Repositioning Candidate Details
| Candidate ID: | R0126 |
| Source ID: | DB00448 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Lansoprazole |
| Synonyms: | |
| Molecular Formula: | C16H14F3N3O2S |
| SMILES: | CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 |
| Structure: |
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| DrugBank Description: | Lansoprazole marketed under the brand Prevacid, is a proton pump inhibitor (PPI) and is structurally classified as a substituted benzimidazole.[A177065] It reduces gastric acid secretion by targeting gastric H,K-ATPase pumps and is thus effective at promoting healing in ulcerative diseases, and treating gastroesophageal reflux disease (GERD) along with other pathologies caused by excessive acid secretion.[A177053] |
| CAS Number: | 103577-45-3 |
| Molecular Weight: | 369.361 |
| DrugBank Indication: | Lansoprazole is used to reduce gastric acid secretion and is approved for short term treatment of active gastric ulcers, active duodenal ulcers, erosive reflux oesophagitis, symptomatic gastroesophageal reflux disease, and non-steroidal anti-inflammatory drug (NSAID) induced gastric and duodenal ulcers. [A4892][A177065][FDA Label] It may be used in the maintenance and healing of several gastric conditions including duodenal ulcers, NSAID related gastric ulcers, and erosive esophagitis.[FDA Label] Lansoprazole prevents recurrence of gastric ulcers in patients who have a documented history of gastric ulcers who also use NSAIDs chronically. [FDA Label] Predictably, it is also useful in the management of hypersecretory conditions including Zollinger-Ellison syndrome. [FDA Label] Lansoprazole is effective at eradicating H. pylori when used in conjunction with amoxicillin and clarithromycin (triple therapy) or with amoxicillin alone (dual therapy). [FDA Label] |
| DrugBank Pharmacology: | Lansoprazole decreases gastric acid secretion by targeting H+,K+-ATPase, which is the enzyme that catalyzes the final step in the acid secretion pathway in parietal cells. [A177080] Conveniently, lansoprazole administered any time of day is able to inhibit both daytime and nocturnal acid secretion.[A177080] The result is that lansoprazole is effective at healing duodenal ulcers, reduces ulcer-related pain, and offers relief from symptoms of heartburn [A177080] Lansoprazole also reduces pepsin secretion, making it a useful treatment option for hypersecretory conditions such as Zollinger-Ellison syndrome. [A177089][A177080][F4352] |
| DrugBank MoA: | As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment to become activated. [A174244] Once protonated, lansoprazole is able to react with cysteine residues, specifically Cys813 and Cys321, on parietal H+,K+-ATPase resulting in stable disulfides. [A174244][A177077] PPI's in general are able to provide prolonged inhibition of acid secretion due to their ability to bind covalently to their targets. [A174244] |
| Targets: | Potassium-transporting ATPase alpha chain 1; Microtubule-associated protein tau |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T37 | Neurogenic locus notch homolog protein 2 | NOTCH2 | INHIBITOR | Target is a single protein chain | Q04721 | NOTCH2_HUMAN | Details |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details |