Target Information

Target General Infomation
Target ID
T92687
Target Name
H+ K+ ATPase
Target Type
Successful
Disease Duodenal ulcers [ICD10: K25-K27]
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21]
Gastrointestinal disease [ICD10: K00-K93]
Nsaid-related gastric ulcer [ICD9: 531; ICD10: K25]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
Ulcerative colitis [ICD9: 556; ICD10: K51]
Unspecified [ICD code not available]
BioChemical Class
Hydrolases (EC:3)
UniProt ID
P20648||P51164
EC Number
EC 3.6.3.10
Drugs and Mode of Action
Drug(s) Esomeprazole Drug Info Approved Peptic ulcer [536779], [540887]
Lansoprazole Drug Info Approved Peptic ulcer [535862], [542222]
Omeprazole Drug Info Approved Gastroesophageal reflux disease [467616], [537527]
Pantoprazole Drug Info Approved Gastroesophageal reflux disease [535862], [542279]
Lansoprazole Drug Info Phase 3 Nsaid-related gastric ulcer [535862], [542222]
RQ-00000004 Drug Info Phase 3 Gastroesophageal reflux disease [549204]
TAK-438 Drug Info Phase 3 Gastroesophageal reflux disease [525119]
AZD-0865 Drug Info Phase 2 Gastrointestinal disease [521710]
S-tenatoprazole Drug Info Phase 2 Peptic ulcer [521790]
YH-4808 Drug Info Phase 2 Duodenal ulcers [523802]
LEMINOPRAZOLE Drug Info Discontinued in Preregistration Ulcerative colitis [544691]
PUMAPRAZOLE Drug Info Discontinued in Phase 3 Duodenal ulcers [545964]
SKF-96067 Drug Info Discontinued in Phase 3 Peptic ulcer [544818]
AR-H047108 Drug Info Discontinued in Phase 2 Duodenal ulcers [547136]
SORAPRAZAN Drug Info Discontinued in Phase 2 Peptic ulcer [547328]
TY-11345 Drug Info Discontinued in Phase 2 Peptic ulcer [544845]
CS-526 Drug Info Discontinued in Phase 1 Gastroesophageal reflux disease [547339]
SKF-97574 Drug Info Discontinued in Phase 1 Peptic ulcer [545026]
Saviprazole Drug Info Terminated Peptic ulcer [544684]
SK&F-95601 Drug Info Terminated Peptic ulcer [544683]
Modulator AR-H047108 Drug Info
AZD-0865 Drug Info [528510]
CS-526 Drug Info [528949]
Esomeprazole Drug Info [556264]
Lansoprazole Drug Info [556264]
LEMINOPRAZOLE Drug Info
Omeprazole Drug Info [556264]
Pantoprazole Drug Info [556264]
PUMAPRAZOLE Drug Info
RQ-00000004 Drug Info [529788]
S-tenatoprazole Drug Info
Saviprazole Drug Info [528168]
SK&F-95601 Drug Info
SKF-96067 Drug Info [1572591]
SKF-97574 Drug Info [1572591]
SORAPRAZAN Drug Info
TAK-438 Drug Info
TY-11345 Drug Info [533944]
YH-1238 Drug Info
YH-4808 Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
Ref 467616(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4279).
Ref 521710ClinicalTrials.gov (NCT00206284) A Dose-finding Phase IIb Study With AZD0865 and Esomeprazole in GERD Patients Without Erosive Esophagitis.. U.S. National Institutes of Health.
Ref 521790ClinicalTrials.gov (NCT00282555) Efficiency Study of S-Tenatoprazole-Na to Treat Erosive or Ulcerative Esophagitis. U.S. National Institutes of Health.
Ref 523802ClinicalTrials.gov (NCT01538849) Study to Investigate the Safety, Tolerability and Efficacy of YH4808 in Patients With Reflux Esophagitis. U.S. National Institutes of Health.
Ref 525119ClinicalTrials.gov (NCT02388724) Efficacy and Safety of Oral Once-Daily Vonoprazan (TAK-438) in Patients With Erosive Esophagitis. U.S. National Institutes of Health.
Ref 535862An overview of proton pump inhibitors. Gastroenterol Nurs. 2003 Sep-Oct;26(5):182-90.
Ref 536779Esomeprazole: a review of its use in the management of gastric acid-related diseases in adults. Drugs. 2008;68(11):1571-607.
Ref 537527Generic omeprazole delayed-release capsules: in vitro performance evaluations. Drug Dev Ind Pharm. 2009 Aug;35(8):917-21.
Ref 540887(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5488).
Ref 542222(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7208).
Ref 542279(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7260).
Ref 544683Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000578)
Ref 544684Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000579)
Ref 544691Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000604)
Ref 544818Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001218)
Ref 544845Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001313)
Ref 545026Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001921)
Ref 545964Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005537)
Ref 547136Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013302)
Ref 547328Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015211)
Ref 547339Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015294)
Ref 549204Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033657)
Ref
Ref 528168Gastric acid inhibitory profile of saviprazole (HOE 731) compared to omeprazole. Pharmacology. 1991;43(6):293-303.
Ref 528510Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase. Biochem Pharmacol. 2007 Jan 15;73(2):198-205. Epub 2006 Sep 24.
Ref 528949Pharmacological profile of novel acid pump antagonist 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526). J Pharmacol Exp Ther. 2007 Oct;323(1):308-17. Epub 2007 Jul 13.
Ref 529788N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-chromen-4-yl]amino}imidazo[1,2-a]pyridine-6-carboxamide (PF-03716556), a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. J Pharmacol Exp Ther. 2009 Feb;328(2):671-9.
Ref 533944Biochemical and pharmacological properties of a newly synthesized proton pump (H+/K(+)-ATPase) inhibitor, TY-11345 in experimental animals. Jpn J Pharmacol. 1993 Aug;62(4):363-71.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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