Page last updated: 2024-11-04

omeprazole

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Description

Omeprazole is a proton pump inhibitor (PPI) medication that is used to treat conditions like heartburn, ulcers, and gastroesophageal reflux disease (GERD). Its synthesis involves a multi-step process starting with the reaction of benzimidazole with substituted pyridines. It acts by irreversibly blocking the hydrogen potassium adenosine triphosphatase (H+/K+ ATPase) enzyme in the stomach lining, thereby inhibiting the production of stomach acid. Omeprazole is widely studied for its efficacy in managing acid-related disorders, its safety profile, and potential applications in other medical conditions. Its importance lies in its effectiveness in alleviating symptoms and promoting healing in patients with these conditions. Researchers continue to investigate its long-term effects, optimal dosing, and potential interactions with other medications.'

Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID4594
CHEMBL ID1503
CHEBI ID77260
CHEBI ID91766
CHEBI ID7772
SCHEMBL ID1191
SCHEMBL ID11995456
MeSH IDM0015293

Synonyms (379)

Synonym
BIDD:GT0189
AC-401
MLS001076112
HMS3394G17
HMS3269D17
BRD-A55962179-001-04-9
5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl)benzimidazole
5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methylsulfinyl]-1h-benzimidazole
agi-010
nuclosina
omeprazone
dm-3458
san-15
omepradex
h-168/68
omez
emilok
omesek
nopramin
omed
ortanol
omisec
erbolin
zimor
zefxon
nilsec
pepticus
paprazol
omeprazolum [inn-latin]
parizac
ccris 7099
ompanyt
miol
exter
secrepina
ulcozol
pepticum
prysma
lomac
2-(((3,5-dimethyl-4-methoxy-2-pyridyl)methyl)sulfinyl)-5-methoxy-1h-benzimidazole
antra mups
omz ,
h168/68
miracid
morecon
omizac
ceprandal
desec
zoltum
ozoken
epirazole
demeprazol
audazol
omeprazon
prazentol
omid
ulsen
logastric
danlox
1h-benzimidazole, 5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)sulfinyl)-
gasec
proclor
emeproton
prilosec
omeprol
ulcometion
prazidec
inhipump
ulcsep
prazolit
ulzol
2-({[3,5-dimethyl-4-(methyloxy)pyridin-2-yl]methyl}sulfinyl)-5-(methyloxy)-1h-benzimidazole
dizprazol
hsdb 3575
ulceral
omezolan
victrix
mepral
h 168/68
gastroloc
zepral
antra
elgam
losec
gibancer
omepral
omebeta 20
result
omegast
mopral
omeprazol [inn-spanish]
ramezol
belmazol
olexin
aulcer
ocid
indurgan
osiren
peptilcer
sanamidol
regulacid
ultop
tedec ulceral
procelac
dudencer
omapren
ulcesep
inhibitron
( -)-omeprazole
omep
lensor
gastrimut
omezol
5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1h-benzimidazole
zegerid
IDI1_032523
PRESTWICK_808 ,
cas-73590-58-6
NCGC00016925-01
BSPBIO_000385
PRESTWICK2_000493
119141-88-7
UPCMLD-DP075:001
MLS001424148
C07324
73590-58-6
omeprazole
omeprazole, solid
UPCMLD-DP075
DB00338
D00455
prilosec (tn)
omeprazole (jp17/usp/inn)
BPBIO1_000425
NCGC00021522-04
NCGC00021522-03
smr000058847
MLS000069373 ,
MAYBRIDGE4_002645
SPBIO_002306
PRESTWICK0_000493
PRESTWICK1_000493
PRESTWICK3_000493
NCGC00021522-05
NCGC00016925-02
h 16868
HMS2090F11
HMS2052G17
HMS2090E16
HMS1528I05
5-methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole
6-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl)-1h-benzo[d]imidazole
5-methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole(omeprazole)
(rs)-6-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl)-1h-benzo[d]imidazole
5-methoxy-2-(2-(4-methoxy-3,5-dimethylpyridin-2-yl)ethylsulfinyl)-1h-benzo[d]imidazole
bdbm50241343
2-(3-methoxy-2,4-dimethylbenzylsulfinyl)-6-methoxy-1h-benzo[d]imidazole
(omeprazole)5-methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole
5-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl)-1h-benzo[d]imidazole
5-methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-1h-benzoimidazole (omeprazole)
cid_4594
O0359 ,
CHEMBL1503 ,
chebi:77260 ,
nsc-751450
nsc-759192
AKOS005066653
FT-0652860
FT-0653294
HMS1569D07
6-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1h-benzimidazole
STK623746
NCGC00016925-06
6-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]-1h-benzimidazole
6-methoxy-2-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl]-1h-benzimidazole
A837865
5-methoxy-2-((s)-((4-methoxy-3,5-dimethyl-2- pyridinyl)methyl)sulfinyl)-
A19447
HMS2096D07
omeprazol
kg60484qx9 ,
nsc 751450
omeprazole [usan:usp:inn:ban:jan]
omeprazole delayed-release
omeprazolum
gastrogard
nsc 759192
(+-)-omeprazole
unii-kg60484qx9
NCGC00258063-01
tox21_200509
pharmakon1600-01505693
nsc759192
dtxcid501080
tox21_110686
dtxsid6021080 ,
esomperazole
5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methanesulfinyl]-1h-1,3-benzodiazole
nsc751450
(rs)-5-methoxy-2-(4-methoxy-3,5-dimethyl-2-pyridylmethylsulphinyl)benzimidazole
HMS2232B21
CCG-101130
NCGC00016925-08
NCGC00016925-05
NCGC00016925-03
NCGC00016925-04
NCGC00016925-07
FT-0601585
FT-0689771
NCGC00016925-10
S1389
AKOS015895343
gtpl4279
5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methane]sulfinyl}-1h-1,3-benzodiazole
omeprazole [orange book]
omeprazole [usp monograph]
omeprazole [inn]
omeprazole [who-dd]
omeprazole component of zegerid
omeprazole [mart.]
5-methoxy-2-(((4-methoxy-3,5,-dimethyl-2-pyridinyl)-methyl)sulphinyl)-1h-benzimidazole
yosprala component omeprazole
omeprazole [hsdb]
omeprazole [jan]
5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]benzimidazole
omeprazole [vandf]
omeprazole [usp impurity]
omeprazole [usp-rs]
omeprazole [mi]
omeprazole component of yosprala
omeprazole [green book]
(rs)-6-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl)-1h-benzo(d)imidazole
omeprazole [usan]
zegerid component omeprazole
(r)-5-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)-1h-benzo[d]imidazole
CCG-213517
DL-462
CS-1868
HY-B0113
MLS006010400
NC00380
BBL028172
SCHEMBL1191
tox21_110686_1
NCGC00016925-11
HS-0055
6-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1h-benzimidazole
5-methoxy 2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1 h-benzimidazole
5-methoxy 2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1h-benzimidazole
6-methoxy-2-[[(4methoxy-3,5-dimethyl2-pyridinyl)methyl]sulfinyl]-1h-benzimidazole
5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulphinyl]-1h-benzimidazole
5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1h-benzimidazole
5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl- 1h-benzimidazole
6-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1h-benzimidazole
5-methoxy-2-[[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl]sulfinyl]-1h-benzimidazole
6-methoxy-2-[[(4-methoxy3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1h-benzimidazole
(-)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-sulfinyl]-1h-benzimidazole
(+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-sulfinyl]-1h-benzimidazole
6-methoxy-2-[[(4-methoxy-3,5dimethyl-2-pyridinyl)-methyl]sulfinyl]-1h-benzimidazole
5-methoxy-2-[[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulphinyl]1h-benzimidazole
esomeprazole sodium salt
5-methoxy 2-[[(4-methoxy-3,5-dimethyl-2-pyrdinyl)-methyl]sulfinyl]-1h-benzimidazole
F0001-2386
6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)-1h-benzo[d]imidazole
omerprazole
MLS006011759
326602-80-6
SCHEMBL11995456
omeprazen
(.+/-.)-omeprazole
omeprazole pellets
5-methoxy-2-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl]-3h-benzoimidazole
OPERA_ID_1863
mfcd00083192
omebeta
olit
omeprazole 13cd3
AC-4676
CHEBI:91766
omeprazole, united states pharmacopeia (usp) reference standard
omeprazole, analytical reference material
HMS3651A11
5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-benzimidazole
2,3,5-trimethylpyridine/omeprazole
bdbm50103597
omeprazole, pharmaceutical secondary standard; certified reference material
omeprazole, european pharmacopoeia (ep) reference standard
omeprazole for peak identification, european pharmacopoeia (ep) reference standard
SR-01000003003-8
SR-01000003003-4
SR-01000003003-7
sr-01000003003
SBI-0206896.P001
HMS3713D07
5-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)-1h-benzo[d]imidazole
omeprazole, british pharmacopoeia (bp) reference standard
SW196942-4
FT-0673283
BCP05852
h 199
BCP21299
Q422210
73590-58-6 (free form)
SY077145
1h-benzimidazole,5-methoxy-2-[(r)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-
Z1501475006
omesec
omeprazole (prilosec)
HMS3677J07
5-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl)
omeprazole,(s)
6-methoxy-2-(((4-methoxy-3,5-dimethyl pyridin-2-yl)methyl)sulfinyl)-1h-benzo[d]imidazole
BCP13592
HMS3413J07
BRD-A88691025-001-07-4
BRD-A55962179-001-20-5
BRD-A55962179-001-08-0
EN300-117238
AMY30573
aisi'aomeilazuona esomeprazole sodium
omeprazole-[d3]
A892647
1h-benzimidazole,6-methoxy-2-[(r)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-
(s)-5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-3h-benzoimidazole
SY009746
mfcd23135254
A937349
BO164173
omeprazole - bio-x
leader omeprazole
omeprazole (usp impurity)
core values omeprazole
quality choice omeprazole
equaline omeprazole delayed release
family wellness omeprazole
omeprazole (mart.)
harris teeter omeprazole
caring mill omeprazole
sunmark omeprazole
(rs)-5-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)-1h-benzimidazole
kirkland signature omeprazole
5-methoxy-2-
good sense omeprazole
rac-5-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)-1h-benzimidazole
topcare omeprazole delayed release
up and up omeprazole
5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)sulfinyl)-1h-benzimidazole
a02bc01
careone omeprazole
equaline omeprazole
dg health omeprazole
omeprazoledr
24 hr omeprazole
good neighbor pharmacy omeprazole
omeprazole (usp monograph)
omeprazole dr
care one omeprazole
topcare omeprazole
omeprazol (inn-spanish)
omeprazolo
omeprazolum (inn-latin)
health mart omeprazole
berkley and jensen omeprazole
welby omeprazole
omeprazole (usan:usp:inn:ban:jan)
dg health omperazole
exchange select omeprazole
members mark omeprazole
ulcergard
foster and thrive omeprazole
good now omeprazole
chebi:7772
sound body omeprazole
equate omeprazole delayed release
signature care omeprazole
omeprazoledelayed release
omeprazole (usp-rs)
equate omeprazole delayed releaseacid reducer
good sense omeprazole delayed release

Research Excerpts

Overview

Omeprazole (OPZ) is a proton pump inhibitor commonly used for the treatment of gastric acid hypersecretion. It irreversibly binds to H+-K+ ATPase enzyme system in the gastric parietal cells. Little is known about its possible liver protective effects.

ExcerptReferenceRelevance
"Omeprazole (OMZ) is a proton pump inhibitor that is used to reduce gastric acid secretion, but little is known about its possible liver protective effects. "( Omeprazole Increases Survival Through the Inhibition of Inflammatory Mediaters in Two Rat Sepsis Models.
Hashimoto, Y; Hatta, M; Kaibori, M; Kotsuka, M; Nakatake, R; Nishizawa, M; Okumura, T; Okuyama, T; Sekimoto, M; Yoshida, T, 2022
)
3.61
"Omeprazole (OPZ) is a proton pump inhibitor commonly used for the treatment of gastric acid hypersecretion. "( Evidence for Metabolic Activation of Omeprazole In Vitro and In Vivo.
Hu, Z; Peng, Y; Shi, J; Su, M; Sun, C; Zhao, Y; Zheng, J, 2022
)
2.44
"Omeprazole is a part of PPIs most commonly prescribed worldwide; it irreversibly binds to H+-K+ ATPase enzyme system in the gastric parietal cells to reduce secretion of H+ ions into the lumen of stomach."( Long-Term Use of Omeprazole: Effect on Haematological and Biochemical Parameters.
Al Ali, HS; Ibrahim, NK; Jabbar, AS; Neamah, NF, 2022
)
1.78
"Omeprazole (OM) is a proton pump inhibitor from the benzimidazole group used for treatment of gastric acid-related disorders (2)."( Occupational Airborne Contact Dermatitis Caused by Omeprazole.
Balić, A; Bartolić, L; Jurakić Tončić, R; Ljubojević Hadžavdić, S; Pavičić, B; Petković, M; Žužul, K, 2019
)
1.49
"Omeprazole is a proton pump inhibitor which is reported to have antiparasitic properties."( Assessment of the potential therapeutic effects of omeprazole in Schistosoma mansoni infected mice.
Abdel Ghaffar, AE; Alshenawy, HA; Elgendy, DI; Ellakany, AR, 2019
)
1.49
"Omeprazole is a commonly used drug in patients with ulcerative colitis (UC). "( Pharmacokinetics of omeprazole in rats with dextran sulfate sodium-induced ulcerative colitis.
Dong, L; Hu, N; Jiang, Y; Ling, J; Zhou, Q; Zou, S, 2020
)
2.32
"Omeprazole (OME) is a representative of proton pump inhibitors and widely used in anti-ulcer treatment. "( A potential drug combination of omeprazole and patchouli alcohol significantly normalizes oxidative stress and inflammatory responses against gastric ulcer in ethanol-induced rat model.
Chen, YR; Guo, YL; Wang, B; Wang, ZC; Xie, L; Zhang, LY; Zhang, T, 2020
)
2.28
"Omeprazole is a proton pump inhibitor that is used in acid suppression therapy in infants. "( Rectal Omeprazole in Infants With Gastroesophageal Reflux Disease: A Randomized Pilot Trial.
Bestebreurtje, P; de Koning, BAE; de Wildt, SN; Knibbe, CAJ; Plötz, FB; Roeleveld, N; Tibboel, D; van de Ven, CP; van Groen, B, 2020
)
2.46
"Omeprazole is a proton pump inhibitor (PPI) that is used in acid suppression therapy in infants. "( Development and Stability Study of an Omeprazole Suppository for Infants.
Bestebreurtje, P; de Wildt, SN; Knibbe, CAJ; Plötz, FB; Roeleveld, N; van Sorge, AA, 2020
)
2.27
"Omeprazole is a potent inhibitor of gastric acid secretion. "( Ultrastructural intestinal mucosa change after prolonged inhibition of gastric acid secretion by omeprazole in male rats.
Chamniansawat, S; Kampuang, N; Suksridechacin, N; Thongon, N, 2021
)
2.28
"Omeprazole is a common proton pump inhibitor that interferes with the hepatic activation of clopidogrel and potentially reduces its platelet-inhibitory effect. "( Omeprazole-clopidogrel interaction and neurovascular complications after flow-diverter device placement.
Albuquerque, FC; Baranoski, JF; Catapano, JS; Cole, TS; Ducruet, AF; Fredrickson, VL; Lundberg, JN; Rahmani, R; Rutledge, C; Srinivasan, VM; Wakim, AA, 2022
)
3.61
"Omeprazole is a widely used over-the-counter (20 mg) proton pump inhibitor, usually supplied as oral enteric-coated pellets intended to release at pH 5.5 and higher; however, it is sensitive to acidic pH. "( Effect of Elevated pH on the Commercial Enteric-Coated Omeprazole Pellets Resistance: Patent Review and Multisource Generics Comparison.
Katynska, M; Mohylyuk, V; Patel, K; Sirko, V; Yerkhova, A, 2021
)
2.31
"Omeprazole is a proton pump inhibition and ranitidine is an H2 histamine receptor antagonist widely used in the treatment of gastroesophageal reflex disease, peptic ulcer disease, Zollinger-Ellison syndrome and as a protector of the gastric mucosae. "( Occupational contact allergy to omeprazole and ranitidine.
Herrera-Mozo, I; Martí-Amengual, G; Sanz-Gallen, P, 2017
)
2.18
"Omeprazole is a proton pump inhibition and ranitidine is an H2 histamine receptor antagonist widely used in the treatment of gastroesophageal reflex disease, peptic ulcer disease, Zollinger-Ellison syndrome and as a protector of the gastric mucosae. "( Occupational contact allergy to omeprazole and ranitidine.
Herrera-Mozo, I; Martí-Amengual, G; Sanz-Gallen, P, 2017
)
2.18
"Omeprazole is a widely prescribed proton pump inhibitor to treat various gastric acid hyper secretion disorders. "( Renal clearance and urinary excretion of omeprazole in healthy female volunteers in Pakistan.
Asharaf, S; Hussain, RA; Khaliq, T; Noor, N; Qadir, N; Raza, A; Shah, GA, 2017
)
2.16
"Omeprazole is a proton pump inhibitor used for decreasing gastric acid production."( A pharmacokinetic model of drug-drug interaction between clopidogrel and omeprazole at CYP2C19 in humans.
Lohitnavy, M; Lohitnavy, O; Morasuk, T; Tangamornsuksan, W; Thiansupornpong, P, 2017
)
1.41
"Omeprazole is a proton pump inhibitor used to treat the symptoms of gastro esophageal reflux disease, ulcers, excess stomach acid, infection with Helicobacter pylori, and to control the gastric side effects of various drugs. "( To Flavor or Not to Flavor Extemporaneous Omeprazole Liquid.
Chuong, MC; Kerr, SG; Taglieri, CA,
)
1.84
"Omeprazole is a proton pump inhibitor that inhibits gastric acid secretion and, theoretically, may cause the premature release of cysteamine by increasing intragastric pH, thereby affecting the PK of CBDR."( A Phase 1 Pharmacokinetic Study of Cysteamine Bitartrate Delayed-Release Capsules Following Oral Administration with Orange Juice, Water, or Omeprazole in Cystinosis.
Armas, D; Brannagan, M; Checani, GC; Confer, NF; Holt, RJ; Obaidi, M; Xie, Y, 2018
)
1.4
"Omeprazole (OME) is a proton pump inhibitor used for the treatment of various gastric and intestinal disease; however, studies on its effects on the genetic materials are still restricted. "( Toxicogenetic study of omeprazole and the modulatory effects of retinol palmitate and ascorbic acid on Allium cepa.
Ali, ES; Alves, LBDS; Braga, AL; da Mata, AMOF; Das, AK; de Lima, RMT; de Meneses, APM; Dev, S; Dos Reis, AC; E Sousa, JMC; Islam, MT; Khan, IN; Melo-Cavalcante, AAC; Mishra, SK; Mubarak, MS; Paz, MFCJ; Rouf, R; Santos, JVO; Shaw, S; Shil, MC; Shilpi, JA; Uddin, SJ, 2018
)
2.23
"Omeprazole is a well-established and most studied drug in the PPI class."( Reliving 25 years of Experience with Omeprazole in Acid-peptic Diseases.
Sharma, P, 2018
)
1.48
"Omeprazole is an important cause of drug-induced acute interstitial nephritis (AIN). "( Omeprazole-induced acute interstitial nephritis: a possible Th1-Th17-mediated injury?
Berney-Meyer, L; Hung, N; Kitching, AR; Schollum, JB; Slatter, T; Walker, RJ, 2014
)
3.29
"Omeprazole is a proton pump inhibitor for the treatment of gastric acid-related disorders. "( Sensitization to omeprazole in the occupational setting.
Björkheden, C; Cederbrant, K; Ghatan, PH; Lundborg, P; Marcusson-Ståhl, M; Matura, M, 2014
)
2.18
"Omeprazole is a proton pump inhibitor used in the treatment of peptic ulcer disease and gastrosophageal reflux disease and acts by irreversibly blocking ATP4A, a P-type H+/K+ ATPase in gastric parietal cells. "( Omeprazole, a gastric proton pump inhibitor, inhibits melanogenesis by blocking ATP7A trafficking.
Ichihashi, M; Karaman-Jurukovska, N; Matsui, MS; Muizzuddin, N; Niki, Y; Petris, MJ; Yarosh, DB, 2015
)
3.3
"Omeprazole is a proton pump inhibitor which is mainly metabolized by cytochrome P450 2C19 (CYP2C19)."( Hydroxylation index of omeprazole in relation to CYP2C19 polymorphism and sex in a healthy Iranian population.
Ghahremani, MH; Payan, M; Rouini, MR; Tahvilian, R; Tajik, N, 2014
)
1.43
"Omeprazole (OME) is a proton pump inhibitor with a 58% bioavailability after a single oral dose. "( Improvement and validation of a high-performance liquid chromatography in tandem mass spectrometry method for monitoring of omeprazole in plasma.
Abad-Santos, F; Gil García, AI; Ochoa-Mazarro, D; Román-Martínez, M; Ruiz-Nuño, A; Wojnicz, A, 2015
)
2.07
"Omeprazole is an acid suppressant and CYP2C9, CYP3A4, and CYP2C19 substrate and inhibitor, as well as inhibitor of transporters (like P-gp)."( Effect of Omeprazole on the Pharmacokinetics of Rosuvastatin in Healthy Male Volunteers.
Ahmad, L; Iqbal, Z; Khan, A; Khan, MI; Khuda, F; Shah, Y,
)
1.26
"Omeprazole (OM) is a proton pump inhibitor that is used to treat humans with gastric acid related disorders."( Omeprazole Attenuates Pulmonary Aryl Hydrocarbon Receptor Activation and Potentiates Hyperoxia-Induced Developmental Lung Injury in Newborn Mice.
Jiang, W; Moorthy, B; Patel, A; Shivanna, B; Wang, L; Welty, SE; Zhang, S, 2015
)
2.58
"Omeprazole (Prilosec®) is a selective and irreversible proton pump inhibitor used to treat various medical conditions related to the production of excess stomach acids. "( Site selective syntheses of [(3)H]omeprazole using hydrogen isotope exchange chemistry.
Pollack, SR; Schenk, DJ,
)
1.85
"Omeprazole (OM) is an aryl hydrocarbon receptor (AhR) agonist and a proton pump inhibitor that is used to treat humans with gastric acid related disorders. "( Omeprazole induces heme oxygenase-1 in fetal human pulmonary microvascular endothelial cells via hydrogen peroxide-independent Nrf2 signaling pathway.
Maturu, P; Moorthy, B; Patel, A; Shivanna, B; Shrestha, AK; Zhang, S, 2016
)
3.32
"Omeprazole is a drug used for treating gastro-oesophageal reflux disease and duodenal ulcers. "( Omeprazole alleviates benzo[a]pyrene cytotoxicity by inhibition of CYP1A1 activity in human and mouse hepatoma cells.
Kawanishi, M; Ohsako, S; Shiizaki, K; Yagi, T, 2008
)
3.23
"Omeprazole is a selective inhibitor of gastric acid secretion and is one of the most widely prescribed drugs internationally. "( Analysis of omeprazole and its main metabolites by liquid chromatography using hybrid micellar mobile phases.
Carda-Broch, S; Esteve-Romero, J; Rambla-Alegre, M, 2009
)
2.17
"Omeprazole is a proton-pump inhibitor recently approved in the United States for the treatment of gastric ulcer disease in horses. "( Evaluation of the effects of omeprazole on physiological indices of performance of horses during incremental treadmill exercise.
Cox, K; Jones, J; Kollias-Baker, C, 2001
)
2.04
"Omeprazole is a mainstay of therapy for gastroesophageal reflux disease (GERD) and gastritis, and is increasingly used as an over-the-counter remedy for dyspepsia. "( Antioxidant pre-treatment prevents omeprazole-induced toxicity in an in vitro model of infectious gastritis.
Blass, AL; Kohler, JE; Liu, J; Soybel, DI; Tai, K, 2010
)
2.08
"Omeprazole is a potent CYP2C19 inhibitor."( Omeprazole preferentially inhibits the metabolism of (+)-(S)-citalopram in healthy volunteers.
Coelho, EB; Lanchote, VL; Rocha, A; Sampaio, SA, 2010
)
2.52
"Omeprazole is a proton pump inhibitor with proven efficacy in the prevention and treatment of PUD."( Prophylactic use of omeprazole associated with a reduced risk of peptic ulcer disease among maintenance hemodialysis patients.
Chang, CT; Hsu, WM; Huang, CC; Kuo, HL; Liang, CC; Lin, HH; Liu, JH; Wang, IK; Yeh, HC, 2011
)
1.41
"Omeprazole is a proton pump inhibitor, a widely used drug to treat ulcers and gastroesophageal refluxdisease. "( Anti-carcinogenic properties of omeprazole against human colon cancer cells and azoxymethane-induced colonic aberrant crypt foci formation in rats.
Li, Q; Patlolla, JM; Rao, CV; Steele, VE; Zhang, Y, 2012
)
2.11
"Omeprazole is a very widely used proton-pump inhibitor. "( Comparative bioavailability of two oral formulations of omeprazole.
Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Herrera, JE; Medina-Santillán, R; Reyes-García, G, 2009
)
2.04
"Omeprazole is a drug used in the prophylaxis of the gastrointestinal bleeding in these patients, but its cardiovascular effects are unknown."( [Hemodynamic effects of intravenous omeprazole in critically ill children].
Botrán, M; Del Castillo, J; Garrido, B; López-Herce, J; Solana, MJ; Urbano, J, 2013
)
1.39
"Omeprazole is a potent inhibitor of gastric acid secretion. "( Comparison of oral omeprazole and endoscopic ethanol injection therapy for prevention of recurrent bleeding from peptic ulcers with nonbleeding visible vessels or fresh adherent clots.
Jung, HK; Jung, SA; Kim, DY; Lee, HC; Moon, IH; Son, HY; Yi, SY; Yoo, K, 2002
)
2.09
"Esomeprazole is an effective agent in the treatment of gastroesophageal reflux disease (GERD) and erosive esophagitis."( Esomeprazole: update and clinical review.
Baker, DE, 2002
)
1.59
"Omeprazole is a class referred to as proton pump inhibitor; it acts to regulate acid production in the stomach and is used to treat various acid-related gastrointestinal disorders. "( Stereospecific analysis of omeprazole in human plasma as a probe for CYP2C19 phenotype.
Higaki, M; Kanazawa, H; Mashige, F; Nakahara, K; Okada, A; Yokota, H, 2003
)
2.06
"Esomeprazole is an enantiomorph of omeprazole, which inhibits gastric acid secretion more effectively than omeprazole. "( Antimicrobial activity of esomeprazole versus omeprazole against Helicobacter pylori.
D'Anna, L; Figura, N; Gatta, L; Holton, J; Miglioli, M; Perna, F; Ricci, C; Vaira, D, 2003
)
1.33
"Omeprazole is a unique and effective agent for suppression of gastric acid secretion. "( In vitro study on capsule formulations of omeprazole containing enteric coated granules.
Livingston, J; Manavalan, R; Pandey, VP; Phanindrudu, A,
)
1.84
"Omeprazole is a racemate, from which the R- and S-isomers can be isolated. "( Review article: esomeprazole--the first proton pump inhibitor to be developed as an isomer.
Kendall, MJ, 2003
)
2.1
"Esomeprazole (Nexium) is a new proton pump inhibitor that provides more effective acid control compared with other proton pump inhibitors. "( Efficacy of esomeprazole in patients with acid-peptic disorders.
Beck, J,
)
1.21
"Omeprazole is a drug widely used in the treatment of gastroesophageal reflux disease and peptic ulcer disease."( [Acute interstitial nephritis associated with omeprazole therapy].
Calvo, C; García, H; Hernández-Jaras, J; Maduell, F; Rovira, RE; Torregrosa, E, 2004
)
1.3
"Omeprazole is a proton pump inhibitor, which is used for the treatment of peptic ulcers, reflux esophagitis and Zollinger-Ellison syndrome. "( Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology.
Achleitner, G; Möschwitzer, J; Müller, RH; Pomper, H, 2004
)
2
"Esomeprazole 40 mg is an effective and safe drug at least comparable to omeprazole in treating Chinese EE patients."( Esomeprazole tablet vs omeprazole capsule in treating erosive esophagitis.
Chang, FY; Chen, CY; Lai, YL; Lee, SD; Lu, CL; Luo, JC, 2005
)
1.77
"Omeprazole is a well known activator of the aryl hydrocarbon receptor (AhR)."( Role of CYP3A4 in the regulation of the aryl hydrocarbon receptor by omeprazole sulphide.
Daujat-Chavanieu, M; Fabre, JM; Gerbal-Chaloin, S; Maurel, P; Pichard-Garcia, L; Poellinger, L; Sa-Cunha, A, 2006
)
1.29
"Omeprazole is a commonly prescribed drug for patients with peptic ulcerations. "( Omeprazole affects neither electroconvulsive threshold nor anticonvulsant activity of diphenylhydantoin and carbamazepine in mice.
Czuczwar, SJ; Kozicka, M; Luszczki, JJ; Parada-Turska, J; Pilip, S; Swiader, MJ,
)
3.02
"Omeprazole (OMP) is a proton pump inhibitor used as an oral treatment for acid-related gastrointestinal disorders. "( Effect of Cimetidine and Phenobarbital on metabolite kinetics of Omeprazole in rats.
Cho, HY; Lee, YB; Park, EJ, 2005
)
2.01
"Omeprazole is a proton pump inhibitor with a number of pharmacokinetic drug interactions due to interference with cytochrome P450. "( Interaction between omeprazole and tacrolimus in renal allograft recipients: a clinical-analytical study.
Alarcón, MC; Burgos, FJ; Marcén, R; Navarro, M; Ocaña, J; Orea, OE; Ortuño, J; Pascual, J; Villafruela, JJ, 2005
)
2.09
"Omeprazole is a proton pump inhibitor which reduces both basal and stimulated gastric acid secretion by inhibiting the parietal cell enzyme H(+)-K(+)-adenosine triphosphatase. "( [Anaphylaxis caused by omeprazole].
Bauer, C; Fackler, I; Kamann, S; Przybilla, B, 2006
)
2.09
"Omeprazole is an inhibitor of the parietal cell enzyme H+/K+ adenosine triphosphatase. "( Anaphylaxis to omeprazole: diagnosis and desensitization protocol.
Confino-Cohen, R; Goldberg, A, 2006
)
2.13
"Omeprazole is a commonly prescribed inhibitor of the gastric proton pump and has numerous indications in the treatment of gastrointestinal diseases. "( Omeprazole-associated digoxin toxicity.
Cragin, DJ; Kiley, CA; Roth, BJ, 2007
)
3.23
"Omeprazole is an effective treatment for gastroesophageal reflux in children younger than 2 years. "( Omeprazole for gastroesophageal reflux disease in the first 2 years of life: a dose-finding study with dual-channel pH monitoring.
Bishop, J; Furman, M; Thomson, M, 2007
)
3.23
"Omeprazole is a proton pump inhibitor drug in widespread use for the reduction of gastric acid production. "( Enantioselective quantification of omeprazole and its main metabolites in human serum by chiral HPLC-atmospheric pressure photoionization tandem mass spectrometry.
Bode-Böger, SM; Malfertheiner, P; Martens-Lobenhoffer, J; Mönkemüller, K; Reiche, I; Tröger, U, 2007
)
2.06
"Omeprazole is a proton-pump inhibitor that acts to reduce acid secretion in the stomach and is used for treating various acid-related gastrointestinal disorders. "( Bioavailability of two single-dose oral formulations of omeprazole 20 mg: an open-label, randomized sequence, two-period crossover comparison in healthy Mexican adult volunteers.
Burke-Fraga, V; de Lago, A; Galán, JF; González-de la Parra, M; Jiménez, P; Namur, S; Oliva, I; Poo, JL; Rosete, A, 2008
)
2.03
"Omeprazole is a potent inhibitor of gastric acid secretion (GAS). "( Omeprazole, a long-lasting inhibitor of gastric secretion.
Larson, GM; Sullivan, HW, 1984
)
3.15
"Omeprazole is a highly effective antisecretory compound without any effect on the basal hormone levels tested."( [4 weeks' administration of omeprazole: effect on acid behavior and basal hormone levels].
Dammann, HG; Feurle, G; Huefner, M; Lichtwald, K; Müller, P; Schmidt-Gayk, H; Seitz, HK; Simon, B, 1984
)
1.28
"Omeprazole is an acid-accumulated, acid-activated, prodrug that binds covalently to two cysteine residues at positions 813 (or 822) and 892, accessible from the acidic face of the pump."( Gastric acid secretion: activation and inhibition.
Bamberg, K; Besancon, M; Loo, D; Prinz, C; Sachs, G; Shin, JM,
)
0.85
"Omeprazole is a potent antisecretory drug that acts by inhibiting the gastric proton pump. "( Omeprazole administration does not impair gastrointestinal mucosal perfusion, oxygenation, and hexosamine generation.
Ikegami, M; Iwao, T; Shigemori, H; Tanikawa, K; Toyonaga, A, 1995
)
3.18
"Omeprazole is a powerful inhibitor of gastric acid and may suppress Helicobacter pylori by effecting the pKa of H pylori urease, by altering the pattern of infection, or by promoting overgrowth of other bacteria. "( Changes in the intragastric distribution of Helicobacter pylori during treatment with omeprazole.
Baron, JH; Gummett, PA; Karim, QN; Logan, RP; Misiewicz, JJ; Walker, MM, 1995
)
1.96
"Omeprazole is a proton pump inhibitor of increasingly wide use in the treatment of peptic ulcers. "( Lack of evidence of omeprazole genotoxicity in Sprague-Dawley rats.
Brambilla, G; Ghia, M; Martelli, A; Mereto, E, 1993
)
2.05
"Omeprazole is an inhibitor of gastric H+,K(+)-ATPase. "( Effect of omeprazole, an inhibitor of H+,K(+)-ATPase, on bone resorption in humans.
Abe, K; Furukawa, Y; Katano, K; Mizunashi, K, 1993
)
2.13
"Omeprazole is a substituted benzimidazole that has gained widespread use in the treatment of acidic and peptic ulcer disease. "( Angioedema and urticaria associated with omeprazole confirmed by drug rechallenge.
Bowlby, HA; Dickens, GR,
)
1.84
"Omeprazole is an effective drug for treating active peptic ulcer, whereas tripotassium dicitrato bismuthate can prevent ulcer relapse if Helicobacter pylori is eradicated. "( Omeprazole-induced increase in the absorption of bismuth from tripotassium dicitrato bismuthate.
Klotz, U; Treiber, G; Walker, S, 1994
)
3.17
"Omeprazole is a specific inhibitor in vivo of the functioning gastric acid pump, the H(+)-K(+)-adenosinetriphosphatase (ATPase), in the secretory canaliculus of the parietal cell. "( Role of histamine2 receptor in increased expression of rat gastric H(+)-K(+)-ATPase alpha-subunit induced by omeprazole.
Haruma, K; Kajiyama, G; Sachs, G; Sumii, K; Sumii, M; Takehara, Y; Tari, A; Walsh, JH; Wu, V; Yamamoto, G, 1993
)
1.94
"Omeprazole is an antagonist to the H+K+ ATPase of the gastric parietal cell. "( Electrolyte disturbance with omeprazole therapy.
Matthew, D; Melville, C; Milla, P; Shah, A, 1994
)
2.02
"Omeprazole is a member of a new class of substituted benzimidazoles. "( Omeprazole: a comprehensive review.
Destache, CJ; Massoomi, F; Savage, J,
)
3.02
"Omeprazole is a safe and specific probe of the CYP2C19 enzyme system that correlates well with genotype."( Determination of CYP2C19 phenotype in black Americans with omeprazole: correlation with genotype.
Balian, JD; Daus, JC; Flockhart, DA; Foxworth, JW; Marinac, JS; Owen, R; Willsie, SK, 1996
)
1.26
"Omeprazole (OP) is a potent antiulcer drug that is metabolized by liver cytochrome P450 (P450) enzymes. "( Human CYP2C19 is a major omeprazole 5-hydroxylase, as demonstrated with recombinant cytochrome P450 enzymes.
Ghanayem, BI; Goldstein, JA; Karam, WG; Lasker, JM, 1996
)
2.04
"Omeprazole is a proton pump inhibitor widely used for the treatment of peptic ulcer disease. "( Omeprazole-induced acute interstitial nephritis.
d'Adamo, G; Forte, F; Gangeri, F; Spinelli, C, 1997
)
3.18
"Omeprazole is an effective agent for gastroduodenal prophylaxis in patients taking NSAIDs. "( Primary gastroduodenal prophylaxis with omeprazole for non-steroidal anti-inflammatory drug users.
Bardhan, KD; Cullen, D; Eisner, M; Hawkey, CJ; Kogut, DG; Peacock, RA; Thomson, JM, 1998
)
2.01
"Omeprazole is a well studied proton pump inhibitor that reduces gastric acid secretion. "( Omeprazole. A review of its use in Helicobacter pylori infection, gastro-oesophageal reflux disease and peptic ulcers induced by nonsteroidal anti-inflammatory drugs.
Langtry, HD; Wilde, MI, 1998
)
3.19
"Omeprazole is a well studied and well tolerated agent effective in adults or children as a component in regimens aimed at eradicating H. "( Omeprazole. A review of its use in Helicobacter pylori infection, gastro-oesophageal reflux disease and peptic ulcers induced by nonsteroidal anti-inflammatory drugs.
Langtry, HD; Wilde, MI, 1998
)
3.19
"Omeprazole is a non-competitive inhibitor of the parietal cell enzyme H+-K--adenosine triphosphatase. "( Anaphylaxis to omeprazole.
Borja, J; Cabrera, M; Feo, F; Galindo, PA; García, R; Gómez, E; Martínez, C, 1999
)
2.1
"Omeprazole is an inducer of human cytochrome P450 1A (CYP1A) enzymes, but shows inhibitory effects on CYP2C19 and CYP3A4. "( Omeprazole weakly inhibits CYP1A2 activity in man.
Bohnemeier, H; Brockmöller, J; Fuhr, U; Roots, I; Rost, KL; Thomsen, T; Zaigler, M, 1999
)
3.19
"Esomeprazole (Nexium) is a new proton pump inhibitor for the treatment of acid-related diseases."( Esomeprazole provides improved acid control vs. omeprazole In patients with symptoms of gastro-oesophageal reflux disease.
Andersson, T; Hasselgren, G; Holmberg, J; Jonsson, A; Kylebäck, A; Lind, T; Röhss, K; Rydberg, L, 2000
)
1.75
"Omeprazole is a proton pump inhibitor widely used in the treatment of gastro-esophageal reflux disease and peptic ulcer disease. "( Reversible renal failure after treatment with omeprazole.
Post, AT; Voorhorst, G; Zanen, AL, 2000
)
2.01
"Omeprazole is an antisecretory drug used against gastric ulcers. "( Adsorption of omeprazole on latex particles and characterization of the complex.
Gallardo, V; Parera, A; Reyes, I; Ruiz, MA, 2000
)
2.11
"Omeprazole is a valuable therapeutic instrument to detect and treat patients with GERD in general practice."( High dose proton pump inhibitor response as an initial strategy for a clinical diagnosis of gastro-oesophageal reflux disease (GERD). Swedish multi-centre group in primary health care.
Brun, J; Sörngård, H, 2000
)
1.03
"Omeprazole is a proton pump inhibitor of increasingly wide application in the treatment of different gastroenterological diseases. "( Level of malondialdehyde after short-time omeprazole administration.
Burak, B; Burdan, F; Sek, A,
)
1.84
"Omeprazole is an effective long-term drug for gastroesophageal reflux disease after failed fundoplication in children. "( Omeprazole maintenance therapy for gastroesophageal reflux disease after failure of fundoplication.
Blair, GK; Israel, DM; Pashankar, D, 2001
)
3.2
"Omeprazole is a proton pump inhibitor, acting selectively on the gastric parietal cell H+K+-adenosine triphosphatase. "( Intravenous omeprazole in children: pharmacokinetics and effect on 24-hour intragastric pH.
Faure, C; Jacqz-Aigrain, E; Michaud, L; Navarro, J; Popon, M; Shaghaghi, EK; Turck, D, 2001
)
2.13
"Esomeprazole is a new proton pump inhibitor, which has been compared to omeprazole for the treatment of reflux oesophagitis in clinical trials."( Systematic review of proton pump inhibitors for the acute treatment of reflux oesophagitis.
Edwards, SJ; Lind, T; Lundell, L, 2001
)
1.03
"Omeprazole is a proton pump inhibitor that is used commonly in the treatment of acid-peptic disorders. "( Acute interstitial nephritis due to omeprazole.
Hollomby, DJ; McLaughlin, K; Myers, RP, 2001
)
2.03
"Omeprazole is a potent proton pump inhibitor and usually is well tolerated. "( Cutaneous leucocytoclastic vasculitis associated with omeprazole.
Lurie, M; Odeh, M; Oliven, A, 2002
)
2.01
"Omeprazole is an inhibitor of the H+K+ ATPase of the gastric parietal cell, which is used clinically to suppress gastric acid secretion. "( Effect of omeprazole-induced achlorhydria on trefoil peptide expression in the rat stomach.
Alderman, BM; Cook, GA; Giraud, AS; Kang, B; Nicoll, AJ, 2001
)
2.16
"Esomeprazole is a new PPI and is the S-isomer of racemic omeprazole. "( Esomeprazole for acid peptic disorders.
Kale-Pradhan, PB; Landry, HK; Sypula, WT, 2002
)
1.76
"Esomeprazole is a safe and effective PPI. "( Esomeprazole for acid peptic disorders.
Kale-Pradhan, PB; Landry, HK; Sypula, WT, 2002
)
1.76
"Esomeprazole is an effective and well tolerated treatment for managing GORD and for eradicating H. "( Esomeprazole: a review of its use in the management of acid-related disorders in the US.
Dunn, CJ; Mallarkey, G; Scott, LJ; Sharpe, M, 2002
)
1.76
"Omeprazole is a benzimidazole compound that acts as a proton-pump inhibitor. "( Determination of omeprazole and its metabolites in human plasma by liquid chromatography-mass spectrometry.
Kanazawa, H; Mashige, F; Matsushima, Y; Nakahara, K; Okada, A; Okubo, S; Yokota, H, 2002
)
2.1
"Esomeprazole is an effective, well tolerated treatment for managing GORD and for eradicating H. "( Esomeprazole: a review of its use in the management of acid-related disorders.
Dunn, CJ; Mallarkey, G; Scott, LJ; Sharpe, M, 2002
)
1.76
"Omeprazole is a benzimidazole derivative which induces both P450 1A1 and 1A2 in human liver in vitro and in vivo. "( Omeprazole, an inducer of human CYP1A1 and 1A2, is not a ligand for the Ah receptor.
Daujat, M; Domergue, J; Fourtanier, G; Lesca, P; Maurel, P; Peryt, B, 1992
)
3.17
"Omeprazole is a drug for short term use in patients with acid-peptic disease."( [Omeprazole and liver functions].
Sauvet, P; Schouler, L,
)
1.76
"Omeprazole is a weak base that reaches the parietal cell through the bloodstream, diffuses through the cytoplasm, and becomes activated and trapped as a sulfenamide in the acidic canaliculus of the parietal cell."( Control of gastric acid secretion. Histamine H2-receptor antagonists and H+K(+)-ATPase inhibitors.
Schubert, ML; Shamburek, RD, 1992
)
1
"Omeprazole is an effective inhibitor of gastric acid secretion through inhibition of the parietal cell H+K+ATPase."( A double-blind placebo-controlled trial of omeprazole on urinary pH in healthy subjects.
Osther, PJ; Pedersen, SA; Rasmussen, L, 1992
)
1.27
"Omeprazole (OPZ) is a proton pump inhibitor in gastric parietal cells. "( Simultaneous determination of omeprazole and its metabolites in plasma and urine by reversed-phase high-performance liquid chromatography with an alkaline-resistant polymer-coated C18 column.
Chiba, K; Ishizaki, T; Kato, Y; Kobayashi, K; Sohn, DR, 1992
)
2.01
"Omeprazole is a substituted benzimidazole that causes dose-dependent intracellular inhibition of gastric acid secretion in humans. "( Single-dose oral omeprazole for reduction of gastric residual acidity in adults for outpatient surgery.
Haskins, DA; Jahr, JS; Ramadhyani, U; Texidor, M, 1992
)
2.07
"Omeprazole is a new hydrogen-potassium adenosine triphosphatase antagonist with indications for severe reflux esophagitis and Zollinger-Ellison syndrome. "( Fulminant hepatic failure related to omeprazole.
Brogan, M; Cook-Glenn, C; Greenson, J; Jochem, V; Kirkpatrick, R; Sturgis, T, 1992
)
2
"Omeprazole is a potent, highly specific, and clinically efficacious anti-secretory agent. "( Experience with omeprazole in erosive oesophagitis.
Decktor, DL; Robinson, MG, 1991
)
2.07
"Omeprazole is a potent and effective antisecretory drug. "( Omeprazole.
Langman, MJ, 1991
)
3.17
"Omeprazole is a powerful inhibitor of gastric acid secretion."( Omeprazole. Overview and opinion.
Holt, S; Howden, CW, 1991
)
2.45
"Omeprazole is a specific inhibitor of H+,K(+)-ATPase or 'proton pump' in parietal cells. "( Clinical pharmacology of omeprazole.
Howden, CW, 1991
)
2.03
"Omeprazole is a new drug used for its high efficiency as an inhibitor of gastric acid secretion. "( Omeprazole is an aryl hydrocarbon-like inducer of human hepatic cytochrome P450.
Bories, P; Daujat, M; Diaz, D; Fabre, I; Maurel, P; Michel, H; Saint Aubert, B, 1990
)
3.16
"2. Omeprazole is an antagonist of the proton pump of the acid-producing cell of the human stomach."( [Current perspectives in ulcer disease].
Beglinger, C, 1990
)
0.79
"Omeprazole is a very potent and long-acting inhibitor of gastric acid secretion. "( Omeprazole in the treatment of Zollinger-Ellison syndrome and histamine H2-antagonist refractory ulcers.
Jansen, JB; Lamers, CB; Meijer, JL, 1989
)
3.16
"Omeprazole is a valuable alternative in modern treatment of gastric ulcer, being superior to histamine H2-receptor antagonists."( Omeprazole in the acute treatment of gastric ulcer.
Classen, M; Schepp, W, 1989
)
2.44
"Omeprazole is a highly effective treatment for erosive/ulcerative peptic oesophagitis, 40 mg daily being marginally superior to 20 mg."( Evaluation of omeprazole in reflux oesophagitis.
Dent, J; Hetzel, DJ; MacKinnon, MA; Narielvala, FM; Reed, WD, 1989
)
1.36
"Omeprazole is a very potent inhibitor of gastric acid secretion and has proven to be efficacious in the healing of peptic ulcer and reflux oesophagitis. "( Safety profile of omeprazole. Adverse events with short-term treatment.
Nelis, GF, 1989
)
2.05
"Omeprazole is a prodrug which is converted to its active form only at the site of action, namely the parietal cell. "( Omeprazole: pharmacology, pharmacokinetics and interactions.
Jonkman, JH; Oosterhuis, B, 1989
)
3.16
"Omeprazole is a substituted benzimidazole which inhibits profoundly and long-lasting human acid secretion. "( [Omeprazole in the therapy of acid-induced diseases].
Dammann, HG; Müller, P; Simon, B, 1987
)
2.63
"Omeprazole (OME) is a novel acid secretion inhibitor, believed to act directly on the gastric proton pump, the (H+ + K+)-ATPase. "( The specificity of omeprazole as an (H+ + K+)-ATPase inhibitor depends upon the means of its activation.
Fallowfield, C; Keeling, DJ; Underwood, AH, 1987
)
2.04
"Omeprazole is a highly effective treatment for peptic esophagitis."( Healing and relapse of severe peptic esophagitis after treatment with omeprazole.
Beveridge, BR; Dent, J; Gibson, GG; Hetzel, DJ; Laurence, BH; Mackinnon, M; McCarthy, JH; Mitchell, B; Narielvala, FM; Reed, WD, 1988
)
1.23
"Omeprazole is an efficient treatment for patients with prepyloric gastric ulcers."( Effect of omeprazole and cimetidine on prepyloric gastric ulcer: double blind comparative trial.
Astrup, L; Bendtsen, F; Bytzer, P; Havelund, T; Lauritsen, K; Laursen, LS; Linde, J; Olsen, JH; Rune, SJ; Wulff, HR, 1988
)
1.4
"Omeprazole is a proton pump inhibitor which induces a dose-dependent reduction of gastric acid secretion. "( [Comparative efficacy of omeprazole and cimetidine in the treatment of duodenal ulcer in the acute stage. A French multicenter, controlled therapeutic trial].
Bader, JP; Bigard, MA; Ebrard, F; Galmiche, JP; Isal, JP, 1987
)
2.02
"Omeprazole is a potent and long-acting inhibitor of pentagastrin stimulated gastric acid secretion in normal subjects, and this prompted a study of the effect of omeprazole on gastric acid hypersecretion and acid peptic disease resulting from endogenous hypergastrinaemia in Zollinger-Ellison patients."( Present experiences with omeprazole in the Zollinger-Ellison syndrome.
Lamers, CB, 1986
)
1.3
"Omeprazole is a long acting inhibitor of gastric acid secretion in different species including rat and dog. "( Pharmacology and toxicology of omeprazole--with special reference to the effects on the gastric mucosa.
Carlsson, E; Larsson, H; Mattsson, H; Ryberg, B; Sundell, G, 1986
)
2
"Omeprazole is a substituted benzimidazole derivative which markedly inhibits basal and stimulated gastric acid secretion. "( Omeprazole. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in peptic ulcer disease and Zollinger-Ellison syndrome.
Campoli-Richards, DM; Clissold, SP, 1986
)
3.16
"Omeprazole is a substituted benzimidazole which blocks gastric acid secretion by inhibiting H+K+ATPase. "( Localization of omeprazole and metabolites in the mouse.
Helander, HF; Ramsay, CH; Regårdh, CG, 1985
)
2.06
"Omeprazole is a highly effective inhibitor of gastric acid secretion in patients with Zollinger-Ellison syndrome."( Omeprazole: effective, convenient therapy for Zollinger-Ellison syndrome.
Cherner, JA; Ciarleglio, CA; Collen, MJ; Cornelius, MJ; Gardner, JD; Howard, JM; Jensen, RT; Maton, PN; McArthur, KE, 1985
)
2.43

Effects

Omeprazole has a cytostatic effect on one of three colorectal cancer cell lines. The mechanism for this effect of omeprazol and its potential role in treatment awaits elucidation. A relatively low dose (0.6 mg/kg per day) appears to be optimal in most patients.

Omeprazole has a lethal effect over some cancer cells, and cell death is a key process in kidney disease. It can increase gastric mucosal blood flow and related to many factors.

ExcerptReferenceRelevance
"Omeprazole has a lethal effect over some cancer cells, and cell death is a key process in kidney disease."( Molecular pathways driving omeprazole nephrotoxicity.
Cardenas-Villacres, D; Carrasco, S; Fontecha-Barriuso, M; Martín-Sanchez, D; Martinez-Moreno, JM; Ortiz, A; Ruiz-Ortega, M; Sanchez-Niño, MD; Sanz, AB, 2020
)
1.58
"Omeprazole, which has a free terminal secondary amino group, reacted with 4-chloro-7-nitrobenzo-2-oxa-1, 3-diazole (NBD-Cl) by a nucleophilic substitution mechanism to form a highly fluorescent dark yellow fluorophore."( Application of different spectrofluorimetric approaches for quantitative determination of acetylsalicylic acid and omeprazole in recently approved pharmaceutical preparation and human plasma.
Abdelazim, AH; Almrasy, AA; El-Olemy, A; Hasan, MA; Madkour, AW; Ramzy, S; Shahin, M, 2021
)
1.55
"Omeprazole has an important protective effect on gastric mucosal and it can increase gastric mucosal blood flow and related to many factors."( Protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.
Cai, CJ; Gao, JL; Gao, W; Hao, LJ; Li, HY; Si, YL; Wang, LX; Zheng, RJ, 2014
)
2.16
"Esomeprazole has a good tolerability profile and a low potential for drug interaction."( The pharmacology of esomeprazole and its role in gastric acid related diseases.
Saccar, CL, 2009
)
1.23
"Esomeprazole has an improved pharmacokinetic profile, resulting in increased systemic exposure and less interindividual variability compared with omeprazole, and more effective suppression of gastric acid production compared with other proton pump inhibitors."( Review of esomeprazole in the treatment of acid disorders.
Johnson, DA, 2003
)
1.26
"Omeprazole has a potential to decrease FDG uptake rate in a limited part of the GI tract."( Gastrointestinal uptake of FDG after N-butylscopolamine or omeprazole treatment in the rat.
Asaka, M; Nakada, K; Satoh, M; Tamaki, N; Yamamoto, F; Zhao, S, 2004
)
1.29
"Omeprazole has a cytostatic effect on one of three colorectal cancer cell lines but the mechanism for this effect of omeprazole and its potential role in treatment awaits elucidation."( Omeprazole inhibits growth of cancer cell line of colonic origin.
Chintalapani, S; Goo, R; Luk, G; Lundqvist, M; Maliakkal, B; Oberg, K; Reddy, J; Tobi, M, 1995
)
2.46
"Omeprazole has a potent antisecretory effect and is a suitable alternative for short-term treatment of refractory acid-related diseases; a relatively low dose (0.6 mg/kg per day) appears to be optimal in most patients. "( Effect of omeprazole in the treatment of refractory acid-related diseases in childhood: endoscopic healing and twenty-four-hour intragastric acidity.
Chiba, H; Ebina, K; Fujii, K; Kato, S; Nakagawa, H, 1996
)
2.14
"Omeprazole has a strong inhibitory effect on H."( Effect of omeprazole on Helicobacter pylori urease activity in vivo.
Domínguez-Muñoz, JE; Kalhori, N; Malfertheiner, P; Sauerbruch, T; Stoschus, B, 1996
)
1.42
"Omeprazole has a greater intragastric pH elevating effect in Helicobacter pylori positive than negative subjects. "( Helicobacter pylori infection potentiates the inhibition of gastric acid secretion by omeprazole.
Ardill, JE; Gillen, D; McColl, KE; Neithercut, WD; Wirz, AA, 1999
)
1.97
"Omeprazole has a particularly flat dose response curve, making it difficult to differentiate pH or clinical effects of 20 vs."( Drugs, bugs, and esophageal pH profiles.
Robinson, M,
)
0.85
"Omeprazole, which has a long duration of action and is a potent inhibitor of gastric acid secretion, has simplified management."( Role of acid suppressants in patients with Zollinger-Ellison syndrome.
Maton, PN, 1991
)
1
"Omeprazole has a simple treatment regimen: 20 mg once daily is recommended in the routine treatment of DU, GU and RO."( Treatment of acid-related disorders with gastric acid inhibitors: the state of the art.
Blum, AL, 1990
)
1
"Omeprazole has a marked effect on the duration and the degree of inhibition of intragastric acidity which is dose-dependent."( Relationship between inhibition of acid secretion and healing of peptic ulcers.
Chiverton, SG; Hunt, RH, 1989
)
1
"Omeprazole has an anti-ulcerogenic effect and protects rat gastric mucosa against drug-induced damage in vivo. "( Protection of gastric epithelial cell monolayers from a human cell line by omeprazole in vitro.
Ivey, KJ; Razandi, M; Romano, M, 1989
)
1.95
"Omeprazole has a low water solubility and is chemically labile in an acid environment. "( Development of an oral formulation of omeprazole.
Cederberg, C; Pilbrant, A, 1985
)
1.98
"Omeprazole has a lethal effect over some cancer cells, and cell death is a key process in kidney disease."( Molecular pathways driving omeprazole nephrotoxicity.
Cardenas-Villacres, D; Carrasco, S; Fontecha-Barriuso, M; Martín-Sanchez, D; Martinez-Moreno, JM; Ortiz, A; Ruiz-Ortega, M; Sanchez-Niño, MD; Sanz, AB, 2020
)
1.58
"Omeprazole has been shown to increase P2Y"( Omeprazole-clopidogrel interaction and neurovascular complications after flow-diverter device placement.
Albuquerque, FC; Baranoski, JF; Catapano, JS; Cole, TS; Ducruet, AF; Fredrickson, VL; Lundberg, JN; Rahmani, R; Rutledge, C; Srinivasan, VM; Wakim, AA, 2022
)
2.89
"Omeprazole, which has a free terminal secondary amino group, reacted with 4-chloro-7-nitrobenzo-2-oxa-1, 3-diazole (NBD-Cl) by a nucleophilic substitution mechanism to form a highly fluorescent dark yellow fluorophore."( Application of different spectrofluorimetric approaches for quantitative determination of acetylsalicylic acid and omeprazole in recently approved pharmaceutical preparation and human plasma.
Abdelazim, AH; Almrasy, AA; El-Olemy, A; Hasan, MA; Madkour, AW; Ramzy, S; Shahin, M, 2021
)
1.55
"Omeprazole has (R)- and (S)-enantiomers, which exhibit different pharmacokinetics (PK) among patients with cytochrome P450 (CYP) 2C19 genotype groups. "( The (R)-omeprazole hydroxylation index reflects CYP2C19 activity in healthy Japanese volunteers.
Akamine, Y; Shiohira, H; Tateishi, T; Uno, T; Yamada, S; Yasui-Furukori, N, 2013
)
2.27
"Omeprazole has an important protective effect on gastric mucosal and it can increase gastric mucosal blood flow and related to many factors."( Protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.
Cai, CJ; Gao, JL; Gao, W; Hao, LJ; Li, HY; Si, YL; Wang, LX; Zheng, RJ, 2014
)
2.16
"Omeprazole has been shown to significantly reduce these events without compromising cardiovascular safety in patients treated with dual anti-platelet therapy."( The effects of proton pump inhibition on patient-reported severity of dyspepsia when receiving dual anti-platelet therapy with clopidogrel and low-dose aspirin: analysis from the Clopidogrel and the Optimization of Gastrointestinal Events Trial.
Bhatt, DL; Cannon, CP; Cohen, M; Cryer, BL; Doros, G; Goldsmith, MA; Laine, L; Lanas, A; Lapuerta, P; Liu, Y; McIntosh, AI; Schnitzer, TJ; Vardi, M, 2015
)
1.14
"Oral omeprazole has consequently been recommended to reduce CSF production in dogs with conditions in which clinical signs may be attributable to an accumulation of CSF in the central nervous system (e.g."( Evaluation of the effect of oral omeprazole on canine cerebrospinal fluid production: A pilot study.
Allerton, F; de Marchin, J; Girod, M; Gommeren, K; Peeters, D; Ramery, E; Tutunaru, AC; Van Soens, I, 2016
)
1.17
"S-Omeprazole has been developed as a single enantiomer medicine, which has been reported not to be associated with polymorphic human P450 2C19 phenotypes."( Oxidation of R- and S-omeprazole stereoselectively mediated by liver microsomal cytochrome P450 2C19 enzymes from cynomolgus monkeys and common marmosets.
Inoue, T; Kawano, M; Murayama, N; Sasaki, E; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2016
)
1.31
"Esomeprazole has a good tolerability profile and a low potential for drug interaction."( The pharmacology of esomeprazole and its role in gastric acid related diseases.
Saccar, CL, 2009
)
1.23
"Omeprazole has recently been described as a modulator of tumour chemoresistance, although its underlying molecular mechanisms remain controversial. "( Omeprazole inhibits proliferation and modulates autophagy in pancreatic cancer cells.
Ellinger, S; Henne-Bruns, D; Klapperstueck, T; Knippschild, U; Kreyes, A; Landfester, K; Udelnow, A; Walther, P; Wohlrab, J; Würl, P, 2011
)
3.25
"Omeprazole, a PPI, has been reported to weaken the antiplatelet effects of clopidogrel."( Effects of PPIs and an H2 blocker on the antiplatelet function of clopidogrel in Japanese patients under dual antiplatelet therapy.
Horiuchi, H; Ikeda, T; Imai, M; Jinnai, T; Kato, Y; Kimura, T; Makiyama, T; Shirakawa, R; Tada, T; Tazaki, J; Yamane, K, 2012
)
1.1
"Esomeprazole has FDA-approved labeling for use in the treatment of symptomatic gastroesophageal reflux disease (GERD), including healing and maintenance of healing of erosive esophagitis and as part of a triple-drug regimen for Helicobocter pylori infection."( Esomeprazole: a clinical review.
Hedge, DD; Johnson, TJ, 2002
)
1.59
"Esomeprazole has an improved pharmacokinetic profile, resulting in increased systemic exposure and less interindividual variability compared with omeprazole, and more effective suppression of gastric acid production compared with other proton pump inhibitors."( Review of esomeprazole in the treatment of acid disorders.
Johnson, DA, 2003
)
1.26
"Esomeprazole has higher and more consistent bio-availability than omeprazole, which results in a greater area under the plasma concentration-time curve."( Review article: Esomeprazole--enhanced bio-availability, specificity for the proton pump and inhibition of acid secretion.
Andersson, T; Carlsson, E; Fryklund, J; Keeling, D; Lindberg, P; Lundborg, P, 2003
)
1.21
"Omeprazole has been used as a drug probe for CYP2C19, but no systematic data are available for Mexican populations. "( CYP2C19- and CYP3A4-dependent omeprazole metabolism in West Mexicans.
de J Chávez, T; Escobar-Islas, E; Gonzalez, HM; Hoyo-Vadillo, C; Lozano, F; Peregrina, AA; Romero, EM, 2003
)
2.05
"Esomeprazole has been studied clinically for a variety of acid-related conditions, showing that the compound is as well tolerated and more effective with regard to healing and symptom relief than the recommended treatment with omeprazole."( Single-isomer drugs: true therapeutic advances.
Andersson, T, 2004
)
0.88
"Omeprazole has the same inhibitory effect on T."( Pyruvate decarboxylase, the target for omeprazole in metronidazole-resistant and iron-restricted Tritrichomonas foetus.
Hrdý, I; Kulda, J; Sutak, R; Tachezy, J, 2004
)
1.31
"Esomeprazole has higher oral bioavailability and increased antimicrobial activity against Helicobacter pylori than omeprazole."( Esomeprazole versus omeprazole for the eradication of Helicobacter pylori infection: results of a randomized controlled study.
Anagnostopoulos, GK; Arvanitidis, D; Kostopoulos, P; Margantinis, G; Tsiakos, S, 2004
)
1.77
"Omeprazole has a potential to decrease FDG uptake rate in a limited part of the GI tract."( Gastrointestinal uptake of FDG after N-butylscopolamine or omeprazole treatment in the rat.
Asaka, M; Nakada, K; Satoh, M; Tamaki, N; Yamamoto, F; Zhao, S, 2004
)
1.29
"Esomeprazole has been shown to be more effective than lansoprazole in relieving GORD symptoms, and esomeprazole and pantoprazole appear to be equally effective in resolving GORD symptoms in a comparative study."( Night-time gastro-oesophageal reflux disease: prevalence, hazards, and management.
Orr, WC, 2005
)
0.89
"Omeprazole has significantly elevated the expression level of COX-2 protein, PGE2 level (19.37%), and decreased myeloperoxidase activity (81.92%), thereby causing the most effective ulcer healing (89.74%)."( Cyclo-oxygenase-2 expression and prostaglandin E2 production in experimental chronic gastric ulcer healing.
Gautam, P; Poonam, D; Vinay, CS, 2005
)
1.05
"Omeprazole has been associated with multiple adverse effects including skin reactions but, to date, cutaneous hyperpigmentation has not been described as an adverse effect of this drug."( Cutaneous hyperpigmentation induced by omeprazole mimicking ashy dermatosis.
Alcolea-Rubio, LA; Ibarra-Berrocal, IJ; Martínez-Barba, E; Martínez-Escribano, JA; Ramírez-Hernández, M, 2006
)
2.05
"Omeprazole has been determined in formulations and biological fluids by a variety of methods such as spectrophotometry, high-performance liquid chromatography with ultraviolet detection and liquid chromatography coupled with tandem mass spectrometry."( Analytical methodologies for the determination of omeprazole: an overview.
Bosch Ojeda, C; Espinosa Bosch, M; Ruiz Sánchez, AJ; Sánchez Rojas, F, 2007
)
1.31
"Omeprazole has previously been shown to be a potent inhibitor of gastric acid secretion in man. "( Omeprazole, a gastric 'proton pump inhibitor': lack of effect on renal handling of electrolytes and urinary acidification.
Howden, CW; Reid, JL, 1984
)
3.15
"Omeprazole (OM) has been shown to be superior to H2-Blockers in terms of complete healing rates of gastric (GU) and duodenal ulcers (DU). "( [Treatment of acute peptic gastroduodenal ulcer: omeprazole is superior to ranitidine especially in the early phase of ulcer healing. A prospective controlled randomized serial endoscopy study].
Guthke, A; Hotz, J; Kark, W; Otten, O; Plein, K; Wiedbrauck, F, 1995
)
1.99
"Omeprazole has a cytostatic effect on one of three colorectal cancer cell lines but the mechanism for this effect of omeprazole and its potential role in treatment awaits elucidation."( Omeprazole inhibits growth of cancer cell line of colonic origin.
Chintalapani, S; Goo, R; Luk, G; Lundqvist, M; Maliakkal, B; Oberg, K; Reddy, J; Tobi, M, 1995
)
2.46
"Omeprazole has been shown to have a good long-term safety profile, as evaluated in these trials."( Long-term treatment of gastro-oesophageal reflux disease with omeprazole.
Lundell, L, 1994
)
1.25
"Omeprazole has been reported to increase cytochrome P450IA2 (CYP1A2) activity in vitro, but whether this effect also occurs in vivo is controversial. "( Omeprazole does not enhance the metabolism of phenacetin, a marker of CYP1A2 activity, in healthy volunteers.
Bartoli, A; Cipolla, G; Crema, F; Gatti, G; Perucca, E; Xiaodong, S, 1994
)
3.17
"Omeprazole has been marketed in France since 1989, for the healing of peptic ulcers, erosive reflux esophagitis and the Zollinger Ellison syndrome. "( [Evaluation of unexpected and toxic effects of omeprazole (Mopral) reported to the regional centers of pharmacovigilance during the first 22 postmarketing months].
Bidault, I; Castot, A; Dahan, R; Efthymiou, ML,
)
1.83
"Omeprazole has previously been shown to induce hepatic cytochrome P4501A2 activity, as evidenced by an accelerated N-3-demethylation in the 13C-[N-3-methyl]-caffeine breath test. "( Accelerated caffeine metabolism after omeprazole treatment is indicated by urinary metabolite ratios: coincidence with plasma clearance and breath test.
Roots, I; Rost, KL, 1994
)
2
"Omeprazole has been investigated for the treatment of gastric ulcer, duodenal ulcer, gastroesophageal reflux, and various hypersecretory states."( Omeprazole: a comprehensive review.
Destache, CJ; Massoomi, F; Savage, J,
)
2.3
"Omeprazole has been marketed successfully after a prolonged development phase characterized by difficult problems with the toxicity studies."( Problems with toxicity studies in the assessment of new drugs.
Werkö, L, 1993
)
1.01
"Omeprazole has a potent antisecretory effect and is a suitable alternative for short-term treatment of refractory acid-related diseases; a relatively low dose (0.6 mg/kg per day) appears to be optimal in most patients. "( Effect of omeprazole in the treatment of refractory acid-related diseases in childhood: endoscopic healing and twenty-four-hour intragastric acidity.
Chiba, H; Ebina, K; Fujii, K; Kato, S; Nakagawa, H, 1996
)
2.14
"Omeprazole has been shown to have a suppressive effect on Helicobacter pylori. "( Prolonged treatment with omeprazole does not improve the eradication rate of Helicobacter pylori infection--a short report [corrected].
Anderson, PE; Goh, KL; Parasakthi, N; Peh, SC; Tan, KK, 1995
)
2.04
"Omeprazole has a strong inhibitory effect on H."( Effect of omeprazole on Helicobacter pylori urease activity in vivo.
Domínguez-Muñoz, JE; Kalhori, N; Malfertheiner, P; Sauerbruch, T; Stoschus, B, 1996
)
1.42
"Omeprazole has shown remarkable efficacy and safety in the treatment of patients with gastroesophageal reflux disease (GERD); similarly, laparoscopic techniques have allowed less morbidity in patients undergoing fundoplication procedures. "( Choice of long-term strategy for the management of patients with severe esophagitis: a cost-utility analysis.
Centor, RM; Heudebert, GR; Marks, R; Wilcox, CM, 1997
)
1.74
"Omeprazole has been shown previously to be metabolized by the two cytochrome P450 isoforms CYP2C19 (hydroxylation) and CYP3A4 (sulphoxidation). "( Carbamazepine treatment induces the CYP3A4 catalysed sulphoxidation of omeprazole, but has no or less effect on hydroxylation via CYP2C19.
Bertilsson, L; Chang, M; Tomson, T; Tybring, G; Widén, J, 1997
)
1.97
"Omeprazole has the potential to mask other disorders such as peptic ulcer disease, thereby delaying appropriate testing for and eradication of Helicobacter pylori."( Value of a therapeutic trial to diagnose gastroesophageal reflux disease: step up versus step down therapy.
Da Costa, LR, 1997
)
1.02
"Omeprazole has been used with increasing frequency for the treatment of conditions such as reflux oesophagitis, peptic ulcer disease, and Zollinger-Ellison syndrome. "( Omeprazole and the development of acute hepatitis.
Koury, SI; La Charité, DD; Stone, CK, 1998
)
3.19
"Omeprazole has a greater intragastric pH elevating effect in Helicobacter pylori positive than negative subjects. "( Helicobacter pylori infection potentiates the inhibition of gastric acid secretion by omeprazole.
Ardill, JE; Gillen, D; McColl, KE; Neithercut, WD; Wirz, AA, 1999
)
1.97
"Omeprazole has been marketed in France since 1989, for the healing of peptic ulcers, erosive reflux oesophagitis, and the Zollinger-Ellison syndrome. "( Omeprazole-induced leukopenia. A case report.
Brunet, C; Dehee, D; Dine, T; Gressier, B; Luyckx, MM; Martin, P; Membré, S; Moulron, S; Odou, P; Tamiji, L, 1999
)
3.19
"Omeprazole has been shown to promote healing of spontaneously occurring gastric ulcers in horses when administered for 28 days at a dose of 4 mg/kg bwt/day and to prevent recurrence of ulcers in almost all horses when treatment is continued at a dose of at least 2 mg/kg bwt/day. "( Safety of omeprazole paste in foals and mature horses.
Attebery, DK; Cox, JL; Daurio, C; Plue, RE; Wall, HG; Wallace, DH, 1999
)
2.15
"Omeprazole has a particularly flat dose response curve, making it difficult to differentiate pH or clinical effects of 20 vs."( Drugs, bugs, and esophageal pH profiles.
Robinson, M,
)
0.85
"Omeprazole has become available in a tablet formulation, a Multiple Unit Pellet System (MUPS) containing a large number of small individually enteric-coated micropellets."( Pharmacodynamics and kinetics of omeprazole MUPS 20 mg and pantoprazole 40 mg during repeated oral administration in Helicobacter pylori-negative subjects.
Geus, WP; Lamers, CB; Mathôt, RA; Mulder, PG, 2000
)
2.03
"Esomeprazole has significantly higher oral bioavailability than omeprazole, resulting in greater acid suppression."( Esomeprazole, a new proton pump inhibitor: pharmacological characteristics and clinical efficacy.
Talley, NJ; Thitiphuree, S, 2000
)
1.59
"Omeprazole has been shown to be effective in the treatment of acid-related diseases. "( A review of omeprazole use in the treatment of acid-related disorders in children.
Katona, BG; Levine, D; Souney, PE; Walters, JK; Zimmermann, AE, 2001
)
2.13
"Omeprazole has long been used as an effective agent to treat peptic ulcer. "( Anticonvulsant activity of omeprazole in rats.
Balakrishnan, S; Bhargava, VK; Pandhi, P, 2001
)
2.05
"Esomeprazole has demonstrated higher healing rates than omeprazole at 4 and 8 weeks. "( Systematic review of proton pump inhibitors for the acute treatment of reflux oesophagitis.
Edwards, SJ; Lind, T; Lundell, L, 2001
)
1.03
"Esomeprazole has demonstrated acid control comparable to that of the other PPIs currently available."( Esomeprazole for acid peptic disorders.
Kale-Pradhan, PB; Landry, HK; Sypula, WT, 2002
)
1.59
"Omeprazole has been shown to induce cytochrome P450IA1 and P450IA2 activity in vitro. "( Increase of cytochrome P450IA2 activity by omeprazole: evidence by the 13C-[N-3-methyl]-caffeine breath test in poor and extensive metabolizers of S-mephenytoin.
Brockmöller, J; Brösicke, H; Helge, H; Roots, I; Rost, KL; Scheffler, M, 1992
)
1.99
"Omeprazole has been used successfully in the treatment of reflux esophagitis and the Zollinger-Ellison syndrome in the United States over the past year and has received approval recently as first-line therapy for duodenal ulcer disease."( Proton-pump inhibition for acid-related disease.
Holt, S, 1991
)
1
"Omeprazole, which has a long duration of action and is a potent inhibitor of gastric acid secretion, has simplified management."( Role of acid suppressants in patients with Zollinger-Ellison syndrome.
Maton, PN, 1991
)
1
"Omeprazole has been shown in previous studies to inhibit the hepatic metabolism of selected drugs. "( Quinidine single dose pharmacokinetics and pharmacodynamics are unaltered by omeprazole.
Ching, MS; Devenish-Meares, S; Elliott, SL; Morgan, DJ; Murdoch, RT; Smallwood, RA; Stead, CK, 1991
)
1.95
"Omeprazole has a simple treatment regimen: 20 mg once daily is recommended in the routine treatment of DU, GU and RO."( Treatment of acid-related disorders with gastric acid inhibitors: the state of the art.
Blum, AL, 1990
)
1
"Omeprazole has produced short term healing rates superior to the histamine H2-receptor antagonists in duodenal ulcer, gastric ulcer and reflux oesophagitis."( Clinical pharmacology of omeprazole.
Howden, CW, 1991
)
1.31
"Omeprazole has been subjected to an unusually extensive range of genotoxicity tests ranging from mutational assays in bacteria (e.g. "( Tests for genotoxicity: principles and findings in relation to omeprazole.
Evans, HJ, 1990
)
1.96
"Omeprazole has been shown to provide more rapid symptom relief and to heal ulcers more quickly and reliably than H2-receptor antagonists in duodenal ulcer, gastric ulcer and reflux oesophagitis. "( Clinical development programme for omeprazole.
Walan, A, 1990
)
2
"Omeprazole has been approved by the Food and Drug Administration for short-term therapy of severe erosive esophagitis, poorly responsive symptomatic gastroesophageal reflux disease, and long-term management of Zollinger-Ellison syndrome."( Omeprazole: a novel antisecretory agent for the treatment of acid-peptic disorders.
Dukes, GE; Hak, LJ; Lampkin, TA; Ouellet, D, 1990
)
2.44
"Omeprazole has given healing rates of 58-83% after treatment for 2 weeks and 84-100% after 4 weeks."( Clinical experience with omeprazole: assessment of efficacy and safety.
Walan, A, 1989
)
1.3
"Omeprazole has also had a more pronounced effect on ulcer symptoms."( The clinical utility and safety of omeprazole.
Walan, A, 1989
)
1.28
"Omeprazole therapy has been well tolerated and no side effects, significant changes in laboratory variables or toxicity have been noted."( Omeprazole in the treatment of Zollinger-Ellison syndrome and histamine H2-antagonist refractory ulcers.
Jansen, JB; Lamers, CB; Meijer, JL, 1989
)
2.44
"Omeprazole has been shown to give significantly higher healing rates than ranitidine or cimetidine in patients with duodenal ulcer and gastric ulcer."( Clinical utility and safety of omeprazole.
Walan, A, 1989
)
1.28
"Omeprazole has a marked effect on the duration and the degree of inhibition of intragastric acidity which is dose-dependent."( Relationship between inhibition of acid secretion and healing of peptic ulcers.
Chiverton, SG; Hunt, RH, 1989
)
1
"Omeprazole and placebo have been compared in 64 patients with erosive or ulcerative oesophagitis; the 4-week healing rates were 81% with omeprazole, 20 mg or 40 mg daily, and 6% with placebo."( Evaluation of omeprazole in reflux oesophagitis.
Dent, J; Hetzel, DJ; MacKinnon, MA; Narielvala, FM; Reed, WD, 1989
)
1.36
"Omeprazole has an anti-ulcerogenic effect and protects rat gastric mucosa against drug-induced damage in vivo. "( Protection of gastric epithelial cell monolayers from a human cell line by omeprazole in vitro.
Ivey, KJ; Razandi, M; Romano, M, 1989
)
1.95
"Omeprazole has been shown to be an inhibitor of acid secretion in vivo, but also in in vitro test models for acid secretion, including partly purified H+,K+-ATPase, the inhibitory action of omeprazole has been demonstrated (Wallmark, B., Jaresten, B."( The relationship between gastric acid secretion and gastric H+,K+-ATPase activity.
Humble, L; Larsson, H; Wallmark, B, 1985
)
0.99
"Omeprazole has been previously shown to block gastric acid secretion by specific inhibition of gastric parietal cell membrane H+-K+-ATPase. "( Omeprazole, a specific inhibitor of H+-K+-ATPase, inhibits bone resorption in vitro.
Tuukkanen, J; Väänänen, HK, 1986
)
3.16
"Omeprazole has no documented effect on esophageal motility or lower esophageal sphincter pressure."( Therapeutic evaluation of omeprazole.
Adams, MH; Kirkwood, CF; Ostrosky, JD, 1988
)
1.3
"Omeprazole has also been shown to dose-dependently inhibit vagally stimulated and meal stimulated acid secretion."( Effect of omeprazole on gastric acid secretion in man.
Cederberg, C; Ekenved, G; Lind, T; Olbe, L, 1986
)
1.39
"Omeprazole has been given to more than 2500 subjects, mostly in short-term studies for 2-4 weeks, but also to some patients for more than 2 years. "( Safety aspects of omeprazole.
Sölvell, L, 1986
)
2.05
"Omeprazole has been reported to prolong the half-life of diazepam which may be due to inhibition of the demethylation of diazepam."( Pharmacokinetics and metabolism of omeprazole in man.
Regårdh, CG, 1986
)
1.27
"Omeprazole has a low water solubility and is chemically labile in an acid environment. "( Development of an oral formulation of omeprazole.
Cederberg, C; Pilbrant, A, 1985
)
1.98

Actions

Omeprazole was found to inhibit acid secretion, and the inhibition could be reversed with glutathione or 2-mercaptoethanol. Patients remained free of toxicity or side effects related to omeprazoles. Omeprazol is able to inhibit neutrophil chemotaxis to fMLP and IL-8.

ExcerptReferenceRelevance
"Omeprazole with lower water solubility could not generate sufficient osmotic pressure to create a crack in the membrane to activate pulsatile release, whereas the two other model drugs with higher solubilities could."( Formulation and process optimization of multiparticulate pulsatile system delivered by osmotic pressure-activated rupturable membrane.
Chen, YC; Ho, HO; Hsieh, CM; Hung, SF; Lin, CM; Sheu, MT, 2015
)
1.14
"Omeprazole does not inhibit Th2 cytokine-stimulated eotaxin-3 expression by esophageal fibroblasts, suggesting that PPIs will have limited impact on subepithelial EoE processes such as fibrosis. "( JAK-STAT6 Pathway Inhibitors Block Eotaxin-3 Secretion by Epithelial Cells and Fibroblasts from Esophageal Eosinophilia Patients: Promising Agents to Improve Inflammation and Prevent Fibrosis in EoE.
Cheng, E; Huo, X; Park, JY; Souza, RF; Spechler, SJ; Wang, DH; Wilson, KS; Yu, C; Zhang, Q; Zhang, X, 2016
)
1.88
"Omeprazole did not inhibit when present in the internal proteoliposomal compartment, indicating that the inhibition was specifically due to interaction with external site(s) of the protein."( Inactivation by omeprazole of the carnitine transporter (OCTN2) reconstituted in liposomes.
Indiveri, C; Pochini, L; Scalise, M, 2009
)
1.42
"Omeprazole could inhibit human hepatoma cell line HepG2 cell proliferation and promote apoptosis."( [Effects of omeprazole on the proliferation and apoptosis of hepatoma cell line HepG2].
Liang, NL; Liu, XJ; Wei, Y; Wu, WC; Yang, L; Zhu, YJ, 2012
)
2.2
"Omeprazole is able to inhibit neutrophil chemotaxis to fMLP and IL-8. "( The inhibitory effects of H+ K+ ATPase inhibitors on human neutrophils in vitro: restoration by a K+ ionophore.
Antunes, E; Gambero, A; Martins de Oliveira, R; Pedrazzoli, J, 2007
)
1.78
"Omeprazole can enhance efficacy of single and double antibiotic protocols and is particularly effective when combined with clarithromycin and a nitroimidazole."( Omeprazole enhances efficacy of triple therapy in eradicating Helicobacter pylori.
Andrews, P; Bae, H; Borody, TJ; Brandl, S; Fracchia, G; Shortis, NP, 1995
)
2.46
"Omeprazole abolished the increase in bicarbonate secretion produced by neuromedin C."( Mechanisms of stimulatory effect of neuromedin C on pancreatic exocrine secretion in conscious rats.
Funakoshi, A; Matsumoto, M; Miyasaka, K; Okubo, K, 1994
)
1.01
"Omeprazole caused an increase of the systemic availability of bismuth from tripotassium dicitrato bismuthate. "( Omeprazole-induced increase in the absorption of bismuth from tripotassium dicitrato bismuthate.
Klotz, U; Treiber, G; Walker, S, 1994
)
3.17
"The omeprazole-induced increase in ECL-cell histamine is associated with an increase in the compartment composed of secretory vesicles and vacuoles."( Ultrastructure of enterochromaffin-like cells in rat stomach: effects of alpha-fluoromethylhistidine-evoked histamine depletion and hypergastrinemia.
Andersson, K; Chen, D; Håkanson, R; Sundler, F; Zhao, CM, 1996
)
0.77
"omeprazole does not cause increased bacterial shall bowel overgrowth in elderly subjects."( The effect of long-term omeprazole on the glucose-hydrogen breath test in elderly patients.
Hutchinson, S; Logan, R, 1997
)
2.05
"Omeprazole can suppress gastric acid remarkably and may be beneficial for patients with peptic ulcer bleeding."( Can optimal acid suppression prevent rebleeding in peptic ulcer patients with a non-bleeding visible vessel: a preliminary report of a randomized comparative study.
Lee, FY; Lin, HJ; Lo, WC; Perng, CL; Wang, K,
)
0.85
"Omeprazole does increase intragastric pH in bleeding peptic ulcer patients with H. "( Will Helicobacter pylori affect short-term rebleeding rate in peptic ulcer bleeding patients after successful endoscopic therapy?
Chang, FY; Hsieh, YH; Lee, FY; Lee, SD; Lin, HJ; Perng, CL; Tseng, GY, 1999
)
1.75
"Omeprazole can inhibit renal elimination of the hydrogen ion and block the active tubular secretion of MTX."( Potential interaction between methotrexate and omeprazole.
Aldaz, A; Aquerreta, I; Beorlegui, B; Giráldez, J; Ortega, A; Sierrasesúmega, L, 2000
)
1.29
"Omeprazole 20-40 mg may cause a moderate increase in fasting plasma gastrin."( Omeprazole in elderly duodenal ulcer patients: relationship between reduction in gastric acid secretion and fasting plasma gastrin.
Cederberg, C; Lind, T; Olausson, M; Olbe, L, 1991
)
2.45
"Omeprazole, believed to inhibit H+, K+-ATPase, was used to study acid secretion dynamics in isolated gastric mucosa. "( Omeprazole: inhibitor of both acid formation and translocation in gastric mucosa.
Ekblad, EB, 1989
)
3.16
"Omeprazole did not increase the amount of sulfhydryl compounds in cultured cells."( Protection of gastric epithelial cell monolayers from a human cell line by omeprazole in vitro.
Ivey, KJ; Razandi, M; Romano, M, 1989
)
1.23
"Omeprazole was found to inhibit the K+-stimulated ATPase activity of the gastric (H+ + K+)-ATPase in parallel with the K+-stimulated p-nitrophenylphosphatase activity and the phosphoenzyme formation. "( The mechanism for inhibition of gastric (H+ + K+)-ATPase by omeprazole.
Brändström, A; Eklundh, B; Lorentzon, P; Wallmark, B, 1985
)
1.95
"Omeprazole was found to inhibit the (H+ + K+)-ATPase activity in a time-dependent manner."( Studies on the mechanism of action of omeprazole.
Fallowfield, C; Ife, RJ; Keeling, DJ; Milliner, KJ; Tingley, SK; Underwood, AH, 1985
)
1.26
"Omeprazole was found to inhibit the (H+ + K+)-ATPase activity in isolated gastric vesicles only when acid was accumulated in the vesicle lumen. "( Inhibition of (H+ + K+)-ATPase by omeprazole in isolated gastric vesicles requires proton transport.
Jackson, R; Lorentzon, P; Sachs, G; Wallmark, B, 1987
)
1.99
"Omeprazole in doses lower than 20 mg daily did not suppress pentagastrin-stimulated acid secretion in all subjects 6 h after dosing on the 5th day."( Relationship between reduction of gastric acid secretion and plasma gastrin concentration during omeprazole treatment.
Cederberg, C; Forssell, H; Lind, T; Olausson, M; Olbe, L, 1988
)
1.21
"Omeprazole was found to inhibit acid secretion, and the inhibition could be reversed with glutathione or 2-mercaptoethanol."( Acid secretion by frog gastric mucosa is electroneutral.
Hersey, SJ; Kasbekar, DK; Sachs, G, 1985
)
0.99
"Omeprazole continued to inhibit gastric acid secretion during 1-9 mo of therapy and patients remained free of toxicity or side effects related to omeprazole."( Omeprazole: effective, convenient therapy for Zollinger-Ellison syndrome.
Cherner, JA; Ciarleglio, CA; Collen, MJ; Cornelius, MJ; Gardner, JD; Howard, JM; Jensen, RT; Maton, PN; McArthur, KE, 1985
)
2.43

Treatment

Omeprazole treatment resulted in anacidity (pH values above 6.0) in 14 individuals 30 min after the liver dose and in 15 individuals after 60 min. Dogs treated with omeprazoles had a significantly higher MPT ± SD intragastric pH (91.2%) than dogs treated with placebo (19.7%)

ExcerptReferenceRelevance
"Omeprazole treatment of LLC cells inhibited Hsp70/90 and Hsp70/90-carrying EV release in a dose-dependent manner (1 to 10 μM) and attenuated the catabolic activity of LLC cell-conditioned medium on C2C12 myotubes. "( Ameliorating cancer cachexia by inhibiting cancer cell release of Hsp70 and Hsp90 with omeprazole.
Gao, S; Li, M; Li, YP; Liu, Z; Sun, K; Xiong, J; Zhang, G; Zhu, MX, 2022
)
2.39
"Omeprazole treatment increased R-R intervals (P = .01) and decreased ratio of low frequency/high frequency signal (P = .008) as compared to horses receiving water."( Changes in Heart Rate Variability with Induction of Gastric Ulcers in Adult Horses.
Berryhill, EH; Finno, CJ; Knych, H; Louie, EW; Morgan, JM; Nieto, J; Wensley, F, 2023
)
1.63
"Omeprazole treatment inhibits gastric acidity, rescuing morphine-induced gastric dysbiosis and preventing inflammation."( Morphine use induces gastric microbial dysbiosis driving gastric inflammation through TLR2 signalling which is attenuated by proton pump inhibition.
Chupikova, I; Ghosh, N; Kesh, K; Ramakrishnan, S; Roy, S; Sharma, U; Singh, PK, 2023
)
1.63
"Omeprazole-treated rats had significantly decreased the width of tight junction, villous length, and absorptive area of duodenum, jejunum, and ileum compared to control rats."( Ultrastructural intestinal mucosa change after prolonged inhibition of gastric acid secretion by omeprazole in male rats.
Chamniansawat, S; Kampuang, N; Suksridechacin, N; Thongon, N, 2021
)
1.56
"Omeprazole treatment increased the aortic cross-sectional area and media/lumen ratio by 25% (P < 0.05)."( Omeprazole induces vascular remodeling by mechanisms involving xanthine oxidoreductase and matrix metalloproteinase activation.
Castro, MM; Conde, SO; Nogueira, RC; Oliveira-Paula, GH; Parente, JM; Pinheiro, LC; Sanches-Lopes, JM; Tanus-Santos, JE, 2021
)
2.79
"Omeprazole treatment (10 mg/kg) for 2 weeks significantly improved the impaired motor coordinative function of demyelinated mice, increased the expression of myelin basic protein (MBP) and up-regulated the expression of genes related to remyelination."( Repurposing of omeprazole for oligodendrocyte differentiation and remyelination.
Harris, RA; Kang, Z; Sun, J; Wang, J; Wang, Y; Wu, G; Wu, X; Zhu, K; Zou, Z, 2019
)
1.59
"Omeprazole treatment also resulted in increased activity of the enzymes catalase and ascorbate peroxidase, reduced accumulation of the reactive oxygen species hydrogen peroxide, increase in the essential oil ratio, and improvement in essential oil composition."( Omeprazole alleviates water stress in peppermint and modulates the expression of menthol biosynthesis genes.
Elansary, HO; Zin El-Abedin, TK, 2019
)
2.68
"Omeprazole treatment had no significant effect on lowering the blood glucose levels of diabetic mice, when compared to control, although it improved the antihyperglycemic actions of exendin-4. "( Combination of omeprazole with GLP-1 agonist therapy improves insulin sensitivity and antioxidant activity in liver in type 1 diabetic mice.
Bahekar, R; Detroja, J; Dhanesha, N; Gandhi, T; Jain, M; Joharapurkar, A; Kshirsagar, S; Patel, K; Patel, V, 2013
)
2.19
"Omeprazole treatment decreases the expression of genes that have important functions in colonocyte integrity. "( Proton pump inhibitors induce changes in colonocyte gene expression that may affect Clostridium difficile infection.
Harris, LR; Hegarty, JP; Sangster, W; Stewart, DB, 2014
)
1.85
"Omeprazole treatment resulted in decreases in Akkermansia muciniphila and Coprococcus sp. "( The effect of omeprazole on the development of experimental autoimmune encephalomyelitis in C57BL/6J and SJL/J mice.
Ericsson, AC; LeVine, SM; Parker, BL; Sands, SA; Tsau, S; Yankee, TM, 2014
)
2.21
"Omeprazole treatment increased the proportion of EndoH sensitive tyrosinase, indicating that tyrosinase maturation was impaired."( Omeprazole, a gastric proton pump inhibitor, inhibits melanogenesis by blocking ATP7A trafficking.
Ichihashi, M; Karaman-Jurukovska, N; Matsui, MS; Muizzuddin, N; Niki, Y; Petris, MJ; Yarosh, DB, 2015
)
2.58
"Omeprazole-treated rats presented larger cortical defects (2.75 ± 0.59 mm(3) , p = 0.003 versus 2.11 ± 0.36 mm(3) ; p = 0.002) and a lower percentage of newly formed bone in the defects (28.62 ± 13.12; 45.89 ± 9.73; p = 0.003) than controls. "( Systemic administration of omeprazole interferes with bone healing and implant osseointegration: an in vivo study on rat tibiae.
Abdallah, MN; Al Subaie, A; Eimar, H; Emami, E; Laurenti, M; Tamimi, F; Tamimi, I, 2016
)
2.17
"Omeprazole treatment caused a nonsignificant reduction in the mean iron level (iron 159 ± 42, 136 ± 54,167 ± 34 µg/dl, p  =  0.302)."( Proton pump inhibitors use suppresses iron absorption in congenital dyserythropoietic anemia.
Harosh, MB; Kapelushnik, J; Quider, AA; Shalev, H,
)
0.85
"Omeprazole treatment have caused considerable changes in stool culture results. "( The effect of omeprazole treatment on the gut microflora and neutrophil function.
Dabrowski, A; Garley, M; Jabłońska, E; Jamiołkowski, J; Jurkowska, G; Kostrzewska, M; Olszańska, D; Ratajczak-Wrona, W; Świdnicka-Siergiejko, A, 2017
)
2.26
"Omeprazole treatment significantly increased the AUC(0-infinity) (41,387 ng h/mL, P = 0.004) and t1/2 (46.4 hours, P = 0.017) of R-warfarin in hmEMs to levels comparable to those in the PMs."( The role of cytochrome P2C19 in R-warfarin pharmacokinetics and its interaction with omeprazole.
Sugawara, K; Sugimoto, K; Tateishi, T; Uno, T, 2008
)
1.29
"Omeprazole pre-treatment delayed the post-prandial acidification of the gastric chyme, slowed the rise in Cl(-) concentration of the chyme and altered the patterns of other ions, indicating inhibition of H(+) and accompanying Cl(-) secretion."( Using omeprazole to link the components of the post-prandial alkaline tide in the spiny dogfish, Squalus acanthias.
Munger, RS; Schultz, AG; Walsh, PJ; Wood, CM, 2009
)
1.56
"Omeprazole treatment did not result in mucosal injury or inflammation; however, there were marked shifts in numbers and types of enteric bacteria, including a significant reduction (∼80%) of jejunal Actinobacteria and Bifidobacteria spp."( Proton pump inhibitors exacerbate NSAID-induced small intestinal injury by inducing dysbiosis.
Bercik, P; Bolla, M; Collins, SM; de Palma, G; Denou, E; Jury, J; McKnight, W; Ongini, E; Syer, S; Verdu, E; Vong, L; Wallace, JL, 2011
)
1.09
"Omeprazole treatment in human colon cancer cell lines HCT-116 and HCA-7 cells resulted in induction of p21waf1/cip1 and decreased the expression of anti-apoptotic proteins Bcl-2, Bcl-XL and survivin in a dose-dependent manner."( Anti-carcinogenic properties of omeprazole against human colon cancer cells and azoxymethane-induced colonic aberrant crypt foci formation in rats.
Li, Q; Patlolla, JM; Rao, CV; Steele, VE; Zhang, Y, 2012
)
1.38
"Omeprazole treatment exerts its effects mostly on bone mineralization and cancellous bone, adversely affecting bone properties. "( Can 2-oxoglutarate prevent changes in bone evoked by omeprazole?
Bienko, M; Dobrowolski, P; Pierzynowski, SG; Radzki, RP; Tomaszewska, E; Wydrych, J; Zdybel, A, 2013
)
2.08
"Omeprazole treatment of such patients relieves BA and GERD symptoms."( [Clinico-functional evaluation of the efficacy of treating gastroesophageal reflux disease combined with bronchial asthma with omeprazole].
Agapova, NR; Busarova, GA; Maev, IV; Samsonov, AA, 2002
)
1.24
"Omeprazole treatment does not affect the pharmacokinetics or systemic effects of budesonide controlled-release capsules when the two medications are taken simultaneously."( Pharmacokinetics of budesonide controlled-release capsules when taken with omeprazole.
Bergstrand, M; Edsbäcker, S; Larsson, P, 2003
)
1.99
"Omeprazole treatment success occurred more frequently in patients with a total diagnostic score of > 7 and oesophagitis II-IV in patients with a total diagnostic score of > 9."( Reflux symptoms in general practice: diagnostic evaluation of the Carlsson-Dent gastro-oesophageal reflux disease questionnaire.
de Wit, NJ; Numans, ME, 2003
)
1.04
"Omeprazole treatment produced reciprocal changes in A(1) receptor and gastrin gene expression, and parallel changes in A(2A) receptor and somatostatin gene expression."( Effect of omeprazole on gastric adenosine A1 and A2A receptor gene expression and function.
Kwok, YN; Leung, HC; Yip, L, 2004
)
1.45
"the omeprazole-treated group were 148% vs."( Gastrointestinal uptake of FDG after N-butylscopolamine or omeprazole treatment in the rat.
Asaka, M; Nakada, K; Satoh, M; Tamaki, N; Yamamoto, F; Zhao, S, 2004
)
1.05
"Omeprazole treatment did not improve asthma symptoms or lung function in children with asthma and GORD."( Acid suppression does not change respiratory symptoms in children with asthma and gastro-oesophageal reflux disease.
Bentsen, BS; Carlsen, KC; Closs, O; Handeland, M; Holm, HK; Johannesdottir, GB; Knudsen, PK; Sandvik, L; Størdal, K, 2005
)
1.77
"Omeprazole pretreatment ameliorated DMP-777-induced parietal cell loss as well as foveolar hyperplasia."( Omeprazole treatment ameliorates oxyntic atrophy induced by DMP-777.
Car, BD; Goldenring, JR; Nomura, S; Ogawa, M, 2006
)
2.5
"Omeprazole treats gastro-oesophageal reflux disease (GORD) by inhibition of acid secretion whereas alginate based reflux suppressants work by forming a low density raft of near neutral pH which floats on the stomach contents and physically impedes gastro-oesophageal reflux. "( Administration of an alginate based gastric reflux suppressant on the bioavailability of omeprazole.
Baxter, T; Choubey, S; Dettmar, PW; Hampson, FC; Jain, A; Little, SL, 2006
)
2
"All omeprazole-treated patients showed improvement of laryngeal features and symptoms. "( Silent reflux: ex juvantibus criteria for diagnosis and treatment of laryngeal disorders.
Barbara, M; Di Stadio, A; Monini, S; Vestri, A, 2006
)
0.89
"Omeprazole treatment increased bacteria colonization and MPO activity in mice stomachs. "( Effects of a one-week treatment with acid gastric inhibitors on Helicobacter pylori-infected mice.
Arçari, DP; Bartchewsky, W; Gambero, A; Hoehr, NF; Maróstica, M; Pedrazzoli, J; Ribeiro, ML; Trevisan, M, 2007
)
1.78
"Omeprazole treatment (10(-8), 10(-6) and 10(-4)M) for 12 and 24 h did not promote cell proliferation."( Omeprazole promotes gastric epithelial cell migration.
Chang, FY; Chi, CW; Cho, CH; Lee, SD; Lin, HC; Lin, HY; Luo, JC; Ng, KM, 2008
)
2.51
"Omeprazole pretreatment did not prevent the development of canaliculi and the reduction in the number of tubulovesicles in parietal cells after histamine."( Comparison of the effect of omeprazole--a substituted benzimidazole--and ranitidine--a potent H2-receptor antagonist--on histamine-induced gastric acid secretion and the ultrastructure of canine parietal cells.
Cieszkowsky, M; Dabroś, W; Konturek, J; Konturek, SJ; Stachura, J; Zakrzewska, J, 1983
)
1.28
"Omeprazole treatment reduced corpus somatostatin mRNA to 59 +/- 5% (P < 0.05), and elevated SSTR mRNA to 140 +/- 3% of control (P < 0.01)."( Differential expression and regulation of SSTR2 messenger RNA in rat gastric antrum and corpus.
Brenna, E; Dimaline, R; Sandvik, AK; Waldum, HL, 1995
)
1.01
"Omeprazole remains a treatment of choice in patients with Zollinger-Ellison syndrome."( Omeprazole. An update of its pharmacology and therapeutic use in acid-related disorders.
McTavish, D; Wilde, MI, 1994
)
2.45
"Omeprazole treatment produced a greater colonization of the body with bacteria traversing the entire gland."( The importance of local acid production in the distribution of Helicobacter felis in the mouse stomach.
Danon, SJ; Lee, A; Moss, ND; O'Rourke, JL, 1995
)
1.01
"Omeprazole pretreatment significantly raised the median gastric pH (from pH 1.1 to pH 4.7, p < 0.0001), but had no significant influence on gastric emptying time of the pH capsule (median = 4.3 vs 4.9 hours)."( The influence of gastric pH on the pharmacokinetics of fluconazole: the effect of omeprazole.
Lach, P; Laufen, H; Riedel, KD; Yeates, RA; Zimmermann, T, 1994
)
1.24
"Omeprazole treatment and small ulcer size significantly increased the probability of healing, but smoking had no significant effect."( A double-blind, randomized, parallel group study of omeprazole and ranitidine in Korean patients with gastric ulcer.
Chang, R; Choi, KW; Chung, JM; Lee, SI; Min, YI; Park, KN; Sun, HS; Wong, EC; Yang, US; Yoon, CM,
)
1.1
"Omeprazole treatment did not improve asthma symptoms during the day or night, or peak expiratory flow rate readings."( Omeprazole in the treatment of asthmatics with nocturnal symptoms and gastro-oesophageal reflux: a placebo-controlled cross-over study.
Butland, RJ; Ford, GA; Oliver, PS; Prior, JS; Wilkinson, SP, 1994
)
2.45
"For omeprazole-treated tissues, altered and degenerated parietal cells occurred throughout the gland and averaged 62% of total parietal cells."( Inhibiting gastric H(+)-K(+)-ATPase activity by omeprazole promotes degeneration and production of parietal cells.
Forte, JG; Karam, SM, 1994
)
1.03
"Omeprazole treatment rapidly caused an increase in the serum gastrin concentration and the antral gastrin mRNA level after 3 days."( Expression of the gastric H+/K(+)-ATPase and histidine decarboxylase during omeprazole treatment.
Arnold, R; Eissele, R; Gross, M; Koop, H; Körtner, G; Simon, B; Swarovsky, B, 1994
)
1.24
"Omeprazole treatment of normal volunteers resulted in a significant change in postprandial gastric pH (pH 6.4 +/- 0.3 vs."( Hypochlorhydria from short-term omeprazole treatment does not inhibit intestinal absorption of calcium, phosphorus, magnesium or zinc from food in humans.
Pedrosa, M; Russell, RR; Saltzman, JR; Sepe, TE; Serfaty-Lacrosniere, C; Voytko, D; Wood, RJ, 1995
)
1.3
"Omeprazole treated animals (group II) showed statistically significant lower levels of serum amylase and pancreatic trypsinogen content (P < 0.05)."( [Effect of omeprazole administration on pancreatic content of enzymes in rats].
Coelho, AM; da Cunha, JE; Kubrusly, MS; Machado, MC; Molan, NA; Montagnini, AL; Pinotti, HW,
)
1.24
"Omeprazole treatment (20 mg twice daily) does not affect the pharmacokinetics of orally ingested ethanol in healthy male subjects."( Omeprazole therapy does not affect pharmacokinetics of orally administered ethanol in healthy male subjects.
Brier, ME; Levinson, SS; Minocha, A; Rahal, PS, 1995
)
2.46
"Omeprazole treatment leads to the appearance of numerous vacuoles (with profile diameter greater than 500 nm); such vacuoles are not observed in the ECL cells of rats treated with alpha-FMH or alpha-FMH+omeprazole."( Ultrastructure of enterochromaffin-like cells in rat stomach: effects of alpha-fluoromethylhistidine-evoked histamine depletion and hypergastrinemia.
Andersson, K; Chen, D; Håkanson, R; Sundler, F; Zhao, CM, 1996
)
1.02
"Omeprazole treatment produced a significant fall in the number of H."( Suppression of Helicobacter pylori colonization with omeprazole.
Fukuda, Y, 1996
)
1.26
"Omeprazole pretreatment did not change the absorption parameters."( Influence of gastric acid secretion blockade and food intake on the bioavailability of a potassium diclofenac suspension in healthy male volunteers.
De Nucci, G; Dias, HB; Moreno, H; Moreno, RA; Muscara, MN; Poli, A; Ribeiro, W, 1996
)
1.02
"Omeprazole treatment produces lower intragastric pH values 4 weeks after cure of Helicobacter pylori infection than before. "( Intragastric pH during treatment with omeprazole: role of Helicobacter pylori and H. pylori-associated gastritis.
Armstrong, D; Blum, AL; Börsch, G; Idström, JP; Labenz, J; Stolte, M; Verdú, EF, 1996
)
2.01
"The omeprazole treated group showed the highest and more sustained plasma gastrin levels."( Comparative study of plasma gastrin levels in rats after two months of ebrotidine administration.
Ballesta, A; Gómez, F; Ortiz, JA; Romero, A; Sacristán, A; Villamayor, F, 1997
)
0.78
"The omeprazole-treated groups also showed an increase in the number of immunoreactive gastrin cells in the pyloric mucosa and an enhancement in the intensity of immunoreaction."( Alterations in gastrin cells induced by short-term omeprazole treatment in the rat antrum: an immunocytochemical and in situ hybridization study.
Bolkent, S; Yilmazer, S, 1997
)
1.03
"In omeprazole-treated rats, the healing of gastric mucosal lesions was accelerated in comparison with those of untreated rats. "( Increased hepatocyte growth factor content in rat stomach during omeprazole treatment.
Chiba, T; Fukui, H; Hassan, MS; Kawamura, M; Kinoshita, Y; Kishi, K; Maekawa, T; Matsushima, Y; Okada, A; Waki, S, 1998
)
1.16
"Omeprazole treatment led to higher mean overall scores on the Asthma Quality of Life Questionnaire, and on the subdomains of activity limitation, symptoms, and emotions (p = 0.039, 0.049, 0.024, 0.040)."( Omeprazole improves peak expiratory flow rate and quality of life in asthmatics with gastroesophageal reflux.
Levin, TR; McQuaid, KR; Sperling, RM, 1998
)
2.46
"Omeprazole pretreatment did not influence eradication rates."( Dual versus triple therapy: comparison of five antibiotic regimens for eradication of Helicobacter pylori in a prospective, randomized study.
Bojarski, C; Epple, HJ; Fromm, M; Kirstein, FW; Riecken, EO; Schulzke, JD; Victor, L, 1998
)
1.02
"Omeprazole treatment significantly reduced persistent reflux-related symptoms and normalized psychological well-being compared with ranitidine in poorly responsive symptomatic patients with GERD."( Health-related quality of life outcomes of omeprazole versus ranitidine in poorly responsive symptomatic gastroesophageal reflux disease.
Maton, PN; Orlando, RC; Revicki, DA; Sorensen, S,
)
1.84
"With omeprazole treatment, gastric nitrite levels after the nitrate meal were markedly increased at 154 micromol/L (range, 49-384 micromol/L; P < 0.001)."( Omeprazole and dietary nitrate independently affect levels of vitamin C and nitrite in gastric juice.
Carswell, A; McColl, KE; Mowat, C; Wirz, A, 1999
)
2.2
"Omeprazole treatment resulted in a decrease of acid reflux per 24 h from 23.4% (7.9-39.3) to 0.0% (0.0-2.9) in H."( The influence of Helicobacter pylori on oesophageal acid exposure in GERD during acid suppressive therapy.
Ganesh, S; Kleibeuker, JH; Klinkenberg-Knol, EC; Kuipers, EJ; Lamers, CB; Peters, FT; Sluiter, WJ, 1999
)
1.02
"More omeprazole-treated patients reported improved heartburn resolution at 2 weeks (49.0% vs 33.3%; P=.007) and 4 weeks (58.6% vs 35.0%; P<.001) compared with ranitidine-treated patients. "( Effectiveness and costs of omeprazole vs ranitidine for treatment of symptomatic gastroesophageal reflux disease in primary care clinics in West Virginia.
Kaplan-Machlis, B; Revicki, DA; Spiegler, GE; Zodet, MW, 2000
)
1.12
"Omeprazole treatment increased meal-stimulated plasma gastrin concentrations from day 0 to day 8 in the homozygous EMs and heterozygous EMs by 16% (NS) and 157% (P = 0."( Effects of omeprazole on intragastric pH and plasma gastrin are dependent on the CYP2C19 polymorphism.
Bertilsson, L; Dahl, ML; Sagar, M; Seensalu, R; Tybring, G, 2000
)
1.42
"In omeprazole treated animals, serum gastrin levels showed statistically significant increases compared with the control and ethanol treated animals."( Effects of omeprazole on ethanol lesions.
Abdel Fattaha, NA; Abdel-Rahman, MS, 2000
)
1.21
"Omeprazole treatment stimulated expression of the transgene and the endogenous CgA gene selectivity in the gastric corpus (3-4-fold)."( Neuroendocrine-specific and gastrin-dependent expression of a chromogranin A-luciferase fusion gene in transgenic mice.
Cramer, T; Höcker, M; O'Connor, DT; Rosewicz, S; Wang, TC; Wiedenmann, B, 2001
)
1.03
"Omeprazole treatment is associated with hypergastrinaemia, resulting in growth of the oxyntic mucosa in general and the enterochromaffin-like (ECL) cells in particular."( Long-term omeprazole treatment suppresses body weight gain and bone mineralization in young male rats.
Chen, D; Cui, GL; Syversen, U; Waldum, HL; Zhao, CM, 2001
)
1.43
"Omeprazole treatment of young male rats reduces body weight and bone mass gain. "( Long-term omeprazole treatment suppresses body weight gain and bone mineralization in young male rats.
Chen, D; Cui, GL; Syversen, U; Waldum, HL; Zhao, CM, 2001
)
2.16
"The omeprazole-treated groups also showed an increase in the number of somatostatin-containing cells in fundus mucosa."( Effects of acid inhibition on somatostatin-producing cells in the rat gastric fundus.
Bolkent, S; Kaya, F; Oztürk, M; Yilmazer, S, 2001
)
0.79
"When omeprazole-treated mice were treated with antibiotics alone, elevated plasma gastrin levels returned to baseline and D cell numbers returned to resting levels despite persistent hypochlorhydria."( Hypergastrinemia in response to gastric inflammation suppresses somatostatin.
Ferguson, A; Merchant, JL; Rieder, G; Samuelson, LC; Zavros, Y, 2002
)
0.77
"Omeprazole treatment further augmented clarithromycin Cmax and AUC0-2h in gastric juice approximately 2-fold (P < 0.05)."( Transfer of clarithromycin to gastric juice is enhanced by omeprazole in Helicobacter pylori-infected individuals.
Bento, AP; Calafatti, SA; de Nucci, G; Deguer, M; Dias, FE; Ferraz, JG; Lerner, F; Mendes, FD; Ortiz, RA; Pedrazzoli, J; Pereira, AA; Piovesana, H, 2001
)
1.28
"Omeprazole treatment for 4 weeks increased the oxyntic mucosal weight and thickness by 15-20%."( Effects of CCK2 receptor blockade on growth parameters in gastrointestinal tract and pancreas in rats.
Björkqvist, M; Chen, D; de la Cour, CD; Gagnemo-Persson, C; Håkanson, R; Kitano, M; Norlén, P; Zhao, CM, 2001
)
1.03
"Omeprazole treatment of portacaval--shunted rats suppressed or even reversed the somatostatin cell hyperplasia after portacaval shunt alone."( Somatostatin cells in the oxyntic mucosa of hypo- or hypergastrinemic rats.
Chen, D; Håkanson, R; Sundler, F; Uribe, A, 1992
)
1
"In omeprazole (0.3 mM)-pretreated frog fundic mucosae, in which H+ secretion was totally inhibited, 16,16-dimethyl prostaglandin E2 (dmPGE2) induced a significant decrease in intracellular pH (pHi) in OPC simultaneously with a significant increase in pHi in adjacent muscularis mucosae, an effect abolished by removal of ambient Cl- or addition of 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS) (0.5 mM)."( Prostaglandin stimulates Cl(-)-HCO3- exchange in amphibian oxynticopeptic cells.
Carter, KJ; Goddard, PJ; Silen, W; Yanaka, A, 1992
)
0.8
"Omeprazole treatment healed duodenal ulceration, improved gastritis temporarily, and suppressed but did not eradicate H."( Short report: the effect of omeprazole on Helicobacter pylori and associated gastritis.
Daw, MA; Deegan, P; Leen, E; O'Moráin, C, 1991
)
1.3
"Omeprazole-treated rats gavaged with nitrosation-proficient bacteria were treated with nitrosamines and/or precursors and compared to control animals that received no omeprazole treatment/no bacteria."( Bacterial formation of N-nitroso compounds from administered precursors in the rat stomach after omeprazole-induced achlorhydria.
Bartsch, H; Béréziat, JC; Calmels, S; Ohshima, H, 1991
)
1.22
"Omeprazole-treated patients reported significantly less daytime epigastric pain (P = 0.02) and heartburn (P = 0.04) after two weeks than ranitidine-treated patients."( A comparison of omeprazole and ranitidine for duodenal ulcer in South African patients. A multiracial study.
Danilewitz, MD; Garisch, JA; Marks, IN, 1991
)
1.35
"Omeprazole has a simple treatment regimen: 20 mg once daily is recommended in the routine treatment of DU, GU and RO."( Treatment of acid-related disorders with gastric acid inhibitors: the state of the art.
Blum, AL, 1990
)
1
"Omeprazole-treated rats on the normal diet had no significant reduction in the absorption of ferric, ferrous, or food iron."( Inhibition of iron absorption by omeprazole in rat model.
Adams, P; Flanagan, P; Golubov, J, 1991
)
1.28
"In omeprazole pretreated rats, gavage with ethanol resulted in a significant twofold worsening of duodenal injury."( Chronic omeprazole treatment increases duodenal susceptibility to ethanol injury in rats.
Bezabah, S; Erickson, RA; Jonas, G; Lifrak, E; Tarnawski, AS, 1991
)
1.23
"Omeprazole-treated patients took fewer antacids (p less than 0.05) over the first 2 wk."( Omeprazole provides quicker symptom relief and duodenal ulcer healing than ranitidine.
Bateson, MC; Burke, GJ; Dickinson, RJ; Dronfield, MW; Green, JR; Keeling, PW; McFarland, RJ; O'Donoghue, DP; Peers, EM; Shreeve, DR, 1990
)
2.44
"In omeprazole-treated dogs, a sustained gastrin release was observed during a 10-h period after feeding, although greater than 95% of the meal had left the stomach after 4 h."( Effect of acute suppression of acid secretion by omeprazole on postprandial gastrin release in conscious dogs.
De Graef, J; Simoens, C; Woussen-Colle, MC, 1989
)
1.05
"Omeprazole treatment was well tolerated by the women and Apgar scores and subsequent progress of the babies were acceptable."( Effect of single-dose omeprazole on intragastric acidity and volume during obstetric anaesthesia.
Flynn, RJ; Gillon, KR; Moore, J; Sampaio, M; Wilson, CM, 1989
)
1.31
"Omeprazole treatment resulted in anacidity (pH values above 6.0) in 14 individuals 30 min after the liver dose and in 15 individuals after 60 min."( The effect of omeprazole on gastric acidity and the absorption of liver cobalamins.
Aadland, E; Kittang, E; Røhss, K; Schjønsby, H, 1987
)
1.35
"Omeprazole pretreatment 50 mg/kg s.c."( The influence of omeprazole on the protective effects of secretagogues against ethanol-induced gastric ulceration in rats.
Cho, CH; Ogle, CW; Wong, SH, 1987
)
1.33
"Omeprazole treatment resulted in a 3- to 5-fold increase in the ECL cell density."( Hypergastrinemia after blockade of acid secretion in the rat: trophic effects.
Carlsson, E; Håkanson, R; Larsson, H; Mattsson, H; Sundler, F, 1986
)
0.99
"Omeprazole treatment resulted in an increased mucosal thickness as a result of a proportional increase in all types of epithelial cells with the exception of the endocrine cells."( Alterations in gastric mucosal morphology induced by long-term treatment with omeprazole in rats.
Blom, H, 1986
)
1.22
"Dogs treated with omeprazole had a significantly higher MPT ± SD intragastric pH ≥3 (91.2% ± 11.0%), ≥4 (86.9% ± 13.7%) and mean ± SD pH (5.4 ± 0.8) than dogs treated with placebo (19.7% ± 15.5%, 28.3 ± 20.7, and 2.4 ± 1.0, respectively) (P < .001 for all)."( A prospective, randomized, masked, placebo-controlled crossover study for the effect of 10 mg omeprazole capsules on gastric pH in healthy dogs.
Fitzgerald, S; Gaier, A; Grubb, L; Price, J; Tolbert, MK, 2021
)
1.17
"Treatment with omeprazole (OMP) (20 μM), a non-specific inducer of CYP450 induced approximately 10-fold increase in CYP1A1 activity after 2 h of treatment."( Involvement of astrocytic CYP1A1 isoform in the metabolism and toxicity of the alkaloid pyrrolizidine monocrotaline.
Batatinha, MJM; Carvalho, JLC; Costa, SL; El-Bachá, RS; Nascimento, RP; Oliveira, JL; Pires, TRC; Santos, WA; Silva, VDA, 2017
)
0.79
"Cotreatment with omeprazole did not reduce indomethacin-induced intestinal bleeding."( Suppression of contractile activity in the small intestine by indomethacin and omeprazole.
Bhattarai, D; Dial, EJ; Lichtenberger, LM; Phan, TM; Uray, K, 2015
)
0.97
"Treatment with omeprazole significantly reduced serum Mg2+ and Ca2+ levels. "( Dietary Inulin Fibers Prevent Proton-Pump Inhibitor (PPI)-Induced Hypocalcemia in Mice.
Bindels, RJ; de Baaij, JH; Gommers, LM; Hess, MW; Hoenderop, JG, 2015
)
0.77
"Pretreatment with omeprazole or MDLA led to an increase in the uptake of Periodic Acid Schiff (PAS) stain in the glandular part of the gastric tissue, raised levels of prostaglandin E2 (PGE2) and superoxide dismutase (SOD), and a reduction in malondialdehyde (MDA) concentrations."( Acute Toxicity and Gastroprotection Studies of a New Schiff Base Derived Manganese (II) Complex against HCl/Ethanol-Induced Gastric Ulcerations in Rats.
Adam, H; Al-Obaidi, MM; Ali, HM; Alkotaini, B; Batran, RA; Dhiyaaldeen, SM; El-Ferjani, RM; Hashim, NM; Ibrahim, MY, 2016
)
0.76
"Treatment with omeprazole reduced endothelium-dependent aortic responses to acetylcholine without causing hypertension."( Omeprazole impairs vascular redox biology and causes xanthine oxidoreductase-mediated endothelial dysfunction.
de Angelis, CD; Guimarães, DA; Oliveira-Paula, GH; Pinheiro, LC; Portella, RL; Tanus-Santos, JE, 2016
)
2.22
"Treatment with omeprazole or pantoprazole had no effect on spontaneous nitroblue tetrazolium (NBT) test results."( The effect of short-term oral treatment with omeprazole or pantoprazole on the function of polymorphonuclear neutrophils.
Dabrowski, A; Garley, M; Jabłońska, E; Jamiołkowski, J; Kostrzewska, M; Ratajczak-Wrona, W, 2017
)
1.05
"Treatment with omeprazole did not result in C. difficile positive stool culture and had no significant effect on neutrophil function."( The effect of omeprazole treatment on the gut microflora and neutrophil function.
Dabrowski, A; Garley, M; Jabłońska, E; Jamiołkowski, J; Jurkowska, G; Kostrzewska, M; Olszańska, D; Ratajczak-Wrona, W; Świdnicka-Siergiejko, A, 2017
)
1.16
"Treatment by omeprazole is effective for treatment of asthmatic patients with GERD."( The effect of omeprazole on asthmatic adolescents with gastroesophageal reflux disease.
Fallahi, GH; Khorasani, EN; Mansouri, F; Rezaei, N,
)
0.84
"Treatment with omeprazole significantly improved voice quality showing the greatest changes in the mean scores of majority of voice range profile parameters."( [Usefulness of assessment of voice capabilities in female patients with reflux-related dysphonia].
Adamonis, K; Siupsinskiene, N; Toohill, RJ, 2009
)
0.69
"Treatment with omeprazole alone modifies clinical manifestations and endoscopic findings in patients with PL. "( Posterior laryngitis: effects of treatment with omeprazole alone.
Argüelles-Arias, F; Carmona, I; Galera-Ruiz, H; Herrerías, JM; Muñoz-Borje, F; Rodríguez-Téllez, M, 2002
)
0.92
"Treatment with omeprazole, clarithromycin and amoxycillin triple therapy eradicated H."( The role of triple therapy, age, gender and smoking on the genotoxic effects of Helicobacter pylori infection.
Demiray, M; Ercan, I; Evke, E; Gulten, M; Gulten, T; Karakaya, AE; Sardas, S; Tokyay, N,
)
0.47
"Treatment with omeprazole significantly reduced mean gastric severity score compared to placebo (omeprazole: 0.65 +/- 0.17, placebo: 1.09 +/- 0.18; P = .028), but also was associated with increased frequency of diarrhea during the race (omeprazole 54%, placebo 21%; P = .017)."( Efficacy of omeprazole for the prevention of exercise-induced gastritis in racing Alaskan sled dogs.
Davis, MS; Mandsager, RE; McCullough, SM; Nelson, SL; Payton, ME; Roberts, J; Willard, MD,
)
0.85
"Treatment with omeprazole or pantoprazole prior to urea breath test (UBT) was associated with low false negative results, while lansoprazole and esomeprazole caused clinically unacceptable high false negative rates (pantoprazole 2.2% vs."( Masking of 13C urea breath test by proton pump inhibitors is dependent on type of medication: comparison between omeprazole, pantoprazole, lansoprazole and esomeprazole.
Aeed, H; Avni, Y; Boaz, M; Levine, A; Moss, SF; Niv, Y; Shabat-Sehayek, V; Shevah, O; Shirin, H, 2004
)
0.87
"Pretreatment with omeprazole did not change the RX-77368 (15 ng)-induced increase in permeability, but quickened the recovery of permeability after the peak."( Evaluation of early gastric mucosal permeability induced by central thyrotropin-releasing hormone administration.
Itoh, M; Joh, T; Kaneko, H; Kataoka, H; Nomura, T; Ohara, H; Oshima, T; Sasaki, M; Sobue, M; Suzuki, H; Takahashi, N; Watanabe, K, 2005
)
0.65
"Treatment with omeprazole provides superior symptom relief compared to ranitidine, cisapride, and placebo in the treatment of H. "( A randomized trial comparing omeprazole, ranitidine, cisapride, or placebo in helicobacter pylori negative, primary care patients with dyspepsia: the CADET-HN Study.
Armstrong, D; Barkun, A; Chiba, N; Escobedo, S; Lee, J; Sinclair, P; Smyth, S; Thomson, A; Veldhuyzen van Zanten, SJ, 2005
)
0.97
"Treatment with omeprazole or melatonin prevented this damage as well as the changes in biochemical parameters, and melatonin appeared to be more efficient than omeprazole in protecting the mucosa."( Protective effect of melatonin and omeprazole against alendronat-induced gastric damage.
Arbak, S; Dülger, GA; Ersoy, Y; Goren, FO; Sener, G; Ulusoy, NB, 2005
)
0.95
"Treatment with omeprazole significantly improved QL in both LPR subgroups patients."( Quality of life in laryngopharyngeal reflux patients.
Adamonis, K; Siupsinskiene, N; Toohill, RJ, 2007
)
0.68
"Treatment with omeprazole did not change bronchial responsiveness to methacholine (basal: 0.16 mg, 0.02-1.27; omeprazole: 0.15 mg, 0.02-1.60); omeprazole decreased the tussive response to capsaicin (basal: 0.08 nmol, 0.08-2.46; omeprazole: 0.61 nmol, 0.08-9.84, p<0.001) only in patients with pathological reflux."( Omeprazole reduces the response to capsaicin but not to methacholine in asthmatic patients with proximal reflux.
Benini, L; Bonella, F; Brotto, E; Corradini, G; De Iorio, F; Ferrari, M; Lo Cascio, V; Locatelli, F; Tacchella, N; Vantini, I, 2007
)
2.12
"Treatment with omeprazole at an initial dosage of 0.7 mg x kg(-1) x day(-1) (in 2 divided doses) was followed by dual-channel pH study after 14 days."( Omeprazole for gastroesophageal reflux disease in the first 2 years of life: a dose-finding study with dual-channel pH monitoring.
Bishop, J; Furman, M; Thomson, M, 2007
)
2.12
"Pretreatment of omeprazole does not affect the absorption of domperidone maleate, but leads to a moderately decreased rate of absorption of the free base."( Influence of omeprazole on pharmacokinetics of domperidone given as free base and maleate salt in healthy Chinese patients.
Chen, XY; Dai, XJ; Liu, QZ; Yu, HL; Zhang, YF; Zhang, YN; Zhong, DF, 2007
)
1.05
"Pretreatment with omeprazole (1 mg/kg) or ranitidine (0.5 mg/kg) almost completely prevented subsequent stimulation of acid secretion by histamine (40 micrograms/kg-h)."( Comparison of the effect of omeprazole--a substituted benzimidazole--and ranitidine--a potent H2-receptor antagonist--on histamine-induced gastric acid secretion and the ultrastructure of canine parietal cells.
Cieszkowsky, M; Dabroś, W; Konturek, J; Konturek, SJ; Stachura, J; Zakrzewska, J, 1983
)
0.88
"Treatment with omeprazole plus two different antibiotics has also been used in a number of studies."( The role of omeprazole and antibiotic combinations in the eradication of Helicobacter pylori--an update.
Axon, AT, 1994
)
1.01
"Treatment with omeprazole plus amoxicillin or clarithromycin resulted in encouraging Helicobacter pylori cure rates in pilot and controlled studies. "( High-dose omeprazole plus amoxicillin or clarithromycin cures Helicobacter pylori infection in duodenal ulcer disease.
Bertrams, J; Börsch, G; Domian, C; Labenz, J; Stolte, M, 1995
)
1.05
"Treatment of omeprazole induces profound inhibition of gastric acid secretion, resulting in hypergastrinaemia. "( Effect of enprostil on serum gastrin and pepsinogen A and C levels in patients on long-term treatment with omeprazole.
Biemond, I; Jansen, JB; Kuijpers, IJ; Lamers, CB; Meijer, JL, 1994
)
0.87
"Pretreatment with omeprazole did not significantly influence the bioavailability of CdA (51% vs 46% without), or the interindividual variability in bioavailability in the fasting state (C."( On the bioavailability of 2-chloro-2'-deoxyadenosine (CdA). The influence of food and omeprazole.
Albertioni, F; Juliusson, G; Liliemark, J, 1993
)
0.83
"Pretreatment with omeprazole (5-40 mumol/kg) also, significantly attenuated the ET-1-induced mucosal damage."( Gastric ulcer induced by submucosal injection of ET-1: role of potent vasoconstriction and intraluminal acid.
Fukutomi, H; Goto, K; Kashimura, H; Lazaratos, S; Miyauchi, T; Nakahara, A; Osuga, T; Urushidani, T, 1993
)
0.61
"Treatment with omeprazole for 2 weeks was also associated with lower cumulative antacid intake (P < 0.05) and reduced absenteeism from work."( Omeprazole versus famotidine in the healing and relapse of duodenal ulcer.
Dasarathy, S; Misra, SC; Sharma, MP, 1993
)
2.07
"Treatment with omeprazole and amoxycillin could provide both rapid healing of ulcers and eradication of H."( Compliance, adverse events and antibiotic resistance in Helicobacter pylori treatment.
Malfertheiner, P, 1993
)
0.63
"Pretreatment with omeprazole (60 mg/kg, intraperitoneally) completely inhibited the acid secretory response and the enhancement of GMBF induced by both submaximal (60 micrograms/kg/hr) and maximal doses of pentagastrin."( Pathways mediating pentagastrin-induced mucosal blood flow response in rat stomachs.
Kato, S; Okabe, S; Takeuchi, K, 1996
)
0.62
"Treatment with omeprazole 80 mg b.d."( Dose-response of omeprazole combined with amoxycillin on duodenal ulcer healing and eradication of Helicobacter pylori.
Braden, B; Lembcke, B; Londong, W; Pommerien, W; Schultze, V; Wrangstadh, M, 1996
)
0.97
"Treatment with omeprazole, a proton pump inhibitor, for 2 months, followed by famotidine, resulted in clinical improvement with resolution of the gastroduodenal lesions and protein loss."( Varioliform gastritis and duodenitis associated with protein-losing gastroenteropathy, treated with omeprazole.
Kuroda, T; Miura, T; Murata, I; Otsuki, M; Tabaru, A; Yoshikawa, I, 1996
)
0.85
"Treatment with omeprazole or placebo lasted 4 wk; those whose ulcers remained unhealed continued the same treatment regimen for an additional 4 wk. "( Comparison of once-daily doses of omeprazole (40 and 20 mg) and placebo in the treatment of benign gastric ulcer: a multicenter, randomized, double-blind study.
Colón Pagán, JR; Gilde, LR; Kogut, DG; McCullough, AJ; Shah, U; Simon, TJ; Valenzuela, JE; Whipple, J, 1996
)
0.93
"Treatment with omeprazole 20 mg and amoxycillin 1000 mg twice daily for 14 days altered the normal microflora in the oral, gastric and intestinal tract and antibiotic resistant microorganisms increased in numbers in the intestinal microflora."( Effects of omeprazole and amoxycillin on the human oral and gastrointestinal microflora in patients with Helicobacter pylori infection.
Adamsson, I; Edlund, C; Nord, CE; Seensalu, R; Sjösted, S; Stark, CA; Wikström, B, 1996
)
1.02
"Pretreatment with omeprazole evoked a 54% reduction in TNF-alpha, but had no effect on ethanol-induced mucosal damage or apoptosis, the sucralfate reduced the extent of mucosal damage by 95%, apoptosis by 39% and TNF-alpha by 52%, while ebrotidine not only prevented mucosal injury and rise in TNF-alpha, but also caused a 70% reduction in epithelial cells' apoptosis."( Gastric mucosal apoptosis induced by ethanol: effect of antiulcer agents.
Piotrowski, E; Piotrowski, J; Skrodzka, D; Slomiany, A; Slomiany, BL, 1997
)
0.62
"Treatment with omeprazole, a long-acting proton pump inhibitor of acid secretion, induces hypergastrinemia. "( Chicken parathyroid hormone gene expression in response to gastrin, omeprazole, ergocalciferol, and restricted food intake.
Gagnemo-Persson, R; Hâkanson, R; Persson, P; Samuelsson, A, 1997
)
0.89
"Pretreatment with omeprazole reduced gastric emptying rates. "( A double-blind placebo-controlled study on the effects of omeprazole on gut hormone secretion and gastric emptying rate.
Holst, JJ; Oster-Jørgensen, E; Pedersen, SA; Qvist, N; Rasmussen, L; Rehfeld, JF, 1997
)
0.88
"Only treatment with omeprazole (P < 0.0001) and lower severity of heartburn at entry (P < 0.01) were significant in predicting heartburn relief."( Omeprazole is more effective than cimetidine for the relief of all grades of gastro-oesophageal reflux disease-associated heartburn, irrespective of the presence or absence of endoscopic oesophagitis.
Axon, AT; Bate, CM; Emmas, CE; Green, JR; Murray, FE; Taylor, MD; Tildesley, G, 1997
)
2.05
"Treatment with omeprazole 20 mg every morning maintained significantly more patients in remission than treatment with ranitidine 150 mg at bedtime."( Omeprazole and ranitidine in long-term treatment of duodenal ulcer: a double-blind comparison of length of time in remission.
Aran-Suau, R; Berenguer, J; Caswell, C; Clerch, L; Da Silveira, JC; Diaz de Rojas, F; Garcia Aparicio, P; Rodrigo, L, 1998
)
2.08
"Treatment with omeprazole 20-80 mg over 1-3 years has yielded conflicting but largely disappointing results."( Continuous treatment with omeprazole 20 mg daily for up to 6 years in Barrett's oesophagus.
Cooper, BT; Cox, MA; Iqbal, TH; Neumann, CS, 1998
)
0.94
"Pretreatment with omeprazole did not reduce the cure rate for this new quadruple therapy."( A new quadruple therapy for the eradication of Helicobacter pylori. Effect of pretreatment with omeprazole on the cure rate.
Maeda, K; Nishimura, H; Oda, K; Ohkuma, K; Okabe, N; Okada, M; Oki, K; Seo, M; Shirotani, T, 1998
)
0.84
"Treatment with omeprazole reduces the effect of ranitidine in H. "( Treatment with proton pump inhibitors induces tolerance to histamine-2 receptor antagonists in Helicobacter pylori-negative patients.
Arnestad, JS; Brenna, E; Qvigstad, G; Waldum, HL, 1998
)
0.65
"Treatment with omeprazole (OME), azithromycin (AZI) and amoxicillin (AMO) resulted in encouraging Helicobacter pylori cure rates in pilot and control studies. "( Omeprazole, azithromycin and amoxicillin or amoxicillin plus clavulanic acid in eradication of Helicobacter pylori in duodenal ulcer disease.
Blazanović, A; Dmitrović, B; Ivandić, A; Karner, I; Kovac, D; Pezerović, D; Stimac, D; Stimac, T; Takac, B; Vcev, A; Vceva, A, 1998
)
2.1
"Pretreatment with omeprazole significantly decreased this adherence in a dose-dependent manner (10(-6)-10(-4)mol/L)."( Omeprazole attenuates neutrophil-endothelial cell adhesive interaction induced by extracts of Helicobacter pylori.
Fukumura, D; Ishii, H; Miura, S; Mori, M; Suzuki, H; Suzuki, M, 1999
)
2.07
"Treatment with omeprazole once daily has been shown to be superior to that with ranitidine and misoprostol in this respect."( Quality of life in arthritis patients using nonsteroidal anti-inflammatory drugs.
Wiklund, I, 1999
)
0.64
"Pretreatment with omeprazole (30 mg/kg s.c.) did not suppress the gastric hemorrhage."( Influence of rebamipide on indometacin-induced gastric hemorrhage in rats under restraint stress.
Arakawa, T; Higuchi, K; Kobayashi, K; Kuroki, T; Takaishi, O; Yamasaki, K, 1999
)
0.63
"Pretreatment with omeprazole was followed by a delay in gastric emptying of liquid at 30 min (64% (49%-66%) (omeprazole series) versus 78% (67%-83%); P < 0.01) and solid at 180 min (71% (48%-86%) (omeprazole series) versus 96% (87%-100%); P < 0.01)."( The effects of omeprazole on intragastric pH, intestinal motility, and gastric emptying rate.
Oster-Jørgensen, E; Pedersen, SA; Qvist, N; Rasmussen, L, 1999
)
0.98
"Treatment with omeprazole not only decreased the need for further dilatations, but also prolonged the mean time between any further dilatations to 26.3 months compared to 9.3 months for those on an H2-receptor antagonist (P<0.0001)."( Omeprazole therapy decreases the need for dilatation of peptic oesophageal strictures.
Barbezat, GO; Lubcke, R; Schlup, M, 1999
)
2.09
"Treatment with omeprazole or ranitidine, which completely suppressed gastric acid secretion and significantly raised plasma gastrin level, greatly reduced the formation of erosive lesions preventing the progression of these lesions to chronic gastric ulcers, and this was accompanied by the rise in gastric blood flow and plasma gastrin levels and the significant attenuation of plasma interleukin-1beta"( Role of gastric acid secretion in progression of acute gastric erosions induced by ischemia-reperfusion into gastric ulcers.
Bielanski, W; Brzozowski, T; Drozdowicz, D; Hahn, EG; Konturek, PC; Konturek, SJ; Kwiecieñ, S; Pajdo, R, 2000
)
0.65
"Treatment with omeprazole, amoxicillin, and clarithromycin resulted in eradication of the infection in all and in resolution of the clinical symptoms in 15 (80%) of 19 patients who had a follow-up examination."( Helicobacter pylori infection in recurrent abdominal pain.
Braegger, CP; Frank, F; Stallmach, T; Stricker, T, 2000
)
0.65
"Pretreatment with omeprazole (15 mumol/kg) to suppress gastric acid secretion or with L-364,718 (5 mumol/kg) to antagonize CCK receptors in the diverted state, resulted in the decline in pancreatic secretion similar to that observed after opening the GF."( Feedback control of pancreatic secretion in rats. Role of gastric acid secretion.
Bilski, J; Konturek, PK; Konturek, SJ; Krzyzek, E, 1992
)
0.61
"Treatment with omeprazole proved to be effective by stopping the vomiting immediately."( [Severe hyperemesis gravidarum--pathophysiologic observations and new therapeutic approach].
Ditschuneit, H; Glasbrenner, B; Malfertheiner, P; Swobodnik, W, 1991
)
0.62
"Treatment with omeprazole also failed to bring about healing of the ulceration which, at times, measured up to 10 cm in diameter."( Failure of ranitidine and omeprazole treatment in eosinophilic gastritis with ulceration.
Gail, K; Mihaljevic, L; Stolte, M, 1991
)
0.92
"Pretreatment with omeprazole to suppress completely gastric acid secretion in the diverted state resulted in a decline in pancreatic secretion similar to that observed after opening the GF."( The importance of gastric secretion in the feedback control of interdigestive and postprandial pancreatic secretion in rats.
Bilski, J; Konturek, SJ; Krzyzek, E, 1991
)
0.6
"Treatment with omeprazole for 14 days led to a profound hypergastrinemia, a twofold increase in antral gastrin stores, and a tenfold increase in messenger RNA."( The secretory kinetics of the G cell in omeprazole-treated rats.
Dimaline, R; Dockray, GJ; Evans, D; Hamer, C; Varro, A, 1991
)
0.89
"100) treated with omeprazole and 31 of 69 patients (45 p."( [Omeprazole (20 mg daily) compared to ranitidine (150 mg twice daily) in the treatment of esophagitis caused by reflux. Results of a double-blind randomized multicenter trial in France and Belgium].
Barbier, P; Carlsson, R; Eriksson, S; Isal, JP; Rampal, P; Zeitoun, P, 1989
)
1.51
"Treatment with omeprazole, 20 mg, increased 24-hour plasma gastrin to the same extent as after highly selective vagotomy."( Effect of omeprazole on gastric acid secretion and plasma gastrin in man.
Cederberg, C; Lind, T; Olausson, M; Olbe, L, 1989
)
1.02
"Treatment with omeprazole resulted not only in improvement of gastro-oesophageal reflux but also in alleviation of asthmatic symptoms and increases in expiratory peak flow values."( Gastro-oesophageal reflux in patients with bronchial asthma.
Depla, AC, 1989
)
0.62
"Pretreatment with omeprazole significantly reduced the amount of cell damage brought about by sodium taurocholate (p less than 0.001)."( Protection of gastric epithelial cell monolayers from a human cell line by omeprazole in vitro.
Ivey, KJ; Razandi, M; Romano, M, 1989
)
0.83
"Treatment with omeprazole also gave faster and more pronounced pain relief."( Clinical perspectives of drugs inhibiting acid secretion--H+K+-ATPase inhibitors.
Walan, A, 1986
)
0.61
"Treatment with omeprazole also raised stomach weight and antral gastrin and gastrin cell density, reduced antral somatostatin cell density, but did not affect enterochromaffin cell density."( Time-course of development and reversal of gastric endocrine cell hyperplasia after inhibition of acid secretion. Studies with omeprazole and ranitidine in intact and antrectomized rats.
Carlsson, E; Håkanson, R; Larsson, H; Mattsson, H; Nilsson, G; Seensalu, R; Sundler, F; Wallmark, B, 1988
)
0.82
"Pretreatment with omeprazole partially restored a quantitative reduction and a qualitative change of carbohydrate portion in corpus mucus glycoprotein induced by acetylsalicylic acid."( Effects of omeprazole on rat gastric mucus glycoproteins with acetylsalicylic acid-induced gastric damage.
Hotta, K; Ishihara, K; Kuwata, H; Murayama, N; Ohara, S,
)
0.84
"Treatment with omeprazole was evaluated in nine patients with the Zollinger-Ellison syndrome, in whom the effect of H2-receptor antagonists had become inadequate. "( Omeprazole in the Zollinger-Ellison syndrome.
Bardram, L; Stadil, F, 1986
)
2.07

Toxicity

Omeprazole has been linked to methotrexate toxicity. Since September 1989, 143 adverse reactions have been reported to pharmacovigilance centres. 37 neurological and psychiatric side effects, especially confusion in patients with hepatic diseases and/or advanced age.

ExcerptReferenceRelevance
" The pattern of adverse events reported during long-term treatment was similar to the adverse-event profile in short-term treatment with omeprazole (n = 2,818), ranitidine (n = 1,572) and cimetidine (n = 891)."( Safety experience from long-term treatment with omeprazole.
Joelson, IB; Joelson, S; Lundborg, P; Walan, A; Wallander, MA, 1992
)
0.74
"Although most clinical trials encompass aspects of safety, methods for assessing the safety of a drug by recording adverse events have been poorly studied."( Adverse event monitoring in clinical trials of felodipine and omeprazole.
Lundborg, P; Svärdsudd, K; Wallander, MA, 1992
)
0.52
" In conclusion, omeprazole was far superior to ranitidine in preventing recurrence, a goal achieved without adverse events and significant abnormalities in the oxyntic mucosal exocrine or endocrine cells but with a moderate increase in basal gastrin levels."( Prevention of relapse of reflux esophagitis after endoscopic healing: the efficacy and safety of omeprazole compared with ranitidine.
Backman, L; Ekström, P; Enander, LK; Falkmer, S; Fausa, O; Grimelius, L; Havu, N; Lind, T; Lönroth, H; Lundell, L, 1991
)
0.84
" Both drugs were generally well tolerated, and the number of adverse events in the two treatment groups were similar."( The effect of omeprazole and ranitidine on ulcer healing, relief of symptoms, and incidence of adverse events in the treatment of duodenal ulcer patients.
Backman, L; Granström, L; Kager, L; Kollberg, B; Lindberg, G; Moberg, S; Nilsson, LH; Seensalu, R; Sidenvall, L; Sörstad, J, 1991
)
0.64
" Isolated, non-specific adverse events which might be attributable to omeprazole have included nausea, dizziness, headache and diarrhoea."( The clinical safety of omeprazole.
Sölvell, L, 1990
)
0.82
" During maintenance therapy with omeprazole, no endoscopically verified relapses occurred, and no drug-related adverse effects were seen."( Efficacy and safety of omeprazole in the long-term treatment of peptic ulcer and reflux oesophagitis resistant to ranitidine.
Brunner, GH; Creutzfeldt, W; Lamberts, R, 1990
)
0.87
" This therapeutic advantage was achieved without adverse events and without significant abnormalities in the endocrine or exocrine cell population of the oxyntic mucosa."( Prevention of relapse of reflux oesophagitis after endoscopic healing: the efficacy and safety of omeprazole compared with ranitidine.
Lundell, L, 1990
)
0.5
" The incidence of serious adverse events reported in comparative short-term studies with H2-receptor antagonists and placebo were similar."( The clinical safety of omeprazole.
Sölvell, L, 1989
)
0.59
" A search for adverse events during short-term treatment with omeprazole has been made, based on data from published comparative trials, data on file at the manufactor's (Hässle Research Laboratories, Mölndal, Sweden) and personal series."( Safety profile of omeprazole. Adverse events with short-term treatment.
Nelis, GF, 1989
)
0.85
"Based on the experience from more than 10,000 individuals omeprazole has been found to be safe and is well tolerated."( Omeprazole: long-term safety.
Arnold, R; Koop, H, 1989
)
1.96
" The lack of significant adverse effects has revealed a degree of tolerability that, to write a review of the adverse effects, poses a difficult task."( A comparative overview of the adverse effects of antiulcer drugs.
Piper, DW, 1995
)
0.29
"There is an extensive literature on the adverse effects of drugs that inhibit gastric acid secretion."( Safety of acid-suppressing drugs.
Berlin, RG; Castagnoli, N; Festen, HP; Hawkey, CJ; Lam, SK; Langman, MJ; Lundborg, P; Parkinson, A; Smallwood, RA, 1995
)
0.29
" The H2 antagonists differ in potency, pharmacodynamic effect, pharmacokinetics in certain patient groups, drug interactions, and adverse effects."( Efficacy, safety, and cost issues in managing patients with gastroesophageal reflux disease.
Garnett, WR, 1993
)
0.29
" Since September 1989, 143 adverse reactions have been reported to pharmacovigilance centres and Astra France: 37 neurological and psychiatric side effects, especially confusion in patients with hepatic diseases and/or advanced age; 35 cutaneous reactions, generally rash and urticaria; 22 hematological effects: leucopenia and agranulocytosis have been reported but the relation with omeprazole is very uncertain; 10 gastrointestinal effects, generally diarrhoea, nausea, vomiting and abdominal pain; 8 hepatic disorders, especially moderate elevation of aminotransferases."( [Evaluation of unexpected and toxic effects of omeprazole (Mopral) reported to the regional centers of pharmacovigilance during the first 22 postmarketing months].
Bidault, I; Castot, A; Dahan, R; Efthymiou, ML,
)
0.56
" Minor adverse events include headache, diarrhoea, dizziness, pruritus and rash."( Safety of proton pump inhibitors--an overview.
Arnold, R, 1994
)
0.29
" No significant pathological findings were noted, and no adverse events were attributable to the study treatments."( Omeprazole v ranitidine for prevention of relapse in reflux oesophagitis. A controlled double blind trial of their efficacy and safety.
Dent, J; Hetzel, DJ; Mackinnon, M; Narielvala, FM; Reed, W; Shearman, DJ; Solcia, E; Yeomans, ND, 1994
)
1.73
" Omeprazole appears to be safe for short-term use, but further studies are needed to assess long-term safety because the significance of chronically elevated gastrin levels in children is unknown."( Efficacy and safety of omeprazole for severe gastroesophageal reflux in children.
Gunasekaran, TS; Hassall, EG, 1993
)
1.51
" The use of such therapies, however, may be impeded by a number of major disadvantages, including reduced patient compliance, the incidence of adverse events and primary or acquired antibiotic resistance."( Compliance, adverse events and antibiotic resistance in Helicobacter pylori treatment.
Malfertheiner, P, 1993
)
0.29
" These results demonstrate that lansoprazole is a safe and effective inhibitor of gastric acid hypersecretion in patients with Zollinger-Ellison syndrome."( Prospective study of efficacy and safety of lansoprazole in Zollinger-Ellison syndrome.
Feigenbaum, K; Gardner, JD; Jensen, RT; Koviack, PD; Maton, PN; Metz, DC; Pisegna, JR; Ringham, GL, 1993
)
0.29
" Zimeldine was launched in the international market but had to be withdrawn when it caused severe unexpected adverse reactions."( Problems with toxicity studies in the assessment of new drugs.
Werkö, L, 1993
)
0.29
" These results demonstrate that long-term treatment with lansoprazole is both safe and effective in patients with Zollinger-Ellison syndrome, and suggest that this drug will be useful in such patients."( Prospective study of the long-term efficacy and safety of lansoprazole in patients with the Zollinger-Ellison syndrome.
Feigenbaum, KM; Jensen, RT; Koviack, PD; Metz, DC, 1993
)
0.29
"7%) were the most commonly reported adverse events."( Safety of lansoprazole.
Colin-Jones, DG, 1993
)
0.29
"The LCM1 regimen consisting of 30 mg lansoprazole once daily, 200 mg clarithromycin twice daily, and 250 mg metronidazole twice daily (the regular doses in ordinary use in Japan) is a highly effective and safe regimen for Japanese patients."( The efficacy and safety of one-week triple therapy with lansoprazole, clarithromycin, and metronidazole for the treatment of Helicobacter pylori infection in Japanese patients.
Ido, K; Kihira, K; Kimura, K; Saifuku, K; Satoh, K; Seki, M; Takimoto, T; Taniguchi, Y; Yoshida, Y, 1997
)
0.3
" Fifty-four (24%) patients experienced adverse events; 15 of these withdrew."( One-year prophylactic efficacy and safety of pantoprazole in controlling gastro-oesophageal reflux symptoms in patients with healed reflux oesophagitis.
Koop, H; Maier, C; Mössner, J; Porst, H; Schneider, A; Wübbolding, H, 1997
)
0.3
" There were no clinically significant effects on patient laboratory tests or serious adverse events."( An ascending single-dose safety and tolerance study of an oral formulation of rabeprazole (E3810).
Barbuti, RC; Humphries, TJ; Kovacs, TO; Lew, EA; Sytnic, B; Walsh, JH, 1998
)
0.3
" The most common side effects were loose stools, headache, and taste disturbance, but there were no serious adverse events related to the study medication."( Safety and efficacy of rabeprazole in combination with four antibiotic regimens for the eradication of Helicobacter pylori in patients with chronic gastritis with or without peptic ulceration.
Atherton, JC; Cockayne, A; Hawkey, CJ; Jenkins, D; Knifton, A; Stack, WA; Thirlwell, D, 1998
)
0.3
" Neither adverse events nor carcinoid tumors were observed."( [Effectiveness and safety of lansoprazole in the treatment of Zollinger-Ellison syndrome. First six months of treatment].
Cadiot, G; Coste, T; Escourrou, J; Forestier, S; Mignon, M; Pospaï, D; Ruszniewski, P, 1998
)
0.3
" Adverse events, laboratory value changes and gastric biopsy changes that occurred during treatment were compared statistically for differences between treatments."( Safety profile of Lansoprazole: the US clinical trial experience.
Freston, JW; Haber, M; Heller, CA; Jennings, D; Rose, PA, 1999
)
0.3
"The incidence of adverse events and number of patients discontinuing treatment because of adverse events was similar for lansoprazole and comparative agents."( Safety profile of Lansoprazole: the US clinical trial experience.
Freston, JW; Haber, M; Heller, CA; Jennings, D; Rose, PA, 1999
)
0.3
"Argon plasma coagulation in an acid-controlled environment was both efficacious and safe in the treatment of Barrett's esophagus."( The efficacy and safety of argon plasma coagulation therapy in Barrett's esophagus.
Grade, AJ; Medlin, SM; Ramirez, FC; Shah, IA, 1999
)
0.3
" For patients, temporarily unable to take oral medications, this regimen offers safe and reliable gastric acid suppression and allows the possibility of changing between the oral and intravenous administration without the need for dose adjustment."( Efficacy and safety of pantoprazole in patients with gastroesophageal reflux disease using an intravenous-oral regimen. Austrian Intravenous Pantoprazole Study Group.
Bethke, T; Fischer, R; Luhmann, R; Riesenhuber, C; Schutze, K; Wurzer, H,
)
0.13
"Of the 178 adverse events, experienced by 88 (56%) patients (intention-to-treat population), 12 (7%) were assessed by the investigators as possibly related to the study medication."( Safety and efficacy of pantoprazole 40 mg daily as relapse prophylaxis in patients with healed reflux oesophagitis-a 2-year follow-up.
Eloff, FP; Fischer, R; Grundling, HD; Honiball, PJ; Louw, JA; Simjee, AE; Spies, SK; Theron, I; Van Rensburg, CJ; Van Zyl, JH, 1999
)
0.3
"Pantoprazole 40 mg proved to be safe and efficacious during a 2-year prophylaxis treatment in patients with healed reflux oesophagitis."( Safety and efficacy of pantoprazole 40 mg daily as relapse prophylaxis in patients with healed reflux oesophagitis-a 2-year follow-up.
Eloff, FP; Fischer, R; Grundling, HD; Honiball, PJ; Louw, JA; Simjee, AE; Spies, SK; Theron, I; Van Rensburg, CJ; Van Zyl, JH, 1999
)
0.3
"The adverse effect profile of proton-pump inhibitors is presented."( Safety profile of the proton-pump inhibitors.
Reilly, JP, 1999
)
0.3
" In conclusion, omeprazole paste is safe for use in horses as demonstrated in studies with foals and mature horses."( Safety of omeprazole paste in foals and mature horses.
Attebery, DK; Cox, JL; Daurio, C; Plue, RE; Wall, HG; Wallace, DH, 1999
)
1.05
" A paste formulation of omeprazole, administered at a dose of 4 mg/kg bwt once daily for 28 days, was determined to be highly acceptable to the foals and yearlings we studied, and no adverse effects attributable to the medication were noted."( Safety, acceptability and endoscopic findings in foals and yearling horses treated with a paste formulation of omeprazole for twenty-eight days.
Cooper, VA; Cooper, WL; Cox, JL; Eichorn, ES; Holste, JE; Murray, MJ; Stanier, WB, 1999
)
0.82
" Safety evaluations, which included adverse events, vital signs, clinical laboratory determinations, ECG, and physical examinations, revealed no unexpected clinically significant findings and did not suggest a drug-drug interaction."( Lack of interaction between lansoprazole and propranolol, a pharmacokinetic and safety assessment.
Cavanaugh, JH; Karol, MD; Locke, CS, 2000
)
0.31
" The adverse event profile was as might be expected from this elderly group of patients."( Long-term omeprazole treatment in resistant gastroesophageal reflux disease: efficacy, safety, and influence on gastric mucosa.
Dent, J; Frame, MH; Havu, N; Klinkenberg-Knol, EC; Lloyd, D; Mitchell, B; Nelis, F; Prichard, P; Romàn, J; Snel, P; Walan, A, 2000
)
0.71
"Long-term omeprazole therapy (up to 11 years) is highly effective and safe for control of reflux esophagitis."( Long-term omeprazole treatment in resistant gastroesophageal reflux disease: efficacy, safety, and influence on gastric mucosa.
Dent, J; Frame, MH; Havu, N; Klinkenberg-Knol, EC; Lloyd, D; Mitchell, B; Nelis, F; Prichard, P; Romàn, J; Snel, P; Walan, A, 2000
)
1.11
"We compared the gastric toxic effect of aspirin (ASA) in both normal and diabetic rats, with that of NCX-4016, a derivative of ASA with nitric oxide (NO) releasing moiety."( Lack of gastric toxicity of nitric oxide-releasing aspirin, NCX-4016, in the stomach of diabetic rats.
Fujita, A; Takeuchi, K; Tashima, K; Umeda, M, 2000
)
0.31
"To estimate the rates of common adverse events in patients treated with the proton pump inhibitors omeprazole, lansoprazole and pantoprazole in general practice in England."( The rates of common adverse events reported during treatment with proton pump inhibitors used in general practice in England: cohort studies.
Dunn, NR; Freemantle, S; Martin, RM; Shakir, S, 2000
)
0.52
"Omeprazole is well tolerated, highly effective, and safe for treatment of erosive esophagitis and symptoms of gastroesophageal reflux in children, including children in whom antireflux surgery or other medical therapy has failed."( Omeprazole for treatment of chronic erosive esophagitis in children: a multicenter study of efficacy, safety, tolerability and dose requirements. International Pediatric Omeprazole Study Group.
Dalväg, A; Hassall, E; Israel, D; Junghard, O; Lundborg, P; Radke, M; Shepherd, R; Sköld, B, 2000
)
3.19
" Gastrointestinal symptoms, documentation of adverse events, and standard laboratory examinations were assessed at each visit."( Comparison of the efficacy and safety of different formulations of omeprazole-based triple therapies in the treatment of Helicobacter pylori-positive peptic ulcer.
Baik, SK; Cho, MY; Jeong, YS; Kim, HS; Kim, JW; Kim, KH; Kwon, SO; Lee, DK; Seo, JI, 2001
)
0.55
" The most common adverse events in both treatment groups were headache, diarrhea, and nausea."( Efficacy and safety of esomeprazole compared with omeprazole in GERD patients with erosive esophagitis: a randomized controlled trial.
Breiter, JR; Hamelin, B; Hwang, C; Johanson, J; Kahrilas, PJ; Levine, JG; Marino, V; Maton, P; Richter, JE, 2001
)
0.61
" We performed serial endoscopy, checked for adverse events, and laboratory values."( Pantoprazole therapy in the long-term management of severe acid peptic disease: clinical efficacy, safety, serum gastrin, gastric histology, and endocrine cell studies.
Bardhan, KD; Bishop, AE; Cherian, P; Fischer, R; Lühmann, R; McCaldin, B; Morris, P; Ng, W; Perry, MJ; Polak, JM; Romanska, H; Rowland, A; Schneider, A; Thompson, M, 2001
)
0.31
" Treatment was safe; only four patients had adverse events definitely related to pantoprazole."( Pantoprazole therapy in the long-term management of severe acid peptic disease: clinical efficacy, safety, serum gastrin, gastric histology, and endocrine cell studies.
Bardhan, KD; Bishop, AE; Cherian, P; Fischer, R; Lühmann, R; McCaldin, B; Morris, P; Ng, W; Perry, MJ; Polak, JM; Romanska, H; Rowland, A; Schneider, A; Thompson, M, 2001
)
0.31
" We conclude that the use of intravenous P allows a safe and efficient control of the acid ipersecretion in patients with ZES."( [Efficacy and safety of intravenously administered pantoprazole in the treatment of gastrinoma].
Modlin, IM,
)
0.13
" No drug related severe adverse event was reported."( [Complementary observational study of the efficacy, tolerance and safety of lansoprazole 15 mg as maintenance therapy of reflux esophagitis in daily medical practice in Belgium (record RU49749/R002].
Azerad, MA; Fassotte, C; Penson, J; Puttemans, M, 2001
)
0.31
" The adverse effects were minimal and transitory."( [Evaluation of efficacy, safety and tolerability rabeprazole in treatment of acid-peptic diseases ].
Chinzon, D; de Freitas, JA; Fragoso, HJ; Lima, LM; Olivieri, JC; Ranieri, JL,
)
0.13
" Pre- and post-treatment peripheral blood lymphocyte cultures were prepared from 17 patients and 25 metaphases per patients were analysed for sister chromatid exchange (SCE), a well-established technique for the evaluation of human exposure to toxic agents."( The role of triple therapy, age, gender and smoking on the genotoxic effects of Helicobacter pylori infection.
Demiray, M; Ercan, I; Evke, E; Gulten, M; Gulten, T; Karakaya, AE; Sardas, S; Tokyay, N,
)
0.13
" Pantoprazole was safe and well tolerated."( Efficacy and safety of oral pantoprazole 20 mg given once daily for reflux esophagitis in children.
Delgado, J; Dibildox, M; Gonzalez, J; Madrazo-de la Garza, A; Vargas, A; Yañez, P, 2003
)
0.32
" All three were safe and well tolerated during 5 years of treatment."( A randomized, double-blind trial of the efficacy and safety of 10 or 20 mg rabeprazole compared with 20 mg omeprazole in the maintenance of gastro-oesophageal reflux disease over 5 years.
Bardhan, KD; Fiocca, R; Humphries, TJ; Miller, N; Morocutti, A; Rindi, G; Thjodleifsson, B, 2003
)
0.53
" Safety for all study participants was monitored by adverse event reports and laboratory evaluations."( Safety of lansoprazole in the treatment of gastroesophageal reflux disease in children.
Fitzgerald, J; Hassall, E; Huang, B; Kane, R; Pilmer, B; Tolia, V, 2002
)
0.31
" Throughout the treatment period, no child discontinued therapy because of an adverse event and no clinically significant changes in laboratory values were observed."( Safety of lansoprazole in the treatment of gastroesophageal reflux disease in children.
Fitzgerald, J; Hassall, E; Huang, B; Kane, R; Pilmer, B; Tolia, V, 2002
)
0.31
"Lansoprazole, when administered on the basis of body weight in children between 1 and 11 years of age, is safe and well-tolerated."( Safety of lansoprazole in the treatment of gastroesophageal reflux disease in children.
Fitzgerald, J; Hassall, E; Huang, B; Kane, R; Pilmer, B; Tolia, V, 2002
)
0.31
"To estimate the frequency of adverse events and drug interactions reported to the Food and Drug Administration in patients receiving omeprazole, lansoprazole or pantoprazole."( A summary of Food and Drug Administration-reported adverse events and drug interactions occurring during therapy with omeprazole, lansoprazole and pantoprazole.
Koelz, HR; Labenz, J; Petersen, KU; Rösch, W, 2003
)
0.73
"The study involved a search of the Food and Drug Administration's database for adverse events and drug interactions with omeprazole, lansoprazole or pantoprazole as primary or secondary suspect drug."( A summary of Food and Drug Administration-reported adverse events and drug interactions occurring during therapy with omeprazole, lansoprazole and pantoprazole.
Koelz, HR; Labenz, J; Petersen, KU; Rösch, W, 2003
)
0.74
"Outpatient management is safe for patients with non-variceal upper-GI bleeding who are at low risk of recurrent bleeding and death."( A randomized study of the safety of outpatient care for patients with bleeding peptic ulcer treated by endoscopic injection.
Brullet, E; Cabrol, J; Calvet, X; Campo, R; Garcia-Monforte, N; Guell, M, 2004
)
0.32
" Safety evaluations included adverse events and laboratory assessments."( Efficacy and safety of pantoprazole versus ranitidine in the treatment of patients with symptomatic gastroesophageal reflux disease.
Fischer, R; van Rensburg, C; van Zyl, J; Vieweg, W, 2004
)
0.32
"3%) and there were no serious adverse events."( The efficacy, safety and tolerability of pantoprazole-based one-week triple therapy in H. pylori eradication and duodenal ulcer healing.
Akarsu, M; Bozbas, A; Hulagu, S; Kadayifci, A; Koruk, M; Savas, MC; Simsek, I; Sivri, B; Tozun, N; Uraz, S, 2004
)
0.32
" Only four patients had adverse events considered to be definitely related to pantoprazole."( Pantoprazole in severe acid-peptic disease: the effectiveness and safety of 5 years' continuous treatment.
Bardhan, KD; Bishop, AE; Luehmann, R; McCaldin, B; Morris, P; Polak, JM; Romanska, HM; Rowland, A; Schaefer-Preuss, S; Thompson, M, 2005
)
0.33
" Treatment-related adverse events were reported by 19% of patients with non-erosive and 4% of patients with erosive esophagitis."( Efficacy and safety of lansoprazole in adolescents with symptomatic erosive and non-erosive gastroesophageal reflux disease.
Fiedorek, S; Gold, BD; Gremse, D; Huang, B; Lee, C; Stolle, J; Tolia, V, 2005
)
0.33
"A total of 119 Japanese patients with recurrent reflux oesophagitis underwent cytochrome P450 2C19 genotyping prior to receiving daily omeprazole 10 mg or 20 mg for 6-12 months, during which adverse event frequency, serum gastrin levels and endoscopic findings were monitored."( Effect of CYP2C19 polymorphism on the safety and efficacy of omeprazole in Japanese patients with recurrent reflux oesophagitis.
Aoyama, N; Arakawa, T; Chida, N; Fujimoto, K; Hamada, S; Hoshino, E; Inoue, M; Kawahara, Y; Konda, Y; Maekawa, T; Mine, T; Mitachi, Y; Nagai, T; Nakajima, M; Ohkusa, T; Sato, N; Seno, H; Shimatani, T; Tadokoro, K; Yoshida, N, 2005
)
0.77
"The incidences of adverse events, serious adverse events and adverse events leading to withdrawal did not differ between homozygous extensive metabolizer (n = 46), heterozygous extensive metabolizer (n = 53) or poor metabolizer (n = 20) groups."( Effect of CYP2C19 polymorphism on the safety and efficacy of omeprazole in Japanese patients with recurrent reflux oesophagitis.
Aoyama, N; Arakawa, T; Chida, N; Fujimoto, K; Hamada, S; Hoshino, E; Inoue, M; Kawahara, Y; Konda, Y; Maekawa, T; Mine, T; Mitachi, Y; Nagai, T; Nakajima, M; Ohkusa, T; Sato, N; Seno, H; Shimatani, T; Tadokoro, K; Yoshida, N, 2005
)
0.57
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" No significant adverse effects were reported."( Efficacy and safety of rabeprazole, amoxicillin, and gatifloxacin after treatment failure of initial Helicobacter pylori eradication.
Abdul-Baki, H; Aoun, E; Araj, GF; Chaar, HF; Kanj, SS; Sharara, AI, 2006
)
0.33
" In the present article, the adverse effects of PPIs are reviewed, with special emphasis on those related to their continued administration and on the special circumstances of patients, as in the case of the elderly, those with liver failure, pregnant and breastfeeding mothers and children."( [Safety of proton pump inhibitors].
Esplugues, JV; Martí-Cabrera, M; Ponce, J, 2006
)
0.33
" Protonic pump inhibitors (PPI) are considered to be the correct therapy in the treatment of peptic ulcers, as they have proven to be safe and efficient."( [Protonic pump inhibitors in kidney transplant patients: efficacy and safety].
Cianciolo, G; Comai, G; Feliciangeli, G; Stefoni, S, 2007
)
0.34
" A retrospective review of children receiving PPI therapy continuously for 1 year or more with baseline and follow-up esophageal and gastric biopsies on treatment was conducted to assess type, frequency, and duration of PPI dosing, symptom relief, gastrin levels, histologic findings, and adverse events."( Long-term proton pump inhibitor use in children: a retrospective review of safety.
Boyer, K; Tolia, V, 2008
)
0.35
" However, the adverse event database of newly marketed drugs is limited, and it is only after widespread clinical use that the adverse effect profile of a drug is ascertained more comprehensively."( Safety profile of esomeprazole: results of a prescription-event monitoring study of 11 595 patients in England.
Davies, M; Shakir, SA; Wilton, LV, 2008
)
0.67
" Adverse events that occurred significantly more often in the first month of treatment with esomeprazole compared with months 2-6 included diarrhoea, nausea/vomiting, abdominal pain, dyspepsia, headache/migraine, intolerance, malaise/lassitude, pruritus, unspecified adverse effects and abnormal sensation."( Safety profile of esomeprazole: results of a prescription-event monitoring study of 11 595 patients in England.
Davies, M; Shakir, SA; Wilton, LV, 2008
)
0.89
"The AstraZeneca ARIADNE safety database was searched for comparative, controlled phase II-IV randomized, blinded clinical studies with esomeprazole and standard reporting of all adverse events (AEs)."( Occurrence of community-acquired respiratory tract infection in patients receiving esomeprazole: retrospective analysis of adverse events in 31 clinical trials.
Estborn, L; Joelson, S, 2008
)
0.77
" CYP1A1-inducible chemicals, such as benzo[a]pyrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin, are known to have adverse effects (i."( Omeprazole alleviates benzo[a]pyrene cytotoxicity by inhibition of CYP1A1 activity in human and mouse hepatoma cells.
Kawanishi, M; Ohsako, S; Shiizaki, K; Yagi, T, 2008
)
1.79
"To explore whether proton pump inhibitors (PPIs) possess anti-inflammatory effects on microglia, we investigated the effect of lansoprazole (LPZ) and omeprazole (OPZ) on the toxic action towards SH-SY5Y neuroblastoma cells of supernatants from human microglia and THP-1 cells stimulated by lipopolysaccharide combined with interferon-gamma."( Proton pump inhibitors exert anti-inflammatory effects and decrease human microglial and monocytic THP-1 cell neurotoxicity.
Hashioka, S; Klegeris, A; McGeer, PL, 2009
)
0.55
" The secondary outcome measure was the proportion of patients who experienced therapy-related adverse effects during anti-H pylori treatment."( Randomized, double-blind, placebo-controlled trial: effect of lactobacillus GG supplementation on Helicobacter pylori eradication rates and side effects during treatment in children.
Albrecht, P; Szajewska, H; Topczewska-Cabanek, A, 2009
)
0.35
" The groups did not differ with respect to adverse effects."( Randomized, double-blind, placebo-controlled trial: effect of lactobacillus GG supplementation on Helicobacter pylori eradication rates and side effects during treatment in children.
Albrecht, P; Szajewska, H; Topczewska-Cabanek, A, 2009
)
0.35
" No major adverse events occurred in both groups."( A randomized controlled trial: efficacy and safety of azithromycin, ofloxacin, bismuth, and omeprazole compared with amoxicillin, clarithromycin, bismuth, and omeprazole as second-line therapy in patients with Helicobacter pylori infection.
Davarpanah Jazi, AH; Fatahi, F; Minakari, M; Moghareabed, N; Shavakhi, A, 2010
)
0.58
" Secondary end-points were the rate of control of chronic cough at each step of therapy, the duration of treatment required, changes in cough symptom score, health-related quality of life and possible adverse effects."( Efficacy and safety of modified sequential three-step empirical therapy for chronic cough.
Li, X; Liang, S; Liu, B; Lü, H; Qiu, Z; Wang, L; Wang, Y; Wei, W; Yu, L, 2010
)
0.36
" Omeprazole acts by selectively oxidizing thiol targets in the gastric proton pump, but it also appears to be toxic to the gastric mucosa."( Antioxidant pre-treatment prevents omeprazole-induced toxicity in an in vitro model of infectious gastritis.
Blass, AL; Kohler, JE; Liu, J; Soybel, DI; Tai, K, 2010
)
1.55
" There was no difference among the treatment groups with regard to the incidence and severity of adverse events reported."( Efficacy and safety of Levofloxacin, Clarithromycin and Esomeprazol as first line triple therapy for Helicobacter pylori eradication in Middle East. Prospective, randomized, blind, comparative, multicenter study.
Abdelfatah, M; Assem, M; El Azab, G; Rasheed, MA; Shastery, M, 2010
)
0.36
" Rates of congenital malformations in PPIs exposed and unexposed pregnancies, as well as other adverse fetal effects were compared."( The safety of fetal exposure to proton-pump inhibitors during pregnancy.
Gorodischer, R; Koren, G; Levy, A; Matok, I; Uziel, E; Wiznitzer, A, 2012
)
0.38
" However, a randomized controlled trial that compared clopidogrel alone with the combination of clopidogrel and omeprazole found no increase in adverse cardiovascular outcomes and a reduction in the rate of adverse gastrointestinal outcomes attributable to omeprazole."( Recent safety concerns with proton pump inhibitors.
Chen, J; Howden, CW; Leontiadis, GI; Yuan, YC, 2012
)
0.59
"The physicochemical properties of racemates and stereoisomers of medicines can differ significantly, and this may affect the side-effect profile in addition to the pharmacokinetics and intended pharmacology."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
"This is a study to investigate the profile of adverse drug reactions of racemic and enantiomeric forms of drugs."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" A case-noncase approach was used to measure the disproportionality of combination between adverse drug reaction (ADR) and exposure to drug."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" Although use of the Naranjo adverse reaction probability scale indicated a probable relationship (score of 6) between the patient's development of methotrexate toxicity and omeprazole use, we believe this was a drug-drug interaction case consistent with previous reports in the literature."( Suspected methotrexate toxicity from omeprazole: a case review of carboxypeptidase G2 use in a methotrexate-experienced patient with methotrexate toxicity and a review of the literature.
Antonia, SJ; Goetz, D; Haura, EB; McBride, A, 2012
)
0.85
" In this study, the reports submitted to the Adverse Event Reporting System (AERS) of the US Food and Drug Administration (FDA) were evaluated to assess omeprazole and esomeprazole in terms of susceptibility to hypomagnesaemia."( Omeprazole- and esomeprazole-associated hypomagnesaemia: data mining of the public version of the FDA Adverse Event Reporting System.
Kadoyama, K; Okuno, Y; Sakaeda, T; Tamura, T, 2012
)
2.02
", an association between a drug and an adverse drug event, including the proportional reporting ratio, the reporting odds ratio, the information component given by a Bayesian confidence propagation neural network, and the empirical Bayes geometric mean."( Omeprazole- and esomeprazole-associated hypomagnesaemia: data mining of the public version of the FDA Adverse Event Reporting System.
Kadoyama, K; Okuno, Y; Sakaeda, T; Tamura, T, 2012
)
1.82
"A total of 22,017,956 co-occurrences were found in 1,644,220 reports from 2004 to 2009, where a co-occurrence was a pair of a drug and an adverse drug event."( Omeprazole- and esomeprazole-associated hypomagnesaemia: data mining of the public version of the FDA Adverse Event Reporting System.
Kadoyama, K; Okuno, Y; Sakaeda, T; Tamura, T, 2012
)
1.82
" Incidence of moderate-to-severe abdominal symptoms and discontinuation of treatment due to GI adverse events (AEs) were lower in the celecoxib group."( Efficacy and safety of celecoxib versus diclofenac and omeprazole in elderly arthritis patients: a subgroup analysis of the CONDOR trial.
Essex, MN; Kellner, HL; Li, C, 2012
)
0.63
" Adverse events were rare (2."( [Efficacy and safety of OTC omeprazole].
Labenz, J; Willmer, C, 2012
)
0.67
" No serious adverse events were observed in any of the patients in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" Serious adverse events were not observed in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" We used recombinant technology and enzyme inactivation to demonstrate the capacity of omeprazole to inactivate giardial triosephosphate isomerase, with no adverse effects on its human counterpart."( Giardial triosephosphate isomerase as possible target of the cytotoxic effect of omeprazole in Giardia lamblia.
Castillo-Villanueva, A; de la Mora-de la Mora, I; Enríquez-Flores, S; Figueroa-Salazar, R; García-Torres, I; Gómez-Manzo, S; Gutiérrez-Castrellón, P; Hernández-Alcántara, G; López-Velázquez, G; Marcial-Quino, J; Méndez, ST; Oria-Hernández, J; Reyes-Vivas, H; Torres-Arroyo, A; Vanoye-Carlo, A; Yépez-Mulia, L, 2014
)
0.85
"To establish the efficiency and adverse effects of the addition of bismuth subsalicylate to triple eradication therapy for Helicobacter pylori infection."( [Addition of bismuth subsalicylate to triple eradication therapy for Helicobacter pylori infection: efficiency and adverse events].
Díaz Ferrer, J; Hinostroza Morales, D,
)
0.13
" The adverse events of both groups were: diarrhea (10."( [Addition of bismuth subsalicylate to triple eradication therapy for Helicobacter pylori infection: efficiency and adverse events].
Díaz Ferrer, J; Hinostroza Morales, D,
)
0.13
" Reported serious adverse events (SAEs) and changes in laboratory variables were analysed."( Long-term safety of proton pump inhibitor therapy assessed under controlled, randomised clinical trial conditions: data from the SOPRAN and LOTUS studies.
Attwood, SE; Eklund, S; Ell, C; Fiocca, R; Galmiche, JP; Hasselgren, B; Hatlebakk, JG; Jahreskog, M; Långström, G; Lind, T; Lundell, L, 2015
)
0.42
" Adverse events (AEs) caused study withdrawal in 13."( Long-Term Safety of a Coordinated Delivery Tablet of Enteric-Coated Aspirin 325 mg and Immediate-Release Omeprazole 40 mg for Secondary Cardiovascular Disease Prevention in Patients at GI Risk.
Cryer, BL; Eisen, GM; Fort, JG; Goldstein, JL; Lanas, A; Scheiman, JM; Whellan, DJ, 2016
)
0.65
"Proton-pump inhibitors (PPIs) have been proved as safe and effective ways to treat patients with non-erosive reflux disease (NERD)."( The efficacy and safety of proton-pump inhibitors in treating patients with non-erosive reflux disease: a network meta-analysis.
Chen, L; Chen, Y; Li, B, 2016
)
0.43
" About 76% of the patients experienced adverse events (35% diarrhea, 14% nausea and 24% metallic taste), none of which was serious."( Efficacy and safety of rifaximin associated with standard triple therapy (omeprazole, clarithromycin and amoxicillin) for H. pylori eradication: A phase IV pilot clinical trial.
Donday, MG; Gisbert, JP; McNicholl, AG; Ramas, M, 2017
)
0.69
" For the duration of 4 months, weight, body mass index, and the occurrence of adverse events was documented."( The safety and efficacy of the procedureless intragastric balloon.
Al Haddad, E; Al Kendari, M; Al-Subaie, S; Almulla, A; Alsabah, S; Ekrouf, S, 2018
)
0.48
" Roxadustat was considered safe and well tolerated when administered alone or in combination with multiple daily oral doses of 40 mg omeprazole in healthy subjects."( Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects.
Barroso-Fernandez, B; den Adel, M; El Galta, R; Golor, G; Groenendaal-van de Meent, D; Schaddelee, M; van Dijk, J, 2018
)
0.98
" Adverse events were recorded by patients in specially developed diaries."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
" The incidence of adverse events between the groups was comparable: 22."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
" Adverse events were recorded by patients in specially developed diaries."( Evaluation of the efficacy and safety of the hybrid scheme for eradication therapy of Helicobacter pylori infection.
Andreev, DN; Dicheva, DT; Maiev, IV; Partzvania-Vinogradova, EV; Yurenev, GL, 2018
)
0.48
" The incidence of adverse events with the use of triple, four-component and hybrid ET regimens was 15; 18."( Evaluation of the efficacy and safety of the hybrid scheme for eradication therapy of Helicobacter pylori infection.
Andreev, DN; Dicheva, DT; Maiev, IV; Partzvania-Vinogradova, EV; Yurenev, GL, 2018
)
0.48
"Risks regarding hospital admission due to adverse drug reactions and drug interactions from use of omeprazole have been reported."( Safety assessment of omeprazole use: a review.
Forgerini, M; Mastroianni, PC; Mieli, S,
)
0.67
" Studies evaluating adverse events were screened."( Safety assessment of omeprazole use: a review.
Forgerini, M; Mastroianni, PC; Mieli, S,
)
0.45
"72 articles were included, among which 58 reported on adverse drug events (47, adverse drug reactions; 5, drug interactions; and 6, situations of ineffectiveness)."( Safety assessment of omeprazole use: a review.
Forgerini, M; Mastroianni, PC; Mieli, S,
)
0.45
"Use of omeprazole should be monitored primarily in patients with heart disorders using antiplatelet agents concomitantly, and in newly transplanted patients using mycophenolic acid, in order to avoid serious adverse reactions."( Safety assessment of omeprazole use: a review.
Forgerini, M; Mastroianni, PC; Mieli, S,
)
0.91
" However, whether omeprazole is toxic to renal cells is unknown."( Molecular pathways driving omeprazole nephrotoxicity.
Cardenas-Villacres, D; Carrasco, S; Fontecha-Barriuso, M; Martín-Sanchez, D; Martinez-Moreno, JM; Ortiz, A; Ruiz-Ortega, M; Sanchez-Niño, MD; Sanz, AB, 2020
)
1.19
" In terms of individual toxicity, omeprazole is the most toxic of the active ingredients, followed by simvastatin, diazepam and, finally, metformin."( Diazepam, metformin, omeprazole and simvastatin: a full discussion of individual and mixture acute toxicity.
d'Auriol, M; de Souza Santos, LV; Jacob, RS; Lange, LC; Lebron, YAR; Moreira, VR, 2020
)
1.16
" No serious adverse events/deaths were reported."( Napabucasin Drug-Drug Interaction Potential, Safety, Tolerability, and Pharmacokinetics Following Oral Dosing in Healthy Adult Volunteers.
Brantley, SJ; Dai, X; Goulet, MT; Hard, ML; Hitron, M; Karol, MD; McLaughlin, CF, 2021
)
0.62
"To assess the impact of prophylactic omeprazole and famotidine on the incidence and severity of gastrointestinal (GI) adverse events (AEs) in dogs with cancer treated with single agent piroxicam."( A prospective, randomized, placebo-controlled, double-blinded clinical trial comparing the incidence and severity of gastrointestinal adverse events in dogs with cancer treated with piroxicam alone or in combination with omeprazole or famotidine.
Fulkerson, CM; Moore, GE; Shaevitz, MH, 2021
)
1.08
" The treatment efficiency and the incidence of adverse reactions were used as the main outcome indicators."( The clinical efficacy and safety of atropine combined with omeprazole in the treatment of patients with acute gastritis: a systematic review and meta-analysis.
Chen, H; Lin, X; Lin, YN, 2021
)
0.86
"The combination of atropine with omeprazole in the treatment of acute gastritis demonstrated a high effective rate with few adverse reactions than."( The clinical efficacy and safety of atropine combined with omeprazole in the treatment of patients with acute gastritis: a systematic review and meta-analysis.
Chen, H; Lin, X; Lin, YN, 2021
)
1.15
" The inclusion of Bifiform in the eradication scheme dramatically reduces the frequency of adverse events and increases patient compliance, and also maintains the protective factors of the gastrointestinal mucosa at a higher level."( [A prospective randomized comparative study of the efficacy and safety of a two-week bismuth-based quadrotherapy of
Iakovenko, AV; Ivanov, AN; Soluyanova, IP; Strokova, TV; Vasilyev, NN; Yakovenko, EP, 2021
)
0.62
" Adverse events were monitored for safety."( Effect and safety of anaprazole in the treatment of duodenal ulcers: a randomized, rabeprazole-controlled, phase III non-inferiority study.
Ding, J; Du, Y; Fan, H; Huang, C; Li, Z; Lyu, N; Pan, X; Pan, Z; Shi, Z; Sun, H; Wang, Q; Zhang, L; Zhu, H, 2022
)
0.72
" The incidence of treatment-emergent adverse events was similar for anaprazole (72/220, 32."( Effect and safety of anaprazole in the treatment of duodenal ulcers: a randomized, rabeprazole-controlled, phase III non-inferiority study.
Ding, J; Du, Y; Fan, H; Huang, C; Li, Z; Lyu, N; Pan, X; Pan, Z; Shi, Z; Sun, H; Wang, Q; Zhang, L; Zhu, H, 2022
)
0.72
" Secondary outcomes included adverse events, dropout rate, and subgroup analysis."( Efficacy and Safety of Vonoprazan and Amoxicillin Dual Therapy for Helicobacter pylori Eradication: A Systematic Review and Meta-Analysis.
Ding, YM; Han, ZX; Ji, R; Li, YY; Lin, BS; Zhang, WL, 2023
)
0.91
" The adverse effects of vonoprazan/amoxicillin dual therapy were lower than those of triple therapy (21."( Efficacy and Safety of Vonoprazan and Amoxicillin Dual Therapy for Helicobacter pylori Eradication: A Systematic Review and Meta-Analysis.
Ding, YM; Han, ZX; Ji, R; Li, YY; Lin, BS; Zhang, WL, 2023
)
0.91
" Therefore, the competition for CYP3A4 may affect the metabolism of tacrolimus and result in its increased plasma concentrations, as well as in adverse reactions."( Safety analysis of co-administering tacrolimus and omeprazole in renal transplant recipients - A review.
Idasiak-Piechocka, I; Miedziaszczyk, M, 2023
)
1.16

Pharmacokinetics

AUC0-24 and Cmax of active clopidogrel metabolite decreased with both omeprazole and rabeprazoles. The mean elimination half-life of omepazole in the patients with cirrhosis was 2.

ExcerptReferenceRelevance
" The single dose of omeprazole had no significant effect on any pharmacokinetic parameter of nifedipine, nor on gastric pH, or blood pressure or heart rate."( Influence of single- and multiple-dose omeprazole treatment on nifedipine pharmacokinetics and effects in healthy subjects.
Breimer, DD; Danhof, M; Jansen, JB; Lamers, CB; Soons, PA; van Brummelen, P; van den Berg, G, 1992
)
0.88
" The range of clinically acceptable variation in the pharmacokinetic characteristics of drug A defines the equivalence range."( Lack of pharmacokinetic interaction as an equivalence problem.
Hartmann, M; Huber, R; Radtke, HW; Steinijans, VW, 1991
)
0.28
" The principal pharmacokinetic parameters were estimated for the two studied populations."( Pharmacokinetics of omeprazole in cirrhotic patients.
Regazzi, MB; Rinetti, M; Sivelli, R; Tizzoni, M; Villani, P, 1991
)
0.6
" On average, Cmax and AUC values for digoxin were approximately 10% higher and tmax tended to be shorter during the administration of omeprazole, while the elimination rate constant was unaffected."( Minor effect of multiple dose omeprazole on the pharmacokinetics of digoxin after a single oral dose.
Andersson, T; Jedema, JN; Jonkman, JH; Oosterhuis, B; Zuiderwijk, PB, 1991
)
0.77
" A good dose linearity was observed for AUC (0, infinity) and Cmax over the dose range from 5 to 80 mg."( Single intravenous administration of the H+, K(+)-ATPase inhibitor BY 1023/SK&F 96022--inhibition of pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man.
Bliesath, H; Hartmann, M; Huber, R; Lühmann, R; Müller, P; Simon, B; Wurst, W, 1990
)
0.28
" AUC, Cmax and t1/2 of the drug after repeated oral intake were not significantly different when compared with a single dose at either 20 mg or 40 mg."( Effect of repeated oral administration of BY 1023/SK&F 96022--a new substituted benzimidazole derivative--on pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man.
Hartmann, R; Huber, R; Lühmann, R; Marinis, E; Müller, P; Simon, B; Wurst, W, 1990
)
0.28
" Repeated once-daily infusion (15 min) of pantoprazole resulted in a rapidly increasing pharmacodynamic effect: as compared to placebo the mean percent inhibition of acid output measured from 1 to 3 h after start of infusion was 22%, 63% and 78% for the 15 mg dose, and 56%, 97% and 99% for the 30 mg dose on days 1, 4 and 5, respectively."( Pentagastrin-stimulated gastric acid secretion and pharmacokinetics following single and repeated intravenous administration of the gastric H+, K(+)-ATPase-inhibitor pantoprazole (BY1023/SK&F96022) in healthy volunteers.
Bliesath, H; Bohnenkamp, W; Hartmann, M; Huber, R; Lühmann, R; Müller, P; Simon, B; Wurst, W, 1990
)
0.28
" The half-life is less than 1 hour, and omeprazole is almost entirely cleared from plasma within 3-4 hours."( Omeprazole: pharmacokinetics and metabolism in man.
Andersson, T; Cederberg, C; Skånberg, I, 1989
)
1.99
" The pharmacokinetic profile of omeprazole is rather complicated, showing concentration-dependent elimination kinetics and an oral bioavailability which increases with the dose and during repeated administration."( Omeprazole: pharmacology, pharmacokinetics and interactions.
Jonkman, JH; Oosterhuis, B, 1989
)
2
" Following 10 mg intravenous omeprazole, plasma clearance was reduced, and plasma half-life and area under the concentration curve were increased, in comparison with previous studies in healthy subjects."( The anti-secretory effect and pharmacokinetics of omeprazole in chronic liver disease.
Carter, DC; Forrest, JA; Garden, OJ; MacGilchrist, AJ; McKee, RF, 1988
)
0.82
" Increasing the intravenous dose of omeprazole from 10 mg to 40 mg had no significant effect on the pharmacokinetic parameters determined."( Pharmacokinetics and metabolism of omeprazole in man.
Regårdh, CG, 1986
)
0.82
" The peak concentration, and apparent elimination half-life of phenytoin also tended to be increased though not significantly."( Oral phenytoin pharmacokinetics during omeprazole therapy.
Kitchingman, GK; Langman, MJ; Prichard, PJ; Richens, A; Somerville, KW; Walt, RP; Williams, J, 1987
)
0.54
" Derived pharmacokinetic constants of intact omeprazole were within the range of those reported in healthy individuals."( Pharmacokinetics of [14C]omeprazole in patients with impaired renal function.
Andersson, T; Bodemar, G; Larsson, R; Naesdal, J; Regårdh, CG; Skånberg, I; Walan, A, 1986
)
0.83
" Omeprazole was rapidly absorbed (peak plasma levels were reached within one hour) and the elimination half-life was approximately one hour."( Animal pharmacodynamics of omeprazole. A survey of its pharmacological properties in vivo.
Carlsson, E; Larsson, H; Mattson, H; Sundell, G, 1985
)
1.48
" The mean elimination half-life in man and in the dog is about 1 hour, whereas half-lives in the range of 5 to 15 minutes have been recorded in the mouse."( Pharmacokinetics and metabolism of omeprazole in animals and man--an overview.
Gabrielsson, M; Hoffman, KJ; Löfberg, I; Regårdh, CG; Skånberg, I, 1985
)
0.55
"Pharmacodynamic and pharmacokinetic studies of omeprazole, a new gastric antisecretory agent, were undertaken in 8 healthy subjects."( Omeprazole: a study of its inhibition of gastric pH and oral pharmacokinetics after morning or evening dosage.
Buckle, PJ; Jones, DB; Louis, WJ; Mihaly, GW; Prichard, PJ; Smallwood, RA; Yeomans, ND, 1985
)
1.97
" The absorption and pharmacokinetic profile of omeprazole were not affected by dialysis."( Antisecretory effect and oral pharmacokinetics of omeprazole in patients with chronic renal failure.
Forrest, JA; Howden, CW; Hughes, DM; Macdougall, AI; Meredith, PA; Payton, CD; Reid, JL, 1985
)
0.78
" We concluded that pharmacokinetic elimination patterns of OPZ and LPZ were different, whereas the pharmacodynamic characteristics of both drugs are nearly the same in rats."( Comparative pharmacokinetic/pharmacodynamic study of proton pump inhibitors, omeprazole and lansoprazole in rats.
Iga, T; Katashima, M; Sawada, Y; Sugiura, M; Yamamoto, K, 1995
)
0.52
" None of the pharmacokinetic parameters differed significantly after prior treatment with omeprazole compared with placebo."( Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics.
Koeppe, P; Lode, H; Rost, KL; Schaberg, T; Stuht, H, 1995
)
0.76
"A pharmacodynamic interactional study with omeprazole was undertaken in rats."( Pharmacodynamic interactions of omeprazole with CNS active drugs in rats.
Chakrabarti, A; Chandrashekhar, SM; Garg, SK, 1995
)
0.84
" Three separate studies were conducted to evaluate the safety and to establish the pharmacokinetic profile of E3810 after oral administration to healthy male subjects."( Pharmacokinetic properties of E3810, a new proton pump inhibitor, in healthy male volunteers.
Hasegawa, J; Morishita, N; Nakai, H; Ogawa, T; Ohnishi, A; Shimamura, Y; Tomono, Y; Yasuda, S, 1994
)
0.29
" The variation between different subjects dominated the total variance for all of the pharmacokinetic parameters studied except the rate of disappearance of ethanol from blood (ko)."( Between-subject and within-subject variations in the pharmacokinetics of ethanol.
Jones, AW; Jönsson, KA, 1994
)
0.29
"The experience with long-term treatment of peptic ulcer with omeprazole is still scant, but the possibility cannot be excluded that its better pharmacodynamic effect on gastric acidity also has a positive result in the relapse rate."( A pharmacodynamic study of two omeprazole regimens suitable for long-term treatment of duodenal ulcer.
Badalamenti, S; Di Mario, F; Mela, GS; Muratore, F; Pantalena, M; Savarino, V; Scialabba, A; Termini, R; Vigneri, S; Zentilin, P, 1994
)
0.82
"The two omeprazole regimens we tested are effective in reducing gastric acidity, and their pharmacodynamic action does not decrease with time."( A pharmacodynamic study of two omeprazole regimens suitable for long-term treatment of duodenal ulcer.
Badalamenti, S; Di Mario, F; Mela, GS; Muratore, F; Pantalena, M; Savarino, V; Scialabba, A; Termini, R; Vigneri, S; Zentilin, P, 1994
)
1.01
"Key pharmacokinetic and pharmacodynamic aspects of gastric acid-suppressive agents in patients with gastroesophageal reflux disease (GERD) are discussed."( Pharmacokinetics and pharmacodynamics of acid-suppressive agents in patients with gastroesophageal reflux disease.
Goss, TF; Schentag, JJ, 1993
)
0.29
" If two drugs of the same class have a similar dose-efficacy profile, then the favourable/unfavourable balance of the pharmacokinetic characteristics of the drugs may determine the drug of choice."( Pharmacokinetics--a relevant factor for the choice of a drug?
Benet, LZ; Zech, K, 1994
)
0.29
" The dose-dependency of a range of pantoprazole pharmacokinetic characteristics was studied."( Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration.
Bliesath, H; Hartmann, M; Huber, R; Lühmann, R; Wurst, W, 1994
)
0.29
" In renal failure, the absorption of L was unchanged, its half-life being similar to that in healthy subjects; a small change seen in mild renal failure patients (creatinine clearance between 40 and 60 ml/min) was attributed to the age of the patients."( Pharmacokinetics of lansoprazole in patients with renal or liver disease of varying severity.
Delhotal-Landes, B; Dellatolas, F; Duchier, J; Flouvat, B; Lemaire, M; Molinie, P, 1993
)
0.29
" Our results do not rule out a possible effect on psychomotor function as a result of a pharmacodynamic interaction."( Omeprazole therapy does not affect pharmacokinetics of orally administered ethanol in healthy male subjects.
Brier, ME; Levinson, SS; Minocha, A; Rahal, PS, 1995
)
1.73
"The pharmacokinetic interaction potential of the new proton-pump inhibitor lansoprazole and theophylline was assessed in a double-blind, two-period (13-day duration per period), multiple-dose crossover study in 14 healthy male volunteers."( Pharmacokinetic interaction between lansoprazole and theophylline.
Cavanaugh, JH; Granneman, GR; Karol, MD; Locke, CS, 1995
)
0.29
" The pharmacokinetic parameters of theophylline were determined, and the urinary recovery of unchanged theophylline and its major metabolites were calculated."( Effects of lansoprazole on pharmacokinetics and metabolism of theophylline.
Ihara, N; Kokufu, T; Koyama, H; Mori, S; Nakajima, K; Ohta, T; Sugioka, N, 1995
)
0.29
"The pharmacokinetic profile of omeprazole was examined in 27 healthy Japanese volunteers, and the results were analyzed in relation to genotype for the two mutations, CgammaP2C19m1 in exon 5 and CgammaP2C19m2 in exon 4, associated with the poor metabolizer phenotype."( Pharmacokinetics of omeprazole (a substrate of CYP2C19) and comparison with two mutant alleles, C gamma P2C19m1 in exon 5 and C gamma P2C19m2 in exon 4, in Japanese subjects.
Amamoto, T; Higuchi, S; Ieiri, I; Irie, S; Kimura, M; Kubota, T; Mamiya, K; Nakamura, K; Nakano, S; Urae, A; Wada, Y; Yoshioka, S, 1996
)
0.9
"Stereoselective and sensitive methods employing chiral stationary phase columns for HPLC determination of enantiomers of lansoprazole in the human serum were developed and pharmacokinetic behaviors of the enantiomers were evaluated in seven subjects."( Determination of R(+)- and S(-)-lansoprazole using chiral stationary-phase liquid chromatography and their enantioselective pharmacokinetics in humans.
Arimori, K; Fujioka, Y; Fujiyama, S; Katafuchi, S; Katsuki, H; Nakamura, C; Nakano, M; Yagi, H, 1996
)
0.29
" The mean Cmax and the AUC values of R(+)-enantiomer were 3-5 times greater than those of S(-)-enantiomer following oral administration of 30 mg of racemic lansoprazole."( Determination of R(+)- and S(-)-lansoprazole using chiral stationary-phase liquid chromatography and their enantioselective pharmacokinetics in humans.
Arimori, K; Fujioka, Y; Fujiyama, S; Katafuchi, S; Katsuki, H; Nakamura, C; Nakano, M; Yagi, H, 1996
)
0.29
" The dose-dependency of a range of pantoprazole pharmacokinetic characteristics was studied."( Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration.
Bliesath, H; Hartmann, M; Huber, R; Lühmann, R; Wurst, W, 1996
)
0.29
" The range of clinically acceptable variation in the pharmacokinetic characteristics of drug A defines the equivalence range."( Lack of pharmacokinetic interaction as an equivalence problem.
Hartmann, M; Huber, R; Radtke, HW; Steinijans, VW, 1996
)
0.29
" Lack of pharmacokinetic interaction was handled as an equivalence problem."( Lack of pharmacokinetic interaction between pantoprazole and diclofenac.
Bliesath, H; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.29
" Lack of pharmacokinetic interaction was handled as an equivalence problem."( Lack of pharmacokinetic interaction between pantoprazole and diclofenac.
Bliesath, H; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.29
"021 1 h-1 kg-1 for test and reference) and elimination half-life (36."( Lack of pharmacokinetic interaction of pantoprazole with diazepam in man.
Bliesath, H; Brod, I; Gugler, R; Hartmann, M; Huber, R; Klotz, U; Rudi, J; Steinijans, VW; Wurst, W, 1996
)
0.29
" The primary pharmacokinetic characteristics for extent and rate of absorption were AUC(0-24h) and % PTF, respectively."( Pantoprazole has no influence on steady state pharmacokinetics and pharmacodynamics of metoprolol in healthy volunteers.
Bliesath, H; Hartmann, M; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.29
" Eighteen volunteers entered the study; pharmacokinetic data were evaluable for 15 participants."( Lack of pharmacokinetic interaction after administration of lansoprazole or omeprazole with prednisone.
Cavanaugh, JH; Karol, MD, 1996
)
0.52
" As a pharmacodynamic parameter, the prothrombin time ratio was determined on days 9 and 10 (reference value) and on days 14 and 15 (test value), and the ratio test/reference was evaluated according to equivalence criteria."( Lack of pharmacodynamic and pharmacokinetic interaction between pantoprazole and phenprocoumon in man.
Birkel, M; Bliesath, H; Ehrlich, A; Fuder, H; Hartmann, M; Huber, R; Lücker, PW; Steinijans, VW; Timmer, W; Wieckhorst, G; Wurst, W, 1996
)
0.29
" The pharmacokinetic characteristics AUC0-24h and Cmax of S(-)- and R(+)-phenprocoumon were also investigated using equivalence criteria."( Lack of pharmacodynamic and pharmacokinetic interaction between pantoprazole and phenprocoumon in man.
Birkel, M; Bliesath, H; Ehrlich, A; Fuder, H; Hartmann, M; Huber, R; Lücker, PW; Steinijans, VW; Timmer, W; Wieckhorst, G; Wurst, W, 1996
)
0.29
"Pantoprazole does not interact with the anticoagulant phenprocoumon on a pharmacodynamic or pharmacokinetic level."( Lack of pharmacodynamic and pharmacokinetic interaction between pantoprazole and phenprocoumon in man.
Birkel, M; Bliesath, H; Ehrlich, A; Fuder, H; Hartmann, M; Huber, R; Lücker, PW; Steinijans, VW; Timmer, W; Wieckhorst, G; Wurst, W, 1996
)
0.29
" The ideal therapy for GORD will have linear pharmacokinetics, a relatively long plasma half-life (t1/2), a duration of action allowing once daily administration, and a stable effect independent of interactions with food, antacids and other drugs."( Pharmacokinetic optimisation in the treatment of gastro-oesophageal reflux disease.
Berstad, A; Hatlebakk, JG, 1996
)
0.29
" A significant, although weak, relationship existed between creatinine clearance (CLCR) and area under the plasma concentration versus time curve (AUC) and terminal disposition half-life (t1/2), calculated with total concentration data."( Lansoprazole pharmacokinetics in subjects with various degrees of kidney function.
Cavanaugh, JM; Karol, MD; Machinist, JM, 1997
)
0.3
"A rapid and sensitive high-performance thin-layer chromatography (HPTLC) method has been developed for the measurement of lansoprazole in human plasma and its use for pharmacokinetic study has been evaluated."( High-performance thin-layer chromatographic method for the detection and determination of lansoprazole in human plasma and its use in pharmacokinetic studies.
Chakravarthy, BK; Gandhi, TP; Modi, IA; Modi, RI; Mody, VD; Pandya, KK; Satia, MC, 1997
)
0.3
"We investigated whether interindividual differences in the pharmacokinetic disposition of lansoprazole are attributed to the genetic polymorphism of CYP2C19 which occurred by two mutations."( Genetic polymorphism of CYP2C19 and lansoprazole pharmacokinetics in Japanese subjects.
Arimori, K; Fujiyama, S; Katsuki, H; Nakamura, C; Nakano, M, 1997
)
0.3
" Pharmacokinetic parameters for metronidazole and hydroxymetronidazole were calculated, and the significance of the mean differences in parameters between omeprazole and placebo co-administration was assessed using a two-tailed, paired t-test."( The effect of omeprazole on the pharmacokinetics of metronidazole and hydroxymetronidazole in human plasma, saliva and gastric juice.
Barrett, DA; Goddard, AF; Jessa, MJ; Shaw, PN; Spiller, RC, 1997
)
0.86
"05) in any of the plasma or saliva pharmacokinetic parameter values for metronidazole between volunteers receiving omeprazole or placebo when metronidazole was administered either as an intravenous infusion or orally."( The effect of omeprazole on the pharmacokinetics of metronidazole and hydroxymetronidazole in human plasma, saliva and gastric juice.
Barrett, DA; Goddard, AF; Jessa, MJ; Shaw, PN; Spiller, RC, 1997
)
0.87
" On day 2 of each study period, a single 10 mg oral dose of racemic acenocoumarol was administered and venous blood samples were collected for pharmacokinetic and pharmacodynamic assessments."( No effect of short-term omeprazole intake on acenocoumarol pharmacokinetics and pharmacodynamics.
Beysens, AJ; de Hoon, JN; Thijssen, HH; Van Bortel, LM, 1997
)
0.6
"Haemodialysis has no influence on the pharmacokinetic characteristics of pantoprazole."( Pharmacokinetics of pantoprazole in patients with end-stage renal failure.
Bahlmann, J; Hartmann, M; Huber, R; Kliem, V; Lühmann, R; Wurst, W, 1998
)
0.3
" With concomitant omeprazole treatment, the mean AUC0-24 and Cmax of itraconazole were significantly reduced by 64% and 66%, respectively."( Effect of omeprazole on the pharmacokinetics of itraconazole.
Jaruratanasirikul, S; Sriwiriyajan, S, 1998
)
1.04
" Cmax (maximum serum concentration) and AUC (area under the serum concentration-time curve) for (+)-lansoprazole were 5-6 times greater than those for (-)-lansoprazole, whereas for (+)-5-hydroxylansoprazole both values were significantly smaller than those for the (-) enantiomer."( Pharmacokinetic differences between lansoprazole enantiomers in rats.
Arimori, K; Katsuki, H; Nakano, M; Yasuda, K, 1998
)
0.3
" For pantoprazole, no differences were observed in AUC and Cmax after single and repeated dosing."( Comparison of the pharmacodynamics and pharmacokinetics of pantoprazole (40 mg) as compared to omeprazole MUPS (20 mg) after repeated oral dose administration.
Ehrlich, A; Huber, R; Lücker, PW; Mascher, H; Sander, P; Wiedemann, A,
)
0.35
" The pharmacokinetic parameters, Cmax, t(max), AUC and t1/2, showed no statistically significant differences when rabeprazole was administered alone, concomitantly with antacid or one hour after antacid administration."( Antacids have no influence on the pharmacokinetics of rabeprazole, a new proton pump inhibitor, in healthy volunteers.
Higashi, S; Kawaguchi, M; Murakami, M; Tomono, Y; Yasuda, S, 1999
)
0.3
"This single-center, open-label study was undertaken to compare the tolerability and pharmacokinetic profiles of rabeprazole, a new proton-pump inhibitor (PPI), in healthy volunteers and in subjects with chronic cirrhosis."( Rabeprazole: pharmacokinetics in patients with stable, compensated cirrhosis.
Grimes, I; Hoyumpa, AM; Humphries, TJ; Trevino-Alanis, H, 1999
)
0.3
" Neither the elimination half-life nor the area under the curve was significantly different between the two sessions."( Pharmacokinetic interaction between acetaminophen and lansoprazole.
Enatsu, I; Hanada, Y; Kuyama, Y; Makino, H; Mineshita, S; Qi, J; Sanaka, M; Tanaka, H; Yamanaka, M, 1999
)
0.3
"Within both the patient and volunteers groups, there were no significant differences between day 1 and day 7 in any of the pharmacokinetic parameters including maximum concentration (Cmax), area under the concentration-time curve (AUC), and terminal half-life of elimination (t(1/2))."( Lansoprazole pharmacokinetics differ in patients with oesophagitis compared to healthy volunteers.
Barclay, ML; Begg, EJ; Ketelbey, JW; Peters, WA; Robson, RA, 1999
)
0.3
"The authors compare the pharmacokinetic profiles, safety, and tolerability of rabeprazole, a new proton pump inhibitor (PPI), in healthy volunteers and in subjects with stable, end-stage renal failure."( Rabeprazole: pharmacokinetics and tolerability in patients with stable, end-stage renal failure.
Grimes, I; Humphries, TJ; Keane, WF; Swan, SK, 1999
)
0.3
" As increased cisapride concentrations may result in longer electrocardiogram (ECG) QTc intervals, a crossover study was conducted in healthy subjects to evaluate the oral pharmacokinetic interaction between cisapride (20 mg) and pantoprazole (40 mg)."( Lack of pharmacokinetic interaction between oral pantoprazole and cisapride in healthy adults.
Ferron, GM; Fruncillo, RJ; Martin, PT; Mayer, PR; Paul, JC; Yacoub, L, 1999
)
0.3
" The maximum plasma concentration (Cmax) and the area under the plasma concentration time curve (AUC) are linearly related to dose, while the time to maximum plasma concentration (tmax) and elimination half-life (t1/2) are dose-independent."( Review article: the pharmacokinetics of rabeprazole in health and disease.
Hoyumpa, AM; Merritt, GJ; Swan, SK, 1999
)
0.3
" As a result of structural and functional similarities, the PPIs share many pharmacokinetic features."( Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy.
Lew, EA, 1999
)
0.3
" Blood was sampled for 48 h after dosing for determination of pharmacokinetic parameters."( Effect of omeprazole on the pharmacokinetics of oral gemifloxacin in healthy volunteers.
Allen, A; Lewis, A; Vousden, M,
)
0.53
" There were no statistically significant differences between the two regimens for mean phenytoin Cmax or tmax."( Lack of pharmacokinetic interaction between lansoprazole and intravenously administered phenytoin.
Cavanaugh, JH; Karol, MD; Locke, CS, 1999
)
0.3
" Dengue patients manifested the same pharmacokinetic responses to a 20 g Ala-Gln bolus as healthy controls."( The pharmacokinetic responses of humans to 20 g of alanyl-glutamine dipeptide differ with the dosing protocol but not with gastric acidity or in patients with acute Dengue fever.
Fürst, P; Klassen, P; Mazariegos, M; Solomons, NW, 2000
)
0.31
"To study the potential pharmacokinetic interaction between lansoprazole or pantoprazole and theophylline at steady state."( Lack of a pharmacokinetic interaction between lansoprazole or pantoprazole and theophylline.
Goldwater, DR; Hunt, RH; Pan, WJ; Pilmer, BL; Zhang, Y, 2000
)
0.31
"No significant changes in the steady-state theophylline maximum plasma concentration (Cmax), time to Cmax (Tmax), minimum plasma concentration (Cmin), area under the plasma concentration-time curve over the 12-h dosing interval (AUC0-12), or apparent total oral clearance (CL/F) were observed within the two treatment groups when theophylline was administered alone or in combination with lansoprazole or pantoprazole."( Lack of a pharmacokinetic interaction between lansoprazole or pantoprazole and theophylline.
Goldwater, DR; Hunt, RH; Pan, WJ; Pilmer, BL; Zhang, Y, 2000
)
0.31
" Serial blood samples were taken on days 1 and 5 of each course for pharmacokinetic measurements."( Oral pharmacokinetics of omeprazole and lansoprazole after single and repeated doses as intact capsules or as suspensions in sodium bicarbonate.
Howden, CW; Peyton, B; Raufman, JP; Sharma, VK; Spears, T, 2000
)
0.61
"To evaluate and compare the pharmacodynamic effects of IY-81149 and omeprazole on gastric pH in patients with gastroesophageal reflux disease."( A comparative pharmacodynamic study of IY-81149 versus omeprazole in patients with gastroesophageal reflux disease.
Boileau, F; Cho, KD; Goldwater, R; Jung, WT; Kim, DY; Lee, SM; Park, DW; Periclou, AP, 2000
)
0.79
" Pharmacokinetic study was optional for subjects and was performed in 25 of the 57 enrolled."( Pharmacokinetics of orally administered omeprazole in children. International Pediatric Omeprazole Pharmacokinetic Group.
Andersson, T; Becker, M; Behrens, R; Dalväg, A; Drouin, E; Göthberg, G; Hassall, E; Koletzko, S; Lundborg, P; Marcon, M; Martin, S; Radke, M; Shepherd, R, 2000
)
0.57
" An irreversible pharmacodynamic response model was successfully developed and validated."( Pharmacodynamic modeling of pantoprazole's irreversible effect on gastric acid secretion in humans and rats.
Ferron, GM; Mayer, PR; McKeand, W, 2001
)
0.31
" Sequential blood samples were collected over 24 h to characterize SOS absorption and pharmacokinetic parameters."( A randomized, pharmacokinetic and pharmacodynamic, cross-over study of duodenal or jejunal administration compared to nasogastric administration of omeprazole suspension in patients at risk for stress ulcers.
Metzler, MH; Miedema, BW; Olsen, KM; Phillips, JO; Rangnekar, NJ; Rebuck, JA, 2001
)
0.51
"In critically ill surgical patients, pharmacokinetic parameters and subsequent pH control after the administration of SOS are similar by the jejunal, nasogastric, or duodenal route."( A randomized, pharmacokinetic and pharmacodynamic, cross-over study of duodenal or jejunal administration compared to nasogastric administration of omeprazole suspension in patients at risk for stress ulcers.
Metzler, MH; Miedema, BW; Olsen, KM; Phillips, JO; Rangnekar, NJ; Rebuck, JA, 2001
)
0.51
" To determine the role of cytochrome P450 (CYP) 2C19 in the stereoselective metabolism of pantoprazole, we investigated the pharmacokinetic disposition of (+)- and (-)-pantoprazole in 7 extensive metabolizers and 7 poor metabolizers of S-mephenytoin."( Stereoselective pharmacokinetics of pantoprazole, a proton pump inhibitor, in extensive and poor metabolizers of S-mephenytoin.
Ishizaki, T; Kaneko, S; Ohkubo, T; Otani, K; Ryokawa, Y; Sugawara, K; Suzuki, A; Tanaka, M, 2001
)
0.31
" The mean Cmax and area under the curve (AUC) values of (+)-lansoprazole were 4-5 times greater than those of (-)-lansoprazole following oral administration of 30-mg racemic lansoprazole to dogs."( Pharmacokinetic differences between lansoprazole enantiomers and contribution of cytochrome P450 isoforms to enantioselective metabolism of lansoprazole in dogs.
Arimori, K; Fujii, J; Hamada, A; Masa, K; Nakano, M, 2001
)
0.31
" To confirm the involvement of CYP2C19, we performed a pharmacokinetic interaction study."( Effect of omeprazole on the pharmacokinetics of moclobemide according to the genetic polymorphism of CYP2C19.
Bae, KS; Cho, JY; Jang, IJ; Lee, KH; Park, JY; Park, SS; Shin, SG; Yi, SY; Yim, DS; Yu, KS, 2001
)
0.71
" On the eighth morning, 300 mg of moclobemide and 40 mg of placebo were coadministered with 200 mL of water, and a pharmacokinetic study was performed."( Effect of omeprazole on the pharmacokinetics of moclobemide according to the genetic polymorphism of CYP2C19.
Bae, KS; Cho, JY; Jang, IJ; Lee, KH; Park, JY; Park, SS; Shin, SG; Yi, SY; Yim, DS; Yu, KS, 2001
)
0.71
" After daily administration of omeprazole for 1 week, the pharmacokinetic parameters of moclobemide and its metabolites in extensive metabolizers changed to values similar to those in poor metabolizers."( Effect of omeprazole on the pharmacokinetics of moclobemide according to the genetic polymorphism of CYP2C19.
Bae, KS; Cho, JY; Jang, IJ; Lee, KH; Park, JY; Park, SS; Shin, SG; Yi, SY; Yim, DS; Yu, KS, 2001
)
1
" Plasma omeprazole concentrations were determined by a validated high-performance liquid chromatographic method, and pharmacokinetic values were determined."( Pharmacokinetic comparison of omeprazole capsules and a simplified omeprazole suspension.
Fan, C; Quercia, RA; Song, JC; Tsikouris, J; White, CM, 2001
)
1.03
" Based on the metabolic and pharmacokinetic differences among other proton pump inhibitors such as omeprazole, lansoprazole and pantoprazole, rabeprazole appears to be the least affected proton pump inhibitor by the CYP2C19-related genetic polymorphism."( Pharmacodynamic effects and kinetic disposition of rabeprazole in relation to CYP2C19 genotypes.
Furuie, H; Horai, Y; Irie, S; Ishizaki, T; Kimura, M; Koga, Y; Matsuguma, K; Matsui, T; Murakami, M; Nagahama, T; Urae, A; Yao, T, 2001
)
0.53
"To determine whether the pharmacodynamic effects of rabeprazole on intragastric pH and serum gastrin levels, and its pharmacokinetics depend on the CYP2C19 genotype status."( Pharmacodynamic effects and kinetic disposition of rabeprazole in relation to CYP2C19 genotypes.
Furuie, H; Horai, Y; Irie, S; Ishizaki, T; Kimura, M; Koga, Y; Matsuguma, K; Matsui, T; Murakami, M; Nagahama, T; Urae, A; Yao, T, 2001
)
0.31
"The pharmacodynamic effects of rabeprazole and its pharmacokinetics depend on the CYP2C19 genotype status."( Pharmacodynamic effects and kinetic disposition of rabeprazole in relation to CYP2C19 genotypes.
Furuie, H; Horai, Y; Irie, S; Ishizaki, T; Kimura, M; Koga, Y; Matsuguma, K; Matsui, T; Murakami, M; Nagahama, T; Urae, A; Yao, T, 2001
)
0.31
"A comparative pharmacokinetic study with each PPI was designed as an open, randomized, and crossover study of 18 Japanese healthy volunteers who were classified into the homozygous, heterozygous extensive metabolizer and the poor metabolizer based on the CYP2C19 genotype determined by PCR-RFLP method."( CYP2C19 genotype and pharmacokinetics of three proton pump inhibitors in healthy subjects.
Aoyama, N; Hohda, T; Kasuga, M; Kita, T; Nishiguchi, K; Nishitora, Y; Okumura, K; Sakaeda, T; Sakai, T; Sirasaka, D; Tamura, T; Tanigawara, Y, 2001
)
0.31
" As for rabeprazole, the pharmacokinetic profile was independent of the CYP2C19 genotype."( CYP2C19 genotype and pharmacokinetics of three proton pump inhibitors in healthy subjects.
Aoyama, N; Hohda, T; Kasuga, M; Kita, T; Nishiguchi, K; Nishitora, Y; Okumura, K; Sakaeda, T; Sakai, T; Sirasaka, D; Tamura, T; Tanigawara, Y, 2001
)
0.31
" Patients with gastro-oesophageal reflux disease exhibit a pharmacokinetic pattern similar to that in healthy individuals, whereas elderly individuals exhibited a slightly lower metabolism rate."( Pharmacokinetic studies with esomeprazole, the (S)-isomer of omeprazole.
Andersson, T; Hassan-Alin, M; Hasselgren, G; Röhss, K; Weidolf, L, 2001
)
0.6
" Pharmacokinetic parameters were similar in responders and non-responders to the higher dose."( Lansoprazole in children: pharmacokinetics and efficacy in reflux oesophagitis.
Faure, C; Hankard, R; Jacoz-Aigrain, E; Laurence, M; Michaud, L; Mougenot, JF; Navarro, J; Popon, M; Shaghaghi, EK, 2001
)
0.31
"This study sought to determine whether dosage adjustment of pantoprazole is required in patients with moderate or severe hepatic impairment by comparing the pharmacokinetic profile of pantoprazole in such patients with that in healthy slow metabolizers of pantoprazole, in whom no dosage adjustment is required."( Pharmacokinetics of pantoprazole in patients with moderate and severe hepatic dysfunction.
Abell, M; Ferron, GM; Getsy, J; Mayer, P; Noveck, RJ; Paul, J; Pockros, P; Preston, RA; Turner, M, 2001
)
0.31
" Pharmacokinetic data were compared between the 2 groups with hepatic impairment and against historical data from 17 healthy subjects who were genetically slow CYP2C19 metabolizers of pantoprazole."( Pharmacokinetics of pantoprazole in patients with moderate and severe hepatic dysfunction.
Abell, M; Ferron, GM; Getsy, J; Mayer, P; Noveck, RJ; Paul, J; Pockros, P; Preston, RA; Turner, M, 2001
)
0.31
" CL(int,in vivo) was calculated from in vivo pharmacokinetic data using three frequent mathematical models (the well stirred, parallel-tube, and dispersion models)."( Prediction of human hepatic clearance from in vivo animal experiments and in vitro metabolic studies with liver microsomes from animals and humans.
Kagayama, A; Kimura, S; Naritomi, Y; Sugiyama, Y; Suzuki, A; Terashita, S, 2001
)
0.31
" At day 3, a 24-hour intragastric pH and a pharmacokinetic study of omeprazole were performed."( Intravenous omeprazole in children: pharmacokinetics and effect on 24-hour intragastric pH.
Faure, C; Jacqz-Aigrain, E; Michaud, L; Navarro, J; Popon, M; Shaghaghi, EK; Turck, D, 2001
)
0.92
"The influence of synthetic drugs prescribed for peptic ulcer on the pharmacokinetic fate of glycyrrhizin (GL) from Shaoyao-Gancao-tang (SGT, a traditional Chinese formulation, Shakuyaku-Kanzo-to in Japanese) was investigated in rats."( The influence of commonly prescribed synthetic drugs for peptic ulcer on the pharmacokinetic fate of glycyrrhizin from Shaoyao-Gancao-tang.
Akao, T; He, JX; Nishino, T; Tani, T, 2001
)
0.31
" When administered intravenously, the half-life during the elimination phase was significantly prolonged by 30 min of immobilization stress, but the AUC value remained unchanged."( The effect of immobilization stress on the pharmacokinetics of omeprazole in rats.
Araki, H; Gomita, Y; Hashimoto, Y; Matsuka, N; Okazaki, M; Watanabe, K, 2002
)
0.55
" In treated group, the area under the plasma concentration-time curve of omeprazole from time zero to time infinity (AUC) was significantly greater (3090 vs 491 ng h/ml), terminal half-life of omeprazole was significantly longer (2."( Influence of fluconazole on the pharmacokinetics of omeprazole in healthy volunteers.
Cho, HK; Kang, BC; Shin, WG; Suh, OK; Yang, CQ, 2002
)
0.8
" For the iv groups (CO(iv) and OP(iv)), the Cp-analgesic effect relationship was described by an E(max) sigmoid model and omeprazole did not affect the pharmacodynamic parameters."( Effect of omeprazole on oral and intravenous RS-methadone pharmacokinetics and pharmacodynamics in the rat.
Calvo, R; Carlos, MA; Carlos, R; Du Souich, P; Lukas, JC; Suarez, E, 2002
)
0.92
" After each dose was administered, the pharmacokinetic profiles of omeprazole and its two metabolites were significantly different between extensive metabolizers and poor metabolizers."( Optimal dose of omeprazole for CYP2C19 extensive metabolizers in anti-Helicobacter pylori therapy: pharmacokinetic considerations.
Aoyama, N; Kasuga, M; Kawahara, Y; Kita, T; Okumura, K; Sakaeda, T; Sakai, T, 2002
)
0.9
" For lansoprazole, the elimination half-life (t(1/2)) was significantly prolonged (1."( Pharmacokinetics of lansoprazole, amoxicillin and clarithromycin after simultaneous and single administration.
Borner, K; Koeppe, P; Kotwas, J; Lode, H; Mainz, D, 2002
)
0.31
" Here, we identify factors in specific disease therapy and proton pump inhibitor (PPI) pharmacokinetic and pharmacodynamic characteristics that help us achieve this goal."( The clinical importance of proton pump inhibitor pharmacokinetics.
Thomson, AB; Yacyshyn, BR, 2002
)
0.31
"Proton pump inhibitors, the reference standard in adults with acid-related disorders, are increasingly being used in children despite limited pediatric safety and pharmacokinetic data."( Safety and pharmacokinetics of oral lansoprazole in preadolescent rats exposed from weaning through sexual maturity.
Fort, FL; Turck, P; Youssef, AF,
)
0.13
"A mechanism-based pharmacodynamic model was used to describe the inhibitory effect by omeprazole on gastric acid secretion measured after histamine stimulation in the dog."( Gastric acid secretion in the dog: a mechanism-based pharmacodynamic model for histamine stimulation and irreversible inhibition by omeprazole.
Abelö, A; Eriksson, UG; Gabrielsson, J; Holstein, B; Karlsson, MO, 2002
)
0.74
" Blood samples were collected on day 1 of both periods to determine the pharmacokinetic parameters."( Comparative pharmacokinetics and safety of lansoprazole oral capsules and orally disintegrating tablets in healthy subjects.
Ballard, ED; Chiu, YL; Freston, JW; Mulford, DJ, 2003
)
0.32
" Blood samples for pharmacokinetic evaluation and urine samples for cortisol assessments were collected before and after the budesonide doses."( Pharmacokinetics of budesonide controlled-release capsules when taken with omeprazole.
Bergstrand, M; Edsbäcker, S; Larsson, P, 2003
)
0.55
" The effects of lansoprazole on 24-hour median intragastric pH, the percentages of time intragastric pH was above 3 and 4, and pharmacokinetic parameters were assessed at the day-5 visit and compared to baseline."( Pharmacokinetics and pharmacodynamics of lansoprazole in children with gastroesophageal reflux disease.
Book, L; Chiu, YL; Gremse, D; Gunasekaran, T; Karol, M; Pan, WJ; Pilmer, B; Tolia, V; Winter, H, 2002
)
0.31
"The observed pharmacokinetic properties of lansoprazole in children between 1 and 11 years of age with GERD were similar to those previously observed in healthy adult subjects."( Pharmacokinetics and pharmacodynamics of lansoprazole in children with gastroesophageal reflux disease.
Book, L; Chiu, YL; Gremse, D; Gunasekaran, T; Karol, M; Pan, WJ; Pilmer, B; Tolia, V; Winter, H, 2002
)
0.31
"The pharmacokinetic parameters of lansoprazole observed in this study of adolescents are similar to those observed in studies of healthy adults."( Lansoprazole in adolescents with gastroesophageal reflux disease: pharmacokinetics, pharmacodynamics, symptom relief efficacy, and tolerability.
Chiu, YL; Fitzgerald, J; Gremse, D; Gunasekaran, T; Gupta, S; Karol, M; Keith, R; Pan, WJ, 2002
)
0.31
"To determine the pharmacokinetic and pharmacodynamic rationale for the optimum regimen of rabeprazole in the treatment of Helicobacter pylori infection in patients who are cytochrome P450 (CYP) 2C19 poor metabolizers or extensive metabolizers."( Time-dependent amplified pharmacokinetic and pharmacodynamic responses of rabeprazole in cytochrome P450 2C19 poor metabolizers.
Chern, HD; Lin, CJ; Uang, YS; Wang, TH; Yang, JC, 2003
)
0.32
"Prospective, multiple-dose pharmacokinetic and pharmacodynamic study."( Time-dependent amplified pharmacokinetic and pharmacodynamic responses of rabeprazole in cytochrome P450 2C19 poor metabolizers.
Chern, HD; Lin, CJ; Uang, YS; Wang, TH; Yang, JC, 2003
)
0.32
"Pharmacokinetic and pharmacodynamic parameters were compared between CYP2C19 poor and extensive metabolizers on day 1 and day 4 of dosing."( Time-dependent amplified pharmacokinetic and pharmacodynamic responses of rabeprazole in cytochrome P450 2C19 poor metabolizers.
Chern, HD; Lin, CJ; Uang, YS; Wang, TH; Yang, JC, 2003
)
0.32
"Mean Cmax and AUCtau of voriconazole were increased by 15%[90% confidence interval (CI) 5, 25] and 41% (90% CI 29, 55), respectively, with no effect on tmax during coadministration of omeprazole."( Effect of omeprazole on the steady-state pharmacokinetics of voriconazole.
Hamlin, J; Kleinermans, D; Layton, G; Nichols, D; Purkins, L; Tan, K; Wood, N, 2003
)
0.91
" Because of the apparent safety of PPIs and a well-demonstrated dose-response-effect relationship in adults, pediatric pharmacokinetic data and an exposure correlate, such as the dose-area-under-the-plasma-concentration-versus-time-curve relationship, can be used as a bridge to determine pediatric dosing."( Proton pump inhibitors in pediatrics: relevant pharmacokinetics and pharmacodynamics.
Kearns, GL; Winter, HS,
)
0.13
" Population pharmacokinetic parameters were calculated using NONMEM."( Pharmacokinetics of omeprazole in healthy adults and in children with gastroesophageal reflux disease.
Alvarez, F; Brazier, JL; Drouin, E; Dubuc, MC; Ducharme, MP; Marier, JF, 2004
)
0.65
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" The pharmacokinetic parameters of omeprazole and pantoprazole were compared to those after intake of both agents alone."( Pharmacokinetic interactions between omeprazole/pantoprazole and clarithromycin in health volunteers.
Calabresi, L; Di Paolo, A; Ferrara, S; Pazzucconi, F; Sirtori, C; Tacca, MD, 2004
)
0.87
" Analysis of variance was performed to determine whether lumiracoxib alone differed from lumiracoxib plus omeprazole or from lumiracoxib plus Al/Mg antacid for overall exposure (area under the concentration-time curve from zero to infinity [AUC( infinity )]) and peak concentration (C(max)), with treatment sequence, subject, period and treatment as factors."( Lack of effect of omeprazole or of an aluminium hydroxide/magnesium hydroxide antacid on the pharmacokinetics of lumiracoxib.
Langholff, W; Milosavljev, S; Rordorf, C; Scott, G; Shenouda, M; Vinluan Reynolds, C, 2004
)
0.87
" Comparison of the pharmacokinetic parameters of omeprazole before and after fexofenadine revealed that there were no differences in peak concentration, time to peak concentration, area under the time concentration curve up to 8 hr, and elimination half-life."( Fexofenadine does not affect omeprazole pharmacokinetics: both are putative P-glycoprotein substrates.
Sugawara, K; Takahata, T; Tateishi, T; Uno, T; Yasui-Furukori, N; Yoshiya, G, 2004
)
0.87
" In the homo EMs and the PMs groups, the main kinetic parameters were as follows: Tmax (2."( Pharmacokinetics of lansoprazole in Chinese healthy subjects in relation to CYP2C19 genotypes.
Hu, YR; Kan, QC; Qiao, HL, 2004
)
0.32
" The mean terminal half-life of approximately 6 min was found across genotype and gender groups."( Altered pharmacokinetics of omeprazole in cystic fibrosis knockout mice relative to wild-type mice.
Ali, SY; Smith, PC; Tallman, MN, 2004
)
0.62
"05) in heterozygous EMs, whereas no difference in any pharmacokinetic parameters was found in PMs."( Effects of fluvoxamine on lansoprazole pharmacokinetics in relation to CYP2C19 genotypes.
Saito, M; Sugawara, K; Takahata, T; Tateishi, T; Uno, T; Yasui-Furukori, N, 2004
)
0.32
"Limited data characterize pharmacokinetic interactions between cephalexin and ranitidine, and no data exist for an interaction with proton pump inhibitors."( A randomized crossover study investigating the influence of ranitidine or omeprazole on the pharmacokinetics of cephalexin monohydrate.
Adejare, A; George, M; Madaras-Kelly, K; May, MP; Michas, P, 2004
)
0.55
" By comparing these pharmacokinetic parameters, we may state that there was no significant difference between the two administration modes."( Effect of water intake on pharmacokinetics of lansoprazole from fast disintegrating tablet in human subjects.
Irie, S; Ito, Y; Iwasaki, K; Nakamura, K; Sakurai, Y; Shibata, N; Takada, K; Takagi, N, 2004
)
0.32
" Pharmacokinetic parameters of S-omeprazole, R-omeprazole, racemic omeprazole and the two main metabolites (5-hydroxy and sulphone) were calculated using non-compartmental analysis."( A pharmacokinetic study comparing single and repeated oral doses of 20 mg and 40 mg omeprazole and its two optical isomers, S-omeprazole (esomeprazole) and R-omeprazole, in healthy subjects.
Andersson, T; Hassan-Alin, M; Niazi, M; Röhss, K, 2005
)
0.83
" Pharmacokinetic parameters were calculated with compartmental and non-compartmental analysis, using the computer program Kinetica (Inna Phase)."( A pharmacokinetic interaction study between omeprazole and the H2-receptor antagonist ranitidine.
Farcau, D; Leucuta, A; Nanulescu, M; Vlase, L, 2004
)
0.58
" The elimination half-life of rabeprazole sodium (1."( Pharmacokinetics of rabeprazole following single intravenous and oral administration to healthy subjects.
Hasegawa, J; Humphries, T; Laurent, A; Setoyama, T, 2005
)
0.33
"The pharmacokinetic profiles of single doses of lansoprazole 15- and 30-mg sachets for suspension were compared with those of corresponding doses of lansoprazole oral capsules."( Comparison of the pharmacokinetics of lansoprazole 15- and 30-mg sachets for suspension versus intact capsules.
Amer, F; Chiu, YL; Griffin, JS; Karol, MD; Locke, CS; Lukasik, NL; Pan, WJ, 2004
)
0.32
" Blood samples were collected before and after each administration to assess the pharmacokinetic parameters of lansoprazole and bioequivalence between suspension and capsule."( Comparison of the pharmacokinetics of lansoprazole 15- and 30-mg sachets for suspension versus intact capsules.
Amer, F; Chiu, YL; Griffin, JS; Karol, MD; Locke, CS; Lukasik, NL; Pan, WJ, 2004
)
0.32
" The pharmacokinetic parameters of the 15- and 30-mg lansoprazole sachets for suspension were similar to those of the corresponding doses of the oral capsules."( Comparison of the pharmacokinetics of lansoprazole 15- and 30-mg sachets for suspension versus intact capsules.
Amer, F; Chiu, YL; Griffin, JS; Karol, MD; Locke, CS; Lukasik, NL; Pan, WJ, 2004
)
0.32
" These pharmacokinetic characteristics confirm the suitability of this oral solid dosage form for use in future clinical trials."( Pharmacokinetic profile of the oral direct thrombin inhibitor dabigatran etexilate in healthy volunteers and patients undergoing total hip replacement.
Ahnfelt, L; Dahl, OE; Eriksson, BI; Nehmiz, G; Rathgen, K; Stähle, H; Stangier, J; Svärd, R, 2005
)
0.33
" The peak concentration ratios for oxybutynin and metabolite also conformed to this range; those for tolterodine did not."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.6
" Intragastric pH was recorded for 24 h after drug administration for pharmacodynamic evaluation."( Pharmacokinetics and pharmacodynamics of pantoprazole in clinically normal neonatal foals.
Giguère, S; Ryan, CA; Sanchez, LC; Vickroy, T, 2005
)
0.33
" The method was suitable for therapeutic drug monitoring and was applied to pharmacokinetic study in human volunteers."( Determination of rabeprazole and its active metabolite, rabeprazole thioether in human plasma by column-switching high-performance liquid chromatography and its application to pharmacokinetic study.
Shimizu, M; Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.33
"In view of the good tolerability of escitalopram, the pharmacokinetic changes observed on co-administration with cimetidine or omeprazole are unlikely to be of clinical concern."( The effect of cimetidine or omeprazole on the pharmacokinetics of escitalopram in healthy subjects.
Malling, D; Poulsen, MN; Søgaard, B, 2005
)
0.83
" After oral administration of DA-8159 at a dose of 30 mg/kg to rats without or with cola beverage, the pharmacokinetic parameters of DA-8159 and DA-8164 were not significantly different between two groups of rats."( Effects of omeprazole or cola beverage on the pharmacokinetics of oral DA-8159, a new erectogenic, in rats.
Bae, SK; Kim, WB; Kwon, JW; Lee, JH; Lee, MG, 2005
)
0.72
" In this open-label study, the effect of lansoprazole 30 mg qd and naproxen 500 mg bid on the pharmacokinetic profile of methotrexate was investigated."( Coadministration of lansoprazole and naproxen does not affect the pharmacokinetic profile of methotrexate in adult patients with rheumatoid arthritis.
Amer, F; Andhivarothai, N; Kukulka, MJ; Vakily, M, 2005
)
0.33
" The pharmacokinetic differences between pantoprazole enantiomers were evaluated by the experiments of the in situ perfusion into rat small intestine, the protein binding, and the in vitro metabolism in rat liver microsomes of pantoprazole enantiomers."( Pharmacokinetic differences between pantoprazole enantiomers in rats.
Xie, Z; Xu, H; Zhang, Y; Zhong, D, 2005
)
0.33
" Pharmacokinetic parameters were obtained by noncompartmental analysis."( The effect of aging on the relationship between the cytochrome P450 2C19 genotype and omeprazole pharmacokinetics.
Ishizawa, Y; Sasaki, M; Takahata, T; Tateishi, T; Yasui-Furukori, N, 2005
)
0.55
" ADP-induced platelet aggregation was measured as a pharmacodynamic index."( Interaction magnitude, pharmacokinetics and pharmacodynamics of ticlopidine in relation to CYP2C19 genotypic status.
Ieiri, I; Irie, S; Ishizaki, T; Kimura, M; Otsubo, K; Urae, A, 2005
)
0.33
" No significant intergenotypic differences in the pharmacokinetic parameters of ticlopidine were observed, although the accumulation ratio tended to be greater in hmEMs than in PMs (2."( Interaction magnitude, pharmacokinetics and pharmacodynamics of ticlopidine in relation to CYP2C19 genotypic status.
Ieiri, I; Irie, S; Ishizaki, T; Kimura, M; Otsubo, K; Urae, A, 2005
)
0.33
" Pharmacokinetic parameters calculated included the area under the curve (AUC(0-infinity)), peak plasma concentration (Cmax), time of peak plasma concentration (Tmax), and terminal half-life (t(1/2))."( Pharmacokinetics of oral omeprazole in llamas.
Davis, JL; Papich, MG; Poulsen, KP; Smith, GW, 2005
)
0.63
"There were some differences for the area under the plasma concentration-time curve (AUC), the elimination half-life (t(1/2 ke)) and the maximum plasma concentration (c(max)) in the three groups."( Pharmacokinetics of three proton pump inhibitors in Chinese subjects in relation to the CYP2C19 genotype.
Gao, N; Guo, YZ; Hu, YR; Jia, LJ; Qiao, HL; Tian, X; Zhang, LR, 2006
)
0.33
"The pharmacokinetic characteristics of the three PPIs are significantly dependent on the CYP2C19 genotype status."( Pharmacokinetics of three proton pump inhibitors in Chinese subjects in relation to the CYP2C19 genotype.
Gao, N; Guo, YZ; Hu, YR; Jia, LJ; Qiao, HL; Tian, X; Zhang, LR, 2006
)
0.33
" Cmax and AUC increased linearly between 10 to 80 mg."( Pharmacokinetics of tenatoprazole, a newly synthesized proton pump inhibitor, in healthy male Caucasian volunteers.
Barré, J; Domagala, F; Ficheux, H; Houin, G, 2006
)
0.33
"01) in heterozygous EMs, and significantly prolonged the elimination half-life of rabeprazole and rabeprazole thioether in homozygous EMs and in heterozygous EMs, whereas no difference in any pharmacokinetic parameters was found in PMs."( Different effects of fluvoxamine on rabeprazole pharmacokinetics in relation to CYP2C19 genotype status.
Shimizu, M; Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2006
)
0.33
" This method was suitable for use in pharmacokinetic studies in human volunteers, and provides a useful tool for measuring CYP2C19 activity."( Sensitive determination of omeprazole and its two main metabolites in human plasma by column-switching high-performance liquid chromatography: application to pharmacokinetic study in relation to CYP2C19 genotypes.
Niioka, T; Shimizu, M; Sugawara, K; Takahata, T; Tateishi, T; Uno, T; Yaui-Furukori, N, 2006
)
0.63
" The present study was conducted to evaluate pharmacokinetic parameters of omeprazole after a single dose in healthy Jordanian Arabic subjects and to compare the results with data published for other populations."( Possible interethnic differences in omeprazole pharmacokinetics : comparison of Jordanian Arabs with other populations.
Shilbayeh, S; Tutunji, MF, 2006
)
0.84
" Omeprazole pharmacokinetic parameters were determined from the plasma concentration-time profiles using the WinNonlin software."( Possible interethnic differences in omeprazole pharmacokinetics : comparison of Jordanian Arabs with other populations.
Shilbayeh, S; Tutunji, MF, 2006
)
1.52
"The mean pharmacokinetic parameters and their corresponding coefficient of variation (CV%) for peak plasma concentration (Cmax), AUC from time zero to infinity (AUCinfinity), time to reach Cmax (tmax), apparent oral clearance (CL/F) and elimination half-life (t(1/2)) were 314."( Possible interethnic differences in omeprazole pharmacokinetics : comparison of Jordanian Arabs with other populations.
Shilbayeh, S; Tutunji, MF, 2006
)
0.61
"The current pharmacokinetic study revealed that the majority of the Jordanian Arabics seemed to be more properly classified within the EM phenotype."( Possible interethnic differences in omeprazole pharmacokinetics : comparison of Jordanian Arabs with other populations.
Shilbayeh, S; Tutunji, MF, 2006
)
0.61
" Serial plasma samples were collected for 12-h pharmacokinetic profiles of saquinavir and ritonavir on days 10 and 15 and safety analysis on days 1, 4, 10, 15 and 29."( Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers.
Back, D; Boffito, M; Fletcher, C; Gazzard, B; Pozniak, AL; Robinson, L; Schutz, M; Tolowinska, I; Unsworth, J; Winston, A, 2006
)
0.74
" No significant changes were observed in saquinavir elimination half life, ritonavir pharmacokinetic parameters or in safety laboratory tests."( Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers.
Back, D; Boffito, M; Fletcher, C; Gazzard, B; Pozniak, AL; Robinson, L; Schutz, M; Tolowinska, I; Unsworth, J; Winston, A, 2006
)
0.74
"To evaluate the pharmacodynamic effect, efficacy, and safety of omeprazole 10 mg and 20 mg once daily in patients with nonerosive reflux disease (NERD) in Japan."( The pharmacodynamic effect of omeprazole 10 mg and 20 mg once daily in patients with nonerosive reflux disease in Japan.
Aoshima, M; Asahina, K; Ashida, K; Haruma, K; Hirayama, M; Inoue, S; Kabemura, T; Kato, M; Kinoshita, Y; Kiyama, S; Kobayashi, T; Kurosawa, S; Kuwayama, H; Matsumoto, K; Shimatani, T; Suzuki, H; Suzuki, J; Yamamoto, M, 2006
)
0.86
" An open-label, randomized, crossover, phase I, pharmacokinetic interaction design was used."( Lack of pharmacokinetic interaction between omeprazole or lansoprazole and ivabradine in healthy volunteers: an open-label, randomized, crossover, pharmacokinetic interaction clinical trial.
Calvo, A; Gorostiaga, C; Laredo, L; Moreno, A; Portolés, A; Resplandy, G; Terleira, A, 2006
)
0.59
" This method developed can be easily applied to the pharmacokinetic study of tenatoprazole in dog plasma after oral administration of an enteric-coated capsule."( HPLC determination and pharmacokinetic study of tenatoprazole in dog plasma after oral administration of enteric-coated capsule.
Li, F; Liu, P; Lu, X; Qin, F; Sun, B, 2007
)
0.34
"02 ng/ml) and paricalcitol pharmacokinetic parameters were estimated using non-compartmental methods."( Effect of omeprazole on the pharmacokinetics of paricalcitol in healthy subjects.
Awni, W; Chan, J; Chira, T; Galitz, L; Palaparthy, R; Pradhan, RS; Rieser, M; Williams, LA, 2007
)
0.74
" Hence, it could be expected that some pharmacokinetic parameters of omeprazole might change in PCM rats and partially restore to control levels in PCMC rats."( Effects of cysteine on the pharmacokinetic parameters of omeprazole in rats with protein-calorie malnutrition: partial restoration of some parameters to control levels by oral cysteine supplementation.
Lee, DY; Lee, I; Lee, MG,
)
0.61
"The following pharmacokinetic parameters were changed in PCM rats and partially returned to control levels in PCMC rats: the area under the plasma concentration-time curve (AUC; 387, 762, and 539 microg min/mL for control, PCM, and PCMC rats, respectively, after intravenous [IV] administration, and the corresponding values after oral administration: 115, 304, and 201 microg min/mL), total body clearance (51."( Effects of cysteine on the pharmacokinetic parameters of omeprazole in rats with protein-calorie malnutrition: partial restoration of some parameters to control levels by oral cysteine supplementation.
Lee, DY; Lee, I; Lee, MG,
)
0.38
"PCM was associated with significant changes in some omeprazole pharmacokinetics and the pharmacokinetic parameters restored to control levels by oral cysteine."( Effects of cysteine on the pharmacokinetic parameters of omeprazole in rats with protein-calorie malnutrition: partial restoration of some parameters to control levels by oral cysteine supplementation.
Lee, DY; Lee, I; Lee, MG,
)
0.63
"Darunavir (DRV; TMC114; Prezista) is a human immunodeficiency virus (HIV) protease inhibitor used in combination with low-dose ritonavir (RTV) (DRV/r) as a pharmacokinetic enhancer."( Pharmacokinetic interaction between darunavir boosted with ritonavir and omeprazole or ranitidine in human immunodeficiency virus-negative healthy volunteers.
De Marez, T; De Paepe, E; De Pauw, M; Hoetelmans, RM; Lefebvre, E; Parys, W; Sekar, VJ, 2007
)
0.57
" This validated method is simple and repeatable enough to be used in pharmacokinetic studies."( Quantification of tenatoprazole in rat plasma by HPLC: validation and its application to pharmacokinetic studies.
Bhyrapuneni, G; Kandikere, V; Mudigonda, K; Nirogi, R, 2007
)
0.34
" However, for maleate salt, with the exception of an increase in t(1/2), no pharmacokinetic parameters were significantly changed."( Influence of omeprazole on pharmacokinetics of domperidone given as free base and maleate salt in healthy Chinese patients.
Chen, XY; Dai, XJ; Liu, QZ; Yu, HL; Zhang, YF; Zhang, YN; Zhong, DF, 2007
)
0.71
"A prospective, open-label, single-site, two-period, crossover pharmacokinetic study was carried out in healthy volunteers."( Steady-state pharmacokinetics of once-daily fosamprenavir/ritonavir and atazanavir/ritonavir alone and in combination with 20 mg omeprazole in healthy volunteers.
Brower, R; Frank, I; Kim, D; Luber, AD; Peloquin, CA; Silverman, R, 2007
)
0.54
" OMP reduced ATV exposure [area under the concentration curve at 0-24 h (AUC0-24 h)] and the minimum drug concentration (Cmin) by 27% each."( Steady-state pharmacokinetics of once-daily fosamprenavir/ritonavir and atazanavir/ritonavir alone and in combination with 20 mg omeprazole in healthy volunteers.
Brower, R; Frank, I; Kim, D; Luber, AD; Peloquin, CA; Silverman, R, 2007
)
0.54
"The pharmacodynamic effects of OPZ and its pharmacokinetics depend on the CYP2C19 genotype status in Chinese people."( Effects of CYP2C19 genetic polymorphism on the pharmacokinetics and pharmacodynamics of omeprazole in Chinese people.
Hu, XP; Hu, YM; Mei, Q; Xu, JM; Xu, XH, 2007
)
0.56
"In a single-dose pharmacokinetic study, 17 healthy White volunteers genotyped as either CYP2C19*17/*17 or CYP2C19*1/*1 received an oral dose of 40 mg of omeprazole."( Increased omeprazole metabolism in carriers of the CYP2C19*17 allele; a pharmacokinetic study in healthy volunteers.
Baldwin, RM; Bertilsson, L; Eliasson, E; Ingelman-Sundberg, M; Mwinyi, J; Ohlsson, S; Pedersen, RS, 2008
)
0.95
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"Previous studies reported omeprazole to be an inhibitor of cytochrome P450 (CYP) 2C19 and suggested the pharmacokinetic interaction of omeprazole with R-warfarin."( The role of cytochrome P2C19 in R-warfarin pharmacokinetics and its interaction with omeprazole.
Sugawara, K; Sugimoto, K; Tateishi, T; Uno, T, 2008
)
0.87
" Serial plasma samples were collected; and the pharmacokinetic behavior of each enantiomer was characterized using a sequential achiral and chiral liquid chromatographic method."( Determination of tenatoprazole enantiomers and their enantioselective pharmacokinetics in rats.
Guan, J; Li, F; Li, J; Li, X; Yang, J, 2009
)
0.35
" This novel method has been applied to a pharmacokinetic study of OPZ in humans."( Highly sensitive method for the determination of omeprazole in human plasma by liquid chromatography-electrospray ionization tandem mass spectrometry: application to a clinical pharmacokinetic study.
Bharathi, DV; Ganneboina, R; Hotha, KK; Layek, B; Mullangi, R; Trivedi, RK; Vittal, S, 2009
)
0.61
"Several pharmacokinetic (PK) parameters were determined from the plasma samples, and data from reference and test formulations in the plasma were represented such as AUC0-t (1,223."( Pharmacokinetics and bioequivalence of 20 mg omeprazole capsule in 24 healthy Korean male volunteers.
Hwang, KG; Kang, JS; Kim, YS; Lee, MH; Lee, YS; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2009
)
0.61
" The aim of the study is to assess the relative bioavailability and pharmacokinetic properties of two oral formulations of 20 mg omeprazole tablet, namely LOSEC(R) as reference product and Losectil DR as test product using serum data."( Relative bioavailability and pharmacokinetic study of omeprazole 20 mg enteric-coated tablet in healthy Bangladeshi volunteers.
Abul Kalam Azad, M; Hasan, A; Hasnat, A; Mahbub Latif, AH; Ullah, MA, 2009
)
0.81
" The pharmacokinetic parameters were determined by a non-compartmental method."( Relative bioavailability and pharmacokinetic study of omeprazole 20 mg enteric-coated tablet in healthy Bangladeshi volunteers.
Abul Kalam Azad, M; Hasan, A; Hasnat, A; Mahbub Latif, AH; Ullah, MA, 2009
)
0.6
" No statistically significant differences were observed between two formulations by analyzing different pharmacokinetic parameters in terms of period, sequence and formulation."( Relative bioavailability and pharmacokinetic study of omeprazole 20 mg enteric-coated tablet in healthy Bangladeshi volunteers.
Abul Kalam Azad, M; Hasan, A; Hasnat, A; Mahbub Latif, AH; Ullah, MA, 2009
)
0.6
" The developed assay method was applied to a pharmacokinetic study in human volunteers."( Simultaneous estimation of four proton pump inhibitors--lansoprazole, omeprazole, pantoprazole and rabeprazole: development of a novel generic HPLC-UV method and its application to clinical pharmacokinetic study.
Bharathi, DV; Chatki, PK; Hotha, KK; Jagadeesh, B; Mullangi, R; Naidu, A; Thriveni, K, 2009
)
0.59
"This open-label, crossover, pharmacokinetic drug-drug interaction study was conducted at seven institutions in the US and Europe between January 2005 and August 2006."( Effect of the cytochrome P450 2C19 inhibitor omeprazole on the pharmacokinetics and safety profile of bortezomib in patients with advanced solid tumours, non-Hodgkin's lymphoma or multiple myeloma.
Acharya, M; Britten, CD; Chan, K; Cohen, N; Dudov, A; Fuloria, J; Gabrail, N; Nemunaitis, J; Quinn, DI; Yee, L, 2009
)
0.61
" Bortezomib pharmacokinetic parameters were similar when bortezomib was administered alone or with omeprazole (maximum plasma concentration 120 vs 123 ng/mL; area under the plasma concentration-time curve from 0 to 72 hours 129 vs 135 ng ."( Effect of the cytochrome P450 2C19 inhibitor omeprazole on the pharmacokinetics and safety profile of bortezomib in patients with advanced solid tumours, non-Hodgkin's lymphoma or multiple myeloma.
Acharya, M; Britten, CD; Chan, K; Cohen, N; Dudov, A; Fuloria, J; Gabrail, N; Nemunaitis, J; Quinn, DI; Yee, L, 2009
)
0.83
" The aim of the study is to assess the bioequivalence and pharmacokinetic properties of two oral formulations of 20 mg omeprazole capsule, the reference product and Omep-20 as test product using serum data."( Bioequivalence and pharmacokinetic study of two different omeprazole capsule formulations in healthy Bangladeshi volunteers.
Azad, MA; Hasan, A; Hasnat, A; Islam, SM; Joti, JJ; Nahar, K; Ullah, MA, 2009
)
0.81
" The half-life of omeprazole was also increased after both acute and chronic administration of soybean."( Effect of soybean administration on the pharmacokinetics of carbamazepine and omeprazole in rats.
Asad, M; Singh, D, 2010
)
0.92
" Additionally, the in vivo pharmacokinetic characterization of the chosen compounds was not hampered by the reduction of calibration standards (from n = 8 to n = 3)."( Influence of number of calibration standards within a defined range on pharmacokinetic disposition-case studies with omeprazole and clopidogrel carboxylic acid.
D'Souza, HJ; Kristjansson, F; Kumar, A; Pai, B; Shekar, R; Srinivas, NR, 2010
)
0.57
"97), or half-life (13."( Effect of a proton pump inhibitor on the pharmacokinetics of imatinib.
Appleman, LR; Beumer, JH; Christner, SM; Egorin, MJ; Komazec, KA; Miller, BM; Redner, RL; Shah, DD; Yerk, MA, 2009
)
0.35
" Blood samples were collected predose and 0 to 96 hours postdose for pharmacokinetic analysis."( Effects of omeprazole on the pharmacokinetic profiles of lisdexamfetamine dimesylate and extended-release mixed amphetamine salts in adults.
Buckwalter, M; Ermer, JC; Haffey, MB; Homolka, R; Lasseter, KC; Martin, P; Zhang, P, 2009
)
0.74
" h/mL, for Cmax and AUCinf, respectively."( Effects of omeprazole on the pharmacokinetic profiles of lisdexamfetamine dimesylate and extended-release mixed amphetamine salts in adults.
Buckwalter, M; Ermer, JC; Haffey, MB; Homolka, R; Lasseter, KC; Martin, P; Zhang, P, 2009
)
0.74
" However, approximately 50% of subjects receiving MAS XR showed an earlier Tmax while on omeprazole, indicating unpredictable release of active drug by the second bead of MAS XR, most likely related to reduced stomach acid while on a PPI compromising the pulsed delivery of MAS XR."( Effects of omeprazole on the pharmacokinetic profiles of lisdexamfetamine dimesylate and extended-release mixed amphetamine salts in adults.
Buckwalter, M; Ermer, JC; Haffey, MB; Homolka, R; Lasseter, KC; Martin, P; Zhang, P, 2009
)
0.96
" Pharmacokinetic profile was less variable for immediate compared with delayed-release omeprazole."( Pharmacokinetic profile of immediate-release omeprazole in patients with gastro-oesophageal reflux associated with gastroparesis.
Eversmann, J; Mann, S; Wo, JM, 2010
)
0.84
"Immediate-release omeprazole was associated with a more rapid absorption and less variable pharmacokinetic profile compared with delayed-release omeprazole in reflux patients associated with gastroparesis."( Pharmacokinetic profile of immediate-release omeprazole in patients with gastro-oesophageal reflux associated with gastroparesis.
Eversmann, J; Mann, S; Wo, JM, 2010
)
0.95
"There were authentic distinctions between the groups of healthy volunteers and patients with a peptic ulcer disease in Cmax, Tmax, AUC(0-t), AUC(0-infinity), CIt, Vd of omeprazole and Cmax of esomeprazole (Nexium, AstraZeneca)."( [Omeprazol and ezomeprazol pharmacokinetics, duration of antisecretory effect, and reasons for their probable changes in duodenal ulcer].
Dobrovol'skiĭ, OV; Kondratenko, SN; Pisarev, VV; Serebrova, SIu; Starodubtsev, AK; Vasilenko, GF, 2009
)
0.55
" This assay was successfully applied to a pharmacokinetic omeprazole study in children with cerebral palsy and mental retardation."( A bio-analytical hydrophilic interaction LC-MS/MS method for the simultaneous quantification of omeprazole and lansoprazole in human plasma in support of a pharmacokinetic omeprazole study in children.
Boussery, K; De Cock, P; De Paepe, P; De Smet, J; Remon, JP; Van Bocxlaer, J; Van Winckel, M, 2010
)
0.82
" Different pharmacokinetic parameters for both drugs were determined using non-compartmental method."( Interaction study between levofloxacin and omeprazole using urinary pharmacokinetic data.
Azad, MA; Faruquee, CF; Hasnat, A; Parveen, S; Rayhan, I; Ullah, A, 2010
)
0.62
"After a single dose, both the area under the plasma concentration-time curve (AUC) and peak concentration (C(max)) were higher in PMs than in EMs."( Influence of CYP2C19 on the relationship between pharmacokinetics and intragastric pH of omeprazole administered by successive intravenous infusions in Chinese healthy volunteers.
Li, Z; Meng, L; Ou, N; Shi, R; Wang, M; Wang, Y; Yuan, H; Zhang, H, 2010
)
0.58
" It has been suggested that staggering administration of clopidogrel and omeprazole may overcome this pharmacodynamic (PD) interaction."( Pharmacodynamic effects of concomitant versus staggered clopidogrel and omeprazole intake: results of a prospective randomized crossover study.
Angiolillo, DJ; Bass, TA; Capodanno, D; Charlton, RK; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Ueno, M, 2010
)
0.82
" The pharmacokinetic parameters were estimated using previously developed barrier-limited and space-distributed models."( Liver fibrosis impairs hepatic pharmacokinetics of liver transplant drugs in the rat model.
Asadian, P; Crawford, DH; Fletcher, LM; Khlentzos, AM; Li, P; Liu, X; Roberts, MS; Robertson, TA; Thorling, CA; Zou, YH, 2010
)
0.36
" Pharmacokinetic analyses were performed on day 1 without sorafenib and day 28 after steady-state sorafenib exposure; sorafenib pharmacokinetics were evaluated on day 28."( Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study.
Flaherty, KT; Frye, RF; Lathia, C; O'Dwyer, PJ; Redlinger, M; Rosen, M; Schuchter, L, 2011
)
0.37
" The present method was successfully applied to a chiral pharmacokinetic study of omeprazole in human volunteers with different CYP2C19 genotypes."( Chiral assay of omeprazole and metabolites and its application to a pharmacokinetics related to CYP2C19 genotypes.
Shiohira, H; Tateishi, T; Uno, T; Yasui-Furukori, N, 2011
)
0.94
" These observations support the investigation of potential pharmacokinetic and pharmacodynamic interactions between PPIs and anticoagulants."( Effect of multiple doses of omeprazole on the pharmacokinetics, pharmacodynamics, and safety of a single dose of rivaroxaban.
Ariyawansa, J; Burton, PB; Moore, KT; Plotnikov, AN; Thyssen, A; Vaccaro, N, 2011
)
0.66
" In conclusion, omeprazole did not affect the pharmacokinetic profile of vinpocetine."( Omeprazole does not change the oral bioavailability or pharmacokinetics of vinpocetine in rats.
Karaźniewicz-Łada, M; Kiełbowicz, G; Ksiądzyna, D; Magdalan, J; Merwid-Ląd, A; Sozański, T; Szeląg, A; Szumny, A; Słupski, W; Trocha, M, 2011
)
2.16
" Pharmacokinetic profiling of orally dosed DPG or DPG with 60% loading of FA (DPG/FA60) was carried out in omeprazole-treated rats as a hypochlorhydric model."( Improved dissolution and pharmacokinetic behavior of dipyridamole formulation with microenvironmental pH-modifier under hypochlorhydria.
Inoue, R; Kawabata, Y; Onoue, S; Taniguchi, C; Wada, K; Yamada, S; Yamashita, K; Yamauchi, Y, 2012
)
0.59
" Pharmacodynamic end-points were vasodilator-stimulated phosphoprotein P2Y(12) platelet reactivity index, maximal platelet aggregation to 5 and 20 μmol/l adenosine diphosphate, and VerifyNow P2Y12 platelet response units."( A randomized, 2-period, crossover design study to assess the effects of dexlansoprazole, lansoprazole, esomeprazole, and omeprazole on the steady-state pharmacokinetics and pharmacodynamics of clopidogrel in healthy volunteers.
Bhatt, DL; Brooks, JK; Frelinger, AL; Lee, RD; Michelson, AD; Mulford, DJ; Nigam, A; Nudurupati, S; Wu, J, 2012
)
0.59
"Pharmacokinetic and pharmacodynamic responses with omeprazole demonstrated assay sensitivity."( A randomized, 2-period, crossover design study to assess the effects of dexlansoprazole, lansoprazole, esomeprazole, and omeprazole on the steady-state pharmacokinetics and pharmacodynamics of clopidogrel in healthy volunteers.
Bhatt, DL; Brooks, JK; Frelinger, AL; Lee, RD; Michelson, AD; Mulford, DJ; Nigam, A; Nudurupati, S; Wu, J, 2012
)
0.84
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
" The present study was conducted to evaluate the pharmacokinetic parameters of omeprazole after a single oral administration to a random Iranian population."( Variation in omeprazole pharmacokinetics in a random Iranian population: a pilot study.
Keyhanfar, F; Kobarfard, F; Motevalian, M; Noubarani, M, 2012
)
0.98
" Plasma samples obtained, up to 24 hr after dosing, from four male and four female Microminipigs were analyzed by liquid chromatography tandem mass spectrometry to estimate typical pharmacokinetic parameters for each analyte."( Simultaneous pharmacokinetics assessment of caffeine, warfarin, omeprazole, metoprolol, and midazolam intravenously or orally administered to Microminipigs.
Iwasaki, K; Izumi, H; Kusumoto, S; Mogi, M; Murayama, N; Shimizu, M; Takehara, H; Toda, A; Utoh, M; Yamazaki, H, 2012
)
0.62
"We conducted a pharmacokinetic (PK) study and a pharmacodynamic (PD) study to assess whether Roux-en-Y gastric bypass (RYGB) surgery is associated with significant changes to PK and PD of oral medications."( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients.
Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013
)
0.39
" Compared with controls, the RYGB group had brisk natriuresis, with significantly lower tmax for urine sodium (1."( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients.
Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013
)
0.39
"RYGB recipients have significantly shorter tmax for the studied orally administered medications, but otherwise no other significant changes in PK were reported."( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients.
Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013
)
0.39
"This study aimed to determine whether the PPI omeprazole influences the pharmacokinetic (PK) and pharmacodynamic (PD) behavior of ASA+ER-DP."( Pharmacokinetics and pharmacodynamics of the antiplatelet combination aspirin (acetylsalicylic acid) plus extended-release dipyridamole are not altered by coadministration with the potent CYP2C19 inhibitor omeprazole.
Brickl, R; Ehrlich, J; Eisert, W; Offman, E; Schobelock, MJ; VanderMaelen, CP, 2013
)
0.84
"The present study was conducted to describe the pharmacokinetic profile of immediate-release compound omeprazole capsule and compare it with the enteric-coated formulation under fasting and fed condition."( Pharmacokinetics of a new immediate-release compound omeprazole capsule and its comparison with the enteric-coated formulation under fasting and fed conditions.
Cao, X; Ding, L; Duan, H; Jiang, L; Liu, Z; Zhong, S, 2013
)
0.85
"This review provides an update on the following points: pharmacokinetic profile and metabolism of ilaprazole in relation to its pharmacodynamic properties; comparative data on the pharmacokinetics and pharmacodynamics of ilaprazole with currently available PPIs; and implications for studies on the therapeutic efficacy of ilaprazole in GERD."( The pharmacokinetics of ilaprazole for gastro-esophageal reflux treatment.
Blandizzi, C; de Bortoli, N; Giacchino, M; Marchi, S; Martinucci, I; Savarino, E; Savarino, V, 2013
)
0.39
"Different studies show that ilaprazole, a benzimidazole derivative, has an extended plasma half-life in comparison with all other approved PPIs."( The pharmacokinetics of ilaprazole for gastro-esophageal reflux treatment.
Blandizzi, C; de Bortoli, N; Giacchino, M; Marchi, S; Martinucci, I; Savarino, E; Savarino, V, 2013
)
0.39
" Clinical studies in healthy subjects were performed to evaluate potential pharmacokinetic interactions between vortioxetine (Lu AA21004) and co-administered agents, including fluconazole (cytochrome P450 [CYP] 2C9, CYP2C19 and CYP3A inhibitor), ketoconazole (CYP3A and P-glycoprotein inhibitor), rifampicin (CYP inducer), bupropion (CYP2D6 inhibitor and CYP2B6 substrate), ethinyl estradiol/levonorgestrel (CYP3A substrates) and omeprazole (CYP2C19 substrate and inhibitor)."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
0.55
", area under the plasma concentration-time curve [AUC] and maximum plasma concentration [C max]) was used to assess pharmacokinetic interactions."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
0.39
" DNV AUC0-∞, Cmax and C12h GMR% (90% CI) with ranitidine: 81."( Effect of meal and antisecretory agents on the pharmacokinetics of danoprevir/ritonavir in healthy volunteers.
Bech, N; Brennan, BJ; Morcos, PN; Moreira, SA; Navarro, MT; Quatkemeyer, A; Smith, PF, 2014
)
0.4
" The AUC0-24 and Cmax of active clopidogrel metabolite decreased with both omeprazole and rabeprazole, and conditions of bioequivalence were not met, except for AUC0-24 with rabeprazole."( Effects of rabeprazole on the antiplatelet effects and pharmacokinetics of clopidogrel in healthy volunteers.
Azizi, M; Ducint, D; Funck-Brentano, C; Gaussem, P; Molimard, M; Remones, V; Steichen, O; Szymezak, J, 2013
)
0.62
" However, under our experimental conditions and proton-pump inhibitor doses, there was no significant pharmacodynamic interaction between rabeprazole or omeprazole and clopidogrel, despite a significant decrease in the formation of clopidogrel active metabolite."( Effects of rabeprazole on the antiplatelet effects and pharmacokinetics of clopidogrel in healthy volunteers.
Azizi, M; Ducint, D; Funck-Brentano, C; Gaussem, P; Molimard, M; Remones, V; Steichen, O; Szymezak, J, 2013
)
0.59
"To develop a population pharmacokinetic model for intravenous omeprazole in critically ill children."( Population pharmacokinetics of omeprazole in critically ill pediatric patients.
Carrillo, A; Colom, H; González, R; López, J; López-Herce, J; Manzanares, C; Solana, MJ; Urbano, J, 2014
)
0.93
"The pharmacokinetic profile was best described by a 2-compartment model with a first-order elimination process."( Population pharmacokinetics of omeprazole in critically ill pediatric patients.
Carrillo, A; Colom, H; González, R; López, J; López-Herce, J; Manzanares, C; Solana, MJ; Urbano, J, 2014
)
0.69
"An allometric size model allows changes to be predicted in all the pharmacokinetic parameters, making dose adjustment by body weight important to achieve the most effective omeprazole exposure."( Population pharmacokinetics of omeprazole in critically ill pediatric patients.
Carrillo, A; Colom, H; González, R; López, J; López-Herce, J; Manzanares, C; Solana, MJ; Urbano, J, 2014
)
0.88
" A single oral dose, open-label, non-controlled, pharmacokinetic study of omeprazole was conducted in healthy young/premenopausal females (n = 16)."( Pharmacokinetics of omeprazole and its metabolites in three phases of menstrual cycle.
Ahmad, L; Iqbal, Z; Nasir, F; Nazir, S; Shah, Y, 2015
)
0.97
"This phase I, randomized, open-label, two-way crossover trial evaluated the pharmacokinetic effects of lacosamide and omeprazole coadministration."( Pharmacokinetics of lacosamide and omeprazole coadministration in healthy volunteers: results from a phase I, randomized, crossover trial.
Cawello, W; Fichtner, A; Mueller-Voessing, C, 2014
)
0.89
" Area under the concentration-time curve (AUC) and peak concentration (C(max)) were the primary pharmacokinetic parameters measured for lacosamide or omeprazole administered alone (reference) or in combination (test)."( Pharmacokinetics of lacosamide and omeprazole coadministration in healthy volunteers: results from a phase I, randomized, crossover trial.
Cawello, W; Fichtner, A; Mueller-Voessing, C, 2014
)
0.88
"The objective of this study is to develop a physiologically-based pharmacokinetic (PBPK) model for each omeprazole enantiomer that accounts for nonlinear PK of the two enantiomers as well as omeprazole racemic drug."( Predicting nonlinear pharmacokinetics of omeprazole enantiomers and racemic drug using physiologically based pharmacokinetic modeling and simulation: application to predict drug/genetic interactions.
Bashaw, ED; Gaohua, L; Huang, SM; Jamei, M; Lee, SC; Wu, F; Zhao, P, 2014
)
0.88
" Pharmacokinetic effects were estimated by measuring active metabolite of clopidogrel, and pharmacodynamic effects by inhibition of adenosine diphosphate (ADP)-induced platelet aggregation."( Effect of esomeprazole with/without acetylsalicylic acid, omeprazole and lansoprazole on pharmacokinetics and pharmacodynamics of clopidogrel in healthy volunteers.
Andersson, T; Galbraith, H; Nagy, P; Niazi, M; Nylander, S; Ranjan, S; Wallentin, L, 2014
)
0.78
" The purpose of the study was to investigate the pharmacokinetic of four probe drugs in adriamycin (ADR)-induced nephropathy rat."( Pharmacokinetic of four probe drugs in adriamycin-induced nephropathy rat.
Chen, WH; Chen, ZB; Hu, LF; Li, D; Lin, FY; Yu, XG; Zhi, AY, 2014
)
0.4
"To evaluate felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions (PK-DDIs) involving cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp)."( Evaluation of felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions.
Doogue, MP; Miners, JO; Polasek, TM; Rowland, A; Snyder, BD, 2014
)
0.4
" Vandetanib + digoxin increased digoxin area under the concentration-time curve from zero to the last quantifiable concentration (AUC0-last) and Cmax by 23 and 29 %, respectively, versus digoxin alone, with only a 9 % decrease in CLR."( Pharmacokinetic evaluations of the co-administrations of vandetanib and metformin, digoxin, midazolam, omeprazole or ranitidine.
Johansson, S; Leese, PT; Li, Y; Lisbon, E; Martin, P; Mathews, D; Oliver, S; Read, J; Steinberg, M, 2014
)
0.62
" No significant differences were present between the ECO-Fasted and ECO-Fed groups with regards to bioavailability, Cmax , Tmax or AUC0-∞ ."( Pharmacokinetics of intravenous, plain oral and enteric-coated oral omeprazole in the horse.
McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2015
)
0.65
"The aim of this study was to evaluate the effect of coadministration of acid-reducing agents on the pharmacokinetic exposure of orally administered epidermal growth factor receptor inhibitor erlotinib, a drug that displays pH-dependent solubility."( Effect of gastric pH on erlotinib pharmacokinetics in healthy individuals: omeprazole and ranitidine.
Abt, M; Ducray, PS; Giraudon, M; Hamilton, M; Kletzl, H; Lum, BL, 2015
)
0.65
"The objectives of this study were to investigate the impact of formulation (enteric coated and buffered) and feeding on pharmacokinetic variables associated with the oral administration of omeprazole in the horse."( The effect of feeding on the pharmacokinetic variables of two commercially available formulations of omeprazole.
McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2015
)
0.82
" The metabolism of these drugs by CYP1A2, CYP2C19 and CYP3A4 was evaluated by the calculation of bioavailabilities and of intrinsic clearances using a pharmacokinetic (PK) model."( Investigation of omeprazole and phenacetin first-pass metabolism in humans using a microscale bioreactor and pharmacokinetic models.
Bois, F; Bricks, T; Fleury, MJ; Hamon, J; Herpe, YE; Jellali, R; Leclerc, E; Merlier, F; Regimbeau, JM; Seyer, A, 2015
)
0.76
" Pharmacokinetic parameters were assessed for up to 48 hours after administration of the investigational product."( A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults.
Corcoran, M; Hoppenbrouwers, M; Hossack, S; Martin, P; Pierce, D; Velinova, M, 2015
)
0.67
" The pharmacokinetic parameters of revexepride were similar without or with omeprazole co-administration."( A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults.
Corcoran, M; Hoppenbrouwers, M; Hossack, S; Martin, P; Pierce, D; Velinova, M, 2015
)
0.9
" Published pharmacokinetic data of omeprazole after intravenous or oral administration in Caucasian, Chinese, and Japanese were used for the evaluation."( Evaluating a physiologically based pharmacokinetic model for prediction of omeprazole clearance and assessing ethnic sensitivity in CYP2C19 metabolic pathway.
Cleary, Y; Feng, S; Hu, P; Parrott, N; Shi, J; Wang, Y; Weber, C; Yin, OQ, 2015
)
0.92
" Blood samples for pharmacokinetic analysis were collected pre-dose and serially for 72 h post-dose."( Lisdexamfetamine Dimesylate Effects on the Pharmacokinetics of Cytochrome P450 Substrates in Healthy Adults in an Open-Label, Randomized, Crossover Study.
Corcoran, M; Ermer, J; Martin, P, 2015
)
0.42
"The advances in pharmaceutical development and drug discovery impose the availability of reliable high-throughput screening methods for the rapid evaluation of drug metabolism and pharmacokinetic (PK) in biological samples."( Development and validation of a DESI-HRMS/MS method for the fast profiling of esomeprazole and its metabolites in rat plasma: a pharmacokinetic study.
Barocelli, E; Bettini, R; Castrati, L; Colombo, P; Elviri, L; Flammini, L; Rossi, A, 2016
)
0.66
" No significant differences were present between three of the formulations and the reference formulation, while the fourth formulation had a lower Cmax and longer Tmax than the reference formulation."( Pharmacokinetics and bioequivalence testing of five commercial formulations of omeprazole in the horse.
Greer, R; McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2016
)
0.66
" Plasma concentrations of slowly eliminated caffeine and R-/S-warfarin and rapidly eliminated omeprazole and midazolam previously observed in cynomolgus monkeys were scaled to human oral biomonitoring equivalents using known species allometric scaling factors and in vitro metabolic clearance data with a simple physiologically based pharmacokinetic (PBPK) model."( Human plasma concentrations of cytochrome P450 probes extrapolated from pharmacokinetics in cynomolgus monkeys using physiologically based pharmacokinetic modeling.
Murayama, N; Shida, S; Shimizu, M; Uno, Y; Utoh, M; Yamazaki, H, 2015
)
0.64
" There was a 37% decrease in Cmax and a 16% decrease in AUC (0-∞) following administration of danirixin in the presence of food."( The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects.
Bloomer, JC; Carpenter, DC; Connolly, P; Cooray, H; Lazaar, AL; Miller, BE; Mistry, S; Smart, K; Tal-Singer, R, 2015
)
0.42
" However, its pharmacokinetic and chemical instability does not allow simple aqueous dosage form formulation synthesis for therapy of, especially child, these patients."( Pharmacokinetic Comparison of Omeprazole Granule and Suspension Forms in Children: A Randomized, Parallel Pilot Trial.
Dehghanzadeh, G; Haghighat, M; Karami, S; Mirzaei, R; Rahimi, HR, 2016
)
0.72
"The pharmacokinetics of cytochrome P450 probes in humans can be extrapolated from corresponding data in cynomolgus monkeys using simplified physiologically based pharmacokinetic (PBPK) modeling."( Human plasma concentrations of five cytochrome P450 probes extrapolated from pharmacokinetics in dogs and minipigs using physiologically based pharmacokinetic modeling.
Shida, S; Yamazaki, H, 2016
)
0.43
"For SA, Tmax significantly decreased after RYGB, while both Cmax and AUC0-24 significantly increased."( The Effect of Roux-en-Y Gastric Bypass Surgery in Morbidly Obese Patients on Pharmacokinetics of (Acetyl)Salicylic Acid and Omeprazole: the ERY-PAO Study.
Mitrov-Winkelmolen, L; Overdiek, HWPM; Swank, DJ; Touw, DJ; van Buul-Gast, MW; van Schaik, RHN, 2016
)
0.64
" The pharmacokinetic data of cytochrome P450 probes in humans can be extrapolated from corresponding data in cynomolgus monkeys, dogs and minipigs using simplified physiologically based pharmacokinetic (PBPK) modeling."( Human plasma concentrations of cytochrome P450 probe cocktails extrapolated from pharmacokinetics in mice transplanted with human hepatocytes and from pharmacokinetics in common marmosets using physiologically based pharmacokinetic modeling.
Kawano, M; Mitsui, M; Sasaki, E; Shimizu, M; Suemizu, H; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2016
)
0.43
" Based on clearance of CYP isoform-specific substrates at the microsomal level (CLM), microsomal protein per gram of liver (MPPGL), liver weight, hepatic blood flow, hepatic clearance values (CLH) for 10 CYPs in HCC patients (n=102) were extrapolated using a predictive bottom-up pharmacokinetic model."( Changes in cytochrome P450s-mediated drug clearance in patients with hepatocellular carcinoma in vitro and in vivo: a bottom-up approach.
Fang, Y; Gao, J; Gao, N; He, XP; Jia, LJ; Jin, H; Qiao, HL; Tian, X; Wen, Q; Zhang, YF; Zhou, J, 2016
)
0.43
" Here, we assessed the potential for pharmacokinetic drug-drug interaction of LCZ696 (400 mg, single dose or once daily [q."( Pharmacokinetic drug-drug interaction assessment of LCZ696 (an angiotensin receptor neprilysin inhibitor) with omeprazole, metformin or levonorgestrel-ethinyl estradiol in healthy subjects.
Akahori, M; Dahlke, M; Gan, L; Jiang, X; Langenickel, T; Mendonza, A; Neelakantham, S; Nguyen, J; Pal, P; Rajman, I; Rebello, S; Reynolds, C; Sunkara, G; Swan, T; Zhou, W, 2016
)
0.65
" Blood and urine samples were collected on days 6 and 12 to evaluate rotigotine pharmacokinetic parameters alone and in the presence of omeprazole."( No influence of the CYP2C19-selective inhibitor omeprazole on the pharmacokinetics of the dopamine receptor agonist rotigotine.
Andreas, JO; Braun, M; Cawello, W; Elshoff, JP, 2014
)
0.86
" It was fully validated and applied to a pharmacokinetic study after per os administration of 20mg tablet formulations of omeprazole."( Study of the effect of CYP2C19 polymorphisms on omeprazole pharmacokinetics by utilizing validated LC-MS/MS and Real Time-PCR methods.
Chatzidaki, M; Dotsikas, Y; Koukoula, M; Loukas, YL; Molou, E; Schulpis, KH; Thodi, G; Triantafylli, O, 2017
)
0.92
"We report a case of Pisa syndrome (PS) due to the acetylcholinesterase inhibitor donepezil which may have been precipitated by pharmacokinetic interactions with commonly used medications."( Pisa syndrome due to donepezil: pharmacokinetic interactions to blame?
Cunningham, E; McGuinness, B; Passmore, AP; Pollock, D, 2017
)
0.46
"To compare pharmacokinetic and pharmacodynamic effects of a novel omeprazole formulation against a currently registered product."( Pharmacokinetic and pharmacodynamic effects of two omeprazole formulations on stomach pH and gastric ulcer scores.
Andrews, FM; Nielsen, SG; Raidal, SL; Trope, G, 2017
)
0.94
" The mean hepatic clearances determined by in silico fitting for individual pharmacokinetic models of warfarin and midazolam in the aged group were, respectively, 23% and 56% smaller than those for the young group."( Effects of aging and rifampicin pretreatment on the pharmacokinetics of human cytochrome P450 probes caffeine, warfarin, omeprazole, metoprolol and midazolam in common marmosets genotyped for cytochrome P450 2C19.
Inoue, T; Kusama, T; Mogi, M; Sasaki, E; Shimizu, M; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2018
)
0.69
" To expand and verify this modeling procedure, simulations of R/S-omeprazole and R/S-warfarin clearances after oral administrations in individual marmosets were performed using individual simplified physiologically based pharmacokinetic (PBPK) modeling consisting of gut, liver and central compartments."( Association with polymorphic marmoset cytochrome P450 2C19 of in vivo hepatic clearances of chirally separated R-omeprazole and S-warfarin using individual marmoset physiologically based pharmacokinetic models.
Inoue, T; Kusama, T; Sasaki, E; Shimizu, M; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2018
)
0.93
" Combining epidemiological studies with pharmacokinetic modeling, we detected and evaluated high-dimensional DDIs among 30 frequent drugs."( Translational High-Dimensional Drug Interaction Discovery and Validation Using Health Record Databases and Pharmacokinetics Models.
Chiang, CW; Li, L; Ning, X; Quinney, SK; Shen, L; Wang, L; Wang, X; Zhang, P; Zhang, S, 2018
)
0.48
"Searching for pharmacokinetic interaction studies between clopidogrel and omeprazole in humans was performed in PubMed."( A pharmacokinetic model of drug-drug interaction between clopidogrel and omeprazole at CYP2C19 in humans.
Lohitnavy, M; Lohitnavy, O; Morasuk, T; Tangamornsuksan, W; Thiansupornpong, P, 2017
)
0.92
"Our clopidogrel-omeprazole pharmacokinetic interaction model with a description of competitive inhibition at CYP2C19 could successfully describe concentration-time courses from the selected datasets."( A pharmacokinetic model of drug-drug interaction between clopidogrel and omeprazole at CYP2C19 in humans.
Lohitnavy, M; Lohitnavy, O; Morasuk, T; Tangamornsuksan, W; Thiansupornpong, P, 2017
)
1.03
" There were no significant differences in the pharmacokinetic parameters of caffeine, omeprazole, metoprolol, chlorzoxazone, and midazolam between the SGI-pretreated and control groups."( Influence of Shenxiong Glucose Injection on the Activities of Six CYP Isozymes and Metabolism of Warfarin in Rats Assessed Using Probe Cocktail and Pharmacokinetic Approaches.
Gong, Z; Huang, J; Li, Y; Liu, C; Liu, T; Lu, Y; Pan, J; Sun, J; Wang, Y; Zheng, J; Zheng, L, 2017
)
0.68
" Blood samples were collected at prespecified time points for pharmacokinetic analyses."( The Effect of Food or Omeprazole on the Pharmacokinetics of Osimertinib in Patients With Non-Small-Cell Lung Cancer and in Healthy Volunteers.
Bui, K; Cassier, PA; Dickinson, PA; Greystoke, A; Lisbon, E; Moreno, V; Plummer, R; So, K; Thomas, K; Vishwanathan, K; Weilert, D; Yap, TA, 2018
)
0.8
" The present study aimed to develop a novel amorphous solid dispersion (ASD) of CAR with acidic counter ions for pH modifications in microenvironment to improve the pharmacokinetic properties under hypochlorhydric conditions."( Amorphous solid dispersions of carvedilol along with pH-modifiers improved pharmacokinetic properties under hypochlorhydoria.
Halder, S; Onoue, S; Sato, H; Seto, Y; Tabata, A, 2018
)
0.48
"A single-center, randomized, open-label, parallel-group trial investigated pharmacokinetic interactions of oral semaglutide with omeprazole (40 mg once-daily) in 54 healthy subjects."( A randomized study investigating the effect of omeprazole on the pharmacokinetics of oral semaglutide.
Breitschaft, A; Bækdal, TA; Hansen, CW; Navarria, A, 2018
)
0.94
"An in vitro-in vivo (IVIV) pharmacokinetic model of itraconazole and hydroxyitraconazole was developed including data from an omeprazole interaction study with SUBA itraconazole."( Mechanistic Assessment of the Effect of Omeprazole on the In Vivo Pharmacokinetics of Itraconazole in Healthy Volunteers.
Abuhelwa, AY; Foster, DJR; Mudge, S; Upton, RN, 2019
)
0.99
"A physiologically based pharmacokinetic (PBPK) model was used to simulate the impact of elevated levels of interleukin (IL)-6 on the exposure of several orally administered cytochrome P450 (CYP) probe substrates (caffeine, S-warfarin, omeprazole, dextromethorphan, midazolam, and simvastatin)."( Simulating the Impact of Elevated Levels of Interleukin-6 on the Pharmacokinetics of Various CYP450 Substrates in Patients with Neuromyelitis Optica or Neuromyelitis Optica Spectrum Disorders in Different Ethnic Populations.
Ducray, PS; Endo-Tsukude, C; Gardner, I; Gill, KL; Hatley, OJ; Machavaram, KK; Parrott, N; Terao, K, 2019
)
0.7
" Pharmacokinetic analyses of the CYP2C19 probe drug, omeprazole, were performed before and after rifampicin or fluvoxamine administration."( Effect of co-administered inducer or inhibitor on omeprazole pharmacokinetics based on CYP2C19 genotype.
Hakamata, A; Inui, N; Kamiya, C; Miyakawa, S; Namiki, N; Odagiri, K; Tanaka, S; Uchida, S; Watanabe, H, 2019
)
1.02
"Physiologically based pharmacokinetic (PBPK) modelling and simulation is a useful tool in predicting the PK profiles of a drug, assessing the effects of covariates such as demographics, ethnicity, genetic polymorphisms and disease status on the PK, and evaluating the potential of drug-drug interactions."( Development of a Korean-specific virtual population for physiologically based pharmacokinetic modelling and simulation.
Chung, JY; Hatley, O; Kim, Y; Lee, H; Lee, HA; Rhee, SJ; Yi, S; Yoon, S; Yu, KS, 2019
)
0.51
" The purpose of this study is to apply a physiologically based pharmacokinetic (PBPK) modeling approach to investigate the DDI mechanism for an immediate release formulation of nifedipine with omeprazole."( Physiologically Based Pharmacokinetic Modeling Approach to Identify the Drug-Drug Interaction Mechanism of Nifedipine and a Proton Pump Inhibitor, Omeprazole.
Babiskin, A; Le Merdy, M; Lee, SC; Ni, Z; Sun, D; Tan, ML; Zhao, L, 2021
)
1.01
"A prospective, blinded randomized interventional study was trial, conducted in 3 parts: (a) bioavailability study, (b) dose titration study, and (c) comparative clinical pharmacodynamic study, each using a blocked crossover design."( Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses.
Edwards, S; Hughes, KJ; Jacobson, GA; Narkowicz, CK; Raidal, SL; Wise, JC, 2021
)
0.86
"Consistent with the larger dose administered, Cmax (median, 1032 ng/mL; range, 576-1766) and AUC0-24 (median, 63."( Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses.
Edwards, S; Hughes, KJ; Jacobson, GA; Narkowicz, CK; Raidal, SL; Wise, JC, 2021
)
0.86
"For decades, inflammation has been considered a cause of pharmacokinetic variability, mainly in relation to the inhibitory effect of pro-inflammatory cytokines on the expression level and activity of cytochrome P450 (CYP)."( Modeling Approach to Predict the Impact of Inflammation on the Pharmacokinetics of CYP2C19 and CYP3A4 Substrates.
Chenel, M; Gautier-Veyret, E; Payen, L; Simon, F; Stanke-Labesque, F; Tod, M; Truffot, A, 2021
)
0.62
"Changes in pharmacokinetic profiles and parameters induced by inflammation seem to be captured accurately by the models."( Modeling Approach to Predict the Impact of Inflammation on the Pharmacokinetics of CYP2C19 and CYP3A4 Substrates.
Chenel, M; Gautier-Veyret, E; Payen, L; Simon, F; Stanke-Labesque, F; Tod, M; Truffot, A, 2021
)
0.62
" Coadministration of OM with omeprazole was not associated with any clinically significant pharmacokinetic drug interactions."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Omeprazole, a Proton Pump Inhibitor, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Sohn, W; Terminello, B; Trivedi, A; Zhang, H, 2022
)
1.25
"The aim of this work is the development of a mechanistic physiologically-based pharmacokinetic (PBPK) model using in vitro to in vivo extrapolation to conduct a drug-drug interaction (DDI) assessment of treosulfan against two cytochrome p450 (CYP) isoenzymes and P-glycoprotein (P-gp) substrates."( Evaluation of the drug-drug interaction potential of treosulfan using a physiologically-based pharmacokinetic modelling approach.
Balazki, P; Baumgart, J; Beelen, DW; Böhm, S; Hemmelmann, C; Hilger, RA; Martins, FS; Ring, A; Schaller, S, 2022
)
0.72
" However, considering the comprehensive treosulfan-based conditioning treatment schedule and the respective pharmacokinetic properties of the concomitantly used drugs (eg, half-life), the potential for interaction on all evaluated mechanisms would be low (AUCR < 1."( Evaluation of the drug-drug interaction potential of treosulfan using a physiologically-based pharmacokinetic modelling approach.
Balazki, P; Baumgart, J; Beelen, DW; Böhm, S; Hemmelmann, C; Hilger, RA; Martins, FS; Ring, A; Schaller, S, 2022
)
0.72
" In this study, a physiologically-based pharmacokinetic (PBPK) model was developed to assess CYPs mediated therapeutic protein drug interactions (TP-DIs) in patients with immune-mediated inflammatory diseases (IMIDs) with elevated systemic IL-6 levels when treated by anti-IL-6 therapies."( Utilization of physiologically-based pharmacokinetic model to assess disease-mediated therapeutic protein-disease-drug interaction in immune-mediated inflammatory diseases.
Chen, Y; Miao, X; Wang, L; Zhou, H; Zhou, W, 2022
)
0.72
" The aim of our study was to develop a physiologically based pharmacokinetic (PBPK) model to foresee the impact of elevated IL-6 levels in combination with drug interactions with esomeprazole on CYP3A and CYP2C19."( Prediction of cytochromes P450 3A and 2C19 modulation by both inflammation and drug interactions using physiologically based pharmacokinetics.
Daali, Y; Desmeules, JA; Lenoir, C; Niederer, A; Rollason, V; Samer, CF, 2022
)
0.91
" The principal aim was to evaluate whether gastric bypass surgery modifies the bioavailability and pharmacokinetic (PK) parameters of omeprazole."( Effect of Obesity and Roux-En-Y Gastric Surgery on Omeprazole Pharmacokinetics.
Bandrés, F; Castrillón, EV; Chicharro, LM; López-Picado, A; Moreno Lopera, C; Paterna, ABR; Portolés-Pérez, A; Rubio, MA; Sánchez Pernaute, A; Torres García, AJ, 2022
)
1.18
" Cmax and AUC corrected by dose/body weight were significantly different between the baseline surgery subjects and controls."( Effect of Obesity and Roux-En-Y Gastric Surgery on Omeprazole Pharmacokinetics.
Bandrés, F; Castrillón, EV; Chicharro, LM; López-Picado, A; Moreno Lopera, C; Paterna, ABR; Portolés-Pérez, A; Rubio, MA; Sánchez Pernaute, A; Torres García, AJ, 2022
)
0.97
" The drug dissolution and the gastrointestinal tract pH conditions are likely to influence the in vivo pharmacokinetic behavior of LTD tablets."( Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug-Drug Interaction.
Li, X; Wang, W; Wang, Y; Wu, W; Xu, Q; Zhang, J; Zhang, T; Zhang, Y, 2021
)
0.82
" Pharmacokinetic results showed in the fasting state the three LTD tablets were equivalent in beagles in terms of effective components."( Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug-Drug Interaction.
Li, X; Wang, W; Wang, Y; Wu, W; Xu, Q; Zhang, J; Zhang, T; Zhang, Y, 2021
)
0.82
" The aim of this study was to develop a physiologically based pharmacokinetic (PBPK) model to mechanistically describe absorption of immediate release capsule formulation of acalabrutinib in humans."( Physiologically Based Absorption Modelling to Explore the Formulation and Gastric pH Changes on the Pharmacokinetics of Acalabrutinib.
Chen, B; Pepin, X; Sharma, S; Tang, W; Zhou, D, 2023
)
0.91
" Omeprazole is the most common option utilized for acid-related disorders ; however, the pharmacokinetic (PK) and dosing recommendations for the obese patient population are lacking."( Population pharmacokinetics of omeprazole in obese and normal-weight adults.
Chen, K; Deng, C; Ding, J; Lin, Y; Luo, P; Pei, Q; Yang, G; Zhu, L; Zhu, S, 2022
)
1.92
" Although some studies have explored the roles of gut microbiota and host Cyp450s in drug pharmacokinetics, few have explored their effects on pharmacokinetic variability, especially in disease states."( Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug.
Chen, LJ; Chen, XP; Chen, Y; Guo, J; Liou, YL; Tan, ZR; Xu, Y; Zhang, SX; Zhang, W; Zhou, HH, 2022
)
0.72
"In this study, we aim to investigate the effects of gut microbiota and host Cyp450s on pharmacokinetic variability in mice with non-alcoholic steatohepatitis (NASH), and to elucidate the contribution of gut microbiota and host Cyp450s to pharmacokinetic variability in this setting."( Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug.
Chen, LJ; Chen, XP; Chen, Y; Guo, J; Liou, YL; Tan, ZR; Xu, Y; Zhang, SX; Zhang, W; Zhou, HH, 2022
)
0.72
"The pharmacokinetic variability of mice with NASH was explored under intragastric and intravenous administrations of a cocktail mixture of omeprazole, phenacetin, midazolam, tolbutamide, chlorzoxazone, and metoprolol, after which the results were compared with those obtained from the control group."( Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug.
Chen, LJ; Chen, XP; Chen, Y; Guo, J; Liou, YL; Tan, ZR; Xu, Y; Zhang, SX; Zhang, W; Zhou, HH, 2022
)
0.92
" The pharmacokinetic variabilities of phenacetin, midazolam, omeprazole, and chlorzoxazone were mainly associated with decreased elimination activity in the gut microbiota."( Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug.
Chen, LJ; Chen, XP; Chen, Y; Guo, J; Liou, YL; Tan, ZR; Xu, Y; Zhang, SX; Zhang, W; Zhou, HH, 2022
)
0.96
"Gut microbiota and host Cyp450s co-contribute to the pharmacokinetic variability in mice with NASH, and the degree of contribution varies from drug to drug."( Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug.
Chen, LJ; Chen, XP; Chen, Y; Guo, J; Liou, YL; Tan, ZR; Xu, Y; Zhang, SX; Zhang, W; Zhou, HH, 2022
)
0.72
" A noncompartmental method was used to calculate pharmacokinetic parameters, and 47 subjects were divided into two groups based on the calculation of the median age."( Development of a particle swarm optimization-backpropagation artificial neural network model and effects of age and gender on pharmacokinetics study of omeprazole enteric-coated tablets in Chinese population.
Chen, J; Hu, Y; Jiang, B; Lou, H; Ruan, Z; Xu, Y; Yang, D, 2022
)
0.92
" This study aimed to build a physiologically based pharmacokinetic (PBPK) model reflecting observed changes in physiological and molecular parameters relevant to drug disposition that are associated with MAFLD."( A Physiologically Based Pharmacokinetic Model to Predict the Impact of Metabolic Changes Associated with Metabolic Associated Fatty Liver Disease on Drug Exposure.
Newman, EM; Rowland, A, 2022
)
0.72
" Pharmacokinetic characteristics of probe drugs were subsequently assessed in a Phase I, open-label, single-sequence crossover study in healthy male participants."( Pharmacokinetic-Interactions of BI 425809, a Novel Glycine Transporter 1 Inhibitor, With Cytochrome P450 and P-Glycoprotein Substrates: Findings From In Vitro Analyses and an Open-Label, Single-Sequence Phase I Study.
Chan, T; Desch, M; Hohl, K; Ishiguro, N; Keller, S; Liesenfeld, KH; Müller, F; Schlecker, C; Wind, S; Wunderlich, G,
)
0.13
" With BI 425809, area under the plasma concentration curve from administration to the last measurement (AUC 0-tz ) and maximum plasma concentration ( Cmax ) for midazolam were lower than when administered alone."( Pharmacokinetic-Interactions of BI 425809, a Novel Glycine Transporter 1 Inhibitor, With Cytochrome P450 and P-Glycoprotein Substrates: Findings From In Vitro Analyses and an Open-Label, Single-Sequence Phase I Study.
Chan, T; Desch, M; Hohl, K; Ishiguro, N; Keller, S; Liesenfeld, KH; Müller, F; Schlecker, C; Wind, S; Wunderlich, G,
)
0.13
"To compare intragastric rifabutin concentrations between low-dose rifabutin (50 mg three time daily; as in RHB-105) and generically dosed rifabutin 150 mg once daily, 150 mg twice daily, and 300 mg once daily using a validated Physiologically-based pharmacokinetic (PBPK) model."( Physiologically-based pharmacokinetic modelling to predict intragastric rifabutin concentrations in the treatment of Helicobacter pylori infection.
Almenoff, JS; Howden, CW; Offman, E; Pendse, SN; Shah, S; Sheldon, KL, 2023
)
0.91
"We obtained plasma pharmacokinetic data from the RHB-105 clinical development programs and used it to develop and validate a whole-body PBPK model using PK-SIM software."( Physiologically-based pharmacokinetic modelling to predict intragastric rifabutin concentrations in the treatment of Helicobacter pylori infection.
Almenoff, JS; Howden, CW; Offman, E; Pendse, SN; Shah, S; Sheldon, KL, 2023
)
0.91
"The successful establishment of this PBPK-PD model highlights that pharmacokinetic and pharmacodynamic profiles of drugs can be predicted using preclinical data."( Prediction of Omeprazole Pharmacokinetics and its Inhibition on Gastric Acid Secretion in Humans Using Physiologically Based Pharmacokinetic-Pharmacodynamic Model Characterizing CYP2C19 Polymorphisms.
Jiang, L; Li, S; Liu, L; Liu, X; Xie, L; Yang, H; Yang, L; Yang, Y; Zhi, H, 2023
)
1.27
" After cocktail alone or in combination with adavosertib administration, 24-h pharmacokinetic sampling occurred for probe substrates and their respective metabolites paraxanthine, 5-hydroxyomeprazole (5-HO), and 1'-hydroxymidazolam (1'-HM)."( Phase I study to assess the effect of adavosertib (AZD1775) on the pharmacokinetics of substrates of CYP1A2, CYP2C19, and CYP3A in patients with advanced solid tumors.
Ah-See, ML; Edenfield, WJ; Lewis, LD; Li, Y; Mugundu, GM; Nadeau, L; Någård, M; Ottesen, LH; Safran, HP; Strauss, J; Wise-Draper, T, 2023
)
1.1
" We investigated potential effects of comedication on pharmacokinetic exposure of nifedipine ER products with different formulation designs and manufacturing processes."( Effect of Omeprazole Administration on the Pharmacokinetics of Oral Extended-Release Nifedipine in Healthy Subjects.
Feng, K; Kinjo, M; Lionberger, R; Sun, D; Tan, ML; Wang, H; Xu, M; Zhao, L, 2023
)
1.31

Compound-Compound Interactions

Omeprazole contains a benzimidazole moiety and thus has the potential to interact with the cytochrome P-450 enzyme group. The overall effect of lansoprazole combined with antibiotics in the treatment of Hp positive gastric ulcer in the elderly is better than that of omeprazoles combined with antidepressants.

ExcerptReferenceRelevance
"The effect of a proton pump inhibitor, omeprazole (OPZ), in combination with mouse epidermal growth factor (EGF), on the healing of chronic gastric ulcers induced by acetic acid in submandibular glands removed rats (SMR rat) was investigated."( [Effect of proton pump inhibitor, in combination with epidermal growth factor, on the healing of chronic gastric ulcer in submandibular gland removed rats].
Imai, S; Itoh, M; Joh, T; Takeuchi, T; Yokoyama, Y, 1992
)
0.55
" Omeprazole contains a benzimidazole moiety and thus has the potential to interact with the cytochrome P-450 enzyme group."( Clinical implications of drug interactions with the cytochrome P-450 enzyme system associated with omeprazole.
Humphries, TJ, 1991
)
1.41
" This suggests that further stimulation of ulcer healing may be expected if EGF is given with an acid-suppressive agent or with an agent allowing EGF to remain in rat gastric lumen at high concentrations."( Effect of epidermal growth factor in combination with sucralfate or omeprazole on the healing of chronic gastric ulcers in the rat.
Endoh, K; Imai, S; Itoh, M; Iwai, A; Joh, T; Kawai, T; Matsusako, K; Takeuchi, T; Yasue, N; Yokoyama, Y, 1990
)
0.51
"To establish the efficacy of omeprazole combined with two antibiotics for Helicobacter pylori eradication and duodenal ulcer relapse."( Efficacy of omeprazole combined with antibiotics for Helicobacter pylori eradication and duodenal ulcer recurrence.
Bargiggia, S; Bianchi Porro, G; Lazzaroni, M; Maconi, G; Minguzzi, M, 1995
)
0.96
"Serum gastrin levels in 44 peptic ulcer patients (26 gastric ulcer patients and 18 duodenal ulcer patients) were determined after they had been treated with omeprazole (OPZ) (20 mg/day) alone or in combination with pirenzepine (PZP) (100 mg/day)."( Serum gastrin levels following administration of omeprazole alone or in combination with pirenzepine.
Arakawa, Y; Ito, K; Iwasaki, A; Kawamura, Y; Matsuo, Y; Miyazawa, K; Sakai, Y; Tashiro, Y, 1994
)
0.74
" Different mechanisms have to be considered as causes for potential drug-drug interactions."( Lack of pantoprazole drug interactions in man.
Bliesath, H; Hartmann, M; Huber, R; Radtke, HW; Steinijans, VW; Wurst, W; Zech, K, 1994
)
0.29
" A number of studies have now been undertaken using an acid inhibitor in combination with two antibiotics."( Eradication of Helicobacter pylori: omeprazole in combination with antibiotics.
Axon, AT; Moayyedi, P, 1996
)
0.57
" Various mechanisms have to be considered as causes for potential drug-drug interactions."( Lack of pantoprazole drug interactions in man: an updated review.
Bliesath, H; Hartmann, M; Huber, R; Radtke, HW; Steinijans, VW; Wurst, W; Zech, K, 1996
)
0.29
" Various mechanisms have to be considered as causes for potential drug-drug interactions."( Lack of pantoprazole drug interactions in man: an updated review.
Bliesath, H; Hartmann, M; Huber, R; Radtke, HW; Steinijans, VW; Wurst, W; Zech, K, 1996
)
0.29
" In conclusion, H pylori eradication rates using high dose ranitidine plus amoxycillin and metronidazole may be similar to that of low dose omeprazole in combination with the same antibiotics for omeprazole with clarithromycin."( Randomised controlled trial of ranitidine versus omeprazole in combination with antibiotics for eradication of Helicobacter pylori.
Bamford, KB; Collins, JS; Molloy, C; Sloan, JM; Tham, TC; Watson, RG, 1996
)
0.75
"An agar dilution checkerboard method was used to evaluate the in vitro activity of omeprazole combined with clarithromycin, amoxicillin, and ceftibuten, respectively, against clinical isolates of Helicobacter pylori."( In vitro activity of omeprazole in combination with several antimicrobial agents against clinical isolates of Helicobacter pylori.
Alarcón, T; Díaz de Rojas, F; Domingo, D; López-Brea, M; Sánchez, I, 1996
)
0.84
" The aim of this study was to evaluate rabeprazole in combination with antibiotics for the eradication of Helicobacter pylori (H."( Safety and efficacy of rabeprazole in combination with four antibiotic regimens for the eradication of Helicobacter pylori in patients with chronic gastritis with or without peptic ulceration.
Atherton, JC; Cockayne, A; Hawkey, CJ; Jenkins, D; Knifton, A; Stack, WA; Thirlwell, D, 1998
)
0.3
"To evaluate the efficacy of polaprezinc, a mucosal protective agent, in combination with a 7-day triple therapy containing lansoprazole, amoxycillin and clarithromycin, as a treatment for Helicobacter pylori."( Polaprezinc, a mucosal protective agent, in combination with lansoprazole, amoxycillin and clarithromycin increases the cure rate of Helicobacter pylori infection.
Hassan, M; Ikezawa, K; Kashimura, H; Mutoh, H; Nakahara, A; Sawahata, T; Suzuki, K; Tanaka, N; Watanabe, T, 1999
)
0.3
" Thus, it is important to understand the potential for clinically significant drug-drug interactions in this setting."( Review article: drug interactions with agents used to treat acid-related diseases.
Humphries, TJ; Merritt, GJ, 1999
)
0.3
" This study assessed the comparative frequency of potential drug-drug interactions in patients receiving either omeprazole or lansoprazole."( Prevalence of potential proton-pump inhibitor drug interactions: a retrospective review of prescriptions in community pharmacies.
Fask, A; Saltiel, E, 1999
)
0.51
"The effect of omeprazole, a clinically used proton pump inhibitor, alone or in combination with clarithromycin was evaluated against Mycobacterium avium, Mycobacterium intracellulare and Mycobacterium tuberculosis, using a human alveolar macrophage model of infection."( Effect of proton pump inhibitor alone or in combination with clarithromycin on mycobacterial growth in human alveolar macrophages.
Amitani, R; Matsumoto, H; Niimi, A; Suzuki, K; Tanaka, E; Tsuyuguchi, K, 2000
)
0.67
" The aim of this study was to determine the optimal dose and duration of lansoprazole (LA) administration in combination with amoxicillin (AMPC) and metronidazole (MNZ)."( Eradication of Helicobacter pylori using 30 mg or 60 mg lansoprazole combined with amoxicillin and metronidazole: one and two weeks of a new triple therapy.
Asaka, M; Ishizuka, J; Kagaya, H; Katagiri, M; Kato, M; Komatsu, Y; Kudo, M; Kudo, T; Nishikawa, K; Sugiyama, T; Sukegawa, M; Takeda, H; Toyota, J, 1999
)
0.3
" Time-kill curve assays of RPZ, when combined with amoxicillin, clarithromycin, or metronidazole, disclosed that synergistic effects were demonstrated in combination with each antibiotic examined."( In vitro activities of rabeprazole, a novel proton pump inhibitor, and its thioether derivative alone and in combination with other antimicrobials against recent clinical isolates of Helicobacter pylori.
Akahane, T; Gotoh, A; Katsuyama, T; Kawakami, Y; Oana, K; Okabe, T; Okimura, Y; Takahashi, Y; Yamaguchi, M, 2000
)
0.31
" The aim of this prospective study was to assess the efficacy of argon plasma coagulation in combination with high-dose omeprazole therapy to ablate nondysplastic Barrett's epithelium."( Ablation of Barrett's epithelium by endoscopic argon plasma coagulation in combination with high-dose omeprazole.
Antos, D; Bayerdörffer, E; Miehlke, S; Schentke, KU; Schulz, H; Stolte, M; Vieth, M, 2000
)
0.73
"In 73 patients with histologically confirmed Barrett's epithelium, argon plasma coagulation was used in combination with maximal acid suppression (omeprazole 40 mg three times a day)."( Ablation of Barrett's epithelium by endoscopic argon plasma coagulation in combination with high-dose omeprazole.
Antos, D; Bayerdörffer, E; Miehlke, S; Schentke, KU; Schulz, H; Stolte, M; Vieth, M, 2000
)
0.72
"In our experience, argon plasma coagulation in combination with high-dose omeprazole treatment is an effective and safe technique for complete ablation of nondysplastic Barrett's epithelium."( Ablation of Barrett's epithelium by endoscopic argon plasma coagulation in combination with high-dose omeprazole.
Antos, D; Bayerdörffer, E; Miehlke, S; Schentke, KU; Schulz, H; Stolte, M; Vieth, M, 2000
)
0.75
"The primary objective of the present study was to evaluate the efficacy of 30 and 60 mg of lansoprazole administered in combination with two antibiotics for 7 or 10 days in eradicating Helicobacter pylori in duodenal ulcer patients."( [Treatment of Helicobacter pylori infection with lansoprazole 30 mg or 60 mg combined with two antibiotics for duodenal ulcers].
Joubert-Collin, M; Lamouliatte, H; Perie, F, 2000
)
0.31
" This study is designed to determine the efficacy of omeprazole 20 mg bd in combination with amoxycillin 500 mg tid (Group A), amoxycillin 750 mg tds (Group B) and clarithromycin 500 mg tid (Group C) in Singapore."( A randomised trial of amoxycillin versus clarithromycin in combination with omeprazole for eradication of Helicobacter pylori infection in Singapore.
Fock, KM; Law, NM; Lim, CC; Ng, HS; Ng, TM, 2000
)
0.79
" This is a multicenter trial defining the efficacy and safety of multipolar electrocoagulation combined with high-dose acid inhibition."( Effective and safe endoscopic reversal of nondysplastic Barrett's esophagus with thermal electrocoagulation combined with high-dose acid inhibition: a multicenter study.
Faigel, D; Fennerty, MB; Ippoliti, A; Lewin, K; Lieberman, D; Sampliner, RE; Weinstein, WM, 2001
)
0.31
" PPIs may interact with other drugs through numerous mechanisms."( Proton pump inhibitors and their drug interactions: an evidence-based approach.
Gerson, LB; Triadafilopoulos, G, 2001
)
0.31
" No studies have yet compared the effects of different dosages of clarithromycin in combination with a proton pump inhibitor and amoxicillin in elderly patients."( Cure of Helicobacter pylori infection in elderly patients: comparison of low versus high doses of clarithromycin in combination with amoxicillin and pantoprazole.
Bozzola, L; Di Mario, F; Franceschi, M; Leandro, G; Pilotto, A; Rassu, M; Soffiati, G; Valerio, G, 2001
)
0.31
") in combination with pantoprazole and amoxicillin in elderly patients."( Cure of Helicobacter pylori infection in elderly patients: comparison of low versus high doses of clarithromycin in combination with amoxicillin and pantoprazole.
Bozzola, L; Di Mario, F; Franceschi, M; Leandro, G; Pilotto, A; Rassu, M; Soffiati, G; Valerio, G, 2001
)
0.31
" Altered absorption or metabolism are 2 of the major mechanisms for drug-drug interactions."( Drug interaction studies with esomeprazole, the (S)-isomer of omeprazole.
Andersson, T; Hassan-Alin, M; Hasselgren, G; Röhss, K, 2001
)
0.59
" pylori status on the incidence of gastrointestinal (GI) events in rheumatic patients receiving longterm conventional nonsteroidal antiinflammatory drug (NSAID) therapy combined with omeprazole."( Influence of Helicobacter pylori eradication therapy on the occurrence of gastrointestinal events in patients treated with conventional nonsteroidal antiinflammatory drugs combined with omeprazole.
Bannwarth, B; Barthelemy, P; Caekaert, A; Dorval, E, 2002
)
0.7
" We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole, amoxicillin and clarithromycin for Helicobacter pylori infection."( Sofalcone, a mucoprotective agent, increases the cure rate of Helicobacter pylori infection when combined with rabeprazole, amoxicillin and clarithromycin.
Furusu, H; Inoue, K; Isomoto, H; Kohno, S; Ohnita, K; Wen, CY, 2005
)
0.33
"The addition of sofalcone, but not polaprezinc, significantly increased the cure rate of H pylori infection when combined with the rabeprazole-amoxicillin-clarithromycin regimen."( Sofalcone, a mucoprotective agent, increases the cure rate of Helicobacter pylori infection when combined with rabeprazole, amoxicillin and clarithromycin.
Furusu, H; Inoue, K; Isomoto, H; Kohno, S; Ohnita, K; Wen, CY, 2005
)
0.33
"To study the efficacy and safety of rabeprazole in peptic ulcer patients alone or combined with anti-Helicobacter pylori (Hp) agents."( [The clinical applications of rabeprazole either alone or combined with anti-Helicobacter pylori agents in peptic ulcer patients].
Lin, SR, 2005
)
0.33
"Whether labeprazole was used alone or combined with anti-Hp agents, it is an effective and safe therapy for the treatment of peptic ulcer."( [The clinical applications of rabeprazole either alone or combined with anti-Helicobacter pylori agents in peptic ulcer patients].
Lin, SR, 2005
)
0.33
" The aim of our study was to evaluate the effects of proton pump inhibitors alone or in combination with H2 receptor blockers on gastric acidity with 24-hour gastric pH monitoring."( The effect of rabeprazole alone or in combination with H2 receptor blocker on intragastric pH: a pilot study.
Bektaş, M; Cetinkaya, H; Ozden, A; Soykan, I; Törüner, M, 2004
)
0.32
" Although interactions based on the change of gastric pH are a group-specific effect and thus may occur with all proton pump inhibitors, individual proton pump inhibitors differ in their propensities to interact with other drugs and the extent to which their interaction profiles have been defined."( Pharmacokinetic drug interaction profiles of proton pump inhibitors.
Blume, H; Donath, F; Schug, BS; Warnke, A, 2006
)
0.33
" The purpose of this study was to determine the steady-state pharmacokinetics of once-daily (qd) fosamprenavir/ritonavir (FPV/r) and atazanavir/ritonavir (ATV/r) alone and in combination with 20 mg qd omeprazole (OMP) in healthy volunteers."( Steady-state pharmacokinetics of once-daily fosamprenavir/ritonavir and atazanavir/ritonavir alone and in combination with 20 mg omeprazole in healthy volunteers.
Brower, R; Frank, I; Kim, D; Luber, AD; Peloquin, CA; Silverman, R, 2007
)
0.73
"The effects of omeprazole on indinavir when administered alone or in combination with ritonavir were evaluated."( Effect of omeprazole on the plasma concentrations of indinavir when administered alone and in combination with ritonavir.
Donovan, BJ; Hollowell, SB; Kashuba, AD; Min, SS; Raasch, RH; Rezk, NL; Rublein, JC; Smith, PC; Tallman, MN; Tappouni, HL; Theodore, D; Tien, HC, 2008
)
1.1
" After seven days, the single-dose pharmacokinetic profile of an 800-mg dose of indinavir alone or in combination with 200 mg of ritonavir was evaluated."( Effect of omeprazole on the plasma concentrations of indinavir when administered alone and in combination with ritonavir.
Donovan, BJ; Hollowell, SB; Kashuba, AD; Min, SS; Raasch, RH; Rezk, NL; Rublein, JC; Smith, PC; Tallman, MN; Tappouni, HL; Theodore, D; Tien, HC, 2008
)
0.75
" The addition of 200 mg of ritonavir to 800 mg of indinavir in combination with 40 mg of omeprazole significantly increased the mean indinavir AUC from 30."( Effect of omeprazole on the plasma concentrations of indinavir when administered alone and in combination with ritonavir.
Donovan, BJ; Hollowell, SB; Kashuba, AD; Min, SS; Raasch, RH; Rezk, NL; Rublein, JC; Smith, PC; Tallman, MN; Tappouni, HL; Theodore, D; Tien, HC, 2008
)
0.97
" Proton pump inhibitors and H(2)-antagonists are frequently used in the HIV-negative-infected population, and drug-drug interactions have been described with other antiretrovirals."( A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in HIV-negative volunteers.
Bouche, MP; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Vanaken, H; Woodfall, B, 2008
)
0.57
" In situations in which both clopidogrel and a PPI are indicated, pantoprazole should be used since it is the PPI least likely to interact with clopidogrel."( Drug-drug interaction between clopidogrel and the proton pump inhibitors.
Mathews, KD; Norgard, NB; Wall, GC, 2009
)
0.35
"To review all currently published drug-drug interaction studies with the HIV-integrase inhibitor raltegravir."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
0.35
"A total of 14 drug-drug interaction studies were found."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
0.35
"Raltegravir is not without drug-drug interactions but due to the lack of an effect on CYP450 or UGT by raltegravir and the broad therapeutic range of raltegravir itself, this agent can safely combined with almost all tested agents."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
0.35
"To study the efficacy and side effects of furazolidone when given for 1 week in combination with bismuth subcitrate, amoxicillin, and omeprazole."( Short-duration furazolidone therapy in combination with amoxicillin, bismuth subcitrate, and omeprazole for eradication of Helicobacter pylori.
Hasan, SR; Reza, PM; Roham, SR; Vahid, V,
)
0.55
"One week of furazolidone in combination with 2 weeks of amoxicillin, omeprazole, and bismuth subcitrate is a safe and cost-effective regimen for the eradication of H pylori."( Short-duration furazolidone therapy in combination with amoxicillin, bismuth subcitrate, and omeprazole for eradication of Helicobacter pylori.
Hasan, SR; Reza, PM; Roham, SR; Vahid, V,
)
0.59
" The method is simple, rapid and rugged, and has been applied successfully to sample analysis in support of a drug-drug interaction study."( Simultaneous determination of tolbutamide, omeprazole, midazolam and dextromethorphan in human plasma by LC-MS/MS--a high throughput approach to evaluate drug-drug interactions.
Bertelsen, K; Guo, P; Han, F; Huang, MQ; Lin, ZJ; Weng, N; Zhang, W; Zhao, H, 2010
)
0.62
" Neither were there significant differences in the absolute nadir and percentage decrease of WBC and ANC, nor on the incidence and severity of neutropenia, febrile neutropenia, diarrhoea, nausea and vomiting when irinotecan was combined with omeprazole."( Effect of omeprazole on the pharmacokinetics and toxicities of irinotecan in cancer patients: a prospective cross-over drug-drug interaction study.
de Bruijn, P; de Jong, FA; Konings, IR; Lam, MH; Loos, WJ; Mathijssen, RH; van der Bol, JM; van Meerten, E; Verweij, J; Wiemer, EA, 2011
)
0.95
" In this article, the authors review the current studies that reported a possible drug-drug interaction between clopidogrel and PPIs, particularly omeprazole."( Clopidogrel and proton pump inhibitors: is there a significant drug-drug interaction?
Azab, AN; Friger, M; Gilutz, H; Shmulevich, E, 2011
)
0.57
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"The aim of this study was to evaluate the contribution of metabolites to drug-drug interactions (DDI) using the inhibition of CYP2C19 and CYP3A4 by omeprazole and its metabolites as a model."( Inhibition of CYP2C19 and CYP3A4 by omeprazole metabolites and their contribution to drug-drug interactions.
Davis, C; Isoherranen, N; Lutz, JD; Sager, JE; Shirasaka, Y, 2013
)
0.86
"The identification and quantification of potential drug-drug interactions is important for avoiding or minimizing the interaction-induced adverse events associated with specific drug combinations."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
0.39
" This observed discrepancy between in vitro risk assessment and in vivo drug-drug interaction (DDI) profile was rationalized by time-varying dynamic pharmacokinetic models that incorporated circulating concentrations of fluoxetine and norfluoxetine enantiomers, mutual inhibitor-inhibitor interactions, and CYP3A4 induction."( Fluoxetine- and norfluoxetine-mediated complex drug-drug interactions: in vitro to in vivo correlation of effects on CYP2D6, CYP2C19, and CYP3A4.
Davis, C; Foti, RS; Isoherranen, N; Kunze, KL; Lutz, JD; Sager, JE, 2014
)
0.4
"To evaluate the clinical effect of proton pump inhibitor-based triple therapy combined with Saccharomyces boulardii in the treatment of Helicobacter pylori (Hp) infection among children in terms of Hp eradication rate and incidence of adverse events."( [Clinical effect of triple therapy combined with Saccharomyces boulardii in the treatment of Helicobacter pylori infection in children].
Chen, ZY; Duan, BP; Ou-Yang, HJ; Tang, J; Xu, B; You, JY; Zhao, HM, 2014
)
0.4
"Triple therapy combined with Saccharomyces boulardii cannot significantly increase Hp eradication rate, but can significantly reduce the incidence of stomatitis, constipation, and diarrhea during treatment."( [Clinical effect of triple therapy combined with Saccharomyces boulardii in the treatment of Helicobacter pylori infection in children].
Chen, ZY; Duan, BP; Ou-Yang, HJ; Tang, J; Xu, B; You, JY; Zhao, HM, 2014
)
0.4
" Therefore, the potential pharmacokinetic drug-drug interactions between sucroferric oxyhydroxide and selected drugs commonly taken by dialysis patients were investigated."( Drug-drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects.
Chong, E; Kalia, V; Willsie, S; Winkle, P, 2014
)
0.63
"Systemic exposure based on AUC0-∞ for all drugs, and AUC0-24 for all drugs except omeprazole (for which AUC 0-8 h was measured), was unaffected to a clinically significant extent by the presence of sucroferric oxyhydroxide, irrespective of whether sucroferric oxyhydroxide was administered with the drug or 2 h earlier."( Drug-drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects.
Chong, E; Kalia, V; Willsie, S; Winkle, P, 2014
)
0.85
"There is a low risk of drug-drug interactions between sucroferric oxyhydroxide and losartan, furosemide, digoxin and warfarin."( Drug-drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects.
Chong, E; Kalia, V; Willsie, S; Winkle, P, 2014
)
0.63
"To evaluate felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions (PK-DDIs) involving cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp)."( Evaluation of felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions.
Doogue, MP; Miners, JO; Polasek, TM; Rowland, A; Snyder, BD, 2014
)
0.4
"To quantify the drug-drug interactions between dabigatran etexilate (DE) and proton pump inhibitors (PPI) and in particular the role of P-gp activity modulation."( In vitro and in vivo evaluation of drug-drug interaction between dabigatran and proton pump inhibitors.
Accassat, S; Basset, T; Bertoletti, L; Delavenne, X; Hodin, S; Mismetti, P; Ollier, E, 2015
)
0.42
"Many systematic reviews resulted in claims on drug-drug interactions (DDIs) with proton pump inhibitors (PPIs)."( Adverse drug reactions due to drug-drug interactions with proton pump inhibitors: assessment of systematic reviews with AMSTAR method.
Okuyan, B; Sancar, M; Yucel, A; Yucel, E, 2016
)
0.43
" To further validate this cocktail, in this study, we have verified whether probe drugs contained in the latter cause mutual drug-drug interactions."( Evaluation of Mutual Drug-Drug Interaction within Geneva Cocktail for Cytochrome P450 Phenotyping using Innovative Dried Blood Sampling Method.
Bosilkovska, M; Daali, Y; Déglon, J; Desmeules, J; Samer, C; Thomas, A; Walder, B, 2016
)
0.43
" Here, we assessed the potential for pharmacokinetic drug-drug interaction of LCZ696 (400 mg, single dose or once daily [q."( Pharmacokinetic drug-drug interaction assessment of LCZ696 (an angiotensin receptor neprilysin inhibitor) with omeprazole, metformin or levonorgestrel-ethinyl estradiol in healthy subjects.
Akahori, M; Dahlke, M; Gan, L; Jiang, X; Langenickel, T; Mendonza, A; Neelakantham, S; Nguyen, J; Pal, P; Rajman, I; Rebello, S; Reynolds, C; Sunkara, G; Swan, T; Zhou, W, 2016
)
0.65
" Drug-drug interactions between 2D (ombitasvir/paritaprevir/ritonavir) or 3D (ombitasvir/paritaprevir/ritonavir and dasabuvir) regimens and omeprazole, a CYP2C19 substrate and acid-reducing agent, were evaluated in 24 healthy volunteers."( Drug-Drug Interaction of Omeprazole With the HCV Direct-Acting Antiviral Agents Paritaprevir/Ritonavir and Ombitasvir With and Without Dasabuvir.
Awni, WM; Dutta, S; Hu, B; Menon, RM; Podsadecki, TJ; Polepally, AR, 2016
)
0.94
"The efficacy and safety of polaprezinc combined with triple therapy was compared with triple therapy alone in the eradication of Helicobacter pylori."( Polaprezinc combined with clarithromycin-based triple therapy for Helicobacter pylori-associated gastritis: A prospective, multicenter, randomized clinical trial.
Fang, JY; Ji, F; Li, JS; Li, YQ; Luo, HQ; Luo, HS; Lv, NH; Qian, JM; Ren, JL; Shi, RH; Tan, B; Xu, H; Zou, YY, 2017
)
0.46
"A microdose drug-drug interaction (DDI) study may be a valuable tool for anticipating drug interaction at therapeutic doses."( Drug-drug interaction of microdose and regular-dose omeprazole with a CYP2C19 inhibitor and inducer.
Bae, SH; Han, S; Park, GJ; Park, MH; Park, WS; Shin, SH; Shin, YG; Yim, DS, 2017
)
0.71
" Triple therapy group in combination with Curcumin significantly decreased all active, chronic and endoscopic inflammation scores of patients compared to the baseline and triple therapy group (P<0."( CURCUMIN IN COMBINATION WITH TRIPLE THERAPY REGIMES AMELIORATES OXIDATIVE STRESS AND HISTOPATHOLOGIC CHANGES IN CHRONIC GASTRITIS-ASSOCIATED HELICOBACTER PYLORI INFECTION.
Asadollahi, K; Feizi, J; Hafezi Ahmadi, MR; Judaki, A; Rahmani, A,
)
0.13
"This phase 1, open-label, crossover study sought to evaluate drug-drug interactions between tivantinib and cytochrome P450 (CYP) substrates and tivantinib and P-glycoprotein."( Evaluation of the pharmacokinetic drug interaction potential of tivantinib (ARQ 197) using cocktail probes in patients with advanced solid tumours.
Gajee, R; Papadopoulos, KP; Puzanov, I; Strickler, JH; Tachibana, M; Wang, Y; Zahir, H, 2018
)
0.48
"The data suggest that tivantinib 360 mg twice daily has either a minimal or no effect on the pharmacokinetics of probe drugs for CYP1A2, CYP2C9, CYP2C19 and CYP3A4 substrates, and decreases the systemic exposure of P-glycoprotein substrates when administered with tivantinib."( Evaluation of the pharmacokinetic drug interaction potential of tivantinib (ARQ 197) using cocktail probes in patients with advanced solid tumours.
Gajee, R; Papadopoulos, KP; Puzanov, I; Strickler, JH; Tachibana, M; Wang, Y; Zahir, H, 2018
)
0.48
"Polypharmacy increases the risk of drug-drug interactions (DDIs)."( Translational High-Dimensional Drug Interaction Discovery and Validation Using Health Record Databases and Pharmacokinetics Models.
Chiang, CW; Li, L; Ning, X; Quinney, SK; Shen, L; Wang, L; Wang, X; Zhang, P; Zhang, S, 2018
)
0.48
"We aimed to develop a mathematical model describing a drug-drug interaction between clopidogrel and omeprazole in humans."( A pharmacokinetic model of drug-drug interaction between clopidogrel and omeprazole at CYP2C19 in humans.
Lohitnavy, M; Lohitnavy, O; Morasuk, T; Tangamornsuksan, W; Thiansupornpong, P, 2017
)
0.9
"To evaluate the capacity for modafinil to be a perpetrator of metabolic drug-drug interactions by altering cytochrome P450 activity following a single dose and dosing to steady state."( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol.
Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018
)
0.48
"These data support consideration of the risk of clinically relevant metabolic drug-drug interactions perpetrated by modafinil when this drug is co-administered with drugs that are primarily cleared by CYP2C19 (single modafinil dose or steady state modafinil dosing) or CYP3A4 (steady state modafinil dosing only) catalysed metabolic pathways."( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol.
Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018
)
0.48
"To assess the efficacy and safety of omeprazole given with the new single capsule of bismuth, metronidazole and tetracycline (OBMT) compared with quadruple treatment consisting of omeprazole, bismuth, amoxicillin and clarithromycin (OBAC) for Helicobacter pylori eradication in duodenal ulcer patients."( New single capsule of bismuth, metronidazole and tetracycline given with omeprazole versus quadruple therapy consisting of bismuth, omeprazole, amoxicillin and clarithromycin for eradication of Helicobacter pylori in duodenal ulcer patients: a Chinese pro
Chen, Y; Du, Y; Li, Y; Liu, D; Lv, N; Pan, X; Wang, H; Wang, J; Wu, K; Xie, Y; Xu, J; Zeng, Z; Zhang, G, 2018
)
0.99
" This study confirmed that the Inje cocktail approach was able to detect relevant drug-drug interactions impacting further development of ASP8477 and future therapeutic use."( A Cocktail Interaction Study Evaluating the Drug-Drug Interaction Potential of the Perpetrator Drug ASP8477 at Multiple Ascending Dose Levels.
Collins, C; Ernault, E; Fuhr, R; Gangaram-Panday, S; Passier, P; Treijtel, N; van Bruijnsvoort, M, 2019
)
0.51
"This study aimed to investigate the effect of ticagrelor combined with omeprazole on patients with acute myocardial infarction (AMI) undergoing primary percutaneous coronary intervention (PCI)."( Effects (MACE and bleeding events) of ticagrelor combined with omeprazole on patients with acute myocardial infarction undergoing primary PCI.
Hou, Y; Liu, F; Su, S; Wang, Z; Wu, F; Zhang, F; Zhang, L; Zhao, L,
)
0.6
"Cytochrome P450 (CYP) downregulation is a mechanism of drug-drug interaction encountered in pharmaceutical development which is difficult to evaluate in vitro because of the scarcity of evidence."( CYP1A2 Downregulation by Obeticholic Acid: Usefulness as a Positive Control for the In Vitro Evaluation of Drug-Drug Interactions.
Ishida, C; Kotake, Y; Sanoh, S, 2019
)
0.51
" The probe cocktail was generally well-tolerated when administered in combination with guselkumab in patients with psoriasis."( Evaluating Potential Disease-Mediated Protein-Drug Interactions in Patients With Moderate-to-Severe Plaque Psoriasis Receiving Subcutaneous Guselkumab.
Chen, D; Piantone, A; Sharma, A; Shu, C; Xu, Y; Xu, Z; Zhou, H; Zhu, Y; Zhuang, Y, 2020
)
0.56
"In the present study the electrochemical system based on recombinant cytochrome P450 3A4 (CYP3A4) was used for the investigation of potential drug-drug interaction between medicinal preparations employed for Helicobacter pylori eradication therapy."( [Modeling of drug-drug interactions between omeprazole and erythromycin with cytochrome P450 3A4 in vitro assay].
Bulko, TV; Dmitriev, AV; Filimonov, DA; Gilep, AA; Koroleva, PI; Kuzikov, AV; Makhova, AA; Masamrekh, RA; Rikova, SM; Shich, EV; Shumyantseva, VV; Zaviyalova, MG, 2020
)
0.82
" Previous studies have demonstrated that drug-drug interaction (DDI) existed between omeprazole and nifedipine with significantly increased systemic exposure of nifedipine in subjects after pre-treatment for 7 days with omeprazole compared to the subjects without omeprazole treatment."( Physiologically Based Pharmacokinetic Modeling Approach to Identify the Drug-Drug Interaction Mechanism of Nifedipine and a Proton Pump Inhibitor, Omeprazole.
Babiskin, A; Le Merdy, M; Lee, SC; Ni, Z; Sun, D; Tan, ML; Zhao, L, 2021
)
1.05
" The validity of a cocktail study for use as a quantitative drug-drug interactions (DDIs) assessment was evaluated."( Verification of a cocktail approach for quantitative drug-drug interaction assessment: a comparative analysis between the results of a single drug and a cocktail drug.
Hakamata, A; Inui, N; Kamiya, C; Katayama, N; Kawakami, J; Miura, M; Namiki, N; Odagiri, K; Tanaka, S; Uchida, S; Watanabe, H, 2021
)
0.62
" The aim of this systematic review is to evaluate the effectiveness and safety of Chinese medicine combined with omeprazole for GU."( Effectiveness and safety of Chinese medicine combined with omeprazole in the treatment of gastric ulcer: A protocol for systematic review and meta-analysis.
Liu, L; Wei, M; Xie, C; Zhu, S, 2021
)
1.08
"The efficacy and safety of Chinese medicine combined with omeprazole for the treatment of GU will be evaluated, and the conclusion will be published to provide medical evidence for a better clinical decision of patients with GU."( Effectiveness and safety of Chinese medicine combined with omeprazole in the treatment of gastric ulcer: A protocol for systematic review and meta-analysis.
Liu, L; Wei, M; Xie, C; Zhu, S, 2021
)
1.11
" RNAi therapeutics, such as givosiran, have a low liability for drug-drug interactions (DDIs) because they are not metabolized by cytochrome 450 (CYP) enzymes, and do not directly inhibit or induce CYP enzymes in the liver."( A Drug-Drug Interaction Study Evaluating the Effect of Givosiran, a Small Interfering Ribonucleic Acid, on Cytochrome P450 Activity in the Liver.
Agarwal, S; Clausen, VA; Harper, P; Najafian, N; Robbie, GJ; Sardh, E; Simon, AR; Vassiliou, D, 2021
)
0.62
"The aim of this work is the development of a mechanistic physiologically-based pharmacokinetic (PBPK) model using in vitro to in vivo extrapolation to conduct a drug-drug interaction (DDI) assessment of treosulfan against two cytochrome p450 (CYP) isoenzymes and P-glycoprotein (P-gp) substrates."( Evaluation of the drug-drug interaction potential of treosulfan using a physiologically-based pharmacokinetic modelling approach.
Balazki, P; Baumgart, J; Beelen, DW; Böhm, S; Hemmelmann, C; Hilger, RA; Martins, FS; Ring, A; Schaller, S, 2022
)
0.72
"To date, guidelines on the impact and value of atropine combined with omeprazole in the treatment of acute gastritis have not been well established or well defined."( The clinical efficacy and safety of atropine combined with omeprazole in the treatment of patients with acute gastritis: a systematic review and meta-analysis.
Chen, H; Lin, X; Lin, YN, 2021
)
1.1
" Atropine combined with omeprazole significantly alleviated the clinical symptoms of the patients."( The clinical efficacy and safety of atropine combined with omeprazole in the treatment of patients with acute gastritis: a systematic review and meta-analysis.
Chen, H; Lin, X; Lin, YN, 2021
)
1.17
"Xenobiotics can interact with cytochromes P450 (CYPs), resulting in drug-drug interactions, but CYPs can also contribute to drug-disease interactions, especially in the case of inflammation, which downregulates CYP activities through pretranscriptional and posttranscriptional mechanisms."( Prediction of cytochromes P450 3A and 2C19 modulation by both inflammation and drug interactions using physiologically based pharmacokinetics.
Daali, Y; Desmeules, JA; Lenoir, C; Niederer, A; Rollason, V; Samer, CF, 2022
)
0.72
" A comparative pharmacokinetics study of three LTD tablets with different dissolution rates was conducted in male beagles in fasting state and an omeprazole-induced drug-drug interaction (DDI) study was subsequently performed under pretreatment of omeprazole."( Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug-Drug Interaction.
Li, X; Wang, W; Wang, Y; Wu, W; Xu, Q; Zhang, J; Zhang, T; Zhang, Y, 2021
)
1.02
" Moreover, significant changes in LTD and DL pharmacokinetics parameters were observed under the effect of omeprazole-induced pH increase in gastrointestinal tract, suggesting that DDI effects are of concern for the curative effect of LTD when combined with omeprazole."( Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug-Drug Interaction.
Li, X; Wang, W; Wang, Y; Wu, W; Xu, Q; Zhang, J; Zhang, T; Zhang, Y, 2021
)
1.03
" To investigate the drug-drug interaction mechanism between CDK inhibitors and proton pump inhibitors, the in-silico docking approach was designed by applying computer simulation modules to predict the binding and inhibitory potential."( Inhibition of Cytochrome P450 Enzyme and Drug-Drug Interaction Potential of Acid Reducing Agents Used in Management of CDK Inhibitors for Breast Cancer Chemotherapy.
Birangal, S; Farooqui, J; Fatima, F; Jagadish, PC; Patil, PH; Pinjari, J; Rao, M; Rastogi, H; Sharma, T; Shenoy, GG, 2022
)
0.72
"Proton pump inhibitors alter the conformation of the CYP3A4 and CYP2C19 enzymes and interact with the heme prosthetic group, as determined by docking studies."( Inhibition of Cytochrome P450 Enzyme and Drug-Drug Interaction Potential of Acid Reducing Agents Used in Management of CDK Inhibitors for Breast Cancer Chemotherapy.
Birangal, S; Farooqui, J; Fatima, F; Jagadish, PC; Patil, PH; Pinjari, J; Rao, M; Rastogi, H; Sharma, T; Shenoy, GG, 2022
)
0.72
"Using dynamic models, we determined that proton pump inhibitors such as rabeprazole and omeprazole indeed have the potential to cause clinically significant drug-drug interactions with CDK inhibitors in the treatment of estrogen receptor (ER) positive and HER2-positive breast cancer."( Inhibition of Cytochrome P450 Enzyme and Drug-Drug Interaction Potential of Acid Reducing Agents Used in Management of CDK Inhibitors for Breast Cancer Chemotherapy.
Birangal, S; Farooqui, J; Fatima, F; Jagadish, PC; Patil, PH; Pinjari, J; Rao, M; Rastogi, H; Sharma, T; Shenoy, GG, 2022
)
0.94
" As such, this 2-part clinical drug-drug interaction study was conducted to assess the effect of itraconazole (a strong CYP3A4 inhibitor), rifampicin (a strong CYP3A4 inducer), rabeprazole, and omeprazole (both proton pump inhibitors) on the pharmacokinetics of belumosudil."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
0.91
" Numerous drug-drug interactions have been described with PPIs, but all the described interactions do not have clinical significance."( An update on drug-drug interactions associated with proton pump inhibitors.
Bardou, M; Ben Ghezala, I; Luu, M, 2022
)
0.72
"This review will discuss the latest updates on drug-drug interactions with PPIs, focusing on the last 10-year publications in the following areas: anti-infective agents, anticancer drugs, antiplatelet agents and anticoagulants, and antidiabetics."( An update on drug-drug interactions associated with proton pump inhibitors.
Bardou, M; Ben Ghezala, I; Luu, M, 2022
)
0.72
"To evaluate the potential gastric pH-dependent drug-drug interaction (DDI), safety and tolerability of famitinib co-administered with omeprazole in healthy subjects."( Phase I study to evaluate of the gastric pH-dependent drug interaction between famitinib and the proton pump inhibitor omeprazole in healthy subjects.
Cai, M; Dou, T; Hu, L; Qian, W; Sun, Q; Tang, L; Wang, H, 2022
)
1.13
"In this study, the drug-drug interaction potential of vatiquinone with cytochrome P450 (CYP) substrates was investigated in both in vitro and clinical studies."( Evaluation of vatiquinone drug-drug interaction potential in vitro and in a phase 1 clinical study with tolbutamide, a CYP2C9 substrate, and omeprazole, a CYP2C19 substrate, in healthy subjects.
Barrett, R; Lee, L; Ma, J; Murase, K; Thoolen, M, 2022
)
0.92
" In an open-label, drug-drug interaction study in 18 healthy human subjects, a single oral dose of 500 mg tolbutamide and 40 mg omeprazole was administered on day 1, followed by a washout of 7 days."( Evaluation of vatiquinone drug-drug interaction potential in vitro and in a phase 1 clinical study with tolbutamide, a CYP2C9 substrate, and omeprazole, a CYP2C19 substrate, in healthy subjects.
Barrett, R; Lee, L; Ma, J; Murase, K; Thoolen, M, 2022
)
1.13
"To observe the effect of lansoprazole and omeprazole combined with antibiotics on gastric juice pH and inflammatory factors in elderly patients with Hp positive gastric ulcer."( Effects of lansoprazole and omeprazole Combined With Antimicrobial Agents on Gastric Juice pH and Inflammatory Factors in Elderly Patients With Hp Positive Gastric Ulcer.
Chen, B; Gao, N; Yan, S, 2023
)
1.47
"The control group was treated with omeprazole combined with antibiotics, and the observation group was treated with lansoprazole combined with antibiotics."( Effects of lansoprazole and omeprazole Combined With Antimicrobial Agents on Gastric Juice pH and Inflammatory Factors in Elderly Patients With Hp Positive Gastric Ulcer.
Chen, B; Gao, N; Yan, S, 2023
)
1.48
"The overall effect of lansoprazole combined with antibiotics in the treatment of Hp positive gastric ulcer in the elderly is better than that of omeprazole combined with antibiotics."( Effects of lansoprazole and omeprazole Combined With Antimicrobial Agents on Gastric Juice pH and Inflammatory Factors in Elderly Patients With Hp Positive Gastric Ulcer.
Chen, B; Gao, N; Yan, S, 2023
)
1.4
" Whether used alone or combined with omeprazole (OME), it shows a significant effect."( Weikangling capsules combined with omeprazole ameliorates ethanol-induced chronic gastritis by regulating gut microbiota and EGF-EGFR-ERK pathway.
Li, X; Liu, F; Nong, X; Qu, W, 2023
)
1.46
" Then chronic gastritis model rats were induced by 56 % ethanol and treated with OME, low dose of WKLCs (WKL), high dose of WKLCs (WKH), WKLCs combined with OME (WO), and EA fraction (EA) to evaluate the mechanisms of WKLCs, drug combination and EA fraction."( Weikangling capsules combined with omeprazole ameliorates ethanol-induced chronic gastritis by regulating gut microbiota and EGF-EGFR-ERK pathway.
Li, X; Liu, F; Nong, X; Qu, W, 2023
)
1.19
"This study elucidated that the effect of WKLCs and its combination with OME in the treatment of chronic gastritis was attributed to regulating the composition of the gut microbiota and inhibiting the EGF-EGFR-ERK pathway."( Weikangling capsules combined with omeprazole ameliorates ethanol-induced chronic gastritis by regulating gut microbiota and EGF-EGFR-ERK pathway.
Li, X; Liu, F; Nong, X; Qu, W, 2023
)
1.19
" The in vitro efficacy of OME alone and in combination with other antifungal compounds was evaluated for all isolates using the BM chequerboard method."( In vitro effects of omeprazole in combination with antifungal compounds against Malassezia pachydermatis.
Bae, S; Shin, J, 2023
)
1.23

Bioavailability

Omeprazole treatment did not influence the bioavailability from uncoated acetylsalicylic acid tablets but the absorption rate of salicylate from enteric-coated tablets was increased significantly. Mean (+/- SEM) bioavailability of oral omeprazoles for all patients was 68% +/- 16%.

ExcerptReferenceRelevance
" This effect may result from enhancement of antibiotic bioavailability and optimizing host defense mechanisms."( Progress with proton pump inhibition.
Bell, NJ; Hunt, RH,
)
0.13
" A limited prevalence of hepatotoxic effects is reported by some authors (transitory rise in serum aminotransferase level) and it may be prescribed in patients with chronic liver disease although slower metabolism and greater bioavailability are observed."( [Omeprazole and liver functions].
Sauvet, P; Schouler, L,
)
1.04
" This was reflected in an increase in bioavailability from 56 to 76%, a reduction in mean systemic clearance by approximately 50% (0."( Pharmacokinetic study of omeprazole in elderly healthy volunteers.
Andersson, T; Landahl, S; Larsson, M; Lernfeldt, B; Lundborg, P; Regårdh, CG; Sixt, E; Skånberg, I, 1992
)
0.59
" Lansoprazole bioavailability demonstrated a circadian effect manifested by higher plasma concentrations following morning dosing."( The effects of lansoprazole, a new H+,K(+)-ATPase inhibitor, on gastric pH and serum gastrin.
Greski, PA; Hoyos, PA; Jennings, DE; Page, JG; Sanders, SW; Tolman, KG, 1992
)
0.28
" Measurement of serum concentrations of 1 mg/kg saviprazole after intravenous or intraduodenal administration revealed a bioavailability of about 60% in dogs."( Gastric acid inhibitory profile of saviprazole (HOE 731) compared to omeprazole.
Bickel, M; Herling, AW; Lang, HJ; Rippel, R; Scheunemann, KH; Scholl, T; Weidmann, K, 1991
)
0.52
" Omeprazole, and presumably other gastric-acid inhibitors, may increase the bioavailability of unchanged digoxin."( Influence of gastric acidity on the bioavailability of digoxin.
Cohen, AF; Hoogkamer, H; Kroon, R; Schoemaker, R; van Vliet, A, 1991
)
1.19
" Mean (+/- SEM) bioavailability of oral omeprazole for all patients was 68% +/- 16%, which was similar to the bioavailability reported previously for normal subjects."( Pharmacokinetics of oral and intravenous omeprazole in patients with the Zollinger-Ellison syndrome.
Amantea, MA; Frucht, H; Gardner, JD; Jensen, RT; Maton, PN; Vinayek, R, 1991
)
0.81
" This study investigated the mechanism of the increase in oral bioavailability of omeprazole during repeated oral dosing."( Oral bioavailability of omeprazole before and after chronic therapy in patients with duodenal ulcer.
Angus, PW; Ching, MS; Devenish-Meares, S; Mihaly, GW; Morgan, DJ; Smallwood, RA; Yeomans, ND, 1991
)
0.81
" Bioavailability appears to be dose-dependent, with more drug being absorbed with increasing dosage as well as after repeated dosing."( Omeprazole: a novel antisecretory agent for the treatment of acid-peptic disorders.
Dukes, GE; Hak, LJ; Lampkin, TA; Ouellet, D, 1990
)
1.72
" The slight dose-dependency of the bioavailability of the solution is considered to be of no or limited clinical relevance."( Pharmacokinetics of various single intravenous and oral doses of omeprazole.
Andersson, T; Cederberg, C; Regårdh, CG; Skånberg, I, 1990
)
0.52
" The median bioavailability was 39% (25-117%) and the median systemic plasma clearance was 624 ml/min (range of 59-828 ml/min)."( The pharmacokinetics of omeprazole in humans--a study of single intravenous and oral doses.
Andersson, T; Lagerström, PO; Lundborg, P; Regårdh, CG; Skånberg, I, 1990
)
0.59
" Bioavailability after a single dose is 35% and increases during repeated once-daily dosing to 60%."( Omeprazole: pharmacokinetics and metabolism in man.
Andersson, T; Cederberg, C; Skånberg, I, 1989
)
1.72
" The pharmacokinetic profile of omeprazole is rather complicated, showing concentration-dependent elimination kinetics and an oral bioavailability which increases with the dose and during repeated administration."( Omeprazole: pharmacology, pharmacokinetics and interactions.
Jonkman, JH; Oosterhuis, B, 1989
)
2
" Hypoacidity as such does not reduce the bioavailability of amoxycillin or bacampicillin."( No effect of omeprazole-induced hypoacidity on the bioavailability of amoxycillin or bacampicillin.
Höglund, P; Paulsen, O; Walder, M, 1989
)
0.65
" A water suspension of omeprazole was tested in a pilot bioavailability study."( Development of an oral formulation of omeprazole.
Cederberg, C; Pilbrant, A, 1985
)
0.85
" The bioavailability (AUC0-2 h) of omeprazole in all patients was greater than that required for total suppression of acid secretion."( The effect of omeprazole on gastric emptying in patients with duodenal ulcer disease.
Buckle, PJ; Chatterton, BE; Hetzel, DJ; Horowitz, M; Shearman, DJ, 1984
)
0.91
" Measurement of the plasma concentration of unchanged omeprazole revealed an intraduodenal bioavailability of approximately 70% whereas the oral bioavailability was only approximately 15%."( Inhibition of gastric acid secretion by omeprazole in the dog and rat.
Carlsson, E; Junggren, U; Larsson, H; Olbe, L; Sjöstrand, SE; Skånberg, I; Sundell, G, 1983
)
0.78
"A single-dose, open-label, randomized, fasting, two-period, crossover bioavailability study was conducted in 24 healthy adult men to assess an alternative method of administration of lansoprazole capsules."( Lansoprazole: an alternative method of administration of a capsule dosage formulation.
Cavanaugh, JH; Chun, AH; Eason, CJ; Shi, HH,
)
0.13
" Second, the effect of magnesium/aluminium hydroxide on the relative bioavailability of nizatidine, famotidine, cimetidine and ranitidine was evaluated in healthy volunteers."( Drug interactions of H2-receptor antagonists.
Bachmann, KA; Jauregui, L; Levine, L; Miller, K; Reese, J; Sullivan, TJ, 1994
)
0.29
"The effect of increased gastric pH (obtained by pre-treatment with omeprazole) on the bioavailability of doxycycline monohydrate and doxycycline carrageenate has been investigated in 24 healthy volunteers, using an open, randomised, four-treatment, four-period, cross-over, 2 x 2 factorial design."( Doxycycline carrageenate--an improved formulation providing more reliable absorption and plasma concentrations at high gastric pH than doxycycline monohydrate.
Eckernäs, SA; Grahnén, A; Johansson, G; Olsson, B, 1994
)
0.52
" Food intake did not significantly influence the bioavailability of CdA (42% after food intake vs 46% while fasting) but it did reduce the maximum plasma concentration (Cmax) by 40%; 83 compared to 116 nM while fasting."( On the bioavailability of 2-chloro-2'-deoxyadenosine (CdA). The influence of food and omeprazole.
Albertioni, F; Juliusson, G; Liliemark, J, 1993
)
0.51
"The enteral bioavailability of magnesium firmly bound to a fire-proof, inert SiO2-Al2O3 matrix (ground magnesia boats) was studied in magnesium-deficient albino Sprague-Dawley rats, with and without blocking gastric hydrochloric acid secretion with omeprazole."( Erythema formation in magnesium-deficient albino rats. A non-invasive model for the screening of anti-inflammatory agents and oral mineral supplements.
Abele, C; Classen, CU; Classen, HG; Friedberg, KD; Haubold, W; Schimatschek, HF, 1993
)
0.47
" Pantoprazole was well absorbed following oral administration; the absolute systemic bioavailability of the compound was estimated as 77% (95% CI, 67 to 89%)."( Pharmacokinetics of pantoprazole following single intravenous and oral administration to healthy male subjects.
de Mey, C; Laroche, J; Meineke, I; Pue, MA, 1993
)
0.29
"A comparative bioavailability study was carried out on two enteric-coated capsules (20 mg each) of omeprazole (omeprazole, Alembic: "A" and Losec, Astra, England: "B")."( Comparative bioavailability of two enteric-coated capsules of omeprazole in healthy volunteers.
Chugh, Y; Garg, SK; Kumar, N; Sharma, PL; Tripathi, SK, 1993
)
0.74
" Pantoprazole formulated in an enteric-coated tablet displays high bioavailability and linear pharmacokinetics whether on single or multiple dose regimens."( Review article: the continuing development of proton pump inhibitors with particular reference to pantoprazole.
Huber, R; Kohl, B; Sachs, G; Senn-Bilfinger, J; Simon, WA; Sturm, E, 1995
)
0.29
"We compared the bioavailability and the efficacy of omeprazole provided either as encapsulated enteric-coated granules or as enteric-coated granules delivered via a nasogastric tube in 10 healthy subjects."( Bioavailability and efficacy of omeprazole given orally and by nasogastric tube.
Cavuto, NJ; Flockhart, DA; Larson, C; Weinberg, RB, 1996
)
0.83
" Its absolute bioavailability is 77% and does not change upon multiple dosing."( Pharmacokinetics of pantoprazole in man.
Bliesath, H; Hartmann, M; Huber, R; Lühmann, R; Steinijans, VW; Zech, K, 1996
)
0.29
" The bioavailability of lansoprazole is 85%; that of omeprazole is 54%."( Lansoprazole and omeprazole in the treatment of acid peptic disorders.
Blum, RA, 1996
)
0.88
" Limited information exists about intragastric pH and bioavailability of amoxycillin during combination therapy."( Pharmacokinetic and pharmacodynamic interactions between omeprazole and amoxycillin in Helicobacter pylori-positive healthy subjects.
Braun, M; Idström, JP; Londong, W; Pommerien, W; Wrangstadh, M, 1996
)
0.54
" Its absolute bioavailability is 77% and does not change upon multiple dosing."( Pharmacokinetics of pantoprazole in man.
Bliesath, H; Hartmann, M; Huber, R; Lühmann, R; Steinijans, VW; Zech, K, 1996
)
0.29
"min-1, and the absolute bioavailability was 91% for the 30-mg and 81% for the 15-mg enteric-coated formulation."( Pharmacokinetics and absolute bioavailability of lansoprazole.
Barth, H; Gerloff, J; Heintze, K; Mignot, A, 1996
)
0.29
" The relationship between drug effect and the systemic bioavailability of methadone, measured as the area under the plasma concentration-time curve (AUC0-180), was also evaluated."( The effect of changes in gastric pH induced by omeprazole on the absorption and respiratory depression of methadone.
Aguirre, C; Calvo, R; de Castro, J; Garrido, MJ; Gómez, E; Rodríguez-Sasiaín, JM, 1996
)
0.55
" The primary pharmacokinetic characteristics for extent and rate of absorption were AUC(0-24h) and % PTF, respectively."( Pantoprazole has no influence on steady state pharmacokinetics and pharmacodynamics of metoprolol in healthy volunteers.
Bliesath, H; Hartmann, M; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.29
"The bioavailability of a single dose of a potassium diclofenac (KDIC) suspension (Flogan, Merck, 7ml, 105 mg) was studied in 13 healthy male volunteers in the fasting state (placebo phase, PLA), after gastric acid secretion blockade (subacute pretreatment with omeprazole, OME phase) and after food intake (FOOD phase)."( Influence of gastric acid secretion blockade and food intake on the bioavailability of a potassium diclofenac suspension in healthy male volunteers.
De Nucci, G; Dias, HB; Moreno, H; Moreno, RA; Muscara, MN; Poli, A; Ribeiro, W, 1996
)
0.47
"A single-dose, open-label, randomized, crossover bioavailability study was conducted in 24 healthy adult male volunteers to assess an alternative method of administration of lansoprazole capsules."( Lansoprazole: administration of the contents of a capsule dosage formulation through a nasogastric tube.
Achari, R; Cavanaugh, JH; Chun, AH; Dennis, S; Shi, HH,
)
0.13
" It has a high and constant bioavailability (approximately 77%) which does not change on multiple dosing, so that maximum blood levels are achieved after the first dose."( Pantoprazole, a new proton-pump inhibitor, has a precise and predictable profile of activity.
Parsons, ME, 1996
)
0.29
"To investigate, by means of meal-stimulated acid secretion, the extent to which differences in plasma half-life, bioavailability and the recommended therapeutic dose can influence the antisecretory potency of lansoprazole and omeprazole."( Lansoprazole versus omeprazole: influence on meal-stimulated gastric acid secretion.
Burkhardt, F; Dammann, HG; Fuchs, W; Richter, G; Walter, TA; Wolf, N, 1997
)
0.8
"To determine the effect of the concurrent administration of Maalox and omeprazole in the bioavailability of trovafloxacin (CP-99,219), an open, placebo-controlled, randomized, four-way crossover study was conducted in 12 healthy male volunteers."( Effect of Maalox and omeprazole on the bioavailability of trovafloxacin.
Dogolo, LC; Friedman, HL; Teng, R; Vincent, J; Willavize, SA, 1997
)
0.85
" In the present study, we evaluated the potential of omeprazole to interfere with the bioavailability of aspirin administered to rats either alone or complexed with the zwitterionic phospholipid, dipalmitoylphosphatidylcholine (DPPC)."( Effect of omeprazole on the bioavailability of unmodified and phospholipid-complexed aspirin in rats.
Dial, EJ; Felder, TB; Giraud, MN; Illich, PA; Lichtenberger, LM; Sanduja, SK, 1997
)
0.95
"Gastric absorption of aspirin and its relative bioavailability were reduced by an antisecretory dose of omeprazole; its inhibitory effect on gastric prostaglandin synthesis was consequently attenuated."( Effect of omeprazole on the bioavailability of unmodified and phospholipid-complexed aspirin in rats.
Dial, EJ; Felder, TB; Giraud, MN; Illich, PA; Lichtenberger, LM; Sanduja, SK, 1997
)
0.91
"This study compared the 24 h intragastric pH profile and bioavailability at repeated dosing conditions of the omeprazole 20 mg enteric-coated tablet versus the 20 mg capsule."( Pharmacokinetics and pharmacodynamics during treatment with the omeprazole 20 mg enteric-coated tablet and 20 mg capsule in asymptomatic duodenal ulcer patients.
Kirdeikis, P; Lastiwka, R; Olofsson, B; Röhss, K; Sinclair, P; Thomson, AB,
)
0.58
"The objective of this study was to investigate the influence of food on the bioavailability of omeprazole (20 mg) given as an enteric-coated tablet under repeated dose conditions."( Influence of food on the bioavailability of an enteric-coated tablet formulation of omeprazole 20 mg under repeated dose conditions.
Andersson, T; Matisko, A; Olofsson, B; Rosen, E; Sinclair, P; Thomson, AB,
)
0.57
"Omeprazole affects itraconazole kinetics, leading to a reduction in bioavailability and Cmax."( Effect of omeprazole on the pharmacokinetics of itraconazole.
Jaruratanasirikul, S; Sriwiriyajan, S, 1998
)
2.15
" There was no significant change in the bioavailability of theses NSAIDs during omeprazole therapy in this study."( Lack of drug-drug interaction between three different non-steroidal anti-inflammatory drugs and omeprazole.
Andersson, T; Bredberg, E; Lagerström, PO; Naesdal, J; Wilson, I, 1998
)
0.75
" The presented study was performed to determine the influence of the gastric acid secretion inhibitor omeprazole on bioavailability and pharmacokinetics of cerivastatin."( The effect of omeprazole pre- and cotreatment on cerivastatin absorption and metabolism in man.
Mück, W; Ochmann, K; Rohde, G; Sachse, R, 1998
)
0.88
" According to our results, omeprazole treatment did not influence the bioavailability from uncoated acetylsalicylic acid tablets but the absorption rate of salicylate from enteric-coated tablets was increased significantly."( Interaction of omeprazole with enteric-coated salicylate tablets.
Ayanoglu-Dülger, G; Imeryüz, N; Nefesoglu, FZ; Ulusoy, NB, 1998
)
0.95
"Findings of the present study demonstrate that omeprazole treatment significantly increases the rate of absorption of single-unit enteric-coated medication."( Interaction of omeprazole with enteric-coated salicylate tablets.
Ayanoglu-Dülger, G; Imeryüz, N; Nefesoglu, FZ; Ulusoy, NB, 1998
)
0.91
"The present study examined whether the intestinal microflora could affect the bioavailability and vitamin A activity of dietary alpha- and beta-carotene in the rat."( The bioavailability of alpha- and beta-carotene is affected by gut microflora in the rat.
Alexandre-Gouabau, MC; Azais-Braesco, V; Borel, P; Duszka, C; Grolier, P; Lory, S; Nugon-Baudon, L, 1998
)
0.3
" Differences in physical and physicochemical properties of products A, B, and C indicated that they did not maintain the required stability and that bioavailability might be affected by the poor dissolution of omeprazole from the pellets."( In vitro evaluation of dissolution properties and degradation products of omeprazole in enteric-coated pellets.
Rodrigues, D; Storpirtis, S, 1998
)
0.72
" There was no significant difference between the absorption rate constants of the lansoprazole enantiomers in the in-situ absorption study."( Pharmacokinetic differences between lansoprazole enantiomers in rats.
Arimori, K; Katsuki, H; Nakano, M; Yasuda, K, 1998
)
0.3
" However, the new omeprazole MUPS formulation still showed the well-known effect of initial low bioavailability increasing after repeated dosing."( Comparison of the pharmacodynamics and pharmacokinetics of pantoprazole (40 mg) as compared to omeprazole MUPS (20 mg) after repeated oral dose administration.
Ehrlich, A; Huber, R; Lücker, PW; Mascher, H; Sander, P; Wiedemann, A,
)
0.68
"To determine the relative bioavailability of Ulceral (study formula) with respect to Losec (reference standard formula) and establish their bioequivalence daily doses of 20 mg of omeprazole were given during 5 consecutive days to 24 healthy volunteers."( [A relative bioavailability study of 2 oral formulations of omeprazole after their administration in repeated doses to healthy volunteers].
Gimeno, M; McEwen, J; Moreland, TA; Richards, JP, 1999
)
0.74
" Its bioavailability is not influenced by the coingestion of either food or antacids."( Review article: the pharmacokinetics of rabeprazole in health and disease.
Hoyumpa, AM; Merritt, GJ; Swan, SK, 1999
)
0.3
" The relative bioavailability of omeprazole can be accurately assessed using this multiple-dose study design."( High-dose omeprazole: use of a multiple-dose study design to assess bioequivalence and accuracy of CYP2C19 phenotyping.
Edwards, DJ; Kovacs, P; Lalka, D; Scheiwe, WM; Stoeckel, K, 1999
)
0.99
" They have comparable rates of absorption, maximum plasma concentrations, and total drug absorptions resulting in similar bioavailability after single-dose administration."( Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy.
Lew, EA, 1999
)
0.3
"This study was designed to compare the bioavailability of lansoprazole when administered as an intact capsule and when the contents are admixed with various soft foods."( Effect on bioavailability of admixing the contents of lansoprazole capsules with selected soft foods.
Achari, R; Cavanaugh, JH; Chun, AH; Erdman, K; Zhang, Y, 2000
)
0.31
" Bioavailability was assessed by the two 1-sided tests procedure using a 90% CI for the AUC0-infinity ratio of test-to-reference regimens."( Effect on bioavailability of admixing the contents of lansoprazole capsules with selected soft foods.
Achari, R; Cavanaugh, JH; Chun, AH; Erdman, K; Zhang, Y, 2000
)
0.31
"Proton pump inhibitors and roxithromycin do not alter the systemic bioavailability of each other."( Pharmacokinetic interaction between proton pump inhibitors and roxithromycin in volunteers.
Grobecker, H; Holstege, A; Ittner, KP; Kees, F; Lock, G; Schölmerich, J; Zimmermann, M, 2000
)
0.31
" Although there is no significant difference between proton pump inhibitors with respect to healing of esophagitis, symptom relief occurs earlier with lansoprazole than omeprazole, and this is probably due to the greater oral bioavailability and faster onset of action of lansoprazole when compared to omeprazole."( pH, healing rate, and symptom relief in patients with GERD.
Huang, JQ; Hunt, RH,
)
0.33
" Relative bioavailability of omeprazole from simplified omeprazole suspension compared to the capsule was 58."( Oral pharmacokinetics of omeprazole and lansoprazole after single and repeated doses as intact capsules or as suspensions in sodium bicarbonate.
Howden, CW; Peyton, B; Raufman, JP; Sharma, VK; Spears, T, 2000
)
0.9
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"For the development of omeprazole buccal adhesive tablets, we studied the release and bioavailability of omeprazole delivered by buccal adhesive tablets composed of sodium alginate, hydroxypropylmethylcellulose (HPMC), magnesium oxide and croscarmellose sodium."( Formulation and in vivo evaluation of omeprazole buccal adhesive tablet.
Choi, H; Han, J; Jung, J; Kim, C; Lee, M; Park, K; Rhee, C; Yong, CS, 2000
)
0.89
" The bioavailability of pantoprazole is not altered by concomitant administration of food or antacids or with repeated dosing."( Clinical experience with pantoprazole in gastroesophageal reflux disease.
Avner, DL, 2000
)
0.31
" Pantoprazole is well absorbed when administered as an enteric-coated, delayed-release tablet, with an oral bioavailability of approximately 77%."( Pantoprazole: a new proton pump inhibitor.
Jungnickel, PW, 2000
)
0.31
" Esomeprazole has significantly higher oral bioavailability than omeprazole, resulting in greater acid suppression."( Esomeprazole, a new proton pump inhibitor: pharmacological characteristics and clinical efficacy.
Talley, NJ; Thitiphuree, S, 2000
)
1.65
" Pantoprazole is well absorbed, undergoes little first-pass metabolism, and has an absolute bioavailability of approximately 77%."( Pantoprazole.
Poole, P, 2001
)
0.31
" The release and bioavailability of omeprazole delivered by the buccal adhesive tablets were studied."( Physicochemical characterization and evaluation of buccal adhesive tablets containing omeprazole.
Choi, HG; Jung, JH; Kim, CK; Rhee, JD; Yong, CS, 2001
)
0.81
" Short-term treatment with omeprazole did alter the relative bioavailability of this drug, probably through an effect on absorption kinetics or first-pass metabolism."( Effect of acid secretion blockade by omeprazole on the relative bioavailability of orally administered furazolidone in healthy volunteers.
Calafatti, SA; Deguer, M; Martinez, M; Ortiz, RA; Pedrazzoli, J, 2001
)
0.88
"The encapsulation of omeprazole MUPS 20 mg tablets does not influence the extent and rate of absorption as indicated by the AUC and Cmax ratios."( Bioequivalence between omeprazole MUPS 20 mg as tablet and omeprazole MUPS 20 mg as tablet encapsulated in a hard gelatine capsule.
Cotoraci, CA; Hole, U; Huber, R; Mascher, H; Potthast, H; Schaltenbrand, R, 2001
)
0.94
" The similar holds true for the value of time to reach the maximal concentration of lansoprazole in serum, although this parameter was previously described as less sensitive in comparative bioavailability studies."( A bioavailability/bioequivalence study of two oral lansoprazole formulations after single administration to healthy volunteers.
Jovanović, D; Kilibarda, V; Maksimović, M, 2001
)
0.31
"To compare the bioavailability of three brands of omeprazole capsule (Losec, Aoke-Changzhou No."( [Bioavailability of three brands of omeprazole capsule and their effects on 24 hour intragastric pH in healthy volunteers].
Dong, H, 1999
)
0.83
" The superior acid control achieved by esomeprazole is mainly due to an advantageous metabolism compared with racemate omeprazole, leading to improved bioavailability and to enhanced delivery of the drug to the gastric proton pump."( Clinical pharmacology and safety profile of esomeprazole, the first enantiomerically pure proton pump inhibitor.
Savarino, V; Scarpignato, C; Tonini, M; Vigneri, S, 2001
)
0.83
" However, decreased bioavailability may limit the value of intragastric delivery of PPIs because of the high frequency of gastric emptying problems in critically ill patients."( Pharmacology of acid suppression in the hospital setting: focus on proton pump inhibition.
Pisegna, JR, 2002
)
0.31
"The ability to administer the contents of an encapsulated-dose formulation in liquids or soft foods without compromising drug bioavailability is highly desirable for patients who are unable to swallow or have difficulty swallowing."( Bioavailability of lansoprazole granules administered in juice or soft food compared with the intact capsule formulation.
Achari, R; Cavanaugh, JH; Chiu, YL; Chun, AH; Erdman, K; Pilmer, BL, 2002
)
0.31
"The purpose of this study was to compare the bioavailability of lansoprazole granules administered in 2 types of juice and a soft food with that of the intact capsule administered with water."( Bioavailability of lansoprazole granules administered in juice or soft food compared with the intact capsule formulation.
Achari, R; Cavanaugh, JH; Chiu, YL; Chun, AH; Erdman, K; Pilmer, BL, 2002
)
0.31
" Bioavailability of the 3 test regimens was assessed using the two 1-sided tests procedure for mean maximum plasma concentration and area under the plasma concentration-time curve (AUC) from time 0 through the last measurable concentration and AUC from time 0 to infinity."( Bioavailability of lansoprazole granules administered in juice or soft food compared with the intact capsule formulation.
Achari, R; Cavanaugh, JH; Chiu, YL; Chun, AH; Erdman, K; Pilmer, BL, 2002
)
0.31
"The results of this study indicate that the bioavailability of lansoprazole granules, when administered in orange juice, tomato juice, or a small amount of strained pears, was similar to that of the intact capsule in these healthy adult volunteers."( Bioavailability of lansoprazole granules administered in juice or soft food compared with the intact capsule formulation.
Achari, R; Cavanaugh, JH; Chiu, YL; Chun, AH; Erdman, K; Pilmer, BL, 2002
)
0.31
" The substance has an absolute bioavailability upon oral administration of approximately 52% which is robust against food intake or administration of antacids."( Rabeprazole: pharmacokinetics and pharmacokinetic drug interactions.
Fuhr, U; Jetter, A, 2002
)
0.31
" These include differences in PPI bioavailability and acid-suppressive effects."( The clinical importance of proton pump inhibitor pharmacokinetics.
Thomson, AB; Yacyshyn, BR, 2002
)
0.31
" Studies have shown that the bioavailability of LFDT is comparable to lansoprazole capsules, at both 15 and 30 mg doses; the indications and recommended dosages for LFDT are therefore identical to lansoprazole capsules."( Lansoprazole fast disintegrating tablet: a new formulation for an established proton pump inhibitor.
Baldi, F; Malfertheiner, P, 2003
)
0.32
"The bioavailability of pantoprazole when administered as a suspension in sodium bicarbonate solution and as the oral tablet was studied."( Oral bioavailability of pantoprazole suspended in sodium bicarbonate solution.
Abell, M; Ferron, GM; Getsy, J; Ku, S; Mayer, PR; Paul, J; Unruh, M, 2003
)
0.32
" Physiologic factors that may contribute to a poor response to these drugs include the considerable variation in the bioavailability of PPIs, the need to take PPIs with meals, the influence of Helicobacter pylori-associated gastritis, and genetic variation in enzyme capacity, resulting in rapid and slow metabolizers of PPIs."( Medical management of patients with esophageal or supraesophageal gastroesophageal reflux disease.
Richter, JE, 2003
)
0.32
" The absorption rate is not related to food."( [Therapeutic effect of gastrozolum in stomach ulcers].
Dolgova, NIu; Goncharenko, LS; Kuz'mina, OS; Lopatina, IN; Manannikov, IV; Melik-Ogandzhanian, NB; Serova, TI; Sukhareva, GV; Trubitsina, IE; Tsaregorodtseva, TM; Zarudnaia, SI, 2003
)
0.32
" The present results suggest that the protective effects of lansoprazole can be ascribed to a reduction of gastric oxidative injury, resulting in an increased bioavailability of mucosal sulfhydryl compounds."( Mechanisms of gastroprotection by lansoprazole pretreatment against experimentally induced injury in rats: role of mucosal oxidative damage and sulfhydryl compounds.
Blandizzi, C; Colucci, R; Del Tacca, M; Fornai, M; Lazzeri, G; Lubrano, V; Natale, G; Vassalle, C, 2004
)
0.32
" The bioavailability of omeprazole might, to some extent, be increased through inhibition of P-glycoprotein during fluvoxamine treatment."( Different inhibitory effect of fluvoxamine on omeprazole metabolism between CYP2C19 genotypes.
Inoue, Y; Kaneko, S; Nakagami, T; Takahata, T; Tateishi, T; Yasui-Furukori, N; Yoshiya, G, 2004
)
0.89
" At comparable doses, these properties lead to several clinical advantages: higher bioavailability in extensive metabolisers (the majority of patients), lower exposure in poor metabolisers, less interindividual variation and a steeper dose-response curve at steady state resulting in a more pronounced inhibition of gastric acid secretion."( Single-isomer drugs: true therapeutic advances.
Andersson, T, 2004
)
0.32
"The objective of this study was to determine the impact of omeprazole on bismuth (Bi) bioavailability when given in a three-in-one capsule containing bismuth biskalcitrate, metronidazole, and tetracycline."( Influence of omeprazole on bioavailability of bismuth following administration of a triple capsule of bismuth biskalcitrate, metronidazole, and tetracycline.
Aumais, C; Lefebvre, M; Massicotte, J; Spénard, J; Tremblay, C, 2004
)
0.94
" The pharmacokinetic parameters (C(max), AUC(o-t), t(max)) of this drug have been evaluated to compare the single dose (20 mg) bioavailability of rabeprazole sodium with the standard reference."( Bioequivalence study of rabeprazole sodium on healthy human volunteers.
Banerjee, SN; Chattaraj, TK; Ganesan, M; Jayakumar, M; Mondal, U; Pal, TK; Roy, K, 2004
)
0.32
"Esomeprazole has higher oral bioavailability and increased antimicrobial activity against Helicobacter pylori than omeprazole."( Esomeprazole versus omeprazole for the eradication of Helicobacter pylori infection: results of a randomized controlled study.
Anagnostopoulos, GK; Arvanitidis, D; Kostopoulos, P; Margantinis, G; Tsiakos, S, 2004
)
1.77
" Clinical observations have suggested reduced responses to omeprazole in CF children, which may reflect alterations in bioavailability or clearance."( Altered pharmacokinetics of omeprazole in cystic fibrosis knockout mice relative to wild-type mice.
Ali, SY; Smith, PC; Tallman, MN, 2004
)
0.86
" pylori-infected mucosa and that inhibited the loss of CAM bioavailability in the acidic environment."( Effect of sucralfate on antibiotic therapy for Helicobacter pylori infection in mice.
Fujioka, T; Kashimura, K; Kodama, M; Miura, M; Miyajima, H; Murakami, K; Nasu, M; Okimoto, T; Ootsu, S; Sato, R; Watanabe, K, 2004
)
0.32
"Lansoprazole (LPZ) is a representative drug that shows a high inter-subject variation of bioavailability (BA)."( Effect of adsorbents on the absorption of lansoprazole with surfactant.
Arai, H; Ito, Y; Iwasaki, K; Shibata, N; Takada, K; Uchino, K, 2005
)
0.33
"Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) are important determinants of the oral bioavailability and clearance of tacrolimus."( Impact of gastric acid suppressants on cytochrome P450 3A4 and P-glycoprotein: consequences for FK506 assimilation.
Lemahieu, WP; Maes, BD; Vanrenterghem, Y; Verbeke, K, 2005
)
0.33
"The study was designed to determine the absolute bioavailability of 20 mg rabeprazole tablets in normal, healthy subjects in comparison with intravenous administration of 20 mg rabeprazole."( Pharmacokinetics of rabeprazole following single intravenous and oral administration to healthy subjects.
Hasegawa, J; Humphries, T; Laurent, A; Setoyama, T, 2005
)
0.33
" The bioavailability of lansoprazole might, to some extent, be increased through inhibition of P-glycoprotein during clarithromycin treatment."( Effects of clarithromycin on lansoprazole pharmacokinetics between CYP2C19 genotypes.
Munakata, A; Saito, M; Sugawara, K; Takahata, T; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.33
"This study assessed the effect of the proton pump inhibitor omeprazole on the bioavailability of the extended-release formulations of oxybutynin and tolterodine."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.85
" Bioavailability of intragastric-administered pantoprazole was 41%."( Pharmacokinetics and pharmacodynamics of pantoprazole in clinically normal neonatal foals.
Giguère, S; Ryan, CA; Sanchez, LC; Vickroy, T, 2005
)
0.33
" In the in situ absorption study, the absorption rate constants were of no significant differences between the two enantiomers."( Pharmacokinetic differences between pantoprazole enantiomers in rats.
Xie, Z; Xu, H; Zhang, Y; Zhong, D, 2005
)
0.33
"Methadone is an opioid, which has a high oral bioavailability (>70%) and a long elimination half-life (>20 h) in human beings."( The effects of inhibiting cytochrome P450 3A, p-glycoprotein, and gastric acid secretion on the oral bioavailability of methadone in dogs.
Aman, AM; Kukanich, B; Lascelles, BD; Mealey, KL; Papich, MG, 2005
)
0.33
" There are minor formulation-based pharmacokinetic differences among these agents, primarily reflected in their bioavailability following the first few doses."( Review article: similarities and differences among delayed-release proton-pump inhibitor formulations.
Horn, JR; Howden, CW, 2005
)
0.33
" Further, the bioavailability of tenatoprazole was two-fold greater in the (S)-tenatoprazole sodium salt hydrate form as compared to the free form in dogs which is due to differences in the crystal structure and hydrophobic nature of the two forms."( Characterization of the inhibitory activity of tenatoprazole on the gastric H+,K+ -ATPase in vitro and in vivo.
Domagala, F; Ficheux, H; Homerin, M; Sachs, G; Shin, JM, 2006
)
0.33
"Acid suppression markedly reduced the bioavailability of atazanavir in this group of healthy volunteers."( Inhibition of atazanavir oral absorption by lansoprazole gastric acid suppression in healthy volunteers.
Bednarczyk, E; Berenson, CS; Difrancesco, R; Eberhardt, E; Morse, GD; Ogundele, AB; Smith, PF; Tomilo, DL, 2006
)
0.33
" This study has examined the physical and thermal properties of both forms and in highlighting their differences provides an explanation for the potential differences in bioavailability and therapeutic efficacy."( Physical and thermal characterisation of chiral omeprazole sodium salts.
Agotonovic-Kustrin, S; Glass, B; Markovic, N; Prestidge, CA, 2006
)
0.59
"The effect of omeprazole on the oral bioavailability and urinary exposure of the Depomed formulation of extended-release (ER) ciprofloxacin was studied."( Effect of omeprazole on bioavailability of an oral extended-release formulation of ciprofloxacin.
Berner, B; Hou, E; Hughes, N; Washington, C, 2006
)
1.1
" The bioavailability of tenatoprazole was improved by administration of enteric-coated capsule."( HPLC determination and pharmacokinetic study of tenatoprazole in dog plasma after oral administration of enteric-coated capsule.
Li, F; Liu, P; Lu, X; Qin, F; Sun, B, 2007
)
0.34
"Cyclodextrins are known to be good solubility enhancers for several drugs, improving bioavailability when incorporated in pharmaceutical formulations."( Interaction of omeprazole with a methylated derivative of beta-cyclodextrin: phase solubility, NMR spectroscopy and molecular simulation.
Carvalho, RA; Figueiras, A; Pais, AA; Sarraguça, JM; Veiga, FJ, 2007
)
0.69
"The aim of this study was to evaluate the absolute bioavailability and the metabolism of omeprazole following single intravenous and oral administrations to healthy subjects in relation to CYP2C19 genotypes."( Absolute bioavailability and metabolism of omeprazole in relation to CYP2C19 genotypes following single intravenous and oral administrations.
Hayakari, M; Niioka, T; Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2007
)
0.82
"This study indicates that the absolute bioavailability of omeprazole differs among the three different CYP2C19 genotypes after a single dose of omeprazole orally or intravenously."( Absolute bioavailability and metabolism of omeprazole in relation to CYP2C19 genotypes following single intravenous and oral administrations.
Hayakari, M; Niioka, T; Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2007
)
0.85
"The effect of coadministration of omeprazole on the bioavailability of oral garenoxacin was evaluated in an open-label study in 14 healthy subjects."( The effect of omeprazole on the bioavailability and safety of garenoxacin in healthy volunteers.
Grasela, DM; Kisicki, JC; Krishna, G; Olsen, S; Wang, Z, 2007
)
0.98
"A randomized, single-dose, crossover study was conducted to assess the bioavailability of two omeprazole (CAS 73590-58-6) capsule formulations, Emilok (test) and a commercially available original preparation (reference), under fasting conditions."( Bioequivalence assessment of two capsule formulations of omeprazole in healthy volunteers.
Hammami, MM; Hussein, RF; Lockyer, M, 2007
)
0.8
"Pretreatment of omeprazole does not affect the absorption of domperidone maleate, but leads to a moderately decreased rate of absorption of the free base."( Influence of omeprazole on pharmacokinetics of domperidone given as free base and maleate salt in healthy Chinese patients.
Chen, XY; Dai, XJ; Liu, QZ; Yu, HL; Zhang, YF; Zhang, YN; Zhong, DF, 2007
)
1.05
", nonligand binding, AhR activation by omeprazole upon human insulin-like growth factor binding protein (hIGFBP)-1, a secreted phosphoprotein involved in regulation of insulin-like growth factor-I/II bioavailability and mitogenic activity."( Omeprazole stimulates the induction of human insulin-like growth factor binding protein-1 through aryl hydrocarbon receptor activation.
Murray, IA; Perdew, GH, 2008
)
2.06
" Since S-omeprazole shows more predictable bioavailability and excipients have been known to interact with active pharmaceutical ingredients to produce altered bioavailability, it was decided to investigate the compatibility of omeprazole sodium isomers with mannitol, the major excipient in omeprazole formulations using differential scanning calorimetry (DSC) for bulk drug, attenuated total reflectance (ATR) infrared (IR) spectroscopy in a powder mixture and localized thermal analysis (LTA) from a drug disk."( Compatibility studies between mannitol and omeprazole sodium isomers.
Agatonovic-Kustrin, S; Ginic-Markovic, M; Glass, BD; Mangan, M; Markovic, N, 2008
)
1.03
" The results indicated that lopinavir bioavailability was not affected by the coadministration of omeprazole or ranitidine."( Effects of acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir and ritonavir-boosted atazanavir.
Beck, K; Cai, Y; Causemaker, SJ; Chiu, YL; Doan, T; Esslinger, HU; Hanna, GJ; King, KR; Klein, CE; Podsadecki, TJ, 2008
)
0.56
" There are several generic formulations of omeprazole available in Mexico; however, a literature search failed to identify published data concerning the bioavailability of these formulations in the Mexican population."( Bioavailability of two single-dose oral formulations of omeprazole 20 mg: an open-label, randomized sequence, two-period crossover comparison in healthy Mexican adult volunteers.
Burke-Fraga, V; de Lago, A; Galán, JF; González-de la Parra, M; Jiménez, P; Namur, S; Oliva, I; Poo, JL; Rosete, A, 2008
)
0.85
"The aim of this study was to compare the bioavailability of 2 oral formulations of omeprazole 20-mg capsules, marketed for use in Mexico, in healthy volunteers: Inhibitron (test formulation) and LosecA 20 mg (reference formulation)."( Bioavailability of two single-dose oral formulations of omeprazole 20 mg: an open-label, randomized sequence, two-period crossover comparison in healthy Mexican adult volunteers.
Burke-Fraga, V; de Lago, A; Galán, JF; González-de la Parra, M; Jiménez, P; Namur, S; Oliva, I; Poo, JL; Rosete, A, 2008
)
0.82
" Raltegravir plasma concentration increases with omeprazole coadministration in healthy subjects; this is likely secondary to an increase in bioavailability attributable to increased gastric pH."( Effects of omeprazole on plasma levels of raltegravir.
Azrolan, N; Breidinger, SA; Chodakewitz, JA; Farmer, HF; Hanley, WD; Harvey, CM; Isaacs, RD; Iwamoto, M; Jin, B; Moreau, AR; Nguyen, BY; Rhodes, RR; Stone, JA; Teppler, H; Wagner, JA; Wenning, LA, 2009
)
1
"The results of this study show that the nasogastric route of administration does not appear to cause marked, clinically unsuitable alterations in the bioavailability of the tested drugs."( The bioavailability of bromazepam, omeprazole and paracetamol given by nasogastric feeding tube.
Berger-Gryllaki, M; Buclin, T; Pannatier, A; Podilsky, G; Roulet, M; Testa, B, 2009
)
0.63
" The aim of the study is to assess the relative bioavailability and pharmacokinetic properties of two oral formulations of 20 mg omeprazole tablet, namely LOSEC(R) as reference product and Losectil DR as test product using serum data."( Relative bioavailability and pharmacokinetic study of omeprazole 20 mg enteric-coated tablet in healthy Bangladeshi volunteers.
Abul Kalam Azad, M; Hasan, A; Hasnat, A; Mahbub Latif, AH; Ullah, MA, 2009
)
0.81
" Wet-milling using an ULTRA APEX MILL offers a highly effective approach to produce stable drug nanopowders and is a very useful tool for bioavailability enhancement of poorly water soluble and heat labile drugs."( Nanoparticulation of poorly water soluble drugs using a wet-mill process and physicochemical properties of the nanopowders.
Inkyo, M; Nagai, J; Nagata, S; Takano, M; Tanaka, Y; Yumoto, R, 2009
)
0.35
"Oral omeprazole undergoes marked extraction in the small intestine, and increased bioavailability of the drug after id administration of ketoconazole and verapamil suggests that this increase results from inhibition of CYP3A4 and P-gp function in the intestine rather than the liver."( Involvement of cytochrome P450 3A4 and P-glycoprotein in first-pass intestinal extraction of omeprazole in rabbits.
Chen, ML; Diao, L; Fang, HM; Jin, J; Mei, Q; Xu, JM; Xu, XH, 2009
)
1.09
" The method is sensitive and repeatable enough to be used in pharmacokinetic and bioavailability studies."( Simultaneous determination of omeprazole and domperidone in dog plasma by LC-MS method.
Li, Z; Yao, J; Zhang, L; Zhang, Z,
)
0.42
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" This bioavailability study evaluates this practice in tube-fed patients with severe neurodevelopmental problems."( Pharmacokinetics of two formulations of omeprazole administered through a gastrostomy tube in patients with severe neurodevelopmental problems.
Boussery, K; De Cock, P; De Paepe, P; De Smet, J; Mehuys, E; Remon, JP; Van Bocxlaer, JF; Van Winckel, M; Vande Velde, S, 2011
)
0.64
"In seven of 10 patients, bioavailability was higher for the suspension formulation than for the MUPS® formulation."( Pharmacokinetics of two formulations of omeprazole administered through a gastrostomy tube in patients with severe neurodevelopmental problems.
Boussery, K; De Cock, P; De Paepe, P; De Smet, J; Mehuys, E; Remon, JP; Van Bocxlaer, JF; Van Winckel, M; Vande Velde, S, 2011
)
0.64
" PPIs can reduce the antiplatelet activity of clopidogrel through cytochrome P450 2C19 inhibition, and pantoprazole reduces the bioavailability of dabigatran, a direct thrombin inhibitor that acts via cytochrome P450 2C19-independent mechanisms."( Effect of multiple doses of omeprazole on the pharmacokinetics, pharmacodynamics, and safety of a single dose of rivaroxaban.
Ariyawansa, J; Burton, PB; Moore, KT; Plotnikov, AN; Thyssen, A; Vaccaro, N, 2011
)
0.66
" The bioavailability of MPA following administration of MMF or EC-MPS was similar except for the time to peak concentration, which was longer in the EC-MPS group."( Omeprazole impairs the absorption of mycophenolate mofetil but not of enteric-coated mycophenolate sodium in healthy volunteers.
Bucher, M; Faerber, L; Kees, F; Kees, MG; Moritz, S; Paulus, EM; Rupprecht, K; Steinke, T, 2012
)
1.82
" This study was conducted to compare the relative bioavailability and pharmacokinetic properties of two omeprazole 20 mg capsule formulations namely Xeldrin®20 (ACI Ltd."( Bioavailability of omeprazole 20 mg capsules containing omeprazole 22.5% enteric coated pellets versus a reference product in healthy Bangladeshi male subjects: an open-label, single-dose, randomized-sequence, two-way crossover study.
Ahmed, MU; Hasnat, A; Islam, MS; Maruf, AA; Shohag, H; Trini, AB, 2011
)
0.91
" The purpose of this study was to compare the bioavailability of two of them, Losec and Omelcid."( Comparative bioavailability of two oral formulations of omeprazole.
Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Herrera, JE; Medina-Santillán, R; Reyes-García, G, 2009
)
0.6
"Previous studies proved that food strongly enhanced the bioavailability of vinpocetine."( Omeprazole does not change the oral bioavailability or pharmacokinetics of vinpocetine in rats.
Karaźniewicz-Łada, M; Kiełbowicz, G; Ksiądzyna, D; Magdalan, J; Merwid-Ląd, A; Sozański, T; Szeląg, A; Szumny, A; Słupski, W; Trocha, M, 2011
)
1.81
"In order to comply with the requirements for a drug listed in China, the study was developed to compare the pharmacokinetics and relative bioavailability of two different enteric formulations of omeprazole (OPZ) in healthy Chinese subjects."( Relative bioavailability and pharmacokinetic comparison of two different enteric formulations of omeprazole.
Chen, JC; Dou, J; Hu, XJ; Huang, MZ; Liu, J; Shentu, JZ; Wu, GL; Wu, LH; Xu, QY; Zhou, HL, 2012
)
0.79
"Due to the multi-factorial physiological implications of bariatric surgery, attempts to explain trends in oral bioavailability following bariatric surgery using singular attributes of drugs or simplified categorisations such as the biopharmaceutics classification system have been unsuccessful."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"The trends in oral bioavailability pre to post surgery were found to be dependent on a combination of drug parameters, including solubility, permeability and gastrointestinal metabolism as well as the surgical procedure carried out."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"2-(4-(4-(tert-Butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid (AMG 853) is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors."( Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
Amore, BM; Banfield, C; Boudreaux, MD; Davis, JA; Emery, MG; Foti, RS; Pearson, JT; Prokop, SP; Rock, DA; Wahlstrom, JL; Wienkers, LC; Wong, SL; Zalikowski, JA, 2012
)
0.38
" The CGA is well absorbed orally, and its effects on gastric ulcer have not been previously reported."( Antiulcerogenic activity of chlorogenic acid in different models of gastric ulcer.
de Melo, IL; de Oliveira e Silva, AM; Farsky, SH; Machado, ID; Mancini-Filho, J; Santin, JR; Shimoyama, AT, 2013
)
0.39
" However, maximum plasma concentration, half-life, area under the curve, and oral bioavailability were not different."( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients.
Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013
)
0.39
"The aim of this study was to develop new dipyridamole (DP) salts with pH-independent solubility for improving oral bioavailability under hypochlorhydria."( New dipyridamole salt with improved dissolution and oral bioavailability under hypochlorhydric conditions.
Inoue, R; Kato, M; Kawabata, Y; Onoue, S; Taniguchi, C; Wada, K; Yamada, S; Yamashita, K, 2013
)
0.39
"A new series of novel benzimidazole derivatives containing substituted pyrid-2-yl moiety and polyhydroxy sugar conjugated to the N-benzimidazole moiety has been synthesized and evaluated as orally bioavailable anti-inflammatory agents with anti-ulcerogenic activity."( Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
Biuomy, AR; El-Nezhawy, AO; Hassan, FS; Ismaiel, AK; Omar, HA, 2013
)
0.64
"As the bioavailability of erlotinib is dependent on gastric pH, an increase in gastric pH via the concurrent use of gastric acid suppressive medications (AS) may reduce its bioavailability and efficacy."( An evaluation of the possible interaction of gastric acid suppressing medication and the EGFR tyrosine kinase inhibitor erlotinib.
Bradbury, PA; Hilton, JF; Seymour, L; Shepherd, FA; Tu, D, 2013
)
0.39
" The goals of the clinical development program were to demonstrate the following: improved gastrointestinal safety of PA relative to enteric-coated aspirin alone; bioequivalence and comparative bioavailability between the PA compounds and currently marketed enteric-coated aspirin; and long-term safety."( PA tablets: investigational compounds combining aspirin and omeprazole for cardioprotection.
Bliden, KP; Brener, M; Franzese, CJ; Gesheff, MG; Gurbel, PA; Tabrizchi, A; Tantry, U, 2013
)
0.63
" The study was conducted from January 2006 to April 2007 and was designed to find out the bioavailability of omeprazole in capsule form in healthy Bangladeshi population and to compare this with that of the other population in the world."( Bioavailability and plasma concentration of omeprazole in healthy bangladeshi population after ingestion.
Bachar, SC; Ghosh, CK; Hasan, M; Ishaque, SM; Mahmuduzzaman, M; Uddoula, MS, 2013
)
0.86
"The objectives were to document the pharmacokinetics of intravenous, enteric-coated oral and plain oral omeprazole in fasted horses and to investigate the impact of feeding on the bioavailability of an enteric-coated omeprazole."( Pharmacokinetics of intravenous, plain oral and enteric-coated oral omeprazole in the horse.
McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2015
)
0.87
"Omeprazole (OME) is a proton pump inhibitor with a 58% bioavailability after a single oral dose."( Improvement and validation of a high-performance liquid chromatography in tandem mass spectrometry method for monitoring of omeprazole in plasma.
Abad-Santos, F; Gil García, AI; Ochoa-Mazarro, D; Román-Martínez, M; Ruiz-Nuño, A; Wojnicz, A, 2015
)
2.07
" However, a wider-than-expected degree of variation was present and examination of the raw data suggests that an effect of feeding, wherein the bioavailability of omeprazole may be reduced in the fed animal, may be present."( The effect of feeding on the pharmacokinetic variables of two commercially available formulations of omeprazole.
McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2015
)
0.83
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates."( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
Bharate, SS; Vishwakarma, RA, 2015
)
0.42
" Bioavailability of midazolam was 4% in marmosets, presumably because of contribution of marmoset P450 3A4 expressed in small intestine and liver, with a high catalytic efficiency for midazolam 1'-hydroxylation as evident in the recombinant system."( Simultaneous pharmacokinetics evaluation of human cytochrome P450 probes, caffeine, warfarin, omeprazole, metoprolol and midazolam, in common marmosets (Callithrix jacchus).
Inoue, T; Sasaki, E; Shimizu, M; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2016
)
0.65
"This study was conducted to investigate the effect of food and coadministration of omeprazole on the relative bioavailability (BA) of faldaprevir (FDV)."( Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants.
Elgadi, M; Gießmann, T; Huang, F; Lang, B; Wu, J, 2016
)
0.93
"Short-term fasting can alter drug exposure but it is unknown whether this is an effect of altered oral bioavailability and/or systemic clearance."( Effect of Short-Term Fasting on Systemic Cytochrome P450-Mediated Drug Metabolism in Healthy Subjects: A Randomized, Controlled, Crossover Study Using a Cocktail Approach.
Achterbergh, R; Lammers, LA; Mathôt, RAA; Romijn, JA; van Schaik, RHN, 2017
)
0.46
" Comparison of mean log area under time-plasma concentration curves demonstrated that, although the lower limit of the 90% confidence interval was within the -20% limit for bioequivalence, the upper limit was exceeded, suggesting that the test product could have greater bioavailability than the reference product."( Pharmacokinetic and pharmacodynamic effects of two omeprazole formulations on stomach pH and gastric ulcer scores.
Andrews, FM; Nielsen, SG; Raidal, SL; Trope, G, 2017
)
0.71
"The small sample size, large interhorse plasma omeprazole concentrations, and low bioavailability of omeprazole impacted the sensitivity of the bioequivalence analysis."( Pharmacokinetic and pharmacodynamic effects of two omeprazole formulations on stomach pH and gastric ulcer scores.
Andrews, FM; Nielsen, SG; Raidal, SL; Trope, G, 2017
)
0.96
" In this study, the relative bioavailability of the tablet formulation versus the initial capsule formulation and the effect of food and omeprazole on the pharmacokinetics of a single-dose momelotinib tablet were evaluated in healthy subjects."( The Relative Bioavailability, Food Effect, and Drug Interaction With Omeprazole of Momelotinib Tablet Formulation in Healthy Subjects.
Deng, W; Hemenway, J; Maltzman, J; Shao, L; Silverman, JA; Stefanidis, D; Tarnowski, T; Xin, Y, 2018
)
0.92
" absorption rate constants or systemic circulation volumes, were not likely determining factors."( Association with polymorphic marmoset cytochrome P450 2C19 of in vivo hepatic clearances of chirally separated R-omeprazole and S-warfarin using individual marmoset physiologically based pharmacokinetic models.
Inoue, T; Kusama, T; Sasaki, E; Shimizu, M; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2018
)
0.69
" Although dissolution profiles similar to the original product were obtained, the unexpected results of omeprazole low bioavailability in the fed bioequivalence study (BES I) showed the necessity to investigate the formulation in greater depth."( The effect of the composition of a fixed dose combination on bioequivalence results.
Beránek, J; Červená, T; Dumicic, A; Franc, A; Hofmann, J; Kukačková, L; Repický, A; Šalandová, J; Srbek, J; Vetchý, D; Vladovičová, B, 2018
)
0.7
" This phase 1 study in healthy subjects evaluated the relative bioavailability of filgotinib maleate tablets versus the reference tablet (filgotinib hydrochloride) and effects of food and acid-reducing agents (ARAs) on the pharmacokinetics of filgotinib and its major metabolite."( The Relative Bioavailability and Effects of Food and Acid-Reducing Agents on Filgotinib Tablets in Healthy Subjects.
Anderson, K; Cuvin, J; Kotecha, M; Namour, F; Qin, AR; Scott, B; Sharma, S; Xin, Y; Zheng, H, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Omeprazole preparations vary in bioavailability in horses."( Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses.
Edwards, S; Hughes, KJ; Jacobson, GA; Narkowicz, CK; Raidal, SL; Wise, JC, 2021
)
2.31
"A prospective, blinded randomized interventional study was trial, conducted in 3 parts: (a) bioavailability study, (b) dose titration study, and (c) comparative clinical pharmacodynamic study, each using a blocked crossover design."( Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses.
Edwards, S; Hughes, KJ; Jacobson, GA; Narkowicz, CK; Raidal, SL; Wise, JC, 2021
)
0.86
" No differences were observed between products for absolute oral bioavailability (NOV 55% range, 15-88; REF 17% range, 10-77; P = ."( Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses.
Edwards, S; Hughes, KJ; Jacobson, GA; Narkowicz, CK; Raidal, SL; Wise, JC, 2021
)
0.86
"A novel, integrated, in vitro gastrointestinal (GI) system is presented to study oral bioavailability parameters of small molecules."( A versatile, compartmentalised gut-on-a-chip system for pharmacological and toxicological analyses.
Bouwmeester, H; de Haan, P; Nielen, MWF; Santbergen, MJC; van der Zande, M; Verpoorte, E, 2021
)
0.62
" The principal aim was to evaluate whether gastric bypass surgery modifies the bioavailability and pharmacokinetic (PK) parameters of omeprazole."( Effect of Obesity and Roux-En-Y Gastric Surgery on Omeprazole Pharmacokinetics.
Bandrés, F; Castrillón, EV; Chicharro, LM; López-Picado, A; Moreno Lopera, C; Paterna, ABR; Portolés-Pérez, A; Rubio, MA; Sánchez Pernaute, A; Torres García, AJ, 2022
)
1.18
"Controlled, open-label, bioavailability clinical trial in patients undergoing Roux-en-Y gastric bypass (RYGB)."( Effect of Obesity and Roux-En-Y Gastric Surgery on Omeprazole Pharmacokinetics.
Bandrés, F; Castrillón, EV; Chicharro, LM; López-Picado, A; Moreno Lopera, C; Paterna, ABR; Portolés-Pérez, A; Rubio, MA; Sánchez Pernaute, A; Torres García, AJ, 2022
)
0.97
" Discusion/Conclusions: Omeprazole bioavailability is reduced in patients with obesity at 1 and 6 months after RYGB."( Effect of Obesity and Roux-En-Y Gastric Surgery on Omeprazole Pharmacokinetics.
Bandrés, F; Castrillón, EV; Chicharro, LM; López-Picado, A; Moreno Lopera, C; Paterna, ABR; Portolés-Pérez, A; Rubio, MA; Sánchez Pernaute, A; Torres García, AJ, 2022
)
1.28
" In a bioavailability study comparing formulations containing 110."( Dasatinib anhydrate containing oral formulation improves variability and bioavailability in humans.
Bartůněk, A; Beránek, J; Hauser, T; Hofmann, J; Ryšánek, P; Sedmak, G; Šíma, M; Slanař, O, 2023
)
0.91

Dosage Studied

Omeprazole had no clinically relevant effect on voriconazole exposure. Median pH during combined dosing was significantly lower, compared to omepraz.

ExcerptRelevanceReference
"3%) had received previous therapy with H2-receptor antagonists and in 33% of these patients it was at an inadequate dose or for an inadequate period of dosing or both."( A drug usage review of omeprazole.
Kay, EA; McManus, PV; Norris, CM; Petty, D, 1992
)
0.59
" Lansoprazole (both doses) as well as omeprazole raised the plasma gastrin levels about 11-fold 2 h after dosing and 8-to 10-fold 24 h after dosing, reflecting complete (2 h) and 70-80% (24 h) reductions of gastric acid secretion."( Lansoprazole and omeprazole have similar effects on plasma gastrin levels, enterochromaffin-like cells, gastrin cells and somatostatin cells in the rat stomach.
Håkanson, R; Karlsson, A; Lee, H; Mattsson, H; Sundler, F, 1992
)
0.89
" Successful control of reflux disease in these patients was achieved by increasing omeprazole therapy to a regime and dosage that achieved elevation of intragastric pH above 4 throughout the 24-hour period."( Medical therapy of patients with reflux oesophagitis poorly responsive to H2-receptor antagonist therapy.
Klinkenberg-Knol, EC; Meuwissen, SG, 1992
)
0.51
" Estimation of fasting serum gastrin concentration (RIA) was performed before treatment and 24 hours after the last dosage of OME, and HP was searched for an antral biopsies at the end of the treatment as well."( Preliminary observations in the fasting serum gastrin in patients with duodenal ulcer; further evidence of the "clearing" effect of omeprazole on H pylori?
Alevizou, V; Archimandritis, A; Davaris, P; Fertakis, A; Kapsalas, D; Kyriaki, D; Tjivras, M, 1992
)
0.49
" Despite these findings, the considerable overlap in these parameters between young and old volunteers, together with data from previous pharmacodynamic studies and the wide therapeutic range of omeprazole, indicate that dosage reductions are not needed in the elderly."( Pharmacokinetic study of omeprazole in elderly healthy volunteers.
Andersson, T; Landahl, S; Larsson, M; Lernfeldt, B; Lundborg, P; Regårdh, CG; Sixt, E; Skånberg, I, 1992
)
0.78
"Prolonged fasting and longer time between dosing and sampling reduced the plasma gastrin concentrations after omeprazole (80 mumol/kg x 2 for 14 days) treatment in male rats whereas the amounts of tissue gastrin were essentially unchanged during these initial experiments."( Effects of omeprazole and ranitidine on plasma gastrin concentration and stomach gastrin content in rats.
Girma, K; Nilsson, G; Romell, B; Seensalu, R, 1992
)
0.89
"Omeprazole, an inhibitor of gastric acid secretion, was administered to rats at a dosage of 20 mg/kg/day for 14 and 35 days, and subsequent changes in subcellular structures of parietal cells were analyzed using morphometry and immunocytochemistry."( Changes in subcellular structures of parietal cells in the rat gastric gland after omeprazole.
Fukutomi, H; Furuhashi, M; Kominami, E; Nakahara, A; Uchiyama, Y, 1992
)
1.95
" The purpose of this study was to determine whether morning or evening dosage gave better control of 24-hr intragastric pH."( Effect of lansoprazole on intragastric pH. Comparison between morning and evening dosing.
Abe, S; Asaki, S; Hirasawa, Y; Hongo, M; Ohara, S; Toyota, T, 1992
)
0.28
" Conventional dosing with H2-receptor antagonists has been successful in only about 50% of the patients with reflux esophagitis."( The role of omeprazole in healing and prevention of reflux disease.
Klinkenberg-Knol, EC, 1992
)
0.66
" Dosing included continuous intravenous infusion ranitidine (50 mg bolus followed by 12."( Circadian differences in pharmacological blockade of meal-stimulated gastric acid secretion.
Day, GM; Moore, JG; Sanders, SW; Tolman, KG, 1992
)
0.28
" An additional 18 subjects received once daily 30 mg oral doses of lansoprazole or placebo; these subjects were dosed at either 08."( The effects of lansoprazole, a new H+,K(+)-ATPase inhibitor, on gastric pH and serum gastrin.
Greski, PA; Hoyos, PA; Jennings, DE; Page, JG; Sanders, SW; Tolman, KG, 1992
)
0.28
" To define a dosage regimen for clinical trials we compared the effect of pantoprazole 40 and 60 mg daily on 24-h intragastric acidity and plasma gastrin concentrations using a double-blind, randomized, cross-over design."( Effects of oral pantoprazole on 24-hour intragastric acidity and plasma gastrin profiles.
Broom, C; Hannan, A; Walt, RP; Weil, J, 1992
)
0.28
" The present study indicates that 24-hour oesophageal pH monitoring is a practical approach to the determination of drug dosage in patients with gastro-oesophageal reflux."( Effect of different doses of omeprazole on 24-hour oesophageal acid exposure in patients with gastro-oesophageal reflux.
Allen, ML; Bradstreet, TE; Cagliola, AJ; Humphries, TJ; Maton, PN; McIntosh, D; Robinson, M, 1991
)
0.57
" Six dogs were given cimetidine at dosage of 10 mg/kg orally every 8 hours, and 6 dogs were given omeprazole orally at dosage of 2 mumol/kg (0."( Comparison of effects of cimetidine and omeprazole on mechanically created gastric ulceration and on aspirin-induced gastritis in dogs.
Bright, RM; DeNovo, RC; Jenkins, CC; Patton, CS; Rohrbach, BW, 1991
)
0.77
" This randomized, double-blind multicentre trial studied the dose-response relationship of lansoprazole on ulcer healing and compared it with ranitidine in 314 out-patients with endoscopically assessed, symptomatic duodenal ulcer."( Dose-related healing of duodenal ulcer with the proton pump inhibitor lansoprazole.
Barth, H; Dammann, HG; Hengels, KJ; Kleinert, R; Londong, W; Müller, P; Rohde, H; Simon, B, 1991
)
0.28
"This study was performed to investigate the possible influence of repeated omeprazole dosing on the metabolism of caffeine, which has been shown to reflect the activity of one specific enzyme within the hepatic cytochrome P450 family, P450IA2."( Omeprazole treatment does not affect the metabolism of caffeine.
Andersson, T; Bergstrand, R; Cederberg, C; Eriksson, S; Lagerström, PO; Skånberg, I, 1991
)
1.95
"We determined the effect of four times daily dosing with intravenous omeprazole on 24-h intragastric acidity, serum gastrin, and serum pepsinogen A and C in 10 fasting subjects (median age, 23."( Repeated intravenous bolus injections of omeprazole: effects on 24-hour intragastric pH, serum gastrin, and serum pepsinogen A and C.
Baak, LC; Biemond, I; Jansen, JB; Lamers, CB, 1991
)
0.78
" Post-evening meal (PEM) dosing of H2-receptor antagonists appears to be a rational method of suppressing late evening gastric acidity, but on balance the symptomatic response of twice daily dosing is superior to once daily dosing."( Reflux esophagitis.
Nio, CY; Schotborgh, RH; Tytgat, GN, 1990
)
0.28
" Omeprazole, which suppresses acid very effectively, may be problematic in the critically ill, limited by its oral dosage form, acid-labile properties, and potential drug interactions."( Controlling gastric pH: the impact of newer agents on the critically ill patient.
Earnest, DL, 1990
)
1.19
"The magnitude and duration of changes in nocturnal intragastric acidity caused by 25 days of dosing with the antisecretory drugs ranitidine and omeprazole were investigated in a double-blind study of 22 healthy subjects."( Nocturnal intragastric acidity during and after a period of dosing with either ranitidine or omeprazole.
Hudson, M; Nwokolo, CU; Pounder, RE; Prewett, EJ; Sawyerr, AM, 1991
)
0.7
" The dose of omeprazole required in individual patients ranged from 10 to 180 mg/24 hr with 20-60% requiring a split dosage regimen."( Use of omeprazole in patients with Zollinger-Ellison syndrome.
Frucht, H; Jensen, RT; Maton, PN, 1991
)
1.11
" Rats were orally dosed with 40 mumol/kg of omeprazole or placebo daily for two days prior to iron absorption studies."( Inhibition of iron absorption by omeprazole in rat model.
Adams, P; Flanagan, P; Golubov, J, 1991
)
0.82
" dosage following the course of treatment."( Oral bioavailability of omeprazole before and after chronic therapy in patients with duodenal ulcer.
Angus, PW; Ching, MS; Devenish-Meares, S; Mihaly, GW; Morgan, DJ; Smallwood, RA; Yeomans, ND, 1991
)
0.59
" Use of the insert achieved an earlier steady secretory response which allowed cumulative dosing to be performed in each animal."( Use of a cannula insert in erratic emptying Heidenhain pouch dogs: effect of single and cumulative doses of omeprazole.
Ghelani, A; Radziwonik, H, 1990
)
0.49
"To determine the effect of three times daily dosing with intravenous omeprazole on intragastric acidity, 24 h intragastric pH was measured continuously with a monocrystalline antimony electrode system in II patients with inactive duodenal ulceration during fasting conditions."( Intravenous omeprazole: effect of a loading dose on 24-h intragastric pH.
Andersen, J; Leire, K; Naesdal, J; Ström, M; Walan, A, 1990
)
0.89
" Blood was collected up to 120 hours after diazepam dosing (still during one-daily omeprazole and placebo administration) for measurement of diazepam and its major metabolite desmethyldiazepam."( Effect of omeprazole treatment on diazepam plasma levels in slow versus normal rapid metabolizers of omeprazole.
Andersson, T; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990
)
0.91
" Bioavailability appears to be dose-dependent, with more drug being absorbed with increasing dosage as well as after repeated dosing."( Omeprazole: a novel antisecretory agent for the treatment of acid-peptic disorders.
Dukes, GE; Hak, LJ; Lampkin, TA; Ouellet, D, 1990
)
1.72
"The effects of steady state dosing with omeprazole and cimetidine on plasma diazepam levels have been studied in 12 healthy males."( Effect of omeprazole and cimetidine on plasma diazepam levels.
Andersson, T; Andrén, K; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990
)
0.95
" Omeprazole, a substituted benzimidazole inhibitor of the gastric H+/K(+)-APT-ase, was administered orally at a dose of 20 mg in the morning of 3 consecutive days, followed by a period of 4 days without medication, and this intermittent dosage regimen was continued for 4 weeks."( Effect of intermittent administration of omeprazole on serum pepsinogens in duodenal ulcer patients and healthy volunteers.
Biemond, I; Crobach, LF; Jansen, JB; Lamers, CB, 1990
)
1.46
" tracer dose were unchanged on repeated dosing while AUC increased by approximately 40% for the solution and 60% for the EC granules."( Pharmacokinetics and bioavailability of omeprazole after single and repeated oral administration in healthy subjects.
Andersson, T; Andrén, K; Cederberg, C; Lagerström, PO; Lundborg, P; Skånberg, I, 1990
)
0.55
" During repeated once daily dosing with this formulation the degree of acid suppression increased over the first days after the start of treatment but stabilized within about 4 days."( Effect of omeprazole on gastric acid secretion and plasma gastrin.
Cederberg, C; Lind, T; Olausson, M; Olbe, L, 1989
)
0.68
"To investigate the efficacy of standard and low dosage of omeprazole in the healing of duodenal ulcer, 270 patients with endoscopically active duodenal ulcer were randomized to receive omeprazole, 10 mg or 20 mg every morning, or ranitidine, 150 mg twice daily, using the double-dummy technique."( Omeprazole and ranitidine in duodenal ulcer healing and subsequent relapse: a randomized double-blind study with weekly endoscopic assessment.
Branicki, FJ; Hui, WM; Lai, CL; Lam, SK; Lau, WY; Lok, AS; Ng, MM; Poon, GP, 1989
)
1.96
" Seven days' dosing with 60 mg AG-1749 induced a more than threefold increment of fasting serum gastrin concentration, but this increase was still within the normal range."( Human gastric acid secretion following repeated doses of AG-1749.
Dammann, HG; Leucht, U; Müller, P; Simon, B, 1989
)
0.28
"8 mM Ca2+, the rate of glycogen breakdown was increased by theophylline in a dose-dependent manner and the dose-response curve was somewhat similar to that obtained with oxygen uptake."( Ca2+ requirement for metabolic effects of secretagogues in the amphibian gastric mucosa.
Chacín, J; Lobo, P; Subero, O, 1989
)
0.28
" During dosing with omeprazole, basal gastric acid output diminished by 94%, and pentagastrin-stimulated acid output by 97%."( Repeated high oral doses of omeprazole do not affect intrinsic factor secretion: proof of a selective mode of action.
Den Hollander, W; Festen, HP; Meuwissen, SG; Tuynman, HA, 1989
)
0.89
" Omeprazole caused a non-competitive inhibition of the dose-response curve to dimaprit, whereas famotidine induced a parallel shift to the right without depressing the maximum response."( Antisecretory activity of omeprazole in the conscious gastric fistula cat: comparison with famotidine.
Bertaccini, G; Coruzzi, G,
)
1.34
" No changes in DNA synthesis, percentage of labelled nuclei and transaminase were detected when the agents were added to the hepatocytes in culture at concentrations within the effective pharmacological dosage and 30 times higher."( Effect of cimetidine, ranitidine, famotidine and omeprazole on hepatocyte proliferation in vitro.
Amoruso, A; Barone, M; Di Leo, A; Francavilla, A; Ingrosso, M; Makowka, L; Panella, C; Polimeno, L; Starzl, TE, 1989
)
0.53
" SK&F Wistar rats were dosed orally with omeprazole (up to 500 mg kg-1) or vehicle."( Studies on the effects of omeprazole on thyroid function in the rat.
Atterwill, CK; Brown, CG; Fowler, KL; Jones, CA, 1989
)
0.84
" Dinnertime dosing of cimetidine appears to be a rational method of suppressing late-evening gastric acidity."( Drug therapy of reflux oesophagitis: an update.
Tytgat, GN, 1989
)
0.28
" During repeated once-daily dosing with an enteric-coated granule capsule formulation, inhibition of acid secretion increased initially, and stabilized within about 4 days."( Effect of omeprazole on gastric acid secretion and plasma gastrin in man.
Cederberg, C; Lind, T; Olausson, M; Olbe, L, 1989
)
0.68
" Bioavailability after a single dose is 35% and increases during repeated once-daily dosing to 60%."( Omeprazole: pharmacokinetics and metabolism in man.
Andersson, T; Cederberg, C; Skånberg, I, 1989
)
1.72
" This gastrin-carcinoid sequence is unlikely to occur in man with an omeprazole dosage recommended for treatment of peptic diseases."( Omeprazole: long-term safety.
Arnold, R; Koop, H, 1989
)
1.95
" For the choice of dosage regimens this has minor consequences, in view of the wide therapeutic range of omeprazole and because an almost continuous maximum effect is obtained with once daily oral administration of 20-40 mg."( Omeprazole: pharmacology, pharmacokinetics and interactions.
Jonkman, JH; Oosterhuis, B, 1989
)
1.93
" Omeprazole, in contrast, did not alter gastric emptying at a similar antisecretory dosage level."( Effects of H2-receptor antagonists upon physiological acid secretory states in animals.
Cook, PG; Mangel, AW; Pendleton, RG; Shepherd-Rose, A, 1985
)
1.18
" The other five patients, who were free of complication, initially received a standard regimen of omeprazole 60 mg orally once a day; dosage was subsequently adjusted until the basal acid output, measured 1 hr before the next dose of the drug, was less than 10 mmol/hr."( Effectiveness of omeprazole in seven patients with Zollinger-Ellison syndrome resistant to histamine H2-receptor antagonists.
Bader, JP; Cortot, A; Delchier, JC; Goldfain, D; Isal, JP; Mignon, M; Soule, JC; Travers, B, 1986
)
0.83
" Investigative studies showed evidence for marked and sustained hypergastrinemia increasing on chronic dosing which was capable of restoring gastric acid secretion and pH to near control values."( Gastric ECL-cell hyperplasia and carcinoids in rodents following chronic administration of H2-antagonists SK&F 93479 and oxmetidine and omeprazole.
Betton, GR; Buckley, P; Dormer, CS; Pert, P; Price, CA; Wells, T, 1988
)
0.48
" Dosage was adjusted primarily on the basis of basal acid output, but also if symptoms recurred."( Omeprazole in the treatment of Zollinger-Ellison syndrome: a 4-year international study.
Lloyd-Davies, KA; Rutgersson, K; Sölvell, L, 1988
)
1.72
"The effect of 7 days of oral dosing with 5 mg day-1 and 20 mg day-1 omeprazole on basal and pentagastrin-stimulated gastric acid output was studied in nine duodenal ulcer patients."( Effect of low-dose omeprazole on gastric acid secretion in duodenal ulcer patients.
Crean, GP; McColl, KE; McLauchlan, G, 1988
)
0.84
" The dose which inhibited 50% of the enzyme activity was 1 mg/kg from dose-response profiles obtained 3 h after the drug dosing."( Irreversible inactivation of rat gastric (H+-K+)-ATPase in vivo by omeprazole.
Blakeman, DP; Davis, JP; Im, WB, 1985
)
0.51
" The 40-mg/day dosage produces endoscopic healing slightly more quickly than the 20-mg/day dosage, and the initial endoscopic gradings are of prognostic value."( Healing and relapse of severe peptic esophagitis after treatment with omeprazole.
Beveridge, BR; Dent, J; Gibson, GG; Hetzel, DJ; Laurence, BH; Mackinnon, M; McCarthy, JH; Mitchell, B; Narielvala, FM; Reed, WD, 1988
)
0.51
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of omeprazole are reviewed."( Therapeutic evaluation of omeprazole.
Adams, MH; Kirkwood, CF; Ostrosky, JD, 1988
)
0.79
"The effect of intermittent dosage with omeprazole on basal and pentagastrin stimulated gastric acid secretion and fasting plasma gastrin was assessed in eight duodenal ulcer subjects who were in remission."( Effect of 'weekend therapy' with omeprazole on basal and stimulated acid secretion and fasting plasma gastrin in duodenal ulcer patients.
Angus, PW; Brook, CW; Hewson, EG; Sewell, RB; Shulkes, A; Smallwood, RA; Yeomans, ND, 1988
)
0.83
" Omeprazole in doses lower than 20 mg daily did not suppress pentagastrin-stimulated acid secretion in all subjects 6 h after dosing on the 5th day."( Relationship between reduction of gastric acid secretion and plasma gastrin concentration during omeprazole treatment.
Cederberg, C; Forssell, H; Lind, T; Olausson, M; Olbe, L, 1988
)
1.4
" Daily dosing at high dose levels results in virtually complete 24-hour inhibition of acid secretion in experimental animals."( Pharmacology and toxicology of omeprazole--with special reference to the effects on the gastric mucosa.
Carlsson, E; Larsson, H; Mattsson, H; Ryberg, B; Sundell, G, 1986
)
0.56
" Comparative trials clearly demonstrated that omeprazole 20 to 40 mg administered once daily was significantly more effective than usual dosage regimens of cimetidine and ranitidine in healing duodenal ulcers during 2 to 4 weeks of treatment."( Omeprazole. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in peptic ulcer disease and Zollinger-Ellison syndrome.
Campoli-Richards, DM; Clissold, SP, 1986
)
1.97
" Rats were dosed orally for 4 days with the histamine H2-receptor antagonist ranitidine or the H+,K+-sensitive ATPase inhibitor omeprazole, and examined on day 5 for effects on gastric acid secretion and serum gastrin."( Use of a five-day test to predict the long-term effects of gastric antisecretory agents on serum gastrin in rats.
Katz, LB; Schoof, RA; Shriver, DA, 1987
)
0.48
"This study was aimed to identify an intravenous dosage regime of omeprazole which would sufficiently suppress acid secretion to maintain intragastric pH greater than 4 continuously."( Intravenous omeprazole: effect on 24-hour intragastric pH in duodenal ulcer patients.
Lind, T; Moore, M; Olbe, L, 1986
)
0.89
" The expected antisecretory effect of a particular dosage regimen in patients with duodenal ulcer can be predicted mathematically from data derived from studies in normal volunteers."( Comparison of the effects of gastric antisecretory agents in healthy volunteers and patients with duodenal ulcer.
Burget, DW; Howden, CW; Hunt, RH; Jones, DB, 1986
)
0.27
" Achlorhydria, induced by omeprazole at a dosage of 250-500 times that required for effective acid inhibition in man and animals, therefore resulted in reciprocal changes in gastrin and somatostatin cells."( Gastric regulatory peptides in rats with reduced acid secretion.
Allen, JM; Bishop, AE; Bloom, SR; Carlsson, E; Daly, MJ; Larsson, H; Polak, JM, 1986
)
0.57
" The quantity of gastric ulceration was inversely proportional to the omeprazole dosage with nearly complete prevention of ulceration at the highest dose."( Effect of omeprazole on acute gastric stress ulceration in cervical cord transected rats.
Hardy, KJ; MacLellan, DG; Shulkes, A, 1987
)
0.91
" In the formulation of an oral dosage form of omeprazole the possibilities of dissolution rate limited absorption and preabsorption degradation must be kept in mind."( Development of an oral formulation of omeprazole.
Cederberg, C; Pilbrant, A, 1985
)
0.8
" The effects of different dosage regimens of intravenous omeprazole was compared with placebo."( Intravenous omeprazole rapidly raises intragastric pH.
Hawkey, CJ; Kitchingman, G; Langman, MJ; Reynolds, JR; Smart, HL; Somerville, KW; Walt, RP, 1985
)
0.89
" The peak acid output to pentagastrin measured 24 h after dosing was reduced by 54% on day 3 of the study and by 74% on day 14."( Gastric acid secretion and duodenal ulcer healing during treatment with omeprazole. A Scandinavian Multicentre Study.
, 1984
)
0.5
" After four weeks the ulcer had healed in 41 of the 43 patients who completed the course of treatment; the proportions of patients whose ulcer healed were similar between the four dosage groups."( Omeprazole in duodenal ulceration: acid inhibition, symptom relief, endoscopic healing, and recurrence. Cooperative study.
, 1984
)
1.71
" An oral daily dose of 15 mg omeprazole in humans produced about 80% acid inhibition just after dosage and about 40% 24 hours later."( [Acid secretion inhibition with new mechanisms of action: substituted benzimidazole].
Carlsson, E; Cederberg, C; Helander, H; Lind, T; Olbe, L; Wallmark, B, 1984
)
0.56
" From these results we conclude that, following endoscopic hemostasis of bleeding ulcers, Omeprazol has no advantage over Ranitidin using our dosage regimes."( [Do proton pump inhibitors after endoscopic control of acute ulcer hemorrhage have an advantage over H2 receptor antagonists?].
Barnert, J; Fleischmann, R; Hendrich, H; Prassler, R; Richter, G; Wienbeck, M, 1995
)
0.29
" In this model, duration of action studies showed that significant residual inhibition of acid secretion remained 8 hours after intravenous dosing with SK&F 97574 (producing peak inhibition of 92%)."( Properties of the reversible, K(+)-competitive inhibitor of the gastric (H+/K+)-ATPase, SK&F 97574. II. Pharmacological properties.
Ife, RJ; Leach, C; Parsons, ME; Pope, AJ; Postius, S; Rasmussen, TC; Rushant, B, 1995
)
0.29
" Increasing concentrations of PD 136450 caused a monophasic dose-response curve in contrast to the well-known biphasic amylase release in response to CCK8."( A new CCK-B/gastrin receptor antagonist acts as an agonist on the rat pancreas.
Arnold, R; Eissele, R; Koop, H; Koop, I; Meyer, F; Mössner, J; Patberg, H; Richter, S, 1994
)
0.29
" Lansoprazole granules contained in a standard capsule dosage formulation may be removed and placed directly into applesauce and administered to appropriate patients."( Lansoprazole: an alternative method of administration of a capsule dosage formulation.
Cavanaugh, JH; Chun, AH; Eason, CJ; Shi, HH,
)
0.13
" The optimal dosage and duration of treatment need to be specified."( Lansoprazole versus lansoprazole plus amoxicillin treatment for eradication of Helicobacter pylori in patients with gastric ulcer.
Fujita, N; Hisano, K; Kobayashi, T; Kurokawa, I; Ochiai, T; Sugiyama, T; Yabana, T; Yachi, A, 1995
)
0.29
"To compare pantoprazole 40 mg with omeprazole 20 mg as once daily dosing in the treatment of reflux oesophagitis (grades II and III)."( A double-blind study of pantoprazole and omeprazole in the treatment of reflux oesophagitis: a multicentre trial.
Herz, R; Hölscher, AH; Mössner, J; Schneider, A, 1995
)
0.83
" HP was eradicated by combined treatment with high-dose omeprazole (2 x 40 mg) and amoxicillin (2 x 1,000 mg; n = 27) administered for 10 days (OME + AMX); alternatively, patients were treated with omeprazole monotherapy (OME) using the same dosage (n = 25)."( Two-year follow-up of duodenal ulcer patients treated with omeprazole and amoxicillin.
Bayerdörffer, E; Dirschedl, P; Hatz, R; Höchter, W; Lehn, N; Mannes, GA; Miehlke, S; Ruckdeschel, G; Sommer, A; Weingart, J, 1995
)
0.78
" When lansoprazole was used in dual therapy with amoxicillin, pooled data from four trials employing various dosage schedules showed Hp eradication in 38."( Adjuvant therapy for Helicobacter pylori eradication: role of lansoprazole in clinical studies.
Lamouliatte, H, 1995
)
0.29
" Considerably more work, however, is required to identify the ideal dosage and combination that will give the best eradication rates with the simplest regimen and fewest side effects."( The potential value of lansoprazole in Helicobacter pylori eradication.
Axon, AT, 1995
)
0.29
" These results indicate that lansoprazole at a dosage of 30 mg once daily in the morning produced the most potent inhibition of acid secretion in young Japanese volunteers, compared with famotidine 20 mg twice daily and omeprazole 20 mg once in the morning."( Evaluation of the effect of lansoprazole in suppressing acid secretion using 24-hour intragastric pH monitoring.
Asaka, M; Hokari, K; Takeda, H, 1995
)
0.48
" The inhibitory effect of omeprazole on pepsinogen secretion and its effect on the mRNA level showed similar dose-response relationship, suggesting that pepsinogen secretion and the gene expression are regulated coordinately."( Omeprazole, a proton pump inhibitor, reduces the secretion, synthesis and gene expression of pepsinogen in the rat stomach.
Ichinose, M; Kakei, N; Kurokawa, K; Matsushima, M; Miki, K; Takahashi, K; Tatematsu, M; Tezuka, N; Tsukada, S; Yahagi, N, 1993
)
2.03
" The drug dosage can be reduced, freeing the patient of the adverse reaction, but leaving behind a background activity adequate to produce a therapeutically beneficial effect."( A comparative overview of the adverse effects of antiulcer drugs.
Piper, DW, 1995
)
0.29
" No appreciable change in drug pharmacokinetics was observed during repeated oral dosing of E3810."( Pharmacokinetic properties of E3810, a new proton pump inhibitor, in healthy male volunteers.
Hasegawa, J; Morishita, N; Nakai, H; Ogawa, T; Ohnishi, A; Shimamura, Y; Tomono, Y; Yasuda, S, 1994
)
0.29
"The aim of this study was to identify dosage regimens using intravenous omeprazole and ranitidine that would elevate and consistently maintain intragastric pH > 6 in the first 24 hr of therapy."( Effect of repeated boluses of intravenous omeprazole and primed infusions of ranitidine on 24-hour intragastric pH in healthy human subjects.
Chari, ST; Scheid, J; Singer, MV; Teyssen, S, 1995
)
0.79
" We aimed to see whether the intragastric distribution and gastric retention of a therapeutic agent could be improved, either by giving omeprazole or by dosing after a meal."( Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor.
Atherton, JC; Bracewell, MA; Greaves, JL; Hawkey, CJ; Perkins, AC; Spiller, RC; Sutton, LJ; Washington, N, 1994
)
0.49
" Post-prandial dosing may, therefore, be useful for improving delivery of some anti-Helicobacter agents."( Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor.
Atherton, JC; Bracewell, MA; Greaves, JL; Hawkey, CJ; Perkins, AC; Spiller, RC; Sutton, LJ; Washington, N, 1994
)
0.29
" Amoxycillin dosing was randomised to either 1 h before or 10 min after food."( Amoxycillin capsules with omeprazole for the eradication of Helicobacter pylori. Assessment of the importance of antibiotic dose timing in relation to meals.
Atherton, JC; Hawkey, CK; Hudson, N; Kirk, GE; Spiller, RC, 1994
)
0.59
"Nine patients with non-resected gastrinoma(s) an previously well controlled by omeprazole (mean dosage 75 +/- 12."( [Comparative efficacy of lansoprazole and omeprazole on the intragastric pH measured over a period of 24 hours and on the basal].
Cadiot, G; Forestier, S; Joubert-Collin, M; Mignon, M; Paul, G; Ramdani, A; Ruszniewski, P; Vallot, T, 1994
)
0.78
" Moreover, the inhibitory effect of YM-14471 was more prolonged than those of famotidine and cimetidine by either route, and it was as long as that of omeprazole dosed orally."( Antisecretory effects of a novel and long-lasting histamine H2-receptor antagonist, YM-14471, in rats and dogs.
Fujihara, A; Kamato, T; Miyata, K; Nishida, A; Takeda, M; Yuki, H, 1993
)
0.48
" Cytochrome P-450 1A2 activity was monitored by means of the 13C-[N3-methyl]caffeine breath test and by means of plasma caffeine clearance before omeprazole treatment with 120 mg/day, on the seventh day of dosage and after a 7-day washout."( Specific and dose-dependent enzyme induction by omeprazole in human beings.
Brösicke, H; Heinemeyer, G; Roots, I; Rost, KL, 1994
)
0.74
" The YM022 dosage required in this model was much greater than that required in the inhibition of gastric acid."( YM022 [(R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl- 1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea], a potent and selective gastrin/cholecystokinin-B receptor antagonist, prevents gastric and duodenal lesions in rats.
Akuzawa, S; Ito, H; Kamato, T; Kobayashi, A; Miyata, K; Nagakura, Y; Nishida, A; Takinami, Y; Yamano, M; Yuki, H, 1994
)
0.29
" Moreover, if omeprazole is administered at a pharmacologically effective dosage for a short period of time, it may not have serious effects on the ultrastructure of human parietal cells."( The effects of omeprazole on the ultrastructure of gastric parietal cells.
Fujii, T; Kato, S; Naganuma, H; Nakagawa, H; Nakano, K, 1994
)
1
", in the dosage used and in a selected group of patients with gastrointestinal bleeding, is similar."( [The treatment of upper digestive hemorrhage of peptic origin: intravenous ranitidine versus intravenous omeprazole].
Blasco Colmenarejo, MM; Cabot Lozano, A; Caneiro Alcubilla, E; García Molinero, MJ; García-Rayo Somoza, M; Herrero Quirós, C; Pérez Flores, R, 1994
)
0.5
" Antipyrine plasma concentrations were measured without pantoprazole (day 1), on the last day of chronic dosing with pantoprazole (day 12) and 48 hours after the last dose of pantoprazole (day 14) to differentiate between inhibition and induction, respectively."( Pantoprazole lacks interaction with antipyrine in man, either by inhibition or induction.
Bliesath, H; De Mey, C; Hartmann, M; Huber, R; Meineke, I; Steinijans, VW; Wurst, W, 1994
)
0.29
"High-dose once daily oral omeprazole dosing can inhibit acid secretion almost completely but several days elapse before maximum efficacy is established."( Comparison of acid inhibition by either oral high-dose ranitidine or omeprazole.
Abbühl, B; Halter, F; Hurlimann, S; Inauen, W, 1994
)
0.82
" Twenty-eight healthy volunteers were randomly assigned to a 2-week dosing with omeprazole or ranitidine in a double-blind, double-dummy, parallel-group study design."( Comparison of acid inhibition by either oral high-dose ranitidine or omeprazole.
Abbühl, B; Halter, F; Hurlimann, S; Inauen, W, 1994
)
0.75
" Prolonged high-dose histamine H2-receptor dosing compromises the feedback mechanism regulating gastrin release, whilst this is maintained during dosing with omeprazole."( Comparison of acid inhibition by either oral high-dose ranitidine or omeprazole.
Abbühl, B; Halter, F; Hurlimann, S; Inauen, W, 1994
)
0.72
" It is concluded that at the dosage used omeprazole does not increase the rate of oxidative and conjugative reactions involved in the metabolism of phenacetin and paracetamol respectively."( Omeprazole does not enhance the metabolism of phenacetin, a marker of CYP1A2 activity, in healthy volunteers.
Bartoli, A; Cipolla, G; Crema, F; Gatti, G; Perucca, E; Xiaodong, S, 1994
)
2
" The durations of action of cimetidine, ranitidine, and famotidine are similar to the dosage intervals usually chosen (6, 8, and 12 hours, respectively)."( Pharmacokinetics and pharmacodynamics of acid-suppressive agents in patients with gastroesophageal reflux disease.
Goss, TF; Schentag, JJ, 1993
)
0.29
" Tests of gastric acidity, in particular 24-h acidity studies, have provided considerable insight into normal and abnormal gastric physiology, and have largely determined the dosing regimens for the management of acid-peptic diseases."( Gastric acid secretion and intragastric acidity: measurement in health and disease.
Fraser, AG; Pounder, RE, 1993
)
0.29
" Moderate hypergastrinaemia occurs in some patients, especially if an omeprazole dosage of 40 mg/day is needed."( Risk-benefit assessment of omeprazole in the treatment of gastrointestinal disorders.
Creutzfeldt, W, 1994
)
0.82
" A strong dose-response relation was present among cimetidine users."( Risk of gynaecomastia associated with cimetidine, omeprazole, and other antiulcer drugs.
García Rodríguez, LA; Jick, H, 1994
)
0.54
" The area under the concentration curve (AUC) was not affected by dosing over 7 years and was in good agreement with the AUC in humans given a dose of 20 mg omeprazole daily."( Effect of 7 years' daily oral administration of omeprazole to beagle dogs.
Forssell, H; Havu, N; Mattsson, H; Säfholm, C; Sundell, G, 1994
)
0.74
" Our group first performed a dose-response analysis of the efficacy of lansoprazole in reducing basal acid output (BAO) in four patients with severe Zollinger-Ellison syndrome (mean BAO 52 +/- 9 [SD] mmol H+/h) who had previously been treated with a mean omeprazole dosage of 75 mg/day."( Treatment of patients with Zollinger-Ellison syndrome.
Forestier, S; Mignon, M; Pospai, D; Vallot, T; Vatier, J, 1993
)
0.47
" (3) Group C, after healing of DU, 54 patients received a maintenance dosage of cimetidine 400 at night for up to 1 year."( [Study on omeprazole 20 mg twice weekly in prevention of duodenal ulcer relapse].
Bei, L; Chen, SP; Wen, SH, 1993
)
0.69
" Gastric pH and dosing requirements were compared."( Do continuous infusions of omeprazole and ranitidine retain their effect with prolonged dosing?
Merki, HS; Wilder-Smith, CH, 1994
)
0.59
", demonstrating the existence of a dose-response relationship for omeprazole."( Does 40 mg omeprazole daily offer additional benefit over 20 mg daily in patients requiring more than 4 weeks of treatment for symptomatic reflux oesophagitis?
Bate, CM; Booth, SN; Crowe, JP; Hepworth-Jones, B; Richardson, PD; Taylor, MD, 1993
)
0.91
" H2-receptors blocking drugs or gastric acidity buffers were withdrawn for 2 weeks, then omeprazole was administered for 4 weeks at a daily dosage of 20 mg."( Effects of omeprazole therapy on peptic disease and serum gastrin levels in hemodialysis patients. A preliminary study.
Di Maggio, A; Franceschi, M; Loperfido, A; Montemurro, NE; Scatizzi, A, 1993
)
0.9
" The animals were killed at the end of the dosing period, and the stomach was removed and weighed."( Effects of hydrochloric acid on the development of enterochromaffin-like (ECL) cell hyperplasia in the rat stomach induced by omeprazole.
Fujihira, S; Fujii, T; Matsuo, M; Oishi, Y; Tomoi, M, 1993
)
0.49
" A repeated dosing study would be necessary to evaluate the repercussions of the possible accumulation in cirrhotic patients."( Pharmacokinetics of lansoprazole in patients with renal or liver disease of varying severity.
Delhotal-Landes, B; Dellatolas, F; Duchier, J; Flouvat, B; Lemaire, M; Molinie, P, 1993
)
0.29
" A standardized dosage of cyclosporine was given orally, and the duration was calculated for the maximum whole blood level of cyclosporine to be achieved; the dosage/level quotient was calculated."( The influence of gastrointestinal agents on resorption and metabolism of cyclosporine after heart transplantation: experimental and clinical results.
Markewitz, A; Meiser, BM; Muschiol, F; Nollert, G; Pfeiffer, M; Reichart, B; Reichenspurner, H; Uberfuhr, P; Wagner, F,
)
0.13
" No differences in cell cycle distribution of the antrum, body, and fundus were found in the two different dosage groups after 1 month of therapy, considering the synthetic phase (S-phase) of the cell cycle."( Effect of short- and long-term treatment with omeprazole on cell cycle distribution in the gastric mucosa. Results of a flow cytometric study.
Bertolissi, E; Bortoluzzi, F; Cannizzaro, R; Cernigoi, C; Fornasarig, M; Sozzi, M; Toffoli, G; Valentini, M, 1993
)
0.54
" From these data, we conclude that personalized maintenance therapy with omeprazole is the most cost-effective: a dosage of 20 mg/day is extremely effective in maintaining remission, and is therefore most indicated in patients at risk; omeprazole 20 mg/day every-other-day affords better compliance, lower costs and fewer relapses with respect to standard H2-antagonist dosages."( [Evaluation of the cost of maintenance therapy (6 months) with 150 mg ranitidine vs 20 mg omeprazole vs 20 mg omeprazole every other day in duodenal ulcer].
Battaglia, G; Chiozzini, G; De Bona, M; De Boni, M; Di Mario, F; Grasso, GA; Pasquino, M; Saggioro, A; Vianello, F, 1993
)
0.74
" A dose-response curve for omeprazole induction at 24 hr was determined and the EC50 for omeprazole induction of the human CYP1A1 gene was estimated to be 100 microM."( Nuclear uptake of the Ah (dioxin) receptor in response to omeprazole: transcriptional activation of the human CYP1A1 gene.
Quattrochi, LC; Tukey, RH, 1993
)
0.83
" Because it has a long duration of action, lansoprazole can be used to control gastric acid hypersecretion in most patients with Zollinger-Ellison syndrome using a once daily dosing schedule."( Prospective study of efficacy and safety of lansoprazole in Zollinger-Ellison syndrome.
Feigenbaum, K; Gardner, JD; Jensen, RT; Koviack, PD; Maton, PN; Metz, DC; Pisegna, JR; Ringham, GL, 1993
)
0.29
" The prolonged inhibition of gastric acid secretion allows for once-daily dosing in patients with peptic ulcer disease and gastroesophageal reflux, and once- or twice-daily dosing in patients with Zollinger-Ellison syndrome."( Omeprazole: a comprehensive review.
Destache, CJ; Massoomi, F; Savage, J,
)
1.57
"05) was seen during repeated dosing with 40 mg intravenously, while no significant change occurred with the two other doses."( Effect of once daily intravenous and oral omeprazole on 24-hour intragastric acidity in healthy subjects.
Cederberg, C; Lundborg, P; Olbe, L; Röhss, K, 1993
)
0.55
" Our results indicate that the omeprazole dosage to be used in the treatment of Zollinger-Ellison syndrome must be chosen principally on the basis of basal acid secretion determination."( Efficacy of long-term therapy with low doses of omeprazole in the control of gastric acid secretion in Zollinger-Ellison syndrome patients.
Annibale, B; Cassetta, MR; Corleto, V; D'Ambra, G; Delle Fave, G; Ferrua, B; Saggioro, A, 1993
)
0.83
"Seven days of dosing with either 30 mg or 60 mg of lansoprazole were compared with placebo in a double-blind, randomized, three-way cross-over study in 12 male healthy volunteers."( The effects of lansoprazole, 30 or 60 mg daily, on intragastric pH and on endocrine function in healthy volunteers.
Balks, HJ; Damaschke, A; Dammann, HG; Fuchs, W; Hennig, U; Schwarz, JA; Steinhoff, J; von zur Mühlen, A, 1993
)
0.29
" Among the various lansoprazole dosage regimens that have been tested, 30 mg daily for 4 weeks appears to be the optimal regimen to relieve pain rapidly and to heal ulceration in up to 90-95% of patients."( Acute treatment of duodenal ulcer: experience with lansoprazole.
Mignon, M; Vallot, T, 1993
)
0.29
" For patients refractory to these drugs or for which once-a-day dosing is desirable, omeprazole has an advantage."( Antiulcer therapy.
Papich, MG, 1993
)
0.51
" Multiple blood and dialysate samples were collected after dosing and were assayed for lansoprazole and metabolite content via high-performance liquid chromatography."( Pharmacokinetics of lansoprazole in hemodialysis patients.
Cavanaugh, JM; Karol, MD; Machinist, JM, 1995
)
0.29
" Another group of 17 patients with Barrett's oesophagus was treated with an H2-receptor antagonist in standard dosage for 12-36 (mean 23) months."( Long term continuous omeprazole treatment of patients with Barrett's oesophagus.
Cooper, BT; Iqbal, TH; Neumann, CS, 1995
)
0.61
" The omeprazole metabolic ratio may serve the double purpose of phenotyping for CYP2C19 and to individualize dosing in omeprazole-treated patients."( Phenocopies of poor metabolizers of omeprazole caused by liver disease and drug treatment.
Brockmöller, J; Esdorn, F; Roots, I; Rost, KL, 1995
)
1.08
" These observations suggest that a large dosage of OMP suppresses liver regeneration, while FAM appears to have no meaningful effect on regeneration."( The liver regenerative response elicited by antisecretory agents in partially hepatectomized rats: a comparison between omeprazole and famotidine.
Aono, T, 1995
)
0.5
"We estimated fasting and peptone meal stimulated plasma gastrin in nine patients (seven female) with pernicious anaemia and achlorhydria, before and on the final day of 4 weeks' dosing with omeprazole 40 mg daily."( Effect of omeprazole and feeding on plasma gastrin in patients with achlorhydria.
Ardill, JE; Banerjee, S; Beattie, AD; McColl, KE, 1995
)
0.88
"4% in the lansoprazole 15, 30 and 60 mg dosage groups, respectively, and 25."( A comparison of three doses of lansoprazole (15, 30 and 60 mg) and placebo in the treatment of duodenal ulcer. The Lansoprazole Study Group.
Avner, DL; Dorsch, ER; Greski-Rose, PA; Jennings, DE, 1995
)
0.29
" Theophylline area under the plasma concentration-versus-time curve over the 6-h dosing interval decreased slightly (13%) but statistically significantly during lansoprazole coadministration."( Pharmacokinetic interaction between lansoprazole and theophylline.
Cavanaugh, JH; Granneman, GR; Karol, MD; Locke, CS, 1995
)
0.29
"This review provides an updated overview on Helicobacter pylori (HP) trials, focusing on drug dosage and cost:benefit ratio."( The influence of drug dosage on Helicobacter pylori eradication: a cost-effectiveness analysis.
Treiber, G, 1996
)
0.29
" Dosage adjustment is not necessary in patients with impaired renal or hepatic function or in the elderly."( Comparative role of omeprazole in the treatment of gastroesophageal reflux disease.
Hara, DS; Joe, RH; Skoutakis, VA, 1995
)
0.61
" These drawbacks have thus stimulated research aimed at identifying better drug combinations, with a simpler dosage for a shorter period, fewer side-effects, and greater and more consistent efficacy."( Eradication of Helicobacter pylori: omeprazole in combination with antibiotics.
Axon, AT; Moayyedi, P, 1996
)
0.57
"The pharmacology, pharmacokinetics, efficacy, safety, and dosage and administration of lansoprazole and omeprazole are reviewed."( Lansoprazole and omeprazole in the treatment of acid peptic disorders.
Blum, RA, 1996
)
0.85
"Sixteen healthy male subjects underwent two dosing periods."( Twenty-four-hour intragastric pH profiles and pharmacokinetics following single and repeated oral administration of the proton pump inhibitor pantoprazole in comparison to omeprazole.
Bliesath, H; Hartmann, M; Huber, R; Lücker, PW; Lühmann, R; Theiss, U; Wurst, W, 1996
)
0.49
" On the sixth day of dosing they underwent 24-h gastric pH-metry."( The effects of omeprazole 20 and 40 mg twice daily on intragastric acidity in duodenal ulcer patients.
Celle, G; Mansi, C; Mela, GS; Mele, MR; Savarino, V; Vigneri, S; Zentilin, P, 1996
)
0.65
" Both dosing schedules were well tolerated and the patients experienced remarkable symptom relief."( Efficacy and tolerability of pantoprazole 40 mg versus 80 mg in patients with reflux oesophagitis.
Bethke, TD; Botha, JF; Cariem, AK; Eloff, FP; Grundling, HD; Honiball, PJ; Marks, IN; Segal, I; Simjee, AE; Spies, SK; Theron, I; van Rensburg, CJ; van Zyl, JH, 1996
)
0.29
"The 40 mg pantoprazole dosage is comparable to 80 mg in reflux oesophagitis, both in efficacy and tolerability."( Efficacy and tolerability of pantoprazole 40 mg versus 80 mg in patients with reflux oesophagitis.
Bethke, TD; Botha, JF; Cariem, AK; Eloff, FP; Grundling, HD; Honiball, PJ; Marks, IN; Segal, I; Simjee, AE; Spies, SK; Theron, I; van Rensburg, CJ; van Zyl, JH, 1996
)
0.29
" Antipyrine plasma concentrations were measured without pantoprazole (day 1), on the last day of chronic dosing with pantoprazole (day 12) and 48 hours after the last dose of pantoprazole (day 14) to differentiate between inhibition and induction, respectively."( Pantoprazole lacks interaction with antipyrine in man, either by inhibition or induction.
Bliesath, H; De Mey, C; Hartmann, M; Huber, R; Meineke, I; Steinijans, VW; Wurst, W, 1996
)
0.29
"To test our standard dosing regimen in omeprazole treatment of gastro-oesophageal reflux disease (GORD) and to determine whether 'non-responders' could be pinpointed."( Monitoring of omeprazole treatment in gastro-oesophageal reflux disease.
Aggestrup, S; Hage, E; Hendel, J; Hendel, L; Nielsen, OH, 1996
)
0.92
"A reverse dose-response examination using increasing doses of omeprazole."( Monitoring of omeprazole treatment in gastro-oesophageal reflux disease.
Aggestrup, S; Hage, E; Hendel, J; Hendel, L; Nielsen, OH, 1996
)
0.9
" Gastric pH profiles showed a high inter-individual variation; paired statistics, however, revealed a significant impact of dosage timing on the gastric pH profile."( Morning or evening dosage of omeprazole for gastro-oesophageal reflux disease?
Aggestrup, S; Hendel, J; Hendel, L, 1995
)
0.58
"The timing of a 40 mg omeprazole dosage regimen has a clinically significant impact on the 24-h pH profile, and that--by relating to the patient 24-hour oesophageal pH-metry in combination with the patient symptomatology--the timing of this dosage is highly important for therapeutic efficacy."( Morning or evening dosage of omeprazole for gastro-oesophageal reflux disease?
Aggestrup, S; Hendel, J; Hendel, L, 1995
)
0.9
"Morning dosing is usually recommended with proton pump inhibitors, but there are few data from 24-h intragastric acidity studies comparing times of dosing."( Morning versus evening dosing of lansoprazole 30 mg daily on twenty-four-hour intragastric acidity in healthy subjects.
Fraser, AG; Hudson, M; Pounder, RE; Sawyerr, AM; Smith, MS, 1996
)
0.29
"A double-blind, placebo-controlled study was performed on the seventh day of dosing to compare the effects of lansoprazole 30 mg given either in the morning or evening on 24-h intragastric acidity in 32 healthy volunteers."( Morning versus evening dosing of lansoprazole 30 mg daily on twenty-four-hour intragastric acidity in healthy subjects.
Fraser, AG; Hudson, M; Pounder, RE; Sawyerr, AM; Smith, MS, 1996
)
0.29
"The median integrated 24-h intragastric acidity on the seventh day of morning dosing with lansoprazole 30 mg was decreased to 36% of the placebo value, compared with 42% for evening dosing."( Morning versus evening dosing of lansoprazole 30 mg daily on twenty-four-hour intragastric acidity in healthy subjects.
Fraser, AG; Hudson, M; Pounder, RE; Sawyerr, AM; Smith, MS, 1996
)
0.29
"These data favour morning dosing of lansoprazole 30 mg for routine use, but patients with mainly nocturnal symptoms may be best treated by evening dosing."( Morning versus evening dosing of lansoprazole 30 mg daily on twenty-four-hour intragastric acidity in healthy subjects.
Fraser, AG; Hudson, M; Pounder, RE; Sawyerr, AM; Smith, MS, 1996
)
0.29
" Large comparative studies will be needed to define the optimal duration, dose and dosing interval if this combination of drugs is to become competitive."( One-week triple therapy with omeprazole, amoxycillin and clarithromycin for treatment of Helicobacter pylori infection.
el-Zimaity, HM; Genta, RM; Graham, DY; Yousfi, MM, 1996
)
0.59
" Post-prandial dosing with antibiotics prolongs their gastric residence time and improves their intragastric distribution, leading to improved local delivery compared with pre-prandial dosing."( Enhanced eradication of Helicobacter pylori by pre- versus post-prandial amoxycillin suspension with omeprazole: implications for antibiotic delivery.
Atherton, JC; Cullen, DJ; Hawkey, CJ; Kirk, GE; Spiller, RC, 1996
)
0.51
"Rats were dosed with famotidine, omeprazole, or buffer control for 4 weeks."( The effects of omeprazole and famotidine on mucin and PGE2 release in the rat stomach.
Boland, CR; Delbarre, SG; Kraus, E; Yoshimura, K, 1996
)
0.93
" Total glycoprotein synthesis was inhibited at all times by omeprazole, but only after the cessation of dosing with famotidine."( The effects of omeprazole and famotidine on mucin and PGE2 release in the rat stomach.
Boland, CR; Delbarre, SG; Kraus, E; Yoshimura, K, 1996
)
0.89
" Although the administration of omeprazole suspension buffered by NaHCO3 solution did not produce a significant increase in the area under the concentration-time curve (AUC) value compared with non-buffered group, the administration of NaHCO3 buffer immediately after dosing of omeprazole suspension buffered by NaHCO3 caused a significant increase in the AUC value."( Pharmacokinetic evaluation of omeprazole suspension following oral administration in rats: effect of neutralization of gastric acid.
Eto, K; Furuno, K; Gomita, Y; Kawasaki, H; Matsuka, N; Watanabe, K, 1996
)
0.87
"5 mg) to fine-titrate the dosage to obtain optimal antihypertensive effects with minimal adverse effects."( Higher AUCs on oral administration of omeprazole and felodipine in Indian volunteers--are they clinically important?
Gowrishankar, R; Joseph, T, 1996
)
0.57
"The time to maximum inhibition of gastric acidity resulting from repeated oral dosing with lansoprazole 30 mg daily for 7 days was studied in nine healthy male volunteers."( Time to maximum effect of lansoprazole on gastric pH in normal male volunteers.
Bell, NJ; Hunt, RH, 1996
)
0.29
"Twenty-four hour intragastric pH monitoring was performed before treatment and on days 1, 3, 5 and 7 of dosing with lansoprazole."( Time to maximum effect of lansoprazole on gastric pH in normal male volunteers.
Bell, NJ; Hunt, RH, 1996
)
0.29
" Ambulatory 24-h intragastric pH levels were measured before dosing, after the first and fifth doses in each period, and 15 days after each dosing period."( The effects of oral doses of lansoprazole and omeprazole on gastric pH.
Buchi, KN; Jennings, DE; Karol, MD; Ringham, GL; Sanders, SW; Tolman, KG, 1997
)
0.56
" A dosage of 30 mg/day produced higher healing rates and equivalent or faster relief of ulcer symptoms than ranitidine or famotidine in patients with duodenal or gastric ulcers and reflux esophagitis."( Lansoprazole: a comprehensive review.
Katona, BG; Zimmermann, AE,
)
0.13
" After 3 and 5 days of dosing the decreases were 53% and 48% with 15 mg lansoprazole, 82% and 82% with 30 mg lansoprazole, 43% and 39% with 20 mg omeprazole, and 76% and 83% with 40 mg omeprazole."( Lansoprazole versus omeprazole: influence on meal-stimulated gastric acid secretion.
Burkhardt, F; Dammann, HG; Fuchs, W; Richter, G; Walter, TA; Wolf, N, 1997
)
0.82
"These results show that after healing of erosive oesophagitis with 4-8 weeks of omeprazole, relapse of oesophagitis and recurrence of reflux symptoms can be prevented in 70% of patients with a maintenance regimen of 20 mg daily, but that intermittent dosing comprising 3 consecutive days each week significantly compromises efficacy."( Daily omeprazole surpasses intermittent dosing in preventing relapse of oesophagitis: a US multi-centre double-blind study.
Behar, J; Berman, R; Dayal, Y; Hirschowitz, BI; Kranz, KR; Peterson, WL; Robinson, M; Roufail, W; Sabesin, SM; Simon, TJ; Sontag, SJ; Tarnawski, A; Wu, WC, 1997
)
1
" Via the gastrostomy, they then received 7 days of dosing with 20 mg omeprazole as intact granules in orange juice."( Nonencapsulated, intact omeprazole granules effectively suppress intragastric acidity when administered via a gastrostomy.
Heinzelmann, EJ; Howden, CW; Sharma, VK; Steinberg, EN; Vasudeva, R, 1997
)
0.84
" In children, data on its use are limited, and problems about the dosage are unresolved."( Omeprazole for severe reflux esophagitis in children.
Bawa, P; De Giacomo, C; Fiocca, R; Franceschi, M; Luinetti, O, 1997
)
1.74
"Individual data from 1154 patients included in five independently conducted, randomized, long-term clinical trials of the efficacy of different dosage regimens of omeprazole, standard ranitidine treatment and placebo for the prevention of relapse of oesophagitis were pooled for this meta-analysis."( Prognostic factors influencing relapse of oesophagitis during maintenance therapy with antisecretory drugs: a meta-analysis of long-term omeprazole trials.
Carlsson, R; Dent, J; Frison, L; Galmiche, JP; Lundell, L, 1997
)
0.7
" Thus, a true dose-response relationship exists between omeprazole and treatment success."( Doubling the omeprazole dose (40 mg b.d. vs. 20 mg b.d.) in dual therapy with amoxycillin increases the cure rate of Helicobacter pylori infection in duodenal ulcer patients.
Beker, JA; Dekker, CP; Farley, A; Jönsson, A; Klör, HU; Labenz, J, 1997
)
0.91
" Increases in median pH over 24 h were observed in all subjects with both dosage regimens."( Morning and evening administration of pantoprazole: a study to compare the effect on 24-hour intragastric pH.
Lühmann, R; Müssig, S; Schneider, A; Witzel, L, 1997
)
0.3
"The study supports the recommendation of a once-daily morning dosage regimen of pantoprazole 40 mg in the treatment of acid-related diseases."( Morning and evening administration of pantoprazole: a study to compare the effect on 24-hour intragastric pH.
Lühmann, R; Müssig, S; Schneider, A; Witzel, L, 1997
)
0.3
"To evaluate the effect of omeprazole on the pharmacokinetics of metronidazole and hydroxymetronidazole in plasma, gastric juice and saliva following intravenous infusion or oral dosing of metronidazole."( The effect of omeprazole on the pharmacokinetics of metronidazole and hydroxymetronidazole in human plasma, saliva and gastric juice.
Barrett, DA; Goddard, AF; Jessa, MJ; Shaw, PN; Spiller, RC, 1997
)
0.96
"This study examined the dose-response effects of the new proton-pump inhibitor rabeprazole on oesophageal and gastric pH in patients with gastro-oesophageal reflux disease."( Effects of oral rabeprazole on oesophageal and gastric pH in patients with gastro-oesophageal reflux disease.
Greenwood, B; Humphries, TJ; Maton, PN; Robinson, M; Rodriguez, S, 1997
)
0.3
" A dosage was considered effective if reflux time was reduced to < 6%, a number which has been our internal laboratory reference."( Effects of oral rabeprazole on oesophageal and gastric pH in patients with gastro-oesophageal reflux disease.
Greenwood, B; Humphries, TJ; Maton, PN; Robinson, M; Rodriguez, S, 1997
)
0.3
" Ambulatory 24-hour intragastric pH values were monitored in each subject at baseline (2 days before crossover period 1) and again before dosing on day 5 of each of the four crossover treatment periods."( The comparative effects of lansoprazole, omeprazole, and ranitidine in suppressing gastric acid secretion.
Blum, RA; Greski-Rose, PA; Hunt, RH; Karol, MD; Shi, H,
)
0.4
" It produced a rightward shift of the gastrin dose-response curve, consistent with competitive inhibition."( Evaluation of three novel cholecystokinin-B/gastrin receptor antagonists: a study of their effects on rat stomach enterochromaffin-like cell activity.
Ding, XQ; Håkanson, R; Lindström, E, 1997
)
0.3
"Clarithromycin, a new acid stable macrolide antibiotic with proven efficacy against Helicobacter pylori, has been widely incorporated into eradication regimens but its optimal dosage schedule remains controversial."( One week triple therapy for Helicobacter pylori: does high-dose clarithromycin confer additional benefit?
Bhutta, AS; Bindel, H; Cunnane, K; Loane, J; O'Connor, HJ, 1997
)
0.3
" pylori infection and to establish the adequate dosage of a new triple therapy for Japanese patients."( The efficacy and safety of one-week triple therapy with lansoprazole, clarithromycin, and metronidazole for the treatment of Helicobacter pylori infection in Japanese patients.
Ido, K; Kihira, K; Kimura, K; Saifuku, K; Satoh, K; Seki, M; Takimoto, T; Taniguchi, Y; Yoshida, Y, 1997
)
0.3
"This study compared the 24 h intragastric pH profile and bioavailability at repeated dosing conditions of the omeprazole 20 mg enteric-coated tablet versus the 20 mg capsule."( Pharmacokinetics and pharmacodynamics during treatment with the omeprazole 20 mg enteric-coated tablet and 20 mg capsule in asymptomatic duodenal ulcer patients.
Kirdeikis, P; Lastiwka, R; Olofsson, B; Röhss, K; Sinclair, P; Thomson, AB,
)
0.58
"05), confirming a dose-response effect."( A placebo-controlled dose-ranging study of lansoprazole in the management of reflux esophagitis.
Dorsch, E; Earnest, DL; Greski-Rose, PA; Jennings, DE; Jones, J, 1998
)
0.3
" It seems that twice daily omeprazole is no better than single daily dosage and that ornidazole is as effective as metronidazole."( One-week therapy with omeprazole, clarithromycin and metronidazole or ornidazole, followed by 3 weeks' treatment with omeprazole, eradicates Helicobacter pylori equally and heals duodenal ulcer.
Archimandritis, A; Balatsos, V; Davaris, P; Delis, V; Kanellopoulou, E; Manika, Z; Skandalis, N; Souyioultzis, S; Tzivras, M, 1997
)
0.91
"On a randomly selected day the clinical charts of 3685 inpatients were reviewed by a gastroenterologist and data were collected concerning the drug used, its dosage and indications for the prescription."( Are we correctly using the inhibitors of gastric acid secretion and cytoprotective drugs? Results of a multicentre study.
Comin, U; Cortelezzi, C; Curzio, M; Ferrara, A; Ferraris, L; Gullotta, R; Minoli, G; Prada, A; Rocca, F, 1997
)
0.3
" A major part of this sum was spent for patients who needed to increase the initial 20 mg dosage of Omeprazol within 5 years."( [Laparoscopic interventions in gastroesophageal reflux--a cost-benefit analysis].
Freys, SM; Fuchs, KH; Heimbucher, J; Thiede, A; Tigges, H, 1997
)
0.3
" pylori-negative patients, current dosing with a proton-pump inhibitor may result in insufficient acid control for optimal treatment of gastro-oesophageal reflux disease (GORD)."( Is the sensitivity to gastric acid inhibition Helicobacter pylori status-dependent?
Smout, AJ, 1998
)
0.3
" Studies to define the optimal duration, dose, and dosing interval of this combination therapy in Korea are needed."( One-week triple therapy with lansoprazole, clarithromycin, and metronidazole to cure Helicobacter pylori infection in peptic ulcer disease in Korea.
El-Zimaity, HM; Graham, DY; Kim, JG; Osato, MS; Perng, CL, 1998
)
0.3
" Having these information will aid in determining dosage of certain medications to the patients with an inherited abnormality of drug metabolizing enzyme."( [Individualization of drug therapy and pharmacogenetics].
Azuma, J; Yamamoto, I, 1998
)
0.3
" Group II (n = 47) treated with the same drug and dosage for 2 weeks."( [Omeprazole, clarithromycin and amoxicillin therapy for Helicobacter pylori infection].
Bei, L; Chen, S; Chen, Z, 1996
)
1.2
" The two groups were not different in regard to their symptom frequency and severity before therapy, amount of lansoprazole dosage required to eliminate symptoms, length of Barrett's metaplasia, presence of hiatal hernia, lower esophageal sphincter resting tone and length, or esophageal peristaltic function."( Complete elimination of reflux symptoms does not guarantee normalization of intraesophageal acid reflux in patients with Barrett's esophagus.
Ouatu-Lascar, R; Triadafilopoulos, G, 1998
)
0.3
"To assess NSAID-associated ulcer healing during treatment with either standard (20 mg) or high dosage (40 mg) omeprazole."( Omeprazole 20 or 40 mg daily for healing gastroduodenal ulcers in patients receiving non-steroidal anti-inflammatory drugs.
Annibale, B; Capurso, L; Del Veccho Blanco, C; Fusillo, M; Massimo Claar, G; Monaco, S, 1998
)
1.95
"Omeprazole dosing increased serum gastrin 4-fold, ciprofibrate 5-fold, and the combination 24-fold."( Potentiating hypergastrinemic effect by the peroxisome proliferator ciprofibrate and omeprazole in the rat.
Hammer, TA; Sandvik, AK; Waldum, HL, 1998
)
1.97
"Both dosing regimens of omeprazole and lansoprazole significantly increased median gastric pH and percentages of time above pH 4 during the entire 24-h period, night- and daytime, compared to baseline."( Acid-inhibitory effects of omeprazole and lansoprazole in Helicobacter pylori-negative healthy subjects.
Geus, WP; Lamers, CB; Mulder, PG; Nicolai, JJ; Van den Boomgaard, DM, 1998
)
0.9
" Dosage and treatment duration were evaluated, along with the way in which morbidity, self-evaluated health, the demographic pattern and life-style characteristics influence drug prescription."( Antacid (A02A) and antiulcer (A02B) drug prescription patterns: predicting factors, dosage and treatment duration.
Girbes Pelechano, VJ; Llopis-González, A; Morales Suárez-Varela, MM; Pérez-Benajas, MA, 1998
)
0.3
" The effects of a minimum of 2 weeks of dosing with cimetidine, ranitidine and omeprazole were examined."( Omeprazole, ranitidine, and cimetidine have no effect on peak blood ethanol concentrations, first pass metabolism or area under the time-ethanol curve under 'real-life' drinking conditions.
Brown, AS; James, OF, 1998
)
1.97
"These results suggest that, in contrast to cimetidine, the inhibitory effect of omeprazole on AII-stimulated aldosterone production following dosing with furosemide is negligible."( Effect of omeprazole and cimetidine on plasma aldosterone response to angiotensin II.
Fujimura, A; Maeda, A; Sasaki, M, 1998
)
0.93
" Sixty patients received 40 mg of omeprazole twice a day, 1500 mg of amoxicillin three times a day, and 300 mg of rebamipide three times a day (group OAR); the other 60 patients received the same dosage of omeprazole and amoxicillin but no rebamipide for two weeks (group OA)."( Effect of rebamipide on Helicobacter pylori infection in patients with peptic ulcer.
Ando, K; Arakawa, T; Harihara, S; Higuchi, K; Ito, H; Kobayashi, K; Kuroki, T; Nebiki, H; Uchida, T, 1998
)
0.58
"Diclofenac, naproxen, and piroxicam can be administered together with omeprazole 20 mg daily without need for dosage alteration."( Lack of drug-drug interaction between three different non-steroidal anti-inflammatory drugs and omeprazole.
Andersson, T; Bredberg, E; Lagerström, PO; Naesdal, J; Wilson, I, 1998
)
0.75
" Pirenzepine was administered intramuscularly at a dosage of 20 mg/kg twice daily; and lansorprazole, subcutaneously at 50 mg/kg once daily, both every day for 4 weeks."( Effect of pirenzepine on gastric endocrine cell kinetics during lansoprazole administration.
Aoki, T; Gang, C; Kashiwagi, H; Omura, K; Omura, N, 1998
)
0.3
" pylori therapy are those that administer the drug at a dosage of 40 mg/day (in 1 or 2 divided doses) for 7, 10 or 14 days in combination with 2 antibacterial agents."( Omeprazole. A review of its use in Helicobacter pylori infection, gastro-oesophageal reflux disease and peptic ulcers induced by nonsteroidal anti-inflammatory drugs.
Langtry, HD; Wilde, MI, 1998
)
1.74
" The AUCs of (-)-PAN after intravenous and oral dosing of (+)-PAN were 36."( Stereoselective chiral inversion of pantoprazole enantiomers after separate doses to rats.
Masubuchi, N; Tanaka, M; Yamazaki, H, 1998
)
0.3
"In a 1400-bed teaching hospital, an audit (by specially trained personnel) was conducted to monitor inpatient prescribing of omeprazole (1) in preference to H2-antagonists and other drugs according to agreed criteria (Helicobacter pylori eradication, severe reflux esophagitis, rapid ulcer healing deemed urgent because of severe symptoms or complications, high-dose steroid therapy of > or =30 mg/day prednisolone) and (2) appropriateness of intravenous dosing (oral route not feasible or contraindicated)."( Antiulcer drug prescribing in hospital successfully influenced by "immediate concurrent feedback".
Chan, CK; Cheung, E; Ching, TY; Chu, KM; Kong, Y; Kou, M; Kumana, CR; Lam, SK; Seto, WH, 1998
)
0.51
" pylori infection by serology and 13C-urea breath test, were studied on the 1st and 8th day of dosing with either placebo, rabeprazole 20 mg or omeprazole 20 mg, once each morning, in a crossover fashion."( A placebo-controlled trial to assess the effects of 8 days of dosing with rabeprazole versus omeprazole on 24-h intragastric acidity and plasma gastrin concentrations in young healthy male subjects.
Hamilton, MI; Pounder, RE; Sercombe, J; Williams, MP, 1998
)
0.72
" Via the gastrostomy, they then received 7 days of once-daily dosing with 30 mg lansoprazole as intact granules in 3 fl."( The pharmacodynamics of lansoprazole administered via gastrostomy as intact, non-encapsulated granules.
Howden, CW; Sharma, VK; Ugheoke, EA; Vasudeva, R, 1998
)
0.3
"To compare the effect of three different dosing regimens of omeprazole 40 mg daily with regard to suppressing nocturnal gastric acidity and avoiding NAB."( Nocturnal gastric acidity and acid breakthrough on different regimens of omeprazole 40 mg daily.
Castell, DO; Hatlebakk, JG; Katz, PO; Kuo, B, 1998
)
0.77
"3) dosing (P=0."( Nocturnal gastric acidity and acid breakthrough on different regimens of omeprazole 40 mg daily.
Castell, DO; Hatlebakk, JG; Katz, PO; Kuo, B, 1998
)
0.53
"In healthy volunteers, dinner time or split dosing of omeprazole 40 mg daily is significantly more effective than dosing before breakfast in preventing NAB and controlling gastric acidity."( Nocturnal gastric acidity and acid breakthrough on different regimens of omeprazole 40 mg daily.
Castell, DO; Hatlebakk, JG; Katz, PO; Kuo, B, 1998
)
0.78
" Dosing was adjusted by monitoring intragastric pH, and esophagoscopy was repeated after 8-12 weeks of omeprazole treatment."( Histological esophagitis: clinical and histological response to omeprazole in children.
Calenda, KA; Dayal, Y; Mobassaleh, M; Strauss, RS, 1999
)
0.76
" Therefore, impaired CYP2C19 activity combined with partial saturation of omeprazole metabolism during multiple dosing may have contributed to the discrepancy between CYP2C19 genotyping and phenotyping."( Reliability of the omeprazole hydroxylation index for CYP2C19 phenotyping: possible effect of age, liver disease and length of therapy.
Higuchi, S; Ieiri, I; Iimori, E; Kimura, M; Mamiya, K; Otsubo, K; Sakai, T; Urae, A; Wada, Y, 1999
)
0.86
" Further study may permit development of optimal once-daily dosing and enhance eradication rates."( Once-daily therapy for H. pylori infection: a randomized comparison of four regimens.
Cheybani, K; Estrada, R; Laine, L; Neil, G; Smith, S; Trujillo, M; Yeramian, P, 1999
)
0.3
" The suggested methods were used to determine drugs in bulk powder, laboratory-prepared mixtures, and pharmaceutical dosage forms."( Stability-indicating methods for determining omeprazole and octylonium bromide in the presence of their degradation products.
Bebawy, LI; el-Kousy, NM,
)
0.39
" The experiments had a randomized cross-over design with a two-week washout period between dosing regimens."( Effect of clarithromycin and other macrolides on the sulfoxidation and 5-hydroxylation of lansoprazole in dogs.
Arimori, K; Fujii, J; Masa, K; Miyamoto, S; Nakano, M; Nakayama, T, 1999
)
0.3
" One group was dosed with lansoprazole 30 mg at 08."( The effect of Helicobacter pylori eradication on intragastric pH during dosing with lansoprazole or ranitidine.
Mulder, PG; Samsom, M; Smout, AJ; van Herwaarden, MA; van Nispen, CH, 1999
)
0.3
" Pre-treatment with a proton pump inhibitor, higher doses or more frequent dosing may be necessary to increase the cure rate of short duration regimens."( Comparison of two 3-day Helicobacter pylori eradication regimens with a standard 1-week regimen.
Cross, R; Grimley, CE; Illing, RC; Lismore, JR; Loft, DE; Nwokolo, CU; O'sullivan, M; Penny, A; Shebani, M, 1999
)
0.3
"In vitro, we observed the effect of omeprazole at concentrations between 10(-8)-10(-4) M on purified CA I and CA II, and also on isolated gastric mucosa CA IV, renal and pulmonary CA IV activity, using the dose-response relationship."( A new concept regarding the mechanism of action of omeprazole.
Baican, M; Coltau, M; Domuta, G; Puscas, I, 1999
)
0.83
"In vitro omeprazole inhibits pH-dependent purified CA I and CA II and gastric mucosa CA IV according to dose-response relationship."( A new concept regarding the mechanism of action of omeprazole.
Baican, M; Coltau, M; Domuta, G; Puscas, I, 1999
)
0.97
" Through the gastrostomy, they then received 7 days of once-daily dosing with 30 mg lansoprazole as intact granules in orange juice."( Simplified lansoprazole suspension--a liquid formulation of lansoprazole--effectively suppresses intragastric acidity when administered through a gastrostomy.
Howden, CW; Sharma, VK; Vasudeva, R, 1999
)
0.3
"Animal experiments suggest that omeprazole dosing increases shedding of Helicobacter into the gastric lumen, and hence into gastric juice."( The effect of omeprazole dosing on the isolation of Helicobacter pylori from gastric aspirates.
Lawson, AJ; Owen, RJ; Pounder, RE; Sercombe, JC; Slater, E; Williams, MP, 1999
)
0.95
" pylori from 77% of infected subject aspirates before, and 67% of aspirates during dosing with omeprazole."( The effect of omeprazole dosing on the isolation of Helicobacter pylori from gastric aspirates.
Lawson, AJ; Owen, RJ; Pounder, RE; Sercombe, JC; Slater, E; Williams, MP, 1999
)
0.88
" These results indicate that no dosage adjustment of rabeprazole is required in patients with renal dysfunction."( Rabeprazole: pharmacokinetics and tolerability in patients with stable, end-stage renal failure.
Grimes, I; Humphries, TJ; Keane, WF; Swan, SK, 1999
)
0.3
" Therefore, no dosage adjustment is needed when pantoprazole and cisapride are coadministered."( Lack of pharmacokinetic interaction between oral pantoprazole and cisapride in healthy adults.
Ferron, GM; Fruncillo, RJ; Martin, PT; Mayer, PR; Paul, JC; Yacoub, L, 1999
)
0.3
" A once-daily dose of 20 mg has consistently achieved profound decreases in 24-h intragastric acidity in single and repeat dosing studies, in healthy volunteers and patients with either peptic ulcer disease or gastro-oesophageal reflux disease."( Review article: the pharmacology of rabeprazole.
Pounder, RE; Williams, MP, 1999
)
0.3
" These findings suggest that dosage adjustment is not required in these special patient populations."( Review article: the pharmacokinetics of rabeprazole in health and disease.
Hoyumpa, AM; Merritt, GJ; Swan, SK, 1999
)
0.3
" Primary metronidazole resistance may reduce its effectiveness, but an increased daily dosing of metronidazole may partly overcome this problem."( Omeprazole, amoxycillin and metronidazole for the cure of Helicobacter pylori infection.
Bardhan, KD; Bayerdörffer, E; Delchier, JC; Díte, P; Lind, T; Mégraud, F; O'Morain, C; Sipponen, P; Spiller, R; Veldhuyzen van Zanten, S; Zeijlon, L, 1999
)
1.75
" The interindividual response to omeprazole in intragastric pH elevation under the study dosage had insignificant variations to alter the success of eradication."( A three-day course of intravenous omeprazole plus antibiotics for H. pylori-positive bleeding duodenal ulcer.
Chi, CH; Jen, CM; Lin, XZ; Sheu, BS; Yang, HB,
)
0.69
" However, the pharmacokinetic findings suggest that no dosage adjustment is required in these special populations."( Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy.
Lew, EA, 1999
)
0.3
"The selection of agents to treat patients with acid-related gastrointestinal diseases requires knowledge of their efficacy, tolerability, and ease of dosing among individuals with differing disease severities and other baseline characteristics."( Review article: rabeprazole's profile in patients with gastrointestinal diseases.
Barth, J; Humphries, TJ, 1999
)
0.3
" At all measuring points during the 5-day dosing periods, 40 mg pantoprazole proved superior to 20 mg omeprazole in inhibiting meal-stimulated gastric acid secretion."( Pantoprazole versus omeprazole: influence on meal-stimulated gastric acid secretion.
Burkhardt, F; Dammann, HG, 1999
)
0.84
" Thirteen healthy male volunteers received a 320 mg oral dose of gemifloxacin after 4 days of dosing with either omeprazole (40 mg once daily) or matching placebo."( Effect of omeprazole on the pharmacokinetics of oral gemifloxacin in healthy volunteers.
Allen, A; Lewis, A; Vousden, M,
)
0.74
"The objective of this randomized, double-blind, two-period crossover study was to investigate whether concomitant steady-state lansoprazole influences the pharmacokinetics of CYP2C9 substrates using single intravenously dosed phenytoin as a model substrate."( Lack of pharmacokinetic interaction between lansoprazole and intravenously administered phenytoin.
Cavanaugh, JH; Karol, MD; Locke, CS, 1999
)
0.3
"While addition of metronidazole to the omeprazole-amoxycillin combination has been shown to be advantageous, the optimal dosage and drug distribution of the antimicrobials has not been sufficiently evaluated."( Efficacy of two different dosage regimens of omeprazole, amoxycillin and metronidazole for the cure of Helicobacter pylori infection.
Bayerdörffer, E; Burman, CF; Díete, U; Dité, P; Domján, L; Kisfalvi, I; Lonovics, J; Mégraud, F; Pap, A; Sipponen, P; Zeijlon, L, 1999
)
0.83
" The total daily dose, and the choice of twice or three times daily dosing does not seem critical with this regimen."( Efficacy of two different dosage regimens of omeprazole, amoxycillin and metronidazole for the cure of Helicobacter pylori infection.
Bayerdörffer, E; Burman, CF; Díete, U; Dité, P; Domján, L; Kisfalvi, I; Lonovics, J; Mégraud, F; Pap, A; Sipponen, P; Zeijlon, L, 1999
)
0.56
" In this study, we focused on whether 20 mg of rabeprazole is effective in our patient population by comparing that dosage with 40 mg of rabeprazole and 60 mg of lansoprazole."( Efficacy of reduced dosage of rabeprazole in PPI/AC therapy for Helicobacter pylori infection: comparison of 20 and 40 mg rabeprazole with 60 mg lansoprazole.
Miwa, H; Murai, T; Nagahara, A; Ogihara, T; Ohkura, R; Ohta, K; Sato, K; Sato, N; Takei, Y; Yamada, T, 2000
)
0.31
" A prototype oral paste formulation containing either acid-stable omeprazole granules or uncoated omeprazole powder was equipotent when compared to a similar dosage of acid-stable omeprazole granules administered by nasogastric tube."( Comparison of the antisecretory effects of omeprazole when administered intravenously, as acid-stable granules and as an oral paste in horses.
Burrow, JA; Dave, K; Harris, D; Haven, ML; Hickey, GJ; Merritt, AM; Zhang, D, 1999
)
0.8
" The purpose of the 3 studies reported here was to 1) evaluate the evolution of potential effects of omeprazole paste (GastroGard), at a dose of 20 mg/kg bwt/day (5x the recommended dose) for 91 days in mature Thoroughbred horses; 2) evaluate the safety in young horses of omeprazole paste when dosed at 4 mg/kg bwt/day (1x), 12 mg/kg bwt/day (3x) or 20 mg/kg bwt/day (5x) for 91 days in Tennessee walking horse foals; and 3) evaluate the safety of omeprazole paste when dosed at 40 mg/kg bwt/day (10x) for 21 days in mature Thoroughbred horses."( Safety of omeprazole paste in foals and mature horses.
Attebery, DK; Cox, JL; Daurio, C; Plue, RE; Wall, HG; Wallace, DH, 1999
)
0.92
" The results of this study suggest that omeprazole, employing a once daily dosing schedule, is effective at reducing the severity or eliminating gastric ulcers in Thoroughbreds in active race training."( Acceptability of a paste formulation and efficacy of high dose omeprazole in healing gastric ulcers in horses maintained in race training.
Holste, J; Nieto, J; Pollmeier, M; Snyder, JR; Thompson, D; Vatistas, NJ, 1999
)
0.81
" At Day 28, 25 of treated horses continued on this dosing regimen while 25 received a half dose (2 mg/kg bwt once daily) and 25 horses were sham-dosed."( Efficacy of omeprazole paste in the treatment and prevention of gastric ulcers in horses.
Alva, R; Andrews, FM; Bernard, W; Cox, JL; Daurio, CP; Holste, JE; Hughes, FE; Sifferman, RL, 1999
)
0.68
"Two different ultraviolet (UV) spectroscopic methods were developed for determination of Lansoprazole in pharmaceutical dosage forms."( Determination of Lansoprazole in pharmaceutical dosage forms by two different spectroscopic methods.
Ozaltín, N, 1999
)
0.3
") dosage form."( Oral and intravenous dosage forms of pantoprazole are equivalent in their ability to suppress gastric acid secretion in patients with gastroesophageal reflux disease.
Lew, E; Martin, P; Maton, PN; Metz, DC; Paul, J; Pisegna, JR; Pratha, V, 2000
)
0.31
" pantoprazole dosage forms had similar favorable safety and tolerability profiles."( Oral and intravenous dosage forms of pantoprazole are equivalent in their ability to suppress gastric acid secretion in patients with gastroesophageal reflux disease.
Lew, E; Martin, P; Maton, PN; Metz, DC; Paul, J; Pisegna, JR; Pratha, V, 2000
)
0.31
"Pharmacokinetic responses to oral doses of the dipeptide, L-alanyl-glutamine (Ala-Gln), were evaluated after a single, bolus load or an intermittent dosing in normal healthy subjects (n = 8) to find the optimal mode of oral administration."( The pharmacokinetic responses of humans to 20 g of alanyl-glutamine dipeptide differ with the dosing protocol but not with gastric acidity or in patients with acute Dengue fever.
Fürst, P; Klassen, P; Mazariegos, M; Solomons, NW, 2000
)
0.31
"No significant changes in the steady-state theophylline maximum plasma concentration (Cmax), time to Cmax (Tmax), minimum plasma concentration (Cmin), area under the plasma concentration-time curve over the 12-h dosing interval (AUC0-12), or apparent total oral clearance (CL/F) were observed within the two treatment groups when theophylline was administered alone or in combination with lansoprazole or pantoprazole."( Lack of a pharmacokinetic interaction between lansoprazole or pantoprazole and theophylline.
Goldwater, DR; Hunt, RH; Pan, WJ; Pilmer, BL; Zhang, Y, 2000
)
0.31
"1 mmol; a phosphodiasterase inhibitor) were added to the Eppendorf tubes containing the PPIs and AP and dose-response curves were done for each drug after incubating for 5, 10 and 20 min at 37 degrees C and AP accumulation was determined using a scintillation counter."( Comparison of five antisecretory agents acting via gastric H+/K+-ATPase.
Bastaki, SM; Chandranath, I; Garner, A,
)
0.13
" pylori eradication rate with a standard triple therapy regardless of the regimen utilized, the dosage and/or the duration of the therapy used appearing not to be sufficient to eradicate the infection efficiently."( Efficacy of different Helicobacter pylori eradication regimens in patients affected by insulin-dependent diabetes mellitus.
Armuzzi, A; Gasbarrini, A; Gasbarrini, G; Ghirlanda, G; Ojetti, V; Pitocco, D; Pola, P; Silveri, NG, 2000
)
0.31
" Subsequent studies confirmed that multiple daily dosing of histamine-2 receptor antagonists (H2RAs) was mandatory for GERD treatment, with clear dose-response relationships for each agent."( Drugs, bugs, and esophageal pH profiles.
Robinson, M,
)
0.13
"Twenty-four healthy male volunteers were studied on the 7th day of morning dosing with either placebo or rabeprazole 10, 20 or 40 mg in a crossover fashion."( A placebo-controlled study to assess the effects of 7-day dosing with 10, 20 and 40 mg rabeprazole on 24-h intragastric acidity and plasma gastrin in healthy male subjects.
Blanshard, C; Millson, C; Pounder, RE; Sercombe, J; Williams, MP, 2000
)
0.31
" Few data exist to compare the ability of the most-often used proton pump inhibitors, omeprazole and lansoprazole, to control gastric acid at twice-daily dosage regimens."( Gastric acidity and acid breakthrough with twice-daily omeprazole or lansoprazole.
Castell, DO; Hatlebakk, JG; Katz, PO, 2000
)
0.78
" on gastric acidity and the relative ability of each dosage regimen to prevent acid breakthrough."( Gastric acidity and acid breakthrough with twice-daily omeprazole or lansoprazole.
Castell, DO; Hatlebakk, JG; Katz, PO, 2000
)
0.55
" Each dosage regimen was separated by a minimum 7-day period where no medication was administered."( Gastric acidity and acid breakthrough with twice-daily omeprazole or lansoprazole.
Castell, DO; Hatlebakk, JG; Katz, PO, 2000
)
0.55
"Analysis of daily diary data during the first 4 weeks and for the entire 8 weeks of treatment revealed that patients who were treated with either dosage of lansoprazole reported significantly (P<."( Lansoprazole compared with ranitidine for the treatment of nonerosive gastroesophageal reflux disease.
Campbell, DR; Fludas, C; Huang, B; Kahrilas, PJ; Richter, JE, 2000
)
0.31
" On day 5 of each dosing period, 24-h intragastric pH and pharmacokinetic variables were measured."( Esomeprazole provides improved acid control vs. omeprazole In patients with symptoms of gastro-oesophageal reflux disease.
Andersson, T; Hasselgren, G; Holmberg, J; Jonsson, A; Kylebäck, A; Lind, T; Röhss, K; Rydberg, L, 2000
)
1.03
" pylori infection appears to be closely related to the occurrence of nocturnal gastric acid breakthrough during dosing with a proton pump inhibitor."( Helicobacter pylori infection influences nocturnal gastric acid breakthrough.
Adachi, K; Amano, K; Katsube, T; Kawamura, A; Kinoshita, Y; Uchida, Y; Watanabe, M, 2000
)
0.31
"To determine the effect of CYP2C19 genotype status on intragastric pH during dosing with lansoprazole or rabeprazole."( CYP2C19 genotype status and intragastric pH during dosing with lansoprazole or rabeprazole.
Adachi, K; Amano, K; Fukuda, R; Ishihara, S; Katsube, T; Kawamura, A; Kinoshita, Y; Takashima, T; Watanabe, M; Yuki, M, 2000
)
0.31
" On the other hand, the median pH in PMs during lansoprazole dosing was higher than in homo-EMs and hetero-EMs."( CYP2C19 genotype status and intragastric pH during dosing with lansoprazole or rabeprazole.
Adachi, K; Amano, K; Fukuda, R; Ishihara, S; Katsube, T; Kawamura, A; Kinoshita, Y; Takashima, T; Watanabe, M; Yuki, M, 2000
)
0.31
" The dose-response relationship for IY-81149 was also evaluated."( A comparative pharmacodynamic study of IY-81149 versus omeprazole in patients with gastroesophageal reflux disease.
Boileau, F; Cho, KD; Goldwater, R; Jung, WT; Kim, DY; Lee, SM; Park, DW; Periclou, AP, 2000
)
0.55
" Intravenous pantoprazole is especially distinguished in its lack of clinically relevant drug interactions, and it requires no dosage adjustment for patients with renal insufficiency or with mild to moderate hepatic dysfunction."( Potential uses of intravenous proton pump inhibitors to control gastric acid secretion.
Metz, DC, 2000
)
0.31
" Patients with gastric ulcer (GU) or duodenal ulcer (DU) were enrolled in this study; 583 eligible patients (GU, 325; DU, 258) were administered lansoprazole (30 mg/day for 8 weeks for GU, and the same dosage for 6 weeks for DU) as first-line therapy, and a half dose of H2RA as maintenance therapy for 12 months."( Peptic ulcer recurrence during maintenance therapy with H2-receptor antagonist following first-line therapy with proton pump inhibitor.
Asaka, M; Asaki, S; Ashida, K; Harasawa, S; Hoshihara, Y; Kajiyama, G; Kaneko, E; Kobayashi, K; Muto, Y; Nakamura, T; Nakazawa, S; Ogawa, N; Sakaki, N; Takemoto, T; Yao, T, 2000
)
0.31
"The aim of this dose-response study was to compare the effectiveness of 10 mg, 20 mg, and 40 mg of pantoprazole with that of placebo tablets in the healing and symptom relief of gastroesophageal reflux disease associated with erosive esophagitis, and to determine the optimal dose."( Oral pantoprazole for erosive esophagitis: a placebo-controlled, randomized clinical trial. Pantoprazole US GERD Study Group.
Bochenek, W; Richter, JE, 2000
)
0.31
" The oral and IV formulations of pantoprazole are equally potent in inhibiting gastric acid secretion; thus, switching between formulations requires no dosage adjustments."( Clinical experience with pantoprazole in gastroesophageal reflux disease.
Avner, DL, 2000
)
0.31
" Another advantage over the histamine 2 receptor antagonists is that pantoprazole does not require dosage adjustment in patients with renal impairment."( Intravenous pantoprazole: a new tool for acutely ill patients who require acid suppression.
Trépanier, EF, 2000
)
0.31
" The dosage of omeprazole was 50 mg/kg body weight, once daily via gavage."( Effects of omeprazole on ethanol lesions.
Abdel Fattaha, NA; Abdel-Rahman, MS, 2000
)
1.05
" Intravenous pantoprazole has been shown to maintain acid suppression in patients switched from oral PPIs, so no change in dosage is required when switching from one formulation to the other."( Switching between intravenous and oral pantoprazole.
Pisegna, JR, 2001
)
0.31
" However, eradication rates with different dosages and dosing vary, and data on the impact of resistance are sparse."( The HOMER Study: the effect of increasing the dose of metronidazole when given with omeprazole and amoxicillin to cure Helicobacter pylori infection.
Bardhan, K; Bayerdörffer, E; Burman, CF; Delchier, JC; Gromark, P; Hellblom, M; Lind, T; Mégraud, F; Stubberöd, A; Veldhuyzen Van Zanten, SJ; Zeijlon, L, 2000
)
0.53
"Rabeprazole 20 mg in two different dosing schedules is as effective as omeprazole 20 mg QD with regard to efficacy and tolerability in patients with erosive GERD."( Rabeprazole, 20 mg once daily or 10 mg twice daily, is equivalent to omeprazole, 20 mg once daily, in the healing of erosive gastrooesophageal reflux disease.
Cohen, G; Delchier, JC; Humphries, TJ, 2000
)
0.77
" and oral pantoprazole on gastric secretion and may be used to predict effects under other dosage regimens."( Pharmacodynamic modeling of pantoprazole's irreversible effect on gastric acid secretion in humans and rats.
Ferron, GM; Mayer, PR; McKeand, W, 2001
)
0.31
" Instances in which laparoscopic Nissen fundoplication should be considered include: 1) Individuals who are intolerant of proton pump inhibitor therapy because of side effects, 2) When patients are inadequately responsive to proton pump inhibitor therapy even after dosage and dose interval have been optimized, and 3) When a patient desires a permanent solution to their reflux problem that frees them of the need to chronically consume pharmaceuticals."( Management of GERD: medical versus surgical.
Kahrilas, PJ, 2001
)
0.31
"Nasogastric administration of SOS resulted in lower maximum mean +/- SD serum concentrations compared to jejunal/duodenal dosing (0."( A randomized, pharmacokinetic and pharmacodynamic, cross-over study of duodenal or jejunal administration compared to nasogastric administration of omeprazole suspension in patients at risk for stress ulcers.
Metzler, MH; Miedema, BW; Olsen, KM; Phillips, JO; Rangnekar, NJ; Rebuck, JA, 2001
)
0.51
"Patients were divided into 2 groups, one group received Lansoprazole (30 mg) once a day, and amoxycilline (500 mg) three times a day (group I), while the second group received Lansoparazole and amoxycillin in similar dosage with the addition of Roxythromycin (150 mg) twice a day (group II)."( Two weeks triple therapy with lansoprazole, amoxycillin and roxythromycin is better than dual therapy with lansoprazole and amoxycillin for H. pylori infection: a randomised, clinical trial.
Alam, E; Mehdi, I; Qureshi, H, 2000
)
0.31
" A model was applied to multiple-dose data from a crossover study of four dosage regimens of lansoprazole in two groups of normal male subjects."( Pharmacodynamic modeling of lansoprazole using an indirect irreversible response model.
Blum, RA; Jusko, WJ; Krzyzanski, W; Puchalski, TA, 2001
)
0.31
" Any interfering co-medication can pose a challenge to establishing a stable anticoagulant dosage regimen and thus present a serious risk for the patient."( Drug interaction: omeprazole and phenprocoumon.
Enderle, C; Grass, U; Müller, W, 2001
)
0.64
"A total of 23 patients with reflux esophagitis underwent 24-h intragastric and intraesophageal pH-metry after 7, 90, and 180 days of continued dosing with 20 mg of omeprazole once daily before breakfast."( Stability of gastric secretory inhibition during 6-month treatment with omeprazole in patients with gastroesophageal reflux disease.
Berstad, A; Hatlebakk, JG; Tefera, S, 2001
)
0.74
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of pantoprazole are reviewed."( Pantoprazole.
Poole, P, 2001
)
0.31
" The time of dosing and ingestion of meals may also influence the pharmacokinetics of these agents as well as their ability to suppress gastric acid secretion."( Shortcomings of the first-generation proton pump inhibitors.
Tytgat, GN, 2001
)
0.31
"CYP2C19 genotyping is a very useful method to determine the effective and safe dosage regimen including the selection of the dual and triple therapy in anti-H."( CYP2C19 genotype related effect of omeprazole on intragastric pH and antimicrobial stability.
Aoyama, N; Hohda, T; Kasuga, M; Kita, T; Komada, F; Okumura, K; Saijoh, Y; Sakaeda, T; Sakai, T; Tanigawara, Y, 2001
)
0.59
" pantoprazole in patients who are unable to swallow solid dosage formulations."( Effects on 24-hour intragastric pH: a comparison of lansoprazole administered nasogastrically in apple juice and pantoprazole administered intravenously.
Chiu, YL; Freston, J; Lukasik, N; Pan, WJ; Täubel, J, 2001
)
0.31
"To investigate the pharmacokinetics, optimal dosage and efficacy of lansoprazole in paediatric patients."( Lansoprazole in children: pharmacokinetics and efficacy in reflux oesophagitis.
Faure, C; Hankard, R; Jacoz-Aigrain, E; Laurence, M; Michaud, L; Mougenot, JF; Navarro, J; Popon, M; Shaghaghi, EK, 2001
)
0.31
" The dosage was doubled in non-responders."( Lansoprazole in children: pharmacokinetics and efficacy in reflux oesophagitis.
Faure, C; Hankard, R; Jacoz-Aigrain, E; Laurence, M; Michaud, L; Mougenot, JF; Navarro, J; Popon, M; Shaghaghi, EK, 2001
)
0.31
"Patients with impaired hepatic function usually require gastric acid-suppressant therapy but are at increased risk for drug interactions and may require dosage adjustments."( Pharmacokinetics of pantoprazole in patients with moderate and severe hepatic dysfunction.
Abell, M; Ferron, GM; Getsy, J; Mayer, P; Noveck, RJ; Paul, J; Pockros, P; Preston, RA; Turner, M, 2001
)
0.31
"This study sought to determine whether dosage adjustment of pantoprazole is required in patients with moderate or severe hepatic impairment by comparing the pharmacokinetic profile of pantoprazole in such patients with that in healthy slow metabolizers of pantoprazole, in whom no dosage adjustment is required."( Pharmacokinetics of pantoprazole in patients with moderate and severe hepatic dysfunction.
Abell, M; Ferron, GM; Getsy, J; Mayer, P; Noveck, RJ; Paul, J; Pockros, P; Preston, RA; Turner, M, 2001
)
0.31
"The pharmacokinetics and tolerability of pantoprazole were similar in patients with moderate hepatic impairment, patients with severe hepatic impairment, and healthy slow metabolizers of pantoprazole, in whom no dosage adjustment is required."( Pharmacokinetics of pantoprazole in patients with moderate and severe hepatic dysfunction.
Abell, M; Ferron, GM; Getsy, J; Mayer, P; Noveck, RJ; Paul, J; Pockros, P; Preston, RA; Turner, M, 2001
)
0.31
"This study was designed to determine the pharmacokinetics and the optimal dosage of intravenous omeprazole in patients younger than 30 months of age."( Intravenous omeprazole in children: pharmacokinetics and effect on 24-hour intragastric pH.
Faure, C; Jacqz-Aigrain, E; Michaud, L; Navarro, J; Popon, M; Shaghaghi, EK; Turck, D, 2001
)
0.91
" Results were further analyzed to compare failure rates based on different dosage regimens."( Proton pump inhibitor resistance in the treatment of laryngopharyngeal reflux.
Amin, MR; Digges, N; Johnson, P; Koufman, JA; Postma, GN, 2001
)
0.31
"Little is known about differences in the disposition kinetics and pharmacological effects on gastrin levels between lansoprazole and rabeprazole given in a repeated dosing scheme with respect to the polymorphic CYP2C19."( Comparison of the kinetic disposition of and serum gastrin change by lansoprazole versus rabeprazole during an 8-day dosing scheme in relation to CYP2C19 polymorphism.
Fukushima, Y; Hasegawa, J; Ieiri, I; Ishizaki, T; Kishimoto, Y; Kitano, M; Momiyama, K; Morisawa, T; Morita, T; Nakagawa, K; Okochi, H; Otsubo, K, 2001
)
0.31
" Five of the homozygous extensive metabolizer subjects underwent the 24-hour intragastric pH monitoring on day 8 of dosing of lansoprazole 30 mg 4 times daily."( Effect of high-dose lansoprazole on intragastic pH in subjects who are homozygous extensive metabolizers of cytochrome P4502C19.
Furuta, T; Ishizaki, T; Ohashi, K; Shirai, N; Xiao, F, 2001
)
0.31
" A genotyping test of CYP2C19 status appears useful for prescribing an optimal dosing scheme of lansoprazole."( Effect of high-dose lansoprazole on intragastic pH in subjects who are homozygous extensive metabolizers of cytochrome P4502C19.
Furuta, T; Ishizaki, T; Ohashi, K; Shirai, N; Xiao, F, 2001
)
0.31
"The acid inhibitory effects of omeprazole and rabeprazole are significantly dependent on the CYP2C19 genotype status, as well as on their intrinsic pharmacokinetic and pharmacodynamic characteristics and dosing schemes."( Effects of CYP2C19 genotypic differences in the metabolism of omeprazole and rabeprazole on intragastric pH.
Chiba, K; Furuta, T; Hanai, H; Ishizaki, T; Kobayashi, K; Kosuge, K; Moriyama, Y; Nakagawa, K; Ohashi, K; Okochi, H; Shirai, N; Takashima, M; Xiao, F, 2001
)
0.84
" No dosage adjustment is necessary in renal and mild to moderate hepatic impairment."( Rabeprazole: an update of its use in acid-related disorders.
Carswell, CI; Goa, KL, 2001
)
0.31
" If the results were still abnormal, the proton pump inhibitor dosage was doubled and 24-h pH-metry was repeated after 20-30 days."( Lansoprazole vs. omeprazole for gastro-oesophageal reflux disease: a pH-metric comparison.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.65
" In all such cases, repeat pH monitoring after doubling the proton pump inhibitor dosage gave normal results."( Lansoprazole vs. omeprazole for gastro-oesophageal reflux disease: a pH-metric comparison.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.65
" Nocturnal acid breakthrough occurs on any dosing regimen of oral proton pump inhibitors."( Over-the-counter H(2)-receptor antagonists do not compromise intragastric pH control with proton pump inhibitors.
Ahmed, F; Castell, DO; Katz, PO; Korn, S; Tutuian, R, 2002
)
0.31
"Assess intragastric acid control on omeprazole, 20 mg, taken every morning, after variable dosing of over-the-counter famotidine, 10 mg."( Over-the-counter H(2)-receptor antagonists do not compromise intragastric pH control with proton pump inhibitors.
Ahmed, F; Castell, DO; Katz, PO; Korn, S; Tutuian, R, 2002
)
0.59
" One EM subject had a very low oral clearance of fluvoxamine after both single and multiple dosing of the drug."( Low daily 10-mg and 20-mg doses of fluvoxamine inhibit the metabolism of both caffeine (cytochrome P4501A2) and omeprazole (cytochrome P4502C19).
Andersson, K; Bertilsson, L; Carrillo, JA; Christensen, M; Dahl, ML; Mihara, K; Ramos, SI; Tybring, G; Yasui-Furokori, N, 2002
)
0.53
" The daily dosage could be influenced by the presence of hiatal hernia."( Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.31
"To assess the lansoprazole daily dosage required to normalize oesophageal acid exposure in patients with and without hiatal hernia."( Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.31
" If the results were still abnormal, the lansoprazole dosage was doubled and 24-h pH-metry was repeated 20-30 days thereafter."( Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.31
"A 30-mg daily dosage of lansoprazole normalized oesophageal acid exposure in 70% of cases, whilst a 60-mg daily dosage was necessary in the remainder: the two groups differed only in the presence of hiatal hernia (28% vs."( Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.31
"Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression in complicated and atypical gastro-oesophageal reflux disease."( Hiatal hernia is the key factor determining the lansoprazole dosage required for effective intra-oesophageal acid suppression.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2002
)
0.31
" Intravenous pantoprazole inhibited acid output in a dose-response fashion, with maximal inhibition (99."( Proton pump activation in stimulated parietal cells is regulated by gastric acid secretory capacity: a human study.
Bochenek, WJ; Ferron, GM; Metz, DC; Paul, J; Pisegna, JR; Soffer, E; Turner, MB, 2002
)
0.31
" Sixty-eight patients received 30 mg of lansoprazole once daily, 500 mg of amoxicillin and 250 mg of metronidazole thrice daily for 2 weeks (LAM group), while the other 67 patients received the same dosage of those agents plus 18,000 tyrosine units of pronase thrice daily for 2 weeks (LAMP group)."( Additive effect of pronase on the efficacy of eradication therapy against Helicobacter pylori.
Akamatsu, T; Gotoh, A; Ikeno, T; Ishida, K; Kaneko, T; Katsuyama, T; Kawakami, Y; Kiyosawa, K; Ota, H; Shimizu, T; Shimodaira, K; Sugiyama, A, 2002
)
0.31
" These patients underwent a 24-hour intragastric pH-metry, measurement of basal acid output and of serum gastrin first while receiving their usual therapy and second after 7 to 10 days of pantoprazole treatment at a mean dosage of 116 mg/day (range: 40-200 mg/day)."( Effect of pantoprazole versus other proton pump inhibitors on 24-hour intragastric pH and basal acid output in Zollinger-Ellison syndrome.
Mignon, M; Ramdani, A; Samoyeau, R, 2002
)
0.31
" This suggests that for stress ulcer prophylaxis, intermittent dosing with an intravenous proton pump inhibitor may be an alternative to high-dose continuous infusions of a histamine-2-receptor antagonist."( Stress-related mucosal disease in the critically ill patient: risk factors and strategies to prevent stress-related bleeding in the intensive care unit.
Steinberg, KP, 2002
)
0.31
"For the long term maintenance treatment of reflux esophagitis several strategies have been proposed with the aim of reducing the daily dosage or the frequency of drug administration."( Daily low-dose versus alternate day full-dose lansoprazole in the maintenance treatment of reflux esophagitis.
Baldi, F; Cappiello, R; Ghersi, S; Morselli-Labate, AM, 2002
)
0.31
" This study was designed to investigate the dosing patterns of patients on on-demand treatment and to compare lansoprazole with omeprazole in this regard."( On-demand treatment in patients with oesophagitis and reflux symptoms: comparison of lansoprazole and omeprazole.
Grove, O; Johnsson, F; Moum, B; Simren, M; Thoring, M; Vilien, M, 2002
)
0.74
" In order to document dosing patterns, the medication was dispensed in bottles supplied with a Medication Event Monitoring System recording date and time the bottles were opened."( On-demand treatment in patients with oesophagitis and reflux symptoms: comparison of lansoprazole and omeprazole.
Grove, O; Johnsson, F; Moum, B; Simren, M; Thoring, M; Vilien, M, 2002
)
0.53
" A dosing pattern was found of an increased intake mornings and evenings and constant intervals between intakes."( On-demand treatment in patients with oesophagitis and reflux symptoms: comparison of lansoprazole and omeprazole.
Grove, O; Johnsson, F; Moum, B; Simren, M; Thoring, M; Vilien, M, 2002
)
0.53
" The present study was undertaken to help predict the optimal dosage of omeprazole for extensive metabolizers in this therapy."( Optimal dose of omeprazole for CYP2C19 extensive metabolizers in anti-Helicobacter pylori therapy: pharmacokinetic considerations.
Aoyama, N; Kasuga, M; Kawahara, Y; Kita, T; Okumura, K; Sakaeda, T; Sakai, T, 2002
)
0.89
" The large variability limited our ability to test for a difference in fat absorption and has significant implication for the use of this test, considered the gold standard, for determining enzyme dosage adequacy."( Ranitidine and omeprazole as adjuvant therapy to pancrelipase to improve fat absorption in patients with cystic fibrosis.
Bowser, E; Francisco, MP; Novak, DA; Sherman, JM; Theriaque, D; Wagner, MH, 2002
)
0.67
" Compliance (as measured by a medication-possession ratio), dosage escalation (> 25 percent of initial dose), and daily average consumption (DACON) were measured."( Impact of proton pump inhibitor utilization patterns on gastroesophageal reflux disease-related costs.
Dodd, S; Durkin, M; Hall, J; Sloan, S, 2002
)
0.31
" Treatment of transformants with various concentrations of rifampicin produced a dose-response curve with maximal induction at 10 microM (5."( A cell-based reporter gene assay for determining induction of CYP3A4 in a high-volume system.
Allen, SW; Raucy, J; Warfe, L; Yueh, MF, 2002
)
0.31
" Drug elimination intervals were at least 9 days between the dosing periods."( Pharmacokinetics of lansoprazole, amoxicillin and clarithromycin after simultaneous and single administration.
Borner, K; Koeppe, P; Kotwas, J; Lode, H; Mainz, D, 2002
)
0.31
" Available data indicate that PPIs appear to have similar potency on a milligram basis, and that omeprazole and lansoprazole are more frequently double dosed than pantoprazole."( The clinical importance of proton pump inhibitor pharmacokinetics.
Thomson, AB; Yacyshyn, BR, 2002
)
0.53
" Awareness and application of this knowledge will improve drug use in clinical practice and provide the physician with further appreciation that standard drug dosing may not be appropriate in all patients."( Pharmacogenetics affects dosing, efficacy, and toxicity of cytochrome P450-metabolized drugs.
Bertino, JS; Nafziger, AN; Rogers, JF, 2002
)
0.31
" By modeling the histamine-induced baseline response simultaneously with active treatment, predictions of the response are possible not only following different dosing regimens of omeprazole, but also following different degrees of histamine stimulation."( Gastric acid secretion in the dog: a mechanism-based pharmacodynamic model for histamine stimulation and irreversible inhibition by omeprazole.
Abelö, A; Eriksson, UG; Gabrielsson, J; Holstein, B; Karlsson, MO, 2002
)
0.71
" Dose-response studies on gastroprotection in stress and indomethacin-induced ulcer and inhibition of pylorus ligation-induced acid secretion indicate that omeprazole significantly blocks gastric lesions at lower dose (2."( A novel antioxidant and antiapoptotic role of omeprazole to block gastric ulcer through scavenging of hydroxyl radical.
Ali, E; Bandyopadhyay, U; Banerjee, RK; Biswas, K; Chattopadhyay, I; Varadaraj, A, 2003
)
0.77
" If the results were improved but still abnormal, the dosage was doubled and pH monitoring was repeated."( Effective intra-oesophageal acid suppression in patients with gastro-oesophageal reflux disease: lansoprazole vs. pantoprazole.
De Micheli, E; Frazzoni, M; Grisendi, A; Savarino, V, 2003
)
0.32
" in combination with amoxicillin and clarithromycin produced Helicobacter pylori eradication rates similar to those obtained using triple therapy involving twice-daily dosing with other proton pump inhibitors."( Review of esomeprazole in the treatment of acid disorders.
Johnson, DA, 2003
)
0.7
" This novel dosage formulation represents an option for patients who have difficulty in swallowing oral agents."( Comparative pharmacokinetics and safety of lansoprazole oral capsules and orally disintegrating tablets in healthy subjects.
Ballard, ED; Chiu, YL; Freston, JW; Mulford, DJ, 2003
)
0.32
" At the discretion of the investigator, the dosage of lansoprazole was increased up to 60 mg daily in children who continued to be symptomatic after 2 weeks of treatment."( Safety of lansoprazole in the treatment of gastroesophageal reflux disease in children.
Fitzgerald, J; Hassall, E; Huang, B; Kane, R; Pilmer, B; Tolia, V, 2002
)
0.31
" At the discretion of the investigator, the dosage of lansoprazole was increased up to 60 mg daily in children who continued to be symptomatic after 2 weeks of treatment."( Efficacy of lansoprazole in the treatment of gastroesophageal reflux disease in children.
Book, L; Ferry, G; Gunasekaran, T; Huang, B; Keith, R; Tolia, V, 2002
)
0.31
" Lansoprazole significantly increased the mean 24-hour intragastric pH and the percentages of time intragastric pH was above 3 and 4 when children were dosed with either 15 or 30 mg according to body weight."( Pharmacokinetics and pharmacodynamics of lansoprazole in children with gastroesophageal reflux disease.
Book, L; Chiu, YL; Gremse, D; Gunasekaran, T; Karol, M; Pan, WJ; Pilmer, B; Tolia, V; Winter, H, 2002
)
0.31
" Adolescents in both dosage groups exhibited reductions from baseline in the percentage of days and nights with heartburn (or other predominant symptom of GERD), the severity of heartburn, the percentage of days antacids were used, and the number of antacid tablets used per day."( Lansoprazole in adolescents with gastroesophageal reflux disease: pharmacokinetics, pharmacodynamics, symptom relief efficacy, and tolerability.
Chiu, YL; Fitzgerald, J; Gremse, D; Gunasekaran, T; Gupta, S; Karol, M; Keith, R; Pan, WJ, 2002
)
0.31
"To compare the effectiveness of two different pantoprazole dosage regimens (20 and 40 mg/day), in controlling symptoms and healing esophageal lesions of patients with mild erosive esophagitis."( Assessment of effectiveness of different dosage regimens of pantoprazole in controlling symptoms and healing esophageal lesions of patients with mild erosive esophagitis.
Brito, EM; Castro, Lde P; Coelho, LG; Moretzsohn, LD; Reis, MS,
)
0.13
"Pantoprazole dosage regimens of 20 mg/day and 40 mg/day provide equivalent effectiveness in controlling symptoms and healing esophageal lesions of mild esophagitis."( Assessment of effectiveness of different dosage regimens of pantoprazole in controlling symptoms and healing esophageal lesions of patients with mild erosive esophagitis.
Brito, EM; Castro, Lde P; Coelho, LG; Moretzsohn, LD; Reis, MS,
)
0.13
" pylori eradication on intragastric acidity and plasma gastrin during dosing with lansoprazole, omeprazole, rabeprazole and placebo."( Eradication of Helicobacter pylori increases nocturnal intragastric acidity during dosing with rabeprazole, omeprazole, lansoprazole and placebo.
Chilton, A; Nwokolo, CU; Pounder, RE; Sercombe, J; Usselmann, B; Williams, MP, 2003
)
0.75
" pylori eradication during dosing with proton pump inhibitors is a drug-class effect, particularly affecting nocturnal acid control."( Eradication of Helicobacter pylori increases nocturnal intragastric acidity during dosing with rabeprazole, omeprazole, lansoprazole and placebo.
Chilton, A; Nwokolo, CU; Pounder, RE; Sercombe, J; Usselmann, B; Williams, MP, 2003
)
0.53
" Gastrin probably plays an important role in gastric tumorgenesis, and long-term dosing with ciprofibrate results in enterochromaffin-like (ECL) cell carcinoids in the oxyntic mucosa of rats."( Antral G cells in rats during dosing with a PPAR alpha agonist: a morphometric and immunocytochemical study.
Bendheim, MØ; Martinsen, TC; Skogaker, NE; Waldum, HL, 2003
)
0.32
"We undertook a broad data review of the efficacy of nine different 7-day triple therapies consisting of a proton pump inhibitor (lansoprazole, pantoprazole, omeprazole) in its standard dosage and two antibiotics."( Recent use of proton pump inhibitor-based triple therapies for the eradication of H pylori: a broad data review.
Beckerling, A; Gatz, G; Ulmer, HJ, 2003
)
0.52
" Furthermore, the data indicate that 1-week treatment with a once-daily dosage is sufficient to ensure adequate diagnosis."( One-week esomeprazole treatment: an effective confirmatory test in patients with suspected gastroesophageal reflux disease.
Edin, R; Falk, A; Hatlebakk, JG; Johnsson, F; Klintenberg, AC; Román, J; Stubberöd, A; Toth, E, 2003
)
0.71
" The method was applied successfully for the analysis of pantoprazole in tablet dosage form."( Determination of pantoprazole by adsorptive stripping voltammetry at carbon paste electrode.
Radi, A, 2003
)
0.32
" However, no significant difference was noted between day 1 and day 4 of dosing within the same genotype groups."( Time-dependent amplified pharmacokinetic and pharmacodynamic responses of rabeprazole in cytochrome P450 2C19 poor metabolizers.
Chern, HD; Lin, CJ; Uang, YS; Wang, TH; Yang, JC, 2003
)
0.32
"Rapid and consistent acid suppression on the first day of dosing may be important in treating acid-related disorders."( Acid inhibition on the first day of dosing: comparison of four proton pump inhibitors.
Blum, AL; Dorta, G; Jornod, P; Pantoflickova, D; Ravic, M, 2003
)
0.32
" According to the dosage regimen the patients were divided into two groups."( [Effectiveness of eradication anti-helicobacter therapy in patients with duodenal ulcer in different drug dosage regimens].
Nurbaev, FE; Orziev, ZM; Rakhimova, GSh, 2003
)
0.32
"Amoxicillin concentrations 2 hours after high dosage were gastric juice > gastric body > antral mucosa > plasma."( Gastric juice, gastric tissue and blood antibiotic concentrations following omeprazole, amoxicillin and clarithromycin triple therapy.
Barrett, DA; Kumagai, N; Nakamura, M; Spiller, RC; Tanaka, T; Tsuchimoto, K; Wibawa, JI, 2003
)
0.55
"Both dosage regimens provided effective antibiotic concentrations in gastric juice at 2 hours."( Gastric juice, gastric tissue and blood antibiotic concentrations following omeprazole, amoxicillin and clarithromycin triple therapy.
Barrett, DA; Kumagai, N; Nakamura, M; Spiller, RC; Tanaka, T; Tsuchimoto, K; Wibawa, JI, 2003
)
0.55
"Omeprazole is frequently used to treat gastroesophageal reflux in infants and children despite the lack of age-specific pharmacokinetic and dosing information in the approved product labeling."( Omeprazole disposition in children following single-dose administration.
Abdel-Rahman, SM; Andersson, T; Gaedigk, A; James, LP; Kearns, GL; Kraynak, RA; Ramabadran, K; van den Anker, JN, 2003
)
3.2
" Plasma concentrations and urinary excretion of lansoprazole and its metabolites, and gastric acid secretion were monitored after dosing on days 1 and 7 of each treatment period."( Age-related differences in the pharmacokinetics and pharmacodynamics of lansoprazole.
Granneman, GR; Hogan, DL; Hussein, Z; Isenberg, JI; Koss, MA; Mukherjee, D; Samara, E, 1993
)
0.29
" Steady state plasma concentrations of lansoprazole were reached after 3 days of dosing with lansoprazole."( Single and multiple dose pharmacokinetics of lansoprazole in elderly subjects.
Cournot, A; Delhotal-Landes, B; Dellatolas, F; Flouvat, B, 1993
)
0.29
" Male Sprague-Dawley rats were dosed with lansoprazole (150 mg/kg/day) or vehicle for 14 days."( Lansoprazole increases testosterone metabolism and clearance in male Sprague-Dawley rats: implications for Leydig cell carcinogenesis.
Coulson, M; Gibson, GG; Graham, M; Hammond, T; Plant, N, 2003
)
0.32
" The optimum assay conditions are investigated and the recovery of the cited drugs from their dosage forms ranges from 97."( Validation of the spectrophotometric determination of omeprazole and pantoprazole sodium via their metal chelates.
Abdel Razeq, SA; El-Abasawy, N; Fouad, MM; Ismail, MM; Salama, F, 2003
)
0.57
" Split dosing of rabeprazole was more effective than the single morning dose for inhibiting nocturnal gastric acid secretion."( Nocturnal gastric acid breakthrough during the administration of rabeprazole and ranitidine in Helicobacter pylori-negative subjects: effects of different regimens.
Adachi, K; Amano, Y; Fujishiro, H; Karim Rumi, MA; Kawamura, A; Kinoshita, Y; Komazawa, Y; Mihara, T; Ono, M; Yuki, M, 2003
)
0.32
" These data suggest that administration of a PPI before the evening meal maximizes acid control and would be the preferred dosing schedule in GERD patients, particularly those with nocturnal symptoms."( Comparison of morning and evening administration of rabeprazole for gastro-oesophageal reflux and nocturnal gastric acid breakthrough in patients with reflux disease: a double-blind, cross-over study.
McCallum, RW; Olyaee, M; Pehlivanov, ND; Sarosiek, I, 2003
)
0.32
"Omeprazole had no clinically relevant effect on voriconazole exposure, suggesting that no voriconazole dosage adjustment is necessary for patients in whom omeprazole therapy is initiated."( Effect of omeprazole on the steady-state pharmacokinetics of voriconazole.
Hamlin, J; Kleinermans, D; Layton, G; Nichols, D; Purkins, L; Tan, K; Wood, N, 2003
)
2.16
" Multicentre randomised controlled studies are needed to better define the efficacy profile, the optimal dosage with respect to the different indications and the safety profile for chronic therapy of proton pump inhibitors in children."( Proton pump inhibitors in children: a review.
Gerarduzzi, T; Marchetti, F; Ventura, A, 2003
)
0.32
" The dosage form is a capsule containing 20 mg of Omeprazole in the form of pellets."( [Therapeutic effect of gastrozolum in stomach ulcers].
Dolgova, NIu; Goncharenko, LS; Kuz'mina, OS; Lopatina, IN; Manannikov, IV; Melik-Ogandzhanian, NB; Serova, TI; Sukhareva, GV; Trubitsina, IE; Tsaregorodtseva, TM; Zarudnaia, SI, 2003
)
0.57
" The use of differential pulse voltammetry for the determination of pantoprazole in pharmaceutical dosage forms and human plasma using a glassy carbon electrode has been examined."( Differential pulse anodic voltammetric determination of pantoprazole in pharmaceutical dosage forms and human plasma using glassy carbon electrode.
Erk, N, 2003
)
0.32
" The voltammetric procedure was applied successfully to give a rapid and precise assay of pantoprazole in a tablet dosage form."( Square-wave adsorptive cathodic stripping voltammetry of pantoprazole.
Radi, A, 2003
)
0.32
"Optimal timing for daily dosing of athletic horses with an effective OME preparation, in order to suppress gastric squamous ulceration, might be 4-8 h prior to a training session."( Effect of GastroGard and three compounded oral omeprazole preparations on 24 h intragastric pH in gastrically cannulated mature horses.
Burrow, JA; Church, M; Ludzia, S; Merritt, AM; Sanchez, LC, 2003
)
0.58
" Therefore, a clear understanding of alternative dosing formulations and related efficacies is key in order for the clinician to select the most appropriate agent and strategy to optimize outcomes and cost-effectiveness for each patient."( Alternative dosing for PPI therapy: rationale and options.
Johnson, DA, 2003
)
0.32
"To achieve more potent and long-lasting acid suppression, different dosage regimens of rabeprazole were compared in relation to the CYP2C19 genotype status."( Rabeprazole 10 mg twice daily is superior to 20 mg once daily for night-time gastric acid suppression.
Horikawa, Y; Inoue, M; Kuroiwa, T; Shimatani, T, 2004
)
0.32
" pylori) positive after gastrectomy for the treatment of gastric cancer, and we determined the difference in amoxicillin dosage between the therapeutic successes and failures."( How to eradicate Helicobacter pylori using amoxicillin and omeprazole in the remnant stomach.
Hasuo, K; Imada, T; Inaba, M; Kabara, T; Kawamoto, M; Ohshima, T; Rino, Y; Shiozawa, M; Takahashi, M; Takanashi, Y; Tokunaga, M; Yoneyama, K; Yoshikawa, T; Yukawa, H,
)
0.37
" The amoxicillin dosage in the therapeutic successes was compared with that in the therapeutic failures, and we found that the dosage was 14."( How to eradicate Helicobacter pylori using amoxicillin and omeprazole in the remnant stomach.
Hasuo, K; Imada, T; Inaba, M; Kabara, T; Kawamoto, M; Ohshima, T; Rino, Y; Shiozawa, M; Takahashi, M; Takanashi, Y; Tokunaga, M; Yoneyama, K; Yoshikawa, T; Yukawa, H,
)
0.37
"We assumed that the optimal dosage of amoxicillin was over 15."( How to eradicate Helicobacter pylori using amoxicillin and omeprazole in the remnant stomach.
Hasuo, K; Imada, T; Inaba, M; Kabara, T; Kawamoto, M; Ohshima, T; Rino, Y; Shiozawa, M; Takahashi, M; Takanashi, Y; Tokunaga, M; Yoneyama, K; Yoshikawa, T; Yukawa, H,
)
0.37
" Each patient had received omeprazole 80 mg bolus loading and 40 mg twice daily for three days (total dosage of 320 mg within 3 days)."( Increased risk of rebleeding of peptic ulcer bleeding in patients with comorbid illness receiving omeprazole infusion.
Cheng, HC; Chuang, CH; Chuang, SA; Kao, AW; Kao, YH; Sheu, BS,
)
0.65
" As patients with comorbid illness had a higher risk of rebleeding, a higher dosage or prolonged duration of omeprazole infusion would be rationally indicated to prevent risk of rebleeding."( Increased risk of rebleeding of peptic ulcer bleeding in patients with comorbid illness receiving omeprazole infusion.
Cheng, HC; Chuang, CH; Chuang, SA; Kao, AW; Kao, YH; Sheu, BS,
)
0.56
" Measurement of the 24-h oesophageal and intragastric pH, gastro-oesophageal reflux disease symptoms and quality of life was performed at baseline and during the last week of each dosing period."( Double-blind, randomized controlled study to assess the effects of lansoprazole 30 mg and lansoprazole 15 mg on 24-h oesophageal and intragastric pH in Chinese subjects with gastro-oesophageal reflux disease.
Chan, AO; Hu, WH; Huang, JQ; Hui, WM; Lai, KC; Lam, CL; Lam, KF; Lam, SK; Wong, BC; Wong, NY; Wong, WM; Xia, HH, 2004
)
0.32
" This dosage was significantly different for duodenal ulcer (40."( [Cost-minimization study on the prescription of intravenous proton pump inhibitors: pantoprazole versus omeprazole].
García González, F; Hedo Aparicio, G; Soler Company, E,
)
0.35
"Trough concentrations of tacrolimus should be monitored closely for optimizing the dosage regimen in patients receiving concomitant lansoprazole."( Lansoprazole-tacrolimus interaction in Japanese transplant recipient with CYP2C19 polymorphism.
Inui, K; Ito, N; Motohashi, H; Ogawa, O; Okuda, M; Takahashi, K; Yamamoto, S; Yonezawa, A, 2004
)
0.32
" In addition, L-OMP is advantageous in its once-a-day dosing and might be an alternative to S-H2RA, especially in Korean patients with MMRE."( [Therapeutic effect of low-dose omeprazole vs. standard-dose ranitidine in mild to moderate reflux esophagitis].
Baik, SK; Cho, MY; Kim, HS; Kim, JM; Kim, JW; Kwon, SO; Lee, DK; Suk, KT, 2004
)
0.61
" At comparable doses, these properties lead to several clinical advantages: higher bioavailability in extensive metabolisers (the majority of patients), lower exposure in poor metabolisers, less interindividual variation and a steeper dose-response curve at steady state resulting in a more pronounced inhibition of gastric acid secretion."( Single-isomer drugs: true therapeutic advances.
Andersson, T, 2004
)
0.32
" Lumiracoxib can, therefore, be administered concurrently with either of these agents without need for lumiracoxib dosage alteration."( Lack of effect of omeprazole or of an aluminium hydroxide/magnesium hydroxide antacid on the pharmacokinetics of lumiracoxib.
Langholff, W; Milosavljev, S; Rordorf, C; Scott, G; Shenouda, M; Vinluan Reynolds, C, 2004
)
0.66
" This dosing route provides an additional, convenient dosing option for lansoprazole."( A novel option for dosing of proton pump inhibitors: dispersion of lansoprazole orally disintegrating tablet in water via oral syringe.
Donnelly, JR; Gremse, DA; Kukulka, MJ; Lee, C; Lloyd, E, 2004
)
0.32
" The proposed method was applied to the determination of rabeprazole in the tablet dosage form."( Voltammetric behaviour of rabeprazole at a glassy carbon electrode and its determination in tablet dosage form.
Abd El-Ghany, N; Radi, A; Wahdan, T, 2004
)
0.32
"Lansoprazole orally disintegrating tablet, which rapidly disintegrates on the tongue or in water, provides a dosing alternative for patients with difficulty in swallowing."( A novel option in proton pump inhibitor dosing: lansoprazole orally disintegrating tablet dispersed in water and administered via nasogastric tube.
Freston, JW; Kukulka, MJ; Lee, C; Lloyd, E, 2004
)
0.32
"The total plasma exposure to lansoprazole was comparable following both dosing regimens; mean AUC values for the lansoprazole orally disintegrating tablet nasogastric dispersion were < or =8."( A novel option in proton pump inhibitor dosing: lansoprazole orally disintegrating tablet dispersed in water and administered via nasogastric tube.
Freston, JW; Kukulka, MJ; Lee, C; Lloyd, E, 2004
)
0.32
" This alternative dosing method may be useful in patients with nasogastric or gastric tubes."( A novel option in proton pump inhibitor dosing: lansoprazole orally disintegrating tablet dispersed in water and administered via nasogastric tube.
Freston, JW; Kukulka, MJ; Lee, C; Lloyd, E, 2004
)
0.32
" Omeprazole was dosed intravenously and orally in a crossover fashion to age-matched CF-KO and wild-type male and female mice."( Altered pharmacokinetics of omeprazole in cystic fibrosis knockout mice relative to wild-type mice.
Ali, SY; Smith, PC; Tallman, MN, 2004
)
1.53
"To compare the effect of esomeprazole 40 mg with lansoprazole 30 mg, omeprazole 20 mg, pantoprazole 40 mg and rabeprazole 20 mg on intragastric pH during single and repeated dosing in four separate studies in patients with symptoms of gastro-oesophageal reflux disorder (GERD)."( Esomeprazole 40 mg provides more effective intragastric acid control than lansoprazole 30 mg, omeprazole 20 mg, pantoprazole 40 mg and rabeprazole 20 mg in patients with gastro-oesophageal reflux symptoms.
Lind, T; Röhss, K; Wilder-Smith, C, 2004
)
1.34
" We aimed to develop optimal dosage regimens for rabeprazole to control nocturnal acidity in relation to cytochrome P450 (CYP) 2C19 genotypes."( Different dosage regimens of rabeprazole for nocturnal gastric acid inhibition in relation to cytochrome P450 2C19 genotype status.
Furuta, T; Hishida, A; Ishizaki, T; Kajimura, M; Ohashi, K; Sakurai, M; Shirai, N; Sugimoto, M, 2004
)
0.32
"We propose that rabeprazole dosage regimens for sufficient acid inhibition are 20 mg once daily for PMs, 20 mg twice daily for heterozygous EMs, and 10 mg 4 times daily for homozygous EMs or heterozygous EMs."( Different dosage regimens of rabeprazole for nocturnal gastric acid inhibition in relation to cytochrome P450 2C19 genotype status.
Furuta, T; Hishida, A; Ishizaki, T; Kajimura, M; Ohashi, K; Sakurai, M; Shirai, N; Sugimoto, M, 2004
)
0.32
" Novel dosage formulations of lansoprazole that may be appropriate for patients with dysphagia include the commercially manufactured lansoprazole strawberry-flavored enteric-coated granules for suspension and lansoprazole orally disintegrating tablets."( Management of acid-related disorders in patients with dysphagia.
Howden, CW, 2004
)
0.32
" The percentage of time that serum concentrations remain above the MIC(90) during the dosing interval (T > MIC(90)) for Streptococcus pyogenes and Staphylococcus aureus associated with the pharmacokinetic profiles was calculated."( A randomized crossover study investigating the influence of ranitidine or omeprazole on the pharmacokinetics of cephalexin monohydrate.
Adejare, A; George, M; Madaras-Kelly, K; May, MP; Michas, P, 2004
)
0.55
" Daytime heartburn, night-time heartburn and regurgitation were significantly better controlled with pantoprazole (with a dose-response at most time-points)."( Pantoprazole provides rapid and sustained symptomatic relief in patients treated for erosive oesophagitis.
Bochenek, WJ; Fraga, PD; Mack, ME; Metz, DC, 2004
)
0.32
"To determine whether an increased dosage of esomeprazole 40 mg twice daily in triple therapy improved the Helicobacter pylori eradication rate for patients with different genotypes of S-mephenytoin 4'-hydroxylase (CYP2C19)."( Esomeprazole 40 mg twice daily in triple therapy and the efficacy of Helicobacter pylori eradication related to CYP2C19 metabolism.
Chen, TW; Cheng, HC; Hunag, SF; Kao, AW; Lu, CC; Sheu, BS; Wu, JJ, 2005
)
1.31
"To determine the efficacy of nasogastric administration of omeprazole suspension in raising the gastric pH >4 in critically ill pediatric patients and to determine the most appropriate dosing regimen for this indication."( Failure of nasogastric omeprazole suspension in pediatric intensive care patients.
Cash, JJ; Haizlip, JA; Lugo, RA; Vernon, DD, 2005
)
0.88
"Continuous gastric pH monitoring was performed during administration and dose titration of omeprazole suspension to achieve the goal of gastric pH >4 for greater than 75% of the dosing interval."( Failure of nasogastric omeprazole suspension in pediatric intensive care patients.
Cash, JJ; Haizlip, JA; Lugo, RA; Vernon, DD, 2005
)
0.86
" Our aim was to study responses to potent acid inhibition by characterizing genome-wide gene expression changes in gastric corpus mucosa in rats dosed with the PPI omeprazole."( Molecular characterization of rat gastric mucosal response to potent acid inhibition.
Fossmark, R; Laegreid, A; Langaas, M; Nørsett, KG; Sandvik, AK; Waldum, HL; Wörlund, S, 2005
)
0.52
" These pharmacokinetic characteristics confirm the suitability of this oral solid dosage form for use in future clinical trials."( Pharmacokinetic profile of the oral direct thrombin inhibitor dabigatran etexilate in healthy volunteers and patients undergoing total hip replacement.
Ahnfelt, L; Dahl, OE; Eriksson, BI; Nehmiz, G; Rathgen, K; Stähle, H; Stangier, J; Svärd, R, 2005
)
0.33
"A concomitant dosage regimen of a histamine 2 receptor antagonist with a proton pump inhibitor (PPI) effectively decreases the incidence of nocturnal acid breakthrough, which is one of the problems encountered when acid-related diseases are treated with a PPI alone."( Comparison of an increased dosage regimen of rabeprazole versus a concomitant dosage regimen of famotidine with rabeprazole for nocturnal gastric acid inhibition in relation to cytochrome P450 2C19 genotypes.
Furuta, T; Hishida, A; Ishizaki, T; Kajimura, M; Nakamura, A; Ohashi, K; Shirai, N; Sugimoto, M, 2005
)
0.33
"The combination regimen of famotidine plus rabeprazole is more effective for nocturnal acid inhibition in homozygous and heterozygous EMs than the increased dosage regimen of rabeprazole."( Comparison of an increased dosage regimen of rabeprazole versus a concomitant dosage regimen of famotidine with rabeprazole for nocturnal gastric acid inhibition in relation to cytochrome P450 2C19 genotypes.
Furuta, T; Hishida, A; Ishizaki, T; Kajimura, M; Nakamura, A; Ohashi, K; Shirai, N; Sugimoto, M, 2005
)
0.33
"To determine the minimal effective dosage of omeprazole oral paste for the prevention of naturally occurring ulcers in horses starting race training."( Efficacy of omeprazole paste for prevention of gastric ulcers in horses in race training.
Alva, R; Bernard, W; Cramer, LG; Doucet, MY; Fleishman, C; Holste, JE; McClure, SR; Sifferman, RL; Vrins, A; White, GW, 2005
)
0.97
" CONCLUSIONS AND CLINICAL RELEVANCE; Results indicated that omeprazole administered at a dosage of 1 mg/kg, PO, every 24 hours for 28 days was effective for prevention of gastric ulcers in horses starting race training."( Efficacy of omeprazole paste for prevention of gastric ulcers in horses in race training.
Alva, R; Bernard, W; Cramer, LG; Doucet, MY; Fleishman, C; Holste, JE; McClure, SR; Sifferman, RL; Vrins, A; White, GW, 2005
)
0.95
"Horses with gastric ulcers were treated with omeprazole at a dosage of 4 mg/kg (1."( Efficacy of omeprazole paste for prevention of recurrence of gastric ulcers in horses in race training.
Alva, R; Bernard, W; Cramer, LG; Fleishman, C; Holste, JE; Hughes, FE; McClure, SR; Sifferman, RL; White, GW, 2005
)
0.97
"Omeprazole oral paste administered at a dosage of 1 mg/kg, PO, every 24 hours for 28 days was effective for prevention of recurrence of gastric ulcers in horses in race training."( Efficacy of omeprazole paste for prevention of recurrence of gastric ulcers in horses in race training.
Alva, R; Bernard, W; Cramer, LG; Fleishman, C; Holste, JE; Hughes, FE; McClure, SR; Sifferman, RL; White, GW, 2005
)
2.15
"Ten normal subjects underwent two 8-day oral dosing regimens with placebo or rabeprazole 20 mg each morning in a randomized, double-blind protocol."( The effect of rabeprazole on regional gastric acidity and the postprandial cardia/gastro-oesophageal junction acid layer in normal subjects: a randomized, double-blind, placebo-controlled study.
Doma, S; Fisher, RS; Parkman, HP; Simonian, HP; Vo, L, 2005
)
0.33
" In all genotype groups, serum gastrin increased during the first 3 months of dosing but stabilized thereafter."( Effect of CYP2C19 polymorphism on the safety and efficacy of omeprazole in Japanese patients with recurrent reflux oesophagitis.
Aoyama, N; Arakawa, T; Chida, N; Fujimoto, K; Hamada, S; Hoshino, E; Inoue, M; Kawahara, Y; Konda, Y; Maekawa, T; Mine, T; Mitachi, Y; Nagai, T; Nakajima, M; Ohkusa, T; Sato, N; Seno, H; Shimatani, T; Tadokoro, K; Yoshida, N, 2005
)
0.57
" Fifty-four gastro-oesophageal reflux disease patients were assigned to treatment with famotidine at a dosage of 20 mg twice daily; or omeprazole, 20 mg once daily, for a period of 8 weeks."( Efficacy of famotidine and omeprazole in healing symptoms of non-erosive gastro-oesophageal reflux disease: randomized-controlled study of gastro-oesophageal reflux disease.
Fujita, F; Itoh, K; Itoh, M; Joh, T; Kataoka, H; Kubota, E; Mori, Y; Nakao, H; Ogasawara, N; Ohara, H; Oshima, T; Sasaki, M; Sobue, S; Tanida, S; Togawa, S; Wada, T; Yamada, T, 2005
)
0.83
"To compare the ability of immediate-release omeprazole with pantoprazole to control nocturnal gastric acidity, when they were dosed once daily and twice daily."( Comparison of the effects of immediate-release omeprazole powder for oral suspension and pantoprazole delayed-release tablets on nocturnal acid breakthrough in patients with symptomatic gastro-oesophageal reflux disease.
Bagin, R; Castell, D; Goldlust, B; Hepburn, B; Major, J, 2005
)
0.85
"Dosed once daily at bedtime, immediate-release omeprazole reduced nocturnal gastric acidity to a degree not observed with once daily dosing of delayed-release proton-pump inhibitors."( Comparison of the effects of immediate-release omeprazole powder for oral suspension and pantoprazole delayed-release tablets on nocturnal acid breakthrough in patients with symptomatic gastro-oesophageal reflux disease.
Bagin, R; Castell, D; Goldlust, B; Hepburn, B; Major, J, 2005
)
0.84
" Lansoprazole was dosed after breakfast and dinner."( Effect of concomitant dosing of famotidine with lansoprazole on gastric acid secretion in relation to CYP2C19 genotype status.
Furuta, T; Hishida, A; Kajimura, M; Nakamura, A; Okudaira, K; Shirai, N; Sugimoto, M, 2005
)
0.33
" For the better PPI-based treatment, doses and dosing schemes of PPIs should be optimized based on CYP2C19 genotype status."( Influence of CYP2C19 pharmacogenetic polymorphism on proton pump inhibitor-based therapies.
Furuta, T; Hishida, A; Ishizaki, T; Nakamura, A; Shirai, N; Sugimoto, M, 2005
)
0.33
"Laryngopharyngeal reflux (LPR) is frequently treated with empiric proton-pump inhibitors (PPI), but the optimal dosing and duration is unknown."( Laryngopharyngeal reflux: prospective cohort study evaluating optimal dose of proton-pump inhibitor therapy and pretherapy predictors of response.
Abelson, TI; Hicks, DM; Khandwala, F; Milstein, C; Park, W; Richter, JE; Vaezi, MF, 2005
)
0.33
" Therefore it is administered at reduced as well as high dosages in eradication therapy for Helicobacter pylori; however, there is incomplete assessment of the efficacy of a reduced dosage of rabeprazole as might be employed in therapy."( Acid-suppressive efficacy of a reduced dosage of rabeprazole: comparison of 10 mg twice daily rabeprazole with 20 mg twice daily rabeprazole, 30 mg twice daily lansoprazole, and 20 mg twice daily omeprazole by 24-hr intragastric pH-metry.
Horikawa, Y; Inoue, M; Kuroiwa, T; Nakamura, M; Shimatani, T; Tazuma, S; Xu, J, 2005
)
0.52
" dosing of rabeprazole."( Lack of predictors of normalization of oesophageal acid exposure in Barrett's oesophagus.
Hall, M; Higbee, A; Mathur, S; Sampliner, RE; Sharma, P; Wani, S; Weston, AP, 2005
)
0.33
" The results of studies comparing the clinical efficacy of different PPI dosage forms and routes of administration, safety considerations, and cost-effectiveness analyses are among the factors to consider when making formulary decisions for this class of drugs."( Proton pump inhibitor formulary considerations in the acutely ill. Part 2: Clinical efficacy, safety, and economics.
Devlin, JW; Olsen, KM; Welage, LS, 2005
)
0.33
" Long-term dosing schedule (high dose or step-down dose) was based on current market data."( Cost-effectiveness comparison of current proton-pump inhibitors to treat gastro-oesophageal reflux disease in the UK.
Brown, RE; Remák, E; Robinson, A; Yuen, C, 2005
)
0.33
" We found out that in the same period she had autonomously increased the dosage of omeprazole to 80 mg/day, due to worsening of dyspepsia."( Gastric pH, sevelamer hydrochloride and omeprazole.
Capitanini, A; Del Corso, C; Gallieni, M; Lupi, A; Osteri, F; Petrone, I; Rossi, A; Straniti, M, 2005
)
0.82
" Administration of immediate-release omeprazole at bedtime results in a rapid and sustained elevation of gastric pH, and seems to provide better night time control of gastric acidity than that observed with conventional morning dosing of delayed-release proton pump inhibitors."( Review of immediate-release omeprazole for the treatment of gastric acid-related disorders.
Castell, D, 2005
)
0.9
" Methods to optimize nocturnal acid control include careful attention to dosing schedule, using higher doses of PPIs, adding an histamine H2-receptor antagonist at bedtime to once or twice daily delayed-release PPI, or using immediate-release omeprazole (Zegerid powder for oral suspension; Santarus, Inc."( Review article: putting immediate-release proton-pump inhibitors into clinical practice--improving nocturnal acid control and avoiding the possible complications of excessive acid exposure.
Katz, PO, 2005
)
0.51
" In humans, once-daily dosing of 5-40 mg of rabeprazole inhibits gastric acid secretion in a dose-dependent manner."( Rabeprazole: the role of proton pump inhibitors in Helicobacter pylori eradication.
Sharara, AI, 2005
)
0.33
" When a single esomeprazole dose and multiple dosing were compared, the low contribution of CYP2C19 to the elimination of esomeprazole decreased further by 50%."( Esomeprazole-induced healing of gastroesophageal reflux disease is unrelated to the genotype of CYP2C19: evidence from clinical and pharmacokinetic data.
Hofmann, U; Klotz, U; Leodolter, A; Malfertheiner, P; Schaeffeler, E; Schwab, M; Treiber, G, 2005
)
1.39
" The setting-specific appropriateness of the IV PPI indication and dosing regimen was determined."( Inappropriate use of intravenous pantoprazole: extent of the problem and successful solutions.
Bates, D; Kaplan, GG; McDonald, D; Panaccione, R; Romagnuolo, J, 2005
)
0.33
" Both indication and dosing regimen were appropriate in 21%."( Inappropriate use of intravenous pantoprazole: extent of the problem and successful solutions.
Bates, D; Kaplan, GG; McDonald, D; Panaccione, R; Romagnuolo, J, 2005
)
0.33
" A therapeutical scheme (omeprazole, metronidazole, amoxicilline) obtained a further pathogenetic substantiation of B type CG patient treatment with additional antioxidant vitamin E use at the dosage of 300 mg/day for three weeks."( [Lipid peroxidation and antioxidant system in treatment dynamics of patients with chronic gastritis].
Postavnyĭ, VE, 2005
)
0.63
"Lansoprazole administered as a 60-mg intravenous bolus followed by 6-mg/h continuous infusion produced intragastric pH effects comparable with those of higher dosage regimens."( Dose-response evaluation of the antisecretory effect of continuous infusion intravenous lansoprazole regimens over 48 h.
Amer, F; Howden, CW; Hunt, B; Kukulka, M; Metz, DC; Samra, N; Vakily, M, 2006
)
0.33
"To compare the effects on intragastric acidity of times of dosing of tenatoprazole, a novel imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life."( Comparison of the effects of fasting morning, fasting evening and fed bedtime administration of tenatoprazole on intragastric pH in healthy volunteers: a randomized three-way crossover study.
Cohen, P; Domagala, F; Ficheux, H; Fiorentini, P; Homerin, M; Taccoen, A; Thomson, AB, 2006
)
0.33
" Rats were dosed daily for 3 days with FLU at 500, 250, 62."( Profiling the hepatic effects of flutamide in rats: a microarray comparison with classical aryl hydrocarbon receptor ligands and atypical CYP1A inducers.
Caguyong, M; Cheng, O; Coe, KJ; Dai, X; He, Y; Nelson, SD; Roberts, CJ; Slatter, JG; Ulrich, RG, 2006
)
0.33
" Pre-meal dosing maximizes efficacy while sub-optimal dose timing may limit efficacy."( Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastro-oesophageal reflux disease.
Gunaratnam, NT; Inadomi, J; Jessup, TP; Lascewski, DP, 2006
)
0.33
"To determine the prevalence of sub-optimal proton pump inhibitor dosing in a community-based gastro-oesophageal reflux disease population."( Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastro-oesophageal reflux disease.
Gunaratnam, NT; Inadomi, J; Jessup, TP; Lascewski, DP, 2006
)
0.33
"One hundred patients on proton pump inhibitors referred for persistent gastro-oesophageal reflux disease symptoms were questioned about their proton pump inhibitor dosing habits and classified as optimal or sub-optimal dosers."( Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastro-oesophageal reflux disease.
Gunaratnam, NT; Inadomi, J; Jessup, TP; Lascewski, DP, 2006
)
0.33
"Forty-six percent dosed optimally."( Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastro-oesophageal reflux disease.
Gunaratnam, NT; Inadomi, J; Jessup, TP; Lascewski, DP, 2006
)
0.33
"In this study, 54% of patients dosed proton pump inhibitors sub-optimally and only 12% dosed in a manner that maximized acid suppression."( Sub-optimal proton pump inhibitor dosing is prevalent in patients with poorly controlled gastro-oesophageal reflux disease.
Gunaratnam, NT; Inadomi, J; Jessup, TP; Lascewski, DP, 2006
)
0.33
" Consequently, higher dosage requirements can be expected among most of the Jordanian Arabics."( Possible interethnic differences in omeprazole pharmacokinetics : comparison of Jordanian Arabs with other populations.
Shilbayeh, S; Tutunji, MF, 2006
)
0.61
" The method could be successfully applied to the determination of pure, laboratory prepared mixtures and pharmaceutical dosage forms."( Reversed-phase high performance liquid chromatographic method for the determination of lansoprazole, omeprazole and pantoprazole sodium sesquihydrate in presence of their Acid-induced degradation products.
El-Bardicy, MG; El-Sherif, ZA; El-Tarras, MF; Mohamed, AO, 2006
)
0.55
" Each treatment was dosed for 3 consecutive days with a washout period of 7 days between dosing periods."( Administration of an alginate based gastric reflux suppressant on the bioavailability of omeprazole.
Baxter, T; Choubey, S; Dettmar, PW; Hampson, FC; Jain, A; Little, SL, 2006
)
0.56
" Because the design, dosage and duration of the treatments were different between the studies, it was not possible to conduct meta-analysis."( Additional bedtime H2-receptor antagonist for the control of nocturnal gastric acid breakthrough: a Cochrane systematic review.
Liu, FC; Pan, T; Wang, YP; Yang, JL, 2006
)
0.33
" Section headings with the least conformity with study references were those related to dosage (57 +/- 28%) and side effects (54 +/- 30%)."( Assessment of prescribing information for generic drugs manufactured in the Middle East and marketed in Saudi Arabia.
Al Haidari, K; Gebran, N,
)
0.13
" Proton pump inhibitors can modify the intragastric release of other drugs from their dosage forms by elevating pH (e."( Pharmacokinetic drug interaction profiles of proton pump inhibitors.
Blume, H; Donath, F; Schug, BS; Warnke, A, 2006
)
0.33
" Patients were randomized double-blindly to taper down or continue a constant dosage of omeprazole for three weeks."( Discontinuation of proton pump inhibitors in patients on long-term therapy: a double-blind, placebo-controlled trial.
Abrahamsson, H; Agerforz, P; Björnsson, E; Jensen, C; Kilander, A; Mattsson, N; Simrén, M, 2006
)
0.56
" Based on the calculated metabolic ratios it could be shown that CYP3A4 plays a major role in kinetics of esomeprozale, particularly after multiple dosing when there is a metabolic shift in favor of the formation of the sulfone."( Clinical impact of CYP2C19 polymorphism on the action of proton pump inhibitors: a review of a special problem.
Klotz, U, 2006
)
0.33
"To compare repeated once daily bedtime dosing of IR-OME, lansoprazole and esomeprazole on nocturnal gastric acidity."( Comparison of the effects of immediate-release omeprazole oral suspension, delayed-release lansoprazole capsules and delayed-release esomeprazole capsules on nocturnal gastric acidity after bedtime dosing in patients with night-time GERD symptoms.
Bagin, RG; Ballard, ED; Checani, GC; Gautille, TC; Hogan, DL; Katz, PO; Koch, FK; Pratha, VS, 2007
)
0.83
" Bedtime dosing with IR-OME may be effective for patients with night-time heartburn."( Comparison of the effects of immediate-release omeprazole oral suspension, delayed-release lansoprazole capsules and delayed-release esomeprazole capsules on nocturnal gastric acidity after bedtime dosing in patients with night-time GERD symptoms.
Bagin, RG; Ballard, ED; Checani, GC; Gautille, TC; Hogan, DL; Katz, PO; Koch, FK; Pratha, VS, 2007
)
0.6
" The oral administration of omeprazole has been shown to be effective in both treating horses with gastric ulceration and at preventing re-occurrence whilst the horses are in training, provided that daily dosing is maintained."( Equine gastric ulcer syndrome in adult horses: a review.
Bell, RJ; Kingston, JK; Mogg, TD, 2007
)
0.63
"Horses at 4 trial locations were allocated into replicates and sham dosed orally (empty syringe) or treated with a paste formulation of omeprazole (1 mg/kg [0."( Effects of short-term light to heavy exercise on gastric ulcer development in horses and efficacy of omeprazole paste in preventing gastric ulceration.
Cramer, LG; Fleishman, C; Holste, JE; McClure, SR; Murray, MJ; Sifferman, R; White, G, 2007
)
0.76
" Moreover, rabeprazole may be administered safely in standard doses with no need to change the dosage of the other pharmaceutical drugs taken simultaneously in nephropathic patients, patients undergoing dialysis and transplanted patients."( [Protonic pump inhibitors in kidney transplant patients: efficacy and safety].
Cianciolo, G; Comai, G; Feliciangeli, G; Stefoni, S, 2007
)
0.34
"To identify the optimal pharmacodynamic dosing regimen for esomeprazole administered intravenously (i."( Suppression of gastric acid with intravenous esomeprazole and omeprazole: results of 3 studies in healthy subjects.
Fjellman, M; Kilhamn, J; Lind, T; Röhss, K; Wilder-Smith, C, 2007
)
0.84
" dosage regimen of 80 + 8 mg/h appeared to be optimal for acid suppression in healthy subjects under study."( Suppression of gastric acid with intravenous esomeprazole and omeprazole: results of 3 studies in healthy subjects.
Fjellman, M; Kilhamn, J; Lind, T; Röhss, K; Wilder-Smith, C, 2007
)
0.6
" The results of this study will be useful for drug dosage recommendations in Colombian mestizos."( Phenotype-genotype analysis of CYP2C19 in Colombian mestizo individuals.
Beltrán, L; Henao, J; Isaza, C; Martínez, JH; Sepúlveda Arias, JC, 2007
)
0.34
" Elevated serum gastrin levels occurred in 73% of children with no statistically significant differences in gastrin level by PPI type, dose, and dosing frequency or treatment duration."( Long-term proton pump inhibitor use in children: a retrospective review of safety.
Boyer, K; Tolia, V, 2008
)
0.35
" For eradication, European, Canadian, and American guidelines recommend a regimen consisting of a proton pump inhibitor, clarithromycin, and metronidazole or amoxicillin dosed twice daily for at least 7 days."( An alternative salvage regimen for Helicobacter pylori-resistant patients with heart failure.
Cantu, M; Ferguson, D; Page, RL, 2008
)
0.35
" Medical charts were reviewed in a subset of patients to gather dosing information."( Proton pump inhibitor utilization patterns in infants.
Bakst, AW; Barron, JJ; Singer, J; Spalding, J; Tan, H, 2007
)
0.34
" These data offer valuable information on current PPI dosing patterns that may be used to design future clinical trials for assessment of gastroesophageal reflux disease regimens and clinical outcomes in the infant population."( Proton pump inhibitor utilization patterns in infants.
Bakst, AW; Barron, JJ; Singer, J; Spalding, J; Tan, H, 2007
)
0.34
" In the presence of omeprazole, nelfinavir area under the concentration-time curve over the dosing interval (AUC(tau)), maximum observed plasma concentration (C(max)), and minimum observed plasma concentration (C(min)) were reduced by an average of 36%, 37%, and 39%, respectively, relative to administration of nelfinavir alone."( Significant decrease in nelfinavir systemic exposure after omeprazole coadministration in healthy subjects.
Crownover, PH; Damle, BD; Fang, AF; Glue, PW; Hewlett, D; LaBadie, RR, 2008
)
0.91
"In this study, the influence of CYP2C19 on both the pharmacokinetics and dynamics in Caucasian subjects after single and repeated dosing has been investigated."( Effect of CYP2C19*2 and *17 mutations on pharmacodynamics and kinetics of proton pump inhibitors in Caucasians.
Franck, PF; Geus, WP; Hunfeld, NG; Kuipers, EJ; Mathot, RA; Mulder, PG; Touw, DJ; van Schaik, RH, 2008
)
0.35
" *1/*2 genotype showed a significant acid-inhibitory effect after repeated dosing with L15 and O10."( Effect of CYP2C19*2 and *17 mutations on pharmacodynamics and kinetics of proton pump inhibitors in Caucasians.
Franck, PF; Geus, WP; Hunfeld, NG; Kuipers, EJ; Mathot, RA; Mulder, PG; Touw, DJ; van Schaik, RH, 2008
)
0.35
" Because of the accelerated temperature conditions during DSC experiments applied in this work, ATR-IR was undertaken to determine whether these results occurred at room temperature for the solid dosage form."( Compatibility studies between mannitol and omeprazole sodium isomers.
Agatonovic-Kustrin, S; Ginic-Markovic, M; Glass, BD; Mangan, M; Markovic, N, 2008
)
0.61
"Comparative studies of proton pump inhibitors (PPIs) have revealed that acid reflux is influenced by PPI treatment, formulations and dosing regimens."( Ninety-six-hour wireless oesophageal pH monitoring following proton pump inhibitor administration in NERD patients.
Brugnera, R; Calabrese, C; Di Febo, G; Gabusi, V; Gionchetti, P; Liguori, G; Rizzello, F; Straforini, G, 2008
)
0.35
"Because of its unique pharmacokinetic properties, immediate-release omeprazole does not need to be dosed before a meal to control intragastric acidity."( Control of 24-hour intragastric acidity with morning dosing of immediate-release and delayed-release proton pump inhibitors in patients with GERD.
Bagin, RG; Ballard, ED; Gautille, TC; Howden, CW; Koch, FK, 2009
)
0.59
"To compare the effects of prebreakfast dosing of immediate-release omeprazole 40 mg capsules, lansoprazole 30 mg capsules, and pantoprazole 40 mg tablets on 24-hour intragastric acidity."( Control of 24-hour intragastric acidity with morning dosing of immediate-release and delayed-release proton pump inhibitors in patients with GERD.
Bagin, RG; Ballard, ED; Gautille, TC; Howden, CW; Koch, FK, 2009
)
0.59
"When dosed in the morning, immediate-release omeprazole provided significantly better control of 24-hour intragastric acidity than lansoprazole and pantoprazole."( Control of 24-hour intragastric acidity with morning dosing of immediate-release and delayed-release proton pump inhibitors in patients with GERD.
Bagin, RG; Ballard, ED; Gautille, TC; Howden, CW; Koch, FK, 2009
)
0.61
" The behavior of pharmaceutical hydrates has become the object of increasing attention over the past decade, primarily due to the potential impact of hydrates on the development process and dosage form performance."( Physico-chemical solid-state characterization of omeprazole sodium: thermal, spectroscopic and crystallinity studies.
Carvalho Filho, MA; Cruz, AP; Lang, KL; Mendes, C; Murakami, FS; Silva, MA, 2009
)
0.61
"A four-part, randomized, crossover study with healthy subjects evaluated the effects of gastric pH, the dosing frequency and prandial state, food consumption timing, and gastric motility on the absorption of posaconazole."( Pharmacokinetics and absorption of posaconazole oral suspension under various gastric conditions in healthy volunteers.
Krishna, G; Ma, L; McLeod, J; Medlock, MM; Moton, A, 2009
)
0.35
" However, this does not appear to be clinically relevant given the usual dosage range and the drug's half-life (approx."( The bioavailability of bromazepam, omeprazole and paracetamol given by nasogastric feeding tube.
Berger-Gryllaki, M; Buclin, T; Pannatier, A; Podilsky, G; Roulet, M; Testa, B, 2009
)
0.63
"Subjects were administered single dosage of 1 capsule of 20 mg of each formulation with 240 ml of water after 10 hs overnight fasting on 2 treatment days separated by one-week washout period."( Pharmacokinetics and bioequivalence of 20 mg omeprazole capsule in 24 healthy Korean male volunteers.
Hwang, KG; Kang, JS; Kim, YS; Lee, MH; Lee, YS; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2009
)
0.61
" He was successfully treated by increasing his dosage of omeprazol (20 mg/day) for two weeks."( Acute gastroduodenal injury after ingestion of diluted herbicide pendimethalin.
Azuhata, H; Katoh, H; Kuwano, H; Tsukada, K, 2009
)
0.35
" In a dose-response study, fecal ANC levels were proportional to the nitrite concentration squared."( Effect of feeding nitrite, ascorbate, hemin, and omeprazole on excretion of fecal total apparent N-nitroso compounds in mice.
Davis, ME; Gaikwad, NW; Lisowyj, MP; Mirvish, SS, 2008
)
0.6
" We conducted a prospective controlled study with the aim of testing whether the vitamin C supplement to the therapy includes lower dosage of clarithromycin could have an acceptable influence on Helicobacter pylori eradication in comparison with routine anti-Helicobacter pylori regimen."( Effect of addition of vitamin C to clarithromycin-amoxicillin-omeprazol triple regimen on Helicobacter pylori eradication.
Derakhshan, F; Kaboli, SA; Mirsattari, D; Sheikhvatan, M; Talaie, R; Zali, MR; Zojaji, H,
)
0.13
"Adding vitamin C might reduce the needed dosage of clarithromycin for eradication of Helicobacter pylori."( Effect of addition of vitamin C to clarithromycin-amoxicillin-omeprazol triple regimen on Helicobacter pylori eradication.
Derakhshan, F; Kaboli, SA; Mirsattari, D; Sheikhvatan, M; Talaie, R; Zali, MR; Zojaji, H,
)
0.13
" The literature suggests three possibilities to explain the inadequacy of the substitution: (a) biphasic metabolism where the raised pH in the stomach may prematurely inactivate the PPI, with an unpredictable effect, (b) differences in acid-resistant coating of the generic products, and (c) influence of multiple dosing of PPIs after several days' use."( [Why some proton pump inhibitors are more equal than others].
Lekkerkerker, JF; Mulder, CJ; Otten, MH, 2009
)
0.35
" As there are specific characteristics of these patients that could alter the pharmacokinetics of the drugs, studies need to be performed to determine the most suitable dose and dosage interval."( Pharmacokinetics of intravenous omeprazole in critically ill paediatric patients.
López-Herce, J; Solana, MJ, 2010
)
0.64
" Twenty-four hours after a 300 mg loading dose of clopidogrel, one group received a dosage of 75 mg/day of clopidogrel and a placebo for 14 days, followed 3 weeks later by the same protocol but with coadministration of 75 mg/day clopidogrel and 20 mg/day omeprazole instead."( Effects of omeprazole on the antiplatelet activity of clopidogrel.
Jeong, JW; Kim, NH; Oh, SK; Park, HY; Rhee, SJ; Yoo, NJ; Yun, KH, 2010
)
0.93
" lansoprazole 15 mg, dosed before breakfast."( Omeprazole-Mg 20.6 mg is superior to lansoprazole 15 mg for control of gastric acid: a comparison of over-the-counter doses of proton pump inhibitors.
Erasala, GN; Gibb, RD; McKean, LA; McRorie, JW; Miner, PB; Ramsey, DL, 2010
)
1.8
" Half of these patients were candidates for switching to the oral dosage form during their hospitalization, while only 36."( Clinical and cost impact of intravenous proton pump inhibitor use in non-ICU patients.
Dimassi, HI; Nasser, SC; Nassif, JG, 2010
)
0.36
"1 mol/l HCl-KCl buffer should be administered orally, 15 min before the dosage form."( Modification of gastric pH in the fasted dog.
Abrahamsson, B; Albery, T; Dressman, J; Polentarutti, B, 2010
)
0.36
" However, as with all drugs, PPIs should be dosed appropriately, and should be reserved for patients with conditions for which there is clear evidence of benefit from therapy."( Editorial: just how "difficult" is it to withdraw PPI treatment?
Howden, CW; Kahrilas, PJ, 2010
)
0.36
"A novel HPTLC method has been developed and validated for quantitative determination of omeprazole (OPZ) in capsule dosage form."( Stability-indicating high-performance thin-layer chromatographic method for quantitative determination of omeprazole in capsule dosage form.
Ahmad, S; Alam, O; Jha, P; Khan, SA; Parveen, R,
)
0.57
"To investigate the efficacy and safety of a new proton pump inhibitor (PPI), ilaprazole (IY-81149) in the treatment of duodenal ulcers and provide some characteristics of the dose-response relationship for later studies."( A new PPI, ilaprazole compared with omeprazole in the treatment of duodenal ulcer: a randomized double-blind multicenter trial.
Hu, H; Lin, S; Wang, L; Xia, J; Zhou, L, 2011
)
0.64
"Four randomized, placebo-controlled, crossover studies were conducted among 282 healthy subjects to investigate whether an interaction exists between clopidogrel (300-mg loading dose/75-mg/day maintenance dose) and the proton-pump inhibitor (PPI) omeprazole (80 mg) when they are administered simultaneously (study 1); whether the interaction, if any, can be mitigated by administering clopidogrel and omeprazole 12 h apart (study 2) or by increasing clopidogrel to 600-mg loading/150-mg/day maintenance dosing (study 3); and whether the interaction applies equally to the PPI pantoprazole (80 mg) (study 4)."( Differential effects of omeprazole and pantoprazole on the pharmacodynamics and pharmacokinetics of clopidogrel in healthy subjects: randomized, placebo-controlled, crossover comparison studies.
Angiolillo, DJ; Bergougnan, L; Cheng, S; Dubar, M; Gibson, CM; Hurbin, F; LaCreta, FP; Nicolas, O; Ollier, C; Perrin, L, 2011
)
0.86
" The optimum assay conditions were investigated and the recovery of the drugs from their dosage forms ranged from 99."( Spectrophotometric determination of peptic ulcer sulfur-containing drugs in bulk form and in tablets.
El-Tantawy, AS; Khalil, SM; Mohamed, GG; Nour El-Dien, FA, 2010
)
0.36
" If both Clopidogrel and PPI need to be prescribed, a split dosage regimen of PPI in the morning and clopidogrel in the evening can be recommended."( [Dilemma between gastroprotection and cardiovascular prevention].
Kandulski, A; Malfertheiner, P; Venerito, M, 2010
)
0.36
" The methodology developed was successfully applied to OMP quality control in pure drugs and tablet dosage forms without previous treatment, with good tolerance to common excipient, and a high level of concordance between the nominal and experimental values."( Precision improvement for omeprazole determination through stability evaluation.
Fernández, LP; Masi, AN; Peralta, CM, 2012
)
0.68
" The results indicated that the structures of omeprazole or pantoprazole and kinds of metal ions together affected the binding interaction with BSA, which may have relevant consequence in rationalizing dosage for patients with gastric ulcer."( Differential effects of Cu(II) and Fe(III) on the binding of omeprazole and pantoprazole to bovine serum albumin: toxic effect of metal ions on drugs.
Chen, X; Liu, Y; Peng, M; Shi, S; Zhang, Y, 2011
)
0.87
" Omeprazole produced significant dose-response effects on inhibition of multi-crypt foci (≥4)."( Anti-carcinogenic properties of omeprazole against human colon cancer cells and azoxymethane-induced colonic aberrant crypt foci formation in rats.
Li, Q; Patlolla, JM; Rao, CV; Steele, VE; Zhang, Y, 2012
)
1.57
" Dose-response analyses were performed for various AhR ligands, including TCDD, 3-methylcholanthrene, indirubin, resveratrol, omeprazole, and SP600125."( Novel stably transfected gene reporter human hepatoma cell line for assessment of aryl hydrocarbon receptor transcriptional activity: construction and characterization.
Dvorak, Z; Novotna, A; Pavek, P, 2011
)
0.58
" Pharmacokinetic profiling of orally dosed DPG or DPG with 60% loading of FA (DPG/FA60) was carried out in omeprazole-treated rats as a hypochlorhydric model."( Improved dissolution and pharmacokinetic behavior of dipyridamole formulation with microenvironmental pH-modifier under hypochlorhydria.
Inoue, R; Kawabata, Y; Onoue, S; Taniguchi, C; Wada, K; Yamada, S; Yamashita, K; Yamauchi, Y, 2012
)
0.59
" The significant reduction in the AUC of 5-hydroxyomeprazole after repeated efavirenz dosing suggests induction of sequential metabolism and mixed inductive/inhibitory effects of efavirenz on CYP2C19."( Induction of CYP2C19 and CYP3A activity following repeated administration of efavirenz in healthy volunteers.
Aregbe, AO; Desta, Z; Flockhart, DA; Michaud, V; Ogburn, E; Quigg, TC; Thong, N, 2012
)
0.63
" To compare the effect of once daily bedtime dosing of VECAM 40 and VECAM 20 without food vs OMP 20 mg administered before breakfast on gastric acidity."( The effect of once daily omeprazole and succinic acid (VECAM) vs once daily omeprazole on 24-h intragastric pH.
Atarot, T; Chowers, Y; Fass, R; Pratha, VS, 2012
)
0.68
"To elucidate the stereoselective pharmacokinetics of omeprazole enantiomers and their metabolites after racemic IV dosing because there is little information about the stereoselective metabolism of omeprazole in in vivo study."( Hydroxylation of R(+)- and S(-)-omeprazole after racemic dosing are different among the CYP2C19 genotypes.
Akamine, Y; Shiohira, H; Tateishi, T; Uno, T; Yamada, S; Yasui-Furukori, N, 2012
)
0.91
" Thus, the in vivo disposition of S(-)- and R(+)-omeprazole after racemic dosing may be different among the CYP2C19 genotypes."( Hydroxylation of R(+)- and S(-)-omeprazole after racemic dosing are different among the CYP2C19 genotypes.
Akamine, Y; Shiohira, H; Tateishi, T; Uno, T; Yamada, S; Yasui-Furukori, N, 2012
)
0.92
" The primary outcome measure of recurrent bleeding was compared between the two dosage regimens and between early and late endoscopy."( Effect of intravenous proton pump inhibitor regimens and timing of endoscopy on clinical outcomes of peptic ulcer bleeding.
Ding, J; Fan, D; Gyawali, PC; Liu, L; Liu, N; Wu, K; Yang, Y; Yao, L; Zhang, D; Zhang, H, 2012
)
0.38
" The specificity of the developed methods is investigated by analyzing laboratory prepared mixtures of the three drugs and their combined dosage form."( Comparative study of novel spectrophotometric methods manipulating ratio spectra: an application on pharmaceutical ternary mixture of omeprazole, tinidazole and clarithromycin.
Abdel-Monem Hagazy, M; Lotfy, HM, 2012
)
0.58
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
" In Experiment 2, the same experiment as Experiment 1 was performed, but the dosage of OPZ was 0 or 276 mg/kg."( Liver tumor promoting effect of omeprazole in rats and its possible mechanism of action.
Hayashi, H; Ishii, Y; Mitsumori, K; Morita, R; Shibutani, M; Shimamoto, K; Suzuki, K; Taniai, E, 2012
)
0.66
" Omeprazole shifted the %maximum passive Mg(2+) transport-Mg(2+) concentration curves to the right, and increased the half maximal effective concentration of those dose-response curves, indicating a lower Mg(2+) affinity of the paracellular channel."( Apical acidity decreases inhibitory effect of omeprazole on Mg(2+) absorption and claudin-7 and -12 expression in Caco-2 monolayers.
Krishnamra, N; Thongon, N, 2012
)
1.55
" Two 7-day treatments were separated by 14-day washout periods: (a) PA32540 + clopidogrel (300 mg loading/75 mg maintenance) 10 hours later and (b) synchronous dosing of clopidogrel + EC aspirin (81 mg) + EC omeprazole (40 mg)."( Spaced administration of PA32540 and clopidogrel results in greater platelet inhibition than synchronous administration of enteric-coated aspirin and enteric-coated omeprazole and clopidogrel.
Antonino, M; Bliden, KP; Chai, S; Fort, JG; Gesheff, M; Gesheff, T; Gurbel, PA; Jeong, YH; Shuldiner, A; Tantry, US; Zhang, Y, 2013
)
0.77
"This single-centre, open-label, randomised, two-way crossover study in healthy volunteers compared 7 days of once-daily dosing with PA32540 with 7 days of once-daily EC-ASA 325 mg + EC-omeprazole 40 mg dosed concomitantly."( Intragastric acidity and omeprazole exposure during dosing with either PA32540 (enteric-coated aspirin 325 mg + immediate-release omeprazole 40 mg) or enteric-coated aspirin 325 mg + enteric-coated omeprazole 40 mg - a randomised, phase 1, crossover study
Fort, JG; Miner, PB; Zhang, Y, 2013
)
0.88
"Twice-daily dosing of proton pump inhibitors (PPIs) is used to treat Helicobacter pylori or acid-related diseases, such as gastro-oesophageal reflux disease (GERD) refractory to standard dose of a PPI."( Twice-daily dosing of esomeprazole effectively inhibits acid secretion in CYP2C19 rapid metabolisers compared with twice-daily omeprazole, rabeprazole or lansoprazole.
Furuta, T; Ichikawa, H; Iwaizumi, M; Miyajima, H; Osawa, S; Sahara, S; Sugimoto, K; Sugimoto, M; Umemura, K; Uotani, T; Yamada, T; Yamade, M, 2013
)
0.7
"To compare acid-inhibitory effects of the four PPIs dosed twice daily in relation to CYP2C19 genotype."( Twice-daily dosing of esomeprazole effectively inhibits acid secretion in CYP2C19 rapid metabolisers compared with twice-daily omeprazole, rabeprazole or lansoprazole.
Furuta, T; Ichikawa, H; Iwaizumi, M; Miyajima, H; Osawa, S; Sahara, S; Sugimoto, K; Sugimoto, M; Umemura, K; Uotani, T; Yamada, T; Yamade, M, 2013
)
0.7
"In intermediate and rapid metabolisers of CYP2C19, PPIs dosed twice daily could attain sufficient acid suppression, while in CYP2C19 RMs, esomeprazole 20 mg twice daily caused the strongest inhibition of the four PPIs."( Twice-daily dosing of esomeprazole effectively inhibits acid secretion in CYP2C19 rapid metabolisers compared with twice-daily omeprazole, rabeprazole or lansoprazole.
Furuta, T; Ichikawa, H; Iwaizumi, M; Miyajima, H; Osawa, S; Sahara, S; Sugimoto, K; Sugimoto, M; Umemura, K; Uotani, T; Yamada, T; Yamade, M, 2013
)
0.9
"Co-administration of probe substrates midazolam, pioglitazone, omeprazole, and rosuvastatin following repeat dosing of vercirnon 500 mg BID demonstrated vercirnon had no clinically significant effect on CYP3A4, CYP2C8, CYP2C19 enzyme activity or BCRP or OATP1B1 transporter activity."( Effects of vercirnon on the activity of CYP3A4, CYP2C19 and CYP2C8 enzymes and BCRP and OATP1B1 transporters using probe substrates.
Cargill, A; Haberer, LJ; McCarthy, L; McSherry, I, 2014
)
0.64
"A blinded, randomised, dose-response clinical trial."( A comparison of two doses of omeprazole in the treatment of equine gastric ulcer syndrome: a blinded, randomised, clinical trial.
Hallowell, GD; Sykes, BW; Sykes, KM, 2014
)
0.69
"The results suggest that a dose-response exists for the treatment of both squamous and glandular ulcers."( A comparison of two doses of omeprazole in the treatment of equine gastric ulcer syndrome: a blinded, randomised, clinical trial.
Hallowell, GD; Sykes, BW; Sykes, KM, 2014
)
0.69
" All subjects also received omeprazole 20 mg each morning beginning 4 days prior to the first treatment period and continuing through danirixin dosing in the final treatment period."( The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers.
Ambery, CL; Bloomer, JC; Connolly, P; Lazaar, AL; Miller, BE; Mistry, S; Sanderson, D; Shreeves, T; Smart, K; Smith, R, 2014
)
0.7
" Therefore, sucroferric oxyhydroxide may be administered concomitantly without the need to adjust the dosage regimens of these drugs."( Drug-drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects.
Chong, E; Kalia, V; Willsie, S; Winkle, P, 2014
)
0.63
"A blinded, randomised, dose-response clinical trial."( A comparison of three doses of omeprazole in the treatment of equine gastric ulcer syndrome: A blinded, randomised, dose-response clinical trial.
Hallowell, GD; Sykes, BW; Sykes, KM, 2015
)
0.7
"Pelletized dosage forms can be prepared by different methods which, in general, are time consuming and labor intensive."( Development and evaluation of omeprazole pellets fabricated by sieving-spheronization and extrusion - spheronization process.
Baie, SH; Bukhari, NI; Hay, YK; Karim, S, 2014
)
0.69
"Using pH monitoring, we compared acid inhibition at standard dosage of omeprazole (20 mg, 50 times), lansoprazole (30 mg, 68 times), and rabeprazole (10 mg, 65 times) in Helicobacter pylori-negative healthy young Japanese volunteers."( Comparison of acid inhibition with standard dosages of proton pump inhibitors in relation to CYP2C19 genotype in Japanese.
Furuta, T; Ichikawa, H; Kagami, T; Kodaira, C; Nishino, M; Sahara, S; Shirai, N; Sugimoto, K; Sugimoto, M; Uotani, T, 2014
)
0.64
"Twenty-one patients with primary hypothyroidism who had been using a stabilized levothyroxine dosage for at least one year were selected and randomly assigned to take omeprazole at the dosage of 40 mg or 20 mg per day."( Is it necessary to increase the dose of levothyroxine in patients with hypothyroidism who use omeprazole?
Abi-Abib, Rde C; Vaisman, M, 2014
)
0.82
"Omeprazole in the dosage of 20 or 40 mg/day does not interfere in a clinically relevant manner in the treatment of patients with hypothyroidism that was previously under control."( Is it necessary to increase the dose of levothyroxine in patients with hypothyroidism who use omeprazole?
Abi-Abib, Rde C; Vaisman, M, 2014
)
2.06
" Examination of eradication rates according to CAM dosage revealed an eradication rate of 65."( Changes in the first line Helicobacter pylori eradication rates using the triple therapy-a multicenter study in the Tokyo metropolitan area (Tokyo Helicobacter pylori study group).
Asaoka, D; Ito, M; Kawai, T; Kawakami, K; Kurihara, N; Masaoaka, T; Matsuhisa, T; Mine, T; Mizuno, S; Nagahara, A; Nishizawa, T; Ohkusa, T; Omata, F; Sakaki, N; Sasaki, H; Suzuki, H; Suzuki, M; Takahashi, S; Tokunaga, K; Torii, A, 2014
)
0.4
" In the ranitidine study, on day 13, participants were randomized to either concomitant dosing (treatment B) or staggered administration (treatment C) of erlotinib and ranitidine and crossed over to the other treatment starting on day 27."( Effect of gastric pH on erlotinib pharmacokinetics in healthy individuals: omeprazole and ranitidine.
Abt, M; Ducray, PS; Giraudon, M; Hamilton, M; Kletzl, H; Lum, BL, 2015
)
0.65
" This may lead to early identification of ethnic sensitivity in clearance and the need for different dosing regimens in a specific ethnic group for substrates of CYP2C19 which can support the rational design of bridging clinical trials."( Evaluating a physiologically based pharmacokinetic model for prediction of omeprazole clearance and assessing ethnic sensitivity in CYP2C19 metabolic pathway.
Cleary, Y; Feng, S; Hu, P; Parrott, N; Shi, J; Wang, Y; Weber, C; Yin, OQ, 2015
)
0.65
"To examine the effects of PO administered ranitidine and omeprazole on intragastric pH in cats and to compare the efficacy of once-daily versus twice-daily dosage regimens for omeprazole."( The effect of orally administered ranitidine and once-daily or twice-daily orally administered omeprazole on intragastric pH in cats.
Hartnack, S; Kook, PH; Reusch, CE; Ruetten, M; Šutalo, S,
)
0.6
"01) by subgroup according to dosage by random effects model, and a significant difference between esomeprazole 40 mg vs."( Comparative effectiveness and tolerability of esomeprazole and omeprazole in gastro-esophageal reflux disease: A systematic review and meta-analysis.
Liu, L; Qi, Q; Wang, R; Wang, S; Zhao, F, 2015
)
0.89
" However, its pharmacokinetic and chemical instability does not allow simple aqueous dosage form formulation synthesis for therapy of, especially child, these patients."( Pharmacokinetic Comparison of Omeprazole Granule and Suspension Forms in Children: A Randomized, Parallel Pilot Trial.
Dehghanzadeh, G; Haghighat, M; Karami, S; Mirzaei, R; Rahimi, HR, 2016
)
0.72
" The daily dosage of GERD medications, measured as omeprazole equivalents (mean ± SD, mg), decreased from 66."( Long-term follow-up results of endoscopic treatment of gastroesophageal reflux disease with the MUSE™ endoscopic stapling device.
Bapaye, A; Bonavina, L; Kessler, WR; Kim, HJ; Kwon, CI; Lehman, GA; McNulty, G; Selzer, DJ, 2016
)
0.69
"A high-throughput 96-microwell plate fluorometric method was developed and validated to determine omeprazole (OMZ) in its dosage forms."( A Validated High-Throughput Fluorometric Method for Determination of Omeprazole in Quality Control Laboratory via Charge Transfer Sensitized Fluorescence.
Ahmed, SA; Mahmoud, AM, 2016
)
0.89
"A novel, simple, sensitive, selective and reproducible stability-indicating high performance liquid chromatographic method was developed for the quantitative determination of degradation products and process-related impurities of ketoprofen (KET) and omeprazole (OMZ) in combined oral solid dosage form."( Development and Validation of a Novel Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Related Substances of Ketoprofen and Omeprazole in Combined Capsule Dosage Form.
Anireddy, JS; Koppala, S; Reddy, VR,
)
0.51
"Randomized patients with available aspirin dosing information in COGENT (N = 3,752) were divided into "low-dose" (≤ 100 mg) and "high-dose" (>100 mg) aspirin groups."( Proton-Pump Inhibitors Reduce Gastrointestinal Events Regardless of Aspirin Dose in Patients Requiring Dual Antiplatelet Therapy.
Bhatt, DL; Cannon, CP; Cohen, M; Cryer, BL; Doros, G; Goldsmith, MA; Hsieh, WH; Laine, L; Lanas, A; Lapuerta, P; Liu, Y; Schnitzer, TJ; Shook, TL; Vaduganathan, M, 2016
)
0.43
" dosing for 5 days."( Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants.
Elgadi, M; Gießmann, T; Huang, F; Lang, B; Wu, J, 2016
)
0.7
" Generally, maintenance doses depend upon drug clearance, so individual dosage regimens should be customized for HCC patients based on the condition of patients."( Changes in cytochrome P450s-mediated drug clearance in patients with hepatocellular carcinoma in vitro and in vivo: a bottom-up approach.
Fang, Y; Gao, J; Gao, N; He, XP; Jia, LJ; Jin, H; Qiao, HL; Tian, X; Wen, Q; Zhang, YF; Zhou, J, 2016
)
0.43
"Twice-daily dosing of proton pump inhibitor (PPI), the standard therapy for gastro-oesophageal reflux disease (GERD), is an effective therapy for GERD in SSc."( Effectiveness of add-on therapy with domperidone vs alginic acid in proton pump inhibitor partial response gastro-oesophageal reflux disease in systemic sclerosis: randomized placebo-controlled trial.
Chunlertrith, K; Foocharoen, C; Mahakkanukrauh, A; Mairiang, P; Namvijit, S; Nanagara, R; Suwannaroj, S; Wantha, O, 2017
)
0.46
" Each rat to receive nebivolol and omeprazole was given the agent orally (by gavage) daily for 10 days prior to induction of ulcer by oral dosing with INDO."( Nebivolol prevents indomethacin-induced gastric ulcer in rats.
El-Ashmawy, NE; El-Bahrawy, HA; Khedr, EG; Selim, HM, 2016
)
0.71
" Therefore, the use of singular dosing recommendations that encompass all horse types and management conditions may not be appropriate and dosing recommendations that take into account the diet of the horse may be advantageous."( The effects of dose and diet on the pharmacodynamics of omeprazole in the horse.
Greer, R; McGowan, CM; Mills, PC; Sykes, BW; Underwood, C, 2017
)
0.7
" The blood samples for PK analysis were collected at the scheduled time-points, prior to dosing to 10 hours after dosing."( A bioequivalence study of two omeprazole formulations in healthy male volunteers.
Kim, BH; Kim, YK; Yim, SV; Yoon, S; Yu, KS, 2016
)
0.72
" Clinical trials validating omeprazole dosage in neonates are limited."( Dose-Finding Study of Omeprazole on Gastric pH in Neonates with Gastro-Esophageal Acid Reflux Using a Bayesian Sequential Approach.
Alberti, C; Biran, V; Bourdon, O; Farnoux, C; Jacqz-Aigrain, E; Kaguelidou, F; Zohar, S, 2016
)
1.04
" We compared the acid inhibitory effects of CDFR0209 and delayed-release omeprazole (omeprazole-DR, Losec 40 mg) after repeated dosing in Helicobacter pylori-negative healthy adult male subjects."( Acid Inhibitory Effect of a Combination of Omeprazole and Sodium Bicarbonate (CDFR0209) Compared With Delayed-Release Omeprazole 40 mg Alone in Healthy Adult Male Subjects.
Cho, DY; Kim, H; Kim, KN; Kim, YS; Kwak, SS; Yang, SW, 2018
)
0.98
" The method was fully validated for the determination of S-isomers of each drug in their dosage form."( High performance liquid chromatography with photo diode array for separation and analysis of naproxen and esomeprazole in presence of their chiral impurities: Enantiomeric purity determination in tablets.
El-Kimary, EI; Ragab, MAA, 2017
)
0.67
" This work intends to evaluate once-daily, 40 mg omeprazole and once-nightly, 300 mg ranitidine (QD/QHS) dosing as an alternative regimen, and use this study's cohort to evaluate empiric regimens prescribed for LPR as compared to up-front testing with pH impedance multichannel intraluminal impedance (MII) with dual pH probes and high-resolution manometry (HRM) for potential cost minimization."( Rethinking the laryngopharyngeal reflux treatment algorithm: Evaluating an alternate empiric dosing regimen and considering up-front, pH-impedance, and manometry testing to minimize cost in treating suspect laryngopharyngeal reflux disease.
Carroll, TL; Dezube, A; Nahikian, K; Roth, DF; Werner, A, 2017
)
0.71
" Initial QD/QHS dosing increased after 3 months to BID if no improvement and ultimately prescribed MII and HRM if they failed BID dosing."( Rethinking the laryngopharyngeal reflux treatment algorithm: Evaluating an alternate empiric dosing regimen and considering up-front, pH-impedance, and manometry testing to minimize cost in treating suspect laryngopharyngeal reflux disease.
Carroll, TL; Dezube, A; Nahikian, K; Roth, DF; Werner, A, 2017
)
0.46
" In a phase 1/2 study in myelofibrosis patients, once-daily dosing of a 300-mg momelotinib capsule was selected for further development based on a favorable benefit:risk profile."( The Relative Bioavailability, Food Effect, and Drug Interaction With Omeprazole of Momelotinib Tablet Formulation in Healthy Subjects.
Deng, W; Hemenway, J; Maltzman, J; Shao, L; Silverman, JA; Stefanidis, D; Tarnowski, T; Xin, Y, 2018
)
0.72
"To evaluate the capacity for modafinil to be a perpetrator of metabolic drug-drug interactions by altering cytochrome P450 activity following a single dose and dosing to steady state."( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol.
Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018
)
0.48
"These data support consideration of the risk of clinically relevant metabolic drug-drug interactions perpetrated by modafinil when this drug is co-administered with drugs that are primarily cleared by CYP2C19 (single modafinil dose or steady state modafinil dosing) or CYP3A4 (steady state modafinil dosing only) catalysed metabolic pathways."( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol.
Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018
)
0.48
" Our aim was to compare effectiveness of increased PPI dosing with laparoscopic magnetic sphincter augmentation (MSA) in patients with moderate-to-severe regurgitation despite once-daily PPI therapy."( Laparoscopic magnetic sphincter augmentation versus double-dose proton pump inhibitors for management of moderate-to-severe regurgitation in GERD: a randomized controlled trial.
Abbas, G; Bell, R; Buckley, FP; Dunst, C; Gould, J; Hill, M; Jacobsen, G; Katz, P; Khaitan, L; Kothari, S; Lipham, J; Lister, D; Louie, B; Luketich, J; McDowell-Jacobs, L; Park, A; Reardon, P; Richards, W; Smith, C; Smith, CD; Williams, V; Woods, K, 2019
)
0.51
" No study to date has assessed whether correcting dosing regimens would improve symptom control."( Optimal Omeprazole Dosing and Symptom Control: A Randomized Controlled Trial (OSCAR Trial).
Perzynski, AT; Votruba, M; Waghray, A; Waghray, N; Wolfe, MM, 2019
)
0.95
"Patients with persistent heartburn symptoms ≥ 3 times per week treated with omeprazole 20 mg daily were enrolled and randomized to commonly recommended dosing or continued suboptimal dosing of omeprazole."( Optimal Omeprazole Dosing and Symptom Control: A Randomized Controlled Trial (OSCAR Trial).
Perzynski, AT; Votruba, M; Waghray, A; Waghray, N; Wolfe, MM, 2019
)
1.18
" GSAS symptom, frequency, and severity scores were significantly better when dosing was optimized for overall and heartburn-specific symptoms (P < 0."( Optimal Omeprazole Dosing and Symptom Control: A Randomized Controlled Trial (OSCAR Trial).
Perzynski, AT; Votruba, M; Waghray, A; Waghray, N; Wolfe, MM, 2019
)
0.95
"Low-cost efforts to promote commonly recommended PPI dosing can dramatically reduce GERD symptoms and related economic costs."( Optimal Omeprazole Dosing and Symptom Control: A Randomized Controlled Trial (OSCAR Trial).
Perzynski, AT; Votruba, M; Waghray, A; Waghray, N; Wolfe, MM, 2019
)
0.95
"Modified-release oral dosage forms are commonly used in pharmaceutics to delay or sustain the release of drugs."( Development and evaluation of an omeprazole-based delayed-release liquid oral dosage form.
Amighi, K; Goole, J; Guillaume, G; Paide, M; Ronchi, F; Sacré, P; Sereno, A; Stéphenne, V, 2019
)
0.8
" The physicians should more carefully interpret whether there is an essential indication before prescribing PPIs and, if there is, to approve the proper dosing for the situation."( A potential risk factor for paraoxonase 1: in silico and in-vitro analysis of the biological activity of proton-pump inhibitors.
Türkeş, C, 2019
)
0.51
"Introduction: On the pharmaceutical market of Ukraine, there are six international non-proprietary names of proton pump inhibitors (PPIs) - Omeprazole, Pantoprazole, Lansoprazole, Rabeprazole, Esomeprazole, Dexlansoprazole, which differ in a number of pharmacokinetic and pharmacodynamic parameters, safety profile, range of dosage forms and their cost."( Qualimetric analysis of proton pump inhibitors in Ukraine.
Karimova, MM; Makarenko, OV; Masheiko, AM; Onul, NM, 2019
)
0.72
"Proton pump inhibitor (PPI) twice daily dosing is a standard therapy for gastroesophageal reflux disease (GERD) in systemic sclerosis (SSc) but there is no data on its response rate or the predictors of PPI-partial response GERD."( Prevalence and predictors of proton pump inhibitor partial response in gastroesophageal reflux disease in systemic sclerosis: a prospective study.
Chunlertrith, K; Foocharoen, C; Mahakkanukrauh, A; Mairiang, P; Namvijit, S; Nanagara, R; Suwannaroj, S; Wantha, O, 2020
)
0.56
"In New Zealand, there are no liquid formulations of omeprazole commercially available, therefore suspensions must be extemporaneously compounded from solid dosage forms for patients with swallowing difficulties."( The Effect of Manufacturer on the Compounding of Omeprazole Suspensions and Their Stability Assessment.
Bansal, M; Dela, CPD; Hanning, S; Meissner, S; Svirskis, D,
)
0.64
" The time points and dosing of OME and CP were calculated based on previous studies and the therapeutic dose for patients."( Omeprazole attenuates cisplatin-induced kidney injury through suppression of the TLR4/NF-κB/NLRP3 signaling pathway.
Gao, H; Qu, X; Song, Y; Tao, L; Wang, X; Zhai, J; Zhang, W; Zhang, Y, 2020
)
2
" An efficient and sensitive method to measure multiple serum drugs and metabolites could inform drug dosing in polypharmacy."( Quantification of serum levels in mice of seven drugs (and six metabolites) commonly taken by older people with polypharmacy.
Hilmer, SN; Mach, J; Wang, X, 2021
)
0.62
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" The aim of this study is to develop OME loaded nanoparticles with a view to the obtention of a liquid pharmaceutical dosage form."( Omeprazole nanoparticles suspension: Development of a stable liquid formulation with a view to pediatric administration.
Bender, ET; Bender, JG; Bianchin, MD; Cichota, LC; Diefenthaeler, HS; Külkamp-Guerreiro, IC; Marques, MS; Nery, SF; Nonnenmacher, JL, 2020
)
2
" Reviewing the manner of administration and stated indications for use of both drugs, we find omeprazole is often administered outside dosing recommendations, and both drugs are frequently administered for aims that are unlikely to be achieved when considering their known biological effects in dogs."( Prospective observational study of the use of omeprazole and maropitant citrate in veterinary specialist care.
Glanemann, B; McCormack, R; Olley, L; Swann, JW, 2020
)
1.04
"Proton pump inhibitors (PPIs) can affect the intragastric release of other drugs from their dosage forms by elevating the gastric pH."( Physiologically Based Pharmacokinetic Modeling Approach to Identify the Drug-Drug Interaction Mechanism of Nifedipine and a Proton Pump Inhibitor, Omeprazole.
Babiskin, A; Le Merdy, M; Lee, SC; Ni, Z; Sun, D; Tan, ML; Zhao, L, 2021
)
0.82
"We developed and validated a simple, convenient and reproducible method for simultaneous estimation of six proton-pump inhibitors (PPIs), omeprazole (OPZ), esomeprazole (EOPZ), lansoprazole (LPZ), pantoprazole (PPZ), rabeprazole (RPZ) and ilaprazole (IPZ) in pharmaceutical dosage forms by a single marker."( Simultaneous Quantitative Analysis of Six Proton-Pump Inhibitors with a Single Marker and Evaluation of Stability of Investigated Drugs in Polypropylene Syringes for Continuous Infusion Use.
Chen, F; Fang, B; He, X; Wang, S, 2020
)
0.76
"The proposed method, which is selective, economical and accurate, was applied successfully for determination of the cited PPIs in their respective pharmaceutical dosage forms."( Simultaneous Quantitative Analysis of Six Proton-Pump Inhibitors with a Single Marker and Evaluation of Stability of Investigated Drugs in Polypropylene Syringes for Continuous Infusion Use.
Chen, F; Fang, B; He, X; Wang, S, 2020
)
0.56
" The vitamin B12 was dosage using a chemiluminescent immunoassay and oxidative stress analysis, based on the evaluation of malondialdehyde, enzymatic activity of extracellular superoxide dismutase, glutathione peroxidase, catalase and the ferric reducing antioxidant power in plasma."( Cognition, oxidative stress and vitamin B12 levels evaluation on patients under long-term omeprazole use.
Cardoso, CO; de Lima, AG; Dries, LS; Haefliger, R; Perassolo, MS; Seibert, BS, 2022
)
0.94
" In the current work, two different high precision sensitive fluorescence spectroscopic methods were developed for quantitative analysis of the above drugs in pharmaceutical dosage form and spiked human plasma."( Application of different spectrofluorimetric approaches for quantitative determination of acetylsalicylic acid and omeprazole in recently approved pharmaceutical preparation and human plasma.
Abdelazim, AH; Almrasy, AA; El-Olemy, A; Hasan, MA; Madkour, AW; Ramzy, S; Shahin, M, 2021
)
0.83
" Blood samples were collected up to 144 hours after dosing following administration of OM on days 1 and 9 to characterize plasma concentrations of OM."( Pharmacokinetic Drug-Drug Interaction Study of Omecamtiv Mecarbil With Omeprazole, a Proton Pump Inhibitor, in Healthy Subjects.
Abbasi, S; Dutta, S; Flach, S; Jafarinasabian, P; Lee, E; Sohn, W; Terminello, B; Trivedi, A; Zhang, H, 2022
)
0.95
"A recent combination of aspirin (ASP) and omeprazole (OMP) has been presented in a fixed dosage form for the treatment of many cardiovascular diseases, particularly in patients with gastric diseases."( Spectrophotometric Determination of Aspirin and Omeprazole in the Presence of Salicylic Acid as a Degradation Product: A Comparative Evaluation of Different Univariate/Multivariate Post Processing Algorithms.
Badrawy, M; El-Mammli, MY; Elmasry, MS; Hassan, WS; Serag, A, 2022
)
1.24
"25), if concomitantly administered drugs are dosed either 2 hours before or 8 hours after the 2-hour intravenous infusion of treosulfan."( Evaluation of the drug-drug interaction potential of treosulfan using a physiologically-based pharmacokinetic modelling approach.
Balazki, P; Baumgart, J; Beelen, DW; Böhm, S; Hemmelmann, C; Hilger, RA; Martins, FS; Ring, A; Schaller, S, 2022
)
0.72
" Six smart and different spectrophotometric methods were developed for the analysis of omeprazole and aspirin in binary mixture and pharmaceutical dosage form."( Earth friendly spectrophotometric methods based on different manipulation approaches for simultaneous determination of aspirin and omeprazole in binary mixture and pharmaceutical dosage form: Comparative statistical study.
Badrawy, M; El-Mammli, MY; Elmasry, MS; Hassan, WS, 2022
)
1.15
"A sensitive and selective method needs to be developed and validated for simultaneous determination of four drugs (amoxacillin, tinidazole, naproxen and lansoprazole), used for treating Helicobacter pylori infection, in their combined dosage forms."( RP-HPLC-DAD Method Development and Validation for Simultaneous Determination of Lansoprazole, Tinidazole, Amoxicillin, and Naproxen in Their Raw Materials and Combined Dosage Form: DOE Approach for Optimization of the Proposed Method.
Hassib, ST; Mostafa, EA; Sharf, MG; Taha, EA, 2022
)
0.72
"The method can be easily implemented in QC studies of the cited drugs in their dosage forms."( RP-HPLC-DAD Method Development and Validation for Simultaneous Determination of Lansoprazole, Tinidazole, Amoxicillin, and Naproxen in Their Raw Materials and Combined Dosage Form: DOE Approach for Optimization of the Proposed Method.
Hassib, ST; Mostafa, EA; Sharf, MG; Taha, EA, 2022
)
0.72
" Serial blood samples for assay of omeprazole and its metabolites were collected for 24 h after dosing on days 1 and 11."( Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women.
Kim, E; Mostafa, NM; Nader, A; Shebley, M, 2022
)
1.26
" When a 200-mg single oral dose of belumosudil was coadministered with both rabeprazole and omeprazole, parent and metabolite exposures were largely reduced, suggesting that belumosudil dosage should be increased when given with PPIs."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
0.94
" Omeprazole is the most common option utilized for acid-related disorders ; however, the pharmacokinetic (PK) and dosing recommendations for the obese patient population are lacking."( Population pharmacokinetics of omeprazole in obese and normal-weight adults.
Chen, K; Deng, C; Ding, J; Lin, Y; Luo, P; Pei, Q; Yang, G; Zhu, L; Zhu, S, 2022
)
1.92
" For rifabutin, differing intragastric concentrations based on dosing regimen may account for differences in reported eradication rates."( Physiologically-based pharmacokinetic modelling to predict intragastric rifabutin concentrations in the treatment of Helicobacter pylori infection.
Almenoff, JS; Howden, CW; Offman, E; Pendse, SN; Shah, S; Sheldon, KL, 2023
)
0.91
"To compare intragastric rifabutin concentrations between low-dose rifabutin (50 mg three time daily; as in RHB-105) and generically dosed rifabutin 150 mg once daily, 150 mg twice daily, and 300 mg once daily using a validated Physiologically-based pharmacokinetic (PBPK) model."( Physiologically-based pharmacokinetic modelling to predict intragastric rifabutin concentrations in the treatment of Helicobacter pylori infection.
Almenoff, JS; Howden, CW; Offman, E; Pendse, SN; Shah, S; Sheldon, KL, 2023
)
0.91
" Although the result of the current study improves, a high dosage of aqueous extracts of plants has more effectiveness than a low dosage of aqueous extracts plants."( Gastro-Protective and Therapeutic Effect of Punica granatum against Stomach Ulcer Caused by Helicobacter Pylori.
Alamri, ZZ; Faraj, RK; Hussein, MM; M Hussein, A; Mojarradgandoukmolla, S; Muhialdin, AJ; Taha, ZB, 2023
)
0.91
" This study has demonstrated that the resulting liquid formulation is suitable for all patients, in particular children or adults who are unable to take other pharmaceutical dosage forms, which overcomes the limitations of the medicines currently available on the market."( Stability of Omeprazole Extemporaneous Oral Solution in Chopin Base.
Denora, N; Fontana, S; la Forgia, FM; Lopalco, A; Lopedota, AA; Spennacchio, A,
)
0.5
" Results indicate that buccal foams of omeprazole may address the stability and ease of administration issues related to oral administration of the drug, particularly for children and elderly patients who have difficulty swallowing solid dosage forms."( Pediatric and Geriatric-Friendly Buccal Foams: Enhancing Omeprazole Delivery for Patients Encountering Swallowing Difficulties.
Andreadis, D; Bouropoulos, N; Chachlioutaki, K; Fatouros, DG; Gika, H; Iordanopoulou, A; Karavasili, C; Meikopoulos, T; Ritzoulis, C, 2023
)
1.42
"Oral extended-release (ER) dosage forms have been used to sustain blood drug levels, reduce adverse events, and improve patient compliance."( Effect of Omeprazole Administration on the Pharmacokinetics of Oral Extended-Release Nifedipine in Healthy Subjects.
Feng, K; Kinjo, M; Lionberger, R; Sun, D; Tan, ML; Wang, H; Xu, M; Zhao, L, 2023
)
1.31
" Of the 35 cases in which gastroprotectant therapy was indicated, the medication chosen or dosage administered was considered suboptimal in 16 (45."( Evaluation of gastroprotectant administration in hospitalized cats in a tertiary referral hospital.
Evenhuis, JV; Figueroa, ME; Forsythe, LR; Marks, SL; Pomerantz, LK; Ullal, TV, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
sulfoxideAn organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
sulfoxideAn organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

PathwayProteinsCompounds
Omeprazole Action Pathway1014
Omeprazole Metabolism Pathway23

Protein Targets (122)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency24.04910.140911.194039.8107AID2451; AID2785
Chain A, HADH2 proteinHomo sapiens (human)Potency15.84890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency15.84890.025120.237639.8107AID893
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency28.18380.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency18.16950.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency35.93860.007215.758889.3584AID1224835; AID624030
acetylcholinesteraseHomo sapiens (human)Potency78.73200.002541.796015,848.9004AID1347398
ClpPBacillus subtilisPotency22.38721.995322.673039.8107AID651965
phosphopantetheinyl transferaseBacillus subtilisPotency32.32000.141337.9142100.0000AID1490; AID2701
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency54.28963.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency18.11010.006038.004119,952.5996AID1159521
SMAD family member 2Homo sapiens (human)Potency12.15390.173734.304761.8120AID1346859
USP1 protein, partialHomo sapiens (human)Potency31.62280.031637.5844354.8130AID743255
SMAD family member 3Homo sapiens (human)Potency12.15390.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency25.14840.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency15.73130.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency28.45420.180013.557439.8107AID1460; AID1468
AR proteinHomo sapiens (human)Potency43.15590.000221.22318,912.5098AID1259243; AID1259247; AID588515; AID588516; AID743035; AID743036; AID743042; AID743054; AID743063
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency19.95260.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency26.96800.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency23.80610.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency31.82190.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency0.05310.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency50.11870.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.30180.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency26.45510.001310.157742.8575AID1259252; AID1259253; AID1259256
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency53.24210.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency32.82170.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency30.89120.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency44.66840.375827.485161.6524AID588526
pregnane X nuclear receptorHomo sapiens (human)Potency41.69670.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency37.17090.000229.305416,493.5996AID1259244; AID1259248; AID588513; AID588514; AID743069; AID743075; AID743078; AID743079
GVesicular stomatitis virusPotency27.54040.01238.964839.8107AID1645842
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency31.62280.707936.904389.1251AID504333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency39.47230.001024.504861.6448AID588534; AID588535
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency54.64980.001019.414170.9645AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency36.28410.023723.228263.5986AID743241
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.49870.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency24.92940.000723.06741,258.9301AID651777; AID743085; AID743122
activating transcription factor 6Homo sapiens (human)Potency17.97400.143427.612159.8106AID1159516; AID1159519
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency60.913919.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency54.64980.057821.109761.2679AID1159526; AID1159528
cytochrome P450 2C19 precursorHomo sapiens (human)Potency2.51190.00255.840031.6228AID899
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency16.92440.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency27.34910.354828.065989.1251AID504847; AID602199; AID602200; AID602201; AID602202
chromobox protein homolog 1Homo sapiens (human)Potency14.12540.006026.168889.1251AID540317
heat shock protein beta-1Homo sapiens (human)Potency39.45750.042027.378961.6448AID743210; AID743228
huntingtin isoform 2Homo sapiens (human)Potency25.11890.000618.41981,122.0200AID1688
pyruvate kinase PKM isoform aHomo sapiens (human)Potency7.07950.04017.459031.6228AID1631; AID1634
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency23.77810.168316.404067.0158AID720504
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency21.38990.000627.21521,122.0200AID651741; AID720636; AID743202; AID743219
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency12.58930.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.87990.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency16.36010.004611.374133.4983AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency1.41250.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.00000.031610.279239.8107AID884; AID885
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency31.62280.251215.843239.8107AID504327
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency25.11890.316212.765731.6228AID881
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency47.96580.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency27.54040.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency76.02060.002319.595674.0614AID651631
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency47.96580.001551.739315,848.9004AID1259244
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency25.11890.00638.235039.8107AID881
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mcl-1Homo sapiens (human)IC50 (µMol)3.14480.40007.134454.0000AID1417
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.28000.00001.18439.6140AID167650
N(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)IC50 (µMol)20.00007.80008.25708.7140AID1342731
Bile salt export pumpHomo sapiens (human)IC50 (µMol)87.00000.11007.190310.0000AID1443980; AID1473738
Sodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)IC50 (µMol)31.62280.00480.78076.0000AID146855
Sodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)73.77500.00022.318510.0000AID150618; AID679462
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)77.98300.00011.753610.0000AID428564
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Cytochrome P450 2C9 Homo sapiens (human)Ki45.00000.00031.684210.0000AID54410
Sodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
Sodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50 (µMol)228.20000.10002.50004.9000AID1802994
Potassium-transporting ATPase subunit betaSus scrofa (pig)IC50 (µMol)50.00000.03001.32255.2000AID78877
Potassium-transporting ATPase alpha chain 1Sus scrofa (pig)IC50 (µMol)50.00000.03001.06405.2000AID78877
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50 (µMol)228.20004.90004.90004.9000AID1802994
Potassium-transporting ATPase alpha chain 1Homo sapiens (human)IC50 (µMol)1.45000.04001.09603.8000AID165460; AID167650; AID167652; AID78730; AID79088
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50 (µMol)228.20000.30003.25807.3000AID1802994
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50 (µMol)228.20004.72004.81004.9000AID1802994
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)2.31500.00002.398310.0000AID1781974; AID1911191
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50 (µMol)228.20004.90004.90004.9000AID1802994
Fatty acid synthaseHomo sapiens (human)IC50 (µMol)29.60000.00772.46245.8000AID1195927
Fatty acid synthaseHomo sapiens (human)Ki3.40000.28003.44675.9000AID1195927
Sodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
Potassium-transporting ATPase subunit betaHomo sapiens (human)IC50 (µMol)1.45000.04001.09603.8000AID165460; AID167650; AID167652; AID78730; AID79088
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Sodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
Sodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
WD repeat-containing protein 5Homo sapiens (human)IC50 (µMol)1.70000.22302.45625.9000AID1688549
Glutathione S-transferase omega-1Homo sapiens (human)IC50 (µMol)4.60000.02801.60404.6000AID1384565
Histone-lysine N-methyltransferase 2AHomo sapiens (human)IC50 (µMol)1.70000.45002.30935.9000AID1688549
Sodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)IC50 (µMol)31.62280.00480.81346.0000AID146855
Cytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)IC50 (µMol)25.00004.47004.47004.4700AID1453445
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)IC50 (µMol)3.80000.00040.81213.8000AID79088
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)17.60000.00401.966610.0000AID1873205
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bifunctional cytochrome P450/NADPH--P450 reductasePriestia megaterium NBRC 15308 = ATCC 14581Kd16.96070.00400.41151.6700AID1802380
Bombesin receptor subtype-3Homo sapiens (human)EC50 (µMol)14.00000.01401.30933.9000AID348839
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 2C19Homo sapiens (human)Km7.37891.70005.38338.7500AID1220669; AID1220670; AID1220671; AID1220672; AID1220673; AID1220674; AID1220675; AID1220676; AID1220677; AID1220678; AID1220679; AID1220680; AID1220681; AID1220682; AID1220683; AID1220684; AID1220685; AID1220686
Potassium-transporting ATPase alpha chain 2Homo sapiens (human)Inhibition3.30003.30003.30003.3000AID78909
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (451)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
citrulline metabolic processN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
regulation of systemic arterial blood pressureN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
arginine catabolic processN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
nitric oxide mediated signal transductionN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
negative regulation of cell population proliferationN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
negative regulation of vascular permeabilityN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
positive regulation of angiogenesisN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
nitric oxide metabolic processN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
negative regulation of cellular response to hypoxiaN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
arginine metabolic processN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of the force of heart contractionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
regulation of sodium ion transportSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
osmosensory signaling pathwaySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
regulation of blood pressureSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
response to xenobiotic stimulusSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
negative regulation of glucocorticoid biosynthetic processSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
negative regulation of heart contractionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
positive regulation of heart contractionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
positive regulation of striated muscle contractionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
relaxation of cardiac muscleSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
cellular response to steroid hormone stimulusSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
membrane repolarizationSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
response to glycosideSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
intracellular calcium ion homeostasisSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
cell adhesionSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
regulation of gene expressionSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
regulation of cardiac muscle contraction by calcium ion signalingSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of ATP-dependent activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
sodium ion transmembrane transportSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein transport into plasma membrane raftSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
innate immune responseSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
ATP metabolic processSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein stabilizationSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
relaxation of cardiac muscleSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
cardiac muscle contractionSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein localization to plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
membrane repolarizationSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
monoatomic cation transmembrane transportSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of potassium ion transmembrane transporter activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of calcium:sodium antiporter activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
positive regulation of P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
regulation of resting membrane potentialSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
cellular response to steroid hormone stimulusSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
response to glycosideSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
cellular response to amyloid-betaSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
neuron projection maintenanceSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
retina homeostasisSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
lateral ventricle developmentSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
third ventricle developmentSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
neuronal-glial interaction involved in hindbrain glial-mediated radial cell migrationSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
photoreceptor cell maintenanceSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
motor behaviorSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
plasma membrane bounded cell projection organizationSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
positive regulation of neuron projection developmentSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cell-substrate adhesionSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
positive regulation of ATP-dependent activitySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
protein stabilizationSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
membrane repolarizationSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
transport across blood-brain barrierSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
positive regulation of potassium ion transmembrane transporter activitySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
positive regulation of sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
positive regulation of potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
negative regulation of glial cell migrationSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1-6Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1-6Homo sapiens (human)
response to xenobiotic stimulusPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
regulation of proton transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
monoatomic ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
pH reductionPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucose metabolic processBombesin receptor subtype-3Homo sapiens (human)
neuropeptide signaling pathwayBombesin receptor subtype-3Homo sapiens (human)
regulation of blood pressureBombesin receptor subtype-3Homo sapiens (human)
adult feeding behaviorBombesin receptor subtype-3Homo sapiens (human)
bombesin receptor signaling pathwayBombesin receptor subtype-3Homo sapiens (human)
G protein-coupled receptor signaling pathwayBombesin receptor subtype-3Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
osteoblast differentiationFatty acid synthaseHomo sapiens (human)
glandular epithelial cell developmentFatty acid synthaseHomo sapiens (human)
fatty acid metabolic processFatty acid synthaseHomo sapiens (human)
fatty acid biosynthetic processFatty acid synthaseHomo sapiens (human)
inflammatory responseFatty acid synthaseHomo sapiens (human)
ether lipid biosynthetic processFatty acid synthaseHomo sapiens (human)
neutrophil differentiationFatty acid synthaseHomo sapiens (human)
monocyte differentiationFatty acid synthaseHomo sapiens (human)
mammary gland developmentFatty acid synthaseHomo sapiens (human)
modulation by host of viral processFatty acid synthaseHomo sapiens (human)
cellular response to interleukin-4Fatty acid synthaseHomo sapiens (human)
establishment of endothelial intestinal barrierFatty acid synthaseHomo sapiens (human)
fatty-acyl-CoA biosynthetic processFatty acid synthaseHomo sapiens (human)
behavioral fear responseSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of the force of heart contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of muscle contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
amygdala developmentSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
olfactory cortex developmentSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
locomotionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
negative regulation of heart contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
positive regulation of heart contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
negative regulation of cytosolic calcium ion concentrationSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
neurotransmitter uptakeSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
potassium ion transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
sodium ion transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of smooth muscle contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of striated muscle contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of blood pressureSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
adult locomotory behaviorSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
visual learningSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
response to auditory stimulusSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
neuronal action potential propagationSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of vasoconstrictionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
L-ascorbic acid metabolic processSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
response to nicotineSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
locomotory exploration behaviorSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
sodium ion transmembrane transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
response to potassium ionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
negative regulation of striated muscle contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
ATP metabolic processSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of glutamate uptake involved in transmission of nerve impulseSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
relaxation of cardiac muscleSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cardiac muscle contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cellular response to mechanical stimulusSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cellular response to steroid hormone stimulusSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
potassium ion transmembrane transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
regulation of cardiac muscle cell contractionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
membrane repolarizationSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
monoatomic cation transmembrane transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
transport across blood-brain barrierSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
negative regulation of calcium ion transmembrane transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
negative regulation of calcium:sodium antiporter activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
response to glycosideSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cell adhesionPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to organonitrogen compoundPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to lipopolysaccharidePotassium-transporting ATPase subunit betaHomo sapiens (human)
pH reductionPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of pHPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
positive regulation of ATP-dependent activitySodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
sodium ion transmembrane transportSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
protein stabilizationSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
potassium ion transmembrane transportSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
protein localization to plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
membrane repolarizationSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
positive regulation of potassium ion transmembrane transporter activitySodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
positive regulation of sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
positive regulation of potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
transmembrane transportSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
positive regulation of P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
regulation of sodium ion transmembrane transporter activitySodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIWD repeat-containing protein 5Homo sapiens (human)
skeletal system developmentWD repeat-containing protein 5Homo sapiens (human)
gluconeogenesisWD repeat-containing protein 5Homo sapiens (human)
regulation of DNA-templated transcriptionWD repeat-containing protein 5Homo sapiens (human)
regulation of transcription by RNA polymerase IIWD repeat-containing protein 5Homo sapiens (human)
positive regulation of gluconeogenesisWD repeat-containing protein 5Homo sapiens (human)
transcription initiation-coupled chromatin remodelingWD repeat-containing protein 5Homo sapiens (human)
positive regulation of DNA-templated transcriptionWD repeat-containing protein 5Homo sapiens (human)
regulation of embryonic developmentWD repeat-containing protein 5Homo sapiens (human)
regulation of cell divisionWD repeat-containing protein 5Homo sapiens (human)
regulation of cell cycleWD repeat-containing protein 5Homo sapiens (human)
regulation of tubulin deacetylationWD repeat-containing protein 5Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumGlutathione S-transferase omega-1Homo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionGlutathione S-transferase omega-1Homo sapiens (human)
positive regulation of skeletal muscle contraction by regulation of release of sequestered calcium ionGlutathione S-transferase omega-1Homo sapiens (human)
L-ascorbic acid metabolic processGlutathione S-transferase omega-1Homo sapiens (human)
xenobiotic catabolic processGlutathione S-transferase omega-1Homo sapiens (human)
negative regulation of ryanodine-sensitive calcium-release channel activityGlutathione S-transferase omega-1Homo sapiens (human)
positive regulation of ryanodine-sensitive calcium-release channel activityGlutathione S-transferase omega-1Homo sapiens (human)
cellular response to arsenic-containing substanceGlutathione S-transferase omega-1Homo sapiens (human)
cellular oxidant detoxificationGlutathione S-transferase omega-1Homo sapiens (human)
glutathione metabolic processGlutathione S-transferase omega-1Homo sapiens (human)
apoptotic processHistone-lysine N-methyltransferase 2AHomo sapiens (human)
visual learningHistone-lysine N-methyltransferase 2AHomo sapiens (human)
post-embryonic developmentHistone-lysine N-methyltransferase 2AHomo sapiens (human)
anterior/posterior pattern specificationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
methylationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
circadian regulation of gene expressionHistone-lysine N-methyltransferase 2AHomo sapiens (human)
embryonic hemopoiesisHistone-lysine N-methyltransferase 2AHomo sapiens (human)
exploration behaviorHistone-lysine N-methyltransferase 2AHomo sapiens (human)
response to potassium ionHistone-lysine N-methyltransferase 2AHomo sapiens (human)
protein modification processHistone-lysine N-methyltransferase 2AHomo sapiens (human)
T-helper 2 cell differentiationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
transcription initiation-coupled chromatin remodelingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
positive regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase 2AHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase 2AHomo sapiens (human)
fibroblast proliferationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
negative regulation of fibroblast proliferationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
regulation of short-term neuronal synaptic plasticityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
spleen developmentHistone-lysine N-methyltransferase 2AHomo sapiens (human)
homeostasis of number of cells within a tissueHistone-lysine N-methyltransferase 2AHomo sapiens (human)
membrane depolarizationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
definitive hemopoiesisHistone-lysine N-methyltransferase 2AHomo sapiens (human)
protein-containing complex assemblyHistone-lysine N-methyltransferase 2AHomo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone-lysine N-methyltransferase 2AHomo sapiens (human)
negative regulation of DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase 2AHomo sapiens (human)
monoatomic ion transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
potassium ion transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
sodium ion transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
cell surface receptor signaling pathwaySodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
spermatogenesisSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
fertilizationSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
flagellated sperm motilitySodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
regulation of cellular pHSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
sodium ion transmembrane transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
regulation of membrane potentialSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
establishment of localization in cellSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
potassium ion transmembrane transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
transport across blood-brain barrierSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
proton transmembrane transportSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
sodium ion export across plasma membraneSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
potassium ion import across plasma membraneSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
intracellular potassium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
intracellular sodium ion homeostasisSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
protein foldingCytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)
protein deglycosylationCytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (182)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
catalytic activityN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
dimethylargininase activityN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
metal ion bindingN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
amino acid bindingN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
ATP bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
phosphatase activitySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
ATP hydrolysis activitySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
potassium ion bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sodium ion bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
transmembrane transporter bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
protein heterodimerization activitySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
protein-folding chaperone bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
steroid hormone bindingSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
ATPase activator activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein kinase bindingSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
MHC class II protein complex bindingSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein-macromolecule adaptor activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein heterodimerization activitySodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
ATPase bindingSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
amyloid-beta bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
ATP bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
ATP hydrolysis activitySodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
metal ion bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
protein-folding chaperone bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
steroid hormone bindingSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
ATPase activator activitySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
protein-macromolecule adaptor activitySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
protein heterodimerization activitySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
ATPase bindingSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
magnesium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP hydrolysis activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
bombesin receptor activityBombesin receptor subtype-3Homo sapiens (human)
neuropeptide receptor activityBombesin receptor subtype-3Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
UDP-glycosyltransferase activityUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
RNA bindingFatty acid synthaseHomo sapiens (human)
[acyl-carrier-protein] S-acetyltransferase activityFatty acid synthaseHomo sapiens (human)
[acyl-carrier-protein] S-malonyltransferase activityFatty acid synthaseHomo sapiens (human)
3-oxoacyl-[acyl-carrier-protein] synthase activityFatty acid synthaseHomo sapiens (human)
3-oxoacyl-[acyl-carrier-protein] reductase (NADPH) activityFatty acid synthaseHomo sapiens (human)
(3R)-3-hydroxypalmitoyl-[acyl-carrier-protein] dehydratase activityFatty acid synthaseHomo sapiens (human)
protein bindingFatty acid synthaseHomo sapiens (human)
(3R)-3-hydroxymyristoyl-[acyl-carrier-protein] dehydratase activityFatty acid synthaseHomo sapiens (human)
(3R)-3-hydroxydecanoyl-[acyl-carrier-protein] dehydratase activityFatty acid synthaseHomo sapiens (human)
fatty acyl-[ACP] hydrolase activityFatty acid synthaseHomo sapiens (human)
phosphopantetheine bindingFatty acid synthaseHomo sapiens (human)
cadherin bindingFatty acid synthaseHomo sapiens (human)
(3R)-3-hydroxybutanoyl-[acyl-carrier-protein] hydratase activityFatty acid synthaseHomo sapiens (human)
(3R)-3-hydroxyoctanoyl-[acyl-carrier-protein] dehydratase activityFatty acid synthaseHomo sapiens (human)
enoyl-[acyl-carrier-protein] reductase (NADPH) activityFatty acid synthaseHomo sapiens (human)
fatty acid synthase activityFatty acid synthaseHomo sapiens (human)
P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
steroid bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
ATP bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
phosphatase activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
ATP hydrolysis activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
potassium ion bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
sodium ion bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
protein heterodimerization activitySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
protein-folding chaperone bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
steroid hormone bindingSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
protein bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
heterocyclic compound bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
ATPase activator activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activityPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
ATP bindingPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
ATP hydrolysis activityPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
metal ion bindingPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
ATPase activator activitySodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
protein-macromolecule adaptor activitySodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
ATPase bindingSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
ATPase activator activitySodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
protein-macromolecule adaptor activitySodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
sodium channel regulator activitySodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
protein bindingWD repeat-containing protein 5Homo sapiens (human)
methylated histone bindingWD repeat-containing protein 5Homo sapiens (human)
histone H3K4 methyltransferase activityWD repeat-containing protein 5Homo sapiens (human)
histone bindingWD repeat-containing protein 5Homo sapiens (human)
glutathione transferase activityGlutathione S-transferase omega-1Homo sapiens (human)
protein bindingGlutathione S-transferase omega-1Homo sapiens (human)
oxidoreductase activityGlutathione S-transferase omega-1Homo sapiens (human)
glutathione dehydrogenase (ascorbate) activityGlutathione S-transferase omega-1Homo sapiens (human)
methylarsonate reductase activityGlutathione S-transferase omega-1Homo sapiens (human)
minor groove of adenine-thymine-rich DNA bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
chromatin bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
protein bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
histone H3K4 methyltransferase activityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
identical protein bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
protein homodimerization activityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
unmethylated CpG bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
lysine-acetylated histone bindingHistone-lysine N-methyltransferase 2AHomo sapiens (human)
protein-cysteine methyltransferase activityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
histone H3K4 monomethyltransferase activityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
histone H3K4 trimethyltransferase activityHistone-lysine N-methyltransferase 2AHomo sapiens (human)
P-type sodium:potassium-exchanging transporter activitySodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
protein bindingSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
ATP bindingSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
ATP hydrolysis activitySodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activitySodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
kinase bindingSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
metal ion bindingSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
mannosyl-glycoprotein endo-beta-N-acetylglucosaminidase activityCytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)
hydrolase activity, hydrolyzing O-glycosyl compoundsCytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (98)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
extracellular exosomeN(G),N(G)-dimethylarginine dimethylaminohydrolase 1Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
Golgi apparatusSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
postsynaptic densitySodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
basolateral plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
apical plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
lateral plasma membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
T-tubuleSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
axonSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
organelle membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sperm flagellumSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sarcolemmaSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
melanosomeSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
membrane raftSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
photoreceptor inner segment membraneSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
extracellular exosomeSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
extracellular vesicleSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
protein-containing complexSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
sarcolemmaSodium/potassium-transporting ATPase subunit alpha-1 Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
intercalated discSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
basolateral plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
apical plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
lateral plasma membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
T-tubuleSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
organelle membraneSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
sperm flagellumSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
sarcolemmaSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
extracellular exosomeSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
extracellular vesicleSodium/potassium-transporting ATPase subunit beta-1Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
photoreceptor inner segmentSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
endoplasmic reticulumSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
Golgi apparatusSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
axonSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
organelle membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
neuronal cell body membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
neuronal cell bodySodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
synapseSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
photoreceptor inner segment membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
neuron to neuron synapseSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
extracellular vesicleSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-3Homo sapiens (human)
photoreceptor inner segmentSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cytoplasmSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
external side of plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
apical plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
lateral plasma membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cell projection membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cell body membraneSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
cell peripherySodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
astrocyte projectionSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
astrocyte end-footSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
neuron to neuron synapseSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit beta-2Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1-6Homo sapiens (human)
intracellular membrane-bounded organelleUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
extracellular spacePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
apical plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
membraneBombesin receptor subtype-3Homo sapiens (human)
plasma membraneBombesin receptor subtype-3Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
Golgi apparatusFatty acid synthaseHomo sapiens (human)
cytosolFatty acid synthaseHomo sapiens (human)
plasma membraneFatty acid synthaseHomo sapiens (human)
membraneFatty acid synthaseHomo sapiens (human)
melanosomeFatty acid synthaseHomo sapiens (human)
glycogen granuleFatty acid synthaseHomo sapiens (human)
extracellular exosomeFatty acid synthaseHomo sapiens (human)
cytoplasmFatty acid synthaseHomo sapiens (human)
cytoplasmSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
endosomeSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
endoplasmic reticulumSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
caveolaSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cell surfaceSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
intercalated discSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
T-tubuleSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
organelle membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cell projectionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
neuronal cell bodySodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
dendritic spineSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
extracellular vesicleSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
cell projectionSodium/potassium-transporting ATPase subunit alpha-2Homo sapiens (human)
plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
apical plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium:potassium-exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
cytosolPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
actin cytoskeletonPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
basolateral plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
apical plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase alpha chain 2Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 2Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
basolateral plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
apical plasma membraneSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
sperm flagellumSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
melanosomeSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
extracellular exosomeSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit beta-3Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
extracellular exosomeSodium/potassium-transporting ATPase subunit gammaHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
nucleusWD repeat-containing protein 5Homo sapiens (human)
nucleoplasmWD repeat-containing protein 5Homo sapiens (human)
NSL complexWD repeat-containing protein 5Homo sapiens (human)
MLL1/2 complexWD repeat-containing protein 5Homo sapiens (human)
MLL3/4 complexWD repeat-containing protein 5Homo sapiens (human)
Set1C/COMPASS complexWD repeat-containing protein 5Homo sapiens (human)
MLL1 complexWD repeat-containing protein 5Homo sapiens (human)
mitotic spindleWD repeat-containing protein 5Homo sapiens (human)
ATAC complexWD repeat-containing protein 5Homo sapiens (human)
histone acetyltransferase complexWD repeat-containing protein 5Homo sapiens (human)
histone methyltransferase complexWD repeat-containing protein 5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmGlutathione S-transferase omega-1Homo sapiens (human)
cytosolGlutathione S-transferase omega-1Homo sapiens (human)
extracellular exosomeGlutathione S-transferase omega-1Homo sapiens (human)
cytoplasmGlutathione S-transferase omega-1Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase 2AHomo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase 2AHomo sapiens (human)
cytosolHistone-lysine N-methyltransferase 2AHomo sapiens (human)
MLL1 complexHistone-lysine N-methyltransferase 2AHomo sapiens (human)
histone methyltransferase complexHistone-lysine N-methyltransferase 2AHomo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
membrane raftSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
sperm midpieceSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
photoreceptor cell ciliumSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
rod photoreceptor outer segmentSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
sodium:potassium-exchanging ATPase complexSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
plasma membraneSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
cell projectionSodium/potassium-transporting ATPase subunit alpha-4Homo sapiens (human)
cytosolCytosolic endo-beta-N-acetylglucosaminidaseHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (613)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1301345Inhibition of CYP2C19 (unknown origin) at 24 uM by P450-glo assay2016Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.
AID1220740Activity of human recombinant CYP2C19.19 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID558350Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as inhibition of inducible nitric oxide synthase expression in infected cells at 200 uM by Immunoblotting relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1611375Clearance in rat liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1210405Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation measured as intrinsic unbound clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID561705Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins post last dose (Rvb2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1195927Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Repositioning proton pump inhibitors as anticancer drugs by targeting the thioesterase domain of human fatty acid synthase.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1473871Drug concentration at steady state in human at 20 to 40 mg, iv QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID289459Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 1.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID561698Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins post last dose (Rv2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID561693Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in luminal mucus layer at 35 ug/ml administered as single dose in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID558347Antimicrobial activity against sseF gene-deficient Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM after 2 to 16 hrs postinfection by flow cytometry relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID428564Inhibition of CYP3A42009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
AID19846Relative retention time at pH 61995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID1220579Activity of human recombinant CYP2C19.1B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID165393Antisecretory effect in isolated rabbit gastric glands as measured by aminopyrine uptake1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID60891Percent inhibition of histamine-stimulated gastric acid secretion in Heidenhain pouch dog after intraduodenal administration of compound (1 umol/kg)1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID631763Antiprotozoan activity against Trichomonas vaginalis GT3 trophozoites compound treated for 48 hrs measured after 48 hrs washout period2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Antiprotozoal activity of proton-pump inhibitors.
AID561714Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as decrease in bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as single dose for 5 days measured after 90 mins2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1220707Activity of human recombinant CYP2C19 M74T mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID23085pKa value of the compound (benzimidazole ring substitutions dependent) at pH 61995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID1220588Activity of human recombinant CYP2C19.15 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1210412Drug metabolism in human liver metabolism assessed as 5OH-omeprazole depletion measured as plasma fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1210416Drug metabolism in human hepatocytes assessed as omeprazole sulfone depletion measured per 10^6 cells as intrinsic unbound clearance2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID561689Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 100 uM, ip administered as single dose through dialysis measured after 90 mins post l2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID561699Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval measured after 90 m2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID283068Increase in 5 ug sparfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1210396Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation measured as microsomal fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1220737Activity of human recombinant CYP2C19.15 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561704Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval measured after 90 m2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID24471Chemical stability at pH 7.01992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.
AID729508Antiulcerogenic activity in ethanol-induced gastric ulcer Swiss albino mouse model assessed as lesion length at 3.6 mg/kg administered intragastrically for 3 days2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID561701Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 0.25 mg, ip administered as two doses of solvent in 24 hrs dosing interval measured after 90 mins post la2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1220594Activity of human recombinant CYP2C19 D360N mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID283065Increase in 5 ug levofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID289473Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 1.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1220688Activity of human recombinant CYP2C19.1B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID106806Inhibition of malate dehydrogenase (MDH) at 400 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID561928Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in central mucus layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID24522t1/2 is the time taken for the conversion of nicotinamides to isothiazolopyridine at pH=5.01997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.
AID1220600Activity of human recombinant CYP2C19.1B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID52790Inhibition of chymotrypsin at 250 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1220657Activity of human recombinant CYP2C19 W212C mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1220582Activity of human recombinant CYP2C19.8 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID167650Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by dibutyryl cyclic adenosine 3', 5' -monophosphate (dcAMP)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID1220590Activity of human recombinant CYP2C19.18 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1879669Antibacterial activity against Helicobacter pylori infected in C57/BL6 mouse assessed as bacterial load in stomach at 1 mg/kg administered twice daily via oral gavage starting from 7 days post inoculation and administered for 7 days in presence of 10 mg/k2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1210415Drug metabolism in human liver metabolism assessed as omeprazole sulfone depletion measured as intrinsic unbound clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID758794Inhibition of sheep gastric H(+)/K(+)-ATPase-mediated inorganic phosphate liberation after 15 mins by Fiske Subbarow method in presence of ATP2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K(+)-ATPase inhibitors.
AID558351Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in TNF-alpha secretion from infected cells at 200 Um after 16 hrs postinfection by ELISA relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID558345Antimicrobial activity against ssaV gene-deficient Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM after 2 to 16 hrs postinfection by flow cytometry relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID1472631Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate upto 10 uM after 45 mins in presence of NADPH by LC-MS/MS analysis2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID1756363Metabolic stability in rat hepatocytes assessed as intrinsic clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID283066Increase in 5 ug levofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220602Activity of human recombinant CYP2C19.6 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220634Activity of human recombinant CYP2C19 A161P mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID561715Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 min2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26380Dissociation constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID26312pKa value (pyridine)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID558352Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in IL-6 secretion from infected cells at 200 uM after 16 hrs postinfection by ELISA relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID25144t1/2 (pH 3)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID24469Chemical stability at pH 2.01992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.
AID150618Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID283061Increase in 5 ug ofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID283073Increase in 5 ug moxifloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID283074Increase in 5 ug moxifloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID558339Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in bacterial growth yield at 200 uM after 16 hrs postinfection by flow cytometry in presence of 10 ug/ml of intracellular replication inh2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID562045Bacteriostatic activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in bacterial growth yield at 200 uM after 16 hrs postinfection by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1220591Activity of human recombinant CYP2C19.19 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID562046bacteriostatic activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease intracellular bacteria at 200 uM after 16 hrs postinfection by GFP-based fluorescent reduction assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID283063Increase in 5 ug ofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID289486Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 100 uM in presence of 5.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID170442Acid output from the stomach (control value = 120.3+/-19.7) in pylorus ligated rats (20 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID561712Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses of solvent in 24 hrs dosing interval measured 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1220738Activity of human recombinant CYP2C19.16 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1756360Metabolic stability in human hepatocytes assessed as clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1220684Activity of human recombinant CYP2C19 F168L mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1682814Metabolic stability in rat liver microsomes assessed as half life
AID283056Increase in 5 ug ciprofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID182463Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 15 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID561681Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in luminal mucus layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1220586Activity of human recombinant CYP2C19.13 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561692Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two subsequent doses in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1210404Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation measured as intrinsic clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID289465Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 3.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID283086Increase in 16 ug/ml Norfloxacin accumulation in Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml after 20 mins2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1193492Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1220681Activity of human recombinant CYP2C19 A161P mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1210411Drug metabolism in human hepatocytes assessed as 5OH-omeprazole depletion measured per 10^6 cells as intrinsic unbound clearance2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID165460Inhibition of [14C]aminopyrine (AP) accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.
AID1220632Activity of human recombinant CYP2C19.19 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561707Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post last dose (Rvb = 90+/-2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID729506Antiulcerogenic activity in ethanol-induced gastric ulcer Swiss albino mouse model assessed as inhibition of ulceration at 3.6 mg/kg administered intragastrically for 3 days relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID1220705Activity of human recombinant CYP2C19 A161P mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220736Activity of human recombinant CYP2C19.14 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561930Cmax in Mongolian gerbils plasma2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1210401Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation measured per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID283053Increase in 5 ug Norfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID325357Growth inhibition of Leishmania donovani promastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID183860Gastric antisecretory activity was tested in rats at 30 mg/kg, po expressed as the percentage of inhibition against the acid output of the control group1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID79070Effect in vivo on gastric H+/K+ ATPase activity at 48 hrs following intraduodenal administration of 40 mg/Kg in rats injected intraperitoneally with 1 mg/Kg of cycloheximide1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID561684Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 0 to 15 um above the Juxtamucosal layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post last2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID283064Increase in 5 ug levofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1210398Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation measured as intrinsic unbound clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1220636Activity of human recombinant CYP2C19 M74T mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1911191Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 5 to 45 mins in presence of NADPH by LC/MS analysis
AID1321802Induction of CYP1A2 expression in human primary hepatocytes at 30 uM incubated for 48 hrs by RT-PCR method
AID1220595Activity of human recombinant CYP2C19 M74T mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID11917pH of the gastric juice (Control value = 1.42+/-0.02) of stomach content of pylorus ligated rats was measured (5 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID289479Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 100 uM in presence of 3.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID191889Volume of the gastric juice (Control value = 4.7+/-0.4) of stomach content of pylorus ligated rats was measured (20 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1220647Activity of human recombinant CYP2C19.15 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID283075Increase in 5 ug moxifloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220578Activity of human recombinant CYP2C19.1A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID78913In vitro evaluation for the inhibition of H+/K+ ATPase at pH < 3 in the gastric glands of isolated rabbit stomach.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID283052Increase in 5 ug Norfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID558341Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM treated 4 hr postinfection measured after 16 hrs of postinfection by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1220599Activity of human recombinant CYP2C19.1A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561506Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins p2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID79064Effect in vivo on gastric H+/K+ ATPase activity at 1.5 hrs following intraduodenal administration of 40 mg/Kg in rats1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID561510Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval m2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1220593Activity of human recombinant CYP2C19 A161P mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1688524Antiproliferative activity against human MOLM-13 cells harboring MLL1-AF92020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID561708Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as decrease in bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as single dose for 5 days measured after 90 min2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1220675Activity of human recombinant CYP2C19.14 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1873205Inhibition of human ABCG2 expressed in human HEK293 cells membrane vesicles mediated transport of 3[H]-MTX for 2 mins using [3H]-methotrexate as substrate by rapid filtration technique2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID561929Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in luminal mucus layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID182458Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 2.5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1220583Activity of human recombinant CYP2C19.9 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID28959Partition coefficient at 37 degrees Celsius at pH 7.41989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID729504Antiulcerogenic activity in pylorus ligation-induced gastric ulcer Sprague-Dawley rat model assessed as stomach H+/K+-ATPase activity measuring Pi release per hour per mg protein at 3.6 mg/kg, po for 3 days (Rvb =11.44 +/-1.5 umol )2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID561505Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID215494Urease activity was determined in wild type-H pylori, CCUG 15818, at a concentration of 1 uM1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID283083Increase in 16 ug/ml Norfloxacin accumulation in wild type Staphylococcus aureus SA1199 at 128 ug/ml after 20 mins2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID604278Inhibition of H+/K+ATPase in pig gastric microsome assessed as liberation of inorganic phosphate using ATP2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A reverse method for diversity introduction of benzimidazole to synthesize H(+)/K(+)-ATP enzyme inhibitors.
AID558355Induction of apoptosis in mouse RAW264.7 cells assessed as early apoptotic cells at 200 uM after 16 hrs using annexin V-propidium iodide staining by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID1220689Activity of human recombinant CYP2C19.9 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220710Activity of human recombinant CYP2C19 W212C mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220653Activity of human recombinant CYP2C19 D360N mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561682Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in central mucus layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID679462TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells2001Naunyn-Schmiedeberg's archives of pharmacology, Dec, Volume: 364, Issue:6
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein.
AID79063Effect in vivo on gastric H+/K+ -ATPase activity at 6 hrs following intraduodenal administration of 40 mg/Kg in rats1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID1688527Cytotoxicity against HUVEC cells2020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID191888Volume of the gastric juice (Control value = 4.7+/-0.4) of stomach content of pylorus ligated rats was measured (10 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1743055Antigiardial activity against Giardia lamblia WB incubated for 48 hrs by haemocytometric counting method2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Anti-
AID679457TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells2001Naunyn-Schmiedeberg's archives of pharmacology, Dec, Volume: 364, Issue:6
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein.
AID283069Increase in 5 ug sparfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID23086pKa value of the compound (pyridine ring substitutions dependent)1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID558353Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as delayed degradation of IkappaB-alpha in infected cells at 200 uM after 20 mins postinfection by Immunoblotting relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID325355Growth inhibition of Trypanosoma cruzi epimastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID561694Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in central layer at 35 ug/ml administered as single dose in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID679654TP_TRANSPORTER: Western blot, HepG2 cells2003The Journal of pharmacology and experimental therapeutics, Feb, Volume: 304, Issue:2
Influence of omeprazole on multidrug resistance protein 3 expression in human liver.
AID1220671Activity of human recombinant CYP2C19.9 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID685502HARVARD: Inhibition of blood stage Plasmodium falciparum 3D7 infection2012Proceedings of the National Academy of Sciences of the United States of America, May-29, Volume: 109, Issue:22
Liver-stage malaria parasites vulnerable to diverse chemical scaffolds.
AID1220654Activity of human recombinant CYP2C19 M74T mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1611374Half life in rat liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID561927Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1070214Inhibition of Trichomonas vaginalis uridine nucleoside ribohydrolase using 5-fluorouridine as substrate after 40 mins by NMR spectrometric analysis2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID215489Urease activity was determined in wild type-H pylori, CCUG 15818, at a concentration of 100 uM at pH 51995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID556020Antibacterial activity against Helicobacter pylori infected in human assessed as bacterial eradication rate at 1 g, po BID for 10 days by 13C-urea breath test2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1403540Clearance in rat liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1220598Activity of human recombinant CYP2C19 W212C mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220651Activity of human recombinant CYP2C19 E92D mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1193496Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1756362Metabolic stability in rat hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID25146t1/2 (pH 5)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID561926Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post la2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID561925Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses of solvent in 24 hrs dosing interval measured a2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1688525Antiproliferative activity against human K562 cells harboring MLL12020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1453445Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Repurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease.
AID1193494Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1220680Activity of human recombinant CYP2C19 E92D mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID289483Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 5.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID1600080Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using ATTO 655- Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Trp as substrate at 100 uM preincubated for 10 mins followed by substrate addition and measured after 30 mins by spectro2019European journal of medicinal chemistry, Oct-01, Volume: 179Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.
AID178054Inhibition of histamine induced gastric acid secretion in pylorus-ligated rats1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.
AID1473872Ratio of drug concentration at steady state in human at 20 to 40 mg, iv QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID29344Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID283079Increase in 30 ug chloramphenicol antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID289477Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 3.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID90865Compound was evaluated for gastric acid suppression on intravenous administration of a single dose up to 7 hr2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Perspectives in animal health: old targets and new opportunities.
AID1220635Activity of human recombinant CYP2C19 D360N mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID185319Reduction in length (control value = 59.8+/-6) of gastric lesions induced by endomethacin was measured, after administration of 7.5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID561690Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in central layer at 0.25 mg, ip administered as two subsequent doses in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID283058Increase in 5 ug ciprofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID78877Activity was evaluated by measuring the inhibition of isolated hog H+/K+ ATPase1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1220656Activity of human recombinant CYP2C19 E122A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561511Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in luminal mucus layer at 0.25 mg, ip administered as two doses of solvent measured after 90 mins post last dose (Rvb = 4560+/-400 ba2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID379409Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 10 mg/kg, po administered 1 hr prior to ethanol challenge relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Triterpene saponins with gastroprotective effects from tea seed (the seeds of Camellia sinensis).
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID558343Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM treated 3 hr before infection measured after 16 hrs of postinfection by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID1348173Anti-Trichomonas activity against Trichomonas vaginalis JT assessed as reduction in parasite growth after 24 hrs by haemocytometry2018European journal of medicinal chemistry, Jan-01, Volume: 143Recent developments in anti-Trichomonas research: An update review.
AID1220741Activity of human recombinant CYP2C19 E92D mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1849435Stability of the compound in simulated gastric fluid at pH 1 to 2 assessed as compound remaining at 120 mins by LC-MS/MS analysis
AID1220641Activity of human recombinant CYP2C19.1B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220643Activity of human recombinant CYP2C19.10 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID78909Evaluated for the inhibition of H+/K+ ATPase enzyme from fundic mucosa of white rabbits at 100 uM1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID1220682Activity of human recombinant CYP2C19 D360N mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID43581Inhibition of beta-lactamase at 100 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID283059Increase in 5 ug ciprofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1761180Giardicidal activity against Giardia intestinalis incubated for 48 hrs by hemocytometric counting method2021European journal of medicinal chemistry, Feb-05, Volume: 211The giardicidal activity of lobendazole, fabomotizole, tenatoprazole and ipriflavone: A ligand-based virtual screening and in vitro study.
AID1220633Activity of human recombinant CYP2C19 E92D mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID325356Growth inhibition of Trypanosoma brucei rhodesiense trypomastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1193495Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID59467Antisecretory activity calculated in heidenhain-pouch dog after iv administration of the drug1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID283054Increase in 5 ug Norfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220687Activity of human recombinant CYP2C19.1A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1193500Thermodynamic equilibrium solubility, log S of the compound2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID23087pKa value of the compound (pyridine ring substitutions dependent) at pH 61995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID1067101Half life in human liver microsomes at 0.5 uM in presence of NADPH2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a]pyrimidin-4-imines as potent 5-HT₆ antagonists.
AID1195928Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Repositioning proton pump inhibitors as anticancer drugs by targeting the thioesterase domain of human fatty acid synthase.
AID1220732Activity of human recombinant CYP2C19.9 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID252861Gastric cytoprotective effect as ulcerative index was calculated in male wistar rat after 20 mg/kg dosage2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Gastric cytoprotective activity of ilicic aldehyde: structure-activity relationships.
AID1210413Drug metabolism in human liver metabolism assessed as omeprazole sulfone depletion measured as microsomal fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID78888In vitro inhibition against H+/K+ ATPase from porcine gastric mucosal membrane vesicles1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID1220678Activity of human recombinant CYP2C19.18 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220670Activity of human recombinant CYP2C19.1B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID182462Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 10 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID79062Effect in vivo on gastric H+/K+ -ATPase activity at 48 hrs following intraduodenal administration of 40 mg/Kg in rats1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID185318Reduction in length (control value = 59.8+/-6) of gastric lesions induced by endomethacin was measured, after administration of 5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID78907Compound was tested in vitro for H+/K+ ATPase activity in rabbit stomach preparations1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.
AID170443Acid output from the stomach (control value = 120.3+/-19.7) in pylorus ligated rats (5 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID561716Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1416192Inhibition of H+/K+-ATPase in sheep stomach parietal cells assessed as reduction in inorganic phosphate liberation using ATP as substrate measured after 10 to 15 mins
AID558346Antimicrobial activity against sseG gene-deficient Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM after 2 to 16 hrs postinfection by flow cytometry relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID685503HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection2012Proceedings of the National Academy of Sciences of the United States of America, May-29, Volume: 109, Issue:22
Liver-stage malaria parasites vulnerable to diverse chemical scaffolds.
AID1220649Activity of human recombinant CYP2C19.18 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID289478Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 3.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID283072Increase in 5 ug moxifloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID289467Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 3.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID253087Percent inhibition ethanol induced necrotic damage of gastric mucosa in male wistar rat after dosage; Dose range 25-100 mg/kg2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Gastric cytoprotective activity of ilicic aldehyde: structure-activity relationships.
AID561709Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mi2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID561508Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in central mucus layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval measured after 90 min2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1193493Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID283084Increase in 16 ug/ml Norfloxacin accumulation in Staphylococcus aureus SA1199B mutant overexpressing NorA measured per mg of cell protein at 128 ug/ml after 5 mins2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID29165Dissociation constant at 37 degrees Centigrade1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID561696Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in 0 to 15 um above the Juxtamucosal layer at 35 ug/ml administered as single dose in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID283076Increase in 30 ug chloramphenicol antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220581Activity of human recombinant CYP2C19.6 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID729498Antiulcerogenic activity in pylorus ligation-induced gastric ulcer Sprague-Dawley rat model assessed as pH of gastric juice at 3.6 mg/kg, po for 3 days (Rvb =2.60 +/-0.55 )2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID561502Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1213966Induction of CYP1A2 in human hepatocytes using phenacetin as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1220686Activity of human recombinant CYP2C19 W212C mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561680Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses of solvent measured after 90 mins post last dose 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1220646Activity of human recombinant CYP2C19.14 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1384565Inhibition of GSTO1-1 (unknown origin) by enzymatic assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example.
AID556019Antibacterial activity against Helicobacter pylori infected in human assessed as bacterial eradication rate at 20 mg, po BID for 10 days by 13C-urea breath test2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID1220639Activity of human recombinant CYP2C19 W212C mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID177135In vivo antisecretory activity was determined for inhibition of gastric secretion in rat1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines.
AID685500HARVARD: Cytotoxicity in HepG2 cell line2012Proceedings of the National Academy of Sciences of the United States of America, May-29, Volume: 109, Issue:22
Liver-stage malaria parasites vulnerable to diverse chemical scaffolds.
AID729500Antiulcerogenic activity in pylorus ligation-induced gastric ulcer Sprague-Dawley rat model assessed as volume of gastric juice at 3.6 mg/kg, po for 3 days (Rvb =5.96 +/-0.80 ml )2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1368109Half-life in rat liver microsomes at 1 uM in presence of NADPH regenerating system by LC-MS/MS analysis
AID1220733Activity of human recombinant CYP2C19.10 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID685501HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells2012Proceedings of the National Academy of Sciences of the United States of America, May-29, Volume: 109, Issue:22
Liver-stage malaria parasites vulnerable to diverse chemical scaffolds.
AID310878Dissociation constant, pKa of the compound2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Recent advances in proton pump inhibitors and management of acid-peptic disorders.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID283077Increase in 30 ug chloramphenicol antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1210400Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation measured as plasma fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID283062Increase in 5 ug ofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID289453Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 0.3 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID215491Urease activity in H pylori, CCUG 15818, at 10 uM1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID283080Antibacterial activity against Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID561509Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1210410Drug metabolism in human liver metabolism assessed as 5OH-omeprazole depletion measured as intrinsic unbound clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID215495Urease activity was determined in wild type-H pylori, CCUG 15818, at a concentration of 1 uM at pH 51995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID1220587Activity of human recombinant CYP2C19.14 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220631Activity of human recombinant CYP2C19.18 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561679Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses of solvent measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID79088Inhibition of H+/K+ ATPase activity in buffered solution (pH 7.4)1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K(+)-ATPase inhibitor.
AID289461Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 1.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1743057Antigiardial activity against nitazoxanide resistant Giardia lamblia N1-INP incubated for 48 hrs by haemocytometric counting method2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Anti-
AID289472Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 1.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID561685Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 100 uM, ip administered as single dose through dialysis measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1220709Activity of human recombinant CYP2C19 E122A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID215492Urease activity was determined in wild type-H pylori, CCUG 15818, at a concentration of 10 uM at pH 51995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID289474Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 100 uM in presence of 1.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID1688549Inhibition of MLL1-WDR5 interaction in human MV4-11 cells assessed as reduction in MLL1 binding to WDR5 WIN site by 5-FAM probe based fluorescence polarization assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID453203Lipophilicity, log D of the compound2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID561711Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 min2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1210414Drug metabolism in human liver metabolism assessed as omeprazole sulfone depletion measured as intrinsic clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1220708Activity of human recombinant CYP2C19 F168L mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220652Activity of human recombinant CYP2C19 A161P mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID289485Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 5.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID185317Reduction in length (control value = 59.8+/-6) of gastric lesions induced by endomethacin was measured, after administration of 2.5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1220672Activity of human recombinant CYP2C19.10 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220640Activity of human recombinant CYP2C19.1A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220731Activity of human recombinant CYP2C19.8 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID283082Increase in 64 ug/ml Norfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by checker board method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220629Activity of human recombinant CYP2C19.15 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID679623TP_TRANSPORTER: inhibition of MTX uptake in membrane vesicle from BCRP-expressing Sf9 cell2004Cancer research, Aug-15, Volume: 64, Issue:16
Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions.
AID1220690Activity of human recombinant CYP2C19.10 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID558354Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as delayed degradation of IkappaB-alpha in infected cells at 200 uM after 40 mins postinfection by Immunoblotting relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID1210399Drug metabolism in human hepatocytes assessed as 5OH-omeprazole formation measured per 10^6 cells as intrinsic unbound clearance2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID59465Antisecretory activity calculated in heidenhain-pouch dog after id administration of the drug1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1220601Activity of human recombinant CYP2C19.5B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID561702Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post last dose (Rvb = 60+/-2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID182465Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 20 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1220596Activity of human recombinant CYP2C19 F168L mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID182459Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1220648Activity of human recombinant CYP2C19.16 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID558361Cytotoxicity against mouse RAW264.7 cells at 200 uM by LDH release assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID11916pH of the gastric juice (Control value = 1.42+/-0.02) of stomach content of pylorus ligated rats was measured (20 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1220735Activity of human recombinant CYP2C19.13 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID289452Inhibition of gastric proton pump activity of gastric H(+)/K(+) ATPase in Sprague-Dawley rat microsomal vesicles after washing at 10 uM2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID289449Antisecretory activity in rat pylorus ligation-induced ulcer model assessed as inhibition of free acidity of gastric juice at 10 mg/kg2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID561512Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in central layer at 0.25 mg, ip administered as two doses of solvent measured after 90 mins post last dose (Rvb = 4560+/-400 bacteria2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID178936Effective dose required for the inhibition of total acid secretion in pylorus-ligated rats at 20 mg/kg1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID283078Increase in 30 ug chloramphenicol antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1403539Half life in rat liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID289484Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 5.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID283060Increase in 5 ug ofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 128 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1688526Cytotoxicity against human L02 cells2020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID79068Effect in vivo on gastric H+/K+ ATPase activity at 24 hrs following intraduodenal administration of 40 mg/Kg in rats injected intraperitoneally with 1 mg/Kg of cycloheximide1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID1210402Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1220580Activity of human recombinant CYP2C19.5B mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1368110Clearance in rat liver microsomes at 1 uM measured after 90 mins in presence of NADPH regenerating system by LC-MS/MS analysis
AID558365Cytotoxicity against mouse RAW264.7 cells assessed as change vacuolar pH at 100 nM using acridine orange stain by fluorescent microscope2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1220638Activity of human recombinant CYP2C19 E122A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID60720Inhibitory activity when administered intravenously in histamine-stimulated gastric fistula dog at 3 mg/kg, id1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase.
AID1220674Activity of human recombinant CYP2C19.13 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID561687Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 100 uM, ip administered as single dose through dialysis measured after 90 mins post 2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID561710Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interva2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID561686Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 100 uM, ip administered as single dose through dialysis measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID24470Chemical stability at pH 5.01992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.
AID1220592Activity of human recombinant CYP2C19 E92D mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220644Activity of human recombinant CYP2C19.11 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID283081Increase in 2 ug/ml Norfloxacin antibacterial activity against wild type Staphylococcus aureus SA1199 at 128 ug/ml by checker board method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID561713Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 15 to 25 um above the Juxtamucosal layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post l2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID289466Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 3.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID78730In vitro inhibitory activity against H+/K+ ATPase prepared from canine fundic mucosa1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase.
AID1210407Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation measured as plasma fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1220628Activity of human recombinant CYP2C19.14 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID24888Half life at pH 7 is a measure of the rate by which the compound is converted to the active species1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID19845Relative retention time of the compound1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID1193498Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1220650Activity of human recombinant CYP2C19.19 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561706Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 0.25 mg, ip administered as two doses of solvent in 24 hrs dosing interval measured after 90 mins post la2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID79089Inhibition of H+/K+ ATPase activity in buffered solution (pH 7.4) at concentration 400 mM1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K(+)-ATPase inhibitor.
AID678718Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID24887Half life at pH 6 is a measure of the rate by which the compound is converted to the active species.1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID289471Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 1.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID1193497Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1210395Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1210394Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation measured per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1210406Drug metabolism in human hepatocytes assessed as omeprazole sulfone formation measured per 10^6 cells as intrinsic unbound clearance2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID27263Half-life at pH 7.41989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID561504Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in central mucus layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1743056Antigiardial activity against drug susceptible Giardia lamblia incubated for 48 hrs by haemocytometric counting method2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Anti-
AID283085Increase in 16 ug/ml Norfloxacin accumulation in Staphylococcus aureus SA1199B mutant overexpressing NorA measured per milligram of cell protein at 128 ug/ml after 20 mins2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID348839Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID24523t1/2 is the time taken for the conversion of nicotinamides to isothiazolopyridine at pH=7.01997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.
AID561717Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in 0 to 15 um above the Juxtamucosal layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1379263Inhibition of hydrogen potassium ATPase in goat stomach mucosal membrane assessed as decrease in inorganic phosphate production using ATP as substrate after 10 to 15 mins by spectrophotometric analysis
AID558348Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as inhibition of nitric oxide production in infected cells at 200 uM2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID78915Effect in vivo on gastric H+/K+ -ATPase activity at 24 hrs following intraduodenal administration of 40 mg/Kg in rats1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID192008Volume of the gastric juice (Control value = 4.7+/-0.4) of stomach content of pylorus ligated rats was measured (5 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID283067Increase in 5 ug levofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1220683Activity of human recombinant CYP2C19 M74T mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1781974Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Discovery of 1-Amino-1
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID54410Binding affinity towards cytochrome P450 2C92004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors.
AID561700Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in luminal mucus layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins post last dose (Rvb2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1238337Inhibition of CYP2C19 (unknown origin) at 24 uM by luminescent readout-based method2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40).
AID1682812Metabolic stability in rat liver microsomes assessed as intrinsic clearance
AID1220589Activity of human recombinant CYP2C19.16 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID26125pKa value (imidazole)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID289480Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 3.0 mM of p-NPP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID622649Antiulcerogenic activity in Kunming mouse assessed as inhibition of ethanol-induced gastric ulcer at 13.4 mg/kg, po qd for 5 days measured 1 hr post last dose relative to control2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and antigastric ulcer activity of novel 5-isoproyl-3,8-dimethylazulene derivatives.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1210397Drug metabolism in human liver metabolism assessed as 5OH-omeprazole formation measured as intrinsic clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID185184Reduction in length (control value = 159.2+/-21) of gastric lesions induced by endomethacin was measured, after administration of 20 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1220585Activity of human recombinant CYP2C19.11 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID561695Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in 15 to 25 um above the Juxtamucosal layer at 35 ug/ml administered as single dose in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1210409Drug metabolism in human liver metabolism assessed as 5OH-omeprazole depletion measured as intrinsic clearance per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1220673Activity of human recombinant CYP2C19.11 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID146855In vitro evaluation for its ability to inhibit the Na+/K+ ATPase at pH 7.4.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID631764Antiprotozoan activity against Giardia intestinalis IMSS:0989:1 trophozoites compound treated for 48 hrs measured after 48 hrs washout period2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Antiprotozoal activity of proton-pump inhibitors.
AID1220630Activity of human recombinant CYP2C19.16 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID729502Antiulcerogenic activity in pylorus ligation-induced gastric ulcer Sprague-Dawley rat model assessed as stomach peptic activity measuring tyrosine release for 4 hrs at 3.6 mg/kg, po for 3 days (Rvb =5.70 +/-2.40 ug/ml )2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.
AID1220739Activity of human recombinant CYP2C19.18 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID27262Half-life at pH 1.01989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID1688523Antiproliferative activity against human MV4-11 cells harboring MLL1-AF42020European journal of medicinal chemistry, Feb-15, Volume: 188Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1220642Activity of human recombinant CYP2C19.9 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID79073Inhibition of isolated rat H+/K+ ATPase.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID177881Inhibition of acid secretion was determined by the compound administered subcutaneously in rats1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.
AID289450Antisecretory activity in rat pylorus ligation-induced ulcer model assessed as inhibition of total acidity of gastric juice at 20 mg/kg2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID289460Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 1.0 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID185185Reduction in length (control value = 159.2+/-21) of gastric lesions induced by ethanol was measured, after administration of 10 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1210408Drug metabolism in human liver metabolism assessed as 5OH-omeprazole depletion measured as microsomal fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID561507Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in luminal mucus layer at 0.25 mg, ip followed by second dose administered as solvent in 24 hrs dosing interval measured after 90 min2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID1849436Stability of the compound in simulated gastric fluid at pH 1 to 2 assessed as half life at 120 mins by LC-MS/MS analysis
AID379411Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 20 mg/kg, po administered 1 hr prior to ethanol challenge relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Triterpene saponins with gastroprotective effects from tea seed (the seeds of Camellia sinensis).
AID1220677Activity of human recombinant CYP2C19.16 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID170441Acid output from the stomach (control value = 120.3+/-19.7) in pylorus ligated rats (10 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1220655Activity of human recombinant CYP2C19 F168L mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID631830Antiprotozoan activity against Entamoeba histolytica HM1-IMSS trophozoites compound treated for 48 hrs measured after 48 hrs washout period2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Antiprotozoal activity of proton-pump inhibitors.
AID1193499Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID558356Induction of apoptosis in mouse RAW264.7 cells assessed as late apoptotic cells at 200 uM after 16 hrs using annexin V-propidium iodide staining by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID185308Reduction in length (control value = 159.2+/-21) of gastric lesions induced by ethanol was measured, after administration of 15 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID23084pKa value of the compound (benzimidazole ring substitutions dependent)1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID558357Induction of apoptosis in mouse RAW264.7 cells assessed as necrotic cells at 200 uM after 16 hrs using annexin V-propidium iodide staining by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID283055Increase in 5 ug Norfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID558363Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in segregation of plasmid at 200 uM2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1220706Activity of human recombinant CYP2C19 D360N mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220597Activity of human recombinant CYP2C19 E122A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1220691Activity of human recombinant CYP2C19.11 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID604277Inhibition of H+/K+ATPase in pig gastric microsome assessed as liberation of inorganic phosphate using ATP at 10 uM relative to control2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A reverse method for diversity introduction of benzimidazole to synthesize H(+)/K(+)-ATP enzyme inhibitors.
AID1220645Activity of human recombinant CYP2C19.13 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as intrinisic clearance foromeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID167652Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID1220584Activity of human recombinant CYP2C19.10 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 5 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID289451Inhibition of gastric proton pump activity of gastric H(+)/K(+) ATPase in Sprague-Dawley rat microsomal vesicles before washing at 10 uM2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID78916Effect in vivo on gastric H+/K+ -ATPase activity at 3 hrs following intraduodenal administration of 40 mg/Kg in rats1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors.
AID1610342Clearance in rat liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID384956Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID453204Permeability in human skin after 48 hrs by Franz cell permeability assay2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1210417Drug metabolism in human liver metabolism assessed as omeprazole sulfone depletion measured as plasma fraction unbound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1220679Activity of human recombinant CYP2C19.19 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID283057Increase in 5 ug ciprofloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 64 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID283070Increase in 5 ug sparfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 32 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID310879Inhibition of H+/K+ ATPase2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Recent advances in proton pump inhibitors and management of acid-peptic disorders.
AID679655TP_TRANSPORTER: RT-PCR in HepG2 cells2003The Journal of pharmacology and experimental therapeutics, Feb, Volume: 304, Issue:2
Influence of omeprazole on multidrug resistance protein 3 expression in human liver.
AID1220685Activity of human recombinant CYP2C19 E122A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID182457Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 10 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID283071Increase in 5 ug sparfloxacin antibacterial activity against Staphylococcus aureus SA1199B mutant overexpressing NorA at 16 ug/ml by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID1220734Activity of human recombinant CYP2C19.11 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed as omeprazole 5'-hydroxylation per pmol protein at 100 uM after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1210403Drug metabolism in human liver metabolism assessed as omeprazole sulfone formation measured as microsomal fraction unbound per mg of microsomal protein2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID25148Half life at pH 7.41992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
AID1610341Half life in rat liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID11915pH of the gastric juice (Control value = 1.42+/-0.02) of stomach content of pylorus ligated rats was measured (10 mg/kg po of the Compound was administered 1 hr before the pylorus ligation)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1220692Activity of human recombinant CYP2C19.13 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID215488Urease activity in wild type H pylori, CCUG 15818, at 100 uM1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors.
AID182460Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 7.5 mg/kg po in rats2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Protective effects of steroid saponins from Paris polyphylla var. yunnanensis on ethanol- or indomethacin-induced gastric mucosal lesions in rats: structural requirement for activity and mode of action.
AID1070215Inhibition of Trichomonas vaginalis uridine nucleoside ribohydrolase using 5-fluorouridine as substrate at 0.04 to 200 uM after 40 mins by NMR spectrometric analysis2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase.
AID561503Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in luminal mucus layer at 0.25 mg, ip administered as two doses in 8 hrs dosing interval measured after 90 mins post last dose2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID348840Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as maximum response of intracellular calcium mobilization by FLIPR assay relative to D-Phe-Gln-Trp-Ala-Val-beta-Ala-His-Phe-Nle-NH22008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID561688Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in luminal mucus layer at 0.25 mg, ip administered as two subsequent doses in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID561683Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial disorientation in 15 to 25 um above the Juxtamucosal layer at 20 uM, ip administered as single dose through dialysis measured after 90 mins post las2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID379410Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 15 mg/kg, po administered 1 hr prior to ethanol challenge relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Triterpene saponins with gastroprotective effects from tea seed (the seeds of Camellia sinensis).
AID1756359Metabolic stability in human hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID558342Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM treated 6 hr postinfection measured after 16 hrs of postinfection by flow cytometry2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID289454Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 0.3 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID558344Antimicrobial activity against sifA gene-deficient Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as growth inhibition at 200 uM after 2 to 16 hrs postinfection by flow cytometry relative to untreated control2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Omeprazole antagonizes virulence and inflammation in Salmonella enterica-infected RAW264.7 cells.
AID561691Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial orientation in 15 to 25 um above the Juxtamucosal layer at 0.25 mg, ip administered as two subsequent doses in 8 hrs dosing interval2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID60001Inhibition of histamine-stimulated gastric acid secretion in conscious Heidenhain pouch dog after intravenous administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1220676Activity of human recombinant CYP2C19.15 mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1220669Activity of human recombinant CYP2C19.1A mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1379264Inhibition of hydrogen potassium ATPase in goat stomach mucosal membrane assessed as decrease in inorganic phosphate production using ATP as substrate after 10 to 15 mins by spectrophotometric analysis relative to omeprazole
AID289455Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 0.3 mM of ATP2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID561703Antibacterial activity against Helicobacter pylori SS1 infected in Mongolian gerbils assessed as bacterial density in mucus in central mucus layer at 0.25 mg, ip administered as two doses in 24 hrs dosing interval measured after 90 mins post last dose (Rv2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1220637Activity of human recombinant CYP2C19 F168L mutant expressed in Saccharomyces cerevisiae BJ5457 assessed asomeprazole 5'-hydroxylation per pmol protein after 60 mins2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
Evaluation of the effects of 20 nonsynonymous single nucleotide polymorphisms of CYP2C19 on S-mephenytoin 4'-hydroxylation and omeprazole 5'-hydroxylation.
AID1473870AUC in human at 20 to 40 mg, iv QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID176170Compound was tested in vivo for gastric antisecretory activity after 5 hr of pylorus ligation of SD rat1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.
AID561697Cmax in Mongolian gerbils plasma at 0.5 mg, ip2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Specific therapeutic schemes of omeprazole affect the orientation of Helicobacter pylori.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1802994UDP-glucuronosyltransferase Activity Assay from Article 10.3109/14756366.2010.518965: \\The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors.\\2011Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 26, Issue:3
The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors.
AID1802380Optical Titration Assay from Article 10.1074/jbc.M113.479717: \\Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.\\2013The Journal of biological chemistry, Aug-30, Volume: 288, Issue:35
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,515)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990526 (6.18)18.7374
1990's3126 (36.71)18.2507
2000's3188 (37.44)29.6817
2010's1304 (15.31)24.3611
2020's371 (4.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 105.41

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index105.41 (24.57)
Research Supply Index9.38 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index277.75 (26.88)
Search Engine Supply Index2.80 (0.95)

This Compound (105.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2,737 (30.13%)5.53%
Reviews962 (10.59%)6.00%
Case Studies867 (9.54%)4.05%
Observational19 (0.21%)0.25%
Other4,500 (49.53%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (386)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Proton Pump Inhibitor (PPI) Response in Eosinophilic Esophagitis Assessed by Transnasal Endoscopy (TNE) [NCT04149470]Phase 490 participants (Anticipated)Interventional2020-10-07Recruiting
Evaluation of the Effects of GERDOFF in Combination With a 6-week Therapy Based on Proton Pump Inhibitors Versus Proton Pump Inhibitors Alone on GERD-high Symptoms in Patients With Primary Diagnosis of Gastroesophageal Reflux Disease. [NCT03793556]72 participants (Actual)Interventional2017-05-05Completed
A Study to Evaluate the Effect of Coadministration of a Proton Pump Inhibitor (Omeprazole) on the Pharmacokinetics of BMS-986205 in Healthy Subjects [NCT03936374]Phase 116 participants (Actual)Interventional2019-05-08Completed
Randomized Drug Interaction Study of RO4929097 for Advanced Solid Tumors [NCT01218620]Phase 117 participants (Actual)Interventional2010-09-30Completed
A Randomized, Placebo-controlled, Two-period, Two-treatment, Two Sequence, Cross-over Pharmacodynamic and Pharmacokinetic Interaction Study After 5-days Repeated Oral Doses of Clopidogrel (300 mg Loading Dose Followed by 75 mg/Day) Alone or Given With Ome [NCT01129388]Phase 172 participants (Actual)Interventional2009-03-31Completed
Comparing Omeprazole With Fluoxetine for Treatment of Non Erosive Reflux Disease and Its Subgroups: a Double-blind Placebo-controlled Clinical Trial [NCT01269788]Phase 2/Phase 3144 participants (Actual)Interventional2010-08-31Completed
A Randomized, Two-treatment, Two-period, Two-sequence, Single Dose, Crossover Bioequivalence Study to Compare Omeprazole 40 mg DR Capsules Dr. Reddy's Laboratories Ltd.,With Prilosec® 40 mg Merck & Co., Inc.,USA Under Fed Condition [NCT01170182]Phase 154 participants (Actual)Interventional2006-02-28Completed
Helicobacter Pylori Eradication Using a Bismuth Quadruple Therapy Among Asymptomatically Infected Adults in El Paso, Texas: A Pilot Study. [NCT01335334]Phase 450 participants (Anticipated)Interventional2011-03-31Recruiting
A Open-Label, Two-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of Leritrelvir With Midazolam, Omeprazole, Rosuvastatin, Verapamil, and Rifampin in Healthy Participants [NCT06031454]Phase 156 participants (Anticipated)Interventional2023-09-01Recruiting
"Single-center, Randomized, Five-way Crossover Study to Investigate Low-dose Combinations of Caffeine, Efavirenz, Losartan, Omeprazole, Metoprolol, Chlorzoxazone and Midazolam (Basel Cocktail) for Simultaneous Phenotyping of CYP1A2, CYP2B6, CYP2C9, CYP2C1 [NCT01187862]Phase 116 participants (Actual)Interventional2010-07-31Completed
Randomized Controlled Trial Comparing Fluticasone Plus Omeprazole With Fluticasone Alone for Eosinophilic Esophagitis [NCT03781596]Phase 4100 participants (Anticipated)Interventional2018-10-02Recruiting
THE EFFECT OF HELICOBACTER PYLORI ERADICATION THERAPY TO GASTRIC WALL THICKNESS BEFORE THE LAPAROSCOPIC SLEEVE GASTRECTOMY [NCT03757650]Phase 43 participants (Actual)Interventional2018-10-01Completed
A Pharmacokinetic/Pharmacodynamic Study to Evaluate the Effect of Omeprazole of Vicagrel in Healthy Subjects [NCT05651074]Phase 120 participants (Anticipated)Interventional2022-11-14Recruiting
Exploratory Study of the Impact of Lactobacillus Rhamnosus GG on Proton Pump Inhibitor-Induced Gut Dysbiosis [NCT05517928]30 participants (Anticipated)Interventional2023-03-03Recruiting
An Open-label Study to Evaluate the Impact of Omeprazole, A Proton Pump Inhibitor, on the Pharmacokinetics of Sotorasib Co-administered With an Acidic Beverage in Healthy Volunteers [NCT05497557]Phase 116 participants (Actual)Interventional2022-08-04Completed
Comparison of Nexium Versus Secretol in the Healing and Controlling of Symptoms in Gastroesophageal Reflux Disease(GERD)Patients With Severe Erosive Esophagitis(EE). [NCT01129713]Phase 1/Phase 240 participants (Anticipated)Interventional2010-05-31Recruiting
A Randomized Controlled Trial of Triple Therapy With Conventional Proton Pump Inhibitor vs Triple Therapy With Vonoprazan as First Line Therapy for Helicobacter Pylori Gastritis [NCT03908619]Phase 4252 participants (Anticipated)Interventional2019-04-16Recruiting
Impact of Omeprazole and Fluvoxamine on Platelet Response to Clopidogrel. a Randomized, Double-blind Placebo Controlled, Crossover Trial [NCT01269333]Phase 115 participants (Actual)Interventional2011-01-31Completed
Treatment Outcomes in Patients With Globus: A Randomized Control Trial of Psychoeducation, Anxiolytics and Proton Pump Inhibitors [NCT03205228]Phase 340 participants (Actual)Interventional2017-07-07Completed
A Single-center, Open-label, Two-period, Fixed-sequence Study to Investigate the Effect of a Single Oral Dose of ACT-1014-6470 on the Pharmacokinetics of Omeprazole, Midazolam, and Their Metabolites in Healthy Male Subjects [NCT05123820]Phase 120 participants (Actual)Interventional2021-11-13Completed
A Phase 1, Open-label, Drug Interaction Study to Evaluate the Effect of Guselkumab (CNTO 1959) on Cytochrome P450 Enzyme Activities Following a Single Subcutaneous Administration in Subjects With Moderate to Severe Plaque-type Psoriasis [NCT02397382]Phase 116 participants (Actual)Interventional2015-06-18Completed
[NCT02391688]Phase 130 participants (Actual)Interventional2014-11-30Completed
A Two Part, Randomized, Open-label, Cross Over Study in Healthy Elderly Participants to Evaluate the Relative Bioavailability of Hydrobromide Salt Tablet Formulations of Danirixin in the Fed and Fasted States, and to Evaluate the Effect of Food and Gastri [NCT03457727]Phase 140 participants (Actual)Interventional2018-03-07Completed
A Phase 1, Multi-center, Open-label, 3-arm, Fixed Sequence Study to Assess the Effect of Co-administration of AZD9833 on the Pharmacokinetics of Midazolam (CYP3A4/5 Substrate), of Omeprazole (CYP2C19 Substrate), of Celecoxib (CYP2C9 Substrate) and of Dabi [NCT05438303]Phase 159 participants (Actual)Interventional2022-06-13Completed
A New System for Diagnosis and Treatment of Gastroesophageal Refulx Diseases : Based on Endoscopy, pH Parameter, Impedence Parameter, High Resolution Manometry and Psychology [NCT03600974]200 participants (Anticipated)Observational2019-02-01Not yet recruiting
Efficacy of Proton Pump Inhibitors in Cirrhotic Patients With Acute Variceal Bleeding [NCT05624229]Phase 4672 participants (Anticipated)Interventional2023-10-01Not yet recruiting
An Open-Label Drug Interaction Study in Healthy Subjects to Evaluate the Effects of Multiple Doses of JNJ55308942 on the Cytochrome P450 CYP3A4, CYP2D6 and CYP2C19 Activity and on the Pharmacokinetics of Levonorgestrel/Ethinyl Estradiol [NCT03547024]Phase 114 participants (Actual)Interventional2018-06-08Completed
A Multi-center, Double-blind, Randomized, Parallel Study to Evaluate the Efficacy and Safety of Sodium Alginate Oral Suspension (50 mg/ml) in Comparison to Omeprazole (20 mg/Cap) to Treat Non-erosive Gastro-esophageal Reflux Disease (NERD) [NCT01338077]Phase 3195 participants (Actual)Interventional2010-10-31Completed
An Open-label, Multi Centre Drug-drug Interaction Trial to Investigate the Effects of Tralokinumab on the Pharmacokinetics of Selected Cytochrome P450 Substrates in Adult Subjects With Moderate-to-severe Atopic Dermatitis [NCT03556592]Phase 140 participants (Actual)Interventional2018-08-13Completed
The Study of the Diagnosis of Eustachian Tube Dysfunction (ETD): Identifying the Relationship of Ear Fullness to Laryngopharyngeal Reflux (LPR) [NCT02123498]Phase 40 participants (Actual)InterventionalWithdrawn(stopped due to IRB not approved)
The Effect of Multiple Doses of BI 187004 on the Single Dose Pharmacokinetics of Cytochrome P450 Substrates (Caffeine, Warfarin, Omeprazole, Metoprolol and Midazolam) and a P-glycoprotein Substrate (Digoxin) Administered Orally in an Open-label, One-seque [NCT02254148]Phase 124 participants (Actual)Interventional2014-10-31Completed
An Open-label Therapeutic Efficacy Study of Tirosint (Levothyroxine Sodium) Capsules in Thyroidectomized Patients Taking Proton Pump Inhibitors [NCT03094416]Phase 466 participants (Actual)Interventional2018-07-30Completed
An Open-label, Randomized, 4-treatment, 3-period, Crossover Interaction Study, Evaluating the Effect of Esomeprazole 40 mg, Omeprazole 80 mg or Lansoprazole 60 mg on the Pharmacodynamics and the Pharmacokinetics of Clopidogrel in Healthy Volunteers [NCT01147588]Phase 1149 participants (Actual)Interventional2010-05-31Completed
A Prospective Randomized, Multi-center Study to Assess the Safety and Efficacy of Mucosta (Rebamipide), in Combination With Omeprazole as Adjuvant Therapy in Gastric Ulcer Patients [NCT01150162]Phase 3129 participants (Actual)Interventional2010-10-31Completed
A Phase I, Non-randomized Open-label Study to Evaluate the Effect of BAY73-4506 (Regorafenib) on Probe Substrates of CYP 2C9 (Warfarin), 2C19 (Omeprazole) and 3A4 (Midazolam) in a Cocktail Approach (Group A) and on a Probe Substrate of CYP 2C8 (Rosiglitaz [NCT01287598]Phase 141 participants (Actual)Interventional2011-08-02Completed
Effect of Inhibitors of the Proton Pump on Intestinal Transporters and Their Impact on the Pharmacokinetics of Dabigatran - Mechanistic and Clinical Approach -BIPP Study [NCT02524210]Phase 112 participants (Actual)Interventional2014-05-31Completed
A Phase 1, Open-label, Study in Subjects With Rheumatoid Arthritis to Evaluate the Effect of a Single Dose of Olokizumab on the Pharmacokinetics of Substrates for CYP1A2, CYP2C9, CYP2C19, and CYP3A4 [NCT04246762]Phase 116 participants (Actual)Interventional2021-04-06Completed
Relief of Heartburn and Epigastric Pain Comparing Neobianacid® With Omeprazole: a Randomized, Double Blind, Double Dummy, Reference Product Controlled, Parallel Group, Non-inferiority Clinical Study [NCT03238534]Phase 4275 participants (Actual)Interventional2017-09-12Completed
Double-Blind, Triple Dummy, Parallel-Group, Randomized, Six-Month Study To Compare Celecoxib (200 Mg BID) With Diclofenac Sr (75 Mg BID) Plus Omeprazole (20 Mg QD) For Gastrointestinal Events In Subjects With Osteoarthritis And Rheumatoid Arthritis At Hig [NCT00141102]Phase 44,484 participants (Actual)Interventional2005-10-31Completed
A Phase 1 Open-label Study to Assess the Effect of BMS-986419 on the Single Dose Pharmacokinetics of Probe Substrates (Caffeine, Bupropion, Flurbiprofen, Omeprazole, Midazolam, and Fexofenadine) in Healthy Participants [NCT05932277]Phase 122 participants (Actual)Interventional2023-06-29Completed
Effect of Acute Ethanol Consumption on The Activity of Major Cytochrome P450 Enzymes, NAT2 and P-glycoprotein [NCT02515526]16 participants (Actual)Interventional2015-06-30Completed
A Phase I Open-label Study to Evaluate the Effect of Multiple Doses of AZD1775 on the Pharmacokinetics of Substrates for CYP3A, CYP2C19, CYP1A2 and to Provide Data on the Effect of AZD1775 on QT Interval in Patients With Advanced Solid Tumours [NCT03333824]Phase 133 participants (Actual)Interventional2017-12-01Completed
A Study to Evaluate the Effect of Multiple Doses of 500 mg of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Warfarin, Omeprazole, Caffeine, and Dextromethorphan Dosed Orally and Midazolam Dosed IV, in Healthy Male Volunteers [NCT02256813]Phase 120 participants (Actual)Interventional2005-09-30Completed
A Double-blind, Randomized, Placebo-controlled Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Ascending Oral Doses of ASP8477 in Healthy Postmenopausal Females and Healthy Young Vasectomized Males, Including a Fo [NCT02220777]Phase 172 participants (Actual)Interventional2010-11-30Completed
Phase I Study in Healthy Subjects to Evaluate the Pharmacodynamics (PD) of AZD1722 Given With and Without Food (Part A) and a 2-way Crossover to Evaluate the PD of AZD1722 Given as a Free-base Tablet With and Without Omeprazole (Part B) [NCT02226783]Phase 137 participants (Actual)Interventional2013-03-31Completed
Effectiveness of Vonoprazan vs Omeprazole as Empiric Therapy for Gastroesophageal Reflux Disease (GERD) Patients Without Alarm Features in a Primary Care Setting: A Pragmatic, Randomized, Single Blind Study [NCT04028466]Phase 482 participants (Actual)Interventional2019-05-26Terminated(stopped due to Budget for the study was withdrawn and discontinued)
Open-Label Pharmacokinetics Study to Evaluate Drug-Drug Interactions and Safety of ELPIDA® in Co-Administration With Other Drugs in Healthy Volunteers [NCT03709355]Phase 156 participants (Actual)Interventional2018-11-14Completed
Cocktail Phenotypic Approach to Explore Antidepressant Pharmacokinetic Variability: a Pilot Study [NCT02438072]100 participants (Anticipated)Interventional2014-12-31Recruiting
Study of Nitazoxanide (NTZ) Based New Therapeutic Regimens for Helicobacter Pylori [NCT02422706]Phase 3120 participants (Anticipated)Interventional2015-01-31Recruiting
A Phase Ib Study to Assess the Safety, Tolerability and Immunologic Activity of Preoperative IRX 2 In Early Stage Breast Cancer [NCT02950259]Phase 116 participants (Actual)Interventional2017-02-09Active, not recruiting
Influence of the Acidic Beverage Cola on the Absorption of the HCV Agent Velpatasvir in Healthy Volunteers Being Treated With the Proton Pump Inhibitor Omeprazole. [NCT03513393]Phase 111 participants (Actual)Interventional2018-08-01Completed
Effects of Concomitant Administration of BMS-986195 on the Single-dose Pharmacokinetics of Methotrexate and Probe Substrates for Cytochrome P450 1A2, 2C8, 2C9, 2C19, 3A4, Organic Anion Transporter Polypeptide 1B1 and P-glycoprotein in Healthy Participants [NCT03131973]Phase 126 participants (Actual)Interventional2017-05-13Completed
Indomethacin for Refractory Chronic Cough: a Randomized, Double-blind, Placebo-controlled Trial [NCT03662269]Phase 384 participants (Anticipated)Interventional2018-10-22Recruiting
Evaluation of the Effect of Ixekizumab on the Pharmacokinetics of Cytochrome P450 Substrates in Patients With Moderate-to-Severe Plaque Psoriasis [NCT02993471]Phase 128 participants (Actual)Interventional2016-12-22Completed
Buspirone Plus Omeprazole for Functional Dyspepsia: A Randomised Placebo Clinical Trial [NCT03444831]Phase 470 participants (Actual)Interventional2016-03-01Completed
Effect of the CYP2C19 Polymorphism in Helicobacter Pylori Eradication [NCT03650543]Phase 4133 participants (Actual)Interventional2012-09-10Completed
Assessment of Gastric pH Changes Induced by Ascorbic Acid Tablets [NCT04199624]Phase 110 participants (Anticipated)Interventional2021-10-01Recruiting
Relation of Metabolic Rate of Omeprazole and Eradication of Helicobacter Pylori Infection - A Combination of Clinical and Pharmacogenetic Study [NCT00854451]Phase 4128 participants (Actual)Interventional1996-08-31Completed
Bioequivalence Study of 20 mg Omeprazole Capsules in Indonesia Healthy Subject [NCT05849883]36 participants (Actual)Interventional2020-12-10Completed
The Effect of Multiple Doses of BI 730357 on the Single Dose Pharmacokinetics of Caffeine, Warfarin, Omeprazole and Midazolam Administered Orally as a Cocktail in Healthy Subjects (an Open-label, Two-period Fixed Sequence Design Trial) [NCT04679948]Phase 116 participants (Actual)Interventional2020-12-21Completed
A Randomised, Placebo-controlled Trial of Omeprazole in Idiopathic Pulmonary Fibrosis (IPF) [NCT02085018]Phase 245 participants (Actual)Interventional2014-03-28Completed
High-Dose Dual Therapy vs Standard Triple Therapy for Treatment-Naïve H. Pylori: A Prospective Randomized Control Trial in a Diverse Urban New York City Population [NCT05342532]Phase 4112 participants (Actual)Interventional2019-06-12Completed
Effects of Type 2 Diabetes on CYP450s Activities; Intersubject Variability in Drug Metabolism. [NCT02291666]Phase 473 participants (Actual)Interventional2015-04-30Completed
A Phase I, Open Label Study to Assess the Effects of PQ912 on the Pharmacokinetics of Midazolam and Omeprazole in Healthy Male Subjects [NCT02190708]Phase 118 participants (Actual)Interventional2014-06-30Completed
Clinical Trials on Evaluate the Red Ginseng and Fermented-Red Ginseng Affect to Drug Metabolizing Enzyme and Transporter in Healthy Volunteers; Open-label, Parallel Group [NCT02056743]Phase 130 participants (Actual)Interventional2013-09-30Completed
A Trial Investigating the Influence of Omeprazole on the Pharmacokinetics of Oral Semaglutide in Healthy Subjects [NCT02249871]Phase 154 participants (Actual)Interventional2014-09-24Completed
Randomized, Double-Blind, Placebo-Controlled, Non-inferiority Clinical Trial on the Efficacy and Safety of Houtou Jianweiling Tablet in the Treatment of Chronic Non-Atrophic Gastritis [NCT04672018]Phase 2240 participants (Actual)Interventional2022-11-08Completed
Helicobacter Pylori and Chronic Dyspepsia in Eastern Uganda [NCT04525664]Early Phase 1376 participants (Actual)Interventional2018-10-01Completed
A Randomized, Placebo-controlled, Two-period, Two-treatment, Two Sequence, Cross-over Pharmacodynamic and Pharmacokinetic Interaction Study After 5-days Repeated Oral Doses of Clopidogrel (600 mg Loading Dose Followed by 150 mg/Day) Alone or Given Concomi [NCT01129414]Phase 172 participants (Actual)Interventional2009-06-30Completed
Evaluation of the Effects of Single Oral Dose and Multiple Oral Doses of BI 201335 NA on Cytochrome P450 and P-glycoprotein Activity Using a Probe Drug Cocktail. An Open-label, Single-arm Phase I Study in Healthy Human Volunteers [NCT02182336]Phase 123 participants (Actual)Interventional2008-06-30Completed
A Single Dose, Comparative, Open-label, Randomized, Crossover Bioequivalence Study of Omeprazole Administered as Zegerid® Powder for Oral Suspension 20 mg and Prilosec 40 mg Capsule in Healthy Subjects [NCT01337804]Phase 150 participants (Actual)Interventional2011-01-31Completed
A Randomized, Placebo-controlled, Two-period, Two-treatment, Two Sequence, Cross-over Pharmacodynamic and Pharmacokinetic Interaction Study After 5-days Repeated Oral Doses of Clopidogrel (300 mg Loading Dose Followed by 75 mg/Day) Alone or Given Concomit [NCT01129375]Phase 172 participants (Actual)Interventional2009-02-28Completed
[NCT01136317]Phase 20 participants Interventional2010-04-30Completed
A Single-Dose, Open-label, Randomized, Crossover, Drug-Drug Interaction Study of Nifedipine Extended-release Tablets With or Without Multiple-dose Administration of Proton-Pump Inhibitor Omeprazole/Sodium Bicarbonate in Healthy Volunteers [NCT03100838]Phase 164 participants (Actual)Interventional2017-03-20Completed
A Randomized, Two-treatment, Two-period, Two-sequence, Single Dose, Crossover Bioequivalence Study to Compare Omeprazole 40 mg DR Capsules Dr. Reddy's Laboratories Ltd.,With Prilosec® 40 mg Merck & Co.Inc., USA Under Fasting Conditions [NCT01170169]Phase 144 participants (Actual)Interventional2006-01-31Completed
A Fixed-Sequence Trial to Examine the Effect of Multiple-Dose CT1812 Administration on Standard Probes of CYP2C19 (Omeprazole), CYP2C9 (Tolbutamide), CYP2D6 (Dextromethorphan), and CYP3A4/5 (Midazolam) Activity in Healthy Adult Volunteers [NCT03716427]Phase 116 participants (Actual)Interventional2016-11-10Completed
A Randomised, Single Blind, Two-way Cross-over, Single-centre Study to Assess the Pharmacodynamics (Intragastric pH) and Pharmacokinetics After Repeated Oral Administration of D961H 10 mg and Omeprazole 10 mg in Japanese Healthy Male Subjects [NCT01159145]Phase 142 participants (Anticipated)Interventional2010-07-31Completed
A Randomized Double Blind Active Comparator Controlled Phase III Study to Assess the Safety and Efficacy of RHB-105 in the Treatment of Confirmed Helicobacter Pylori (H. Pylori) Infection [NCT03198507]Phase 3455 participants (Actual)Interventional2017-06-18Completed
Safety and Efficacy of Oral Administration of Anti-CD3 Monoclonal Antibody in Patients With the Metabolic Syndrome PHASE IIa A Single-blinded Placebo-controlled Clinical Trial [NCT01205087]Phase 236 participants (Anticipated)Interventional2010-09-30Completed
High Eradication Rate of Helicobacter Pylori Infection With Moxifloxacin-Based Triple Therapy in Comparison With Levofloxacin-Based Sequential Therapy: Randomized Controlled Trials [NCT05863858]Phase 3162 participants (Actual)Interventional2020-06-01Completed
Oral Anti-CD3 for the Treatment of Active Ulcerative Colitis [NCT01287195]Phase 1/Phase 26 participants (Actual)Interventional2011-04-07Completed
Randomized, Placebo-Controlled, Crossover Pharmacodynamic Study Comparing the Effects of Two Different Forms of Omeprazole [NCT01077076]Phase 330 participants (Actual)Interventional2008-12-31Completed
A Phase 1, Open-label, Drug-Drug Interaction Study to Investigate the Effect of Rocatinlimab (AMG 451) on the Pharmacokinetics of Multiple CYP450 Substrates in Patients With Moderate to Severe Atopic Dermatitis [NCT05891119]Early Phase 120 participants (Anticipated)Interventional2023-06-03Recruiting
A Phase 1, Single-center, Open-label, Sequential Study to Evaluate the Drug-drug Interaction Potential of BMS-986196 in Healthy Participants [NCT05852769]Phase 118 participants (Actual)Interventional2023-05-31Completed
BRAIN MECHANISMS FOR CLINICAL PLACEBO IN CHRONIC PAIN: A Partially-Blind Randomized Clinical Trial of Placebo and Chronic Back Pain [NCT02013427]Phase 482 participants (Actual)Interventional2014-10-31Completed
A Phase 1, Single and Multiple-Dose, Open-Label Study in Healthy Subjects to Assess the Effect of the Acid Reducing Agents, Omeprazole (OME) and Famotidine (FAM), on the Pharmacokinetics (PK) of Cenicriviroc Mesylate (CVC) [NCT02684799]Phase 148 participants (Actual)Interventional2016-01-31Completed
Double-Blind, Placebo-Controlled, Randomized Two-Week Study, Comparing Small Bowel Lesions Associated With Celecoxib (200 mg BID) vs. Ibuprofen (800 mg TID) Plus Omeprazole (20 mg QD) [NCT00640809]Phase 4408 participants (Actual)Interventional2003-10-31Completed
A Single-center, Single-arm, Open-label, Fixed-sequence, Self-controlled Study of the Effects of HRS5091 on the Pharmacokinetics of Midazolam, S-warfarin, Omeprazole, Digoxin and Rosuvastatin in Healthy Volunteers [NCT05273775]Phase 122 participants (Actual)Interventional2022-04-29Completed
Randomized, Crossover, Pharmacodynamic Study Comparing the Effects of Two Proton Pump Inhibitors [NCT01005719]Phase 363 participants (Actual)Interventional2009-09-30Completed
An 8 Week Non-selected Cohort Study to Investigate Whether the Treatment of Reflux Induced Cough Alters Associated Bronchial Hyper-responsiveness [NCT00668317]Phase 35 participants (Actual)Interventional2006-09-30Terminated(stopped due to Primary care physicians began prescribing antacid therapy for chronic cough)
Efficacy and Safety of Quadruple Therapy by Bismuth Subcitrate Potassium, Metronidazole, and Tetracycline Given X 10 Days With Omeprazole in Eradication of Helicobacter Pylori: A Comparison to Omeprazole, Amoxicillin and Clarithromycin Given X 7 Days [NCT00669955]Phase 3440 participants (Actual)Interventional2008-06-30Completed
Effect of Eradication of Helicobacter Pylori on the Dyspeptic Symptoms. [NCT00772837]370 participants (Actual)Interventional2006-08-31Completed
Tailored Therapy Versus Standard Triple Therapy for Helicobacter Pylori Eradication in Children: A Randomized Trial [NCT02635191]Phase 4200 participants (Anticipated)Interventional2014-03-31Recruiting
Clopidogrel Pharmacogenetics Bench to Bedside - A Practical Application [NCT01341600]18 participants (Actual)Interventional2010-07-31Completed
Effects of Different Omeprazole Dosing on Gastric pH in Non- Variceal Upper Gastrointestinal Bleeding: A Randomized Prospective Study [NCT03980496]Phase 450 participants (Actual)Interventional2010-09-09Completed
Study of the Effect of PROGRESSive Withdrawal Esomeprazole of on Acid-related Symptoms, PROGRESS Study A Randomized, Placebo-controlled, Double Blinded Study [NCT02476097]Phase 458 participants (Anticipated)Interventional2015-06-30Active, not recruiting
The Effect of Helicobacter Pylori Eradication on Liver Fat Content in Subjects With Non-alcoholic Fatty Liver Disease [NCT01876108]Phase 2100 participants (Anticipated)Interventional2012-07-31Completed
A Study in Healthy Subjects to Assess the Multiple- Dose Pharmacokinetics of Three AF-219 Formulations [NCT02790840]Phase 132 participants (Actual)Interventional2016-05-16Completed
A Study to Investigate the Effects of Multiple Doses of BI 425809 on the Single Dose Pharmacokinetics of Cytochrome P450 Substrates (Midazolam, Warfarin and Omeprazole) and a P Glycoprotein Substrate (Digoxin) Administered Orally in an Open-label, One-seq [NCT02783040]Phase 113 participants (Actual)Interventional2015-09-30Completed
DLBS2411 Treatment for Ulcer Healing in Non-Bleeding Peptic Ulcers [NCT02262169]Phase 332 participants (Actual)Interventional2014-10-31Terminated(stopped due to This study was terminated due to internal technical issues at study site)
A Randomized Phase 2 Trial of Neoadjuvant and Adjuvant Therapy With the IRX 2 Regimen in Patients With Newly Diagnosed Stage II, III, or IVA Squamous Cell Carcinoma of the Oral Cavity [NCT02609386]Phase 2105 participants (Actual)Interventional2015-12-31Completed
A Randomized, Placebo-controlled ,Double-blind, Phase IIa Assessment of the Safety of Foralumab, an Oral Anti-CD3 Antibody, in Patients With Nonalcoholic Steatohepatitis (NASH) and Type 2 Diabetes Mellitus (T2DM) [NCT03291249]Phase 20 participants (Actual)Interventional2017-12-01Withdrawn(stopped due to Due to MOH request.)
An Open-Label, Maximal Use Study Evaluating the Drug Interaction Potential of Luliconazole Cream 1% in Subjects With Tinea Pedis and Tinea Cruris [NCT02394340]Phase 420 participants (Actual)Interventional2015-02-03Completed
Prevalence and Predictors of Proton Pump Inhibitor Partial Response in Gastroesophageal Reflux Disease in Systemic Sclerosis [NCT03561233]Phase 1250 participants (Actual)Interventional2013-05-31Completed
The Effect of Multiple Doses of Cenobamate (YKP3089) on the Single Dose Pharmacokinetics of Cytochrome P450 Substrates (Midazolam, Warfarin, Omeprazole and Bupropion) Administered Orally in an Open-label, One-sequence Study in Healthy Subjects [NCT03234699]Phase 124 participants (Actual)Interventional2017-02-22Completed
Open, Comparative Study To Evaluate The Performance And Safety Of The Medical Device Marial® In Association With Proton-Pump Inhibitors Versus PPI Alone In Patients Affected By Gastroesophageal Reflux Disease [NCT04130659]110 participants (Anticipated)Interventional2019-08-08Recruiting
Research of Efficient Use of Omeprazole in Combination With Domperidone in Gastroesophageal Reflux Disease of Mild to Moderate Severity [NCT02140073]Phase 460 participants (Anticipated)Interventional2013-12-31Active, not recruiting
A Single-centre, Open-label Study in Healthy Adult Volunteers to Determine the Effects of Multiple-dose Omeprazole (ANTRA® 40 mg qd) on the Single-dose Pharmacokinetics of Tipranavir 500 mg Coadministered With Ritonavir 200 mg [NCT02253875]Phase 115 participants (Actual)Interventional2005-11-30Completed
PROUD Study - Preventing Opioid Use Disorders [NCT04766996]Phase 457 participants (Actual)Interventional2021-05-17Terminated(stopped due to Loss of surgery team member deemed the study procedures impossible to achieve, and no replacement could be found in a timely manner to complete trial as initially planned.)
Rectal and Oral Omeprazole Treatment of Gastroesophageal Reflux in Infants With Esophageal Atresia or Congenital Diaphragmatic Hernia; A Pharmacodynamic and Pharmacokinetic Study. [NCT00226044]Phase 317 participants (Actual)Interventional2005-09-30Completed
The Effect of NSAIDs After a Rotator Cuff Repair Surgery. A Prospective Randomized Controlled Trial [NCT02153177]Phase 40 participants (Actual)Interventional2015-01-31Withdrawn(stopped due to The study was withdrawn prior to any participants being enrolled.)
An Open-label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Cytochrome P450 Probe Drugs in Healthy Adult Subjects [NCT00964106]Phase 187 participants (Actual)Interventional2009-08-26Completed
An Open-Label, Multicenter, Two-Part, Phase 1 Study to Characterize the Effects of a Moderate CYP3A Inhibitor on the Pharmacokinetics of Tazemetostat (EPZ-6438) (Part A), the Effects of Tazemetostat on the Pharmacokinetics of CYP2C8 and CYP2C19 Substrates [NCT03028103]Phase 132 participants (Actual)Interventional2017-03-27Completed
Influence of Rabeprazole on the Magnitude of the Antiplatelet Action of Clopidogrel. A Prospective, placebo-and Active Treatment-controlled, Open Label, Randomized 3-way Cross Over Study in Healthy Subjects [NCT00989300]Phase 139 participants (Actual)Interventional2009-11-30Completed
Role of CYP2C19 Polymorphism in the Drug Interaction Between Clopidogrel and Omeprazole [NCT01094275]75 participants (Actual)Observational [Patient Registry]2010-01-31Completed
Comparison of Voice Therapy and Antireflex Therapy in the Treatment of Laryngopharyngeal Reflux-related Hoarseness: A Prospective Randomized Control Trial [NCT02530879]Phase 40 participants (Actual)Interventional2016-05-31Withdrawn(stopped due to Inability to recruit patients)
Integrated Approaches to Food Allergen and Allergy Risk Management: iFAAM: The Impact of Proton-pump Inhibitors (Antacids) on Threshold Dose Distributions [NCT02552537]Phase 444 participants (Actual)Interventional2015-09-30Completed
Open Label Balanced Randomized,Two-treatment,Two-period,Two-sequence,Single Dose,Crossover Oral Bioequivalence Study of Omeprazole Mg 20mg DR Capsules With Prilosec OTCTM 20mg in 38 Healthy,Adult,Human Subjects Under Fasting Conditions [NCT01045642]Phase 138 participants (Actual)Interventional2006-12-31Completed
A Single-center, Open-label, Four-period, Fixed-sequence Study to Investigate the Effect of Single and Repeated Oral Doses of ACT-539313 on the Pharmacokinetics of Flurbiprofen, Omeprazole, Midazolam, and Their Respective Metabolites in Healthy Subjects [NCT05254548]Phase 122 participants (Actual)Interventional2022-02-18Completed
Profiling Study for the Hepatic Cytochrome P450 (CYP) Isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A in Healthy Subjects and in Patients With Stage 4 (F4) Liver Fibrosis / Cirrhosis by the Combined Administration of the Probe Substrates (the Cocktail) [NCT05741385]30 participants (Anticipated)Interventional2023-04-25Recruiting
A Phase 1, Open Label, Single Center, Randomized, Six-Sequence, Crossover Study to Evaluate the Effect of Food, Formulation Strength, and a Proton Pump Inhibitor on GED 0301 Pharmacokinetics in Healthy Adult Subjects [NCT02957474]Phase 118 participants (Actual)Interventional2016-11-30Completed
Low Dose Against High Dose of Proton Pump Inhibitors in Treatment Acute Peptic Ulcer Bleeding [NCT02724150]Phase 40 participants (Actual)Interventional2017-12-01Withdrawn(stopped due to No participants enrolled)
Comparison of High Dose Infusion and Low Dose Bolus Intravenous Omeprazole for Treatment of Bleeding Ulcer With Adherent Clot [NCT02536989]Phase 440 participants (Actual)Interventional2009-03-31Completed
Comparison of the Clinical Efficacy of Ketoprofen, Associated or Not With Omeprazole, in the Control of Pain, Swelling and Trismus in Lower Third Molar Removal [NCT02730026]Phase 450 participants (Actual)Interventional2015-06-30Completed
"Effect of Orally Administered Two Successive Doses of PPIs and/ or H2RAs Without or With a Prokinetic Drug, on the Intragastric pH and Volume and Bile Refluxate in Adults Patients Undergoing Elective Surgery." [NCT02703896]Phase 41,920 participants (Actual)Interventional2012-01-31Completed
The Role of Endoscopic Tri-Modal Imaging in Distinguishing Functional Dyspepsia From Reflux Disease [NCT02685150]157 participants (Actual)Interventional2016-01-31Completed
Oral Versus Intravenous Omeprazole in Management of Bleeding Peptic Ulcer: Randomized Controlled Trial [NCT04170270]Early Phase 1100 participants (Anticipated)Interventional2019-11-30Not yet recruiting
An Open-Label, Drug-Drug Interaction Study to Examine the Effects of Dupilumab on the Pharmacokinetics of Selected Cytochrome P450 Substrates in Adult Patients With Moderate to Severe Atopic Dermatitis [NCT02647086]Phase 114 participants (Actual)Interventional2015-12-31Completed
Laryngopharyngeal Reflux Health Related Quality of Life (LPR-HRQL) Questionnaire Development and Psychometric Testing in Patients Receiving Omeprazole 20 mg Bid as Treatment for Laryngopharyngeal Reflux. [NCT00641264]Phase 490 participants (Anticipated)Interventional2001-05-31Completed
Open-Label, Sequential-Design Drug Interaction Study of the Effect of Omeprazole on the Pharmacokinetics of Ibrutinib in Healthy Adults [NCT02638116]Phase 120 participants (Actual)Interventional2016-01-31Completed
Safety, Tolerability and Efficacy of FDC Ketoprofen + Omeprazole in Patients With Rheumatological Conditions With History or Who Are at Risk of Developing NSAID Associated Benign Gastric Ulcers, Duodenal Ulcers and Gastroduodenal Erosions [NCT00971581]Phase 352 participants (Actual)Interventional2009-08-31Completed
Effects of Concomitant Administration of BMS-986142 on the Single-dose Pharmacokinetics of Probe Substrates for CYP2C8, CYP2C9, CYP2C19, CYP3A4, and P-gp in Healthy Subjects [NCT02762123]Phase 128 participants (Actual)Interventional2016-05-31Completed
Argon Plasma Coagulation for Barrett's Esophagus With Low Grade Dysplasia: A Randomized Trial With Long Term Follow-up Evaluating the Impact of Power Setting and Proton Pump Inhibitor Dose [NCT04154748]71 participants (Actual)Interventional2002-06-04Completed
A Randomized Controlled Trial of Transoral Incisionless Fundoplication (TIF) Versus Proton Pump Inhibitors (PPIs) for Treatment of GERD: The TIF vs. PPIs Study [NCT00857597]Phase 360 participants (Actual)Interventional2009-03-31Terminated(stopped due to Study was terminated after unplanned interim analysis of single centre data and results were reported)
Evaluation of Omeprazole Effect on Glaucoma [NCT01000220]Phase 10 participants InterventionalRecruiting
A Phase I, Open-Label, Three-Period, Fixed-Sequence Study To Estimate The Steady-State Effect Of Ketoconazole And Omeprazole On The Single-Dose Pharmacokinetics Of Dimebon [PF-01913539] In Healthy CYP2D6 EM And PM Subjects [NCT00931073]Phase 124 participants (Anticipated)Interventional2009-07-31Completed
Platelet Inhibitory Effect of Clopidogrel in Patients Treated With Omeprazole, Pantoprazole, or Famotidine [NCT00950339]Phase 463 participants (Actual)Interventional2009-08-31Completed
Efficacy and Safety of Ilaprazole for Acute Duodenal Ulcer: A Randomized,Double-Blind,Omeprazole-Controlled,Multicenter,and Phase2 Trial in China [NCT00953381]Phase 2235 participants (Actual)Interventional2004-10-31Completed
Melatonin Associated to Acid Inhibition for Chemoprevention in Barret Esophagus: a Pilot Study [NCT01566474]Phase 380 participants (Actual)Interventional2012-04-30Completed
Development of Cocktail for Measuring the Activity of Important Cytochrome P450 Enzymes [NCT00981929]412 participants (Anticipated)Interventional2009-09-30Terminated(stopped due to Unexpected non-serious adverse events)
A Phase I, Double Blind, Randomized, Two-Way Cross Over, Single- Centre Study in Healthy CYP2D6 Extensive Metabolizers and Poor Metabolizers to Investigate the Potential of AZD3480 to Inhibit Cytochrome P450 1A2, 2C19, 3A4, 2C8, 2B6 and UGT1A1 Activity [NCT00692510]Phase 118 participants (Anticipated)Interventional2007-11-30Completed
A Phase 1, Open-label, Drug Interaction Study to Evaluate the Effect of Ustekinumab on Cytochrome P450 Enzyme Activities Following Induction and Maintenance Dosing in Participants With Active Crohn's Disease or Ulcerative Colitis. [NCT03358706]Phase 157 participants (Anticipated)Interventional2018-02-02Suspended(stopped due to unavailability of probe substrates)
Effect of High-dose Oral Rabeprazole on Recurrent Bleeding After the Endoscopic Treatment of Bleeding Peptic Ulcers [NCT00838682]Phase 4106 participants (Actual)Interventional2006-04-30Terminated(stopped due to Terminated before the complete enrollment due to slow enrollment)
Impact of OCT1 Genotype and OCT1 Inhibiting Drugs on an Individual's Tolerance of Metformin [NCT02586636]Phase 461 participants (Actual)Interventional2016-03-31Completed
Does Omeprazole Decrease Intestinal Calcium Absorption? [NCT00582972]Phase 423 participants (Actual)Interventional2008-01-31Completed
Impact of Timing on the Efficacy of Omeprazole/Sodium Bicarbonate Zegerid 40 mg in Healing Reflux Esophagitis [NCT00693225]Phase 491 participants (Actual)Interventional2008-01-31Completed
An Open-Label, 3-Period, Fixed Sequence Study to Evaluate the Effect of an H2 Antagonist and a Proton Pump Inhibitor on the Single Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects [NCT05338502]Phase 120 participants (Actual)Interventional2019-07-08Completed
Helicobacter Pylori Eradication and Motor Fluctuations in Parkinson's Disease [NCT00664209]Phase 364 participants (Actual)Interventional2008-01-31Terminated(stopped due to Prevalence of H Pylori in the study population was much lower than anticipated)
A Randomized Clinical Trial to Examine the Efficacy of a Clarithromycin-, Amoxicillin-, and Metronidazole-Based Regimen to Eradicate Helicobacter Pylori Infections in Pasto, Colombia [NCT00719420]Phase 3151 participants (Actual)Interventional2006-04-30Completed
EFFICACY OF ORAL AROEIRA (Schinus Terebinthifolius Raddi), AMOXYCILLIN AND CLARITROMYCIN COMPARED WITH CONVENTIONAL TRIPLE THERAPY FOR Helicobacter Pylori ERADICATION IN GASTRITE AND SYMPTOM PATIENTS: A RANDOMIZED AND DOUBLE-BLIND STUDY [NCT04069286]Phase 2/Phase 3200 participants (Anticipated)Interventional2021-08-31Not yet recruiting
Effect of Concomitant Administration of BMS-708163 on the Pharmacokinetics of Midazolam, Warfarin, Caffeine, Omeprazole and Dextromethorphan in Healthy Male Subjects by Administration of a Modified Cooperstown Cocktail [NCT00726726]Phase 122 participants (Actual)Interventional2008-08-31Completed
Open-label, Non-randomized, Two-treatment, Single-period, Single Dose, Drug-drug Interaction Study to Evaluate the Effects of Omeprazole 40mg on the Pharmacokinetics of SPRYCEL® 100 mg Film-coated Tablets (Dasatinib) in Adult Human Subjects [NCT06145217]Phase 118 participants (Actual)Interventional2023-08-22Completed
A Phase Ib, Open-Label Study Evaluating the Safety, Pharmacokinetics, and Activity of GDC-1971 in Combination With Atezolizumab in Patients With Locally Advanced or Metastatic Solid Tumors [NCT05487235]Phase 1232 participants (Anticipated)Interventional2022-08-17Recruiting
Effect of Helicobacter Pylori Treatment on Remission of Idiopathic Central Serous Chorioretinopathy (ICSCR) [NCT00817245]Phase 1/Phase 250 participants (Actual)Interventional2008-03-31Completed
A Two Week Nitazoxanidebased Quadruple Regimen for Helicobacter Pylori Therapy After Failure of Standard Triple Therapy: A Single Center Experience [NCT02621359]Phase 3100 participants (Anticipated)Interventional2015-01-31Recruiting
Traditional Chinese Medicine Combined With Standard Triple Region for Eradication of Helicobacter Pylori: a Prospective, Double-blinded, Randomized Trial [NCT02803216]Phase 1/Phase 2576 participants (Actual)Interventional2013-01-31Completed
Evaluation of the Influence of Statins and Proton Pump Inhibitors on Clopidogrel Antiplatelet Effects [NCT00930670]Phase 4320 participants (Actual)Interventional2009-06-30Completed
The Official Study Title Exceeds the 300 Character Limit for This Field. See Detailed Study Description Section for Official Study Title. [NCT00942136]Phase 124 participants (Actual)Interventional2009-07-31Completed
Efficacy and Safety of Ilaprazole for Acute Duodenal Ulcer: A Randomized,Double-Blind,Omeprazole-Controlled,Multicenter,and Phase3 Trial in China [NCT00952978]Phase 3496 participants (Actual)Interventional2005-09-30Completed
Salivary Epidermal Growth Factor (EGF) Concentration Before and After Treatment of Reflux Laryngitis: Final Results [NCT01389401]36 participants (Actual)Observational2009-01-31Completed
Conventional Therapy vs Sequential Therapy for the Treatment of Helicobacter Pylori Infection [NCT01723059]184 participants (Anticipated)Interventional2012-02-29Recruiting
Comparison of GERD and the Effects of Anti-Reflux Therapy on Pulmonary Function Between Able-Bodied and SCI Individuals [NCT02584751]Phase 1110 participants (Anticipated)Interventional2016-08-31Recruiting
A Phase I, Open Label, Randomized, 4-way Crossover Trial to Evaluate the Pharmacokinetics of TMC278 25mg and 50mg in the Presence of Omeprazole 20mg q.d., in Healthy Subjects [NCT01001247]Phase 118 participants (Actual)Interventional2010-01-31Completed
Comparison of Gut Microbiota Composition and Systemic Inflammatory Markers Prior to and Post-Proton Pump Inhibitor Use in Older Adults [NCT02844621]Early Phase 125 participants (Actual)Interventional2016-05-31Completed
An Open-Label, 2-Part, Multicenter, Post-marketing Study to Evaluate the Effect of Moderately or Severely Active Ulcerative Colitis or Crohn's Disease on Cytochrome P-450 Enzyme Substrates Compared to Healthy Subjects and the Effect of Vedolizumab Treatme [NCT02760615]Phase 40 participants (Actual)Interventional2016-11-01Withdrawn(stopped due to No enrollment)
The Effect of Omeprazole on the Pharmacokinetics of Dasatinib (BMS-354825) in Healthy Subjects [NCT00655746]Phase 114 participants (Actual)Interventional2008-04-30Completed
Evaluation of the Effect of Food, Omeprazole, Itraconazole, and Carbamazepine on the Pharmacokinetics of LY3484356 in Healthy Females of Non-Child-Bearing Potential [NCT04840888]Phase 182 participants (Actual)Interventional2021-04-26Completed
Confocal Endomicroscopy for Non-Erosive Reflux Disease (CE NERD) [NCT02039869]0 participants (Actual)InterventionalWithdrawn(stopped due to Could not recruit patients - modifying protocol and plan resubmission to our IRB)
Proton Pump Inhibitors and the Risk of Hospitalization for Community-acquired Pneumonia: Replicated Cohort Studies With Meta-analysis [NCT02555852]4,238,504 participants (Actual)Observational2011-09-30Completed
The Use of Oral Omeprazole and Intravenous Pantoprazole in Patients With Hypersecretion of Gastric Acid [NCT00001191]Phase 20 participants Interventional1983-02-03Completed
A Phase 1, Open-Label, Single-Sequence Crossover Study in Healthy Subjects to Determine the Effect of Relacorilant on Exposure to Probe Substrates for Cytochrome P450s 3A4, 2C8, 2C9, 2C19, and 2D6 [NCT03457597]Phase 127 participants (Actual)Interventional2018-03-06Completed
A Randomized, Open-Label, Cross-Over, Dose-Ranging Study to Assess the Effect of Vecam 40/300 and Vecam 20/300 Administered at Bedtime Compared to Omeprazole 20 mg Administered Before Breakfast on Gastric pH [NCT00818870]Phase 160 participants (Anticipated)Interventional2008-12-31Completed
An Open-Label, Randomized, Crossover Study to Evaluate the Effect of Food and a Proton Pump Inhibitor on the Single-Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects [NCT05468164]Phase 119 participants (Actual)Interventional2018-05-31Completed
A Phase I, Open Label, Multi Centre Study in Healthy Volunteers to Estimate the Effect of Multiple Doses of AZD2066 on the Activity of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 by Administering a Cocktail of Caffeine, Bupropion, Tolbutamide, Omep [NCT00930306]Phase 115 participants (Actual)Interventional2009-06-30Completed
An Open-Label, Two-Way Crossover, Drug-Interaction Study to Determine the Effect of Omeprazole on the Pharmacokinetics of an Immediate-Release Capsule of CG5503 in Healthy Subjects [NCT03979989]Phase 132 participants (Actual)Interventional2005-09-28Completed
Open Label, Balanced, Randomized, Two-treatment,Two-period,Single-dose, Cross-over Oral Bioequivalence Study of Omeprazole Magnesium 20 mg DR Capsule With Prilosec® OTCTM 20 mg Tablets in Healthy Human Adult Subjects, Under Fed Conditions [NCT01045434]Phase 162 participants (Actual)Interventional2006-12-31Completed
Clopidogrel Proton-Pump Inhibitors Study [NCT01016717]Phase 40 participants (Actual)Interventional2012-12-31Withdrawn(stopped due to Since the published data resolved the study goals we decided not to start it)
The Effects of Gastric Acid Suppression on the Colonic Microbiome [NCT01901276]Phase 412 participants (Actual)Interventional2013-08-31Completed
A Phase I Open-label Study to Evaluate the Effect of Multiple Doses of MDV3100 (ASP9785) on the Pharmacokinetics of Substrates for CYP2C8, CYP2C9, CYP2C19, and CYP3A4 in Patients With Castration-resistant Prostate Cancer [NCT01911728]Phase 114 participants (Actual)Interventional2011-07-25Completed
Evaluation Of The Effect Of PF-05089771 On The Metabolism Of Multiple Cytochrome P450 And OATP1B1 Transporter Substrates [NCT01934569]Phase 117 participants (Actual)Interventional2013-09-30Completed
A Phase 0 Study of High Dose Omeprazole in Patients With Pancreatic Cancer Planning to Undergo Surgical Therapy for Evaluating Changes of Biomarkers [NCT04930991]Early Phase 160 participants (Anticipated)Interventional2021-09-07Recruiting
Comparing Different Regimens for Eradication of Helicobacter Pylori in Kuwait [NCT04617613]Phase 4603 participants (Actual)Interventional2016-09-30Completed
A Phase 1, Single-Center, Randomized, 3-Period Crossover Study to Evaluate the Relative Bioavailability of WTX101 in Healthy Subjects After Single Dose Administration of a Non-Coated Formulation With and Without a Proton Pump Inhibitor and With a Proton P [NCT05319899]Phase 118 participants (Actual)Interventional2014-01-20Completed
The Role of High-resolution Esophageal Manometry and Specific Biomarkers of Inflammation in the Diagnosis of Patients With Dysphagia and Suspected Eosinophilic Esophagitis [NCT04803162]58 participants (Actual)Observational2017-11-14Active, not recruiting
A Phase II Randomized Trial Evaluating the Use of Proton Pump Inhibitors (PPIs) in Conjunction With Chemotherapy, in Patients With Recurrent Unresectable or Metastatic Cancers of the Head and Neck [NCT02013453]Phase 20 participants (Actual)Interventional2013-12-31Withdrawn(stopped due to Lack of funding)
"Pharmacodynamic Comparison of Omeprazole Versus Pantoprazole on Platelet Reactivity in Patients With Acute Coronary Syndromes on Dual Antiplatelet Therapy With New P2Y12 Inhibitors" [NCT02028234]Phase 4150 participants (Anticipated)Interventional2014-02-28Not yet recruiting
An Open-Label, 3-Period, Fixed-Sequence Study to Evaluate the Effect of Famotidine and Omeprazole on MK0518 Pharmacokinetics in HIV-Infected Patients on a Stable MK0518-Containing Regimen [NCT01000818]Phase 118 participants (Actual)Interventional2008-06-30Completed
The Possible Protective Role of Omeprazole Against Oxaliplatin Induced Neuropathy in Patients With Cancer Treated With Oxaliplatin-fluorouracil Chemotherapy Protocols [NCT05680870]Phase 346 participants (Anticipated)Interventional2023-02-28Not yet recruiting
Drug-drug Interaction Study of the Effect of Omeprazole 80 mg q.d. at Steady State on the Pharmacokinetics and Pharmacodynamics of Aggrenox® Every 12 Hours at Steady State in Healthy Male and Female Volunteers (an Open-label, Randomised, Crossover Study) [NCT01303445]Phase 160 participants (Actual)Interventional2011-03-31Completed
The Effects of Melatonin on GERD Symptoms and Esophageal Acid Exposure [NCT00564590]Phase 1/Phase 2150 participants (Anticipated)Interventional2008-10-31Not yet recruiting
Efficacy of Traditional Chinese Medicine Jianpi Qinghua Granule Combined With Low Dose Omeprazole in Patients With Non-erosive Reflux Disease (NERD) [NCT02892357]Phase 1/Phase 2204 participants (Anticipated)Interventional2017-01-31Recruiting
Fecal Microbial Transplant in Pediatric Crohn's Disease: A Double Blind Placebo Control Study [NCT02272868]Phase 1/Phase 27 participants (Actual)Interventional2015-01-31Terminated
Factors Influencing the Human Gut Microbiome Profile in Multi-ethnic Groups of the Singapore Community (FAMES) [NCT02893709]36 participants (Actual)Interventional2015-06-30Completed
The Comparison of Oral Rabeprazole vs. Intravenous Omeprazole in the Treatment of Patients With Mild to Moderate Nonvariceal Upper Gastrointestinal Bleeding [NCT00861640]Phase 4200 participants (Anticipated)Interventional2009-03-31Recruiting
Study to Evaluate the Drug-drug Interaction Effect of Omeprazole on the Pharmacokinetics of SHR2554 in Healthy Subjects: A Single-center, Open-label, Single-dose, Two-period, Fixed Sequence, Self-controlled Study [NCT06093945]Phase 120 participants (Actual)Interventional2023-11-06Completed
A Single-center, Open-label, Single-arm, Fixed-sequence Study to Evaluate the Pharmacokinetic Effects of SHR0302 Tablets on Substrates of CYP3A4, CYP2C8, CYP2C9, CYP2C19 in Healthy Volunteers [NCT05392127]Phase 124 participants (Actual)Interventional2022-07-15Completed
Does Intensive Acid Suppression Reduce Esophageal Inflammation and Recurrent Barrett's Esophagus Following Ablation?: A Randomized Controlled Trial [NCT01093755]Phase 430 participants (Actual)Interventional2010-03-31Completed
The Effect of Multiple Subcutaneous Doses of Risankizumab on the Single Dose Pharmacokinetics of Cytochrome P450 Substrates (Caffeine, Warfarin, Omeprazole, Metoprolol and Midazolam) Administered Orally in an Open-label, One-sequence Trial in Patients Wit [NCT02772601]Phase 121 participants (Actual)Interventional2016-09-15Completed
A Study to Evaluate the Effects of Two Different Meal Types, Omeprazole and Ranitidine on Danoprevir Pharmacokinetics When Coadministered With Ritonavir in Healthy Subjects [NCT01392755]Phase 132 participants (Actual)Interventional2011-07-31Completed
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE, 2-PERIOD STUDY TO ESTIMATE THE EFFECT OF MULTIPLE DOSE ABROCITINIB ON THE PHARMACOKINETICS OF SINGLE DOSES OF CAFFEINE, EFAVIRENZ, AND OMEPRAZOLE IN HEALTHY PARTICIPANTS [NCT05067439]Phase 113 participants (Actual)Interventional2021-10-21Completed
Use of Maytenus Ilicifolia Mart. ex Reiss in the Treatment of Dyspepsia [NCT01408849]Phase 24 participants (Actual)Interventional2015-02-28Terminated(stopped due to Lack of adherence and huge loss of follow up.)
A PHASE I, SINGLE-CENTER, OPEN-LABEL, CROSSOVER STUDY OF THE EFFECT OF AVANAFIL ON THE PHARMACOKINETICS OF OMEPRAZOLE, DESIPRAMINE AND ROSIGLITAZONE IN HEALTHY MALE SUBJECTS [NCT01415128]Phase 160 participants (Actual)Interventional2010-04-30Completed
Effects of GSK3640254 on the Single-Dose Pharmacokinetics of Probe Substrates (Caffeine, Metoprolol, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin) in Healthy Subjects [NCT04425902]Phase 120 participants (Actual)Interventional2020-12-16Completed
A Study in Healthy Subjects to Assess the Multiple-Dose Pharmacokinetics of Two AF-219 Formulations [NCT02492776]Phase 114 participants (Actual)Interventional2015-07-07Completed
A Study in Healthy Subjects to Assess the Effect of Intragastric pH and Fasting on the Multiple-Dose Pharmacokinetics of AF-219 [NCT02229877]Phase 118 participants (Actual)Interventional2014-10-06Completed
A Phase 1, Open-Label, Two-Part, Fixed-Sequence, Drug-Drug Interaction Study to Evaluate the Effect of Voxelotor on the Pharmacokinetics of Selected CYP and Transporter Probe Substrates in Healthy Participants [NCT05981365]Phase 118 participants (Actual)Interventional2023-04-17Completed
An Open-Label, 3-Part, 2-Period Study to Examine the Effect of Omeprazole (Part 1), Famotidine (Part 2), and of an Acidic Beverage (Part 3) on the Single-Dose Pharmacokinetics of Entinostat in Healthy Adult Subjects [NCT02922933]Phase 166 participants (Actual)Interventional2016-10-25Completed
A Two-Cohort Randomized Phase 2 Trial of the IRX-2 Regimen in Women With Squamous Cervical Intraepithelial Neoplasia 3 (CIN 3) or Vulvar Intraepithelial Neoplasia 3 (VIN 3) [NCT03267680]Phase 211 participants (Actual)Interventional2017-11-08Active, not recruiting
Impact of Genetic Polymorphism on Drug Interactions Involving CYP2C19: Risk of Phenoconversion in Healthy CYP2C19 Fast, Normal and Intermediate Metabolizers Status [NCT05264142]Phase 145 participants (Anticipated)Interventional2022-04-01Recruiting
A Phase 1, Open Label, Randomized, 2-Way Crossover, 3-Period Study to Evaluate the Effect of Food and a Proton Pump Inhibitor on the Pharmacokinetics of LOXO-305 in Healthy Adult Subjects [NCT05134350]Phase 110 participants (Actual)Interventional2020-02-06Completed
An Open-Label, 3-Period, Fixed-Sequence, Study to Examine the Effect of Aluminum Hydroxide/Magnesium Hydroxide/Simethicone and Omeprazole on the Single-Dose Pharmacokinetics of Tebipenem Pivoxil Hydrobromide (TBPM-PI-HBr) in Healthy Adult Subjects [NCT04368585]Phase 120 participants (Actual)Interventional2020-07-01Completed
A Single Centre, Single Sequence, Open-Label, Repeat-Dose Study to Investigate the Effect of GSK1605786 on Hepatic Cytochrome P450, and BCRP and OATP1B1 Transport in Healthy Adult Subjects [NCT01489943]Phase 124 participants (Actual)Interventional2011-09-19Completed
Effect of a Proton Pump Inhibitor (Omeprazole, Prilosec®) on Imatinib Mesylate (Gleevec®) Pharmacokinetics in Healthy Volunteers (CSTI571BUS258) [NCT00446004]Phase 115 participants (Actual)Interventional2007-04-30Completed
[NCT00475527]Phase 40 participants (Actual)InterventionalWithdrawn(stopped due to problem of accrual)
An Open-Label, Investigator-Blinded, Randomized, Parellel Group Study to Compare the Gastroprotective Effects and Pharmacokinetic Profile of PA 325 Versus Enteric-Coated Aspirin. [NCT00442052]Phase 180 participants Interventional2006-11-30Completed
Evaluation of the Impact of Increased Gastric pH Following Omeprazole Administration on the Absorption of Baricitinib in Healthy Subjects [NCT01925144]Phase 130 participants (Actual)Interventional2013-10-31Completed
Inhibiting Fatty Acid Synthase to Improve Efficacy of Neoadjuvant Chemotherapy [NCT02595372]Phase 242 participants (Actual)Interventional2015-11-12Completed
Intravenous Infusion of High Dose Omeprazole Versus Regular Dose Omeprazole on Recurrent Bleeding After Endoscopic Treatment of Bleeding Peptic Ulcers [NCT00519519]Phase 3126 participants (Actual)Interventional2004-07-31Completed
A Phase 1, Single-Center, Randomized, 3-Period Crossover Study in Healthy Volunteers to Evaluate the Absorption of WTX101 After Single Dose Administration of an Enteric Coated Formulation With and Without Food and a Non-Coated Formulation Coadministered W [NCT05319912]Phase 118 participants (Actual)Interventional2014-04-07Completed
A Prospective, Randomized, Open-label Comparative Study to Evaluate the Efficacy and Safety of Two First-line H.Pylori Eradication Regimens Including the Omeprazole 40 or 80 mg, Clarithromycin and Amoxicillin. [NCT02922699]Phase 4120 participants (Actual)Interventional2013-01-31Completed
Omeprazole and Reflux Disease - Improvement of Clinical Outcome by Genotype-adjusted Dosing [NCT00537732]Phase 468 participants (Actual)Interventional2007-04-30Terminated(stopped due to recruitment problems)
A Randomized, Double-Blind, Double-Dummy, Parallel Group, Phase 3 Efficacy and Safety Study of CGT-2168 Compared With Clopidogrel to Reduce Upper Gastrointestinal Events Including Bleeding and Symptomatic Ulcer Disease [NCT00557921]Phase 35,000 participants (Anticipated)Interventional2007-12-31Terminated(stopped due to Terminated by Sponsor)
A Phase I, Single-center, Open-label, Fixed Sequence Study in Chinese Healthy Male Adults to Evaluate the Effect of Omeprazole on the Pharmacokinetics of AB-106 [NCT05609929]Phase 124 participants (Actual)Interventional2022-11-02Completed
Evaluating the Effects of Tipranavir (With Ritonavir) Capsule and Liquid Formulation on Cytochrome P450 and P-glycoprotein Activity Using a Biomarker Cocktail in Healthy Human Volunteers [NCT02243553]Phase 134 participants (Actual)Interventional2006-01-31Completed
CURRENT PRACTICE STUDY OF ANTIBIOTIC TREATMENT OF GASTRIC MALT LYMPHOMA [NCT00002682]Phase 25 participants (Actual)Interventional1995-08-10Completed
Randomized, Open-Label, Multiple-Dose Study to Evaluate the Effect of Omeprazole 20 mg on the Pharmacokinetics of Atazanavir Administered With Ritonavir in Healthy Subjects [NCT00357240]Phase 156 participants Interventional2006-06-30Completed
The Effect of Imlunestrant on CYP2C8, CYP2C19, CYP2D6, P-gp, and BCRP Activity and the Effect of P-gp Inhibition on Imlunestrant Pharmacokinetics in Healthy Women of Non-childbearing Potential [NCT05444556]Phase 1113 participants (Actual)Interventional2022-07-07Completed
Pharmacokinetic Study of the HCV Protease Inhibitor Bo-cePRevir and the Proton Pump Inhibitor OMeprazOle (PROMO) [NCT01470690]Phase 124 participants (Actual)Interventional2011-10-31Completed
Usefulness of Antimicrobial Susceptibility in the Eradication of Helicobacter Pylori [NCT01486082]1 participants (Anticipated)Observational2011-02-28Recruiting
Comparison of Efficacy and Safety of Triple Regimen Based on Clarithromycin VS Metronidazole in Pediatric Population in Pakistan [NCT04721704]36 participants (Anticipated)Interventional2020-09-14Recruiting
A Double-blind, Randomised, Parallel-group, Multicentre, Phase III Study to Investigate the Pharmacodynamic Effect by Assessment of the 24 Hours Intraesophageal pH Level, the Efficacy and Safety of Omeprazole 10mg and 20mg od in Patients With Non-erosive [NCT00259051]Phase 340 participants Interventional2004-01-31Completed
Assessment of the Effects of Zegerid Powder for Oral Suspension 40 mg on 24-Hour and Nocturnal Esophageal Acid Exposure in Patients With Gastroesophageal Reflux Disease and Barrett's Esophagus [NCT01129778]27 participants (Actual)Interventional2009-11-30Terminated(stopped due to change in the business strategy of the sponsor)
A Comparative Study on the Healing Effects of Rebamipide and Omeprazole in Helicobacter Pylori-positive Gastric Ulcer After Eradication Therapy [NCT00272467]Phase 4132 participants (Actual)Interventional2005-07-31Completed
Pharmacokinetics of Enteral Omeprazole Suspension in Patients With Cerebral Palsy and Mental Retardation [NCT00426595]Phase 214 participants (Anticipated)Interventional2007-04-30Completed
Single-center Randomized Controlled Study of Omeprazole and Pantoprazole Antiplatelet Effect of Clopidogrel Clinical Randomized Controlled Trials [NCT01735227]Phase 4620 participants (Anticipated)Interventional2012-11-30Not yet recruiting
An Open Label Phase I Study to Evaluate the Effects of Patupilone on the Pharmacokinetics of Midazolam and Omeprazole in Patients With Advanced Malignancies (Extension) [NCT00442741]Phase 10 participants (Actual)Interventional2007-07-31Withdrawn(stopped due to pts. will be captured in core)
A Randomized, Blinded, Placebo-controlled Study to Investigate the Safety, and Pharmacokinetics of Single and Repeat Dose Escalation of the Oral YAK3/DYRK3 Inhibitor GSK626616AC in Healthy Subjects [NCT00443170]Phase 190 participants (Actual)Interventional2006-11-30Completed
Dyspeptic Symptoms Evolution After Eradication of Helicobacter Pylori in Patients With Different Endoscopic Findings: a Randomized Double-blind Placebo-controlled Clinical Trial With 12 Months of Follow-up [NCT00404534]Phase 3407 participants (Actual)Interventional2006-10-31Completed
Effect of Proton Pump Inhibitors on the Colonic Microbiome in Children [NCT02016820]7 participants (Actual)Interventional2014-11-30Terminated(stopped due to Lack of funding)
[NCT01795794]Phase 412 participants (Anticipated)Interventional2013-04-30Not yet recruiting
Risdiplam - A Phase I, Open-Label, Multi-Period Crossover Study to Investigate the Safety, Food Effect, Bioavailability and Bioequivalence of Oral Doses of Two Different Formulations in Healthy Subjects [NCT04718181]Phase 1131 participants (Actual)Interventional2021-02-01Completed
An Open-Label, Multiple-Dose, Non-Randomized Study to Assess the Drug-Drug Interactions of Proellex® (CDB-4124) With Cytochrome P450 Isoenzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 in Healthy Female Subjects [NCT00741468]Phase 118 participants (Actual)Interventional2008-07-31Completed
The Effect of Proton Pump Inhibitor (Omeprazole) on Acetosalisylic Acid Absorption. [NCT01061034]9 participants (Actual)Interventional2007-03-31Completed
[NCT01458990]60 participants (Actual)Interventional2011-10-31Completed
Phase 3 Study of Prospective Randomized Trial Comparing Adjunctive High Dose Omeprazole Infusion Against Scheduled Second Endoscopy in the Prevention of Peptic Ulcer Rebleeding After Therapeutic Endoscopy [NCT00164931]Phase 3240 participants (Anticipated)Interventional2003-10-31Completed
Comparison of the Gastric Acid Suppressive Effects of Esomeprazole and Generic Omeprazole [NCT00542347]Phase 320 participants (Actual)Interventional2007-09-30Terminated(stopped due to Enrollment target not met due to high number of disqualified studies.)
A Phase 1, Randomized, Open-Label, 2-Period, Crossover Design Study to Assess the Effects of Multiple Oral Doses of Dexlansoprazole, Lansoprazole, Omeprazole or Esomeprazole on the Steady-State Pharmacokinetics and Pharmacodynamics of Clopidogrel in Healt [NCT00942175]Phase 1160 participants (Actual)Interventional2009-12-31Completed
A Phase 1, Open-label Drug-drug Interaction Study to Evaluate the Effects of Omeprazole and Rifampin on the Pharmacokinetics of VX-548 in Healthy Subjects [NCT05635110]Phase 131 participants (Actual)Interventional2022-12-15Completed
An Open-Label, Investigator-Blinded, Stratified, Randomized, Parallel Group Study to Compare the Gastroprotective Effects of PA 325 Versus 81 mg Enteric Coated Aspirin [NCT00441519]Phase 180 participants (Anticipated)Interventional2007-02-28Completed
The CALIBER Study Randomized Controlled Trial of LINX Versus Double-Dose Proton Pump Inhibitor Therapy for Reflux Disease [NCT02505945]Phase 4152 participants (Actual)Interventional2015-06-30Completed
A Phase 1, Open-Label, Single-Sequence Crossover Study Assessing the Effect of Tivantinib (ARQ 197) on the Pharmacokinetics of Omeprazole/S-Warfarin/Caffeine/Midazolam and Digoxin in Cancer Subjects [NCT01517399]Phase 128 participants (Actual)Interventional2011-12-31Completed
A Phase I, Randomized, Open-label, Single-center Study to Assess the Pharmacokinetics of Vandetanib (CAPRELSA) in Healthy Subjects When a Single Oral Dose of Vandetanib 300 mg is Administered Alone and in Combination With Omeprazole or Ranitidine [NCT01539655]Phase 134 participants (Actual)Interventional2012-02-29Completed
Safety & Efficacy of Omeprazole Sodium Bicarbonate for the Prevention of Upper GI Bleeding in the Critically Ill [NCT00045799]Phase 3354 participants (Actual)Interventional2002-05-31Completed
Possible Drug Interaction Between Clopidogrel and Ranitidin or Omeprazole in Patients With Stable Coronary Heart Disease: a Comparative Study [NCT01896557]Phase 492 participants (Actual)Interventional2011-10-31Completed
Effect of Vitamin D Supplementation on 15-Prostaglandin Dehydrogenase Expression in Barrett's Esophagus [NCT01465113]Early Phase 126 participants (Actual)Interventional2010-05-31Completed
A Phase 1, Single-Center, Randomized, 3-Way Cross-Over, Open Label Study to Evaluate the Pharmacodynamics of Different Formulations of AZD1722 in Healthy Volunteers Taking Omeprazole [NCT02249936]Phase 118 participants (Actual)Interventional2013-02-28Completed
An Open Label, Non-Randomized, Two-Treatment, Single-Period, Single-Dose, Drug-Drug Interaction Study to Evaluate the Effects of Omeprazole on the Pharmacokinetics of XS004 (Dasatinib) 90 mg Film-Coated Tablets in Healthy Adult Subjects Under Fasting Cond [NCT05433896]Phase 117 participants (Actual)Interventional2020-11-01Completed
A Randomised, Double-Blind, Double-Dummy, Active-Controlled, Multicenter Study to Assess the Efficacy and Safety of Esomeprazole or Omeprazole for 5 Days in Subjects With Acute Non-Variceal Upper Gastrointestinal Bleeding [NCT00402259]Phase 3440 participants (Anticipated)Interventional2006-08-31Completed
A Large, International, Randomized, Placebo-controlled Trial to Assess the Impact of Dabigatran (a Direct Thrombin Inhibitor) and Omeprazole (a Proton-pump Inhibitor) in Patients Suffering Myocardial Injury After Noncardiac Surgery [NCT01661101]Phase 31,754 participants (Actual)Interventional2013-01-31Completed
An Open-label Drug Interaction Study in Healthy Subjects to Evaluate the Effect of Oral Doses of JNJ-54175446 on the Inhibition of Cytochrome P450 CYP3A4, CYP2C9, CYP1A2 and CYP2D6 Activity and the Induction of CYP2B6 and CYP2C19 Activity Using a Multiple [NCT03058419]Phase 116 participants (Actual)Interventional2017-03-14Completed
Administration of Intravenous Proton Pump Inhibitor Prior to Endoscopy [APPE] in Patients With Upper Gastrointestinal Bleeding; a Double-Blind Placebo-Controlled Randomised Study. [NCT00164866]Phase 4638 participants Interventional2004-02-29Completed
Phase I, Open-label, Three-Period Crossover Study to Investigate the Effect of a Proton Pump Inhibitor (Omeprazole) on the PK of Tepotinib in Healthy Subjects [NCT03531762]Phase 112 participants (Actual)Interventional2018-05-14Completed
Role of Bronchoalveolar Lavage Pepsin Assay in Wheezy Infants [NCT02685436]Phase 452 participants (Actual)Interventional2013-03-31Completed
Treating Gastrointestinal Problems in Children With Autism Using Beneficial Bacteria Treatment (BBT) [NCT02504554]Phase 1/Phase 218 participants (Actual)Interventional2014-07-31Completed
CYP2C19 Genotype as a Predictor of Gastric Acid Suppression and Healing of Erosive Esophagitis [NCT01824199]Early Phase 10 participants (Actual)Interventional2013-03-31Withdrawn(stopped due to funding)
Omeprazole Versus Anti-reflux Surgery in the Long-term Management of Peptic Esophagitis - a 10 Year Follow up Study of Patients Previously Studied for 5 Years - A Nordic Multicentre Study [NCT00256737]Phase 3219 participants Interventional1998-01-31Completed
Eradication of Helicobacter Pylori in the Management of Stage IE & IIE-1 Primary Low-grade B Cell Lymphoma of Mucosa-associated Lymphoid Tissue Type of The Stomach [NCT00201422]70 participants (Actual)Interventional1996-06-30Completed
A Double-blind, Randomised, Parallel-group, Multicentre, Phase III Study to Compare the Efficacy of Omeprazole 20mg and 10mg od for the Four-week Treatment of Non-erosive Reflux Disease (NERD) With That of Placebo od and to Investigate Safety [NCT00259077]Phase 3270 participants Interventional2003-10-31Completed
A Phase 1, Open-label, Multiple-probe Drug-drug Interaction Study to Determine the Effect of Rucaparib on Pharmacokinetics of Caffeine, S-Warfarin, Omeprazole, Midazolam, and Digoxin in Patients With Advanced Solid Tumors [NCT02740712]Phase 117 participants (Actual)Interventional2016-04-30Completed
A Prospective, Randomized Trial Comparing the Effect of Intravenous Omeprazole to That of Intravenous Ranitidine on the Maintenance of Hemostasis After Successful Endoscopic Treatment of Bleeding Peptic Ulcer [NCT00247130]Phase 40 participants (Actual)Interventional2005-10-31Withdrawn(stopped due to Superiority of iv omeprazole to ranitidine has already been proven by others.)
A Study To Estimate The Effect Of Omeprazole On The Pharmacokinetics Of Nelfinavir In Healthy Subjects [NCT00251030]Phase 420 participants (Actual)Interventional2005-11-30Completed
Pharmacokinetics of Immediate-Release vs. Delayed-Release Omeprazole in Patients With Heartburn Associated With Gastroparesis [NCT00492622]Phase 412 participants (Actual)Interventional2007-06-30Completed
Treatment of Intraparenchymal Neurocysticercosis: Effect of Increased Dosing of Corticosteroids on Seizure Frequency [NCT00290823]Phase 3110 participants (Anticipated)Interventional2006-04-30Completed
An Open-Label Study to Assess the Effect of Omeprazole Administration on the Pharmacokinetics of VELCADE in Subjects With Either Advanced Solid Tumors or Non-Hodgkin's Lymphoma [NCT00298779]Phase 120 participants (Anticipated)InterventionalCompleted
Multicentre,Prospective Study of First-line Antibiotic Therapy for Early-stage Low-grade and High-grade Gastric Mucosa-associated Lymphoid Tissue-type Lymphoma and Potential Predicting Factor for Treatment Outcome [NCT00327132]47 participants (Actual)Interventional2006-07-31Completed
An Open Label Phase I Study to Evaluate the Effects of Patupilone on the Pharmacokinetics of Midazolam and Omeprazole in Patients With Advanced Malignancies [NCT00420615]Phase 134 participants (Actual)Interventional2006-12-31Completed
High Dose Oral Omeprazole Versus Standard Continuous Intravenous Pantoprazole in Patient With Peptic Ulcer Bleeding and Undergo Successful Therapeutic Endoscopy; Non-inferiority Randomized Controlled Trial [NCT04394663]76 participants (Anticipated)Interventional2020-10-01Recruiting
Randomized Multi-Intervention Trial to Inhibit Precancerous Gastric Lesions in Lingu, Shandong Province, China [NCT00339768]Phase 33,411 participants (Actual)Interventional1995-07-01Completed
Effect of Iron Repletion in Women With Chronic Cough and Iron Deficiency [NCT01507792]22 participants (Actual)Interventional2002-01-31Completed
A Study to Investigate the Effects of BI 1181181 on the Pharmacokinetics of Midazolam, Warfarin, Omeprazole and Digoxin in Healthy Male Subjects [NCT02345304]Phase 10 participants (Actual)Interventional2015-03-31Withdrawn
A Phase I, Open-label, Drug Interaction Study to Evaluate the Effect of a Single-dose of CNTO 136 (Sirukumab) on CYP450 Enzyme Activities After Subcutaneous Administration in Subjects With Rheumatoid Arthritis [NCT01636557]Phase 112 participants (Actual)Interventional2012-10-11Completed
Optimal Dose and Population Pharmacokinetics of Omeprazole in Neonates With Gastroesophageal Reflux Disease (GERD) [NCT01657578]Phase 255 participants (Actual)Interventional2007-06-30Completed
A Randomized Controlled Trial Comparing Proton Pump Inhibitor Therapy With and Without Interarytenoid Botulinum Toxin Injection for Vocal Fold Granuloma [NCT01678053]Phase 20 participants (Actual)Interventional2012-09-30Withdrawn(stopped due to Was not able to recruit patients for randomization.)
Effect of Omeprazole, an OCT Inhibitor, on the Pharmacodynamics and Pharmacokinetics of Metformin, Involved the Mechanism of Attenuating AMPK Phosphorylation [NCT01711320]Phase 120 participants (Actual)Interventional2012-09-30Completed
[NCT01731067]Phase 110 participants (Anticipated)Interventional2012-11-30Completed
Helicobacter Pylori and Body Iron in Adults [NCT03146325]Phase 40 participants (Actual)Interventional2012-11-30Withdrawn(stopped due to Study was not funded and PI has left the institution)
Proton Pump Inhibitors (PPI) and Fat Absorption in Subjects With Cystic Fibrosis (CF) and Exocrine Pancreatic Insufficiency (EPI) [NCT03551691]Phase 219 participants (Actual)Interventional2018-08-07Completed
A Phase IIB/III Multicenter Randomized Trial to Evaluate the Combination of Low-Dose Cyclosporine and Omeprazole Versus Omeprazole Alone in Participants With New Onset Type 1 Diabetes. [NCT01762644]Phase 30 participants (Actual)Interventional2015-08-31Withdrawn(stopped due to This study was withdrawn prior to enrollment.)
Comparison of Prilosec OTC® Versus Prevacid ® for Gastric Acid Suppression [NCT00903448]Phase 440 participants (Actual)Interventional2009-04-30Completed
Improving Care For Infants With Laryngomalacia: A Pilot Randomized Controlled Trial of Omeprazole Versus Placebo [NCT01782560]Phase 10 participants (Actual)Interventional2013-02-28Withdrawn(stopped due to Unable to recruit a sufficient amount of subjects)
A Phase 1, Open-Label Study to Evaluate the Potential Effects of PPI-668 on the Pharmacokinetics of Midazolam and Omeprazole, and Potentially Telaprevir, in Healthy Adult Subjects [NCT01786382]Phase 124 participants (Actual)Interventional2013-02-28Completed
A Phase I, Randomized, Open-label Study to Evaluate the Effect of Ritonavir or Omeprazole on the Pharmacokinetics of IDX719 in Healthy Subjects [NCT01813552]Phase 124 participants (Actual)Interventional2013-02-28Completed
The Therapeutic Role of Albumin Supply on Peptic Ulcer Bleeding and the Correlation Between Clinical Course and Expression of Serum Response Factor on Ulcer Tissue and Superoxide Free Radical in Blood [NCT01822600]Phase 491 participants (Actual)Interventional2010-01-31Completed
The Impact of Proton Pump Inhibitors on the Fecal Microbiome and Their Relationship to Clostridium Difficile Infection [NCT01822977]Phase 115 participants (Actual)Interventional2013-03-31Completed
Prospective Study Assessing Patient Satisfaction of Symptom Control With Proton Pump Inhibitor Dosing Regimen [NCT02623816]Phase 464 participants (Actual)Interventional2014-08-31Completed
Efficacy of Low Dose of Proton Pumb Inhabitor in Treatment Upper Gastrointestinal Bleeding [NCT03163680]295 participants (Actual)Observational2012-01-31Completed
Protocol PT 11-29: Randomized, Open-label, Cross-over Pilot Study to Evaluate and Compare Two Omeprazole Containing Products for Relief of Frequent Heartburn [NCT01587885]Phase 448 participants (Actual)Interventional2012-01-31Completed
The Effect of Gastric Acid Suppression on Probiotic Colonization [NCT03327051]Phase 439 participants (Actual)Interventional2018-03-20Completed
A Multicenter, Randomized, Double-blind, Parallel, Placebo-controlled, Phase III Study to Assess the Safety and Efficacy of Viokase® 16 for the Correction of Steatorrhea in Patients With Exocrine Pancreatic Insufficiency [NCT00559364]Phase 350 participants (Actual)Interventional2007-11-30Completed
Investigation of the Effect of Food and of Increased Gastric pH on the Relative Bioavailability of a Single Oral Dose of 240 mg Faldaprevir in an Open-label, Randomised, Three-way Cross-over Trial in Healthy Subjects [NCT01694706]Phase 115 participants (Actual)Interventional2012-09-30Completed
A Phase I, Open-label, Randomised, Crossover Study in 3 Parallel Groups to Evaluate the Effect of Rifampicin, Ketoconazole, and Omeprazole on the Pharmacokinetics of Sativex in Healthy Volunteers [NCT01323465]Phase 136 participants (Actual)Interventional2008-02-29Completed
An Open-label Study to Evaluate the Drug-drug Interaction Effect of Omeprazole, a Proton-pump Inhibitor, on the Pharmacokinetics of AMG 510 in Healthy Subjects [NCT05581992]Phase 114 participants (Actual)Interventional2020-01-06Completed
Brain Mechanisms For Clinical Placebo in Chronic Pain: A Randomized Clinical Trial of Placebo, Active Treatment, and No Treatment in Chronic Back Pain [NCT02986334]Phase 494 participants (Actual)Interventional2016-08-31Completed
A Multicentre, Randomised, Double-blind, Parallel-group, Comparative Study to Compare the Efficacy and Safety of Esomeprazole 20 mg and 40 mg Once Daily Oral Administration With Omeprazole 20 mg Once Daily Oral Administration in Patients With Reflux Esoph [NCT00633932]Phase 3602 participants (Actual)Interventional2007-12-31Completed
A Clinical Trial to Investigate the Influence of CYP2C19 Polymorphism on Pharmacokinetic/Pharmacodynamic Characteristics of Omeprazole in Healthy Korean Volunteers [NCT02299687]Phase 124 participants (Actual)Interventional2014-09-30Completed
A Phase 1, Open-label, Single-sequence, Non-randomized, Crossover, Drug-Drug Interaction Study to Evaluate the Effect of Omeprazole on the Pharmacokinetics of SPD422 (Anagrelide Hydrochloride) in Healthy Adult Subjects [NCT03866434]Phase 120 participants (Actual)Interventional2019-02-26Completed
Interaction Between Omeprazole and Gliclazide in CYP2C19 Normal/ Ultrarapid Metabolisers [NCT04198948]Phase 115 participants (Actual)Interventional2019-03-04Completed
Association Between Variations in CYP Pheno- and Genotypes and Plasma Concentration of Chlordiazepoxide in the Treatment of Alcohol Withdrawal Symptoms [NCT05563350]26 participants (Anticipated)Observational [Patient Registry]2022-01-29Recruiting
An Open-label Study to Evaluate the Impact of Acid-reducing Agents on the Pharmacokinetics of AMG 510 in Healthy Subjects Under Fed Conditions [NCT05599828]Phase 114 participants (Actual)Interventional2020-07-17Completed
Efficacy and Safety of DLBS2411 Compared to Omeprazole in the Management of Gastroesophageal Reflux Disease (GERD) [NCT03367195]Phase 332 participants (Actual)Interventional2018-08-16Terminated(stopped due to Very low recruitment rate. The Study Site classifies as tertiary referral hospital. Therefore, GERD Patients being referred to the site are mostly those with comorbidities included in the exclusion criteria.)
A Three-Part Phase 1 Study to Evaluate the Potential Drug Interaction Between ACH-0144471 and Cyclosporine, Tacrolimus, Antacids, and Omeprazole in Healthy Adult Subjects [NCT05109390]Phase 172 participants (Actual)Interventional2018-07-27Completed
Confocal Endomicroscopy for Non-Erosive Reflux Disease Detection (CENERDD) [NCT02788591]5 participants (Actual)Interventional2015-08-31Terminated(stopped due to lack of accrual)
A Phase 1, Open-Label Study to Compare the Relative Bioavailability of Two AG-881 Formulations and to Evaluate the Effect of Food and Multiple-Dose Omeprazole on the Pharmacokinetics of a Single Dose of AG-881 in Healthy Adult Subjects [NCT04128787]Phase 136 participants (Actual)Interventional2019-09-30Completed
The Effects of Multiple Dose Fluoxetine and Metabolites on CYP1A2, CYP2C19, CYP2D6 and CYP3A4 Activity [NCT01361217]10 participants (Actual)Interventional2011-09-30Completed
A Phase 1, Single-Center, Open-Label, Fixed-Sequence, 2-Period, 3-Part Study to Evaluate the One-Way Interaction of Calcium Carbonate, Omeprazole, or Rifampin on ACP-196 in Healthy Adult Subjects [NCT04914936]Phase 172 participants (Actual)Interventional2014-09-21Completed
Effect of Histamine 2 Receptor Antagonist (H2RA) and Proton Pump Inhibitor (PPI) on the Positivity Rates and Clinical Outcomes of Coronavirus Disease-19 (COVID-19). [NCT04834752]400,000 participants (Anticipated)Observational2021-05-01Not yet recruiting
A Phase I Dose Escalation Study of MK-8033 in Patients With Advanced Solid Tumors [NCT00559182]Phase 147 participants (Actual)Interventional2007-12-05Completed
A Phase 1, Single-center, Open-label, Fixed-sequence, 4-period, 3-part Study in Healthy Adult Subjects to Evaluate the Effect of an Acidic Formulation of Acalabrutinib (ACP-196), Acidic Beverage, or Grapefruit Juice on the Pharmacokinetics of Acalabrutini [NCT04876807]Phase 136 participants (Actual)Interventional2016-01-28Completed
A Randomized, Open-Label, Cross-Over, Study to Evaluate the Inhibitory Effect of Clopidogrel, EC Aspirin 81 mg and EC Omeprazole 40 mg All Dosed Concomitantly and PA32540 and Clopidogrel Dosed Separately on Platelet Aggregation in Healthy Volunteers [NCT01557335]Phase 130 participants (Actual)Interventional2010-11-30Completed
Development of High-throughput Minidose Inje Cocktail Method for Simultaneous Evaluating Five Cytochrome P450 Isoforms in Human [NCT01570569]Phase 126 participants (Actual)Interventional2011-01-31Completed
An Open-label Volunteer Study of the Effect of G17DT on the Elevation of Plasma Gastrin Levels After Therapy With a Proton Pump Inhibitor (Omeperazole) in Patients With Treated Stage II/III Colorectal Cancer [NCT02518373]Phase 222 participants (Actual)Interventional2000-04-30Completed
A Phase I, Multi-center, Open-label, Drug-drug Interaction Study to Assess the Effect of TKI258 on the Pharmacokinetics of Caffeine, Diclofenac, Omeprazole and Midazolam Administered as a Four-drug Cocktail in Patients With Advanced Solid Tumors, Excludin [NCT01596647]Phase 139 participants (Actual)Interventional2012-05-31Completed
YF476: Effects of Repeated Dosing at 2 Dose Levels on 24-hour Ambulatory Gastric pH Compared With Placebo and Omeprazole in Healthy Volunteers [NCT01599858]Phase 149 participants (Actual)Interventional1996-08-31Completed
Omeprazole 20 mg in Patients With Laryngopharyngeal reflux and Comorbid Chronic Rhinosinusitis - a Randomized, Double Blind, Placebo Controlled Trial [NCT03086070]Phase 460 participants (Actual)Interventional2010-01-01Completed
An Open-label, Randomized, Single-center, 4-way Crossover, Single Dose Bioequivalence Study Comparing Omeprazole 20 and 40-mg Aqueous Solvent Based Capsules Manufactured by AstraZeneca With Omeprazole 20 and 40-mg Organic-solvent Based Capsules Manufactur [NCT01921920]Phase 154 participants (Actual)Interventional2013-08-31Completed
A Single-centre, Open-label, Three-period Study of the Pharmacokinetic Effect of PA21 on Omeprazole in Healthy Male and Female Adults [NCT01452906]Phase 145 participants (Actual)Interventional2011-09-30Completed
Phase 1, Open Label Study to Evaluate the Effect of Omeprazole and Ritonavir on GSK2336805 Pharmacokinetics in Healthy Adults [NCT01458054]Phase 128 participants (Actual)Interventional2011-09-27Completed
Compliance With Antidepressant Medication in Treatment of Functional Dyspepsia: A Randomized Comparison of Different Prescribing Behaviors [NCT01851863]Phase 4262 participants (Actual)Interventional2013-05-31Completed
A Phase I, Fixed Sequence, Open-label, Study to Assess the Pharmacokinetics of AZD9291 in Healthy Male Volunteers When a Single Oral Dose of AZD9291 80 mg is Administered Alone and in Combination With Omeprazole [NCT02224053]Phase 1136 participants (Actual)Interventional2014-09-30Completed
A Phase II Clinical Trial of Anti-Helicobacter Pylori Treatment in Endoscopically Diagnosed Low-Grade Localized Gastric Lymphoma [NCT00003151]Phase 296 participants (Anticipated)Interventional1997-09-30Completed
Comparison of Prilosec OTC® Versus Zegerid® for Gastric Acid Suppression [NCT00808769]Phase 430 participants (Actual)Interventional2008-11-30Completed
"An Open-label, Single-sequence Study of the Effect of Belatacept on the Pharmacokinetics of Caffeine, Losartan, Omeprazole, Dextromethorphan, and Midazolam Administered as Inje Cocktail in Healthy Subjects" [NCT01766050]Phase 445 participants (Actual)Interventional2013-01-31Completed
Lactobacillus Reuteri in Management of Helicobacter Pylori Infection in Dyspeptic Patients: a Double Blind Placebo Controlled Randomized Clinical Trial [NCT01593592]70 participants (Actual)Interventional2012-06-30Completed
Effectiveness of Tongue Exercises and Laryngopharyngeal Reflux Therapy on Upper Airway Resistance Syndrome [NCT00364481]Phase 10 participants (Actual)Interventional2006-08-31Withdrawn(stopped due to Not enough subjects enrolled)
A 6-Month, Phase 3, Randomized, Double-Blind, Parallel-Group, Controlled, Multi-Center Study to Evaluate the Incidence of Gastric Ulcers Following Administration of Either PN 200 or Naproxen in Subjects Who Are at Risk for Developing NSAID-Associated Ulce [NCT00367211]Phase 3400 participants Interventional2006-09-30Completed
Investigation of the Effect of Food and of Increased Gastric pH on the Relative Bioavailability of Deleobuvir Following Single Oral Administration in Healthy Caucasian and Japanese Subjects (an Open-label, Randomised, Four-way Crossover Study) [NCT01983566]Phase 116 participants (Actual)Interventional2013-11-30Terminated
A Single-center, Open-label, Fixed-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of SHR3680 With Midazolam (CYP3A4 Substrates), S-Warfarin (CYP2C9 Substrates) and Omeprazole (CYP2C19 Substrates) in Prostate Canc [NCT04676035]Phase 118 participants (Actual)Interventional2020-06-15Completed
Proton Pump Inhibitors in Conjunction to Endoscopic Therapy for Bleeding Peptic Ulcers: a Randomized Clinical Trial of High vs Standard Doses [NCT00374101]Phase 3450 participants Interventional2005-01-31Completed
The Effect of Intensive Urate Lowering Therapy (ULT) With Febuxostat in Comparison With Allopurinol on Cardiovascular Risk in Patients With Gout Using Surrogate Markers: a Randomized, Controlled Trial [NCT02500641]Phase 4196 participants (Actual)Interventional2015-08-17Completed
OPEN Versus InTact Capsule Proton Pump Inhibitors for the Treatment of Marginal Ulcers After Bariatric Surgery [NCT05799105]Phase 4122 participants (Anticipated)Interventional2023-03-14Recruiting
FASN Fatty Acid Synthase Inhibition in Castration Refractory Prostate Cancer Salvaging Taxane Failure [NCT04337580]Phase 220 participants (Anticipated)Interventional2021-03-05Recruiting
An Open-label, Phase 1, Randomized, Seven-treatment, Seven-period, Crossover Study to Assess the Relative Bioavailability, pH Effect, Food Effect and Dose Proportionality of CC-292 Spray Dried Dispersion Formulation in Healthy Volunteers [NCT02433457]Phase 124 participants (Actual)Interventional2014-05-26Completed
A Phase I, Open-label, Fixed-sequence, Crossover, Drug-drug Interaction Study to Investigate the Inhibition Potential of KL1333 on CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 in Healthy Subjects [NCT04643249]Phase 114 participants (Actual)Interventional2020-11-10Completed
"The Effects of the Synbiotic Bifidobacterium Lactis B94 Plus Inulin Addition on Standard Triple Therapy of Helicobacter Pylori Eradication in Children" [NCT03165253]69 participants (Actual)Interventional2011-06-30Completed
A Phase I, Open-Label Study to Assess the Effects of PRC-4016 (Icosabutate) on the Pharmacokinetics of Midazolam, Omeprazole, Flurbiprofen and Simvastatin in Healthy Male/Female Subjects [NCT02367937]Phase 116 participants (Actual)Interventional2014-08-31Completed
A Phase I, Multi-center Study to Determine the Effect of Fluzoparib on Pharmacokinetics of Caffeine, S-Warfarin, Omeprazole, Midazolam, Repaglinide and Bupropion in Patients With Recurrent Ovarian Cancer [NCT04718740]Phase 133 participants (Actual)Interventional2021-06-25Completed
A Randomized, Double-blind Clinical Trial Comparing Zegerid Capsule to Famotidine in Preventing Anastomotic (Marginal) Ulcers in Post Gastric Bypass Patients [NCT00557349]Phase 440 participants (Actual)Interventional2006-11-30Completed
a Single-center, One-arm, Open, and Fixed Sequences Study to Evaluate the Effects of Omeprazole on the Pharmacokinetics of Fluzoparib in Healthy Male Volunteers [NCT04108676]Phase 116 participants (Actual)Interventional2019-09-07Completed
Randomized, Crossover Pharmacodynamic Study Comparing the Effects of Zegerid® (20 mg Omeprazole/Sodium Bicarbonate) and Prilosec OTC® (20 Mg-equivalent Omeprazole) [NCT00674115]Phase 360 participants (Actual)Interventional2008-04-30Completed
A Phase 2, Open-label Trial of the Safety and Biological Effect of Subcutaneous IRX-2 (With Cyclophosphamide, Indomethacin, and Zinc) in Patients With Resectable Cancer of the Head and Neck [NCT00210470]Phase 227 participants (Actual)Interventional2005-07-31Completed
Effects of PPI Therapy on Clopidogrel-Induced Antiplatelet Effects: A Randomized Study [NCT01170533]Phase 120 participants (Actual)Interventional2009-03-31Completed
Randomized, Crossover Pharmacodynamic Study Comparing the Effects of Zegerid® (20 mg Omeprazole/Sodium Bicarbonate) and Prilosec OTC® Tablets (20 Mg-equivalent Omeprazole) [NCT00765206]Phase 360 participants (Actual)Interventional2008-05-31Completed
Evaluation of the Impact of Increased Gastric pH Following Omeprazole Administration on the Pharmacokinetics of Evacetrapib in Healthy Subjects [NCT02365558]Phase 134 participants (Actual)Interventional2015-01-31Completed
A Multicentre, Randomised, Double-blind, Parallel-group, Comparative Study to Compare the Efficacy and Safety of Esomeprazole 20 mg Once Daily Oral Administration With Omeprazole 10 mg and Esomeprazole 10 mg Once Daily Oral Administration in Maintenance T [NCT00634114]Phase 3540 participants (Actual)Interventional2008-01-31Completed
A Phase 1, Open-label, Randomized, 2-period Crossover Drug Interaction Study in Healthy Adult Subjects to Evaluate the Effect of the Proton Pump Inhibitor Omeprazole on the Pharmacokinetics of SSP-002358 [NCT01415349]Phase 142 participants (Actual)Interventional2011-08-11Completed
Efficacy and Safety of Intravenous IIaprazole for Peptic Ulcer Bleeding: A Randomized, Double-Blind, Omeprazole-Controlled, Multicenter, and Phase 2 Trail in China [NCT03362268]Phase 2180 participants (Actual)Interventional2014-02-28Completed
Preventing Cardiac Complication of COVID-19 Disease With Early Acute Coronary Syndrome Therapy: A Randomised Controlled Trial. [NCT04333407]320 participants (Actual)Interventional2020-04-03Terminated(stopped due to Difficulty in recruiting eligible participants)
Gastric pH as a Possible Determinant of Anthocyanin Absorption [NCT01122160]13 participants (Actual)Interventional2010-05-31Completed
Randomized, Double-Blind, Placebo-Controlled Three-Part Phase 1 Study of Safety, Tolerability, Pharmacokinetics, and Food Effect of MRX-4 Administered Orally to Healthy Volunteers in Single and Multiple Ascending Dose Cohorts to Evaluate Drug Interactions [NCT03033342]Phase 1122 participants (Actual)Interventional2016-08-02Completed
Effect of Helicobacter Pylori Eradication on Glandular Atrophy and Metachronous Cancer in Patients Undergoing Endoscopic Mucosal Resection for Gastric Cancer [NCT02407119]Phase 3470 participants (Actual)Interventional2003-06-30Active, not recruiting
Phase 1, Open-label, Partially Randomized, Parallel-group Study in Healthy Adult Subjects to Assess the Relative Bioavailability of Single-dose Simeprevir (SMV), Odalasvir (ODV), and AL-335 Administered as a Fixed-dose Combination (FDC) Compared With the [NCT03059303]Phase 172 participants (Actual)Interventional2017-02-20Terminated(stopped due to Decision to discontinue development of investigational Hep C treatment regimen JNJ-4178: 3 direct acting antivirals - AL-335, ODV & SMV.)
Comparison of Vonoprazan and Amoxicillin Dual Therapy With Standard Triple Therapy With Proton Pump Inhibitor for Helicobacter Pylori Eradication; a Randomized Control Trial [NCT04901663]Phase 4179 participants (Actual)Interventional2021-06-21Completed
A Single-center, Non-randomized, Open-lable, Self-controlled Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects [NCT06162169]Phase 166 participants (Anticipated)Interventional2023-11-25Recruiting
Protocol for a Randomised Trial of Observation Versus Chlorambucil After Anti-Helicobacter Therapy in Low Grade Gastric Lymphoma [NCT00003617]Phase 3200 participants (Anticipated)Interventional1995-03-31Active, not recruiting
A Single-centre, One-arm, Open-label, Fixed-sequence Study to Evaluate the Effect of Omeprazole on the Pharmacokinetics of SHR6390 in Healthy Male and Female Subjects [NCT04989829]Phase 120 participants (Actual)Interventional2021-12-27Completed
An Open-label Phase 1 Study to Evaluate Drug-Drug Interactions of Agents Co-Administered With Encorafenib and Binimetinib in Patients With BRAF V600-mutant Unresectable or Metastatic Melanoma or Other Advanced Solid Tumors [NCT03864042]Phase 156 participants (Actual)Interventional2018-01-02Active, not recruiting
A Single-Dose Study to Investigate the Pharmacokinetics of MK-7655 in Subjects With Impaired Renal Function [NCT01275170]Phase 149 participants (Actual)Interventional2011-01-28Completed
Bioavailability Study of Omeprazole (20 mg) at Steady State (Multiple Dose) in Patients Who Have Undergone Bariatric Surgery [NCT03378960]Phase 443 participants (Actual)Interventional2014-10-31Completed
A Randomized Controlled Multicenter Trial of a Five Day Course of Oral Colistin and Neomycin Followed by Restoration of the Gut Microbiota Using Fecal Transplantation to Eradicate Intestinal Carriage of Extended Spectrum Beta-lactamase or Carbapenemase-pr [NCT02472600]Phase 239 participants (Actual)Interventional2016-02-29Active, not recruiting
Flucloxacillin as an Inducer of CYP-enzymes [NCT04840641]Phase 114 participants (Actual)Interventional2021-03-25Completed
Anti-reflux Control to Decrease Post Tonsillectomy Pain [NCT01777854]Phase 46 participants (Actual)Interventional2013-01-31Terminated(stopped due to Lack of patient interest in the study.)
A Multi-center, Randomized, Double-blind Phase III Clinical Trial to Assess and Compare to the Efficacy and Safety of Lafutidine, Famotidine and Omeprazole-referenced in Koran Erosive Esophagitis Patients [NCT01499368]Phase 3495 participants (Actual)Interventional2011-11-30Completed
Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of X842 in Healthy Subjects [NCT03105375]Early Phase 139 participants (Actual)Interventional2017-02-21Completed
A Phase I, Open-label, Non-randomised Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor), Rifampicin (a CYP3A4 Inducer), and Omeprazole (a Proton Pump Inhibitor) on the Pharmacokinetics of a Single Oral Dose of Adavosertib in Patients With Ad [NCT04959266]Phase 15 participants (Actual)Interventional2021-06-28Terminated(stopped due to The study terminated because the clinical development programme for Adavosertib has been discontinued)
A 2-Part, Non-randomized, Open-label Study to Evaluate the Effect of Itraconazole, Rifampicin, Rabeprazole, and Omeprazole on the Pharmacokinetics of Belumosudil (KD025) [NCT03530995]Phase 173 participants (Actual)Interventional2018-04-09Completed
The Effectiveness of Standard Single Dose Omeprazole Versus High Dose Continuous Infusion in High-risk Critically Ill Patients. [NCT03388463]110 participants (Actual)Interventional2016-05-11Completed
Efficacy and Safety of Intravenous IIaprazole for Peptic Ulcer Bleeding: A Randomized, Double-Blind, Omeprazole-Controlled, Multicenter, and Phase 3 Trail in China [NCT03362281]Phase 3540 participants (Actual)Interventional2014-10-31Completed
Pathophysiological Evidence Driven Management of GERD in Neonatal ICU Infants: Randomized Controlled Trial [NCT06114836]369 participants (Anticipated)Interventional2023-11-01Not yet recruiting
A Single-centre, Single-arm, Open-label and Fixed-sequence Study to Evaluate the Effect of Omeprazole on Pharmacokinetics of Famitinib Malate in Healthy Adult Subjects [NCT05041920]Phase 120 participants (Actual)Interventional2021-09-07Completed
A Multicenter, Single-Arm, Open-Label Study to Evaluate the Immunogenicity and Pharmacokinetics of BIIB019, Daclizumab High Yield Process (DAC HYP), Prefilled Syringe Administered by Subcutaneous Injection in Subjects With Relapsing-Remitting Multiple Scl [NCT01462318]Phase 3133 participants (Actual)Interventional2011-11-30Completed
Efficacy on Helicobacter Pylori Eradication With Sequential Antibiotic Compared to Triple Therapy for 14 Days [NCT02395458]Phase 4142 participants (Actual)Interventional2013-03-31Completed
A PHASE 1, OPEN-LABEL, CROSS-OVER, FIXED SEQUENCE STUDY TO EVALUATE THE EFFECT OF MULTIPLE DOSES OF DS-1971A ON THE SINGLE DOSE PHARMACOKINETICS OF PROBE SUBSTRATES FOR CYP2B6, CYP2C8, CYP2C9, CYP2C19 AND CYP3A4 ENZYMES IN HEALTHY MALE AND FEMALE SUBJECTS [NCT02473627]Phase 118 participants (Actual)Interventional2015-05-31Completed
A Phase 1, Open-label, Parallel Group, Drug-drug Pharmacokinetic Interaction Study to Evaluate the Effects of Multiple-dose Omeprazole and Famotidine on the Absorption of Single-dose Telotristat Ethyl in Healthy Male and Female Subjects [NCT03302845]Phase 132 participants (Actual)Interventional2017-09-21Completed
The Effect of High Dose Rifampicin on the Activity of Cytochrome P450 Enzymes and P-glycoprotein in Patients With Pulmonary Tuberculosis: a Cocktail Phenotyping Study [NCT04525235]Phase 125 participants (Actual)Interventional2021-01-07Completed
A Phase 1, Four-part, Fixed-sequence, Open-label Study to Evaluate the Effect of Multiple Doses of CC-90001 on the Pharmacokinetics of Omeprazole, Midazolam, Warfarin, Rosuvastatin, Metformin, Digoxin, and Nintedanib in Healthy Adult Subjects [NCT03363815]Phase 156 participants (Actual)Interventional2017-12-04Completed
A Single Centre, Open-label, 5-Period, Cross Over, Randomized Study in Healthy Elderly Subjects to Evaluate the Relative Bioavailability of Hydrobromide Salt and Free Base Immediate Release Tablet Formulations of Danirixin in the Fed State, and to Evaluat [NCT02453022]Phase 118 participants (Actual)Interventional2015-05-18Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00141102 (17) [back to overview]Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)
NCT00141102 (17) [back to overview]Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIEs by History of GD Ulceration
NCT00141102 (17) [back to overview]Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Ferretin to Month 6/ET
NCT00141102 (17) [back to overview]Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)
NCT00141102 (17) [back to overview]Number of Subjects With Moderate to Severe Abdominal Symptoms
NCT00141102 (17) [back to overview]Number of Subjects With SUs
NCT00141102 (17) [back to overview]Number of Subjects Withdrawn Due to GI Adverse Events (AEs)
NCT00141102 (17) [back to overview]Change From Baseline in C-Reactive Protein to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Hematocrit at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Hemoglobin at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Iron Binding Capacity to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)
NCT00141102 (17) [back to overview]Number of Subjects Alive at the Post Trial Interview
NCT00141102 (17) [back to overview]Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview
NCT00210470 (8) [back to overview]Disease-free Survival
NCT00210470 (8) [back to overview]Number of Participants With High Lymphocyte Infiltration (LI) According to the Visual Analog Scale (VAS)
NCT00210470 (8) [back to overview]Relationship Between Overall Survival (OS) and Immune Competence (Lymphocyte Infiltration, LI) in Participants With High LI and Low LI
NCT00210470 (8) [back to overview]Overall Survival
NCT00210470 (8) [back to overview]Patient Tolerance of Surgery and Post-operative Adjuvant Therapy;
NCT00210470 (8) [back to overview]Immune Competence as Measured by Skin Test Reactivity
NCT00210470 (8) [back to overview]Number of Participants With Adverse Events and Serious Adverse Events
NCT00210470 (8) [back to overview]Clinical and Histological Tumor Responses
NCT00492622 (3) [back to overview]Maximal Concentration of Omerazole
NCT00492622 (3) [back to overview]Area Under the Curve for Omeprazole Plasma Concentration
NCT00492622 (3) [back to overview]Time to Maximal Omeprazole Concentration (Tmax)
NCT00557349 (2) [back to overview]Number of Participants With Upper Endoscopy Indicated Due to Complaints
NCT00557349 (2) [back to overview]Number of Participants With Complaints, Specifically About Pain, Vomiting, Dyspepsia, and/or Dysphagia.
NCT00559364 (3) [back to overview]Percentage of Stools Categorized as Per Consistency
NCT00559364 (3) [back to overview]Mean Daily Number of Stools
NCT00559364 (3) [back to overview]Percent Coefficient of Fat Absorption (CFA)
NCT00582972 (2) [back to overview]Change in Bone Resorption From Baseline to 1 Month
NCT00582972 (2) [back to overview]Change in Intestinal Calcium Absorption From Baseline to One Month
NCT00633932 (2) [back to overview]"Number of Participants With Healing of Reflux Esophagitis (RE) Who Were Graded O at Week 8 Out of Patients Who Were Graded A, B, C or D at Baseline According to Los Angeles Classification."
NCT00633932 (2) [back to overview]"Number of Participants With Healing of Reflux Esophagitis (RE) Who Were Graded O at Week 4 Out of Patients Who Were Graded A, B, C or D at Baseline According to Los Angeles Classification"
NCT00634114 (3) [back to overview]Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification up to 12 Weeks After Treatment
NCT00634114 (3) [back to overview]Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification Throughout the Treatment Period.
NCT00634114 (3) [back to overview]Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification up to 4 Weeks After Treatment
NCT00655746 (6) [back to overview]Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations
NCT00655746 (6) [back to overview]Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax)
NCT00655746 (6) [back to overview]Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T])
NCT00655746 (6) [back to overview]Dasatinib PK Parameter: Plasma Half-Life (T-HALF)
NCT00655746 (6) [back to overview]Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF])
NCT00655746 (6) [back to overview]Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax)
NCT00664209 (1) [back to overview]Participants With Side Effects From Study Treatment
NCT00668317 (1) [back to overview]Change in Methacholine Sensitivity
NCT00669955 (7) [back to overview]H. Pylori Eradication and Presence or Past History of Peptic Ulcers
NCT00669955 (7) [back to overview]Helicobacter Pylori Eradication Confirmed by Urea Breath Test
NCT00669955 (7) [back to overview]Metronidazole Resistance
NCT00669955 (7) [back to overview]Number of Patients Experiencing Treatment Emergent Adverse Events.
NCT00669955 (7) [back to overview]Number of Patients With Bismuth Plasma Concentrations Above the Toxic Level
NCT00669955 (7) [back to overview]Clarithromycin Resistance
NCT00669955 (7) [back to overview]Overall Compliance to Study Medications
NCT00674115 (1) [back to overview]Change From Baseline in Median 24-hour Intragastric pH on the 7th Day of Drug Administration
NCT00693225 (3) [back to overview]Percent of Subjects Overall Who Healed, Improved, or Stayed the Same or Worsened After 8 Weeks of Treatment
NCT00693225 (3) [back to overview]Percent of Subjects With Moderate Esophagitis (LA Grade C) Who Healed, Improved, or Stayed the Same or Worsened After 8 Weeks of Treatment
NCT00693225 (3) [back to overview]Percent of Subjects With Severe Esophagitis (LA Grade D) Who Healed, Improved, or Stayed the Same After 8 Weeks of Treatment
NCT00741468 (1) [back to overview]Plasma AUC Ratio of Day 1 and Day 8
NCT00765206 (1) [back to overview]Change From Baseline in Median 24-hour Intragastric pH on the 7th Day of Drug Administration
NCT00838682 (6) [back to overview]Rebleeding After 3 Days
NCT00838682 (6) [back to overview]Mean Units of Blood Transfusion
NCT00838682 (6) [back to overview]Death
NCT00838682 (6) [back to overview]Duration of Hospital Stay
NCT00838682 (6) [back to overview]Surgery
NCT00838682 (6) [back to overview]Rebleeding Within 3 Days
NCT00903448 (1) [back to overview]Mean Percent Time That Gastric pH > 4.0 on Day 5
NCT00942175 (5) [back to overview]Pharmacodynamic Parameter Platelet Reactivity Index (PRI) From Vasodilator-stimulated Phosphoprotein (VASP) Phosphorylation State (Flow Cytometry).
NCT00942175 (5) [back to overview]Pharmacokinetic Parameter Area Under the Plasma Concentration Versus Time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration (AUC[0-tlqc]) of Clopidogrel's Active Metabolite.
NCT00942175 (5) [back to overview]Pharmacokinetic Parameter Peak Plasma Concentration (Cmax) of Clopidogrel's Active Metabolite.
NCT00942175 (5) [back to overview]Pharmacodynamic Parameter Maximum Platelet Aggregation (MPA) From Aggregometry (Turbidimetric) With 5 µM Adenosine Diphosphate.
NCT00942175 (5) [back to overview]Pharmacodynamic Parameter MPA From Aggregometry (Turbidimetric) With 20 µM Adenosine Diphosphate.
NCT01000818 (1) [back to overview]Plasma Area Under Curve (AUC 0-12 hr ) for Raltegravir
NCT01005719 (18) [back to overview]Time to Achieve Sustained Advantage Over No Treatment During the First 4 Hours After Dosing
NCT01005719 (18) [back to overview]The Difference in the Onset of Action Based on Median pH Values Between the Two Active Treatments Compared to No Treatment on Day 1 and Day 7
NCT01005719 (18) [back to overview]Median Time to Achieve Intragastric pH > = 3.5 for a 10-Minute Period
NCT01005719 (18) [back to overview]Time to Achieve Sustained Intragastric pH > 3.5 at Steady-state on Day 7
NCT01005719 (18) [back to overview]Achievement of Sustained Difference in Inhibition of Intragastric Acidity Based on Median pH Values Between the Two Active Study Treatments at Steady-state on Day 7
NCT01005719 (18) [back to overview]Achievement of Sustained Difference in Inhibition of Intragastric Acidity Based on Median pH Values Between the Two Active Study Treatments at Steady-state on Day 1
NCT01005719 (18) [back to overview]Time to Onset of Inhibition of Acid Secretion on Day 1
NCT01005719 (18) [back to overview]Percentage Time Intragastric pH >4 During the First 4 Hours After Dosing on Day 7
NCT01005719 (18) [back to overview]Percentage of Time Intragastric pH >4 Over the Nocturnal Period on Day 7
NCT01005719 (18) [back to overview]Percentage of Time Intragastric pH >4 Over the Nocturnal Period on Day 1
NCT01005719 (18) [back to overview]Percentage of Time Intragastric pH >4 During the First 4 Hours on Day 1
NCT01005719 (18) [back to overview]Percentage of Time Intragastric pH >3.5 Over 24-hour Period on Day 7
NCT01005719 (18) [back to overview]Percentage of Time Intragastric is pH >4 Over 24-hour Period on Day 7
NCT01005719 (18) [back to overview]Number of Participants With Intragastric pH >4 for More Than 50% of the Time on Day 7
NCT01005719 (18) [back to overview]Number of Participants With Intragastric pH >3.5 for More Than 50% of the Time on Day 7
NCT01005719 (18) [back to overview]Number of Participants Maintaining Intragastric pH > 3.5 for at Least 12 Hours on Day 1
NCT01005719 (18) [back to overview]Median 24-hr Intragastric pH on Day 7
NCT01005719 (18) [back to overview]Number of Participants Maintaining Intragastric pH > 4 for at Least 12 Hours on Day 1
NCT01061034 (2) [back to overview]Platelet Function Tests
NCT01061034 (2) [back to overview]Aspirin Level in Blood (Area Under the Curve)
NCT01077076 (1) [back to overview]Percent Time With Intragastric pH>4 During the First 4 Hours Following Administration on Day 4 of Treatment
NCT01093755 (2) [back to overview]Change in Inflammation Biomarker Tissue PGE2 Level
NCT01093755 (2) [back to overview]Change in Esophageal Inflammation Biomarker COX-2 Gene Expression
NCT01122160 (1) [back to overview]Gastric pH
NCT01129778 (2) [back to overview]Percentage of Time Esophageal pH< 4
NCT01129778 (2) [back to overview]Reflux Disease Questionnaire Score on Day 1 After Therapy Completion
NCT01170533 (1) [back to overview]Platelet Function as Assessed by the P2Y12 Reactivity Index
NCT01275170 (27) [back to overview]Parts 1 and 2: Percentage of Participants With ≥1 Adverse Events (AEs)
NCT01275170 (27) [back to overview]Dialysis Clearance (CLD) of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)
NCT01275170 (27) [back to overview]Part 2: Plasma AUC0-∞ of Caffeine as a Probe Substrate of Cytochrome P450 Enzyme (CYP)1A2
NCT01275170 (27) [back to overview]Part 1: Apparent Plasma Half-life (t½) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 1: VZpred of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Extraction Coefficient of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)
NCT01275170 (27) [back to overview]Part 1: VZpred of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Tmax of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Tmax of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Time of Maximum Plasma Concentration (Tmax) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 2: Plasma AUC0-∞ of Midazolam as a Probe Substrate of Cytochrome P450 Enzyme (CYP)3A4
NCT01275170 (27) [back to overview]Part 1: Renal Clearance (CLR) of MK-7655 in Urine
NCT01275170 (27) [back to overview]Part 1: Predicted Volume of Distribution During the Terminal Phase (VZpred) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 1: Predicted Clearance (CLpred) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 1: Concentration at End of Infusion (Ceoi) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 1: CLR of Imipenem in Urine
NCT01275170 (27) [back to overview]Part 1: CLR of Cilastin in Urine
NCT01275170 (27) [back to overview]Part 1: CLpred of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: CLpred of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: AUC0-inf of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Ceoi of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Ceoi of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: AUC0-inf of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Area Under the Plasma Concentration-time Curve From Dosing to Infinity (AUC0-inf) of MK-7655 in Combination With PRIMAXIN®
NCT01275170 (27) [back to overview]Part 1: Apparent t½ of Imipenem in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 1: Apparent t½ of Cilastin in Combination With MK-7655
NCT01275170 (27) [back to overview]Part 2: Plasma AUC0-∞ of Omeprazole as a Probe Substrate of Cytochrome P450 Enzyme (CYP)2C19
NCT01287195 (8) [back to overview]Percentage of Biomarker-positive Immune Cells
NCT01287195 (8) [back to overview]Score in Histologic Evaluation of Flexible Sigmoidoscopy
NCT01287195 (8) [back to overview]T Cell Proliferation of PBMCs in Cell Culture
NCT01287195 (8) [back to overview]Simple Clinical Colitis Activity Index (SCCAI) Score
NCT01287195 (8) [back to overview]Number of Participants With Adverse Events
NCT01287195 (8) [back to overview]Number of Participants With Anti-Drug Antibodies
NCT01287195 (8) [back to overview]Cytokine Production by PBMCs in Cell Culture
NCT01287195 (8) [back to overview]Mayo Score
NCT01303445 (6) [back to overview]Inhibition of Platelet Aggregation at 4 Hours Post Dose (IPA4)
NCT01303445 (6) [back to overview]Plasma Dipyridamole Minimum Concentration (Cmin)
NCT01303445 (6) [back to overview]Plasma Dipyridamole Maximum Concentration (Cmax)
NCT01303445 (6) [back to overview]Inhibition of Platelet Aggregation at 12 Hours Post Dose (IPA12)
NCT01303445 (6) [back to overview]Plasma Dipyridamole Area Under Plasma Concentration-time Curve From Zero to 12 Hours (AUC0-12)
NCT01303445 (6) [back to overview]Percentage Peak-to-trough Fluctuation (%PTF)
NCT01341600 (4) [back to overview]Level of Active Clopidogrel Metabolite
NCT01341600 (4) [back to overview]Change in Platelet Aggregation Following Therapy With Clopidogrel
NCT01341600 (4) [back to overview]Change in Platelet Aggregation Following Therapy With Clopidogrel
NCT01341600 (4) [back to overview]Change in Platelet Aggregation Following Therapy With Clopidogrel and Omeprazole
NCT01361217 (2) [back to overview]AUC of Dextromethorphan, Midazolam and Omeprazole in the Presence of Fluoxetine
NCT01361217 (2) [back to overview]Lovastatin AUC in the Presence of Fluoxetine
NCT01415349 (2) [back to overview]Maximum Plasma Concentration (Cmax) for SSP-002358
NCT01415349 (2) [back to overview]Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) for SSP-002358
NCT01458990 (2) [back to overview]Number of Patients With Overgrowth of Oral Microbiota in Their Stool After PPI Therapy Withdrawal or Initiation
NCT01458990 (2) [back to overview]Number of Patients With Adverse Events During Initiation or Withdrawal of PPI Therapy
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Time to Reach Maximum Concentration (Tmax) of DAC HYP
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Cmax of DAC HYP
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Area-Under-the-Curve From Start to End of the Dosing Interval (AUCtau) of DAC HYP
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Elimination Half-life (t½) of DAC HYP
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Minimum Concentrations (Cmin) of DAC HYP
NCT01462318 (14) [back to overview]Number of Participants With Anti-DAC HYP Neutralizing Antibodies (NAbs): ECL ADA Assay
NCT01462318 (14) [back to overview]TP-DI Sub-study: Area-Under-the-Curve From Zero to Infinity (AUCinf) of Each Probe Drug
NCT01462318 (14) [back to overview]TP-DI Sub-study: CL/F of Each Probe Drug
NCT01462318 (14) [back to overview]TP-DI Sub-study: Cmax of Each Probe Drug
NCT01462318 (14) [back to overview]TP-DI Sub-study: Omeprazole/Hydroxyomeprazole Concentration Ratio at 2 Hours Post-omeprazole Dosing
NCT01462318 (14) [back to overview]TP-DI Sub-study: Dextromethorphan to Dextrorphan Urine Concentration Ratio
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Apparent Clearance (CL/F) of DAC HYP
NCT01462318 (14) [back to overview]Intensive PK Sub-study: Apparent Volume of Distribution (V/F) of DAC HYP
NCT01462318 (14) [back to overview]Number of Participants With Anti-DAC HYP Binding Antibodies (ADAbs): Electrochemiluminescent (ECL) Anti-Drug Antibody (ADA) Assay
NCT01499368 (3) [back to overview]The Proportion of Nighttimes Without 'Cardinal Symptom'
NCT01499368 (3) [back to overview]The Proportion of Daytimes Without 'Cardinal Symptom'
NCT01499368 (3) [back to overview]The Proportion of Days Without 'Cardinal Symptom'
NCT01587885 (6) [back to overview]Percentage of Participants Affected By Heartburn Symptoms: End of Treatment Quality of Life Questionnaire
NCT01587885 (6) [back to overview]Percentage of Participants Experiencing Onset and Demonstrating Duration of Heartburn Relief Over Time
NCT01587885 (6) [back to overview]Time-to-onset of Heartburn Relief
NCT01587885 (6) [back to overview]Number of Participants Preferring Each Treatment for Heartburn Control: Final Subjective Questionnaire
NCT01587885 (6) [back to overview]Number of Participants Preferring Each Treatment for Heartburn Relief: Final Subjective Questionnaire
NCT01587885 (6) [back to overview]Number of Participants Preferring Each Treatment Overall: Final Subjective Questionnaire
NCT01593592 (3) [back to overview]Eradication of H Pylori Infection 4 Weeks After Completion of Therapy
NCT01593592 (3) [back to overview]Severe Adverse Effects to the Used Medications and Dietary Supplements.
NCT01593592 (3) [back to overview]The Secondary End Point Was the Development of Severe Adverse Effects to the Used Medications and Dietary Supplements.
NCT01694706 (3) [back to overview]Faldaprevir: Area Under the Curve Over the Time Interval From 0 Extrapolated to Infinity (AUC 0-infinity)
NCT01694706 (3) [back to overview]Faldaprevir: Area Under the Curve 0 to the Last Quantifiable Data Point (AUC0-tz)
NCT01694706 (3) [back to overview]Faldaprevir: Maximum Measured Concentration (Cmax)
NCT01766050 (36) [back to overview]Ratio of 1'-Hydroxy-Midazolam AUC(0-T) to Midazolam AUC(0-T) and 1'-Hydroxy-Midazolam AUC(INF) to Midazolam AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Plasma Half-Life (T-HALF) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of 5-Hydroxyomeprazole AUC(0-T) to Omeprazole AUC(0-T) and 5-Hydroxyomeprazole AUC(INF) to Omeprazole AUC(INF) , Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of E-3174 AUC(0-T) to Losartan AUC(0-T) and E3174 AUC (INF) to Losartan AUC (INF) Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of 5-Dextrorphan AUC(0-T) to Dextromethorphan AUC(0-T) and 5-Dextrorphan AUC(INF) to Dextromethorphan AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of Paraxanthine AUC(0-T) to Caffeine AUC(0-T) and Paraxanthine AUC (INF) to Caffeine AUC (INF), Corrected for Molecular Weight [MR_AUC(0-T) and MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]T-HALF of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Time of Maximum Observed Plasma Concentration (Tmax) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Tmax of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Mean Change From Baseline in Heart Rate at Study Discharge (Day 46±2 Days)
NCT01766050 (36) [back to overview]AUC(0-T) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Cmax of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths, and AEs Leading to Discontinuation - All Treated Participants
NCT01766050 (36) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Study Discharge (Day 46±2 Days)
NCT01766050 (36) [back to overview]Mean Change From Baseline in Sitting Heart Rate - All Treated Participants
NCT01766050 (36) [back to overview]Cmax of Inje Cocktail Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]AUC(INF) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of E-3174 (Cmax) to Losartan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Apparent Total Body Clearance (CLT/F) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Losartan With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Area Under the Concentration Time Curve (AUC) From Zero to Last Concentration (0-T) and AUC Extrapolated to Infinity (INF) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]Ratio of Paraxanthine (Cmax) to Caffeine (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of 1'-Hydroxy-Midazolam (Cmax) to Midazolam (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Cmax of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Number of Participants With Marked Hematology and Urinalysis Laboratory Abnormalities - All Treated Participants
NCT01766050 (36) [back to overview]Mean Change From Baseline in Sitting Systolic and Diastolic Blood Pressure - All Treated Participants
NCT01766050 (36) [back to overview]Number of Participants With Marked Serum Chemistry Laboratory Abnormalities - All Treated Participants
NCT01766050 (36) [back to overview]Number of Participants With Out-of-Range Electrocardiogram Intervals - All Treated Participants
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Maximum Drug Concentration (Cmax) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Cmax of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]Adjusted Geometric Mean Cmax of Losartan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of 5-Hydroxyomeprazole (Cmax) to Omeprazole (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]Ratio of 5-Dextrorphan (Cmax) to Dextromethorphan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01851863 (4) [back to overview]Change From Baseline in Psychiatric Symptom on Hospital Anxiety and Depression Scale at Week 8
NCT01851863 (4) [back to overview]Number of Participants With Adverse Reaction
NCT01851863 (4) [back to overview]Compliance of Flupentixol-Melitracen
NCT01851863 (4) [back to overview]Change From Baseline in Dyspepsia Symptom Questionnaire at Week 8
NCT01896557 (4) [back to overview]Comparison of the Primary Outcome With Bioimpedance Aggregometry
NCT01896557 (4) [back to overview]Comparing Platelet Function of Patients on Dual Antiplatelet Therapy With ASA + Clopidogrel, Between the Groups Ranitidin and Omeprazole, Using VerifyNow Method.
NCT01896557 (4) [back to overview]Comparing Platelet Function of Patients on Dual Antiplatelet Therapy With ASA + Clopidogrel, Between the Groups Ranitidin and Omeprazole, After One Week of Randomized Treatment
NCT01896557 (4) [back to overview]Comparison of the Primary Outcome With PFA-100 (Collagen/ADP Cartridge)
NCT01925144 (3) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Baricitinib
NCT01925144 (3) [back to overview]PK: Area Under the Plasma Concentration-Time Curve From Time 0 Hour to Infinity [AUC(0-∞)] of Baricitinib
NCT01925144 (3) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Baricitinib
NCT01983566 (2) [back to overview]AUC(0-tz)
NCT01983566 (2) [back to overview]Cmax
NCT02013427 (1) [back to overview]Change in Pain Assessed by Visual Analogue Scale (VAS)
NCT02224053 (14) [back to overview]Vz/F of AZD9291
NCT02224053 (14) [back to overview]Cmax of AZD9291
NCT02224053 (14) [back to overview]CL/F of AZD9291
NCT02224053 (14) [back to overview]AUC of AZD9291
NCT02224053 (14) [back to overview]AUC(0-72)
NCT02224053 (14) [back to overview]λz
NCT02224053 (14) [back to overview]Tmax
NCT02224053 (14) [back to overview]Tlag
NCT02224053 (14) [back to overview]t(1/2)
NCT02224053 (14) [back to overview]Parent to Metabolite Ratios of AZ5104 and AZ7550 Cmax
NCT02224053 (14) [back to overview]Parent to Metabolite Ratios of AZ5104 and AZ7550 AUC
NCT02224053 (14) [back to overview]Cmax of AZ5104 and AZ7550
NCT02224053 (14) [back to overview]AUC(0-t)
NCT02224053 (14) [back to overview]AUC of AZ5104 and AZ7550
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞])
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Concentration (Tmax) of Evacetrapib
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib
NCT02394340 (2) [back to overview]Circulating Levels (Plasma Concentration) of Omeprazole Prior to Treatment With Luliconazole Cream 1%
NCT02394340 (2) [back to overview]Circulating Levels (Plasma Concentration) of Omeprazole After 1 Week of Treatment With Luliconazole Cream 1%
NCT02500641 (1) [back to overview]Pulse Wave Velocity
NCT02504554 (7) [back to overview]Parent Global Impressions-Revised (PGI-R)
NCT02504554 (7) [back to overview]Social Responsiveness Scale (SRS)
NCT02504554 (7) [back to overview]Gastrointestinal Symptom Responsiveness Scale (GSRS)
NCT02504554 (7) [back to overview]Daily Stool Record (DSR)
NCT02504554 (7) [back to overview]Childhood Autism Rating Scale (CARS)
NCT02504554 (7) [back to overview]Blood Safety Markers (Assessment of Blood Chemistry Panel and Complete Blood Count)
NCT02504554 (7) [back to overview]Vineland Adaptive Behavior Scale (VABS)
NCT02505945 (2) [back to overview]Percentage of Subjects With ≥50% Reduction in Total Gastroesophageal Reflux Disease-Health Related Quality of Life (GERD-HRQL) Scores
NCT02505945 (2) [back to overview]Elimination of Moderate-severe Regurgitation at 6 Months
NCT02595372 (6) [back to overview]FASN Positivity Expression at Baseline and After 4-7 Days of Omeprazole Treatment
NCT02595372 (6) [back to overview]Number of Patients With Treatment Related Adverse Events Grade 3 or Above
NCT02595372 (6) [back to overview]Percent of Patients With FASN Expression
NCT02595372 (6) [back to overview]Percentage of Patients With Pathological Complete Response (pCR) in All Patients
NCT02595372 (6) [back to overview]Percentage of Patients With Pathological Complete Response (pCR) in Patients Who Have Fatty Acid Synthase (FASN) Expression
NCT02595372 (6) [back to overview]FASN Activity at Baseline and After 4-7 Days of Omeprazole Treatment
NCT02623816 (1) [back to overview]Symptom Frequency and Severity/Distress Scores From Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) (Overall)
NCT02986334 (1) [back to overview]Percent Change in Pain Assessed by Visual Analogue Scale (VAS)
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to 48 Hours (AUC[0-48h]) of CYP450 Substrate-Caffeine
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Warfarin
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Dextromethorphan
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Midazolam
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Caffeine
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Dextromethorphan
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Warfarin
NCT02993471 (10) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Cytochrome P450 (CYP450) Substrate-Midazolam
NCT03028103 (19) [back to overview]Part A: PK of Tazemetostat and Its Metabolites After Administration Alone and With Fluconazole (AUC0-t, AUC0-8)
NCT03028103 (19) [back to overview]Part A: t1/2 of Tazemetostat After Administration Alone and With Fluconazole
NCT03028103 (19) [back to overview]Part A: t1/2 of Tazemetostat Metabolites After Administration Alone and With Fluconazole
NCT03028103 (19) [back to overview]Part A: Tmax of Tazemetostat After Administration Alone and With Fluconazole
NCT03028103 (19) [back to overview]Part A: Tmax of Tazemetostat Metabolites After Administration Alone and With Fluconazole
NCT03028103 (19) [back to overview]Part B: Cmax of Omeprazole During Co-administration With Tazemetostat
NCT03028103 (19) [back to overview]Part B: Cmax of Repaglinide During Co-administration With Tazemetostat
NCT03028103 (19) [back to overview]Part B: Cmax of Tazemetostat During Co-administration With Omeprazole
NCT03028103 (19) [back to overview]Part B: Effect of Increased Gastric pH by Omeprazole on the PK of Tazemetostat (AUC0-t, AUC0-8)
NCT03028103 (19) [back to overview]Part B: The Potential of Tazemetostat to Inhibit or Induce CYP2C19 Using Omeprazole as Probe a Substrate (AUC0-t, AUC0-∞)
NCT03028103 (19) [back to overview]Part B: The Potential of Tazemetostat to Inhibit or Induce CYP2C8 Using Repaglinide as a Probe Substrate (AUC0-t, AUC0-∞)
NCT03028103 (19) [back to overview]The Antitumor Activity of Tazemetostat Will be Assessed in Patients With Diffuse Large B-cell Lymphoma (DLBCL), Marginal Zone Lymphoma (MZL), Follicular Lymphoma (FL) or Advanced Solid Tumors .
NCT03028103 (19) [back to overview]Part A: Exposure of Fluconazole After Administration of 400 mg Once Daily for 4 Days (AUC0-8)
NCT03028103 (19) [back to overview]Part A: Cmax of Fluconazole After Administration of 400mg Once Daily for 4 Days
NCT03028103 (19) [back to overview]Part A: Tmax of Fluconazole After Administration of 400mg Once Daily for 4 Days
NCT03028103 (19) [back to overview]Incidence of Treatment-emergent Adverse Events as a Measure of Safety
NCT03028103 (19) [back to overview]Part A: Cmax of Tazemetostat During Co-administration With Fluconazole
NCT03028103 (19) [back to overview]Part A: Cmax of Tazemetostat Metabolites After Administration Alone and With Fluconazole
NCT03028103 (19) [back to overview]Part A: Effect of CYP3A Inhibition by Fluconazole on the PK of Tazemetostat (AUC0-t, AUC0-8)
NCT03094416 (14) [back to overview]Sex Hormone Binding Globulin (SHBG)
NCT03094416 (14) [back to overview]Thyroid Stimulating Hormone (TSH)
NCT03094416 (14) [back to overview]Total Thyroxine (TT4)
NCT03094416 (14) [back to overview]Total Triiodothyronine (TT3)
NCT03094416 (14) [back to overview]Triglycerides
NCT03094416 (14) [back to overview]Very Low Density Lipoprotein (VLDL)-Cholesterol
NCT03094416 (14) [back to overview]High Density Lipoprotein (HDL)-Cholesterol
NCT03094416 (14) [back to overview]Ferritin
NCT03094416 (14) [back to overview]Free Triiodothyronine (FT3)
NCT03094416 (14) [back to overview]Free Thyroxine (FT4)
NCT03094416 (14) [back to overview]Angiotensin Converting Enzyme (ACE)
NCT03094416 (14) [back to overview]Cholesterol, Total
NCT03094416 (14) [back to overview]Creatine Phosphokinase (CPK)
NCT03094416 (14) [back to overview]Low Density Lipoprotein (LDL)-Cholesterol
NCT03100838 (5) [back to overview]Area Under the Concentration (AUC 0-t)
NCT03100838 (5) [back to overview]Adverse Events
NCT03100838 (5) [back to overview]Time at Maximum Plasma Concentration (Tmax)
NCT03100838 (5) [back to overview]Maximum Plasma Concentration (Cmax)
NCT03100838 (5) [back to overview]Half-life
NCT03198507 (4) [back to overview]Number of Participants With Eradication of H. Pylori in the Pharmacokinetic Population (PKP)
NCT03198507 (4) [back to overview]Number of Participants With Eradication of H. Pylori
NCT03198507 (4) [back to overview]Number of Participants With H. Pylori Cultures That Presented Antibiotic Resistance and Susceptibility
NCT03198507 (4) [back to overview]Number of Participants With Adverse Events That Are Related to Treatment
NCT03327051 (5) [back to overview]Change in Peak Intensity of the Metabolite 1H-Indole-4-carbaldehyde Before and After VSL#3 Probiotic Administration (Omeprazole and VSL #3).
NCT03327051 (5) [back to overview]Relative Abundance of VSL#3 Probiotic Bacterial Strains When Ingested in the Presence or Absence of the Proton Pump Inhibitor (PPI) Omeprazole at Week 4.
NCT03327051 (5) [back to overview]Change in Peak Intensity of Metabolites of Interest Before and After VSL#3 Probiotic Administration (Placebo and VSL#3 Group).
NCT03327051 (5) [back to overview]Number of Participants With Symptoms Related to VSL#3 Treatment.
NCT03327051 (5) [back to overview]Relative Abundance (Mean Value) of Most Abundant Bacterial Phylum Before and After VSL#3 Probiotic Administration
NCT03457727 (24) [back to overview]Maximum Observed Concentration (Cmax) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Maximum Observed Concentration (Cmax) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Number of Participants With 12-lead Electrocardiogram (ECG) Values of Potential Clinical Concern in Part 1
NCT03457727 (24) [back to overview]Number of Participants With Laboratory Values of Potential Clinical Concern in Part 1
NCT03457727 (24) [back to overview]Number of Participants With Laboratory Values of Potential Clinical Concern in Part 2
NCT03457727 (24) [back to overview]Time to Occurrence of Cmax (Tmax) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Number of Participants With Any Adverse Event (AE) and Serious Adverse Events in Part 2
NCT03457727 (24) [back to overview]Number of Participants With Any Adverse Event (AE) and Serious Adverse Events (SAEs) in Part 1
NCT03457727 (24) [back to overview]Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Number of Participants With 12-lead Electrocardiogram (ECG) Values of Potential Clinical Concern in Part 2
NCT03457727 (24) [back to overview]Time to Maximum Observed Concentration (Tmax) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Time to Last Quantifiable Concentration (Tlast) of the Blood Concentration of Danirixin for Part 2
NCT03457727 (24) [back to overview]Time to Last Quantifiable Concentration (Tlast) of the Blood Concentration of Danirixin for Part 1
NCT03457727 (24) [back to overview]Terminal Half-life (t1/2) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Terminal Half-life (t1/2) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Number of Participants With Vital Signs of Potential Clinical Concern in Part 2
NCT03457727 (24) [back to overview]Number of Participants With Vital Signs of Potential Clinical Concern in Part 1
NCT03457727 (24) [back to overview]Lag Time Before Observable Concentration (Tlag) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to t (AUC [0-t]) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to t (AUC [0-t]) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to Infinity (AUC [0-inf]) of Danirixin for Part 2
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to Infinity (AUC [0-inf]) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose (AUC [0-24]) of Danirixin for Part 1
NCT03457727 (24) [back to overview]Area Under the Concentration-time Curve From Time 0 to 24 Hours (AUC [0-24]) of Danirixin for Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025m1 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2
NCT03531762 (12) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment A and Treatment C
NCT03531762 (12) [back to overview]Apparent Volume of Distribution During Terminal Phase (Vz/f) of Tepotinib in Treatments A, B and C
NCT03531762 (12) [back to overview]Apparent Total Body Clearance (CL/f) of Tepotinib in Treatments A, B and C
NCT03531762 (12) [back to overview]Apparent Terminal Half-life (t1/2) of Tepotinib in Treatments A, B and C
NCT03531762 (12) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment B
NCT03531762 (12) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment A and Treatment C
NCT03531762 (12) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment B
NCT03531762 (12) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment A and Treatment C
NCT03531762 (12) [back to overview]Number of Participants With Clinically Significant Changes in Laboratory Parameters, 12-lead Electrocardiogram (ECG) Findings and Vital Signs
NCT03531762 (12) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) of Tepotinib in Treatments A, B and C
NCT03531762 (12) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs)
NCT03531762 (12) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment B
NCT03793556 (14) [back to overview]Score of Difficulty in Swallowing Food, Fluids or Pills of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Difficulty in Breathing or Episodes of Choking of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Cough of the RSI Questionnaire Measured at Baseline and in the Visit 4 After the Meal or After Lying
NCT03793556 (14) [back to overview]Presence of Upper Symptoms at Visit 4, Using the RSI Questionnaire
NCT03793556 (14) [back to overview]Change From Baseline to Visit V4 of the Total Score of RSI Questionnaire
NCT03793556 (14) [back to overview]Patients'Satisfaction
NCT03793556 (14) [back to overview]Total Score of Reflux Symptom Index Questionnaire in All Time-points Assessed
NCT03793556 (14) [back to overview]Score of Upper Symptoms Using the Likert Scale at Baseline and in the Visit V4
NCT03793556 (14) [back to overview]Score of Throat of the RSI Questionnarie Measured at the Baseline and in the Visit 4 of the RSI Questionnaire Score of Throat Clearance
NCT03793556 (14) [back to overview]Score of Stomach Burning, Thoracic Pain, Poor Digestion of Gastric Acid That Moves Upright of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Sensation of Something Blocked or Mass in the Throat of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Problematic or Troublesome Cough of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Hoarseness or Vocal Problem of the RSI Questionnaire Measured at the Baseline and in the Visit 4
NCT03793556 (14) [back to overview]Score of Excess of Mucus in the Throat or Retrosternal Fall of Secretions of the RSI Questionnaire Measured at Baseline and in the Visit 4
NCT03866434 (7) [back to overview]Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Anagrelide (SPD422) in Plasma
NCT03866434 (7) [back to overview]Area Under the Concentration Versus Time Curve From Zero to Last Time Point (AUC[0-t]) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide) in Plasma
NCT03866434 (7) [back to overview]Maximum Observed Plasma Concentration (Cmax) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide)
NCT03866434 (7) [back to overview]Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide) in Plasma
NCT03866434 (7) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Anagrelide (SPD422)
NCT03866434 (7) [back to overview]Area Under the Concentration Versus Time Curve From Zero to Last Time Point (AUC[0-t]) of Anagrelide (SPD422) in Plasma
NCT03866434 (7) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Treatment Emergent Serious Adverse Events (TESAEs)
NCT04198948 (3) [back to overview]Insulin
NCT04198948 (3) [back to overview]Gliclazide AUC
NCT04198948 (3) [back to overview]Glucose
NCT04425902 (171) [back to overview]Treatment A: Absolute Values for Electrocardiogram (ECG) Parameters: PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Fridericia's Formula (QTcF)
NCT04425902 (171) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT04425902 (171) [back to overview]Treatment C: Tmax for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: t1/2 for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: Plasma Concentration at the End of the Dosing Interval (Ctau) for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: Cmax for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: AUC(0-t) for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: AUC From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) for GSK3640254
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Respiratory Rate
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Pulse Rate
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Oral Temperature
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Hemoglobin
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Hematocrit
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Erythrocytes
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Respiratory Rate
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Pulse Rate
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Oral Temperature
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Hemoglobin
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Hematocrit
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Erythrocytes
NCT04425902 (171) [back to overview]Tmax for Pravastatin
NCT04425902 (171) [back to overview]Tmax for Omeprazole
NCT04425902 (171) [back to overview]Tmax for Montelukast
NCT04425902 (171) [back to overview]Tmax for Midazolam
NCT04425902 (171) [back to overview]Tmax for Metoprolol
NCT04425902 (171) [back to overview]Tmax for Flurbiprofen
NCT04425902 (171) [back to overview]Tmax for Digoxin
NCT04425902 (171) [back to overview]Tmax for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]Tmax for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]Tmax for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]Tmax for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]Time to Cmax (Tmax) for Caffeine
NCT04425902 (171) [back to overview]t1/2 for Pravastatin
NCT04425902 (171) [back to overview]t1/2 for Omeprazole
NCT04425902 (171) [back to overview]t1/2 for Montelukast
NCT04425902 (171) [back to overview]t1/2 for Midazolam
NCT04425902 (171) [back to overview]t1/2 for Metoprolol
NCT04425902 (171) [back to overview]t1/2 for Flurbiprofen
NCT04425902 (171) [back to overview]t1/2 for Digoxin
NCT04425902 (171) [back to overview]t1/2 for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]t1/2 for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]t1/2 for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]t1/2 for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]Ratio of Cmax of Alpha-hydroxymetoprolol to Metoprolol
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Ratio of Cmax of 5-hydroxyomeprazole to Omeprazole
NCT04425902 (171) [back to overview]Ratio of Cmax of 36-hydroxymontelukast to Montelukast
NCT04425902 (171) [back to overview]Ratio of Cmax of 1-hydroxymidazolam to Midazolam
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of Alpha-hydroxymetoprolol to Metoprolol
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of 5-hydroxyomeprazole to Omeprazole
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of 36-hydroxymontelukast to Montelukast
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of 1-hydroxymidazolam to Midazolam
NCT04425902 (171) [back to overview]Maximum Observed Plasma Concentration (Cmax) for Caffeine
NCT04425902 (171) [back to overview]Cmax for Pravastatin
NCT04425902 (171) [back to overview]Cmax for Omeprazole
NCT04425902 (171) [back to overview]Cmax for Montelukast
NCT04425902 (171) [back to overview]Cmax for Midazolam
NCT04425902 (171) [back to overview]Cmax for Metoprolol
NCT04425902 (171) [back to overview]Cmax for Flurbiprofen
NCT04425902 (171) [back to overview]Cmax for Digoxin
NCT04425902 (171) [back to overview]Cmax for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]Cmax for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]Cmax for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]Cmax for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]AUC(0-t) for Pravastatin
NCT04425902 (171) [back to overview]AUC(0-t) for Omeprazole
NCT04425902 (171) [back to overview]AUC(0-t) for Montelukast
NCT04425902 (171) [back to overview]AUC(0-t) for Midazolam
NCT04425902 (171) [back to overview]AUC(0-t) for Metoprolol
NCT04425902 (171) [back to overview]AUC(0-t) for Flurbiprofen
NCT04425902 (171) [back to overview]AUC(0-t) for Digoxin
NCT04425902 (171) [back to overview]AUC(0-t) for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]AUC(0-t) for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]AUC(0-t) for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]AUC(0-t) for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]AUC(0-infinity) for Pravastatin
NCT04425902 (171) [back to overview]AUC(0-infinity) for Omeprazole
NCT04425902 (171) [back to overview]AUC(0-infinity) for Montelukast
NCT04425902 (171) [back to overview]AUC(0-infinity) for Midazolam
NCT04425902 (171) [back to overview]AUC(0-infinity) for Metoprolol
NCT04425902 (171) [back to overview]AUC(0-infinity) for Flurbiprofen
NCT04425902 (171) [back to overview]AUC(0-infinity) for Digoxin
NCT04425902 (171) [back to overview]AUC(0-infinity) for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]AUC(0-infinity) for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]AUC(0-infinity) for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]AUC(0-infinity) for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]AUC From Time Zero Extrapolated to Infinity (AUC[0-infinity]) for Caffeine
NCT04425902 (171) [back to overview]Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Time t (AUC[0-t]) for Caffeine
NCT04425902 (171) [back to overview]Apparent Terminal Phase Half-life (t1/2) for Caffeine
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in SBP and DBP
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment B: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Erythrocytes
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Hematocrit
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Hemoglobin
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Oral Temperature
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Pulse Rate
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Respiratory Rate
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of SBP and DBP
NCT04425902 (171) [back to overview]Treatment B: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in SBP and DBP
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment C: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Erythrocytes
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Hematocrit
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Respiratory Rate
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Hemoglobin
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Oral Temperature
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Pulse Rate
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Respiratory Rate
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of SBP and DBP
NCT04425902 (171) [back to overview]Treatment C: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Erythrocytes
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Hematocrit
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Hemoglobin
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Oral Temperature
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Pulse Rate
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Respiratory Rate
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in SBP and DBP
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Erythrocytes
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Gamma-glutamyl Transferase
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Amylase, Lipase
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Hematocrit
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Hemoglobin
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Oral Temperature
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Pulse Rate
NCT04679948 (8) [back to overview]Maximum Measured Concentration of the S-warfarin in Plasma (Cmax, S-warfarin)
NCT04679948 (8) [back to overview]Maximum Measured Concentration of the Caffeine in Plasma (Cmax, Caffeine)
NCT04679948 (8) [back to overview]Maximum Measured Concentration of Omeprazole in Plasma (Cmax, Omeprazole)
NCT04679948 (8) [back to overview]Maximum Measured Concentration of Midazolam in Plasma (Cmax, Midazolam)
NCT04679948 (8) [back to overview]Area Under the Concentration-time Curve of S-warfarin in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, S-warfarin)
NCT04679948 (8) [back to overview]Area Under the Concentration-time Curve of Omeprazole in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Omeprazole)
NCT04679948 (8) [back to overview]Area Under the Concentration-time Curve of Midazolam in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Midazolam)
NCT04679948 (8) [back to overview]Area Under the Concentration-time Curve of Caffeine in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Caffeine)
NCT04766996 (2) [back to overview]Nebraska Interprofessional Education Attitude Scale (NIPEAS) Score for Professional Staff Arm
NCT04766996 (2) [back to overview]Total Post-operative Opioid Requirements With Non-opioid Drug Regimen
NCT05319899 (3) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT05319899 (3) [back to overview]Maximum Measured Plasma Concentration (Cmax) of Total Mo
NCT05319899 (3) [back to overview]Area Under the Plasma Concentration Versus Time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Total Molybdenum (Mo)
NCT05319912 (3) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT05319912 (3) [back to overview]Maximum Measured Plasma Concentration (Cmax) of Total Mo
NCT05319912 (3) [back to overview]Area Under the Plasma Concentration Versus Time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Total Molybdenum (Mo)
NCT05342532 (3) [back to overview]Number of Participants Completing at Least 90% of All Prescribed Medications
NCT05342532 (3) [back to overview]Number of Participants With Protocol Specific Adverse Events
NCT05342532 (3) [back to overview]Number of Participant With Eradication of Disease

Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)

GGT ULN was 49 international units (IU)/liter (L) for females and 61 IU/L for males, AST ULN was 37 IU/L for females and 39 IU/L for males, and ALT ULN was 43 IU/L for females and 45 IU/L for males. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
GGTASTALT
Celecoxib26813
Oral Diclofenac Plus Omeprazole861227

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Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin

A clinically significant decrease from baseline was defined as a fall in hematocrit > = 10 percentage points and/or hemoglobin > = 2 g/dL. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib45
Oral Diclofenac Plus Omeprazole123

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Number of Subjects With CSULGIEs by History of GD Ulceration

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
History of GD Ulceration (n=395, 400)No History of GD Ulceration (n=1843, 1846)
Celecoxib713
Oral Diclofenac Plus Omeprazole1368

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Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

,
InterventionIU/L (Least Squares Mean)
GGTASTALT
Celecoxib-2.689-0.901-1.151
Oral Diclofenac Plus Omeprazole7.4551.4905.213

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Change From Baseline in Ferretin to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionug/dL (Least Squares Mean)
Celecoxib-3.396
Oral Diclofenac Plus Omeprazole-1.990

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Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib20
Oral Diclofenac Plus Omeprazole81

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Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)

CSULGIE=any of the following: GD hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib25
Oral Diclofenac Plus Omeprazole92

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Number of Subjects With Moderate to Severe Abdominal Symptoms

"Abdominal symptoms were defined by the Medical Dictionary for Regulatory Activities MedDRA System Organ Class (SOC) 'Gastrointestinal Disorders' and keeping high level group term (HLGT) equal to Gastrointestinal Signs and Symptoms." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib132
Oral Diclofenac Plus Omeprazole162

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Number of Subjects With SUs

Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib5
Oral Diclofenac Plus Omeprazole11

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Number of Subjects Withdrawn Due to GI Adverse Events (AEs)

"GI AEs were defined using MedDRA SOC Gastrointestinal Disorders but excluding the following HLGTs: Benign Neoplasms Gastrointestinal; Dental and Gingival Conditions; Oral Soft Tissue Conditions; Salivary Gland Conditions; and Tongue Conditions." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib114
Oral Diclofenac Plus Omeprazole167

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Change From Baseline in C-Reactive Protein to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmg/dL (Least Squares Mean)
Celecoxib0.058
Oral Diclofenac Plus Omeprazole0.073

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Change From Baseline in Hematocrit at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionpercent (Least Squares Mean)
Celecoxib-0.306
Oral Diclofenac Plus Omeprazole-1.425

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Change From Baseline in Hemoglobin at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventiongrams (g)/deciliter (dL) (Least Squares Mean)
Celecoxib-0.017
Oral Diclofenac Plus Omeprazole-0.423

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Change From Baseline in Iron Binding Capacity to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmicrogram (ug)/dL (Least Squares Mean)
Celecoxib2.517
Oral Diclofenac Plus Omeprazole1.952

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Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)

"Subjects rated response to question: Considering all the ways the osteoarthritis or rheumatoid arthritis affects you, how are you doing today? using a 1 to 5 grading scale where 1=very good and 5=very poor." (NCT00141102)
Timeframe: Month 6/Early Termination (ET)

Interventionscores on a scale (Least Squares Mean)
Celecoxib0.754
Oral Diclofenac Plus Omeprazole0.773

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Number of Subjects Alive at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib2018
Oral Diclofenac Plus Omeprazole2023

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Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib82
Oral Diclofenac Plus Omeprazole79

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Disease-free Survival

Estimate disease-free survival (DFS) (time from surgery to death or clinically apparent, biopsy confirmed recurrent or progressive disease after the completion of initial therapy, assessed up to 3 years; margins of resection positive for tumor will not be considered disease recurrence). (NCT00210470)
Timeframe: Time from surgery to death or clinically apparent, biopsy confirmed recurrent or progressive disease after the completion of initial therapy, assessed up to 3 years; margins of resection positive for tumor will not be considered disease recurrence

InterventionDFS Probability (Number)
1-year disease free survival probability2-year disease free survival probability3-year disease free survival probability
IRX-2 Regimen0.7210.6410.620

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Number of Participants With High Lymphocyte Infiltration (LI) According to the Visual Analog Scale (VAS)

"Immunologic response features were extracted and quantified using a VAS of 0-100 mm to provide for a more continuous variable than the 0-4+ scale that is often used to assess histological responses. The scoring was such that 100 represented the maximum for any sample and 0 represented the lack of any parameter of interest.~See publication of Berinstein, et al., 2012 for complete details." (NCT00210470)
Timeframe: On approximately Day 21 (last day of treatment) prior to undergoing post-treatment surgery

Interventionparticipants with high LI (>34 mm) VAS (Number)
IRX-2 Regimen18

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Relationship Between Overall Survival (OS) and Immune Competence (Lymphocyte Infiltration, LI) in Participants With High LI and Low LI

"After participants completed the IRX-2 regimen and the tumor resection was performed, tumor pathology was evaluated from tissue specimens obtained at tumor resection. Formalin-fixed, paraffin-embedded blocks, or unstained slides from the primary tumor were submitted to an independent pathology laboratory for hematoxylin and eosin staining, and evaluation of lymphocyte infiltration (LI). Participants were grouped into a low LI and high LI group based on the change in lymphocyte infiltration from the pretreatment tumor biopsy to the post-treatment tumor surgical resection. 5-year overall survival probabilities were then estimated (Kaplan-Meier) between the low LI and high LI groups" (NCT00210470)
Timeframe: At time of surgery, after treatment with IRX-2 Regimen, assessed up to 5 years

Intervention5-Year OS Probability (Number)
High Lymphocyte Infiltration (LI)0.80
Low Lymphocyte Infiltration0.50

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Overall Survival

Estimate overall survival (OS) in patients receiving the IRX-2 regimen. IRX-2 is currently being studied in an on-going Phase 2b clinical trial in patients with newly diagnosed Stage II, III, and IVA squamous cell carcinoma of the oral cavity (INSPIRE) (NCT00210470)
Timeframe: Time from surgery to death or confirmed recurrent or progressive disease, assessed up to 3 years

Interventionpercentage of subjects (Number)
First Year (%)Second Year (%)Third Year (%)
IRX-2 Regimen927369

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Patient Tolerance of Surgery and Post-operative Adjuvant Therapy;

Patient Tolerance of Surgery and Post-operative Adjuvant Therapy as measured by median days spent in the hospital, intensive care unit, and step down unit. (NCT00210470)
Timeframe: Following surgery and post-operative therapy (up to 39 days post surgery)

Interventiondays (Median)
Median Days in hospitalMedian Days in intensive care unitMedian Days in step-down unit
IRX-2 Regimen8.50.50.5

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Immune Competence as Measured by Skin Test Reactivity

To assess measures of immune competence following administration of the IRX-2 regimen, including skin test reactivity. (NCT00210470)
Timeframe: At approx. 21 days, prior to surgery

InterventionParticipants (Count of Participants)
Positive at both Baseline and at Day 21 (%)Negative at both Baseline and Day 21 (%)Positive at Baseline and Negative Day 21 (%)Negative at Baseline and Positive at Day 21Induration at Day 21
IRX-2 Regimen126623

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Number of Participants With Adverse Events and Serious Adverse Events

The frequency of all Adverse Events (greater than 5%) is reported. All Serious Adverse Events were described. (NCT00210470)
Timeframe: Enrollment through 30 days post-surgery

InterventionParticipants (Count of Participants)
Adverse Event: Injection Site PainAdverse Event: HeadacheAdverse Event: NauseaAdverse Event: ConstipationAdverse Event: DizzinessAdverse Event: FatigueAdverse Event: Pneumonia AspirationAdverse Event: AnaemiaAdverse Event: Injection Site DiscomfortAdverse Event: MyalgiaAdverse Event: ContusionAdverse Event: Dry MouthAdverse Event: VomitingAdditional AE Categories w lower frequencySerious Adverse Events
IRX-2 Regimen686443333222247

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Clinical and Histological Tumor Responses

Number of participants with the specified percent change in size of target lesion is presented (NCT00210470)
Timeframe: On approximately Day 21 (last day of treatment) prior to undergoing post-treatment surgery

InterventionParticipants (Count of Participants)
-20% to < -10%-10% to < 0%0% to < 10%10% to < 20%20% to < 30%>= 30%
IRX-2 Regimen479102

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Maximal Concentration of Omerazole

Maximal concentration of immediate-release vs. delayed-release omeprazole (NCT00492622)
Timeframe: 10, 20, 30, 45, 60, 90, 120, 150, 180, 210, 240 and 300 min after the study drug was ingested on day 7 of treatment

Interventionng/mL plasma (Mean)
All Study Participants Immediate Release Arm1979
All Study Subjects Delayed Release Arm1625

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Area Under the Curve for Omeprazole Plasma Concentration

The area under the curve for omeprazole concentration-time curve for immediate release and delayed release omeprazole. (NCT00492622)
Timeframe: 0 to 5 hrs after the study drug was ingested on treatment day 7

Interventionmg*h/mL (Mean)
All Study Participants Immediate Release Arm3842
All Study Subjects Delayed Release Arm3745

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Time to Maximal Omeprazole Concentration (Tmax)

Time to max concentration for Immediate release vs. Delayed release omeprazole (NCT00492622)
Timeframe: 10, 20, 30, 45, 60, 90, 120, 150, 180, 210, 240 and 300 min after the study drug was ingested on day 7 of treatment

Interventionminutes (Mean)
All Study Participants Immediate Release Arm32
All Study Subjects Delayed Release Arm97

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Number of Participants With Upper Endoscopy Indicated Due to Complaints

Endoscopic visualization of presence or absence of anastomotic ulcers if upper endoscopy indicated due to patient complaints - based upon severity of complaints (NCT00557349)
Timeframe: during first 14 weeks after surgery

Interventionparticipants (Number)
Omeprazole1
Famotidine13

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Number of Participants With Complaints, Specifically About Pain, Vomiting, Dyspepsia, and/or Dysphagia.

(NCT00557349)
Timeframe: during first 14 weeks after surgery

Interventionparticipants (Number)
Omeprazole17
Famotidine13

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Percentage of Stools Categorized as Per Consistency

Stool consistency was categorized as hard, formed/normal, soft and watery. Percentage of stools of a specific consistency for each patient was calculated as: (total number of stools of specific consistency during the completed days of the inpatient period/ total number of stools during the completed days of the inpatient period)*100. Mean percentage of stool categorized as per consistency for total patients was summarized. (NCT00559364)
Timeframe: Day 1 up to Day 4 or Day 5 in inpatient period of treatment phase

,
Interventionpercentage of stools (Mean)
Hard stoolsFormed/normal stoolsSoft stoolsWatery stools
Placebo0.6737.2355.485.80
Viokase®5.0845.8647.801.26

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Mean Daily Number of Stools

Mean daily number of stools of each patient was calculated from frequency of stools by the patient per day. Mean daily number of stools during the collection period (Day 1 to Day 4 or Day 5 in inpatient period of treatment phase) for total patients was summarized. (NCT00559364)
Timeframe: Day 1 up to Day 4 or Day 5 in inpatient period of treatment phase

Interventionstools per day (Mean)
Viokase®1.93
Placebo2.33

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Percent Coefficient of Fat Absorption (CFA)

Percent CFA was calculated as ([fat intake - fat excretion]/fat intake)*100, determined in the stools which was collected from Day 1 to Day 4 or Day 5 during the inpatient period of treatment phase. Mean percent (%) CFA was calculated for Day 1 to Day 4 or Day 5 in inpatient period of treatment phase. (NCT00559364)
Timeframe: Day 1 up to Day 4 or Day 5 in inpatient period of treatment phase

Interventionpercent CFA (Mean)
Viokase®85.52
Placebo58.02

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Change in Bone Resorption From Baseline to 1 Month

urine n-telopeptide (normalized to creatinine levels) (NCT00582972)
Timeframe: change in bone resorption from baseline to 1 month

Interventionmcg/mmol creatinine (Mean)
Experimental1.9

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Change in Intestinal Calcium Absorption From Baseline to One Month

percent calcium absorption (NCT00582972)
Timeframe: change in calcium absorption from baseline to 1 month

Interventionpercent calcium absorption (Mean)
Experimental5

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"Number of Participants With Healing of Reflux Esophagitis (RE) Who Were Graded O at Week 8 Out of Patients Who Were Graded A, B, C or D at Baseline According to Los Angeles Classification."

Los Angeles classification consists of 5 grades (Grade O, Grade A, Grade B, Grade C, Grade D). The subjects who were definitely diagnosed to have RE classified into LA classification Grade A, B, C or D based on the EGD on Visit 1 were randomised. A subject classified into LA classification Grade O was considered no reflux esophagitis. The definitions of each grade are: Grade A (Mucosal break < 5 mm in length), Grade B (Mucosal break > 5mm), Grade C (Mucosal break continuous between > 2 mucosal folds) and Grade D (Mucosal break >75% of esophageal circumference). (NCT00633932)
Timeframe: 8 weeks

Interventionparticipants (Number)
Experimental: Esomeprazole 40mg171
Experimental: Esomeprazole 20mg165
Comparator: Omeprazole 20mg166

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"Number of Participants With Healing of Reflux Esophagitis (RE) Who Were Graded O at Week 4 Out of Patients Who Were Graded A, B, C or D at Baseline According to Los Angeles Classification"

Los Angeles classification consists of 5 grades (Grade O, Grade A, Grade B, Grade C and Grade D). The subjects who were definitely diagnosed to have RE classified into LA classification Grade A, B, C or D based on the EGD on Visit 1 were randomised. A subject classified into LA classification Grade O was considered no reflux esophagitis. The definitions of each grade are: Grade A (Mucosal break < 5 mm in length), Grade B (Mucosal break > 5mm), Grade C (Mucosal break continuous between > 2 mucosal folds) and Grade D (Mucosal break >75% of esophageal circumference). (NCT00633932)
Timeframe: 4 weeks

Interventionparticipants (Number)
Experimental: Esomeprazole 40mg141
Experimental: Esomeprazole 20mg147
Comparator: Omeprazole 20mg143

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Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification up to 12 Weeks After Treatment

Los Angels classification consists of 5 grades (Grade O, Grade A, Grade B, Grade C and Grade D). A patient classfied into Grade O was considered no reflux esophagitis. The participants who had a healing of reflux esophagitis with Grade O at Visit 1 were randomised. Number of participants who did not have Grades A-D up to 12 weeks after treatment was evaluated. (NCT00634114)
Timeframe: Up to 12 weeks

InterventionParticipants (Number)
Experimental: Esomeprazole 20 mg179
Experimental: Esomeprazole 10 mg172
Comparator: Omeprazole 10 mg163

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Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification Throughout the Treatment Period.

Los Angels classification consists of 5 grades (Grade O, Grade A, Grade B, Grade C and Grade D). A patient classfied into Grade O was considered no reflux esophagitis. The participants who had a healing of reflux esophagitis with Grade O at Visit 1 were randomised. Number of participants who did not have Grades A-D throughout the treatment period was evaluated. (NCT00634114)
Timeframe: Up to 24 weeks

InterventionParticipants (Number)
Experimental: Esomeprazole 20 mg174
Experimental: Esomeprazole 10 mg166
Comparator: Omeprazole 10 mg156

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Absence of Recurrence of Reflux Esophagitis According to Los Angeles Classification up to 4 Weeks After Treatment

Los Angels classification consists of 5 grades (Grade O, Grade A, Grade B, Grade C and Grade D). A patient classfied into Grade O was considered no reflux esophagitis. The participants who had a healing of reflux esophagitis with Grade O at Visit 1 were randomised. Number of participants who did not have Grades A-D up to 4 weeks after treatment was evaluated. (NCT00634114)
Timeframe: up to 4 weeks

InterventionParticipants (Number)
Experimental: Esomeprazole 20 mg184
Experimental: Esomeprazole 10 mg180
Comparator: Omeprazole 10 mg171

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Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Deaths and Discontinuations

An AE is defined as any new untoward medical occurrence or worsening of a pre-existing medical condition in a patient or clinical investigation subject administered an investigational (medicinal) product and that does not necessarily have a causal relationship with this treatment. An SAE is any untoward medical occurrence that at any dose results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is an important medical event. (NCT00655746)
Timeframe: At Informed Consent (within 21 days of Day 1) through Study Discharge (Day 7)

,,,
InterventionParticipants (Number)
Number of Participants with ≥1 AEDeathSAEDiscontinuation due to AEs
All Participants4000
Dasatinib (Day 1)3000
Dasatinib + Omeprazole (Day 6)2000
Omeprazole (Days 2-5)2000

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Dasatinib PK Parameter Time of Maximum Observed Plasma Concentration(Tmax)

Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Tmax=time of maximum observed plasma concentration (NCT00655746)
Timeframe: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose

Interventionhours (Median)
Dasatinib (Day 1)0.75
Dasatinib + Omeprazole (Day 6)1.00

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Dasatinib PK Parameter: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC[0-T])

area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUC[0-T])for dasatinib (NCT00655746)
Timeframe: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose

Interventionng∙h/mL (Geometric Mean)
Dasatinib (Day 1)249.46
Dasatinib + Omeprazole (Day 6)137.49

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Dasatinib PK Parameter: Plasma Half-Life (T-HALF)

Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. T-Half=plasma half-life (NCT00655746)
Timeframe: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose

Interventionhours (Mean)
Dasatinib (Day 1)4.00
Dasatinib + Omeprazole (Day 6)4.29

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Dasatinib PK Parameters: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF])

Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. AUC(INF)=area under the plasma concentration-time curve from time zero extrapolated to infinite time (NCT00655746)
Timeframe: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose

Interventionng∙h/mL (Geometric Mean)
Dasatinib (Day 1)265.40
Dasatinib + Omeprazole (Day 6)152.84

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Dasatinib Pharmacokinetic (PK) Parameter: Maximum Observed Plasma Concentration (Cmax)

Pharmacokinetics is a branch of pharmacology concerned with the rate at which drugs are absorbed, distributed, metabolized, and eliminated by the body. Cmax=maximum observed plasma concentration of dasatinib (NCT00655746)
Timeframe: Day 1 and Day 6 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours post dose

Interventionng/mL (Geometric Mean)
Dasatinib (Day 1)65.58
Dasatinib + Omeprazole (Day 6)38.64

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Participants With Side Effects From Study Treatment

Side effects profile (NCT00664209)
Timeframe: 2 months

Interventionparticipants (Number)
Active0

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Change in Methacholine Sensitivity

"Concentration of methacholine (mg/ml) at which participants forced expired volume in 1 sec (FEV1) is reduced by 20% (the provocation concentration of methacholine causing a 20% fall in FEV1-PC20).~To measure if there is a significant difference in PC20 recorded at baseline to that recorded following 8 weeks treatment with omeprazole and ranitidine" (NCT00668317)
Timeframe: baseline and 8 weeks

Interventionmg/ml (Mean)
Omeprazole and Ranitidine0.598

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H. Pylori Eradication and Presence or Past History of Peptic Ulcers

Eradication rates in the subset of patients with peptic ulcer (current or past history) at baseline are reported based on the per protocol population. Eradication must be confirmed at week 6 and week 10 by a negative Urea Breath Test conducted within the allocated windows. (NCT00669955)
Timeframe: Week 6 and week 10 follow-up visits

InterventionParticipants (Number)
Quadruple Therapy (OBMT) 10 Days18
Triple Therapy (OAC) 7 Days15

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Helicobacter Pylori Eradication Confirmed by Urea Breath Test

H. pylori Eradication defined as a negative C13-UBT (urea breath test) result at both Week 6 and Week 10 follow-up visits. (NCT00669955)
Timeframe: Week 6 and week 10 follow-up visits

InterventionParticipants (Number)
Quadruple Therapy (OBMT) 10 Days166
Triple Therapy (OAC) 7 Days112

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Metronidazole Resistance

Eradication rates in subset of patients infected with a bacterial strain confirmed as resistant to metronidazole at baseline. Resistance to metronidazole defined as Minimum Inhibitory Concentration (MIC) above 8 ug/ml (NCT00669955)
Timeframe: Measured at baseline

Interventionparticipants (Number)
Quadruple Therapy (OBMT) 10 Days38
Triple Therapy (OAC) 7 Days28

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Number of Patients Experiencing Treatment Emergent Adverse Events.

"A treatment-emergent adverse event is defined as an event not present prior to exposure to the study medication or any event already present that worsens in either intensity or frequency following exposure to study medication up to 30 days after study discontinuation.~All safety analysis based on the safety population." (NCT00669955)
Timeframe: at the end of treatment (day 8-14), week 6 and wek 10 follow-up visits.

InterventionParticipants (Number)
Quadruple Therapy (OBMT) 10 Days101
Triple Therapy (OAC) 7 Days112

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Number of Patients With Bismuth Plasma Concentrations Above the Toxic Level

Tolerability of OBMT with respect to plasma bismuth concentrations: number of patients with bismuth concentrations above the toxic level (50 ug per liter) (NCT00669955)
Timeframe: Baseline (both arms), end of treatment (Day 11-14) and end of study (Day 70) OBMT arm only

Interventionparticipants (Number)
Quadruple Therapy (OBMT) 10 Days0

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Clarithromycin Resistance

Eradication rates in subset of patients infected with a bacterial strain confirmed as resistant to clarithromycin at baseline. Resistance to clarithromycin defined as Minimum Inhibitory Concentration (MIC) of 1 ug/ml and above (NCT00669955)
Timeframe: Measured at baseline

Interventionparticipants (Number)
Quadruple Therapy (OBMT) 10 Days30
Triple Therapy (OAC) 7 Days2

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Overall Compliance to Study Medications

Overall compliance: number of capsules dispensed - number of capsules returned/Number of prescribed capsules X 100. Percentages based on safety population (NCT00669955)
Timeframe: At the end of the treatment phase (days 8-14)

Interventionparticipants (Mean)
Quadruple Therapy (OBMT) 10 Days97.58
Triple Therapy (OAC) 7 Days97.47

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Change From Baseline in Median 24-hour Intragastric pH on the 7th Day of Drug Administration

The change from Baseline in median pH was calculated as: median pH on Day 7 minus median pH at Baseline. PH measures how acidic or basic a substance is. The pH scale ranges from 0 to 14. A pH of 7 is neutral. A pH less than 7 is acidic. A pH greater than 7 is basic. (NCT00674115)
Timeframe: Baseline and 7 days

,
InterventionpH scale (Median)
Day 7 ScoreChange from Baseline in PH
Prilosec4.1602.900
Zegerid3.2502.180

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Percent of Subjects Overall Who Healed, Improved, or Stayed the Same or Worsened After 8 Weeks of Treatment

"After 8 weeks of treatment a follow-up esophagogastroduodenoscopy (EGD) was performed by an endoscopist blinded to the study and subject allocation. The evaluation results were grouped as follows:~LA C esophagitis at baseline: healed = no erosions in the esophagus; improved= LA grades A or B; Same or worse = C or D at follow-up LA D esophagitis at baseline: healed = no erosions in the esophagus; improved=LA grades A, B, or C; Same=LA grade D at follow-up." (NCT00693225)
Timeframe: 8 weeks

,
Interventionpercentage of patients (Number)
HealedImprovedSame or worse
Omeprazole/Sodium Bicarbonate AM Dose83152
Omeprazole/Sodium Bicarbonate PM Dose81145

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Percent of Subjects With Moderate Esophagitis (LA Grade C) Who Healed, Improved, or Stayed the Same or Worsened After 8 Weeks of Treatment

"After 8 weeks of treatment a follow-up esophagogastroduodenoscopy (EGD) was performed by an endoscopist blinded to the study and subject allocation. The evaluation results were grouped as follows:~LA C esophagitis at baseline: healed = no erosions in the esophagus; improved= LA grades A or B; Same or worse = C or D at follow-up LA D esophagitis at baseline: healed = no erosions in the esophagus; improved=LA grades A, B, or C; Same=LA grade D at follow-up." (NCT00693225)
Timeframe: 8 weeks

,
Interventionpercentage of participants (Number)
HealedImprovedSame or worse
Omeprazole/Sodium Bicarbonate AM Dose88120
Omeprazole/Sodium Bicarbonate PM Dose79147

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Percent of Subjects With Severe Esophagitis (LA Grade D) Who Healed, Improved, or Stayed the Same After 8 Weeks of Treatment

"After 8 weeks of treatment a follow-up esophagogastroduodenoscopy (EGD) was performed by an endoscopist blinded to the study and subject allocation. The evaluation results were grouped as follows:~LA C esophagitis at baseline: healed = no erosions in the esophagus; improved= LA grades A or B; Same or worse = C or D at follow-up LA D esophagitis at baseline: healed = no erosions in the esophagus; improved=LA grades A, B, or C; Same=LA grade D at follow-up." (NCT00693225)
Timeframe: 8 weeks

,
Interventionpercentage of participants (Number)
HealedImprovedSame
Omeprazole/Sodium Bicarbonate AM Dose75196
Omeprazole/Sodium Bicarbonate PM Dose86140

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Plasma AUC Ratio of Day 1 and Day 8

"Assessment of the drug-drug interactions of Proellex® (CDB-4124) with cytochrome P450 isoenzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 in healthy female subjects administered 50 mg Proellex® once daily (QD). The Day 8 AUC was compared to the Day 1 AUC to determine inhibition.~For CYP1A2 the plasma paraxanthine/caffeine MR ratio (metabolic ratio) was used. For CYP2D6 the MR ratio of dextromethorphan/dextrorphan was used." (NCT00741468)
Timeframe: 8 days

InterventionRatio of geometric means Day 8 to Day 1 (Mean)
CYP1A21.093
CYP2C91.029
CYP2C191.104
CYP2D61.914
CYP3A42.245

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Change From Baseline in Median 24-hour Intragastric pH on the 7th Day of Drug Administration

The change from Baseline in median pH was calculated as: median pH on Day 7 minus median pH at Baseline. The pH scale ranges from 0 to 14. A pH of 7 is neutral. A pH less than 7 is acidic. A pH greater than 7 is basic. (NCT00765206)
Timeframe: Baseline and 7 days

,
InterventionpH scale (Median)
Day 7 ScoreChange from Baseline in pH
Prilosec3.9802.550
Zegerid4.5753.165

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Rebleeding After 3 Days

Rebleeding after 3 days was assessed by checking the patients from day 3 to discharge and bleeding event or regular follow-up after discharge to week 6. (NCT00838682)
Timeframe: 6wk

Interventionparticipants (Number)
Rabeprazole Sodium1
Omeprazole0

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Mean Units of Blood Transfusion

In order to compare the total amount of blood transfusion, mean units of blood transfusion was used. (NCT00838682)
Timeframe: day 3

InterventionMean units of blood transfusion (Mean)
Rabeprazole Sodium1.3
Omeprazole1.4

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Death

(NCT00838682)
Timeframe: 6wk

Interventionparticipants (Number)
Rabeprazole Sodium1
Omeprazole0

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Duration of Hospital Stay

(NCT00838682)
Timeframe: 6wk

Interventiondays (Mean)
Rabeprazole Sodium8.0
Omeprazole6.7

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Surgery

"This sencodary endpoint surgery is the operation for bleeding control of peptic ulcer bleeding such as gastric or duodenal primary closure, and subtotal gastrectomy with/without vagotomy." (NCT00838682)
Timeframe: 6wk

Interventionparticipants (Number)
Rabeprazole Sodium2
Omeprazole0

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Rebleeding Within 3 Days

(NCT00838682)
Timeframe: day 3

Interventionparticipants (Number)
Rabeprazole Sodium2
Omeprazole1

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Mean Percent Time That Gastric pH > 4.0 on Day 5

for 24 hours starting Day 5 for each period (NCT00903448)
Timeframe: 24 hours

Interventionpercent time gastric pH exceeds 4.0 (Mean)
Prilosec OTC Then Prevacid Then Prevacid36.8
Prevacid Then Prilosec OTC Then Prilosec OTC45.7

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Pharmacodynamic Parameter Platelet Reactivity Index (PRI) From Vasodilator-stimulated Phosphoprotein (VASP) Phosphorylation State (Flow Cytometry).

PRI is the platelet reactivity index from VASP phosphorylation state (flow cytometry). (NCT00942175)
Timeframe: 24-hour post Day 9 dose in each period.

Interventionpercent inhibition (Mean)
PPI Group 1: Regimen A42.3
PPI Group 1: Regimen B46.4
PPI Group 2: Regimen A41.3
PPI Group 2: Regimen C43.0
PPI Group 3: Regimen A47.9
PPI Group 3: Regimen D59.1
PPI Group 4: Regimen A46.5
PPI Group 4: Regimen E58.0

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Pharmacokinetic Parameter Area Under the Plasma Concentration Versus Time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration (AUC[0-tlqc]) of Clopidogrel's Active Metabolite.

Area under the plasma concentration versus time curve (AUC(0-tlqc)) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC[0-tlqc]). (NCT00942175)
Timeframe: Day 9 of each period

Interventionng*hr/ML (Mean)
PPI Group 1: Regimen A41.69
PPI Group 1: Regimen B36.42
PPI Group 2: Regimen A41.25
PPI Group 2: Regimen C37.75
PPI Group 3: Regimen A37.78
PPI Group 3: Regimen D26.28
PPI Group 4: Regimen A42.35
PPI Group 4: Regimen E31.23

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Pharmacokinetic Parameter Peak Plasma Concentration (Cmax) of Clopidogrel's Active Metabolite.

Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. (NCT00942175)
Timeframe: Day 9 of each period

Interventionng/mL (Mean)
PPI Group 1: Regimen A39.14
PPI Group 1: Regimen B30.01
PPI Group 2: Regimen A38.85
PPI Group 2: Regimen C29.33
PPI Group 3: Regimen A38.25
PPI Group 3: Regimen D22.55
PPI Group 4: Regimen A40.98
PPI Group 4: Regimen E24.69

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Pharmacodynamic Parameter Maximum Platelet Aggregation (MPA) From Aggregometry (Turbidimetric) With 5 µM Adenosine Diphosphate.

Maximum platelet aggregation (MPA) from aggregometry (turbidimetric) with 5 µM adenosine diphosphate. (NCT00942175)
Timeframe: 24-hour post Day 9 dose in each period.

Interventionpercentage of MPA (Mean)
PPI Group 1: Regimen A28.1
PPI Group 1: Regimen B30.8
PPI Group 2: Regimen A34.6
PPI Group 2: Regimen C36.2
PPI Group 3: Regimen A34.2
PPI Group 3: Regimen D42.5
PPI Group 4: Regimen A29.3
PPI Group 4: Regimen E38.2

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Pharmacodynamic Parameter MPA From Aggregometry (Turbidimetric) With 20 µM Adenosine Diphosphate.

MPA from aggregometry (turbidimetric) with 20 µM adenosine diphosphate. (NCT00942175)
Timeframe: 24-hour post Day 9 dose in each period.

Interventionpercentage of MPA (Mean)
PPI Group 1: Regimen A36.7
PPI Group 1: Regimen B41.6
PPI Group 2: Regimen A43.1
PPI Group 2: Regimen C46.3
PPI Group 3: Regimen A43.5
PPI Group 3: Regimen D53.5
PPI Group 4: Regimen A39.3
PPI Group 4: Regimen E47.9

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Plasma Area Under Curve (AUC 0-12 hr ) for Raltegravir

Area Under the Plasma Concentration-Time Curve and peak concentration (NCT01000818)
Timeframe: 12 hours postdose

InterventionµM*hr (Geometric Mean)
400 mg Raltegravir12.36
20 mg Famotidine + 400 mg Raltegravir17.95
20 mg Omeprazole + 400 mg Raltegravir17.12

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Time to Achieve Sustained Advantage Over No Treatment During the First 4 Hours After Dosing

"The earliest time during the first 4 hours after dosing that the median~pH for the treatment is over 1 unit higher than that for the No treatment during the next three 5 minute intervals. (When this condition does not occur, the time to sustained advantage will be imputed as 4 hours.)" (NCT01005719)
Timeframe: Treatment dose to event on Day 1 and Day 7

,
InterventionMinutes (Median)
Day 1 (N=59, N=57)Day 7 (N=59, N=59)
Prevacid®85.0005.000
Zegerid35.00010.000

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The Difference in the Onset of Action Based on Median pH Values Between the Two Active Treatments Compared to No Treatment on Day 1 and Day 7

Median intragastric pH scores were collected at 5 minute intervals after treatment dose. The difference in the onset of action was the earliest 5 minute interval (from start of interval to end of interval) for which each active treatment presented a statistically significantly advantage over No treatment based on median pH values. The earliest 5 minute interval showing the difference in onset of action is reported here. (NCT01005719)
Timeframe: Treatment dose to 4-hr post-dose on Day 1 and Day 7

,,
InterventionpH (Median)
Day 1 (0-5 mins), (N=59, N=57, N=59)Day 7 (0-5 mins), (N=59, N=59, N=59)
No Treatment0.920.82
Prevacid®1.1801.950
Zegerid1.0501.840

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Median Time to Achieve Intragastric pH > = 3.5 for a 10-Minute Period

The time required to achieve an intragastric pH ≥3.5 that is reached for 10 consecutive minutes after drug administration on the 1st and 7th days of dosing. (NCT01005719)
Timeframe: Treatment dose to 4-hr post-dose on Day 1 and Day 7

,,
InterventionMinutes (Median)
Day 1 (N=59, N=57, N=59)Day 7 (N=59, N=59, N=59)
No Treatment240.00240.00
Prevacid®108.86766.667
Zegerid64.86722.667

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Time to Achieve Sustained Intragastric pH > 3.5 at Steady-state on Day 7

The first time to sustain median pH > 3.5 for at least 3 successive 5-minute periods within the first 2 hours after dosing with Zegerid Capsules, and Prevacid Capsules, or No treatment on the 7th day of respective treatments. If this condition was not met for any time point within the first 2 hours following dosing, a score of 120 minutes was imputed. (NCT01005719)
Timeframe: Treatment dose to 2-hours post-dose on Day 7

InterventionMinutes (Median)
Zegerid25.000
Prevacid®65.000
No Treatment100.000

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Achievement of Sustained Difference in Inhibition of Intragastric Acidity Based on Median pH Values Between the Two Active Study Treatments at Steady-state on Day 7

Median intragastric pH scores were collected at 5 minute intervals after treatment dose. The achievement of sustained difference was the earliest time for which a statistically significant difference was observed in the median intragastric pH scores for 3 consecutive 5-minute intervals. The earliest 3 time points for which a statistically significant difference was observed between the median intragastric pH values for the two active treatments for three consecutive 5-minute intervals are shown here. (NCT01005719)
Timeframe: Treatment dose to 4-hr post-dose on Day 7

,
InterventionpH (Median)
10-15 Minutes Post-dose on Day 715-20 Minutes Post-dose on Day 720-25 Minutes Post-dose on Day 7
Prevacid®1.8201.7601.950
Zegerid2.6003.2304.920

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Achievement of Sustained Difference in Inhibition of Intragastric Acidity Based on Median pH Values Between the Two Active Study Treatments at Steady-state on Day 1

Median intragastric pH scores were collected at 5 minute intervals after treatment dose. The achievement of sustained difference was the earliest time for which a statistically significant difference was observed in the median intragastric pH scores for 3 consecutive 5-minute intervals. The earliest 3 time points for which a statistically significant difference was observed between the median intragastric pH values for the two active treatments for three consecutive 5-minute intervals are shown here. (NCT01005719)
Timeframe: Treatment dose to 4-hr post-dose on Day 1

,
InterventionpH (Median)
10-15 Minutes Post-dose on Day 115-20 Minutes Post-dose on Day 120-25 Minutes Post-dose on Day 1
Prevacid®1.0701.0800.990
Zegerid1.3301.4201.590

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Time to Onset of Inhibition of Acid Secretion on Day 1

The onset of inhibition of acid secretion was the first time to sustain median pH >3.5 for each of the twenty-four successive 5-minute periods. If this condition was not met for any time point within the first 4 hours following dosing, a score of 240 minutes was imputed. (NCT01005719)
Timeframe: Treatment dose to onset of event on Day 1

InterventionMinutes (Median)
Zegerid240.00
Prevacid®240.00
No Treatment240.00

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Percentage Time Intragastric pH >4 During the First 4 Hours After Dosing on Day 7

(NCT01005719)
Timeframe: Treatment dose to 4 hours Post-dose on Day 7

InterventionPercentage of time (Median)
Zegerid64.639
Prevacid®44.194
No Treatment6.056

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Percentage of Time Intragastric pH >4 Over the Nocturnal Period on Day 7

(NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 7

InterventionPercentage of Time (Median)
Zegerid9.236
Prevacid®9.685
No Treatment0.028

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Percentage of Time Intragastric pH >4 Over the Nocturnal Period on Day 1

(NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 1

InterventionPercentage of Time (Median)
Zegerid0.681
Prevacid®1.987
No Treatment0.111

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Percentage of Time Intragastric pH >4 During the First 4 Hours on Day 1

(NCT01005719)
Timeframe: Treatment dose to 4-hours post-dose on Day 1

InterventionPercentage of Time (Median)
Zegerid21.500
Prevacid®9.525
No Treatment3.667

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Percentage of Time Intragastric pH >3.5 Over 24-hour Period on Day 7

(NCT01005719)
Timeframe: Treatment dose to 24-hours post-dose on Day 7

InterventionPercentage of Time (Median)
Zegerid51.321
Prevacid®43.990
No Treatment7.927

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Percentage of Time Intragastric is pH >4 Over 24-hour Period on Day 7

(NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 7

InterventionPercentage of time (Median)
Zegerid40.538
Prevacid®36.917
No Treatment4.852

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Number of Participants With Intragastric pH >4 for More Than 50% of the Time on Day 7

"Number of participants maintaining intragastric pH > 4 for at least 12 hrs at~steady-state on Day 7" (NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 7

InterventionParticipants (Number)
Zegerid26
Prevacid®18
No Treatment0

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Number of Participants With Intragastric pH >3.5 for More Than 50% of the Time on Day 7

"Number of participants maintaining intragastric pH > 3.5 for at least 12 hrs at~steady-state on Day 7" (NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 7

InterventionParticipants (Number)
Zegerid30
Prevacid®23
No Treatment0

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Number of Participants Maintaining Intragastric pH > 3.5 for at Least 12 Hours on Day 1

(NCT01005719)
Timeframe: Treatment dose to 24-hr post-dose on Day 1

InterventionParticipants (Number)
Zegerid11
Prevacid®11
No Treatment0

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Median 24-hr Intragastric pH on Day 7

The median intragastric pH values were recorded over a 24-hr period. (NCT01005719)
Timeframe: Treatment dose to 24-hour post-dose on Day 7

InterventionpH (Median)
Zegerid3.600
Prevacid®3.100
No Treatment0.800

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Number of Participants Maintaining Intragastric pH > 4 for at Least 12 Hours on Day 1

(NCT01005719)
Timeframe: Treatment dose to 24-hr post-dose on Day 1

InterventionParticipants (Number)
Zegerid8
Prevacid®5
No Treatment0

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Platelet Function Tests

"Platelet function tests were determined by optical whole blood aggregometry in response to arachidonic acid and adenosine diphosphate.~the results reflects the percent of active platelets." (NCT01061034)
Timeframe: on day 0 as a baseline and on day 7 and 21 of the study.

Interventionpercent (Mean)
day 0day 7day 21
Aspirin Then Aspirin Plus Omeprazole808.558.77

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Aspirin Level in Blood (Area Under the Curve)

"Aspirins pharmacokinetics: aspirin blood level determined by use of high performance liquid chromatography (HPLC) at baseline, 1, 2,4,6,10 and 24 hours after administration of aspirin on day 7 and on day 21.~The area unther the time vs. concentration curve of the reccurent measurments(AUC) reflects bioavailability of aspirin." (NCT01061034)
Timeframe: on day 7,on day 21

Interventionmg*hour/mL (Mean)
aspirin area under the curve on day 7aspirin area under the curve on day 211 hour after admission day 7 (aspirin alone)1 hour after admission day 21 (aspirin+omeprazole)
Aspirin Then Aspirin Plus Omeprazole49.450.78.76.5

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Percent Time With Intragastric pH>4 During the First 4 Hours Following Administration on Day 4 of Treatment

Early effectiveness of treatment is evaluated as the percent time with intragastric pH>4 during the first 4 hours following administration of respective treatments (NCT01077076)
Timeframe: 4 hours after dose on Day 4

InterventionPercentage of Time (Mean)
Zegerid OTC Capsules53.265
Prilosec OTC Tablets46.933
Placebo Capsules17.215

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Change in Inflammation Biomarker Tissue PGE2 Level

Change from baseline in esophageal tissue biopsy prostaglandin E2 (PGE2) level, as determined by enzyme immunoassay (NCT01093755)
Timeframe: 3 months, 6 months

,
Interventionnanograms/gram of tissue (Mean)
Change from baseline at 3 monthsChange from baseline at 6 months
Dexlansoprazole1.351.19
Omeprazole-0.02-0.06

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Change in Esophageal Inflammation Biomarker COX-2 Gene Expression

Change from baseline in esophageal issue biopsy cyclooxygenase-2 (COX-2) gene expression, as determined by Western blot. (NCT01093755)
Timeframe: 3 months, 6 months

,
Intervention% of tubulin (Mean)
Change from baseline at 3 monthsChange from baseline at 6 months
Dexlansoprazole36.8156.54
Omeprazole27.1725.49

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Gastric pH

(NCT01122160)
Timeframe: 1 hour prior to gastric emptying on Day 7 of the given intervention

InterventionpH (Mean)
Experimental0.96
Placebo2.31

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Percentage of Time Esophageal pH< 4

Reported as the the average percentage over 24 hours of total time, upright time, and supine time per day with pH <4 (symptomatic acid state) as evaluated with the Bravo pH monitoring technique. (NCT01129778)
Timeframe: Days 1 and 2

Interventionpercentage of hours (Mean)
Total time pH <4 First DayTotal time pH <4 Second DayUpright time pH <4 First DayUpright time pH <4 Second DaySupine time pH <4 First DaySupine time pH <4 Second Day
Received Zegerid (Ome-NaBic)0.40.60.710.060.05

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Reflux Disease Questionnaire Score on Day 1 After Therapy Completion

The RDQ is a 12 item survey that asks the patient to rate the frequency and severity of GERD symptoms. Each item is scored from 0 to 5 where a score of 0 is equivalent to an asymptomatic state and 5 indicates the worst severity of GERD symptoms. The total RDQ is a sum of all 12 items, and can range from 0 to 60. (NCT01129778)
Timeframe: Day 1 after therapy period completion

InterventionUnits on a scale (Mean)
Received Zegerid (Ome-NaBic)0.5

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Platelet Function as Assessed by the P2Y12 Reactivity Index

P2Y12 reactivity index which will be assessed by flow cytometry determination of vasodilator-stimulated phosphoprotein (VASP). (NCT01170533)
Timeframe: 1 week

InterventionPercentage of platelet reactivity index (Least Squares Mean)
Omeprazole Concomitant56.1
Omeprazole Staggered61.6
Pantoprazole Concomitant56
Pantoprazole Staggered61
Clopidogrel Only (Omeprazole Phase)48.8
Clopidogrel Only (Pantoprazole Phase)61.0

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Parts 1 and 2: Percentage of Participants With ≥1 Adverse Events (AEs)

An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT01275170)
Timeframe: Up to 14 days after the last dose of study drug in Part 2 (up to 11 weeks)

InterventionPercentage of Participants (Number)
Panel A: Mild Renal Impairment28.6
Panel C: Moderate Renal Impairment16.7
Panel E: Severe Renal Impairment16.7
Panel G: ESRD/HD Participants33.3
Healthy Matched Controls (Part 1)0.0
Panel E: Severe Renal Impairment (Part 2)33.3
Panel G: ESRD/HD (Part 2)33.3
Healthy Matched Controls (Part 2)0.0

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Dialysis Clearance (CLD) of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)

The CLD of MK-7655 was determined in ESRD/HD participants for 4.5 hours during HD. The formula for calculating CLD was: CLd = (1-Hct)*QB*[(pre-dialyzer concentration - post-dialyzer concentration) / (pre-dialyzer concentration)] where QB=350 mL/min and Hct=hematocrit. (NCT01275170)
Timeframe: 1, 1.5, 2, 2.5, 3, 3.5, 4, and 4.5 hours postdose

InterventionmL/min (Geometric Mean)
1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3.0 hours postdose3.5 hours postdose4 hours postdose4.5 hours postdose
Panel G: ESRD/HD Period 2 Predialysis172158170166171177204198

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Part 2: Plasma AUC0-∞ of Caffeine as a Probe Substrate of Cytochrome P450 Enzyme (CYP)1A2

Caffeine was selected as a substrate of CYP1A2. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose

InterventionµM*hr (Geometric Mean)
Panel E: Severe Renal Impairment336
Panel F: Healthy Controls to Panel E221
Panel G: ESRD/HD Period 1 Postdialysis190
Panel G: ESRD/HD Period 2 Predialysis200
Panel H: Healthy Controls to Panel G300

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Part 1: Apparent Plasma Half-life (t½) of MK-7655 in Combination With PRIMAXIN®

Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Geometric Mean)
Panel A: Mild Renal Impairment2.63
Panel B: Healthy Controls to Panel A1.75
Panel C: Moderate Renal Impairment4.51
Panel D: Healthy Controls to Panel C2.10
Panel E: Severe Renal Impairment8.65
Panel F: Healthy Controls to Panel E2.00
Panel G: ESRD/HD Period 1 Postdialysis15.6
Panel H: Healthy Controls to Panel G1.79
Panel G: ESRD/HD Period 2 Predialysis10.5

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Part 1: VZpred of Imipenem in Combination With MK-7655

Imipenem is 1 of the 2 constituents of PRIMAXIN®. VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionliters (L) (Geometric Mean)
Panel A: Mild Renal Impairment21.1
Panel B: Healthy Controls to Panel A26.1
Panel C: Moderate Renal Impairment22.3
Panel D: Healthy Controls to Panel C23.4
Panel E: Severe Renal Impairment20.0
Panel F: Healthy Controls to Panel E24.8
Panel G: ESRD/HD Period 1 Postdialysis20.5
Panel H: Healthy Controls to Panel G24.9
Panel G: ESRD/HD Period 2 Predialysis63.3

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Extraction Coefficient of MK-7655 in Participants With End-stage Renal Diseases Requiring Hemodialysis (ESRD/HD)

The extraction coefficient of MK-7655 was determined in ESRD/HD participants for 4.5 hours during HD. The formula for calculating extraction coefficient was: Extraction Coefficient = ABS[100*(post-dialyzer concentration - pre-dialyzer concentration) / pre-dialyzer concentration]. (NCT01275170)
Timeframe: 1, 1.5, 2, 2.5, 3, 3.5, 4, and 4.5 hours postdose

InterventionExtraction coefficient (Geometric Mean)
1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3.0 hours postdose3.5 hours postdose4 hours postdose4.5 hours postdose
Panel G: ESRD/HD Period 2 Predialysis7367737173768784

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Part 1: VZpred of Cilastin in Combination With MK-7655

Cilastin is 1 of the 2 constituents of PRIMAXIN®. VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionliters (L) (Geometric Mean)
Panel A: Mild Renal Impairment19.2
Panel B: Healthy Controls to Panel A23.9
Panel C: Moderate Renal Impairment19.4
Panel D: Healthy Controls to Panel C21.4
Panel E: Severe Renal Impairment16.9
Panel F: Healthy Controls to Panel E21.2
Panel G: ESRD/HD Period 1 Postdialysis15.9
Panel H: Healthy Controls to Panel G21.0
Panel G: ESRD/HD Period 2 Predialysis59.1

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Part 1: Tmax of Imipenem in Combination With MK-7655

Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Median)
Panel A: Mild Renal Impairment0.50
Panel B: Healthy Controls to Panel A0.50
Panel C: Moderate Renal Impairment0.49
Panel D: Healthy Controls to Panel C0.48
Panel E: Severe Renal Impairment0.48
Panel F: Healthy Controls to Panel E0.48
Panel G: ESRD/HD Period 1 Postdialysis0.48
Panel H: Healthy Controls to Panel G0.48
Panel G: ESRD/HD Period 2 Predialysis0.48

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Part 1: Tmax of Cilastin in Combination With MK-7655

Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Median)
Panel A: Mild Renal Impairment0.50
Panel B: Healthy Controls to Panel A0.50
Panel C: Moderate Renal Impairment0.49
Panel D: Healthy Controls to Panel C0.48
Panel E: Severe Renal Impairment0.48
Panel F: Healthy Controls to Panel E0.48
Panel G: ESRD/HD Period 1 Postdialysis0.48
Panel H: Healthy Controls to Panel G0.48
Panel G: ESRD/HD Period 2 Predialysis0.48

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Part 1: Time of Maximum Plasma Concentration (Tmax) of MK-7655 in Combination With PRIMAXIN®

Tmax is the time at which the highest plasma drug concentration was observed. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Median)
Panel A: Mild Renal Impairment0.50
Panel B: Healthy Controls to Panel A0.50
Panel C: Moderate Renal Impairment0.50
Panel D: Healthy Controls to Panel C0.49
Panel E: Severe Renal Impairment0.48
Panel F: Healthy Controls to Panel E0.48
Panel G: ESRD/HD Period 1 Postdialysis0.48
Panel H: Healthy Controls to Panel G0.48
Panel G: ESRD/HD Period 2 Predialysis0.48

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Part 2: Plasma AUC0-∞ of Midazolam as a Probe Substrate of Cytochrome P450 Enzyme (CYP)3A4

Midazolam was selected as a substrate of CYP3A4. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose

InterventionµM*hr (Geometric Mean)
Panel E: Severe Renal Impairment0.130
Panel F: Healthy Controls to Panel E0.121
Panel G: ESRD/HD Period 1 Postdialysis0.0681
Panel G: ESRD/HD Period 2 Predialysis0.0700
Panel H: Healthy Controls to Panel G0.114

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Part 1: Renal Clearance (CLR) of MK-7655 in Urine

CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment69.8
Panel B: Healthy Controls to Panel A118
Panel C: Moderate Renal Impairment38.4
Panel D: Healthy Controls to Panel C110
Panel E: Severe Renal Impairment22.3
Panel F: Healthy Controls to Panel E107
Panel H: Healthy Controls to Panel G110

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Part 1: Predicted Volume of Distribution During the Terminal Phase (VZpred) of MK-7655 in Combination With PRIMAXIN®

VZpred is the predicted volume of distribution during the terminal phase. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionliters (L) (Geometric Mean)
Panel A: Mild Renal Impairment21.4
Panel B: Healthy Controls to Panel A21.6
Panel C: Moderate Renal Impairment22.2
Panel D: Healthy Controls to Panel C21.9
Panel E: Severe Renal Impairment20.1
Panel F: Healthy Controls to Panel E22.4
Panel G: ESRD/HD Period 1 Postdialysis16.2
Panel H: Healthy Controls to Panel G17.0
Panel G: ESRD/HD Period 2 Predialysis55.7

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Part 1: Predicted Clearance (CLpred) of MK-7655 in Combination With PRIMAXIN®

CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment81.3
Panel B: Healthy Controls to Panel A133
Panel C: Moderate Renal Impairment52.1
Panel D: Healthy Controls to Panel C114
Panel E: Severe Renal Impairment25.3
Panel F: Healthy Controls to Panel E123
Panel G: ESRD/HD Period 1 Postdialysis14.4
Panel H: Healthy Controls to Panel G135
Panel G: ESRD/HD Period 2 Predialysis76.6

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Part 1: Concentration at End of Infusion (Ceoi) of MK-7655 in Combination With PRIMAXIN®

Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose

InterventionµM (Geometric Mean)
Panel A: Mild Renal Impairment22.4
Panel B: Healthy Controls to Panel A20.4
Panel C: Moderate Renal Impairment23.5
Panel D: Healthy Controls to Panel C22.5
Panel E: Severe Renal Impairment23.6
Panel F: Healthy Controls to Panel E18.1
Panel G: ESRD/HD Period 1 Postdialysis53.1
Panel H: Healthy Controls to Panel G22.7
Panel G: ESRD/HD Period 2 Predialysis19.3

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Part 1: CLR of Imipenem in Urine

CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment75.0
Panel B: Healthy Controls to Panel A115
Panel C: Moderate Renal Impairment41.1
Panel D: Healthy Controls to Panel C109
Panel E: Severe Renal Impairment17.4
Panel F: Healthy Controls to Panel E104
Panel H: Healthy Controls to Panel G99.1

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Part 1: CLR of Cilastin in Urine

CLR represents renal clearance in urine. Urine was collected for 24 hours postdose. (NCT01275170)
Timeframe: Predose to 24 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment99.4
Panel B: Healthy Controls to Panel A144
Panel C: Moderate Renal Impairment59.6
Panel D: Healthy Controls to Panel C136
Panel E: Severe Renal Impairment24.5
Panel F: Healthy Controls to Panel E140
Panel H: Healthy Controls to Panel G146

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Part 1: CLpred of Imipenem in Combination With MK-7655

Imipenem is 1 of the 2 constituents of PRIMAXIN®. CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment180
Panel B: Healthy Controls to Panel A253
Panel C: Moderate Renal Impairment138
Panel D: Healthy Controls to Panel C211
Panel E: Severe Renal Impairment87.0
Panel F: Healthy Controls to Panel E218
Panel G: ESRD/HD Period 1 Postdialysis62.5
Panel H: Healthy Controls to Panel G194
Panel G: ESRD/HD Period 2 Predialysis195

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Part 1: CLpred of Cilastin in Combination With MK-7655

Cilastin is 1 of the 2 constituents of PRIMAXIN®. CLpred is the predicted apparent total body clearance of drug. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionmL/min (Geometric Mean)
Panel A: Mild Renal Impairment162
Panel B: Healthy Controls to Panel A259
Panel C: Moderate Renal Impairment116
Panel D: Healthy Controls to Panel C217
Panel E: Severe Renal Impairment38.7
Panel F: Healthy Controls to Panel E217
Panel G: ESRD/HD Period 1 Postdialysis15.0
Panel H: Healthy Controls to Panel G206
Panel G: ESRD/HD Period 2 Predialysis56.6

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Part 1: AUC0-inf of Cilastin in Combination With MK-7655

Cilastin is 1 of the 2 constituents of PRIMAXIN®. AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionµM*hr (Geometric Mean)
Panel A: Mild Renal Impairment71.7
Panel B: Healthy Controls to Panel A44.8
Panel C: Moderate Renal Impairment100.0
Panel D: Healthy Controls to Panel C53.6
Panel E: Severe Renal Impairment300
Panel F: Healthy Controls to Panel E53.7
Panel G: ESRD/HD Period 1 Postdialysis777
Panel H: Healthy Controls to Panel G56.5
Panel G: ESRD/HD Period 2 Predialysis205

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Part 1: Ceoi of Imipenem in Combination With MK-7655

Imipenem is 1 of the 2 constituents of PRIMAXIN®. Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose

InterventionµM (Geometric Mean)
Panel A: Mild Renal Impairment40.7
Panel B: Healthy Controls to Panel A35.3
Panel C: Moderate Renal Impairment45.6
Panel D: Healthy Controls to Panel C42.6
Panel E: Severe Renal Impairment46.9
Panel F: Healthy Controls to Panel E35.5
Panel G: ESRD/HD Period 1 Postdialysis103
Panel H: Healthy Controls to Panel G41.8
Panel G: ESRD/HD Period 2 Predialysis35.9

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Part 1: Ceoi of Cilastin in Combination With MK-7655

Cilastin is 1 of the 2 constituents of PRIMAXIN®. Ceoi is the observed plasma drug concentration at the end of IV infusion. (NCT01275170)
Timeframe: At 0.5 hours postdose

InterventionµM (Geometric Mean)
Panel A: Mild Renal Impairment43.4
Panel B: Healthy Controls to Panel A34.8
Panel C: Moderate Renal Impairment48.7
Panel D: Healthy Controls to Panel C42.9
Panel E: Severe Renal Impairment53.3
Panel F: Healthy Controls to Panel E35.8
Panel G: ESRD/HD Period 1 Postdialysis111
Panel H: Healthy Controls to Panel G44.5
Panel G: ESRD/HD Period 2 Predialysis41.7

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Part 1: AUC0-inf of Imipenem in Combination With MK-7655

Imipenem is 1 of the 2 constituents of PRIMAXIN®. AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionµM*hr (Geometric Mean)
Panel A: Mild Renal Impairment77.3
Panel B: Healthy Controls to Panel A55.0
Panel C: Moderate Renal Impairment101
Panel D: Healthy Controls to Panel C66.0
Panel E: Severe Renal Impairment160
Panel F: Healthy Controls to Panel E63.8
Panel G: ESRD/HD Period 1 Postdialysis223
Panel H: Healthy Controls to Panel G71.8
Panel G: ESRD/HD Period 2 Predialysis71.2

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Part 1: Area Under the Plasma Concentration-time Curve From Dosing to Infinity (AUC0-inf) of MK-7655 in Combination With PRIMAXIN®

AUC0-∞ is a measure of the mean (extrapolated) plasma drug concentration after dosing to infinity. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

InterventionµM*hr (Geometric Mean)
Panel A: Mild Renal Impairment73.5
Panel B: Healthy Controls to Panel A45.0
Panel C: Moderate Renal Impairment115
Panel D: Healthy Controls to Panel C52.3
Panel E: Severe Renal Impairment236
Panel F: Healthy Controls to Panel E48.5
Panel G: ESRD/HD Period 1 Postdialysis414
Panel H: Healthy Controls to Panel G44.5
Panel G: ESRD/HD Period 2 Predialysis78.0

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Part 1: Apparent t½ of Imipenem in Combination With MK-7655

Imipenem is 1 of the 2 constituents of PRIMAXIN®. Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Geometric Mean)
Panel A: Mild Renal Impairment1.54
Panel B: Healthy Controls to Panel A1.24
Panel C: Moderate Renal Impairment2.18
Panel D: Healthy Controls to Panel C1.40
Panel E: Severe Renal Impairment2.78
Panel F: Healthy Controls to Panel E1.32
Panel G: ESRD/HD Period 1 Postdialysis3.24
Panel H: Healthy Controls to Panel G1.21
Panel G: ESRD/HD Period 2 Predialysis3.20

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Part 1: Apparent t½ of Cilastin in Combination With MK-7655

Cilastin is 1 of the 2 constituents of PRIMAXIN®. Apparent t½ is the amount of time for the maximum drug concentration to decrease by 50%. (NCT01275170)
Timeframe: Predose and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4.5, 6, 8, 10, and 14 hours postdose

Interventionhours (Geometric Mean)
Panel A: Mild Renal Impairment1.43
Panel B: Healthy Controls to Panel A1.08
Panel C: Moderate Renal Impairment2.11
Panel D: Healthy Controls to Panel C1.19
Panel E: Severe Renal Impairment5.08
Panel F: Healthy Controls to Panel E1.09
Panel G: ESRD/HD Period 1 Postdialysis12.2
Panel H: Healthy Controls to Panel G1.14
Panel G: ESRD/HD Period 2 Predialysis12.2

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Part 2: Plasma AUC0-∞ of Omeprazole as a Probe Substrate of Cytochrome P450 Enzyme (CYP)2C19

Omeprazole was selected as a substrate of CYP2C19. AUC0-∞ was determined in participants with severe renal impairment and ESRD/HD participants. (NCT01275170)
Timeframe: Predose and 0.5, 1, 2,3, 4, 8, 12, and 24 hours postdose

InterventionµM*hr (Geometric Mean)
Panel E: Severe Renal Impairment9.10
Panel F: Healthy Controls to Panel E6.20
Panel G: ESRD/HD Period 1 Postdialysis4.56
Panel G: ESRD/HD Period 2 Predialysis4.08
Panel H: Healthy Controls to Panel G5.03

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Percentage of Biomarker-positive Immune Cells

Peripheral blood mononuclear cells were (PBMCs) were isolated from blood samples taken from each participant at baseline and Week 5. PBMCs were stained with a panel of fluorochrome-conjugated antibodies against multiple surface and intracellular biomarkers, including Cluster of Differentiation (CD) 3, CD4, CD8, Forkhead box P3 protein (FOXP3) and latency-associated peptide (LAP). The percentage of T cells positive for each of these biomarkers was determined by fluorescence activated cell sorting (FACS) and the mean percentage of positive T cells for each biomarker for all analyzed participants is reported. (NCT01287195)
Timeframe: Baseline, Week 5

Interventionpercentage of biomarker-positive T cells (Mean)
CD3, BaselineCD3, Week 5CD4, BaselineCD4, Week 5CD8, BaselineCD8, Week 5FOXP3, BaselineFOXP3, Week 5LAP, BaselineLAP, Week 5
Oral OKT3383059753124540.90.5

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Score in Histologic Evaluation of Flexible Sigmoidoscopy

Mucosal biopsies were obtained from the most inflamed area seen during flexible sigmoidoscopy and blindly scored by a single pathologist with scores ranging 0-3 with a higher score indicating a worse outcome. (NCT01287195)
Timeframe: Baseline, Week 5

Interventionscore on a scale (Mean)
BaselineWeek 5
Oral OKT32.21.75

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T Cell Proliferation of PBMCs in Cell Culture

PBMCs isolated from whole blood obtained from participants at baseline, Weeks 1, 3, and 5 were assessed for proliferation in cell culture using a radioactive thymidine incorporation assay. A higher number indicates a higher level of proliferation. (NCT01287195)
Timeframe: Baseline, Weeks 1, 3 and 5

Interventionradioactive counts of cells per minute (Mean)
BaselineWeek 1Week 3Week 5
Oral OKT327470496174657520993

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Simple Clinical Colitis Activity Index (SCCAI) Score

SCCAI is a symptom based questionnaire addressing five assessments, including bowel frequency day, bowel frequency night, urgency of defecation, blood in stool and general well-being. Score ranges from 0-15 with one additional point added for each manifestation of extracolonic features. A higher score indicates a worse outcome. (NCT01287195)
Timeframe: Baseline, Week 5

Interventionscore on a scale (Mean)
BaselineWeek 5
Oral OKT37.76

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Number of Participants With Adverse Events

An adverse event is any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. (NCT01287195)
Timeframe: From baseline to Week 10

InterventionParticipants (Count of Participants)
Oral OKT33

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Number of Participants With Anti-Drug Antibodies

Serum samples were obtained to measure anti-drug antibodies during the study. (NCT01287195)
Timeframe: From baseline to Week 10

InterventionParticipants (Count of Participants)
Oral OKT30

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Cytokine Production by PBMCs in Cell Culture

Cytokine production was assessed in cell cultures of PBMCs obtained from participants at baseline, Weeks 1, 3 and 5. The following cytokines were detected and are reported here: interferon gamma (IFN-gamma), interleukin (IL)-17A, IL-6, IL-1 beta, tumor necrosis factor (TNF) and IL-10. (NCT01287195)
Timeframe: Baseline, Weeks 1, 3 and 5

Interventionpicograms/milliliter (pg/mL) (Mean)
IFN gamma, BaselineIFN gamma, Week 1IFN gamma, Week 3IFN gamma, Week 5IL-17A, BaselineIL-17A, Week 1IL-17A, Week 3IL-17A, Week 5IL-6, BaselineIL-6, Week 1IL-6, Week 3IL-6, Week 5IL-1 beta, BaselineIL-1 beta, Week 1IL-1 beta, Week 3IL-1 beta, Week 5TNF, BaselineTNF, Week 1TNF, Week 3TNF, Week 5IL-10, BaselineIL-10, Week 1IL-10, Week 3IL-10, Week 5
Oral OKT34935115211017828326911418174147026781978567110155185383615857151956311512015

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Mayo Score

The Mayo Score is determined by the investigator by assigning a score to the following four assessments: stool frequency, rectal bleeding, physician's global assessment and endoscopy. Total range for Mayo score is 0-12 with a higher score indicating a worse outcome. (NCT01287195)
Timeframe: Baseline, Week 5

Interventionscore on a scale (Mean)
BaselineWeek 5
Oral OKT38.87.5

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Inhibition of Platelet Aggregation at 4 Hours Post Dose (IPA4)

IPA4 equals the platelet aggregation measured 4 hours post dose divided by the platelet aggregation measured at baseline (multiplied by 100). (NCT01303445)
Timeframe: 7 days

Interventionpercent of baseline platelet aggregation (Mean)
Aggrenox Alone BID97.89
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone96.34
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone97.02

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Plasma Dipyridamole Minimum Concentration (Cmin)

Minimum measured concentration of dipyridamole in plasma (NCT01303445)
Timeframe: 7 days

Interventionnanogram/milliliter (Geometric Mean)
Aggrenox Alone BID679
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone723
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone713

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Plasma Dipyridamole Maximum Concentration (Cmax)

Maximum measured concentration of dipyridamole in plasma (NCT01303445)
Timeframe: 7 days

Interventionnanogram/milliliter (Geometric Mean)
Aggrenox Alone BID2750
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone2550
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone2550

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Inhibition of Platelet Aggregation at 12 Hours Post Dose (IPA12)

IPA12 equals the platelet aggregation measured 12 hours post dose divided by the platelet aggregation measured at baseline (multiplied by 100). (NCT01303445)
Timeframe: 7 days

Interventionpercent of baseline platelet aggregation (Mean)
Aggrenox Alone BID98.78
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone97.80
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone98.11

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Plasma Dipyridamole Area Under Plasma Concentration-time Curve From Zero to 12 Hours (AUC0-12)

Area under the concentration time curve of the analyte in plasma from 0 to 12 hours at steady state (NCT01303445)
Timeframe: 7 days

Intervention(nanogram/milliliter)*hours (Geometric Mean)
Aggrenox Alone BID17100
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone16700
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone16500

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Percentage Peak-to-trough Fluctuation (%PTF)

PTF = 100*((Cmax-Cmin)/Cavg) where Cavg=(AUC0-12)/12. (NCT01303445)
Timeframe: 7 days

Interventionpercent of average hourly plasma conc. (Mean)
Aggrenox Alone BID144
Aggrenox BID Plus Omeprazole QD Following Aggrenox Alone132
Aggrenox BID Plus Omeprazole QD Following Omeprazole Alone134

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Level of Active Clopidogrel Metabolite

The level of the active clopidogrel metabolite will be measured at at 0.25, 0.5, 1, 2, and 4 hours after the Day One dose is administered for pharmacokinetic analysis. The analysis will measure the Area Under the Curve. (NCT01341600)
Timeframe: Baseline, 0.25, 0.5, 1, 2, and 4 hours

,,
Interventionng h/mL (Mean)
Clopidogrel 75mgClopidogrel 150mgClopidogrel 300mg
Extensive Metabolizers32.753.680.4
Intermediate Metabolizers33.343.873.7
Poor Metabolizers17.424.236

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Change in Platelet Aggregation Following Therapy With Clopidogrel

ADP mediated platelet aggregation measured 4 hours post Day 8 clopidogrel dose (NCT01341600)
Timeframe: 4 hours post Day 8 dose

,,
Interventionpercentage of aggregation (Mean)
Clopidogrel 75mgClopidogrel 150mgClopidogrel 300mg
Extensive Metabolizers31.325.119.5
Intermediate Metabolizers37.833.225.7
Poor Metabolizers55.044.232.6

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Change in Platelet Aggregation Following Therapy With Clopidogrel

Adenosine diphosphate (ADP) mediated platelet aggregation measured 4 hours post-dose of clopidogrel on Day 1. (NCT01341600)
Timeframe: Day 1, 4 hours post clopidogrel dose

,,
Interventionpercentage of aggregation (Mean)
Clopidogrel 75mgClopidogrel 150mgClopidogrel 300mg
Extensive Metabolizers62.553.938.6
Intermediate Metabolizers68.157.847.8
Poor Metabolizers62.963.253.3

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Change in Platelet Aggregation Following Therapy With Clopidogrel and Omeprazole

The change in maximum platelet aggregation in response to ADP 4-hours post dose on day 8 of therapy with clopidogrel and omeprazole will be compared to the baseline measure of platelet aggregation at day 1 prior to drug therapy (NCT01341600)
Timeframe: Baseline, Day 8

Interventionpercentage of aggregation (Mean)
Poor Metabolizers11.6
Intermediate Metabolizers27.9
Extensive Metabolizers37.5

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AUC of Dextromethorphan, Midazolam and Omeprazole in the Presence of Fluoxetine

Our secondary outcome measure will be the interaction between fluoxetine and each CYP evaluated in the cocktail. A 50% increase in the AUC of caffeine (CYP1A2), dextromethorphan (CYP2D6), omeprazole (CYP2C19) or midazolam (CYP3A4) between treatment and control days is considered clinically significant. The interaction of fluoxetine with caffeine (CYP1A2) will be considered as a negative control for the study. These AUCs will be measured on study day 1 (control day) and study day 18 (NCT01361217)
Timeframe: The secondary outcome will be assessed within 2 months after the last subject is enrolled or at 2 years from the start of study enrollment, which ever is sooner.

Interventionnmol*hr/L (Mean)
caffeine control AUCCaffeine treatment AUCdextromethophan control AUCDextromethorphan treatment AUCOmeprazole control AUComeprazole treatment AUCmidazolam control AUCmidazolam treatment AUC
Midazolam, Caffeine, Omeprazole, Caffeine AUC After Fluoxetine4300043000681850120085003024

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Lovastatin AUC in the Presence of Fluoxetine

Our primary outcome measure will be the interaction of fluoxetine with CYP3A4. A 50% increase in the AUC for lovastatin plus hydroxy-lovastatin acid (the active form of lovastatin) between treatment day 14 (study day 20) and control days (study day 2) is considered clinically significant. (NCT01361217)
Timeframe: The primary outcome will be assessed within 2 months after the last subject is enrolled or at 2 years from the start of study enrollment, which ever is sooner.

Interventionnmol*hr/L (Mean)
Lovastatin AUC After Fluoxetine Dosing170
Lovastatin Before Fluoxetine180

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Maximum Plasma Concentration (Cmax) for SSP-002358

Cmax is a term that refers to the maximum (or peak) concentration that a drug achieves in the body after the drug has been administrated. (NCT01415349)
Timeframe: Assessed over 48 hours post-dose

Interventionng/ml (Mean)
SSP-002358 Alone3.89
SSP-002358 + Omeprazole4.12

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Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) for SSP-002358

Area under the plasma concentration versus time curve from time 0 to infinity. AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body. (NCT01415349)
Timeframe: Assessed over 48 hours post-dose

Interventionng*h/ml (Mean)
SSP-002358 Alone23.3
SSP-002358 + Omeprazole24.6

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Number of Patients With Overgrowth of Oral Microbiota in Their Stool After PPI Therapy Withdrawal or Initiation

Analysis at baseline will be compared to that at 2 weeks using Multitagged sequencing. Number of patients with overgrowth of oral microbiota in their stool after PPI therapy withdrawal or initiation were specifically analyzed. (NCT01458990)
Timeframe: 2 weeks

InterventionParticipants (Count of Participants)
PPI Inititation45
PPI Withdrawal15

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Number of Patients With Adverse Events During Initiation or Withdrawal of PPI Therapy

Analysis at baseline will be compared to that at 2 weeks. This will be specifically, changes in those with PPI withdrawal compared to those with PPI initiation (NCT01458990)
Timeframe: 2 weeks

InterventionParticipants (Count of Participants)
PPI Initiation0
PPI Withdrawal0

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Intensive PK Sub-study: Time to Reach Maximum Concentration (Tmax) of DAC HYP

(NCT01462318)
Timeframe: Day 1 and Day 141 (Week 20) at pre-dose and 8, 24, 72, and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

Interventionday (Mean)
Day 1 (Week 0); n=25Day 141 (Week 20); n=24
Main Study9.316.41

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Intensive PK Sub-study: Cmax of DAC HYP

(NCT01462318)
Timeframe: Day 1 and Day 141 (Week 20) at pre-dose and 8, 24, 72, and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

Interventionmcg/mL (Mean)
Day 1 (Week 0); n=25Day 141 (Week 20); n=24
Main Study12.6329.07

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Intensive PK Sub-study: Area-Under-the-Curve From Start to End of the Dosing Interval (AUCtau) of DAC HYP

(NCT01462318)
Timeframe: Day 1 and Day 141 (Week 20) at pre-dose and 8, 24, 72, and 120 hours post-dose and 7, 10, 14, and 21 days post-dose

Interventionday*mcg/mL (Mean)
Week 0 (Day 1); n=25Week 20; n=24
Main Study255.25638.10

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Intensive PK Sub-study: Elimination Half-life (t½) of DAC HYP

(NCT01462318)
Timeframe: Day 141 (Week 20) at pre-dose and 8, 24, 72 and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

Interventionday (Mean)
Main Study21.92

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Intensive PK Sub-study: Minimum Concentrations (Cmin) of DAC HYP

(NCT01462318)
Timeframe: Day 141 (Week 20) at pre-dose and 8, 24, 72 and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

Interventionmcg/mL (Mean)
Main Study14.93

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Number of Participants With Anti-DAC HYP Neutralizing Antibodies (NAbs): ECL ADA Assay

Participants with PB NAbs through Week 44, in the treatment period (extends up to 42 days after the last dose during the main study), and in the post-treatment period (43 days after the last dose until the end of the post-treatment period dose). (NCT01462318)
Timeframe: Up to 44 weeks

Interventionparticipants (Number)
PB NAbs through Week 44=negative; n=113PB NAbs through Week 44=positive; n=113PB NAbs in treatment period=negative; n=113PB NAbs in treatment period=positive; n=113PB NAbs in post-treatment period=negative; n=110PB NAbs in post-treatment period=positive; n=110
Main Study105810941046

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TP-DI Sub-study: Area-Under-the-Curve From Zero to Infinity (AUCinf) of Each Probe Drug

AUCinf of each of the following cytochrome P450 (CYP) isoenzyme substrates: midazolam (CYP3A), S-warfarin + vitamin K (CYP2C9), and omeprazole (CYP2C19). The AUC from zero to 12 hours (AUC0-12) was calculated for caffeine (CYP1A2). (NCT01462318)
Timeframe: Week 43 (7 days prior to DAC HYP administration) and Week 53 (7 days after DAC HYP administration), pre-cocktail dose and at 0.5 and 1, 2, 3, 4, 6, 8, 10 , 24, 48, 72 and 96 hours post-probe drug cocktail administration

Interventionhr*ng/mL (Mean)
Midazolam (Period 1) AUCinf; n=20Midazolam+DAC HYP (Period 2) AUCinf; n=19S-warfarin (Period 1) AUCinf; n=17S-warfarin+DAC HYP (Period 2) AUCinf; n=18Omeprazole (Period 1) AUCinf; n=18Omeprazole+DAC HYP (Period 2) AUCinf; n=19Caffeine (Period 1) AUC0-12; n=20Caffeine+DAC HYP (Period 2) AUC0-12; n=20
TP-DI Sub-study786.75816.8719292.919609.32214.51770.035742.437449.2

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TP-DI Sub-study: CL/F of Each Probe Drug

CL/F of each of the following CYP isoenzyme substrates: midazolam (CYP3A), warfarin + vitamin K (CYP2C9), and omeprazole (CYP2C19). (NCT01462318)
Timeframe: Week 43 (7 days prior to DAC HYP administration) and Week 53 (7 days after DAC HYP administration), pre-cocktail dose and at 0.5 and 1, 2, 3, 4, 6, 8, 10 , 24, 48, 72 and 96 hours post-probe drug cocktail administration

InterventionmL/hr (Mean)
Midazolam (Period 1); n=20Midazolam+DAC HYP (Period 2); n=19S-Warfarin (Period 1); n=17S-Warfarin+DAC HYP (Period 2); n=18Omeprazole (Period 1); n=18Omeprazole+DAC HYP (Period 2); n=19
TP-DI Sub-study7625.77298.6565.86541.4641612.441772.4

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TP-DI Sub-study: Cmax of Each Probe Drug

Cmax of each of the following CYP isoenzyme substrates: midazolam (CYP3A), caffeine (CYP1A2), warfarin + vitamin K (CYP2C9), and omeprazole (CYP2C19). (NCT01462318)
Timeframe: Week 43 (7 days prior to DAC HYP administration) and Week 53 (7 days after DAC HYP administration), pre-cocktail dose and at 0.5 and 1, 2, 3, 4, 6, 8, 10 , 24, 48, 72 and 96 hours post-probe drug cocktail administration

Interventionng/mL (Mean)
Midazolam (Period 1); n=20Midazolam+DAC HYP (Period 2); n=19Caffeine (Period 1); n=20Caffeine+DAC HYP (Period 2); n=19S-Warfarin (Period 1); n=20S-Warfarin+DAC HYP (Period 2); n=19Omeprazole (Period 1); n=19Omeprazole+DAC HYP (Period 2); n=19
TP-DI Sub-study271.05311.214965.05399.5635.65649.74776.95771.16

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TP-DI Sub-study: Omeprazole/Hydroxyomeprazole Concentration Ratio at 2 Hours Post-omeprazole Dosing

(NCT01462318)
Timeframe: Week 43 (7 days prior to DAC HYP administration) and Week 53 (7 days after DAC HYP administration) at 2 hours after probe drug cocktail administration

Interventionratio (Mean)
Omeprazole (Period 1)Omeprazole+ DAC HYP (Period 2)
TP-DI Sub-study2.6731.028

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TP-DI Sub-study: Dextromethorphan to Dextrorphan Urine Concentration Ratio

(NCT01462318)
Timeframe: Week 43 (7 days prior to DAC HYP administration) and Week 53 (7 days after DAC HYP administration), pre-cocktail dose and for 12 hours after probe-drug cocktail administration

Interventionratio (Mean)
Dextromethorphan (Period 1)Dextromethorphan+DAC HYP (Period 2)
TP-DI Sub-study0.424680.48939

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Intensive PK Sub-study: Apparent Clearance (CL/F) of DAC HYP

(NCT01462318)
Timeframe: Day 141 (Week 20) at pre-dose and 8, 24, 72 and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

InterventionL/day (Mean)
Main Study0.27

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Intensive PK Sub-study: Apparent Volume of Distribution (V/F) of DAC HYP

(NCT01462318)
Timeframe: Day 141 (Week 20) at pre-dose and 8, 24, 72 and 120 hours post-dose and 7, 10, 14 and 21 days post-dose

InterventionLiters (Mean)
Main Study8.21

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Number of Participants With Anti-DAC HYP Binding Antibodies (ADAbs): Electrochemiluminescent (ECL) Anti-Drug Antibody (ADA) Assay

Participants with post-baseline (PB) ADAbs through Week 44, in the treatment period (extends up to 42 days after the last dose during the main study), and in the post-treatment period (43 days after the last dose until the end of the post-treatment period dose). (NCT01462318)
Timeframe: Up to 44 weeks

Interventionparticipants (Number)
PB ADAbs through Week 44=negative; n=113PB ADAbs through Week 44=positive; n=113PB ADAbs in treatment period=negative; n=113PB ADAbs in treatment period=positive; n=113PB ADAbs in post-treatment period=negative; n=110PB ADAbs in post-treatment period=positive; n=110
Main Study783592218921

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The Proportion of Nighttimes Without 'Cardinal Symptom'

The proportion of Nighttimes without 'Cardinal symptom' after 4 or 8 treatment-FAS 'Cardinal symptom': Burning sensation in the chest, Acid reflux, Heartburn including chest pain (NCT01499368)
Timeframe: 4 or 8 week

,,
Interventionproportion of days (Mean)
week 4week 8week 8(LOCF)
Famotidine0.720.780.78
Lafutidine0.750.870.87
Omeprazole0.820.890.89

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The Proportion of Daytimes Without 'Cardinal Symptom'

The proportion of daytimes without 'Cardinal symptom' after 4 or 8 week treatment-FAS 'Cardinal symptom': Burning sensation in the chest, Acid reflux, Heartburn including chest pain (NCT01499368)
Timeframe: 4 or 8 week

,,
Interventionproportion of days (Mean)
week 4week 8week 8(LOCF)
Famotidine0.680.760.76
Lafutidine0.740.830.83
Omeprazole0.770.870.87

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The Proportion of Days Without 'Cardinal Symptom'

The proportion of days without 'Cardinal symptom' after 4 or 8 week treatment-FAS 'Cardinal symptom': Burning sesation in the chest, Acid reflux, Heartburn including chest pain (NCT01499368)
Timeframe: 4 or 8 week

,,
Interventionproportion of days (Mean)
week 4week 8week 8(LOCF)
Famotidine0.560.670.67
Lafutidine0.640.770.77
Omeprazole0.690.820.82

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Percentage of Participants Affected By Heartburn Symptoms: End of Treatment Quality of Life Questionnaire

End of Treatment Quality of Life was based on a questionnaire regarding quality-of-life issues associated with heartburn, completed by participants at the end of treatment period 1 and the end of treatment period 2. (NCT01587885)
Timeframe: End of treatment period 1 and end of treatment period 2

,
Interventionpercentage of partcipants (Number)
heartburn symptoms affected daily activitiesheartburn symtoms caused trouble falling asleepheartburn symptoms awoke participantslept on incline due to heartburn symptomsmedicine helped with full night's rest
Omeprazole 20 mg30.025.032.547.595.0
Omeprazole 20 mg + Sodium Bicarbonate 1100 mg30.027.522.535.090.0

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Percentage of Participants Experiencing Onset and Demonstrating Duration of Heartburn Relief Over Time

"Onset of heartburn relief was defined as a reduction of at least one grade from baseline in the severity of heartburn following start of treatment. Severity of heartburn was evaluated by the participant using the 4-point Likert Scale, which rated heartburn severity as follows:~Absent (0): Heartburn is not present.~Mild (1): Heartburn did not last long or was easily tolerated.~Moderate (2): Heartburn caused discomfort and interrupted usual activities.~Severe (3): Heartburn caused great interference with usual activities and may have been incapacitating." (NCT01587885)
Timeframe: Start of treatment until onset of heartburn relief, up to 72 hours

,
Interventionpercentage of participants (Number)
≤15 minutes≤30 minutes≤60 minutes≤90 minutes≤120 minutes≤180 minutes≤1440 minutes (24 hours)≤2880 minutes (48 hours)≤4320 minutes (72 hours)
Omeprazole 20 mg13.627.361.475.088.690.993.295.5100.0
Omeprazole 20 mg + Sodium Bicarbonate 1100 mg20.552.375.090.995.5100.0100.0100.0100.0

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Time-to-onset of Heartburn Relief

"Time-to-onset of heartburn relief was defined as earliest time following start of treatment that participant experienced a reduction of at least one grade from baseline in the severity of heartburn. Severity of heartburn was evaluated by the participant using the 4-point Likert Scale, which rated heartburn severity as follows:~Absent (0): Heartburn is not present.~Mild (1): Heartburn did not last long or was easily tolerated.~Moderate (2): Heartburn caused discomfort and interrupted usual activities.~Severe (3): Heartburn caused great interference with usual activities and may have been incapacitating." (NCT01587885)
Timeframe: Start of treatment until onset of heartburn relief, up to 24 hours

InterventionMinutes (Median)
Omeprazole 20 mg + Sodium Bicarbonate 1100 mg30.0
Omeprazole 20 mg60.0

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Number of Participants Preferring Each Treatment for Heartburn Control: Final Subjective Questionnaire

Participants completed a Final Subjective Questionnaire for Treatment Preference. Question 1 asked participants to compare the 2 treatments for Heartburn Control. (NCT01587885)
Timeframe: At end of study (approx. Study Day 40)

Interventionparticipants (Number)
Preferred omeprazole+sodium bicarbonatePreferred omeprazolePreferred both equallyMissing data
All Treated Participants141798

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Number of Participants Preferring Each Treatment for Heartburn Relief: Final Subjective Questionnaire

Participants completed a Final Subjective Questionnaire for Treatment Preference. Question 2 asked participants to compare the 2 treatments for Heartburn Relief. (NCT01587885)
Timeframe: At end of study (approx. Study Day 40)

Interventionparticipants (Number)
Preferred omeprazole+sodium bicarbonatePreferred omeprazolePreferred both equallyPreferred neitherMissing data
All Treated Participants1616718

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Number of Participants Preferring Each Treatment Overall: Final Subjective Questionnaire

Participants completed a Final Subjective Questionnaire for Treatment Preference. Question 3 asked participants to compare the 2 treatments for their overall preference. (NCT01587885)
Timeframe: At end of study (approx. Study Day 40)

Interventionparticipants (Number)
Preferred omeprazole+sodium bicarbonatePreferred omeprazolePreferred both equallyMissing data
All Treated Participants171768

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Eradication of H Pylori Infection 4 Weeks After Completion of Therapy

H. pylori eradication is defined in this study as concomitant negativity to all previously positive tests (H. pylori antigen in stool; histopathological confirmation of H. pylori bacilli; and rapid urease test.) 4 weeks after the end of therapy. (NCT01593592)
Timeframe: 4 weeks therapy

Interventionparticipants (Number)
Control Group23
Lactobacillus Reuteri Group26

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Severe Adverse Effects to the Used Medications and Dietary Supplements.

(NCT01593592)
Timeframe: 4 weeks

Interventionpercentage of participants (Number)
Control Group0
Lactobacillus Reuteri Group0

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The Secondary End Point Was the Development of Severe Adverse Effects to the Used Medications and Dietary Supplements.

Severe adverse effects to the used medications and dietary supplements, these may expose the participants to major morbidity and may change the outcomes in them. (NCT01593592)
Timeframe: 8 weeks

Interventionparticipants (Number)
Control Group0
Lactobacillus Reuteri Group0

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Faldaprevir: Area Under the Curve Over the Time Interval From 0 Extrapolated to Infinity (AUC 0-infinity)

"Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 extrapolated to infinity~In this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01694706)
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administration

Intervention[ng*h/mL] (Geometric Mean)
Faldaprevir in Fasting37900
Faldaprevir After a High-fat Meal48200
Faldaprevir and Omeprazole36000

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Faldaprevir: Area Under the Curve 0 to the Last Quantifiable Data Point (AUC0-tz)

"Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 to the last quantifiable drug plasma concentration~In this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01694706)
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administration

Interventionng*h/mL (Geometric Mean)
Faldaprevir in Fasting36300
Faldaprevir After a High-fat Meal46400
Faldaprevir and Omeprazole34400

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Faldaprevir: Maximum Measured Concentration (Cmax)

"Maximum measured concentration of the faldaprevir in plasma~In this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01694706)
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administration

Interventionng/mL (Geometric Mean)
Faldaprevir in Fasting2030
Faldaprevir After a High-fat Meal2600
Faldaprevir and Omeprazole1920

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Ratio of 1'-Hydroxy-Midazolam AUC(0-T) to Midazolam AUC(0-T) and 1'-Hydroxy-Midazolam AUC(INF) to Midazolam AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (1'-hydroxy-midazolam) to parent (midazolam) ratio was corrected for molecular weight. AUC (0-T) and AUC (INF) measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionratio (Geometric Mean)
MR_AUC (0-T) ratio; N=22, 21, 21, 20MR_(INF) ratio; N=22, 21, 20, 20
Day 1 Inje Cocktail0.4210.428
Day 11 Inje Cocktail0.4720.478
Day 4 Inje Cocktail Plus Belatacept0.4470.460
Day 7 Inje Cocktail0.4950.479

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Plasma Half-Life (T-HALF) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of dextromethorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. T-HALF was measured in hours (h). (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionh (Mean)
Midazolam (N=22, 21, 21, 20)Losartan (N=22, 21, 21, 20)Omeprazole (N= 22, 19, 21, 18)Dextromethorphan (N=18, 17, 18, 15)Caffeine (N=22, 21, 21, 18)
Day 1 Inje Cocktail4.012.961.196.765.61
Day 11 Inje Cocktail4.052.871.366.706.03
Day 4 Inje Cocktail Plus Belatacept4.432.561.396.985.71
Day 7 Inje Cocktail4.273.301.286.336.17

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Ratio of 5-Hydroxyomeprazole AUC(0-T) to Omeprazole AUC(0-T) and 5-Hydroxyomeprazole AUC(INF) to Omeprazole AUC(INF) , Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (5-Hydroxyomeprazole) to parent (omeprazole) ratio was corrected for molecular weight. AUC (0-T) and AUC (INF) measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionratio (Geometric Mean)
MR_AUC (0-T) ratio; N=22,21,21,20MR_AUC (INF) ratio; N=22,19,21,17
Day 1 Inje Cocktail0.7000.705
Day 11 Inje Cocktail0.6100.679
Day 4 Inje Cocktail Plus Belatacept0.6090.558
Day 7 Inje Cocktail0.5510.553

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Ratio of E-3174 AUC(0-T) to Losartan AUC(0-T) and E3174 AUC (INF) to Losartan AUC (INF) Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (E-3174) to parent (losartan) ratio was corrected for molecular weight. AUC (0-T) and AUC (INF) measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionratio (Geometric Mean)
MR_AUC (0-T) ratio; N=22,21,21,20MR_AUC (INF) ratio; N=22,20,21,20
Day 1 Inje Cocktail5.816.02
Day 11 Inje Cocktail6.176.37
Day 4 Inje Cocktail Plus Belatacept5.755.99
Day 7 Inje Cocktail5.996.16

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Ratio of 5-Dextrorphan AUC(0-T) to Dextromethorphan AUC(0-T) and 5-Dextrorphan AUC(INF) to Dextromethorphan AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (5-dextrorphan ) to parent (dextromethorphan) ratio was corrected for molecular weight. AUC (0-T) and AUC (INF) measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionratio (Geometric Mean)
MR_AUC (0-T) ratio; N=21,20,20,19MR_AUC (INF) ratio; N=18,17,18,15
Day 1 Inje Cocktail201173
Day 11 Inje Cocktail193173
Day 4 Inje Cocktail Plus Belatacept200177
Day 7 Inje Cocktail177170

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Ratio of Paraxanthine AUC(0-T) to Caffeine AUC(0-T) and Paraxanthine AUC (INF) to Caffeine AUC (INF), Corrected for Molecular Weight [MR_AUC(0-T) and MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (paraxanthine) to parent (caffeine) ratio was corrected for molecular weight. AUC (0-T) and AUC (INF) measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionratio (Geometric Mean)
MR_AUC(0-T) ratio; N=17,19,18,18MR_AUC(INF) ratio; N=7, 8, 6, 6
Day 1 Inje Cocktail0.6270.827
Day 11 Inje Cocktail0.6030.781
Day 4 Inje Cocktail Plus Belatacept0.6770.827
Day 7 Inje Cocktail0.6350.799

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T-HALF of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population

Plasma half-life (T-HALF) was measured in hours (h). Samples for assessment of plasma concentrations of Inje cocktail components metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionh (Mean)
1'-Hydroxy-Midazolam (N=22,21,20,20)E-3174 (N=22, 20, 21, 20)5-Hydroxyomeprazole (N=22,20,21,17)Dextrorphan (N=21,20,20,19)Paraxanthine (N=7,8,6,6)
Day 1 Inje Cocktail5.294.861.434.267.33
Day 11 Inje Cocktail5.314.881.544.087.44
Day 4 Inje Cocktail Plus Belatacept6.354.571.554.366.86
Day 7 Inje Cocktail5.614.751.524.237.33

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Time of Maximum Observed Plasma Concentration (Tmax) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of dextromethorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. Tmax was measured in hours (h). (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionh (Median)
Midazolam (N=22,21,21,20)Losartan (N= 22, 21, 21, 20)Omeprazole (N=22,21,21,20)Dextromethorphan (N=21, 19, 19, 19)Caffeine (N= 22,21,21,18)
Day 1 Inje Cocktail0.501.522.003.001.00
Day 11 Inje Cocktail1.01.503.003.001.50
Day 4 Inje Cocktail Plus Belatacept0.502.003.003.001.00
Day 7 Inje Cocktail0.501.503.003.001.50

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Tmax of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. Time of maximum observed plasma concentration (Tmax) was measured in hours (h). (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionh (Median)
1'-Hydroxy-Midazolam (N=22,21,21,20)E-3174 (N=22, 21, 21, 20)5-Hydroxyomeprazole (N=22,21,21,20)Dextrorphan (N=21,20,20,19)Paraxanthine (N=17, 19, 18, 18)
Day 1 Inje Cocktail1.004.002.002.008.00
Day 11 Inje Cocktail1.004.002.532.008.00
Day 4 Inje Cocktail Plus Belatacept1.004.003.002.008.00
Day 7 Inje Cocktail1.004.003.002.008.00

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Mean Change From Baseline in Heart Rate at Study Discharge (Day 46±2 Days)

Heart Rate was taken after the participant had been sitting quietly for at least 5 minutes and was measured in beats per minute (bpm). Hear rate was taken on Day 46 (day of discharge) during the follow up period. Baseline was defined as last non-missing result with a collection date-time less than the date-time of the first active dose of study drug. (NCT01766050)
Timeframe: Baseline and Day 46 ±2 days

Interventionbpm (Mean)
Post Treatment1.0

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AUC(0-T) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population

Area under the plasma concentration-time curve from zero to the last time of the last quantifiable concentration [AUC(0-T)] was measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
1'-hydroxy-midazolam (N=22, 21, 21, 20)E-3174 (N= 22,21,21,20)5-hydroxyomeprazole (N=22,21,21,20)dextrorphan (N=21,20,20,19)paraxanthine (N=17,19,18,18)
Day 1 Inje Cocktail28.91995997163620592
Day 11 Inje Cocktail33.62072995164421353
Day 4 Inje Cocktail Plus Belatacept31.81999967157021077
Day 7 Inje Cocktail32.52089929151920680

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Adjusted Geometric Mean Cmax of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. Cmax was measured in ng/mL. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionng/mL (Geometric Mean)
Day 1 Inje Cocktail4696.505
Day 4 Inje Cocktail Plus Belatacept4450.019
Day 7 Inje Cocktail4332.326
Day 11 Inje Cocktail4479.687

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Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths, and AEs Leading to Discontinuation - All Treated Participants

Adverse events were coded according to the Medical Dictionary for Regulatory Activities (MedDRA), version 15.1. AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. Events captured from Day 1 (pre-dose) to last day prior to discharge (Day 46 ±2). In the total group, a participant with an AE is only counted once (ie, data reflected in Days 1, 4, 7, and 11 below could be the same participant with an AE on multiple days of the study). (NCT01766050)
Timeframe: Day 1 to Day of discharge (Day 46±2)

,,,,
Interventionparticipants (Number)
Adverse EventsSAEsDeathsAEs leading to discontinuation
All Participants5001
Day 1 Inje Cocktail4000
Day 11 Inje Cocktail1000
Day 4 Inje Cocktail Plus Belatacept2000
Day 7 Inje Cocktail1001

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Study Discharge (Day 46±2 Days)

Systolic and Diastolic blood pressures were taken after the participant had been sitting quietly for at least 5 minutes and the pressures were measured in millimeters of mercury (mm Hg). Systolic and Diastolic blood pressures were taken on Day 46 (day of discharge from the study). Baseline was defined as last non-missing result with a collection date-time less than the date-time of the first active dose of study drug. (NCT01766050)
Timeframe: Baseline and Day 46 ±2 days

Interventionmm Hg (Mean)
Systolic (N=18)Diastolic (N=18)
Post Treatment-5.9-5.7

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Mean Change From Baseline in Sitting Heart Rate - All Treated Participants

Heart Rate was taken after the participant had been sitting quietly for at least 5 minutes and the heart rate was measured in beats per minute (bpm). Heart Rates were obtained at screening visit, Day -1, and at 0 hour (pre-dose), 0.5 hour (post dose), and 2 hours (post dose) on Days 1, 4, 7, 11. Baseline was defined as last non-missing result with a collection date-time less than the date-time of the first active dose of study drug. (NCT01766050)
Timeframe: Baseline and 0.5 and 2.0 hours Post Dose on Days 1, 4, 7, and 11

,,,
Interventionbpm (Mean)
Heart Rate 0.5 hour post dose (N=22, 21, 21, 20)Heart Rate 2.0 hour post dose (N=22, 21, 21, 20)
Day 1 Inje Cocktail-3.3-3.5
Day 11 Inje Cocktail-1.63.1
Day 4 Inje Cocktail Plus Belatacept-4.20.2
Day 7 Inje Cocktail-1.80.5

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Cmax of Inje Cocktail Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail component metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail component metabolites were each measured using HPLC with MS/MS detection. Cmax was measured in ng/mL. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng/mL (Geometric Mean)
1'-Hydroxy-Midazolam (N=22, 21, 21, 20)E-3174 (N=22, 21, 21, 20)5-Hydroxyomeprazole (N=22, 21, 21, 20)Dextrorphan (N=21,20,20,19)Paraxanthine (N=17,19,18,18)
Day 1 Inje Cocktail11.12623353421291
Day 11 Inje Cocktail12.32913373311358
Day 4 Inje Cocktail Plus Belatacept11.92763603241367
Day 7 Inje Cocktail11.43003323121320

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AUC(INF) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population

Area under the plasma concentration-time curve from time zero extrapolated to infinite time [AUC(INF)] was measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
1'-hydroxy-midazolam (N=22,21,20,20)E-3174 (N=22,20,21,20)5-hydroxyomeprazole (N=22,20,21,17dextrorphan (N=21,20,20,19)paraxanthine (N=7,8,6,6)
Day 1 Inje Cocktail30.521031010167922401
Day 11 Inje Cocktail35.121821063168221874
Day 4 Inje Cocktail Plus Belatacept33.82060990161022905
Day 7 Inje Cocktail32.92187938156222063

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Ratio of E-3174 (Cmax) to Losartan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (E-3174) to parent (losartan) ratio was corrected for molecular weight. Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionratio (Geometric Mean)
Day 1 Inje Cocktail2.31
Day 4 Inje Cocktail Plus Belatacept2.24
Day 7 Inje Cocktail2.26
Day 11 Inje Cocktail2.26

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Apparent Total Body Clearance (CLT/F) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of dextromethorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. CLT/F was measured as liters/hour (L/h) (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
InterventionL/h (Geometric Mean)
Midazolam (N=22, 21, 21, 20)Losartan (N=22, 21, 21, 20)Omeprazole (N=22, 19, 21, 18)Dextromethorphan (N=18,17,18,18)Caffeine (N=22, 21, 21, 18)
Day 1 Inje Cocktail73.814829.239164.99
Day 11 Inje Cocktail71.415125.339684.83
Day 4 Inje Cocktail Plus Belatacept71.314623.742475.30
Day 7 Inje Cocktail77.314624.742644.97

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Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population

AUC(0-T): Area under the plasma concentration-time curve from time zero zero to the time of the last quantifiable concentration and AUC (INF): AUC extrapolated to infinity were measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for omeprazole with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Inje cocktail components (omeprazole) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
AUC (0-T); (N= 22, 21, 21, 20)AUC (INF); (N= 22, 19, 21, 18)
Day 1 Inje Cocktail1361.0241368.593
Day 11 Inje Cocktail1653.4911779.717
Day 4 Inje Cocktail Plus Belatacept1577.0171632.455
Day 7 Inje Cocktail1671.1731679.693

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Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Losartan With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population

AUC (0-T): area under the concentration curve from time 0 to the time of the last quantifiable concentration and AUC (INF) extrapolated to infinity were measured in ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for losartan with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Inje cocktail components (losartan) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
AUC (0-T) N=22, 21, 21, 20)AUC (INF) N=22, 21, 21, 20)
Day 1 Inje Cocktail332.191338.033
Day 11 Inje Cocktail332.400338.646
Day 4 Inje Cocktail Plus Belatacept336.531341.644
Day 7 Inje Cocktail337.487343.508

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Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population

AUC(0-T): area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration and AUC (INF): AUC extrapolated to infinity, were measured as ng*h/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for dextromethorphan with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. The poor metabolizer of CYP2D6 was excluded from the statistical analysis. Inje cocktail components (dextromethorphan) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
AUC (0-T); N= 21, 19, 19, 19AUC (INF); N= 18, 17, 18, 15
Day 1 Inje Cocktail6.1766.220
Day 11 Inje Cocktail5.9496.359
Day 4 Inje Cocktail Plus Belatacept5.6515.455
Day 7 Inje Cocktail6.1956.412

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Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population

Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. AUC (0-T) and AUC (INF) were measured as ng*h/mL. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

,,,
Interventionng*h/mL (Geometric Mean)
AUC (0-T); N= 22, 21, 21, 18AUC (INF); N= 22, 21, 21, 18
Day 1 Inje Cocktail37394.540084.1
Day 11 Inje Cocktail38407.041537.6
Day 4 Inje Cocktail Plus Belatacept35200.337647.8
Day 7 Inje Cocktail36853.440149.9

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Adjusted Geometric Mean Area Under the Concentration Time Curve (AUC) From Zero to Last Concentration (0-T) and AUC Extrapolated to Infinity (INF) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population

AUC(0-T): area under the plasma concentration-time curve from zero to the last time of the last quantifiable concentration and AUC (INF): AUC from time zero extrapolated to infinite time were measured in ng*h/mL. Samples for the assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for midazolam with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Midazolam measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7and 11

,,,
Interventionng*h/mL (Geometric Mean)
AUC (0-T);N=22, 21, 21, 20)AUC (INF);N=22, 21, 21, 20)
Day 1 Inje Cocktail65.54867.743
Day 11 Inje Cocktail67.71769.841
Day 4 Inje Cocktail Plus Belatacept68.83371.039
Day 7 Inje Cocktail63.30365.555

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Ratio of Paraxanthine (Cmax) to Caffeine (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (paraxanthine) to parent (caffeine) ratio was corrected for molecular weight. Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components and their metabolites were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionratio (Geometric Mean)
Day 1 Inje Cocktail0.303
Day 4 Inje Cocktail Plus Belatacept0.337
Day 7 Inje Cocktail0.333
Day 11 Inje Cocktail0.323

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Ratio of 1'-Hydroxy-Midazolam (Cmax) to Midazolam (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (1'-hydroxy-midazolam) to parent (midazolam) ratio was corrected for molecular weight. Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionratio (Geometric Mean)
Day 1 Inje Cocktail0.432
Day 4 Inje Cocktail Plus Belatacept0.476
Day 7 Inje Cocktail0.497
Day 11 Inje Cocktail0.490

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Adjusted Geometric Mean Cmax of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population

Cmax was measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for dextromethorphan with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. The poor metabolizer of CYP2D6 was excluded from the statistical analysis. Inje cocktail components (dextromethorphan) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionng/mL (Geometric Mean)
Day 1 Inje Cocktail0.927
Day 4 Inje Cocktail Plus Belatacept0.800
Day 7 Inje Cocktail0.855
Day 11 Inje Cocktail0.794

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Number of Participants With Marked Hematology and Urinalysis Laboratory Abnormalities - All Treated Participants

Samples for laboratory tests were obtained at Screening visit, Day -1 or prior to dosing on Day 1, Days 3, 6, 10, 46 ±2, and at early termination, after 10 hours fasting. Leukocytes: *10^9 cells per liter (c/L) < 0.85*Pre-Rx if Pre-Rx < LLN or <0.9*LLN if LLN <= Pre-Rx or Pre-Rx is missing. Neutrophils (absolute): *10^12 c/L < 0.85* Pre-Rx if Pre-Rx < 1.5, <1.5 if Pre-Rx >= 1.5, < 1.5 if Pre-Rx missing. Urine blood from dipstick: >=2 if Pre-Rx <1 or was missing or if Pre-Rx >=1. Urinary microscopic white blood cells (WBC) and red blood cells (RBC) >= 2 if Pre-Rx <2 or if Pre-Rx was missing or >=4 if Pre-Rx >=2. (NCT01766050)
Timeframe: Day -1 to Day 46 ±2 days or at early termination

Interventionparticipants (Number)
Leukocytes <0.85*Pre-Rx *10^9 c/L (N=22)Neutrophils <0.85*Pre-Rx *10^12 c/L (N=22)Urine Blood >= 2 (N=22)Urinary RBC microscopic >= 2 (N=8)Urinary WBC microscopic >= 2 (N=8)
Inje Cocktail Alone and Inje Cocktail Plus Belatacept14211

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Mean Change From Baseline in Sitting Systolic and Diastolic Blood Pressure - All Treated Participants

Systolic and Diastolic blood pressures were taken after the participant had been sitting quietly for at least 5 minutes and the pressures were measured in millimeters of mercury (mm Hg). Pressures were obtained at screening visit, Day -1, and at 0 hour (pre-dose), 0.5 hour (post dose), and 2 hours (post dose) on Days 1, 4, 7, 11. Baseline was defined as last non-missing result with a collection date-time less than the date-time of the first active dose of study drug. (NCT01766050)
Timeframe: Baseline and 0.5 and 2.0 hours Post Dose on Days 1, 4, 7, and 11

,,,
Interventionmm Hg (Mean)
Systolic 0.5 hour post dose (N=22,21,21,20)Systolic 2.0 hour post dose (N=22,21,21,20)Diastolic 0.5 hour post dose (N=22,21,21,20)Diastolic 2.0 hour post dose (N=22,21,21,20)
Day 1 Inje Cocktail-0.60.2-1.70.9
Day 11 Inje Cocktail-4.7-2.9-2.2-1.0
Day 4 Inje Cocktail Plus Belatacept0.12.0-0.2-2.0
Day 7 Inje Cocktail-4.9-2.7-2.2-3.4

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Number of Participants With Marked Serum Chemistry Laboratory Abnormalities - All Treated Participants

Samples for laboratory tests were obtained at Screening visit, Day -1 or prior to dosing on Day 1, Days 3, 6, 10, 46, and at early termination, after 10 hours fasting. Upper limits of normal (ULN); Lower limits of normal (LLN); Pre-therapy (Rx); micromoles per liter (µmol/L); millimoles per liter (mmol/L); grams per liter (g/L); Units per liter (U/L); Aspartate Aminotransferase (AST); Blood Urea Nitrogen (BUN) Total Bilirubin: >1.1*ULN if Pre-Rx<= ULN or Pre-Rx is missing, or >1.2*Pre-Rx if Pre-Rx >ULN. AST: >1.25*Pre-Rx if Pre-Rx >ULN or 1.25*ULN if Pre-Rx <= ULN or Pre-Rx is missing. BUN: >1.1*ULN if Pre-Rx<= ULN or Pre-Rx is missing, or >1.2*Pre-Rx if Pre-Rx >ULN. Phosphorus: <0.85*LLN if Pre-RX >= LLN or is missing or if Pre-Rx < LLN. total Protein: <0.9*LLN if Pre-Rx>= LLN or is missing or Pre-Rx > LLN. Creatine Kinase: >1.5*Pre-Rx if Pre-Rx > ULN or is missing or Pre-Rx is <= ULN. Lactate Dehydrogenase: >1.25*ULN if Pre-Rx <= ULN or missing, >1.5*Pre-Rx if Pre-Rx > ULN. (NCT01766050)
Timeframe: Day -1 to Day 46 ±2 days or at early termination

Interventionparticipants (Number)
Total bilirubin >1.1*ULN µmol/L (N=22)AST >1.25*Pre-Rx U/L (N=22)BUN >1.1*ULN mmol/L (N=22)Inorganic Phosphorus <0.85*LLN mmol/L (N=22)Total Protein <0.9*LLN g/L (N=22)Creatine Kinase > 1.5* Pre-Rx U/L (N=22)Lactate Dehydrogenase >1.25*ULN U/L (N=22)
Inje Cocktail Alone and Inje Cocktail Plus Belatacept1111121

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Number of Participants With Out-of-Range Electrocardiogram Intervals - All Treated Participants

Participants had 12-Lead electrocardiograms (ECGs) performed at Screening Visit, Day 1 prior to dosing, Day 46 ±2, and at early termination. Definition of out-of-range: PR Interval >210 milliseconds (msec); QRS > 120 msec, QT > 500 msec or > 30 msec change from baseline (Day 1); QT with Fridericia correction (QTcF) > 450 msec or change from baseline of > 30 msec to <= 60 msec or change from baseline > 60 msec. (NCT01766050)
Timeframe: Day 1 to Day 46 ±2 days or at early termination

Interventionparticipants (Number)
Day 46 (N=18)Early Termination (N=2)
Inje Cocktail Alone and Inje Cocktail Plus Belatacept00

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Adjusted Geometric Mean Maximum Drug Concentration (Cmax) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population

Samples for the assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for midazolam with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Cmax measured in nanograms per milliliter (ng/mL). Inje cocktail components (Midazolam) measured using High Performance Liquid Chromatography (HPLC) with Tandem Mass Spectrometry (MS/MS) Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionng/mL (Geometric Mean)
Day 1 Inje Cocktail24.376
Day 4 Inje Cocktail Plus Belatacept24.152
Day 7 Inje Cocktail22.211
Day 11 Inje Cocktail24.220

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Adjusted Geometric Mean Cmax of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population

Cmax: Maximum observed plasma concentration was measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for omeprazole with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Inje cocktail components (omeprazole) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionng/mL (Geometric Mean)
Day 1 Inje Cocktail583.047
Day 4 Inje Cocktail Plus Belatacept734.776
Day 7 Inje Cocktail753.126
Day 11 Inje Cocktail686.929

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Adjusted Geometric Mean Cmax of Losartan With and Without the Coadministration of Belatacept - PK Evaluable Population

Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components (midazolam, losartan, omeprazole, dextromethorphan and caffeine) and their metabolites (1'-hydroxy-midazolam, E-3174, 5-hydroxyomeprazole, dextrorphan, and paraxanthine) were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Adjusted geometric mean for losartan with and without belatacept, along with adjusted geometric mean ratios for Days 4, 7, and 11 versus Day 1, respectively, are presented. Inje cocktail components (losartan) measured using HPLC with MS/MS Detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionng/mL (Geometric Mean)
Day 1 Inje Cocktail119.789
Day 4 Inje Cocktail Plus Belatacept118.663
Day 7 Inje Cocktail127.184
Day 11 Inje Cocktail126.461

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Ratio of 5-Hydroxyomeprazole (Cmax) to Omeprazole (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (5-hydroxyomeprazole) to parent (omeprazole) ratio was corrected for molecular weight. Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionratio (Geometric Mean)
Day 1 Inje Cocktail0.548
Day 4 Inje Cocktail Plus Belatacept0.471
Day 7 Inje Cocktail0.424
Day 11 Inje Cocktail0.478

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Ratio of 5-Dextrorphan (Cmax) to Dextromethorphan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population

Metabolite (5-dextrorphan) to parent (dextromethorphan) ratio was corrected for molecular weight. Cmax measured in ng/mL. Samples for assessment of plasma concentrations of Inje cocktail components and the metabolites of those components were collected at time = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours relative to the dosing of belatacept on Day 4 and Inje cocktail dosing on Days 1, 4, 7, and 11, respectively. The poor metabolizer of CYP2D6 was excluded from summary of Dextrorphan parameters. Inje cocktail components were each measured using HPLC with MS/MS detection. (NCT01766050)
Timeframe: Pre-dose to 24 hours after dose of the Inje Cocktail on Days 1, 4, 7 and 11

Interventionratio (Geometric Mean)
Day 1 Inje Cocktail280
Day 4 Inje Cocktail Plus Belatacept303
Day 7 Inje Cocktail275
Day 11 Inje Cocktail303

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Change From Baseline in Psychiatric Symptom on Hospital Anxiety and Depression Scale at Week 8

Each patient was surveyed using the Hospital Anxiety and Depression Scale to assess the psychiatric symptom at week 0 and 8.The HADS consists of 14 items, seven of which assess anxiety, and seven assess depression. The anxiety and depression subscales were calculated independently. The patients were asked to answer each item on a four-point (0 - 3) scale. Scores of 0 to 7 on either subscale can be regarded as within the normal range, scores of 8 to 10 are suggestive of the presence of the respective state, and scores of 11 or higher indicate the probable presence of the respective mood disorder. The change of HADS scores was calculated by HADS anxiety and depression scores of 8 weeks minus baseline, with lower values indicate better outcome. (NCT01851863)
Timeframe: week 0 and 8

,,,
Interventionunits on HADS score (Mean)
HADS anxiety scoreHADS depression score
Deanxit(Psychological and GI) + Omeprazole-4.46-4.82
Deanxit(Psychological) + Omeprazole-2.29-2.25
Deanxit(Without Explanation) + Omeprazole-2.78-2.86
Proton Pump Inhibitor-1.68-1.88

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Number of Participants With Adverse Reaction

Number of participants with adverse reactions were recorded to analyze the safety profile of treatment. (NCT01851863)
Timeframe: 8 weeks

Interventionparticipants (Number)
Deanxit(Psychological and GI) + Omeprazole6
Deanxit(Psychological) + Omeprazole9
Deanxit(Without Explanation) + Omeprazole5
Proton Pump Inhibitor2

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Compliance of Flupentixol-Melitracen

The patients were asked to keep a diary to record their medication intake. At each visit (weeks 1, 2, 4, 8), the patient bring back the drug bottle and the diary, then the physician recorded the number of pills remaining in the bottle. Pills remained more than 20% at any visit or seven days of consecutive abstinence were adopted as the criterion for identifying therapy noncompliance. (NCT01851863)
Timeframe: weeks 1, 2, 4, 8

Interventionparticipants (Number)
Deanxit(Psychological and GI) + Omeprazole44
Deanxit(Psychological) + Omeprazole28
Deanxit(Without Explanation) + Omeprazole31

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Change From Baseline in Dyspepsia Symptom Questionnaire at Week 8

The severity of patients' dyspeptic symptoms were assessed using the Leeds Dyspepsia Questionnaire (LDQ) at week 0 and 8. The LDQ contains eight items about epigastric pain, retro-sternal pain, regurgitation, nausea, vomiting, belching, early satiety and dysphagia with six grades for each item and a sum of the eight symptom scores make the LDQ score.LDQ scores of 0 - 4 were classified as very mild dyspepsia, 4 - 8 as mild dyspepsia, 9 -15 as moderate dyspepsia, and > 15 as severe or very severe dyspepsia. The change of LDQ scores was calculated by LDQ scores of 8 weeks minus baseline, with lower values represent a better outcome. (NCT01851863)
Timeframe: week 0 and 8

Interventionunits on LDQ scale (Mean)
Deanxit(Psychological and GI) + Omeprazole-3.85
Deanxit(Psychological) + Omeprazole-2.51
Deanxit(Without Explanation) + Omeprazole-2.49
Proton Pump Inhibitor-1.31

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Comparison of the Primary Outcome With Bioimpedance Aggregometry

After 1 week of randomization to ranitidin or omeprazole, the platelet function will also be analysed by other method: bioimpedance aggregometry with ADP 10 mcM as reagent (NCT01896557)
Timeframe: 1 week after drug exposure

InterventionOhms (Mean)
Omeprazole2
Ranitidine2.77

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Comparing Platelet Function of Patients on Dual Antiplatelet Therapy With ASA + Clopidogrel, Between the Groups Ranitidin and Omeprazole, Using VerifyNow Method.

One week after starting double-blind, double-dummy, randomized therapy with ranitidin or omeprazole on patients treated with DAPT, platelet function will be compared with the method VerifyNow, in percent Inhibition of Platelet Aggregation (IPA) from baseline. IPA was calculated as the percent change in aggregability from baseline, with the formula IPA = (on-treatment aggregability minus baseline aggregability)/baseline aggregability. Since baseline aggregation is always, per definition, equal or more than on-treatment aggregation, there is no possibility that this number might be negative. (NCT01896557)
Timeframe: One week after drug exposure (omeprazole/ranitidine); 2 weeks after baseline

InterventionPercentage (Mean)
Omeprazole17.4
Ranitidine30.1

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Comparing Platelet Function of Patients on Dual Antiplatelet Therapy With ASA + Clopidogrel, Between the Groups Ranitidin and Omeprazole, After One Week of Randomized Treatment

One week after starting double-blind, double-dummy, randomized therapy with ranitidin or omeprazole on patients treated with DAPT, platelet function will be compared with the method VerifyNow, in P2Y12 Reactivity Units. (NCT01896557)
Timeframe: One week after randomized treatment exposure (omeprazole or ranitidine)

InterventionP2Y12 Reactivity Units (Mean)
Omeprazole173.54
Ranitidine153.61

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Comparison of the Primary Outcome With PFA-100 (Collagen/ADP Cartridge)

After 1 week of randomization to ranitidin or omeprazole, the platelet function will also be analysed by other method: PFA-100(Collagen/ADP cartridge). (NCT01896557)
Timeframe: 1 week after drug exposure

Interventionseconds (Mean)
Omeprazole95.1
Ranitidine97.2

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Baricitinib

(NCT01925144)
Timeframe: Days 1 and 10: predose of baricitinib, 0.5, 0.75, 1, 2, 3, 4, 6, 12, 24, 36 and 48 hours postdose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Baricitinib99.2
Baricitinib + Omeprazole76.8

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PK: Area Under the Plasma Concentration-Time Curve From Time 0 Hour to Infinity [AUC(0-∞)] of Baricitinib

(NCT01925144)
Timeframe: Days 1 and 10: predose of baricitinib, 0.5, 0.75, 1, 2, 3, 4, 6, 12, 24, 36 and 48 hours postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
Baricitinib663
Baricitinib + Omeprazole712

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Baricitinib

(NCT01925144)
Timeframe: Days 1 and 10: predose of baricitinib, 0.5, 0.75, 1, 2, 3, 4, 6, 12, 24, 36 and 48 hours postdose

Interventionhours (Median)
Baricitinib1.00
Baricitinib + Omeprazole2.00

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AUC(0-tz)

Area under the concentration-time curve of deleobuvir in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) (NCT01983566)
Timeframe: 1 hour (h) before drug administration and 30 minutes (min), 1h, 1h 30min, 2h, 2h 30min, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h and 48h after drug administration

Interventionnmol*h/L (Geometric Mean)
Dele Fasted9790
Dele High Fat16900
Dele Low Fat14200
Dele + OMP15800

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Cmax

Maximum measured concentration of deleobuvir in plasma (Cmax) (NCT01983566)
Timeframe: 1 hour (h) before drug administration and 30 minutes (min), 1h, 1h 30min, 2h, 2h 30min, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h and 48h after drug administration

Interventionnmol/L (Geometric Mean)
Dele Fasted2140
Dele High Fat3930
Dele Low Fat3160
Dele + OMP3190

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Change in Pain Assessed by Visual Analogue Scale (VAS)

"The primary outcome was changes (% change) in self-reported pain levels using VAS - from 0 (no pain) to 10 (worst imaginable pain).~Results are presented as largest percentage (%) change in pain before and after the interventions (baseline and post-intervention, 6 weeks).~Percentage change is calculated with post-intervention pain minus baseline pain, divided by baseline pain i.e. (post - baseline) / baseline." (NCT02013427)
Timeframe: 6 weeks

Interventionpercentage of change in pain (Mean)
Observational-0.03
Naproxen & Omeprazole-0.10
Placebo Only-0.21

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Vz/F of AZD9291

Assessment of the PK of AZD9291 using the apparent volume of distribution, Vz/F (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

InterventionL (Geometric Mean)
AZD9291 and Omeprazole Co-administration2037
AZD9291 Alone2343

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Cmax of AZD9291

Rate and extent of absorption of AZD9291 following single oral doses of AZD9291 tablet formulation by assessment of maximum plasma concentration (Cmax). (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

InterventionnM (Geometric Mean)
AZD9291 and Omeprazole Co-administration127.8
AZD9291 Alone126.1

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CL/F of AZD9291

Assessment of the PK of AZD9291 using the apparent plasma clearance, CL/F (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

InterventionL/h (Geometric Mean)
AZD9291 and Omeprazole Co-administration23.93
AZD9291 Alone25.55

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AUC of AZD9291

Area under the plasma concentration-time curve from zero to infinity for AZD9291 (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose

InterventionnM.h (Geometric Mean)
AZD9291 and Omeprazole Co-administration6690
AZD9291 Alone6269

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AUC(0-72)

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using area under the plasma concentration curve from time zero to 72 hours, AUC(0-72) (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72 hours post AZD9291 dose.

,
InterventionnM.h (Geometric Mean)
AZD9291AZ5104AZ7550
AZD9291 Alone4106304.0231.3
AZD9291 and Omeprazole Co-administration4404301.5216.5

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λz

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using the terminal rate constant, λz (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
Intervention1/h (Geometric Mean)
AZD9291AZ5104AZ7550
AZD9291 Alone0.0108980.0127220.009606
AZD9291 and Omeprazole Co-administration0.0117480.0135770.009718

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Tmax

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using time to reach maximum plasma concentration, tmax (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
Interventionh (Median)
AZD9291AZ5104AZ7550
AZD9291 Alone6710
AZD9291 and Omeprazole Co-administration6810

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Tlag

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using lag time before observation of quantifiable analyte concentrations in plasma, tlag (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
Interventionh (Median)
AZD9291AZ5104AZ7550
AZD9291 Alone0.000.000.00
AZD9291 and Omeprazole Co-administration0.000.000.00

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t(1/2)

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using the terminal half-life, t(1/2) (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
Interventionh (Geometric Mean)
AZD9291AZ5104AZ7550
AZD9291 Alone63.6054.4772.16
AZD9291 and Omeprazole Co-administration58.9951.0671.34

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Parent to Metabolite Ratios of AZ5104 and AZ7550 Cmax

Assessment of the PK of AZ5104 and AZ7550 Cmax using the parent (AZD9291) to metabolite ratios (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
InterventionRatio (Geometric Mean)
AZ5104AZ7550
AZD9291 Alone0.046710.03491
AZD9291 and Omeprazole Co-administration0.043350.03061

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Parent to Metabolite Ratios of AZ5104 and AZ7550 AUC

Assessment of the PK of AZ5104 and AZ7550 AUC using the parent (AZD9291) to metabolite ratios (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
InterventionRatio (Geometric Mean)
AZ5104AZ7550
AZD9291 Alone0.087850.09166
AZD9291 and Omeprazole Co-administration0.083180.08019

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Cmax of AZ5104 and AZ7550

Assessment of the PK of AZ5104 and AZ7550 (metabolites to AZD9291) using the maximum plasma concentration, Cmax (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
InterventionnM (Geometric Mean)
AZ5104AZ7550
AZD9291 Alone5.8894.402
AZD9291 and Omeprazole Co-administration5.5433.913

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AUC(0-t)

Assessment of the PK of AZD9291 (parent compound), AZ5104 (metabolite) and AZ7550 (metabolite) using area under the plasma concentration curve from zero extrapolated to o the time of the last quantifiable concentration, AUC(0-t) (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
InterventionnM.h (Geometric Mean)
AZD9291AZ5104AZ7550
AZD9291 Alone6249539.2560.0
AZD9291 and Omeprazole Co-administration6673546.5520.0

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AUC of AZ5104 and AZ7550

Area under the plasma concentration-time curve from zero to infinity of AZ5104 and AZ7550 (metabolites to AZD9291) (NCT02224053)
Timeframe: PK samples collected in both period 1 and 2 at pre-dose, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 48, 72, 120, 168, 216, 336, and 504 hours post AZD9291 dose.

,
InterventionnM.h (Geometric Mean)
AZ5104AZ7750
AZD9291 Alone550.7574.9
AZD9291 and Omeprazole Co-administration556.6536.5

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞])

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

Interventionnanogram*hour per milliliter (ng·h/mL) (Geometric Mean)
Evacetrapib12400
Evacetrapib + Omeprazole14100

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Pharmacokinetics (PK): Time of Maximum Observed Concentration (Tmax) of Evacetrapib

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

InterventionHours (Median)
Evacetrapib3.00
Evacetrapib + Omeprazole3.00

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Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8,12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Evacetrapib748
Evacetrapib + Omeprazole959

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Circulating Levels (Plasma Concentration) of Omeprazole Prior to Treatment With Luliconazole Cream 1%

Circulating plasma levels of omeprazole were measured using validated liquid chromatography with tandem mass spectrometry detection (LS/MS-MS) methods. The range for omeprazole determination was 4.64-9.27 nanograms/milliliter (ng/mL). Serial blood sampling occurred in each enrolled participant up to 24 hours post treatment (Day 1) with omeprazole (before the start of luliconazole cream 1% treatment on Day 2). (NCT02394340)
Timeframe: 15 minutes predose; 15, 30, 45, and 60 minutes postdose; and 1.5, 2, 2.5, 3, 4, 6, 8, 10, and 24 hours postdose of omeprazole on Day 1

Interventionng/mL (Mean)
Predose15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose4 hours postdose6 hours postdose8 hours postdose10 hours postdose24 hours postdose
Luliconazole Cream 1%0023.67196.30463.74526.98655.70621.08636.60468.79235.20129.7074.243.32

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Circulating Levels (Plasma Concentration) of Omeprazole After 1 Week of Treatment With Luliconazole Cream 1%

Circulating plasma levels of omeprazole were measured using validated LS/MS-MS methods. The range for omeprazole determination was 4.64-9.27 ng/mL. Serial blood sampling occurred in each enrolled participant up to 24 hours post treatment (Day 8) with omeprazole (after using luliconazole cream 1% treatment for 1 week). (NCT02394340)
Timeframe: 15 minutes predose; 15, 30, 45, and 60 minutes postdose; and 1.5, 2, 2.5, 3, 4, 6, 8, 10, and 24 hours postdose of omeprazole on Day 8

Interventionng/mL (Mean)
Predose15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose4 hours postdose6 hours postdose8 hours postdose10 hours postdose24 hours postdose
Luliconazole Cream 1%0018.11142.72317.21637.56763.51700.91730.56586.83323.40190.15111.516.84

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Pulse Wave Velocity

Comparison of the effects of Febuxostat and Allopurinol on Pulse Wave Velocity (PWV) after 36 weeks of treatment. (NCT02500641)
Timeframe: 36 weeks of treatment

Interventionm/s (Mean)
Febuxostat 80/120 mg/Day9.0
Allopurinol 100 up to 600 mg/Day9.05

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Parent Global Impressions-Revised (PGI-R)

The PGI-R is a rating of change of 18 autism symptoms compared to baseline, with each symptom rated on a Likert scale from -3 (much worse) to zero (no change) to +3 (much better). We report the average change of the 18 symptoms, so the possible range is from -3 to +3. (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionunits on a scale (Mean)
Combined Group1.4

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Social Responsiveness Scale (SRS)

The SRS is an assessment of social skills based on 65 items, where each item is scored on a range of 0 (no symptoms) to 3 (severe symptoms). The total score is a sum of the individual scores, so the total possible range is from 0 to 195, with a higher score indicating greater severity of symptoms. (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionunits on a scale (Mean)
Baseline10 weeks
Combined Group116.297.8

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Gastrointestinal Symptom Responsiveness Scale (GSRS)

The GSRS is a measure of gastrointestinal symptoms. It includes 15 questions, rated on a Likert scale of 1-7, from no symptoms to severe symptoms, respectively (i.e., higher is worse). We report an average score for all 15 questions, so the possible range for the average score is also 1-7. (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionunits on a scale (Mean)
Baseline10 weeks
Combined Group2.741.31

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Daily Stool Record (DSR)

The DSR is a record of the type of stool that a participant had each day, using the Bristol Stool Form which ranges from 1 (very hard) to 7 (liquid). We then analyzed the data as % days of abnormal stools over a 14 day period, where an abnormal stool is defined as an unusually hard stool (types 1-2), unusually soft stool (types 6-7), or no stool that day. So, the possible range of % days of abnormal stools is from 0% to 100%, with a higher score indicating a more severe problem. (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionpercentage of days with abnormal stool (Mean)
Baseline10 weeks
Combined Group6234

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Childhood Autism Rating Scale (CARS)

The CARS is an assessment of 15 autism-related symptoms. Each item is scored on a scale of 1 (no symptoms) to 4 (severe symptoms), and the scores for each symptom are summed to obtain a total score. So, the possible scores range from 15 to 60, with a higher score indicating greater severity. (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionunits on a scale (Mean)
Baseline10 weeks
Combined Group39.734.1

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Blood Safety Markers (Assessment of Blood Chemistry Panel and Complete Blood Count)

Number of participants who had a clinically significant change in their blood safety markers (comprehensive metabolic panel including kidney/liver function and complete blood count with differential) (NCT02504554)
Timeframe: Baseline and 10 weeks (end of treatment)

Interventionparticipants (Number)
Combined Group0

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Vineland Adaptive Behavior Scale (VABS)

The VABS is an assessment of adaptive behaviors, and we analyzed it to determine the developmental age of the participants, with possible scores ranging from 0 years to 21 years. (NCT02504554)
Timeframe: baseline and 18 weeks (8 weeks after treatment stopped)

Interventionyears (Mean)
Baseline18 weeks
Combined Group5.396.84

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Elimination of Moderate-severe Regurgitation at 6 Months

The primary endpoint was the percent of patients in both treatment arms who achieved elimination of moderate-severe regurgitation at 6 months, as reported on the foregut symptom questionnaire. (NCT02505945)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Control Arm10
Treatment Arm42

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FASN Positivity Expression at Baseline and After 4-7 Days of Omeprazole Treatment

The mean and standard deviation of FASN positivity expression determined at baseline and after 4-7 days of Omeprazole treatment. FASN expression is evaluated using immunohistochemistry in core biopsy samples. (NCT02595372)
Timeframe: baseline and after 4-7 days

Interventionpercentage of positivity (Mean)
BaselineAfter 4-7 days
High Dose Omeprazole Treatment53.941.7

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Percent of Patients With FASN Expression

FASN expression was evaluated using immunohistochemistry in core biopsy samples. FASN expression was determined if the positivity was >= 15%. The percent of patients who had FASN expression and the exact 95% confidence intervals were calculated. (NCT02595372)
Timeframe: up to 1 week

Interventionpercentage of participants (Number)
High Dose Omeprazole Treatment93.3

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Percentage of Patients With Pathological Complete Response (pCR) in All Patients

pCR is defined as no invasive disease in the breast or axilla at the time of definitive surgery. The percentage of patients who achieve pCR along with exact 95% confidence intervals were calculated. (NCT02595372)
Timeframe: Up to 6 months

Interventionpercentage of participants (Number)
High Dose Omeprazole Treatment74.4

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Percentage of Patients With Pathological Complete Response (pCR) in Patients Who Have Fatty Acid Synthase (FASN) Expression

pCR is defined as no invasive disease in the breast of axilla at the time of definitive surgery. A patient is considered to have FASN expression if the positivity was >= 15% at the baseline or after 4-7 days of Omeprazole monotherapy. FASN expression is evaluated using immunohistochemistry in core biopsy samples. The percent of patients with FASN expression that have pCR will be calculated with an exact 95% confidence interval. (NCT02595372)
Timeframe: Up to 6 months

Interventionpercentage of participants (Number)
High Dose Omeprazole Treatment72.4

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FASN Activity at Baseline and After 4-7 Days of Omeprazole Treatment

The mean and standard deviation of FASN activity determined at baseline and after 4-7 days of Omeprazole treatment. FASN activity was evaluated using immunohistochemistry in core biopsy samples. (NCT02595372)
Timeframe: baseline and after 4-7 days

Interventionng/mg (Mean)
BaselineAfter 4-7 days
High Dose Omeprazole Treatment2.11.3

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Symptom Frequency and Severity/Distress Scores From Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) (Overall)

"The 15-symptom GSAS questionnaire includes measures of: Gastrointestinal distress, Regurgitation/heartburn and Upper respiratory manifestations. The outcome measures were the number, frequency, and severity of GSAS symptoms reported at 6 weeks. Measures were based on aggregate GSAS scores. Symptom numbers range from 0 to 15. Frequency is based on the total number of reported days of symptomatic episodes in the past week divided by the number of potential symptoms (number reported divided by 15 for GSAS score. The range for frequency score:0 to 7 with higher scores indicative of greater frequency of symptoms. Severity is the average distress score reported by individuals (zero if no symptoms). Symptom distress is based on a 4 point Likert scale (0= not at all, 1=somewhat, 2=quite a bit and 3=very much). The higher the score the worse outcome.~." (NCT02623816)
Timeframe: 6 weeks

,
Interventionscore on a scale (Mean)
GSAS Symptoms ScoreGSAS Frequency ScoreGSAS Severity Score
Optimal Dosing5.21.00.6
Sub-optimal Dosing8.52.21.0

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Percent Change in Pain Assessed by Visual Analogue Scale (VAS)

"Self-report pain using a VAS scale (0-10) : 0 represents no pain and 10 the worst imaginable pain.~Results are presented as percentage (%) change in pain before and after the intervention (baseline and post-intervention, 12 weeks).~Percentage change is calculated with post-intervention pain minus baseline pain, divided by baseline pain i.e. (post - baseline) / baseline." (NCT02986334)
Timeframe: 12 weeks

Interventionpercentage of pain change (Mean)
No Treatment Intervention-0.0145
Active Treatment Intervention-0.2082
Placebo Treatment Intervention-0.1109

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to 48 Hours (AUC[0-48h]) of CYP450 Substrate-Caffeine

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve from Zero to 48 hours (AUC[0-48h]) of CYP450 Substrate (Caffeine) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, and 48 hours postdose

Interventionng*h/mL (Geometric Mean)
100 mg Caffeine25000
160 mg Ixekizumab + 100 mg Caffeine22400
80 mg Ixekizumab Q2W + 100 mg Caffeine22400

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Warfarin

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve from Zero to Infinity (AUC[0-∞]) of CYP450 Substrate (Warfarin) (NCT02993471)
Timeframe: Predose, 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose

Interventionng*h/mL (Geometric Mean)
10 mg Warfarin17600
160 mg Ixekizumab + 10 mg Warfarin17700
80 mg Ixekizumab Q2W + 10 mg Warfarin16200

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Dextromethorphan

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve from Zero to Infinity (AUC[0-∞]) of CYP450 Substrate (Dextromethorphan) (NCT02993471)
Timeframe: Predose, 1, 2, 4, 6, 8, 10, 24, 48, and 72 hours postdose

Interventionng*h/mL (Geometric Mean)
30 mg Dextromethorphan11.7
160 mg Ixekizumab + 30 mg Dextromethorphan12.6
80 mg Ixekizumab Q2W + 30 mg Dextromethorphan8.53

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Midazolam

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve from Zero to Infinity (AUC[0-∞]) of CYP450 Substrate (Midazolam) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours postdose

Interventionnanogram*hour per milliliter (ng*h/mL) (Geometric Mean)
1 mg Midazolam16.6
160 mg Ixekizumab + 1 mg Midazolam15.9
80 mg Ixekizumab Q2W + 1 mg Midazolam15.4

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole

Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate (Omeprazole and its metabolite 5-Hydroxyomeprazole) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, and 48 hours postdose

,,
Interventionng/mL (Geometric Mean)
Omeprazole5-Hydroxyomeprazole
160 mg Ixekizumab + 20 mg Omeprazole340143
20 mg Omeprazole333148
80 mg Ixekizumab Q2W + 20 mg Omeprazole368137

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve from Zero to Infinity (AUC[0-∞]) of CYP450 Substrate (Omeprazole and its metabolite 5-Hydroxyomeprazole) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, and 48 hours postdose

,,
Interventionng*h/mL (Geometric Mean)
Omeprazole5-Hydroxyomeprazole
160 mg Ixekizumab + 20 mg Omeprazole829475
20 mg Omeprazole1060519
80 mg Ixekizumab Q2W + 20 mg Omeprazole913455

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Caffeine

Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate (Caffeine) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, and 48 hours postdose

Interventionng/mL (Geometric Mean)
100 mg Caffeine2230
160 mg Ixekizumab + 100 mg Caffeine2220
80 mg Ixekizumab Q2W + 100 mg Caffeine2240

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Dextromethorphan

Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate (Dextromethorphan) (NCT02993471)
Timeframe: Predose, 1, 2, 4, 6, 8, 10, 24, 48, and 72 hours postdose

Interventionng/mL (Geometric Mean)
30 mg Dextromethorphan0.691
160 mg Ixekizumab + 30 mg Dextromethorphan0.878
80 mg Ixekizumab Q2W + 30 mg Dextromethorphan0.658

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Warfarin

Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate (Warfarin) (NCT02993471)
Timeframe: Predose, 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose

Interventionng/mL (Geometric Mean)
10 mg Warfarin510
160 mg Ixekizumab + 10 mg Warfarin525
80 mg Ixekizumab Q2W + 10 mg Warfarin510

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Cytochrome P450 (CYP450) Substrate-Midazolam

Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Cytochrome P450 (CYP450) Substrate (Midazolam) (NCT02993471)
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours postdose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
1 mg Midazolam4.56
160 mg Ixekizumab + 1 mg Midazolam4.92
80 mg Ixekizumab Q2W (Once Every Two Weeks) + 1 mg Midazolam4.83

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Part A: PK of Tazemetostat and Its Metabolites After Administration Alone and With Fluconazole (AUC0-t, AUC0-8)

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6930 (ER-897387)Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6930 (ER-897387)Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ006931Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ006931Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ034163Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ034163
Part A25902860770921276295

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Part A: t1/2 of Tazemetostat After Administration Alone and With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionhours (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6438Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6438
Part A2.883.56

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Part A: t1/2 of Tazemetostat Metabolites After Administration Alone and With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionhours (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6930 (ER-897387)Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6930 (ER-897387)Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ006931
Part A2.893.923.24

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Part A: Tmax of Tazemetostat After Administration Alone and With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionhours (Median)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6438Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6438
Part A1.132

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Part A: Tmax of Tazemetostat Metabolites After Administration Alone and With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionhours (Median)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6930 (ER-897387)Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6930 (ER-897387)Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ006931Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ006931Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ034163Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ034163
Part A2.012.022.012.472.022.02

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Part B: Cmax of Omeprazole During Co-administration With Tazemetostat

(NCT03028103)
Timeframe: Days 1 and 16, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part: B; Day 1; Treatment: Omeprazole Alone; Analyte: OmeprazolePart: B; Day 16; Treatment: Omeprazole with Tazemetostat; Analyte: Omeprazole
Part B253207

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Part B: Cmax of Repaglinide During Co-administration With Tazemetostat

(NCT03028103)
Timeframe: Days 1 and 16, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part: B; Day 1; Treatment: Repaglinide Alone; Analyte: RepaglinidePart: B; Day 16; Treatment: Repaglinide with Tazemetostat; Analyte: Repaglinide
Part B5.147.75

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Part B: Cmax of Tazemetostat During Co-administration With Omeprazole

(NCT03028103)
Timeframe: Days 16 and 19, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part: B; Day 16; Treatment: Omeprazole with Tazemetostat; Analyte: EPZ-6438Part: B; Day 19; Treatment: Tazemetostat Alone; Analyte: EPZ-6438
Part B521641

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Part B: Effect of Increased Gastric pH by Omeprazole on the PK of Tazemetostat (AUC0-t, AUC0-8)

(NCT03028103)
Timeframe: Days 16 and 19, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part: B; Day 16; Treatment: Omeprazole with Tazemetostat; Analyte: EPZ-6438 - AUC(0-t)Part: B; Day 19; Treatment: Tazemetostat Alone; Analyte: EPZ-6438 - AUC(0-t)
Part B17802150

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Part B: The Potential of Tazemetostat to Inhibit or Induce CYP2C19 Using Omeprazole as Probe a Substrate (AUC0-t, AUC0-∞)

(NCT03028103)
Timeframe: Days 1 and 16, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part: B; Day 1; Treatment: Omeprazole Alone; Analyte: Omeprazole - AUC(0-t)Part: B; Day 16; Treatment: Omeprazole with Tazemetostat; Analyte: Omeprazole - AUC(0-t)Part: B; Day 1; Treatment: Omeprazole Alone; Analyte: Omeprazole - AUC(0-∞)Part: B; Day 16; Treatment: Omeprazole with Tazemetostat; Analyte: Omeprazole - AUC(0-∞)
Part B6004806721120

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Part B: The Potential of Tazemetostat to Inhibit or Induce CYP2C8 Using Repaglinide as a Probe Substrate (AUC0-t, AUC0-∞)

(NCT03028103)
Timeframe: Days 1 and 16, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part: B; Day 1; Treatment: Repaglinide Alone; Analyte: Repaglinide - AUC(0-t)Part: B; Day 16; Treatment: Repaglinide with Tazemetostat; Analyte: Repaglinide - AUC(0-t)Part: B; Day 1; Treatment: Repaglinide Alone; Analyte: Repaglinide - AUC(0-∞)Part: B; Day 16; Treatment: Repaglinide with Tazemetostat; Analyte: Repaglinide - AUC(0-∞)
Part B8.1614.712.717

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The Antitumor Activity of Tazemetostat Will be Assessed in Patients With Diffuse Large B-cell Lymphoma (DLBCL), Marginal Zone Lymphoma (MZL), Follicular Lymphoma (FL) or Advanced Solid Tumors .

Objective response rate (ORR: complete response [CR] or PR) and disease control rate (DCR: CR or PR, or stable disease lasting 24 weeks or longer from start of treatment with tazemetostat) using Lugano Classification for subjects with lymphoma, or Response Evaluation Criteria in Solid Tumors (RECIST) v1.1 for subjects with solid tumors. (NCT03028103)
Timeframe: Within 28 days of Day 1, 8 weeks, 16 weeks, 24 weeks

,
InterventionParticipants (Count of Participants)
Complete response (CR)Partial response (PR)Stable disease (SD)Progressive disease (PD)Not evaluable, missing, or unknownObjective Response Rate (ORR)Disease control rate (DCR) at 24 weeksNumber of responders (achieving a CR or PR)
Advanced Solid Tumors02953242
Lymphoma11029222

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Part A: Exposure of Fluconazole After Administration of 400 mg Once Daily for 4 Days (AUC0-8)

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part A170000

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Part A: Cmax of Fluconazole After Administration of 400mg Once Daily for 4 Days

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part A25900

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Part A: Tmax of Fluconazole After Administration of 400mg Once Daily for 4 Days

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Interventionhours (Median)
Part A1.48

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Incidence of Treatment-emergent Adverse Events as a Measure of Safety

(NCT03028103)
Timeframe: From the first dose of study treatment until the earlier of either 30 days after the discontinuation of study treatment or until the initiation of subsequent anticancer therapy, up to 2 years.

,
InterventionParticipants (Count of Participants)
Any TEAEAny TEAE Grade 3 or 4Any Treatment-Related TEAEAny Treatment-Related TEAE Grade 3 or 4Any TEAE Leading to Dose ReductionAny TEAE Leading to Study Drug InterruptionAny TEAE Leading to Study Drug DiscontinuationAny TESAEAny Treatment-Related TESAEAny Protocol Defined AE of Special Interest
Part A12794230410
Part B148103260600

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Part A: Cmax of Tazemetostat During Co-administration With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6438Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6438
Part A426968

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Part A: Cmax of Tazemetostat Metabolites After Administration Alone and With Fluconazole

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionng/mL (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6930 (ER-897387)Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6930 (ER-897387)Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ006931Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ006931Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ034163Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ034163
Part A6295481661674647.1

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Part A: Effect of CYP3A Inhibition by Fluconazole on the PK of Tazemetostat (AUC0-t, AUC0-8)

(NCT03028103)
Timeframe: Days 15 and 19, 0 to 8 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Part: A; Day 15; Treatment: Tazemetostat Alone; Analyte: EPZ-6438Part: A; Day 19; Treatment: Tazemetostat with Fluconazole; Analyte: EPZ-6438
Part A13404100

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Sex Hormone Binding Globulin (SHBG)

Change in Serum Levels of SHBG (sex hormone binding globuline) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionnmol/L (Mean)
Tirosint Capsules0.884

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Thyroid Stimulating Hormone (TSH)

Change in Serum Levels of TSH (Thyroid Stimulating Hormone) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

InterventionmIU/L (Mean)
Tirosint Capsules-0.676

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Total Thyroxine (TT4)

Change in Serum Levels of TT4 (total thyroxine) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionnmol/L (Mean)
Tirosint Capsules2.558

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Total Triiodothyronine (TT3)

Change in Serum Levels of TT3 (total triiodothyronine) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionnmol/L (Mean)
Tirosint Capsules0.098

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Triglycerides

Change in triglycerides levels from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmmol/L (Mean)
Tirosint Capsules0.075

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Very Low Density Lipoprotein (VLDL)-Cholesterol

Change in Very Low Density Lipoprotein (VLDL)-cholesterol levels from baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmmol/L (Mean)
Tirosint Capsules0.049

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High Density Lipoprotein (HDL)-Cholesterol

Change in High Density Lipoprotein (HDL)-cholesterol levels from baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmmol/L (Mean)
Tirosint Capsules-0.029

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Ferritin

Change in Serum Levels of ferritin from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmcg/L (Mean)
Tirosint Capsules-6.442

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Free Triiodothyronine (FT3)

Change in Serum Levels of FT3 (free triiodothyronine) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionpmol/L (Mean)
Tirosint Capsules0.263

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Free Thyroxine (FT4)

Change in Serum Levels of FT4 (free thyroxine) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionpmol/L (Mean)
Tirosint Capsules0.593

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Angiotensin Converting Enzyme (ACE)

Change in Serum Levels of ACE (angiotensin converting enzyme) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

InterventionU/L (Mean)
Tirosint Capsules-0.395

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Cholesterol, Total

Change in total cholesterol levels from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmmol/L (Mean)
Tirosint Capsules-0.198

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Creatine Phosphokinase (CPK)

Change in Serum Levels of creatine phosphokinase (CPK) from Baseline (NCT03094416)
Timeframe: baseline and 12 weeks

InterventionU/L (Mean)
Tirosint Capsules-35.073

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Low Density Lipoprotein (LDL)-Cholesterol

Change in low density lipoprotein (LDL)-cholesterol levels from baseline (NCT03094416)
Timeframe: baseline and 12 weeks

Interventionmmol/L (Mean)
Tirosint Capsules-0.210

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Area Under the Concentration (AUC 0-t)

Time curve from time zero to last measurable concentration. Measurement of plasma nifedipine prior to dosing and at times 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 20, 24, 36 and 48 hr after nifedipine administration. (NCT03100838)
Timeframe: 48 hours

Interventionng.h/mL (Mean)
Nifedipine (Generic)1166.21
Nifedipine (Brand)1061.49
Nifedipine (Generic) + PPI1514.83
Nifedipine (Brand) + PPI1239.26

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Adverse Events

Reported from the start of the first session to the follow-up visit. (NCT03100838)
Timeframe: 66 days

InterventionEvents (Number)
Nifedipine (Generic)37
Nifedipine (Brand)19
Nifedipine (Generic) + PPI51
Nifedipine (Brand) + PPI38

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Time at Maximum Plasma Concentration (Tmax)

Measurement of plasma nifedipine prior to dosing and at times 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 20, 24, 36 and 48 hr after nifedipine administration. (NCT03100838)
Timeframe: 48 hours

Interventionhr (Mean)
Nifedipine (Generic)4
Nifedipine (Brand)16
Nifedipine (Generic) + PPI6
Nifedipine (Brand) + PPI16

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Maximum Plasma Concentration (Cmax)

Measurement of plasma nifedipine prior to dosing and at times 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 20, 24, 36 and 48 hr after nifedipine administration. (NCT03100838)
Timeframe: 48 hours

Interventionng/mL (Mean)
Nifedipine (Generic)94.37
Nifedipine (Brand)43.84
Nifedipine (Generic) + PPI106.35
Nifedipine (Brand) + PPI51.65

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Half-life

The apparent terminal exponential half-life. Measurement of plasma nifedipine prior to dosing and at times 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 20, 24, 36 and 48 hr after nifedipine administration. (NCT03100838)
Timeframe: 48 hours

Interventionhr (Mean)
Nifedipine (Generic)8.59
Nifedipine (Brand)11.29
Nifedipine (Generic) + PPI8.10
Nifedipine (Brand) + PPI12.71

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Number of Participants With Eradication of H. Pylori in the Pharmacokinetic Population (PKP)

"A pre-specified responder analysis of eradication of H. pylori confirmed via 13C Urea Breath Test (UBT) was performed in the PK population.~The PK population was generated based on the measurement of plasma concentrations of amoxicillin, omeprazole, rifabutin, and the rifabutin metabolite 25-O-desacetyl-rifabutin (on Day 13). It included those subjects in the FAS who had demonstrable presence of any component of investigational drug at Visit 3 or had no levels detected >250 hours after the last dose. For all subjects, the reason for exclusion from the PKP was the absence of any pharmacokinetic component of study drug at Visit 3 within 250 hours of the last reported dose. Two hundred fifty hours was selected to account for approximately 10 times the terminal half-life of rifabutin." (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
RHB-105187
Active Comparator119

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Number of Participants With Eradication of H. Pylori

Eradication of H. pylori confirmed via 13C Urea Breath Test (UBT) testing. Subjects with negative test results (eradication of H. pylori) were considered treatment successes. Subjects who tested positive for H. pylori infection (no eradication) were considered treatment failures. (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
RHB-105191
Active Comparator131

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Number of Participants With H. Pylori Cultures That Presented Antibiotic Resistance and Susceptibility

"The primary endpoint was summarized within subgroups formed by the presence of H. pylori susceptibility and resistance to amoxicillin, clarithromycin, metronidazole, and rifabutin from H. pylori cultures from samples obtained prior to initiating study treatment (i.e. baseline).~A participant is considered a responder when H. pylori is eradicated after treatment as confirmed via 13C Urea Breath Test (UBT). A participant is considered a non-responder when H. pylori is not eradicated after treatment." (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
Rifabutin resistant72525830Rifabutin resistant72525831Rifabutin Susceptible72525830Rifabutin Susceptible72525831Amoxicillin Resistant72525830Amoxicillin Resistant72525831Amoxicillin Susceptible72525830Amoxicillin Susceptible72525831Clarithromycin Resistant72525831Clarithromycin Resistant72525830Clarithromycin Susceptible72525831Clarithromycin Susceptible72525830Metronidazole Resistant72525830Metronidazole Resistant72525831Metronidazole Susceptible72525830Metronidazole Susceptible72525831
ResponderNon-responder
RHB-1050
Active Comparator0
RHB-105147
Active Comparator99
RHB-10527
Active Comparator72
RHB-1059
Active Comparator4
Active Comparator5
RHB-105138
Active Comparator95
Active Comparator67
RHB-10521
Active Comparator22
RHB-1054
Active Comparator13
RHB-105126
Active Comparator77
RHB-10523
Active Comparator59
RHB-10557
Active Comparator45
RHB-10514
Active Comparator34
RHB-10590
Active Comparator53
RHB-10513
Active Comparator38

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Change in Peak Intensity of the Metabolite 1H-Indole-4-carbaldehyde Before and After VSL#3 Probiotic Administration (Omeprazole and VSL #3).

"From week 0 to week 4, relative change in metabolites (e.g. short chain fatty acids, bile acid derivatives, flavonoids, amino acids) found in the GI track by mass spectrometry after ingesting VSL#3. Serum samples are assessed.~MZ = mass/charge ratio; RT = retention time. MZ/RT data were obtained by mass spectrometry analysis. This is a metabolite of interest for the Omeprazole and VSL#3 group only." (NCT03327051)
Timeframe: Week 0 and Week 4

InterventionMZ/RT (Mean)
1H-Indole-4-carbaldehyde at Week 01H-Indole-4-carbaldehyde at Week 4
Omeprazole and VSL #380809.5286707.9

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Relative Abundance of VSL#3 Probiotic Bacterial Strains When Ingested in the Presence or Absence of the Proton Pump Inhibitor (PPI) Omeprazole at Week 4.

Relative abundance is reported as the percent of combined VSL #3 probiotic bacteria strains in the bacteria sample (S. thermophiles, B. breve, B. longum, B. infantis, L. acidophilus, L. plantarum, L. paracasei, L. delbrueckii subsp. bulgaricus) following their ingestion in the presence or absence of the gastric acid suppression drug omeprazole. Stool samples were assessed. (NCT03327051)
Timeframe: Week 4

Interventionpercentage of abundance (Mean)
Omeprazole and VSL #31.002
Placebo and VSL #30.8186

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Change in Peak Intensity of Metabolites of Interest Before and After VSL#3 Probiotic Administration (Placebo and VSL#3 Group).

"From week 0 to week 4, relative change in metabolites (e.g. short chain fatty acids, bile acid derivatives, flavonoids, amino acids) found in the GI track by mass spectrometry after ingesting VSL#3. Serum samples are assessed.~MZ = mass/charge ratio; RT = retention time. MZ/RT data were obtained by mass spectrometry analysis. These are metabolites of interest for the Placebo and VSL#3 group only." (NCT03327051)
Timeframe: Week 0 and Week 4

InterventionMZ/RT (Mean)
11-OXOURSOLIC ACID ACETATE at Week 011-OXOURSOLIC ACID ACETATE at Week 4FA(14:0) at Week 0FA(14:0) at Week 4Iloprost S-isomer at Week 0Iloprost S-isomer at Week 4
Placebo and VSL #395819.84726.2539032.9249632.387765.622405.5

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Relative Abundance (Mean Value) of Most Abundant Bacterial Phylum Before and After VSL#3 Probiotic Administration

From week 0 to week 4, change in the relative abundance (percentage) of most common types of bacteria phyla normally found in the lower GI track (e.g. Firmicutes, Bacteroidetes, Actinobacteria and Proteobacteria) after ingesting VSL#3 in the presence or absence of omeprazole. Stool samples are assessed. (NCT03327051)
Timeframe: Week 0 and Week 4

,
Interventionpercentage of abundance (Mean)
Bacteroidetes at Week 0Bacteroidetes at Week 4Firmicutes at Week 0Firmicutes at Week 4Proteobacteria at Week 0Proteobacteria at Week 4Actinobacteria at Week 0Actinobacteria at Week 4
Omeprazole and VSL #366.466.225.625.74.13.122.53.7
Placebo and VSL #365.668.127.225.02.72.73.23.2

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Maximum Observed Concentration (Cmax) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionNanograms/milliliter (Geometric Mean)
600RC High Fat761.5
475DC High Fat712.8
600DC High Fat762.3
600DC 5%HPMC High Fat659.2
600RC Fasted2708.2
475DC Fasted2418.5
600DC Fasted2607.1
600DC 5%HPMC Fasted2511.8

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Maximum Observed Concentration (Cmax) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionNanograms/milliliter (Geometric Mean)
475DC-Fasted2317.4
475DC-Normal Meal989.9
475DC-High Fat969.9
475DC-MONO High Fat1019.8
475DC Fasted OMP2292.5
475DC Normal Meal OMP1389.7
475DC High Fat OMP1132.5

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Number of Participants With 12-lead Electrocardiogram (ECG) Values of Potential Clinical Concern in Part 1

Single 12-lead ECGs were obtained using an ECG machine that automatically calculated the heart rate and measured PR, QRS, and QT intervals, and QT interval corrected by Fridericia's formula (QTcF). Number of participants with 12-lead ECG values of potential clinical concern in Part 1 are presented. (NCT03457727)
Timeframe: Up to 29 days in Part 1

InterventionParticipants (Count of Participants)
600RC High Fat1
475DC High Fat2
600DC High Fat2
600DC 5%HPMC High Fat2
600RC Fasted2
475DC Fasted1
600DC Fasted2
600DC 5%HPMC Fasted1

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Number of Participants With Laboratory Values of Potential Clinical Concern in Part 1

Hematology parameters included platelet count, RBC Count, hemoglobin, hematocrit, MCV, MCH, %Reticulocytes, neutrophils, lymphocytes, monocytes, eosinophils, basophils. Clinical chemistry parameters included potassium aspartate aminotransferase(AST)/Serum Glutamic-Oxaloacetic Transaminase (SGOT), total and direct bilirubin, creatinine, sodium alanine, aminotransferase, (ALT)/ Serum Glutamic-Pyruvic, Transaminase (SGPT), total protein, fasting glucose, calcium, alkaline phosphatase and albumin. Urinalysis included specific gravity, potential of hydrogen (pH), glucose, protein, blood and ketones by dipstick and microscopic examination of urine. (NCT03457727)
Timeframe: Up to 29 days in Part 1

InterventionParticipants (Count of Participants)
600RC High Fat0
475DC High Fat0
600DC High Fat0
600DC 5%HPMC High Fat0
600RC Fasted0
475DC Fasted0
600DC Fasted1
600DC 5%HPMC Fasted0

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Number of Participants With Laboratory Values of Potential Clinical Concern in Part 2

Hematology parameters included platelet count, RBC Count, hemoglobin, hematocrit, MCV, MCH, %Reticulocytes, neutrophils, lymphocytes, monocytes, eosinophils, basophils. Clinical chemistry parameters included potassium aspartate, Aminotransferase(AST)/Serum Glutamic-Oxaloacetic Transaminase (SGOT), total and direct, bilirubin, creatinine sodium alanine, Aminotransferase, (ALT)/ Serum Glutamic-Pyruvic, Transaminase (SGPT), total protein, fasting glucose, calcium, alkaline phosphatase and albumin. Urinalysis included specific gravity, potential of hydrogen (pH), glucose, protein, blood and ketones by dipstick and microscopic examination of urine. (NCT03457727)
Timeframe: Up to 52 days in Part 2

InterventionParticipants (Count of Participants)
475DC-Fasted0
475DC-Normal Meal0
475DC-High Fat0
475DC-MONO High Fat0
475DC Fasted OMP0
475DC Normal Meal OMP0
475DC High Fat OMP1

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Time to Occurrence of Cmax (Tmax) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours (Mean)
600RC High Fat3.897
475DC High Fat3.653
600DC High Fat3.585
600DC 5%HPMC High Fat4.158
600RC Fasted1.165
475DC Fasted1.331
600DC Fasted1.214
600DC 5%HPMC Fasted1.342

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Number of Participants With Any Adverse Event (AE) and Serious Adverse Events in Part 2

AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. (NCT03457727)
Timeframe: Up to 52 days in Part 2

,,,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
475DC Fasted OMP00
475DC High Fat OMP30
475DC Normal Meal OMP00
475DC-Fasted10
475DC-High Fat10
475DC-MONO High Fat00
475DC-Normal Meal10

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Number of Participants With Any Adverse Event (AE) and Serious Adverse Events (SAEs) in Part 1

AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. An SAE is any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect or is medically significant. (NCT03457727)
Timeframe: Up to 29 days in Part 1

,,,,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
475DC Fasted10
475DC High Fat00
600DC 5%HPMC Fasted10
600DC 5%HPMC High Fat00
600DC Fasted10
600DC High Fat00
600RC Fasted20
600RC High Fat10

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Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours (Mean)
600RC High Fat0.323
475DC High Fat0.383
600DC High Fat0.383
600DC 5%HPMC High Fat0.511
600RC Fasted0.000
475DC Fasted0.065
600DC Fasted0.000
600DC 5%HPMC Fasted0.000

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Number of Participants With 12-lead Electrocardiogram (ECG) Values of Potential Clinical Concern in Part 2

Single 12-lead ECGs were obtained using an ECG machine that automatically calculated the heart rate and measured PR, QRS, and QT intervals, and QT interval corrected by Fridericia's formula (QTcF). Number of participants with 12-lead ECG values of potential clinical concern in Part 2 are presented. (NCT03457727)
Timeframe: Up to 52 days in Part 2

InterventionParticipants (Count of Participants)
475DC-Fasted1
475DC-Normal Meal2
475DC-High Fat1
475DC-MONO High Fat3
475DC Fasted OMP1
475DC Normal Meal OMP2
475DC High Fat OMP2

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Time to Maximum Observed Concentration (Tmax) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours (Geometric Mean)
475DC-Fasted1.271
475DC-Normal Meal3.749
475DC-High Fat4.150
475DC-MONO High Fat3.355
475DC Fasted OMP1.978
475DC Normal Meal OMP2.887
475DC High Fat OMP3.752

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Time to Last Quantifiable Concentration (Tlast) of the Blood Concentration of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours (Geometric Mean)
475DC-Fasted45.139
475DC-Normal Meal47.144
475DC-High Fat47.200
475DC-MONO High Fat46.741
475DC Fasted OMP45.217
475DC Normal Meal OMP45.242
475DC High Fat OMP40.869

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Time to Last Quantifiable Concentration (Tlast) of the Blood Concentration of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours (Mean)
600RC High Fat47.660
475DC High Fat47.587
600DC High Fat44.657
600DC 5%HPMC High Fat44.757
600RC Fasted44.372
475DC Fasted41.789
600DC Fasted41.699
600DC 5%HPMC Fasted44.531

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Terminal Half-life (t1/2) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours (Geometric Mean)
475DC-Fasted10.647
475DC-Normal Meal11.424
475DC-High Fat11.484
475DC-MONO High Fat11.652
475DC Fasted OMP11.304
475DC Normal Meal OMP10.913
475DC High Fat OMP8.975

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Terminal Half-life (t1/2) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours (Geometric Mean)
600RC High Fat9.638
475DC High Fat10.904
600DC High Fat8.916
600DC 5%HPMC High Fat9.888
600RC Fasted8.298
475DC Fasted9.498
600DC Fasted9.391
600DC 5%HPMC Fasted9.107

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Number of Participants With Vital Signs of Potential Clinical Concern in Part 2

Vital signs included systolic and diastolic blood pressure, temperature, respiratory rate and pulse rate were measured with participants in semi-supine position after 5 minutes rest. (NCT03457727)
Timeframe: Up to 52 days in Part 2

InterventionParticipants (Count of Participants)
475DC-Fasted2
475DC-Normal Meal3
475DC-High Fat4
475DC-MONO High Fat4
475DC Fasted OMP4
475DC Normal Meal OMP3
475DC High Fat OMP4

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Number of Participants With Vital Signs of Potential Clinical Concern in Part 1

Vital signs included systolic and diastolic blood pressure, temperature, respiratory rate and pulse rate were measured with participants in semi-supine position after 5 minutes rest. (NCT03457727)
Timeframe: Up to 29 days in Part 1

InterventionParticipants (Count of Participants)
600RC High Fat2
475DC High Fat2
600DC High Fat2
600DC 5%HPMC High Fat2
600RC Fasted0
475DC Fasted0
600DC Fasted0
600DC 5%HPMC Fasted0

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Lag Time Before Observable Concentration (Tlag) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours (Geometric Mean)
475DC-Fasted0.000
475DC-Normal Meal0.283
475DC-High Fat0.641
475DC-MONO High Fat0.386
475DC Fasted OMP0.000
475DC Normal Meal OMP0.423
475DC High Fat OMP0.370

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Area Under the Concentration-time Curve From Time 0 to t (AUC [0-t]) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours*nanograms/milliliter (Geometric Mean)
475DC-Fasted12026.9
475DC-Normal Meal7484.2
475DC-High Fat7757.2
475DC-MONO High Fat6986.9
475DC Fasted OMP12903.9
475DC Normal Meal OMP9023.8
475DC High Fat OMP7885.4

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Area Under the Concentration-time Curve From Time 0 to t (AUC [0-t]) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours*nanograms/milliliter (Geometric Mean)
600RC High Fat5515.9
475DC High Fat5573.6
600DC High Fat5524.7
600DC 5%HPMC High Fat5287.0
600RC Fasted11480.1
475DC Fasted10977.2
600DC Fasted10636.5
600DC 5%HPMC Fasted11015.8

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Area Under the Concentration-time Curve From Time 0 to Infinity (AUC [0-inf]) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours*nanograms/milliliter (Geometric Mean)
475DC-Fasted12426.4
475DC-Normal Meal7761.2
475DC-High Fat8136.7
475DC-MONO High Fat7356.4
475DC Fasted OMP14615.2
475DC Normal Meal OMP10185.0
475DC High Fat OMP8782.5

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Area Under the Concentration-time Curve From Time 0 to Infinity (AUC [0-inf]) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the pharmacokinetic (PK) profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours*nanograms per milliliter (Geometric Mean)
600RC High Fat6166.7
475DC High Fat6052.9
600DC High Fat5816.4
600DC 5%HPMC High Fat5996.1
600RC Fasted11394.6
475DC Fasted11285.7
600DC Fasted10957.4
600DC 5%HPMC Fasted11230.8

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Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose (AUC [0-24]) of Danirixin for Part 1

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 1

InterventionHours*nanograms/milliliter (Geometric Mean)
600RC High Fat4919.5
475DC High Fat4952.0
600DC High Fat4984.8
600DC 5%HPMC High Fat4705.2
600RC Fasted10744.8
475DC Fasted10419.9
600DC Fasted10029.3
600DC 5%HPMC Fasted10319.9

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Area Under the Concentration-time Curve From Time 0 to 24 Hours (AUC [0-24]) of Danirixin for Part 2

Blood samples were collected at the indicated time points after administration of study treatment to investigate the PK profile of Danirixin. PK parameters were calculated by standard non-compartmental analysis using WinNonlin based on actual sampling times. (NCT03457727)
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48 hours in Part 2

InterventionHours*nanograms/milliliter (Geometric Mean)
475DC-Fasted11096.7
475DC-Normal Meal6482.2
475DC-High Fat6706.6
475DC-MONO High Fat6187.1
475DC Fasted OMP12762.9
475DC Normal Meal OMP8681.0
475DC High Fat OMP7590.8

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Pharmacokinetics: Cmax of KD025m1 in Part 1

Maximum concentration (Cmax) of Metabolite 1 (KD025m1) for belumosudil alone and for belumosudil + rifampicin up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

Interventionng/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone23.2
Part 1, Period 4: Belumosudil + Rifampicin52.5

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Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2

Area under concentration-time curve from zero hours to 24 hours post-dose (AUC[0-24]) for Metabolite 1, KD025m1, for subjects in Part 1 and for subjects in Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12, and 24 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22, and 24 hours post-dose

Intervention(ng*h)/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone75.6
Part 1, Period 4: Belumosudil + Rifampicin148
Part 2, Period 1: Belumosudil Alone138
Part 2, Period 2: Belumosudil + Omeprazole91.5

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Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2

Area under concentration-time curve from zero hours to infinity (AUC[0-inf]) and from zero hours to 24 hours post-dose (AUC[0-24)) for the parent drug KD025, and Metabolite 2, KD025m2, for subjects up to 48 hours each for Part 1 and for Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,,,,,
Intervention(ng*h)/mL (Geometric Mean)
AUC(0-inf): KD025AUC(0-inf): KD025m2AUC(0-24): KD025AUC(0-24): KD025m2
Part 1, Period 1: Belumosudil Alone9080123084301100
Part 1, Period 2: Belumosudil + Itraconazole1120084310400745
Part 1, Period 3: Belumosudil + Rabeprazole16801741510110
Part 1, Period 4: Belumosudil + Rifampicin25003962490376
Part 2, Period 1: Belumosudil Only188001900168001950
Part 2, Period 2: Belumosudil + Omeprazole988011107970767

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Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1

Maximum concentration (Cmax) of the parent drug, KD025, Metabolite 1 (KD025m1), and Metabolite 2 (KD025m2) for belumosudil alone, belumosudil + itraconazole, belumosudil + rabeprazole, and belumosudil + rifampicin at 0 to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

,,,
Interventionng/mL (Geometric Mean)
Parent Drug KD025KD025m2
Part 1, Period 1: Belumosudil Alone1770337
Part 1, Period 2: Belumosudil + Itraconazole2130221
Part 1, Period 3: Belumosudil + Rabeprazole22723.5
Part 1, Period 4: Belumosudil + Rifampicin712148

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Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2

Maximum concentration (Cmax) of the parent drug (KD025), for Metabolite 1 (KD025m1), and for Metabolite 2 (KD025m2), for belumosudil alone and for belumosudil + omeprazole up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,
Interventionng/mL (Geometric Mean)
Cmax--1st dose: KD025Cmax--2nd dose: KD025Cmax--1st Dose: KD025m1Cmax--2nd Dose: KD025m1Cmax--1st Dose: KD025m2Cmax--2nd Dose: KD025m2
Part 2, Period 1: Belumosudil Alone1790176023.823.6282257
Part 2, Period 2: Belumosudil + Omeprazole57590318.018.972.3115

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Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment A and Treatment C

AUC0-inf was calculated by combining AUC0-t and AUCextra. AUC extra represents an extrapolated value obtained by Clast/Lambda z, where Clast is the calculated plasma concentration at the last sampling time point at which the measured plasma concentration is at or above the Lower Limit of quantification (LLOQ) and Lambda z is the apparent terminal rate constant determined by log-linear regression analysis of the measured plasma concentrations of the terminal log-linear phase. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment C)

Interventionh*ng/mL (Geometric Mean)
Treatment A23081
Treatment C25343

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Apparent Volume of Distribution During Terminal Phase (Vz/f) of Tepotinib in Treatments A, B and C

Vz/f is defined as the distribution of a study drug between plasma and the rest of the body after oral dosing. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment B and C)

InterventionLiters (Geometric Mean)
Treatment A912
Treatment B1181
Treatment C860

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Apparent Total Body Clearance (CL/f) of Tepotinib in Treatments A, B and C

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment B and C)

InterventionLiter per hour (L/h) (Geometric Mean)
Treatment A19.5
Treatment B25.8
Treatment C17.8

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Apparent Terminal Half-life (t1/2) of Tepotinib in Treatments A, B and C

Terminal half-life is the time measured for the concentration to decrease by one half. Terminal half-life calculated by natural log 2 divided by lambda z. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment B and C)

Interventionhour (Median)
Treatment A32.9
Treatment B30.7
Treatment C31.7

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Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment B

Area under the plasma concentration versus time curve from time zero to the last sampling time t at which the concentration was at or above the lower limit of quantification (LLOQ). AUC0-t was to be calculated according to the mixed log-linear trapezoidal rule. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 5 for Treatment B

Interventionh*ng/mL (Geometric Mean)
Treatment B16220

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Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment A and Treatment C

Cmax was obtained directly from the concentration versus time curve. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment C)

InterventionNanogram per milliliter (ng/mL) (Geometric Mean)
Treatment A428
Treatment C445

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Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment B

AUC0-inf was calculated by combining AUC0-t and AUCextra. AUC extra represents an extrapolated value obtained by Clast/Lambda z, where Clast is the calculated plasma concentration at the last sampling time point at which the measured plasma concentration is at or above the Lower Limit of quantification (LLOQ) and Lambda z is the apparent terminal rate constant determined by log-linear regression analysis of the measured plasma concentrations of the terminal log-linear phase. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 5 for Treatment B

Interventionh*ng/mL (Geometric Mean)
Treatment B17412

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Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment A and Treatment C

Area under the plasma concentration versus time curve from time zero to the last sampling time t at which the concentration was at or above the lower limit of quantification (LLOQ). AUC0-t was to be calculated according to the mixed log-linear trapezoidal rule. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment C)

InterventionHour*nanogram per milliliter (h*ng/mL) (Geometric Mean)
Treatment A21722
Treatment C23649

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Number of Participants With Clinically Significant Changes in Laboratory Parameters, 12-lead Electrocardiogram (ECG) Findings and Vital Signs

The laboratory measurements included hematology, biochemistry, virology, drugs of abuse, hormones, and urinalysis. ECG recordings included PR, QRS, RR, QT and corrected QT intervals (QTcF). Vital sign assessment included blood pressure, pulse rate, body temperature. Number of participants with clinically significant abnormalities in laboratory parameters, 12-lead ECG findings, vital signs were reported. Clinically significance was decided by investigator. (NCT03531762)
Timeframe: Baseline up to Day 4 for Treatment A and up to Day 8 for Treatment B and C

,,
InterventionParticipants (Count of Participants)
Laboratory Parameters12-lead Electrocardiogram (ECG) FindingsVital Signs
Treatment A000
Treatment B000
Treatment C000

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Time to Reach Maximum Plasma Concentration (Tmax) of Tepotinib in Treatments A, B and C

Time to reach the maximum plasma concentration (Tmax) was obtained directly from the concentration versus time curve. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 1 (for Treatment A) and on Day 5 (for Treatment B and C)

InterventionHours (Median)
Treatment A8.0
Treatment B12.0
Treatment C8.0

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Number of Participants With Treatment-emergent Adverse Events (TEAEs)

An Adverse event (AE) was defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease associated with the use of study drug, whether/not considered related to the study drug or worsening of pre-existing medical condition, whether or not related to study drug. A serious adverse event (SAE) was an AE that resulted in any of the following outcomes: death; life threatening; persistent/significant disability/incapacity; initial or prolonged inpatient hospitalization; congenital anomaly/birth defect or was otherwise considered medically important. An AE was considered as 'treatment emergent' if it occurred after the first drug administration or if it was present prior to drug administration but exacerbated after the drug administration. TEAEs included both serious TEAEs and non-serious TEAEs. (NCT03531762)
Timeframe: Baseline up to Day 7 for Treatment A and up to Day 11 for Treatment B and C

InterventionParticipants (Count of Participants)
Treatment A1
Treatment B3
Treatment C1

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Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment B

Cmax was obtained directly from the concentration versus time curve. (NCT03531762)
Timeframe: Pre-dose, 15, 30, 45, 60, 90 minutes, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120 and 144 hour post-dose on Day 5 for Treatment B

Interventionng/mL (Geometric Mean)
Treatment B227

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Score of Difficulty in Swallowing Food, Fluids or Pills of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including difficulty in swallowing food, fluids or pills that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole1.90.4
Omeprazole1.90.6

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Score of Difficulty in Breathing or Episodes of Choking of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including difficulty in breathing or episodes of choking that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole1.50.5
Omeprazole1.90.6

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Score of Cough of the RSI Questionnaire Measured at Baseline and in the Visit 4 After the Meal or After Lying

The Reflux Symptom Index questionnaire examines 9 items, including cough that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole2.50.7
Omeprazole3.31.7

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Presence of Upper Symptoms at Visit 4, Using the RSI Questionnaire

The Reflux Symptom Index questionnaire examines 9 items, to be scored from 0 to 5, with a higher score indication a higher severity of the symptom (range of total score: 0-45). (NCT03793556)
Timeframe: At visit 4 after weeks of treatment

,
InterventionParticipants (Count of Participants)
Missing1 symptom2 symptoms3 symptoms4 symptoms5 symptoms6 symptoms
GERDOFF® + Omeprazole17613400
Omeprazole42911721

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Change From Baseline to Visit V4 of the Total Score of RSI Questionnaire

After 6 weeks of treatment, the changes from baseline in the score of Reflux Symptom Index questionnaire were evaluated to verify the effects of treatments on high symptoms. The RSI questionnaire examines 9 items that are scored from 0 to 5, with a higher score that indicates a higher severity of the symptom (range of total score: 0-45). (NCT03793556)
Timeframe: In the first visit (baseline) and in the visit 4 (after 6 weeks of treatment)

InterventionScore on a scale (Mean)
GERDOFF® + Omeprazole-16.2
Omeprazole-13.7

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Patients'Satisfaction

This evaluation was expressed with a semi-quantitative ordinal scale: 0 = low, 1 = discrete, 2 = good, 3 = excellent). (NCT03793556)
Timeframe: At visit 4 after weeks of treatment

,
InterventionParticipants (Count of Participants)
MissingLowDiscreteGoodExcellent
GERDOFF® + Omeprazole1311115
Omeprazole0171117

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Total Score of Reflux Symptom Index Questionnaire in All Time-points Assessed

"Total score of the Reflux Symptom Index questionnaire assessed in all time-points.~The RSI questionnaire examines 9 items, that are scored from 0 to 5, with a higher score that indicates a higher severity of the symptom (range of total score: 0-45)." (NCT03793556)
Timeframe: In baseline Visit, Visit 2 (after 1 week), Visit 3 (after 3 weeks) and Visit 4 (after 6 weeks of treatment)

,
Interventionscore on a scale (Mean)
BaselineVisit 2Visit 3Visit 4
GERDOFF® + Omeprazole24.215.312.97.9
Omeprazole26.019.615.312.3

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Score of Upper Symptoms Using the Likert Scale at Baseline and in the Visit V4

"The Likert scale examines 9 symptoms, to be scored from 0 to 4, with a higher score indication a higher frequency of the symptom (i.e. 0=never, 1=occasionally, 2=sometimes, 3= often, 4=Always);~The Likert scale scores of single items are as following:~Hoarseness or vocal problem 0 1 2 3 4~Throat clearance 0 1 2 3 4~Excess of mucus in the throat or retrosternal fall of secretions 0 1 2 3 4~Difficulty in swallowing food, fluids or pills 0 1 2 3 4~Cough after the meal or after lying 0 1 2 3 4~Difficulty in breathing or episodes of choking 0 1 2 3 4~Problematic or troublesome cough 0 1 2 3 4~Sensation of something blocked or mass in the throat 0 1 2 3 4~Stomach burning, thoracic pain, poor digestion of gastric acid that moves upright 0 1 2 3 4.~Subscales are summarized to compute a total score (total score ranges from 0-36). The mean values of Likert scale total score are reported." (NCT03793556)
Timeframe: At baseline and in the visit 4

,
InterventionScore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole19.07.4
Omeprazole2111.6

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Score of Throat of the RSI Questionnarie Measured at the Baseline and in the Visit 4 of the RSI Questionnaire Score of Throat Clearance

The Reflux Symptom Index questionnaire examines 9 items, including throat that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole3.41.4
Omeprazole3.61.8

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Score of Stomach Burning, Thoracic Pain, Poor Digestion of Gastric Acid That Moves Upright of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including stomach burning, thoracic pain, poor digestion of gastric acid that moves upright that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
InterventionScore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole3.40.8
Omeprazole3.53.5

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Score of Sensation of Something Blocked or Mass in the Throat of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including sensation of something blocked or mass in the throat that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole3.00.8
Omeprazole2.61.6

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Score of Problematic or Troublesome Cough of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including problematic or troublesome cough that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole2.50.8
Omeprazole3.71.5

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Score of Hoarseness or Vocal Problem of the RSI Questionnaire Measured at the Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including hoarseness or vocal problem that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole3.21.1
Omeprazole2.81.6

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Score of Excess of Mucus in the Throat or Retrosternal Fall of Secretions of the RSI Questionnaire Measured at Baseline and in the Visit 4

The Reflux Symptom Index questionnaire examines 9 items, including excess of mucus in the throat or retrosternal fall of secretions that is score from 0 to 5, with a higher score that indicates a higher severity of the symptom. (NCT03793556)
Timeframe: At baseline and in the visit 4, after 6 weeks of treatment

,
Interventionscore on a scale (Mean)
BaselineVisit 4
GERDOFF® + Omeprazole2.71.4
Omeprazole2.81.9

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Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Anagrelide (SPD422) in Plasma

AUC(0-infinity) of Anagrelide (SPD422) in plasma on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionh*ng/mL (Mean)
SPD422 (Day 1)13.54
SPD422 + Omeprazole (Day 8)10.27

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Area Under the Concentration Versus Time Curve From Zero to Last Time Point (AUC[0-t]) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide) in Plasma

AUC(0-t) of 3-OH-Anagrelide (Active Metabolite of Anagrelide) in Plasma on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionh*ng/mL (Mean)
SPD422 (Day 1)39.51
SPD422 + Omeprazole (Day 8)33.14

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Maximum Observed Plasma Concentration (Cmax) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide)

Cmax of 3-OH-Anagrelide (Active Metabolite of Anagrelide) on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionng/mL (Mean)
SPD422 (Day 1)10.30
SPD422 + Omeprazole (Day 8)8.341

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Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of 3-Hydroxy (OH)-Anagrelide (Active Metabolite of Anagrelide) in Plasma

AUC(0-infinity) of 3-OH-Anagrelide (Active Metabolite of Anagrelide) in Plasma on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionh*ng/mL (Mean)
SPD422 (Day 1)40.85
SPD422 + Omeprazole (Day 8)35.51

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Maximum Observed Plasma Concentration (Cmax) of Anagrelide (SPD422)

Cmax of Anagrelide (SPD422) on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionnanogram per milliliter (ng/mL) (Mean)
SPD422 (Day 1)5.028
SPD422 + Omeprazole (Day 8)3.180

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Area Under the Concentration Versus Time Curve From Zero to Last Time Point (AUC[0-t]) of Anagrelide (SPD422) in Plasma

AUC(0-t) of Anagrelide (SPD422) in plasma on Day 1 and Day 8 was reported. For PK outcome measures the reporting groups were split based on administration of Anagrelide alone (Day 1) and Anagrelide in combination with Omeprazole (Day 8) to provide statistical comparison in this single arm study. (NCT03866434)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 8, 12 hours on Day 1 and Day 8, 24 hours on Day 8

Interventionhour*nanogram per milliliter (h*ng/mL) (Mean)
SPD422 (Day 1)13.25
SPD422 + Omeprazole (Day 8)9.683

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Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Treatment Emergent Serious Adverse Events (TESAEs)

An adverse event (AE) was any untoward medical occurrence in a clinical investigation participant administered a pharmaceutical product and that does not necessarily had a causal relationship with this treatment. An AE was considered a TEAE if it started on or after dosing on Day 1 or if it started before dosing on Day 1 but increased in severity on or after dosing on Day 1 through the end of the study. Number of participants with TEAEs and TESAEs were reported. (NCT03866434)
Timeframe: From start of study drug administration up to follow-up (up to Day 18)

InterventionParticipants (Count of Participants)
Treatment Emergent Adverse Events (TEAEs)Treatment Emergent Serious Adverse Events (TESAEs)
SPD422 + Omeprazole90

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Insulin

Change in insulin concentration - incremental area under the insulin concentration-time curve from 0 to 12 h (NCT04198948)
Timeframe: 12 hours

InterventionmIU x h/L (Mean)
Gliclazide + Omeprazole231.6
Gliclazide + Placebo265.9

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Gliclazide AUC

Area under the concentration-time curve (AUC) up to the last concentration measured (NCT04198948)
Timeframe: 24 hours

Interventionμgh/mL (Geometric Mean)
Gliclazide + Omeprazole3.73
Gliclazide + Placebo3.29

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Glucose

Change in glucose concentration - incremental area under the glucose concentration-time curve from 0 to 12 h (NCT04198948)
Timeframe: 12 hours

Interventionmmol x h/L (Mean)
Gliclazide + Omeprazole4.6
Gliclazide + Placebo4.0

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Treatment A: Absolute Values for Electrocardiogram (ECG) Parameters: PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Fridericia's Formula (QTcF)

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-Dose) and Day 10

InterventionMilliseconds (Mean)
Baseline (Day 1, Pre-dose): PR IntervalDay 10: PR IntervalBaseline (Day 1, Pre-dose): QRS DurationDay 10: QRS DurationBaseline (Day 1, Pre-dose): QT IntervalDay 10: QT IntervalBaseline (Day 1, Pre-dose): QTcF IntervalDay 10: QTcF Interval
Treatment A: Probe Substrates154.8158.292.595.0391.2398.3401.0405.8

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. SAE was defined as any untoward medical occurrence that, at any dose, results in death, was life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect and other situations according to medical or scientific judgement. (NCT04425902)
Timeframe: Up to Day 26

,,
InterventionParticipants (Count of Participants)
AEsSAEs
Treatment A: Probe Substrates10
Treatment B: GSK3640254 200 mg50
Treatment C: Probe Substrates + GSK3640254 200 mg50

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Treatment C: Tmax for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

InterventionHours (Median)
Treatment C: Probe Substrates + GSK3640254 200 mg4.500

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Treatment C: t1/2 for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

InterventionHours (Geometric Mean)
Treatment C: Probe Substrates + GSK3640254 200 mg29.556

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Treatment C: Plasma Concentration at the End of the Dosing Interval (Ctau) for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

Interventionng/mL (Geometric Mean)
Treatment C: Probe Substrates + GSK3640254 200 mg729.5

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Treatment C: Cmax for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

Interventionng/mL (Geometric Mean)
Treatment C: Probe Substrates + GSK3640254 200 mg1450

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Treatment C: AUC(0-t) for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

Interventionh*ng/mL (Geometric Mean)
Treatment C: Probe Substrates + GSK3640254 200 mg51840

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Treatment C: AUC From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) for GSK3640254

Blood samples were collected at the indicated time points for steady-state pharmacokinetic analysis of GSK3640254. (NCT04425902)
Timeframe: Pre-dose and at 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 24, 48, 72, 96, and 120 hours post-dose in treatment period 3

Interventionh*ng/mL (Geometric Mean)
Treatment C: Probe Substrates + GSK3640254 200 mg22920

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Treatment B: Change From Baseline in Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionBreaths per minute (Mean)
Treatment B: GSK3640254 200 mg-0.3

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Treatment B: Change From Baseline in Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionBeats per minute (Mean)
Treatment B: GSK3640254 200 mg1.3

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Treatment B: Change From Baseline in Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionDegrees Celsius (Mean)
Treatment B: GSK3640254 200 mg-0.03

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Treatment B: Change From Baseline in Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionGrams per liter (Mean)
Treatment B: GSK3640254 200 mg2.3

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Treatment B: Change From Baseline in Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionProportion of red blood cells in blood (Mean)
Treatment B: GSK3640254 200 mg0.0118

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Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionFemtoliter (Mean)
Treatment B: GSK3640254 200 mg0.94

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Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionPicograms (Mean)
Treatment B: GSK3640254 200 mg-0.05

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Treatment B: Change From Baseline in Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

Intervention10^12 cells per liter (Mean)
Treatment B: GSK3640254 200 mg0.083

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Treatment A: Change From Baseline in Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 2

InterventionBreaths per minute (Mean)
Treatment A: Probe Substrates-0.3

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Treatment A: Change From Baseline in Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionBeats per minute (Mean)
Treatment A: Probe Substrates0.5

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Treatment A: Change From Baseline in Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionDegrees Celsius (Mean)
Treatment A: Probe Substrates-0.12

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Treatment A: Change From Baseline in Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionGrams per liter (Mean)
Treatment A: Probe Substrates-4.2

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Treatment A: Change From Baseline in Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionProportion of red blood cells in blood (Mean)
Treatment A: Probe Substrates-0.0090

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Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionFemtoliter (Mean)
Treatment A: Probe Substrates1.31

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Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionPicograms (Mean)
Treatment A: Probe Substrates0.20

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Treatment A: Change From Baseline in Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

Intervention10^12 cells per liter (Mean)
Treatment A: Probe Substrates-0.172

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Tmax for Pravastatin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of pravastatin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates1.500
Treatment C: Probe Substrates + GSK3640254 200 mg3.000

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Tmax for Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates6.000
Treatment C: Probe Substrates + GSK3640254 200 mg6.000

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Tmax for Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates5.000
Treatment C: Probe Substrates + GSK3640254 200 mg6.000

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Tmax for Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates1.000
Treatment C: Probe Substrates + GSK3640254 200 mg1.000

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Tmax for Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates2.000
Treatment C: Probe Substrates + GSK3640254 200 mg3.000

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Tmax for Flurbiprofen

Blood samples were collected at the indicated time points for pharmacokinetic analysis of flurbiprofen. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates3.000
Treatment C: Probe Substrates + GSK3640254 200 mg4.000

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Tmax for Digoxin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of digoxin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates3.000
Treatment C: Probe Substrates + GSK3640254 200 mg2.000

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Tmax for Alpha-hydroxymetoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of alpha-hydroxymetoprolol. Alpha-hydroxymetoprolol is a metabolite of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates3.033
Treatment C: Probe Substrates + GSK3640254 200 mg4.000

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Tmax for 5-hydroxyomeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 5-hydroxyomeprazole. 5-hydroxyomeprazole is a metabolite of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates6.000
Treatment C: Probe Substrates + GSK3640254 200 mg6.000

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Tmax for 36-hydroxymontelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 36-hydroxymontelukast. 36-hydroxymontelukast is a metabolite of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates6.000
Treatment C: Probe Substrates + GSK3640254 200 mg6.000

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Tmax for 1-hydroxymidazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 1-hydroxymidazolam. 1-hydroxymidazolam is a metabolite of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates1.000
Treatment C: Probe Substrates + GSK3640254 200 mg1.000

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Time to Cmax (Tmax) for Caffeine

Blood samples were collected at the indicated time points for pharmacokinetic analysis of caffeine. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Median)
Treatment A: Probe Substrates2.000
Treatment C: Probe Substrates + GSK3640254 200 mg3.000

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t1/2 for Pravastatin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of pravastatin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates3.189
Treatment C: Probe Substrates + GSK3640254 200 mg3.156

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t1/2 for Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates1.439
Treatment C: Probe Substrates + GSK3640254 200 mg1.219

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t1/2 for Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates5.035
Treatment C: Probe Substrates + GSK3640254 200 mg5.135

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t1/2 for Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates5.756
Treatment C: Probe Substrates + GSK3640254 200 mg5.222

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t1/2 for Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates4.872
Treatment C: Probe Substrates + GSK3640254 200 mg5.342

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t1/2 for Flurbiprofen

Blood samples were collected at the indicated time points for pharmacokinetic analysis of flurbiprofen. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates6.123
Treatment C: Probe Substrates + GSK3640254 200 mg6.088

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t1/2 for Digoxin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of digoxin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates40.279
Treatment C: Probe Substrates + GSK3640254 200 mg38.784

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t1/2 for Alpha-hydroxymetoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of alpha-hydroxymetoprolol. Alpha-hydroxymetoprolol is a metabolite of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates8.040
Treatment C: Probe Substrates + GSK3640254 200 mg8.339

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t1/2 for 5-hydroxyomeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 5-hydroxyomeprazole. 5-hydroxyomeprazole is a metabolite of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates1.580
Treatment C: Probe Substrates + GSK3640254 200 mg1.569

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t1/2 for 36-hydroxymontelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 36-hydroxymontelukast. 36-hydroxymontelukast is a metabolite of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates5.310
Treatment C: Probe Substrates + GSK3640254 200 mg5.644

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t1/2 for 1-hydroxymidazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 1-hydroxymidazolam. 1-hydroxymidazolam is a metabolite of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates3.632
Treatment C: Probe Substrates + GSK3640254 200 mg3.717

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Ratio of Cmax of Alpha-hydroxymetoprolol to Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (metoprolol) and its metabolite (alpha-hydroxymetoprolol). Ratio of Cmax of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.7869
Treatment C: Probe Substrates + GSK3640254 200 mg0.7066

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Treatment C: Absolute Values of Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionGrams per liter (Mean)
Baseline (Day 20): AlbuminDay 22: AlbuminDay 25: AlbuminBaseline (Day 20): GlobulinDay 22: GlobulinDay 25: GlobulinBaseline (Day 20): ProteinDay 22: ProteinDay 25: Protein
Treatment C: Probe Substrates + GSK3640254 200 mg41.640.542.026.925.126.668.565.668.6

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Treatment A: Absolute Values of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionMillimeters of mercury (Mean)
Baseline (Day 1, Pre-dose): SBPDay 10: SBPBaseline (Day 1, Pre-dose): DBPDay 10: DBP
Treatment A: Probe Substrates111.0107.765.159.7

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Treatment A: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionMicromoles per liter (Mean)
Baseline (Day -1): UrateDay 10: UrateBaseline (Day -1): CreatinineDay 10: CreatinineBaseline (Day -1): BilirubinDay 10: BilirubinBaseline (Day -1): Direct bilirubinDay 10: Direct bilirubin
Treatment A: Probe Substrates347.3632365.504684.952486.41109.83258.00282.05201.7015

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Treatment A: Change From Baseline in Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionGrams per liter (Mean)
AlbuminGlobulinProtein
Treatment A: Probe Substrates-0.7-1.5-2.2

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Treatment A: Change From Baseline in Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionUnits per liter (Mean)
LipaseAmylase
Treatment A: Probe Substrates2.2-2.6

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Treatment A: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST and gamma-glutamyl transferase. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionInternational units per liter (Mean)
Creatine kinaseLactate dehydrogenaseALTALPASTGamma-glutamyl transferase
Treatment A: Probe Substrates-36.9-16.54.5-1.91.0-0.2

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Ratio of Cmax of 5-hydroxyomeprazole to Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (omeprazole) and its metabolite (5-hydroxyomeprazole). Ratio of Cmax of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.9461
Treatment C: Probe Substrates + GSK3640254 200 mg0.8810

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Ratio of Cmax of 36-hydroxymontelukast to Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (montelukast) and its metabolite (36-hydroxymontelukast). Ratio of Cmax of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.06766
Treatment C: Probe Substrates + GSK3640254 200 mg0.06308

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Ratio of Cmax of 1-hydroxymidazolam to Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (midazolam) and its metabolite (1-hydroxymidazolam). Ratio of Cmax of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.5286
Treatment C: Probe Substrates + GSK3640254 200 mg0.4955

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Ratio of AUC(0-infinity) of Alpha-hydroxymetoprolol to Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (metoprolol) and its metabolite (alpha-hydroxymetoprolol). Ratio of AUC(0-infinity) of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates1.733
Treatment C: Probe Substrates + GSK3640254 200 mg1.449

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Ratio of AUC(0-infinity) of 5-hydroxyomeprazole to Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (omeprazole) and its metabolite (5-hydroxyomeprazole). Ratio of AUC(0-infinity) of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates1.151
Treatment C: Probe Substrates + GSK3640254 200 mg1.077

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Ratio of AUC(0-infinity) of 36-hydroxymontelukast to Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (montelukast) and its metabolite (36-hydroxymontelukast). Ratio of AUC(0-infinity) of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.09182
Treatment C: Probe Substrates + GSK3640254 200 mg0.08562

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Ratio of AUC(0-infinity) of 1-hydroxymidazolam to Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of parent drug (midazolam) and its metabolite (1-hydroxymidazolam). Ratio of AUC(0-infinity) of metabolite to parent drug has been presented. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionRatio (Mean)
Treatment A: Probe Substrates0.4677
Treatment C: Probe Substrates + GSK3640254 200 mg0.4618

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Maximum Observed Plasma Concentration (Cmax) for Caffeine

Blood samples were collected at the indicated time points for pharmacokinetic analysis of caffeine. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionNanograms per milliliter (ng/mL) (Geometric Mean)
Treatment A: Probe Substrates4340
Treatment C: Probe Substrates + GSK3640254 200 mg4110

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Cmax for Pravastatin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of pravastatin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates19.45
Treatment C: Probe Substrates + GSK3640254 200 mg15.19

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Cmax for Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates224.4
Treatment C: Probe Substrates + GSK3640254 200 mg256.6

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Cmax for Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionNanograms per milliliter (ng/mL) (Geometric Mean)
Treatment A: Probe Substrates379.8
Treatment C: Probe Substrates + GSK3640254 200 mg393.5

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Cmax for Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates15.44
Treatment C: Probe Substrates + GSK3640254 200 mg13.95

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Cmax for Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates127.4
Treatment C: Probe Substrates + GSK3640254 200 mg141.1

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Cmax for Flurbiprofen

Blood samples were collected at the indicated time points for pharmacokinetic analysis of flurbiprofen. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates10220
Treatment C: Probe Substrates + GSK3640254 200 mg10710

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Cmax for Digoxin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of digoxin. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionPicogram per milliliter (pg/mL) (Geometric Mean)
Treatment A: Probe Substrates1026
Treatment C: Probe Substrates + GSK3640254 200 mg1282

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Cmax for Alpha-hydroxymetoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of alpha-hydroxymetoprolol. Alpha-hydroxymetoprolol is a metabolite of metoprolol. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates45.70
Treatment C: Probe Substrates + GSK3640254 200 mg39.21

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Cmax for 5-hydroxyomeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 5-hydroxyomeprazole. 5-hydroxyomeprazole is a metabolite of omeprazole. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates181.1
Treatment C: Probe Substrates + GSK3640254 200 mg203.3

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Cmax for 36-hydroxymontelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 36-hydroxymontelukast. 36-hydroxymontelukast is a metabolite of montelukast. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates24.62
Treatment C: Probe Substrates + GSK3640254 200 mg23.22

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Cmax for 1-hydroxymidazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 1-hydroxymidazolam. 1-hydroxymidazolam is a metabolite of midazolam. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionng/mL (Geometric Mean)
Treatment A: Probe Substrates7.933
Treatment C: Probe Substrates + GSK3640254 200 mg6.722

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AUC(0-t) for Pravastatin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of pravastatin. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates69.92
Treatment C: Probe Substrates + GSK3640254 200 mg51.03

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AUC(0-t) for Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of omeprazole. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates728.1
Treatment C: Probe Substrates + GSK3640254 200 mg817.9

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AUC(0-t) for Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of montelukast. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates2724
Treatment C: Probe Substrates + GSK3640254 200 mg2940

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AUC(0-t) for Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of midazolam. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates67.11
Treatment C: Probe Substrates + GSK3640254 200 mg62.95

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AUC(0-t) for Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of metoprolol. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates655.0
Treatment C: Probe Substrates + GSK3640254 200 mg807.3

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AUC(0-t) for Flurbiprofen

Blood samples were collected at the indicated time points for pharmacokinetic analysis of flurbiprofen. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates64930
Treatment C: Probe Substrates + GSK3640254 200 mg66170

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AUC(0-t) for Digoxin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of digoxin. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours*picogram per milliliter (h*pg/mL) (Geometric Mean)
Treatment A: Probe Substrates16690
Treatment C: Probe Substrates + GSK3640254 200 mg17840

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AUC(0-t) for Alpha-hydroxymetoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of alpha-hydroxymetoprolol. Alpha-hydroxymetoprolol is a metabolite of metoprolol. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates531.3
Treatment C: Probe Substrates + GSK3640254 200 mg487.9

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AUC(0-t) for 5-hydroxyomeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 5-hydroxyomeprazole. 5-hydroxyomeprazole is a metabolite of omeprazole. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates713.5
Treatment C: Probe Substrates + GSK3640254 200 mg785.1

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AUC(0-t) for 36-hydroxymontelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 36-hydroxymontelukas. 36-hydroxymontelukast is a metabolite of montelukast. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates234.2
Treatment C: Probe Substrates + GSK3640254 200 mg230.9

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AUC(0-t) for 1-hydroxymidazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 1-hydroxymidazolam. 1-hydroxymidazolam is a metabolite of midazolam. The AUC(0-t) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates31.07
Treatment C: Probe Substrates + GSK3640254 200 mg28.07

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AUC(0-infinity) for Pravastatin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of pravastatin. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates72.09
Treatment C: Probe Substrates + GSK3640254 200 mg43.70

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AUC(0-infinity) for Omeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of omeprazole. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates1127
Treatment C: Probe Substrates + GSK3640254 200 mg1093

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AUC(0-infinity) for Montelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of montelukast. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates2859
Treatment C: Probe Substrates + GSK3640254 200 mg3109

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AUC(0-infinity) for Midazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of midazolam. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates70.08
Treatment C: Probe Substrates + GSK3640254 200 mg65.46

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AUC(0-infinity) for Metoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of metoprolol. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates659.1
Treatment C: Probe Substrates + GSK3640254 200 mg813.1

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AUC(0-infinity) for Flurbiprofen

Blood samples were collected at the indicated time points for pharmacokinetic analysis of flurbiprofen. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates66700
Treatment C: Probe Substrates + GSK3640254 200 mg68660

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AUC(0-infinity) for Digoxin

Blood samples were collected at the indicated time points for pharmacokinetic analysis of digoxin. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*pg/mL (Geometric Mean)
Treatment A: Probe Substrates19180
Treatment C: Probe Substrates + GSK3640254 200 mg20090

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AUC(0-infinity) for Alpha-hydroxymetoprolol

Blood samples were collected at the indicated time points for pharmacokinetic analysis of alpha-hydroxymetoprolol. Alpha-hydroxymetoprolol is a metabolite of metoprolol. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates682.8
Treatment C: Probe Substrates + GSK3640254 200 mg632.8

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AUC(0-infinity) for 5-hydroxyomeprazole

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 5-hydroxyomeprazole. 5-hydroxyomeprazole is a metabolite of omeprazole. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates767.4
Treatment C: Probe Substrates + GSK3640254 200 mg762.0

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AUC(0-infinity) for 36-hydroxymontelukast

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 36-hydroxymontelukast. 36-hydroxymontelukast is a metabolite of montelukast. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates252.5
Treatment C: Probe Substrates + GSK3640254 200 mg249.3

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AUC(0-infinity) for 1-hydroxymidazolam

Blood samples were collected at the indicated time points for pharmacokinetic analysis of 1-hydroxymidazolam. 1-hydroxymidazolam is a metabolite of midazolam. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates31.86
Treatment C: Probe Substrates + GSK3640254 200 mg28.99

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AUC From Time Zero Extrapolated to Infinity (AUC[0-infinity]) for Caffeine

Blood samples were collected at the indicated time points for pharmacokinetic analysis of caffeine. The AUC(0-infinity) was determined using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

Interventionh*ng/mL (Geometric Mean)
Treatment A: Probe Substrates39720
Treatment C: Probe Substrates + GSK3640254 200 mg44440

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Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Time t (AUC[0-t]) for Caffeine

Blood samples were collected at the indicated time points for pharmacokinetic analysis of caffeine. Area under the plasma concentration-time curve from time zero to time t, to be calculated using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHour*nanograms per milliliter (h*ng/mL) (Geometric Mean)
Treatment A: Probe Substrates37970
Treatment C: Probe Substrates + GSK3640254 200 mg42230

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Apparent Terminal Phase Half-life (t1/2) for Caffeine

Blood samples were collected at the indicated time points for pharmacokinetic analysis of caffeine. (NCT04425902)
Timeframe: Pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, and 120 hours post-dose in treatment period 1 and 3

InterventionHours (Geometric Mean)
Treatment A: Probe Substrates5.380
Treatment C: Probe Substrates + GSK3640254 200 mg6.085

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Treatment A: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionMilliseconds (Mean)
PR IntervalQRS DurationQT IntervalQTcF Interval
Treatment A: Probe Substrates3.42.57.14.8

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Treatment A: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium, and urea. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionMillimoles per liter (Mean)
GlucoseCarbon DioxideCholesterolTriglyceridesAnion GapCalciumChloridePhosphatePotassiumSodiumUrea
Treatment A: Probe Substrates-0.2137-78.7-0.6452-0.04185.9-0.062478.00.0678-0.050.71.1263

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Treatment A: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

Intervention10^9 cells per liter (Mean)
Platelet countLeukocyte countNeutrophilsLymphocytesMonocytesEosinophilsBasophils
Treatment A: Probe Substrates7.30.660.59260.0748-0.03750.01500.0110

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Treatment A: Change From Baseline in SBP and DBP

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionMillimeters of mercury (Mean)
SBPDBP
Treatment A: Probe Substrates-3.3-5.4

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Treatment A: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionMicromoles per liter (Mean)
UrateCreatinineBilirubinDirect bilirubin
Treatment A: Probe Substrates18.14141.4586-1.8297-0.3506

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Treatment B: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionMilliseconds (Mean)
Baseline (Day 11, Pre-dose): PR IntervalDay 20: PR IntervalBaseline (Day 11, Pre-dose): QRS DurationDay 20: QRS DurationBaseline (Day 11, Pre-dose): QT IntervalDay 20: QT IntervalBaseline (Day 11, Pre-dose): QTcF IntervalDay 20: QTcF Interval
Treatment B: GSK3640254 200 mg158.6161.894.296.4403.1408.8403.5408.6

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Treatment B: Absolute Values of Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionGrams per liter (Mean)
Baseline (Day 10): AlbuminDay 20: AlbuminBaseline (Day 10): GlobulinDay 20: GlobulinBaseline (Day 10): ProteinDay 20: Protein
Treatment B: GSK3640254 200 mg42.241.425.926.868.168.2

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Treatment B: Absolute Values of Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionUnits per liter (Mean)
Baseline (Day 10): LipaseDay 20: LipaseBaseline (Day 10): AmylaseDay 20: Amylase
Treatment B: GSK3640254 200 mg31.632.456.960.1

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Treatment B: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST, and gamma-glutamyl transferase. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionInternational units per liter (Mean)
Baseline (Day 10): Creatine kinaseDay 20: Creatine kinaseBaseline (Day 10): Lactate dehydrogenaseDay 20: Lactate dehydrogenaseBaseline (Day 10): ALTDay 20: ALTBaseline (Day 10): ALPDay 20: ALPBaseline (Day 10): ASTDay 20: ASTBaseline (Day 10): Gamma-glutamyl transferaseDay 20: Gamma-glutamyl transferase
Treatment B: GSK3640254 200 mg66.968.9114.8115.920.120.360.858.515.616.118.918.3

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Treatment B: Absolute Values of Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

Intervention10^12 cells per liter (Mean)
Baseline (Day 10)Day 20
Treatment B: GSK3640254 200 mg4.6644.746

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Treatment A: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium, urea. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionMillimoles per liter (Mean)
Baseline (Day -1): GlucoseDay 10: GlucoseBaseline (Day -1): Carbon DioxideDay 10: Carbon DioxideBaseline (Day -1): CholesterolDay 10: CholesterolBaseline (Day -1): TriglyceridesDay 10: TriglyceridesBaseline (Day -1): Anion GapDay 10: Anion GapBaseline (Day -1): CalciumDay 10: CalciumBaseline (Day -1): ChlorideDay 10: ChlorideBaseline (Day -1): PhosphateDay 10: PhosphateBaseline (Day -1): PotassiumDay 10: PotassiumBaseline (Day -1): SodiumDay 10: SodiumBaseline (Day -1): UreaDay 10: Urea
Treatment A: Probe Substrates5.03484.8211104.125.44.45703.81181.22321.18147.913.82.37652.314125.8103.71.10751.17544.484.43137.7138.44.81955.9458

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Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionPicograms (Mean)
Baseline (Day 10)Day 20
Treatment B: GSK3640254 200 mg29.5729.52

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Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionFemtoliter (Mean)
Baseline (Day 10)Day 20
Treatment B: GSK3640254 200 mg88.0288.96

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Treatment B: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium, and urea. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionMillimoles per liter (Mean)
Baseline (Day 10): GlucoseDay 20: GlucoseBaseline (Day 10): Carbon DioxideDay 20: Carbon DioxideBaseline (Day 10): CholesterolDay 20: CholesterolBaseline (Day 10): TriglyceridesDay 20: TriglyceridesBaseline (Day 10): Anion GapDay 20: Anion GapBaseline (Day 10): CalciumDay 20: CalciumBaseline (Day 10): ChlorideDay 20: ChlorideBaseline (Day 10): PhosphateDay 20: PhosphateBaseline (Day 10): PotassiumDay 20: PotassiumBaseline (Day 10): SodiumDay 20: SodiumBaseline (Day 10): UreaDay 20: Urea
Treatment B: GSK3640254 200 mg4.82114.737825.424.93.81183.69151.18141.082513.814.52.31412.3141103.7103.61.17541.25934.434.39138.4138.65.94585.6335

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Treatment B: Absolute Values of Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionProportion of red blood cells in blood (Mean)
Baseline (Day 10)Day 20
Treatment B: GSK3640254 200 mg0.40980.4216

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Treatment B: Absolute Values of Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionGrams per liter (Mean)
Baseline (Day 10)Day 20
Treatment B: GSK3640254 200 mg137.7140.0

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Treatment B: Absolute Values of Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionDegrees Celsius (Mean)
Baseline (Day 11, Pre-dose)Day 20
Treatment B: GSK3640254 200 mg36.3136.28

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Treatment B: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

Intervention10^9 cells per liter (Mean)
Baseline (Day 10): Platelet countDay 20: Platelet countBaseline (Day 10): Leukocyte countDay 20: Leukocyte countBaseline (Day 10): NeutrophilsDay 20: NeutrophilsBaseline (Day 10): LymphocytesDay 20: LymphocytesBaseline (Day 10): MonocytesDay 20: MonocytesBaseline (Day 10): EosinophilsDay 20: EosinophilsBaseline (Day 10): BasophilsDay 20: Basophils
Treatment B: GSK3640254 200 mg265.9261.96.305.793.74303.26801.89651.83550.45150.44350.16100.19200.04400.0460

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Treatment B: Absolute Values of Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionBeats per minute (Mean)
Baseline (Day 11, Pre-dose)Day 20
Treatment B: GSK3640254 200 mg61.662.8

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Treatment B: Absolute Values of Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionBreaths per minute (Mean)
Baseline (Day 11, Pre-dose)Day 20
Treatment B: GSK3640254 200 mg15.014.7

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Treatment B: Absolute Values of SBP and DBP

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionMillimeters of mercury (Mean)
Baseline (Day 11, Pre-dose): SBPDay 20: SBPBaseline (Day 11, Pre-dose): DBPDay 20: DBP
Treatment B: GSK3640254 200 mg107.7107.261.659.6

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Treatment B: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionMicromoles per liter (Mean)
Baseline (Day 10): UrateDay 20: UrateBaseline (Day 10): CreatinineDay 20: CreatinineBaseline (Day 10): BilirubinDay 20: BilirubinBaseline (Day 10): Direct bilirubinDay 20: Direct bilirubin
Treatment B: GSK3640254 200 mg365.5046337.846486.411090.78688.00288.61841.70151.8126

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Treatment B: Change From Baseline in Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionGrams per liter (Mean)
AlbuminGlobulinProtein
Treatment B: GSK3640254 200 mg-0.90.90.1

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Treatment B: Change From Baseline in Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionUnits per liter (Mean)
LipaseAmylase
Treatment B: GSK3640254 200 mg0.93.2

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Treatment B: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST, and gamma-glutamyl transferase. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionInternational units per liter (Mean)
Creatine kinaseLactate dehydrogenaseALTALPASTGamma-glutamyl transferase
Treatment B: GSK3640254 200 mg2.11.10.3-2.40.6-0.6

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Treatment B: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionMilliseconds (Mean)
PR IntervalQRS DurationQT IntervalQTcF Interval
Treatment B: GSK3640254 200 mg3.22.35.75.1

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Treatment B: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium, and urea. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionMillimoles per liter (Mean)
GlucoseCarbon DioxideCholesterolTriglyceridesAnion GapCalciumChloridePhosphatePotassiumSodiumUrea
Treatment B: GSK3640254 200 mg-0.0833-0.6-0.1203-0.09890.80.0000-0.10.0840-0.050.3-0.3124

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Treatment B: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

Intervention10^9 cells per liter (Mean)
Platelet countLeukocyte countNeutrophilsLymphocytesMonocytesEosinophilsBasophils
Treatment B: GSK3640254 200 mg-4.1-0.51-0.4750-0.0610-0.00800.03100.0020

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Treatment B: Change From Baseline in SBP and DBP

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 11, Pre-Dose), before the first dose in Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 11, Pre-Dose) and Day 20

InterventionMillimeters of mercury (Mean)
SBPDBP
Treatment B: GSK3640254 200 mg-0.5-2.0

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Treatment B: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment B was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 10), before the first dose of Treatment B. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 10) and Day 20

InterventionMicromoles per liter (Mean)
UrateCreatinineBilirubinDirect bilirubin
Treatment B: GSK3640254 200 mg-27.65824.37580.61560.1112

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Treatment C: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionMilliseconds (Mean)
Baseline (Day 21, Pre-dose): PR IntervalDay 22: PR IntervalDay 25: PR IntervalBaseline (Day 21, Pre-dose): QRS DurationDay 22: QRS DurationDay 25: QRS DurationBaseline (Day 21, Pre-dose): QT IntervalDay 22: QT IntervalDay 25: QT IntervalBaseline (Day 21, Pre-dose): QTcF IntervalDay 22: QTcF IntervalDay 25: QTcF Interval
Treatment C: Probe Substrates + GSK3640254 200 mg160.8162.3159.695.898.796.8402.6420.6398.7408.7407.3402.5

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Treatment C: Absolute Values of Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionUnits per liter (Mean)
Baseline (Day 20): LipaseDay 22: LipaseDay 25: LipaseBaseline (Day 20): AmylaseDay 22: AmylaseDay 25: Amylase
Treatment C: Probe Substrates + GSK3640254 200 mg32.933.533.162.264.760.7

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Treatment C: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST, gamma-glutamyl transferase. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionInternational units per liter (Mean)
Baseline (Day 20): Creatine kinaseDay 22: Creatine kinaseDay 25: Creatine kinaseBaseline (Day 20): Lactate dehydrogenaseDay 22: Lactate dehydrogenaseDay 25: Lactate dehydrogenaseBaseline (Day 20): ALTDay 22: ALTDay 25: ALTBaseline (Day 20): ALPDay 22: ALPDay 25:ALPBaseline (Day 20): ASTDay 22: ASTDay 25: ASTBaseline (Day 20): Gamma-glutamyl transferaseDay 22: Gamma-glutamyl transferaseDay 25: Gamma-glutamyl transferase
Treatment C: Probe Substrates + GSK3640254 200 mg71.365.763.8116.6120.6119.320.417.320.958.557.658.616.214.716.418.517.118.7

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Treatment C: Absolute Values of Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

Intervention10^12 cells per liter (Mean)
Baseline (Day 20)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg4.7694.6084.756

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Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionPicograms (Mean)
Baseline (Day 20)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg29.5129.2829.12

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Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionFemtoliter (Mean)
Baseline (Day 20)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg89.0387.3887.74

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Treatment C: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium and urea. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionMillimoles per liter (Mean)
Baseline (Day 20): GlucoseDay 22: GlucoseDay 25: GlucoseBaseline (Day 20): Carbon DioxideDay 22: Carbon DioxideDay 25: Carbon DioxideBaseline (Day 20): CholesterolDay 22: CholesterolDay 25: CholesterolBaseline (Day 20): TriglyceridesDay 22: TriglyceridesDay 25: TriglyceridesBaseline (Day 20): Anion GapDay 22: Anion GapDay 25: Anion GapBaseline (Day 20): CalciumDay 22: CalciumDay 25: CalciumBaseline (Day 20): ChlorideDay 22: ChlorideDay 25: ChlorideBaseline (Day 20): PhosphateDay 22: PhosphateDay 25: PhosphateBaseline (Day 20): PotassiumDay 22: PotassiumDay 25: PotassiumBaseline (Day 20): SodiumDay 22: SodiumDay 25: SodiumBaseline (Day 20): UreaDay 22: UreaDay 25: Urea
Treatment C: Probe Substrates + GSK3640254 200 mg4.71844.80604.870324.925.426.23.68983.25433.39721.07831.08361.107414.613.914.52.32172.28102.3519103.4104.8102.61.26611.19811.34774.384.344.35138.6139.8139.05.73644.90785.3099

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Treatment C: Absolute Values of Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionProportion of red blood cells in blood (Mean)
Baseline (Day 20)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg0.42390.40220.4168

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Treatment A: Absolute Values of Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 2

InterventionBreaths per minute (Mean)
Baseline (Day 1, Pre-dose)Day 2
Treatment A: Probe Substrates16.115.8

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Treatment C: Absolute Values of Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionGrams per liter (Mean)
Baseline (Day 20)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg140.6134.7138.3

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Treatment C: Absolute Values of Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionDegrees Celsius (Mean)
Baseline (Day 21, Pre-dose)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg36.3136.1836.31

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Treatment C: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

Intervention10^9 cells per liter (Mean)
Baseline (Day 20): Platelet countDay 22: Platelet countDay 25: Platelet countBaseline (Day 20): Leukocyte countDay 22: Leukocyte countDay 25: Leukocyte countBaseline (Day 20): NeutrophilsDay 22: NeutrophilsDay 25: NeutrophilsBaseline (Day 20): LymphocytesDay 22: LymphocytesDay 25: LymphocytesBaseline (Day 20): MonocytesDay 22: MonocytesDay 25: MonocytesBaseline (Day 20): EosinophilsDay 22: EosinophilsDay 25: EosinophilsBaseline (Day 20): BasophilsDay 22: BasophilsDay 25: Basophils
Treatment C: Probe Substrates + GSK3640254 200 mg262.3249.2260.75.865.815.983.31793.19253.45291.84371.87871.92800.45050.46890.35760.19530.22820.18370.04740.03800.0408

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Treatment C: Absolute Values of Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionBeats per minute (Mean)
Baseline (Day 21, Pre-dose)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg63.256.261.7

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Treatment C: Absolute Values of Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionBreaths per minute (Mean)
Baseline (Day 21, Pre-dose)Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg15.715.716.5

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Treatment C: Absolute Values of SBP and DBP

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionMillimeters of mercury (Mean)
Baseline (Day 21, Pre-dose): SBPDay 22: SBPDay 25: SBPBaseline (Day 21, Pre-dose): DBPDay 22: DBPDay 25: DBP
Treatment C: Probe Substrates + GSK3640254 200 mg107.5105.6109.762.758.462.2

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Treatment C: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionMicromoles per liter (Mean)
Baseline (Day 20): UrateDay 22: UrateDay 25: UrateBaseline (Day 20): CreatinineDay 22: CreatinineDay 25: CreatinineBaseline (Day 20): BilirubinDay 22: BilirubinDay 25: BilirubinBaseline (Day 20): Direct bilirubinDay 22: Direct bilirubinDay 25: Direct bilirubin
Treatment C: Probe Substrates + GSK3640254 200 mg343.1057303.0349340.601392.168687.376490.58678.74809.88209.03601.84502.07901.9980

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Treatment C: Change From Baseline in Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionGrams per liter (Mean)
Day 22: AlbuminDay 25: AlbuminDay 22: GlobulinDay 25: GlobulinDay 22: ProteinDay 25: Protein
Treatment C: Probe Substrates + GSK3640254 200 mg-1.10.4-1.8-0.3-2.90.2

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Treatment C: Change From Baseline in Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionUnits per liter (Mean)
Day 22: LipaseDay 25: LipaseDay 22: AmylaseDay 25: Amylase
Treatment C: Probe Substrates + GSK3640254 200 mg0.60.22.5-1.5

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Treatment C: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST, gamma-glutamyl transferase. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionInternational units per liter (Mean)
Day 22: Creatine kinaseDay 25: Creatine kinaseDay 22: Lactate dehydrogenaseDay 25: Lactate dehydrogenaseDay 22: ALTDay 25: ALTDay 22: ALPDay 25:ALPDay 22: ASTDay 25: ASTDay 22: Gamma-glutamyl transferaseDay 25: Gamma-glutamyl transferase
Treatment C: Probe Substrates + GSK3640254 200 mg-5.6-7.54.02.6-3.10.5-0.90.1-1.50.2-1.50.2

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Treatment C: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF

Twelve-lead ECGs were obtained to measure PR Interval, QRS Duration, QT Interval and QTcF Interval. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionMilliseconds (Mean)
Day 22: PR IntervalDay 25: PR IntervalDay 22: QRS DurationDay 25: QRS DurationDay 22: QT IntervalDay 25: QT IntervalDay 22: QTcF IntervalDay 25: QTcF Interval
Treatment C: Probe Substrates + GSK3640254 200 mg1.5-1.22.91.018.0-3.9-1.4-6.3

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Treatment C: Change From Baseline in Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

Intervention10^12 cells per liter (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-0.161-0.013

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Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionPicograms (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-0.23-0.39

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Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionFemtoliter (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-1.64-1.28

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Treatment C: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea

Blood samples were collected to analyze the chemistry parameters: glucose, carbon dioxide, cholesterol, triglycerides, anion gap, calcium, chloride, phosphate, potassium, sodium and urea. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionMillimoles per liter (Mean)
Day 22: GlucoseDay 25: GlucoseDay 22: Carbon DioxideDay 25: Carbon DioxideDay 22: CholesterolDay 25: CholesterolDay 22: TriglyceridesDay 25: TriglyceridesDay 22: Anion GapDay 25: Anion GapDay 22: CalciumDay 25: CalciumDay 22: ChlorideDay 25: ChlorideDay 22: PhosphateDay 25: PhosphateDay 22: PotassiumDay 25: PotassiumDay 22: SodiumDay 25: SodiumDay 22: UreaDay 25: Urea
Treatment C: Probe Substrates + GSK3640254 200 mg0.08760.15190.51.2-0.4355-0.29260.00540.0291-0.6-0.1-0.04070.03021.4-0.8-0.06800.0816-0.04-0.031.20.4-0.8286-0.4265

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Treatment C: Change From Baseline in Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionProportion of red blood cells in blood (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-0.0217-0.0071

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Treatment C: Change From Baseline in Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionGrams per liter (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-5.8-2.3

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Treatment C: Change From Baseline in Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionDegrees Celsius (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-0.130.01

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Treatment C: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

Intervention10^9 cells per liter (Mean)
Day 22: Platelet countDay 25: Platelet countDay 22: Leukocyte countDay 25: Leukocyte countDay 22: NeutrophilsDay 25: NeutrophilsDay 22: LymphocytesDay 25: LymphocytesDay 22: MonocytesDay 25: MonocytesDay 22: EosinophilsDay 25: EosinophilsDay 22: BasophilsDay 25: Basophils
Treatment C: Probe Substrates + GSK3640254 200 mg-13.1-1.6-0.050.12-0.12540.13510.03510.08430.0184-0.09290.0329-0.0115-0.0094-0.0066

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Treatment C: Change From Baseline in Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionBeats per minute (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-7.1-1.5

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Treatment C: Change From Baseline in Respiratory Rate

Respiratory rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionBreaths per minute (Mean)
Day 22Day 25
Treatment C: Probe Substrates + GSK3640254 200 mg-0.10.8

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Treatment C: Change From Baseline in SBP and DBP

SBP and DBP were measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 21, Pre-Dose), before the first dose in Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 21, Pre-Dose), Days 22 and 25

InterventionMillimeters of mercury (Mean)
Day 22: SBPDay 25: SBPDay 22: DBPDay 25: DBP
Treatment C: Probe Substrates + GSK3640254 200 mg-1.92.2-4.3-0.5

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Treatment C: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin

Blood samples were collected to analyze the chemistry parameters: urate, creatinine, bilirubin and direct bilirubin. Baseline for treatment C was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 20), before the dose of Treatment C. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04425902)
Timeframe: Baseline (Day 20), Days 22 and 25

InterventionMicromoles per liter (Mean)
Day 22: UrateDay 25: UrateDay 22: CreatinineDay 25: CreatinineDay 22: BilirubinDay 25: BilirubinDay 22: Direct bilirubinDay 25: Direct bilirubin
Treatment C: Probe Substrates + GSK3640254 200 mg-40.0707-2.5044-4.7922-1.58191.13400.28800.23400.1530

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Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Volume

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionFemtoliter (Mean)
Baseline (Day -1)Day 10
Treatment A: Probe Substrates86.7188.02

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Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionPicograms (Mean)
Baseline (Day -1)Day 10
Treatment A: Probe Substrates29.3729.57

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Treatment A: Absolute Values of Erythrocytes

Blood samples were collected to analyze the hematology parameter: erythrocytes. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

Intervention10^12 cells per liter (Mean)
Baseline (Day -1)Day 10
Treatment A: Probe Substrates4.8364.664

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Treatment A: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Gamma-glutamyl Transferase

Blood samples were collected to analyze the chemistry parameters: creatine kinase, lactate dehydrogenase, ALT, ALP, AST and gamma-glutamyl transferase. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionInternational units per liter (Mean)
Baseline (Day -1): Creatine kinaseDay 10: Creatine kinaseBaseline (Day -1): Lactate dehydrogenaseDay 10: Lactate dehydrogenaseBaseline (Day -1): ALTDay 10: ALTBaseline (Day -1): ALPDay 10: ALPBaseline (Day -1): ASTDay 10: ASTBaseline (Day -1): Gamma-glutamyl transferaseDay 10: Gamma-glutamyl transferase
Treatment A: Probe Substrates103.766.9131.3114.815.620.162.760.814.615.619.118.9

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Treatment A: Absolute Values of Amylase, Lipase

Blood samples were collected to analyze the chemistry parameters: amylase and lipase. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionUnits per liter (Mean)
Baseline (Day -1): LipaseDay 10: LipaseBaseline (Day -1): AmylaseDay 10: Amylase
Treatment A: Probe Substrates29.431.659.556.9

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Treatment A: Absolute Values of Albumin, Globulin, Protein

Blood samples were collected to analyze the chemistry parameters: albumin, globulin and protein. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionGrams per liter (Mean)
Baseline (Day -1): AlbuminDay 10: AlbuminBaseline (Day -1): GlobulinDay 10: GlobulinBaseline (Day -1): ProteinDay 10: Protein
Treatment A: Probe Substrates42.942.227.425.970.368.1

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Treatment A: Absolute Values of Hematocrit

Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionProportion of red blood cells in blood (Mean)
Baseline (Day -1)Day 10
Treatment A: Probe Substrates0.41880.4098

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Treatment A: Absolute Values of Hemoglobin

Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

InterventionGrams per liter (Mean)
Baseline (Day -1)Day 10
Treatment A: Probe Substrates141.9137.7

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Treatment A: Absolute Values of Oral Temperature

Oral temperature was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionDegrees Celsius (Mean)
Baseline (Day 1, Pre-dose)Day 10
Treatment A: Probe Substrates36.3836.26

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Treatment A: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils

Blood samples were collected to analyze the hematology parameters: platelet count, leukocyte count, neutrophils, lymphocytes, monocytes, eosinophils and basophils. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day -1), before the dose of Treatment A. (NCT04425902)
Timeframe: Baseline (Day -1) and Day 10

Intervention10^9 cells per liter (Mean)
Baseline (Day -1): Platelet countDay 10: Platelet countBaseline (Day -1): Leukocyte countDay 10: Leukocyte countBaseline (Day -1): NeutrophilsDay 10: NeutrophilsBaseline (Day -1): LymphocytesDay 10: LymphocytesBaseline (Day -1): MonocytesDay 10: MonocytesBaseline (Day -1): EosinophilsDay 10: EosinophilsBaseline (Day -1): BasophilsDay 10: Basophils
Treatment A: Probe Substrates258.6265.95.646.303.15043.74301.82171.89650.48900.45150.14610.16100.03310.0440

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Treatment A: Absolute Values of Pulse Rate

Pulse rate was measured in the supine position after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline for treatment A was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits (Day 1, Pre-Dose), before the dose in Treatment A. (NCT04425902)
Timeframe: Baseline (Day 1, Pre-dose) and Day 10

InterventionBeats per minute (Mean)
Baseline (Day 1, Pre-dose)Day 10
Treatment A: Probe Substrates64.565.0

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Maximum Measured Concentration of the S-warfarin in Plasma (Cmax, S-warfarin)

Warfarin sodium is a racemic mixture of the R-and S-enantiomers. Maximum measured concentration of the S-warfarin in plasma (Cmax) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 48 h, 71 h, 95 h, 119 h, 143 h after warfarin administration in both periods.

Interventionnanomole/Liter (nmol/L) (Geometric Least Squares Mean)
Warfarin (Reference (R))1622.94
BI 730357 + Warfarin (Test (T))1760.38

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Maximum Measured Concentration of the Caffeine in Plasma (Cmax, Caffeine)

Maximum measured concentration of the caffeine in plasma (Cmax, caffeine) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 48 h after caffeine administration in both periods.

Interventionnanomole/Liter (nmol/L) (Geometric Least Squares Mean)
Caffeine (Reference (R))11973.25
BI 730357 + Caffeine (Test (T))11583.25

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Maximum Measured Concentration of Omeprazole in Plasma (Cmax, Omeprazole)

Maximum measured concentration of omeprazole in plasma (Cmax, omeprazole) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h after omeprazole administration in both periods.

Interventionnanomole/Liter (nmol/L) (Geometric Least Squares Mean)
Omeprazole (Reference (R))504.07
BI 730357 + Omeprazole (Test (T))359.50

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Maximum Measured Concentration of Midazolam in Plasma (Cmax, Midazolam)

Maximum measured concentration of midazolam in plasma (Cmax, midazolam) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h after midazolam administration in both periods.

Interventionnanomole/Liter (nmol/L) (Geometric Least Squares Mean)
Midazolam (Reference (R))19.09
BI 730357 + Midazolam (Test (T))24.87

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Area Under the Concentration-time Curve of S-warfarin in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, S-warfarin)

Warfarin sodium is a racemic mixture of the R-and S-enantiomers. Area under the concentration-time curve of S-warfarin in plasma over the time interval from 0 extrapolated to infinity (AUC0-infinity,S-warfain) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 48 h, 71 h, 95 h, 119 h, 143 h after warfarin administration in both periods.

Interventionhours * nanomole/Liter (h*nmol/L) (Geometric Least Squares Mean)
Warfarin (Reference (R))55770.25
BI 730357 + Warfarin (Test (T))61559.60

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Area Under the Concentration-time Curve of Omeprazole in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Omeprazole)

Area under the concentration-time curve of omeprazole in plasma over the time interval from 0 extrapolated to infinity (AUC0-infinity, omeprazole) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h after omeprazole administration in both periods.

Interventionhours * nanomole/Liter (h*nmol/L) (Geometric Least Squares Mean)
Omeprazole (Reference (R))933.62
BI 730357 + Omeprazole (Test (T))931.22

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Area Under the Concentration-time Curve of Midazolam in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Midazolam)

Area under the concentration-time curve of midazolam in plasma over the time interval from 0 extrapolated to infinity (AUC0-infinity, midazolam) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h after midazolam administration in both periods.

Interventionhours * nanomole/Liter (h*nmol/L) (Geometric Least Squares Mean)
Midazolam (Reference (R))56.81
BI 730357 + Midazolam (Test (T))72.07

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Area Under the Concentration-time Curve of Caffeine in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity, Caffeine)

Area under the concentration-time curve of caffeine in plasma over the time interval from 0 extrapolated to infinity (AUC0-infinity, caffeine) is reported. (NCT04679948)
Timeframe: Within 2 hours (h) predose for period 1, within 15 minutes predose for period 2 and 0.5 h, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 48 h after caffeine administration in both periods.

Interventionhours *nanomole/Liter (h*nmol/L) (Geometric Least Squares Mean)
Caffeine (Reference (R))84569.29
BI 730357 + Caffeine (Test (T))94764.64

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Nebraska Interprofessional Education Attitude Scale (NIPEAS) Score for Professional Staff Arm

The Nebraska Interprofessional Education Attitude Scale (NIPEAS) was developed to measure the attitudes of pre-clinical learners to practicing health professionals. The NIPEAS is a 19-item questionnaire assessing attitudes related to interprofessional collaboration. Responses were given using a 5-point Likert scale where 1 = Strongly Disagree to 5 = Strongly Agree. The total score is the average of the average scores for each item and ranges from 1 to 5. A higher total score indicates increased positive perceptions toward interprofessional collaboration. (NCT04766996)
Timeframe: Prior to protocol implementation (baseline), halfway through the recruitment period (2 months) and after the last participant has been discharged from the hospital (4 months)

Interventionscore on a scale (Mean)
Baseline
Professional Staff4.35

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Total Post-operative Opioid Requirements With Non-opioid Drug Regimen

Total post-operative opioid requirements (opioid dose) were calculated for participants receiving the non-opioid drug regimen, among participants who required post-operative opioid medication. (NCT04766996)
Timeframe: Up to 5 weeks

Interventionmilligrams (Mean)
Prospective Cases Undergoing Non-opioid Drug Regimen400

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered with the study drug and which did not necessarily have a causal relationship with the study drug. An AE could therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not related to study drug. A TEAE was defined as an AE that started or worsened at the time of or after study drug administration. An AE that occurred during the washout period between drugs was considered treatment emergent to the last drug given. A summary of all Serious Adverse Events and Other Adverse Events (nonserious) regardless of causality is located in the 'Reported Adverse Events' Section. (NCT05319899)
Timeframe: Day 1 through 14 days following final dose (up to Day 43)

InterventionParticipants (Count of Participants)
Treatment A: ALXN1840 (Fasted)6
Treatment B: Omeprazole + ALXN1840 (Fasted)5
Treatment C: Omeprazole + ALXN1840 (Fed)6

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Maximum Measured Plasma Concentration (Cmax) of Total Mo

(NCT05319899)
Timeframe: Predose (0 hour) up to 192 hours postdose

Interventionng/mL (Mean)
Treatment A: ALXN1840 (Fasted)330
Treatment B: Omeprazole + ALXN1840 (Fasted)401
Treatment C: Omeprazole + ALXN1840 (Fed)385

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Area Under the Plasma Concentration Versus Time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Total Molybdenum (Mo)

AUC0-t was calculated by the linear trapezoidal method. (NCT05319899)
Timeframe: Predose (0 hour) up to 192 hours postdose

Interventionhours*ng/mL (Mean)
Treatment A: ALXN1840 (Fasted)14531
Treatment B: Omeprazole + ALXN1840 (Fasted)18537
Treatment C: Omeprazole + ALXN1840 (Fed)14536

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered with the study drug and which did not necessarily have a causal relationship with the study drug. An AE could therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not related to study drug. A TEAE was defined as an AE that started or worsened at the time of or after study drug administration. An AE that occurred during the washout period between drugs was considered treatment emergent to the last drug given. A summary of all Serious Adverse Events and Other Adverse Events (nonserious) regardless of causality is located in the 'Reported Adverse Events' Section. (NCT05319912)
Timeframe: Day 1 through 14 days following final dose (up to Day 43)

InterventionParticipants (Count of Participants)
Treatment A: ALXN1840 (Fasted)4
Treatment B: ALXN1840 (Fed)2
Treatment C: Omeprazole + ALXN1840 (Fasted)6

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Maximum Measured Plasma Concentration (Cmax) of Total Mo

(NCT05319912)
Timeframe: Predose (0 hour) up to 192 hours postdose

Interventionng/mL (Mean)
Treatment A: ALXN1840 (Fasted)376
Treatment B: ALXN1840 (Fed)187
Treatment C: Omeprazole + ALXN1840 (Fasted)442

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Area Under the Plasma Concentration Versus Time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Total Molybdenum (Mo)

AUC0-t was calculated by the linear trapezoidal method. (NCT05319912)
Timeframe: Predose (0 hour) up to 192 hours postdose

Interventionhours*ng/mL (Mean)
Treatment A: ALXN1840 (Fasted)16026
Treatment B: ALXN1840 (Fed)5740
Treatment C: Omeprazole + ALXN1840 (Fasted)19809

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Number of Participants Completing at Least 90% of All Prescribed Medications

Patients were provided a medication log to self-report drug compliance. After completion of their assigned regimen, subjects were scheduled for a post-treatment visit, 4 weeks after completion of the study. At the post-treatment visit, a medication log and empty pill bottles were brought in to ascertain compliance (defined as completing at least 90% of all prescribed medications). (NCT05342532)
Timeframe: end of study at 6 weeks

InterventionParticipants (Count of Participants)
High Dose Dual Therapy58
Standard Triple Therapy54

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Number of Participants With Protocol Specific Adverse Events

Patient tolerability determined by adverse event rates noted by the presence of abdominal pain, diarrhea, dysgeusia, nausea, vomiting, dysphagia (NCT05342532)
Timeframe: end of study at 6 weeks

InterventionParticipants (Count of Participants)
High Dose Dual Therapy5
Standard Triple Therapy20

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Number of Participant With Eradication of Disease

The number of participants with eradication after high dose dual therapy vs clarithromycin triple therapy after treatment. (NCT05342532)
Timeframe: end of study at 6 weeks

InterventionParticipants (Count of Participants)
High Dose Dual Therapy37
Standard Triple Therapy42

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