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flurbiprofen

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Description

Flurbiprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is used to treat pain and inflammation. It is available as a generic drug and is sold under the brand names Ansaid, Ocufen, and Flo-Nap. Flurbiprofen is a propionic acid derivative. It is a racemate, a mixture of equal amounts of two enantiomers (optical isomers). The synthesis of flurbiprofen involves several steps, including the reaction of 2-fluoro-4-bromobenzoyl chloride with diethyl malonate followed by hydrolysis and decarboxylation to give the desired product. Flurbiprofen inhibits the production of prostaglandins, which are chemicals that cause pain and inflammation. It is used to treat a variety of conditions, including rheumatoid arthritis, osteoarthritis, gout, and menstrual cramps. Flurbiprofen is also used to treat pain associated with dental procedures and surgery. Flurbiprofen is generally well tolerated, but side effects can occur. The most common side effects are gastrointestinal upset, such as heartburn, nausea, and stomach pain. Flurbiprofen can also increase the risk of bleeding in the stomach or intestines. Flurbiprofen is an important drug for the treatment of pain and inflammation. It is effective in treating a variety of conditions and is generally well tolerated. Flurbiprofen is studied to improve its efficacy, reduce its side effects, and develop new formulations. Studies are being conducted to evaluate the potential benefits of flurbiprofen in the treatment of other conditions, such as cancer and Alzheimer's disease. '
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Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. [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 CID3394
CHEMBL ID563
CHEBI ID5130
SCHEMBL ID2248
SCHEMBL ID10029029
MeSH IDM0008647

Synonyms (257)

Synonym
[1,1'-biphenyl]-4-acetic acid, 2-fluoro-?-methyl-
bdbm50074922
2-fluoro-alpha-methyl-(1,1''-biphenyl)-4-acetic acid
2-(2-fluoro-[1,1''-biphenyl-4-yl])propanoic acid
HMS3393A05
HMS3268E10
AB00051999-17
BRD-A86044036-001-05-9
nsc685701
MLS000040873 ,
smr000042823
KBIO1_000804
DIVK1C_000804
NCI60_030812
(+-)-2-fluoro-alpha-methyl-4-biphenylacetic acid
anmetarin
2-(2-fluoro-[1,1'-biphenyl-4-yl])propanoic acid
flugalin
ocuflur
CHEBI:5130 ,
yakuban
mks-11
2-(2-fluorobiphenyl-4-yl)propanoic acid
2-fluoro-alpha-methyl-(1,1'-biphenyl)-4-acetic acid
flurbiprofeno [inn-spanish]
u 27,182
fluriproben
(1,1'-biphenyl)-4-acetic acid, 2-fluoro-alpha-methyl-
flurbiprofene [inn-french]
flurbiprofenum [inn-latin]
einecs 225-827-6
4-biphenylacetic acid, 2-fluoro-alpha-methyl-
(1,1'-biphenyl)-4-acetic acid, 2-fluoro-alpha-methyl-, (+-)-
fp 70
flubiprofen
u 27182
ccris 3708
bts 18322
(+-)-2-(2-fluoro-4-biphenylyl)propionic acid
c15h13fo2
SPECTRUM_001096
cas-5104-49-4
NCGC00016654-01
BSPBIO_000794
BSPBIO_002050
BPBIO1_000874
IDI1_000804
PRESTWICK3_000917
SPECTRUM5_000720
u-27182
zepolas
antadys
froben
bts-18322
stayban
cebutid
flurofen
adfeed
2-fluoro-alpha-methyl-4-biphenylacetic acid
3-fluoro-4-phenylhydratropic acid
FLP ,
BIM-0051387.0001
AB00051999
flurbiprofen
C07013
5104-49-4
flurbiprofen, cyclooxygenase inhibitor
MLS000758198
(+/-)-2-fluoro-alpha-methyl-4-biphenylacetic acid
DB00712
ansaid
rac-flurbiprofen
nsc-685701
D00330
ansaid (tn)
flurbiprofen (jp17/usp/inn)
PRESTWICK2_000917
NCGC00025287-03
NCGC00025287-04
MLS000028441
KBIOSS_001576
KBIO3_001270
KBIO2_006712
KBIOGR_001255
KBIO2_004144
KBIO2_001576
NINDS_000804
SPECTRUM4_000558
SPECTRUM3_000435
SPBIO_001209
PRESTWICK1_000917
SPBIO_002983
SPECTRUM2_001025
PRESTWICK0_000917
SPECTRUM1500308
MLS001201729
MLS001401361
HMS2051A05
HMS2090I06
HMS2091F21
bts 18,322
CHEMBL563 ,
u-27,182
nsc-757037
HMS502I06
FT-0660285
inchi=1/c15h13fo2/c1-10(15(17)18)12-7-8-13(14(16)9-12)11-5-3-2-4-6-11/h2-10h,1h3,(h,17,18)
sytbzmrglbwntm-uhfffaoysa-
F0371 ,
2-(2-fluorobiphenyl-4-yl)propionic acid
HMS1570H16
HMS1920O20
2-(3-fluoro-4-phenylphenyl)propanoic acid
STK802101
AKOS004119934
2-(2-fluoro[1,1'-biphenyl]-4-yl)propanoic acid
AO-295/42284050
NCGC00018157-04
NCGC00018157-08
NCGC00018157-05
NCGC00018157-03
HMS2097H16
HMS3259I12
dtxsid0037231 ,
tox21_302353
dtxcid8017231
NCGC00255457-01
BBL010980
nsc757037
pharmakon1600-01500308
tox21_110547
HMS2232I08
mpc7869
CCG-100759
CCG-40243
flurbiprofen [usan:usp:inn:ban:jan]
unii-5gro578klp
flurbiprofenum
flurbiprofeno
nsc 757037
(1)-2-fluoro-alpha-methyl(1,1'-biphenyl)-4-acetic acid
einecs 257-262-6
flurbiprofene
5gro578klp ,
(1,1'-biphenyl)-4-acetic acid, 2-fluoro-alpha-methyl-, (+/-)-
2-(3-fluoro-4-phenyl-phenyl)propanoic acid
FT-0603668
2-(2-fluoro-[1,1'-biphenyl]-4-yl)propanoic acid
NCGC00018157-11
AKOS016340701
HMS3371I05
HMS3370N14
gtpl4194
flurbiprofen [mart.]
flurbiprofen [usp monograph]
(+/-)-2-fluoro-.alpha.-methyl-4-biphenylacetic acid
flurbiprofen [orange book]
flurbiprofen [usan]
flurbiprofen [vandf]
flurbiprofen [usp-rs]
flurbiprofen [mi]
flurbiprofen [inn]
flurbiprofen [ep monograph]
flurbiprofen [who-dd]
(+/-)-2-(2-fluoro-4-biphenylyl)propionic acid
flurbiprofen [jan]
(1,1'-biphenyl)-4-acetic acid, 2-fluoro-.alpha.-methyl-, (+/-)-
HY-10582
MLS006011431
NC00563
NC00009
SCHEMBL2248
KS-5035
2-(2-fluoro-4-biphenylyl)propionic acid
(r/s)-2-fluoro-alpha-methyl-4-biphenylacetic acid
2(2-fluoro-4-biphenylyl)propionic acid
2-(2-fluoro-4-biphenylyl)-propionic acid
alpha-methyl-2-fluoro-4-biphenylylacetic acid
2 -(2-fluoro-4-biphenylyl)propionic acid
2-(2-fluoro-biphenyl-4-yl)-propionic acid
2-(2-fluoro-biphenyl-4-yl)propionic acid
(rs)-2-(2-fluorobiphenyl-4-yl)propionic acid
flurbiprofen o
SCHEMBL10029029
51543-38-5
MLS006011931
Q-201129
flurbiprofen, antibiotic for culture media use only
2-fluoro-?-methyl-[1,1'-biphenyl]-4-acetic acid
2-fluoro-alpha-methyl-[1,1'-biphenyl]-4-a cetic acid
HB3049
(.+/-.)-2-(2-fluoro-4-biphenylyl)propionic acid
2-fluoro-.alpha.-methyl(1,1'-biphenyl)-4-acetic acid
2-fluoro-.alpha.-methyl-4-biphenylacetic acid
[1,1'-biphenyl]-4-acetic acid, 2-fluoro-.alpha.-methyl-, (.+/-.)-
ocufen (salt/mix)
(.+/-.)-2-fluoro-.alpha.-methyl-4-biphenylacetic acid
4-biphenylacetic acid, 2-fluoro-.alpha.-methyl-
(.+/-.)-flurbiprofen
[1,1'-biphenyl]-4-acetic acid, 2-fluoro-.alpha.-methyl-
2-(2-fluoro[1,1'-biphenyl]-4-yl)propanoic acid #
HMS3649K11
AB00051999_18
OPERA_ID_777
mfcd00079303
dl-flurbiprofen
AC-8106
flurbiprofen, united states pharmacopeia (usp) reference standard
flurbiprofen, european pharmacopoeia (ep) reference standard
HMS3655G19
flurbiprofen, pharmaceutical secondary standard; certified reference material
flurbiprofen; (2rs)-2-(2-fluorobiphenyl-4-yl)propanoic acid
SR-01000003043-5
SR-01000003043-2
sr-01000003043
SR-01000003043-6
SBI-0051387.P003
HMS3714H16
2-fluoro--methyl-(1,1'-biphenyl)-4-acetic acid
flurbiprofen (nsaid)
FT-0771103
Q419890
flurbiprofen - cas 5104-49-4
FT-0668760
flurbiprofen (ansaid)
HMS3678N15
flurbiprofen,(s)
SR-01000003043-14
BCP09086
BCP13426
HMS3414N17
(r)-flurbiprofen;mpc7869
NCGC00018157-13
2-(2-fluoro-1,1'-biphenyl-4-yl)propanoic acid
(s)-(+)-2-fluoro-alpha-methyl-4-biphenylaceticacid
nsc755404
(+-)flurbiprofen
nsc-755404
[1,1'-biphenyl]-4-acetic acid, 2-fluoro-a-methyl-, (a+/-)-
EN300-7479231
Z2216885233
(2rs)-2-(2-fluorobiphenyl-4-yl)propanoic acid
2-fluoro-alpha-methyl(1,1'-biphenyl)-4-acetic acid
flurbiprofen (usan:usp:inn:ban:jan)
flurbiprofen (usp-rs)
flurbiprofen (mart.)
flurbiprofen (ep monograph)
flurbiprofenum (inn-latin)
2-(2-fluoro-(1,1'-biphenyl-4-yl))propanoic acid
flurbiprofeno (inn-spanish)
m02aa19
antiphlamine pain relieving
m01ae09
r02ax01
s01bc04
flurbiprofen (usp monograph)
flurbiprofene (inn-french)

Research Excerpts

Overview

Flurbiprofen axetil (FA) is a commonly prescribed agent to relieve perioperative pain, but the relationship between FA and postoperative acute kidney injury (AKI) remains unclear. R-Flurboprofen is a nonsteroidal antienflammatory drug and has potential anticancer activity.

ExcerptReferenceRelevance
"Flurbiprofen axetil (FA) is a prodrug of flurbiprofen (FP), and it is hydrolyzed to the active FP by carboxylesterase in plasma after intravenous injection. "( Comparison of in vivo pharmacokinetic behaviors of R- and S-flurbiprofen after intravenous injection of flurbiprofen axetil.
He, Y; Li, M; Qin, F; Qin, M; Tian, B; Zhi, D, 2023
)
2.6
"Flurbiprofen (FB) is an effective nonsteroidal anti-inflammatory and BCS class II drug and its poor solubility plays a critical role in limiting its bioavailability. "( The effect of critical process parameters of the high pressure homogenization technique on the critical quality attributes of flurbiprofen nanosuspensions.
Celebi, N; Ilbasmis-Tamer, S; Oktay, AN, 2019
)
2.16
"R-Flurbiprofen is a nonsteroidal antienflammatory drug and has potential anticancer activity."( Combination of Paclitaxel and R-flurbiprofen loaded PLGA nanoparticles suppresses glioblastoma growth on systemic administration.
Caban-Toktas, S; Capan, Y; Dalkara, T; Esendagli, G; Karlı Oguz, K; Khan, M; Lule, S; Mut, M; Sahin, A; Soylemezoglu, F; Vural, I, 2020
)
1.4
"Flurbiprofen, an NSAID, is a water insoluble drug that is also notorious for gastric irritation and inflammation. "( Clove oil based co-surfactant free microemulsion of flurbiprofen: Improved solubility with ameliorated drug-induced gastritis.
Asghar, S; Asif, M; Faran, SA; Gohar, UF; Hussain, T; Khalid, I; Khalid, SH; Khan, IU; Rehman, A; Tanzeem, MU; Ullah, MS, 2019
)
2.21
"Flurbiprofen axetil (FA) is a commonly prescribed agent to relieve perioperative pain, but the relationship between FA and postoperative acute kidney injury (AKI) remains unclear. "( Low dose of flurbiprofen axetil decrease the rate of acute kidney injury after operation: a retrospective clinical data analysis of 9915 cases.
Liao, Q; Ou-Yang, W; Tang, YZ; Wang, D; Yang, SK; Zhang, H; Zhao, MX, 2020
)
2.38
"Flurbiprofen (FB) is an analgesic and anti-inflammatory drug, but its low water solubility (BCS Class II) limits its dermal bioavailability. "( Preparation and in vitro / in vivo evaluation of flurbiprofen nanosuspension-based gel for dermal application.
Celebi, N; Han, S; Ilbasmis-Tamer, S; Oktay, AN; Uludag, O, 2020
)
2.26
"Flurbiprofen is a non-steroidal anti-inflammatory drug. "( Evaluation of bioequivalence of two flurbiprofen axetil injections: A randomized, open-label, double-cycle, and crossover study.
Cai, Y; Dong, L; Wang, J; Wang, R, 2021
)
2.34
"Flurbiprofen axetil is an injectable non-selective cyclooxygenase inhibitor that has a high affinity for inflammatory tissues to achieve targeted drug therapy and prolonged duration of action."( Preoperative flurbiprofen axetil administration for acute postoperative pain: a meta-analysis of randomized controlled trials.
Luo, J; Luo, T; Wang, K; Zheng, L, 2017
)
1.55
"Flurbiprofen axetil is a non-selective cyclooxygenase inhibitor. "( Analgesic effect of different dosage of Flurbiprofen axetil in laparoscopic cholecystectomy in comparison with other analgesic drugs.
Luo, X; Lv, F; Peng, M, 2017
)
2.17
"Flurbiprofen (F) is a nonsteroidal anti-inflammatory drug (NSAID) used therapeutically as the racemate of (R)-enantiomer and (S)-enantiomer. "( Mutual inversion of flurbiprofen enantiomers in various rat and mouse strains.
Angioni, C; de Bruin, N; Ferreirós, N; Geisslinger, G; Hofmann, M; Parnham, MJ; Schmidt, M, 2018
)
2.25
"Flurbiprofen axetil is a targeted analgesic and non steroidal analgesic with lipid microspheres as drug carrier. "( Flurbiprofen axetil: Analgesic effect and adverse reaction.
Ji, L; Zhao, X, 2018
)
3.37
"Flurbiprofen which is a non-steroidal anti-inflammatory drug (NSAID), has been safely used for the control of postoperative patient's morbidity after periodontal plastic surgeries requiring palatal graft harvesting, but there is little information on the efficacy of topical use. "( Oral flurbiprofen spray for mucosal graft harvesting at the palatal area: A randomized placebo-controlled study.
Akkale, H; Eraydin, N; Isler, SC; Ozdemir, B, 2018
)
2.44
"Flurbiprofen is a kind of nonsteroidal anti-inflammatory drug, which has been widely used in clinic for treatment of rheumatoid arthritis and osteoarthritis. "( Enantioseparation of flurbiprofen enantiomers using chiral ionic liquids by liquid-liquid extraction.
Cui, X; Ding, Q; He, CH; Shan, RN; Wu, KJ, 2019
)
2.28
"Flurbiprofen is a nonsteroidal anti-inflammatory agent preferentially used for local oromucosal treatment of painful and/or inflammatory conditions of the oropharynx such as gingivitis, stomatitis, periodontitis, pharyngitis and laryngitis. "( Influence of the oral dissolution time on the absorption rate of locally administered solid formulations for oromucosal use: the flurbiprofen lozenges paradigm.
De Gregori, S; Imberti, R; Lisi, L; Navarra, P, 2014
)
2.05
"Flurbiprofen axetil (FPA) is an injection product and a prodrug of a non-steroidal anti-inflammatory drug (NSAID). "( A novel injection strategy of flurbiprofen axetil by inhibiting protein binding with 6-methoxy-2-naphthylacetic acid.
Ikeda, T; Kawai, K; Nishio, T; Ogata, K; Setoguchi, N; Takamura, N; Tanda, K; Tokunaga, J; Yamasaki, T, 2016
)
2.17
"Flurbiprofen axetil (FA) is a potent non-steroidal anti-inflammatory drug (NSAID). "( Intravenous flurbiprofen axetil accelerates restoration of bowel function after colorectal surgery.
Chen, J; Chen, W; Lou, F; Tan, Z; Xu, Y, 2008
)
2.17
"Flurbiprofen is a non-selective non-steroidal anti-inflammatory drug (NSAID), related to ibuprofen and naproxen, used to treat acute and chronic painful conditions. "( Single dose oral flurbiprofen for acute postoperative pain in adults.
Derry, S; McQuay, HJ; Moore, RA; Sultan, A, 2009
)
2.14
"Flurbiprofen acts as a nonselective inhibitor for cyclooxygenases (COX-1 and COX-2), but its impact on hepatic ischemia/reperfusion (I/R) injury remains unclear. "( Flurbiprofen, a cyclooxygenase inhibitor, protects mice from hepatic ischemia/reperfusion injury by inhibiting GSK-3β signaling and mitochondrial permeability transition.
Chen, H; Fu, H; Guo, M; Liu, F; Shi, X; Wang, C; Wang, Q; Xu, H, 2012
)
3.26
"Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) that is commonly used to control moderate postoperative pain and is not associated with respiratory inhibition."( Intravenous flurbiprofen for post-thymectomy pain relief in patients with myasthenia gravis.
Chen, Z; Chou, CW; Liu, W; Luo, H; Su, C; Su, Y; Zou, J, 2012
)
1.48
"Flurbiprofen is a non-steroidal anti-inflammatory compound with strong antifungal activity, which is not found in two well known and medically used antifungal organic acids like benzoic and salicylic acids."( Flurbiprofen, a unique non-steroidal anti-inflammatory drug with antimicrobial activity against Trichophyton, Microsporum and Epidermophyton species.
Adak, M; Bose, SK; Chowdhury, B, 2003
)
3.2
"Flurbiprofen (FL) is a chiral 2-arylpropionate used clinically as the racemate (rac-FL). "( In vitro release and stereoselective disposition of flurbiprofen loaded to poly(D,L-lactide- co-glycolide) nanoparticles in rats.
Aboul-Enein, HY; Radwan, MA, 2004
)
2.02
"Nitroflurbiprofen is a nitrosylated flurbiprofen analog under development by NicOx for the potential treatment of urinary incontinence, Alzheimer's disease (AD) and the prevention and treatment of accelerated bone resorption associated with disorders such as osteoporosis, inflammatory joint disease and Paget's disease. "( Nitroflurbiprofen (NicOx).
Scatena, R, 2004
)
1.35
"Flurbiprofen is a powerful nonsteroidal anti-inflammatory drug (NSAID)."( Flurbiprofen and HCT1026 protect mice against acute pancreatitis-associated lung injury.
Bhatia, M; Huang, J; Moochhala, SM; Moore, PK, 2005
)
2.49
"Flurbiprofen is a nonsteroidal anti-inflammatory drug used as a racemic mixture. "( Predominant contribution of UDP-glucuronosyltransferase 2B7 in the glucuronidation of racemic flurbiprofen in the human liver.
Kamimura, H; Mano, Y; Usui, T, 2007
)
2
"Flurbiprofen is a potent inhibitor of platelet aggregation as compared to aspirin (160 to 2200 more potent)."( [Effect of flurbiprofen on platelet functions. Study of its interference with the synthesis of platelet thromboxane and production of prostacyclin by the rabbit aorta].
Bara, L; Caen, J; Lecrubier, C; Levy-Toledano, S; Maclouf, J; Samama, M,
)
1.24
"As flurbiprofen is a more potent inhibitor of prostaglandin synthesis than indomethacin, these data cast doubt on the theory that nonsteroidal anti-inflammatory drugs antagonize the action of diuretics by prostaglandin synthetase inhibition."( The effect of flurbiprofen on the responses to frusemide in healthy volunteers.
Hind, ID; Kendall, MJ; Rees, JA; Symmons, DP, 1983
)
1.14
"Flurbiprofen is a useful treatment for idiopathic detrusor instability and is well tolerated by most patients."( Evaluation of flurbiprofen in detrusor instability.
Cardozo, LD; Hole, D; Robinson, H; Stanton, SL, 1980
)
1.34
"Flurbiprofen is a nonsteroidal anti-inflammatory (NSAI) agent currently undergoing clinical investigation. "( Topical flurbiprofen or prednisolone. Effect on corneal wound healing in rabbits.
Bergamini, MV; Gruenberg, P; Miller, D; Miller, R, 1981
)
2.14
"Flurbiprofen is a propionic acid-derived non-steroidal anti-inflammatory drug (NSAID) used widely in the treatment of rheumatism and non-arthritic pain. "( Pharmacokinetic comparison of oral and local action transcutaneous flurbiprofen in healthy volunteers.
Glass, RC; Leutenegger, E; Singlas, E; Taburet, AM; Thomas, F, 1995
)
1.97
"Flurbiprofen is a chiral nonsteroidal anti-inflammatory drug (NSAID) of the 2-arylpropionic acid class. "( Clinical pharmacokinetics of flurbiprofen and its enantiomers.
Davies, NM, 1995
)
2.03
"Flurbiprofen is a chiral non-steroidal anti-inflammatory drug used in the treatment of pain or inflammation. "( Role of cytochrome P450 2C9 and an allelic variant in the 4'-hydroxylation of (R)- and (S)-flurbiprofen.
Gonzalez, FJ; Korzekwa, KR; Rosenbluth, BW; Tracy, TS; Wrighton, SA, 1995
)
1.95
"Flurbiprofen is a chiral 2-arylpropionate used clinically as a racemate. "( Dose-dependency of flurbiprofen enantiomer pharmacokinetics in the rat.
Berry, BW; Jamali, F; Wright, MR, 1994
)
2.06
"Flurbiprofen (Ansaid) is a new NSAID for the treatment of rheumatoid arthritis and osteoarthritis."( Nonsteroidal antiinflammatory drug desensitization using flurbiprofen (Ansaid)
Brown, JS; Douglas, DM; Ward, L, 1993
)
1.25
"Flurbiprofen appears to be an effective drug for the prevention of reinfarction after coronary reperfusion and in reducing the need for secondary revascularization procedures."( Evaluation of flurbiprofen for prevention of reinfarction and reocclusion after successful thrombolysis or angioplasty in acute myocardial infarction. The Flurbiprofen French Trial.
Brochier, ML, 1993
)
1.37
"Flurbiprofen (1) is an analgesic, antipyretic and antiinflammatory agent which is practically insoluble in water. "( Formulation of an aqueous injection of flurbiprofen.
Gupta, GD; Jain, NK; Jain, S, 1997
)
2.01
"Flurbiprofen (Ansaid) is a newly released nonsteroidal antiinflammatory drug (NSAID) that is a potent inhibitor of prostaglandin synthesis. "( Flurbiprofen (Ansaid) cross-sensitivity in an aspirin-sensitive asthmatic patient.
Bosso, JV; Creighton, D; Stevenson, DD, 1992
)
3.17
"Flurbiprofen is a water-soluble, non-steroid anti-inflammatory agent and is capable of marked inhibition of prostaglandin synthesis. "( [Effects of an anti-prostaglandin agent added to the irrigation solution on damage to the anterior segment in monkey eyes induced by pars plana vitrectomy].
Kawamura, A; Matsui, M; Shimada, H; Shingyouchi, F; Shingyouchi, S, 1989
)
1.72
"Flurbiprofen appears to be a satisfactory alternative to phenylbutazone in the management of acute gouty arthritis."( Double-blind trial of flurbiprofen and phenylbutazone in acute gouty arthritis.
Butler, RC; Goddard, DH; Higgens, CS; Hollingworth, P; Pease, CT; Scott, JT; Stodell, MA, 1985
)
1.31
"Flurbiprofen appears to be an excellent alternative to phenylbutazone in the management of patients with ankylosing spondylitis."( Flurbiprofen in the treatment of ankylosing spondylitis. A comparison with phenylbutazone.
Brinn, EL; Lamborn, KR; Lomen, PL; Sattler, LP; Turner, LF, 1986
)
2.44
"Flurbiprofen is an excellent treatment for the control of pain and inflammation in patients with ankylosing spondylitis."( Flurbiprofen in the treatment of ankylosing spondylitis. A comparison with indomethacin.
Brinn, EL; Lamborn, KR; Lomen, PL; Turner, LF, 1986
)
2.44

Effects

Flurbiprofen has been shown to bind more strongly than diclofenac to the same site of albumin. The mechanism remains unclear as to how the drug reduces cerebral ischemia/reperfusion injury.

ExcerptReferenceRelevance
"Flurbiprofen axetil has the efficacy of targeted analgesia."( Effect of oxycodone hydrochloride combined with flurbiprofen axetil for intravenous patient-controlled analgesia in lower abdominal patients: A randomized trial.
Fang, J; Lian, Y; Wu, Y; Xiang, X; Yuan, X, 2018
)
1.46
"Flurbiprofen spray has been successfully used for treatment of oral inflammations, but its effects on postoperative sore throat and hoarseness are unknown."( Oral flurbiprofen spray for postoperative sore throat and hoarseness: a prospective, randomized, double-blind, placebo-controlled study.
Gul, F; Muderris, T; Sancak, M; Tezcan, G; Ugur, G, 2019
)
1.75
"Flurbiprofen has been shown to bind more strongly than diclofenac to the same site of albumin."( Albumin-binding of diclofenac and the effect of a site II inhibitor in the aqueous humor of cataract patients with the instillation of diclofenac.
Arimori, K; Ogata, K; Osaki, T; Ozaki, M; Setoguchi, N; Takamura, N; Tokunaga, J, 2014
)
1.12
"Flurbiprofen axetil has been reported to reduce the pain of injection."( Efficacy and safety of flurbiprofen axetil in the prevention of pain on propofol injection: a systematic review and meta-analysis.
Bao, H; Luo, Z; Shi, H; Wang, H; Xu, L; Yu, Y; Zhang, L; Zhang, X; Zhang, Y; Zhao, Y; Zhu, J, 2014
)
1.43
"Flurbiprofen has been shown to reduce cerebral ischemia/reperfusion injury in both focal and global cerebral ischemia models, but the mechanism remains unclear."( The Akt/GSK-3β pathway mediates flurbiprofen-induced neuroprotection against focal cerebral ischemia/reperfusion injury in rats.
Chen, L; Liu, X; Sun, B; Wei, X; Xiang, Y; Zhang, X, 2011
)
1.37
"(R)-flurbiprofen has been generally well tolerated at high doses in clinical trials."( Drug evaluation: (R)-flurbiprofen--an enantiomer of flurbiprofen for the treatment of Alzheimer's disease.
Geerts, H, 2007
)
1.14
"Flurbiprofen has been shown to be effective in relieving symptoms in the degenerative and inflammatory arthritides and side-effects have not proved a problem."( A long-term assessment of flurbiprofen.
Marsh, BD; Sheldrake, FE; Webber, JM, 1977
)
1.28
"Flurbiprofen has been introduced more recently and has been accepted largely because of a better patient comfort."( [Comparison of the anti-miotic effect of 0.03% flurbiprofen with 1% indomethacin in cataract extraction].
Beati, D; Gennari, G; Ortelli, G; Stucchi, CA; Vignanelli, M, 1991
)
1.26
"Flurbiprofen has been shown to inhibit cyclo-oxygenase metabolism of arachidonic acid to thromboxane A2 (TxA2), resulting in the inhibition of platelet aggregation. "( Relative effects of flurbiprofen on platelet 12-hydroxy-eicosatetraenoic acid and thromboxane A2 production: influence on collagen-induced platelet aggregation and adhesion.
Buchanan, MR; Van Ryan-McKenna, J, 1989
)
2.04
"Flurbiprofen has been compared with phenylbutazone in a double-blind study involving 33 patients with acute gout. "( Double-blind trial of flurbiprofen and phenylbutazone in acute gouty arthritis.
Butler, RC; Goddard, DH; Higgens, CS; Hollingworth, P; Pease, CT; Scott, JT; Stodell, MA, 1985
)
2.03

Actions

R-flurbiprofen was used because it is able to reduce neuropathic pain in young mice in part by increasing anandamide. Flurbip rofen axetil can produce preemptive analgesia and reduce the tramadol dose during postoperative PCIA in patients undergoing postburn plastic operations.

ExcerptReferenceRelevance
"Flurbiprofen axetil can inhibit the growth of cervical cancer transplanted tumor in nude mice and this inhibitory effect was maximal in Cf50 group."( THE INVESTIGATION OF EFFECT OF FLURBIPROFEN AXETIL ON THE TISSUE GROWTH AND THE CONTENT OF PGE2 IN CERVICAL CANCER.
Chen, G; Li, K; Lu, J; Sun, X; Wang, S, 2016
)
1.44
"R-flurbiprofen was used because it is able to reduce neuropathic pain in young mice in part by increasing anandamide."( Anandamide deficiency and heightened neuropathic pain in aged mice.
Bishay, P; Ferreirós, N; Galve-Roperh, I; Häussler, A; Lim, HY; Oertel, B; Tegeder, I, 2013
)
0.95
"Flurbiprofen may increase the concentration of moxifloxacin in aqueous humor."( Comparative evaluation of aqueous and plasma concentration of topical moxifloxacin alone and with flurbiprofen in patients of cataract surgery.
Biswas, S; Dutta, BK; Haldar, M; Halder, S; Mandal, TK; Mondal, KK,
)
1.79
"Flurbiprofen axetil can produce preemptive analgesia and reduce the tramadol dose during postoperative PCIA in patients undergoing postburn plastic operations."( [Effect of preemptive analgesia with flurbiprofen axetil on patient-controlled intravenous analgesia with tramadol in patients undergoing postburn plastic surgery].
Liu, C; Lu, JC; Zhang, XF, 2009
)
2.07
"Nitroflurbiprofen was shown to inhibit nitric oxide synthase induction caused by lipopolysaccharide administration, while flurbiprofen had no effect on nitric oxide synthase induction."( Effect of a new non-steroidal anti-inflammatory drug, nitroflurbiprofen, on the expression of inducible nitric oxide synthase in rat neutrophils.
Adami, A; Benoni, G; Cuzzolin, L; Del Soldato, P; Mariotto, S; Suzuki, H, 1995
)
0.99

Treatment

The flurbiprofen treatment, 30 min prior to ischemia and 4 h post-reperfusion, afforded significant neuroprotection from ischemic injury as evidenced by reduction in cerebral infarct volume and neurobehavioral deficit. The EAE-evoked upregulation of pro-inflammatory genes in the spinal cord was strongly reduced.

ExcerptReferenceRelevance
"Flurbiprofen treatment reduced the expression of immaturely glycosylated SERT and enhanced the expression of maturely glycosylated SERT."( Effects of flurbiprofen on the functional regulation of serotonin transporter and its misfolded mutant.
Adachi, N; Asano, M; Harada, K; Hide, I; Hirakawa, H; Kikkawa, S; Murakawa, S; Noguchi, S; Sakai, N; Taguchi, K; Tanaka, S; Ueyama, T, 2022
)
1.83
"The flurbiprofen treatment simultaneously administered."( Therapeutic potential of flurbiprofen against obesity in mice.
Baba, S; Hosoi, T; Ozawa, K, 2014
)
1.19
"R-flurbiprofen treatment increased CD4(+)CD25(+)FoxP3(+) regulatory T cells, CTLA4(+) inhibitory T cells and interleukin-10, whereas the EAE-evoked upregulation of pro-inflammatory genes in the spinal cord was strongly reduced."( R-flurbiprofen attenuates experimental autoimmune encephalomyelitis in mice.
Altmann, C; Bishay, P; de Bruin, N; Ferreirós, N; Geisslinger, G; Häussler, A; Lötsch, J; Männich, J; Parnham, MJ; Schmitz, K; Tegeder, I; Ultsch, A, 2014
)
1.68
"The flurbiprofen treatment, 30 min prior to ischemia and 4 h post-reperfusion, afforded significant neuroprotection from ischemic injury as evidenced by reduction in cerebral infarct volume and neurobehavioral deficit."( Neuroprotective effect of flurbiprofen in focal cerebral ischemia: the possible role of ASIC1a.
Mishra, V; Raghubir, R; Verma, R, 2010
)
1.14
"Flurbiprofen treatment of ND rats replicated many of the biochemical and physiological abnormalities of EDN, i.e., reduced motor nerve conduction velocity (MNCV), total and endoneurial nerve blood flow (NBF), Na,K-ATPase activity, and myo-inositol (MI) and taurine content."( Dissection of metabolic, vascular, and nerve conduction interrelationships in experimental diabetic neuropathy by cyclooxygenase inhibition and acetyl-L-carnitine administration.
Greene, DA; Larkin, D; Li, F; Marinescu, V; Pop-Busui, R; Stevens, MJ; Sullivan, K; Van Huysen, C, 2002
)
1.04
"Flurbiprofen-treated rats showed severe gastrointestinal ulcerations (bleeding in 3/8 rats) and nefrotoxicity, which was not observed in nitroflurbiprofen-treated cirrhotic rats."( Nitroflurbiprofen, a nitric oxide-releasing cyclooxygenase inhibitor, improves cirrhotic portal hypertension in rats.
Fevery, J; Laleman, W; Nevens, F; Van der Elst, I; Van Landeghem, L; Zeegers, M, 2007
)
1.57
"Flurbiprofen-treated eyes showed a significantly smaller percent (32.6%) decrease in intraocular pressure (IOP) one day after ALT as compared to eyes receiving placebo (43.8%)."( Nonsteroidal anti-inflammatory agents after argon laser trabeculoplasty. A trial with flurbiprofen and indomethacin.
Hotchkiss, ML; Pollack, IP; Quigley, HA; Robin, AL, 1984
)
1.21
"Flurbiprofen is a useful treatment for idiopathic detrusor instability and is well tolerated by most patients."( Evaluation of flurbiprofen in detrusor instability.
Cardozo, LD; Hole, D; Robinson, H; Stanton, SL, 1980
)
1.34
"In flurbiprofen-treated dogs regional function returned to normal within 5 min of reperfusion in both the subendocardium (%SS preocclusion = 17.2+/-2.0%; 5 min reperfusion = 17.8+/-3.1%; P = NS) and in the midmyocardium (%SS preocclusion = 17.8+/-2.2%; 5 min reperfusion = 17.9+/-2.3%; P = NS) and was not significantly different after 5 h of reperfusion from what it was before coronary occlusion."( Early recovery of regional performance in salvaged ischemic myocardium following coronary artery occlusion in the dog.
Braunwald, E; Darsee, JR; Kloner, RA, 1981
)
0.78
"When flurbiprofen-treated cells were exposed to melphalan there was no protection against cytotoxicity."( Flurbiprofen, a non-steroid anti-inflammatory agent, protects cells against hypoxic cell radiosensitizers in vitro.
Jinks, S; Millar, BC; Powles, TJ, 1981
)
2.16
"Flurbiprofen-treated patients achieved good Snellen visual acuity (better than 20/40) sooner than vehicle-treated patients.(ABSTRACT TRUNCATED AT 250 WORDS)"( Efficacy of topical flurbiprofen and indomethacin in preventing pseudophakic cystoid macular edema. Flurbiprofen-CME Study Group I.
Solomon, LD, 1995
)
1.34
"Flurbiprofen treatment improved contrast sensitivity in patients with and without CME significantly at 12 cycles per degree."( Effects of flurbiprofen and indomethacin on acute cystoid macular edema after cataract surgery: functional vision and contrast sensitivity.
Abelson, M; Cheetham, JK; DeGryse, RE; Ginsburg, AP, 1995
)
1.4
"Flurbiprofen-treated patients however, demonstrated a significantly greater proportion of sites (8.0%) with bone gain when compared to the placebo group (3.3%)."( The use of topical flurbiprofen as an adjunct to non-surgical management of periodontal disease.
Aitken, D; Benn, DK; Heasman, PA; Kelly, PJ; Seymour, RA, 1993
)
1.34
"The flurbiprofen-treated group served as the control group."( Topical 0.5% ketorolac vs 0.03% flurbiprofen for inhibition of miosis during cataract surgery.
Apple, DJ; Solomon, KD; Stewart, JA; Turkalj, JW; Whiteside, SB, 1997
)
1.06
"Flurbiprofen co-treatment markedly attenuated these actions of pentoxifylline on nerve conduction and blood flow whereas NG-nitro-L-arginine was without effect."( Pentoxifylline effects on nerve conduction velocity and blood flow in diabetic rats.
Cameron, NE; Cotter, MA; Flint, H, 2000
)
1.03
"In flurbiprofen-treated animals, values were 42 +/- 8 and 160 +/- 18 nmol/gm at day 4, significantly attenuated from burn alone."( Topical flurbiprofen decreases burn wound-induced hypermetabolism and systemic lipid peroxidation.
Daryani, R; Demling, RH; Knox, J; LaLonde, C; Neumann, M; Zhu, DG, 1991
)
1.23
"Flurbiprofen treatment resulted in a significant reduction of the maximum intensity of stromal opacity in some experiments, whereas in other experiments the effect was not statistically significant."( The effect of flurbiprofen on herpes simplex virus type 1 stromal keratitis in mice.
Barfknecht, CF; Epstein, RJ; Hendricks, RL; Schoenwald, RD; Sugar, J, 1990
)
1.36
"The flurbiprofen-treated patients experienced less severe symptoms, demonstrating maximum benefit 3 to 5 days into the drug trial with some loss of effect thereafter."( Hay fever treatment with combined antihistamine and cyclooxygenase-inhibiting drugs.
Brooks, CD; Karl, KJ, 1988
)
0.76
"Flurbiprofen treatment was rated as "excellent" or "good" by approximately half of the patients and physicians following both BID or QID dosing."( Comparison of two dosing schedules of flurbiprofen for patients with rheumatoid arthritis. Twice-daily versus four-times-a-day schedules.
Brown, BL; Daenzer, CL; Hearron, MS; Johnson, JH, 1986
)
1.26
"Many flurbiprofen-treated patients (46 percent) completing the trial followed a relatively low dosage regimen of 50 mg twice daily for more than half the study."( Treatment of osteoarthritis of the knee. A comparison of flurbiprofen and aspirin.
Brinn, EL; Lamborn, KR; Lomen, PL; Porter, GH; Turner, LF, 1986
)
0.97
"Sham treatment and flurbiprofen treatment did not affect Aβ pathology, and a low dose HCT 1026 (10 mg/kg; a nitric oxide-donating flurbiprofen analog that has additional useful properties, including a remarkable gastrointestinal safety) did not affect pathology either, however a higher dose of HCT 1026 (30 mg/kg) did reduce the Aβ load."( Transgenic AD model mice, effects of potential anti-AD treatments on inflammation, and pathology.
Kadish, I; Miettinen, P; van Groen, T, 2011
)
0.69
"Pretreatment with flurbiprofen and thymoxamine appeared to enhance this effect but this was not statistically demonstrated by the study."( Unoprostone isopropyl ester darkens iris color in pigmented rabbits with sympathetic denervation.
Camras, CB; Meza, JL; Toris, CB; Zhan, GL, 2003
)
0.64
"Sham treatment, flurbiprofen, and the low-dose HCT 1026 did not affect pathology; however, a higher dose of HCT 1026 reduced both A load and amount of microglial activation surrounding plaques."( Transgenic AD model mice, effects of potential anti-AD treatments on inflammation and pathology.
Kadish, I; van Groen, T, 2005
)
0.66
"Eyes treated with flurbiprofen and indomethacin showed significantly less conjunctival injection following ALT."( Nonsteroidal anti-inflammatory agents after argon laser trabeculoplasty. A trial with flurbiprofen and indomethacin.
Hotchkiss, ML; Pollack, IP; Quigley, HA; Robin, AL, 1984
)
0.81
"Pretreatment with flurbiprofen completely abolished the febrile reactions to endotoxin."( Endotoxin-induced fever and associated haematological and blood biochemical changes in the goat: the effect of repeated administration and the influence of flurbiprofen.
Schotman, AJ; van Duin, CT; van Miert, AS; Verheijden, JH, 1982
)
0.79
"Eyes treated with flurbiprofen were compared with controls."( Does topical flurbiprofen affect the pupillary response to acetylcholine?
Jackson, H; Mathalone, BM; Patel, CK; Thompson, GM; Westcott, M, 1994
)
0.98
"Pretreatment with flurbiprofen partly antagonized the febrile reactions to r.HuIL-1 alpha."( Effects of flurbiprofen on recombinant human IL-1 alpha-induced fever and associated clinical, haematological and blood biochemical changes in the dwarf goat.
Van Duin, CT; Van Miert, AS; Wensing, T, 1994
)
1
"The treatment with flurbiprofen and indomethacin administered subcutaneously every 12 hours, commenced on the day of S-antigen injection and was continued until the termination of the experiment (12 days)."( Modulation of immune responses by cyclo-oxygenase inhibitors during intraocular inflammation.
Bhattacherjee, P; Jaramillo, A; Paterson, CA; Sonnenfeld, G, 1992
)
0.6
"Pretreatment with flurbiprofen did not affect the IOP lowering that was obtained with timolol or apraclonidine administration."( Effects of topical flurbiprofen on the intraocular pressure lowering effects of apraclonidine and timolol.
Arkin, LM; Cummings, HL; Robin, AL; Sulewski, ME, 1991
)
0.93
"Treatment with flurbiprofen (100 mg twice a day for 5 days), tranexamic acid (1.5 gm three times a day for 3 days and 1 gm twice a day for another 2 days), and an intrauterine contraceptive device releasing 20 micrograms levonorgestrel per day was compared in women with idiopathic menorrhagia. "( A comparison of flurbiprofen, tranexamic acid, and a levonorgestrel-releasing intrauterine contraceptive device in the treatment of idiopathic menorrhagia.
Andersch, B; Andersson, K; Milsom, I; Rybo, G, 1991
)
0.98
"Treatment with flurbiprofen appeared to decrease the severity of inflammation following cataract extraction surgery."( Reduction of inflammation following cataract surgery by the nonsteroidal anti-inflammatory drug, flurbiprofen.
Cheetham, JK; DeGryse, R; Duzman, E; Osterle, C; Sabiston, D; Sumers, K; Tessler, H, 1987
)
0.83

Toxicity

Sustained release formulations of flurbiprofen demonstrate reduced gastroduodenal permeability but shift the site of this side-effect to the more distal intestine. Tarenflurbil is an attractive compound because its usage is not associated with the adverse side effects of NSAIDs.

ExcerptReferenceRelevance
" The other photoproducts, Butibufen and Flurbiprofen did not produce observable toxic effects on cells."( Phototoxicity of non-steroidal anti-inflammatory drugs: in vitro testing of the photoproducts of Butibufen and Flurbiprofen.
Castell, JV; Gómez-Lechón, MJ; Miranda, MA; Morera, IM, 1992
)
0.76
"Data from 58 premarketing studies of the nonsteroidal antiinflammatory drug flurbiprofen were pooled for analyses of adverse drug reactions (ADRs)."( Clinical safety of flurbiprofen.
Assenzo, JR; Brooks, CD; Defesche, CL; Johnson, JH; Linet, OI; Schellenberg, D; Teoh, KW; Turner, LF, 1990
)
0.84
"5 X 10(-3) M was toxic to all cell lines."( Lymphotoxic activity of methyl prednisolone in vitro--I. Comparative toxicity of methyl prednisolone in human cell lines of B and T origin.
Bell, JB; Hall, JG; Hobbs, SM; Jackson, E; Millar, BC, 1987
)
0.27
" Toxic effects were observed for all three drugs at 10 times the therapeutic plasma concentration."( A study of the relative hepatotoxicity in vitro of the non-steroidal anti-inflammatory drugs ibuprofen, flurbiprofen and butibufen.
Castell, JV; Gómez-Lechón, MJ; Larrauri, A, 1988
)
0.49
"Sustained release formulations of flurbiprofen demonstrate reduced gastroduodenal permeability but shift the site of this side-effect to the more distal intestine."( Influence of dosage form on the gastroenteropathy of flurbiprofen in the rat: evidence of shift in the toxicity site.
Davies, NM; Jamali, F, 1997
)
0.83
" They differ mainly in their adverse effects and costs."( Antiplatelet drugs in cardiovascular prevention: take adverse effects and costs into account.
, 2000
)
0.31
"Since assessment of the acute gastrotoxicity of nonsteroidal antiinflammatory drugs (NSAIDs) in rats requires high doses of the drugs, we sought to establish an experimental model with which this adverse NSAID effect can be estimated at therapy-relevant doses."( Estimation of acute flurbiprofen and ketoprofen toxicity in rat gastric mucosa at therapy-relevant doses.
Cabré, F; Holzer, P; Jocic, M; Mauléon, D, 2001
)
0.63
" There was no significant difference in the gastrotoxicity of FBP when the drug was administered subcutaneously or IG, whereas subcutaneously injected R/S-KP was slightly more toxic than IG R/S-KP."( Estimation of acute flurbiprofen and ketoprofen toxicity in rat gastric mucosa at therapy-relevant doses.
Cabré, F; Holzer, P; Jocic, M; Mauléon, D, 2001
)
0.63
"Retrospective analysis of adverse event databases."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
"Reports of adverse events submitted to the FDAs Spontaneous Reporting System and the Adverse Event Reporting System from January 1969-December 2000 for these drugs were analyzed according to the number of adverse events reported for each drug per year from the time the drug was approved until December 2000."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
" Various other factors affected spontaneous reporting of adverse events, as peaks in the number of reports were seen numerous times for each drug after the initial 5-year marketing period."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
"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
"Our results establish that the neurotoxicity related to the Abeta peptide can be captured in vivo by functional imaging and suggest hippocampal subregions most vulnerable to its toxic effects."( Imaging the Abeta-related neurotoxicity of Alzheimer disease.
Brickman, A; Brown, TR; Lee, T; Mayeux, R; Moreno, H; Small, SA; Wu, WE, 2007
)
0.34
" The most common adverse events were diarrhoea (in seven, nine, and five patients in the 800 mg, 400 mg, and placebo groups, respectively), nausea (in seven, seven, and four patients), and dizziness (in five, nine, and four patients)."( Efficacy and safety of tarenflurbil in mild to moderate Alzheimer's disease: a randomised phase II trial.
Black, SE; Hendrix, SB; Laughlin, MA; Swabb, EA; Wilcock, GK; Zavitz, KH, 2008
)
0.35
" Tarenflurbil (R-flurbiprofen, MPC-7869, Myriad Pharmaceuticals) is an attractive compound because its usage is not associated with the adverse side effects of NSAIDs."( Tarenflurbil protection from cytotoxicity is associated with an upregulation of neurotrophins.
Andrews, PM; Hoe, HS; Rebeck, GW; Zhao, X, 2008
)
0.69
"Short-term exposure of transformed cells to cisplatin reduced the clonogenic survival in low-density cultures (without gap junction formation) and in high density (with gap junction formation), but the toxic effect was greater at high density."( Tramadol and flurbiprofen depress the cytotoxicity of cisplatin via their effects on gap junctions.
Harris, AL; He, B; Hong, X; Liu, B; Tao, L; Tong, X; Wang, L; Wang, Q; Ye, H, 2009
)
0.72
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
"Pain on injection is an acknowledged adverse effect (AE) of propofol administration for the induction of general anesthesia."( Efficacy and safety of flurbiprofen axetil in the prevention of pain on propofol injection: a systematic review and meta-analysis.
Bao, H; Luo, Z; Shi, H; Wang, H; Xu, L; Yu, Y; Zhang, L; Zhang, X; Zhang, Y; Zhao, Y; Zhu, J, 2014
)
0.71
" In terms of drug safety, there were no adverse effects (AEs) reported between flurbiprofen axetil-based regimens and placebo regimens."( Efficacy and safety of flurbiprofen axetil in the prevention of pain on propofol injection: a systematic review and meta-analysis.
Bao, H; Luo, Z; Shi, H; Wang, H; Xu, L; Yu, Y; Zhang, L; Zhang, X; Zhang, Y; Zhao, Y; Zhu, J, 2014
)
0.94
" More studies are required to assess its adverse effects."( Efficacy and safety of flurbiprofen axetil in the prevention of pain on propofol injection: a systematic review and meta-analysis.
Bao, H; Luo, Z; Shi, H; Wang, H; Xu, L; Yu, Y; Zhang, L; Zhang, X; Zhang, Y; Zhao, Y; Zhu, J, 2014
)
0.71
" The majority of drug-related adverse events (AEs) included mild dermatitis at the application sites and occurred in 46."( The Long-Term Safety of S-Flurbiprofen Plaster for Osteoarthritis Patients: An Open-Label, 52-Week Study.
Hoshino, Y; Matsumoto, H; Matsushita, I; Otsuka, N; Yataba, I, 2016
)
0.73
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" It is concluded that the synthesized prodrugs have promising pharmacological activities with reduced GI adverse effects than the parent drug."( Flurbiprofen-antioxidant mutual prodrugs as safer nonsteroidal anti-inflammatory drugs: synthesis, pharmacological investigation, and computational molecular modeling.
Abdullah, S; Ahsan, H; Ashraf, Z; Hassan, M; Kanwal, M; Kim, SJ; Waheed, M, 2016
)
1.88
" CDDP-induced nephrotoxicity (CIN) is one of the most severe adverse events associated with the use of CDDP."( Comparison of the nephroprotective effects of non-steroidal anti-inflammatory drugs on cisplatin-induced nephrotoxicity in vitro and in vivo.
Furugen, A; Iseki, K; Kobayashi, M; Narumi, K; Okamoto, K; Saito, Y, 2020
)
0.56
" 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
" Adverse events (AEs) were evaluated as the safety outcome."( Efficacy and safety of S-flurbiprofen plaster in knee osteoarthritis patients: A 2-week randomized controlled Phase III clinical trial compared to diclofenac gel.
Fuady, A; Matsumoto, H; Tomatsu, K; Yasuda, S, 2022
)
1.02
" Adverse drug reactions may be renal, gastrointestinal, hematological, or immunologic."( Efficacy and Safety of NSAIDs in Infants: A Comprehensive Review of the Literature of the Past 20 Years.
Gorenflo, M; Saur, P; van den Anker, JN; van Dyk, M; Welzel, T; Ziesenitz, VC, 2022
)
0.72
" The incidence of adverse drug reactions was 55% in the SFPP group, which is not significantly different from 50% incidence in the control group."( Comparison of efficacy and safety in the combination therapies of duloxetine and S-flurbiprofen plaster, and of duloxetine and conventional NSAIDs for chronic pain in patients with osteoarthritis (OASIS DUAL study).
Koyama, K, 2022
)
0.95
" There were four secondary outcomes, including the extent of pain relief, the change trends of VAS scores, joint function scores measured by the Western Ontario and McMaster University Osteoarthritis Index (WOMAC), and adverse events."( Efficacy and safety of flurbiprofen cataplasms versus loxoprofen sodium cataplasms in knee osteoarthritis: a randomized controlled trial.
Cheng, Y; Guan, Z; Jia, J; Kan, J; Li, D; Liu, J; Wang, Z; Wu, Z; Xue, T; Yuan, P; Zhai, S; Zhang, G; Zhang, H; Zhang, K, 2023
)
1.22
" In addition, the FPC group experienced a significantly lower incidence of adverse events (5."( Efficacy and safety of flurbiprofen cataplasms versus loxoprofen sodium cataplasms in knee osteoarthritis: a randomized controlled trial.
Cheng, Y; Guan, Z; Jia, J; Kan, J; Li, D; Liu, J; Wang, Z; Wu, Z; Xue, T; Yuan, P; Zhai, S; Zhang, G; Zhang, H; Zhang, K, 2023
)
1.22

Pharmacokinetics

Study covers the formulation and pharmacokinetic study of fast-dissolving flurbiprofen tablets using PEG 6000 (hydrophilic carrier) and lactose (adsorbent)

ExcerptReferenceRelevance
" Only minor differences in the pharmacokinetic parameters were observed between the younger and elderly patients."( The pharmacokinetics of flurbiprofen in younger and elderly patients with rheumatoid arthritis.
Antal, EJ; Buchanan, WW; Cauvier, H; Grace, EM; Kean, WF; Rischke, J, 1992
)
0.59
" Flurbiprofen half-life and Tmax were not different."( Pharmacokinetic comparison of flurbiprofen in end-stage renal disease subjects and subjects with normal renal function.
Cefali, EA; Cox, S; Poynor, WJ; Sica, D, 1991
)
1.48
" Pharmacokinetic parameters showed considerable variability within the group of patients, although differences in S(+)/R(-) plasma concentration ratios were small."( The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis.
Aarons, L; Toon, S; Young, MA, 1991
)
0.54
"The pharmacokinetic profile of 200 mg sustained-release flurbiprofen capsules was compared in nine elderly (mean age 84."( A multiple dose pharmacokinetic and tolerance study of once daily 200 mg sustained-release flurbiprofen capsules in young and very elderly patients.
Bird, A; Hamdy, RC; Hill, J; Hind, ID; Le Gallez, P, 1990
)
0.75
" The relative pharmacokinetic parameters of total flurbiprofen determined from plasma samples were Cmax, tmax, Kel, t1/2, and AUC infinity."( Pharmacokinetic interaction between flurbiprofen and antacids in healthy volunteers.
Caillé, G; du Souich, P; Pollock, SR; Stalker, DJ; Vézina, M,
)
0.66
"50 L/h), but an equal half-life (4."( Stereoselective pharmacokinetics of flurbiprofen in humans and rats.
Berry, BW; Jamali, F; Russell, AS; Tehrani, MR, 1988
)
0.55
" No significant differences in elimination rate constant, peak concentration, time to peak concentration, volume of distribution, or elimination half-life were noted among treatments."( Effects of cimetidine or ranitidine on the pharmacokinetics of flurbiprofen.
Cox, SR; Rock, WL; Small, RE; Sullivan, KM; Willis, HE, 1986
)
0.51
" The applicability of the method was demonstrated in a pharmacokinetic ibuprofen experiment in an adult person."( Rapid HPLC-determination of ibuprofen and flurbiprofen in plasma for therapeutic drug control and pharmacokinetic applications.
Askholt, J; Nielsen-Kudsk, F, 1986
)
0.54
" Drug absorption is rapid, drug disappearance half-life is independent of oral dose, and the area under the plasma drug concentration versus time curve increases with increasing oral dose."( Pharmacokinetics of flurbiprofen.
Brooks, CD; Kaiser, DG; Lomen, PL, 1986
)
0.59
" Half-life (2."( Pharmacokinetics of oral and rectal flurbiprofen in children.
Benvenuti, C; D'Amico, E; Hind, ID; Mazzoni, PL; Scaroni, C, 1984
)
0.54
" Plasma concentrations of flurbiprofen and urinary concentrations of the NSAID and its metabolites were measured by high-performance liquid chromatography assay, to enable comparison of the pharmacokinetic parameters for delivery of the drug by both routes."( Pharmacokinetic comparison of oral and local action transcutaneous flurbiprofen in healthy volunteers.
Glass, RC; Leutenegger, E; Singlas, E; Taburet, AM; Thomas, F, 1995
)
0.83
" Sustained release dosage forms are available, which may be beneficial due to the short terminal phase elimination half-life of conventional immediate release flurbiprofen (3 to 6 hours)."( Clinical pharmacokinetics of flurbiprofen and its enantiomers.
Davies, NM, 1995
)
0.78
" This pharmacokinetic study was an effort to understand the pharmacodynamic difference between the two routes of administration observed when the same dose range of drug, given as single daily doses, had been employed in both studies."( Chiral pharmacokinetics of Rac-flurbiprofen and pharmacodynamics of anabolic bone response in the normal rat.
Bigornia, AE; Jee, WS; Murray, ED; Wechter, WJ, 1994
)
0.57
" Previously a significant pharmacokinetic interaction between the enantiomers of flurbiprofen has been reported in both rats and humans."( Dose-dependency of flurbiprofen enantiomer pharmacokinetics in the rat.
Berry, BW; Jamali, F; Wright, MR, 1994
)
0.84
" bolus administration of flurbiprofen to the mouse (n = 4) and the rat (n = 6) with on-line HPLC analysis of microdialysates to unbound concentrations using the in vivo loss of flurbiprofen by retrodialysis carried out just before the start of the pharmacokinetic experiment."( Intravenous microdialysis in the mouse and the rat: development and pharmacokinetic application of a new probe.
Deridder, G; Evrard, PA; Verbeeck, RK, 1996
)
0.6
"The developed techniques can be used to carry out routine pharmacokinetic studies in the mouse and the rat illustrated by our experiments with flurbiprofen, a compound with very high plasma protein binding."( Intravenous microdialysis in the mouse and the rat: development and pharmacokinetic application of a new probe.
Deridder, G; Evrard, PA; Verbeeck, RK, 1996
)
0.49
" The pharmacokinetic data of the S-enantiomer was linked to the effect data using a hypothetical effect compartment."( Pharmacokinetics and pharmacodynamics of enantiomers of ibuprofen and flurbiprofen after oral administration.
Derendorf, H; Grundy, BL; Suri, A, 1997
)
0.53
" The conjugates of FP, an NSAID, with histamine H(2) antagonists were synthesized, in order to investigate the reduction in gastric damage by NSAID, and their pharmaceutical, pharmacokinetic and pharmacological properties were examined."( Improving the pharmacokinetic and pharmacodynamic properties of a drug by chemical conversion to a chimera drug.
Fukuhara, A; Imai, T; Otagiri, M, 1999
)
0.3
" There was no significant difference among pharmacokinetic parameters (AUC, CL, t(1/2z), Vd) for total or unbound flurbiprofen determined after intraperitoneal and intravenous administration."( Validation of subcutaneous microdialysis sampling for pharmacokinetic studies of flurbiprofen in the rat.
Mathy, FX; Preat, V; Verbeeck, RK, 2001
)
0.75
"To determine the effect of arthritis on the disposition of flurbiprofen (FP) and its acyl glucuronide (FPG) as well as formation of covalent adducts with plasma protein, a pharmacokinetic study was carried out in adjuvant-induced arthritic (AA) rats."( Stereoselective pharmacokinetics of flurbiprofen and formation of covalent adducts with plasma protein in adjuvant-induced arthritic rats.
Iwaki, M; Nagao, T; Tanino, T, 2003
)
0.84
" Plasma and urine samples were collected over 24 h, and flurbiprofen and 4'-hydroxyflurbiprofen pharmacokinetic data were compared across genotypes."( Differences in flurbiprofen pharmacokinetics between CYP2C9*1/*1, *1/*2, and *1/*3 genotypes.
Blaisdell, JA; Frye, RF; Goldstein, JA; Hinderliter, AL; Lee, CR; Pieper, JA, 2003
)
0.92
" After the administration of the FBP racemate and individual enantiomers no differences were observed between pharmacokinetic parameters [t(1/2beta) (h), Cl (L/h."( Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion.
Garcia, J; Soraci, AL; Tapia, O, 2005
)
0.58
" In cows, stereoselectivity was observed in Cl(B) and elimination half-life (t(1)/2) only in the early lactation group."( Pharmacokinetic parameters of (R)-(-) and (S)-(+)-flurbiprofen in dairy bovines.
Auza, N; Igarza, L; Soraci, A; Zeballos, H, 2006
)
0.59
" Chemical and plasmatic stability of prodrugs 6a- e as well as pharmacokinetic distribution studies for the prodrugs 6b and 6d were carried out."( Flurbiprofen derivatives in Alzheimer's disease: synthesis, pharmacokinetic and biological assessment of lipoamino acid prodrugs.
Barrio, JR; Bersani, S; Kepe, V; Pantò, V; Pignatello, R; Pistarà, V; Puglisi, G; Salmaso, S, 2008
)
1.79
"To evaluate the safety and tolerability and pharmacokinetic properties of R-flurbiprofen (Tarenflurbil) in normal elderly individuals and to determine the effect of the drug on amyloid beta 42 (Abeta42) levels, we conducted a double-blind, placebo-controlled study of 48 healthy subjects aged 55 to 80."( Safety, tolerability, pharmacokinetics, and Abeta levels after short-term administration of R-flurbiprofen in healthy elderly individuals.
Cottrell, BA; Galasko, DR; Golde, TE; Graff-Radford, N; Hendrix, S; Koo, EH; Laughlin, M; Mather, G; May, S; Murphy, MP; Sagi, SA; Swabb, E; Zavitz, KH,
)
0.58
" After strict validation, the method indicated good performance in terms of reproducibility, specificity, linearity, precision and accuracy, and it was successfully applied to the pharmacokinetic study of flurbiprofen in rats after oral and transdermal administration."( Cloud point extraction-HPLC method for determination and pharmacokinetic study of flurbiprofen in rat plasma after oral and transdermal administration.
Han, F; Jia, Q; Li, SM; Liu, HZ; Shi, XL; Xu, L; Yao, HM; Yin, R, 2008
)
0.76
"The aim of the study was to compare the pharmacokinetic properties and bioequivalence of flurbiprofen 50-mg ODT (test) with a conventional flurbiprofen 50-mg tablet (reference) under fasting conditions in healthy volunteers."( Pharmacokinetic and bioequivalence comparison between orally disintegrating and conventional tablet formulations of flurbiprofen: a single-dose, randomized-sequence, open-label, two-period crossover study in healthy Chinese male volunteers.
Jia, JY; Li, SJ; Li, XN; Liu, GY; Liu, Y; Liu, YM; Lu, C; Yu, C; Zhang, MQ; Zhang, YM, 2009
)
0.78
" Pharmacokinetic parameters, including C(max), T(max), t(1/2), AUC(0-24), and AUC(0-infinity), were calculated and analyzed statistically."( Pharmacokinetic and bioequivalence comparison between orally disintegrating and conventional tablet formulations of flurbiprofen: a single-dose, randomized-sequence, open-label, two-period crossover study in healthy Chinese male volunteers.
Jia, JY; Li, SJ; Li, XN; Liu, GY; Liu, Y; Liu, YM; Lu, C; Yu, C; Zhang, MQ; Zhang, YM, 2009
)
0.56
"This study compared the pharmacokinetic parameters and bioavailability of flurbiprofen from the investigational enteric-coated tablet (test) and from a film-coated immediate-release tablet compounded for the purposes of this study (reference)."( Comparative bioavailability and pharmacokinetics of investigational enteric- and film-coated formulations of flurbiprofen 100-mg tablets: a single-dose, randomized, open-label, two-period, two-way crossover study in healthy Pakistani male volunteers.
Ahmad, M; Pervaiz, F, 2010
)
0.8
" Plasma concentrations of the 2 formulations were determined, and pharmacokinetic parameters were compared using noncompartmental analysis."( Comparative bioavailability and pharmacokinetics of investigational enteric- and film-coated formulations of flurbiprofen 100-mg tablets: a single-dose, randomized, open-label, two-period, two-way crossover study in healthy Pakistani male volunteers.
Ahmad, M; Pervaiz, F, 2010
)
0.57
"In this small study in healthy Pakistani male subjects, there were significant differences in the bioavailability and pharmacokinetic parameters of the enteric- and film-coated tablet formulations of flurbiprofen."( Comparative bioavailability and pharmacokinetics of investigational enteric- and film-coated formulations of flurbiprofen 100-mg tablets: a single-dose, randomized, open-label, two-period, two-way crossover study in healthy Pakistani male volunteers.
Ahmad, M; Pervaiz, F, 2010
)
0.76
" A population pharmacokinetic model was built using the NONMEM software package."( Plasma and cerebrospinal fluid pharmacokinetics of flurbiprofen in children.
Hooker, A; Kokki, H; Kokki, M; Kumpulainen, E; Lehtonen, M; Ranta, VP; Välitalo, P, 2010
)
0.61
" Blood samples were collected periodically in both phases and analyzed for parent drugs and metabolites (dextrorphan, 4'-hydroxy-flurbiprofen and 1'-hydroxy-midazolam) to calculate pharmacokinetic parameters."( Drug metabolism in hemorrhagic shock: pharmacokinetics of selective markers of cytochrome-P450 2C9, 2D6, and 3A4 enzyme activities in a porcine model.
Beilman, GJ; Kumar, A; Mann, HJ; Remmel, RP, 2011
)
0.57
" The on-line DBS automated system was then successfully applied to a pharmacokinetic study performed on healthy male volunteers after oral administration of a single 50-mg dose of FLB."( Automated system for on-line desorption of dried blood spots applied to LC/MS/MS pharmacokinetic study of flurbiprofen and its metabolite.
Daali, Y; Dayer, P; Déglon, J; Desmeules, J; Lauer, E; Mangin, P; Samer, C; Staub, C; Thomas, A, 2011
)
0.58
" The pharmacokinetic parameters observed in Pakistani subjects when compared with other populations (USA, UK, Canadian, French, and Indian) did not show considerable ethnic differences."( Determination of pharmacokinetics of flurbiprofen in Pakistani population using modified HPLC method.
Farooqi, ZU; Najmi, MH; Qayyum, A, 2011
)
0.64
"The paper is to report the establishment of a population pharmacokinetic model for flurbiprofen (FP), an active metabolite of flurbiprofen axetil (FA)."( [Population pharmacokinetic modeling of flurbiprofen].
Gong, SJ; Huang, PF; Lin, WW; Wang, CL, 2010
)
0.85
"This was an open, randomised, two-period, crossover, pharmacokinetic (PK) study in which flurbiprofen plasma levels were compared in 12 healthy volunteers after the administration of single doses (8."( A randomised, two-period, cross-over, open-label study to evaluate the pharmacokinetic profiles of single doses of two different flurbiprofen 8.75-mg lozenges in healthy volunteers.
Annoni, O; Brunner, M; Burian, A; Lauro, V; Martin, W; Matzneller, P; Tacchi, R; Zeitlinger, M, 2012
)
0.81
" The development of NSAIDs having safer therapeutic profile depends on the better understanding of their mechanisms, physicochemical and pharmacokinetic properties."( Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach.
Kumar, M; Sinha, VR; Thareja, S, 2012
)
0.38
" The aim of this study was to determine whether a commercially available curcuminoid/piperine extract alters the pharmacokinetic disposition of probe drugs for these enzymes in human volunteers."( Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers.
Badmaev, V; Court, MH; Greenblatt, DJ; Hanley, MJ; Harmatz, JS; Hazarika, S; Majeed, M; Masse, G; Volak, LP, 2013
)
0.62
" The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery."( Formulation, evaluation and pharmacokinetics of colon targeted pulsatile system of flurbiprofen.
Veerareddy, PR; Vemula, SK, 2012
)
0.6
" Plasma, urine, and cerebrospinal fluid (CSF) samples were collected for measuring drug and main metabolite concentrations and potential biomarkers of pharmacodynamic activity (β-amyloid1-40, β-amyloid1-42, soluble CD40 ligand, and tumor necrosis factor-α)."( Pharmacokinetics and pharmacodynamics of CHF5074 after short-term administration in healthy subjects.
Breda, M; Calzà, L; Casula, D; Fernandez, M; Fiorentini, F; Frigerio, E; Giardino, L; Imbimbo, BP; Norris, D; Shenouda, M; Sivilia, S,
)
0.13
" The studies provide no evidence for concern about clinically important pharmacokinetic drug interactions of BBJ with substrate drugs metabolized by CYP3A or CYP2C9."( Effect of blueberry juice on clearance of buspirone and flurbiprofen in human volunteers.
Cancalon, PF; Court, MH; Dolnikowski, GG; Greenblatt, DJ; Hanley, MJ; Harmatz, JS; Masse, G, 2013
)
0.64
" Despite inhibition of CYP2C9 in vitro, pomegranate juice and extract had no effect on CYP2C9 activity in human subjects, and can be consumed by patients taking CYP2C9 substrate drugs with negligible risk of a pharmacokinetic interaction."( Pomegranate juice and pomegranate extract do not impair oral clearance of flurbiprofen in human volunteers: divergence from in vitro results.
Court, MH; Greenblatt, DJ; Hanley, MJ; Harmatz, JS; Masse, G, 2012
)
0.61
" Pharmacokinetic parameters like AUC(0-t), AUC(0-oo), Cmax, Tmax, t½, Vd and clearance were determined."( Comparative bioavailability and pharmacokinetics of two oral formulations of flurbiprofen: a single-dose, randomized, open-label, two-period, crossover study in Pakistani subjects.
Abbas, M; Najmi, MH; Qayyum, A, 2013
)
0.62
" Then the tablets were optimized with the support of in vitro dissolution studies, and further it was proved by pharmacokinetic studies."( Colon targeted guar gum compression coated tablets of flurbiprofen: formulation, development, and pharmacokinetics.
Bontha, VK; Vemula, SK, 2013
)
0.64
" The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery."( Pharmacokinetics of colon-specific pH and time-dependent flurbiprofen tablets.
Devadasu, VR; Veerareddy, PR; Vemula, SK, 2015
)
0.66
" Then the formulations were evaluated for different physical parameters, solubility studies, DSC, FTIR studies and in vitro dissolution studies to select the best formulation that shows rapid dissolution rate and finally subjected to pharmacokinetic studies."( Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen.
Daravath, B; Tadikonda, RR; Vemula, SK, 2015
)
0.65
" From the pharmacokinetic evaluation, the control tablets produced peak plasma concentration (Cmax) of 9140."( Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen.
Daravath, B; Tadikonda, RR; Vemula, SK, 2015
)
0.65
" This assay was applied to determine the pharmacokinetic parameters of flurbiprofen in healthy Turkish volunteers who had been given 100 mg of flurbiprofen."( Determination of flurbiprofen in human plasma by gas chromatography with mass spectrometry and its pharmacokinetics.
Akba, V; Erdem, AF; Sahin, H; Yilmaz, B,
)
0.7
"In order to assess the preliminary safety and effectiveness of nanostructured lipid carriers-based flurbiprofen gel (FP NLC-gel), the acute irritation test, in vivo pharmacodynamics evaluation and pharmacokinetic study were investigated after topical application."( Nanostructured lipid carriers-based flurbiprofen gel after topical administration: acute skin irritation, pharmacodynamics, and percutaneous absorption mechanism.
Han, F; Li, S; Song, A; Su, Z, 2015
)
0.91
"The study aimed to prepare a transdermal patch for flurbiprofen using isopulegol decanoate (ISO-C10) as a permeation enhancer, and to evaluate the in-vitro and in-vivo percutaneous permeation of the drug, as well as the pharmacodynamic efficacy of the formulation."( Enhancement of skin permeation of flurbiprofen via its transdermal patches using isopulegol decanoate (ISO-C10) as an absorption enhancer: pharmacokinetic and pharmacodynamic evaluation.
Chen, Y; Cun, D; Fang, L; Guo, W; Liu, X; Quan, P; Song, W; Wang, Z, 2015
)
0.95
"The permeation experiments were conducted on rabbit skin, and the pharmacokinetic profiles and synovial fluid drug concentration were measured after in-vivo transdermal administration."( Enhancement of skin permeation of flurbiprofen via its transdermal patches using isopulegol decanoate (ISO-C10) as an absorption enhancer: pharmacokinetic and pharmacodynamic evaluation.
Chen, Y; Cun, D; Fang, L; Guo, W; Liu, X; Quan, P; Song, W; Wang, Z, 2015
)
0.7
" Meanwhile, the ISO-C10 contained patches increased the drug disposition in synovial fluid and enhanced the pharmacodynamic efficacy of the formulation."( Enhancement of skin permeation of flurbiprofen via its transdermal patches using isopulegol decanoate (ISO-C10) as an absorption enhancer: pharmacokinetic and pharmacodynamic evaluation.
Chen, Y; Cun, D; Fang, L; Guo, W; Liu, X; Quan, P; Song, W; Wang, Z, 2015
)
0.7
" Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted."( A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets.
Vemula, SK, 2015
)
0.74
" Cmax and AUC0-∞ were dose-proportional."( Plasma pharmacokinetics and synovial concentrations of S-flurbiprofen plaster in humans.
Hoshino, Y; Kamezawa, M; Matsumoto, H; Matsushita, I; Otsuka, N; Sasaki, S; Uebaba, K; Yamada, I; Yataba, I, 2016
)
0.68
"No adverse events were observed during pharmacokinetic assessment."( Pharmacokinetics and efficacy of intraocular flurbiprofen.
Blazaki, S; Naoumidi, E; Tsatsakis, A; Tsatsanis, C; Tsika, C; Tsilimbaris, MK; Tzatzarakis, M, 2017
)
0.71
" However, the half-life of the drug remains short, necessitating further research to prolong its presence in the vitreous cavity."( Pharmacokinetics and efficacy of intraocular flurbiprofen.
Blazaki, S; Naoumidi, E; Tsatsakis, A; Tsatsanis, C; Tsika, C; Tsilimbaris, MK; Tzatzarakis, M, 2017
)
0.71
" Additionally, the effect of each method on a simulated in vivo pharmacokinetic profile was studied using advanced PBPK modelling."( A comparison of two biorelevant in vitro drug release methods for nanotherapeutics based on advanced physiologically-based pharmacokinetic modelling.
Gao, F; Jung, F; Nothnagel, L; Thurn, M; Vogel, V; Wacker, MG, 2018
)
0.48
"The objective of this study was to optimize the Flurbiprofen (FB) nanosuspension (NS) based gel and to investigate the in vitro release, ex vivo permeation, the plasma concentration-time profile and pharmacokinetic parameters."( Enhanced Dermal Delivery of Flurbiprofen Nanosuspension Based Gel: Development and Ex Vivo Permeation, Pharmacokinetic Evaluations.
Celebi, N; Ilbasmis-Tamer, S; Oktay, AN; Uludag, O, 2021
)
1.17
" Then the in-vitro release, ex vivo permeation studies were performed, and pharmacokinetic studies were evaluated on rats."( Enhanced Dermal Delivery of Flurbiprofen Nanosuspension Based Gel: Development and Ex Vivo Permeation, Pharmacokinetic Evaluations.
Celebi, N; Ilbasmis-Tamer, S; Oktay, AN; Uludag, O, 2021
)
0.92
" The optimized FB nanosuspension gel provided better permeation and pharmacokinetic performance compared to FB coarse suspension gel."( Enhanced Dermal Delivery of Flurbiprofen Nanosuspension Based Gel: Development and Ex Vivo Permeation, Pharmacokinetic Evaluations.
Celebi, N; Ilbasmis-Tamer, S; Oktay, AN; Uludag, O, 2021
)
0.92
" Therefore, it is of great significance to compare the in vivo pharmacokinetic behaviors of R-FP and S-FP."( Comparison of in vivo pharmacokinetic behaviors of R- and S-flurbiprofen after intravenous injection of flurbiprofen axetil.
He, Y; Li, M; Qin, F; Qin, M; Tian, B; Zhi, D, 2023
)
1.15
" This study covers the formulation and pharmacokinetic study of fast-dissolving flurbiprofen tablets using PEG 6000 (hydrophilic carrier) and lactose (adsorbent)."( Quality by design (QbD) approach to develop fast-dissolving tablets using melt-dispersion paired with surface-adsorption method: formulation and pharmacokinetics of flurbiprofen melt-dispersion granules.
Daravath, B; Repka, M; Vemula, SK, 2023
)
1.33

Compound-Compound Interactions

Flurbiprofen axetil combined with fentanyl for postoperative analgesia can significantly reduce fentanyl dose and the incidence of adverse effects associated with fentanyl without obviously affecting the coagulation and gastrointestinal functions.

ExcerptReferenceRelevance
" However, one study did demonstrate differences in the pharmacokinetics of 7-hydroxy-methotrexate, the active metabolite of MTX, when MTX was administered with aspirin."( Methotrexate and nonsteroidal antiinflammatory drug interactions.
Frenia, ML; Long, KS, 1992
)
0.28
" In the present study, we have investigated the effect of oral terfenadine 180 mg, flurbiprofen 100 mg, and the drug combination on AMP-induced bronchoconstriction in eight nonatopic asthmatic subjects with a mean age of 53."( The effect of oral terfenadine alone and in combination with flurbiprofen on the bronchoconstrictor response to inhaled adenosine 5'-monophosphate in nonatopic asthma.
Holgate, ST; Phillips, GD, 1989
)
0.74
"Two patients with orthostatic hypotension, complicating diabetes mellitus, were treated with dopaminergic antagonist metoclopramide alone or combined with the nonsteroidal anti-inflammatory agent flurbiprofen."( Metoclopramide alone or combined with flurbiprofen in the treatment of orthostatic hypotension associated with diabetes mellitus.
Beretta-Piccoli, C; Weidmann, P, 1982
)
0.72
"3 variant exhibits marked decreases in substrate turnover compared with the wild-type enzyme, but little is known regarding the effect this variant form may have on the occurrence of drug-drug interactions."( CYP2C9 genotype-dependent effects on in vitro drug-drug interactions: switching of benzbromarone effect from inhibition to activation in the CYP2C9.3 variant.
Gannett, PM; Hummel, MA; Locuson, CW; Mosher, CM; Rettie, AE; Rock, DA; Tracy, TS, 2005
)
0.33
"To observe the effect of propofol combined with flurbiprofen axetil for abortion anesthesia."( [Clinical observation of propofol combined with flurbiprofen axetil for induced abortion anesthesia].
Guo, QL; Xie, YQ; Yang, HW, 2006
)
0.85
"Propofol combined with flurbiprofen axetil gives more efficient anesthesia for induced abortion patients in gynecology department."( [Clinical observation of propofol combined with flurbiprofen axetil for induced abortion anesthesia].
Guo, QL; Xie, YQ; Yang, HW, 2006
)
0.9
"To investigate the effect of flurbiprofen preemptive analgesia combined with intravenous propofol anesthesia in induced abortion."( [Application of flurbiprofen preemptive analgesia combined with intravenous propofol anesthesia in induced abortion].
Lao, JX; Liu, WX; Tan, SX; Zhang, YF, 2008
)
0.98
"Flurbiprofen preemptive analgesia combined with intravenous propofol is safe and effective for anesthesia during induced abortion."( [Application of flurbiprofen preemptive analgesia combined with intravenous propofol anesthesia in induced abortion].
Lao, JX; Liu, WX; Tan, SX; Zhang, YF, 2008
)
2.13
"a To observe the analgesic effect of fentanyl combined with flurbiprofen axetil for postoperative analgesia after gynecologic surgery."( [Postoperative analgesia with fentanyl combined with flurbiprofen axetil following gynecologic surgery for turnor].
Bai, XH; Cao, LH; Lin, WQ; Wen, LL; Zhong, ZJ, 2009
)
0.84
"Flurbiprofen axetil combined with fentanyl for postoperative analgesia can significantly reduce fentanyl dose and the incidence of adverse effects associated with fentanyl without obviously affecting the coagulation and gastrointestinal functions."( [Postoperative analgesia with fentanyl combined with flurbiprofen axetil following gynecologic surgery for turnor].
Bai, XH; Cao, LH; Lin, WQ; Wen, LL; Zhong, ZJ, 2009
)
2.05
" While grapefruit juice has been extensively studied with respect to its drug-drug interaction potential, numerous other fruit juices such as cranberry juice, orange juice, grape juice, pineapple juice and pomegranate juice have also been investigated for its potential to show drug-drug interaction of any clinical relevance."( Is pomegranate juice a potential perpetrator of clinical drug-drug interactions? Review of the in vitro, preclinical and clinical evidence.
Srinivas, NR, 2013
)
0.39
"EA intervention combined with anesthetics is effective in reducing the dosage of the supplemented Sauteralgyl and the degree of postoperative nausea, and in improving postoperative gastrointestinal functional recovery in patients undergoing pneumectomy."( [Electroacupuncture Intervention Combined with Anesthetics for Analgesia and Post-surgical Gastrointestinal Recovery in Pneumectomy Patients].
Chen, TY; Ma, W; Wang, K; Wu, YY; Xu, JJ; Zhou, J, 2015
)
0.42
" 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
" We hypothesize that different doses of oxycodone hydrochloride combined with flurbiprofen axetil would generate great results on postoperative intravenous analgesia in lower abdominal patients."( Effect of oxycodone hydrochloride combined with flurbiprofen axetil for intravenous patient-controlled analgesia in lower abdominal patients: A randomized trial.
Fang, J; Lian, Y; Wu, Y; Xiang, X; Yuan, X, 2018
)
0.96
"75 mg/kg oxycodone hydrochloride combined with flurbiprofen axetil can provide safe and effective postoperative analgesia for lower abdominal patients, with fewer adverse reactions."( Effect of oxycodone hydrochloride combined with flurbiprofen axetil for intravenous patient-controlled analgesia in lower abdominal patients: A randomized trial.
Fang, J; Lian, Y; Wu, Y; Xiang, X; Yuan, X, 2018
)
0.99
"To evaluate the anesthetic effect of ultrasound-guided (USG) ilioinguinal/iliohypogastric nerve (II/IHN) block combined with genital branch of genitofemoral nerve (GFN) block in the elderly undergoing inguinal hernia repair, 54 old patients (aged 60-96years, ASA I-III) with indirect hernia were enrolled and scheduled for unilateral tension-free herniorrhaphy."( Evaluation of Ultrasound-guided Genitofemoral Nerve Block Combined with Ilioinguinal/iliohypogastric Nerve Block during Inguinal Hernia Repair in the Elderly.
Huang, Z; Ke, JY; Peng, XH; Wang, W; Xia, W, 2019
)
0.51
" Nonetheless, only few studies have evaluated the clinical therapeutic effects of lidocaine combination with flurbiprofen axetil to prevent pain on injection of propofol."( Clinical therapeutic effects of lidocaine combination with flurbiprofen axetil for reducing propofol-induced pain in adults: A protocol for systematic review and meta-analysis.
Fu, J; Lu, G; Sun, W; Ye, X; Yu, J, 2020
)
1.01
"This study will provide high-quality evidence for the clinical therapeutic effects of lidocaine combination with flurbiprofen axetil for reducing pain on injection of propofol in adult patients."( Clinical therapeutic effects of lidocaine combination with flurbiprofen axetil for reducing propofol-induced pain in adults: A protocol for systematic review and meta-analysis.
Fu, J; Lu, G; Sun, W; Ye, X; Yu, J, 2020
)
1.01
"To evaluate the safety and efficacy of sedation and analgesia using dexmedetomidine combined with flurbiprofen axetil in multiple complex teeth extraction under local anesthesia."( [Evaluation of the application of dexmedetomidine combined with flurbiprofen axetil in extraction of multiple complex teeth under local anesthesia].
He, H; Liu, H; Qi, M; Shao, Y; Sheng, L, 2021
)
1.08
"According to the inclusion and exclusion criteria of the study, 40 patients scheduled for multiple complex teeth (4-6) extraction were randomly divided into 2 groups: experimental group (sedation and analgesia using dexmedetomidine combined with flurbiprofen axetil in addition to local anesthesia, n=20) and control group (local anesthesia, n=20)."( [Evaluation of the application of dexmedetomidine combined with flurbiprofen axetil in extraction of multiple complex teeth under local anesthesia].
He, H; Liu, H; Qi, M; Shao, Y; Sheng, L, 2021
)
1.04
"Sedation and analgesia using dexmedetomidine combined with flurbiprofen axetil in addition to local anesthesia is a safe and effective approach in multiple complex teeth extraction."( [Evaluation of the application of dexmedetomidine combined with flurbiprofen axetil in extraction of multiple complex teeth under local anesthesia].
He, H; Liu, H; Qi, M; Shao, Y; Sheng, L, 2021
)
1.1
"To explore the effect of dexmedetomidine combined with flurbiprofen axetil on postoperative analgesia and immune function in patients with lung cancer after radical operation."( Application effect of dexmedetomidine combined with flurbiprofen axetil and flurbiprofen axetil monotherapy in radical operation of lung cancer and evaluation of the immune function.
Chen, Y; Du, J; Tao, H; Zong, S,
)
0.63
"60 lung cancer patients undergoing open chest radical surgery were selected and randomly divided into D & F Group (dexmedetomidine combined with flurbiprofen axetil) and F Group (flurbiprofen axetil), with 30 cases in each group."( Application effect of dexmedetomidine combined with flurbiprofen axetil and flurbiprofen axetil monotherapy in radical operation of lung cancer and evaluation of the immune function.
Chen, Y; Du, J; Tao, H; Zong, S,
)
0.58
"Flurbiprofen axetil can improve postoperative pain, but combined with dexmedetomidine better effect, postoperative comfort and immune function of patients were significantly improved."( Application effect of dexmedetomidine combined with flurbiprofen axetil and flurbiprofen axetil monotherapy in radical operation of lung cancer and evaluation of the immune function.
Chen, Y; Du, J; Tao, H; Zong, S,
)
1.82
"To investigated the effects of sufentanil in combination with flurbiprofen axetil and dexmedetomidine for patient-controlled intravenous analgesia (PCIA) on patients after open gastrointestinal tumor surgery, and compared this combination with traditional PCIA with pure opioids or epidural analgesia (PCEA)."( Analgesic effects of sufentanil in combination with flurbiprofen axetil and dexmedetomidine after open gastrointestinal tumor surgery: a retrospective study.
Chen, YJ; Huang, J; Li, TT; Liu, F; Wang, TH; Xiong, LL; Yin, L, 2022
)
1.21
"The analgesic effects of PCIA with sufentanil in combination with flurbiprofen axetil and dexmedetomidine on postoperative analgesia was better than that of traditional pure opioids PCIA, and similar with that of PCEA."( Analgesic effects of sufentanil in combination with flurbiprofen axetil and dexmedetomidine after open gastrointestinal tumor surgery: a retrospective study.
Chen, YJ; Huang, J; Li, TT; Liu, F; Wang, TH; Xiong, LL; Yin, L, 2022
)
1.21
" This study aimed to compare the analgesic effects of tramadol alone and combined with butorphanol or flurbiprofen axetil after a cesarean section."( Analgesic outcomes of tramadol alone and in combination with Butorphanol or Flurbiprofen Axetil after cesarean section: a retrospective study with propensity score matching analysis.
Bao, X; Deng, Q; Li, H; Liang, Y; Liu, W; Peng, J; Tan, D; Wu, Z; Yan, G; Yang, G, 2022
)
1.17
"To determine the analgesic effect of flurbiprofen axetil (FBA) combined with half standard-dose opioids in patients undergoing primary unilateral total knee arthroplasty (TKA)."( Analgesia with reduced incidence of adverse reactions using flurbiprofen axetil in combination with half standard-dose opioids in primary total knee arthroplasty.
Cai, H; Lin, Q; Liu, J; Shen, J; Wu, X; Xiao, J; Zhao, C; Zhu, J, 2023
)
1.43
" All patients received the same dose of FBA in the form of a patient-controlled intravenous analgesia but in the control group this was combined with a standard-dose of opioids and in the experimental group with a half standard-dose of opioids."( Analgesia with reduced incidence of adverse reactions using flurbiprofen axetil in combination with half standard-dose opioids in primary total knee arthroplasty.
Cai, H; Lin, Q; Liu, J; Shen, J; Wu, X; Xiao, J; Zhao, C; Zhu, J, 2023
)
1.15
"The analgesic effect of FBA in combination with half standard-dose opioids was similar to that of FBA in combination with conventional standard-dose opioids, but the incidence of adverse effects involving nausea/vomiting in the experimental group were significantly reduced."( Analgesia with reduced incidence of adverse reactions using flurbiprofen axetil in combination with half standard-dose opioids in primary total knee arthroplasty.
Cai, H; Lin, Q; Liu, J; Shen, J; Wu, X; Xiao, J; Zhao, C; Zhu, J, 2023
)
1.15
" Plant-based therapeutic agents including essential oils in combination with low-dose synthetic drugs have been shown to produce synergistic effects and reduce complications of synthetic drugs."( Anti-inflammatory mechanisms of eucalyptol rich Eucalyptus globulus essential oil alone and in combination with flurbiprofen.
Arooj, B; Asghar, S; Asif, M; Chohan, T; Khalid, SH; Khan, IU; Saleem, M; Yaseen, HS; Zubair, HM, 2023
)
1.12

Bioavailability

No significant differences were found for Cmax, tmax or AUC, using a nonstereoisomeric assay. The apparent bioavailability of oral flurbiprofen syrup was 81%.

ExcerptReferenceRelevance
"In this randomized, crossover study comparing the bioavailability of a film-coated (Ansaid) with a sugar-coated (Froben) 100 mg tablets of racemic flurbiprofen in 23 healthy young men, no significant differences were found for Cmax, tmax or AUC, using a nonstereoisomeric assay for flurbiprofen."( Comparative bioavailability of two flurbiprofen products: stereospecific versus conventional approach.
Berry, BW; Cheung, H; Cheung, R; Collins, DS; Jamali, F; McColl, K; Molder, S,
)
0.61
" After rectal administration, the rate of absorption evaluated through tmax and calculation of mean absorption times was always slower than after oral dosing."( Biopharmaceutical evaluation of carprofen following single intravenous, oral, and rectal doses in dogs.
Guentert, TW; Schmitt, M, 1990
)
0.28
" Dialysis was carried out using plasma samples obtained from five of 15 subjects participating in a crossover bioavailability study."( Pharmacokinetics of flurbiprofen in man. II. Plasma protein binding.
Albert, KS; Szpunar, GJ; Wagner, JG, 1989
)
0.6
"The bioavailability of granules and tablet flurbiprofen in 100 mg single dose was crossover compared in 6 healthy volunteers (mean aged 26."( Single-dose pharmacokinetics of flurbiprofen granules and tablets in healthy volunteers.
Bandi, G; Benvenuti, C; Gambaro, V; Lodi, F; Scaroni, C; Valenti, M, 1989
)
0.82
" Flurbiprofen was buccally absorbed by a passive diffusional mechanism and the rate of absorption was pH dependent."( Human buccal absorption of flurbiprofen.
Adkins, EL; Barsuhn, CL; Gleason, DD; Ho, NF; Olanoff, LS, 1988
)
1.48
"The ocular bioavailability of radiolabeled flurbiprofen was determined after single or multiple topical dosing of rabbits."( Multiple dosing increases the ocular bioavailability of topically administered flurbiprofen.
Anderson, JA; Chen, CC, 1988
)
0.77
" Following a single oral dose of 100 mg of flurbiprofen, drug bioavailability is equivalent using regimens of four 25-mg tablets, two 50-mg tablets, or one 100-mg tablet once daily."( Pharmacokinetics of flurbiprofen.
Brooks, CD; Kaiser, DG; Lomen, PL, 1986
)
0.86
" Flurbiprofen showed equivalent bioavailability after oral and rectal administration and the same pharmacokinetic profile was confirmed in children as observed in adults."( Pharmacokinetics of oral and rectal flurbiprofen in children.
Benvenuti, C; D'Amico, E; Hind, ID; Mazzoni, PL; Scaroni, C, 1984
)
1.45
" The method is applicable to human bioavailability and pharmacokinetic studies with flurbiprofen."( Determination of flurbiprofen in human serum by reverse-phase high-performance liquid chromatography with fluorescence detection.
Albert, KS; Garry, M; Gillespie, WR; Raabe, A, 1984
)
0.83
" The ocular bioavailability of the ophthalmic dose was defined by using intracameral administration as a standard measurement."( Ocular and systemic bioavailability of ophthalmic flurbiprofen.
Liu, SS; Tang-Liu, DD; Weinkam, RJ, 1984
)
0.52
"In a study of the ocular absorption and elimination of a topically applied non-steroidal anti-inflammatory drug (NSAID), flurbiprofen, the compound was well absorbed into rabbit ocular tissues and was highly concentrated in the rabbit cornea."( Disposition of topical flurbiprofen in normal and aphakic rabbit eyes.
Anderson, JA; Chen, CC; Shackleton, M; Vita, JB, 1982
)
0.78
" Flurbiprofen did not seem to alter the bioavailability of the chemotherapeutic agents."( Increased survival of cancer-bearing mice treated with inhibitors of prostaglandin synthesis alone or with chemotherapy.
Bennett, A; Berstock, DA; Carroll, MA, 1982
)
1.17
" The enhanced bioavailability of flurbiprofen suggests the possible utility of tri-O-methyl-beta-cyclodextrin in pharmaceutical formulation."( Enhanced oral bioavailability of antiinflammatory drug flurbiprofen in rabbits by tri-O-methyl-beta-cyclodextrin complexation.
Imai, T; Otagiri, M; Uekama, K, 1982
)
0.79
" These methods were applied to bioavailability studies in dogs."( Determination of flurbiprofen and ibuprofen in dog serum with automated sample preparation.
Beaubien, LJ; Rahn, PD; Sears, DJ; Snider, BG, 1981
)
0.6
" The absorption rate constant was increased significantly after multiple administration as compared to that of single administration."( Effect of oral multiple-dose administration of anti-inflammatory flurbiprofen chimera drug on gastric lesion, other toxicities and disposition kinetics.
Fukuhara, A; Imai, T; Inoue, K; Otagiri, M, 1995
)
0.53
" Although with these preparations the peak plasma drug concentration is reduced and time taken to achieve peak concentrations is prolonged, the bioavailability is the same as that with regular release counterparts."( Clinical pharmacokinetics of flurbiprofen and its enantiomers.
Davies, NM, 1995
)
0.58
"To compare the bioavailability and pupillary effect of flurbiprofen and indomethacin during phacoemulsification and intraocular lens implantation."( Intraocular availability and pupillary effect of flurbiprofen and indomethacin during cataract surgery.
Cheetham, JK; DeGryse, R; Garcia, CG; Gimbel, H; Van Westenbrugge, J, 1996
)
0.8
" In humans, the bioavailability of racemic flurbiprofen absorbed from the oral cavity has been studied measuring the total concentration of S- and R-flurbiprofen, and the pharmacokinetics of S- and R-flurbiprofen have been studied after oral administration of racemic flurbiprofen."( Human plasma concentrations of R, S, and racemic flurbiprofen given as a toothpaste.
Arnett, RL; Clifford, KH; Cutler, RE; Forland, SC; Wechter, WJ; Witchwoot, S, 1996
)
0.81
" Although food did not affect the bioavailability of this formulation, there was a statistically significant increase in the mean (+/-SE) concentration of the first peak (Cpeak 1) from 14."( The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations.
Kelkar, MG; Nayak, PJ; Pargal, A, 1996
)
0.54
"The interactions between flurbiprofen (FB) and different polymers are studied in order to improve the bioavailability of FB."( An investigation of FB interactions with poly(ethylene glycol) 6000, poly(ethylene glycol) 4000, and poly-epsilon-caprolactone by thermoanalytical and spectroscopic methods and modeling.
Chauvet, A; Egea, MA; Garcia, ML; Lacoulonche, F; Masse, J, 1998
)
0.6
" Thus, alterations in both plasma extravasation and tissue pH seem to be relevant factors regulating the delivery and bioavailability of this nonsteroidal anti-inflammatory drug to dental pulp."( Effect of inflammation on the delivery of drugs to dental pulp.
Bunczak-Reeh, MA; Hargreaves, KM, 1998
)
0.3
"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
" FP (1%) gel containing ethanol (25%) and l-menthol (3%) as penetration enhancers was applied to rabbit dorsal skin and the in vivo absorption rate of FP was compared with the in vitro penetration rate through excised skin."( Effect of l-menthol-ethanol-water system on the systemic absorption of flurbiprofen after repeated topical applications in rabbits.
Hayashi, T; Kawabata, S; Morimoto, Y; Seki, T; Sugibayashi, K, 2000
)
0.54
" The oral bioavailability of Flu from Flu or Flu/beta-CD at doses of 1, 3, 10, and 30 mg/kg (as Flu) was examined in rats."( Evaluation of the bioavailability of flurbiprofen and its beta-cyclodextrin inclusion complex in four different doses upon oral administration to rats.
Machida, Y; Muraoka, A; Tokumura, T, 2004
)
0.6
" The bioavailability of drug when administered as SD was evaluated in humans."( Formulation studies and in vivo evaluation of a flurbiprofen-hydroxypropyl beta-cyclodextrin system.
Govindarajan, R; Nagarsenker, MS, 2005
)
0.58
" Therefore, a semi-solid dispersion of flurbiprofen with Gelucire and Labrasol may have the potential of improved bioavailability because of the enhanced in vitro properties."( Preparation and in vitro characterization of a semi-solid dispersion of flurbiprofen with Gelucire 44/14 and Labrasol.
Khan, MA; Soliman, MS, 2005
)
0.83
" In rats, some of the compounds appeared to be well absorbed after oral administration and to penetrate into the central nervous system."( Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
Bigogno, C; Biscaioli, M; Bolzoni, PT; Caruso, P; Catinella, S; Cenacchi, V; Del Giudice, E; Dondio, G; Facchinetti, F; Fontanella, L; Imbimbo, BP; Marchetti, S; Misiano, P; Moretto, N; Parini, C; Peretto, I; Puccini, P; Radaelli, S; Raveglia, LF; Riccardi, B; Rizzi, A; Rondelli, I; Villetti, G; Zandi, M, 2005
)
0.6
"84% relative bioavailability compared to immediate release tablet of flurbiprofen."( Wet process-induced phase-transited drug delivery system: a means for achieving osmotic, controlled, and level A IVIVC for poorly water-soluble drug.
Pathak, K; Philip, AK, 2008
)
0.58
"Improvement of the oral bioavailability of flurbiprofen (Flu) after oral administration of flurbiprofen/beta-cyclodextrin inclusion complex (Flu/beta-CD) by the action of cinnarizine (CN) was investigated."( Improvement of oral bioavailability of flurbiprofen from flurbiprofen/beta-cyclodextrin inclusion complex by action of cinnarizine.
Machida, Y; Muraoka, A; Tokumura, T, 2009
)
0.88
"The main purpose of this study was to evaluate the effect of a mixed drug solution containing a surfactant and beta-cyclodextrin (beta-CD) on the solubility and bioavailability of a poorly water soluble drug, flurbiprofen."( Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound.
Balakrishnan, P; Choi, HG; Han, MJ; Joe, JH; Kim, JO; Li, DX; Oh, DH; Park, SM; Seo, Y; Yan, YD; Yong, CS, 2010
)
0.83
"The feasibility of alpha-glucosyl hesperidin (Hsp-G) to improve the dissolution and bioavailability of poorly water-soluble drug was investigated."( Improvement of dissolution and absorption properties of poorly water-soluble drug by preparing spray-dried powders with alpha-glucosyl hesperidin.
Imono, M; Takeuchi, H; Tozuka, Y; Uchiyama, H, 2010
)
0.36
"This study compared the pharmacokinetic parameters and bioavailability of flurbiprofen from the investigational enteric-coated tablet (test) and from a film-coated immediate-release tablet compounded for the purposes of this study (reference)."( Comparative bioavailability and pharmacokinetics of investigational enteric- and film-coated formulations of flurbiprofen 100-mg tablets: a single-dose, randomized, open-label, two-period, two-way crossover study in healthy Pakistani male volunteers.
Ahmad, M; Pervaiz, F, 2010
)
0.8
"In this small study in healthy Pakistani male subjects, there were significant differences in the bioavailability and pharmacokinetic parameters of the enteric- and film-coated tablet formulations of flurbiprofen."( Comparative bioavailability and pharmacokinetics of investigational enteric- and film-coated formulations of flurbiprofen 100-mg tablets: a single-dose, randomized, open-label, two-period, two-way crossover study in healthy Pakistani male volunteers.
Ahmad, M; Pervaiz, F, 2010
)
0.76
"The capability of transglycosylated materials, α-glycosyltransferase-treated stevia (Stevia-G) and α-glycosyl hesperidin (Hsp-G), to enhance the bioavailability of poorly water-soluble drugs was investigated."( Transglycosylated stevia and hesperidin as pharmaceutical excipients: dramatic improvement in drug dissolution and bioavailability.
Imono, M; Takeuchi, H; Tozuka, Y; Uchiyama, H, 2010
)
0.36
" These results suggest that FP from LM chitosan kneaded mixture increases the dissolution rate and improves the bioavailability of the drug by the formation of a water-soluble complex."( Enhancement of dissolution and bioavailability of flurbiprofen by low molecular weight chitosans.
Anraku, M; Arahira, M; Imai, T; Khaled, KA; Mady, FM; Otagiri, M; Seo, H; Yamasaki, K, 2010
)
0.61
" The dissolution and bioavailability in rats were evaluated compared to commercial product."( Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change.
Choi, HG; Kang, JH; Oh, DH; Park, YJ; Yong, CS, 2011
)
0.61
" The apparent bioavailability of oral flurbiprofen syrup was 81%."( Plasma and cerebrospinal fluid pharmacokinetics of flurbiprofen in children.
Hooker, A; Kokki, H; Kokki, M; Kumpulainen, E; Lehtonen, M; Ranta, VP; Välitalo, P, 2010
)
0.88
"9 times higher than that of the flurbiprofen sodium eye drops respectively, which meant that the ocular bioavailability was improved greatly by the novel preparation."( [Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil].
Gan, L; Gan, Y; Shen, JQ; Zhu, CL; Zhu, JB, 2010
)
0.88
" To improve the solubility and bioavailability of flurbiprofen (poor water solubility), a solid dispersion was spray dried with a solution of flurbiprofen and cycloamylose at a weight ratio of 1:1."( Enhanced solubility and bioavailability of flurbiprofen by cycloamylose.
Baek, HH; Choi, HG; Hah, JM; Kim, YR; Kwon, SY; Lee, WS; Rho, SJ; Yang, HJ; Yong, CS, 2011
)
0.89
"α-Glucosylhesperidin (Hsp-G), a functional food additive, significantly enhances the solubility and bioavailability of poorly water-soluble drugs despite little surface activity."( NMR investigation of a novel excipient, α-glucosylhesperidin, as a suitable solubilizing agent for poorly water-soluble drugs.
Higashi, K; Moribe, K; Takeuchi, H; Tozuka, Y; Uchiyama, H; Yamamoto, K; Zhang, J, 2011
)
0.37
" Similarly, they greatly improved the dissolution rate and oral bioavailability of flurbiprofen in rats due to the fast spontaneous emulsion formation and the decreased droplet size."( Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier.
Choi, HG; Kang, JH; Kim, DW; Kim, JO; Lee, BJ; Oh, DH; Yong, CS, 2011
)
0.59
"In order to investigate the effects of solid carriers on the crystalline properties, dissolution and bioavailability of flurbiprofen in a solid self-nanoemulsifying drug delivery system (solid SNEDDS), different solid SNEDDS formulations were prepared by spray-drying the solutions containing liquid SNEDDS and various carriers."( Effects of solid carriers on the crystalline properties, dissolution and bioavailability of flurbiprofen in solid self-nanoemulsifying drug delivery system (solid SNEDDS).
Choi, HG; Kang, JH; Oh, DH; Oh, YK; Yong, CS, 2012
)
0.81
"To develop a novel flurbiprofen-loaded solid self-microemulsifying drug delivery system (solid SMEDDS) with improved oral bioavailability using gelatin as a solid carrier, the solid SMEDDS formulation was prepared by spray-drying the solutions containing liquid SMEDDS and gelatin."( Development of novel flurbiprofen-loaded solid self-microemulsifying drug delivery system using gelatin as solid carrier.
Choi, HG; Kang, JH; Kim, DW; Oh, DH; Yong, CS, 2012
)
1.03
"2-fold increase in relative oral bioavailability compared with that of the suspension."( Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function.
Choi, HG; Kim, JO; Marasini, N; Poudel, BK; Yan, YD; Yong, CS, 2012
)
0.38
" Therefore, these flurbiprofen-loaded nanoparticles can be convenient for distributing a poorly water-soluble flurbiprofen with improved bioavailability using uniform nano-sized particles."( Flurbiprofen-loaded nanoparticles prepared with polyvinylpyrrolidone using Shirasu porous glass membranes and a spray-drying technique: nano-sized formation and improved bioavailability.
Choi, HG; Din, FU; Kim, DW; Kim, JO; Oh, DH; Yong, CS, 2013
)
2.17
" Furthermore, dissolution and bioavailability in rats were evaluated compared to a flurbiprofen-loaded commercial product."( Development of flurbiprofen-loaded nanoparticles with a narrow size distribution using sucrose.
Choi, HG; Kim, DW; Kim, JO; Oh, DH; Yan, YD; Yong, CS, 2014
)
0.98
" The bioavailability of flurbiprofen from optimized nanoparticles was assessed in male Wistar rats at a dose of 15 mg/kg."( Enhanced bioavailability of orally administered flurbiprofen by combined use of hydroxypropyl-cyclodextrin and poly(alkyl-cyanoacrylate) nanoparticles.
Li, W; Luo, Q; Zhang, X; Zhao, X, 2014
)
0.96
"Comparative bioavailability studies are conducted to establish the bioequivalence of generic formulation with that of branded reference formulation, providing confidence to clinicians to use these products interchangeably."( Comparative bioavailability and pharmacokinetics of two oral formulations of flurbiprofen: a single-dose, randomized, open-label, two-period, crossover study in Pakistani subjects.
Abbas, M; Najmi, MH; Qayyum, A, 2013
)
0.62
"This study aimed to develop an oral delivery system using clay-based organic-inorganic hybrid materials to improve the bioavailability of the drug, flurbiprofen, which is poorly soluble in water."( 3-aminopropyl functionalized magnesium phyllosilicate as an organoclay based drug carrier for improving the bioavailability of flurbiprofen.
Choi, SK; Han, HK; Shin, HJ; Yang, L, 2013
)
0.8
"Development of solid dispersions is to improve the therapeutic efficacy by increasing the drug solubility, dissolution rate, bioavailability as well as to attain rapid onset of action."( Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen.
Daravath, B; Tadikonda, RR; Vemula, SK, 2015
)
0.65
"From the above results, it is concluded that the formulation of gelucire 44/14 solid dispersions is able to improve the solubility, dissolution rate as well as the absorption rate of flurbiprofen than pure form of drug."( Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen.
Daravath, B; Tadikonda, RR; Vemula, SK, 2015
)
0.85
" In this study, we have investigated the bioavailability of a new generic formulation of flurbiprofen lozenges developed by Epifarma Srl, compared to the originator Benactiv Gola® taken as reference."( Influence of the oral dissolution time on the absorption rate of locally administered solid formulations for oromucosal use: the flurbiprofen lozenges paradigm.
De Gregori, S; Imberti, R; Lisi, L; Navarra, P, 2014
)
0.83
"The purpose of this study was to develop novel solid lipid nanoparticle (SLN)-loaded dual-reverse thermosensitive hydrogel (DRTH) for rectal administration of flurbiprofen with improved bioavailability and reduced initial burst effect."( Novel dual-reverse thermosensitive solid lipid nanoparticle-loaded hydrogel for rectal administration of flurbiprofen with improved bioavailability and reduced initial burst effect.
Choi, HG; Choi, JY; Din, FU; Kim, DW; Kim, JO; Ku, SK; Mustapha, O; Park, JH; Rashid, R; Yong, CS, 2015
)
0.83
" The relative bioavailability of FP-HP-β-CD COE loaded liposomes was 420%, 201% and 402% compared with FP solution, FP-HP-β-CD and FP-liposomes, respectively."( Drug-in-cyclodextrin-in-liposomes: A novel drug delivery system for flurbiprofen.
Chen, F; Lin, C; Pan, W; Wang, X; Yang, X; Zhang, L; Zhang, Q; Zhang, W, 2015
)
0.65
"In this study, a novel controlled release osmotic pump capsule consisting of pH-modulated solid dispersion for poorly soluble drug flurbiprofen (FP) was developed to improve the solubility and oral bioavailability of FP and to minimize the fluctuation of plasma concentration."( A novel osmotic pump-based controlled delivery system consisting of pH-modulated solid dispersion for poorly soluble drug flurbiprofen: in vitro and in vivo evaluation.
Li, S; Liu, D; Pan, W; Wang, X; Wang, Y; Yang, X; Zhang, L; Zhao, Q, 2015
)
0.83
" The LCT-SNEDDS was considered to be superior for enhancement of the drug bioavailability when compared with other SNEDDS formulations and market product."( Studies on self-nanoemulsifying drug delivery system of flurbiprofen employing long, medium and short chain triglycerides.
Daar, J; Khan, A; Khan, GM; Khan, J, 2017
)
0.7
" A significant higher bioavailability of gabapentin administered 30min after meal, compared to fasting conditions or to dose administration 10min before meal, argued in favor of the gastro-retention of gabapentin prolonged release layer."( Multi-kinetics and site-specific release of gabapentin and flurbiprofen from oral fixed-dose combination: in vitro release and in vivo food effect.
Barchielli, M; Bettini, R; Buttini, F; Colombo, G; Colombo, P; Conti, C; Leoni, B; Loprete, L; Rossi, A; Sonvico, F, 2017
)
0.7
"A novel Flurbiprofen (FLB)-in-liposome-in-hydrogel formulation was developed, as a method to sustain the release and increase the ocular bioavailability of FLB following intravitreal injection."( Sustained release of intravitreal flurbiprofen from a novel drug-in-liposome-in-hydrogel formulation.
Antimisiaris, SG; Blazaki, S; Klepetsanis, P; Naoumidi, E; Pachis, K; Tsilimbaris, M; Tzatzarakis, M, 2017
)
1.17
" In this study, we evaluated the intravitreal bioavailability and anti-inflammatory efficacy of flurbiprofen in rabbit eyes."( Pharmacokinetics and efficacy of intraocular flurbiprofen.
Blazaki, S; Naoumidi, E; Tsatsakis, A; Tsatsanis, C; Tsika, C; Tsilimbaris, MK; Tzatzarakis, M, 2017
)
0.93
"A major challenge in ocular therapeutics is poor bioavailability of drug, 1% or even less of the instilled dose is absorbed and frequent administration of conventional products leads to poor adherence to therapy."( Preparation and Evaluation of N-Trimethyl Chitosan Nanoparticles of Flurbiprofen for Ocular Delivery.
Jain, DD; Joshi, PN; Shinde, UA; Singh, K, 2019
)
0.75
"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
"Flurbiprofen (FP) is one of the most potent nonsteroidal anti-inflammatory drugs with very low bioavailability of approximately 12% following transdermal administration, compared to that after oral administration."( Development of galangal essential oil-based microemulsion gel for transdermal delivery of flurbiprofen: simultaneous permeability evaluation of flurbiprofen and 1,8-cineole.
Chen, J; Dong, J; Dong, YF; Feng, H; Gu, W; Wu, FY; Yang, BQ; Zhu, XM, 2020
)
2.22
" Absolute bioavailability was 33% and 58% for microparticles and pellets, respectively."( Flurbiprofen sodium microparticles and soft pellets for nose-to-brain delivery: Serum and brain levels in rats after nasal insufflation.
Balafas, E; Banella, S; Bortolotti, F; Colombo, G; Colombo, P; Kostomitsopoulos, N; Manniello, MD; Napoli, L; Papakyriakopoulou, P; Quarta, E; Rekkas, DM; Russo, P; Tiozzo Fasiolo, L; Valsami, G, 2021
)
2.06
" In the rat model, in vivo pharmacokinetic parameters confirmed the improved relative bioavailability of reduced graphene oxide hydrogel when compared with the control hydrogel (without reduced graphene oxide) and marketed transdermal patch."( Transdermal delivery of flurbiprofen from polyoxypropylene-polyoxyethylene block copolymer stabilized reduced graphene oxide to manage pain in spondylitis: In vitro and in vivo studies.
Li, T; Yang, C, 2021
)
0.93
" Thereby, the increase in the drug bioavailability and efficiency must come from the mucoadhesion optimization of the drug delivery system."( Parametric Drug Release Optimization of Anti-Inflammatory Drugs by Gold Nanoparticles for Topically Applied Ocular Therapy.
Boisselier, E; Loiseau, A; Maranda, C; Poliquin, A; Raiche-Marcoux, G, 2022
)
0.72

Dosage Studied

Flurbiprofen demonstrated linear systemic kinetics throughout the dosing range, with constant body clearance and unbound fraction in plasma. Plasma exposure (both AUC and Cmax) was significantly higher (as much as 2 to 3-fold) than that without surfactant or beta-CD.

ExcerptRelevanceReference
" To date, 1220 patients have received the drug in a dosage varying from 75 mg to 400 mg daily."( A long-term assessment of flurbiprofen.
Marsh, BD; Sheldrake, FE; Webber, JM, 1977
)
0.56
"Fifteen patients with seropositive rheumatoid arthritis were treated for 2-weeks periods with 150 mg flurbiprofen daily and with flubriprofen in the same dosage plus 3 g aspirin daily, the treatments being administered in random allocation."( Flurbiprofen-aspirin interaction: a double-blind crossover study.
Brooks, PM; Khong, TK, 1977
)
1.92
" After dosing with [14C]flurbiprofen, tissue levels of radioactivity in dog and baboon were similar to that in plasma."( The disposition and metabolism of flurbiprofen in several species including man.
Adams, SS; Crampton, EL; Marchant, B; Risdall, PC, 1978
)
0.84
" During the first week, the patients' steroid dosage was stabilized at the minimum necessary to control symptoms."( Steroid-sparing action of flurbiprofen: use of an additional parameter of joint scans with 99m technetium.
Desai, MM; Joshi, VR; Lele, RD; Nagarwala, HK; Pispati, PK; Virani, AR, 1977
)
0.56
" It was planned that, unless withdrawn, patients from matched pairs received either flurbiprofen (150 mg to 300 mg daily) or indomethacin (75 mg to 150 mg daily) over a minimum period of 6 months, dosage being adjusted to suit exacerbations and remission of disease."( A comparative study of the long-term efficacy of flurbiprofen and indomethacin in the treatment of rheumatoid arthritis, with special reference to iron metabolism.
Bulgen, DY; Hazleman, BL, 1977
)
0.74
" 2 Each patient was given a long-term supply of drug and was asked to vary their own dosage within simple limits, according to the severity of their symptoms."( Continued use of non-steroidal anti-inflammatory drugs: an index of clinical efficacy.
Buchanan, WW; Capell, HA; Dick, WC; Paterson, S; Rooney, PJ, 1978
)
0.26
" Superfusion of the arterial segment with PGI2 demonstrates a dose-response related inhibition of ADP-induced thrombosis."( The role of prostaglandins in platelet-vessel wall interaction.
Andries, R; Bourgain, RH; Finne, E, 1979
)
0.26
" Ibuprofen showed suppression in most tissues three hours after dosing with a return to control values by twenty-four hours."( In vivo suppression of prostaglandin biosynthesis by non-steroidal anti-inflammatory agents.
Fitzpatrick, FA; Wynalda, MA, 1976
)
0.26
" The very shallow dose-response curves for flurbiprofen compared with acetylsalicylic acid, especially in the mouse and the rat test systems, are not due to an unreliable or abnormal absorption, which suggests that in these species the mode of action of flurbiprofen is not identical with that of acetylsalicylic acid."( Some biological properties of flurbiprofen, an anti-inflammatory, analgesic and antipyretic agent.
Adams, SS; McCullough, KF; Nicholson, JS, 1975
)
0.81
" The effects of different polymer ratios of Eudragit RS30D and Eudragit RL30D, different particle sizes, and different combination of various formulations of solid dispersions on the in vitro release kinetics of drugs from the dosage forms were investigated."( Development of extended-release solid dispersions of nonsteroidal antiinflammatory drugs with aqueous polymeric dispersions: optimization of drug release via a curve-fitting technique.
Ho, C; Hwang, GC, 1992
)
0.28
" The disposition of flurbiprofen enantiomers was not changed upon multiple dosing and no evidence of futile cycling was found."( Stereoselective disposition of flurbiprofen in uraemic patients.
Brater, DC; Hall, SD; Knadler, MP, 1992
)
0.89
"The pharmacokinetics of flurbiprofen (Ansaid Tablets, Upjohn Company of Canada, Don Mills, Ontario) were evaluated in both younger (40 to 60 years) and elderly (65 to 83 years) rheumatoid arthritic patients after both a 100-mg single-dose administration and at steady state during a 100-mg twice-a-day dosage regimen."( The pharmacokinetics of flurbiprofen in younger and elderly patients with rheumatoid arthritis.
Antal, EJ; Buchanan, WW; Cauvier, H; Grace, EM; Kean, WF; Rischke, J, 1992
)
0.9
" For preliminary dose-response studies, antibiotic sensitivity blank disks loaded with 10 microliters of flurbiprofen 250 micrograms, 50 micrograms and 5 micrograms, or ibuprofen 500 micrograms, 50 micrograms and 5 micrograms were placed on the seeded agar plates."( Antimicrobial activity of flurbiprofen and ibuprofen in vitro against six common periodontal pathogens.
Fleury, AA; Hammond, BF; Hersh, EV, 1991
)
0.8
" Flurbiprofen in 50 mg and 100 mg dosages demonstrated effective analgesic activity with the 100 mg dosage being at least as effective as the acetaminophen/codeine combination."( The analgesic efficacy of flurbiprofen compared to acetaminophen with codeine.
Cooper, SA; Kupperman, A, 1991
)
1.49
" On d 21 and 28, serum and CF samples were taken prior to dosing and afterwards at 1, 2, 4 and 6 hours."( Flurbiprofen in human crevicular fluid analyzed by high-performance liquid chromatography.
Barrett, AW; Edwards, G; Heasman, PA; Seymour, RA; Ward, A, 1990
)
1.72
" No significant difference in rates of absorption of carprofen from rectal solution and suppository was seen; this allowed the conclusion that drug release from the semi-solid dosage form was not the rate-limiting step in carprofen absorption from the suppository."( Biopharmaceutical evaluation of carprofen following single intravenous, oral, and rectal doses in dogs.
Guentert, TW; Schmitt, M, 1990
)
0.28
" This investigation focuses on the changes in CO metabolites which occur during disease progression of ligature-induced periodontitis and on the dose-response relationship of flurbiprofen, as it relates to disease inhibition and the suppression of ARA metabolites within the crevicular fluid (CF)."( Changes in cyclooxygenase metabolites in experimental periodontitis in Macaca mulatta.
Braswell, LD; Green, MD; Hall, CM; Johnson, HG; McClure, H; Odle, BM; Offenbacher, S; Orkin, JL; Strobert, EA, 1989
)
0.47
" This was conducted, first as a dose-response study and, second, as a time-course study."( Inhibition of hypertonic saline-induced bronchoconstriction by terfenadine and flurbiprofen. Evidence for the predominant role of histamine.
Finnerty, JP; Holgate, ST; Wilmot, C, 1989
)
0.5
" There was a significant dose-response regression between flurbiprofen 25 mg and both of the higher dosages."( An evaluation of flurbiprofen, aspirin, and placebo in postoperative oral surgery pain.
Beaver, WT; Forbes, JA; Rosenmertz, SK; Selinger, LR; Yorio, CC, 1989
)
0.86
" Paired milk and plasma samples were obtained during this period of dosing as well as after the last dose."( Flurbiprofen in post-partum women: plasma and breast milk disposition.
Brown, RD; Cook, SM; Hinson, JL; Johnson, VA; Smith, IJ; Whitt, RT; Wilson, JT, 1989
)
1.72
" Flurbiprofen showed a linear dose-response relationship with respect to gastric injury and serum drug levels."( The effects of flurbiprofen, aspirin, cimetidine, and antacids on the gastric and duodenal mucosa of normal volunteers. An endoscopic and photographic study.
Friedman, H; Lanza, FL; Royer, GL; Schwartz, JH; Seckman, CE; Stubbs, CM, 1989
)
1.54
" Increased dosage did not produce a proportional increase in the permeation and maximizing the skin-drug contact did not increase penetration: both factors indicate that absorption from deposited drug films was dissolution rate-limited."( Absorption through human skin of ibuprofen and flurbiprofen; effect of dose variation, deposited drug films, occlusion and the penetration enhancer N-methyl-2-pyrrolidone.
Akhter, SA; Barry, BW, 1985
)
0.53
" Flurbiprofen, a potent non-steroidal anti-inflammatory drug, administered intramuscularly on 3 successive days following the combined infection at a dosage of 1 mg/kg/12 h was without beneficial effect on diarrhoea or mortality."( Pathophysiology of diarrhoea induced by a combined infection with transmissible gastroenteritis virus and enterotoxigenic Escherichia coli in newly-weaned piglets and the effect of flurbiprofen treatment.
Cools, V; Cox, E; Houvenaghel, A, 1988
)
1.38
"Forty patients with classic or definite rheumatoid arthritis were entered into a double-blind, randomized, multiple crossover, sequential trial comparing two doses (300 mg vs 150 mg per day) and two dosing schedules (b."( A comparative analysis of two dosing strategies of flurbiprofen in rheumatoid arthritis: an application of sequential trial design.
Bellamy, N; Kreeft, JH, 1988
)
0.53
"The ocular bioavailability of radiolabeled flurbiprofen was determined after single or multiple topical dosing of rabbits."( Multiple dosing increases the ocular bioavailability of topically administered flurbiprofen.
Anderson, JA; Chen, CC, 1988
)
0.77
" Side-effects were similar in nature to those of other drugs in this group and no correlation in their frequency or severity with the dosage of flurbiprofen was found."( A long-term study of flurbiprofen in rheumatological disorders: II. Osteoarthrosis.
Busson, M, 1986
)
0.79
" Flurbiprofen was administered in a total daily dosage of 200 to 300 mg four times daily."( Treatment of acute shoulder syndrome with flurbiprofen.
Brinn, EL; Lamborn, KR; Lomen, PL; Mena, HR; Turner, LF, 1986
)
1.45
" Flurbiprofen demonstrated linear systemic kinetics throughout the dosing range, with constant body clearance and unbound fraction in plasma."( Relationship between the ocular and systemic disposition of flurbiprofen: the effect of altered protein dynamics at steady state.
Liu, S; Tang-Liu, DD, 1987
)
1.43
" Dose-response curves were studied at 4 h following administration of indomethacin on the 19th, 20th, and 21st days, and flurbiprofen on the 20th and 21st days."( In vivo constriction of the ductus arteriosus by nonsteroidal antiinflammatory drugs in near-term and preterm fetal rats.
Momma, K; Takao, A, 1987
)
0.48
" Dose-response curves to noradrenaline and KCl administered as bolus doses were obtained."( Effect of three loop diuretics and prostaglandins E2 & I2 on the isolated perfused rat mesenteric vasculature.
Foy, JM; Nuhu, SZ, 1985
)
0.27
" These results suggest that modulation of leukotaxis by NSAIDs may reflect a differential dose-response sensitivity of lipoxygenase and cycloxygenase pathways."( In vivo modulation of leukotaxis by non-steroidal anti-inflammatory drugs.
diZerega, GS; Nakamura, RM; Shimanuki, T, 1985
)
0.27
" Many flurbiprofen-treated patients (46 percent) completing the trial followed a relatively low dosage regimen of 50 mg twice daily for more than half the study."( Treatment of osteoarthritis of the knee. A comparison of flurbiprofen and aspirin.
Brinn, EL; Lamborn, KR; Lomen, PL; Porter, GH; Turner, LF, 1986
)
1
" From a practical point of view, 2 seems to be particularly useful for improving the pharmaceutical properties of flurbiprofen in various dosage forms."( Improvement of dissolution and suppository release characteristics of flurbiprofen by inclusion complexation with heptakis(2,6-di-O-methyl)-beta-cyclodextrin.
Hirayama, F; Imai, T; Irie, T; Maeda, T; Otagiri, M; Uekama, K, 1985
)
0.71
"Miniaturised methods have been used to construct dose-response curves for the effects of inhibitory drugs on prostaglandin synthesis using individual rectal biopsies obtained from patients with ulcerative colitis."( Inhibition of prostaglandin synthetase in human rectal mucosa.
Hawkey, CJ; Lo Casto, M, 1983
)
0.27
" Dose-response curves to noradrenaline administered as bolus doses or frequency-response curves from transmural arterial electrical stimulation were obtained."( Effect of bumetanide, frusemide and prostaglandin E2 on the isolated perfused kidney of rat and rabbit.
Foy, JM; Nuhu, SZ, 1984
)
0.27
" Based on the inhibitory effect of the steroidal anti-inflammatory drugs, non-steroidal agents, such as indomethacin, were also expected to show some degree of inhibition; however, repeated tumor experiments demonstrate that indomethacin enhances TPA promotion in a dose-response manner."( Indomethacin enhancement of TPA tumor promotion in mice.
Fischer, SM; Gleason, GL; Mills, GD; Slaga, TJ, 1980
)
0.26
" Sustained release dosage forms are available, which may be beneficial due to the short terminal phase elimination half-life of conventional immediate release flurbiprofen (3 to 6 hours)."( Clinical pharmacokinetics of flurbiprofen and its enantiomers.
Davies, NM, 1995
)
0.78
" Oral dosing had exhibited no significant bone activity."( Chiral pharmacokinetics of Rac-flurbiprofen and pharmacodynamics of anabolic bone response in the normal rat.
Bigornia, AE; Jee, WS; Murray, ED; Wechter, WJ, 1994
)
0.57
" The potency ratio between the dose-response curves was 10 (6-20; 95% confidence intervals)."( Antinociception produced by spinal delivery of the S and R enantiomers of flurbiprofen in the formalin test.
Malmberg, AB; Yaksh, TL, 1994
)
0.52
" The dose-response for ibuprofen and flurbiprofen was roughly equivalent to that of clofibric acid, whereas indomethacin was less active."( Induction of peroxisomal beta-oxidation by nonsteroidal anti-inflammatory drugs.
Eacho, PI; Foxworthy, PS; Perry, DN, 1993
)
0.56
"015), and the dosing frequency of relief medication (P < ."( Flurbiprofen in the prophylaxis of migraine.
Kunkel, RS; Solomon, GD,
)
1.57
"The effect of food on the plasma concentration-time profile of sustained release dosage forms of ibuprofen and flurbiprofen has been investigated in healthy Asian Indian volunteers, in two separate studies."( The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations.
Kelkar, MG; Nayak, PJ; Pargal, A, 1996
)
0.75
" A dose-response study with flurbiprofen (single doses of 5, 10, 20, and 40 mg/kg) and equimolar doses of nitroxybutyl-flurbiprofen was performed; assessing their effect on intestinal permeability (at 18-20 hours), with 51Cr EDTA, and the number of pointed (< 5 mm) and longitudinal (> 5 mm) small intestinal ulcers at 24 hours."( Intestinal tolerability of nitroxybutyl-flurbiprofen in rats.
Bjarnason, I; Jacob, M; Macpherson, A; Mahmud, T; Price, AB; Rafi, S; Scott, D; Sherwood, R; Sigthorsson, G; Somasundaram, S; Wrigglesworth, JM, 1997
)
0.86
" Male Sprague-Dawley rats were dosed with two doses of metronidazole (50 mg/kg, 12 and 1 h pre-NSAID) or a single 100 mg/kg dose of tempo 1 h prior to NSAIDs."( Pharmacological protection of NSAID-induced intestinal permeability in the rat: effect of tempo and metronidazole as potential free radical scavengers.
Davies, NM; Jamali, F, 1997
)
0.3
"5 days of dosing were used to detect newly occurring hemorrhages and erosions."( Clinical endoscopic evaluation of the gastroduodenal tolerance to (R)- ketoprofen, (R)- flurbiprofen, racemic ketoprofen, and paracetamol: a randomized, single-blind, placebo-controlled trial.
Caubet, JF; Handley, DA; Jerussi, TP; McCray, JE, 1998
)
0.52
" Dose-response for intestinal ulcer production was observed for rac- and (S)-flurbiprofen; animals given (R)-flurbiprofen exhibited no ulcers."( Mechanism of enhancement of intestinal ulcerogenicity of S-aryl propionic acids by their R-enantiomers in the rat.
Gibson, K; Kantoci, D; Leipold, D; Liu, Y; McCracken, JD; Mineyama, Y; Murray, ED; Quiggle, D; Wechter, WJ, 1998
)
0.53
" Three dosage forms were selected for this study: capsules, suppositories, and creams."( Effect of chemical structure on the release of certain propionic acid derivatives from their dosage forms.
el-Bary, AA; el-Nabarawi, MA; Mohamed, MI, 1998
)
0.3
" Groups of six rats received either vehicle or analgesic drug and antinociception was evaluated by evaluating the dose-response curves over time."( Antinociceptive effects of S(+)-ketoprofen and other analgesic drugs in a rat model of pain induced by uric acid.
Cabré, F; Díaz, I; Fernández-Guasti, A; López-Muñoz, FJ; Mauleón, D; Tost, D; Ventura, R, 1998
)
0.3
" It is concluded that the current microemulsion system might be applicable to formulate the parenteral dosage form of poorly water-soluble flurbiprofen without chemical modification."( Phospholipid-based microemulsions of flurbiprofen by the spontaneous emulsification process.
Hwang, KJ; Kim, CK; Lee, MK; Park, KM, 1999
)
0.78
"The present investigation was undertaken to explore the ulcer healing and antiangiogenic efficacy of two dosage schedules of topically administered amiloride in mechanically produced corneal ulcers in rabbits and to compare its effect with the conventional topical antiinflammatory angiostatic agent flurbiprofen."( Topical amiloride accelerates healing and delays neovascularization in mechanically produced corneal ulcers in rabbits.
Chugh, P; Gupta, B; Sood, AK, 1999
)
0.48
" Groups of 6 rats received either vehicle or the enantiomer in turn and antinociception was determined by evaluating the dose-response curves over time."( Analysis of antinociceptive effects of flurbiprofen enantiomers in a rat model of arthritic pain.
Cabré, F; Díaz, MI; Domínguez, AM; García, ML; Hernández, GP; López-Muñoz, FJ; Mauleón, D; Ventura, R, 2000
)
0.58
"5 mg; the sore throat pain model is a sensitive assay for demonstration of the dose-response relationship of an analgesic agent."( Demonstration of dose response of flurbiprofen lozenges with the sore throat pain model.
Christian, J; Gibb, IA; Homan, HD; Schachtel, BP, 2002
)
0.59
" Thirteen of the NSAIDs and the enantiomers of flurbiprofen were then tested in acute dosing studies in amyloid beta protein precursor (APP) transgenic mice, and plasma and brain levels of Abeta and the drug were evaluated."( NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo.
Das, P; Eriksen, JL; Golde, TE; Jessing, KW; Koo, EH; McLendon, DC; Ozols, VV; Sagi, SA; Smith, TE; Weggen, S; Zavitz, KH, 2003
)
0.88
" Since the disk assembly in the USP for patch dosage forms was unsuited for use in a release test due to penetration of the dissolution medium into the cataplasm from the screw part of the device and the cataplasm swelled, new holders were designed."( Investigation of the release test method for the topical application of pharmaceutical preparations: release test of cataplasm including nonsteroidal anti-inflammatory drugs using artificial sweat.
Kobayashi, D; Kogo, T; Morimoto, Y; Numajiri, S; Shimamura, T; Tairabune, T; Ueda, H, 2004
)
0.32
" Selected binary systems were used for preparation of direct compression tablets with reduced drug dosage (50 mg)."( Development of fast-dissolving tablets of flurbiprofen-cyclodextrin complexes.
Cirri, M; Corti, G; Maestrelli, F; Mura, P; Rangoni, C, 2005
)
0.59
" Furthermore, to assess time profiles of KP concentration in the skin and plasma, guinea pigs received a repeated topical application of R-KP and S-KP at a dosage of 40 mg/kg over a period of 3 days."( Study on the mechanism of photosensitive dermatitis caused by ketoprofen in the guinea pig.
Chikamatsu, N; Igarashi, T; Nagata, O; Nakazawa, T; Shimo, T; Yamamoto, M, 2006
)
0.33
" In murine models of AD, (R)-flurbiprofen lowered brain levels of Abeta(1-42), and chronic dosing reduced brain amyloid pathology and prevented defects in learning and memory."( Drug evaluation: (R)-flurbiprofen--an enantiomer of flurbiprofen for the treatment of Alzheimer's disease.
Geerts, H, 2007
)
0.95
" This mucoadhesive formulation offers many advantages over buccal lozenges because it allows for reduction in daily administrations and daily drug dosage and is suitable for the treatment of irritation, pain, and discomfort associated with gingivitis, sore throats, laryngopharyngitis, cold, and periodontal surgery."( Mucoadhesive bilayered tablets for buccal sustained release of flurbiprofen.
Ambrogi, V; Blasi, P; Giovagnoli, S; Perioli, L; Ricci, M; Rossi, C, 2007
)
0.58
" We have examined the inhibitory effect of free fatty acid (FFA), a binding inhibitor for site II of HSA, on the binding of flurbiprofen in-vitro and in-vivo by ultrafiltration, to establish an effective dosage of FP-ax."( Dosage plan of a flurbiprofen injection product using inhibition of protein binding by lipid emulsion in rats.
Arimori, K; Higuchi, S; Kawai, K; Ogata, K; Takamura, N; Tokunaga, J, 2008
)
0.89
" The heart rate (HR), mean arterial pressure (MAP) and SpO2 were monitored during the operation, and the induction time, recovery time, propofol dosage and adverse effect were recorded."( [Application of flurbiprofen preemptive analgesia combined with intravenous propofol anesthesia in induced abortion].
Lao, JX; Liu, WX; Tan, SX; Zhang, YF, 2008
)
0.69
" Further experimental work towards identifying the most efficacious COX-2 inhibitors, as well as the mechanism of action and the optimal dosage regimen should be executed."( Cyclooxygenase inhibitors: a novel direction for Alzheimer's management.
Banerjee, A; Nivsarkar, M; Padh, H,
)
0.13
" In three other groups (n = 8 in each group), the selected dosage of 10 mg/kg was administrated intravenously at 6, 12 and 24 hours after I/R."( Therapeutic time window of flurbiprofen axetil's neuroprotective effect in a rat model of transient focal cerebral ischemia.
Dong, HL; Liu, JL; Lu, Y; Sang, HF; Wang, C; Xiong, LZ, 2008
)
0.64
" The effect became less potent with time despite continuous dosing indicating adaptation for both topical and systemic effects."( Influence of prolonged exposure of a short half life non-steroidal anti-inflammatory drugs on gastrointestinal safety.
Campanella, C; Jamali, F, 2009
)
0.35
" The repeated dosing rather than the magnitude of t(1/2) may influence the gut safety profile of NSAIDs."( Influence of prolonged exposure of a short half life non-steroidal anti-inflammatory drugs on gastrointestinal safety.
Campanella, C; Jamali, F, 2009
)
0.35
" Consistent with the enhanced solubility, the plasma exposure (both AUC and Cmax) of flurbiprofen when dosed as the mixed system was significantly higher (as much as 2 to 3-fold) than that without surfactant or beta-CD, with surfactant alone, or with beta-CD alone."( Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound.
Balakrishnan, P; Choi, HG; Han, MJ; Joe, JH; Kim, JO; Li, DX; Oh, DH; Park, SM; Seo, Y; Yan, YD; Yong, CS, 2010
)
0.87
" PGE(2) levels in mice dosed with R-2-phenylpropionic acid were elevated."( Role of COX-2 in nonsteroidal anti-inflammatory drug enteropathy in rodents.
Bjarnason, IT; Hotz-Behofsits, C; Simpson, RJ; Walley, M, 2010
)
0.36
" A novel population pharmacokinetic model is developed to estimate the individual pharmacokinetic parameter for patients intravenous injecting FA in terms of patients' characteristics and dosing history, and to design a prior dosage regimen."( [Population pharmacokinetic modeling of flurbiprofen].
Gong, SJ; Huang, PF; Lin, WW; Wang, CL, 2010
)
0.63
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Blood samples were collected prior to dosing and at predefined intervals for 24 h after dose."( A randomised, two-period, cross-over, open-label study to evaluate the pharmacokinetic profiles of single doses of two different flurbiprofen 8.75-mg lozenges in healthy volunteers.
Annoni, O; Brunner, M; Burian, A; Lauro, V; Martin, W; Matzneller, P; Tacchi, R; Zeitlinger, M, 2012
)
0.58
" However, its multiple dosing due to short elimination half life is a concern for such treatment."( Formulation, characterization and in vitro-in vivo evaluation of flurbiprofen-loaded nanostructured lipid carriers for transdermal delivery.
Chauhan, MK; Kawadkar, J; Kishore, R; Pathak, A, 2013
)
0.63
"To compare tissue concentrations of flurbiprofen resulting from topical application and oral administration according to the regulatory approved dosing guidelines."( Flurbiprofen concentration in soft tissues is higher after topical application than after oral administration.
Kai, S; Kawaguchi, Y; Kitamura, N; Kondo, E; Yasuda, K, 2013
)
2.11
" This was done to evaluate potential degradation and thereby biological conversion of the cyclodextrins if dosed orally, as the intestinal tract contains α-amylase for digestive purposes."( In vitro investigations of α-amylase mediated hydrolysis of cyclodextrins in the presence of ibuprofen, flurbiprofen, or benzo[a]pyrene.
Holm, R; Jørgensen, EB; Larsen, KL; Lumholdt, LR, 2012
)
0.59
" No significant differences between treatment groups were found in neuropsychological tests but a positive dose-response trend was found on executive function in APOE4 carriers."( CHF5074 reduces biomarkers of neuroinflammation in patients with mild cognitive impairment: a 12-week, double-blind, placebo-controlled study.
Bottini, G; Calza, L; Casula, D; Cicirello, H; Fernandez, M; Fiorentini, F; Franceschi, M; Frigerio, E; Giardino, L; Imbimbo, BP; Norris, D; Nunez, M; Ross, J; Scarpini, E; Sharma, S; Sivilia, S; Winston, J, 2013
)
0.39
" No dropsy and erythema were observed after continuous dosing 7 d of FP NLC-gel on the rabbit skin, and the xylene-induced ear drossy could be inhibited by FP NLC-gel at different dosages."( Nanostructured lipid carriers-based flurbiprofen gel after topical administration: acute skin irritation, pharmacodynamics, and percutaneous absorption mechanism.
Han, F; Li, S; Song, A; Su, Z, 2015
)
0.69
" Our data for the given example, however, puts the benefit of individual drug dosing to question, if it is exclusively based on genotype."( CYP2C9 genotype vs. metabolic phenotype for individual drug dosing--a correlation analysis using flurbiprofen as probe drug.
Lutz, RW; Lutz, WK; Schönfelder, G; Vogl, S, 2015
)
0.63
" The novel controlled delivery system with combination of pH-modulated solid dispersion and osmotic pump system is not only a promising strategy to improve the solubility and oral bioavailability of poorly soluble ionizable drugs but also an effective way to reduce dosing frequency and minimize the plasma fluctuation."( A novel osmotic pump-based controlled delivery system consisting of pH-modulated solid dispersion for poorly soluble drug flurbiprofen: in vitro and in vivo evaluation.
Li, S; Liu, D; Pan, W; Wang, X; Wang, Y; Yang, X; Zhang, L; Zhao, Q, 2015
)
0.62
"Compared with the control group, the VAS score at 48 h after surgery, and the dosage of the supplemented Sauteralgyl were evidently lower, and the time of both exhaust and defecation after surgery was significantly earlier, and the degree of nausea after surgery was obviously milder in patients of the EA group (P<0."( [Electroacupuncture Intervention Combined with Anesthetics for Analgesia and Post-surgical Gastrointestinal Recovery in Pneumectomy Patients].
Chen, TY; Ma, W; Wang, K; Wu, YY; Xu, JJ; Zhou, J, 2015
)
0.42
"EA intervention combined with anesthetics is effective in reducing the dosage of the supplemented Sauteralgyl and the degree of postoperative nausea, and in improving postoperative gastrointestinal functional recovery in patients undergoing pneumectomy."( [Electroacupuncture Intervention Combined with Anesthetics for Analgesia and Post-surgical Gastrointestinal Recovery in Pneumectomy Patients].
Chen, TY; Ma, W; Wang, K; Wu, YY; Xu, JJ; Zhou, J, 2015
)
0.42
" The dose-response curve (DRCs) shows that the combination of rac-Flur (31."( Antinociceptive Effect of Racemic Flurbiprofen and Caffeine Co-Administration in an Arthritic Gout-Type Pain in Rats.
Espinosa-Juárez, JV; Jaramillo-Morales, OA; Liévano-Reyes, R; López-Muñoz, FJ; Pérez-Méndez, HI; Solís-Oba, A, 2016
)
0.71
"To develop the first photoactive biomaterial coating capable of controlled drug dosing via inclusion of synthesised drug-3,5-dimethoxybenzoin (DMB) conjugates in a poly(2-methyoxyethyl acrylate) (pMEA) scaffold."( Photochemically Controlled Drug Dosing from a Polymeric Scaffold.
Donnelly, L; Gorman, SP; Hardy, JG; Irwin, NJ; Jones, DS; McCoy, CP, 2017
)
0.46
" Biorelevant release tests have become a standard in the prediction of in vivo pharmacokinetics but also in quality control of novel dosage forms."( A comparison of two biorelevant in vitro drug release methods for nanotherapeutics based on advanced physiologically-based pharmacokinetic modelling.
Gao, F; Jung, F; Nothnagel, L; Thurn, M; Vogel, V; Wacker, MG, 2018
)
0.48
"Tribo-electrification is a common occurrence within the pharmaceutical industry where solid dosage forms constitute majority of pharmaceutical formulations."( The effect of mesoporous silica impregnation on tribo-electrification characteristics of flurbiprofen.
Afzal, MS; Ghori, MU; Granollers, M; Šupuk, E; Zanin, F, 2018
)
0.7
" Consequently, the development of an easy-to-swallow liquid oral dosage form supported by a combined PBPK-IVIVC model was approached."( Predictive PBPK modeling as a tool in the formulation of the drug candidate TMP-001.
Ashtikar, M; Geisslinger, G; Jung, F; Nothnagel, L; Parnham, MJ; Rossmanith, T; Thurn, M; Wacker, MG, 2019
)
0.51
" The pain intensity, consumed sufentanil dosage of the PCA, and the side effects was not different between groups."( Effect of flurbiprofen axetil on postoperative delirium for elderly patients.
Chen, H; Han, F; Hu, Y; Wang, L; Wang, X; Wang, Y; Wei, L; Zhao, W, 2019
)
0.92
" The present study tested the hypothesis that multimodal analgesia with combined ropivacaine wound infiltration and intravenous flurbiprofen axetil after radical thyroidectomy provided better analgesia than a single dosage of tramadol."( Multimodal analgesia with ropivacaine wound infiltration and intravenous flurbiprofen axetil provides enhanced analgesic effects after radical thyroidectomy: a randomized controlled trial.
Li, X; Tan, H; Yang, J; Yu, L, 2019
)
0.95
" The second phase was similar to the first, except each treatment was administered at a dosage of 1 drop/eye, twice daily for 5 days and CS was measured before treatment initiation and at 15 minutes and 24 and 48 hours after the last dose."( Effects of topical instillation of 0.1% diclofenac sodium, 0.5% ketorolac tromethamine, and 0.03% flurbiprofen sodium on corneal sensitivity in ophthalmologically normal cats.
Meekins, JM; Rankin, AJ; Roberts, JK; Roush, JK, 2021
)
0.84
" Flurbiprofen is widely used as an oral formulation (tablet dosage form) to control pain in spondylitis; however, owing to its short half-life (3."( Transdermal delivery of flurbiprofen from polyoxypropylene-polyoxyethylene block copolymer stabilized reduced graphene oxide to manage pain in spondylitis: In vitro and in vivo studies.
Li, T; Yang, C, 2021
)
1.84
" The dosage of sufentanil and the times of pressing analgesia pump in group D & F were significantly less than those in group F (p<0."( Application effect of dexmedetomidine combined with flurbiprofen axetil and flurbiprofen axetil monotherapy in radical operation of lung cancer and evaluation of the immune function.
Chen, Y; Du, J; Tao, H; Zong, S,
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitorA compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.
[role 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]

Drug Classes (2)

ClassDescription
fluorobiphenylAny member of the class of biphenyls that is a mono or poly-substituted biphenyl having fluro group as one of the substituents.
monocarboxylic acidAn oxoacid containing a single carboxy group.
[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 (1)

PathwayProteinsCompounds
Flurbiprofen Action Pathway2967

Protein Targets (43)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency37.62820.007215.758889.3584AID1224835; AID588342
glp-1 receptor, partialHomo sapiens (human)Potency35.48130.01846.806014.1254AID624172
SMAD family member 2Homo sapiens (human)Potency13.80060.173734.304761.8120AID1346859
PPM1D proteinHomo sapiens (human)Potency37.02590.00529.466132.9993AID1347411
SMAD family member 3Homo sapiens (human)Potency13.80060.173734.304761.8120AID1346859
AR proteinHomo sapiens (human)Potency39.15330.000221.22318,912.5098AID743036; AID743053
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency8.63490.013326.981070.7614AID1346978
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency30.63790.000657.913322,387.1992AID1259377
EWS/FLI fusion proteinHomo sapiens (human)Potency19.99700.001310.157742.8575AID1259252; AID1259253; AID1259256
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency62.60190.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency27.53570.000817.505159.3239AID1159527
farnesoid X nuclear receptorHomo sapiens (human)Potency54.94100.375827.485161.6524AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency19.33120.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.51450.000229.305416,493.5996AID743069; AID743075; AID743079
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency13.80140.001019.414170.9645AID743094; AID743191
caspase-3Homo sapiens (human)Potency8.63490.013326.981070.7614AID1346978
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency7.760619.739145.978464.9432AID1159509
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency53.58020.000323.4451159.6830AID743065; AID743067
histone deacetylase 9 isoform 3Homo sapiens (human)Potency45.00330.037617.082361.1927AID1259364; AID1259388
Interferon betaHomo sapiens (human)Potency37.02590.00339.158239.8107AID1347411
Cellular tumor antigen p53Homo sapiens (human)Potency32.58050.002319.595674.0614AID651631
TAR DNA-binding protein 43Homo sapiens (human)Potency15.84891.778316.208135.4813AID652104
[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)
Acid-sensing ion channel 3Rattus norvegicus (Norway rat)IC50 (µMol)229.08709.50009.50009.5000AID1476081
Bile salt export pumpHomo sapiens (human)IC50 (µMol)724.70000.11007.190310.0000AID1449628
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki111.59000.01501.24876.9200AID407366; AID407369
Amyloid-beta precursor proteinHomo sapiens (human)IC50 (µMol)305.00000.00053.889510.0000AID255950
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)0.16830.00032.177410.0000AID1282661; AID162021; AID162150; AID462317
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki1.00000.00162.12129.0000AID162164
Fatty acid-binding protein, intestinalHomo sapiens (human)Ki24.13330.30005.48149.4000AID1801103; AID407368
Aldo-keto reductase family 1 member C4Homo sapiens (human)IC50 (µMol)100.00002.30004.86338.2500AID703399
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.67540.00021.557410.0000AID1330180; AID313126; AID625243
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.57400.00010.995010.0000AID1282662; AID1330181; AID162497; AID313125; AID625244
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC50 (µMol)1.56000.05002.207010.0000AID703400
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC50 (µMol)32.50000.37004.09519.2800AID703401
Acid-sensing ion channel 1Rattus norvegicus (Norway rat)IC50 (µMol)169.82402.00002.00002.0000AID1476078
Aldo-keto reductase family 1 member C1Homo sapiens (human)IC50 (µMol)100.00000.00603.12657.9000AID703402
Prostaglandin G/H synthase 2Mus musculus (house mouse)IC50 (µMol)0.50000.00050.40086.2000AID462318
Solute carrier family 22 member 6Homo sapiens (human)IC50 (µMol)1.50000.27004.53069.9000AID681160
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.17000.00291.823210.0000AID254854
[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)
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km90.00007.34007.34007.3400AID624632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (370)

Processvia Protein(s)Taxonomy
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)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo 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 gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
cognitionAmyloid-beta precursor proteinHomo sapiens (human)
G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglial cell activationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
suckling behaviorAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activation involved in immune responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of translationAmyloid-beta precursor proteinHomo sapiens (human)
protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
intracellular copper ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
endocytosisAmyloid-beta precursor proteinHomo sapiens (human)
response to oxidative stressAmyloid-beta precursor proteinHomo sapiens (human)
cell adhesionAmyloid-beta precursor proteinHomo sapiens (human)
regulation of epidermal growth factor-activated receptor activityAmyloid-beta precursor proteinHomo sapiens (human)
Notch signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
axonogenesisAmyloid-beta precursor proteinHomo sapiens (human)
learning or memoryAmyloid-beta precursor proteinHomo sapiens (human)
learningAmyloid-beta precursor proteinHomo sapiens (human)
mating behaviorAmyloid-beta precursor proteinHomo sapiens (human)
locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
axo-dendritic transportAmyloid-beta precursor proteinHomo sapiens (human)
cholesterol metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of cell population proliferationAmyloid-beta precursor proteinHomo sapiens (human)
adult locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
visual learningAmyloid-beta precursor proteinHomo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglia developmentAmyloid-beta precursor proteinHomo sapiens (human)
axon midline choice point recognitionAmyloid-beta precursor proteinHomo sapiens (human)
neuron remodelingAmyloid-beta precursor proteinHomo sapiens (human)
dendrite developmentAmyloid-beta precursor proteinHomo sapiens (human)
regulation of Wnt signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
extracellular matrix organizationAmyloid-beta precursor proteinHomo sapiens (human)
forebrain developmentAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection developmentAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of chemokine productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-1 beta productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-6 productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of tumor necrosis factor productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of multicellular organism growthAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of neuron differentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of glycolytic processAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of JNK cascadeAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAmyloid-beta precursor proteinHomo sapiens (human)
collateral sprouting in absence of injuryAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of inflammatory responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of synapse structure or activityAmyloid-beta precursor proteinHomo sapiens (human)
synapse organizationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular process controlling balanceAmyloid-beta precursor proteinHomo sapiens (human)
synaptic assembly at neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
neuron apoptotic processAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
neuron cellular homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAmyloid-beta precursor proteinHomo sapiens (human)
response to interleukin-1Amyloid-beta precursor proteinHomo sapiens (human)
modulation of excitatory postsynaptic potentialAmyloid-beta precursor proteinHomo sapiens (human)
NMDA selective glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of spontaneous synaptic transmissionAmyloid-beta precursor proteinHomo sapiens (human)
cytosolic mRNA polyadenylationAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionAmyloid-beta precursor proteinHomo sapiens (human)
cellular response to amyloid-betaAmyloid-beta precursor proteinHomo sapiens (human)
regulation of presynapse assemblyAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection maintenanceAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of T cell migrationAmyloid-beta precursor proteinHomo sapiens (human)
central nervous system developmentAmyloid-beta precursor proteinHomo sapiens (human)
fatty acid metabolic processFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein, intestinalHomo sapiens (human)
intestinal lipid absorptionFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid transportFatty acid-binding protein, intestinalHomo 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)
retinoid metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid biosynthetic processAldo-keto reductase family 1 member C4Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
androgen metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid and bile salt transportAldo-keto reductase family 1 member C4Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C4Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
bile acid secretionUDP-glucuronosyltransferase 1A3Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
G protein-coupled receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
response to nutrientAldo-keto reductase family 1 member C3Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of cell population proliferationAldo-keto reductase family 1 member C3Homo sapiens (human)
male gonad developmentAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to starvationAldo-keto reductase family 1 member C3Homo sapiens (human)
farnesol catabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
cyclooxygenase pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
keratinocyte differentiationAldo-keto reductase family 1 member C3Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinal metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
macromolecule metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of retinoic acid receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
renal absorptionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to calcium ionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to corticosteroid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin D stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
negative regulation of retinoic acid biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of endothelial cell apoptotic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
G protein-coupled receptor signaling pathwayAldo-keto reductase family 1 member C2 Homo sapiens (human)
digestionAldo-keto reductase family 1 member C2 Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
positive regulation of cell population proliferationAldo-keto reductase family 1 member C2 Homo sapiens (human)
epithelial cell differentiationAldo-keto reductase family 1 member C2 Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAldo-keto reductase family 1 member C2 Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C2 Homo sapiens (human)
cellular response to prostaglandin D stimulusAldo-keto reductase family 1 member C2 Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
xenobiotic metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
digestionAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid and bile salt transportAldo-keto reductase family 1 member C1Homo sapiens (human)
intestinal cholesterol absorptionAldo-keto reductase family 1 member C1Homo sapiens (human)
epithelial cell differentiationAldo-keto reductase family 1 member C1Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
retinal metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
cholesterol homeostasisAldo-keto reductase family 1 member C1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
response to organophosphorusAldo-keto reductase family 1 member C1Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C1Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
monoatomic anion transportSolute carrier family 22 member 6Homo sapiens (human)
response to organic cyclic compoundSolute carrier family 22 member 6Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 6Homo sapiens (human)
organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transportSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 6Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 6Homo sapiens (human)
renal tubular secretionSolute carrier family 22 member 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (117)

Processvia Protein(s)Taxonomy
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)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo 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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
serine-type endopeptidase inhibitor activityAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
heparin bindingAmyloid-beta precursor proteinHomo sapiens (human)
enzyme bindingAmyloid-beta precursor proteinHomo sapiens (human)
identical protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
transition metal ion bindingAmyloid-beta precursor proteinHomo sapiens (human)
receptor ligand activityAmyloid-beta precursor proteinHomo sapiens (human)
PTB domain bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein serine/threonine kinase bindingAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor activator activityAmyloid-beta precursor proteinHomo sapiens (human)
long-chain fatty acid transmembrane transporter activityFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
protein bindingFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C4Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid transmembrane transporter activityAldo-keto reductase family 1 member C4Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C4Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
chlordecone reductase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C4Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C3Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin D2 11-ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
geranylgeranyl reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin-F synthase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
15-hydroxyprostaglandin-D dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
Delta4-3-oxosteroid 5beta-reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C3Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C2 Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
carboxylic acid bindingAldo-keto reductase family 1 member C2 Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C2 Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C1Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C1Homo sapiens (human)
carboxylic acid bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
3beta-hydroxy-5beta-steroid dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
steroid dehydrogenase activity, acting on the CH-OH group of donors, NAD or NADP as acceptorAldo-keto reductase family 1 member C1Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
17-alpha,20-alpha-dihydroxypregn-4-en-3-one dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androsterone dehydrogenase (B-specific) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
protein bindingSolute carrier family 22 member 6Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
chloride ion bindingSolute carrier family 22 member 6Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (79)

Processvia Protein(s)Taxonomy
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)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo 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)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
dendriteAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionAmyloid-beta precursor proteinHomo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
nuclear envelope lumenAmyloid-beta precursor proteinHomo sapiens (human)
cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
mitochondrial inner membraneAmyloid-beta precursor proteinHomo sapiens (human)
endosomeAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum lumenAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
Golgi lumenAmyloid-beta precursor proteinHomo sapiens (human)
Golgi-associated vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cytosolAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
clathrin-coated pitAmyloid-beta precursor proteinHomo sapiens (human)
cell-cell junctionAmyloid-beta precursor proteinHomo sapiens (human)
synaptic vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
membraneAmyloid-beta precursor proteinHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleAmyloid-beta precursor proteinHomo sapiens (human)
axonAmyloid-beta precursor proteinHomo sapiens (human)
growth coneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule lumenAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
endosome lumenAmyloid-beta precursor proteinHomo sapiens (human)
trans-Golgi network membraneAmyloid-beta precursor proteinHomo sapiens (human)
ciliary rootletAmyloid-beta precursor proteinHomo sapiens (human)
dendritic spineAmyloid-beta precursor proteinHomo sapiens (human)
dendritic shaftAmyloid-beta precursor proteinHomo sapiens (human)
perikaryonAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
apical part of cellAmyloid-beta precursor proteinHomo sapiens (human)
synapseAmyloid-beta precursor proteinHomo sapiens (human)
perinuclear region of cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
presynaptic active zoneAmyloid-beta precursor proteinHomo sapiens (human)
spindle midzoneAmyloid-beta precursor proteinHomo sapiens (human)
recycling endosomeAmyloid-beta precursor proteinHomo sapiens (human)
extracellular exosomeAmyloid-beta precursor proteinHomo sapiens (human)
receptor complexAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
microvillusFatty acid-binding protein, intestinalHomo sapiens (human)
apical cortexFatty acid-binding protein, intestinalHomo sapiens (human)
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
nucleusFatty acid-binding protein, intestinalHomo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cytoplasmAldo-keto reductase family 1 member C4Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C4Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C4Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C4Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
nucleusAldo-keto reductase family 1 member C3Homo sapiens (human)
cytoplasmAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C2 Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C1Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
caveolaSolute carrier family 22 member 6Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 6Homo sapiens (human)
protein-containing complexSolute carrier family 22 member 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (329)

Assay IDTitleYearJournalArticle
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.
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.
AID1667259Antioxidant activity assessed as AAPH-induced radical scavenging activity by measuring trolox equivalents for oxygen radical absorbance capacity measured every minute for 90 mins by ORAC-FL assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
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).
AID93272Percent inhibition of collagen-induced platelet aggregation at a concentration of 100 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID407369Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID320595Ulcerogenic effect in mouse at 123 umol/kg, po relative to flurbiprophen2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
AID1307689Inhibition of COX in human whole blood assessed as increase in 13-HODE production at 2 uM pre-incubated for 20 mins before stimulation with LPS and A23187 for 120 mins by LC-MS/MS method2016Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
Discovery of Novel 15-Lipoxygenase Activators To Shift the Human Arachidonic Acid Metabolic Network toward Inflammation Resolution.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID592741Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrate production at 10 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess reagent method relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID703400Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID93273Percent inhibition of collagen-induced platelet aggregation at a concentration of 20 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID183692Evaluated for the percentage inhibition by adjuvant arthritis test at a dose of 50 mg/kg administarted perorally1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
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.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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).
AID634118Antineuroinflammatory activity in LPS-stimulated rat microglia cells assessed as inhibition of PMA-stimulated TXB2 release preincubated for 15 mins measured 70 mins after PMA challenge2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Marine sponge Hymeniacidon sp. amphilectane metabolites potently inhibit rat brain microglia thromboxane B2 generation.
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.
AID592754Antiamyloidogenic activity in mouse N2A cells transfected with human APP Swedish mutant assessed as reduction of amyloid beta (1 to 42) level at 100 uM after 24 hrs by ELISA2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID1273102Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID624632Drug glucuronidation reaction catalyzed by human recombinant UGT1A32005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
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).
AID310933Permeability across PAMPA membrane after 7 hrs2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1667274Effect on nitric oxide production in mouse BV2 cells at 0.5 to 10 uM measured after 30 mins by Griess reagent based ELISA2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID574424Displacement of S-phenyl 3-(4-hydroxy-3,5-dimethylstyryl)benzothioate from human TTR assessed as fluorescence at 37 degC after 3 hrs2011Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
A competition assay to identify amyloidogenesis inhibitors by monitoring the fluorescence emitted by the covalent attachment of a stilbene derivative to transthyretin.
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]
AID1822499Antifungal activity against Candida albicans SN152 harbouring erg3delta delta/erg11delta delta assessed as Cyp51-mediated fungal growth inhibition measured every 40 mins for 48 hrs by double dilution method2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Fluconazole-COX Inhibitor Hybrids: A Dual-Acting Class of Antifungal Azoles.
AID1273091Inhibition of COX in human HuH7 cells after 48 hrs by fluorometric assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID162497In vitro inhibitory activity against Prostaglandin G/H synthase 2 (COX-2) in human1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Structure-based design of COX-2 selectivity into flurbiprofen.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1273101Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID320592Antiinflammatory activity against carrageenan-induced hind paw edema in rat at 41 umol/kg, po after 3 hrs relative to flurbiprophen2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
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).
AID1667272Anti-neuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production at 2.5 uM preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess reagent based assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID386885Antibacterial activity against Staphylococcus aureus ATCC 19433 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
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.
AID1053371Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as oxygen consumption at 30 uM measured within 10 to 50 secs2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.
AID1667262Inhibition of recombinant human MAOA expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1221821Cytotoxicity against HEK293 cells expressing UGT1A3 assessed as decrease in cell viability at 1 mM measured at 24 hrs by MTT assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Toxicological evaluation of acyl glucuronides of nonsteroidal anti-inflammatory drugs using human embryonic kidney 293 cells stably expressing human UDP-glucuronosyltransferase and human hepatocytes.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1667276Anti-neuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha production at 2.5 uM preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by ELISA relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1476081Inhibition of rat ASIC3 receptor expressed in xenopus lavies oocytes assessed as inhibition of pH 6.4-gated currents by two electrode voltage clamp2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
AID253569Absolute oral bioavailability after administration to rats at a dose of 7.6 mg/kg orally2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID387119Analgesic activity in Swiss albino mouse assessed as effect on reaction time for tail withdrawal administered at 10 mg/kg, po after 4 hrs by tail immersion method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID320596Inhibition of lipid peroxidation in mouse gastric mucosa tissue assessed as malondialdehyde level per 100 mg tissue relative to flurbiprophen2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
AID407368Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1374201Cytotoxicity against LPS-induced mouse BV2 cells assessed as effect on cell viability at 2.5 to 10 uM pretreated for 30 mins followed by LPS-stimulation after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1667260Inhibition of recombinant human MAOA expressed in baculovirus infected in BTI cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence based assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1054847Inhibition of human recombinant TTR Y78F mutant-mediated fibrillogenesis at 40 uM after 30 mins by turbidimetric assay relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Modulation of the fibrillogenesis inhibition properties of two transthyretin ligands by halogenation.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID255283Concentration required to inhibit A beta 40 peptide; nd is not determined2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID682161TP_TRANSPORTER: inhibition of E217betaG in the presence of Flurbiprofen at a concentration of 50uM in membrane vesicles from MRP4-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID89236In vitro inhibition of collagen-induced platelet aggregation in human platelet rich plasma1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID256360Percent inhibition against beta-amyloid-42 (Abeta42) secretion was evaluated in human neuroglioma cells (H4-APP695NL) at 100 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID703402Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
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.
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
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.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID396392Inhibition of lipid peroxidation in rat assessed as malondialdehyde level per 100 mg of tissue2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.
AID612763Ratio of AUC in plasma to AUC in cerebrospinal fluid in rat2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold.
AID253784Maximum time corresponding to maximum concentration after administration to rats at a dose of 7.6 mg/kg orally2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1273090Inhibition of COX in human Mahlavu cells after 48 hrs by fluorometric assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID1053370Inhibition of human recombinant COX-2 assessed as inhibition of 2-AG cyclooxygenation at 30 uM measured within 10 to 50 secs2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.
AID396389Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema administered orally at equimolar oral dose relative to 10 mg/kg flurbiprofen measured after 4 hrs of carrageenan challenge2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
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).
AID681779TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Flurbiprofen: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, May, Volume: 55, Issue:5
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.
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.
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).
AID540230Dose normalised AUC in rat after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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).
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).
AID745126Inhibition of amyloid beta (1 to 40) formation in Wistar rat primary cortical neurons at 0.5 uM after 24 hrs by ELISA relative to control2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Design, synthesis and evaluation of tacrine-flurbiprofen-nitrate trihybrids as novel anti-Alzheimer's disease agents.
AID377718Lipophilicity, log D at pH 7.42006Journal of natural products, Jul, Volume: 69, Issue:7
Chamazulene carboxylic acid and matricin: a natural profen and its natural prodrug, identified through similarity to synthetic drug substances.
AID1374199Cytotoxicity against mouse BV2 cells assessed as effect on cell viability up to 10 uM after 30 mins by MTT assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1667266Disaggregation of self-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 25 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1060646Antineuroinflammatory activity in rat brain neonatal microglia2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Dactyloditerpenol acetate, a new prenylbisabolane-type diterpene from Aplysia dactylomela with significant in vitro anti-neuroinflammatory activity.
AID396388Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema administered orally at equimolar oral dose relative to 10 mg/kg flurbiprofen measured after 3 hrs of carrageenan challenge2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID624647Inhibition of AZT glucuronidation by human UGT enzymes from liver microsomes2005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID253823Elimination phase half-life after administration to rats at a dose of 7.6 mg/kg orally2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1141095Ulcerogenic activity in albino rat stress model assessed as ulcer index at 10 mg/kg, po after 7 hrs2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID1374194Inhibition of cupric ion-mediated amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin T fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID574422Inhibition of wild type-TTR expressed in Escherichia coli assessed as amyloid fibril formation at pH 4.4 at 7. 2 uM after 72 hrs by acid-mediated aggregation assay relative to control2011Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
A competition assay to identify amyloidogenesis inhibitors by monitoring the fluorescence emitted by the covalent attachment of a stilbene derivative to transthyretin.
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).
AID386899Inhibition of lipid peroxidation in rat assessed as malondialdehyde level per 100 mg of tissue at 30 mg/kg, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID1667265Inhibition of Cu2+-induced HFIP-pretreated amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
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.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID592849Antiamyloidogenic activity in mouse N2A cells assessed as reduction of amyloid beta (1 to 42)/(1 to 40) ratio at 100 uM treated 24 hrs before amyloid beta (1 to 42)/(1 to 40) challenge measured after 8 hrs by MALDI/TOF analysis2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID1625110Inhibition of HFIP-pretreated human amyloid beta (1 to 42) self-induced aggregation at 25 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID162021In vitro inhibitory activity against Prostaglandin G/H synthase 1 in sheep1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Structure-based design of COX-2 selectivity into flurbiprofen.
AID1667264Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-aggregation at 25 uM after 24 hrs by thioflavin-T fluorescence assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID1585853Cytotoxicity against human BV2 cells assessed as decrease in cell viability up to 10 uM measured after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1054848Inhibition of human recombinant TTR Y78F mutant-mediated fibrillogenesis after 30 mins by turbidimetric assay2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Modulation of the fibrillogenesis inhibition properties of two transthyretin ligands by halogenation.
AID1374203Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production at 2.5 uM pretreated for 30 mins followed by LPS-stimulation measured after 24 hrs by Griess assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
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).
AID1175391Inhibition of human TRPV1 overexpressed in BEAS-2B cells assessed as residual activity at 250 uM after 30 mins by Fluo-4 AM fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
AID1273107Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID320593Antiinflammatory activity against carrageenan-induced hind paw edema in rat at 41 umol/kg, po after 4 hrs relative to flurbiprophen2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
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.
AID396390Analgesic activity in Swiss albino mouse assessed as inhibition of tail withdrawal administered orally at equimolar oral dose relative to 10 mg/kg flurbiprofen after 4 hrs2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.
AID377717Dissociation constant, pKa of the compound2006Journal of natural products, Jul, Volume: 69, Issue:7
Chamazulene carboxylic acid and matricin: a natural profen and its natural prodrug, identified through similarity to synthetic drug substances.
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]
AID386886Antibacterial activity against sEscherichia coli ATCC 25922 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID1330181Inhibition of COX-2 (unknown origin)2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis, COX-1/2 inhibition activities and molecular docking study of isothiazolopyridine derivatives.
AID1616921Inhibition of catalytic activity of His6-tagged Lactobacillus johnsonii N6.2 cinnamoyl esterase LJ0536 expressed in Escherichia coli BL21 (DE3) assessed as reduction in hydrolysis of 4-nitrophenyl butyrate in 4-nitrophenol at 400 uM in presence of 2.5 to 2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Exhaustive Repertoire of Druggable Cavities at Protein-Protein Interfaces of Known Three-Dimensional Structure.
AID1625131Inhibition of LPS-induced TNFalpha production in mouse BV2 cells at 2.5 uM pretreated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1667261Inhibition of recombinant human MAOB expressed in baculovirus infected in BTI cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence based assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID243230Binding affinity towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1657546Antiinflammatory activity against LPS-induced rat Primary neonatal microglia assessed as inhibition in TXB2 generation preincubated for 20 mins followed by PMA-stimulation and measured after 70 mins by immunoassay2020Journal of natural products, 05-22, Volume: 83, Issue:5
6-Deoxy- and 11-Hydroxytolypodiols: Meroterpenoids from the Cyanobacterium HT-58-2.
AID1625132Inhibition of LPS-induced TNFalpha production in mouse BV2 cells at 10 uM pretreated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
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.
AID386895Gastrointestinal toxicity in rat assessed as gastric mucosal damage severity index at 30 mg/kg, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1307688Inhibition of COX in human whole blood assessed as increase in 15-HETE production at 2 uM pre-incubated for 20 mins before stimulation with LPS and A23187 for 120 mins by LC-MS/MS method2016Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
Discovery of Novel 15-Lipoxygenase Activators To Shift the Human Arachidonic Acid Metabolic Network toward Inflammation Resolution.
AID1476080Inhibition of rat ASIC2a receptor expressed in xenopus lavies oocytes assessed as inhibition of pH 4-gated currents at 1 mM by two electrode voltage clamp relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
AID253641Area under curve after administration to rats at adose of 1.5 mg/kg intravenously2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
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.
AID1625112Inhibition of Electrophorus electricus AChE at 50 uM using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID253728Maximal concentration in rats after 1.5 mg/kg intravenous dose2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID253844Concentration ratio in cerebrospinal fluid and plasma2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1625113Inhibition of rat serum BuChE at 25 uM using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID320594Analgesic activity in mouse at 41 umol/kg, po by tail immersion method relative to flurbiprophen2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
AID1374207Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM pretreated for 30 mins followed by LPS-stimulation measured after 24 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID692103Inhibition of gamma secretase assessed as reduction in Abeta42 production2011Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs.
AID1374204Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM pretreated for 30 mins followed by LPS-stimulation measured after 24 hrs by Griess assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1273100Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID386887Antimicrobial activity against Candida albicans ATCC 2091 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID93279percent inhibition of serotonin release from platelets at a concentration of 20 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID310931Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID253587Total body clearance after administration to rats at a dose of 1.5 mg/kg intravenously2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
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.
AID1282661Inhibition of ovine COX1 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay2016European journal of medicinal chemistry, Feb-15, Volume: 109Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID592847Antiamyloidogenic activity in mouse N2A cells assessed as degradation of amyloid beta (1 to 42) level at 100 uM treated 24 hrs before amyloid beta (1 to 42) challenge measured after 8 hrs by MALDI/TOF analysis2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID1282662Inhibition of recombinant human COX2 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay2016European journal of medicinal chemistry, Feb-15, Volume: 109Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.
AID1374195Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1585860Anti-inflammatory activity in human BV2 cells assessed as inhibition of LPS-stimulated TNFalpha release at 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1667269Cytotoxicity against mouse BV2 cells assessed as reduction in cell viability at 0.5 to 10 uM measured after 30 mins by MTT assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID253720Maximal concentration in rats after 7.6 mg/kg oral dose2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1175392Inhibition of human TRPV1 overexpressed in BEAS-2B cells assessed as residual activity at 50 uM after 30 mins by Fluo-4 AM fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
AID592744Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1282660Inhibition of FAAH in Sprague-Dawley rat brain homogenates preincubated for 10 mins followed by addition of substrate measured after 30 mins by liquid scintillation counting2016European journal of medicinal chemistry, Feb-15, Volume: 109Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.
AID1476082Inhibition of rat ASIC3 receptor expressed in xenopus lavies oocytes assessed as inhibition of pH 6.4-gated currents at 3 mM by two electrode voltage clamp relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID253786Maximum time corresponding to maximum concentration after administration to rats at a dose of 1.5 mg/kg intravenously2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID346025Binding affinity to beta cyclodextrin2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Convenient QSAR model for predicting the complexation of structurally diverse compounds with beta-cyclodextrins.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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).
AID78137In vitro inhibition of collagen-induced platelet aggregation in guinea pig platelet rich plasma1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1625109Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity at 1 to 10 uM preincubated for 15 mins followed by AAPH addition measured every min for 90 mins by ORAC-FL assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
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
AID1667277Anti-neuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by ELISA relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID574423Displacement of 4-fluorophenyl 3-(4-hydroxy-3,5-dimethylstyryl)benzoate from recombinant TTR assessed as fluorescence at 37 degC after 3 hrs2011Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
A competition assay to identify amyloidogenesis inhibitors by monitoring the fluorescence emitted by the covalent attachment of a stilbene derivative to transthyretin.
AID255950Inhibitory concentration against beta-amyloid-42 (Abeta42) secretion was evaluated in human neuroglioma cells (H4-APP695NL)2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID313126Inhibition of COX12007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1667270Cytotoxicity against LPS-induced mouse BV2 cells assessed as reduction in cell viability at 0.5 to 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by MTT assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID592848Antiamyloidogenic activity in mouse N2A cells assessed as degradation of amyloid beta (1 to 40) level at 100 uM treated 24 hrs before amyloid beta (1 to 40) challenge measured after 8 hrs by MALDI/TOF analysis2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID253826Elimination phase half-life after administration to rats at a dose of 1.5 mg/kg intravenously2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1585856Anti-inflammatory activity in human BV2 cells assessed as inhibition of LPS-stimulated NO release at 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay relative to control2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1211795Dissociation constant, pKa of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID386884Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured 4 hrs after carrageenan challenge2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID681160TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells2000The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1
Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.
AID592746Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 1 uM after 24 hrs by MTT assay relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID592743Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrate production at 100 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess reagent method relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID703401Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID677462Dissociation constant, pKa of the compound2012European journal of medicinal chemistry, Jul, Volume: 53Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach.
AID1625122Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1585855Anti-inflammatory activity in human BV2 cells assessed as inhibition of LPS-stimulated NO release at 2.5 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay relative to control2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID540233Dose normalised AUC in human after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID1273105Cytotoxicity against human SNU475 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID1667273Anti-neuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production at 10 uM preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess reagent based assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1585859Anti-inflammatory activity in human BV2 cells assessed as inhibition of LPS-stimulated TNFalpha release at 2.5 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID162164Binding affinity of compound towards prostaglandin G/H synthase 1 was evaluated2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
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.
AID1625128Inhibition of LPS-induced nitric oxide production in mouse BV2 cells at 2.5 uM pretreated for 30 mins followed by LPS-stimulation and measured after 24 hrs by Griess assay relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1374196Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID540232Dose normalised AUC in monkey after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1625111Inhibition of Cu2+-induced human amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin T-based fluorometric assay relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID1616920Inhibition of catalytic activity of His6-tagged Lactobacillus johnsonii N6.2 cinnamoyl esterase LJ0536 expressed in Escherichia coli BL21 (DE3) assessed as reduction in hydrolysis of 4-nitrophenyl butyrate in 4-nitrophenol pre-incubated for 2 hrs2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Exhaustive Repertoire of Druggable Cavities at Protein-Protein Interfaces of Known Three-Dimensional Structure.
AID256322Compound was tested for interaction with baculovirus-insect cells expressing human cytochrome P450; No interactions at 100 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID253638Area under curve after administration to rats at a dose of 7.6 mg/kg orally2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1374192Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity at 1 to 10 uM pretreated for 15 mins followed by APPH addition measured at 1 min interval for 90 mins by ORAC-FL assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1273106Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID467611Dissociation constant, pKa of the compound2009European 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.
AID253744Intestinal drug absorption was estimated in vitro using human colon adenocarcinoma (Caco-2) cell monolayers2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1374200Cytotoxicity against mouse BV2 cells assessed as reduction in cell viability at 40 uM after 30 mins by MTT assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID396391Gastrointestinal toxicity in rat assessed as gastric mucosal damage severity index administered at equimolar oral dose relative to 30 mg/kg flurbiprofen2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.
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]
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID592745Antiamyloidogenic activity in mouse N2A cells transfected with human APP Swedish mutant assessed as reduction of amyloid beta (1 to 42) level at 1 uM after 24 hrs by ELISA relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
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).
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID235171Selectivity ratio of COX-1 to that of COX-21999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Structure-based design of COX-2 selectivity into flurbiprofen.
AID253891In vivo steady state metabolic clearance of the compound2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
AID1667263Inhibition of recombinant human MAOB expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1330180Inhibition of COX-1 (unknown origin)2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Synthesis, COX-1/2 inhibition activities and molecular docking study of isothiazolopyridine derivatives.
AID93278percent inhibition of serotonin release from platelets at a concentration of 100 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID1273103Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID1273104Cytotoxicity against human FOCUS cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Novel triazolothiadiazines act as potent anticancer agents in liver cancer cells through Akt and ASK-1 proteins.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID592742Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID703399Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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).
AID1374206Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha production at 2.5 uM pretreated for 30 mins followed by LPS-stimulation measured after 24 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1374193Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence method relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID592755Antiamyloidogenic activity in mouse N2A cells transfected with human APP Swedish mutant assessed as increase of amyloid beta (1 to 37) level at 100 uM after 24 hrs by ELISA2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.
AID462317Inhibition of ovine COX12010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
AID313125Inhibition of COX22007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
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.
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).
AID1476078Inhibition of rat ASIC1a receptor expressed in xenopus lavies oocytes assessed as inhibition of pH 6.7-gated currents by two electrode voltage clamp2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
AID1585852Cytotoxicity against human BV2 cells assessed as decrease in cell viability up to 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1616922Non-competive inhibition of catalytic activity of His6-tagged Lactobacillus johnsonii N6.2 cinnamoyl esterase LJ0536 expressed in Escherichia coli BL21 (DE3) assessed as substrate Vmax by measuring hydrolysis of 4-nitrophenyl butyrate in 4-nitrophenol at 2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Exhaustive Repertoire of Druggable Cavities at Protein-Protein Interfaces of Known Three-Dimensional Structure.
AID162166Kinetic constant of compound towards inhibition of prostaglandin G/H synthase 12004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID407366Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID462318Inhibition of mouse COX22010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
AID1476079Inhibition of rat ASIC1a receptor expressed in xenopus lavies oocytes assessed as inhibition of pH 6.7-gated currents at 3 mM by two electrode voltage clamp relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
AID1625129Inhibition of LPS-induced nitric oxide production in mouse BV2 cells at 10 uM pretreated for 30 mins followed by LPS-stimulation and measured after 24 hrs by Griess assay relative to control2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
AID254854Concentration required to inhibit cyclooxygenase-1 in rat blood2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
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]
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).
AID540231Dose normalised AUC in dog after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID162150Reversible competitive inhibition of prostaglandin G/H synthase 12004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
AID239780Percentage plasma protein binding towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID504797Fluorescence polarization-based biochemical high throughput confirmation assay for activators of the Protein Kinase A-R2B (PKA-R2B) complex2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
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.
AID504796Counterscreen for activators of the Protein Kinase A-R2B (PKA-R2B) complex: fluorescence polarization-based biochemical high throughput screening assay to identify fluorescence polarization assay artifacts2006Analytical chemistry, Dec-15, Volume: 78, Issue:24
Assay principle for modulators of protein-protein interactions and its application to non-ATP-competitive ligands targeting protein kinase A.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1801103Fluorophore Displacement Assay from Article 10.1021/cb5005178: \\Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein.\\2014ACS chemical biology, Nov-21, Volume: 9, Issue:11
Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein.
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.
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.
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.
AID1346898Rat ASIC1 (Acid-sensing (proton-gated) ion channels (ASICs))2001The Journal of neuroscience : the official journal of the Society for Neuroscience, Oct-15, Volume: 21, Issue:20
Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors.
AID1345206Human COX-2 (Cyclooxygenase)1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Structure-based design of COX-2 selectivity into flurbiprofen.
AID1345284Human COX-1 (Cyclooxygenase)1999Proceedings of the National Academy of Sciences of the United States of America, Jun-22, Volume: 96, Issue:13
Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,981)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990497 (25.09)18.7374
1990's408 (20.60)18.2507
2000's441 (22.26)29.6817
2010's510 (25.74)24.3611
2020's125 (6.31)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 76.72

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 Index76.72 (24.57)
Research Supply Index7.84 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index147.18 (26.88)
Search Engine Supply Index2.12 (0.95)

This Compound (76.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials466 (22.49%)5.53%
Reviews71 (3.43%)6.00%
Case Studies64 (3.09%)4.05%
Observational1 (0.05%)0.25%
Other1,470 (70.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (65)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT02391688]Phase 130 participants (Actual)Interventional2014-11-30Completed
The Effects of Remimazolam Tosilate Sedation Compared With Midazolam Sedation in Dental Patients: A Double Blind, Prospective , Randomized Controlled Trial [NCT04602845]Phase 481 participants (Actual)Interventional2021-04-01Completed
Evaluation of the Effects of Different Analgesics on Pain and Health-related Quality of Life of Patients With Pericoronitis in the Short-term Period: A Randomized, Double-blind, Clinical Trial [NCT03745599]Phase 460 participants (Actual)Interventional2017-11-01Completed
Effect of Preemptive Analgesia With Flurbiprofen Axetil on Perioperative Sleep Quality and Postoperative Pain in Patients Undergoing Sevoflurane Inhalation. [NCT04611763]Phase 1100 participants (Anticipated)Interventional2021-09-01Recruiting
Effect of Over-the-counter Non-steroidal Anti-inflammatory Treatments on Cough Reflex Sensitivity in Subjects With Upper Respiratory Tract Infection [NCT05955885]Early Phase 1120 participants (Anticipated)Interventional2023-07-01Recruiting
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 BMS-986020 on the Pharmacokinetics of Montelukast, Flurbiprofen, and Digoxin as Probe Substrates for CYP2C8, CYP2C9, and P-gp [NCT02227173]Phase 120 participants (Actual)Interventional2014-09-30Completed
Impact of Perioperative Dexamethasone and Flurbiprofen Axetil on Delirium After Surgery for Non-small Cell Lung Cancer: A 2x2 Factorial Randomized Controlled Trial [NCT03200600]Phase 4126 participants (Actual)Interventional2017-08-02Terminated(stopped due to Protocol violation occurred frequently during the postoperative period.)
Cocktail Phenotypic Approach to Explore Antidepressant Pharmacokinetic Variability: a Pilot Study [NCT02438072]100 participants (Anticipated)Interventional2014-12-31Recruiting
Impact of Perioperative Dexamethasone and Flurbiprofen Axetil on Long-term Survival After Surgery for Non-small Cell Lung Cancer: A 2x2 Factorial Randomized Controlled Trial [NCT03172988]Phase 4126 participants (Actual)Interventional2017-08-02Terminated(stopped due to Protocol violation occurred frequently during the postoperative period.)
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
Efficiency of Flurbiprofen 2.5% in Comparison to 98% Aloe Vera Gel as an Adjunctive Therapy to Scaling and Root Planning in the Initial Treatment of Stage III Chronic Periodontitis in Smoking Patients [NCT06041178]Phase 460 participants (Actual)Interventional2022-09-30Completed
Bioavailability, Pharmacokinetics and Tissue Distribution of R-flurbiprofen Capsules in Healthy Subjects [NCT02206854]Phase 116 participants (Actual)Interventional2014-06-30Completed
Flurbiprofen Axetil and Nalbuphine for Postoperative Pain and Discomfort After Orbital Decompression [NCT03562611]63 participants (Actual)Interventional2018-06-08Completed
The Effects of Non-steroidal Anti-inflammatory Drugs on Circulating Markers of Bone Metabolism Following Plyometric Exercise in Humans [NCT05512013]Phase 112 participants (Actual)Interventional2022-02-15Completed
Comparison of Two Kinds of Postoperative Analgesia After Amputation:a Randomized Clinical Trial [NCT02114463]Phase 436 participants (Anticipated)Interventional2014-03-31Recruiting
Effectiveness, Safety and Economic Evaluation of Chinese Tuina (Chinese Massage and Flurbiprofen Cataplasms) in the Treatment of Chronic Nonspecific Low Back Pain [NCT04976790]90 participants (Anticipated)Interventional2021-10-28Recruiting
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
[NCT02674737]80 participants (Anticipated)Interventional2016-01-31Recruiting
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
The Safety and Efficacy of 5% Lidocaine Patch and Flurbiprofen Patch for Relieving Acute Low Back Pain [NCT03171987]Phase 4120 participants (Anticipated)Interventional2017-06-14Recruiting
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
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
A Single Center, Single Sequence, Open-Label, Repeat-Dose Study to Investigate the Effect of GSK376501 on Hepatic Cytochrome P450 Activity in Healthy Adult Subjects [NCT00615212]Phase 123 participants (Actual)Interventional2008-01-02Completed
[NCT02670954]154 participants (Actual)Interventional2015-10-31Completed
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
Evaluation of the CYP2C9 Activity With Dried Blood Spots on Filter Paper Obtained With a Simple Finger Prick [NCT01026714]Phase 1/Phase 210 participants (Anticipated)Interventional2009-11-30Completed
Analgesia Effects of Nalbuphine vs Sulfentanil in Patient-controlled Intravenous Analgesia After Cesarean Section [NCT02604797]80 participants (Anticipated)Interventional2016-01-31Not yet recruiting
A Phase I Study to Evaluate the Effect of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 Pharmacokinetics and to Assess the Effect of GSK2248761 on CYP450 Probe Drugs in Healthy Adult Subjects [NCT00920088]Phase 124 participants (Actual)Interventional2009-06-30Completed
Tumor Hospital of Guangxi Medical University, China [NCT02569905]Phase 4166 participants (Actual)Interventional2014-04-30Completed
The Effect of Sex Difference in Preemptive Analgesic Effects With Flurbiprofen Axetil on Postoperative Pain and Sleep Quality of Patients Under General Anesthesia [NCT04627779]100 participants (Anticipated)Interventional2021-01-01Not yet recruiting
Benefits of Enhanced Recovery After Surgery in Patients Undergoing Endoscopic Sinus Surgery [NCT04048070]55 participants (Actual)Interventional2018-05-03Completed
Comparative, Randomized, Two-period, Two-treatment, Two-sequence, Single Dose, Open-label, Crossover Bioequivalence Study of FLURBIPROFEN 100 mg FAMOTIDINE 20 mg MULTI-LAYER TABLET (One Tablet) of (Sanovel İlaç San. ve Tic. A.Ş., İstanbul / Türkiye) Versu [NCT01910090]Phase 136 participants (Actual)Interventional2012-12-31Completed
The Efficacy and Safety of PerioChip Plus (Flurbiprofen/Chlorhexidine) Formulation in the Therapy of Adult Periodontitis [NCT00425451]Phase 280 participants (Actual)Interventional2008-08-31Completed
The Efficacy and Safety of Flurbiprofen Chip Versus Chlorhexidine Chip (Periochip®) in Therapy of Adult Chronic Periodontitis [NCT01040286]Phase 20 participants Interventional2009-08-31Completed
Effects of Genotype on CYP2C9 Drug Interactions [NCT01061112]23 participants (Actual)Observational2009-12-31Completed
[NCT01998217]Phase 460 participants (Actual)Interventional2012-09-30Completed
Phase IV Study of Flurbiprofen Axetil for Uterine Contraction Pain After Abortion [NCT00725218]Phase 497 participants (Actual)Interventional2008-05-31Completed
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 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
Pain Treatment in Posterior Thoracolumbar Operation a Randomized Study to Assess the Effect of Local Analgesia After Operation [NCT01872494]Phase 471 participants (Actual)Interventional2013-05-31Completed
Bioequivalence Study of Flurbiprofen 8.75 mg Lozenge vs. the Reference Product Strepfen 8.75 mg Lozenge in Healthy Volunteers [NCT04670601]Phase 124 participants (Actual)Interventional2018-06-19Completed
A Randomized, Double-Blind, Placebo-Controlled Multiple-Dose Study to Determine the Efficacy, Onset, and Duration of Action of Flurbiprofen 8.75 mg Lozenge Compared to Its Vehicle Control Lozenge in Patients With Painful Pharyngitis [NCT01049334]Phase 3204 participants (Actual)Interventional2009-11-30Completed
A Repeat-Dose, Multi-Centre, Randomized, Double-Blind, Placebo-Controlled, Study to Determine the Safety and Efficacy of Flurbiprofen 8.75 mg Lozenge Compared to Its Vehicle Control Lozenge in Patients With Painful Pharyngitis [NCT01048866]Phase 3198 participants (Actual)Interventional2009-11-30Completed
The Comparison of the Analgesic Effects of Dezocine and Sufentanil in Patient-controlled Analgesia After Laryngectomy [NCT06000137]129 participants (Actual)Interventional2022-02-10Completed
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
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Trial of Flurbiprofen Tape for Treatment of Chronic Low Back Pain [NCT00759330]Phase 2127 participants (Actual)Interventional2007-10-31Completed
Phase 3 Multinational, Randomized, Double Blind, Placebo Controlled Study of the Effect of Daily Treatment With MPC-7869 on Measures of Cognition, Activities of Daily Living and Global Function in Subjects With Mild Dementia of the Alzheimer's Type [NCT00322036]Phase 3800 participants (Actual)Interventional2006-05-31Terminated(stopped due to Myriad has discontinued the development of Flurizan.)
Phase 3, Multicenter, Randomized, Double Blind, Placebo Controlled Study of the Effect of Daily Treatment With MPC-7869 on Measures of Cognition, Activities of Daily Living and Global Function in Subjects With Mild Dementia of the Alzheimer's Type [NCT00105547]Phase 31,600 participants (Actual)Interventional2005-02-28Completed
Evaluation of the Analgesic Effects of Locally Applied Flurbiprofen and Bupivacaine in the Oral Surgery Model [NCT00001724]Phase 2100 participants Interventional1997-11-30Completed
Subglottic Instillation of Flurbiprofen to Prevent Laryngeal Inflammation Resulting From Endotracheal Intubation: Prospective Pilot Study, Randomized, Double Blind, Placebo Controlled. [NCT04708964]Phase 270 participants (Anticipated)Interventional2021-01-31Not yet recruiting
[NCT01731067]Phase 110 participants (Anticipated)Interventional2012-11-30Completed
Comparison of Efficacy and Safety of Different Analgesic Modes in Minimally Invasive Esophagectomy for Esophageal Cancer [NCT05504265]Phase 2/Phase 3102 participants (Anticipated)Interventional2022-08-10Not yet recruiting
Effects of BMS-986142 on the Single-dose Pharmacokinetics of Methotrexate and Probe Substrates Montelukast (CYP2C8), Flurbiprofen (CYP2C9), Midazolam (CYP3A4), Digoxin (P-gp), and Pravastatin (OATP1B1) in Healthy Subjects [NCT02456844]Phase 124 participants (Actual)Interventional2015-05-31Completed
Effect of Dexmedetomidine Combined With Dezocine and Flubiprofen for Postoperative Intravenous Patient Controlled Analgesia After Colorectal Surgery [NCT03014713]Phase 450 participants (Anticipated)Interventional2016-09-30Recruiting
Effect of Butorphanol Combined With Flurbiprofen Axetil on Preventing Postoperative Hyperalgesia Induced by Remifentanil in Patients Undergoing Lower Abdomimal Surgery [NCT02043366]180 participants (Actual)Interventional2014-02-28Completed
A Single-Dose, Randomized, Double-Blind, Placebo-Controlled Onset-of-Action Study Utilizing the Double-Stopwatch Method [NCT01986361]Phase 3122 participants (Actual)Interventional2013-09-30Completed
Efficacy of Dezocine for the Prevention of Catheter-related Bladder Discomfort [NCT03147066]Phase 496 participants (Actual)Interventional2017-09-01Completed
The Use of Non-Steroidal Anti-Inflammatory Drugs as a Tool of Positive Change in Peri-Implants Mucositis Microbiome [NCT03090009]Early Phase 1100 participants (Anticipated)Interventional2017-04-30Not yet recruiting
Oral Flurbiprofen Spray for Mucosal Graft Harvesting at the Palatal Area: A Randomized Placebo-controlled Study [NCT03165929]Early Phase 148 participants (Actual)Interventional2016-05-31Completed
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
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
The Effect of Doctor-nurse-patient Cooperative Analgesic Linkage Program on Movement Evoked Pain After Laparotomy for Patients With Hepatobiliary and Pancreatic Disease [NCT03823846]80 participants (Anticipated)Interventional2017-11-01Recruiting
The Application of Transversus Abdominis Plane Block Plus Rectus Sheath Block in Peritoneal Dialysis Catheter Placement and Analgesia Based on Transversus Abdominis Plane Block Combined With κ Receptor Agonist and NSAID(Non-steroidal Anti-inflammatory Dru [NCT02984865]190 participants (Anticipated)Interventional2016-12-20Recruiting
Flurbiprofen Axetil and Nalbuphine for Postoperative Pain and Discomfort After Oculoplastic Surgery [NCT03422887]330 participants (Actual)Interventional2018-01-18Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00759330 (10) [back to overview]Acetaminophen Used During the Tape Treatment Phase
NCT00759330 (10) [back to overview]Acetaminophen Used During the Tape Treatment Phase
NCT00759330 (10) [back to overview]Change From Baseline in Total Tender Point Examination Score
NCT00759330 (10) [back to overview]Percent Change From Baseline in Total Functional Rating Index (FRI)
NCT00759330 (10) [back to overview]Percentage of Patients Who Discontinued
NCT00759330 (10) [back to overview]Average Daily Categorical Pain Scale Scores
NCT00759330 (10) [back to overview]Cumulative Summed Pain Intensity Difference (SPID+)
NCT00759330 (10) [back to overview]Pain Intensity Difference (PID+)
NCT00759330 (10) [back to overview]Patient Assessment of Wearability of Therapy
NCT00759330 (10) [back to overview]Patient Global Impression of Change (PGIC)
NCT01048866 (19) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 24 Hours Post-baseline (STPIS SPID24)
NCT01048866 (19) [back to overview]Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 24 Hours From Baseline
NCT01048866 (19) [back to overview]Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at 24 Hours After Initial Dose
NCT01048866 (19) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale Over 24 Hours Post-baseline (STPIS SPID24) For Participants With Baseline Practitioner's Assessment of Pharyngeal Inflammation (PAIN) of Moderate or Severe
NCT01048866 (19) [back to overview]Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 2 Hours From Baseline
NCT01048866 (19) [back to overview]Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 24 Hours From Baseline
NCT01048866 (19) [back to overview]Change From Baseline in Body Temperature at 2 Hours Post Initial Dose
NCT01048866 (19) [back to overview]Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 2 Hours From Baseline
NCT01048866 (19) [back to overview]Change From Baseline in Body Temperature at End of Study
NCT01048866 (19) [back to overview]Post 24 Hour, Multiple Dose Results: Weighted Sum of Differences Over 2 Hours for Difficulty Swallowing Scale (DSS2)
NCT01048866 (19) [back to overview]Post 24 Hour, Multiple Dose Results: Weighted Sum of Differences Over 2 Hours for Swollen Throat Scale (SwoTS2)
NCT01048866 (19) [back to overview]Post 24 Hour, Multiple Dose Results: Weighted Sum of Pain Intensity Differences (SPID) Over 2 Hours for the Sore Throat Pain Intensity Scale (STPIS SPID2)
NCT01048866 (19) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 2 Hours Post-baseline (STPIS SPID2)
NCT01048866 (19) [back to overview]Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at End of Study (Day 7)
NCT01048866 (19) [back to overview]Participant Satisfaction Score 24 Hours After Initial Dose
NCT01048866 (19) [back to overview]Percentage of Participants Who Took Rescue Pain Medication
NCT01048866 (19) [back to overview]Post 24 Hour, Multiple Dose Results: Sore Throat Relief As Reported by Participants 2 Hours After Dosing
NCT01048866 (19) [back to overview]Sore Throat Relief As Reported by Participants 2 Hours After Initial Dose
NCT01048866 (19) [back to overview]Time to First Rescue Pain Medication
NCT01049334 (16) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale Over 24 Hours Post-baseline (STPIS SPID24) For Participants With Baseline Practitioner's Assessment of Pharyngeal Inflammation (PAIN) of Moderate or Severe
NCT01049334 (16) [back to overview]Change From Baseline at 24 Hours in the Tonsillo-Pharyngitis Assessment (TPA) Scores in Participants With Baseline TPA Scores >=8
NCT01049334 (16) [back to overview]Kaplan-Meier Estimates for Sore Throat Pain Intensity Scale (STPIS) Time to Definite Improvement
NCT01049334 (16) [back to overview]Kaplan-Meier Estimates for Sore Throat Pain Intensity Scale (STPIS) Time to Definite Improvement Duration of Relief Using Participant-Defined Definite Improvement Levels (DIL)
NCT01049334 (16) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 2 Hours Post-baseline (STPIS SPID2)
NCT01049334 (16) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 24 Hours Post-baseline (STPIS SPID24)
NCT01049334 (16) [back to overview]Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 2 Hours From Baseline
NCT01049334 (16) [back to overview]Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 24 Hours From Baseline
NCT01049334 (16) [back to overview]Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 2 Hours From Baseline
NCT01049334 (16) [back to overview]Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 24 Hours From Baseline
NCT01049334 (16) [back to overview]Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at 24 Hours After Initial Dose
NCT01049334 (16) [back to overview]Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at the End of the Study (Day 7)
NCT01049334 (16) [back to overview]Practitioner's Assessment of Pharyngeal Inflammation (P.A.I.N.) Scores at 24 Hours After Initial Dose
NCT01049334 (16) [back to overview]Sore Throat Relief Rating Scale (STRRS) At 2 Hours After Initial Dose
NCT01049334 (16) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) at Each Post-Dose Time Point Until the Time Point at Which Comparison of the Arms Yielded a P-value <=0.05
NCT01049334 (16) [back to overview]Participant Satisfaction Scores 24 Hours After Initial Dose
NCT01986361 (9) [back to overview]Change From Baseline at Individual Timepoints in Sore Throat Scale (STS)
NCT01986361 (9) [back to overview]Kaplan-Meier Estimates for Time of First Indication of Sore Throat Relief as Measured By Any Reduction in the Sore Throat Scale (STS)
NCT01986361 (9) [back to overview]Kaplan-Meier Estimates for Time of First Perceived Pain Reduction on the Sore Throat Scale (STS) Which is Followed by ≥ 20% Pain Reduction on the Sore Throat Pain Intensity Scale (STPIS)
NCT01986361 (9) [back to overview]Kaplan-Meier Estimates for Time of First Perceived Pain Relief
NCT01986361 (9) [back to overview]Kaplan-Meier Estimates for Time to First Perceived Pain Relief That Is Confirmed By Meaningful Pain Relief
NCT01986361 (9) [back to overview]Kaplan-Meier Estimates for Time to Meaningful Pain Relief
NCT01986361 (9) [back to overview]Percentage of Participants With Meaningful Pain Relief
NCT01986361 (9) [back to overview]Percentage of Participants With Perceived Pain Relief
NCT01986361 (9) [back to overview]Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Scale (STS) Over the 3 Hours Post-baseline (STS SPID3)
NCT02043366 (2) [back to overview]Mechanical Hyperalgesia Threshold on the Dominant Inner Forearm
NCT02043366 (2) [back to overview]Normalized Area of Hyperalgesia Around the Incision
NCT04425902 (171) [back to overview]Time to Cmax (Tmax) for Caffeine
NCT04425902 (171) [back to overview]Tmax for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]Tmax for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]Tmax for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]Tmax for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]Tmax for Digoxin
NCT04425902 (171) [back to overview]Tmax for Flurbiprofen
NCT04425902 (171) [back to overview]Tmax for Metoprolol
NCT04425902 (171) [back to overview]Tmax for Midazolam
NCT04425902 (171) [back to overview]Tmax for Montelukast
NCT04425902 (171) [back to overview]Tmax for Omeprazole
NCT04425902 (171) [back to overview]Tmax for Pravastatin
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Erythrocytes
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 Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Hematocrit
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Hemoglobin
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Oral Temperature
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Pulse Rate
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in Respiratory Rate
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Erythrocytes
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 Mean Corpuscular Volume
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Hematocrit
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Hemoglobin
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Oral Temperature
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Pulse Rate
NCT04425902 (171) [back to overview]Treatment B: Change From Baseline in Respiratory Rate
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 C: AUC(0-t) for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: Cmax 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: t1/2 for GSK3640254
NCT04425902 (171) [back to overview]Treatment C: Tmax for GSK3640254
NCT04425902 (171) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
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]Treatment A: Absolute Values of Albumin, Globulin, Protein
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Amylase, Lipase
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 Erythrocytes
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 Mean Corpuscular Volume
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 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
NCT04425902 (171) [back to overview]Treatment A: Absolute Values of Respiratory Rate
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]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]Cmax for Alpha-hydroxymetoprolol
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 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 Albumin, Globulin, Protein
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 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]Apparent Terminal Phase Half-life (t1/2) 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]AUC From Time Zero Extrapolated to Infinity (AUC[0-infinity]) for Caffeine
NCT04425902 (171) [back to overview]AUC(0-infinity) for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]AUC(0-infinity) for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]AUC(0-infinity) for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]AUC(0-infinity) for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]AUC(0-infinity) for Digoxin
NCT04425902 (171) [back to overview]AUC(0-infinity) for Flurbiprofen
NCT04425902 (171) [back to overview]AUC(0-infinity) for Metoprolol
NCT04425902 (171) [back to overview]AUC(0-infinity) for Midazolam
NCT04425902 (171) [back to overview]AUC(0-infinity) for Montelukast
NCT04425902 (171) [back to overview]AUC(0-infinity) for Omeprazole
NCT04425902 (171) [back to overview]AUC(0-infinity) for Pravastatin
NCT04425902 (171) [back to overview]AUC(0-t) for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]AUC(0-t) for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]AUC(0-t) for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]AUC(0-t) for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]AUC(0-t) for Digoxin
NCT04425902 (171) [back to overview]AUC(0-t) for Flurbiprofen
NCT04425902 (171) [back to overview]AUC(0-t) for Metoprolol
NCT04425902 (171) [back to overview]AUC(0-t) for Midazolam
NCT04425902 (171) [back to overview]AUC(0-t) for Montelukast
NCT04425902 (171) [back to overview]AUC(0-t) for Omeprazole
NCT04425902 (171) [back to overview]AUC(0-t) for Pravastatin
NCT04425902 (171) [back to overview]Cmax for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]Cmax for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]Cmax for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]Treatment A: Change From Baseline in SBP and DBP
NCT04425902 (171) [back to overview]Cmax for Digoxin
NCT04425902 (171) [back to overview]Cmax for Flurbiprofen
NCT04425902 (171) [back to overview]Cmax for Metoprolol
NCT04425902 (171) [back to overview]Cmax for Midazolam
NCT04425902 (171) [back to overview]Cmax for Montelukast
NCT04425902 (171) [back to overview]Cmax for Omeprazole
NCT04425902 (171) [back to overview]Cmax for Pravastatin
NCT04425902 (171) [back to overview]Maximum Observed Plasma Concentration (Cmax) for Caffeine
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of 1-hydroxymidazolam to Midazolam
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 5-hydroxyomeprazole to Omeprazole
NCT04425902 (171) [back to overview]Ratio of AUC(0-infinity) of Alpha-hydroxymetoprolol to Metoprolol
NCT04425902 (171) [back to overview]Ratio of Cmax of 1-hydroxymidazolam to Midazolam
NCT04425902 (171) [back to overview]Ratio of Cmax of 36-hydroxymontelukast to Montelukast
NCT04425902 (171) [back to overview]Ratio of Cmax of 5-hydroxyomeprazole to Omeprazole
NCT04425902 (171) [back to overview]Ratio of Cmax of Alpha-hydroxymetoprolol to Metoprolol
NCT04425902 (171) [back to overview]t1/2 for 1-hydroxymidazolam
NCT04425902 (171) [back to overview]t1/2 for 36-hydroxymontelukast
NCT04425902 (171) [back to overview]t1/2 for 5-hydroxyomeprazole
NCT04425902 (171) [back to overview]t1/2 for Alpha-hydroxymetoprolol
NCT04425902 (171) [back to overview]t1/2 for Digoxin
NCT04425902 (171) [back to overview]t1/2 for Flurbiprofen
NCT04425902 (171) [back to overview]t1/2 for Metoprolol
NCT04425902 (171) [back to overview]t1/2 for Midazolam
NCT04425902 (171) [back to overview]t1/2 for Montelukast
NCT04425902 (171) [back to overview]t1/2 for Omeprazole
NCT04425902 (171) [back to overview]t1/2 for Pravastatin
NCT04425902 (171) [back to overview]Treatment C: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin

Acetaminophen Used During the Tape Treatment Phase

The percentage of patients who used rescue medication during the tape treatment phase. (NCT00759330)
Timeframe: Day 1 through Day 7 of the tape treatment phase

Interventionpercentage of patients (Number)
Placebo Tape, Daily for 12 Hours50
Flurbiprofen Tape, Daily for 12 Hours54.8
Placebo Tape, Daily for 24 Hours36.4
Flurbiprofen Tape, Daily for 24 Hours62.8

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Acetaminophen Used During the Tape Treatment Phase

The total amount (mg) of rescue medication used during the tape treatment phase. (NCT00759330)
Timeframe: Day 1 through Day 7 of the tape treatment phase

Interventionmg (Least Squares Mean)
Placebo Tape, Daily for 12 Hours2226.9
Flurbiprofen Tape, Daily for 12 Hours1617.5
Placebo Tape, Daily for 24 Hours1585.4
Flurbiprofen Tape, Daily for 24 Hours2141.3

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Change From Baseline in Total Tender Point Examination Score

"At baseline and Day 7 of the tape treatment phase, patients had an assessment of tenderness bilaterally at the sacroiliac joint, greater trochanter of the hip, gluteus medius and minimus, and paraspinal muscles at L3-L4, L4-L5, and L5-S1. The investigator or research nurse pressed 12 specific areas of the body (6 locations, left and right sides), and patients were asked to rate the intensity of their pain at those 12 areas using an 11-point scale, where:~0 = no pain, 10 = the worst pain the patient has ever experienced. The total tender point examination score ranged from 0 (best outcome) to 120 (worst outcome). Change from baseline = baseline - Day 7. A positive change indicates a favorable treatment effect." (NCT00759330)
Timeframe: Baseline to Day 7 of tape treatment phase

Interventionunits on a scale (Least Squares Mean)
Placebo Tape, Daily for 12 Hours13.9
Flurbiprofen Tape, Daily for 12 Hours11.7
Placebo Tape, Daily for 24 Hours19.2
Flurbiprofen Tape, Daily for 24 Hours9.2

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Percent Change From Baseline in Total Functional Rating Index (FRI)

"Patients completed the FRI, a 10-item back pain-specific measure of function questionnaire describing the condition at the time the questionnaire was completed; each item (pain intensity, sleeping, personal care, travel, etc.) was rated on a 5-point scale, where 0 = best outcome, 4 = worst outcome.~FRI was reported as the percent change from baseline at Day 7 of the tape treatment phase, where:~Total FRI score = sum of the 10 questions. The total FRI score ranged from 0 (best outcome) to 40 (worst outcome). Percent change = ([baseline - Day 7]/baseline)*100.~A positive percent change indicates a favorable treatment effect." (NCT00759330)
Timeframe: baseline to Day 7 of tape treatment phase

Interventionpercent change from baseline (Least Squares Mean)
Placebo Tape, Daily for 12 Hours20.6
Flurbiprofen Tape, Daily for 12 Hours29.0
Placebo Tape, Daily for 24 Hours28.2
Flurbiprofen Tape, Daily for 24 Hours25.4

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Percentage of Patients Who Discontinued

The percentage of patients who discontinued the study during the tape treatment phase due to lack of efficacy. (NCT00759330)
Timeframe: Days 1 through Day 7 of tape treatment phase

Interventionpercentage of patients who discontinued (Number)
Placebo Tape, Daily for 12 Hours0
Flurbiprofen Tape, Daily for 12 Hours2.4
Placebo Tape, Daily for 24 Hours0
Flurbiprofen Tape, Daily for 24 Hours2.3

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Average Daily Categorical Pain Scale Scores

"Patients rated their lower back pain, caused by normal activity and movement, on an 11-point categorical pain scale, where:~0 = no pain, and 10 = worst pain imaginable. Patients rated their lower back pain every 12 hours, at any time they took medication including rescue medication for any type of pain, and if they applied or removed their treatment tapes at a time other than the scheduled time.~Data are reported as the daily average categorical pain scale score by treatment group." (NCT00759330)
Timeframe: Days 1 through 7 of tape treatment phase

,,,
Interventionunits on a scale (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Flurbiprofen Tape, Daily for 12 Hours4.84.74.54.04.44.23.8
Flurbiprofen Tape, Daily for 24 Hours5.74.94.85.04.84.84.4
Placebo Tape, Daily for 12 Hours5.34.75.05.05.14.94.6
Placebo Tape, Daily for 24 Hours5.34.54.34.54.24.24.1

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Cumulative Summed Pain Intensity Difference (SPID+)

"The primary efficacy endpoint was the cumulative summed pain intensity difference (SPID+) at Days 4 and 7 of the tape treatment phase as computed from the daily categorical pain scale score reported on the patient's daily diary during the tape treatment phase; pain was rated on an 11-point scale, where: 0 = no pain, 10 = worst pain imaginable.~Summed pain intensity difference is the sum of the pain intensity differences (PID). PID at each post-baseline evaluation was computed as the average baseline categorical pain scale score minus the post-baseline categorical pain scale score from the daily dairy. For patients with multiple pain scores reported on a given post-baseline study day, the PID scores were averaged to compute one daily PID score for each patient." (NCT00759330)
Timeframe: Days 4 and 7 of tape treatment phase

,,,
Interventionunits on a scale (Least Squares Mean)
SPID for Day 4SPID for Day 7
Flurbiprofen Tape, Daily for 12 Hours6.312.1
Flurbiprofen Tape, Daily for 24 Hours5.210.2
Placebo Tape, Daily for 12 Hours4.68.4
Placebo Tape, Daily for 24 Hours6.713.0

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Pain Intensity Difference (PID+)

"+PID = pre-treatment value at baseline - post-treatment value at day of evaluation, where: pre-treatment value at baseline = average daily pain over the last 3 days of the baseline phase (ie, average of daily averages of the categorical pain scale scores for the last 3 days of the baseline phase). Pain was rated on an 11-point scale, where: 0 = no pain, 10 = worst pain imaginable.~A positive PID indicates a reduction in pain." (NCT00759330)
Timeframe: Days 1 through 7 of tape treatment phase

,,,
Interventionunits on a scale (Least Squares Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Flurbiprofen Tape, Daily for 12 Hours1.31.31.62.11.71.92.2
Flurbiprofen Tape, Daily for 24 Hours0.81.41.61.41.51.51.9
Placebo Tape, Daily for 12 Hours0.91.41.21.11.11.21.6
Placebo Tape, Daily for 24 Hours1.11.82.01.82.12.02.2

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Patient Assessment of Wearability of Therapy

"At Day 7, patients assessed the wearability of their treatment tape (ease of application, stays in place, comfortable to wear) using a 4-point scale, where:~1 = Excellent, 4 = Poor." (NCT00759330)
Timeframe: Day 7

,,,
Interventionparticipants (Number)
Ease of application, 1: ExcellentEase of application, 2: GoodEase of application, 3: FairEase of application, 4: PoorStays in place, 1: ExcellentStays in place, 2: GoodStays in place, 3: FairStays in place, 4: PoorComfortable to wear, 1: ExcellentComfortable to wear, 2: GoodComfortable to wear, 3: FairComfortable to wear, 4: Poor
Flurbiprofen Tape, Daily for 12 Hours1911201611113181490
Flurbiprofen Tape, Daily for 24 Hours3912181020210221424
Placebo Tape, Daily for 12 Hours155883538803
Placebo Tape, Daily for 24 Hours0391065749823

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Patient Global Impression of Change (PGIC)

"At Day 7, patients provided their PGIC with regard to lower back pain response to treatment, using a 7-point scale, where:~1 = very much improved, 7 = very much worse." (NCT00759330)
Timeframe: Day 7

,,,
Interventionparticipants (Number)
1: Very much improved2: Much improved3: Improved4: No change5: Worse6: Much worse7: Very much worse
Flurbiprofen Tape, Daily for 12 Hours7101210200
Flurbiprofen Tape, Daily for 24 Hours941118000
Placebo Tape, Daily for 12 Hours31410100
Placebo Tape, Daily for 24 Hours3388000

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 24 Hours Post-baseline (STPIS SPID24)

"STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. SPID24 was calculated as the sum of the time weighted pain intensity differences from baseline until 24 hours. The full range was -104412 (complete pain relief within 1 hour of dosing that lasts 24 hours) to 27588 (maximum pain within 1 hour lasting 24 hours) using the mean baseline STPIS.~Participants with a last recorded time point <21 hours were considered Not Evaluable. If a participant used rescue medication, all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments were imputed using linear interpolation assuming the time of the missing assessment to be the nominal time since initial dose." (NCT01048866)
Timeframe: baseline (pre-dose), post-dose - hourly up to 24 hours

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-522.9
Placebo Lozenge-326.5

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Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 24 Hours From Baseline

"SwoTS measures how swollen a participant's throat felt using a 100-mm visual analog scale completed by participants. Participants were instructed to swallow and Place a line on the scale that best characterizes how swollen your throat feels now. A mark at 0-mm indicated not swollen and 100-mm indicated very swollen.~The full range of the sum of the time-weighted swollen throat differences from baseline until 24 hours was -100320 (throat did not feel swollen at all within 1 hour of dosing and lasted 24 hours) to 31680 (maximum swollen throat reported within 1 hour and lasting 24 hours) using the mean baseline SwoTS. Negative values for differences indicate improvement." (NCT01048866)
Timeframe: Baseline (pre-dose), hourly readings to 24 hours post-dose

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-542.4
Placebo Lozenge-377.4

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Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at 24 Hours After Initial Dose

"Investigators assessed the effectiveness of study medication on the patient's sore throat at 24 hours following initial dose by answering the following question: Considering the patient's response to the study medicine over the past 24 hours, how do you rate the study medicine as a treatment for sore throat? Responses were poor, fair, good, very good or excellent." (NCT01048866)
Timeframe: 24 hours

,
Interventionpercentage of participants (Number)
PoorFairGoodVery GoodExcellent
Flurbiprofen 8.75 mg Lozenge25.027.026.014.08.0
Placebo Lozenge25.329.524.212.68.4

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale Over 24 Hours Post-baseline (STPIS SPID24) For Participants With Baseline Practitioner's Assessment of Pharyngeal Inflammation (PAIN) of Moderate or Severe

"STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. For the subgroup of patients with moderate/severe pharyngeal inflammation at baseline, SPID24 was calculated as the sum of the time weighted pain intensity differences from baseline until 24 hours. Taking inclusion criteria into account, the full range was -115695 (no pain at any post-dose time (0) - average baseline) to 28505 (maximum possible pain (100) - average baseline).~Participants with their last recorded time point <21 hours were considered Not Evaluable. If a participant used rescue medication, all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments were imput" (NCT01048866)
Timeframe: baseline (pre-dose), 24 hours post dose (measured each hour post dose)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-476.9
Placebo Lozenge-351.3

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Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 2 Hours From Baseline

"DSS measures difficulty swallowing (dysphagia) using a 100-mm visual analog scale completed by participants. Participants were instructed to swallow and Place a line on the scale that best characterizes how difficult it is to swallow now. A mark at 0-mm indicated not difficult and 100-mm indicated very difficult.~Data are reported as the sum of the time-weighted pain intensity differences from baseline until 2 hours post dose. The full range was -9360 (no difficulty swallowing within 1 hour of dosing that lasts 2 hours) to 2640 (maximum difficulty swallowing within 1 hour of dosing lasting 2 hours) using the baseline DSS value.~Missing values of DSS with non-missing values at assessments before and after were calculated using linear interpolation." (NCT01048866)
Timeframe: Baseline (pre-dose), Hours 1 and 2 post-dose

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-37.1
Placebo Lozenge-18.1

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Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 24 Hours From Baseline

"DSS measures difficulty swallowing (dysphagia) using a 100-mm visual analog scale completed by participants. Participants were instructed to swallow and Place a line on the scale that best characterizes how difficult it is to swallow now. A mark at 0-mm indicated not difficult and 100-mm indicated very difficult.~Data are reported as the sum of the time-weighted pain intensity differences from baseline until 24 hours post dose. The full range was -102960 (no difficulty swallowing within 1 hour of dosing that lasts 24 hours) to 29040 (maximum difficulty swallowing within 1 hour of dosing lasting 24 hours) using the baseline DSS value. Negative values indicate improvement in difficulty swallowing.~Missing values of DSS with non-missing values at assessments before and after were calculated using linear interpolation." (NCT01048866)
Timeframe: Baseline (pre-dose), hourly readings to 24 hours post-dose

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-555.5
Placebo Lozenge-379.4

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Change From Baseline in Body Temperature at 2 Hours Post Initial Dose

(NCT01048866)
Timeframe: baseline (pre-dose), 2 hours post-dose

Interventiondegrees Fahrenheit (Mean)
Flurbiprofen 8.75 mg Lozenge-0.2
Placebo Lozenge-0.0

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Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 2 Hours From Baseline

"SwoTS measures how swollen a participant's throat felt using a 100-mm visual analog scale completed by participants. Participants were instructed to swallow and Place a line on the scale that best characterizes how swollen your throat feels now. A mark at 0-mm indicated not swollen and 100-mm indicated very swollen.~The full range of the sum of the time-weighted swollen throat differences from baseline until 2 hours was -9120 (throat did not feel swollen at all within 1 hour of dosing and lasted 2 hours) to 2880 (maximum swollen throat reported within 1 hour and lasting 2 hours) using the mean baseline SwoTS.~Negative values for the differences indicate improvement. Missing values of SwoTS with non-missing values at assessments before and after were calculated using linear interpolation." (NCT01048866)
Timeframe: Baseline (pre-dose), hourly readings to 2 hours post-dose

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-35.5
Placebo Lozenge-16.9

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Change From Baseline in Body Temperature at End of Study

(NCT01048866)
Timeframe: baseline (pre-dose), up to Day 7

Interventiondegrees Fahrenheit (Mean)
Flurbiprofen 8.75 mg Lozenge-0.4
Placebo Lozenge-0.3

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Post 24 Hour, Multiple Dose Results: Weighted Sum of Differences Over 2 Hours for Difficulty Swallowing Scale (DSS2)

"The time weighted summed differences over 2 hours after taking a lozenge for all lozenges taken after the initial 24-hours post-baseline.~To measure the functional effect on pharyngitis, the participant was asked to evaluate his/her difficulty swallowing (dysphagia) using a 100-mm visual analog scale prior to dosing, and 1 hour and 2 hours post dose. The participant was instructed to swallow and Place a line on the scale that best characterizes how difficult it is to swallow now. A mark at 0-mm indicated not difficult and 100-mm indicated very difficult. Data for multiple doses/days were averaged to obtain the values used for calculating DSS2. The full range for differences was -5626 to 6374 with negative values indicating improvement in pain intensity.~Assessments were summarized using a repeated measures mixed model, with treatment and center as a fixed effect, time since Baseline as a covariate, and a random effect for participants." (NCT01048866)
Timeframe: Days 2-7

Interventionunits on a scale (Least Squares Mean)
Flurbiprofen 8.75 mg Lozenge-21.0
Placebo Lozenge-15.5

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Post 24 Hour, Multiple Dose Results: Weighted Sum of Differences Over 2 Hours for Swollen Throat Scale (SwoTS2)

"The time weighted summed differences over 2 hours after taking a lozenge for all lozenges taken after the initial 24-hours post-baseline.~The participant was asked to evaluate how swollen his/her throat felt using a 100-mm visual analog scale prior to dosing, and 1 hour and 2 hours post dose.~The patient was instructed to swallow and Place a line on the scale that best characterizes how swollen your throat feels now. A mark at 0-mm indicated not swollen and 100-mm indicated very swollen. Data for multiple doses/days were averaged to obtain the values used for calculating SWoTS2. The full range for differences was -5396 to 6604 with negative values indicating improvement in pain intensity.~Assessments were summarized using a repeated measures mixed model, with treatment and center as a fixed effect, time since Baseline as a covariate, and a random effect for participants." (NCT01048866)
Timeframe: Days 2-7

Interventionunits on a scale (Least Squares Mean)
Flurbiprofen 8.75 mg Lozenge-19.5
Placebo Lozenge-13.4

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Post 24 Hour, Multiple Dose Results: Weighted Sum of Pain Intensity Differences (SPID) Over 2 Hours for the Sore Throat Pain Intensity Scale (STPIS SPID2)

"The time weighted summed differences over 2 hours after taking a lozenge after the initial 24-hours post-baseline.~STPIS is a validated 100-mm visual analog scale completed by participants that measures pain on swallowing (odynophagia). A mark at 0-mm indicates no pain and 100-mm indicates severe pain. SPID2 was calculated as the sum of the time-weighted pain intensity differences from a measurement taken prior to taking a lozenge and at hours 1 + 2 after taking the lozenge during Days 2-7. Data for multiple doses/days were averaged to obtain the values used for calculating SPID2. The full range for SPID2 was -5843 to 6157 with negative values indicating improvement in pain intensity. Assessments were summarized using a repeated measures mixed model, with treatment and center as a fixed effect, time since Baseline as a covariate, and a random effect for participants." (NCT01048866)
Timeframe: Days 2-7

Interventionunits on a scale (Least Squares Mean)
Flurbiprofen 8.75 mg Lozenge-22.7
Placebo Lozenge-16.8

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 2 Hours Post-baseline (STPIS SPID2)

"STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. SPID2 was calculated as the sum of the time weighted pain intensity differences from baseline until 2 hours post dose. The full range was -9492 (complete pain relief within one hour of dosing that lasts 2 hours) to 2508 (maximum pain within 1 hour lasting 2 hours) using the mean baseline STPIS.~If a participant used rescue medication (acetaminophen 650mg was allowed as needed post dose), all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments (recorded or derived due to rescue) were imputed using linear interpolation assuming the time of the missing assessment to be the nominal time since initial dose." (NCT01048866)
Timeframe: baseline (pre-dose), post-dose: 1 hour, 2 hours

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-37.1
Placebo Lozenge-17.9

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Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at End of Study (Day 7)

"Investigators assessed the effectiveness of study medication on the patient's sore throat at the end of study by answering the following question: Considering the patient's response to the study medicine over the past 7 days, how do you rate the study medicine as a treatment for sore throat? Responses were poor, fair, good, very good or excellent." (NCT01048866)
Timeframe: Day 7 (end of study)

,
Interventionpercentage of participants (Number)
PoorFairGoodVery GoodExcellent
Flurbiprofen 8.75 mg Lozenge19.822.924.026.07.3
Placebo Lozenge25.026.120.722.85.4

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Participant Satisfaction Score 24 Hours After Initial Dose

After 24 hours of treatment, participants rated their satisfaction with the treatment on a 7-step scale from extremely dissatisfied to extremely satisfied. (NCT01048866)
Timeframe: 24 hours

,
Interventionpercentage of participants (Number)
Extremely dissatisfiedVery dissatisfiedDissatisfiedSomewhat satisfiedSatisfiedVery satisifiedExtremely satisfied
Flurbiprofen 8.75 mg Lozenge4.04.010.927.723.824.85.0
Placebo Lozenge5.29.414.632.326.07.35.2

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Percentage of Participants Who Took Rescue Pain Medication

Participants were allowed a dose of rescue medication (acetaminophen 650mg), as needed, post-treatment dosing during the study. (NCT01048866)
Timeframe: Days 1-7

,
Interventionpercentage of participants (Number)
YesNo
Flurbiprofen 8.75 mg Lozenge13.986.1
Placebo Lozenge25.874.2

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Post 24 Hour, Multiple Dose Results: Sore Throat Relief As Reported by Participants 2 Hours After Dosing

"Participants graded the relief of his/her sore throat at 2 hours after taking a lozenge for all lozenges taken after the initial 24-hours post-baseline using the Sore Throat Relief Rating Scale (STRRS), which is a 6-category relief scale.~The patient was instructed to swallow and:~Considering how your throat felt before you took the study medicine, circle the phrase that best describes the relief of your sore throat now. Responses following each lozenge were no relief, slight, mild, moderate, considerable, and complete relief. Results summarize responses 2 hours after taking each lozenge." (NCT01048866)
Timeframe: Days 2-7

,
Interventionpercentage of doses (Number)
No reliefSlight reliefMild reliefModerate reliefConsiderable reliefComplete relief
Flurbiprofen 8.75 mg Lozenge9.721.725.216.518.98.0
Placebo Lozenge23.024.819.013.714.74.9

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Sore Throat Relief As Reported by Participants 2 Hours After Initial Dose

"Participants graded the relief of his/her sore throat at 2 hours post initial dose using the Sore Throat Relief Rating Scale (STRRS), which is a 6-category relief scale.~The patient was instructed to swallow and asked:~Considering how your throat felt before you took the study medicine, circle the phrase that best describes the relief of your sore throat now. Responses were no relief, slight, mild, moderate, considerable, and complete relief." (NCT01048866)
Timeframe: 2 hours

,
Interventionpercentage of participants (Number)
No reliefSlight reliefMild reliefModerate reliefConsiderable relief
Flurbiprofen 8.75 mg Lozenge9.928.727.717.815.8
Placebo Lozenge38.122.717.518.63.1

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Time to First Rescue Pain Medication

Participants were allowed a dose of rescue medication (acetaminophen 650mg), as needed, post-treatment during the study. Time from initial dose to first rescue medication is summarized by time categories. (NCT01048866)
Timeframe: Days 1-7

,
Interventionpercentage of participants (Number)
2 - <4 hours4 - <6 hours6 - <24 hours24 - <72 hours72 - 168 hoursDid not rescue
Flurbiprofen 8.75 mg Lozenge2.02.05.93.01.086.1
Placebo Lozenge6.22.113.43.11.074.2

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale Over 24 Hours Post-baseline (STPIS SPID24) For Participants With Baseline Practitioner's Assessment of Pharyngeal Inflammation (PAIN) of Moderate or Severe

"STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. For the subgroup of patients with moderate/severe pharyngeal inflammation at baseline, SPID24 was calculated as the sum of the time weighted pain intensity differences from baseline until 24 hours. Taking inclusion criteria into account, the full range was -116196 (no pain at any post-dose time (0) - average baseline) to 27804 (maximum possible pain (100) - average baseline).~Participants with their last recorded time point <21 hours were considered Not Evaluable. If a participant used rescue medication (acetaminophen 650mg was allowed as needed), all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments were imputed using linear interpolation." (NCT01049334)
Timeframe: baseline (pre-dose), 24 hours post-dose (every 2 minutes for one hour; every 10 minutes until hour 2; every 30 minutes until hour 6; and every hour the participant was awake between hours 7-24)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-451.4
Placebo Lozenge-283.4

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Change From Baseline at 24 Hours in the Tonsillo-Pharyngitis Assessment (TPA) Scores in Participants With Baseline TPA Scores >=8

"Tonsillo-Pharyngitis Assessment, or TPA, is an index of seven clinical features of the pain-producing condition itself, pharyngeal inflammation. The clinical features concern temperature, oropharyngeal color, size of tonsils, number of enanthems, largest size of cervical lymph node, number of lymph nodes, and maximum tenderness of lymph nodes. Each variable was rated on a scale of 0-3, with 0 representing the normal value, and 3 representing severe inflammation. The seven values are added together to create the TPA, ranging from 0-21.~Negative change values represent improvement of symptoms." (NCT01049334)
Timeframe: Baseline (pre-dose), 24 hours post-dose

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-1.2
Placebo Lozenge-2.0

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Kaplan-Meier Estimates for Sore Throat Pain Intensity Scale (STPIS) Time to Definite Improvement

"As part of a protocol amendment, some participants defined a definite improvement level (DIL) relative to their actual pretreatment STPIS on the 100-mm visual analog scale. This was done after completing the 7 day trial.~An alternative definition of STPIS time to onset of relief was the time from initial dose to the time the participant reaching DIL for at least 30 minutes. Data were censored if DIL was not achieved by 120 minutes following initial dose. Definite improvement must also occur prior to re-dosing or using rescue medication." (NCT01049334)
Timeframe: 2 hours

Interventionminutes (Median)
Flurbiprofen 8.75 mg LozengeNA
Placebo LozengeNA

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Kaplan-Meier Estimates for Sore Throat Pain Intensity Scale (STPIS) Time to Definite Improvement Duration of Relief Using Participant-Defined Definite Improvement Levels (DIL)

"As part of a protocol amendment, some participants defined a definite improvement level (DIL) relative to their actual pretreatment STPIS on the 100-mm visual analog scale. This was done after completing the 7 day trial.~The time of first achieving DIL for 30 minutes within 6 hours (or until rescue or re-dosing) post-dosing will be determined. And the time falling below DIL within 6 hours will be determined. Duration is then defined as the time from first DIL until falling below DIL. Duration was set to zero if the STPIS score does not reach the DIL for at least 30 minutes for STPIS during the 6 hours." (NCT01049334)
Timeframe: 6 hours

Interventionminutes (Mean)
Flurbiprofen 8.75 mg Lozenge75.2
Placebo Lozenge29.4

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 2 Hours Post-baseline (STPIS SPID2)

"STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. SPID2 was calculated as the sum of the time-weighted pain intensity differences from baseline until 2 hours post dosing. The full range was -9405 (complete pain relief within 2 minutes of dosing that lasts 2 hours) to 2395 (maximum pain within 2 minutes lasting 2 hours) using the mean baseline STPIS.~If a participant used rescue medication (acetaminophen 650mg was allowed as needed post dose), all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments (recorded or derived due to rescue) were imputed using linear interpolation assuming the time of the missing assessment to be the nominal time since initial dose." (NCT01049334)
Timeframe: baseline (pre-dose), 2 hours post-dose (every 2 minutes for one hour; every 10 minutes until hour 2)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-43.4
Placebo Lozenge-23.5

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) Over the 24 Hours Post-baseline (STPIS SPID24)

STPIS measures sore throat pain intensity on a 100-mm visual analog scale completed by participants. A mark at 0-mm indicates no pain upon swallowing and 100-mm indicates severe pain. SPID24 was calculated as the sum of the time-weighted pain intensity differences from baseline until 24 hours. The full range was -114609 (complete pain relief within 2 minutes of dosing that lasts 24 hours) to 29191 (maximum pain within 2 minutes lasting 24 hours) using the mean baseline STPIS. Participants with a last recorded time point <21 hours were considered Not Evaluable. If a participant used rescue medication, all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments were imputed using linear interpolation assuming the time of the missing assessment to be the nominal time since initial dose. (NCT01049334)
Timeframe: baseline (pre-dose), 24 hours post-dose (every 2 minutes for one hour; every 10 minutes until hour 2; every 30 minutes until hour 6; and every hour the participant was awake between hours 7-24)

Interventionunits on a scale (Least Squares Mean)
Flurbiprofen 8.75 mg Lozenge-473.7
Placebo Lozenge-322.3

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Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 2 Hours From Baseline

"Participants were asked to evaluate his/her difficulty swallowing (dysphagia) using a 100-mm visual analog scale at Baseline and 2 hours post dose.~Participants were instructed to swallow and Place a line on the scale that best characterizes how difficult it is to swallow now. A mark at 0-mm indicated no difficulty and 100-mm indicated very difficult. Data is reported as the sum of the time-weighted pain intensity differences from baseline until 2 hours post dose. The full range was -9192 (no difficulty swallowing within 10 minutes of dosing that lasts 2 hours) to 2808 (maximum difficulty swallowing within 10 minutes lasting 2 hours) using the baseline DSS value.~Missing values of DSS with non-missing values at assessments before and after were calculated using linear interpolation." (NCT01049334)
Timeframe: baseline (pre-dose), 2 hours post-dose (every 10 minutes until hour 2)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-39.1
Placebo Lozenge-16.6

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Time Weighted Summed Differences in Difficulty Swallowing Scale (DSS) During the Initial 24 Hours From Baseline

"Participants were asked to evaluate his/her difficulty swallowing (dysphagia) using a 100-mm visual analog scale at Baseline and until 24 hours post dose.~Participants were instructed to swallow and Place a line on the scale that best characterizes how difficult it is to swallow now. A mark at 0-mm indicated no difficulty and 100-mm indicated very difficult. Data is reported as the sum of the time-weighted pain intensity differences from baseline until 24 hours post dose. The full range was -110304 (no difficulty swallowing within 10 minutes of dosing that lasts 24 hours) to 33696 (maximum difficulty swallowing within 10 minutes lasting 24 hours) using the baseline DSS value.~Missing values of DSS with non-missing values at assessments before and after were calculated using linear interpolation." (NCT01049334)
Timeframe: baseline (pre-dose), 24 hours post-dose (every 10 minutes until hour 2, every 30 minutes until hour 6, hourly from 7-24 hours)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-460.8
Placebo Lozenge-274.3

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Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 2 Hours From Baseline

"The participant was asked to evaluate how swollen his/her throat felt using a 100-mm visual analog scale at Baseline and at 1 hour, 70 minutes, 80 minutes, 90 minutes, 100 minutes, 110 minutes, and 2 hours.~The patient was instructed to swallow and Place a line on the scale that best characterizes how swollen your throat feels now. A mark at 0-mm indicated not swollen and 100-mm indicated very swollen. The full range of the sum of the time-weighted swollen throat differences from baseline until 2 hours was -9336 (throat did not feel swollen at all within 1 hour of dosing and lasted 2 hours) to 2664 (maximum swollen throat reported within 1 hour and lasting 2 hours) using the mean baseline SwoTS." (NCT01049334)
Timeframe: baseline (pre-dose), 2 hours post-dose (at 1 hour, 70 minutes, 80 minutes, 90 minutes, 100 minutes, 110 minutes, and 2 hours)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-39.9
Placebo Lozenge-20.1

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Time Weighted Summed Differences in Swollen Throat Scale (SwoTS) During the Initial 24 Hours From Baseline

"The participant was asked to evaluate how swollen his/her throat felt using a 100-mm visual analog scale at Baseline and specified timeframes until 24 hours.~The patient was instructed to swallow and Place a line on the scale that best characterizes how swollen your throat feels now. A mark at 0-mm indicated not swollen and 100-mm indicated very swollen. The full range of the sum of the time-weighted swollen throat differences from baseline until 24 hours was -112032 (throat did not feel swollen at all within 1 hour of dosing and lasted 24 hours) to 31968 (maximum swollen throat reported within 1 hour and lasting 24 hours) using the mean baseline SwoTS." (NCT01049334)
Timeframe: baseline (pre-dose), 24 hours post-dose (1 hour, 70 minutes, 80 minutes, 90 minutes, 100 minutes, 110 minutes, 2 hours, 2½ hours, 3 hours, 3½ hours, 4 hours, 4½ hours, 5 hours, 5½ hours, and 6 hours after the first dose, hourly from 7-24 hours)

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-472.2
Placebo Lozenge-355.2

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Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at 24 Hours After Initial Dose

"Investigators assessed the effectiveness of study medication on the patient's sore throat at 24 hours following initial dose by answering the following question: Considering the patient's response to the study medicine over the past 24 hours, how do you rate the study medicine as a treatment for sore throat? Responses were poor, fair, good, very good or excellent." (NCT01049334)
Timeframe: 24 hours

,
Interventionpercentage of participants (Number)
PoorFairGoodVery GoodExcellent
Flurbiprofen 8.75 mg Lozenge15.834.719.813.915.8
Placebo Lozenge38.028.018.013.03.0

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Investigators' Clinical Assessment (CLIN) Of Study Medication as a Treatment for Sore Throat at the End of the Study (Day 7)

"Investigators assessed the effectiveness of study medication on the patient's sore throat at the end of the study by answering the following question: Considering the patient's response to the study medicine over the past 7 days, how do you rate the study medicine as a treatment for sore throat? Responses were poor, fair, good, very good or excellent." (NCT01049334)
Timeframe: Day 7

,
Interventionpercentage of participants (Number)
PoorFairGoodVery GoodExcellent
Flurbiprofen 8.75 mg Lozenge11.828.030.117.212.9
Placebo Lozenge31.634.714.714.74.2

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Practitioner's Assessment of Pharyngeal Inflammation (P.A.I.N.) Scores at 24 Hours After Initial Dose

P.A.I.N is a four step scale in which physicians rate the severity of pharyngeal inflammation: No inflammation, mild, moderate and severe inflammation. (NCT01049334)
Timeframe: 24 hours post-dose

,
Interventionparticipants (Number)
No inflammationMild inflammationModerate inflammationSevere inflammation
Flurbiprofen 8.75 mg Lozenge0484211
Placebo Lozenge142507

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Sore Throat Relief Rating Scale (STRRS) At 2 Hours After Initial Dose

"Participants used a 6-category relief scale (no relief to complete relief) to grade the relief of his/her throat pain.~The patient was instructed to swallow and:~Considering how your throat felt before you took the study medicine, circle the phrase that best describes the relief of your sore throat now." (NCT01049334)
Timeframe: 2 hours

,
Interventionpercentage of participants (Number)
No reliefSlight reliefMild reliefModerate reliefConsiderable reliefComplete relief
Flurbiprofen 8.75 mg Lozenge18.623.523.520.613.70
Placebo Lozenge45.124.511.813.74.90

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Pain Intensity Scale (STPIS) at Each Post-Dose Time Point Until the Time Point at Which Comparison of the Arms Yielded a P-value <=0.05

"Data reported in summary form in Primary Outcome #1 are reported here at each post-dose timepoint until the comparison resulted in a P-value <=0.05 between the two treatment arms.~STPIS was used to measure sore throat pain intensity using a 100-mm visual analog scale completed by participants that measures pain on swallowing (odynophagia). A mark at 0-mm indicates no pain and 100-mm indicates severe pain. The full range of the scale varies by timepoint due to the time weighting sum of SPID. The full scale at 40 minutes post dose was -3188 (complete pain relief within 2 minutes of dosing that lasts 40 minutes) to 812 (maximum pain within 2 minutes lasting 40 minutes) using the mean baseline STPIS.~If a participant used rescue medication (acetaminophen 650mg was allowed as needed), all post-rescue STPIS values in the 24-hour interval were assigned the baseline value for STPIS. Missing scores of STPIS with non-missing STPIS scores at earlier and later assessments (rec" (NCT01049334)
Timeframe: baseline (pre-dose), up to 23 hours post-dose (every 2 minutes for one hour; every 10 minutes until hour 2; every 30 minutes until hour 6; and every hour the participant was awake between hours 7-23)

,
Interventionunits on a scale (Mean)
Minutes post dose: 2Minutes post dose: 4Minutes post dose: 6Minutes post dose: 8Minutes post dose: 10Minutes post dose: 12Minutes post dose: 14Minutes post dose: 16Minutes post dose: 18Minutes post dose: 20Minutes post dose: 22Minutes post dose: 24Minutes post dose: 26Minutes post dose: 28Minutes post dose: 30Minutes post dose: 32Minutes post dose: 34Minutes post dose: 36Minutes post dose: 38Minutes post dose: 40
Flurbiprofen 8.75 mg Lozenge-0.1-0.3-0.6-0.9-1.4-1.9-2.4-3.0-3.5-4.1-4.7-5.2-5.9-6.5-7.2-7.9-8.6-9.3-10.1-10.8
Placebo Lozenge-0.2-0.4-0.8-1.2-1.6-2.1-2.5-2.9-3.3-3.7-4.1-4.5-4.9-5.3-5.8-6.2-6.6-7.1-7.5-7.9

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Participant Satisfaction Scores 24 Hours After Initial Dose

After 24 hours of treatment, participants rated their satisfaction with the treatment on a 7-step scale from extremely dissatisfied to extremely satisfied. (NCT01049334)
Timeframe: 24 hours

,
Interventionpercentage of participants (Number)
Extremely dissatisfiedVery dissatisfiedDissatisfiedSomewhat satisfiedSatisfiedVery satisfiedExtremely satisfied
Flurbiprofen 8.75 mg Lozenge5.06.911.929.720.823.82.0
Placebo Lozenge10.020.014.028.017.09.02.0

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Change From Baseline at Individual Timepoints in Sore Throat Scale (STS)

"The participant was asked to evaluate his/her sore throat when swallowing using a vertical 0-10 Likert scale, where 0=not sore and 10=very sore. The participant was instructed: Circle the number that shows how sore your throat is now when you swallow. The STS was obtained at baseline, every 5 minutes after treatment during the first hour and every 10 minutes during the second and third hours." (NCT01986361)
Timeframe: Baseline (Day 1, pre-dose), up to 3 hours post dose on Day 1

,
Interventionunits on a scale (Mean)
Minute 5Minute 10Minute 15Minute 20Minute 25Minute 30Minute 35Minute 40Minute 45Minute 50Minute 55Minute 60Minute 70Minute 80Minute 90Minute 100Minute 110Minute 120Minute 130Minute 140Minute 150Minute 160Minute 170Minute 180
Flurbiprofen 8.75 mg Lozenge-0.4-0.7-0.9-1.0-1.3-1.6-1.8-2.0-2.2-2.3-2.4-2.5-2.6-2.7-2.7-2.7-2.7-2.7-2.6-2.6-2.5-2.4-2.3-2.3
Placebo Lozenge-0.4-0.6-0.6-0.6-0.7-1.0-1.0-1.1-1.2-1.3-1.1-1.1-1.2-1.1-1.0-1.0-1.0-1.0-1.0-0.9-0.8-0.9-0.8-0.8

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Kaplan-Meier Estimates for Time of First Indication of Sore Throat Relief as Measured By Any Reduction in the Sore Throat Scale (STS)

"Time to first indication of sore throat relief, defined as any reduction or decrease in STS observed during the 3 hours post dose. Participants who did not have any reduction in STS from baseline within 3 hours were censored to 3 hours.~The participant was asked to evaluate his/her sore throat when swallowing using a vertical 0-10 Likert scale, where 0=not sore and 10=very sore. The participant was instructed: Circle the number that shows how sore your throat is now when you swallow. The STS was obtained at baseline, every 5 minutes after treatment during the first hour and every 10 minutes during the second and third hours." (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionminutes (Median)
Flurbiprofen 8.75 mg Lozenge15.000
Placebo Lozenge20.000

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Kaplan-Meier Estimates for Time of First Perceived Pain Reduction on the Sore Throat Scale (STS) Which is Followed by ≥ 20% Pain Reduction on the Sore Throat Pain Intensity Scale (STPIS)

"Time to pain reduction on the STS (defined as any reduction or decrease observed during the 3 hours post dose) for participants whose improvement was confirmed by a >=20% reduction in pain on the STPIS.~STS: The participant was asked to evaluate his/her sore throat when swallowing using a vertical 0-10 Likert scale, where 0=not sore and 10=very sore. The participant was instructed: Circle the number that shows how sore your throat is now when you swallow. The STS was obtained at baseline, every 5 minutes after treatment during the first hour and every 10 minutes during the second and third hours.~STPIS: The participant was instructed to swallow and: Place a line on the Sore Throat Scale that best characterizes the severity of your sore throat now: 0mm=no pain and 100mm=severe pain. The STPIS was obtained at baseline, after the participant depressed the second stopwatch, and at 1, 2, and 3 hours postdose." (NCT01986361)
Timeframe: Baseline (Day 1, pre-dose), up to 3 hours post dose on Day 1

Interventionminutes (Median)
Flurbiprofen 8.75 mg Lozenge15.000
Placebo LozengeNA

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Kaplan-Meier Estimates for Time of First Perceived Pain Relief

"Time to first perceived pain relief is a patient-reported outcome (PRO) captured as part of the double stopwatch method. Participants depress the first stop watch when they experience any pain relief, termed perceived pain relief. Instructions to participants are: Stop the first stopwatch when you first feel any sore throat pain relief whatsoever. This does not mean you feel completely better, although you might, but when you first feel any relief of the throat pain you have now. Participants who did not have perceived pain relief were censored at 3 hours." (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionminutes (Median)
Flurbiprofen 8.75 mg Lozenge10.867
Placebo Lozenge19.317

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Kaplan-Meier Estimates for Time to First Perceived Pain Relief That Is Confirmed By Meaningful Pain Relief

Time to first perceived pain relief on the first stopwatch that was confirmed by meaningful pain relief on the second stopwatch. Participants who had no meaningful pain relief within 3 hours from baseline were censored to 3 hours. (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionminutes (Median)
Flurbiprofen 8.75 mg Lozenge13.200
Placebo LozengeNA

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Kaplan-Meier Estimates for Time to Meaningful Pain Relief

"Time to meaningful pain relief is a patient-reported outcome (PRO) captured as part of the double stopwatch method. Participants depress the second stop watch when they experience what they perceive as meaningful pain relief. Instructions to participants are: Stop the second stopwatch when the sore throat pain relief is meaningful to you. This does not mean you feel completely better, although you might, but when you feel relief of throat pain that is meaningful to you. Participants who did not have perceived pain relief were censored at 3 hours." (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionminutes (Median)
Flurbiprofen 8.75 mg Lozenge42.917
Placebo LozengeNA

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Percentage of Participants With Meaningful Pain Relief

Defined as the percentage of participants who pressed the second stopwatch during the 3 hour evaluation period. (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionpercentage of participants (Number)
Flurbiprofen 8.75 mg Lozenge78.2
Placebo Lozenge47.6

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Percentage of Participants With Perceived Pain Relief

Defined as the percentage of participants who pressed the first stopwatch during the 3 hour evaluation period. (NCT01986361)
Timeframe: up to 3 hours post dose on Day 1

Interventionpercentage of participants (Number)
Flurbiprofen 8.75 mg Lozenge97.0
Placebo Lozenge76.2

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Time Weighted Sum of Pain Intensity Differences (SPID) in Sore Throat Scale (STS) Over the 3 Hours Post-baseline (STS SPID3)

"The participant was asked to evaluate his/her sore throat when swallowing using a vertical 0-10 Likert scale, where 0=not sore and 10=very sore. The participant was instructed: Circle the number that shows how sore your throat is now when you swallow. STS was obtained at baseline, every 5 minutes after treatment during the first hour and every 10 minutes during the second and third hours, for a total of 24 post-dose measurements.~The time-weighted SPID combines relief magnitude (PID = change from baseline) as weighted by duration interval between ratings. SPID3 refers to measurements taken up to 3 hours post-baseline, and has a full range of -1332 (complete pain relief within 5 minutes of dosing that lasts for 3 hours) to 468 (drug escalates level of pain to a score of 10 and the pain stays at that level for 3 hours) using the mean baseline STS value 7.4 for this study." (NCT01986361)
Timeframe: Baseline (Day 1, pre-dose), up to 3 hours post dose on Day 1

Interventionunits on a scale (Mean)
Flurbiprofen 8.75 mg Lozenge-403.9
Placebo Lozenge-166.4

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Mechanical Hyperalgesia Threshold on the Dominant Inner Forearm

The mechanical hyperalgesia threshold was defined as the lowest force (g) necessary to bend a Von Frey filament, which was perceived to be painful by the patient and measured by Von Frey filament at 24 hours postoperatively (NCT02043366)
Timeframe: 24 hours after surgery

Interventiong (Mean)
Normal Saline60.57
Flurbiprofen AxetilⅠ78.29
Flurbiprofen AxetilⅡ68.50
Butorphanol79.7
Butorphanol-Flurbiprofen Axetil81.64
Sufentanil89.5

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Normalized Area of Hyperalgesia Around the Incision

The skin around the incision is stimulated in steps of 5 mm at intervals of 1 s starting outside of the hyperalgesic area in the direction of the incision. The distance from the incision to the first point where a 'painful', 'sore' or 'sharper' feeling occurred is measured and noted. This measurement is repeated at predefined radial lines around the incision. To eliminate the variable length of incision, this length is subtracted from the longer diameter leaving four radial distances from the end and from the middle of the incision. The normalized area of hyperalgesia is calculated by summing up the areas of the remaining four triangles measured by and Von Frey filament. (NCT02043366)
Timeframe: 24 hours after surgery

Interventioncm^2 (Mean)
Normal Saline60.46
Flurbiprofen AxetilⅠ53.64
Flurbiprofen AxetilⅡ56.57
Butorphanol54.00
Butorphanol-Flurbiprofen Axetil52.5
Sufentanil49.89

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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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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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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 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 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 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 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 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 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 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 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 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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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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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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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: 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: 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: 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: 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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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 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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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 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 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 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 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 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 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 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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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 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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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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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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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 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 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 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 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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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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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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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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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(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 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 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 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 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 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 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 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 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 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-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-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 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 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 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 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 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 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 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 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 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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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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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 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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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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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 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 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 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 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 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 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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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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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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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 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 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 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 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 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 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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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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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 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 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 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 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 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 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 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 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 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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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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