

SMILES

CC1=C(OCC(F)(F)F)C=CN=C1C[S@+]([O-])C2=NC3=C(N2)C=CC=C3

InChI

InChIKey=MJIHNNLFOKEZEW-VWLOTQADSA-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-/m0/s1

HIDE SMILES / InChI

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

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdfhttps://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24773330 | https://www.ncbi.nlm.nih.gov/pubmed/25881966 | http://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihub

Dexlansoprazole (trade names Kapidex, Dexilant) is a proton pump inhibitor (PPI) that is marketed by Takeda Pharmaceuticals for the treatment of erosive esophagitis and gastro-oesophageal reflux disease. Dexlansoprazole is used to heal and maintain healing of erosive esophagitis and to treat heartburn associated with gastroesophageal reflux disease (GERD). It lasts longer than lansoprazole, to which it is chemically related, and needs to be taken less often. Dexlansoprazole is supplied for oral administration as a dual delayed-release formulation in capsules and orally disintegrating tablets. The capsules and tablets contain dexlansoprazole in a mixture of two types of enteric-coated granules with different pH-dependent dissolution profiles. The most significant adverse reactions (≥2%) reported in clinical trials were diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Potassium-transporting ATPase 38 Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11693467	Inhibitor 8504
Potassium-transporting ATPase 38 Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20974316	Inhibitor 8504
Potassium-transporting ATPase 38 Target ID: CHEMBL2095173 Sources: http://www.sciencedirect.com/science/article/pii/000629529190584R?via%3Dihub	Inhibitor 8504	5.2 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Active duodenal ulcer 6 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use Use •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 Date 2002
Gastric ulcer 74 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use Use •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 Date 2002
Gastroesophageal reflux disease 68 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use Use •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 Date 2002
Erosive esophagitis 7 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf	Primary	Approved 8583	DEXILANT Approved Use DEXILANT 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 Date 2009
Heartburn 24 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf	Curative	Approved 8583	DEXILANT Approved Use DEXILANT 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 Date 2009
Active duodenal ulcer 6 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use INDICATIONS 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 Date 2002
Gastric ulcer 74 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use INDICATIONS 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 Date 2002
Gastroesophageal reflux disease 68 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf	Primary	Approved 8583	PREVACID Approved Use INDICATIONS 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 Date 2002

C_max

Value	Dose	Analyte	Population
1705 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021566s005lbl.pdf	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
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:
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:
37.3 ng/mL/(mg dose) 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: UNKNOWN food status: UNKNOWN
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: UNKNOWN food status: UNKNOWN
33.5 ng/mL/(mg dose) 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:
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:
16.1 ng/mL/(mg dose) 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:
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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022287s031lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022287s031lbl.pdf	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
0.36 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
337 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
528 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1156 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
167 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
848.13 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
811.63 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
3192 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021566s005lbl.pdf	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
128 μg × h/L/(mg dose) 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: UNKNOWN food status: UNKNOWN
143.2 μg × h/L/(mg dose) 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: UNKNOWN food status: UNKNOWN
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:
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:
96 μg × h/L/(mg dose) 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:
87.6 μg × h/L/(mg dose) 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:
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:
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:
62 μg × h/L/(mg dose) 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:
55.5 μg × h/L/(mg dose) 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:
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:
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:
3275 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022287s031lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022287s031lbl.pdf	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
1.56 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
524 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
967 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3892 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
451 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1161.07 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1180.29 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.3 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021566s005lbl.pdf	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
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:
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:
0.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16755125/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.02 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.87 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31338800/	30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	LEVOLANSOPRAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
5.8% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8710755/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:		LEVOLANSOPRAZOLE serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

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: https://pubmed.ncbi.nlm.nih.gov/28138748	healthy, 18-29 years Health Status: healthy Age Group: 18-29 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28138748	Sources: https://pubmed.ncbi.nlm.nih.gov/28138748
90 mg single, intravenous Dose: 90 mg Route: intravenous Route: single Dose: 90 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28138748	healthy, 18-29 years Health Status: healthy Age Group: 18-29 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28138748	Sources: https://pubmed.ncbi.nlm.nih.gov/28138748
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: https://pubmed.ncbi.nlm.nih.gov/19826060	healthy, 35 years (range: 18 - 50 years) Health Status: healthy Age Group: 35 years (range: 18 - 50 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/19826060	Sources: https://pubmed.ncbi.nlm.nih.gov/19826060
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Abdominal pain... AEs leading to discontinuation/dose reduction: Abdominal pain (0.5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, 48 years (range: 18-90 years) Health Status: unhealthy Age Group: 48 years (range: 18-90 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Diarrhea, Abdominal pain... AEs leading to discontinuation/dose reduction: Diarrhea (0.7%) Abdominal pain (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (3 patients) Eructation (2 patients) Nausea (6 patients) Vomiting (6 patients) Erosive esophagitis (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
90 mg 1 times / day steady, oral Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf	Disc. AE: Dyspepsia, Eructation... AEs leading to discontinuation/dose reduction: Dyspepsia (1 patient) Eructation (1 patient) Nausea (9 patients) Vomiting (6 patients) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022287s000_MedR_P1.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf	Other AEs: Hypertension... Other AEs: Hypertension (serious) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208056lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A1 132 CYP1A2 2153 CYP2A6 879 CYP2B6 926 CYP2C8 1057 CYP2E1 1060 CYP2C19 2057	CYP2C19 1119

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A1 272	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=11 Page: 11.0	unlikely
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=13 Page: 11.0	unlikely
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=14 Page: 11.0	unlikely
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=15 Page: 11.0	unlikely
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=17 Page: 11.0	unlikely
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=18 Page: 11.0	unlikely
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=19 Page: 11.0	unlikely
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=12 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) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=12 Page: 11.0
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=16 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) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=16 Page: 11.0
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=19#page=12; https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4930293/#:~:text=Metabolism,and%2048%25%20in%20the%20feces.&text=No%20dose%20adjustments%20are%20needed,impairment%20or%20mild%20hepatic%20impairment.	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%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=19#page=12; https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4930293/#:~:text=Metabolism,and%2048%25%20in%20the%20feces.&text=No%20dose%20adjustments%20are%20needed,impairment%20or%20mild%20hepatic%20impairment.

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=10 Page: 10.0	yes
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=10 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022287s019lbl.pdf#page=10 Page: 10,12

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:6375	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6375
ChemicalBook	CB6396972	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB6396972
eMolecules	902018	https://www.emolecules.com/cgi-bin/more?vid=902018
MolPort	MolPort-003-666-508	https://www.molport.com/shop/molecule-link/MolPort-003-666-508
Selleck Chemicals	Lansoprazole	http://www.selleckchem.com/products/Lansoprazole.html
001 Chemical	DY521004	https://www.001chemical.com/chem/138530-94-6
abcr GmbH	AB455993	http://www.abcr.com/shop/en/AB455993
AbMole Bioscience	M2627	http://www.abmole.com/products/dexlansoprazole.html
Aceschem	ACF021692	https://www.aceschem.com/catalog/138530-94-6.html
Achemo Scientific Limited	AC-74368	http://www.achemo.com/search/?Keyword= 138530-94-6
Acorn PharmaTech	ACN-046381	http://www.acornpharmatech.com/
AEchem Scientific Corp., USA	AE047759	http://www.aechemsc.com/info_products/AE047759.php
AK Scientific, Inc. (AKSCI)	W0028	http://www.aksci.com/item_detail.php?cat=W0028
Alsachim	890	http://www.alsachim.com/product-C1208-glo.bal-view.html
Ambinter	Amb2444038	http://www.ambinter.com/reference/2444038
Ark Pharm	AK170558	http://www.arkpharminc.com/products/138530-94-6.html
Aurum Pharmatech LLC	Q-1374	http://www.Aurumpharmatech.com/Product/ProductDetails/Q_1374
Chem Scene	CS-2820	http://www.chemscene.com/138530-94-6.html
Chemenu	CM106762	http://www.chemenu.com/products/CM106762
ChemMol	49420692	http://www.chemmol.com/chemmol/49420692.html
ChemMol	99043051	http://www.chemmol.com/chemmol/99043051.html
Chemspace	CSSB00016993951	https://chem-space.com/CSSB00016993951
Combi-Blocks	QC-7636	http://www.combi-blocks.com/cgi-bin/find.cgi?QC-7636
DC Chemicals	DC9092	http://www.dcchemicals.com/product_show-_R_Lansoprazole.html
eNovation Chemicals	D588547	https://www.enovationchem.com/ProductDetails.asp?ProductID=D588547
eNovation Chemicals	D676423	https://www.enovationchem.com/ProductDetails.asp?ProductID=D676423
eNovation Chemicals	D762688	https://www.enovationchem.com/ProductDetails.asp?ProductID=D762688
Hairui	HR111133	http://www.hairuichem.com/en/product/138530-94-6.html
iChemical	EBD14854	http://www.ichemical.com/products/138530-94-6.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01349254	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01349254
MedChem Express	HY-13662B	https://www.medchemexpress.com/_R_-Lansoprazole.html
Molcore	MC521004	https://www.molcore.com/product/138530-94-6
Smolecule	S525777	http://www.smolecule.com/products/s525777
Synblock Inc	PB33188	http://www.synblock.com/product/138530-94-6.html
THE BioTek	bt-267370	https://www.thebiotek.com/product/inhibitors/bt-267370

PubMed

Title	Date	PubMed
Evaluation of the cost-effectiveness of Helicobacter pylori eradication triple therapy vs. conventional therapy for ulcers in Japan.	2001 Nov	11683692
[Submicroscopic aspects of the mechanism of inhibitors of H+/K+-ATPase in gastric parietal cells].	2002	12353402
Gastroesophageal reflux in children: pathogenesis, prevalence, diagnosis, and role of proton pump inhibitors in treatment.	2002	12269842
Determinants of headache in lansoprazole users in The Netherlands: results from a nested case-control study.	2002	11994030
Effect of hypergastrinemia on pancreatic carcinogenesis.	2002 Apr	11975934
Potential role of endocrine gastrin in the colonic adenoma carcinoma sequence.	2002 Aug 27	12189558
Tetany secondary to the use of a proton-pump inhibitor.	2002 Aug 6	12160379
Lansoprazole induces mucosal protection through gastrin receptor-dependent up-regulation of cyclooxygenase-2 in rats.	2002 Dec	12438555
Are proton pump inhibitors the first choice for acute treatment of gastric ulcers? A meta analysis of randomized clinical trials.	2002 Jul 15	12119060
Anaphylaxis to proton pump inhibitors.	2002 Nov-Dec	12464168
ATPase inhibitors suppress actinomycin D-induced apoptosis in leukemia cells.	2002 Sep-Oct	12530016
Formulation study for lansoprazole fast-disintegrating tablet. I. Effect of compression on dissolution behavior.	2003 Aug	12913232
Time-dependent transcriptional induction of CYP1A1, CYP1A2 and CYP1B1 mRNAs by H+/K+ -ATPase inhibitors and other xenobiotics.	2003 Feb	12623754
[New triple therapy for Helicobacter pylori infection in Japan].	2003 Jan	12607326
Safety and pharmacokinetics of oral lansoprazole in preadolescent rats exposed from weaning through sexual maturity.	2003 Jan-Feb	12507665
Does eradication of Helicobacter pylori reduce hypergastrinaemia during long term therapy with proton pump inhibitors?	2003 Mar	12762431
Structural and functional characterization of gastric mucosa and central nervous system in histamine H2 receptor-null mice.	2003 May 2	12729842
Stereoselective metabolism of lansoprazole by human liver cytochrome P450 enzymes.	2003 Oct	12975331
Formulation study for lansoprazole fast-disintegrating tablet. II. Effect of triethyl citrate on the quality of the products.	2003 Sep	12951443
Flavor and taste of lansoprazole strawberry-flavored delayed-release oral suspension preferred over ranitidine peppermint-flavored oral syrup: in children aged between 5-11 years.	2004	15035653
Effect of lansoprazole and rabeprazole on tacrolimus pharmacokinetics in healthy volunteers with CYP2C19 mutations.	2004 Aug	15285851
Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities.	2004 Aug	15258107
Aplastic anemia associated with initiation of nizatidine therapy in a hemodialysis patient.	2004 Jun	15235935
[Myoclonic encephalopathy associated with proton pump inhibitors].	2004 Mar	15037850
Identification and relative contributions of human cytochrome P450 isoforms involved in the metabolism of glibenclamide and lansoprazole: evaluation of an approach based on the in vitro substrate disappearance rate.	2004 May	15370958
Lansoprazole ameliorates intestinal mucosal damage induced by ischemia-reperfusion in rats.	2004 Oct 1	15334676
Interleukin-8 expression in the esophageal mucosa of patients with gastroesophageal reflux disease.	2004 Sep	15513378
Management of acid-related disorders in patients with dysphagia.	2004 Sep 6	15478852
Hyponatremia with consciousness disturbance associated with esomeprazole.	2005 Apr	15741423
Neuropathy associated with lansoprazole treatment.	2005 Jan	15468341
Lansoprazole-associated collagenous colitis: a case report.	2005 Jul	16001348
Laryngopharyngeal reflux: prospective cohort study evaluating optimal dose of proton-pump inhibitor therapy and pretherapy predictors of response.	2005 Jul	15995512
Enhanced ghrelin secretion in rats with cysteamine-induced duodenal ulcers.	2005 Jul	15778430
Effect of concomitant dosing of famotidine with lansoprazole on gastric acid secretion in relation to CYP2C19 genotype status.	2005 Jul 1	15963082
Lansoprazole prevents experimental gastric injury induced by non-steroidal anti-inflammatory drugs through a reduction of mucosal oxidative damage.	2005 Jul 14	15996031
Mechanisms of action of leptin in preventing gastric ulcer.	2005 Jul 21	16015682
Prediction of genotoxicity of chemical compounds by statistical learning methods.	2005 Jun	15962942
Preventive therapy for non-steroidal anti-inflammatory drug-induced ulcers in Japanese patients with rheumatoid arthritis: the current situation and a prospective controlled-study of the preventive effects of lansoprazole or famotidine.	2005 Jun	15943850
CYP35: xenobiotically induced gene expression in the nematode Caenorhabditis elegans.	2005 Jun 1	15910738
Functional involvement of PHOSPHO1 in matrix vesicle-mediated skeletal mineralization.	2007 Apr	17227223
Long-term management of gastroesophageal reflux disease with pantoprazole.	2007 Jun	18360632
Antiulcerogenic effect and acute toxicity of a hydroethanolic extract from the cashew (Anacardium occidentale L.) leaves.	2007 Jun 13	17499463
Influence of H pylori on plasma ghrelin in patients without atrophic gastritis.	2007 Mar 14	17461454
Influence of rabeprazole and lansoprazole on the pharmacokinetics of tacrolimus in relation to CYP2C19, CYP3A5 and MDR1 polymorphisms in renal transplant recipients.	2007 May	17377957
Gastroprotective and antioxidant effects of amiodarone on indomethacin-induced gastric ulcers in rats.	2007 Nov	18087811
Gastroprotective effect of mangiferin, a xanthonoid from Mangifera indica, against gastric injury induced by ethanol and indomethacin in rodents.	2007 Oct	17918041
Immune and Inflammatory Responses in GERD and Lansoprazole.	2007 Sep	18193101
Gastroprotective and antioxidant effects of montelukast on indomethacin-induced gastric ulcer in rats.	2007 Sep	17895592
Lansoprazole protects and heals gastric mucosa from non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy by inhibiting mitochondrial as well as Fas-mediated death pathways with concurrent induction of mucosal cell renewal.	2008 May 23	18375387
Hypersensitivity to proton pump inhibitors: lansoprazole-induced Kounis syndrome.	2009 May 29	18378022

Patents

Sample Use Guides

In Vivo Use Guide

Duodenal Ulcers: 15 mg Once daily for 4 weeks Gastroesophageal Reflux: 30 mg Once daily for up to 8 weeks

Route of Administration: Oral

In Vitro Use Guide

Lansoprazole is a gastric parietal cell proton pump inhibitor that is also active against Helicobacter pylori in vitro. The antimicrobial activity of lansoprazole and of its sulfenamide, a rearrangement product occurring spontaneously in acid environments, was studied by determining the MICs and MBCs for 11 cytotoxic and eight non-cytotoxic H. pylori strains and by measuring the rapidity of bacterial killing. The MIC90 and MBC90 were 2.5 mg/L and 10 mg/L, respectively, both for lansoprazole and for its sulfenamide.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:46:24 GMT 2025` Edited by `admin` on `Mon Mar 31 18:46:24 GMT 2025`
Record UNII	FB55O16184
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LANSOPRAZOLE, (S)-

Preferred Name

English

LEVOLANSOPRAZOLE

Official Name

English

levolansoprazole [INN]

Common Name

English

(-)-2-((S)-((3-METHYL-4-(2,2,2-TRIFLUOROETHOXY)PYRIDIN-2-YL)METHYL)SULFINYL)-1H-BENZAMIDAZOLE

Common Name

English

Code System Code Type Description

INN

8523