Page last updated: 2024-12-04

adenine

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Cross-References

ID SourceID
PubMed CID190
CHEMBL ID226345
CHEBI ID16708
SCHEMBL ID8110
MeSH IDM0000347

Synonyms (217)

Synonym
smr000471871
MLS001066342
6-aminopurine (adenine)
einecs 200-796-1
adenine [jan]
nsc 14666
adenin
CHEBI:16708 ,
KBIO1_001575
DIVK1C_006631
SDCCGMLS-0066584.P001
9h-purine,6-dihydro-6-imino-
wln: t56 bm dn fn hnj iz
1h-purine, 6-amino-
nsc-14666
nsc14666
leucon (tn)
D00034
adenine (jan/usp)
SPECTRUM4_001891
SPECTRUM_001106
SPECTRUM5_000542
CMAP_000085
ADE ,
OPREA1_057274
BSPBIO_002152
inchi=1/c5h5n5/c6-4-3-5(9-1-7-3)10-2-8-4/h1-2h,(h3,6,7,8,9,10
9h-purin-6-amine
6-amino-3h-purine
6-amino-1h-purine
pedatisectine b
adeninimine
9h-purine, 1,6-dihydro-6-imino-
ccris 2556
usaf cb-18
1h-purin-6-amine
1h-purine, 6-amino
6-amino-7h-purine
1,6-dihydro-6-iminopurine
leuco-4
ai3-50679
3,6-dihydro-6-iminopurine
purine, 6-amino-
vitamin b4
6-amino-9h-purine
1h-purin-6-amine (9ci)
adenine (8ci)
73-24-5
ADENINE-RING ,
adenine ,
6-aminopurine
C00147
adenine, >=99%
adenine, bioreagent, plant cell culture tested, >=99%
adenine, suitable for cell culture, bioreagent
1JYS
1NLI
DB00173
1WEI
NCGC00094856-02
NCGC00094856-01
7h-purin-6-amine
KBIO2_004154
KBIO2_001586
KBIOSS_001586
KBIOGR_002562
KBIO3_001652
KBIO2_002562
KBIO2_007698
KBIOGR_002447
KBIO3_003040
KBIOSS_002571
NCI60_000998
KBIO2_006722
KBIO2_005130
SPECPLUS_000535
SPECTRUM3_000616
SPBIO_000426
SPECTRUM2_000583
SPECTRUM1500807
NCGC00094856-03
4, vitamin b
2P8N
vitamin b 4
b 4, vitamin
STK387542
adenine, 1
chembl226345 ,
bdbm33218
HMS2092K20
AC-2028
6379C0E0-C1BB-4087-96C5-1DE281B8EA4C
A0149
2PQJ
P50008
AKOS000118903
BMSE000060
purin-6-amine
FT-0656198
HMS1921I14
jac85a2161 ,
unii-jac85a2161
adenine [usp:jan]
BMSE000861
BBL007925
cas-73-24-5
dtxcid502557
NCGC00255120-01
tox21_302108
dtxsid6022557 ,
nsc-757793
nsc757793
BCP9000233
pharmakon1600-01500807
tox21_111348
BMSE000995
HMS2269I04
71660-30-5
71660-29-2
3h-purin-6-amine (9ci)
7h-purin-6-amine (9ci)
CCG-38506
AKOS005171607
BCPP000433
(s)-norfluoxetine-d5
EPITOPE ID:140097
Z-1043
S1981
BL008313
gtpl4788
AB00052833-19
AB00052833-18
FT-0620943
adenine [mart.]
adenine [usp impurity]
adenine [who-dd]
adenosine impurity a [ep impurity]
adenine [vandf]
adenine [inci]
adenine [usp-rs]
adenine [mi]
adenine [ep monograph]
adenine [usp monograph]
HY-B0152
CS-1984
AM83908
SCHEMBL8110
3KPV
tox21_111348_1
NCGC00094856-05
9h-purin-6-ylamine
[3h]adenine
6-amino purine
7h-purin-6-ylamine
9h-purin-6-yl-amine
1h-purine-6-amine
9h-purin-6-amine #
9h-purine-6-amine
134434-49-4
134454-76-5
W-106856
Q-200595
66224-66-6
3h-purin-6(7h)-imine
1h-purin-6(9h)-imine
AB00052833_23
AB00052833_24
AB00052833_20
AB00052833_22
mfcd00041790
us9138393, adenine
bdbm181146
us9144538, adenine
F0001-1848
adenine, european pharmacopoeia (ep) reference standard
SR-05000001754-2
sr-05000001754
adenine, united states pharmacopeia (usp) reference standard
SR-05000001754-1
6,7-dihydro-3h-purin-6-imine
adenine, vetec(tm) reagent grade, >=99%
adenine, pharmaceutical secondary standard; certified reference material
adenine; 7h-purin-6-amine
3h-adenine
SBI-0052324.P002
6-amino-purine
9h-purin-6-yl-amin
6h-purin-6-imine, 1,9-dihydro-, (e)- (9ci)
6h-purin-6-imine, 3,7-dihydro-, (z)- (9ci)
134461-75-9
6h-purin-6-imine, 1,7-dihydro-, (z)- (9ci)
134434-48-3
6h-purin-6-imine, 3,9-dihydro-, (z)- (9ci)
6-aminopurine;vitamin b4
Z104498572
7h-purin-6-amine, min. 95%
adenine,(s)
AS-11841
1217770-71-2
BCP02865
Q15277
EN300-21472
(z)-3,9-dihydro-6h-purin-6-imine
adenine 100 microg/ml in water
1,9-dihydro-6h-purin-6-imine
A935233
VCA70030
STARBLD0001134
adenine, cell culture grade
bdbm50582699
adenine (usp-rs)
adenine1546
adenine (ep monograph)
adenine (usp:jan)
adenine (usp monograph)
adenine (mart.)
adenine (usp impurity)

Research Excerpts

Overview

Adenine methylation is an epigenetic modification present in DNA (6mA) and RNA (m6A) that has a regulatory function in many cellular processes. Eritadenine is a hypocholesterolemic compound that is found in several mushroom species.

ExcerptReferenceRelevance
"Adenine methylation is an epigenetic modification present in DNA (6mA) and RNA (m6A) that has a regulatory function in many cellular processes."( Same modification, different location: the mythical role of N
De-la-Peña, C; Jiménez-Ramírez, IA; Moreno-Cálix, DM; Pijeira-Fernández, G, 2022
)
1.44
"Adenine is a key nucleobase, adenosine is an endogenous regulator of the immune system, while adenosine triphosphate (ATP) is the energy source of many biological reactions. "( Aptamer-based strategies for recognizing adenine, adenosine, ATP and related compounds.
Li, Y; Liu, J, 2020
)
2.27
"Adenine is an important molecule for biomedical and agricultural research and applications. "( Silver-Based SERS Pico-Molar Adenine Sensor.
Lin, BY; Tzeng, Y, 2020
)
2.29
"Adenine is a purine nucleobase that amalgamates important biomolecules such as DNA, RNA, and ATP."( Radioresistance of Adenine to Cosmic Rays.
Auge, B; Boduch, P; Domaracka, A; Martinez, R; Mejía, CF; Rothard, H; Vignoli Muniz, GS, 2017
)
1.5
"Eritadenine is a hypocholesterolemic compound that is found in several mushroom species such as Lentinula edodes, Marasmius oreades, and Amanita caesarea (1.4, 0.7 and 0.6 mg per g dry weight, respectively). "( Effect of traditional and modern culinary processing, bioaccessibility, biosafety and bioavailability of eritadenine, a hypocholesterolemic compound from edible mushrooms.
Largo, C; Morales, D; Piris, AJ; Polo, G; Soler-Rivas, C; Tabernero, M, 2018
)
1.25
"Adenine auxotrophy is a commonly used genetic marker in haploid yeast strains. "( Adenine auxotrophy--be aware: some effects of adenine auxotrophy in Saccharomyces cerevisiae strain W303-1A.
Kibilds, J; Kokina, A; Liepins, J, 2014
)
3.29
"Adenine is a common organic base and its concentration variations caused by foods, has various effects on the body metabolic systems."( Effects of adenine on the pituitary-gonad axis in newborns rats.
Johari, H; Parhizkar, Z; Talebi, E, 2008
)
1.46
"Adenine serves as an effective matrix for the stabilization of Ag/CdS through interaction of N(1), N(3) and -NH(2) with Ag."( Time resolved emission studies of Ag-adenine-templated CdS (Ag/CdS) nanohybrids.
Chaudhary, V; Kumar, A, 2009
)
1.35
"The adenine molecule is a DNA nucleobase, an essential component of genetic material. "( Ultraviolet photostability of adenine on gold and silicon surfaces.
Martín-Gago, JA; Mateo-Martí, E; Pradier, CM,
)
0.98
"Adenine is a uric acid pathway metabolite of no known function, and has recently been identified as a ligand for a rat G protein-coupled receptor. "( Adenine induces differentiation of rat hepatic stellate cells.
Gautam, S; Gomes, DA; Mehal, WZ; Sohail, MA; Watanabe, A, 2012
)
3.26
"Adenine is an important bio-molecule that plays many crucial roles in food safety and biomedical diagnostics. "( Supramolecular polymeric chemosensor for biomedical applications: design and synthesis of a luminescent zinc metallopolymer as a chemosensor for adenine detection.
Chow, CF, 2012
)
2.02
"Adenine is an important compound in biological systems, such as genetic and energy utilization processes. "( Behavior of adenine in Na-montmorillonite exposed to gamma radiation: implications to chemical evolution studies.
Guzmán, A; Negrón-Mendoza, A; Ramos-Bernal, S, 2002
)
2.14
"Adenine is an approved additive to citrate-phosphate-dextrose anticoagulant for whole blood collection and extends the storage life of red blood cells. "( The effect of adenine on platelet storage.
Rock, G; Wong, SC,
)
1.93
"Adenine N1-oxide is a DNA lesion whose formation involves the specific oxidation of the adenine base by hydrogen peroxide under nonradical conditions. "( Polyclonal antibodies to adenine N1-oxide: characterization and use for the measurement of DNA damage.
Cadet, J; Molko, D; Signorini, N, 1998
)
2.05
"This adenine (A622) is a pH controlled conformational switch that opens up the internal loop at higher pH."( A pH controlled conformational switch in the cleavage site of the VS ribozyme substrate RNA.
Dieckmann, T; Flinders, J, 2001
)
0.77
"Adenine derivative 2a is a substrate for adenosine deaminase whereas both 2a and 2b exhibit 50% inhibition of the growth of murine leukemia L 1210 cell culture at 1 mM concentration."( Synthesis and biological properties of 9-(trans-4-hydroxy-2-buten-1-yl)adenine and guanine: open-chain analogues of neplanocin A.
Phadtare, S; Zemlicka, J, 1987
)
1.23

Effects

Adenine has a largely hydrophobic protein interface. phosphate interacts primarily with hydrophilic residues. ribose is intermediate.

The adenine reaction has been studied experimentally, but there are few theoretical results. Adenine sensitivity has been previously associated with defective purine salvage resulting from impaired synthesis of guanine nucleotides. 8-Azaadenines have been recently proposed as a novel promising class of adenosine A1 receptor antagonists.

ExcerptReferenceRelevance
"Adenine has a unique importance in biochemistry and therefore life."( Radioresistance of Adenine to Cosmic Rays.
Auge, B; Boduch, P; Domaracka, A; Martinez, R; Mejía, CF; Rothard, H; Vignoli Muniz, GS, 2017
)
1.5
"Adenine has a largely hydrophobic protein interface, while phosphate interacts primarily with hydrophilic residues; ribose is intermediate."( Protein recognition of adenylate: an example of a fuzzy recognition template.
Mitchell, JB; Moodie, SL; Thornton, JM, 1996
)
1.02
"Adenine has a unique importance in biochemistry and therefore life."( Radioresistance of Adenine to Cosmic Rays.
Auge, B; Boduch, P; Domaracka, A; Martinez, R; Mejía, CF; Rothard, H; Vignoli Muniz, GS, 2017
)
1.5
"The adenine reaction has been studied experimentally, but there are few theoretical results."( Hydroxyl radical reactions with adenine: reactant complexes, transition states, and product complexes.
Cheng, Q; Compaan, KR; Gu, J; Schaefer, HF, 2010
)
1.13
"The adenine residue has no influence on complex stability except in the Cu(9,8aPMEA) and Zn(9,8aPMEA) systems, where an additional stability increase attributable to the adenine residue is observed and equilibria between four different isomers exist."( Quantification of isomeric equilibria formed by metal ion complexes of 8-[2-(phosphonomethoxy)ethyl]-8-azaadenine (8,8aPMEA) and 9-[2-(phosphonomethoxy)ethyl]-8-azaadenine (9,8aPMEA). Derivatives of the antiviral nucleotide analogue 9-[2-(phosphonomethoxy
Gómez-Coca, RB; González-Vílchez, F; Holý, A; Kapinos, LE; Sigel, H; Vilaplana, RA, 2004
)
1.02
"8-Azaadenines have been recently proposed as a novel promising class of adenosine A1 receptor antagonists. "( QSAR study on a novel series of 8-azaadenine analogues proposed as A1 adenosine receptor antagonists.
Biagi, G; Bianucci, AM; Coi, A; Fiamingo, F; Giorgi, I; Leonardi, M; Massarelli, I; Nofal, FA; Pietra, D, 2008
)
1.13
"Adenine has a largely hydrophobic protein interface, while phosphate interacts primarily with hydrophilic residues; ribose is intermediate."( Protein recognition of adenylate: an example of a fuzzy recognition template.
Mitchell, JB; Moodie, SL; Thornton, JM, 1996
)
1.02
"Adenine sensitivity has been previously associated with defective purine salvage resulting from impaired synthesis of guanine nucleotides from adenine."( Purine catabolism in Escherichia coli and function of xanthine dehydrogenase in purine salvage.
Reitzer, L; Schneider, BL; Xi, H, 2000
)
1.03
"Adenine deaminase has been partially purified and characterized."( Catabolism of adenosine 5'-monophosphate in promastigotes of Leishmania tropica.
Königk, E; Rasoul, SA, 1978
)
0.98
"The adenine action has been proved down to a concentration of 3 X 10(-6) M."( [Regulation of age-dependent phenomena. Influence of C6-substituted purines on cell aggregation and cell migration in primary cultures of lense epithelial cells].
Glässer, D; Iwig, M; Weber, E, 1975
)
0.74

Actions

Adenine plays an essential role in replication in all known living systems today. Adenine led to marked increase of ATP and 2- to 4-fold stimulation of starch synthesis.

ExcerptReferenceRelevance
"Adenine overload promotes intratubular crystal precipitation and interstitial nephritis. "( NF-κB activation mediates crystal translocation and interstitial inflammation in adenine overload nephropathy.
Arias, SC; Barlette, GP; Borges, RL; Camara, NO; de Almeida, DC; Fanelli, C; Fujihara, CK; Machado, FG; Malheiros, DM; Okabe, C; Zatz, R, 2013
)
2.06
"8PT-adenine did not activate PKA or inhibit DNA synthesis by AZF cells."( 8-Phenylthio-adenines stimulate the expression of steroid hydroxylases, Cav3.2 Ca²⁺ channels, and cortisol synthesis by a cAMP-independent mechanism.
Enyeart, JA; Enyeart, JJ; Liu, H, 2011
)
1.22
"Adenine may produce the effects observed by increasing the rate at which ethionine enters the cell and reaches its primary site of antibacterial action."( ENHANCEMENT BY ADENINE OF THE INHIBITION OF SALMONELLA TYPHIMURIUM BY ETHIONINE.
SALMON, WD; SMITH, RC, 1965
)
1.32
"Adenine displays at least two adsorption sites, including a high-energy site (210 degrees C, approximately 136 kJ/mol), wherein the molecule coordinates to the gold substrate via the NH2 group in an sp3-like, strongly perturbed, nonplanar configuration."( On the structure and desorption dynamics of DNA bases adsorbed on gold: a temperature-programmed study.
Demers, LM; Liedberg, B; Mirkin, CA; Ostblom, M, 2005
)
1.05
"Adenine led to marked increase of ATP and 2- to 4-fold stimulation of starch synthesis."( Increased levels of adenine nucleotides modify the interaction between starch synthesis and respiration when adenine is supplied to discs from growing potato tubers.
Geigenberger, P; Loef, I; Stitt, M, 2001
)
1.36
"Adenine plays an essential role in replication in all known living systems today, and is prominent in many other aspects of biochemistry. "( The prebiotic role of adenine: a critical analysis.
Shapiro, R, 1995
)
2.05
"Adenine induced an increase of about three times the initial ATP concentration of this mutant at 42 degrees C which dropped quickly after 10 min."( Effect of adenine, cytidine and guanosine on the expression of the SOS system in Escherichia coli.
Barbé, J; Guerrero, R; Llagostera, M; Villaverde, A, 1985
)
1.39

Treatment

Adenine treatment reduced body weight, creatinine renal clearance, and increased water intake and urine output. Adenine-treated animals exhibited marked azotemia, impaired urinary concentrating capacity, intense tubular and glomerular damage, interstitial inflammation and fibrosis.

ExcerptReferenceRelevance
"Adenine treated rats had a reduction in urine output (‒45%), food intake (‒46%), body weight (‒28%), total proteins (‒66%) and albumin (‒59%) and an increase in creatinine (950%), BUN (73.6%), and kidney weight (43.75%). "( Nephroprotective effects of ethanolic root extract of
Arunachalam, R; Devi, S; Eerike, M; Radhakrishnan, AK; Rao Konda, VG,
)
1.57
"Adenine treatment reduced body weight, creatinine renal clearance, and increased water intake and urine output, as well as the plasma concentrations of urea and creatinine, neutrophil gelatinase-associated lipocalin, and N-acetyl-β-D-glucosaminidase activity, and albumin in urine."( The effect of sildenafil on rats with adenine-Induced chronic kidney disease.
Adham, SA; Al Kalbani, J; Al Suleimani, Y; Al Za'abi, M; Ali, BH; Karaca, T; Manoj, P; Nemmar, A; Yasin, J, 2018
)
1.47
"The adenine-treated animals exhibited marked azotemia, impaired urinary concentrating capacity, intense tubular and glomerular damage, interstitial inflammation and fibrosis. "( Role of impaired Nrf2 activation in the pathogenesis of oxidative stress and inflammation in chronic tubulo-interstitial nephropathy.
Aminzadeh, MA; Nicholas, SB; Norris, KC; Vaziri, ND, 2013
)
0.95
"Adenine treatment impaired kidney function: it lowered creatinine clearance and increased plasma concentrations of creatinine, urea, neutrophil gelatinase-associated lipocalin and vanin-1."( The effect of activated charcoal on adenine-induced chronic renal failure in rats.
Al-Lawati, I; Ali, BH; Alza'abi, M; Beegam, S; Brand, S; Nemmar, A; Ramkumar, A; Schupp, N; Waly, MI, 2014
)
1.4
"Adenine-treated Sprague-Dawley rats were randomly assigned to receive continuous peritoneal injections of PDF with or without MGO for three weeks or were left untreated for the same duration. "( Peritoneal fibrosis induced by intraperitoneal methylglyoxal injection: the role of concurrent renal dysfunction.
Akimoto, T; Hirahara, I; Inoue, M; Kusano, E; Morishita, Y; Nagata, D; Onishi, A, 2014
)
1.85
"Adenine-treated animals experienced weight-loss, polyuria and polydipsia; however, these effects were significantly attenuated in adenine-treated Gunn rats."( Endogenously elevated bilirubin modulates kidney function and protects from circulating oxidative stress in a rat model of adenine-induced kidney failure.
Benzie, IF; Boon, AC; Briskey, D; Bulmer, AC; Coombes, JS; Fassett, RG; Gopalan, V; Lam, AK, 2015
)
1.35
"Adenine treatment in rats has been proposed as an animal model of anemia of CKD with high hepcidin levels that mirrors the condition in human patients."( A hepcidin lowering agent mobilizes iron for incorporation into red blood cells in an adenine-induced kidney disease model of anemia in rats.
Babitt, JL; Brown, DE; Cappellini, MD; Chen, S; Hong, CC; Lin, HY; Stepanek, A; Sun, CC; Theurl, I; Vaja, V; Weiss, G, 2013
)
1.33
"Adenine-treated rats exhibited increased hepatic hepcidin mRNA, decreased serum iron, increased spleen iron content, low hemoglobin (Hb) and inappropriately low erythropoietin (EPO) levels relative to the degree of anemia. "( A hepcidin lowering agent mobilizes iron for incorporation into red blood cells in an adenine-induced kidney disease model of anemia in rats.
Babitt, JL; Brown, DE; Cappellini, MD; Chen, S; Hong, CC; Lin, HY; Stepanek, A; Sun, CC; Theurl, I; Vaja, V; Weiss, G, 2013
)
2.06
"Adenine-treated rats showed marked elevations of serum phosphorus, PTH and FGF23 levels associated with parathyroid hyperplasia and aortic calcification."( [Effects of intermittent treatment with sevelamer hydrochloride on parathyroid hyperplasia and vascular calcification in rats with chronic kidney disease].
Abe, M; Kobayashi, N; Miyata, S; Nagano, N; Wada, M; Wakita, S, 2005
)
1.05
"The adenine-treated rats were divided into the following 3 groups, that is, the group experienced no treatment (control), the group given our Chinese herbal medicine (HAO), and the group given vitamin D3 (VD3) medication."( Effects of the Chinese herbal medicine based on Hachimi-jio-gan in male rats with the adenine-induced osteopenia.
Gao, M; Guo, L; Guo, Y; Ishida, T; Kanehara, M; Ogirima, T; Tano, K; Wang, X; Zhang, Y, 2005
)
1.03
"Adenine-treated rats developed severe CRI, with markedly elevated serum levels of phosphorus, PTH and FGF23, and reduced levels of serum 1,25(OH)(2)D(3)."( Effect of manipulating serum phosphorus with phosphate binder on circulating PTH and FGF23 in renal failure rats.
Abe, M; Kobayashi, N; Miyata, S; Nagano, N; Wada, M; Wakita, S; Yamashita, T, 2006
)
1.06
"Adenine-treated extracts prepared with or without DTT/PMSF showed higher D/O ratios in all post-dialysis samples when compared with their pre-dialysis ratios."( Rat liver xanthine oxidoreductase: effect of adenine on the oxidase and dehydrogenase activities.
Hagopian, K, 2007
)
1.32
"Treatment with adenine, but not AuNPs, reduced the levels of phosphorylated p38 and PI3 kinase expression more effectively than did treatment with the respective inhibitors alone."( Adenine decreases hypertrophic effects through interleukin-18 receptor.
Liang, YJ; Yang, YF,
)
1.91
"Treatment with adenine decreased the hematocrit and the Hb level, which were associated with increases in the blood urea nitrogen and plasma creatinine levels. "( Failure to confirm a sodium-glucose cotransporter 2 inhibitor-induced hematopoietic effect in non-diabetic rats with renal anemia.
Hitomi, H; Kittikulsuth, W; Kobara, H; Konishi, Y; Masaki, T; Morikawa, T; Nakano, D; Nishiyama, A; Osafune, K; Yamazaki, D, 2020
)
0.91
"Pretreatment with adenine significantly reversed this tendency."( Radioprotective effect of adenine on irradiation-induced apoptosis.
Dong, Z; Gao, Y; Hong, Q; Lu, XQ; Ma, ZC; Shao, S; Tan, HL; Wang, XY; Wang, YG, 2013
)
1.01
"Treatment with adenine induced Kidney Yang Deficiency in rats by causing a reduction in urinary 17-hydroxy cortisol, urine creatinine and urine osmolality. "( [Changes of lung, spleen and kidney aquaporin-1 in rats with Kidney Yang Deficiency: the "water metabolism theory" in traditional Chinese medicine].
He, L; Li, J; Lin, R; Liu, N; Wu, F; Zhang, X, 2012
)
0.73
"Treatment with adenine, guanine, guanosine, guanine nucleotides, and uracil nucleotides protected Purkinje cells from cell death in the cerebellar primary cultures."( Neuroprotective effect of adenine on purkinje cell survival in rat cerebellar primary cultures.
Ikekita, M; Watanabe, S; Yoshimi, Y, 2003
)
0.96
"Mice treated with adenine showed marked depletion of brain norepinephrine, dopamine and serotonin, irrespective of whether or not they had been treated with d- or l-amphetamine, and whether or not these agents were capable of reversing adenine-induced depression of locomotor activity."( Reversal of adenine-induced depression of mouse locomotor activity by amphetamine.
Akintonwa, A; Auditore, JV, 1978
)
0.96

Toxicity

Plerixafor (AMD3100, 1,1'-bis-1,4,8,11-tetraazacyclotetradekan) alone or combination with adefovir (PMEA, 9-(2-phosphonylmethoxyethyl)adenine) safe and effective for treating FIV- infected cats.

ExcerptReferenceRelevance
" The toxic effects are discussed on the basis of these results."( Comparison of toxic effects of methylguanidine, guanidinosuccinic acid and creatinine in rats with adenine-induced chronic renal failure.
Mo, ZL; Oura, H; Yokozawa, T, 1989
)
0.49
" The drug was found to be toxic to all of the cell lines tested."( Studies on the mechanism of cytotoxicity of 3-deazaguanosine in human cancer cells.
Jacobsen, SJ; Mangum, JH; Nyhan, WL; Page, T; Robins, RK; Scheele, J; Smejkal, RM, 1985
)
0.27
" Growth studies with various purine salvage pathway mutants and the ability of guanosine to prevent adenine toxicity indicated that adenine exerts its toxic effects by depleting guanine nucleotide pools."( Mechanism of adenine toxicity in Escherichia coli.
Levine, RA; Taylor, MW, 1982
)
0.85
" Cytokines, in particular tumor necrosis factor, are responsible for most of the toxic effects of LPS."( Role for circulating lipoproteins in protection from endotoxin toxicity.
Feingold, KR; Funk, JL; Grunfeld, C; Moser, AH; Rapp, JH; Shigenaga, JK, 1995
)
0.29
" Addition of an intracellular cholesterol transport inhibitor, either progesterone or U18666A, together with CP-113,818 blocked the toxic effect of CP-113,818."( Cell toxicity induced by inhibition of acyl coenzyme A:cholesterol acyltransferase and accumulation of unesterified cholesterol.
Bamberger, M; Johnson, WJ; Rothblat, GH; Stoudt, G; Warner, GJ, 1995
)
0.29
" This indicated that the more oxidised the LDL was, the more toxic it was to the macrophages."( Toxicity of oxidised low density lipoprotein towards mouse peritoneal macrophages in vitro.
Mitchinson, MJ; Reid, VC, 1993
)
0.29
" Repeat infusions of PMEA at a dose of 1000 mg were safe and well tolerated."( Safety of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in patients with human immunodeficiency virus infection: a pilot study.
Arends, S; Kamp, W; Schokker, J; van Halteren, E, 1996
)
0.57
" Secondary endpoints were the assessment of the possible adverse clinical and biochemical effects of transfusing AS-1 RBCs stored for < or = 42 days."( AS-1 red cells for neonatal transfusions: a randomized trial assessing donor exposure and safety.
Bell, EF; Burmeister, LF; Cordle, DG; James, T; Johnson, K; Ludwig, GA; Miller, J; Strauss, RG, 1996
)
0.29
" Gastrointestinal complaints and reversible liver transaminase elevations were the most frequently noted adverse events."( Anti-human immunodeficiency virus (HIV) activity, safety, and pharmacokinetics of adefovir dipivoxil (9-[2-(bis-pivaloyloxymethyl)-phosphonylmethoxyethyl]adenine) in HIV-infected patients.
Barditch-Crovo, P; Cundy, KC; Ebeling, D; Hendrix, CW; Jaffe, HS; Lietman, PS; Toole, J, 1997
)
0.49
"Intracellular killing of Leishmania parasites within activated murine macrophages is thought to result from the toxic activities of nitrogen oxidation products (referred to as NO) released by the activated cells."( Leishmania spp.: mechanisms of toxicity of nitrogen oxidation products.
Mauël, J; Ransijn, A, 1997
)
0.3
" Cytotoxicity was less than for PMEA or azidothymidine (AZT) for culture periods of 7 days, but more toxic after 10 days."( Toxicity associated with high dosage 9-[(2R,5R-2,5-dihydro-5-phosphonomethoxy)-2-furanyl]adenine therapy off attempts to abort early FIV infection.
Ferk, G; Hartmann, K; North, TW; Pedersen, NC, 1997
)
0.52
" Adefovir dipivoxil was determined to be safe and well-tolerated when administered for 12 weeks."( The safety and efficacy of adefovir dipivoxil, a novel anti-human immunodeficiency virus (HIV) therapy, in HIV-infected adults: a randomized, double-blind, placebo-controlled trial.
Cherrington, JM; Collier, A; Deeks, SG; Drew, WL; Hellmann, N; Jaffe, HS; Kahn, J; Lalezari, J; Lamy, PD; Li, W; Mulato, AS; Pavia, A; Rodrigue, D; Toole, J, 1997
)
0.3
" All subjects tolerated dosing without significant adverse events."( Safety, pharmacokinetics, and antiretroviral activity of intravenous 9-[2-(R)-(Phosphonomethoxy)propyl]adenine, a novel anti-human immunodeficiency virus (HIV) therapy, in HIV-infected adults.
Barditch-Crovo, P; Cundy, KC; Deeks, SG; Hellmann, NS; Hwang, F; Kahn, JO; Lietman, PS; Rooney, JF; Safrin, S, 1998
)
0.51
"Changes in HIV RNA from baseline, based on area under the curve and CD4+ cell levels, adverse events, and effect of baseline genotypic resistance on response to adefovir."( Efficacy and safety of adefovir dipivoxil with antiretroviral therapy: a randomized controlled trial.
Basgoz, N; Beall, G; Cherng, D; Cherrington, J; Coakley, D; Cooper, R; Deeks, S; Hardy, D; Kahn, J; Lagakos, S; Miller, M; Murphy, R; Ng, E; Toole, JJ; Winslow, D; Wulfsohn, M,
)
0.13
"Results of both the randomized study and the subsequent evaluation documented that AS-3 RBCs stored < or =42 days and transfused in small volumes (15 mL/kg) were safe for RBC transfusions of preterm infants."( Feasibility and safety of AS-3 red blood cells for neonatal transfusions.
Burmeister, LF; Cordle, D; Cress, G; Johnson, K; Strauss, RG, 2000
)
0.31
" Patients were monitored for adverse effects."( Single-dose pharmacokinetics and safety of the oral antiviral compound adefovir dipivoxil in children infected with human immunodeficiency virus type 1. The Pediatrics AIDS Clinical Trials Group.
Blanchard, S; Burchett, S; Coakley, DF; Culnane, M; Cundy, KC; Fridland, A; Hughes, WT; Purdue, L; Read, JS; Rodman, JH; Shenep, JL; Willoughby, R; Zimmer, B, 2000
)
0.31
"This report investigates the pathomechanism of acute renal failure caused by toxic acute tubular necrosis after treatment with the antiretroviral agent adefovir."( Adefovir nephrotoxicity: possible role of mitochondrial DNA depletion.
Bell, A; D'agati, VD; Kambham, N; Markowitz, GS; Tanji, K; Tanji, N, 2001
)
0.31
" In conclusion, the use of AS-1 red blood cells is safe for small volume transfusions in neonates."( Safety and efficacy of AS-1 red blood cell use in neonates.
Jain, R; Jarosz, C, 2001
)
0.31
"Four patients withdrew from the study (two because of adverse events), leaving 31 patients who received adefovir dipivoxil for a median of 48 weeks (range 44-48)."( Safety and efficacy of adefovir dipivoxil in patients co-infected with HIV-1 and lamivudine-resistant hepatitis B virus: an open-label pilot study.
Benhamou, Y; Bochet, M; Brosgart, C; Calvez, V; Fievet, MH; Fry, J; Gibbs, CS; Katlama, C; Namini, H; Poynard, T; Thibault, V; Vig, P, 2001
)
0.31
" Grade III or IV adverse events were limited to laboratory abnormalities, including elevated creatine phosphokinase and liver function tests, which resolved with or without drug discontinuation and without sequelae."( Phase i/ii trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults.
Barditch-Crovo, P; Coakley, DF; Coleman, RL; Collier, A; Deeks, SG; Kahn, JO; Kearney, BP; Lamy, PD; Lietman, PS; McGowan, I; Miller, M; Safrin, S, 2001
)
0.31
"Drug-associated dysfunction of mitochondria is believed to play a role in the etiology of the various adverse symptoms that occur in human immunodeficiency virus (HIV)-infected patients treated with the nucleoside reverse transcriptase inhibitors (NRTIs)."( Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors.
Birkus, G; Cihlar, T; Hitchcock, MJ, 2002
)
0.31
" This adapter links the toxic moiety and ligand that are usually directly coupled."( A cleavable adapter to reduce nonspecific cytotoxicity of recombinant immunotoxins.
Fuchs, H; Heisler, I; Keller, J; Sutherland, M; Tauber, R, 2003
)
0.32
" Toxic pathway discrimination is needed to group chemicals for potency predictions and identification of structural parameters associated with distinct types of reactive toxicity, a necessary step for development of mechanistically based quantitative structure-activity relationships (QSARs) to predict chemical toxic potential."( Discriminating redox cycling and arylation pathways of reactive chemical toxicity in trout hepatocytes.
Denny, JS; Hammermeister, DE; Kolanczyk, RC; Schmieder, PK; Sheedy, BR; Tapper, MA, 2003
)
0.32
" The aim of this review is to present the structure of all the various known oxidised DNA base lesions known to date and to summarise the present knowledge about the mutagenic and toxic effects of oxidised base modifications and their repair."( Mutagenicity, toxicity and repair of DNA base damage induced by oxidation.
Bjelland, S; Seeberg, E, 2003
)
0.32
" In vitro exposure of leukemia cells to CAde showed that it was eight times less toxic as compared to CdA."( Cytotoxicity and pharmacokinetics of cladribine metabolite, 2-chloroadenine in patients with leukemia.
Albertioni, F; Juliusson, G; Larsson, R; Liliemark, J; Lindemalm, S, 2004
)
0.56
"The rise in didanosine concentrations in plasma when given with tenofovir raises concern for a high risk of toxic effects."( Pancreatic toxic effects associated with co-administration of didanosine and tenofovir in HIV-infected adults.
Blanco, JL; de Lazzari, E; García, F; Gatell, JM; Larrousse, M; Mallolas, J; Martínez, E; Milinkovic, A; Miró, JM; Ravasi, G,
)
0.13
" Twelve subjects in the QD Group (14%) discontinued treatment due to adverse events, mainly nevirapine-related hepatitis (6%)."( Safety and efficacy of once-daily didanosine, tenofovir and nevirapine as a simplification antiretroviral approach.
Burger, D; Clotet, B; Galindos, MJ; Gel, S; Miralles, C; Moltó, J; Muñoz-Moreno, JA; Negredo, E; Pedrol, E; Puig, J; Ribera, E; Rodriguez Fumaz, C; Rodríguez, E; Ruiz, L; Viciana, P; Videla, S, 2004
)
0.32
" On mice with leukaemia P388, this product has no effect on the tumour growth, and it appears to be toxic at the dose of 25 mg/kg."( Cytotoxic effects of kinetin riboside on mouse, human and plant tumour cells.
Bos, R; Griffaut, B; Ledoigt, G; Madelmont, JC; Maurizis, JC, 2004
)
0.32
" These data have now provided a clear and clinically relevant understanding of the individual profiles of drugs within the nucleoside analogue reverse transcriptase inhibitor , HIV protease inhibitor and non-nucleoside analogue reverse transcriptase inhibitor drug classes, and have provided a rational basis for assessing and monitoring these adverse effects in clinical practice."( Adverse effects of antiretroviral therapy for HIV infection: a review of selected topics.
Mallal, S; Nolan, D; Reiss, P, 2005
)
0.33
"These results suggest that adefovir dipivoxil would be an effective and safe treatment for patients with decompensated liver cirrhosis with lamivudine resistance, but its effect might be limited and slower for decompensated cirrhosis."( [Efficacy and safety of adefovir dipivoxil in patients with decompensated liver cirrhosis with Lamivudine resistance compared to patients with compensated liver disease].
Choi, MS; Koh, KC; Lee, JH; Moon, W; Moon, YM; Paik, SW; Rhee, JC; Shim, SG; Yoo, BC, 2005
)
0.33
"Despite the recent publication of case reports describing various manifestations of tenofovir-related nephrotoxicity, data regarding the incidence of and risk factors for this adverse effect are currently lacking."( Incidence of and risk factors for tenofovir-induced nephrotoxicity: a retrospective cohort study.
Antoniou, T; Chirhin, S; Gough, K; Govan, V; Loutfy, M; Raboud, J; Rachlis, A; Yoong, D, 2005
)
0.33
" No serious adverse events related to adefovir dipivoxil occurred during the study, and HIV-1 RNA and CD4+ cell counts were stable."( Safety and efficacy of adefovir dipivoxil in patients infected with lamivudine-resistant hepatitis B and HIV-1.
Benhamou, Y; Biao, L; Brosgart, C; Calvez, V; Chang, CG; Currie, G; Fievet, MH; Marcelin, AG; Poynard, T; Thibault, V; Vig, P; Xiong, S, 2006
)
0.33
" There were no significant clinical and biochemical adverse effects."( Efficacy and safety of adefovir dipivoxil in kidney recipients, hemodialysis patients, and patients with renal insufficiency.
Brosgart, C; Chaix, ML; Currie, G; Fontaine, H; Morales, E; Nalpas, B; Pol, S; Serpaggi, J; Vallet-Pichard, A; Varaut, A; Verkarre, V, 2005
)
0.33
"Adefovir dipivoxil is safe for the treatment of chronic hepatitis B in patients with varying degrees of renal dysfunction and lamivudine-resistant HBV and results in biochemical and virological efficacy similar to that reported in the general population."( Efficacy and safety of adefovir dipivoxil in kidney recipients, hemodialysis patients, and patients with renal insufficiency.
Brosgart, C; Chaix, ML; Currie, G; Fontaine, H; Morales, E; Nalpas, B; Pol, S; Serpaggi, J; Vallet-Pichard, A; Varaut, A; Verkarre, V, 2005
)
0.33
" Our results confirm the efficacy and safety of adefovir treatment in post-liver transplantation patients with lamivudine-resistant HBV, neither were adefovir-resistant mutations identified in patients after 21 months of therapy, nor were there adverse events, especially renal toxicity."( Study on the efficacy and safety of adefovir dipivoxil treatment in post-liver transplant patients with hepatitis B virus infection and lamivudine-resistant hepatitis B virus.
Avilés, JF; Bárcena, R; Barrios, C; Buti, M; Casanovas, T; Cuervas, V; De la Mata, M; Del Campo, S; Delgado, M; Dieguez, ML; Fraga, E; Gonzalez, A; Herrero, JI; Loinaz, C; Mas, A; Moraleda, G; Moreno, JM; Muñoz, R; Otero, A; Prieto, M; Rueda, M; Sousa, JM, 2005
)
0.33
"No significant changes were found in clinical symptoms, vital signs and laboratory tests after dosing, except slight elevations of alanine aminotransferase in 2 subjects and bilirubin in 6 subjects observed and some gastrointestinal symptoms such as nausea and diarrhea found in 3 subjects, but the frequency and severity of all the adverse reactions were not found to be related to the dosages."( [Safety and tolerance study of single oral dose of adefovir dipivoxil tablets in healthy volunteers].
Fan, XP; Guo, RC; Sun, DQ; Wang, BJ; Wang, HS; Wang, K, 2005
)
0.33
"The results showed that single oral dose of adefovir dipivoxil 60 mg or less was safe and tolerable."( [Safety and tolerance study of single oral dose of adefovir dipivoxil tablets in healthy volunteers].
Fan, XP; Guo, RC; Sun, DQ; Wang, BJ; Wang, HS; Wang, K, 2005
)
0.33
" Although 92% of the women reported at least one adverse event, the majority were mild (87%) and involved the genitourinary tract (70%)."( Safety and tolerability of tenofovir vaginal gel in abstinent and sexually active HIV-infected and uninfected women.
El-Sadr, WM; Eshleman, SH; Gai, F; Hendrix, C; Justman, J; Kwiecien, A; Maslankowski, LA; Mâsse, B; Mayer, KH; Morrow, K; Rooney, JF; Soto-Torres, L, 2006
)
0.33
" IC87114 did not have direct adverse effects or enhance the activity of VP16 on the proliferation and survival of normal haemopoietic progenitors."( A selective inhibitor of the p110delta isoform of PI 3-kinase inhibits AML cell proliferation and survival and increases the cytotoxic effects of VP16.
Billottet, C; Gale, RE; Grandage, VL; Khwaja, A; Quattropani, A; Rommel, C; Vanhaesebroeck, B, 2006
)
0.33
" Safety and tolerance were evaluated by monitoring adverse events and laboratory parameters, and pharmacokinetics were assessed by determining PMEA concentrations with a validated LC-MS/MS method."( Pharmacokinetics, safety and tolerance of single- and multiple-dose adefovir dipivoxil in healthy Chinese subjects.
Guo, RC; Ni, MY; Sun, DQ; Wang, BJ; Wang, HS, 2007
)
0.34
"No serious adverse events occurred."( Pharmacokinetics, safety and tolerance of single- and multiple-dose adefovir dipivoxil in healthy Chinese subjects.
Guo, RC; Ni, MY; Sun, DQ; Wang, BJ; Wang, HS, 2007
)
0.34
"ADV is safe and well tolerated in healthy Chinese subjects."( Pharmacokinetics, safety and tolerance of single- and multiple-dose adefovir dipivoxil in healthy Chinese subjects.
Guo, RC; Ni, MY; Sun, DQ; Wang, BJ; Wang, HS, 2007
)
0.34
" Together, these in vitro results indicate that combination with other antiretrovirals does not significantly increase the toxic potential of TFV in RPTECs."( In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells.
Alvarez, ML; Cihlar, T; Cordobilla, B; Domingo, JC; Domingo, P; Giralt, M; Guallar, J; López-Dupla, M; Sánchez de la Rosa, R; Saumoy, M; Torres, F; Vidal, F; Villarroya, F, 2006
)
0.33
" Previous studies of the toxic and mutagenic properties of the DNA adduct EA have been limited to in vitro experiments using mammalian polymerases and have revealed the lesion to be both miscoding and genotoxic."( Alleviation of 1,N6-ethanoadenine genotoxicity by the Escherichia coli adaptive response protein AlkB.
Delaney, JC; Drennan, CL; Essigmann, JM; Frick, LE; Wong, C, 2007
)
0.64
"These results suggest: (i) that suboptimal responses to adefovir 10 mg daily are due to underdosing; and (ii) that increasing the adefovir dose to 20 mg daily is beneficial and safe in patients with lamivudine-resistant HBV and a suboptimal response to adefovir 10 mg daily, especially when alanine aminotransferase levels are elevated and/or the liver disease is severe or rapidly progressive."( Efficacy and safety of adefovir dipivoxil 20 mg daily in HBeAg-positive patients with lamivudine-resistant hepatitis B virus and a suboptimal virological response to adefovir dipivoxil 10 mg daily.
Bouvier-Alias, M; Brillet, R; Chevaliez, S; Dhumeaux, D; Hézode, C; Pawlotsky, JM; Roudot-Thoraval, F; Zafrani, ES, 2007
)
0.34
" The US Food and Drug Administration's Adverse Event Reporting System was searched for reports of nephrolithiasis in HIV-infected patients taking an atazanavir-based regimen."( Atazanavir-associated nephrolithiasis: cases from the US Food and Drug Administration's Adverse Event Reporting System.
Birnkrant, DB; Chan-Tack, KM; Struble, KA; Truffa, MM, 2007
)
0.34
"To assess adverse events associated with antiretroviral regimens for human immunodeficiency virus (HIV) postexposure prophylaxis (PEP), with a particular focus on the treatment combination of zidovudine, lamivudine, and tenofovir (ZDV-3TC-TDF)."( Assessment of adverse events associated with antiretroviral regimens for postexposure prophylaxis for occupational and nonoccupational exposures to prevent transmission of human immunodeficiency virus.
Antenozzi, S; Hulse, S; Luque, A; Shahzad, U; Smith, B; Tanzman, E; Wang, D, 2007
)
0.34
"Retrospective chart review for individuals who received HIV PEP for occupational and nonoccupational exposure, and multivariate analyses to identify risk factors for noncompletion of PEP and adverse events associated with PEP."( Assessment of adverse events associated with antiretroviral regimens for postexposure prophylaxis for occupational and nonoccupational exposures to prevent transmission of human immunodeficiency virus.
Antenozzi, S; Hulse, S; Luque, A; Shahzad, U; Smith, B; Tanzman, E; Wang, D, 2007
)
0.34
"Preventive treatment of adverse events may be necessary to ensure completion of HIV PEP."( Assessment of adverse events associated with antiretroviral regimens for postexposure prophylaxis for occupational and nonoccupational exposures to prevent transmission of human immunodeficiency virus.
Antenozzi, S; Hulse, S; Luque, A; Shahzad, U; Smith, B; Tanzman, E; Wang, D, 2007
)
0.34
"A tenofovir DF expanded access program (EAP) was initiated in 2001; safety data were examined from this program and from the manufacturer's database, which contained reports of all postmarketing adverse drug reactions received up to 30 April 2005."( The safety of tenofovir disoproxil fumarate for the treatment of HIV infection in adults: the first 4 years.
Bischofberger, N; Chen, SS; Clotet, B; Cooper, DA; Curtis, S; Gazzard, B; Katlama, C; Lange, J; Lazzarin, A; Montaner, JS; Nelson, MR; Rooney, JF; Schewe, K; Smith, S; Wyatt, C, 2007
)
0.34
"The EAP enrolled 10 343 patients; serious adverse events (SAEs) were reported in 631 (6%)."( The safety of tenofovir disoproxil fumarate for the treatment of HIV infection in adults: the first 4 years.
Bischofberger, N; Chen, SS; Clotet, B; Cooper, DA; Curtis, S; Gazzard, B; Katlama, C; Lange, J; Lazzarin, A; Montaner, JS; Nelson, MR; Rooney, JF; Schewe, K; Smith, S; Wyatt, C, 2007
)
0.34
"The SCOLTA Project is a prospective, observational, multicenter study involving 25 infectious disease departments in Italy created to assess the incidence of severe adverse events in patients receiving new antiretroviral drugs."( Tenofovir renal safety in HIV-infected patients: results from the SCOLTA Project.
Bonfanti, P; Carradori, S; De Socio, GV; Grosso, C; Landonio, S; Madeddu, G; Marconi, P; Melzi, S; Miccolis, S; Mura, MS; Penco, G; Quirino, T; Ricci, E; Rosella, E, 2008
)
0.35
" No patient discontinued due to renal adverse events."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
" TDF treatment was not associated with renal adverse events or limb fat loss in antiretroviral-naïve patients."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
"Simplification to a once-daily regimen containing TDF, 3TC, and EFV is virologically and immunologically effective, well-tolerated, and safe with benefits in the lipid profile in the majority of patients."( Effectiveness and safety of simplification therapy with once-daily tenofovir, lamivudine, and efavirenz in HIV-1-infected patients with undetectable plasma viral load on HAART.
Aguirrebengoa, K; Alvarez, ML; Arazo, P; Arrizabalaga, J; Chocarro, A; Echevarría, S; Fariñas, MC; Ferrer, P; García-Palomo, D; Iribarren, JA; Labarga, P; Letona, S; Muñoz-Sánchez, MJ; Oteo, JA; Peralta, G; Pinilla, J; Uriz, J,
)
0.13
" All other combinations exhibited more pronounced adverse effects on mitochondrial endpoints."( Mitochondrial toxicity of tenofovir, emtricitabine and abacavir alone and in combination with additional nucleoside reverse transcriptase inhibitors.
Melkaoui, K; Setzer, B; Venhoff, N; Walker, UA, 2007
)
0.34
"Changing from drugs that have significant mitochondrial toxicity to less toxic compounds may be of benefit in human immunodeficiency virus (HIV)-positive patients who receive highly active antiretroviral therapy."( Effects of the change from Stavudine to tenofovir in human immunodeficiency virus-infected children treated with highly active antiretroviral therapy: studies on mitochondrial toxicity and thymic function.
Cossarizza, A; Dentone, C; Di Biagio, A; Esposito, R; Ferraresi, R; Mussini, C; Nasi, M; Nemes, E; Pinti, M; Repetto, E; Rosso, R; Viscoli, C, 2008
)
0.35
" A relatively uncommon adverse effect of this drug is Fanconi syndrome."( Tenofovir-associated Fanconi syndrome: review of the FDA adverse event reporting system.
Gupta, SK, 2008
)
0.35
" Symptoms disappeared after discontinuation of antiretroviral therapy and we suggest that syncope may be a side effect to one of the three antiretroviral drugs that has not been described previously."( Syncope as a probable side effect to combination antiretroviral therapy initiated during primary HIV-1 infection.
Larsen, CS; Lybaek, D, 2008
)
0.35
" Treatment-related adverse events were reported for 12% of ADV-treated and 10% of placebo-treated subjects."( Safety, efficacy, and pharmacokinetics of adefovir dipivoxil in children and adolescents (age 2 to <18 years) with chronic hepatitis B.
Frederick, D; Jonas, MM; Kelly, D; Mizerski, J; Mondou, E; Pollack, H; Rousseau, F; Sokal, E; Sorbel, J, 2008
)
0.35
" There were no serious adverse events related to ADV."( Long-term efficacy and safety of adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B.
Arterburn, S; Borroto-Esoda, K; Chang, TT; Frederick, D; Lim, SG; Marcellin, P; Rousseau, F; Sievert, W; Tong, M, 2008
)
0.35
"100 patients were evaluated; 17 patients discontinued early including 6 for adverse events."( Evaluation of efficacy, safety, pharmacokinetics, and adherence in HIV-1-infected, antiretroviral-naïve patients treated with ritonavir-boosted atazanavir plus fixed-dose tenofovir DF/emtricitabine given once daily.
Cohen, C; Ebrahimi, R; Elion, R; Fisher, A; Flaherty, J; Kearney, B; McColl, D; Ortiz, R; Reddy, YS; Ruane, P; Ward, D,
)
0.13
"In two randomized, controlled trials, small differences in glomerular filtration rate over time were noted but no clinically relevant renal disease or adverse events were demonstrated in antiretroviral-naive patients treated with TDF through 144 weeks."( The 3-year renal safety of a tenofovir disoproxil fumarate vs. a thymidine analogue-containing regimen in antiretroviral-naive patients.
Chen, SS; Cheng, AK; DeJesus, E; Enejosa, JV; Gallant, JE; Pozniak, AL; Winston, JA, 2008
)
0.35
" Although frequency of severe renal toxicity was higher than has been reported in the literature, it was safe in patients with no comorbid renal conditions."( Effectiveness and safety of generic fixed-dose combination of tenofovir/emtricitabine/efavirenz in HIV-1-infected patients in Western India.
Bele, V; Dravid, A; Gupte, N; Joshi, K; Pujari, S, 2008
)
0.35
"To identify adverse effects of tenofovir use during pregnancy in HIV-infected women and their infants."( Adverse effects of tenofovir use in HIV-infected pregnant women and their infants.
Hayes, E; Mondy, K; Nurutdinova, D; Onen, NF; Overton, ET, 2008
)
0.35
" Each woman's chart was reviewed for clinical data and adverse events during the pregnancy; each infant's chart was reviewed for growth parameters from birth to 12 months."( Adverse effects of tenofovir use in HIV-infected pregnant women and their infants.
Hayes, E; Mondy, K; Nurutdinova, D; Onen, NF; Overton, ET, 2008
)
0.35
" One stopped IFN treatment because of adverse events and continued ADV only."( Efficacy and safety of adefovir dipivoxil plus pegylated interferon-alpha2a for the treatment of lamivudine-resistant hepatitis B virus infection in HIV-infected patients.
Benhamou, Y; Dominguez, S; Duvivier, C; Ingiliz, P; Katlama, C; Poynard, T; Thibault, V; Valantin, MA, 2008
)
0.35
"ADV and PEG-IFN is safe and effective for treating 3TC-R HBV in HIV patients."( Efficacy and safety of adefovir dipivoxil plus pegylated interferon-alpha2a for the treatment of lamivudine-resistant hepatitis B virus infection in HIV-infected patients.
Benhamou, Y; Dominguez, S; Duvivier, C; Ingiliz, P; Katlama, C; Poynard, T; Thibault, V; Valantin, MA, 2008
)
0.35
"The use of nucleoside analogues, especially that of thymidine analogues, depletes mitochondrial DNA, which is the cause of many of the adverse effects of this family of antiretroviral drugs, among them lipodystrophy."( [Tenofovir as a strategy to avoid or limit adverse effects].
Portilla, J, 2008
)
0.35
"We have demonstrated that low-dosage adefovir therapy in kidney-transplant patients is relatively safe as far as renal parameters are concerned, even though we observed a slight impairment of renal proximal-tubular function."( Renal side effects of adefovir in hepatitis B virus-(HBV) positive kidney allograft recipients.
Alric, L; Huart, A; Izopet, J; Kamar, N; Rostaing, L; Tack, I, 2009
)
0.35
"Lipoatrophy is the most stigmatizing side effect of stavudine therapy."( Improvements in subcutaneous fat, lipid profile, and parameters of mitochondrial toxicity in patients with peripheral lipoatrophy when stavudine is switched to tenofovir (LIPOTEST study).
Castella, E; Crespo, M; Curran, A; Del Saz, SV; Diaz, M; Falcó, V; Feijoo, M; García-Arumí, E; Ocaña, I; Pahissa, A; Paradiñeiro, JC; Planas, M; Puiggròs, C; Ribera, E; Sauleda, S; Sureda, D,
)
0.13
" Significantly fewer drug-related clinical adverse events occurred in patients on raltegravir (n=124 [44."( Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial.
Barnard, RJ; Berger, DS; DeJesus, E; DiNubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Madruga, JV; Miller, MD; Nguyen, BY; Pollard, RB; Rodgers, AJ; Sklar, P; Williams-Diaz, A; Xu, X; Zhao, J, 2009
)
0.35
" Data on CD4 cell count, HIV viral load, metabolic parameters and adverse events of grade 3-4 are collected through an on-line system every six months."( Efficacy and safety of boosted and unboosted atazanavir-containing antiretroviral regimens in real life: results from a multicentre cohort study.
Abeli, C; Bonfanti, P; Gianelli, E; Giuntini, R; Grosso, C; Madeddu, G; Marconi, P; Martinelli, C; Palvarini, L; Pellicano, G; Penco, G; Quirino, T; Ricci, E; Vichi, F, 2010
)
0.36
"Our results suggest that, in unselected clinical settings, ATV-containing antiretroviral therapy is durable and safe in both its formulations."( Efficacy and safety of boosted and unboosted atazanavir-containing antiretroviral regimens in real life: results from a multicentre cohort study.
Abeli, C; Bonfanti, P; Gianelli, E; Giuntini, R; Grosso, C; Madeddu, G; Marconi, P; Martinelli, C; Palvarini, L; Pellicano, G; Penco, G; Quirino, T; Ricci, E; Vichi, F, 2010
)
0.36
" Treatment-related gastrointestinal adverse events were greater in patients taking lopinavir/ritonavir."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.36
" Atazanavir/ritonavir had a better lipid profile and fewer gastrointestinal adverse events than lopinavir/ritonavir."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.36
" The adverse event rate was similar between arms (except drug hypersensitivity, reported more in the abacavir/lamivudine arm)."( Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study.
Branco, T; Cavassini, M; Domingo, P; Fisher, M; Givens, N; Khuong-Josses, MA; Lim, ML; Moyle, GJ; Norden, AG; Pearce, HC; Podzamczer, D; Post, FA; Rieger, A; Stellbrink, HJ; Vavro, C, 2010
)
0.36
" No increase in the overall adverse event rates was observed."( Effectiveness and safety of tenofovir gel, an antiretroviral microbicide, for the prevention of HIV infection in women.
Abdool Karim, Q; Abdool Karim, SS; Arulappan, N; Baxter, C; Frohlich, JA; Gengiah, TN; Grobler, AC; Kharsany, AB; Maarschalk, S; Mansoor, LE; Mlisana, KP; Mlotshwa, M; Morris, L; Omar, Z; Sibeko, S; Taylor, D, 2010
)
0.36
" Through 96 weeks, 77 subjects from each group discontinued prematurely; adverse or HIV-related events contributed to discontinuation of 36 subjects overall, with no significant differences between treatment groups."( Short communication: Comparable safety and efficacy with once-daily versus twice-daily dosing of lopinavir/ritonavir tablets with emtricitabine + tenofovir DF in antiretroviral-naïve, HIV type 1-infected subjects: 96 week final results of the randomized t
Bernstein, B; Cohen, D; da Silva, B; Fredrick, L; González-García, J; Johnson, M; Naylor, C; Sloan, L, 2010
)
0.36
" Renal biopsy revealed toxic acute tubular necrosis, with distinctive proximal tubular eosinophilic inclusions representing giant mitochondria visible by light microscopy."( Tenofovir nephrotoxicity: acute tubular necrosis with distinctive clinical, pathological, and mitochondrial abnormalities.
D'Agati, VD; Herlitz, LC; Markowitz, GS; Mohan, S; Radhakrishnan, J; Stokes, MB, 2010
)
0.36
" There were no significant adverse effects from these drugs and no alteration of renal function during the follow-up period."( Efficacy and safety of entecavir and/or tenofovir for prophylaxis and treatment of hepatitis B recurrence post-liver transplant.
de la Cruz-Lombardo, J; Jiménez-Pérez, M; Lozano-Rey, JM; Mongil Poce, L; Rodrigo-López, JM; Sáez-Gómez, AB, 2010
)
0.36
"Therapy with ETV and/or TDF seems to be efficient and safe when used in the prophylaxis and treatment of HBV recurrence after liver transplantation."( Efficacy and safety of entecavir and/or tenofovir for prophylaxis and treatment of hepatitis B recurrence post-liver transplant.
de la Cruz-Lombardo, J; Jiménez-Pérez, M; Lozano-Rey, JM; Mongil Poce, L; Rodrigo-López, JM; Sáez-Gómez, AB, 2010
)
0.36
" Adverse event rates were comparable between groups."( Efficacy and safety of entecavir versus adefovir in chronic hepatitis B patients with hepatic decompensation: a randomized, open-label study.
Beebe, S; Bialkowska, J; Brown, RS; Cheinquer, H; Cooney, E; Jeffers, L; Leung, N; Liaw, YF; Myers, RP; Peng, CY; Raptopoulou-Gigi, M; Sarin, SK; Tang, S; Tanwandee, T; Tsai, N, 2011
)
0.37
" In most patients, NUC need to be administered on a long-term basis, thus increasing the risk of adverse effects."( Drug safety evaluation of adefovir in HBV infection.
Colombo, M; Lampertico, P; Viganò, M, 2011
)
0.37
" Although, in short-term clinical trials, a daily dose of 10 mg of ADV was safe owing to a low rate of negligible nephrotoxic effects, the same dose may be associated with a usually reversible, proximal renal tubular toxicity as reflected by hypophosphatemia and elevated creatinine levels."( Drug safety evaluation of adefovir in HBV infection.
Colombo, M; Lampertico, P; Viganò, M, 2011
)
0.37
" Ten percent (13/123) of the subjects discontinued the treatment due to adverse events."( Evaluation of the safety and effectiveness of nevirapine plus coformulated tenofovir/emtricitabine as first-line therapy in routine clinical practice.
Blanch, J; Cervantes, M; Domingo, P; Ferrer, E; Knobel, H; Llibre, JM; Mallolas, J; Pedrol, E; Vallecillo, G, 2012
)
0.38
" All regimens were safe and well tolerated."( Pharmacokinetics and safety of single-dose tenofovir disoproxil fumarate and emtricitabine in HIV-1-infected pregnant women and their infants.
Bardeguez, A; Cotter, A; Fiscus, SA; Flynn, PM; Heckman, B; Huang, S; Jean-Philippe, P; Kearney, B; Mirochnick, M; Mofenson, LM; Purswani, M; Robbins, B; Rodman, J; Rooney, JF; Shapiro, DE; Thorpe, E; Van Rompay, KK; Watts, DH, 2011
)
0.37
" The occurrence of treatment-related, moderate/severe adverse events was similar between treatment groups through 48 weeks of treatment."( Examination of noninferiority, safety, and tolerability of lopinavir/ritonavir and raltegravir compared with lopinavir/ritonavir and tenofovir/ emtricitabine in antiretroviral-naïve subjects: the progress study, 48-week results.
Fredrick, LM; Gathe, J; Lawal, A; Nilius, AM; Podsadecki, TJ; Pulido, F; Reynes, J; Soto-Malave, R; Tian, M,
)
0.13
" There is a need for an effective and safe first-line regimen, to cope with the ever-increasing incidence of non-adherence and primary resistance."( WITHDRAWN. Effectiveness and safety of first-line tenofovir + emtricitabine + efavirenz for patients with HIV.
Okwundu, CI; Omeje, I, 2012
)
0.38
" More patients in the AZT-3TC group than in the TDF-FTC group had adverse events resulting in discontinuation of the study drugs (9% vs."( WITHDRAWN. Effectiveness and safety of first-line tenofovir + emtricitabine + efavirenz for patients with HIV.
Okwundu, CI; Omeje, I, 2012
)
0.38
"US-based prospective cohort study of HEU children to examine potential adverse effects of prenatal TDF exposure."( Safety of tenofovir use during pregnancy: early growth outcomes in HIV-exposed uninfected infants.
DiMeglio, LA; Griner, R; Hazra, R; Jacobson, DL; Kacanek, D; Mendez, H; Miller, T; Mofenson, LM; Rich, KC; Seage, GR; Siberry, GK; Tassiopoulos, K; Watts, DH; Williams, PL, 2012
)
0.38
" Conversely, known activators of autophagy, such as lithium and rapamycin, displayed neuroprotection against this toxic compound."( Role of autophagy inhibitors and inducers in modulating the toxicity of trimethyltin in neuronal cell cultures.
Biagioni, F; Fabrizi, C; Fornai, F; Fumagalli, L; Lenzi, P; Pompili, E; Somma, F, 2012
)
0.38
" Several studies suggest that NAs long-term administration have been associated with low rates of serious adverse events (AEs), including lactic acidosis, renal function impairment, osteopenia and osteoporosis."( Safety of long-term nucleos(t)ide treatment in chronic hepatitis B.
Ridruejo, E; Silva, MO, 2012
)
0.38
" ADV was safe and well-tolerated."( Efficacy and safety of long-term adefovir dipivoxil therapy in children with chronic hepatitis B infection.
Frederick, D; Jonas, MM; Kelly, D; Mizerski, J; Mondou, E; Pollack, H; Rousseau, F; Sokal, E; Sorbel, J, 2012
)
0.38
"Prolonged ADV treatment is safe in children."( Efficacy and safety of long-term adefovir dipivoxil therapy in children with chronic hepatitis B infection.
Frederick, D; Jonas, MM; Kelly, D; Mizerski, J; Mondou, E; Pollack, H; Rousseau, F; Sokal, E; Sorbel, J, 2012
)
0.38
"CXCR4 antagonist plerixafor (AMD3100, 1,1'-bis-1,4,8,11-tetraazacyclotetradekan) alone or combination with adefovir (PMEA, 9-(2-phosphonylmethoxyethyl)adenine) safe and effective for treating FIV-infected cats."( Efficacy and adverse effects of the antiviral compound plerixafor in feline immunodeficiency virus-infected cats.
Balzarini, J; Egberink, H; Hartmann, K; Klein, D; Stengel, C,
)
0.33
" There is a need for an effective and safe first-line regimen, to cope with the ever-increasing incidence of non-adherence and primary resistance."( WITHDRAWN: Effectiveness and safety of first-line tenofovir + emtricitabine + efavirenz for patients with HIV.
Okwundu, CI; Omeje, I, 2012
)
0.38
" More patients in the AZT-3TC group than in the TDF-FTC group had adverse events resulting in discontinuation of the study drugs (9% vs."( WITHDRAWN: Effectiveness and safety of first-line tenofovir + emtricitabine + efavirenz for patients with HIV.
Okwundu, CI; Omeje, I, 2012
)
0.38
" The incidence rates of adverse events between two groups were not statistically significant."( [The clinical efficacy and safety of adefovir dipivoxil in combination with bicyclol for the treatment of senior patients with chronic hepatitis B].
Cai, SP; Fan, ZP; He, WP; Ji, YJ; Zhang, WJ, 2011
)
0.37
" There was no significant increase of any genital adverse event in the tenofovir group."( Safety of tenofovir gel, a vaginal microbicide, in South African women: results of the CAPRISA 004 Trial.
Baxter, C; Frolich, J; Grobler, A; Karim, QA; Karim, SS; Kharsany, AB; Maarshalk, S; Mansoor, LE; Miya, N; Mlisana, K; Sibeko, S; Sokal, DC; Yende-Zuma, N, 2013
)
0.39
" With the increased realization of receptive anal intercourse among heterosexual couples often in conjunction with vaginal intercourse, having a safe and effective microbicide for both mucosal sites is critical."( Safety and efficacy of tenofovir/IQP-0528 combination gels - a dual compartment microbicide for HIV-1 prevention.
Buckheit, KW; Buckheit, RW; Dezzutti, CS; Gwozdz, G; Mahalingam, A; Shetler, C; Ugaonkar, SR, 2012
)
0.38
" Safety endpoints included clinical adverse events (AEs) and mucosal safety parameters."( RMP-02/MTN-006: A phase 1 rectal safety, acceptability, pharmacokinetic, and pharmacodynamic study of tenofovir 1% gel compared with oral tenofovir disoproxil fumarate.
Anton, PA; Bumpus, NN; Carballo-Diéguez, A; Cranston, RD; Cumberland, WG; Dennis, R; Elliott, J; Hendrix, CW; Janocko, L; Ju, C; Kashuba, A; Khanukhova, E; Mauck, C; McGowan, I; Richardson-Harman, N, 2012
)
0.38
" The rings were safe and exhibited sustained release at controlled rates over 28 days."( Safety and pharmacokinetics of intravaginal rings delivering tenofovir in pig-tailed macaques.
Baum, MM; Butkyavichene, I; Cortez, C; Gilman, J; Guenthner, P; Hendry, RM; Holder, A; Kennedy, S; Kopin, E; Malone, AM; Martin, A; McNicholl, J; Mitchell, J; Moss, JA; Nguyen, C; Pau, CP; Sinha, P; Smith, JM; Smith, TJ; Srinivasan, P, 2012
)
0.38
"(R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine (PMPDAP) is active against feline immunodeficiency virus (FIV) in vitro, and is less toxic than other acyclic nucleoside phosphonates."( Efficacy and adverse effects of (R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine in feline immunodeficiency virus-infected cats.
Hartmann, K; Justa, N; Klein, D; Mueller, RS; Sauter-Louis, C; Weber, K,
)
0.13
"PMPDAP is effective in naturally FIV-infected cats with minimal adverse effects."( Efficacy and adverse effects of (R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine in feline immunodeficiency virus-infected cats.
Hartmann, K; Justa, N; Klein, D; Mueller, RS; Sauter-Louis, C; Weber, K,
)
0.13
"Administration of PMPDAP was not associated with significant improvements in clinical, immunological, or virological parameters, but treatment was associated with adverse effects, mainly anemia."( Efficacy and adverse effects of (R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine in feline immunodeficiency virus-infected cats.
Hartmann, K; Justa, N; Klein, D; Mueller, RS; Sauter-Louis, C; Weber, K,
)
0.13
" Adverse events were mostly mild and no serious adverse events or drug discontinuations were reported."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
" Laboratory test results, clinical outcomes, and drug-related adverse events were compared among groups."( Long-term efficacy and safety of lamivudine, entecavir, and tenofovir for treatment of hepatitis B virus-related cirrhosis.
Akbal, E; Akin, E; Alkan, E; Ataseven, H; Aygün, C; Başar, O; Baykal, O; Coban, S; Demir, M; Gülşen, MT; Ibiş, M; Koçkar, MC; Köklü, S; Köksal, AŞ; Küçükazman, M; Nadir, I; Ozdil, K; Pürnak, T; Tuna, Y; Yildirim, B; Yüksel, I; Yüksel, O, 2013
)
0.39
"Tenofovir and entecavir are effective and safe for long-term use in patients with compensated or decompensated cirrhosis from HBV infection."( Long-term efficacy and safety of lamivudine, entecavir, and tenofovir for treatment of hepatitis B virus-related cirrhosis.
Akbal, E; Akin, E; Alkan, E; Ataseven, H; Aygün, C; Başar, O; Baykal, O; Coban, S; Demir, M; Gülşen, MT; Ibiş, M; Koçkar, MC; Köklü, S; Köksal, AŞ; Küçükazman, M; Nadir, I; Ozdil, K; Pürnak, T; Tuna, Y; Yildirim, B; Yüksel, I; Yüksel, O, 2013
)
0.39
"No significant adverse effects, including body weight loss, abnormal blood or biochemistry, were observed in rats treated with AZT or ADV."( [Assessment of mitochondrial toxicity induced by zidovudine and adefovir dipivoxil in rats].
Feng, XM; Huang, SM; Li, AY; Wang, BJ; Wang, JZ; Yang, DL; Zhu, B; Zhu, ZN, 2012
)
0.38
"Significant adverse effects related to mitochondrial toxicity were observed in rats treated with AZT."( [Assessment of mitochondrial toxicity induced by zidovudine and adefovir dipivoxil in rats].
Feng, XM; Huang, SM; Li, AY; Wang, BJ; Wang, JZ; Yang, DL; Zhu, B; Zhu, ZN, 2012
)
0.38
" Overall incidences of all-causality treatment-related or grade 3/4 adverse events (AEs) or AE-related discontinuations were lower with lersivirine than with efavirenz, and serious AEs occurred at similar rates across treatment groups."( Efficacy and safety of lersivirine (UK-453,061) versus efavirenz in antiretroviral treatment-naive HIV-1-infected patients: week 48 primary analysis results from an ongoing, multicenter, randomized, double-blind, phase IIb trial.
Cooper, DA; Craig, C; Goodrich, J; Kaplan, R; Lazzarin, A; Mori, J; Pozniak, A; Pulik, P; Tawadrous, M; Valdez, H; Vernazza, P; Wang, C; Weil, E, 2013
)
0.39
" No severe adverse events associated with entecavir or tenofovir were reported."( Efficacy and safety of entecavir and/or tenofovir in hepatitis B compensated and decompensated cirrhotic patients in clinical practice.
Arenas, J; Canós, AP; Díaz-Sánchez, A; Jiménez, M; Miquel, M; Núñez, Ó; Trapero-Marugán, M,
)
0.13
"Overall, 71 of 281 raltegravir recipients (25%) and 98 of 282 efavirenz recipients (35%) discontinued the study; discontinuations due to adverse events occurred in 14 (5%) and 28 (10%) patients in the respective groups."( Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naive HIV-1-infected patients: final 5-year results from STARTMRK.
DeJesus, E; DiNubile, MJ; Leavitt, R; Lennox, JL; Miller, M; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Yazdanpanah, Y, 2013
)
0.39
" Over the entire study, fewer patients experienced neuropsychiatric and drug-related adverse events in the raltegravir group than in the efavirenz group."( Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naive HIV-1-infected patients: final 5-year results from STARTMRK.
DeJesus, E; DiNubile, MJ; Leavitt, R; Lennox, JL; Miller, M; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Yazdanpanah, Y, 2013
)
0.39
" In conclusion, a combination of LAM and ADV initiated at the time of wait listing provides safe and effective protection against recurrent HBV infection without the high costs and inconvenience associated with long-term HBIG therapy."( Combination of lamivudine and adefovir without hepatitis B immune globulin is safe and effective prophylaxis against hepatitis B virus recurrence in hepatitis B surface antigen-positive liver transplant candidates.
Angus, PW; Gane, EJ; McCaughan, GW; Patterson, S; Strasser, SI, 2013
)
0.39
" HIV serostatus, clinical and laboratory adverse events (AEs), adherence (pill count, Medication Event Monitoring System, and self-report), and sexual and other sociobehavioral data were assessed at 3-month intervals for 24 months."( Randomized trial of clinical safety of daily oral tenofovir disoproxil fumarate among HIV-uninfected men who have sex with men in the United States.
Ackers, ML; Buchbinder, SP; Chillag, KL; Collins, BM; Grant, RM; Grohskopf, LA; Gvetadze, R; Liu, AY; Mayer, KH; Oʼhara, B; Pathak, SR; Paxton, LA; Rose, CE; Thompson, M, 2013
)
0.39
"To investigate 3-year antiviral efficacy and side effect of adefovir dipivoxil (ADV) on the old patients with hepatitis B chronic infection."( [Three-year efficacy and side effect of adefovir dipivoxil for the treatment of the old patients with chronic hepatitis B virus infection].
Lou, GQ; Lu, L; Qian, JC; Shi, JP; Yan, FL; Zhu, MF, 2012
)
0.38
"The way to treat with ADV is safe and effective for old patients with chronic hepatitis B virus infection."( [Three-year efficacy and side effect of adefovir dipivoxil for the treatment of the old patients with chronic hepatitis B virus infection].
Lou, GQ; Lu, L; Qian, JC; Shi, JP; Yan, FL; Zhu, MF, 2012
)
0.38
" There were no significant differences between the numbers of ≥ Grade 2 adverse events across the arms of the study."( A phase 1 randomized, double blind, placebo controlled rectal safety and acceptability study of tenofovir 1% gel (MTN-007).
Andrew, P; Ayudhya, RK; Carballo-Dieguez, A; Cranston, RD; Dai, JY; Hladik, F; Hoesley, C; Janocko, L; Mayer, K; McGowan, I; Piper, J, 2013
)
0.39
"The reduced glycerin formulation of tenofovir 1% gel was safe and well tolerated rectally and should be advanced to Phase 2 development."( A phase 1 randomized, double blind, placebo controlled rectal safety and acceptability study of tenofovir 1% gel (MTN-007).
Andrew, P; Ayudhya, RK; Carballo-Dieguez, A; Cranston, RD; Dai, JY; Hladik, F; Hoesley, C; Janocko, L; Mayer, K; McGowan, I; Piper, J, 2013
)
0.39
" We compared rates of upper digestive serious adverse events (sAEs) between TDF/FTC+EFV and TDF/FTC+ZDV patients during the first six months of treatment."( Early upper digestive tract side effects of zidovudine with tenofovir plus emtricitabine in West African adults with high CD4 counts.
Anglaret, X; Bohoussou, F; Carrou, JL; Danel, C; Eholie, SP; Gabillard, D; Konan, R; Moh, R; Ouattara, E; Peytavin, G, 2013
)
0.39
" We suggest that further early prescriptions of TDF+XTC+ZDV should be carefully monitored and that whenever possible, the rate of early upper digestive adverse events should be compared to that occurring in-patients taking other drug regimens."( Early upper digestive tract side effects of zidovudine with tenofovir plus emtricitabine in West African adults with high CD4 counts.
Anglaret, X; Bohoussou, F; Carrou, JL; Danel, C; Eholie, SP; Gabillard, D; Konan, R; Moh, R; Ouattara, E; Peytavin, G, 2013
)
0.39
"There were no colposcopic findings or adverse events attributable to either applicator."( A randomized, comparative safety study of a prefilled plastic and user-filled paper applicator with candidate microbicide tenofovir 1% gel.
Brache, V; Callahan, M; Cochon, L; Cohen, JA; Foster, J; Schwartz, J, 2013
)
0.39
" These findings suggest that HIV-infected cancer patients receiving nelfinavir might experience both enhanced antitumor efficacy and unexpected adverse toxicity given the role of MRP4/ABCC4 in exporting nucleoside-based antiretroviral medications and cancer chemotherapeutics."( Human immunodeficiency virus protease inhibitors interact with ATP binding cassette transporter 4/multidrug resistance protein 4: a basis for unanticipated enhanced cytotoxicity.
Ambudkar, SV; Cheepala, SB; Ekins, S; Fukuda, Y; Schuetz, JD; Sparreboom, A; Takenaka, K; Wu, CP, 2013
)
0.39
" Tenofovir gel, when used intermittently, was safe to use in women with HBV infection."( Safety of coitally administered tenofovir 1% gel, a vaginal microbicide, in chronic hepatitis B virus carriers: results from the CAPRISA 004 trial.
Abdool Karim, Q; Abdool Karim, SS; Baxter, C; Tshabalala, P; Yende-Zuma, N, 2013
)
0.39
"Combined prophylaxis with TDF/ETV nucleoside plus nucleotide analogs and cessation of immunoglobulin after liver transplantation in chronic hepatitis B is safe and effective."( Nucleoside plus nucleotide analogs and cessation of hepatitis B immunoglobulin after liver transplantation in chronic hepatitis B is safe and effective.
Braat, AE; Claas, EC; Coenraad, MJ; Knoester, M; van Hoek, B; Vossen, AC; Wesdorp, DJ, 2013
)
0.39
" We assessed adherence (compared between groups and with nonstudy controls) and clinical and adverse events at weeks 1, 2 and 4, and efficacy at week 12."( Raltegravir-emtricitabine-tenofovir as HIV nonoccupational post-exposure prophylaxis in men who have sex with men: safety, tolerability and adherence.
Carr, A; Ingersoll, A; McAllister, J; McNulty, A; Read, P; Tong, WW, 2014
)
0.4
" Although information is limited, TDF appears to be safe during pregnancy."( Safety of tenofovir during pregnancy for the mother and fetus: a systematic review.
Bulterys, M; Ellington, S; Kourtis, AP; Legardy-Williams, J; Wang, L, 2013
)
0.39
" Patients underwent serological analysis at 3-6 month intervals during treatment and follow-up to evaluate occurrence of adverse events; serological parameters included blood count, markers of liver, kidney and thyroid function, and levels of autoantibodies and creatine kinase."( [Efficacy and safety of peginterferon alfa-2a (40 kd) plus adefovir for 96 weeks in HBeAg-negative chronic hepatitis B patients].
Cao, ZH; Chen, XY; He, ZM; Jin, Y; Liu, YL; Lu, JF; Ma, LN; Zhang, YH, 2013
)
0.39
" The occurrences of adverse events were similar at week 48 and week 96."( [Efficacy and safety of peginterferon alfa-2a (40 kd) plus adefovir for 96 weeks in HBeAg-negative chronic hepatitis B patients].
Cao, ZH; Chen, XY; He, ZM; Jin, Y; Liu, YL; Lu, JF; Ma, LN; Zhang, YH, 2013
)
0.39
"6% interrupted cART due to adverse events,19."( Safety, efficacy, and persistence of emtricitabine/tenofovir versus other nucleoside analogues in naive subjects aged 50 years or older in Spain: the TRIP study.
Aguirrebengoa, K; Arazo, P; Blanco, JR; Caro-Murillo, AM; Castaño, MA; Domingo, P; Ferrer, P; Gómez-Sirvent, JL; Olalla, J; Pedrol, E; Portilla, J; Pulido, F; Riera, M; Romero-Palacios, A; Vera, F,
)
0.13
"In a population of HIV-infected subjects who were ≥50 years old, our study suggests that the use of FTC/TDF is generally safe and effective, with a longer persistence as compared to other regimens."( Safety, efficacy, and persistence of emtricitabine/tenofovir versus other nucleoside analogues in naive subjects aged 50 years or older in Spain: the TRIP study.
Aguirrebengoa, K; Arazo, P; Blanco, JR; Caro-Murillo, AM; Castaño, MA; Domingo, P; Ferrer, P; Gómez-Sirvent, JL; Olalla, J; Pedrol, E; Portilla, J; Pulido, F; Riera, M; Romero-Palacios, A; Vera, F,
)
0.13
"Due to ongoing neuropsychiatric adverse events in some efavirenz (EFV)-treated patients, a switch to an alternative non-nucleoside reverse transcriptase inhibitor may be considered."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
" No subjects discontinued the study due to an adverse event."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
" No significant adverse event was observed due to TDF administration; renal function pre- and post-LT were also acceptably preserved."( One year of hepatitis B immunoglobulin plus tenofovir therapy is safe and effective in preventing recurrent hepatitis B post-liver transplantation.
Lilly, LB; Renner, EL; Selzner, N; Tanaka, T; Therapondos, G, 2014
)
0.4
"The Toll-like receptor 7 (TLR7) activator imiquimod (IMQ) is safe and effective in treating actinic keratosis; however, an intermittent treatment regimen is necessary because of excessive local reactions."( Inhibition of keratinocyte proliferation by phospholipid-conjugates of a TLR7 ligand in a Myc-induced hyperplastic actinic keratosis model in the absence of systemic side effects.
Barberis, A; Carson, DA; Cottam, HB; Crain, B; Hayashi, T; Holldack, J; Kang, M; Keophilaone, V; Maj, R; Mura, E; Ochoa, R; Passini, N; Promessi, V; Yao, S,
)
0.13
"TMX-202 is safe and efficacious without causing excessive adverse effects, suggesting that it may be an alternative to Aldara for the treatment of proliferative skin conditions."( Inhibition of keratinocyte proliferation by phospholipid-conjugates of a TLR7 ligand in a Myc-induced hyperplastic actinic keratosis model in the absence of systemic side effects.
Barberis, A; Carson, DA; Cottam, HB; Crain, B; Hayashi, T; Holldack, J; Kang, M; Keophilaone, V; Maj, R; Mura, E; Ochoa, R; Passini, N; Promessi, V; Yao, S,
)
0.13
" Factors associated with these drug-related adverse events are poorly characterized."( Low body weight in females is a risk factor for increased tenofovir exposure and drug-related adverse events.
Baldelli, S; Castagnoli, L; Cattaneo, D; Clementi, E; Fucile, S; Galli, M; Gervasoni, C; Landonio, S; Meraviglia, P; Riva, A; Rizzardini, G, 2013
)
0.39
" There were no differences between the groups in terms of adverse events in mothers or congenital deformities, gestational age, height, or weight in infants."( Efficacy and safety of tenofovir disoproxil fumarate in pregnancy for the prevention of vertical transmission of HBV infection.
Ay, M; Ayaz, C; Barcin, T; Celen, MK; Dal, MS; Dal, T; Gulsun, S; Kalkanli, S; Kaya, S; Mert, D; Yildirim, N, 2013
)
0.39
"TDF therapy during the second or third trimester reduced perinatal transmission rates of HBV and no adverse events were observed in mothers or infants."( Efficacy and safety of tenofovir disoproxil fumarate in pregnancy for the prevention of vertical transmission of HBV infection.
Ay, M; Ayaz, C; Barcin, T; Celen, MK; Dal, MS; Dal, T; Gulsun, S; Kalkanli, S; Kaya, S; Mert, D; Yildirim, N, 2013
)
0.39
" The most commonly observed adverse events were headache, nausea and flatulence, which occurred similarly across the three groups."( Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase inhibitor tenofovir, in HIV-infected adults.
Coakley, D; Kearney, B; Lee, WA; Markowitz, M; Miller, MD; Ruane, P; Squires, K; Wulfsohn, M; Zhong, L; Zolopa, A, 2014
)
0.4
"TDF-based rescue treatment is effective in reducing HBV DNA levels and is safe for patients with CHB who failed prior antiviral treatments."( Efficacy and safety of tenofovir-based rescue therapy for chronic hepatitis B patients with previous nucleo(s/t)ide treatment failure.
Byun, KS; Choe, WH; Kim, JH; Kim, YS; Kwon, SY; Lee, CH; Lee, CI; Yeon, JE; Yoon, EL, 2014
)
0.4
" Most adverse events were mild in severity and considered unrelated to study drug."( Efficacy and safety of tenofovir disoproxil fumarate in Asian-Americans with chronic hepatitis B in community settings.
Bae, H; Chan, S; Lou, L; Pan, CQ; Trinh, H; Yao, A, 2014
)
0.4
" No adverse effects were observed by HB-110 cotreated with ADV."( Safety and immunogenicity of therapeutic DNA vaccine with antiviral drug in chronic HBV patients and its immunogenicity in mice.
Bae, SH; Im, SJ; Jang, JW; Jeong, SH; Kim, BM; Kim, CY; Seo, YB; Song, JS; Song, MJ; Suh, YS; Sung, YC; Yang, SH; Yoon, SK; You, CR, 2015
)
0.42
"HB-110 was safe and tolerable in CHB patients."( Safety and immunogenicity of therapeutic DNA vaccine with antiviral drug in chronic HBV patients and its immunogenicity in mice.
Bae, SH; Im, SJ; Jang, JW; Jeong, SH; Kim, BM; Kim, CY; Seo, YB; Song, JS; Song, MJ; Suh, YS; Sung, YC; Yang, SH; Yoon, SK; You, CR, 2015
)
0.42
" Tenofovir released from TDF undergoes active renal secretion via organic anion transporters (OAT1 and OAT3), leading to higher exposure of renal proximal tubules to tenofovir and a potential for renal adverse effects in a small subset of TDF-treated patients."( Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity.
Bam, RA; Cihlar, T; Yant, SR, 2014
)
0.4
" At treatment weeks 12, 24, 48?, 96, 144, 192, and 240 patients were tested for hepatitis B virus (HBV) DNA, HBeAg seroconversion and ALT normalization time; in addition, the incidence and type of adverse drug reactions were recorded."( [Long-term efficacy and safety of telbivudine as monotherapy and as combination therapy with adefovir dipivoxil in HBeAg-positive chronic hepatitis B patients].
Chang, L; Du, Y; Jia, T; Li, H; Li, W; Liu, L; Liu, Y; Peng, D, 2014
)
0.4
" The calculated LD50 was 442."( Acute and subchronic toxicity of arprinocid in Sprague-Dawley rats.
Jiang, S; Wang, X; Wu, H; Xiao, W; Xue, F; Yan, M; Zhang, C; Zhang, K, 2014
)
0.4
"TDF and ETV are similarly effective and safe in chronic HBV patients after 24 weeks and 48 weeks of anti-viral therapy."( Comparison of efficacy and safety of tenofovir and entecavir in chronic hepatitis B virus infection: a systematic review and meta-analysis.
Gao, Y; Ke, W; Liu, L; Yang, Y; Ye, X; Zhang, C; Zhou, S, 2014
)
0.4
" No adverse events were observed, and there were no toxicological findings."( Pharmacokinetics and preliminary safety study of pod-intravaginal rings delivering antiretroviral combinations for HIV prophylaxis in a macaque model.
Baum, MM; Brooks, AA; Butkyavichene, I; Dinh, CT; Lopez, G; Martin, A; Moss, JA; Smith, JM; Smith, TJ; Srinivasan, P, 2014
)
0.4
" Combination therapy with tenofovir plus entecavir in this setting with multidrug resistance is safe and effective."( Efficacy and safety of tenofovir in a kidney transplant patient with chronic hepatitis B and nucleos(t)ide multidrug resistance: a case report.
Shan, C; Wu, P; Yin, GQ, 2014
)
0.4
" Bayesian fixed-effect network meta-analysis models adjusting for the type of nucleoside reverse transcriptase inhibitor backbone (tenofovir disoproxil fumarate/emtricitabine [TDF/FTC] or abacavir/lamivudine [ABC/3TC]) were used to evaluate week 48 efficacy (HIV-RNA suppression to <50 copies/mL and change in CD4+ cells/µL) and safety (lipid changes, adverse events, and discontinuations due to adverse events) of DTG relative to all other treatments."( 48-week efficacy and safety of dolutegravir relative to commonly used third agents in treatment-naive HIV-1-infected patients: a systematic review and network meta-analysis.
Camejo, RR; Cuffe, R; Gilchrist, KA; Lim, JW; Nichols, G; Patel, DA; Pulgar, S; Snedecor, SJ; Stephens, J; Sudharshan, L; Tang, WY, 2014
)
0.4
" Dolutegravir had better or equivalent changes in total cholesterol, LDL, triglycerides, and lower odds of adverse events and discontinuation due to adverse events compared to all treatments."( 48-week efficacy and safety of dolutegravir relative to commonly used third agents in treatment-naive HIV-1-infected patients: a systematic review and network meta-analysis.
Camejo, RR; Cuffe, R; Gilchrist, KA; Lim, JW; Nichols, G; Patel, DA; Pulgar, S; Snedecor, SJ; Stephens, J; Sudharshan, L; Tang, WY, 2014
)
0.4
"This retrospective investigation carried out in Guangdong Province indicated that not only are anti-HBV drugs efficacious for blocking vertical transmission of HBV but also are safe for both mothers and infants when taken by fathers or mothers during the reproduction phases of insemination and pregnancy."( [Retrospective analysis of the efficacy and safety of anti-hepatitis B virus drugs taken during pregnancy in women from the Guangdong Province].
Chen, X; Gao, W; Li, D; Peng, J; Wen, F; Xia, J; Xu, C; Xu, M; Yao, Z, 2014
)
0.4
" Both TBQ and TBE are cytotoxic, but their toxic mechanisms have not been fully characterized."( Protective roles of aldo-keto reductase 1B10 and autophagy against toxicity induced by p-quinone metabolites of tert-butylhydroquinone in lung cancer A549 cells.
Bunai, Y; Chen, H; El-Kabbani, O; Endo, S; Hara, A; Ikari, A; Matsunaga, T; Nishiyama, A; Soda, M; Suyama, M; Tajima, K; Takemura, M, 2015
)
0.42
" This meta-analysis explored the frequency of discontinuation attributed to renal adverse events (AEs) in randomized, controlled clinical studies that used TDF-containing regimens for ART-naïve, HIV-infected patients."( Discontinuation of tenofovir disoproxil fumarate for presumed renal adverse events in treatment-naïve HIV-1 patients: meta-analysis of randomized clinical studies.
Canada, RB; Chonchol, M; Durr, J; Gallant, J; Hindman, J; Liu, H; Martin, P; Patel, K; Piontkowsky, D; Winston, J,
)
0.13
"One of the most common in vitro assays to evaluate the probability of a compound to cause adverse effects is a cytotoxicity assay."( Intracellular concentrations determine the cytotoxicity of adefovir, cidofovir and tenofovir.
Leach, KL; Piotrowski, M; Wang, R; Zhang, H; Zhang, X, 2015
)
0.42
" No subject experienced an adverse event that was serious or severe (grade 3/4)."( Twenty-eight day safety, antiviral activity, and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection.
Agarwal, K; Cheng, W; Flaherty, JF; Foster, GR; Fung, SK; Gane, EJ; Lawson, E; McHutchison, JG; Nguyen, TT; Ryder, SD; Sicard, E; Subramanian, GM; Zhao, S, 2015
)
0.42
"Tenofovir alafenamide was safe and well tolerated; declines in HBV DNA were similar to tenofovir disoproxil fumarate at all doses evaluated."( Twenty-eight day safety, antiviral activity, and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection.
Agarwal, K; Cheng, W; Flaherty, JF; Foster, GR; Fung, SK; Gane, EJ; Lawson, E; McHutchison, JG; Nguyen, TT; Ryder, SD; Sicard, E; Subramanian, GM; Zhao, S, 2015
)
0.42
" During the open-label phase, grade 3/4 drug-related adverse events were uncommon (1."( Seven-year efficacy and safety of treatment with tenofovir disoproxil fumarate for chronic hepatitis B virus infection.
Aguilar Schall, R; Buti, M; Charuworn, P; Flaherty, JF; Flisiak, R; Gane, E; Gurel, S; Kitrinos, KM; Krastev, Z; Marcellin, P; Martins, EB; Petersen, J; Subramanian, GM; Tsai, N, 2015
)
0.42
" No cases of acute renal failure associated with TDF or LAM, mild or serious adverse events, or HBV recurrence were observed among the patients."( The efficacy and safety of tenofovir in the prevention of hepatitis B virus recurrence following liver transplantation.
Akarsu, M; Astarcıoğlu, İ; Hakim, GD; Karademir, S; Unek, T, 2014
)
0.4
"The results of this study, after a 36-month follow-up period, were encouraging and demonstrated that TDF therapy is safe and efficacious in treating HBV-positive organ transplant patients."( The efficacy and safety of tenofovir in the prevention of hepatitis B virus recurrence following liver transplantation.
Akarsu, M; Astarcıoğlu, İ; Hakim, GD; Karademir, S; Unek, T, 2014
)
0.4
" Docetaxel produced significant toxicity in PC-3 cells but was not toxic to LNCaP cells."( Paradoxical effects of the autophagy inhibitor 3-methyladenine on docetaxel-induced toxicity in PC-3 and LNCaP prostate cancer cells.
Anoopkumar-Dukie, S; Bernaitis, N; Chess-Williams, R; Christie, D; Davey, AK; Forbes, A; McDermott, CM; McFarland, AJ; Perkins, AV; Pickard, RD; Spencer, BH, 2015
)
0.66
"Inhibition of early steps of autophagy by 3-MA or Beclin 1 knockdown decreased the toxic effect of arsenic trioxide (ATO) in GBM cell lines."( Impact of autophagy inhibition at different stages on cytotoxic effect of autophagy inducer in glioblastoma cells.
Bi, Y; Chen, X; Cho, K; Hou, X; Li, C; Liu, H; Liu, Y; Peng, F; Shen, C; Wang, K; Wang, X; Yang, Z; Zhang, J; Zhang, W; Zhang, X; Zhao, S; Zheng, Z; Zhong, C; Zou, H, 2015
)
0.42
" No subjects discontinued study drug because of an adverse event in the 48 weeks of randomized phase."( A randomized, open-label study of the safety and efficacy of switching stavudine or zidovudine to tenofovir disoproxil fumarate in HIV-1-infected children with virologic suppression.
Arterburn, S; Castaño, E; Cheng, AK; Chuck, SL; Church, J; Deville, J; Enejosa, JV; Estripeaut, D; Gaur, A; Rathore, M; Rhee, MS; Saez-Llorens, X; White, K, 2015
)
0.42
" No serious adverse event related to tenofovir."( Efficacy, safety and pharmacokinetics of tenofovir disoproxil fumarate in virologic-suppressed HIV-infected children using weight-band dosing.
Aurpibul, L; Chokephaibulkit, K; Cressey, TR; Phongsamart, W; Sirisanthana, V; Sricharoenchai, S; Sudjaritruk, T; Wittawatmongkol, O, 2015
)
0.42
"TDF substitution in children and adolescents who were otherwise stable while receiving a first-line nonnucleoside reverse transcriptase inhibitor-based regimen achieved adequate exposure without clinically significant renal or bone adverse events over 96 weeks."( Efficacy, safety and pharmacokinetics of tenofovir disoproxil fumarate in virologic-suppressed HIV-infected children using weight-band dosing.
Aurpibul, L; Chokephaibulkit, K; Cressey, TR; Phongsamart, W; Sirisanthana, V; Sricharoenchai, S; Sudjaritruk, T; Wittawatmongkol, O, 2015
)
0.42
" The FDA-recommended rabbit vaginal irritation (RVI) model serves as a first line selection tool for vaginal products; however, for decades it has been limited to histopathology scoring, insufficient to select safe anti-HIV microbicides."( A quantitative multiplex nuclease protection assay reveals immunotoxicity gene expression profiles in the rabbit model for vaginal drug safety evaluation.
Chandra, N; Doncel, GF; Fichorova, RN; Mendonca, K; Murray, R; Yamamoto, HS, 2015
)
0.42
" Adverse events and serious adverse events were summarised by treatment group."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" Adverse events were reported by 291 (91%) of 321 patients in the efavirenz 400 mg group and by 285 (92%) of 309 in the 600 mg group (p=0·48)."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" Fewer efavirenz-related adverse events were reported with the 400 mg efavirenz dose than with the 600 mg dose."( Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study.
Amin, J; Belloso, W; Carey, D; Cooper, DA; Crabtree-Ramirez, B; Emery, S; Foulkes, S; Jessen, H; Kumar, S; Lee, MP; Losso, M; Mohapi, L; Phanupak, P; Puls, R; Winston, A, 2015
)
0.42
" The most frequent adverse events (any grade) were diarrhea (70%), infusion-related reaction (45%), and peripheral sensory neuropathy (44%)."( Safety and activity of BTK inhibitor ibrutinib combined with ofatumumab in chronic lymphocytic leukemia: a phase 1b/2 study.
Andritsos, LA; Blum, KA; Byrd, JC; Flynn, JM; Grever, MR; Hall, N; Heerema, NA; Jaglowski, SM; James, DF; Johnson, AJ; Jones, JA; Lozanski, G; Maddocks, KJ; Munneke, B; Nagar, V; Neuenburg, JK; Ruppert, AS; Smucker, K; Stefanos, M; West, JS; Woyach, JA, 2015
)
0.42
"The directed application of the normal nucleobase uracil to the squamous cells of the oral mucosa and palms and soles together with the delivery of the normal nucleobase adenine to the columnar cells of the GI tract may enable the safe delivery of higher 5FU dose intensity."( Differential nucleobase protection against 5-fluorouracil toxicity for squamous and columnar cells: implication for tissue function and oncogenesis.
Albrecht, P; Ford, JP; Kamerow, H; Mandetta, D; Thompson, JT; Vanden Heuvel, JP, 2015
)
0.61
" Discontinuation of ibrutinib is rarely due to adverse events related to the drug."( The clinical safety of ibrutinib in chronic lymphocytic leukemia.
Molica, S, 2015
)
0.42
"The applicability of Density Functional Theory (DFT) based descriptors for the development of quantitative structure-toxicity relationships (QSTR) is assessed for two different series of toxic aromatic compounds, viz."( Toxicity prediction of PHDDs and phenols in the light of nucleic acid bases and DNA base pair interaction.
Mondal Roy, S; Roy, DR; Sahoo, SK, 2015
)
0.42
"Ibrutinib is associated with bleeding-related adverse events of grade ≤ 2 in severity, and infrequently with grade ≥ 3 events."( Incidence and risk factors of bleeding-related adverse events in patients with chronic lymphocytic leukemia treated with ibrutinib.
Cullinane, AM; Farooqui, MZ; Herman, SE; Holland, SM; Lipsky, AH; Lozier, JN; Marti, G; Martyr, S; Nghiem, K; Niemann, CU; Saba, N; Soto, S; Sun, C; Tian, X; Uzel, G; Valdez, J; Wiestner, A, 2015
)
0.42
" The most common (≥ 20% patients) adverse events were neutropenia, anemia, nasopharyngitis, increased bilirubin, and rash."( Safety and tolerability of ibrutinib monotherapy in Japanese patients with relapsed/refractory B cell malignancies.
Aoki, T; Ishizawa, K; Morishita, T; Munakata, W; Ogura, M; Suzuki, T; Takahara, S; Tobinai, K; Uchida, T; Ushijima, Y, 2016
)
0.43
" The N-glycosylation of the lectin involves a plant-specific glycan while that in toxic type II RIPs of known structure involves a glycan which is animal as well as plant specific."( Structural studies on a non-toxic homologue of type II RIPs from bitter gourd: Molecular basis of non-toxicity, conformational selection and glycan structure.
Chandran, T; Sharma, A; Vijayan, M, 2015
)
0.42
" We report a serious side effect of ibrutinib potentially attributable to interaction with the moderate CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.43
"This is the first description of a serious side effect of ibrutinib likely due to an interaction with the CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.43
" Often, renal adverse effects are recognized only during clinical stages of drug development."( A Human Renal Proximal Tubule Cell Line with Stable Organic Anion Transporter 1 and 3 Expression Predictive for Antiviral-Induced Toxicity.
Hilgendorf, C; Jansen, K; Masereeuw, R; Nieskens, TT; Peters, JG; Röring, M; Schreurs, MJ; Smits, N; van der Made, TK; Wilmer, MJ; Woestenenk, R, 2016
)
0.43
" The toxic response in cells either pretreated with PCB 52 and then treated with GO or concurrently treated with GO and PCB 52 did not differ significantly from the toxic response in the cells treated with PCB 52 alone."( Graphene Oxide Attenuates the Cytotoxicity and Mutagenicity of PCB 52 via Activation of Genuine Autophagy.
Chen, S; Dai, H; Deng, Z; Du, H; Hei, TK; Liu, Y; Nie, Y; Wang, J; Wang, M; Wang, X; Wu, L; Xu, A, 2016
)
0.43
" However, tenofovir disoproxil fumarate is associated with renal and bone toxic effects; the novel prodrug tenofovir alafenamide achieves 90% lower plasma tenofovir concentrations."( Efficacy and safety of tenofovir alafenamide versus tenofovir disoproxil fumarate given as fixed-dose combinations containing emtricitabine as backbones for treatment of HIV-1 infection in virologically suppressed adults: a randomised, double-blind, activ
Abram, ME; Brinson, C; Cheng, AK; Clumeck, N; Daar, ES; DeJesus, E; Gallant, JE; Johnson, M; Morales-Ramirez, J; Osiyemi, O; Plummer, A; Raffi, F; Rhee, MS; Ruane, P; Ward, D; Yan, M, 2016
)
0.43
" Seven patients in the tenofovir alafenamide (2%) and three (1%) in the tenofovir disoproxil fumarate group discontinued due to adverse events."( Efficacy and safety of tenofovir alafenamide versus tenofovir disoproxil fumarate given as fixed-dose combinations containing emtricitabine as backbones for treatment of HIV-1 infection in virologically suppressed adults: a randomised, double-blind, activ
Abram, ME; Brinson, C; Cheng, AK; Clumeck, N; Daar, ES; DeJesus, E; Gallant, JE; Johnson, M; Morales-Ramirez, J; Osiyemi, O; Plummer, A; Raffi, F; Rhee, MS; Ruane, P; Ward, D; Yan, M, 2016
)
0.43
" There were no discontinuations due to adverse events."( Pharmacokinetics and Safety of Tenofovir Alafenamide in HIV-Uninfected Subjects with Severe Renal Impairment.
Custodio, JM; Fordyce, M; Garner, W; Kearney, BP; Ling, KH; Ramanathan, S; Vimal, M, 2016
)
0.43
" A total of 8/16 patients (50%) had at least one grade 3 adverse event (AE), and 5 (31."( Efficacy and safety of ibrutinib in Japanese patients with relapsed or refractory mantle cell lymphoma.
Choi, I; Fukuhara, N; Hatake, K; Ishikawa, T; Kinoshita, T; Kitano, T; Maruyama, D; Matsuno, Y; Nagai, H; Nishikawa, T; Nishikori, M; Shibayama, H; Takahara, S; Tobinai, K; Uchida, T, 2016
)
0.43
" MTX was more toxic in equivalent concentrations in all cytotoxicity tests performed [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide reduction, neutral red uptake, and lactate dehydrogenase release assays] and times tested (24 and 48 h)."( Naphthoquinoxaline metabolite of mitoxantrone is less cardiotoxic than the parent compound and it can be a more cardiosafe drug in anticancer therapy.
Bastos, ML; Carvalho, F; Carvalho, RA; Costa, VM; Gomes, AS; Pinto, M; Reis-Mendes, A; Remião, F; Sousa, E, 2017
)
0.46
"TAF has a similar tolerability, safety, and effectiveness to TDF and probably less adverse events related to renal and bone density outcomes in the treatment of naive and experienced patients with HIV-1."( The efficacy and safety of tenofovir alafenamide versus tenofovir disoproxil fumarate in antiretroviral regimens for HIV-1 therapy: Meta-analysis.
Lu, X; Wang, H; Xu, N; Yang, X, 2016
)
0.43
" The regimen was well tolerated and no discontinuations related to adverse events occurred."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
"Long-term TDF treatment appears to be safe and effective in patients with prior failure of LAM and a suboptimal response to ADV therapy."( Five-year efficacy and safety of tenofovir-based salvage therapy for patients with chronic hepatitis B who previously failed LAM/ADV therapy.
Angus, P; Bowden, S; Desmond, P; George, J; Lee, A; Lim, L; Locarnini, S; Marion, K; Nicoll, A; Patterson, S; Roberts, S; Sievert, W; Strasser, S; Thompson, A, 2017
)
0.46
"To improve biosafety of clinical analysis, we used antiviral drugs of adefovir and tenofovir as model drugs and developed a safe pretreatment method combining sealing technique with direct injection technique."( A novel pretreatment method combining sealing technique with direct injection technique applied for improving biosafety.
An, J; Du, C; Gao, JL; Jiang, Y; Li, M; Ma, H; Wang, X; Zhang, L, 2017
)
0.46
" Safety was consistent with prior experience for each drug, with infusion reactions the most prevalent adverse event."( Ublituximab (TG-1101), a novel glycoengineered anti-CD20 antibody, in combination with ibrutinib is safe and highly active in patients with relapsed and/or refractory chronic lymphocytic leukaemia: results of a phase 2 trial.
Brooks, HD; Burke, JM; Fanning, S; Farber, CM; Greenwald, DR; Klein, L; Kolibaba, KS; Mahadevan, D; Miskin, HP; Schreeder, MT; Sharman, JP; Sportelli, P; Weiss, MS, 2017
)
0.46
"Our results demonstrate the efficacy of switching to TDF monotherapy in virologically suppressed CHB patients receiving long-term LAM+ADV therapy, with a low rate of adverse events."( Long-term efficacy and safety of switching from lamivudine+adefovir to tenofovir disoproxil fumarate in virologically suppressed patients.
Angarano, G; Fasano, M; Fiore, JR; Leone, A; Maggi, P; Santantonio, TA; Volpe, A, 2017
)
0.46
" With remarkable efficacy, good oral bioavailability, and modest adverse events profile, ibrutinib use is likely to continue to increase."( Ibrutinib in CLL: a focus on adverse events, resistance, and novel approaches beyond ibrutinib.
Kaur, V; Swami, A, 2017
)
0.46
" In this report, we use metabolomics and proteomics with HK-2 cells and animal models to dissect the molecular pathways underlying nephropathy caused by TFV and its more toxic analog, adefovir (ADV)."( Tenofovir and adefovir down-regulate mitochondrial chaperone TRAP1 and succinate dehydrogenase subunit B to metabolically reprogram glucose metabolism and induce nephrotoxicity.
Chen, J; Chen, L; Cheng, L; Chi, W; Deng, H; Huo, Y; Lan, Z; Liu, X; Siegenthaler, JA; Song, W; Sun, K; Xu, L; Zhao, X, 2017
)
0.46
" Adverse events (AEs) including cytokine release syndrome AEs (CytoRS-AEs) and nasal symptoms were assessed."( Safety and pharmacodynamics of intranasal GSK2245035, a TLR7 agonist for allergic rhinitis: A randomized trial.
Ellis, AK; Lee, LA; Powley, W; Quint, D; Tsitoura, DC, 2017
)
0.46
"Recent toxicological assessments of graphene, graphene oxides, and some other two-dimensional (2D) materials have shown them to be substantially toxic at the nanoscale, where they inhibit and eventually disrupt biological processes."( Gauging the Nanotoxicity of h2D-C
Bhattacharyya, K; Datta, A; Mukhopadhyay, TK, 2018
)
0.48
" The overall incidence and severity of adverse events was similar between groups, although headache occurred more frequently in the bictegravir group than in the boosted protease inhibitor group."( Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentre, ph
Andreatta, K; Cheng, A; Creticos, C; Crofoot, G; Custodio, J; Daar, ES; DeJesus, E; Graham, H; Koenig, E; Liu, YP; Martin, H; Molina, JM; Oguchi, G; Quirk, E; Rockstroh, JK; Ruane, P, 2018
)
0.48
"Fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide might be a safe and efficacious alternative to continued boosted protease inhibitor therapy in adults with HIV-1 infection."( Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentre, ph
Andreatta, K; Cheng, A; Creticos, C; Crofoot, G; Custodio, J; Daar, ES; DeJesus, E; Graham, H; Koenig, E; Liu, YP; Martin, H; Molina, JM; Oguchi, G; Quirk, E; Rockstroh, JK; Ruane, P, 2018
)
0.48
"Oligomerization of human islet amyloid polypeptide (hIAPP) is toxic and contributes to progressive reduction of β cell mass in patients with type 2 diabetes mellitus."( ROS‑mediated autophagy through the AMPK signaling pathway protects INS‑1 cells from human islet amyloid polypeptide‑induced cytotoxicity.
Jin, Y; Li, X; Xia, G; Xiao, J; Zhou, J; Zhu, T, 2018
)
0.48
" Although generally well tolerated, here we describe our institutional experience of unique adverse effects encountered with the use of ibrutinib in patients with B-cell lymphomas."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
"This is a retrospective observational study done at a tertiary care facility, to evaluate adverse events in patients with B-cell malignancies on treatment with ibrutinib between 2014 and 2018."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
"We found 10 patients with unique adverse events related to ibrutinib."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
"We conducted an integrated safety analysis to characterize the frequency, severity, natural history, and outcomes of adverse events (AEs) with ibrutinib versus comparators."( Safety Analysis of Four Randomized Controlled Studies of Ibrutinib in Patients With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma or Mantle Cell Lymphoma.
Barr, PM; Burger, JA; Chang, S; Coutre, S; Cramer, P; Dilhuydy, MS; Fraser, G; Graef, T; Hess, G; Hillmen, P; Howes, A; James, DF; Liu, E; Moreno, C; O'Brien, S; Patel, K; Styles, L; Tedeschi, A; Valentino, R; Vermeulen, J, 2018
)
0.48
" Our data demonstrated that while the animals in the recovery state showed a significant trend to decreased oxidative damage, normalized antioxidative system and ameliorated endoplasmic reticulum (ER) stress compared with Dox-induced toxic model, 3-MA treatment abrogated the recovering process, resulting in sustained oxidative and ER stress and neuronal apoptosis."( The involvement of autophagic flux in the development and recovery of doxorubicin-induced neurotoxicity.
Dang, R; Guo, Y; Jiang, P; Li, G; Liu, Y; Qiao, Y; Xie, R; Xu, P; Zhou, X, 2018
)
0.48
" An animal model (where male and female rats were administered 21 and 10 mg per kg animal per day of eritadenine) indicated that intake of the compound was safe under these concentrations; it reached the liver and reduced the atherogenic index (TC/HDL) in rat sera."( Effect of traditional and modern culinary processing, bioaccessibility, biosafety and bioavailability of eritadenine, a hypocholesterolemic compound from edible mushrooms.
Largo, C; Morales, D; Piris, AJ; Polo, G; Soler-Rivas, C; Tabernero, M, 2018
)
0.91
" The most common all-grade adverse events were diarrhoea (47 [33%] of 141 patients), neutropenia (44 [31%]), and fatigue (37 [26%])."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
" Here side effects of ibrutinib have been summarized and important considerations in the management of these adverse events have been reviewed."( Management of adverse effects/toxicity of ibrutinib.
Paydas, S, 2019
)
0.51
"We pooled clinical renal safety data across 26 treatment-naive and antiretroviral switch studies to compare the incidence of proximal renal tubulopathy and discontinuation due to renal adverse events between participants taking TAF-containing regimens vs."( Renal safety of tenofovir alafenamide vs. tenofovir disoproxil fumarate: a pooled analysis of 26 clinical trials.
Arribas, JR; Brainard, D; Carter, C; Clarke, AE; Das, M; Elion, RA; Eron, JJ; Esser, S; Guo, S; Gupta, SK; Martin, H; Mudrikova, T; Negredo, E; Orkin, C; Podzamczer, D; Post, FA; Pozniak, AL; Rockstroh, JK; Sax, PE; SenGupta, D; Stellbrink, HJ; Waters, L; Wohl, DA; Zhong, L, 2019
)
0.51
"001) discontinued due to a renal adverse event."( Renal safety of tenofovir alafenamide vs. tenofovir disoproxil fumarate: a pooled analysis of 26 clinical trials.
Arribas, JR; Brainard, D; Carter, C; Clarke, AE; Das, M; Elion, RA; Eron, JJ; Esser, S; Guo, S; Gupta, SK; Martin, H; Mudrikova, T; Negredo, E; Orkin, C; Podzamczer, D; Post, FA; Pozniak, AL; Rockstroh, JK; Sax, PE; SenGupta, D; Stellbrink, HJ; Waters, L; Wohl, DA; Zhong, L, 2019
)
0.51
" In the period between Year 8 and Year 10, the safety profile of TDF was similar to previous reports, with few patients experiencing renal- or bone-related adverse events."( Ten-year efficacy and safety of tenofovir disoproxil fumarate treatment for chronic hepatitis B virus infection.
Buggisch, P; Buti, M; Cathcart, AL; Crans, G; Flaherty, J; Flisiak, R; Gaggar, A; Jump, B; Kaita, K; Krastev, Z; Lee, SS; Manns, M; Marcellin, P; Op den Brouw, M; Petersen, J; Sievert, W; Wong, DK, 2019
)
0.51
" Emerging real-world-data shows similar response and survival, but higher discontinuation rates due to adverse events (AEs)."( Safety and efficacy analysis of long-term follow up real-world data with ibrutinib monotherapy in 58 patients with CLL treated in a single-center in Greece.
Angelopoulou, M; Bitsani, C; Dimou, M; Iliakis, T; Kalyva, S; Koudouna, A; Kyrtsonis, MC; Panayiotidis, P; Papaioannou, P; Pardalis, V; Tsaftaridis, P; Vassilakopoulos, TP, 2019
)
0.51
" In the integrated analysis (ibrutinib treatment up to 43 months), the most common adverse events (AEs) were primarily grade 1/2; diarrhea (n = 173, 52% any-grade; n = 15, 5% grade 3) and fatigue (n = 119, 36% any-grade; n = 10, 3% grade 3)."( Long-term safety of single-agent ibrutinib in patients with chronic lymphocytic leukemia in 3 pivotal studies.
Barr, PM; Barrientos, JC; Burger, JA; Byrd, JC; Chang, S; Coutre, SE; Dean, JP; Devereux, S; Furman, RR; Ghia, P; Hillmen, P; James, DF; Kipps, TJ; Moreno, C; O'Brien, SM; O'Dwyer, M; Robak, T; Schuh, A; Valentino, R, 2019
)
0.51
" However, less attention has been put on their adverse events."( Bayesian Network Meta-Analysis for Assessing Adverse Effects of Anti-hepatitis B Drugs.
Ji, J; Jia, Y; Shen, Y; Xun, P; Zhou, J, 2019
)
0.51
" Poisson-prior-based Bayesian NMA was performed to synthesize both direct and indirect evidence with reporting hazard ratios (HRs) and 95% credible intervals (CrIs) for serious adverse events (SAEs) and hepatic/renal impairments."( Bayesian Network Meta-Analysis for Assessing Adverse Effects of Anti-hepatitis B Drugs.
Ji, J; Jia, Y; Shen, Y; Xun, P; Zhou, J, 2019
)
0.51
" Few discontinued due to adverse events (2% D/C/F/TAF arm)."( Week 96 efficacy and safety results of the phase 3, randomized EMERALD trial to evaluate switching from boosted-protease inhibitors plus emtricitabine/tenofovir disoproxil fumarate regimens to the once daily, single-tablet regimen of darunavir/cobicistat/
Brown, K; Cunningham, D; De Wit, S; Eron, JJ; Hufkens, V; Jezorwski, J; Lathouwers, E; Opsomer, M; Orkin, C; Petrovic, R; Post, FA; Pulido, F; Van Landuyt, E, 2019
)
0.51
"There are limited data on treatment patterns, adverse events (AEs), and economic burden in younger, commercially insured patients treated for mantle cell lymphoma (MCL)."( Treatment patterns, adverse events, healthcare resource use and costs among commercially insured patients with mantle cell lymphoma in the United States.
Burudpakdee, C; Kabadi, SM; Near, A; Wada, K, 2019
)
0.51
" The most frequent treatment-emergent adverse events (AEs) in patients with FL and DLBCL, respectively, were diarrhea (16 [59%]; 16 [47%]), fatigue (12 [44%]; 16 [47%]), nausea (9 [33%]; 12 [35%]), peripheral edema (7 [26%]; 13 [38%]), decreased appetite (8 [30%]; 11 [32%]), neutropenia (6 [22%]; 11 [32%]), and vomiting (5 [19%]; 12 [35%])."( Safety and activity of ibrutinib in combination with durvalumab in patients with relapsed or refractory follicular lymphoma or diffuse large B-cell lymphoma.
Goy, A; Guan, S; Herrera, AF; Hill, JS; Kwei, K; Liu, EA; Mehta, A; Pagel, JM; Phillips, T; Ramchandren, R; Svoboda, J, 2020
)
0.56
" Common grade ≥3 adverse events (AEs) included neutropenia (13%), pneumonia (12%), hypertension (8%), anemia (7%), and hyponatremia (6%); occurrence of most events as well as discontinuations due to AEs decreased over time."( Long-term efficacy and safety of first-line ibrutinib treatment for patients with CLL/SLL: 5 years of follow-up from the phase 3 RESONATE-2 study.
Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dai, S; Dean, JP; Devereux, S; Ghia, P; Grosicki, S; Hillmen, P; Kipps, TJ; Lal, I; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Simpson, D; Tedeschi, A, 2020
)
0.56
" Outcomes assessed included overall response rate (ORR), complete response (CR) rate, overall survival (OS), progression-free survival (PFS), and adverse events."( Matching-adjusted Indirect Comparisons of the Efficacy and Safety of Acalabrutinib Versus Other Targeted Therapies in Relapsed/Refractory Mantle Cell Lymphoma.
Abhyankar, S; Kabadi, SM; Signorovitch, J; Song, J; Telford, C; Yao, Z; Zhao, J, 2019
)
0.51
" No subject experienced a serious adverse event or nephrotoxicity."( Safety, efficacy, and pharmacokinetics of pradefovir for the treatment of chronic hepatitis B infection.
Chen, H; Ding, Y; Jin, W; Li, C; Li, X; Liu, C; Liu, J; Niu, J; Wu, M; Zhang, D; Zhang, H; Zhu, X, 2020
)
0.56
" Drug-related grade ≥2 adverse events and withdrawals due to adverse events occurred in 17 (4."( Efficacy and Safety of Switching to Dolutegravir/Lamivudine Fixed-Dose 2-Drug Regimen vs Continuing a Tenofovir Alafenamide-Based 3- or 4-Drug Regimen for Maintenance of Virologic Suppression in Adults Living With Human Immunodeficiency Virus Type 1: Phas
Aboud, M; Ait-Khaled, M; Ajana, F; Bisshop, F; De Wit, S; Gartland, MJ; Nascimento, MC; Osiyemi, O; Pappa, KA; Portilla Sogorb, J; Routy, JP; Smith, KY; Tenorio, AR; van Wyk, J; Wang, R; Wright, J; Wyen, C; Wynne, B, 2020
)
0.56
" Both treatments were safe and well-tolerated, and most adverse events were similar as mild to moderate in severity."( Efficacy and safety of the regimens containing tenofovir alafenamide versus tenofovir disoproxil fumarate in fixed-dose single-tablet regimens for initial treatment of HIV-1 infection: A meta-analysis of randomized controlled trials.
Chen, Y; Lu, Y; Tao, X; Zhang, L; Zhou, Y, 2020
)
0.56
" The purpose of this study was to describe treatment patterns, adverse events (AEs), and economic burden among treated patients with CLL."( Real-World Treatment Patterns, Adverse Events, Resource Use, and Costs Among Commercially Insured, Younger Patients with Chronic Lymphocytic Leukemia in the USA: A Retrospective Cohort Study.
Burudpakdee, C; Kabadi, SM; Near, A; Wada, K, 2020
)
0.56
"6 % patients experienced ≥ grade 3 adverse events and serious adverse events."( Efficacy and safety of ibrutinib in diffuse large B-cell lymphoma: A single-arm meta-analysis.
Fang, H; Feng, Y; Hou, K; Huang, L; Jia, Y; Shao, S; Yu, Z, 2020
)
0.56
" Patient characteristics, ibrutinib use and adverse drug reactions (ADRs) were collected from medical records."( Patterns of use and safety of ibrutinib in real-life practice.
Allouchery, M; Delaunay, P; Delwail, V; Guidez, S; Lafay-Chebassier, C; Pérault-Pochat, MC; Salvo, F; Tomowiak, C, 2021
)
0.62
" These findings provide reassurance that the combination of TAF, boosted PIs and ledipasvir/sofosbuvir is safe in HIV/HCV-coinfected populations."( Pharmacokinetics and renal safety of tenofovir alafenamide with boosted protease inhibitors and ledipasvir/sofosbuvir.
Anderson, PL; Blum, J; Brooks, KM; Bushman, LR; Castillo-Mancilla, JR; Cendali, F; Choi, YJ; Gomez, J; Haas, H; Ibrahim, ME; Johnson, B; Kiser, JJ; MaWhinney, S; Morrow, M; Roon, L; Rowan, SE; Wyles, DL; Zheng, JH, 2020
)
0.56
" Secondary assessments included maternal HBV DNA reduction at delivery, and maternal or infant adverse events during follow up."( Efficacy and safety of tenofovir alafenamide fumarate for preventing mother-to-child transmission of hepatitis B virus: a national cohort study.
Cao, L; Chen, B; Chen, R; Ding, Y; Fan, J; Gan, W; Huang, Y; Lin, C; Liu, Y; Pan, CQ; Sheng, Q; Wang, S; Wang, Y; Zhu, L, 2020
)
0.56
" No severe adverse effects were reported in either mothers or infants."( Efficacy and safety of tenofovir alafenamide fumarate for preventing mother-to-child transmission of hepatitis B virus: a national cohort study.
Cao, L; Chen, B; Chen, R; Ding, Y; Fan, J; Gan, W; Huang, Y; Lin, C; Liu, Y; Pan, CQ; Sheng, Q; Wang, S; Wang, Y; Zhu, L, 2020
)
0.56
" Consistently, a lack of MKP-5 aggravated the adverse effects of lipotoxicity."( MKP-5 Relieves Lipotoxicity-Induced Islet β-Cell Dysfunction and Apoptosis via Regulation of Autophagy.
Jiao, P; Li, L; Ma, J; Ma, Y; Teng, W; Tian, Y; Wang, W; Yan, W; Zhao, T, 2020
)
0.56
" Because TDF can lead to renal impairment and a decrease in bone mineral density (BMD), the prodrug tenofovir alafenamide (TAF) may be considered a viable alternative with fewer adverse effects."( Safety and efficacy of tenofovir alafenamide in liver transplant recipients: A single center experience.
Achterfeld, A; Herzer, K; Rashidi-Alavijeh, J; Straub, K; Wedemeyer, H; Willuweit, K, 2021
)
0.62
" After 1 year, 22 patients were still taking TAF; two patients had been lost to follow-up; one patient had died; and four patients had discontinued therapy because of TAF-related adverse effects."( Safety and efficacy of tenofovir alafenamide in liver transplant recipients: A single center experience.
Achterfeld, A; Herzer, K; Rashidi-Alavijeh, J; Straub, K; Wedemeyer, H; Willuweit, K, 2021
)
0.62
" Most common adverse events (AEs) leading to prior KI discontinuation were rash (27%), arthralgia (18%), and atrial fibrillation (16%)."( Phase 2 study of the safety and efficacy of umbralisib in patients with CLL who are intolerant to BTK or PI3Kδ inhibitor therapy.
Barr, PM; Barrientos, JC; Brander, DM; Cheson, BD; Dorsey, C; Flinn, IW; Fonseca, GA; Ghosh, N; Hamadeh, IS; Kambhampati, S; Lamanna, N; Lansigan, F; LaRatta, N; Luning Prak, ET; Mato, AR; Miskin, HP; Pagel, JM; Paskalis, D; Pu, JJ; Rai, KR; Reeves, JA; Roeker, L; Schuster, SJ; Sitlinger, A; Skarbnik, AP; Sportelli, P; Svoboda, J; Tsao, P; Weiss, MS; Weissbrot, H, 2021
)
0.62
"Limited published real-world data describe adverse events (AEs) among patients treated for mantle-cell lymphoma (MCL)."( Adverse Events and Economic Burden Among Patients Receiving Systemic Treatment for Mantle Cell Lymphoma: A Real-World Retrospective Cohort Study.
Byfield, SD; Kabadi, SM; LE, L; Olufade, T, 2021
)
0.62
" Primary safety outcomes, compared pairwise among treatment groups, were the occurrence of a composite adverse pregnancy outcome (ie, either preterm delivery, the infant being born small for gestational age, stillbirth, or spontaneous abortion) in all participants with a pregnancy outcome, and the occurrence of grade 3 or higher maternal and infant adverse events in all randomised participants."( Efficacy and safety of dolutegravir with emtricitabine and tenofovir alafenamide fumarate or tenofovir disoproxil fumarate, and efavirenz, emtricitabine, and tenofovir disoproxil fumarate HIV antiretroviral therapy regimens started in pregnancy (IMPAACT 2
Amico, KR; Brummel, SS; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, J; Fairlie, L; Frenkel, LM; Hanley, S; Hoffman, RM; Holmes, LB; Jean-Philippe, P; João, E; Johnston, B; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Momper, JD; Moyo, S; Purdue, L; Rooney, JF; Sax, PE; Shapiro, RL; Stranix-Chibanda, L; Stringer, JS; Thoofer, NK; Ziemba, L, 2021
)
0.62
" Significantly fewer participants in the dolutegravir, emtricitabine, and tenofovir alafenamide fumarate group (52 [24%] of 216) had a composite adverse pregnancy outcome than those in the dolutegravir, emtricitabine, and tenofovir disoproxil fumarate group (70 [33%] of 213; estimated difference -8·8% [95% CI -17·3 to -0·3], p=0·043) or the efavirenz, emtricitabine, and tenofovir disoproxil fumarate group (69 [33%] of 211; -8·6% [-17·1 to -0·1], p=0·047)."( Efficacy and safety of dolutegravir with emtricitabine and tenofovir alafenamide fumarate or tenofovir disoproxil fumarate, and efavirenz, emtricitabine, and tenofovir disoproxil fumarate HIV antiretroviral therapy regimens started in pregnancy (IMPAACT 2
Amico, KR; Brummel, SS; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, J; Fairlie, L; Frenkel, LM; Hanley, S; Hoffman, RM; Holmes, LB; Jean-Philippe, P; João, E; Johnston, B; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Momper, JD; Moyo, S; Purdue, L; Rooney, JF; Sax, PE; Shapiro, RL; Stranix-Chibanda, L; Stringer, JS; Thoofer, NK; Ziemba, L, 2021
)
0.62
" The dolutegravir, emtricitabine, and tenofovir alafenamide fumarate regimen had the lowest frequency of composite adverse pregnancy outcomes and of neonatal deaths."( Efficacy and safety of dolutegravir with emtricitabine and tenofovir alafenamide fumarate or tenofovir disoproxil fumarate, and efavirenz, emtricitabine, and tenofovir disoproxil fumarate HIV antiretroviral therapy regimens started in pregnancy (IMPAACT 2
Amico, KR; Brummel, SS; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, J; Fairlie, L; Frenkel, LM; Hanley, S; Hoffman, RM; Holmes, LB; Jean-Philippe, P; João, E; Johnston, B; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Momper, JD; Moyo, S; Purdue, L; Rooney, JF; Sax, PE; Shapiro, RL; Stranix-Chibanda, L; Stringer, JS; Thoofer, NK; Ziemba, L, 2021
)
0.62
" TAF was well tolerated and only 4 patients discontinued therapy due to adverse event during a median duration of TAF dosing of 74 weeks."( Safety and Effectiveness of Tenofovir Alafenamide in Usual Clinical Practice Confirms Results of Clinical Trials: TARGET-HBV.
Bernstein, DE; Fried, MW; Lok, AS; Mospan, AR; Schiff, ER; Smith, CI; Trinh, HN; Zink, RC, 2022
)
0.72
" The treatment using NAs was well-tolerated and there was no serious drug-related adverse event reported."( Short-term and long-term safety and efficacy of tenofovir alafenamide, tenofovir disoproxil fumarate and entecavir treatment of acute-on-chronic liver failure associated with hepatitis B.
Chen, T; Chen, Y; Fu, M; Fu, S; Gao, Z; He, Y; Hu, C; Li, J; Liu, J; Yan, T; Yang, Y; Zhang, R; Zhao, Y; Zhou, M, 2021
)
0.62
" In rats, systemic and local findings were considered not adverse due to their low severity and reversibility; therefore, the "no observed adverse effect level" (NOAEL) was set at 1,000 μg/kg/day."( A 28-Day Toxicity Study of Tenofovir Alafenamide Hemifumarate by Subcutaneous Infusion in Rats and Dogs.
Alessi, T; Feldman, PL; Felx, M; Jain, R; Roller, S; Shelton, J; Singh, R; Wang, Y; Yang, B; Zane, D, 2021
)
0.62
"Emtricitabine and tenofovir alafenamide is safe and effective for longer-term pre-exposure prophylaxis in cisgender men and transgender women who have sex with men."( Long-term safety and efficacy of emtricitabine and tenofovir alafenamide vs emtricitabine and tenofovir disoproxil fumarate for HIV-1 pre-exposure prophylaxis: week 96 results from a randomised, double-blind, placebo-controlled, phase 3 trial.
Asmuth, DM; Baeten, JM; Brainard, DM; Brunetta, JM; Carter, C; Cox, S; Das, M; Ebrahimi, R; Gilson, R; Henry, K; Kintu, A; Kronborg, G; Ogbuagu, O; Podzamczer, D; Ruane, PJ; Salazar, LC; Shao, Y; Spinner, CD; Whitlock, G; Wohl, D, 2021
)
0.62
"Ibrutinib has superior progression-free survival compared with bendamustine plus rituximab (BR) in older CLL patients, however, differences in treatment duration, six monthly BR cycles versus continuous ibrutinib, complicate adverse event (AE) comparisons."( Adverse event burden in older patients with CLL receiving bendamustine plus rituximab or ibrutinib regimens: Alliance A041202.
Abramson, JS; Bartlett, NL; Booth, AM; Brander, DM; Brown, JR; Byrd, JC; Coutre, S; Ding, W; Erba, H; Kuzma, CS; Larson, RA; Little, RF; Litzow, M; Mandrekar, SJ; Nattam, S; Owen, C; Ruppert, AS; Smith, SE; Stone, RM; Woyach, JA, 2021
)
0.62
"The occurrence of adverse events was revealed as a major cause of ibrutinib failure in the real-world."( Keeping a balance in chronic lymphocytic leukemia (CLL) patients taking ibrutinib: ibrutinib-associated adverse events and their management based on drug interactions.
Baek, DW; Cho, HJ; Kim, J; Lee, JM; Moon, JH; Sohn, SK, 2021
)
0.62
" While 176 adverse events (AEs) were reported in 74 (54."( Efficacy and Safety of Ibrutinib Therapy in Patients with Chronic Lymphocytic Leukemia: Retrospective Analysis of Real-Life Data
Akay, OM; Akdeniz, A; Akpınar, S; Aydoğdu, İ; Baştürk, A; Batur, DS; Berber, İ; Çekdemir, D; Çetin, G; Davulcu, EA; Demircioğlu, S; Deveci, B; Dinçyürek, HD; Doğu, MH; Durusoy, SS; Ertop, Ş; Ferhanoğlu, B; Güneş, AK; Gürkan, E; İlhan, G; Kaya, E; Kızıklı, A; Kurtoğlu, E; Mehtap, Ö; Okan, V; Okay, M; Özcan, MA; Özcan, Ö; Özet, G; Özkocamaz, V; Pepedil Tanrıkulu, F; Sahip, B; Saydam, G; Sayınalp, N; Seyhanlı, A; Sönmez, M; Terzi, H; Tombak, A; Turgut, B; Uçar, MA; Ümit, EG; Ünal, A; Yavaşoğlu, İ; Yıldırım, R; Yılmaz, M, 2021
)
0.62
"This real-life analysis confirms the favorable efficacy and safety profile of long-term ibrutinib treatment while emphasizing the potential adverse impacts of poorer ECOG performance status, heavy treatment prior to ibrutinib, and advanced Rai stage on patient compliance, treatment response, and survival outcomes."( Efficacy and Safety of Ibrutinib Therapy in Patients with Chronic Lymphocytic Leukemia: Retrospective Analysis of Real-Life Data
Akay, OM; Akdeniz, A; Akpınar, S; Aydoğdu, İ; Baştürk, A; Batur, DS; Berber, İ; Çekdemir, D; Çetin, G; Davulcu, EA; Demircioğlu, S; Deveci, B; Dinçyürek, HD; Doğu, MH; Durusoy, SS; Ertop, Ş; Ferhanoğlu, B; Güneş, AK; Gürkan, E; İlhan, G; Kaya, E; Kızıklı, A; Kurtoğlu, E; Mehtap, Ö; Okan, V; Okay, M; Özcan, MA; Özcan, Ö; Özet, G; Özkocamaz, V; Pepedil Tanrıkulu, F; Sahip, B; Saydam, G; Sayınalp, N; Seyhanlı, A; Sönmez, M; Terzi, H; Tombak, A; Turgut, B; Uçar, MA; Ümit, EG; Ünal, A; Yavaşoğlu, İ; Yıldırım, R; Yılmaz, M, 2021
)
0.62
" Week 48 virologic suppression (HIV-1 RNA <50 copies/mL), resistance, adverse events (AEs), and laboratory parameters were assessed."( Brief Report: Efficacy and Safety of Bictegravir/Emtricitabine/Tenofovir Alafenamide in Females Living With HIV: An Integrated Analysis of 5 Trials.
Ajana, F; Brainard, D; Chuck, SK; Collins, SE; Gandhi-Patel, B; Kityo, C; Koenig, E; Liu, Y; Makadzange, T; McNicholl, I; Natukunda, E; Orkin, C; Pikora, C; Wang, H; Wei, X; White, K, 2021
)
0.62
"In individuals with a history of PRT on TDF, 96 weeks of TAF was not associated with recurrent PRT or adverse effects on renal tubular function, bone turnover, or BMD."( Safety of Tenofovir Alafenamide in People With HIV Who Experienced Proximal Renal Tubulopathy on Tenofovir Disoproxil Fumarate.
Barbini, B; Burling, K; Campbell, L; Cromarty, B; Hamzah, L; Johnson, M; Jones, R; Post, FA; Samarawickrama, A; Williams, D; Winston, A, 2021
)
0.62
" 1V209-Cho-Lip exerted minimal toxic effects and enhanced the transportation ability in lymph nodes (LNs) compared with 1V209."( Lymph-Node-Targeted Cholesterolized TLR7 Agonist Liposomes Provoke a Safe and Durable Antitumor Response.
Chen, L; He, C; Hong, W; Lan, T; Que, H; Wan, D; Wei, X; Wei, Y; Yang, J, 2021
)
0.62
" The most common grade 3 adverse events were rash/pruritis/dermatitis (19%), diarrhea (11%), hyperglycemia (11%), and hypertension (11%)."( Phase I/Ib Study of the Efficacy and Safety of Buparlisib and Ibrutinib Therapy in MCL, FL, and DLBCL with Serial Cell-Free DNA Monitoring.
Batlevi, CL; De Frank, S; Drullinsky, P; Gerecitano, JF; Hamilton, A; Hamlin, PA; Horwitz, SM; Kumar, A; Matasar, MJ; Michaud, L; Moskowitz, A; Moskowitz, CH; Nakajima, R; Nichols, C; Rademaker, J; Salles, G; Schöder, H; Seshan, V; Stewart, CM; Straus, D; Tsui, DWY; Whiting, K; Younes, A; Zelenetz, AD, 2022
)
0.72
"Adverse events were generally mild, but one case of fatal suspected unexpected serious adverse reaction occurred."( Safety and efficacy of the mRNA BNT162b2 vaccine against SARS-CoV-2 in five groups of immunocompromised patients and healthy controls in a prospective open-label clinical trial.
Akber, M; Aleman, S; Bergman, P; Blennow, O; Blixt, L; Bogdanovic, G; Buggert, M; Chen, MS; Chen, P; Friman, G; Gomez, AC; Hansson, L; Hober, S; Lindgren, G; Ljunggren, HG; Ljungman, P; Loré, K; Mielke, S; Muschiol, S; Nilsson, P; Nordlander, A; Norlin, AC; Nowak, P; Österborg, A; Smith, CIE; Söderdahl, G; Thalme, A; Valentini, D; Vesterbacka, J; Wahren-Borgström, E; Wullimann, D, 2021
)
0.62
"The results showed that the mRNA BNT162b2 vaccine was safe in immunocompromised patients."( Safety and efficacy of the mRNA BNT162b2 vaccine against SARS-CoV-2 in five groups of immunocompromised patients and healthy controls in a prospective open-label clinical trial.
Akber, M; Aleman, S; Bergman, P; Blennow, O; Blixt, L; Bogdanovic, G; Buggert, M; Chen, MS; Chen, P; Friman, G; Gomez, AC; Hansson, L; Hober, S; Lindgren, G; Ljunggren, HG; Ljungman, P; Loré, K; Mielke, S; Muschiol, S; Nilsson, P; Nordlander, A; Norlin, AC; Nowak, P; Österborg, A; Smith, CIE; Söderdahl, G; Thalme, A; Valentini, D; Vesterbacka, J; Wahren-Borgström, E; Wullimann, D, 2021
)
0.62
" Drug-related adverse events were more frequent with DTG/3TC (15%; leading to discontinuation in 4%) than TAF-based regimens (5%; leading to discontinuation in 1%) through week 144, but rates were comparable after week 48 (4%; leading to discontinuation in 1% in both groups)."( Efficacy and Safety of Switching to Dolutegravir/Lamivudine Versus Continuing a Tenofovir Alafenamide-Based 3- or 4-Drug Regimen for Maintenance of Virologic Suppression in Adults Living With Human Immunodeficiency Virus Type 1: Results Through Week 144 F
Aboud, M; Ait-Khaled, M; Ajana, F; Bisshop, F; De Wit, S; George, N; Leone, P; Osiyemi, O; Pappa, KA; Portilla, J; Routy, JP; Smith, KY; van Wyk, J; Wang, R; Wright, J; Wyen, C; Wynne, B, 2022
)
0.72
" No fatal events or related serious adverse events were reported."( Pharmacokinetics and Safety of the Nucleoside Analog Antiviral Drug Galidesivir Administered to Healthy Adult Subjects.
Collins, D; Dobo, S; Mathis, A; Sheridan, WP; Taylor, R; Walling, DM, 2022
)
0.72
"The increasing indications and addition of newer agents to clinical practice and emergence of BTK inhibitor-related cardiac adverse events have complicated the management decisions for utilization of this class of therapy."( Cardiotoxicity of BTK inhibitors: ibrutinib and beyond.
Awan, FT; Christensen, BW; Zaha, VG, 2022
)
0.72
"The newer BTK inhibitor acalabrutinib represents a new standard of care in front-line chronic lymphocytic leukemia (CLL) given the results of the ELEVATE-RR trial demonstrating comparable efficacy and a more favorable toxicity profile especially with regard to cardiac adverse events as compared to ibrutinib."( Cardiotoxicity of BTK inhibitors: ibrutinib and beyond.
Awan, FT; Christensen, BW; Zaha, VG, 2022
)
0.72
" Common nonhematologic adverse events were fatigue (56%), nausea (53%), anorexia (41%), and diarrhea (41%) and were mostly low grade."( Selinexor Combined with Ibrutinib Demonstrates Tolerability and Safety in Advanced B-Cell Malignancies: A Phase I Study.
Baker, S; Bhat, S; Byrd, JC; Canfield, D; Cempre, CB; Fu, Q; Hu, B; Huang, Y; Jaglowski, SM; Lapalombella, R; Lockman, H; Rogers, KA; Ruppert, AS; Shah, H; Stephens, DM; Vadeboncoeur, R; Walker, JS; Woyach, JA, 2022
)
0.72
" Adverse events occurred in 74."( Efficacy and safety of ibrutinib in relapsed/refractory CLL and SLL in Japan: a post-marketing surveillance.
Akizuki, R; Fujino, A; Nomura, F; Omi, A; Tsujioka, S, 2022
)
0.72
" Toxic effects of the combination of ibrutinib and cetuximab have been reported in a patient with metastatic CRC."( Ibrutinib and panitumumab used in combination safely in a patient with metachronous colorectal cancer and chronic lymphocytic leukemia.
Araz, M; Artaç, M; Çeneli, Ö; Karaağaç, M; Karakurt Eryilmaz, M; Korkmaz, M, 2022
)
0.72
" We also synopsize and discuss the cardiovascular adverse effects related to other more selective BTK inhibitors, which may guide the selection of appropriate BTK inhibitors."( Ibrutinib-Associated Cardiotoxicity: From the Pharmaceutical to the Clinical.
Dong, R; Lin, N; Tan, B; Yan, Y; Zeng, X, 2022
)
0.72
" Across the studies, one grade 3/4 adverse event was considered drug-related (intermediate uveitis)."( Effectiveness and safety of tenofovir alafenamide in children and adolescents living with HIV: a systematic review.
Castro, H; Collins, IJ; Jesson, J; Judd, A; Leroy, V; Milanzi, E; O'Rourke, J; Penazzato, M; Renaud, F; Townsend, CL; Vicari, M, 2023
)
0.91
" We analysed the incidence of adverse events (AEs), laboratory abnormalities, and changes in relevant tolerability parameters through 48 weeks."( Efficacy and safety of switching to bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed Asian adults living with HIV: A pooled analysis from three international phase III randomized trials.
Avihingsanon, A; Chetchotisakd, P; Kiertiburanakul, S; Martin, H; Ratanasuwan, W; Siripassorn, K; Supparatpinyo, K; Wang, H; Wang, HY; Wong, T, 2023
)
0.91
" Primary safety analyses were pairwise comparisons between ART regimens of the proportion of maternal and infant adverse events of grade 3 or higher up to 50 weeks post partum."( Efficacy and safety of three antiretroviral therapy regimens started in pregnancy up to 50 weeks post partum: a multicentre, open-label, randomised, controlled, phase 3 trial.
Amico, KR; Boyce, C; Brummel, S; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, JS; Fairlie, L; Frenkel, LM; Hoffman, R; Jean-Philippe, P; Johnston, B; Knowles, K; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Moyo, S; Patel, F; Purdue, L; Rooney, JF; Sax, PE; Shapiro, R; Stranix-Chibanda, L; Stringer, J; van Wyk, J; Ziemba, L, 2023
)
0.91
" Up to the week 50 post-partum visit, the estimated probability of experiencing an adverse event of grade 3 or higher was 25% in the dolutegravir, emtricitabine, and tenofovir alafenamide group; 31% in the dolutegravir, emtricitabine, and tenofovir disoproxil fumarate group; and 28% in the efavirenz, emtricitabine, and tenofovir disoproxil fumarate group (no significant difference between groups)."( Efficacy and safety of three antiretroviral therapy regimens started in pregnancy up to 50 weeks post partum: a multicentre, open-label, randomised, controlled, phase 3 trial.
Amico, KR; Boyce, C; Brummel, S; Cassim, H; Chakhtoura, N; Chinula, L; Coletti, A; Currier, JS; Fairlie, L; Frenkel, LM; Hoffman, R; Jean-Philippe, P; Johnston, B; Knowles, K; Korutaro, V; Krotje, C; Lockman, S; Masheto, G; McCarthy, K; Mmbaga, BT; Moyo, S; Patel, F; Purdue, L; Rooney, JF; Sax, PE; Shapiro, R; Stranix-Chibanda, L; Stringer, J; van Wyk, J; Ziemba, L, 2023
)
0.91
" Tenofovir disoproxil fumarate (TDF) increases the risk of renal tubular toxicity and adverse effects on bone, but Tenofovir alafenamide (TAF) and Tenofovir amibufenamide (TMF) have favorable safety profile on the kidneys and bones."( Medication safety in chronic kidney disease.
Singh, S, 2023
)
0.91
" However, greater adverse effects on renal function were observed for TDF than ETV at 60 months compared to 12 months."( Renal and bone side effects of long-term use of entecavir, tenofovir disoproxil fumarate, and tenofovir alafenamide fumarate in patients with Hepatitis B: a network meta-analysis.
Liu, S; Liu, Z; Ma, X; Xin, Y; Zhao, Z, 2023
)
0.91
"Long-term administration of TDF has resulted in stronger adverse effects than TAF and ETV in regard to both renal function and bone tissue in CHB patients."( Renal and bone side effects of long-term use of entecavir, tenofovir disoproxil fumarate, and tenofovir alafenamide fumarate in patients with Hepatitis B: a network meta-analysis.
Liu, S; Liu, Z; Ma, X; Xin, Y; Zhao, Z, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" In this study, pharmacokinetic profiles were simulated for 23 patients treated with amonafide, using each patient's individual pharmacokinetic parameters."( Limited sampling models for amonafide (NSC 308847) pharmacokinetics.
Malspeis, L; Ratain, MJ; Schilsky, RL; Staubus, AE, 1988
)
0.27
"To determine if variability in toxicity of amonafide during phase II trials could be correlated with pharmacokinetic variability."( Population pharmacodynamic study of amonafide: a Cancer and Leukemia Group B study.
Allen, SL; Costanza, M; Henderson, IC; Ratain, MJ; Rosner, G; Schilsky, RL; Van Echo, DA, 1995
)
0.29
"When a pharmacodynamic model is to be considered as the basis for individualized drug dosing, validation of the model is clearly warranted."( Bootstrap validation of pharmacodynamic models defined via stepwise linear regression.
Mick, R; Ratain, MJ, 1994
)
0.29
"We have investigated the correlation of clinical responses (decreases of white blood cells and peripheral blasts) with pharmacokinetic and pharmacodynamic parameters in patients with acute myelogenous leukemia who are receiving amonafide."( The correlation of response with plasma pharmacokinetics and polyamine concentrations in patients with acute myelogenous leukemia receiving amonafide.
Benvenuto, JA; Johnston, DA; Nishioka, K, 1993
)
0.29
"Amonafide (A) demonstrates dose-related increases in area under the curve (AUC) and Cmax values."( Clinical pharmacokinetics of amonafide (NSC 308847) in 62 patients.
Akerman, S; Allen, SL; Budman, DR; Calabro, A; Chan, K; Fusco, D; Hock, K; Kreis, W; Mittelman, A; Puccio, C; Spigelman, M, 1996
)
0.29
" Pharmacokinetic experiments with mice showed that the oral bioavailabilities of PMEA following oral gavage of bis(POM)-PMEA, diphenyl-PMEA, or PMEA (at a dose equivalent to 50 mg of PMEA per kg) were 53,3, and 16%, respectively."( Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
Balzarini, J; Bischofberger, N; De Clercq, E; Naesens, L, 1996
)
0.51
" The goal of this study was to construct and validate a pharmacodynamic model-based dosing strategy for amonafide, to try to further decrease inter-patient variability in leukopenia."( Individualized dosing of amonafide based on a pharmacodynamic model incorporating acetylator phenotype and gender.
Berezin, F; Janisch, L; Kut, M; Mick, R; Ratain, MJ; Schilsky, RL; Vogelzang, NJ, 1996
)
0.29
" Pharmacokinetic studies with mice showed that the oral bioavailability of bis(POC)-PMPA (calculated from the curves of the concentration of free PMPA in plasma) was 20%."( Antiretroviral efficacy and pharmacokinetics of oral bis(isopropyloxycarbonyloxymethyl)-9-(2-phosphonylmethoxypropyl)adenine in mice.
Annaert, P; Arimilli, MN; Augustijns, P; Bischofberger, N; De Clercq, E; Kim, CU; Naesens, L; Van den Mooter, G, 1998
)
0.51
" Intracellular activation of a small fraction (< 10%) of the dose by cellular kinases leads to prolonged antiviral effects that are not easily predicted from conventional pharmacokinetic studies."( Clinical pharmacokinetics of the antiviral nucleotide analogues cidofovir and adefovir.
Cundy, KC, 1999
)
0.3
" Pharmacokinetic parameters differed by patient age."( Single-dose pharmacokinetics and safety of the oral antiviral compound adefovir dipivoxil in children infected with human immunodeficiency virus type 1. The Pediatrics AIDS Clinical Trials Group.
Blanchard, S; Burchett, S; Coakley, DF; Culnane, M; Cundy, KC; Fridland, A; Hughes, WT; Purdue, L; Read, JS; Rodman, JH; Shenep, JL; Willoughby, R; Zimmer, B, 2000
)
0.31
" Pharmacokinetic parameters were dose proportional and demonstrated no change with repeated dosing."( Phase i/ii trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults.
Barditch-Crovo, P; Coakley, DF; Coleman, RL; Collier, A; Deeks, SG; Kahn, JO; Kearney, BP; Lamy, PD; Lietman, PS; McGowan, I; Miller, M; Safrin, S, 2001
)
0.31
" Pharmacokinetic experiments in mice showed that the oral bioavailabilities of PMEA following oral gavage of Bis-PMEA or PMEA (at a dose equivalent to 28 mg of PMEA/kg) were 50."( Pharmacokinetic and antiretroviral activity in mice of oral [P(1),P(2)-bis[2-(adenin-9-yl)ethoxymethyl]phosphonate], a prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
Cappellacci, L; Casabianca, A; Celeste, AG; Cerasi, A; Chiarantini, L; Dominici, S; Franchetti, P; Grifantini, M; Magnani, M; Rossi, L; Serafini, S, 2002
)
0.51
" A two compartment pharmacokinetic model is employed to determine the time evolution of the intracellular concentrations of the active forms of drugs, and thereby drug efficacy."( Complex patterns of viral load decay under antiretroviral therapy: influence of pharmacokinetics and intracellular delay.
Dixit, NM; Perelson, AS, 2004
)
0.32
" After iv infusion, the half-life was the same for CdA and CAde, but after oral administration the half-life was doubled for CAde."( Cytotoxicity and pharmacokinetics of cladribine metabolite, 2-chloroadenine in patients with leukemia.
Albertioni, F; Juliusson, G; Larsson, R; Liliemark, J; Lindemalm, S, 2004
)
0.56
"Phase I, open-label, fixed-sequence, pharmacokinetic drug-drug interaction study."( Effect of tenofovir disoproxil fumarate on the pharmacokinetics and pharmacodynamics of total, R-, and S-methadone.
Berenson, CS; Booker, BM; Bullock, JM; Cloen, D; Coakley, DF; Flaherty, JF; Haas, CE; Kearney, BP; Liaw, S; Smith, PF; Yale, K, 2004
)
0.32
" Both AUCss and Cmax met the strict criteria for bioequivalence between the two study periods for total, R-, and S-methadone, indicating a lack of drug interaction when tenofovir DF was coadministered with methadone."( Effect of tenofovir disoproxil fumarate on the pharmacokinetics and pharmacodynamics of total, R-, and S-methadone.
Berenson, CS; Booker, BM; Bullock, JM; Cloen, D; Coakley, DF; Flaherty, JF; Haas, CE; Kearney, BP; Liaw, S; Smith, PF; Yale, K, 2004
)
0.32
"On day 1, 12 h pharmacokinetic profiles for saquinavir/ritonavir (1000/100 mg given twice daily) were obtained for 18 subjects."( Pharmacokinetics of saquinavir hard gel/ritonavir (1000/100 mg twice daily) when administered with tenofovir diproxil fumarate in HIV-1-infected subjects.
Back, D; Boffito, M; Di Perri, G; Gazzard, B; Hill, A; Moyle, G; Nelson, M; Pozniak, A; Stainsby-Tron, M; Tomkins, J, 2005
)
0.33
" Pharmacokinetic data for 23 subjects were thus evaluable."( Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers.
Buffels, R; Burger, DM; Droste, JA; Hekster, YA; Kearney, BP; Vanhorssen, PJ; Verweij-van Wissen, CP, 2005
)
0.33
"The nucleotide analogue, tenofovir, has been shown to lower plasma atazanavir levels in pharmacokinetic trials, an interaction that may be partly reversed by the addition of ritonavir, whereas plasma tenofovir levels are themselves raised when the drug is combined with lopinavir/ritonavir."( The steady-state pharmacokinetics of nelfinavir in combination with tenofovir in HIV-infected patients.
Becker, M; Breske, A; Esser, S; Hill, A; Koerber, A; Kopperman, M; Kruse, G; Kurowski, M; Möcklinghoff, C; Ross, B; Stocker, H; Wiehler, H, 2005
)
0.33
"Eighteen patients received nelfinavir 1250 mg twice daily plus prescribed nucleoside reverse transcriptase inhibitors for at least 14 days, with pharmacokinetic measurements performed on day 15."( The steady-state pharmacokinetics of nelfinavir in combination with tenofovir in HIV-infected patients.
Becker, M; Breske, A; Esser, S; Hill, A; Koerber, A; Kopperman, M; Kruse, G; Kurowski, M; Möcklinghoff, C; Ross, B; Stocker, H; Wiehler, H, 2005
)
0.33
" TFV-DP also had persistent intracellular levels on TDF discontinuation (median half-life of 150 hours, range: 60 to >175 hours)."( Intracellular pharmacokinetics of tenofovir diphosphate, carbovir triphosphate, and lamivudine triphosphate in patients receiving triple-nucleoside regimens.
Clark, N; Guyer, B; Hawkins, T; Kearney, BP; St Claire, RL; Veikley, W, 2005
)
0.33
" The validated LC/MS/MS method has been successfully used in a pharmacokinetic study in healthy volunteers treated with oral adefovir dipivoxil at 10 and 20 mg."( Determination of adefovir in human plasma by liquid chromatography/tandem mass spectrometry: application to a pharmacokinetic study.
Bi, HC; Chen, X; Huang, M; Zhong, GP; Zhou, S, 2005
)
0.33
" Steady-state RTV AUCtau and Cmax levels were not significantly altered, whereas Ctau was 23% higher upon coadministration of SQV/RTV and TDF."( Pharmacokinetics of tenofovir disoproxil fumarate and ritonavir-boosted saquinavir mesylate administered alone or in combination at steady state.
Adda, N; Begley, JA; Blum, MR; Chittick, GE; Kearney, BP; Sorbel, JJ; Zong, J, 2006
)
0.33
" Pharmacokinetic sampling was performed on days 1 through 4 and 22 through 25."( Absence of clinically relevant pharmacokinetic interaction between ribavirin and tenofovir in healthy subjects.
Cheng, A; Ebrahimi, R; Kearney, BP; Mittan, A; Ramanathan, S, 2006
)
0.33
"A population pharmacokinetic analysis was performed in the context of therapeutic drug monitoring (87 patients, 121 samples)."( Influence of tenofovir, nevirapine and efavirenz on ritonavir-boosted atazanavir pharmacokinetics in HIV-infected patients.
Arvieux, C; Dailly, E; Jolliet, P; Perré, P; Raffi, F; Tattevin, P; Tribut, O, 2006
)
0.33
"We evaluated the impact of modelling intra-subject variability on the likelihood ratio test (LRT) and the Wald test based on non-linear mixed effects models in pharmacokinetic interaction and bioequivalence cross-over trials."( Impact of modelling intra-subject variability on tests based on non-linear mixed-effects models in cross-over pharmacokinetic trials with application to the interaction of tenofovir on atazanavir in HIV patients.
Mentré, F; Panhard, X; Piketti, C; Taburet, AM, 2007
)
0.34
" Nine and 10 healthy males were enrolled for a single-dose pharmacokinetic profile and assessment of the effect of food on the pharmacokinetics of adefovir (PMEA), respectively."( Pharmacokinetics, safety and tolerance of single- and multiple-dose adefovir dipivoxil in healthy Chinese subjects.
Guo, RC; Ni, MY; Sun, DQ; Wang, BJ; Wang, HS, 2007
)
0.34
" The pharmacokinetic parameters of PMEA following ADV 10, 20 and 40 mg were: geometric mean [95% confidence interval (CI)] for AUC(0-24 h) 227 (205, 253), 423 (361, 506) and 686 (585, 828) microg l(-1) h, C(max) 23."( Pharmacokinetics, safety and tolerance of single- and multiple-dose adefovir dipivoxil in healthy Chinese subjects.
Guo, RC; Ni, MY; Sun, DQ; Wang, BJ; Wang, HS, 2007
)
0.34
" A pharmacokinetic study in healthy volunteers was conducted to assess the potential for a drug interaction between these agents."( Pharmacokinetics and safety of tenofovir disoproxil fumarate on coadministration with lopinavir/ritonavir.
Cheng, AK; Ebrahimi, R; Kearney, BP; Mathias, A; Mittan, A; Sayre, J, 2006
)
0.33
" Pharmacokinetic assessments were performed over 24 hours on days 7, 21, and 35."( Pharmacokinetics and safety of tenofovir disoproxil fumarate on coadministration with lopinavir/ritonavir.
Cheng, AK; Ebrahimi, R; Kearney, BP; Mathias, A; Mittan, A; Sayre, J, 2006
)
0.33
" The pharmacokinetic profile of GBP was examined."( The effect of MDR1 G2677T/A polymorphism on pharmacokinetics of gabapentin in healthy Korean subjects.
Cho, HY; Kang, HA; Lee, YB, 2007
)
0.34
" Pharmacokinetic (PK) blood draws were performed on days 7, 17, and 27."( Pharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137.
Cheng, A; Kearney, BP; Ramanathan, S; Shen, G, 2007
)
0.34
" We evaluated the possibility of a pharmacokinetic interaction between TFV and EFV by assessing cross-sectional and longitudinal data in 169 individuals receiving EFV."( Does tenofovir influence efavirenz pharmacokinetics?
Buclin, T; Colombo, S; Décosterd, L; Furrer, H; Rotger, M; Telenti, A, 2007
)
0.34
"Although there is no clear evidence for a pharmacokinetic interaction between TFV and EFV, we cannot rule out an interaction between these drugs restricted to individuals who are slow EFV metabolizers."( Does tenofovir influence efavirenz pharmacokinetics?
Buclin, T; Colombo, S; Décosterd, L; Furrer, H; Rotger, M; Telenti, A, 2007
)
0.34
" As both drugs are extensively renally eliminated, a randomized, 3-way crossover study was conducted in 19 healthy volunteers to formally evaluate the potential pharmacokinetic interaction when the drugs are administered alone and together (ie, 200 mg emtricitabine qd for 7 days, 300 mg tenofovir disoproxil fumarate qd for 7 days, and 200 mg emtricitabine plus 300 mg tenofovir disoproxil fumarate qd for 7 days) with no washout between treatments."( Steady-state pharmacokinetics of emtricitabine and tenofovir disoproxil fumarate administered alone and in combination in healthy volunteers.
Begley, JA; Blum, MR; Chittick, GE; Zong, J, 2007
)
0.34
"The effect of tenofovir disoproxil fumarate (TDF) in combination with two boosted fosamprenavir regimens on amprenavir pharmacokinetic parameters was assessed in this prospective phase I crossover study with 30 healthy volunteers."( Fosamprenavir/ritonavir plus tenofovir does not affect amprenavir pharmacokinetics: no effect of tenofovir.
Banik, N; Breske, A; Kruse, G; Kurowski, M; Mazur, D; Richter, H; Stocker, H; Walli, RK, 2007
)
0.34
"TMC114 is a new HIV protease inhibitor, used in combination with low-dose ritonavir (TMC114/r) as a pharmacokinetic enhancer."( Pharmacokinetic interaction between TMC114/ritonavir and tenofovir disoproxil fumarate in healthy volunteers.
De Doncker, P; De Pauw, M; Hill, A; Hoetelmans, RM; Lefebvre, E; Mariën, K; Peeters, M; Sekar, V; Woodfall, B, 2007
)
0.34
" Pharmacokinetic parameters estimated by noncompartmental method were reported as 90% confidence intervals (CIs) about the geometric mean ratio (GMR)."( Lopinavir/Ritonavir pharmacokinetic profile: impact of sex and other covariates following a change from twice-daily to once-daily therapy.
Acosta, EP; Binongo, JN; Chuck, SK; Lennox, JL; Ofotokun, I; Palau, M, 2007
)
0.34
"Atazanavir/ritonavir plasma concentrations were measured by liquid chromatography tandem mass spectrometry, and the geometric means of minimum and maximum concentrations (C(min), C(max)), the area under the time-concentration curve (AUC), half-life (t(1/2)) and total clearance (CL(tot)) were subject to a matched pairs-analysis."( Tenofovir comedication does not impair the steady-state pharmacokinetics of ritonavir-boosted atazanavir in HIV-1-infected adults.
Dauer, B; Haberl, A; Harder, S; Klauke, S; Lutz, T; Staszewski, S; von Hentig, N, 2007
)
0.34
"The coadministration of tenofovir-DF did not impair the plasma concentrations of ritonavir-boosted atazanavir in a pharmacokinetic analysis of patient pairs matched for gender, ethnicity, weight and CDC status."( Tenofovir comedication does not impair the steady-state pharmacokinetics of ritonavir-boosted atazanavir in HIV-1-infected adults.
Dauer, B; Haberl, A; Harder, S; Klauke, S; Lutz, T; Staszewski, S; von Hentig, N, 2007
)
0.34
" Pharmacokinetic assessments were performed on days 4 and 24 for adefovir and on days 14 and 24 for entecavir."( Absence of a pharmacokinetic interaction between entecavir and adefovir.
Bifano, M; Grasela, DM; LaCreta, F; Smith, RA; Yan, JH; Zhang, D, 2007
)
0.34
" The clinical consequences of these substantial pharmacokinetic changes should be investigated."( Lopinavir-ritonavir dramatically affects the pharmacokinetics of irinotecan in HIV patients with Kaposi's sarcoma.
Corona, G; Innocenti, F; Sandron, S; Sartor, I; Tirelli, U; Toffoli, G; Vaccher, E, 2008
)
0.35
" HIV-infected subjects > or =18 to <25 years old receiving (> or =28 days) 300/100 mg atazanavir-ritonavir plus 300 mg tenofovir disoproxil fumarate (TDF) plus one or more other nucleoside analogs underwent intensive 24-h pharmacokinetic studies following a light meal."( Pharmacokinetics of antiretroviral regimens containing tenofovir disoproxil fumarate and atazanavir-ritonavir in adolescents and young adults with human immunodeficiency virus infection.
Cunningham, CK; Fletcher, CV; Flynn, PM; Harris, DR; Havens, PL; Kapogiannis, BG; Kiser, JJ; Liu, NX; Major-Wilson, H; Muenz, LR; Viani, RM; Wilson, CM, 2008
)
0.35
"A pharmacokinetic study of blood plasma (BP) and GT TFV concentrations in 9 men was conducted after 1 and > or =14 doses of TDF."( The pharmacokinetics and viral activity of tenofovir in the male genital tract.
Chen, YC; Cohen, MS; Fiscus, SA; Hui, J; Kashuba, AD; Kearney, BP; Patterson, KB; Rezk, NL; Rooney, JF; Tappouni, HL; Vourvahis, M, 2008
)
0.35
"To assess the potential of cotrimoxazole and tenofovir, drugs which are inhibitors and/or substrates of renal transporters, to alter the pharmacokinetic profile of maraviroc."( The effects of cotrimoxazole or tenofovir co-administration on the pharmacokinetics of maraviroc in healthy volunteers.
Abel, S; Muirhead, GJ; Ridgway, CE; Russell, D; Whitlock, LA, 2008
)
0.35
"An open-label, randomized, 3-way crossover, drug-drug interaction study of the investigational anti-HBV combination agent, emtricitabine/tenofovir DF and the antirejection agent, tacrolimus was conducted in healthy volunteers to evaluate the potential for a pharmacokinetic interaction between these drugs."( Pharmacokinetics of emtricitabine/tenofovir disoproxil fumarate and tacrolimus at steady state when administered alone or in combination.
Alianti, JR; Begley, JA; Blum, MR; Chittick, GE; Sorbel, JJ; Zong, J, 2008
)
0.35
" Drug concentrations were measured by LC/MS/MS and steady state pharmacokinetic parameters were calculated for each drug using noncompartmental methods."( Pharmacokinetics of emtricitabine/tenofovir disoproxil fumarate and tacrolimus at steady state when administered alone or in combination.
Alianti, JR; Begley, JA; Blum, MR; Chittick, GE; Sorbel, JJ; Zong, J, 2008
)
0.35
"The 90% confidence intervals (CIs) of the geometric least-squares mean ratio for AUCtau, Cmax and Ctau for each drug together vs."( Pharmacokinetics of emtricitabine/tenofovir disoproxil fumarate and tacrolimus at steady state when administered alone or in combination.
Alianti, JR; Begley, JA; Blum, MR; Chittick, GE; Sorbel, JJ; Zong, J, 2008
)
0.35
"It was concluded that there was no clinically relevant pharmacokinetic interaction between emtricitabine/tenofovir DF and tacrolimus when administered together."( Pharmacokinetics of emtricitabine/tenofovir disoproxil fumarate and tacrolimus at steady state when administered alone or in combination.
Alianti, JR; Begley, JA; Blum, MR; Chittick, GE; Sorbel, JJ; Zong, J, 2008
)
0.35
"6-h half-life (30%)."( Population pharmacokinetics of emtricitabine in human immunodeficiency virus type 1-infected pregnant women and their neonates.
Arrivé, E; Avit, D; Blanche, S; Coffié, P; Dabis, F; Ekouévi, DK; Hirt, D; Lalsab, S; Leang, SK; McIntyre, J; Nerrienet, E; Rey, E; Tréluyer, JM; Urien, S, 2009
)
0.35
"Two open-label, randomized, cross-over trials in healthy volunteers were conducted to investigate the pharmacokinetic interaction between etravirine and tenofovir disoproxil fumarate."( Assessment of the steady-state pharmacokinetic interaction between etravirine administered as two different formulations and tenofovir disoproxil fumarate in healthy volunteers.
Aharchi, F; Beets, G; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, MP; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, BJ, 2009
)
0.35
"Etravirine was administered as either 800 mg twice a day (bid) (phase II formulation in Study 1) or 200 mg bid (phase III formulation in Study 2) for 8 days followed by a 12 h pharmacokinetic evaluation."( Assessment of the steady-state pharmacokinetic interaction between etravirine administered as two different formulations and tenofovir disoproxil fumarate in healthy volunteers.
Aharchi, F; Beets, G; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, MP; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, BJ, 2009
)
0.35
" Statistical analyses were performed on pharmacokinetic parameters: the area under the concentration-time curve from 0 to 4 h (AUC(0-4)), the maximum concentration of the drug (C(max)), and the residual concentration of the drug at the end of the dosing interval (C(trough)) for plasma and the AUC(0-4) and C(trough) for intracellular data."( Pilot pharmacokinetic study of human immunodeficiency virus-infected patients receiving tenofovir disoproxil fumarate (TDF): investigation of systemic and intracellular interactions between TDF and abacavir, lamivudine, or lopinavir-ritonavir.
Ayen, R; Clotet, B; Grassi, J; Levi, M; Negredo, E; Pruvost, A; Puig, J; Théodoro, F, 2009
)
0.35
" Pharmacokinetic (PK) analyses utilized non-compartmental methods."( Pharmacokinetics of tacrolimus co-administered with adefovir dipivoxil to liver transplant recipients.
Brown, RS; Enejosa, J; McGuire, BM; Ramanathan, S; Schiff, E; Terrault, NA; Tran, TT; Tupper, R; Zhong, L; Zong, J, 2009
)
0.35
"The median elimination half-life of tacrolimus was 14."( Pharmacokinetics of tacrolimus co-administered with adefovir dipivoxil to liver transplant recipients.
Brown, RS; Enejosa, J; McGuire, BM; Ramanathan, S; Schiff, E; Terrault, NA; Tran, TT; Tupper, R; Zhong, L; Zong, J, 2009
)
0.35
"Prospective, open-label, pharmacokinetic study in 12 HIV-infected patients stabilized on FPV/RTV 1400 mg/200 mg + tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) 300 mg/200 mg QD (TELEX II)."( Steady-state amprenavir, tenofovir, and emtricitabine pharmacokinetics before and after reducing ritonavir boosting of a fosamprenavir/tenofovir/emtricitabine regimen from 200 mg to 100 mg once daily (TELEX II).
Acosta, EP; Jennings, HC; Pakes, GE; Parks, DA; Taylor, C,
)
0.13
" Four weeks after reducing RTV, changes in Cmin and AUC24h were: APV: +26%, +0."( Steady-state amprenavir, tenofovir, and emtricitabine pharmacokinetics before and after reducing ritonavir boosting of a fosamprenavir/tenofovir/emtricitabine regimen from 200 mg to 100 mg once daily (TELEX II).
Acosta, EP; Jennings, HC; Pakes, GE; Parks, DA; Taylor, C,
)
0.13
"Thirty-day, open-label, fixed-sequence, pharmacokinetic drug-drug interaction study."( Lack of effect of tenofovir disoproxil fumarate on pharmacokinetics of hormonal contraceptives.
Kearney, BP; Mathias, A, 2009
)
0.35
" Geometric mean ratios (90% confidence intervals) for the pharmacokinetic parameters for deacetyl norgestimate and ethinyl estradiol were estimated by using analysis of variance and compared with the no-effect criterion for bioequivalence."( Lack of effect of tenofovir disoproxil fumarate on pharmacokinetics of hormonal contraceptives.
Kearney, BP; Mathias, A, 2009
)
0.35
" Also a complete 12-hour pharmacokinetic profile was recorded for 15 transplant patients who had the polymorphism and for 15 controls who were randomly chosen since they received the same type and dosage of mycophenolate, same posttransplant time and similar renal function."( The prevalence of uridine diphosphate-glucuronosyltransferase 1A9 (UGT1A9) gene promoter region single-nucleotide polymorphisms T-275A and C-2152T and its influence on mycophenolic acid pharmacokinetics in stable renal transplant patients.
Arroyo, M; Barrientos, A; Calvo, N; De la Orden, V; Maestro, ML; Ortega, D; Pérez-Flores, I; Sánchez-Fructuoso, AI; Veganzone, S; Viudarreta, M,
)
0.13
"Objective An open-label, three-period pharmacokinetic study was conducted to investigate the drug interaction potential between fosamprenavir (FPV) and tenofovir disoproxil fumarate (TDF)."( Steady-state amprenavir and tenofovir pharmacokinetics after coadministration of unboosted or ritonavir-boosted fosamprenavir with tenofovir disoproxil fumarate in healthy volunteers.
Andrews, M; Condoluci, DV; Luber, AD; Olson, K; Pakes, GE; Pappa, KA; Peloquin, CA; Slowinski, PD, 2010
)
0.36
" The following pharmacokinetic parameters were elucidated after administering a single dose of 10 mg, 20 mg, and 30 mg of adefovir dipivoxil."( Determination of adefovir by LC-ESI-MS-MS and its application to a pharmacokinetic study in healthy Chinese volunteers.
Dai, L; Di, B; Ding, L; Fan, H; Xiao, D; Zhang, J; Zhu, Y; Zou, J,
)
0.13
"Nucleoside-sparing combination antiretroviral therapy (cART) regimens might be an attractive therapeutic option for HIV type-1 (HIV-1)-infected patients; however, the pharmacokinetic profiles of such regimens are frequently unknown."( The effects of a nucleoside-sparing antiretroviral regimen on the pharmacokinetics of ritonavir-boosted darunavir in HIV type-1-infected patients.
Back, D; Dickinson, L; Erlwein, OW; Garvey, L; Latch, N; Mackie, NE; McClure, MO; Scullard, G; Walsh, J; Winston, A, 2010
)
0.36
"Fourteen HIV-1-infected patients (age 21-55 years, 64% male) on stable cART with plasma HIV RNA <50 copies/ml entered this Phase I pharmacokinetic study."( The effects of a nucleoside-sparing antiretroviral regimen on the pharmacokinetics of ritonavir-boosted darunavir in HIV type-1-infected patients.
Back, D; Dickinson, L; Erlwein, OW; Garvey, L; Latch, N; Mackie, NE; McClure, MO; Scullard, G; Walsh, J; Winston, A, 2010
)
0.36
"A selective, rapid and sensitive hydrophilic interaction liquid chromatography-tandem mass spectrometry (HILIC-MS/MS) method was developed for the first time to determine adefovir in human plasma and applied to a pharmacokinetic study."( Hydrophilic interaction liquid chromatography-tandem mass spectrometry for the determination of adefovir in human plasma and its application to a pharmacokinetic study.
Li, F; Qin, F; Qin, T; Xiong, Z; Yang, S; Zhang, Y, 2010
)
0.36
"A pharmacokinetic trial was conducted to evaluate the potential for once-daily etravirine in antiretroviral regimens without and with darunavir/ritonavir."( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults.
DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010
)
0.36
"Of 23 enrolled patients (male 87%, Caucasian 39%), pharmacokinetic profiles for etravirine were available for 21 and 20 patients on day 14 and 28, respectively."( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults.
DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010
)
0.36
" Pharmacokinetic data were available in 577 patients randomized to receive etravirine."( Pharmacokinetics and pharmacodynamics of the non-nucleoside reverse-transcriptase inhibitor etravirine in treatment-experienced HIV-1-infected patients.
Corbett, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Leopold, L; Nijs, S; Peeters, MP; Schöller-Gyüre, M; Snoeck, E; Vingerhoets, J; Vis, P; Wade, JR; Woodfall, BJ, 2010
)
0.36
" Mean HBIg half-life was 21."( Pharmacokinetics and efficacy of intravenous or intramuscular hepatitis B immunoglobulins in prophylaxis of hepatitis B after liver transplantation.
Andreone, P; Bacci, M; Burra, P; Canova, D; Cursaro, C; Fiorentino, B; Guazzini, S; Marengo, A; Marzano, A; Riili, A; Volpes, R, 2010
)
0.36
" Anti-HBs titers three times higher than aimed and four weeks mean half-life could suggest the reduction of doses and the elongation of the interval of administration of im-HBIg."( Pharmacokinetics and efficacy of intravenous or intramuscular hepatitis B immunoglobulins in prophylaxis of hepatitis B after liver transplantation.
Andreone, P; Bacci, M; Burra, P; Canova, D; Cursaro, C; Fiorentino, B; Guazzini, S; Marengo, A; Marzano, A; Riili, A; Volpes, R, 2010
)
0.36
"Intensive steady-state 24-hour pharmacokinetic profiles were performed during the third trimester and at 6-12 weeks postpartum."( Atazanavir pharmacokinetics with and without tenofovir during pregnancy.
Basar, M; Best, BM; Burchett, SK; Capparelli, EV; Hawkins, E; Hu, C; Mirochnick, M; Read, JS; Rossi, SS; Smith, E; Stek, AM, 2011
)
0.37
" A total of 151 ATV plasma concentrations were obtained, and a population pharmacokinetic model was developed with NONMEM."( Population pharmacokinetics of atazanavir/ritonavir in HIV-1-infected children and adolescents.
Blanche, S; Dollfus, C; Firtion, G; Foissac, F; Hirt, D; Laurent, C; Treluyer, JM; Urien, S, 2011
)
0.37
" We report the pharmacokinetic parameters of tenofovir in combination with efavirenz, darunavir-ritonavir, or atazanavir-ritonavir in HIV-infected children."( Steady-state pharmacokinetics of tenofovir-based regimens in HIV-infected pediatric patients.
Acosta, EP; Britto, P; Carey, V; Graham, B; Hazra, R; Jean-Philippe, P; King, JR; Wiznia, A; Yogev, R, 2011
)
0.37
"Significant pharmacokinetic interactions can result between acid-suppressing agents and some protease inhibitors (PIs) in the management of HIV infection."( Effects of the H2-receptor antagonist famotidine on the pharmacokinetics of atazanavir-ritonavir with or without tenofovir in HIV-infected patients.
Bertz, R; Boffito, M; Child, M; Chung, E; Kashuba, A; Mahnke, L; Patterson, K; Tebas, P; Wang, X; Wu, Y; Zhang, J; Zhu, L, 2011
)
0.37
"Tenofovir concentrations were monitored on a routine basis and measured in 93 children aged 5 to 18 years; 283 tenofovir plasma concentrations were used to perform a population pharmacokinetic analysis."( Population pharmacokinetics of tenofovir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Rey, E; Tréluyer, JM; Urien, S, 2011
)
0.37
" The method was applied to the determination of adefovir in plasma from 12 subjects dosed with adefovir 2 x 10 mg tablets and pharmacokinetic parameters were evaluated."( Rapid high-performance liquid chromatographic method for determination of adefovir in plasma using UV detection: application to pharmacokinetic studies.
Foroutan, SM; Khoddam, A; Movahed, H; Shafaati, A; Zarghi, A, 2011
)
0.37
" The gel also prevents infection in macaques when applied intravaginally or intrarectally prior to challenge with simian-human immunodeficiency virus (SHIV), but very little pharmacokinetic information for macaques is available to help extrapolate the data to humans and thus inform future development activities."( Pharmacokinetics of tenofovir following intravaginal and intrarectal administration of tenofovir gel to rhesus macaques.
Allen, P; Kashuba, A; Nuttall, J; Roberts, J; Romano, J; Wang, R; White, N, 2012
)
0.38
" The alkyl side chains of the 2-cycloalkoxyadenosines were fluorinated, and compounds with moderate antibacterial activity and favorable pharmacokinetic properties in rat and dog were identified."( Discovery of bacterial NAD⁺-dependent DNA ligase inhibitors: improvements in clearance of adenosine series.
Albert, R; Chen, B; Gowravaram, M; Hu, H; Huynh, H; Lu, M; Mills, SD; Mullen, GB; Newman, JV; O'Shea, TJ; Rooney, MT; Stokes, SS, 2012
)
0.38
" More comprehensive in vivo pharmacokinetic data are required to justify the potential use of these agents as safe and effective options during pregnancy."( Pharmacokinetics of antiretroviral drugs in anatomical sanctuary sites: the fetal compartment (placenta and amniotic fluid).
Back, DJ; Else, LJ; Khoo, SH; Taylor, S, 2011
)
0.37
"Comparative pharmacokinetic study in sheep."( Tenofovir and tenofovir disoproxil fumarate pharmacokinetics from intravaginal rings.
Baum, MM; Butkyavichene, I; Gilman, J; Kennedy, S; Kopin, E; Malone, AM; Moss, JA; Motamedi, M; Nguyen, C; Smith, TJ; Vincent, KL; Willis, RA, 2012
)
0.38
" The proposed assay method was found to be applicable to a pharmacokinetic study in human male volunteers."( A novel LC-MS/MS method for simultaneous quantification of tenofovir and lamivudine in human plasma and its application to a pharmacokinetic study.
Burugula, L; Inamadugu, JK; J V L N, SR; Matta, MK; Pilli, NR, 2012
)
0.38
" The impact of changing the current gel formulation to reduce its osmolality was evaluated using pharmacokinetic assessments and local tissue effects in the rabbit."( Pharmacokinetics and topical vaginal effects of two tenofovir gels in rabbits.
Clark, MR; Friend, DR, 2012
)
0.38
" To summarize, the pharmacokinetic profile of efavirenz remained similar in the pregnant and non-pregnant rats."( Pharmacokinetic profiling of efavirenz-emtricitabine-tenofovir fixed dose combination in pregnant and non-pregnant rats.
Bhyrapuneni, G; Kandikere, V; Komarneni, P; Muddana, N; Mudigonda, K; Mukkanti, K; Nirogi, R; Saralaya, R, 2012
)
0.38
" Pharmacokinetic and biodistribution studies were performed in mice to evaluate in vivo fate of the formulations."( Solid lipid nanoparticles and nanosuspension of adefovir dipivoxil for bioavailability improvement: formulation, characterization, pharmacokinetic and biodistribution studies.
Chavhan, S; Dodiya, S; Korde, A; Sawant, KK, 2013
)
0.39
" We developed a pharmacokinetic model for TDF and its active anabolite tenofovir-diphosphate (TFV-DP) and validated it with data from 4 different trials, including 4 distinct dosing regimes."( Pharmacokinetics and pharmacodynamics of the reverse transcriptase inhibitor tenofovir and prophylactic efficacy against HIV-1 infection.
Duwal, S; Schütte, C; von Kleist, M, 2012
)
0.38
"This study was designed to assess the safety, acceptability, pharmacokinetic (PK), and pharmacodynamic (PD) responses to rectal administration of tenofovir (TFV) 1% vaginally formulated gel and oral tenofovir disoproxil fumarate (TDF)."( RMP-02/MTN-006: A phase 1 rectal safety, acceptability, pharmacokinetic, and pharmacodynamic study of tenofovir 1% gel compared with oral tenofovir disoproxil fumarate.
Anton, PA; Bumpus, NN; Carballo-Diéguez, A; Cranston, RD; Cumberland, WG; Dennis, R; Elliott, J; Hendrix, CW; Janocko, L; Ju, C; Kashuba, A; Khanukhova, E; Mauck, C; McGowan, I; Richardson-Harman, N, 2012
)
0.38
"This was a Phase II open-label multiple dose pharmacokinetic and safety study."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"A total of 25 patients (56% male) completed the study; 21 had evaluable pharmacokinetic profiles."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Coadministration of efavirenz, tenofovir and emtricitabine with a standard first-line TB treatment regimen did not significantly alter the pharmacokinetic parameters of these drugs and was tolerated well by Tanzanian TB patients who are coinfected with HIV."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"This is the first pharmacokinetic modelling of antiretroviral disposition in BP and CVF."( Pharmacokinetic modelling of efavirenz, atazanavir, lamivudine and tenofovir in the female genital tract of HIV-infected pre-menopausal women.
Cohen, MS; Dumond, JB; Forrest, A; Garonzik, SM; Kashuba, AD; Kendrick, RN; Nicol, MR; Patterson, KB, 2012
)
0.38
" Twenty-four-hour pharmacokinetic curves were recorded in the third trimester (preferably week 33) and postpartum (preferably week 4-6)."( The pharmacokinetics, safety and efficacy of tenofovir and emtricitabine in HIV-1-infected pregnant women.
Burger, DM; Colbers, AP; Giaquinto, C; Gingelmaier, A; Hawkins, DA; Ivanovic, J; Kabeya, K; Moltó, J; Rockstroh, JK; Sadiq, ST; Taylor, GP; Weizsäcker, K; Wyen, C, 2013
)
0.39
"Although pharmacokinetic exposure of the NRTIs TDF and FTC during pregnancy is approximately 25% lower, this was not associated with virological failure in this study and did not result in mother-to-child transmission."( The pharmacokinetics, safety and efficacy of tenofovir and emtricitabine in HIV-1-infected pregnant women.
Burger, DM; Colbers, AP; Giaquinto, C; Gingelmaier, A; Hawkins, DA; Ivanovic, J; Kabeya, K; Moltó, J; Rockstroh, JK; Sadiq, ST; Taylor, GP; Weizsäcker, K; Wyen, C, 2013
)
0.39
" Drug concentrations at two trough values of 12 and 24 h after dosing (C(12) and C(24)), area under the concentration-curve values (AUC), maximum drug concentration (C(max)), and the time at which this concentration occurred (T(max)) in plasma were estimated with noncompartmental pharmacokinetic methods and compared to data from a subset of white subjects randomized to the RAL twice a day (plus TDF/FTC) arm of the QDMRK study, a phase III study of the safety and efficacy of once daily versus twice daily RAL in treatment naive patients."( Raltegravir pharmacokinetics in treatment-naive patients is not influenced by race: results from the raltegravir early therapy in African-Americans living with HIV (REAL) study.
Blevins, S; Dumond, JB; Eron, JJ; Floris-Moore, M; Hudgens, MG; Kashuba, AD; Massengale, K; Pittard, D; Ragan, D; Richardson, A; Walsh, K; Wang, R; Wohl, DA, 2013
)
0.39
"This study compared the pharmacokinetic profiles of an FDC capsule containing lamivudine/adefovir dipivoxil 100/10 mg and conventional lamivudine 100-mg + adefovir dipivoxil 10-mg tablets to determine bioequivalence."( Pharmacokinetic properties of single-dose lamivudine/adefovir dipivoxil fixed-dose combination in healthy Chinese male volunteers.
Chan, JC; Chen, S; Chu, TT; Fok, BS; Gardner, S; Piscitelli, S; Tomlinson, B, 2013
)
0.39
" The pharmacokinetic profiles of lamivudine and adefovir were similar between the FDC and reference formulations."( Pharmacokinetic properties of single-dose lamivudine/adefovir dipivoxil fixed-dose combination in healthy Chinese male volunteers.
Chan, JC; Chen, S; Chu, TT; Fok, BS; Gardner, S; Piscitelli, S; Tomlinson, B, 2013
)
0.39
" The pharmacokinetic properties and the effects of food intake on tenofovir dipivoxil have not yet been reported in healthy adults."( Pharmacokinetics and food interaction of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy volunteers.
Chen, L; Chen, M; Ding, Y; Jia, Y; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2013
)
0.39
" Pharmacokinetic parameters of tenofovir given in each treatment period were calculated using non-compartmental analysis."( Pharmacokinetics and food interaction of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy volunteers.
Chen, L; Chen, M; Ding, Y; Jia, Y; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2013
)
0.39
"After a single dose of 150, 300 and 600 mg, the main pharmacokinetic parameters for tenofovir were as follows: Cmax 209·6, 456·7, 989·8 ng/mL; AUClast 1744·9, 2663·5, 6010·2 ng h/mL, respectively."( Pharmacokinetics and food interaction of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy volunteers.
Chen, L; Chen, M; Ding, Y; Jia, Y; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2013
)
0.39
" The quantitation method was successfully applied for simultaneous estimation of IC87114, RFM and RFN in a pharmacokinetic drug-drug interaction study in Wistar rats."( Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study.
Mukkanti, K; Thappali, SR; Vakkalanka, SK; Varanasi, KV; Veeraraghavan, S, 2012
)
0.38
"International Maternal Pediatric Adolescent AIDS Clinical Trials Group 1026s is a prospective, nonblinded, pharmacokinetic study of HIV-infected pregnant women taking antiretrovirals for clinical indications, including 2 cohorts (with or without tenofovir) receiving atazanavir/ritonavir 300/100 mg once daily during the second trimester, 400/100 mg during the third trimester, and 300/100 mg postpartum (PP)."( Pharmacokinetics of an increased atazanavir dose with and without tenofovir during the third trimester of pregnancy.
Best, BM; Burchett, SK; Byroads, M; Caparelli, E; Cressey, TR; Hawkins, E; Kreitchmann, R; Mirochnick, M; Rossi, S; Shapiro, DE; Smith, E; Stek, A; Wang, J; Watts, DH, 2013
)
0.39
"Atazanavir pharmacokinetic data were available for 37 women without tenofovir, 35 with tenofovir; median (range) pharmacokinetic parameters are presented for second trimester, third trimester, and PP and number who met target/total."( Pharmacokinetics of an increased atazanavir dose with and without tenofovir during the third trimester of pregnancy.
Best, BM; Burchett, SK; Byroads, M; Caparelli, E; Cressey, TR; Hawkins, E; Kreitchmann, R; Mirochnick, M; Rossi, S; Shapiro, DE; Smith, E; Stek, A; Wang, J; Watts, DH, 2013
)
0.39
" Noncompartmental pharmacokinetic analysis was used to estimate PK parameters [area under the concentration-time curve over 24 h (AUC0-24h ) and maximal concentration (Cmax )]."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
" Compared with the general population, these elderly subjects had 8-13% decreased TFV AUC0-24h and Cmax , and 19-78% increased FTC and RTV AUC0-24h and Cmax ."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
"To investigate pharmacokinetic interactions associated with coadministration of lersivirine with zidovudine, tenofovir disoproxil fumarate (DF)/emtricitabine (Truvada(®)) or abacavir/lamivudine (Epzicom(®)/Kivexa(®))."( Pharmacokinetic interactions between lersivirine and zidovudine, tenofovir disoproxil fumarate/emtricitabine and abacavir/lamivudine.
Choo, HW; Davis, J; Fang, J; Hansson, AG; Langdon, G; Layton, G; Tawadrous, M; Vourvahis, M, 2013
)
0.39
" Pharmacokinetic parameters were calculated by standard non-compartmental methods."( Pharmacokinetic interactions between lersivirine and zidovudine, tenofovir disoproxil fumarate/emtricitabine and abacavir/lamivudine.
Choo, HW; Davis, J; Fang, J; Hansson, AG; Langdon, G; Layton, G; Tawadrous, M; Vourvahis, M, 2013
)
0.39
" Plasma TFV demonstrated triphasic decay with terminal elimination half-life median [interquartile range (IQR)] 69 h (58-77)."( Single dose pharmacokinetics of oral tenofovir in plasma, peripheral blood mononuclear cells, colonic tissue, and vaginal tissue.
Anderson, JR; Bakshi, R; Cao, YJ; Everts, S; Fuchs, EJ; Hendrix, CW; Liberman, RG; Louissaint, NA; Nimmagadda, S; Skipper, PL; Tannenbaum, SR, 2013
)
0.39
" A pharmacokinetic interaction between tenofovir and ritonavir may have resulted in the toxicity."( Tenofovir induced Fanconi syndrome: a possible pharmacokinetic interaction.
Desai, C; Desai, M; Dikshit, RK; Kapadia, J; Patel, S; Shah, AN; Shah, S,
)
0.13
" The method was successfully applied to the pharmacokinetic study of two tenofovir agents."( [Pharmacokinetics of tenofovir in Beagle dogs after oral dosing of tenofovir dipivoxil fumarate using HPLC-MS/MS analysis].
Chen, H; Hu, JP; Li, Y; Sheng, L; Wang, BL, 2013
)
0.39
"The pharmacokinetic data support coadministration of daclatasvir with atazanavir/ritonavir, efavirenz and/or tenofovir."( Assessment of pharmacokinetic interactions of the HCV NS5A replication complex inhibitor daclatasvir with antiretroviral agents: ritonavir-boosted atazanavir, efavirenz and tenofovir.
Bertz, R; Bifano, M; Grasela, D; Hartstra, J; Hwang, C; Kandoussi, H; Oosterhuis, B; Sevinsky, H; Tiessen, R; Velinova-Donga, M, 2013
)
0.39
" Pharmacokinetic sampling was performed on cohort 1 and 3 mothers and all infants."( Pharmacokinetics and safety of tenofovir in HIV-infected women during labor and their infants during the first week of life.
Emel, L; Eshleman, SH; Fowler, MG; George, K; Herron, C; Hudelson, SE; Joao, E; Kearney, B; Kreitchmann, R; Kumwenda, N; Mirochnick, M; Mofenson, L; Nielsen-Saines, K; Parsons, T; Pinto, J; Richardson, P; Santos, B; Sato, P; Taha, T, 2014
)
0.4
" Separate pharmacokinetic properties may be associated with distinct TDF toxicities: tenofovir with parathyroid hormone and altered calcium balance and tenofovir diphosphate with hypophosphatemia and FGF23 regulation."( Association of higher plasma vitamin D binding protein and lower free calcitriol levels with tenofovir disoproxil fumarate use and plasma and intracellular tenofovir pharmacokinetics: cause of a functional vitamin D deficiency?
Baker, A; Bethel, J; Flynn, PM; Gordon, CM; Havens, PL; Hazra, R; Kapogiannis, BG; Kiser, JJ; Liu, N; Lujan-Zilbermann, J; Mulligan, K; Pan, CG; Rutledge, B; Stephensen, CB; Van Loan, MD; Wilson, CM; Woodhouse, LR, 2013
)
0.39
" Increasing epithelial thickness delayed initial TFV delivery to stroma and its decline: tmax increased but AUC at 24 hours was not significantly altered."( Multicompartmental pharmacokinetic model of tenofovir delivery by a vaginal gel.
Gao, Y; Katz, DF, 2013
)
0.39
" In addition to determining the MTD, we evaluated pharmacokinetics of BIIB021 and pharmacodynamic effects of BIIB021 [Hsp70, HER2 extracellular domain (HER2-ECD)]."( A phase 1, dose-escalation, pharmacokinetic and pharmacodynamic study of BIIB021 administered orally in patients with advanced solid tumors.
Banerji, U; Castro, J; Lamanna, N; Mita, M; O'Brien, S; Saif, MW; Stogard, C; Takimoto, C; Von Hoff, D, 2014
)
0.4
" Cmax occurred at approximately 90 minutes and t1/2 was approximately 1 hour across dosing cohorts of 25 to 800 mg BIIB021 twice weekly."( A phase 1, dose-escalation, pharmacokinetic and pharmacodynamic study of BIIB021 administered orally in patients with advanced solid tumors.
Banerji, U; Castro, J; Lamanna, N; Mita, M; O'Brien, S; Saif, MW; Stogard, C; Takimoto, C; Von Hoff, D, 2014
)
0.4
" Although its use for the treatment of HIV has been approved by the Chinese State Food and Drug Administration, there are no data on the pharmacokinetic profile of TDF in Chinese individuals."( Pharmacokinetics and tolerability of Tenofovir disoproxil fumarate 300 mg once daily: an open-label, single- and multiple-dose study in healthy Chinese subjects.
Chen, Q; Dong, J; Hu, CY; Jia, JY; Li, J; Li, X; Liu, Y; Liu, YM; Lu, C; Sun, SX; Wang, W; Wu, K; Yu, C, 2013
)
0.39
"This study aimed to investigate the pharmacokinetic properties and tolerability of TDF in healthy Chinese subjects."( Pharmacokinetics and tolerability of Tenofovir disoproxil fumarate 300 mg once daily: an open-label, single- and multiple-dose study in healthy Chinese subjects.
Chen, Q; Dong, J; Hu, CY; Jia, JY; Li, J; Li, X; Liu, Y; Liu, YM; Lu, C; Sun, SX; Wang, W; Wu, K; Yu, C, 2013
)
0.39
" Pharmacokinetic parameters were estimated using a noncompartmental model."( Pharmacokinetics and tolerability of Tenofovir disoproxil fumarate 300 mg once daily: an open-label, single- and multiple-dose study in healthy Chinese subjects.
Chen, Q; Dong, J; Hu, CY; Jia, JY; Li, J; Li, X; Liu, Y; Liu, YM; Lu, C; Sun, SX; Wang, W; Wu, K; Yu, C, 2013
)
0.39
" TDF exhibited a pharmacokinetic profile similar to that of healthy Western subjects in a historical comparison."( Pharmacokinetics and tolerability of Tenofovir disoproxil fumarate 300 mg once daily: an open-label, single- and multiple-dose study in healthy Chinese subjects.
Chen, Q; Dong, J; Hu, CY; Jia, JY; Li, J; Li, X; Liu, Y; Liu, YM; Lu, C; Sun, SX; Wang, W; Wu, K; Yu, C, 2013
)
0.39
"The objectives of this analysis were to develop a population pharmacokinetic model (PPK) for tenofovir without using potentially unreliable patient reported dosing records and to retrace patient dosing history using pharmacokinetic simulations conditioned on protocol design constraints to assess patient adherence."( Estimation of tenofovir's population pharmacokinetic parameters without reliable dosing histories and application to tracing dosing history using simulation strategies.
Chaturvedula, A; Fossler, MJ; Hendrix, CW, 2014
)
0.4
"To develop a population pharmacokinetic model of adefovir dipivoxil in healthy volunteers and evaluate the effect of individual factors on the pharmacokinetics of adefovir dipivoxil."( Population pharmacokinetics of adefovir dipivoxil tablets in healthy Chinese volunteers.
He, Y; Huang, J; Huang, X; Li, L; Li, Y; Lv, Y; Wang, K; Yang, J; Zhang, Y; Zheng, Q, 2014
)
0.4
" The final pharmacokinetic model was evaluated using a bootstrap method."( Population pharmacokinetics of adefovir dipivoxil tablets in healthy Chinese volunteers.
He, Y; Huang, J; Huang, X; Li, L; Li, Y; Lv, Y; Wang, K; Yang, J; Zhang, Y; Zheng, Q, 2014
)
0.4
"Intensive pharmacokinetic studies of tenofovir in a large, diverse cohort of HIV-infected women over 24 h at steady state were performed and factors that influenced exposure [assessed by areas under the concentration-time curves (AUCs)] identified."( Common clinical conditions - age, low BMI, ritonavir use, mild renal impairment - affect tenofovir pharmacokinetics in a large cohort of HIV-infected women.
Anastos, K; Bacchetti, P; Baxi, SM; Cohen, M; Gandhi, M; Gange, SJ; Greenblatt, RM; Huang, Y; Minkoff, H; Scherzer, R; Shlipak, MG; Young, M, 2014
)
0.4
"HIV-infected women (n = 101) on tenofovir-based therapy underwent intensive 24-h pharmacokinetic sampling."( Common clinical conditions - age, low BMI, ritonavir use, mild renal impairment - affect tenofovir pharmacokinetics in a large cohort of HIV-infected women.
Anastos, K; Bacchetti, P; Baxi, SM; Cohen, M; Gandhi, M; Gange, SJ; Greenblatt, RM; Huang, Y; Minkoff, H; Scherzer, R; Shlipak, MG; Young, M, 2014
)
0.4
" Finally, the method was successfully used in a pharmacokinetic study that measured IC87114 in mouse plasma, BAL fluid and lung tissue after administration of a single 1mg/kg intratracheal dose of IC87114."( Development and validation of a highly sensitive LC-MS/MS method for quantification of IC87114 in mice plasma, bronchoalveolar lavage and lung samples: Application to pharmacokinetic study.
Bhandary, B; Chae, HJ; Kim, SR; Lee, YC; Marahatta, A, 2014
)
0.4
"Administration of 40 mg of tenofovir alafenamide for 14 days resulted in lower tenofovir Cmax (13 versus 207 ng/mL) and lower systemic exposures (AUC0-t, 383 versus 1810 ng · h/mL) compared with subjects who received tenofovir disoproxil fumarate."( Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase inhibitor tenofovir, in HIV-infected adults.
Coakley, D; Kearney, B; Lee, WA; Markowitz, M; Miller, MD; Ruane, P; Squires, K; Wulfsohn, M; Zhong, L; Zolopa, A, 2014
)
0.4
" In this open-label, randomized, three-way crossover study, the pharmacokinetic profiles of elvitegravir, cobicistat, emtricitabine, and tenofovir were evaluated when administered with a standard breakfast, under fasting conditions, or with a nutritional protein-rich drink."( Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Matsuki, S; Nishino, N; Shiomi, M, 2014
)
0.4
" After a single dose, there were no differences in the mean AUC0-∞ values; however, there were significant differences in the mean Tmax values (1."( Pharmacokinetics of single- and multiple-dose emtricitabine in healthy male Chinese volunteers.
Han, WL; Huang, AL; Huang, WX; Shang, JC; Tan, R; Yan, B; Yang, JQ; Zhong, XN, 2014
)
0.4
" The authors studied ATV pharmacokinetic (PK) parameters among children who received atazanavir/ritonavir co-administered with TDF."( Pharmacokinetics of atazanavir/ritonavir among HIV-infected Thai children concomitantly taking tenofovir disoproxil fumarate.
Ananworanich, J; Bunupuradah, T; Keadpudsa, S; Prasitsuebsai, W; Puthanakit, T; Sahakijpicharn, T; Srimuan, A; Techasaensiri, C; Thammajaruk, N, 2014
)
0.4
" We developed a population pharmacokinetic (PK) model for ibrutinib in patients."( Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies.
Advani, R; Byrd, JC; de Jong, J; De Nicolao, G; de Trixhe, XW; Loury, D; Marostica, E; McGreivy, J; O'Brien, S; Poggesi, I; Sukbuntherng, J; Vermeulen, A, 2015
)
0.42
"The objective of this analysis was to develop and qualify a population pharmacokinetic model describing plasma tenofovir (TFV) concentrations and tenofovir-diphosphate (TFV-DP) concentrations in peripheral blood mononuclear cell (PBMC) in healthy women volunteers from the MTN-001 clinical trial, an open label 3-way crossover study of oral tenofovir disoproxil fumarate 300 mg tablet, TFV 1% vaginal gel, or both."( Population pharmacokinetics of tenofovir and tenofovir-diphosphate in healthy women.
Burns, RN; Chaturvedula, A; Hendrix, CW, 2015
)
0.42
" The analytical method was applied to support a pharmacokinetic study of simultaneous estimation of lenalidomide, ibrutinib, and its active metabolite PCI-45227 in Wistar rat."( Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: application to a pharmacokinetic study.
Govindarajulu, B; Rangasamy, M; Thappali, S; Vakkalanka, S; Veeraraghavan, S; Viswanadha, S, 2015
)
0.42
" When corrected for repeated dosing, pharmacokinetic parameters in healthy participants and patients were comparable."( The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia.
Byrd, JC; Chauhan, V; de Jong, J; Hellemans, P; James, D; Jiao, J; Loury, DJ; Mannaert, E; Murphy, J; O'Brien, S; Skee, D; Sukbuntherng, J, 2015
)
0.42
" Finally, the assay was used for a pharmacokinetic study of plasma levels in treated FVB mice."( Liquid chromatography-tandem mass spectrometric assay for the simultaneous determination of the irreversible BTK inhibitor ibrutinib and its dihydrodiol-metabolite in plasma and its application in mouse pharmacokinetic studies.
Beijnen, JH; Rood, JJM; Schellens, JHM; Schinkel, AH; Sparidans, RW; van Hoppe, S, 2016
)
0.43
" The developed method was successfully applied to the pharmacokinetic study of following oral administration of single dose of pradefovir mesylate (10, 30, 60, 90 and 120 mg) and adefovir dipivoxil (10 mg) to healthy Chinese volunteers."( Development and Validation of a Sensitive LC-MS-MS Method for the Determination of Adefovir in Human Serum and Urine: Application to a Clinical Pharmacokinetic Study.
Shen, L; Xiao, QQ; Yang, J; Zhan, Y; Zhang, Y, 2016
)
0.43
" Here, we review the pharmacokinetic and pharmacodynamic information presently available for these drugs, using data obtained in healthy volunteers for pharmacokinetics and data obtained in human clinical trials or animal models for pharmacodynamics."( Ebola Virus Infection: Review of the Pharmacokinetic and Pharmacodynamic Properties of Drugs Considered for Testing in Human Efficacy Trials.
de Lamballerie, X; Guedj, J; Madelain, V; Mentré, F; Nguyen, TH; Olivo, A; Taburet, AM, 2016
)
0.43
" In-vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension."( Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system.
Ezzeldin, E; Iqbal, M; Shakeel, F, 2016
)
0.43
"Based on ibrutinib pharmacokinetics and potential sensitivity towards CYP3A4-mediated drug-drug interactions (DDIs), a physiologically based pharmacokinetic approach was developed to mechanistically describe DDI with various CYP3A4 perpetrators in healthy men under fasting conditions."( Ibrutinib Dosing Strategies Based on Interaction Potential of CYP3A4 Perpetrators Using Physiologically Based Pharmacokinetic Modeling.
De Jong, J; de Zwart, L; Mannaert, E; Monshouwer, M; Snoeys, J; Sukbuntherng, J, 2016
)
0.43
"Between May 22, 2013, and July 22, 2014, we enrolled 50 participants, and all 50 received the assigned treatment; 24 participated in the intensive pharmacokinetic assessment."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
"The elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide regimen was well tolerated and achieved component plasma pharmacokinetic exposures similar to those in adults."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
" Here, we review the available literature on the pharmacokinetic and pharmacodynamic properties of these novel agents to guide the reader in the appropriate use of ibrutinib, idelalisib, and venetoclax."( Pharmacokinetic and Pharmacodynamic Considerations in the Treatment of Chronic Lymphocytic Leukemia: Ibrutinib, Idelalisib, and Venetoclax.
Hill, BT; Waldron, M; Winter, A, 2017
)
0.46
" Pharmacokinetic and biodistribution studies of formula F9 showed a higher accumulation of AD in the liver with enhanced bioavailability compared to AD suspension which highlights its potential advantage for an effective treatment of chronic HBV."( Adefovir dipivoxil loaded proliposomal powders with improved hepatoprotective activity: formulation, optimization, pharmacokinetic, and biodistribution studies.
Abdelbary, GA; Amin, MM; El Awdan, SA; Zakaria, MY, 2018
)
0.48
" To elucidate on-target and pharmacodynamic effects of acalabrutinib, we evaluated several laboratory endpoints, including proteomic changes, chemokine modulation and impact on cell migration."( Pharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy.
Ayres, ML; Balakrishnan, K; Cheung, JP; Gandhi, V; Gay, J; Ivan, C; Keating, MJ; Lamothe, B; Marszalek, JR; Morse, J; Nelson, M; Patel, VK; Wierda, WG, 2018
)
0.48
" Although colonic biopsies should be collected in the absence of medium for accurate TFV concentrations, the presence of medium does not significantly impact TFV-DP-dependent pharmacokinetic or pharmacodynamic assays."( Short Communication: Specimen Processing Impacts Tissue Tenofovir Pharmacokinetic Measurements.
Bakshi, RP; Breakey, J; Fuchs, EJ; Jois, B; Manohar, M; Marzinke, MA, 2018
)
0.48
"A single-arm, prospective, nonrandomized, cross-over, pharmacokinetic study in patients receiving a TDF-containing regimen (TDF 300 mg/FTC 200 mg/EVG 150 mg/COBI 150 mg) switched to a TAF-containing FDC regimen (TAF 10 mg/FTC 200 mg/EVG 150 mg/COBI 150 mg)."( Plasma and intracellular pharmacokinetics of tenofovir in patients switched from tenofovir disoproxil fumarate to tenofovir alafenamide.
Bares, SH; Dyavar, SR; Fletcher, CV; Havens, J; Lee, S; O'Neill, J; Podany, AT; Scarsi, KK; Swindells, S, 2018
)
0.48
"To evaluate and compare the pharmacokinetic and pharmacodynamic properties of 2 investigational Toll-like receptor 7 agonists, TMX-101, and TMX-202 after intravenous and intravesical administration in a rat model."( Pharmacokinetics and pharmacodynamics of intravesical and intravenous TMX-101 and TMX-202 in a F344 rat model.
Falke, J; Hulsbergen-van de Kaa, CA; Maj, R; Oosterwijk, E; Witjes, JA, 2018
)
0.48
" Blood sampling was performed at different time points, including pre-exposure and postexposure to determine the plasma concentrations of study drugs for pharmacokinetic and pharmacodynamic analyses and to determine the plasma concentrations of cytokines (IL-2, IL-6, and TNF-α)."( Pharmacokinetics and pharmacodynamics of intravesical and intravenous TMX-101 and TMX-202 in a F344 rat model.
Falke, J; Hulsbergen-van de Kaa, CA; Maj, R; Oosterwijk, E; Witjes, JA, 2018
)
0.48
"In this study of 14 days each of vaginal and rectal application of TFV reduced-glycerin 1% gel, we found only a small degree of cross-compartment distribution of TFV in RF and vaginal fluids and no pharmacodynamic activity in ex vivo testing."( Pharmacokinetics and Pharmacodynamics of Tenofovir Reduced-Glycerin 1% Gel in the Rectal and Vaginal Compartments in Women: A Cross-Compartmental Study With Directly Observed Dosing.
Balar, B; Dai, JY; Dezzutti, CS; Galaska, B; Hendrix, CW; Justman, JE; Kunjara Na Ayudhya, RP; Levy, L; Marzinke, MA; McGowan, I; Mushamiri, I; Nair, GL; Pan, Z; Piper, JM; Schwartz, JL, 2018
)
0.48
" Population pharmacokinetic models were developed using measured intracellular metabolite, endogenous nucleotide competitors, and extracellular parent drug concentrations."( A Pharmacokinetic/Pharmacodynamic Model to Predict Effective HIV Prophylaxis Dosing Strategies for People Who Inject Drugs.
Chen, J; Cottrell, ML; Dumond, JB; Garrett, KL; Maas, BM; Prince, HA; Schauer, AP; Sykes, C; White, N, 2018
)
0.48
" Here, we describe the pharmacokinetic (PK) observations, along with modeling to further explore the interaction between ibrutinib and rituximab."( Systemic Exposure of Rituximab Increased by Ibrutinib: Pharmacokinetic Results and Modeling Based on the HELIOS Trial.
Avigdor, A; Bartlett, N; Cramer, P; de Jong, J; De Nicolao, G; Demirkan, F; Dilhuydy, MS; Fraser, G; Ganguly, S; Goy, A; Howes, A; Lavezzi, SM; Loscertales, J; Mahler, M; Neyens, M; Poggesi, I; Rule, S; Salman, M; Samoilova, O, 2019
)
0.51
" Its clinical pharmacokinetic profile and influence on the cellular pharmacology of tenofovir diphosphate have not been reported."( Pharmacokinetics of tenofovir monoester and association with intracellular tenofovir diphosphate following single-dose tenofovir disoproxil fumarate.
Alexander, K; Anderson, PL; Brooks, KM; Bushman, LR; Castillo-Mancilla, JR; Ellison, L; Hosek, S; Huhn, GD; Ibrahim, ME; Kerr, BJ; Kiser, JJ; MaWhinney, S; McHugh, C; Tilden, S, 2019
)
0.51
"Tenofovir monoester Cmax and AUC0-4 were 59."( Pharmacokinetics of tenofovir monoester and association with intracellular tenofovir diphosphate following single-dose tenofovir disoproxil fumarate.
Alexander, K; Anderson, PL; Brooks, KM; Bushman, LR; Castillo-Mancilla, JR; Ellison, L; Hosek, S; Huhn, GD; Ibrahim, ME; Kerr, BJ; Kiser, JJ; MaWhinney, S; McHugh, C; Tilden, S, 2019
)
0.51
" The half-life of PMEA in the pradefovir group was 11."( Safety, efficacy, and pharmacokinetics of pradefovir for the treatment of chronic hepatitis B infection.
Chen, H; Ding, Y; Jin, W; Li, C; Li, X; Liu, C; Liu, J; Niu, J; Wu, M; Zhang, D; Zhang, H; Zhu, X, 2020
)
0.56
"A new series of Proteolysis Targeting Chimeras (PROTACs) targeting Bruton's Tyrosine Kinase (BTK) was synthesized, with the goal of improving the pharmacokinetic properties of our previously reported PROTAC, MT802."( Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.
Buhimschi, AD; Crews, CM; Hines, J; Jaime-Figueroa, S; Toure, M, 2020
)
0.56
" The aim of this work is to develop a population pharmacokinetic model for ibrutinib and its dihydrodiol metabolite to quantify pharmacokinetic inter- and intra-individual variability, to evaluate the impact of several covariates on ibrutinib pharmacokinetic parameters, and to examine the relationship between exposure and clinical outcome."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" Pharmacokinetic blood samples were taken from months 1 to 12 after inclusion."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
"A total of 89 patients and 1501 plasma concentrations were included in the pharmacokinetic analysis."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
"We present the first population pharmacokinetic model describing ibrutinib and dihydrodiol-ibrutinib concentrations simultaneously."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" Pharmacokinetic sampling, urine biomarker collection [urine protein (UPCR), retinol binding protein (RBP) and β2 microglobulin (β2M) normalized to creatinine] and safety assessments occurred at the end of each phase."( Pharmacokinetics and renal safety of tenofovir alafenamide with boosted protease inhibitors and ledipasvir/sofosbuvir.
Anderson, PL; Blum, J; Brooks, KM; Bushman, LR; Castillo-Mancilla, JR; Cendali, F; Choi, YJ; Gomez, J; Haas, H; Ibrahim, ME; Johnson, B; Kiser, JJ; MaWhinney, S; Morrow, M; Roon, L; Rowan, SE; Wyles, DL; Zheng, JH, 2020
)
0.56
"In our present experiment, the aim of this paper was to develop and fully validate an accurate and simple ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) assay for simultaneous quantification of acalabrutinib, ibrutinib, and their metabolites (ACP-5862 and PCI-45227) in beagle dog plasma and to survey the pharmacokinetic study of all analytes in beagle dogs."( Simultaneous measurement of acalabrutinib, ibrutinib, and their metabolites in beagle dog plasma by UPLC-MS/MS and its application to a pharmacokinetic study.
Jiang, Z; Lin, G; Shi, L; Wang, Y; Zhang, Y, 2020
)
0.56
"Pregnant women receiving TAF 10 mg with cobicistat or TAF 25 mg without boosting as part of clinical care had intensive pharmacokinetic assessments performed during the second and third trimesters, and 6-12 weeks postpartum."( Pharmacokinetics of tenofovir alafenamide with and without cobicistat in pregnant and postpartum women living with HIV.
Barr, E; Best, BM; Brooks, KM; Capparelli, EV; Chakhtoura, N; Cielo, M; Denson, K; Deville, JG; Espina, R; Febo, IL; George, K; Haubrich, R; Mirochnick, M; Momper, JD; Pinilla, M; Rooney, JF; Rungruengthanakit, K; Shapiro, DE; Smith, E; Stek, AM; Weinberg, A, 2021
)
0.62
"A population pharmacokinetic modeling approach was applied to 39 healthy subjects."( Population Pharmacokinetics of Ibrutinib in Healthy Adults.
Al-Ghazawi, M; Najib, N; Najib, O; Saleh, MI; Salem, I, 2021
)
0.62
" This phase I, open-label, 2-period, 1-way study assessed potential pharmacokinetic (PK) interactions between GSK3640254 and tenofovir alafenamide/emtricitabine (TAF/FTC; including the metabolite tenofovir [TFV]) in healthy volunteers."( A Phase I Evaluation of the Pharmacokinetics and Tolerability of the HIV-1 Maturation Inhibitor GSK3640254 and Tenofovir Alafenamide/Emtricitabine in Healthy Participants.
Butcher, L; Davidson, AM; Johnson, M; Joshi, SR; Lataillade, M; Min, S; Pene Dumitrescu, T; Webster, L; Xu, J; Zhan, J; Zimmerman, E, 2021
)
0.62
" The pharmacokinetic and pharmacodynamic data of acalabrutinib were also discussed."( Assessing the pharmacokinetics of acalabrutinib in the treatment of chronic lymphocytic leukemia.
Li, J; Miao, Y; Xu, W, 2021
)
0.62
"Tenofovir alafenamide (TAF) is a key component of HIV treatment, but pharmacokinetic data supporting the use of TAF during pregnancy are limited."( Pharmacokinetics of Tenofovir Alafenamide With Boosted Protease Inhibitors in Pregnant and Postpartum Women Living With HIV: Results From IMPAACT P1026s.
Barr, E; Best, BM; Brooks, KM; Browning, R; Capparelli, EV; Chakhtoura, N; Deville, JG; Febo, IL; George, K; Knowles, K; Mirochnick, M; Paul, ME; Pinilla, M; Rungruengthanakit, K; Shapiro, DE; Stek, AM, 2022
)
0.72
" Intensive pharmacokinetic assessments were performed during the second and third trimesters and 6-12 weeks postpartum."( Pharmacokinetics of Tenofovir Alafenamide With Boosted Protease Inhibitors in Pregnant and Postpartum Women Living With HIV: Results From IMPAACT P1026s.
Barr, E; Best, BM; Brooks, KM; Browning, R; Capparelli, EV; Chakhtoura, N; Deville, JG; Febo, IL; George, K; Knowles, K; Mirochnick, M; Paul, ME; Pinilla, M; Rungruengthanakit, K; Shapiro, DE; Stek, AM, 2022
)
0.72
" TAF was only quantifiable in 2/25 maternal delivery samples and below the limit of quantification in all cord blood and infant washout samples, likely because of the short half-life of TAF."( Pharmacokinetics of Tenofovir Alafenamide With Boosted Protease Inhibitors in Pregnant and Postpartum Women Living With HIV: Results From IMPAACT P1026s.
Barr, E; Best, BM; Brooks, KM; Browning, R; Capparelli, EV; Chakhtoura, N; Deville, JG; Febo, IL; George, K; Knowles, K; Mirochnick, M; Paul, ME; Pinilla, M; Rungruengthanakit, K; Shapiro, DE; Stek, AM, 2022
)
0.72
" Non-compartmental analyses were performed to quantify the pharmacokinetic parameters."( Plasma and breast milk pharmacokinetics of tenofovir alafenamide in mothers with chronic hepatitis B infection.
Cottrell, M; Crane, H; Di Girolamo, J; Dumond, J; Gane, E; Kashuba, A; Kayes, T; Levy, MT; Lim, TH; Manandhar, S; Symonds, A, 2022
)
0.72
"In this first pharmacokinetic study of TAF monotherapy in breastfeeding women with CHB, concentrations of TAF and TFV were low in breast milk with negligible infant exposure, supporting the use of TAF to prevent MTCT."( Plasma and breast milk pharmacokinetics of tenofovir alafenamide in mothers with chronic hepatitis B infection.
Cottrell, M; Crane, H; Di Girolamo, J; Dumond, J; Gane, E; Kashuba, A; Kayes, T; Levy, MT; Lim, TH; Manandhar, S; Symonds, A, 2022
)
0.72
"The population pharmacokinetic (PK) and exposure-response (E-R) analyses for the safety of ibrutinib for the treatment of chronic graft-versus-host disease (cGVHD) is presented."( Population Pharmacokinetic and Exposure-Safety Analyses of Ibrutinib for the Treatment of Chronic Graft-Versus-Host Disease.
Atluri, H; Iwaki, Y; Mita, S; Ogawa, T, 2023
)
0.91
" Model-based simulations revealed 294% and 515% increases of median tenofovir Cmin in patients with CLCR of 15-29 mL/min (CKD stage 3), and less than 15 mL/min (stage 4), respectively, compared with normal renal function (CLCR = 90-149 mL/min)."( Population pharmacokinetic modelling to characterize the effect of chronic kidney disease on tenofovir exposure after tenofovir alafenamide administration.
Alves Saldanha, S; Andre, P; Buclin, T; Cavassini, M; Courlet, P; Decosterd, LA; Desfontaine, V; Guidi, M; Kusejko, K; Thoueille, P, 2023
)
0.91
" Peer-reviewed publications were included if they met all criteria: adults (≥ 18 years of age) living with or without HIV; report any pharmacokinetic parameter or plasma concentration of at least one of the following ARVs: tenofovir alafenamide fumarate (TAF); doravirine (DOR), rilpivirine (RIL) and etravirine (ETR); darunavir (DRV), tipranavir (TPV) and fostemsavir (FTR); dolutegravir (DTG), raltegravir (RAL), bictegravir (BIC) and elvitegravir (EVG); maraviroc (MVC); ibalizumab (IBA); cobicistat (COBI)."( Pharmacokinetics of Antiretroviral Drugs in Older People Living with HIV: A Systematic Review.
Cardoso, SW; Castro, T; Estrela, R; Grinsztejn, B; Oliveira, VG; Toledo, T; Torres, TS; Veloso, VG, 2023
)
0.91
"Among 97 studies included, 20 reported pharmacokinetic evaluation in older individuals (age ≥ 50 years)."( Pharmacokinetics of Antiretroviral Drugs in Older People Living with HIV: A Systematic Review.
Cardoso, SW; Castro, T; Estrela, R; Grinsztejn, B; Oliveira, VG; Toledo, T; Torres, TS; Veloso, VG, 2023
)
0.91

Compound-Compound Interactions

MPS combined with 3-methyladenine or chloroquine reduced the adhesion rate of AC trophozoites. Proline analogues azetidine-2-carboxylate and hydroxyproline were used to stimulate proline synthesis and benzyladenine-induced shoot organogenesis.

ExcerptReferenceRelevance
" The activity of 9-beta-D-arabinofuranosyladenine 5'-monophosphate, alone or in combination with either of the two inhibitors of adenosine deaminase, was comparable to that of 9-beta-D-arabinofuranosyladenine (ara-A), apparently reflecting the rapid conversion of 9-beta-D-arabinofuranosyladenine 5'-monophosphate to ara-A by L1210/C2 cells."( Antiproliferative effects of 9-beta-D-arabinofuranosyladenine 5'-monophosphate and related compounds in combination with adenosine deaminase inhibitors against mouse leukemia L1210/C2 cells in culture.
Cass, CE; Selner, M; Tan, TH, 1979
)
0.77
"The use of the aqueous extracts of Eleutherococcus senticosus in combination with either cytarabine or N6-(delta 2-isopentenyl)-adenosine gave additive antiproliferative effects against L1210 murine leukemia."( Cytotoxic effects of Eleutherococcus senticosus aqueous extracts in combination with N6-(delta 2-isopentenyl)-adenosine and 1-beta-D-arabinofuranosylcytosine against L1210 leukemia cells.
Hacker, B; Medon, PJ, 1984
)
0.27
" Adefovir and PMPA both demonstrated strong synergistic anti-HIV activity in combination with AZT."( Anti-HIV activity of adefovir (PMEA) and PMPA in combination with antiretroviral compounds: in vitro analyses.
Cherrington, JM; Mulato, AS, 1997
)
0.3
" Proline analogues azetidine-2-carboxylate and hydroxyproline in combination with standardized FPH were used to stimulate proline synthesis and benzyladenine-induced shoot organogenesis by exploiting the proposed proline-linked pentose phosphate pathway (PPP)."( Stimulation of benzyladenine-induced in vitro shoot organogenesis and endogenous proline in melon (Cucumis melo L.) by fish protein hydrolysates in combination with proline analogues.
Haynesworth, K; Kellett, G; Milazzo, MC; Shetty, K; Zheng, Z, 1999
)
0.82
" These drug-drug interactions were not expected, the mechanism(s) is (are) not clear, and additional studies are warranted."( Competing drug-drug interactions among multidrug antiretroviral regimens used in the treatment of HIV- infected subjects: ACTG 884.
Acosta, EP; Cheng, H; Fischl, M; Fletcher, CV; Gulick, RM; Haubrich, R; Hu, XJ; Katzenstein, D; Mills, C; Raasch, R; Remmel, RP, 2000
)
0.31
" We tested MPA alone and in combination with abacavir (ABC), didanosine (DDI), lamivudine (3TC) and tenofovir (TFV) against wild-type human immunodeficiency virus type-1 (HIV-1) and nucleoside reverse transcriptase inhibitor (NRTI)-resistant HIV-1."( Dose proportional inhibition of HIV-1 replication by mycophenolic acid and synergistic inhibition in combination with abacavir, didanosine, and tenofovir.
Coull, JJ; Drusano, GL; Hossain, MM; Margolis, DM, 2002
)
0.31
" This study assessed the safety and efficacy of adefovir dipivoxil alone and in combination with lamivudine compared with ongoing lamivudine therapy in patients with chronic hepatitis B with compensated liver disease and lamivudine-resistant hepatitis B virus (HBV)."( Adefovir dipivoxil alone or in combination with lamivudine in patients with lamivudine-resistant chronic hepatitis B.
Bourliere, M; Brosgart, CL; Buggisch, P; Ebrahimi, R; Gray Df, Df; Hann Hw, Hw; Heathcote, EJ; Kleber, K; Kowdley, K; Martin, P; Peters, MG; Rubin, R; Sullivan, M; Trepo, C; Xiong, S, 2004
)
0.32
"These data, limited to patients with compensated liver disease, indicate that adefovir dipivoxil alone or in combination with ongoing lamivudine therapy provides effective antiviral therapy in patients with lamivudine-resistant HBV."( Adefovir dipivoxil alone or in combination with lamivudine in patients with lamivudine-resistant chronic hepatitis B.
Bourliere, M; Brosgart, CL; Buggisch, P; Ebrahimi, R; Gray Df, Df; Hann Hw, Hw; Heathcote, EJ; Kleber, K; Kowdley, K; Martin, P; Peters, MG; Rubin, R; Sullivan, M; Trepo, C; Xiong, S, 2004
)
0.32
"Mutations selected or deselected during passage of human immunodeficiency virus strain HXB2 or resistant variants with tenofovir (TFV), abacavir (ABC), and lamivudine (3TC) differed depending on the drug combination and virus genotype."( Human immunodeficiency virus type 1 reverse transcriptase mutation selection during in vitro exposure to tenofovir alone or combined with abacavir or lamivudine.
Ait-Khaled, M; Craig, C; Griffin, P; Stone, C; Tisdale, M, 2004
)
0.32
"Tenofovir disoproxil fumarate (tenofovir DF) was studied in combination with rifampin in 24 healthy subjects in a multiple-dose, open-label, single-group, two-period study."( Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers.
Buffels, R; Burger, DM; Droste, JA; Hekster, YA; Kearney, BP; Vanhorssen, PJ; Verweij-van Wissen, CP, 2005
)
0.33
"The nucleotide analogue, tenofovir, has been shown to lower plasma atazanavir levels in pharmacokinetic trials, an interaction that may be partly reversed by the addition of ritonavir, whereas plasma tenofovir levels are themselves raised when the drug is combined with lopinavir/ritonavir."( The steady-state pharmacokinetics of nelfinavir in combination with tenofovir in HIV-infected patients.
Becker, M; Breske, A; Esser, S; Hill, A; Koerber, A; Kopperman, M; Kruse, G; Kurowski, M; Möcklinghoff, C; Ross, B; Stocker, H; Wiehler, H, 2005
)
0.33
" Combination with lamivudine showed no additional benefit over monotherapy during 24 weeks of treatment in these patients."( Adefovir dipivoxil alone or in combination with ongoing lamivudine in patients with decompensated liver disease and lamivudine-resistant hepatitis B virus.
Choi, WB; Chung, YH; Kim, KM; Lee, HC; Lee, YS; Lim, YS; Suh, DJ, 2005
)
0.33
"The drug-drug and drug-food interactions between tenofovir DF and didanosine EC were evaluated in 2 pharmacokinetic studies in healthy adult subjects."( Drug-drug and drug-food interactions between tenofovir disoproxil fumarate and didanosine.
Chen, SS; Cheng, AK; Flaherty, JF; Kaul, S; Kearney, BP; Sayre, JR, 2005
)
0.33
"Tenofovir disoproxil fumarate (DF) has been studied in combination with efavirenz in healthy volunteers and no interaction was found."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.33
" Six different groups were studied: 200 mg nevirapine twice daily, 400 mg nevirapine once daily, 600 mg efavirenz once daily, all without tenofovir DF (groups 1, 2, and 3, respectively), and the same groups with the drugs combined with tenofovir 300 mg once daily (groups 4, 5, and 6, respectively)."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.33
" The most common drugs given with tenofovir were ritonavir or lopinavir-ritonavir (21 of 27 patients), atazanavir (5 of 27 patients), and didanosine (9 of 27 patients)."( Tenofovir-associated acute and chronic kidney disease: a case of multiple drug interactions.
Bedford, J; Braden, G; Hoffman, R; Morris, A; Pizzoferrato, T; Zimmermann, AE, 2006
)
0.33
"Two phase I studies were conducted to assess the plasma pharmacokinetics of telbivudine and potential drug-drug interactions between telbivudine (200 or 600 mg/day) and lamivudine (100 mg/day) or adefovir dipivoxil (10 mg/day) in healthy subjects."( Pharmacokinetics of telbivudine in healthy subjects and absence of drug interaction with lamivudine or adefovir dipivoxil.
Brown, NA; Chao, GC; Fielman, BA; Lloyd, DM; Zhou, XJ, 2006
)
0.33
" Together, these in vitro results indicate that combination with other antiretrovirals does not significantly increase the toxic potential of TFV in RPTECs."( In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells.
Alvarez, ML; Cihlar, T; Cordobilla, B; Domingo, JC; Domingo, P; Giralt, M; Guallar, J; López-Dupla, M; Sánchez de la Rosa, R; Saumoy, M; Torres, F; Vidal, F; Villarroya, F, 2006
)
0.33
"Study 903 is a phase 3 trial with a completed 144-week, double-blind phase comparing tenofovir DF (TDF) to stavudine (d4T) in combination with lamivudine (3TC) and efavirenz (EFV) and an ongoing additional 336-week open-label extension phase."( The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naïve HIV-1-infected patients.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Madruga, JV; Suleiman, JM; Zhong, L,
)
0.13
"We evaluated the mitochondrial toxicity of tenofovir (TFV), emtricitabine (FTC) and abacavir as carbovir (CBV) alone, with each other, and in combination with additional NRTIs."( Mitochondrial toxicity of tenofovir, emtricitabine and abacavir alone and in combination with additional nucleoside reverse transcriptase inhibitors.
Melkaoui, K; Setzer, B; Venhoff, N; Walker, UA, 2007
)
0.34
"Study 903 is a phase 3 trial with a completed 144-week, double-blind phase comparing tenofovir DF (TDF) with stavudine (d4T), in combination with lamivudine (3TC) and efavirenz (EFV), and an ongoing 336-week open-label extension phase."( The safety and efficacy of switching stavudine to tenofovir df in combination with lamivudine and efavirenz in hiv-1-infected patients: three-year follow-up after switching therapy.
Cassetti, I; Cheng, AK; Enejosa, J; Etzel, A; Holmes, CB; Madruga, JR; Suleiman, JM; Zhong, L,
)
0.13
"A prospective cohort study on therapy with adefovir alone (29 patients) or combined with ongoing lamivudine (23 patients) was performed."( Lamivudine-resistant chronic hepatitis B: an observational study on adefovir in monotherapy or in combination with lamivudine.
Alessandria, C; Barbon, V; Carenzi, S; Gaia, S; Lagget, M; Marzano, A; Olivero, A; Rizzetto, M; Smedile, A, 2008
)
0.35
"Most studies of mouse cloning successfully achieved activation of the reconstructed oocytes by strontium (Sr) combined with cytochalasin B (CB) treatment."( Transgenic cloned mice expressing enhanced green fluorescent protein generated by activation stimuli combined with 6-dimethylaminopurine.
Chen, CH; Ju, JC; Lee, KH; Lien, WT; Liu, MS; Stone, L; Tu, CF, 2008
)
0.35
" Pharmacokinetic profiles were also determined in HIV-1-infected patients dosed with raltegravir monotherapy versus raltegravir in combination with TDF and lamivudine."( Lack of a significant drug interaction between raltegravir and tenofovir.
Breidinger, SA; Chen, J; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Kost, JT; Lasseter, KC; Stek, JE; Stone, JA; Teppler, H; Wagner, JA; Wenning, LA, 2008
)
0.35
" regimen and it's recommended by most of the clinical guidelines as a start regimen in combination with two other drugs."( [Clinical data I. Clinical experience with tenofovir in combination with nonnucleoside analogue transcriptase inhibitors].
Arribas López, JR; Bernardino de la Serna, JI; Mora Rillo, M, 2008
)
0.35
" Most data on safety and efficacy in this scenario initially came from clinical trials in which tenofovir was combined with non-nucleoside reverse transcriptase inhibitors."( [Clinical data II. Clinical experience of tenofovir DF in combination with protease inhibitors].
Fiorante, S; Pulido, F, 2008
)
0.35
"Emtricitabine, a nucleoside reverse transcriptase inhibitor (RTI), and tenofovir disoproxil fumarate (tenofovir DF), a nucleotide RTI, as a fixed-dose combination tablet (emtricitabine/tenofovir DF) for once-daily oral administration, are used as the nucleoside/nucleotide RTI backbone in combination with other antiretroviral agents, including ritonavir-boosted protease inhibitors (PIs), in the treatment of adults with HIV-1 infection."( Emtricitabine/tenofovir disoproxil fumarate: in combination with a protease inhibitor in HIV-1 infection.
Perry, CM, 2009
)
0.35
" 43 patients with relapsed/refractory or secondary AML or CML blast crisis were enrolled into two phase I dose-escalation studies investigating amonafide as monotherapy or in combination with cytarabine."( Phase I trials of amonafide as monotherapy and in combination with cytarabine in patients with poor-risk acute myeloid leukemia.
Allen, SL; Bennett, JM; Budman, DR; Capizzi, RL; Kolitz, JE; Lundberg, AS, 2010
)
0.36
"A new drug combination regimen, consisting of raltegravir, emtricitabine and tenofovir disoproxil fumarate (TDF), is described for the treatment of HIV-1 infection."( A new drug combination therapy for treatment-naive patients with HIV-1 infection, consisting of raltegravir, emtricitabine and tenofovir disoproxil fumarate.
De Clercq, E, 2009
)
0.35
" However, N348I significantly decreases tenofovir susceptibility when combined with thymidine analogue mutations and etravirine susceptibility when combined with Y181C."( N348I in HIV-1 reverse transcriptase decreases susceptibility to tenofovir and etravirine in combination with other resistance mutations.
Moore, K; Radzio, J; Sluis-Cremer, N; Sonza, S; Tachedjian, G, 2010
)
0.36
"International, multicenter, open-label, 96-week noninferiority randomized trial of atazanavir/ritonavir 300/100 mg once daily vs lopinavir/ritonavir 400/100 mg twice daily, each in combination with fixed-dose tenofovir/emtricitabine 300/200 mg once daily, in antiretroviral-naive, HIV-1-infected patients."( Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study.
Absalon, J; Andrade-Villanueva, J; Chetchotisakd, P; Corral, J; David, N; Echevarria, J; Lataillade, M; Mancini, M; McGrath, D; Molina, JM; Moyle, G; Percival, L; Wirtz, V; Yang, R, 2010
)
0.36
"To analyze the efficacy of adefovir dipivoxil combined with bicyclol in treatment of HBeAg-positive chronic viral hepatitis B (CHB)."( [The analyse of effectiveness in HBeAg-positive chronic viral hepatitis B treated by adefovir dipivoxil combined with bicyclol].
Sheng, JF; Xiang, DR, 2009
)
0.35
"Forty-eight-week data are presented from this multicenter, randomized, open-label study comparing the safety profiles of abacavir/lamivudine and tenofovir/emtricitabine, both administered with efavirenz, in HLA-B*5701-negative HIV-1-infected adults."( Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study.
Branco, T; Cavassini, M; Domingo, P; Fisher, M; Givens, N; Khuong-Josses, MA; Lim, ML; Moyle, GJ; Norden, AG; Pearce, HC; Podzamczer, D; Post, FA; Rieger, A; Stellbrink, HJ; Vavro, C, 2010
)
0.36
" We investigated the activity of clevudine (CLV) in combination with other nucleoside/nucleotide analogues to determine if these combinations were compatible in vitro."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"Using the HepAD38 cell line, which expresses wild-type HBV, and a real-time PCR assay, we tested the anti-HBV activity of CLV in combination with entecavir, lamivudine, adefovir, tenofovir and telbivudine (TBV)."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"When CLV was combined with entecavir, lamivudine, adefovir or tenofovir, a synergistic antiviral effect was observed; however, the combination of CLV and TBV gave an antagonistic antiviral response."( Evaluation of the in vitro anti-HBV activity of clevudine in combination with other nucleoside/nucleotide inhibitors.
Bao, H; Furman, PA; Korba, B; Micolochick Steuer, HM; Murakami, E; Niu, C; Tolstykh, T, 2010
)
0.36
"Randomised clinical trials addressing benefits and harms of lamivudine or adefovir dipivoxil alone or in combination with hepatitis B immunoglobulins (HBIg) for preventing recurrent HBV infection in patients who are liver transplanted due to HBV infection with or without hepatocellular carcinoma."( Lamivudine or adefovir dipivoxil alone or combined with immunoglobulin for preventing hepatitis B recurrence after liver transplantation.
Guy, DG; Katz, LH; Paul, M; Tur-Kaspa, R, 2010
)
0.36
"A simple, fast and inexpensive method based on dispersive solid phase extraction (DSPE) combined with LC-MS was developed for simultaneous determination of 7 nucleosides and nucleobases (i."( Determination of the nucleosides and nucleobases in Tuber samples by dispersive solid-phase extraction combined with liquid chromatography-mass spectrometry.
Li, HM; Li, YY; Liu, P; Tang, YJ; Wan, DJ, 2011
)
0.37
"We retrospectively evaluated the durability and reasons for discontinuation of nevirapine (NVP) in combination with a tenofovir (TDF) and emtricitabine (FTC) or lamivudine (3TC)-containing antiretroviral therapy (ART) regimen in an Australian outpatient setting."( Clinical experience with nevirapine combined with tenofovir plus emtricitabine or lamivudine-containing regimens in HIV-infected subjects.
Chan, DJ; Jeganathan, S; Maruszak, H; Smith, DE, 2011
)
0.37
" nevirapine on the same background, in naïve HIV-1-infected patients) study compared prospectively ritonavir-boosted atazanavir (ATZ/r) 300 mg/100 mg once daily (qd) with immediate release nevirapine (NVP) 200 mg twice daily or 400 mg qd, each combined with fixed-dose tenofovir 300 mg/emtricitabine 200 mg qd in 569 ARV-naïve HIV-1-infected patients."( Lipid profiles for nevirapine vs. atazanavir/ritonavir, both combined with tenofovir disoproxil fumarate and emtricitabine over 48 weeks, in treatment-naïve HIV-1-infected patients (the ARTEN study).
Andrade-Villanueva, J; Cairns, V; Clotet, B; de Rossi, L; Domingo, P; Gellermann, HJ; Podzamczer, D; Reiss, P; Rockstroh, JK; Soriano, V; Taylor, S, 2011
)
0.37
"ARTEN is a randomized, open-label, non-inferiority trial that compares nevirapine (NVP) 200 mg twice daily or 400 mg once daily to atazanavir/ritonavir (ATZ/r) 300 mg/100 mg once daily, each combined with fixed-dose tenofovir disoproxil fumarate (TDF) 300 mg/emtricitabine (FTC) 200 mg once daily, in antiretroviral-naive HIV-1 patients with CD4(+) T-cell counts <400 (men) and <250 cells/mm(3) (women)."( Nevirapine versus atazanavir/ritonavir, each combined with tenofovir disoproxil fumarate/emtricitabine, in antiretroviral-naive HIV-1 patients: the ARTEN Trial.
Andrade-Villanueva, J; Antunes, F; Arastéh, K; de Rossi, L; Di Perri, G; Domingo, P; Gellermann, H; Lutz, T; Migrone, H; Opravil, M; Podzamczer, D; Soriano, V; Taylor, S, 2011
)
0.37
"NVP demonstrated at week 48 non-inferior antiviral efficacy compared with ATZ/r when given along with TDF/FTC, despite more drug-related discontinuations with NVP than ATZ/r."( Nevirapine versus atazanavir/ritonavir, each combined with tenofovir disoproxil fumarate/emtricitabine, in antiretroviral-naive HIV-1 patients: the ARTEN Trial.
Andrade-Villanueva, J; Antunes, F; Arastéh, K; de Rossi, L; Di Perri, G; Domingo, P; Gellermann, H; Lutz, T; Migrone, H; Opravil, M; Podzamczer, D; Soriano, V; Taylor, S, 2011
)
0.37
" In order to improve ATV exposure, plasma and intracellular (IC) PK of ATV in patients administered with ATV 400 mg once daily and TDF/emtricitabine (FTC) and switched to ATV 200 mg twice daily were studied."( Pharmacokinetics of switching unboosted atazanavir coadministered with tenofovir disoproxil fumarate from 400 mg once daily to 200 mg twice daily in HIV-positive patients.
Baietto, L; Bonora, S; Calcagno, A; D'Avolio, A; Di Perri, G; Gonzalez de Requena, D; Siccardi, M; Simiele, M; Tettoni, M; Trentini, L, 2011
)
0.37
"Entecavir combined with adefovir is an effective rescue therapy in CHB patients after failure of treatment with nucleoside analogs."( [Safety and efficacy of Entecavir combined with Adefovir in patients with chronic hepatitis B who fail to respond to nucleoside analog treatment].
Guo, YB; Hou, JL; Peng, J; Sun, J; Wang, ZH; Yan, L; Yang, J; Zhou, B, 2011
)
0.37
"Limited data are available on the use of unboosted atazanavir in combination with nucleoside reverse transcriptase inhibitors (NRTIs) in treatment-experienced HIV-infected patients."( Efficacy and safety of a switch to unboosted atazanavir in combination with nucleoside analogues in HIV-1-infected patients with virological suppression under antiretroviral therapy.
Ammassari, A; Castagna, A; Delaugerre, C; Ghosn, J; Medrano, J; Molina, JM; Pavie, J; Porcher, R; Rusconi, S; Torti, C; Valin, N, 2011
)
0.37
" NRTIs used in combination with atazanavir were tenofovir, abacavir and emtricitabine/lamivudine in 36."( Efficacy and safety of a switch to unboosted atazanavir in combination with nucleoside analogues in HIV-1-infected patients with virological suppression under antiretroviral therapy.
Ammassari, A; Castagna, A; Delaugerre, C; Ghosn, J; Medrano, J; Molina, JM; Pavie, J; Porcher, R; Rusconi, S; Torti, C; Valin, N, 2011
)
0.37
"In patients with virological suppression and no prior history of virological failure, a switch to unboosted atazanavir in combination with NRTIs is associated with a low probability of virological failure and a good safety profile."( Efficacy and safety of a switch to unboosted atazanavir in combination with nucleoside analogues in HIV-1-infected patients with virological suppression under antiretroviral therapy.
Ammassari, A; Castagna, A; Delaugerre, C; Ghosn, J; Medrano, J; Molina, JM; Pavie, J; Porcher, R; Rusconi, S; Torti, C; Valin, N, 2011
)
0.37
"To investigate the levels of HBsAg in predicting the efficacy of peglated interferon-alpha 2a combined with adefovir dipivoxil (ADV), in HBeAg-positive chronic hepatitis B patients."( [The levels of HBsAg can predict the efficacy of peglated interferon-alpha 2a combined with adefovir dipivoxil, in HBeAg-positive chronic hepatitis B patients].
Cao, H; Li, G; Sun, HX; Xu, QH; Yang, XA; Zhang, K, 2011
)
0.37
"Eligible patients with HIV-1 RNA (vRNA) levels >5000 copies/mL and without baseline resistance to efavirenz, tenofovir, or emtricitabine were randomized in a double-blind, noninferiority study to receive raltegravir or efavirenz, each combined with tenofovir/emtricitabine."( Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK.
Dejesus, E; Dinubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Xu, X; Zhao, J, 2011
)
0.37
"When combined with tenofovir/emtricitabine in treatment-naive patients, raltegravir produced durable viral suppression and immune restoration that was at least equivalent to efavirenz through 156 weeks of therapy."( Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK.
Dejesus, E; Dinubile, MJ; Lazzarin, A; Leavitt, R; Lennox, JL; Nguyen, BY; Rockstroh, JK; Rodgers, AJ; Saag, MS; Sklar, P; Teppler, H; Walker, ML; Wan, H; Xu, X; Zhao, J, 2011
)
0.37
" Mean plasma concentration-time profiles for atazanavir, tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), darunavir (DRV, administered with ritonavir [RTV]), and drospirenone/ethinylestradiol were similar following co-administration of GSK2248761."( Drug interaction profile for GSK2248761, a next generation non-nucleoside reverse transcriptase inhibitor.
de Serres, M; Gould, E; Johnson, M; Kim, J; Lou, Y; Mayers, D; Pietropaolo, K; Piscitelli, S; White, S; Zhou, XJ, 2012
)
0.38
"To study the changes of experimental markers of hepatic fibrosis in patients with chronic hepatitis B treated by Dahuang Zhechong Wan combined with adefovir dipivoxil."( [Experimental study on effect of dahuang zhechong wan combined with adefovir dipivoxil in preventing hepatic fibrosis in patients with chronic hepatitis B].
Chang, Y; Zhang, L, 2012
)
0.38
" The treatment group (50 cases) was orally given 10 mg of adefovir dipivoxil once a day, 1 Wan each time, combined with Dahuang Zhechong Wan, 3 times a day, 1 Wan each time."( [Experimental study on effect of dahuang zhechong wan combined with adefovir dipivoxil in preventing hepatic fibrosis in patients with chronic hepatitis B].
Chang, Y; Zhang, L, 2012
)
0.38
"Dahuang Zhechong Wan combined with adefovir dipivoxil could prevent hepatic fibrosis in patients with chronic hepatitis B, reduce the incidence of liver cirrhosis, improve life quality and prognosis."( [Experimental study on effect of dahuang zhechong wan combined with adefovir dipivoxil in preventing hepatic fibrosis in patients with chronic hepatitis B].
Chang, Y; Zhang, L, 2012
)
0.38
"To investigate the clinical efficacy and safety of adefovir dipivoxil (ADV) in combination with bicyclol for the treatment of chronic hepatitis B (CHB) in seniors."( [The clinical efficacy and safety of adefovir dipivoxil in combination with bicyclol for the treatment of senior patients with chronic hepatitis B].
Cai, SP; Fan, ZP; He, WP; Ji, YJ; Zhang, WJ, 2011
)
0.37
"It suggested that the treatment of ADV in combination with bicyclol for senior patients with CHB is effective and safe."( [The clinical efficacy and safety of adefovir dipivoxil in combination with bicyclol for the treatment of senior patients with chronic hepatitis B].
Cai, SP; Fan, ZP; He, WP; Ji, YJ; Zhang, WJ, 2011
)
0.37
"To explore the durability of three first-line tenofovir/emtricitabine-based regimens in combination with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in HIV-1-infected patients."( Duration of first-line antiretroviral therapy with tenofovir and emtricitabine combined with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in the Italian ARCA cohort.
Borghi, V; Capetti, A; Cicconi, P; Di Biagio, A; Di Giambenedetto, S; Francisci, D; Giacometti, A; Giannarelli, D; Maggiolo, F; Monno, L; Penco, G; Prinapori, R; Sterrantino, G; Zoncada, A, 2013
)
0.39
"To observe the efficacy of adefovir dipivoxil(ADV) in combination with Anluohuaxian capsule in the treatment of chronic hepatitis B (CHB) patients."( [The therapeutic effect of Anluohuaxian capsule combined with adefovir dipivoxil on patients with chronic hepatitis B and influence on hepatic histology].
Gong, GZ; He, B; Jiang, YF; Li, NP; Ma, J; Tang, W, 2012
)
0.38
" 36 cases of treatment group were given ADV combined with Anluohuaxian capsule for 48 weeks."( [The therapeutic effect of Anluohuaxian capsule combined with adefovir dipivoxil on patients with chronic hepatitis B and influence on hepatic histology].
Gong, GZ; He, B; Jiang, YF; Li, NP; Ma, J; Tang, W, 2012
)
0.38
"The results show that the treatment with ADV in combination with Anluohuaxian capsule can play promoting antifibrotic effect and significant improved liver histology of chronic hepatitis B patients."( [The therapeutic effect of Anluohuaxian capsule combined with adefovir dipivoxil on patients with chronic hepatitis B and influence on hepatic histology].
Gong, GZ; He, B; Jiang, YF; Li, NP; Ma, J; Tang, W, 2012
)
0.38
" For TB drugs, equivalence was suggested for peak plasma concentrations when administered with and without efavirenz/tenofovir/emtricitabine."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
0.39
"Drug transporters such as P-glycoprotein and OATPs regulate intestinal permeability of atazanavir and may contribute to its poor oral bioavailability and drug-drug interactions with other protease inhibitors and TDF."( Role of drug efflux and uptake transporters in atazanavir intestinal permeability and drug-drug interactions.
Bendayan, R; Hoque, MT; Kis, O; Walmsley, SL; Zastre, JA, 2013
)
0.39
"Comprehensive information on the effects of cytochrome P450 2B6 (CYP2B6) polymorphisms, clinical factors, and drug-drug interactions on efavirenz concentrations in HIV/tuberculosis-coinfected (HIV/TB) patients is unavailable."( Impact of pharmacogenetic markers of CYP2B6, clinical factors, and drug-drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients.
Lueangniyomkul, A; Mankatitham, W; Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2013
)
0.39
"The study aimed to investigate the efficacy and safety of peginterferon α-2a (PEG IFNα-2a) in combination with lamivudine or adefovir in the treatment of hepatitis B e antigen (HBeAg)-positive chronic hepatitis B (CHB)."( Extended treatment with peginterferon α-2a in combination with lamivudine or adefovir for 96 weeks yields high rates of HBeAg and HBsAg seroconversion.
Cao, ZH; Chen, XY; Liu, YL; Ma, LN; Zhang, HW, 2013
)
0.39
" The objective of this study was to compare changes in body composition between ritonavir-boosted atazanavir (ATV/r) and ritonavir-boosted lopinavir (LPV/r) over 96 weeks using data from a substudy of CASTLE, which compared once-daily ATV/r with twice-daily LPV/r, both in combination with tenofovir disoproxil fumarate/emtricitabine in treatment-naïve patients with HIV-1 infection."( Comparison of body composition changes between atazanavir/ritonavir and lopinavir/ritonavir each in combination with tenofovir/emtricitabine in antiretroviral-naïve patients with HIV-1 infection.
DeGrosky, M; Farajallah, A; Hardy, H; McGrath, D; Moyle, GJ, 2014
)
0.4
" When ATV-LNPs were prepared with ritonavir (RTV), a metabolic and cellular membrane exporter inhibitor, and tenofovir (TFV), an HIV reverse-transcriptase inhibitor, stable, scalable, and reproducible anti-HIV drug combination LNPs were produced."( Evaluation of atazanavir and darunavir interactions with lipids for developing pH-responsive anti-HIV drug combination nanoparticles.
Duan, J; Freeling, JP; Ho, RJ; Koehn, J; Shu, C, 2014
)
0.4
"Electrospun drug-eluting fabrics have enormous potential for the delivery of physicochemically diverse drugs in combination by controlling the underlying material chemistry and fabric microarchitecture."( Delivery of multipurpose prevention drug combinations from electrospun nanofibers using composite microarchitectures.
Blakney, AK; Jiang, YH; Krogstad, EA; Woodrow, KA, 2014
)
0.4
" Finally, we showed that the drug-loaded nanofibers are noncytotoxic and that the antiviral activity of TFV is preserved through the electrospinning process and when combined with LNG."( Delivery of multipurpose prevention drug combinations from electrospun nanofibers using composite microarchitectures.
Blakney, AK; Jiang, YH; Krogstad, EA; Woodrow, KA, 2014
)
0.4
"To investigate the treatment efficacy of adefovir dipivoxil combined with a corticosteroid on hepatitis B virus-associated glomerulonephritis (HBV-GN)."( Efficacy of adefovir dipivoxil combined with a corticosteroid in 38 cases of nephrotic syndrome induced by hepatitis B virus-associated glomerulonephritis.
Li, H; Qiu, L; Xiao, P; Yuan, X; Zhou, Q, 2014
)
0.4
"Adefovir dipivoxil combined with corticosteroids has a certain efficacy on the HBV-GN and displays few adverse reactions."( Efficacy of adefovir dipivoxil combined with a corticosteroid in 38 cases of nephrotic syndrome induced by hepatitis B virus-associated glomerulonephritis.
Li, H; Qiu, L; Xiao, P; Yuan, X; Zhou, Q, 2014
)
0.4
" This study suggests the proof-of-concept that the lower dose of NA in combination with other NA might be the theoretical option for rescue combination therapy in patients with CHB who had failed on prior multiple NA treatments in order to reduce systemic exposure and possible side effects of NA."( Comparison of the efficacies of entecavir 0.5 and 1.0 mg combined with adefovir in patients with chronic hepatitis B who had failed on prior nucleos(t)ide analogue treatments.
Cho, Y; Kim, YJ; Lee, HS; Lee, JH; Yoon, JH; Yu, SJ, 2015
)
0.42
" We investigated the efficacy of the histone deacetylase (HDAC) inhibitor vorinostat combined with one of several B-cell receptor (BCR) signaling inhibitors on MCL cell death and the underlying mechanisms, using MCL cell lines."( The synergistic effect of BCR signaling inhibitors combined with an HDAC inhibitor on cell death in a mantle cell lymphoma cell line.
Hagiwara, K; Iida, H; Kunishima, S; Miyata, Y; Nagai, H; Naoe, T, 2015
)
0.42
" We here compare bortezomib with carfilzomib and LU-102 in MM and MCL in vitro with regard to their effects on pIκB/NF-κB signaling and their cytotoxic activity in combination with ibrutinib."( The novel β2-selective proteasome inhibitor LU-102 decreases phosphorylation of I kappa B and induces highly synergistic cytotoxicity in combination with ibrutinib in multiple myeloma cells.
Bader, J; Besse, L; de Bruin, G; Driessen, C; Geurink, PP; Kisselev, AF; Kraus, J; Kraus, M; Liu, N; Overkleeft, H, 2015
)
0.42
" Anti-CD20 antibodies have improved response and progression-free survival (PFS) when combined with chemotherapy."( Safety and activity of BTK inhibitor ibrutinib combined with ofatumumab in chronic lymphocytic leukemia: a phase 1b/2 study.
Andritsos, LA; Blum, KA; Byrd, JC; Flynn, JM; Grever, MR; Hall, N; Heerema, NA; Jaglowski, SM; James, DF; Johnson, AJ; Jones, JA; Lozanski, G; Maddocks, KJ; Munneke, B; Nagar, V; Neuenburg, JK; Ruppert, AS; Smucker, K; Stefanos, M; West, JS; Woyach, JA, 2015
)
0.42
"International, randomized double-blind active-controlled trial to evaluate the efficacy and safety of COBI vs ritonavir (RTV) as a pharmacoenhancer of atazanavir in combination with emtricitabine/tenofovir disoproxil fumarate in HIV treatment-naive patients followed through week 144."( Brief Report: Cobicistat Compared With Ritonavir as a Pharmacoenhancer for Atazanavir in Combination With Emtricitabine/Tenofovir Disoproxil Fumarate: Week 144 Results.
Abram, ME; Andrade-Villanueva, JF; Antunes, F; Arastéh, K; Cao, H; Chetchotisakd, P; DeJesus, E; Fehr, J; Gallant, JE; Koenig, E; Liu, HC; Rizzardini, G; Szwarcberg, J, 2015
)
0.42
"Ibrutinib combined with rituximab is active and well tolerated in patients with relapsed or refractory mantle cell lymphoma."( Ibrutinib in combination with rituximab in relapsed or refractory mantle cell lymphoma: a single-centre, open-label, phase 2 trial.
Addison, A; Badillo, M; Champlin, R; Chen, W; Chuang, H; DeLa Rosa, M; Fayad, L; Hagemeister, F; Lam, L; Lee, H; Li, S; Medeiros, LJ; Nomie, K; Oki, Y; Romaguera, J; Samaniego, F; Santos, D; Turturro, F; Wagner-Bartak, N; Wang, ML; Westin, J; Young, KH; Zhang, H; Zhang, L; Zhao, D, 2016
)
0.43
"Between Sept 19, 2012, and Jan 21, 2014, 578 eligible patients were randomly assigned to ibrutinib or placebo in combination with bendamustine plus rituximab (289 in each group)."( Ibrutinib combined with bendamustine and rituximab compared with placebo, bendamustine, and rituximab for previously treated chronic lymphocytic leukaemia or small lymphocytic lymphoma (HELIOS): a randomised, double-blind, phase 3 study.
Avigdor, A; Balasubramanian, S; Bartlett, NL; Chanan-Khan, A; Cramer, P; Demirkan, F; Dilhuydy, MS; Fraser, G; Goy, A; Grosicki, S; Hallek, M; Howes, A; Janssens, A; Karlsson, C; Loscertales, J; Mahler, M; Mato, A; Mayer, J; Panagiotidis, P; Pavlovsky, MA; Phelps, C; Pristupa, A; Pylypenko, H; Rule, S; Salman, M; Samoilova, O; Silva, RS; Sun, S; Villa, D, 2016
)
0.43
" Moreover, we show that the efficacy of DSR-29133 was significantly improved when administered in combination with low-dose fractionated radiotherapy (RT)."( Intravenous administration of the selective toll-like receptor 7 agonist DSR-29133 leads to anti-tumor efficacy in murine solid tumor models which can be potentiated by combination with fractionated radiotherapy.
Adlard, AL; Cheadle, EJ; Dovedi, SJ; Eguchi, K; Hirose, Y; Honeychurch, J; Hughes, G; Illidge, TM; Jewsbury, PJ; Koga-Yamakawa, E; Murata, M; Ota, Y; Stratford, IJ; Sugaru, E; Umehara, H; Wilkinson, RW; Yamamoto, S, 2016
)
0.43
" The aim of this study is to investigate the synergistic anticancer effect of resveratrol in combination with cisplatin and the potential anticancer mechanisms involved in A549 cells."( The synergistic effect of resveratrol in combination with cisplatin on apoptosis via modulating autophagy in A549 cells.
Hu, S; Kong, H; Li, X; Wang, H; Xie, W; Xu, R; Ye, L; Zeng, X, 2016
)
0.43
" Here, we report in vivo data for OTX015 in combination with the histone deacetylase inhibitor vorinostat, the Bruton's tyrosine kinase inhibitor ibrutinib, the anti-CD20 monoclonal antibody rituximab, and the mTOR inhibitor everolimus in a diffuse large B cell lymphoma model."( Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma.
Bernasconi, E; Bertoni, F; Cascione, L; Cvitkovic, E; Gaudio, E; Odore, E; Ponzoni, M; Rezai, K; Rinaldi, A; Riveiro, E; Stathis, A; Tarantelli, C; Zucca, E, 2016
)
0.43
" Ublituximab in combination with ibrutinib resulted in rapid and high response rates."( Ublituximab (TG-1101), a novel glycoengineered anti-CD20 antibody, in combination with ibrutinib is safe and highly active in patients with relapsed and/or refractory chronic lymphocytic leukaemia: results of a phase 2 trial.
Brooks, HD; Burke, JM; Fanning, S; Farber, CM; Greenwald, DR; Klein, L; Kolibaba, KS; Mahadevan, D; Miskin, HP; Schreeder, MT; Sharman, JP; Sportelli, P; Weiss, MS, 2017
)
0.46
" Thirteen different TKIs were combined with or without SZU-101 and studied to determine their effects on immunocytes."( Immunomodulatory and Antitumor Effects of a Novel TLR7 Agonist Combined with Lapatinib.
Diao, Y; Gao, N; Jiang, W; Jin, G; Jin, Z; Li, W; Liu, Y; Wang, X; Wang, Z; Zhong, J, 2016
)
0.43
"We investigated whether a fixed-dose combination tablet of elvitegravir, cobicistat, emtricitabine, and tenofovirDF (Stribild) can be crushed and combined with enteral nutrition without influencing pharmacokinetics."( Brief Report: Pharmacokinetics of Crushed Elvitegravir Combination Tablet Given With or Without Enteral Nutrition.
Abbink, E; Burger, D; Colbers, A; Duisenberg-van Essenberg, M; Jongbloed-de Hoon, M; Kruijssen, M; van Crevel, R; Velthoven-Graafland, K, 2017
)
0.46
" To the best of our knowledge, this is the first report of severe hypokalemia and proximal tubular renal dysfunction as a result of a possible drug-drug interaction between vinblastine, tenofovir and ritonavir-boosted atazanavir."( Severe hypokalemia due to a possible drug-drug interaction between vinblastine and antiretrovirals in a HIV-infected patient with Hodgkin's lymphoma.
Arcondo, F; Cordova, E; Morganti, L; Odzak, A; Rodriguez, C; Silva, M; Zylberman, M, 2017
)
0.46
"The aim of the study was to evaluate the effect of multipurpose contact lens (CL) solution (MPS) combined with autophagy inhibitors on the adhesion properties of Acanthamoeba castellanii (AC) trophozoites to silicone hydrogel CLs."( Effect of Multipurpose Solution Combined With Autophagy Inhibitors on Adhesion of Acanthamoeba trophozoites to Silicone Hydrogel Contact Lenses.
Lee, DI; Lee, JE; Lee, JS; Lee, SM; Park, SH; Yu, HS, 2017
)
0.46
" We analyzed the efficacy of MPS combined with autophagy inhibitors, 3-methyladenine (0."( Effect of Multipurpose Solution Combined With Autophagy Inhibitors on Adhesion of Acanthamoeba trophozoites to Silicone Hydrogel Contact Lenses.
Lee, DI; Lee, JE; Lee, JS; Lee, SM; Park, SH; Yu, HS, 2017
)
0.68
"MPS combined with 3-methyladenine or chloroquine reduced the adhesion rate of AC trophozoites rather than MPS containing only polyhexamethylene biguanide."( Effect of Multipurpose Solution Combined With Autophagy Inhibitors on Adhesion of Acanthamoeba trophozoites to Silicone Hydrogel Contact Lenses.
Lee, DI; Lee, JE; Lee, JS; Lee, SM; Park, SH; Yu, HS, 2017
)
0.76
"Our results demonstrate that apigenin regulates OAT1, and can cause TDI or herb-drug interaction (HDI) when used in combination with acyclovir or adefovir."( Apigenin, a novel candidate involving herb-drug interaction (HDI), interacts with organic anion transporter 1 (OAT1).
Cao, Y; Chen, J; Fu, W; Li, H; Pang, J; Wu, T; Zhou, P, 2017
)
0.46
" We conducted a single-center phase 1 study evaluating dose-escalated ibrutinib, in a 3-by-3 design, in combination with rituximab, ifosfamide, carboplatin, and etoposide (R-ICE) in physiologically transplant-eligible rel/ref DLBCL patients."( A phase 1 study of ibrutinib in combination with R-ICE in patients with relapsed or primary refractory DLBCL.
Courtien, AI; Devlin, SM; Drullinsky, P; Gerecitano, J; Kumar, A; Matasar, MJ; McCall, SJ; Miller, ST; Moskowitz, CH; Noy, A; Palomba, ML; Portlock, CS; Sauter, CS; Schoder, H; Straus, DJ; Younes, A; Zelenetz, AD, 2018
)
0.48
" The recommended phase 2 dose of umbralisib when given in combination with ibrutinib was 800 mg once daily."( Umbralisib in combination with ibrutinib in patients with relapsed or refractory chronic lymphocytic leukaemia or mantle cell lymphoma: a multicentre phase 1-1b study.
Arnason, JE; Bazemore, J; Boruchov, AM; Brown, JR; Davids, MS; Fisher, DC; Francoeur, K; Hellman, JM; Jacobsen, ED; Jacobson, CA; Kim, HT; Maegawa, R; Miskin, HP; Nicotra, A; Rueter, J; Savell, A; Sportelli, P; Stampleman, L, 2019
)
0.51
" The aim of this study was to assess the safety and activity of ibrutinib in combination with nivolumab in patients with relapsed or refractory B-cell malignant diseases."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
" The primary objective of part A (dose escalation) was to assess the safety of daily oral ibrutinib (420 mg or 560 mg) in combination with intravenous nivolumab (3 mg/kg every 2 weeks) to ascertain a recommended phase 2 dose in patients with relapsed or refractory high-risk chronic lymphocytic leukaemia or small lymphocytic lymphoma (del17p or del11q), follicular lymphoma, or diffuse large B-cell lymphoma."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
"Ibrutinib alone or in combination with cytarabine or azacitidine demonstrated an acceptable safety profile."( Clinical Experience With Ibrutinib Alone or in Combination With Either Cytarabine or Azacitidine in Patients With Acute Myeloid Leukemia.
Cortes, JE; Graef, T; Jonas, BA; Luan, Y; Stein, AS, 2019
)
0.51
"As a tool to be used in transporter-mediated drug-drug interaction studies, a sensitive LC-MS/MS method for the simultaneous quantification of adefovir and pitavastatin in human plasma and adefovir in urine was developed and successfully validated."( Quantification of adefovir and pitavastatin in human plasma and urine by LC-MS/MS: A useful tool for drug-drug interaction studies.
Fuhr, U; Kinzig, M; Scherf-Clavel, O; Sörgel, F; Stoffel, MS, 2019
)
0.51
"We evaluated ibrutinib, a once-daily inhibitor of Bruton's tyrosine kinase, combined with bortezomib and dexamethasone in patients with relapsed or relapsed/refractory multiple myeloma who had received 1-3 prior therapies."( A phase 2 study of ibrutinib in combination with bortezomib and dexamethasone in patients with relapsed/refractory multiple myeloma.
Anagnostopoulos, A; Briso, EM; Cascavilla, N; Dobkowska, E; García Sanz, R; Hajek, R; Hauns, B; Lee, Y; Martin Sánchez, J; Oriol, A; Ozcan, M; Pour, L; Špička, I; Terjung, A, 2020
)
0.56
"Ibrutinib combined with bortezomib and dexamethasone elicited clinical responses."( A phase 2 study of ibrutinib in combination with bortezomib and dexamethasone in patients with relapsed/refractory multiple myeloma.
Anagnostopoulos, A; Briso, EM; Cascavilla, N; Dobkowska, E; García Sanz, R; Hajek, R; Hauns, B; Lee, Y; Martin Sánchez, J; Oriol, A; Ozcan, M; Pour, L; Špička, I; Terjung, A, 2020
)
0.56
" This study assessed the in vitro and in vivo functionality of CAR T cells transduced to express the anti-CD19 CAR of liso-cel in combination with ibrutinib or acalabrutinib."( Antitumor Potency of an Anti-CD19 Chimeric Antigen Receptor T-Cell Therapy, Lisocabtagene Maraleucel in Combination With Ibrutinib or Acalabrutinib.
Baturevych, A; Clouser, CR; Hause, RJ; Johnstone, TG; Jones, JC; Krejsa, CM; Ponce, R; Ports, MO; Qin, JS; Ragan, SP; Salmon, RA, 2020
)
0.56
" Therefore, we investigated the characteristics of autophagic response to ARN-509 treatment and evaluated the potential effect of a combination with autophagy inhibition."( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells.
Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020
)
0.56
" Cells were treated with ARN-509 (50 µM) alone or in combination with the autophagy inhibitors 3-methyladenine (3MA, 5 mM) or chloroquine (Chl, 20 µM) or with ATG5 siRNA knock-down."( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells.
Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020
)
0.77
" Furthermore, in combination with autophagy inhibitors, ARN-509 provided a significantly elevated antitumor effect, thus providing a new therapeutic approach potentially translatable to patients."( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells.
Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020
)
0.56
" High-dose chemotherapy regimens such as DA-EPOCH should be administered to young patients in combination with rituximab."( Chidamide combined with ibrutinib improved the prognosis of primary bone marrow diffuse large B cell lymphoma.
Chen, Z; Li, Y; Tian, C, 2020
)
0.56
" However, BTKi have a range of drug-drug and drug-food interactions, which may alter drug efficacy and/or increase toxicity."( Drug interactions with Bruton's tyrosine kinase inhibitors: clinical implications and management.
Fancher, KM; Pappacena, JJ, 2020
)
0.56
" These variants were subsequently combined with replacement of the cysteine 481 residue to which irreversible inhibitors, such as ibrutinib, acalabrutinib and zanubrutinib, bind."( BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib.
Berglöf, A; Estupiñán, HY; Mohammad, DK; Schaafsma, GCP; Shi, Y; Smith, CIE; Vihinen, M; Wang, Q; Yu, L; Zain, R; Zhou, L, 2021
)
0.62
" He was placed on intravenous immunoglobulin (IVIg) in combination with ibrutinib."( [Intravenous immunoglobulin in combination with ibrutinib for the treatment of IgM-type M protein associated peripheral neuropathy complicated with chronic lymphocytic leukemia].
Kawano, K; Kawano, Y; Miyazaki, Y; Ohtsuka, E; Saburi, M; Sakata, M; Takata, H; Uchida, H, 2021
)
0.62
" The highest tested dose of ibrutinib, 560 mg once daily, was combined with a fixed dose of pembrolizumab 200 mg every 3 weeks for the phase 2 portion."( A phase 1/2 trial of ibrutinib in combination with pembrolizumab in patients with mismatch repair proficient metastatic colorectal cancer.
Carballido, E; Imanirad, I; Kim, DW; Kim, RD; Martinez, M; Mehta, R; Schell, MJ; Strosberg, J; Tan, E; Yu, J; Zhou, JM, 2021
)
0.62
" Herein, we investigated the effects of the two drugs on UDP-glucuronosyltransferase (UGT) activities to evaluate their potential risk for drug-drug interactions (DDIs) via UGT inhibition."( Comparison of the drug-drug interactions potential of ibrutinib and acalabrutinib via inhibition of UDP-glucuronosyltransferase.
Cao, J; Fan, X; Jiang, L; Liu, Y; Wang, X; Wang, Z; Xia, Y; Yan, M, 2021
)
0.62
"The aim of this international multicentre study was to review potential drug-drug interactions (DDIs) for real-life coadministration of combination antiretroviral therapy (cART) and coronavirus disease 2019 (COVID-19)-specific medications."( Retrospective evaluation of an observational cohort by the Central and Eastern Europe Network Group shows a high frequency of potential drug-drug interactions among HIV-positive patients receiving treatment for coronavirus disease 2019 (COVID-19).
Antoniak, S; Begovac, J; Dragovic, G; Fleischhans, L; Gokengin, D; Harxhi, A; Hofman, S; Jilich, D; Kase, K; Kowalska, J; Lakatos, B; Matulionyte, R; Oprea, C; Papadopoulus, A; Rukhadze, N; Vassilenko, A; Vasyliev, M; Verhaz, A; Wasilewski, P; Yancheva, N, 2022
)
0.72
" We hypothesized that a tailored treatment with ibrutinib in combination with rituximab (IR) could obtain significant responses in these patients."( Ibrutinib in Combination With Rituximab for Indolent Clinical Forms of Mantle Cell Lymphoma (IMCL-2015): A Multicenter, Open-Label, Single-Arm, Phase II Trial.
Aymerich, M; Beà, S; Campo, E; Casanova, M; Cortés-Romera, M; de la Cruz, F; de la Fuente, A; García Sanz, R; Giné, E; González Barca, E; González-López, TJ; Jiménez Ubieto, A; López Jimenez, J; López-Guillermo, A; Marín-Niebla, A; Martín García-Sancho, A; Medina Herrera, A; Muntañola, A; Nadeu, F; Rodríguez, S; Rotger, A; Setoain, X; Terol, MJ, 2022
)
0.72
"We retrospectively enrolled 70 unresectable HCC patients who were seropositive for HBsAg and accepted tenofovir alafenamide fumarate (TAF) therapy before anti-PD-1 in combination with an antiangiogenic treatment."( Interaction between baseline HBV loads and the prognosis of patients with HCC receiving anti-PD-1 in combination with antiangiogenic therapy undergoing concurrent TAF prophylaxis.
Chen, J; Hu, X; Li, Q; Li, R; Yuan, G; Zang, M, 2022
)
0.72
"Baseline HBV loads do not affect the prognosis of HCC patients receiving anti-PD-1 in combination with an antiangiogenic therapy, while PD-1 inhibitors do not aggravate HBV reactivation and hepatic impairment in patients simultaneously subjected to TAF prophylaxis."( Interaction between baseline HBV loads and the prognosis of patients with HCC receiving anti-PD-1 in combination with antiangiogenic therapy undergoing concurrent TAF prophylaxis.
Chen, J; Hu, X; Li, Q; Li, R; Yuan, G; Zang, M, 2022
)
0.72
"Extensive evidence suggests that gut microbiota may interact with the kidneys and play central roles in the pathogenesis of disease."( Gut-Kidney Impairment Process of Adenine Combined with
Deng, N; Li, X; Peng, M; Peng, X; Qiao, B; Tan, Z; Yu, R, 2022
)
1
"Lenacapavir warrants further investigation as a potential antiretroviral used orally and as injection in combination with other antiretroviral drugs."( Lenacapavir administered every 26 weeks or daily in combination with oral daily antiretroviral therapy for initial treatment of HIV: a randomised, open-label, active-controlled, phase 2 trial.
Baeten, JM; Benson, P; Berhe, M; Crofoot, G; Dvory-Sobol, H; Gupta, SK; Koenig, E; Liu, SY; McDonald, C; Ramgopal, M; Rhee, MS; Ruane, P; Sanchez, WE; Scribner, A; Sims, J; VanderVeen, LA, 2023
)
0.91
" The aim was to investigate the expression of IL-1β in CHB patients treated with Peg-IFN-α combination with TDF and TDF/Peg-IFN-α monotherapy."( The expression of interleukin-1β in patients with chronic hepatitis B treated with pegylated-interferon-alpha combined with tenofovir disoproxil fumarate and monotherapy.
Hu, X; Li, Y; Luo, H; Qin, B; Tan, G, 2023
)
0.91
" A single-center cohort study of prospective recruitment of CHB patients: untreated CHB (Group A), TDF combined with Peg-IFN-α therapy (Group B), Peg-IFN-α monotherapy (Group C), TDF monotherapy (Group D)."( The expression of interleukin-1β in patients with chronic hepatitis B treated with pegylated-interferon-alpha combined with tenofovir disoproxil fumarate and monotherapy.
Hu, X; Li, Y; Luo, H; Qin, B; Tan, G, 2023
)
0.91
"The increased expression of IL-1β may enhance the efficacy of TDF combined with Peg-IFN-α therapy in achieving an early response for CHB patients."( The expression of interleukin-1β in patients with chronic hepatitis B treated with pegylated-interferon-alpha combined with tenofovir disoproxil fumarate and monotherapy.
Hu, X; Li, Y; Luo, H; Qin, B; Tan, G, 2023
)
0.91
" However, there is little data regarding the impact of this drug-drug Interaction in PLWH, which makes health care providers reluctant to prescribe them together."( The clinical impact of rifampicin-based anti-TB therapy and tenofovir alafenamide-containing ARV regimen drug Interaction in people living with HIV: Case series report.
Alamer, A; Almulhim, A; Alrashed, A; Alwafai, S; Cahusac, P; Damfu, N; Mohzari, YA; Musawa, MA; Zaeri, B, 2023
)
0.91
" The objective of this study was to report the clinical impact of this drug-drug interaction (rifampicin + TAF-containing antiretroviral (ARV) regimen) on HIV viral load control in PLWH."( The clinical impact of rifampicin-based anti-TB therapy and tenofovir alafenamide-containing ARV regimen drug Interaction in people living with HIV: Case series report.
Alamer, A; Almulhim, A; Alrashed, A; Alwafai, S; Cahusac, P; Damfu, N; Mohzari, YA; Musawa, MA; Zaeri, B, 2023
)
0.91

Bioavailability

A new series of phosphonodiester derivatives incorporating carboxyesterase-labile S-acyl-2-thioethyl (SATE) moieties was prepared in an attempt to increase the oral bioavailability of PMEA. GS-7340 is a prodrug which is orally bioavailable in dogs as the intact prodrug and has demonstrated anti-HIV activity in cell culture of over 1000-fold greater than that of PMPA.

ExcerptReferenceRelevance
"A study was done on the factors which could modify the oral bioavailability of two new cytotoxic molecules (mitonafide and 2HCl amonafide) when administered in solid form."( Studies about the oral bioavailability of mitonafide and 2HCl amonafide, two new cytotoxic molecules.
Camacho Sánchez, MA; Torres Suárez, AI, 1992
)
0.28
"The mechanism of transport of desciclovir (DCV)--a structural analogue and prodrug of acyclovir (ACV) which provides an improved oral bioavailability of ACV--was investigated in human erythrocytes with a "papaverine-stop" assay."( Desciclovir permeation of the human erythrocyte membrane by nonfacilitated diffusion.
Domin, BA; Mahony, WB; Zimmerman, TP, 1991
)
0.28
"Potential oral prodrugs of the antiherpesvirus acyclonucleoside 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (1, BRL 39123) have been synthesized and evaluated for bioavailability of 1 in the blood of mice."( Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.28
" Studies were designed to assess the bioavailability of 5-phosphoribosyl-1-pyrophosphate (PRPP) in the diabetic renal cortex because PRPP is an important determinant of the de novo synthesis of nucleotides."( Phosphoribosylpyrophosphate bioavailability in diabetic rat renal cortex in vivo.
Cortes, P; Levin, NW; Schoenberger, AM; Venkatachalam, KK; Verghese, CP, 1980
)
0.26
" Prospective bioavailability was determined using amylase as indicator enzyme."( Studies on the quality of pancreatic preparations: enzyme content, prospective bioavailability, bile acid pattern, and contamination with purines.
König, J; Molitor, M; Neef, B; Niessen, KH, 1983
)
0.27
"A number of esters and amides of the anti-HIV nucleotide analogue 9-[2-(phosphonomethoxy)-ethoxy]adenine (1) have been synthesized as potential prodrugs and evaluated for oral bioavailability in mice."( Synthesis and in vivo evaluation of prodrugs of 9-[2-(phosphonomethoxy)ethoxy]adenine.
Ashton, RJ; Bailey, S; Harnden, MR; Jackson, SM; Serafinowska, HT; Sutton, D, 1995
)
0.74
"The bioavailability of PMEA from three oral formulations of the prodrug bis(POM)-PMEA has been evaluated in fasted male cynomolgus monkeys."( Oral bioavailability of the antiretroviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) from three formulations of the prodrug bis(pivaloyloxymethyl)-PMEA in fasted male cynomolgus monkeys.
Cundy, KC; Fishback, JA; Lee, ML; Lee, WA; Shaw, JP; Soike, KF; Visor, GC, 1994
)
0.52
"A series of phosphonate prodrugs were evaluated in an attempt to increase the oral bioavailability of the anti-HIV agent 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA; 1)."( Synthesis, oral bioavailability determination, and in vitro evaluation of prodrugs of the antiviral agent 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA).
Hitchcock, MJ; Mansuri, MM; Martin, JC; Russell, J; Starrett, JE; Tortolani, DR; Whiterock, V, 1994
)
0.69
" The oral bioavailability of PMEA in this species (4."( Oral, subcutaneous, and intramuscular bioavailabilities of the antiviral nucleotide analog 9-(2-phosphonylmethoxyethyl) adenine in cynomolgus monkeys.
Cundy, KC; Lee, WA; Shaw, JP, 1994
)
0.5
"The pharmacokinetics and bioavailability of adefovir [9-[2-(phosphonomethoxy)ethyl]adenine] were examined at two dose levels in three phase I/II studies in 28 human immunodeficiency type 1-infected patients."( Clinical pharmacokinetics of adefovir in human immunodeficiency virus type 1-infected patients.
Barditch-Crovo, P; Collier, AC; Cundy, KC; Ebeling, D; Jaffe, HS; Toole, J; Walker, RE, 1995
)
0.52
" Taken together, these promising findings suggest that an orally bioavailable prodrug of MDL 74,968 should be developed for the treatment of HIV infection."( MDL 74,968, a new acyclonucleotide analog: activity against human immunodeficiency virus in vitro and in the hu-PBL-SCID.beige mouse model of infection.
Ahmed, PS; Brennan, TM; Bridges, CG; Casara, P; Hornsperger, JM; Navé, JF; Taylor, DL; Tyms, AS, 1996
)
0.29
", bis(pivaloyloxymethyl)-PMEA [bis(POM)-PMEA] and diphenyl-PMEA, have been synthesized in an attempt to increase the oral bioavailability of this broad-spectrum antiviral agent."( Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
Balzarini, J; Bischofberger, N; De Clercq, E; Naesens, L, 1996
)
0.51
" Additional studies will be needed to determine whether a similar mutation in HIV RT develops in patients receiving PMEA or its orally bioavailable prodrug adefovir dipivoxil (bis-POM PMEA)."( In vitro selection and molecular characterization of human immunodeficiency virus type 1 with reduced sensitivity to 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA).
Anderson, B; Cherrington, JM; Foli, A; Gu, Z; Kavlick, M; Mitsuya, H; Saville, MW; Sogocio, KM; Wainberg, MA; Yarchoan, R, 1996
)
0.49
"A new series of hitherto unknown 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA) phosphonodiester derivatives incorporating carboxyesterase-labile S-acyl-2-thioethyl (SATE) moieties as transient phosphonate-protecting groups was prepared in an attempt to increase the oral bioavailability of the antiviral agent PMEA."( Synthesis, in vitro antiviral evaluation, and stability studies of bis(S-acyl-2-thioethyl) ester derivatives of 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA) as potential PMEA prodrugs with improved oral bioavailability.
Aubertin, AM; Benzaria, S; Gosselin, G; Imbach, JL; Johnson, R; Maury, G; Obert, G; Pélicano, H, 1996
)
0.74
"The oral bioavailability of PMEA [9-[2-(phosphonomethoxy)ethyl]adenine; adefovir) has been determined in rats from three bisester prodrugs of PMEA: bis-(pivaloyloxymethyl) PMEA (bis-POM PMEA), bis-(phenyl) PMEA, and bis-(o-ethoxyphenyl) PMEA."( Pharmacokinetics and metabolism of selected prodrugs of PMEA in rats.
Arimilli, MN; Bidgood, AM; Cundy, KC; Jones, RJ; Krishnamurthy, VV; Lee, WA; Louie, MS; Shaw, JP, 1997
)
0.54
"The effect of formulation on oral bioavailability of the antiviral nucleotide analogue adefovir from the prodrug adefovir dipivoxil was examined in beagle dogs."( Oral formulations of adefovir dipivoxil: in vitro dissolution and in vivo bioavailability in dogs.
Cundy, KC; Lee, WA; Marshburn, J; Nakamura, C; Shaw, JP; Sue, IL; Visor, GC, 1997
)
0.3
" Adefovir dipivoxil, an orally bioavailable prodrug of adefovir is currently in phase III clinical trials for the treatment of HIV and phase II clinical trials for the treatment of HBV infections."( Anti-HIV activity of adefovir (PMEA) and PMPA in combination with antiretroviral compounds: in vitro analyses.
Cherrington, JM; Mulato, AS, 1997
)
0.3
"A series of prodrugs designed to enhance the oral bioavailability of the antiretroviral agent 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA; 1) have been synthesized, including a bis-(acyloxymethyl) ester 2 and a series of bis-(alkoxycarbonyloxymethyl) esters 3-9."( Metabolism and pharmacokinetics of novel oral prodrugs of 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA) in dogs.
Arimilli, MN; Cundy, KC; Kim, CU; Lee, WA; Oliyai, R; Shaw, JP; Sueoko, CM, 1997
)
0.72
" Oral bioavailability of PMPA from each prodrug was determined in fasted beagle dogs."( Metabolism and pharmacokinetics of novel oral prodrugs of 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA) in dogs.
Arimilli, MN; Cundy, KC; Kim, CU; Lee, WA; Oliyai, R; Shaw, JP; Sueoko, CM, 1997
)
0.52
" In fasted beagle dogs, bis-[(pivaloyloxy)methyl] PMPA (bis-POM PMPA) 2 had the highest oral bioavailability as PMPA (37."( Metabolism and pharmacokinetics of novel oral prodrugs of 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA) in dogs.
Arimilli, MN; Cundy, KC; Kim, CU; Lee, WA; Oliyai, R; Shaw, JP; Sueoko, CM, 1997
)
0.52
"5-fold lower than Plumen, (84 +/- 12) x 10(-6) cm/s, which means that 77 +/- 6% of 6-Cl-ddP was metabolized during its intestinal transport, thus qualitatively accounting for the low oral bioavailability (7%) of 6-Cl-ddP observed in vivo in rats."( Absorption and intestinal metabolism of purine dideoxynucleosides and an adenosine deaminase-activated prodrug of 2',3'-dideoxyinosine in the mesenteric vein cannulated rat ileum.
Anderson, BD; Ho, NF; Singhal, D, 1998
)
0.3
"1 microg/mL logarithmic mean lumenal concentration of EHNA was effective in increasing the intestinal bioavailability of Cl-ddP to > 90%."( Optimization of the local inhibition of intestinal adenosine deaminase (ADA) by erythro-9-(2-hydroxy-3-nonyl)adenine: enhanced oral delivery of an ADA-activated prodrug for anti-HIV therapy.
Anderson, BD; Singhal, D, 1998
)
0.51
" We recently described the synthesis, metabolism, and biological activities of bis(isopropyloxymethylcarbonyl)PMPA [bis(poc)PMPA] as an orally bioavailable prodrug for PMPA."( Antiviral activities of 9-R-2-phosphonomethoxypropyl adenine (PMPA) and bis(isopropyloxymethylcarbonyl)PMPA against various drug-resistant human immunodeficiency virus strains.
Fridland, A; Srinivas, RV, 1998
)
0.55
"Adefovir dipivoxil [bis(pivaloyloxymethyl)-ester prodrug], an orally bioavailable prodrug of adefovir [9-(2-phosphonylmethoxyethyl)adenine], is currently in phase III clinical trials for the treatment of human immunodeficiency virus (HIV)."( Genotypic and phenotypic characterization of human immunodeficiency virus type 1 variants isolated from AIDS patients after prolonged adefovir dipivoxil therapy.
Anton, KE; Cherrington, JM; Hellmann, NS; Lamy, PD; Li, WX; Miller, MD; Mulato, AS, 1998
)
0.5
" Cidofovir and adefovir are dianionic at physiological pH and have low oral bioavailability in animals and humans."( Clinical pharmacokinetics of the antiviral nucleotide analogues cidofovir and adefovir.
Cundy, KC, 1999
)
0.3
" It has better oral bioavailability than the parent compound."( Adefovir dipivoxil.
Goa, KL; Noble, S, 1999
)
0.3
" Valganciclovir, a prodrug of ganciclovir, offers excellent oral bioavailability and is the closest to approval of all the new anti-CMV drugs."( Therapeutic developments in cytomegalovirus retinitis.
Hoffman, VF; Skiest, DJ, 2000
)
0.31
"2 h, and the oral bioavailability of adefovir was estimated to be 22."( Antiviral efficacy and pharmacokinetics of oral adefovir dipivoxil in chronically woodchuck hepatitis virus-infected woodchucks.
Brown, C; Cullen, JM; Cundy, KC; Eisenberg, EJ; Gibbs, C; Li, DH; Toole, J; Wolfe, J, 2001
)
0.31
" GS-7340 (9-[(R)-2-[[[[(S)-1-(isopropoxycarbonyl)ethyl] amino] phenoxy-phosphinyl]-methoxy] propyl] adenine) is a prodrug which is orally bioavailable in dogs as the intact prodrug and has demonstrated anti-HIV activity in cell culture of over 1000-fold greater than that of PMPA."( Metabolism of GS-7340, a novel phenyl monophosphoramidate intracellular prodrug of PMPA, in blood.
Eisenberg, EJ; He, GX; Lee, WA,
)
0.35
"The practical synthesis of a mixed phenoxy-amidate derivative of PMPA with high oral bioavailability and favorable pharmacokinetics is described."( Practical synthesis, separation, and stereochemical assignment of the PMPA pro-drug GS-7340.
Chapman, H; Kernan, M; Prisbe, E; Rohloff, J; Sparacino, M; Terhorst, T; Yu, R,
)
0.13
"Intestinal enzyme inhibition may be an effective tool to increase the oral bioavailability of compounds that undergo first-pass intestinal metabolism."( Enhanced oral bioavailability of 2'- beta-fluoro-2',3'-dideoxyadenosine (F-ddA) through local inhibition of intestinal adenosine deaminase.
Anderson, BD; DeGraw, RT, 2001
)
0.31
"5 microg/ml could achieve an intestinal bioavailability of 80% with <20% systemic inhibition."( Enhanced oral bioavailability of 2'- beta-fluoro-2',3'-dideoxyadenosine (F-ddA) through local inhibition of intestinal adenosine deaminase.
Anderson, BD; DeGraw, RT, 2001
)
0.31
" In the present study, the synthesis, oral bioavailability and antiretroviral activity of a new prodrug of PMEA, consisting of two molecules of PMEA bound together by a P-O-P bond (Bis-PMEA), are reported."( Pharmacokinetic and antiretroviral activity in mice of oral [P(1),P(2)-bis[2-(adenin-9-yl)ethoxymethyl]phosphonate], a prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
Cappellacci, L; Casabianca, A; Celeste, AG; Cerasi, A; Chiarantini, L; Dominici, S; Franchetti, P; Grifantini, M; Magnani, M; Rossi, L; Serafini, S, 2002
)
0.51
"1 mg/kg, which was 30-fold potent than that of Imiquimod, and showed a good oral bioavailability (F=81%)."( Synthesis and structure-activity relationships of 2-amino-8-hydroxyadenines as orally active interferon inducing agents.
Hirota, K; Ichii, S; Isobe, Y; Kawakami, H; Kurimoto, A; Ogino, T; Ogita, H; Sajiki, H; Takaku, H; Tobe, M, 2003
)
0.56
"03 mg/kg, which was approximately 100-fold more potent than that of Imiquimod, and showed an excellent oral bioavailability (F=40%) which was 10-fold improved over 5, a lead compound (F=4%)."( Synthesis and evaluation of 2-substituted 8-hydroxyadenines as potent interferon inducers with improved oral bioavailabilities.
Hirota, K; Ichii, S; Isobe, Y; Kawakami, H; Kurimoto, A; Ogino, T; Ogita, H; Sajiki, H; Takaku, H; Tobe, M, 2004
)
0.58
"In order to improve the oral bioavailability of 9-benzyl-8-hydroxy-2-(2-hydroxyethylthio)adenine (SM-295072), a potent interferon (IFN) inducing agent, we synthesized prodrugs of it by utilizing the hydroxy groups at the C(2)-side chain and/or the C(8)-position."( Prodrugs of 9-benzyl-8-hydroxy-2-(2-hydroxyethylthio)adenine: potent interferon inducing agents in monkeys.
Ichii, S; Isobe, Y; Kawakami, H; Kurimoto, A; Ogino, T; Ogita, H; Takaku, H; Tobe, M, 2004
)
0.79
" The oral bioavailability of tenofovir is enhanced by administration with a high-fat meal, but is similar at steady state when administered with or without a typical meal."( Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics.
Flaherty, JF; Kearney, BP; Shah, J, 2004
)
0.32
" Oral absorption and bioavailability were 29."( Single-dose pharmacokinetics and metabolism of [14C]remofovir in rats and cynomolgus monkeys.
Lin, CC; Lourenco, D; Xu, C; Yeh, LT; Zhu, N, 2005
)
0.33
" After a single oral dose of GS 7340 (10 mg-eq/kg tenofovir) to male beagle dogs, the plasma bioavailability of tenofovir compared to an intravenous dose of tenofovir was 17%."( Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.
Cihlar, T; Cundy, KC; Eisenberg, E; He, GX; Lee, WA; Mulato, A; Swaminathan, S, 2005
)
0.33
" However, (S)-HPMPA is not orally bioavailable and has not been developed for clinical use."( Synthesis and antiviral evaluation of alkoxyalkyl derivatives of 9-(S)-(3-hydroxy-2-phosphonomethoxypropyl)adenine against cytomegalovirus and orthopoxviruses.
Beadle, JR; Ciesla, SL; Hartline, C; Hostetler, KY; Keith, KA; Kern, ER; Wan, WB, 2006
)
0.55
" Physicochemical properties, cellular permeation, renal toxicity, and bioavailability all had to be addressed during the development of these compounds."( Perspectives on the development of acyclic nucleotide analogs as antiviral drugs.
Lee, WA; Martin, JC, 2006
)
0.33
" Alkoxyalkyl esters of CDV have an increased oral bioavailability and are more active against orthopoxviruses than the parent compounds."( In vitro evaluation of the anti-orf virus activity of alkoxyalkyl esters of CDV, cCDV and (S)-HPMPA.
Andrei, G; Beadle, JR; Dal Pozzo, F; De Clercq, E; Hostetler, KY; Lebeau, I; Snoeck, R, 2007
)
0.34
" From these results, additional studies will be needed to determine whether a similar mutation in HIV RT develops in patients receiving PMPA or its orally bioavailable prodrug, tenofovir dipivoxil fumarate."( In vitro selection and characterization of human immunodeficiency virus type 1 resistant to Zidovudine and tenofovir.
Hong, SK; Lee, SG; Paik, SY; Park, SS; Yoo, WC; Yoon, JS, 2007
)
0.34
" Tenofovir is not orally bioavailable but becomes orally active against HIV-1 infection as the disoproxil ester (tenofovir disoproxil fumarate [Viread])."( Evaluation of hexadecyloxypropyl-9-R-[2-(Phosphonomethoxy)propyl]- adenine, CMX157, as a potential treatment for human immunodeficiency virus type 1 and hepatitis B virus infections.
Aldern, KA; Almond, MR; Beadle, JR; De Clercq, E; Hostetler, KY; Korba, BE; Lampert, BM; Neyts, J; Painter, GR; Trost, LC, 2007
)
0.58
" However, the ether lipid esters of (S)-HPMPA, hexadecyloxypropyl-[(S)-HPMPA] [HDP-(S)-HPMPA] and octadecyloxyethyl-[(S)-HPMPA] [ODE-(S)-HPMPA], had significantly enhanced activity in vitro and are orally bioavailable in mice."( Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
Beadle, JR; Collins, DJ; Herrod, BP; Hostetler, KY; Keith, KA; Kern, ER; Quenelle, DC; Trahan, J, 2007
)
0.56
" The lead prodrug (14, MB06866, pradefovir), identified from a variety of in vitro and in vivo assays, exhibited good oral bioavailability (F = 42%, mesylate salt, rat) and rate of prodrug conversion to ADV-DP."( Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B.
Boyer, SH; Colby, TJ; Craigo, W; DaRe, J; Erion, MD; Fujitaki, JM; Gómez-Galeno, JE; Matelich, MC; Ollis, K; Reddy, KR; Sun, Z; Ugarkar, BG; van Poelje, PD, 2008
)
0.35
"Cidofovir [(S)-1-(3-hydroxy-2-phosphonomethoxypropyl)cytosine] and (S)-HPMPA [(S)-9-(3-hydroxy-2-phosphonomethoxypropyl)adenine] are potent nucleoside phosphonate antiviral agents that are not orally bioavailable unless one or both of their negative charges are masked."( Synthesis of cidofovir and (S)-HPMPA ether lipid prodrugs.
Beadle, JR, 2007
)
0.55
" This drug is administered orally in the form of disoproxil ester, which is deesterified to achieve a bioavailability of more than 20%."( [Tenofovir: pharmacology and interactions].
Azanza, JR; García Quetglas, E; Gómez-Giu, A; Sádaba, B, 2008
)
0.35
" These findings may be valuable in developing formulation strategies to optimize ocular bioavailability of topically administered ocular agents."( Expression of multidrug resistance associated protein 5 (MRP5) on cornea and its role in drug efflux.
Herndon, BL; Karla, PK; Mitra, A; Pal, D; Quinn, TL; Thomas, P, 2009
)
0.35
" The bioavailability of CsA and FK506 seems to be associated with the cytocrhome P450 IIIA (CYP3A) gene."( Genetic polymorphisms in CYP3A5 and MDR1 genes and their correlations with plasma levels of tacrolimus and cyclosporine in renal transplant recipients.
Breitenfeld, L; Martinho, A; Mendes, J; Mota, A; Pais, L; Simoes, O, 2009
)
0.35
" HDP-(S)-HPMPA is orally bioavailable and provides excellent liver exposure to the drug."( Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
Beadle, JR; Hostetler, KY; Korba, BE; Morrey, JD; Wyles, DL, 2009
)
0.59
" To pursue compounds with better biopharmaceutical properties, we have developed a series of fully synthetic orally bioavailable inhibitors of Hsp90."( BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance.
Burrows, F; Lough, R; Lundgren, K; Neely, L; Timple, N; Yang, YC; Zhang, H, 2010
)
0.36
"Adefovir dipivoxil is a diester prodrug of the antiviral drug adefovir, with much greater oral bioavailability than adefovir."( Role of basolateral efflux transporter MRP4 in the intestinal absorption of the antiviral drug adefovir dipivoxil.
Ming, X; Thakker, DR, 2010
)
0.36
"This study evaluated the relative bioavailability and pharmacokinetics of elvitegravir (EVG), emtricitabine (FTC), tenofovir disoproxil fumarate (TDF), and a investigational pharmacoenhancer, cobicistat (GS-9350, COBI) coformulated as a fixed-dose combination tablet (FDC) compared with ritonavir-boosted EVG and FTC + TDF in healthy subjects."( Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV.
German, P; Hui, J; Kearney, BP; Warren, D; West, S, 2010
)
0.36
" To increase bioavailability of these compounds, synthesis of their structurally diverse ester prodrugs was carried out: alkoxyalkyl (hexadecyloxypropyl, octadecyloxyethyl, hexadecyloxyethyl), pivaloyloxymethyl (POM), 2,2,2-trifluoroethyl, butylsalicylyl, and prodrugs based on peptidomimetics."( Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents.
Andrei, G; Balzarini, J; Brehová, P; Cihlar, T; De Clercq, E; Dracínský, M; Holý, A; Hui, H; Krecmerová, M; Laflamme, G; Masojídková, M; Naesens, L; Neyts, J; Pohl, R; Pomeisl, K; Snoeck, R; Tichý, T, 2010
)
0.36
" The results indicate that the previously observed enhanced oral bioavailability of 2a relative to the parent drug is unlikely to be due to active transport by hPEPT1."( Serine side chain-linked peptidomimetic conjugates of cyclic HPMPC and HPMPA: synthesis and interaction with hPEPT1.
Kashemirov, BA; Krylov, IS; McKenna, CE; Peterson, LW; Sala-Rabanal, M; Serpi, M, 2010
)
0.36
" The lead candidates, both 1a (PBHBV-001) and 3c (PBHBV-2-15), were well-tolerated in both normal and HBV-transgenic mice and exhibited acceptable pharmacokinetics and bioavailability in Sprague-Dawley rats."( Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion.
Block, TM; Clearfield, E; Cuconati, A; Goddard, C; Guo, H; Mills, C; Morrey, JD; Motter, NE; Xiao, T; Xu, X; Yu, W; Zhao, K, 2011
)
0.37
" (l)-Tyr-NH-i-Bu cHPMPA (11) was converted in rat or mouse plasma solely to two active metabolites and had significantly enhanced oral bioavailability vs parent drug 1 in a mouse model (39% vs <5%)."( Tyrosine-based 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine and -adenine ((S)-HPMPC and (S)-HPMPA) prodrugs: synthesis, stability, antiviral activity, and in vivo transport studies.
Borysko, KZ; Breitenbach, JM; Collins, M; Drach, JC; Hilfinger, JM; Kashemirov, BA; Krylov, IS; McKenna, CE; Peterson, LW; Serpi, M; Zakharova, VM, 2011
)
0.6
" A BW allometric scaling was used; and the typical population estimates (interindividual variability), standardized for 70 kg, for apparent clearance, central and peripheral volume of distribution, intercompartmental clearance, and absorption rate constant, were 59."( Population pharmacokinetics of tenofovir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Rey, E; Tréluyer, JM; Urien, S, 2011
)
0.37
" In addition, the bioavailability of tenofovir dipivoxil fumarate was evaluated in healthy male fasted subjects after a single comparatively equivalent dose."( Relative bioavailability study of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy male fasted volunteers.
Ding, Y; Jia, Y; Liu, W; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2012
)
0.38
" Bioavailability of the drug was assessed in accordance with the State Food and Drug Administration bioequivalence criteria."( Relative bioavailability study of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy male fasted volunteers.
Ding, Y; Jia, Y; Liu, W; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2012
)
0.38
"The relative bioavailability of tenofovir dipivoxil was 20% higher compared with tenofovir disoproxil fumarate; this result was consistent with the preclinical data."( Relative bioavailability study of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy male fasted volunteers.
Ding, Y; Jia, Y; Liu, W; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2012
)
0.38
"Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter."( Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
Bradford, C; Bursavich, M; Carlson, RO; Chan, A; Cimbora, DM; Gerrish, D; Hoarau, C; McKinnon, R; Papac, DI; Patton, S; Reeves, L; Roth, BL; Saunders, M; Shenderovich, M; Slattum, P; Vijay Kumar, D; Williams, BL; Yager, K, 2012
)
0.38
"The present study was aimed at developing colloidal formulations like solid lipid nanoparticles (SLN) and nanosuspension (NS) for improving bioavailability of adefovir dipivoxil (AD), a nucleoside reverse transcriptase inhibitor which displays poor oral bioavailability."( Solid lipid nanoparticles and nanosuspension of adefovir dipivoxil for bioavailability improvement: formulation, characterization, pharmacokinetic and biodistribution studies.
Chavhan, S; Dodiya, S; Korde, A; Sawant, KK, 2013
)
0.39
" These efforts led to the identification of orally bioavailable 28g that exhibits good in vitro profiles and a characteristic molecular biomarker signature of Hsp90 inhibition both in vitro and in vivo."( Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor.
Baichwal, V; Bajji, A; Bartel, P; Carlson, R; Cimbora, D; Kim, SH; Markovitz, B; McKinnon, R; Papac, D; Robinson, R; Shenderovich, M; Tangallapally, R; Trovato, R; Wettstein, D; Yager, KM, 2012
)
0.38
" Using an in vivo model system, we report a simple and sensitive liquid chromatography-tandem mass spectrometry assay to quantify the bioavailability of a recently developed novel cyclin-dependent kinase inhibitor VMY-1-103, a purvalanol B-based analog whose biological activity is enhanced via dansylation."( Quantifying the CDK inhibitor VMY-1-103's activity and tissue levels in an in vivo tumor model by LC-MS/MS and by MRI.
Albanese, C; Das, S; Fricke, ST; Karam, S; Lee, YC; Lisanti, MP; Moasser, B; Ozcan, A; Petricoin, E; Pishvaian, M; Ringer, L; Rodriguez, OC; Rood, B; Salinas, P; Schlegel, R; Sirajuddin, P; Sivakumar, A; Üren, A; Wang, SS; Wang, Y; Yenugonda, V, 2012
)
0.38
"Drug transporters such as P-glycoprotein and OATPs regulate intestinal permeability of atazanavir and may contribute to its poor oral bioavailability and drug-drug interactions with other protease inhibitors and TDF."( Role of drug efflux and uptake transporters in atazanavir intestinal permeability and drug-drug interactions.
Bendayan, R; Hoque, MT; Kis, O; Walmsley, SL; Zastre, JA, 2013
)
0.39
" The bioavailability of tenofovir dipivoxil fumarate was increased by approximately 25% as measured by AUClast after a single dose when taken with food, compared with fasting."( Pharmacokinetics and food interaction of a novel prodrug of tenofovir, tenofovir dipivoxil fumarate, in healthy volunteers.
Chen, L; Chen, M; Ding, Y; Jia, Y; Lu, C; Song, Y; Sun, X; Wen, A; Yang, J, 2013
)
0.39
" NVP-BEZ235 is a novel, orally bioavailable dual PI3K/mTOR inhibitor that has exhibited promising activity against HCC in preclinical models."( Dual PI3K/mTOR inhibitor NVP-BEZ235-induced apoptosis of hepatocellular carcinoma cell lines is enhanced by inhibitors of autophagy.
Chang, Z; Guo, H; Guo, X; Jia, X; Jin, J; Luo, F; Shi, G; Song, Y, 2013
)
0.39
" The degree to which this fast reaction with NO by red cell microparticles influences NO bioavailability depends on several factors that are explored here."( Nitric oxide scavenging by red cell microparticles.
Christ, GJ; Gladwin, MT; Kim-Shapiro, DB; Liu, C; Zhao, W, 2013
)
0.39
" Bruton's tyrosine kinase (BTK) shows constitutive activity in CLL and is the target of irreversible inhibition by ibrutinib, an orally bioavailable kinase inhibitor that has shown outstanding activity in CLL."( Bruton's tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL).
Bojnik, E; Buggy, JJ; Byrd, JC; Chang, BY; Davis, ME; Dubovsky, JA; Efremov, DG; Gobessi, S; Goettl, VM; Harrington, BK; Johnson, AJ; Laurenti, L; MacMurray, J; Ruppert, AS; Smith, LL; Smucker, KA; Stefanovski, MR; Towns, WH; Woyach, JA, 2014
)
0.4
" The absolute bioavailability of VMA-99-82 is 66%."( [Absolute bioavailability of the adenine derivative VMA-99-82 possessing antiviral activity].
Kuznetsov, KA; Ozerov, AA; Riabukha, AF; Smirnova, LA; Suchkov, EA, 2013
)
0.67
" These findings suggest that elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate should be administered with food, and that the bioavailability of elvitegravir and tenofovir is not affected by the type of meal ingested."( Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Matsuki, S; Nishino, N; Shiomi, M, 2014
)
0.4
"Nonionic surfactant vesicles (niosomes) were formulated with an aim of enhancing the oral bioavailability of tenofovir disoproxil fumarate (TDF), an anti-HIV drug."( Formulation and characterization of drug loaded nonionic surfactant vesicles (niosomes) for oral bioavailability enhancement.
Bala, S; Kamboj, S; Saini, V, 2014
)
0.4
" We report here the sequential modification of UNC1062 to address DMPK properties and yield a new potent and highly orally bioavailable Mer inhibitor, 11, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow."( UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
Cummings, CT; DeRyckere, D; Earp, HS; Frye, SV; Glaros, TG; Graham, DK; Hunter, D; Janzen, WP; Kireev, D; Lee, M; Liu, J; Minson, KA; Newton, DL; Sather, S; Stashko, MA; Wang, X; Zhang, D; Zhang, W, 2014
)
0.4
"Due to the differences between bioavailability of efavirenz (EFV) and tenofovir (TDF), the single-tablet regimen of EFV/emtricitabine (FTC)/TDF is not approved as initial antiretroviral therapy (ART) in Europe by the European Medical Agency."( Safety and efficacy of coformulated efavirenz/emtricitabine/tenofovir single-tablet regimen in treatment-naive patients infected with HIV-1.
De Castro, N; Delaugerre, C; Flandre, P; Gallien, S; Molina, JM; Nguyen, N, 2015
)
0.42
" The fasting state was characterized by a 67 % relative bioavailability compared with the meal conditions used in the trials and administration after a high-fat meal."( Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies.
Advani, R; Byrd, JC; de Jong, J; De Nicolao, G; de Trixhe, XW; Loury, D; Marostica, E; McGreivy, J; O'Brien, S; Poggesi, I; Sukbuntherng, J; Vermeulen, A, 2015
)
0.42
" An adherence adjustment was included to account for nonadherence by explicitly modeling a bioavailability parameter on the previous day's dose."( Population pharmacokinetics of tenofovir and tenofovir-diphosphate in healthy women.
Burns, RN; Chaturvedula, A; Hendrix, CW, 2015
)
0.42
" Ibrutinib is an orally bioavailable and highly specific BTK inhibitor that was recently approved for treatment of patients with recurrent CLL and mantle cell lymphoma (MCL)."( Mechanisms of ibrutinib resistance in chronic lymphocytic leukaemia and non-Hodgkin lymphoma.
Lynn Wang, Y; Smith, SM; Zhang, SQ; Zhang, SY, 2015
)
0.42
" The present study was designed to investigate the absolute bioavailability (F) of ibrutinib in the fasting and fed state and assess the effect of grapefruit juice (GFJ) on the systemic exposure of ibrutinib in order to determine the fraction escaping the gut (Fg ) and the fraction escaping hepatic extraction (Fh ) in the fed state."( Stable isotope-labelled intravenous microdose for absolute bioavailability and effect of grapefruit juice on ibrutinib in healthy adults.
de Jong, J; de Vries, R; de Zwart, L; Hellemans, P; Jiao, J; Mannaert, E; Murphy, J; Skee, D; Smit, JW; Snoeys, J; Sukbuntherng, J; Vliegen, M, 2016
)
0.43
" Importantly, the total area under the plasma concentration-time curve from time zero to time infinity (AUC), peak plasma concentration (Cmax) and extent of absolute oral bioavailability (F) of adefovir after oral administration of adefovir dipivoxil were significantly higher in 1,25(OH)2D3-treated rats than in control rats."( Effects of 1α,25-Dihydroxyvitamin D3 on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats.
Choi, MK; Kim, SB; Maeng, HJ; Son, JH; Yoon, IS, 2015
)
0.42
" Orally bioavailable inhibitors of spleen tyrosine kinase, Bruton's tyrosine kinase, or PI3Kδ, induce high rates of durable responses."( The role of B-cell receptor inhibitors in the treatment of patients with chronic lymphocytic leukemia.
Wiestner, A, 2015
)
0.42
" Efficient syntheses of novel lipophilic prodrugs of (S)-CPMEA masking either the carboxylic group or preferably both the phosphonate and carboxylic moieties, have been developed in order to increase bioavailability of the parent compound."( Synthesis and biological properties of prodrugs of (S)-3-(adenin-9-yl)-2-(phosphonomethoxy)propanoic acid.
Dračínský, M; Janeba, Z; Kaiser, MM; Lee, YJ; Poštová-Slavětínská, L; Tian, Y, 2016
)
0.43
"These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy."( Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system.
Ezzeldin, E; Iqbal, M; Shakeel, F, 2016
)
0.43
" The most advantageous pharmacokinetic profile and the best oral bioavailability were found in tyrosinebased prodrugs."( Amino Acid Ester Prodrugs of Nucleoside and Nucleotide Antivirals.
Krecmerova, M, 2017
)
0.46
" Here we report the preclinical potential of a novel, orally bioavailable PI3K/mTOR dual inhibitor, DS7423 (hereafter DS), in in-vitro and in-vivo studies."( Preclinical therapeutic efficacy of a novel blood-brain barrier-penetrant dual PI3K/mTOR inhibitor with preferential response in PI3K/PTEN mutant glioma.
Gao, F; Hirota, Y; Kaul, I; Koul, D; Koyama, K; Nakayama, K; Saito, N; Setoguchi, M; Shiose, Y; Sulman, EP; Wang, S; Wu, S; Yung, WKA; Zheng, S, 2017
)
0.46
" The aim of the study was to define MerTK as a therapeutic target using an orally bioavailable inhibitor, UNC2025."( MerTK as a therapeutic target in glioblastoma.
Bash, RE; Cohen, SM; Earp, HS; Ewend, MG; Frady, LN; Frye, SV; Gilbert, MR; Irvin, DM; Miller, CR; Schorzman, AN; Su, YT; Sulman, EP; Wang, X; Wu, J; Zamboni, WC, 2018
)
0.48
"The present study aimed to prepare proliposomal formulae for improving the oral bioavailability of adefovir dipivoxil (AD), a nucleoside reverse transcriptase inhibitor effective against hepatitis B virus (HBV)."( Adefovir dipivoxil loaded proliposomal powders with improved hepatoprotective activity: formulation, optimization, pharmacokinetic, and biodistribution studies.
Abdelbary, GA; Amin, MM; El Awdan, SA; Zakaria, MY, 2018
)
0.48
" Venetoclax is a selective, orally bioavailable inhibitor of BCL-2 active in previously treated patients with relapsed or refractory chronic lymphocytic leukaemia."( Venetoclax for chronic lymphocytic leukaemia progressing after ibrutinib: an interim analysis of a multicentre, open-label, phase 2 trial.
Barr, PM; Byrd, JC; Cheson, BD; Choi, M; Chyla, B; Coutre, S; Davids, MS; Furman, RR; Humerickhouse, RA; Jones, JA; Lamanna, N; Mato, AR; Potluri, J; Salem, AH; Verdugo, M; Wierda, WG; Woyach, J; Zhou, L, 2018
)
0.48
"Adefovir is an antiviral drug that exhibits high hydrophilic properties and negligible bioavailability (less than 12%)."( Evaluation of Ion-pair Formation of Adefovir to Improve Permeation across Artificial and Biological Membranes.
Darsazan, B; Mortazavi, SA; Shafaati, A; Zarghi, A, 2018
)
0.48
" Lactobacillus crispatus actively transported tenofovir leading to a loss in drug bioavailability and culture supernatants from Gardnerella vaginalis, but not Atopobium vaginae, blocked tenofovir endocytosis."( Vaginal microbiome modulates topical antiretroviral drug pharmacokinetics.
Cameron, SA; Cheshenko, N; Frank, B; Fredricks, D; Herold, BC; Keller, MJ; Mesquita, PM; Reagle, K; Sinclair, S; Srinivasan, S; Taneva, E; Weinrick, B, 2018
)
0.48
" However, IBR is insoluble at neutral pH and can dissolve only at low pH: thus, commercial IBR products present poor bioavailability and weakened in vivo antitumor activity."( Novel Self-Assembled Ibrutinib-Phospholipid Complex for Potently Peroral Delivery of Poorly Soluble Drugs with pH-Dependent Solubility.
Deng, Y; Hu, L; Lai, C; Li, C; Liu, M; Liu, X; Lu, M; Luo, X; Qiu, Q; Song, Y; Zhang, H; Zheng, H, 2018
)
0.48
" Ibrutinib is an orally bioavailable bruton tyrosine kinase inhibitor (BTKi) and forms an irreversible covalent bound to BTK at the Cysteine-481 residue."( Management of adverse effects/toxicity of ibrutinib.
Paydas, S, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The oral bioavailability of ibrutinib is low and variable, mainly due to extensive first-pass metabolism by cytochrome P450 (CYP) 3A4."( Itraconazole Increases Ibrutinib Exposure 10-Fold and Reduces Interindividual Variation-A Potentially Beneficial Drug-Drug Interaction.
Backman, JT; Elonen, E; Neuvonen, M; Neuvonen, PJ; Niemi, M; Olkkola, AM; Tapaninen, T; Tornio, A, 2020
)
0.56
" Moreover, the biosafety of the ternary formulation was the same as that of IBR while the in vitro performance advantage of the ternary formulation was converted into higher bioavailability in vivo experiments."( Microcrystalline cellulose as an effective crystal growth inhibitor for the ternary Ibrutinib formulation.
Gan, N; Li, H; Peng, X; Suo, Z; Tang, P; Wei, X; Zhang, M; Zhao, L, 2020
)
0.56
" BIC has demonstrated a high genetic barrier to resistance development in vitro, can be administered with or without food, and has a bioavailability of > 70%."( Bictegravir, a novel integrase inhibitor for the treatment of HIV infection.
Bhatia, R; Rizza, S; Temesgen, Z; Zeuli, J, 2019
)
0.51
" Its poor oral bioavailability leads to frequent administration causing severe adverse effects."( Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator.
Abd El-Halim, SM; Abdelbary, GA; Amin, MM; Ibrahim, AB; Shamsel-Din, HA; Zakaria, MY, 2020
)
0.56
" In this study, a GS-adenine pharmaceutical complex was prepared through solvent evaporation to improve the bioavailability of GS, and a molecular model of a two-component supramolecular pharmacological transport mechanism was established."( Delivery Mechanism of the Pharmaceutical Complex of Genistein-Adenine Based on Spectroscopic and Molecular Modelling at Atomic Scale.
Guo, M; Pan, LY; Shao, Y; Wu, RH; Zhao, XX; Zheng, YL, 2021
)
1.18
" KIN-8194 demonstrated excellent bioavailability and pharmacokinetic parameters, with good tolerance in rodent models at pharmacologically achievable and active doses."( The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance.
Anderson, KC; Buhrlage, SJ; Cameron, M; Castillo, JJ; Che, J; Chen, JG; Demos, MG; Gray, NS; Guerrera, ML; Hunter, ZR; Kofides, A; Liu, X; Meid, K; Munshi, M; Munshi, NC; Patterson, CJ; Tan, L; Treon, SP; Tsakmaklis, N; Wang, J; Xu, L; Yang, G, 2021
)
0.62
" Furthermore, the nanoformulations studied to increase ibrutinib bioavailability are reported."( Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective.
Brullo, C; Russo, E; Spallarossa, A; Tasso, B; Villa, C, 2021
)
0.62
"Curcumin, a polyphenolic compound, is a well-known anticancer agent, although its poor bioavailability remains a big concern."( Curcumin induces autophagic cell death in human thyroid cancer cells.
Bao, J; Cheng, X; Wang, X; Wang, Y; Wu, J; Wu, L; Xu, S; Yu, H; Zhang, L, 2022
)
0.72
"This study aimed to improve the in vitro dissolution, permeability and oral bioavailability of adefovir dipivoxil (ADD) by cocrystal technology and clarify the important role of coformer selection on the cocrystal's properties."( Effect of Coformer Selection on In Vitro and In Vivo Performance of Adefovir Dipivoxil Cocrystals.
Gao, Y; Li, L; Ma, K; Pang, Z; Qian, S; Wei, Y; Zhang, J; Zheng, D, 2021
)
0.62
"Coformer selection had an important role on cocrystal's properties, and cocrystallization of ADD with a suitable coformer was an effective approach to enhance both dissolution and bioavailability of ADD."( Effect of Coformer Selection on In Vitro and In Vivo Performance of Adefovir Dipivoxil Cocrystals.
Gao, Y; Li, L; Ma, K; Pang, Z; Qian, S; Wei, Y; Zhang, J; Zheng, D, 2021
)
0.62
" This limitation was solved by developing a nanoparticles formulation that improves the solubility and bioavailability of several bioactive compounds."( Nanoparticles Formulation Improves the Antifibrogenic Effect of Quercetin on an Adenine-Induced Model of Chronic Kidney Disease.
Bastidas-Ramírez, BE; Gasca-Lozano, LE; Gurrola-Díaz, CM; Hernández-Ortega, LD; Martínez-Limón, FJ; Mena-Enríquez, M; Salazar-Montes, AM; Sánchez-Jaramillo, EA; Vargas-Guerrero, B; Vera-Cruz, JM, 2022
)
0.95
" Tenofovir has a very low oral bioavailability following oral administration."( Treatment of chronic hepatitis B: virological and pharmacological aspects
Foucault, T; Gaudy-Graffin, C; Handala, L; Marlet, J; Paintaud, G, 2022
)
0.72
"A crossover, randomized trial in healthy adults (NCT04244448) investigated the bioavailability of two off-label uses of BIC/TAF/FTC (50/200/25 mg), dissolved in water or crushed in apple compote, compared with the solid tablet."( Bioavailability of dissolved and crushed single tablets of bictegravir, emtricitabine, tenofovir alafenamide in healthy adults: the SOLUBIC randomized crossover study.
Alix, A; Bois, J; Brucato, S; Dargere, S; Fournel, F; Fournier, A; Got, L; Gregoire, N; Hocqueloux, L; Lefeuvre, S; McNicholl, I; Parienti, JJ; Peyro-Saint-Paul, L; Prazuck, T; Valentin, C, 2022
)
0.72
" During its clinical development, a stable isotopologue of ibrutinib was required for the assessment of the drug's absolute oral bioavailability via intravenous microdosing."( Carbon-13 labeling of ibrutinib for human microdosing.
Gong, Y; Salter, R, 2023
)
0.91
" We previously utilized butyrate in order to improve the bioavailability of resveratrol via esterification and generated a resveratrol butyrate monoester (RBM)."( Dietary Resveratrol Butyrate Monoester Supplement Improves Hypertension and Kidney Dysfunction in a Young Rat Chronic Kidney Disease Model.
Chang, CI; Chang-Chien, GP; Hou, CY; Hsu, CN; Lin, S; Tain, YL, 2023
)
0.91

Dosage Studied

Six different treatments of conidial suspensions of H-12 with ICR-170 were used to obtain dose-response curves for inactivation of conidia as well as the overall induction of ad-3 forward mutations. Plasma UN and creatinine levels decreased inversely with the dose of 4APP.

ExcerptRelevanceReference
" When [14C]ribose was administered intraperitoneally to rats at a dosage of 300-750 mug (100-250 muCi)/10o g, approximately 1% of the radioactivity was recovered in the acid (5% CLCCCOOH)-INSOLUBLE MATERIAL OF THE LIVER NUCLEI 2 HR AFTER INJECTION."( Natural occurrence of poly(ADP-ribosyl) histones in rat liver.
Hayaishi, O; Kawaichi, M; Omachi, A; Ueda, K, 1975
)
0.25
" However, on increasing the concentrations of these agents, the reversing effect of guanylic acid decreased gradually, the dose-response curves for the two agents being similar."( Effect of bredinin and its aglycone on L5178Y cells.
Hayano, K; Ishida, N; Mizuno, K; Sakaguchi, K; Tsujino, M, 1975
)
0.25
" An association between increased cAMP contents and increased contractile activity was revealed by both the time-response and the dose-response curves of hearts exposed to isoprenaline and dopamine."( Adenosine 3',5'-cyclic monophosphate in perfused rat hearts exposed to isoprenaline and dopamine.
Osnes, JB; Oye, I, 1976
)
0.26
" The stimulation of mouse locomotor activity caused by dl- and d-amphetamine in mice treated with adenine was less than that caused by equal dosage of these agents in mice not treated with adenine."( Reversal of adenine-induced depression of mouse locomotor activity by amphetamine.
Akintonwa, A; Auditore, JV, 1978
)
0.85
" The use of the ad-3 assay system in experiments with different environmental mutagens has provided precise dose-response curves not only for inactivation, but also the overall induction of ad-3 mutations."( Development of a specific-locus assay in the ad-3 region of two-component heterokaryons of Neurospora: a review.
de Serres, FJ, 1992
)
0.28
" In such assessments with radiation or chemical mutagens, the following information is required: (1) spontaneous and induced forward-mutation frequencies, (2) dose-response curves for the overall induction of specific-locus mutations, (3) genetic characterization of spontaneous and induced mutations, and (4) dose-response curves for the different genotypic classes."( Characteristics of spontaneous and induced specific-locus mutation in the ad-3 region of Neurospora crassa: utilization in genetic risk assessment.
de Serres, FJ, 1992
)
0.28
" However, chromosome losses do not seem to directly cause the metabolic alterations by gene dosage effect."( [Chromosome abnormalities and adenine metabolism in human glial tumors].
Bardot, V; Delattre, JY; Dutrillaux, AM; Dutrillaux, B; Luccioni, C; Poisson, M; Vega, F, 1992
)
0.57
" A2 receptors by N-0861 was evaluated by generating dose-response curves to adenosine-induced bradycardia (A1 effect), and vasodilation in the in situ constant-flow perfused rat hindquarter vasculature (A2 effect)."( N-0861 selectively antagonizes adenosine A1 receptors in vivo.
Barrett, RJ; Droppleman, DA; Wright, KF, 1992
)
0.28
" At this dosage and schedule, there is no evidence that amonafide has meaningful anti-tumor activity in patients with advanced renal cell carcinoma."( Phase II evaluation of amonafide in renal cell carcinoma. A Southwest Oncology Group study.
Craig, JB; Crawford, ED; Goodman, P; Higano, CS; Kish, JA; Rivkin, SE; Wolf, M, 1991
)
0.28
" With the low response rate and the toxicity observed, amonafide at this dosage and schedule has limited use in the treatment of non-small-cell lung cancer."( Phase II trial of amonafide in patients with stage III and IV non-small-cell lung cancer.
Berger, MZ; Dimaggio, JJ; Gralla, RJ; Heelan, RT; Kris, MG; Marks, LD; Potanovich, LM, 1991
)
0.28
" The persistence of activated metabolites suggests that infrequent dosing may be possible due to a prolonged antiviral effect."( Biochemical pharmacology of acyclic nucleotide analogues.
Bronson, JJ; De Boeck, H; Ghazzouli, I; Hitchcock, MJ; Ho, HT; Martin, JC; Woods, K, 1990
)
0.28
" While the infrequent dosage regimen increased the anti-retrovirus activity of PMEA, it did not increase its toxicity for the host."( Anti-retrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in vivo increases when it is less frequently administered.
Balzarini, J; De Clercq, E; Naesens, L, 1990
)
0.53
" Dose-response curves showed that AHA and HAP were about equally mutagenic at low doses but that AHA was more mutagenic than HAP at high doses."( Effect of the uvs-2 allele of Neurospora crassa on the mutagenic potency of two N-hydroxylaminopurines and 2-aminopurine in the ad-3 forward-mutation test.
Brockman, HE; de Serres, FJ; Hung, CY; Ong, T, 1989
)
0.28
" Their dose-response curves showed that they had similar IC50's but the maximum inhibition differed among these agonists."( Inhibition of adenylate cyclase in bovine ciliary process and rabbit iris ciliary body to alpha 2-adrenergic agonists.
Elko, EE; Jin, Y; Tran, T; Yorio, T, 1989
)
0.28
" These subsequent studies confirmed that, after oral dosing with famciclovir, more than half the dose was absorbed and rapidly converted to penciclovir."( Selection of an oral prodrug (BRL 42810; famciclovir) for the antiherpesvirus agent BRL 39123 [9-(4-hydroxy-3-hydroxymethylbut-l-yl)guanine; penciclovir].
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.28
" These findings indicate that adenine at 50 microM dosage can restore ATP concentrations to the normoxic range after 60 in of anoxia in the nonworking rat heart while raising the adenine dose to 1 mM inhibited the tissue ATP content."( Dose effects of adenine on myocardial ATP content in the post-anoxic nonworking rat heart.
Halle, AA; Kang, ES; Mirvis, DM; Sullivan, JM, 1989
)
0.91
" (S)-HPMPA inhibited the development of tail lesions caused by vaccinia virus if it was administered intraperitoneally or subcutaneously at a dosage as low as 5 mg/kg per day."( Efficacy of phosphonylmethoxyalkyl derivatives of adenine in experimental herpes simplex virus and vaccinia virus infections in vivo.
De Clercq, E; Holý, A; Rosenberg, I, 1989
)
0.53
" associated with a fluorescence detector allows the identification of adenine and its dosage at quantities as low as 2 ng; (ii) the direct fluorimetric measurement of the material that had reacted with chloroacetaldehyde."( High-pressure-liquid-chromatographic and fluorimetric methods for the determination of adenine released from ribosomes by ricin and gelonin.
Brigotti, M; Montanaro, L; Rambelli, F; Sperti, S; Zamboni, M, 1989
)
0.73
" Both 5 and its esters (14-17, 21, 22) and also 18 were well absorbed after oral administration and converted efficiently to 1, the diacetyl (14) and dipropionyl (16) esters providing concentrations of 1 in the blood that were more than 15-fold higher than those observed after dosing either 1 or its esters (25-27)."( Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties.
Boyd, MR; Harnden, MR; Jarvest, RL; Sutton, D; Vere Hodge, RA, 1989
)
0.28
" The 1-MeAde dose-response curves for maturation induction and activation of the histone H1 and RRLSSLRA kinases were superimposable."( Differential regulation of histone H1 and ribosomal S6 kinases during sea star oocyte maturation.
Krebs, EG; Meijer, L; Pelech, SL, 1987
)
0.27
" These results correlated closely with the dose-response relationships for tumor initiation by the two hydrocarbons."( Correlation between formation of a specific hydrocarbon-deoxyribonucleoside adduct and tumor-initiating activity of 7,12-dimethylbenz(a)anthracene and its 9- and 10-monofluoroderivatives in mice.
DiGiovanni, J; Fisher, EP; Sawyer, TW, 1986
)
0.27
" From the dose-response data it was possible to quantify accurately and rapidly the antitrichomonal activity of a range of compounds based on the inhibition of adenine uptake."( Measurement of adenine uptake as an in vitro screen for antitrichomonal agents.
Havelec, L; Heyworth, PG; Meingassner, JG, 1985
)
0.82
"A dose-response relation was established between prostaglandins and formation of adenosine 3',5'-monophosphate in the mouse ovary."( Prostaglandin receptor site: evidence for an essential role in the action of luteinizing hormone.
Cirillo, VJ; Ham, EA; Humes, JL; Kuehl, FA; Tarnoff, J, 1970
)
0.25
" Administration of ara-A by several different intermittent dosage regimens showed that change in pattern of response in terms of survivors appears to be influenced more by total amount of drug administered than by schedule or duration of drug treatment."( Treatment of herpes simplex virus types 1 and 2 encephalitis in mice with 9-beta-D-arabinofuranosyladenine.
McLean, IW; Miller, FA; Sloan, BJ, 1973
)
0.47
" Ara-A and IUdR, when administered intraperitoneally by several different dosage schedules, reduced the severity of cutaneous herpetic lesions and the incidence of paralysis and increased significantly the number of survivors."( Herpes simplex virus skin infection in hairless mice: treatment with antiviral compounds.
Brady, E; Friedman-Kien, AE; Klein, RJ, 1974
)
0.25
"Of the 72 pancreatic preparations currently on the market 24 were randomly selected for study and compared with 3 US preparations with different dosage forms."( Studies on the quality of pancreatic preparations: enzyme content, prospective bioavailability, bile acid pattern, and contamination with purines.
König, J; Molitor, M; Neef, B; Niessen, KH, 1983
)
0.27
" Inhibition of adenylate cyclase at the P site attenuates the rise in cellular cyclic AMP and suppresses IgE-dependent mediator release in a parallel and superimposable dose-response fashion."( Role of adenylate cyclase in immunologic release of mediators from rat mast cells: agonist and antagonist effects of purine- and ribose-modified adenosine analogs.
Austen, KF; Holgate, ST; Lewis, RA, 1980
)
0.26
"A dose-response relationship between gamma-irradiation and the cleavage of the imidazole ring of adenine in DNA to form formamidopyrimidine has been demonstrated."( A dose-response study on opening of imidazole ring of adenine in DNA by ionizing radiation.
Chetsanga, CJ; Grigorian, C, 1983
)
0.73
" The optimal dosage level was shown to be 5 ppm in the diet."( CL 259,971: a potent new polyether anticoccidial. 2. Floor-pen trials.
Kantor, S; Kennett, RL; Schenkel, RH, 1984
)
0.27
" Mice dosed with EHNA (100 mg/kg) once daily for 7 days showed the same ADA recovery rate as mice dosed only once."( Pharmacokinetics of inhibition of adenosine deaminase by erythro-9-(2-hydroxy-3-nonyl)adenine in CBA mice.
Lambe, CU; Nelson, DJ, 1982
)
0.49
" Six different treatments of conidial suspensions of H-12 with ICR-170 were used to obtain dose-response curves for inactivation of conidia as well as the overall induction of ad-3 forward mutations using a direct method based on pigment accumulation rather than a requirement for adenine."( Forward-mutation tests on the antitumor agent ICR-170 in Neurospora crassa demonstrate that it induces gene/point mutations in the ad-3 region and an exceptionally high frequency of multiple-locus ad-3 mutations with closely linked sites of recessive leth
de Serres, FJ; Malling, HV, 1994
)
0.47
" When adenine and benzyladenine, a similar substance of adenine, was microinjected into the germinal vesicle of oocytes, the meiotic maturation of oocytes could be obviously arrested depending on the dosage of injection."( [The meiosis arrest of mouse oocytes induced by adenine].
Fan, BQ; Li, CJ; Wang, B, 1994
)
1.03
" Control and ETO-treated conidial suspensions were used to obtain dose-response curves for inactivation as well as the overall induction of ad-3 forward mutations using a non-selective method based on pigment accumulation rather than a requirement for adenine."( Ethylene oxide: induction of specific-locus mutations in the ad-3 region of heterokaryon 12 of Neurospora crassa and implications for genetic risk assessment of human exposure in the workplace.
Brockman, HE; de Serres, FJ, 1995
)
0.47
" Our analysis indicates that HDL-C levels do not vary by genotype, and no gene dosage effect is apparent in men or in women."( Genetic analysis of a polymorphism in the human apolipoprotein A-I gene promoter: effect on plasma HDL-cholesterol levels.
Barre, DE; Cohen, JC; Grundy, SM; Guerra, R; Verstraete, R; Wang, Z, 1994
)
0.29
" Dose-response relationships of ISO or rolipram show a close correlation of the half-maximal effective dose (ED50) for injury reversal and perfusate cAMP production."( Reversal of pulmonary capillary ischemia-reperfusion injury by rolipram, a cAMP phosphodiesterase inhibitor.
Barnard, JW; Prasad, VR; Seibert, AF; Smart, DA; Strada, SJ; Taylor, AE; Thompson, WJ, 1994
)
0.29
" Oral dosing with bis(alkyl) phosphonates 3a,b resulted in apparent absorption of the prodrugs (> or = 40%), although neither of the esters were completely cleaved to liberate the parent phosphonate PMEA."( Synthesis, oral bioavailability determination, and in vitro evaluation of prodrugs of the antiviral agent 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA).
Hitchcock, MJ; Mansuri, MM; Martin, JC; Russell, J; Starrett, JE; Tortolani, DR; Whiterock, V, 1994
)
0.49
"A high performance liquid chromatography (HPLC) method for the qualitative and quantitative determination of amonafide (CAS 69408-81-7) and mitonafide (CAS 54824-17-8), two new antineoplastic molecules, in finished pharmaceutical dosage forms (tablets) is developed and validated."( Qualitative and quantitative determination of two new antitumor agents from 1-8 naphthalimides in tablets. Validation of a high performance liquid chromatography method.
Camacho, MA; Gil, ME; Obregón, MM; Ruz, V; Torres, AI, 1994
)
0.29
" However, plasma UN and creatinine levels decreased inversely with the dose of 4APP when a different dosage of 4APP was administered together with adenine."( Nephrotoxicity induced by a single dose of adenine: effects of 4-aminopyrazolo[3,4-d]pyrimidine and allopurinol.
Ichii, M; Kadota, E; Minami, T; Nakagawa, H; Okazaki, Y, 1994
)
0.75
" Dose-response curves to CPA were shallower and maximal responses were weaker than those produced by the other agonists."( Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II.
Barrett, RJ; Droppleman, DA, 1993
)
0.29
" This protocol was aimed at assessing two sensitive measures of beta-cell dysfunction: the priming effect of glucose on the glucose-insulin secretion rate (ISR) dose-response curve and the ability of oscillatory glucose infusion to entrain insulin secretory oscillations."( Clinical phenotypes, insulin secretion, and insulin sensitivity in kindreds with maternally inherited diabetes and deafness due to mitochondrial tRNALeu(UUR) gene mutation.
Blanché, H; Byrne, MM; Clément, K; Fiet, J; Froguel, P; Passa, P; Polonsky, KS; Pueyo, ME; Robert, JJ; Sturis, J; Velho, G; Vionnet, N, 1996
)
0.29
"8 L/hr/m2) is relatively constant within the dosing range of this study."( Clinical pharmacokinetics of amonafide (NSC 308847) in 62 patients.
Akerman, S; Allen, SL; Budman, DR; Calabro, A; Chan, K; Fusco, D; Hock, K; Kreis, W; Mittelman, A; Puccio, C; Spigelman, M, 1996
)
0.29
" Dose-response studies were performed using previously reported inhibitors of cytosolic calcium oscillation mechanisms."( The mechanisms underlying Bay K 8644-stimulated phasic myometrial contractions.
Chien, EK; Phillippe, M; Saunders, T,
)
0.13
" The goal of this study was to construct and validate a pharmacodynamic model-based dosing strategy for amonafide, to try to further decrease inter-patient variability in leukopenia."( Individualized dosing of amonafide based on a pharmacodynamic model incorporating acetylator phenotype and gender.
Berezin, F; Janisch, L; Kut, M; Mick, R; Ratain, MJ; Schilsky, RL; Vogelzang, NJ, 1996
)
0.29
" It has provided an invaluable tool for the study of gene dosage and plasmid stability."( The red/white colony color assay in the yeast Saccharomyces cerevisiae: epistatic growth advantage of white ade8-18, ade2 cells over red ade2 cells.
Bruschi, CV; Ugolini, S, 1996
)
0.29
" Within < or = 2 weeks of treatment, PMPA in both dosing regimens reduced SIV levels by >99% in the plasma or peripheral blood mononuclear cells; in some macaques SIV levels were reduced to below the lower quantitation limit."( Effects of (R)-9-(2-phosphonylmethoxypropyl)adenine monotherapy on chronic SIV infection in macaques.
Beck, TW; Bischofberger, N; Dailey, PJ; Follis, KE; Sabo, A; Tsai, CC, 1997
)
0.56
" After 14 days of dosing, adefovir dipivoxil demonstrated anti-HIV activity and was best tolerated at the lowest dosage studied, 125 mg daily."( Anti-human immunodeficiency virus (HIV) activity, safety, and pharmacokinetics of adefovir dipivoxil (9-[2-(bis-pivaloyloxymethyl)-phosphonylmethoxyethyl]adenine) in HIV-infected patients.
Barditch-Crovo, P; Cundy, KC; Ebeling, D; Hendrix, CW; Jaffe, HS; Lietman, PS; Toole, J, 1997
)
0.49
" Nine cats received PMEA at a dosage of 10 mg/kg body weight, nine cats received FPMPA at a dosage of 25 mg/kg body weight."( [Comparative investigation of the efficacy of two nucleocapsid analogs in FIV infected cats].
Balzarini, J; Erfle, V; Goebel, F; Goldberg, M; Hartmann, K; Kuffer, M; Rolinski, B, 1997
)
0.3
" Likewise, a clear dose-response relationship was established for the in vivo antitumor activity of PMEA in choriocarcinoma-bearing rats."( In vitro and in vivo inhibitory activity of the differentiation-inducing agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against rat choriocarcinoma.
Balzarini, J; De Clercq, E; Degrève, B; Hatse, S; Naesens, L; Vandeputte, M; Waer, M, 1998
)
0.51
" The antiviral efficacy of oral bis(POC)-PMPA was related to the dosage and treatment period and was not significantly different from that of subcutaneous PMPA given at an equivalent dose."( Antiretroviral efficacy and pharmacokinetics of oral bis(isopropyloxycarbonyloxymethyl)-9-(2-phosphonylmethoxypropyl)adenine in mice.
Annaert, P; Arimilli, MN; Augustijns, P; Bischofberger, N; De Clercq, E; Kim, CU; Naesens, L; Van den Mooter, G, 1998
)
0.51
" All subjects tolerated dosing without significant adverse events."( Safety, pharmacokinetics, and antiretroviral activity of intravenous 9-[2-(R)-(Phosphonomethoxy)propyl]adenine, a novel anti-human immunodeficiency virus (HIV) therapy, in HIV-infected adults.
Barditch-Crovo, P; Cundy, KC; Deeks, SG; Hellmann, NS; Hwang, F; Kahn, JO; Lietman, PS; Rooney, JF; Safrin, S, 1998
)
0.51
" There may be a steep dose-response curve, based on the significant correlation between myelosuppression and response."( Amonafide: An active agent in the treatment of previously untreated advanced breast cancer--a cancer and leukemia group B study (CALGB 8642).
Berkowitz, I; Berry, D; Costanza, ME; Duggan, D; Henderson, IC; Kalra, J; Lyss, AP; Ratain, MJ; Shapiro, C; Wu, K, 1995
)
0.29
" Eight Pekin-Aylesbury ducks congenitally infected with the duck hepatitis B virus (DHBV) were treated with PMEA at a dosage of 15 mg/kg of body weight/day via the intraperitoneal route for 4 weeks."( Inhibition of duck hepatitis B virus replication by 9-(2-phosphonylmethoxyethyl)adenine, an acyclic phosphonate nucleoside analogue.
Angus, PW; Colledge, DL; Locarnini, SA; Nicoll, AJ; Smallwood, RA; Toole, JJ, 1998
)
0.53
" Variables that can be experimentally manipulated to address specific questions relevant to postexposure prophylaxis (PEP) include timing of initiation of treatment, duration of treatment, dosing regimen, virus strain, and virus inoculum."( Animal studies of prophylaxis.
Black, RJ, 1997
)
0.3
" To obtain dose-response curves, single doses (as boluses) of different concentrations of adenosine were infused and the maximal increase in A-V delay induced by each dose was determined."( Intravascular adenosine: the endothelial mediators of its negative dromotropic effects.
Balcells, E; Ceballos, G; Rubio, R, 1999
)
0.3
" Comparative dose-response curves indicated that maximal hormone-stimulated cAMP accumulation was 11- and 24-fold higher in human and rat cells, compared with cAMP production obtained in corresponding membranes, respectively."( Comparative involvement of cyclic nucleotide phosphodiesterases and adenylyl cyclase on adrenocorticotropin-induced increase of cyclic adenosine monophosphate in rat and human glomerulosa cells.
Côté, M; Gallo-Payet, N; Guillon, G; Payet, MD; Rousseau, E, 1999
)
0.3
" Both prophylactic and therapeutic dosing regimens were effective."( Chemokines, nitric oxide and antiarthritic effects of 9-(2-phosphonomethoxyethyl)adenine (Adefovir).
Franková, D; Holý, A; Zídek, Z, 1999
)
0.53
" The inhibitory effect of NE was partially antagonized by propranolol but not by prazosin, and dose-response curves with BRL-37344 (a beta(3)-agonist), isoproterenol (a beta(1)/beta(2)-agonist) and dobutamide (a beta(1)-agonist) were consistent with the involvement of a beta(3)-adrenergic receptor."( Differentiation-dependent inhibition of proteolysis by norepinephrine in brown adipocytes.
Desautels, M; Heal, S, 1999
)
0.3
" The effect of more frequent dosing requires further evaluation."( Effect of weekly adefovir (PMEA) infusions on HIV-1 virus load: results of a phase I/II study.
Boucher, CA; Cambridge, E; De Groot, T; De Jong, S; Kamp, W; Schokker, J; Schuurman, R, 1999
)
0.3
" Advertising that promoted the improved drug has been withdrawn at the request of Project Inform because of the lack of warning labels necessary due to dosing problems."( Update on antivirals.
, 1997
)
0.3
" All three drugs are currently available through expanded access programs, are dosed either once or twice daily, and can be taken with or without food."( I want a new drug. An overview of three new anti-HIV drugs.
Simmons, P, 1998
)
0.3
" The dosage regimens and limitations are described for each drug."( Four new antiretroviral medications will soon offer more options to HIV patients.
Murphy, MJ,
)
0.13
" A clinical trial of the protease inhibitor Nelfinavir (Viracept) has shown that dosing twice a day may be as effective as the currently prescribed three times a day."( Antimicrobial agents and chemotherapy: highlights of the 38th Interscience Conference.
Prescott, LM, 1998
)
0.3
" Information on tenofovir, such as the dosage normally prescribed and cost of treatment is listed."( What they say about: nucleotide drugs.
,
)
0.13
" We compared their toxicity and ability to inhibit tumour development in two different dosage regimes with those of their parent compound PMEDAP, as well with PMEG."( Antitumour activity of N6-substituted PMEDAP derivatives against T-cell lymphoma.
Holy, A; Mandys, V; Otová, B; Valeriánová, M; Votruba, I,
)
0.13
" Data from correlation analysis of the log ratios for normal tissues from cancer were consistent with an age-dependent, dose-response relationship."( Age-related radical-induced DNA damage is linked to prostate cancer.
Barker, EA; Johnson, PM; Malins, DC; Polissar, NL; Vinson, MA; Wheeler, TM, 2001
)
0.31
" ODQ (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one), a potent and selective inhibitor of soluble guanylyl cyclase (sGC), did not significantly affect relaxant actions of ONOO-, but ODQ markedly attenuated SIN-1-elicited relaxation with a rightward shift in the dose-response curve and an unaltered maximal response."( Comparative vasodilation of peroxynitrite and 3-morpholinosydnonimine.
Trakranrungsie, N; Will, JA, 2001
)
0.31
" This study explores various factors involved in inhibitor selection and dosage regimen design to achieve local ADA inhibition with minimal systemic inhibition."( Enhanced oral bioavailability of 2'- beta-fluoro-2',3'-dideoxyadenosine (F-ddA) through local inhibition of intestinal adenosine deaminase.
Anderson, BD; DeGraw, RT, 2001
)
0.31
" The recommended dosage of tenofovir DF in adults is 300 mg/d PO; pharmacokinetic and efficacy studies in children are ongoing."( Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection.
Fung, HB; Piacenti, FJ; Stone, EA, 2002
)
0.31
" The approved dosage of tenofovir is 300 mg (one tablet) once/day with meals."( Tenofovir: a nucleotide analog for the management of human immunodeficiency virus infection.
Antoniou, T; Park-Wyllie, LY; Tseng, AL, 2003
)
0.32
" Preemptive post-transplant lamivudine monotherapy is associated with progressively increasing HBV recurrence rates, but combined therapy with lamivudine and HBIG at relatively low dosage is currently the most effective approach in this setting, even in HBV-DNA-positive patients, who also receive lamivudine in the pretransplant period."( Prevention of and treatment for hepatitis B virus infection after liver transplantation in the nucleoside analogues era.
Burroughs, AK; Papatheodoridis, GV; Sevastianos, V, 2003
)
0.32
" Most patients continued treatment with dosage adjustments."( Adefovir dipivoxil: a review of its use in chronic hepatitis B.
Dando, T; Plosker, G, 2003
)
0.32
" These effects were more pronounced with dosing regimens launched before the time of oviposition."( Activity of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine against Schistosomiasis mansoni in mice.
Botros, S; Hammam, O; Holý, A; William, S; Zídek, Z, 2003
)
0.57
" The steady-state, geometric mean AUC for the 24-h dosing interval was 2,920 ng."( Single-dose and steady-state pharmacokinetics of tenofovir disoproxil fumarate in human immunodeficiency virus-infected children.
Balis, FM; Blanche, S; Bresson, JL; Coakley, DF; DeCarlo, E; Flaherty, JF; Hazra, R; Kearney, BP; Poblenz, M; Steinberg, SM; Tullio, AN; Worrell, CJ; Yale, K; Zeichner, SL; Zhong, L; Zuckerman, JA, 2004
)
0.32
"Our study shows that ADV dosed at 10 mg/day for the treatment of LAM-resistant chronic hepatitis B in patients co-infected with HIV is not associated with renal tubular dysfunction or a significant change in renal function."( The renal tolerance of low-dose adefovir dipivoxil by lamivudine-resistant individuals co-infected with hepatitis B and HIV.
Bagnis, CI; Beaufils, H; Benhamou, Y; Brosgart, C; Deray, G; Hannon, H; Izzedine, H; Poynard, T; Sullivan, M, 2004
)
0.32
" The risk of nephrotoxicity, the most notable adverse effect of adefovir dipivoxil at previously used higher doses, has been substantially reduced at the currently recommended dosage of 10 mg/d."( Adefovir dipivoxil: a new antiviral agent for the treatment of hepatitis B virus infection.
Mattes, KA; Qaqish, RB; Ritchie, DJ, 2003
)
0.32
" Plasma concentration of ddI was prospectively determined in eight of these patients receiving ddI 400 mg + TDF + NVP and 3 weeks after a ddI dosage reduction."( Unexpected CD4 cell count decline in patients receiving didanosine and tenofovir-based regimens despite undetectable viral load.
Burger, D; Clotet, B; Grassi, J; Juan, M; Masmitjà, E; Moltó, J; Negredo, E; Paredes, R; Pruvost, A; Puig, J; Ribera, E; Ruiz, L; Viciana, P, 2004
)
0.32
"Gilead Sciences is developing a fixed-dose co-formulation of two of its reverse transcriptase inhibitors, emtricitabine [Emtriva] and tenofovir disoproxil fumarate [Viread], for once-daily dosing in combination with other antiretrovirals for the treatment of HIV infection."( Emtricitabine/tenofovir disoproxil fumarate.
, 2004
)
0.32
" With the exception of didanosine and atazanavir, which require dosage modifications, no clinically significant drug interactions have been observed with tenofovir DF."( Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics.
Flaherty, JF; Kearney, BP; Shah, J, 2004
)
0.32
" A clear dose-response relationship was seen between dose groups and 8-OH Adenine levels related with time in all periods."( The oxidative DNA base damage in testes of rats after intraperitoneal cadmium injection.
Ates, I; Aydin, A; Karakaya, A; Suzen, HS, 2004
)
0.55
"A statistical method for the evaluation of the dissolution stability results and for selecting the most stable formulation within a solid dosage form development is discussed."( Statistical method for evaluation of dissolution stability in the formulation development of solid dosage forms: tablets of amonafide.
Bernabeu, JA; Camacho, MA; Gil-Alegre, ME; Torres-Suarez, AI, 2004
)
0.32
"To investigate the efficacy, safety, and the tolerability of two dosing regimens of ADV (10 mg daily or 30 mg daily), two double-blind, placebo-controlled studies were performed in patients with chronic hepatitis B and compensated liver disease who were not undergoing current treatment and who had evidence of hepatitis B virus (HBV) replication."( Renal safety of adefovir dipivoxil in patients with chronic hepatitis B: two double-blind, randomized, placebo-controlled studies.
Arterbrun, S; Brosgart, CL; Currie, G; Deray, G; Hadziyannis, SJ; Hulot, JS; Izzedine, H; Launay-Vacher, V; Marcellini, P; Westland, C, 2004
)
0.32
" Bioequivalence testing was conducted of total, R-, and S-methadone area under the serum or plasma concentration-time curve during the 24-hour dosing interval at steady state (AUCss) and maximum concentration in serum or plasma (Cmax)."( Effect of tenofovir disoproxil fumarate on the pharmacokinetics and pharmacodynamics of total, R-, and S-methadone.
Berenson, CS; Booker, BM; Bullock, JM; Cloen, D; Coakley, DF; Flaherty, JF; Haas, CE; Kearney, BP; Liaw, S; Smith, PF; Yale, K, 2004
)
0.32
" Didanosine was prescribed at a reduced dosage due to the known interaction with tenofovir."( Acute onset of pancreatitis with concomitant use of tenofovir and didanosine.
Fulco, PP; Higginson, RT; Kirian, MA, 2004
)
0.32
" Reduced didanosine dosage (250 mg) should be used to reduce serum didanosine concentrations and subsequent toxicities."( Acute onset of pancreatitis with concomitant use of tenofovir and didanosine.
Fulco, PP; Higginson, RT; Kirian, MA, 2004
)
0.32
" Dose-limiting nephrotoxicity necessitates suboptimal dosing at 10 mg/day."( Remofovir mesylate: a prodrug of PMEA with improved liver-targeting and safety in rats and monkeys.
Erion, MD; Hong, Z; Lin, CC; Vitarella, D; Yeh, LT, 2004
)
0.32
" Dosing mice and rats with AA (50 mg/kg) led to presence of glycidamide (GA) in serum and tissues."( DNA adducts derived from administration of acrylamide and glycidamide to mice and rats.
Beland, FA; Churchwell, MI; Doerge, DR; Gamboa da Costa, G; McDaniel, LP; Twaddle, NC, 2005
)
0.33
" Tenofovir DF provides a simple and convenient once-daily dosage regimen, and is generally well tolerated and able to produce sustained suppression of viral replication."( Tenofovir disoproxil fumarate: a review of its use in the management of HIV infection.
Lyseng-Williamson, KA; Plosker, GL; Reynolds, NA, 2005
)
0.33
" dosing of [(14)C]remofovir, fecal excretion of radioactivity accounted for 37."( Single-dose pharmacokinetics and metabolism of [14C]remofovir in rats and cynomolgus monkeys.
Lin, CC; Lourenco, D; Xu, C; Yeh, LT; Zhu, N, 2005
)
0.33
" To limit this interaction, the dosage of ddI may be reduced to 250 mg once daily when co-prescribed with TDF."( The durability of virological success of tenofovir and didanosine dosed at either 400 or 250 mg once daily.
Bower, M; Gazzard, B; Mandalia, S; Nelson, M; Tung, MY, 2005
)
0.33
" All three slowed the rate of RNA decay in a dose-response fashion, they were specific to the b-ARE, and two of them were individually effective."( Increased Bcl2 expression by antisense oligoribonucleotides targeting the adenine-uridine-rich element motif.
Bevilacqua, A; Canti, G; Capaccioli, S; Ghisolfi, L; Lapucci, A; Nicolin, A; Papucci, L; Schiavone, N; Tataranni, G, 2005
)
0.56
" The relevance of a dosage adjustment based on BW/S(CR) should be further evaluated."( Population pharmacokinetics of tenofovir in human immunodeficiency virus-infected patients taking highly active antiretroviral therapy.
Dupin, N; Jaffray, P; Jullien, V; Krivine, A; Lescoat, A; Lillo-Le Louet, A; Moachon, L; Pons, G; Rey, E; Salmon, D; Tréluyer, JM; Urien, S, 2005
)
0.33
" When atazanavir 300 mg was coadministered with ritonavir 100 mg on a once-daily dosage regimen, atazanavir AUC from 0 to 24 hours and minimum plasma concentration were increased by 3- to 4-fold and approximately 10-fold, respectively, compared with atazanavir 300 mg alone."( Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir.
Barrail, A; Goujard, C; Le Tiec, C; Taburet, AM, 2005
)
0.33
" Tenofovir, nelfinavir, and M8 pharmacokinetics was unaltered when tenofovir and nelfinavir were coadministered, and tenofovir administration did not affect the M8/nelfinavir area under the concentration-versus-time curve over the dosing interval (AUC(tau)) ratio."( Lack of pharmacokinetic drug interaction between tenofovir disoproxil fumarate and nelfinavir mesylate.
Boffito, M; Higgs, C; Kearney, BP; Mathias, A; Pozniak, A; Shah, J; Zhong, L, 2005
)
0.33
"The pharmacokinetics of pradefovir and adefovir, 9-(2-phosphonylmethoxyethyl) adenine (PMEA), was evaluated in healthy male volunteers after oral dosing of pradefovir (10, 30, or 60 mg)."( Pharmacokinetics of pradefovir and PMEA in healthy volunteers after oral dosing of pradefovir.
Lin, CC; Peterson, J; Teng, A; Xu, C; Yeh, LT, 2005
)
0.56
"Antiretroviral combinations that reduce the number of pills and dosing frequency have the potential to simplify therapy."( Early virologic nonresponse to tenofovir, abacavir, and lamivudine in HIV-infected antiretroviral-naive subjects.
Berger, DS; Gallant, JE; Johnson, J; Liao, Q; Lim, ML; Rodriguez, AE; Ross, L; Shaefer, MS; Weinberg, WG; Young, B, 2005
)
0.33
" The daily dosage was 10 mg initially and then adjusted according to renal function."( Efficacy and safety of adefovir dipivoxil in kidney recipients, hemodialysis patients, and patients with renal insufficiency.
Brosgart, C; Chaix, ML; Currie, G; Fontaine, H; Morales, E; Nalpas, B; Pol, S; Serpaggi, J; Vallet-Pichard, A; Varaut, A; Verkarre, V, 2005
)
0.33
" When 400 mg was dosed with tenofovir DF, mean didanosine AUC was increased by 44% to 60% following fasted or fed administration."( Drug-drug and drug-food interactions between tenofovir disoproxil fumarate and didanosine.
Chen, SS; Cheng, AK; Flaherty, JF; Kaul, S; Kearney, BP; Sayre, JR, 2005
)
0.33
" We designed this study to provide preliminary pediatric safety and dosing information on tenofovir DF, while also providing potentially efficacious salvage therapy for heavily treatment-experienced, HIV-infected children."( Tenofovir disoproxil fumarate and an optimized background regimen of antiretroviral agents as salvage therapy for pediatric HIV infection.
Balis, FM; DeCarlo, E; Flaherty, J; Gafni, RI; Hazra, R; Kearney, BP; Maldarelli, F; Steinberg, SM; Tullio, AN; Worrell, CJ; Yale, K; Zeichner, SL, 2005
)
0.33
" It was concluded that under controlled study conditions: (1) 1-OHP, S-PMA and t,t-MA are useful biomarkers that could differentiate exposure between smoking conventional and EHCSS cigarettes or between smoking conventional cigarettes and no smoking; between S-PMA and t,t-MA, the former appeared to be more sensitive; (2) 3-MeAd could only differentiate between smoking conventional cigarettes and no smoking; the results for 3-EtAd were not conclusive because contradictory results were observed; (3) 8-OHdG had a questionable association with smoking and therefore the utility of this biomarker for smoking-related exposure could not be established; and (4) urinary excretion of thioethers as a biomarker lacked sensitivity to demonstrate a clear dose-response relationship in conventional cigarette smokers, although it could differentiate the excretion levels between those subjects who smoked a conventional cigarette and those who stopped smoking."( Evaluation of urinary 1-hydroxypyrene, S-phenylmercapturic acid, trans,trans-muconic acid, 3-methyladenine, 3-ethyladenine, 8-hydroxy-2'-deoxyguanosine and thioethers as biomarkers of exposure to cigarette smoke.
Engl, J; Feng, S; Jin, Y; Kinser, R; Liang, Q; Riedel, K; Roethig, HJ; Scherer, G; Urban, M,
)
0.35
" Blood samples for tenofovir (TFV) and SQV/RTV PK were drawn over respective 24- and 12-h dosing intervals, and drug concentrations were measured by liquid chromatography-tandem mass spectrometry."( Pharmacokinetics of tenofovir disoproxil fumarate and ritonavir-boosted saquinavir mesylate administered alone or in combination at steady state.
Adda, N; Begley, JA; Blum, MR; Chittick, GE; Kearney, BP; Sorbel, JJ; Zong, J, 2006
)
0.33
"Tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC) are nucleoside reverse transcriptase inhibitors (NRTIs) with once-daily dosing approved for use in HIV-1 infection."( In vitro evaluation of the anti-HIV activity and metabolic interactions of tenofovir and emtricitabine.
Borroto-Esoda, K; Miller, MD; Myrick, F; Ray, AS; Vela, JE, 2006
)
0.33
" Steady state was reached after daily dosing for 5 to 7 days."( Pharmacokinetics of telbivudine in healthy subjects and absence of drug interaction with lamivudine or adefovir dipivoxil.
Brown, NA; Chao, GC; Fielman, BA; Lloyd, DM; Zhou, XJ, 2006
)
0.33
" However, early HAART often consisted of drugs with complex dosing schedules, strict food requirements, treatment-limiting adverse effects, and the need to take 16-20 pills/day."( An update and review of antiretroviral therapy.
Piacenti, FJ, 2006
)
0.33
" The enzyme induction potential of pradefovir was evaluated in rats following multiple oral dosing and in primary cultures of human hepatocytes."( Metabolic activation of pradefovir by CYP3A4 and its potential as an inhibitor or inducer.
Benetton, S; Fang, C; Lin, CC; Xu, GF; Yeh, LT, 2006
)
0.33
" The single daily dosing was expected to improve adherence to treatment."( Change to a once-daily combination including boosted atazanavir in HIV-1-infected children.
Blanche, S; Delaugerre, C; Jullien, V; Macassa, E; Rouzioux, C; Teglas, JP; Tréluyer, JM; Veber, F, 2006
)
0.33
" Tenofovir requires surveillance of glomerular filtration rate and dosing interval adjustment when creatinine clearance is less than 50 ml/min and avoidance less than 30 ml/min."( Tenofovir disoproxil fumarate-emtricitabine coformulation for once-daily dual NRTI backbone.
Arribas López, JR; Muñoz de Benito, RM, 2006
)
0.33
"As expected for a renally eliminated drug, subjects with and without hepatic impairment displayed similar tenofovir systemic exposures without evidence of substantial alterations in drug disposition, and therefore no dosage adjustments were warranted in these patients."( Pharmacokinetics and dosing recommendations of tenofovir disoproxil fumarate in hepatic or renal impairment.
Flaherty, JF; Kearney, BP; Shah, J; Yale, K; Zhong, L, 2006
)
0.33
"Tenofovir measurements with an area under the concentration-time curve over the dosing interval, maximum concentration, and concentration at the end of the dosing interval (Ctau) were 32%, 15%, and 51% higher, respectively, when TDF was coadministered with LPV/r (n = 24)."( Pharmacokinetics and safety of tenofovir disoproxil fumarate on coadministration with lopinavir/ritonavir.
Cheng, AK; Ebrahimi, R; Kearney, BP; Mathias, A; Mittan, A; Sayre, J, 2006
)
0.33
" A linear dose-response relationship was observed between the GA concentration and the levels of N7-GA-Gua."( Cytogenetic damage induced by acrylamide and glycidamide in mammalian cells: correlation with specific glycidamide-DNA adducts.
Beland, FA; Churchwell, MI; Doerge, DR; Gamboa da Costa, G; Gaspar, JF; Marques, MM; Martins, C; Martins, V; Oliveira, NG; Pingarilho, M; Rueff, J, 2007
)
0.34
" Individually, these agents have long half-lifes that allow for once-daily dosing and may provide a pharmacologic bridge for the occasional missed dose."( Efavirenz/emtricitabine/tenofovir disoproxil fumarate fixed-dose combination: first-line therapy for all?
Best, B; Goicoechea, M, 2007
)
0.34
" Tenofovir is largely prescribed at the standard dosage of 300 mg once daily: therefore, the per kilogram dose is higher in Thailand than in the USA."( No change in calculated creatinine clearance after tenofovir initiation among Thai patients.
Ananworanich, J; Chetchotisakd, P; Gayet-Ageron, A; Hirschel, B; Jupimai, T; Le Braz, M; Prasithsirikul, W; Rooney, JF; Ruxrungtham, K; Ubolyam, S, 2007
)
0.34
" Tenofovir could be safely prescribed at a standard dosage of 300 mg once daily in the Thai population."( No change in calculated creatinine clearance after tenofovir initiation among Thai patients.
Ananworanich, J; Chetchotisakd, P; Gayet-Ageron, A; Hirschel, B; Jupimai, T; Le Braz, M; Prasithsirikul, W; Rooney, JF; Ruxrungtham, K; Ubolyam, S, 2007
)
0.34
" AICA and adenosine excretions increased during the day of MTX dosing (treatment day) compared to the previous baseline day in animals responding well to MTX (i."( Methotrexate and erythro-9-(2-hydroxynon-3-yl) adenine therapy for rat adjuvant arthritis and the effect of methotrexate on in vivo purine metabolism.
Baggott, JE; Morgan, SL, 2007
)
0.6
" Lack of PK alteration for FTC, tenofovir (TFV), and GS-9137 was defined as a 90% confidence interval (CI) for the estimated ratio of geometric least squares means (coadministration/alone) between 70% and 143% for the primary PK parameters: maximum observed plasma concentration (Cmax), area under the plasma concentration-time curve over dosing interval (AUCtau), and trough concentration (Ctau)."( Pharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137.
Cheng, A; Kearney, BP; Ramanathan, S; Shen, G, 2007
)
0.34
" We investigated whether tenofovir plus didanosine at a weight-adjusted dosage could be responsible for such an effect, and factors associated with CD4 + T cell count evolution under this combination."( CD4+ T cell evolution and predictors of its trend before and after tenofovir/didanosine backbone in the presence of sustained undetectable HIV plasma viral load.
Antinori, A; Antonucci, F; Barreiro, P; Carosi, G; De Silvestri, A; El Hamad, I; Ladisa, N; Lapadula, G; Maggiolo, F; Mandalia, S; Maserati, R; Migliorino, G; Pierotti, P; Sighinolfi, L; Soriano, V; Suter, F; Torti, C, 2007
)
0.34
" This study evaluated the pharmacokinetics (PK) and bioequivalence of an investigational coformulation of EFV/FTC/TDF (test) single-tablet regimen compared with the commercially available individual dosage forms (EFV+FTC+TDF; reference treatment) in healthy subjects."( Bioequivalence of efavirenz/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen.
Hinkle, J; Hui, J; Kaul, S; Kearney, BP; Mathias, AA; Menning, M, 2007
)
0.34
"Adefovir dipivoxil, a marketed drug for the treatment of hepatitis B, is dosed at submaximally efficacious doses because of renal toxicity."( Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B.
Boyer, SH; Colby, TJ; Craigo, W; DaRe, J; Erion, MD; Fujitaki, JM; Gómez-Galeno, JE; Matelich, MC; Ollis, K; Reddy, KR; Sun, Z; Ugarkar, BG; van Poelje, PD, 2008
)
0.35
" Group 1 was treated subcutaneously with a human-equivalent dose of emtricitabine (FTC), group 2 received orally the human-equivalent dosing of both FTC and tenofovir-disoproxil fumarate (TDF), and group 3 received subcutaneously a similar dosing of FTC and a higher dose of tenofovir."( Prevention of rectal SHIV transmission in macaques by daily or intermittent prophylaxis with emtricitabine and tenofovir.
Adams, DR; Cong, ME; Delinsky, D; Folks, TM; García-Lerma, JG; Heneine, W; Jackson, E; Janssen, R; Johnson, JA; Kim, C; Lipscomb, J; Luo, W; Masciotra, S; Monsour, M; Otten, RA; Qari, SH; Schinazi, RF, 2008
)
0.35
" Third, oral adenine dosing for induction of hyperphosphataemia and validation as a model using Sev were examined."( Comparison of chronic renal failure rats and modification of the preparation protocol as a hyperphosphataemia model.
Mizukami, K; Okada, M; Terai, K, 2008
)
0.72
" Oral adenine dosing induced hyperphosphataemia by 12 days, and Sev treatment was inhibitory."( Comparison of chronic renal failure rats and modification of the preparation protocol as a hyperphosphataemia model.
Mizukami, K; Okada, M; Terai, K, 2008
)
0.83
"Oral dosing with adenine made the model preparation period definitely shorter, and its usefulness as a hyperphosphataemia model was revealed using Sev."( Comparison of chronic renal failure rats and modification of the preparation protocol as a hyperphosphataemia model.
Mizukami, K; Okada, M; Terai, K, 2008
)
0.69
" Individualized dosing intervals should be further evaluated as a cost-effective alternative to fixed dosing schemes."( Antibody to hepatitis B surface antigen trough levels and half-lives do not differ after intravenous and intramuscular hepatitis B immunoglobulin administration after liver transplantation.
Hadem, J; Hooman, N; Klempnauer, J; Manns, MP; Philipp, G; Priess, A; Rifai, K; Rosenau, J; Tillmann, HL; Vaske, B, 2008
)
0.35
" The dosage of ADV was 100mg daily."( [Adefovir dipivoxil treatment of hepatic cirrhosis complicated with hepatitis B virus associated glomerulonephritis].
Chen, YS; Jin, ZJ; Li, DF; Qiao, LM; Zhou, J, 2008
)
0.35
" The likelihood of renal toxicity (proximal renal tubular dysfunction [PRTD]) correlated with plasma drug concentrations, which depended on the dosage regimen and age-related changes in drug clearance."( Chronic administration of tenofovir to rhesus macaques from infancy through adulthood and pregnancy: summary of pharmacokinetics and biological and virological effects.
Abel, K; Bischofberger, N; Brignolo, LL; Cihlar, T; Durand-Gasselin, L; Jerome, C; Kearney, BP; Marthas, ML; Moore, J; Ray, AS; Reiser, H; Spinner, A; Van Rompay, KK, 2008
)
0.35
" Pharmacokinetic profiles were also determined in HIV-1-infected patients dosed with raltegravir monotherapy versus raltegravir in combination with TDF and lamivudine."( Lack of a significant drug interaction between raltegravir and tenofovir.
Breidinger, SA; Chen, J; Friedman, EJ; Gottesdiener, KM; Iwamoto, M; Kost, JT; Lasseter, KC; Stek, JE; Stone, JA; Teppler, H; Wagner, JA; Wenning, LA, 2008
)
0.35
" Tenofovir concentrations (median 2; range, 1-5) were measured in 175 patients during several dosing intervals."( Population pharmacokinetics of tenofovir in AIDS patients.
Barkil, ME; Boibieux, A; Cotte, L; Gagnieu, MC; Guitton, J; Livrozet, JM; Miailhes, P; Tod, M, 2008
)
0.35
" Dosing whole rats repeatedly with different concentrations of SM360320 confirmed the in vitro results."( Comparison of rat and human responses to toll-like receptor 7 activation.
Clarke, S; Horscroft, N; Laxton, C; Parkinson, T; Richard, V; Thomas, A, 2009
)
0.35
" When implementing HAART, physicians should be aware of and monitor potential patient misunderstanding of instructions on dosage and administration and for possible complications in medicinal combinations and potential side effects."( [A case of acute renal failure involving high amounts of tenofovir after HAART start].
Kasahara, K; Konishi, M; Maeda, K; Mikasa, K; Nakagawa, C; Uno, K; Yonekawa, S; Yoshimoto, E, 2008
)
0.35
" The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation <2%), while being simple, cheap and less time consuming and can be suitably applied for the estimation of tenofovir disoproxil fumarate in different dosage forms."( Application of UV-spectrophotometric methods for estimation of tenofovir disoproxil fumarate in tablets.
A, SA; H, BC; J, SS, 2009
)
0.35
" Because of this latter characteristic, dosage adjustments are required in patients with renal insufficiency."( [Tenofovir: pharmacology and interactions].
Azanza, JR; García Quetglas, E; Gómez-Giu, A; Sádaba, B, 2008
)
0.35
" The only available formulation is an adult tablet, introducing the possibility of dosing errors in children."( Tenofovir use in human immunodeficiency virus-1-infected children in the United kingdom and Ireland.
Boyd, K; Butler, K; Cliff, D; Doerholt, K; Gibb, D; Judd, A; Lyall, H; Menson, E; Riordan, A, 2009
)
0.35
" To attain a better antiviral response the dosage of entecavir was increased to 2mg daily in two patients, resulting in further viral load decline for both of them."( Entecavir shows limited efficacy in HBeAg-positive hepatitis B patients with a partial virologic response to adefovir therapy.
de Man, RA; Janssen, HL; Pas, SD; Reijnders, JG; Schutten, M, 2009
)
0.35
"Entecavir monotherapy dosed at 1mg resulted in a slow reduction of viral load in both lamivudine-experienced and -naïve patients with persistently high HBV DNA during adefovir therapy."( Entecavir shows limited efficacy in HBeAg-positive hepatitis B patients with a partial virologic response to adefovir therapy.
de Man, RA; Janssen, HL; Pas, SD; Reijnders, JG; Schutten, M, 2009
)
0.35
" Statistical analyses were performed on pharmacokinetic parameters: the area under the concentration-time curve from 0 to 4 h (AUC(0-4)), the maximum concentration of the drug (C(max)), and the residual concentration of the drug at the end of the dosing interval (C(trough)) for plasma and the AUC(0-4) and C(trough) for intracellular data."( Pilot pharmacokinetic study of human immunodeficiency virus-infected patients receiving tenofovir disoproxil fumarate (TDF): investigation of systemic and intracellular interactions between TDF and abacavir, lamivudine, or lopinavir-ritonavir.
Ayen, R; Clotet, B; Grassi, J; Levi, M; Negredo, E; Pruvost, A; Puig, J; Théodoro, F, 2009
)
0.35
"Oral dosing with adenine induced CKD in rats in only 10 days."( Vascular calcification and secondary hyperparathyroidism of severe chronic kidney disease and its relation to serum phosphate and calcium levels.
Fujimori, A; Fukushima, S; Itoh, H; Mizukami, K; Nara, H; Okada, M; Sanagi, M; Takakura, K; Terai, K, 2009
)
0.69
"These data suggest that rats dosed orally with adenine provide a more useful model for analysing calcium/phosphate homeostasis in severe CKD."( Vascular calcification and secondary hyperparathyroidism of severe chronic kidney disease and its relation to serum phosphate and calcium levels.
Fujimori, A; Fukushima, S; Itoh, H; Mizukami, K; Nara, H; Okada, M; Sanagi, M; Takakura, K; Terai, K, 2009
)
0.61
" Studies to investigate the antitumor effects of BIIB021 showed activity on both daily and intermittent dosing schedules, providing dose schedule flexibility for clinical studies."( BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.
Boehm, MF; Brekken, J; Burrows, FJ; Busch, DJ; Friedman, J; Hong, K; Huser, N; Kamal, A; Kasibhatla, SR; Lundgren, K; McKenzie, A; Neely, L; Powell, RE; Scannevin, R; Sensintaffar, JL; Timple, N; Yang, YC; Zhang, H, 2009
)
0.35
" A new combination therapy consisting of the TFV pro-drug (300 mg) and another reverse transcriptase inhibitor, emtricitabine (FTC, 200 mg) has become available in a convenient once-daily dosage form (Truvada)."( The simultaneous assay of tenofovir and emtricitabine in plasma using LC/MS/MS and isotopically labeled internal standards.
Bushman, L; Delahunty, T; Fletcher, CV; Robbins, B, 2009
)
0.35
" We report 12-month changes in renal profiles among 19 such patients (6 patients with history of and 13 patients with current renal disease) in the HIV Outpatient Study (HOPS) who initiated TDF-containing highly active antiretroviral therapy (HAART) during 2001-2005 with TDF dosed mostly at 300 mg once daily."( Renal function in patients with preexisting renal disease receiving tenofovir-containing highly active antiretroviral therapy in the HIV outpatient study.
Brooks, JT; Buchacz, K; Moorman, A; Wood, KC; Young, B, 2009
)
0.35
"Tenofovir DF and norgestimate-ethinyl estradiol are not involved in a clinically significant drug-drug interaction; tenofovir DF did not affect the steady-state pharmacokinetics of norgestimate or ethinyl estradiol, including the concentration at the end of the dosing interval."( Lack of effect of tenofovir disoproxil fumarate on pharmacokinetics of hormonal contraceptives.
Kearney, BP; Mathias, A, 2009
)
0.35
" Furthermore, it also demonstrates the benefits of using preclinical models of chemosensitization to radiotherapy to explore clinically relevant radiation dosing schemes."( BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy.
Burrows, F; Lundgren, K; Shores, CG; Wilson, L; Yin, X; Zhang, H, 2010
)
0.36
" However, the dosing interval of ADV should be adjusted according to renal function and serum phosphate levels in patients receiving long-term treatment."( Add-on combination therapy with adefovir dipivoxil induces renal impairment in patients with lamivudine-refractory hepatitis B virus.
Enomoto, M; Habu, D; Imanishi, Y; Iwai, S; Kawada, N; Kobayashi, S; Morikawa, H; Sakaguchi, H; Shiomi, S; Tamori, A, 2010
)
0.36
" Also a complete 12-hour pharmacokinetic profile was recorded for 15 transplant patients who had the polymorphism and for 15 controls who were randomly chosen since they received the same type and dosage of mycophenolate, same posttransplant time and similar renal function."( The prevalence of uridine diphosphate-glucuronosyltransferase 1A9 (UGT1A9) gene promoter region single-nucleotide polymorphisms T-275A and C-2152T and its influence on mycophenolic acid pharmacokinetics in stable renal transplant patients.
Arroyo, M; Barrientos, A; Calvo, N; De la Orden, V; Maestro, ML; Ortega, D; Pérez-Flores, I; Sánchez-Fructuoso, AI; Veganzone, S; Viudarreta, M,
)
0.13
" These cells showed reduced MRP4 protein expression and corresponding reduction in the basolateral egress of adefovir when adefovir dipivoxil was dosed on the apical side."( Role of basolateral efflux transporter MRP4 in the intestinal absorption of the antiviral drug adefovir dipivoxil.
Ming, X; Thakker, DR, 2010
)
0.36
"Once-daily treatment with ritonavir-boosted saquinavir was well tolerated and resulted in similar saquinavir drug exposure despite much lower ritonavir concentrations when compared with a twice-daily dosing schedule."( Once-daily treatment with saquinavir mesylate (2000 mg) and ritonavir (100 mg) together with a fixed-dose combination of abacavir/lamivudine (600/300 mg) or tenofovir/emtricitabine (245/200 mg) in HIV-1-infected patients.
Bickel, M; Bodtländer, A; Gute, P; Klauke, S; Knecht, GK; Kurowski, M; Lutz, T; Stephan, C; von Hentig, N, 2009
)
0.35
" Its favorable profile in terms of high efficacy, low toxicity and once-daily dosing makes TDF one of the most attractive antiretroviral agents, and therefore, it is widely used."( Pharmacogenetics of tenofovir treatment.
Labarga, P; Rodriguez-Novoa, S; Soriano, V, 2009
)
0.35
" No differences were noted in adverse events among dosing periods."( Steady-state amprenavir and tenofovir pharmacokinetics after coadministration of unboosted or ritonavir-boosted fosamprenavir with tenofovir disoproxil fumarate in healthy volunteers.
Andrews, M; Condoluci, DV; Luber, AD; Olson, K; Pakes, GE; Pappa, KA; Peloquin, CA; Slowinski, PD, 2010
)
0.36
" We investigated the relationship of NVP dosing with safety and efficacy."( Safety and efficacy of once-daily nevirapine dosing: a multicohort study.
Battegay, M; Calmy, A; de Wolf, F; Hirschel, B; Hogg, RS; Lange, JM; Lima, VD; Montaner, JS; Nguyen, A; Reiss, P; Vallier, N; Wit, FW; Yip, B, 2009
)
0.35
" Daily drug dosage was 300 mg Tenofovir, 200mg Emtricitabine and 400 mg Nevirapine once daily."( Long-term efficacy and safety of once-daily nevirapine in combination with tenofovir and emtricitabine in the treatment of HIV-infected patients: a 72-week prospective multicenter study (TENOR-trial).
Flux, K; Gholam, P; Hartmann, M; Hueter, E; Weberschock, T, 2009
)
0.35
" We hypothesized that intermittent prophylactic treatment with long-acting antiviral drugs would be as effective as daily dosing in blocking the earliest stages of viral replication and preventing mucosal transmission."( Intermittent prophylaxis with oral truvada protects macaques from rectal SHIV infection.
Barr, JR; Cong, ME; Folks, TM; García-Lerma, JG; Hanson, DL; Heneine, W; Holder, A; Kuklenyik, Z; Lipscomb, J; Martin, A; Masciotra, S; Mitchell, J; Otten, R; Pau, CP; Paxton, L; Youngpairoj, AS; Zheng, Q, 2010
)
0.36
" Following oral dosing (3mg/kg) in Beagle dogs, high levels (>9."( Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.
Birkus, G; Boojamra, CG; Cihlar, T; Desai, MC; Douglas, JL; Gao, Y; Grant, D; Hui, HC; Laflamme, G; Lin, KY; Mackman, RL; Markevitch, DY; McDermott, M; Mishra, R; Pakdaman, R; Petrakovsky, OV; Ray, AS; Vela, JE; Zhang, L, 2010
)
0.36
" Irrespective of the dosing strategy used, the rsIL-7gly administration transiently increased proliferation of both central memory and naive cells, in both CD4(+) and CD8(+) subsets, without increasing SIV levels in the blood."( Increased CD4+ T cell levels during IL-7 administration of antiretroviral therapy-treated simian immunodeficiency virus-positive macaques are not dependent on strong proliferative responses.
Assouline, B; Axthelm, MK; Legasse, A; Leone, A; Lifson, JD; Morre, M; Okoye, A; Piatak, M; Picker, LJ; Rohankhedkar, M; Sodora, DL; Villinger, F, 2010
)
0.36
" Emergence of postbaseline resistance mutations occurred at similar low rates in each dosing group."( Short communication: Comparable safety and efficacy with once-daily versus twice-daily dosing of lopinavir/ritonavir tablets with emtricitabine + tenofovir DF in antiretroviral-naïve, HIV type 1-infected subjects: 96 week final results of the randomized t
Bernstein, B; Cohen, D; da Silva, B; Fredrick, L; González-García, J; Johnson, M; Naylor, C; Sloan, L, 2010
)
0.36
" Relative to ritonavir-boosted EVG, the geometric least-squares means ratios (GMR) [90% confidence interval (CI)] for EVG area under plasma concentration-time curve from time zero until the end of the dosing interval (AUC)tau, maximum concentration (Cmax), and trough concentration (Ctau) were 118 (110 to 126), 108 (100 to 116), and 110 (95."( Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV.
German, P; Hui, J; Kearney, BP; Warren, D; West, S, 2010
)
0.36
"Addition of darunavir/ritonavir to etravirine, all dosed once daily, did not have a clinically significant effect on the pharmacokinetics of etravirine."( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults.
DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010
)
0.36
" Transport studies in a rat model have shown enhanced levels of total cidofovir species in the plasma after oral dosing with L-Val-L-Ser-OMe cHPMPC, 2a."( Serine side chain-linked peptidomimetic conjugates of cyclic HPMPC and HPMPA: synthesis and interaction with hPEPT1.
Kashemirov, BA; Krylov, IS; McKenna, CE; Peterson, LW; Sala-Rabanal, M; Serpi, M, 2010
)
0.36
" Therefore, the results do not support daily ADV dosing using a liquid suspension over the current strategy of adjustment of the ADV dosing interval in patients with impaired renal function."( Efficacy and pharmacokinetics of adefovir dipivoxil liquid suspension in patients with chronic hepatitis B and renal impairment.
Frederick, D; Pol, S; Rostaing, L; Rousseau, F; Schiff, E; Shiffman, ML; Thabut, D; Zeuzem, S; Zong, J, 2011
)
0.37
" This review identifies important cellular pharmacology considerations for tenofovir and emtricitabine, which include drug penetration into relevant tissues and cell types, race/ethnicity/pharmacogenetics, gender, cellular activation state and appropriate episodic or alternative dosing strategies based on pharmacokinetic principles."( Pharmacological considerations for tenofovir and emtricitabine to prevent HIV infection.
Anderson, PL; Gardner, EM; Grant, RM; Kiser, JJ; Meditz, A; Rower, JE, 2011
)
0.37
" Healthy volunteer studies have demonstrated a decrease in glucose disposal associated with dosing with specific antiretrovirals."( Effect of boosted fosamprenavir or lopinavir-based combinations on whole-body insulin sensitivity and lipids in treatment-naive HIV-type-1-positive men.
Back, DJ; Boffito, M; Jackson, AG; Mandalia, S; Moyle, GJ; Randell, PA; Taylor, J; Tjia, JF, 2010
)
0.36
" IFN therapy requires dosage reduction and close monitoring in patients with a GFR <50 ml/min/1."( Does the antiviral therapy of patients with chronic hepatitis exert nephrotoxic effects?
Bob, F; Bozdog, G; Cioca, D; Curescu, M; Gadalean, F; Gluhovschi, C; Gluhovschi, G; Kaycsa, A; Petrica, L; Sporea, I; Velciov, S; Vernic, C, 2011
)
0.37
" Dosing was separated by a wash-out period of 14 days."( Bioequivalence study of two oral tablet formulations containing tenofovir disoproxil fumarate in healthy volunteers.
Feleder, EC; Halabe, EK; Yerino, GA; Zini, E, 2011
)
0.37
" Decreases in estimated glomerular filtration rate occurred within the first few weeks of dosing in participants receiving EVG/COBI/FTC/TDF, remained within the normal range and did not progress at week 24 or 48; no participant experienced a clinical adverse event or discontinued study drug due to changes in serum creatinine or renal function."( Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection.
Chuck, SL; Cohen, C; DeJesus, E; Elion, R; Kearney, BP; Liu, HC; Ramanathan, S; Rashbaum, B; Ruane, P; Shamblaw, D; Warren, DR; Yale, K, 2011
)
0.37
" Nephrotoxicity is dose related and occurred at a daily dosage of >30 mg."( Acquired Fanconi syndrome associated with prolonged adefovir dipivoxil therapy in a chronic hepatitis B patient.
Ho, YY; Law, ST; Li, KK,
)
0.13
" The drug has a 5-position amine that is variably acetylated to form a toxic metabolite in humans, increasing adverse effects and complicating the dosing of amonafide."( Methoxyethylamino-numonafide is an efficacious and minimally toxic amonafide derivative in murine models of human cancer.
Appella, DH; Chen, Z; Huang, S; Liu, Y; Lou, G; Norton, JT; Wang, C; Witschi, MA; Xu, Q, 2011
)
0.37
" The better results of lowering serum uric acid and protecting against renal failure were at the dosage of Que between 10 and 20 mg/kg."( [Preventive and therapeutic effects of quercetin on hyperuricemia and renal injury in rats].
Fu, R; He, W; Yao, F; Zhang, R, 2011
)
0.37
" For patients receiving HBIG and LAM, a lower frequency of HBV recurrence was associated with a high HBIG dosage (≥10,000 IU/day) versus a low HBIG dosage (<10,000 IU/day) during the first week after LT [3."( Hepatitis B immunoglobulin and/or nucleos(t)ide analogues for prophylaxis against hepatitis b virus recurrence after liver transplantation: a systematic review.
Akriviadis, E; Cholongitas, E; Goulis, J; Papatheodoridis, GV, 2011
)
0.37
" The current monitoring modalities, together with dosage adjustments, treatment of patients with ADV-related kidney impairment and the therapeutic algorithm in place at the authors' Liver Center are also summarized."( Drug safety evaluation of adefovir in HBV infection.
Colombo, M; Lampertico, P; Viganò, M, 2011
)
0.37
" Dosage of 200 mg might provide an option to patients showing suboptimal ATV exposure with standard unboosted dosing."( Pharmacokinetics of switching unboosted atazanavir coadministered with tenofovir disoproxil fumarate from 400 mg once daily to 200 mg twice daily in HIV-positive patients.
Baietto, L; Bonora, S; Calcagno, A; D'Avolio, A; Di Perri, G; Gonzalez de Requena, D; Siccardi, M; Simiele, M; Tettoni, M; Trentini, L, 2011
)
0.37
"Adefovir dipivoxil can be nephrotoxic at conventional dosage and therefore, patients treated with long-term ADV should have regular monitoring of renal function, and calcium and phosphate levels."( Nephrotoxicity, including acquired Fanconi's syndrome, caused by adefovir dipivoxil - is there a safe dose?
Ho, YY; Law, ST; Li, KK, 2012
)
0.38
" Modification of the dosing interval or discontinuation of ADV was required in seven and three patients, respectively, and none of them showed a further decline in the eGFR."( Frequency and risk factors of renal impairment during long-term adefovir dipivoxil treatment in chronic hepatitis B patients.
Cho, HC; Choi, MS; Gwak, GY; Kim, YJ; Koh, KC; Lee, JH; Paik, SW; Sinn, DH; Yoo, BC, 2012
)
0.38
" Dosing scheme, according BW and LPV/r coadministration were simulated to produce the same 24-hr exposure as adults after 300-mg TDF dose."( Population pharmacokinetics of tenofovir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Rey, E; Tréluyer, JM; Urien, S, 2011
)
0.37
"Children without LPV/r should receive: 150 mg TDF from 20 to 30 kg, 225 mg TDF from 30 to 40 kg, and the adult dosage of 300 mg TDF over 40 kg."( Population pharmacokinetics of tenofovir in HIV-1-infected pediatric patients.
Benaboud, S; Blanche, S; Bouazza, N; Foissac, F; Frange, P; Hirt, D; Rey, E; Tréluyer, JM; Urien, S, 2011
)
0.37
" Low concentrations at birth support infant dosing as soon after birth as possible."( Pharmacokinetics and safety of single-dose tenofovir disoproxil fumarate and emtricitabine in HIV-1-infected pregnant women and their infants.
Bardeguez, A; Cotter, A; Fiscus, SA; Flynn, PM; Heckman, B; Huang, S; Jean-Philippe, P; Kearney, B; Mirochnick, M; Mofenson, LM; Purswani, M; Robbins, B; Rodman, J; Rooney, JF; Shapiro, DE; Thorpe, E; Van Rompay, KK; Watts, DH, 2011
)
0.37
" The method was applied to the determination of adefovir in plasma from 12 subjects dosed with adefovir 2 x 10 mg tablets and pharmacokinetic parameters were evaluated."( Rapid high-performance liquid chromatographic method for determination of adefovir in plasma using UV detection: application to pharmacokinetic studies.
Foroutan, SM; Khoddam, A; Movahed, H; Shafaati, A; Zarghi, A, 2011
)
0.37
" At all doses, concentrations at the dosing site were typically 1 to 2 log units higher than those in the opposite compartment and 4 to 5 log units higher than those in plasma."( Pharmacokinetics of tenofovir following intravaginal and intrarectal administration of tenofovir gel to rhesus macaques.
Allen, P; Kashuba, A; Nuttall, J; Roberts, J; Romano, J; Wang, R; White, N, 2012
)
0.38
" Forty-seven were randomized to once (QD) or twice daily (BID) dosing for 2 weeks and to collection of genital tract samples at 4, 8 or 24 hrs after the final dose, but two discontinued prior to gel application."( A multi-compartment, single and multiple dose pharmacokinetic study of the vaginal candidate microbicide 1% tenofovir gel.
Brache, V; Creinin, MD; Kashuba, AD; Kearney, BP; Poindexter, A; Rountree, W; Schwartz, JL, 2011
)
0.37
" Despite continued gel dosing postinfection, neither breakthrough infection had evidence of drug resistance by ultrasensitive testing of SHIV in plasma and vaginal lavage."( Durable protection from vaginal simian-human immunodeficiency virus infection in macaques by tenofovir gel and its relationship to drug levels in tissue.
Dobard, C; García-Lerma, JG; Hanson, DL; Heneine, W; Holder, A; Kuklenyik, Z; Lipscomb, J; Martin, A; Novembre, FJ; Pau, CP; Sharma, S; Smith, J, 2012
)
0.38
"Atazanavir geometric mean (CV%) C(max), C(min) and AUC over the dosing interval were 2897 (46) ng/mL, 526 (57) ng/mL and 28 605 (46) ng · h/mL, respectively, and for lopinavir they were 10 655 (51) ng/mL, 5944 (68) ng/mL and 90 946 (59) ng · h/mL, respectively."( Pharmacokinetics and inhibitory quotient of atazanavir/ritonavir versus lopinavir/ritonavir in HIV-infected, treatment-naive patients who participated in the CASTLE Study.
Bertz, R; Child, M; Eley, T; Farajallah, A; Krystal, M; Liao, S; McGrath, D; Molina, JM; Persson, A; Sevinsky, H; Xu, X; Zhang, J; Zhu, L, 2012
)
0.38
" When dosed into the lung the compounds were rapidly metabolized and short-term exposure of the 'antedrug' was sufficient to activate the IFN pathway."( Biological characterization of a novel class of toll-like receptor 7 agonists designed to have reduced systemic activity.
Aoki, M; Benjamin, AD; Biffen, M; Doyle, I; Edwards, S; Eiho, K; Fraser, NJ; Hawkins, SL; Holness, E; Leishman, AJ; Matsui, H; McInally, T; Murray, CM; Satterthwaite, G; Takaku, H; Tomizawa, H; Wada, H, 2012
)
0.38
" Dosing antiretroviral agents with kidney metabolism should be adjusted when eGFR is bellow 50 mL/min/1."( [Kidney and HIV infection].
Lescure, FX; Plaisier, E; Ronco, P, 2012
)
0.38
" Dosing strategies (e."( Formulation, pharmacokinetics and pharmacodynamics of topical microbicides.
Adams, JL; Kashuba, AD, 2012
)
0.38
" Although some trial results appear conflicting, behavioral factors, adherence to dosing and pharmacokinetic properties of the different tenofovir formulations and dosing approaches offer plausible explanations for most of the variations in effectiveness observed in different trials."( A drug evaluation of 1% tenofovir gel and tenofovir disoproxil fumarate tablets for the prevention of HIV infection.
Abdool Karim, SS; Baxter, C; Gengiah, TN; Kharsany, AB; Mansoor, LE, 2012
)
0.38
" Median TFV concentrations in iliac lymph nodes ranged from 44 ng/g to 196 ng/g; differences between iliac lymph node TFV concentrations following dosing of the two gels were insignificant."( Pharmacokinetics and topical vaginal effects of two tenofovir gels in rabbits.
Clark, MR; Friend, DR, 2012
)
0.38
" Raltegravir must be dosed twice daily, as once daily raltegravir displays decreased virologic efficacy compared to twice daily dosing."( Role of raltegravir in HIV-1 management.
Bookstaver, PB; Bryant, JE; Millisor, VE; Rokas, KE; Shamroe, CL; Sutton, SS; Weissman, SB, 2012
)
0.38
"Little is known about safety of and adherence to intermittent HIV PrEP regimens, which may be more feasible than daily dosing in some settings."( Safety and adherence to intermittent pre-exposure prophylaxis (PrEP) for HIV-1 in African men who have sex with men and female sex workers.
Anzala, O; Bangsberg, D; Barin, B; Chetty, P; Fast, P; Haberer, JE; Mark, D; Mugo, P; Mutua, G; Priddy, FH; Rooney, JF; Sanders, E, 2012
)
0.38
"Adherence to intermittent dosing regimens, fixed doses, and in particular coitally-dependent doses, may be more difficult than adherence to daily dosing."( Safety and adherence to intermittent pre-exposure prophylaxis (PrEP) for HIV-1 in African men who have sex with men and female sex workers.
Anzala, O; Bangsberg, D; Barin, B; Chetty, P; Fast, P; Haberer, JE; Mark, D; Mugo, P; Mutua, G; Priddy, FH; Rooney, JF; Sanders, E, 2012
)
0.38
" Adherence by type of ART and dosing frequency were compared by Brown-Mood median tests."( Impact of antiretroviral dosing frequency and pill burden on adherence among newly diagnosed, antiretroviral-naive HIV patients.
Buscher, A; Giordano, TP; Hartman, C; Kallen, MA, 2012
)
0.38
" The use of SF and PK-PD disease models can be a valuable tool to predict dose-response of NMEs and support rational dose selection for monotherapy trials."( From in vitro EC₅₀ to in vivo dose-response for antiretrovirals using an HIV disease model. Part I: a framework.
Fang, J; Jadhav, PR, 2012
)
0.38
" We developed a pharmacokinetic model for TDF and its active anabolite tenofovir-diphosphate (TFV-DP) and validated it with data from 4 different trials, including 4 distinct dosing regimes."( Pharmacokinetics and pharmacodynamics of the reverse transcriptase inhibitor tenofovir and prophylactic efficacy against HIV-1 infection.
Duwal, S; Schütte, C; von Kleist, M, 2012
)
0.38
" Dosing and time course experiments showed that 3-MA's ability to activate lipolysis was more sensitive than its inhibitory effect on autophagy."( The autophagic inhibitor 3-methyladenine potently stimulates PKA-dependent lipolysis in adipocytes.
Heckmann, BL; Liu, J; Yang, X; Zhang, X, 2013
)
0.67
" Many HIV-1-infected patients who are treatment-naive or treatment-experienced with susceptible virus will potentially have more options to reduce pill burden and optimize dosage schedules with one pill once-daily regimens."( Once-daily single-tablet regimens: a long and winding road to excellence in antiretroviral treatment.
Clotet, B; Llibre, JM,
)
0.13
" Optimal PrEP agents and dosing regimens now need to be identified."( Considerations regarding antiretroviral chemoprophylaxis in MSM.
Grulich, AE; Poynten, IM; Zablotska, I, 2012
)
0.38
"The Microbicide Trials Network 003 study, a large phase IIb trial, was unable to show that daily dosing with 1% tenofovir vaginal gel was effective for HIV prevention."( Current status of topical antiretroviral chemoprophylaxis.
Szpir, M; Van Damme, L, 2012
)
0.38
" Phase II and III trials continue to explore different dosing strategies for topical products that contain one or more ARV agents."( Current status of topical antiretroviral chemoprophylaxis.
Szpir, M; Van Damme, L, 2012
)
0.38
" Dosing was discontinued on day 30 and blood was collected on days 35, 45, and 60 during the washout period."( Tenofovir, emtricitabine, and tenofovir diphosphate in dried blood spots for determining recent and cumulative drug exposure.
Anderson, PL; Bushman, LR; Castillo-Mancilla, JR; Fernandez, C; Gardner, EM; Kiser, JJ; Langness, J; Meditz, A; Predhomme, J; Rower, JE; Zheng, JH, 2013
)
0.39
" We conclude that rectal dosing with TFV 1% gel resulted in greater TFV-DP tissue detection than oral dosing with reduced ex vivo biopsy infectibility, enabling PK-PD correlations."( RMP-02/MTN-006: A phase 1 rectal safety, acceptability, pharmacokinetic, and pharmacodynamic study of tenofovir 1% gel compared with oral tenofovir disoproxil fumarate.
Anton, PA; Bumpus, NN; Carballo-Diéguez, A; Cranston, RD; Cumberland, WG; Dennis, R; Elliott, J; Hendrix, CW; Janocko, L; Ju, C; Kashuba, A; Khanukhova, E; Mauck, C; McGowan, I; Richardson-Harman, N, 2012
)
0.38
" Vaginal dosing achieves measurable tenofovir concentrations in the rectum and vice versa."( The clinical pharmacology of antiretrovirals for HIV prevention.
Hendrix, CW, 2012
)
0.38
" Directly observed dosing in a separate study, the STRAND trial, yielded TFV-DP concentrations that, when analyzed according to the iPrEx model, corresponded to an HIV-1 risk reduction of 76% for two doses per week, 96% for four doses per week, and 99% for seven doses per week."( Emtricitabine-tenofovir concentrations and pre-exposure prophylaxis efficacy in men who have sex with men.
Anderson, PL; Bekker, LG; Buchbinder, S; Bushman, LR; Casapía, M; Chariyalertsak, S; Glidden, DV; Grant, RM; Guanira, JV; Kallás, EG; Lama, JR; Liu, A; Mayer, KH; McMahan, V; Montoya-Herrera, O; Schechter, M; Veloso, VG, 2012
)
0.38
" This is the first vaginal dosage form to provide sustained delivery of milligram quantities of TFV for 90 days."( Quantitative evaluation of a hydrophilic matrix intravaginal ring for the sustained delivery of tenofovir.
Clark, JT; Clark, MR; Fabian, J; Friend, DR; Johnson, TJ; Kiser, PF; Nebeker, JS; Ponnapalli, S; Smith, EM; Tuitupou, AL, 2012
)
0.38
"In this highly adherent population, the number of daily pills was related to self-reported health status but not to self-reported adherence, whereas the dosing interval did not influence self-reported adherence or health status."( Number of daily pills, dosing schedule, self-reported adherence and health status in 2010: a large cross-sectional study of HIV-infected patients on antiretroviral therapy.
Bocchiola, B; Cahua, T; Castagna, A; Danise, A; Galli, L; Gianotti, N; Lazzarin, A; Maillard, M; Panzini, P; Pazzi, A; Salpietro, S; Zandonà, D, 2013
)
0.39
" The development of drug-CD complexes as solids allows for potential advantages in dosage form design, such as the preparation of layered formulations, and it also can yield improvements in chemical and physical stability."( 2D solid-state NMR analysis of inclusion in drug-cyclodextrin complexes.
Strohmeier, M; Vogt, FG, 2012
)
0.38
"These data demonstrate that children and adolescents receiving standard TDF dosing of 300 mg once daily achieve higher intracellular TFV-DP concentrations than adults, despite lower plasma TFV concentrations."( Age-related differences in plasma and intracellular tenofovir concentrations in HIV-1-infected children, adolescents and adults.
Acosta, EP; Baheti, G; Fletcher, CV; King, JR, 2013
)
0.39
" Use of exact dosing data halved unexplained variability in ATV clearance."( Effect of adherence as measured by MEMS, ritonavir boosting, and CYP3A5 genotype on atazanavir pharmacokinetics in treatment-naive HIV-infected patients.
Barrail-Tran, A; Descamps, D; Duval, X; Goujard, C; Mentré, F; Nembot, G; Panhard, X; Savic, RM; Taburet, AM; Verstuyft, C; Vrijens, B, 2012
)
0.38
" The results showed that four types of aqueous extracts significantly induced the formation of N7-MeG and N3-MeA in a linear dose-response manner."( Direct-acting DNA alkylating agents present in aqueous extracts of areca nut and its products.
Chao, MR; Hu, CW, 2012
)
0.38
" Model-predicated area under the concentration-time curve during the dosing interval (AUC(τ)) and exposure ratios of CVF AUC(τ):BP AUC(τ) were calculated for each drug."( Pharmacokinetic modelling of efavirenz, atazanavir, lamivudine and tenofovir in the female genital tract of HIV-infected pre-menopausal women.
Cohen, MS; Dumond, JB; Forrest, A; Garonzik, SM; Kashuba, AD; Kendrick, RN; Nicol, MR; Patterson, KB, 2012
)
0.38
"Acetaminophen is a safe antipyretic and analgesic drug within the clinically recommended dosage range, but overdose can cause fatal liver and or kidney damage."( Effect of acetaminophen on the progression of renal damage in adenine induced renal failure model rats.
Arimizu, K; Chuang, VT; Hirata, S; Irie, T; Ishitsuka, Y; Kadowaki, D; Kitamura, K; Maruyama, T; Narita, Y; Otagiri, M; Sumikawa, S; Taguchi, K, 2012
)
0.62
" Through dose-response experiments, we established relative inhibitory potencies of NRTIs on in vitro telomerase activity as compared to the inhibitory potencies of the corresponding dideoxynucleotide triphosphates."( In vitro and ex vivo inhibition of human telomerase by anti-HIV nucleoside reverse transcriptase inhibitors (NRTIs) but not by non-NRTIs.
Côté, HC; Hukezalie, KR; Thumati, NR; Wong, JM, 2012
)
0.38
" Drug concentrations at two trough values of 12 and 24 h after dosing (C(12) and C(24)), area under the concentration-curve values (AUC), maximum drug concentration (C(max)), and the time at which this concentration occurred (T(max)) in plasma were estimated with noncompartmental pharmacokinetic methods and compared to data from a subset of white subjects randomized to the RAL twice a day (plus TDF/FTC) arm of the QDMRK study, a phase III study of the safety and efficacy of once daily versus twice daily RAL in treatment naive patients."( Raltegravir pharmacokinetics in treatment-naive patients is not influenced by race: results from the raltegravir early therapy in African-Americans living with HIV (REAL) study.
Blevins, S; Dumond, JB; Eron, JJ; Floris-Moore, M; Hudgens, MG; Kashuba, AD; Massengale, K; Pittard, D; Ragan, D; Richardson, A; Walsh, K; Wang, R; Wohl, DA, 2013
)
0.39
"Phase 0 studies can provide initial pharmacokinetics (PKs) data in humans and help to facilitate early drug development, but their predictive value for standard dosing is controversial."( Biphasic elimination of tenofovir diphosphate and nonlinear pharmacokinetics of zidovudine triphosphate in a microdosing study.
Chen, J; Flexner, C; Fuchs, EJ; Hendrix, CW; Liberman, RG; Louissaint, NA; Skipper, PL; Tannenbaum, SR, 2012
)
0.38
" A fixed-dose combination (FDC) formulation of lamivudine/adefovir dipivoxil for the treatment of CHB may provide dosing convenience and improve adherence."( Pharmacokinetic properties of single-dose lamivudine/adefovir dipivoxil fixed-dose combination in healthy Chinese male volunteers.
Chan, JC; Chen, S; Chu, TT; Fok, BS; Gardner, S; Piscitelli, S; Tomlinson, B, 2013
)
0.39
" Blood samples were collected immediately before and after dosing for 48 hours for plasma drug concentration measurement."( Pharmacokinetic properties of single-dose lamivudine/adefovir dipivoxil fixed-dose combination in healthy Chinese male volunteers.
Chan, JC; Chen, S; Chu, TT; Fok, BS; Gardner, S; Piscitelli, S; Tomlinson, B, 2013
)
0.39
" Twice daily dosing of GSK2656157 results in dose-dependent inhibition of multiple human tumor xenografts growth in mice."( Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity.
Alsaid, H; Atkins, C; Axten, JM; Choudhry, AE; Figueroa, DJ; Gaul, N; Goetz, A; Jucker, BM; Kumar, R; Liu, Q; Minthorn, E; Moss, K; Sanders, B; Stanley, TB; Zhang, SY, 2013
)
0.39
" Serum concentrations after vaginal dosing were 56-fold lower than after oral dosing (p<0."( MTN-001: randomized pharmacokinetic cross-over study comparing tenofovir vaginal gel and oral tablets in vaginal tissue and other compartments.
Bumpus, NN; Chen, BA; Gandham, S; Gomez, K; Guddera, V; Hendrix, CW; Hoesley, C; Justman, J; Minnis, AM; Nakabiito, C; Patterson, K; Richardson, BA; Salata, R; Soto-Torres, L, 2013
)
0.39
"Compared to oral dosing, vaginal dosing achieved much lower serum concentrations and much higher vaginal tissue concentrations."( MTN-001: randomized pharmacokinetic cross-over study comparing tenofovir vaginal gel and oral tablets in vaginal tissue and other compartments.
Bumpus, NN; Chen, BA; Gandham, S; Gomez, K; Guddera, V; Hendrix, CW; Hoesley, C; Justman, J; Minnis, AM; Nakabiito, C; Patterson, K; Richardson, BA; Salata, R; Soto-Torres, L, 2013
)
0.39
" Blood plasma (for TFV, FTC, EFV, ATV and RTV concentrations) and peripheral blood mononuclear cells [PBMCs; for tenofovir diphosphate (TFV-DP) and emtricitabine triphosphate (FTC-TP) concentrations] were collected at 11 time-points over a 24-hour dosing interval."( Pharmacokinetics of two common antiretroviral regimens in older HIV-infected patients: a pilot study.
Adams, JL; Corbett, AH; Dumond, JB; Forrest, A; Jennings, SH; Kashuba, AD; Kendrick, RL; Malone, S; Patterson, KB; Prince, HM; Sykes, C; Wang, R; White, N, 2013
)
0.39
" The MEMS-defined adherence for correct dosing (-0."( Adherence profiles and therapeutic responses of treatment-naive HIV-infected patients starting boosted atazanavir-based therapy in the ANRS 134-COPHAR 3 trial.
Barrail-Tran, A; Descamps, D; Duval, X; Goujard, C; Mentré, F; Nembot, G; Panhard, X; Parienti, JJ; Taburet, AM; Vigan, M; Vrijens, B, 2013
)
0.39
"HIV seroconversion outcomes in preexposure prophylaxis (PrEP) trials of oral tenofovir (TFV)-containing regimens are highly sensitive to drug concentration, yet less-than-daily dosing regimens are under study."( Single dose pharmacokinetics of oral tenofovir in plasma, peripheral blood mononuclear cells, colonic tissue, and vaginal tissue.
Anderson, JR; Bakshi, R; Cao, YJ; Everts, S; Fuchs, EJ; Hendrix, CW; Liberman, RG; Louissaint, NA; Nimmagadda, S; Skipper, PL; Tannenbaum, SR, 2013
)
0.39
"Possible designs for a PrEP phase 3 efficacy trial are obtained by considering scenarios for potential experimental PrEP and control regimens, including consideration of placebo and active controls, longer acting PrEP and alternate dosing schedules."( Study design considerations for evaluating efficacy of systemic preexposure prophylaxis interventions.
Chen, YQ; Donnell, D; Fleming, TR; Hughes, JP; Wang, L, 2013
)
0.39
"73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg."( Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults.
Berger, D; Bredeek, UF; Callebaut, C; DeJesus, E; Fordyce, MW; Markowitz, M; Ramanathan, S; Rhee, MS; Ruane, PJ; Yale, K; Zhong, L, 2013
)
0.39
" This may translate into greater antiviral efficacy, a higher barrier to resistance, and an improved safety profile relative to TDF, supporting further investigation of TAF dosed once daily in HIV-infected patients."( Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults.
Berger, D; Bredeek, UF; Callebaut, C; DeJesus, E; Fordyce, MW; Markowitz, M; Ramanathan, S; Rhee, MS; Ruane, PJ; Yale, K; Zhong, L, 2013
)
0.39
" However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from BTK inhibition."( Ibrutinib and novel BTK inhibitors in clinical development.
Akinleye, A; Chen, Y; Liu, D; Mukhi, N; Song, Y, 2013
)
0.39
" No clinically relevant interactions between daclatasvir and tenofovir disoproxil fumarate were observed for either drug, and no dosing adjustments were indicated."( Assessment of pharmacokinetic interactions of the HCV NS5A replication complex inhibitor daclatasvir with antiretroviral agents: ritonavir-boosted atazanavir, efavirenz and tenofovir.
Bertz, R; Bifano, M; Grasela, D; Hartstra, J; Hwang, C; Kandoussi, H; Oosterhuis, B; Sevinsky, H; Tiessen, R; Velinova-Donga, M, 2013
)
0.39
"The HIV Prevention Trials Network 057 protocol was a phase 1, open-label study of the pharmacokinetics and safety of tenofovir disoproxil fumarate (TDF) in HIV-infected women during labor and their infants during the first week of life with 4 dosing cohorts: maternal 600 mg doses/no infant dosing; no maternal dosing/infant 4 mg/kg doses on days 0, 3, and 5; maternal 900 mg doses/infant 6 mg/kg doses on days 0, 3, and 5; maternal 600 mg doses/infant 6 mg/kg daily for 7 doses."( Pharmacokinetics and safety of tenofovir in HIV-infected women during labor and their infants during the first week of life.
Emel, L; Eshleman, SH; Fowler, MG; George, K; Herron, C; Hudelson, SE; Joao, E; Kearney, B; Kreitchmann, R; Kumwenda, N; Mirochnick, M; Mofenson, L; Nielsen-Saines, K; Parsons, T; Pinto, J; Richardson, P; Santos, B; Sato, P; Taha, T, 2014
)
0.4
"A TDF dosing regimen of 600 mg during labor and daily infant doses of 6 mg/kg maintains infant tenofovir plasma concentration above 50 ng/mL throughout the first week of life and should be used in the studies of TDF efficacy for HIV prevention of mother-to-child transmission and early infant treatment."( Pharmacokinetics and safety of tenofovir in HIV-infected women during labor and their infants during the first week of life.
Emel, L; Eshleman, SH; Fowler, MG; George, K; Herron, C; Hudelson, SE; Joao, E; Kearney, B; Kreitchmann, R; Kumwenda, N; Mirochnick, M; Mofenson, L; Nielsen-Saines, K; Parsons, T; Pinto, J; Richardson, P; Santos, B; Sato, P; Taha, T, 2014
)
0.4
" Knowledge of concentrations of Tenofovir and its active form Tenofovir diphosphate, at putative sites of anti-HIV functioning, is central to understanding trial outcomes and design of products and dosage regimens."( Multicompartmental pharmacokinetic model of tenofovir delivery by a vaginal gel.
Gao, Y; Katz, DF, 2013
)
0.39
" Thus contrasts predicted by this model can inform design of gels and dosage regimens in clinical trials, and interpretation of PK data."( Multicompartmental pharmacokinetic model of tenofovir delivery by a vaginal gel.
Gao, Y; Katz, DF, 2013
)
0.39
" As a fixed-dose combination tablet given once daily, EFV/FTC/TDF was the first available STR combining efficacy, tolerability and convenience, with the simplest dosing schedule and smallest numbers of pills of any ART combination therapy."( Single-tablet regimens in HIV: does it really make a difference?
Aldir, I; Horta, A; Serrado, M, 2014
)
0.4
" Intermittently dosed vaginal gels containing the HIV-1 reverse transcriptase inhibitor tenofovir protected pigtailed macaques depending on the timing of viral challenge relative to gel application."( Intravaginal ring eluting tenofovir disoproxil fumarate completely protects macaques from multiple vaginal simian-HIV challenges.
Dinh, CT; Hendry, RM; Herold, BC; Kiser, PF; Martin, A; McNicholl, JM; Mesquita, PM; Nagaraja, U; Rastogi, R; Smith, JM; Srinivasan, P; Teller, RS, 2013
)
0.39
" Once-daily dosing without requirement for a pharmacokinetic booster makes dolutegravir-based therapy an attractive treatment option for HIV-1-infected treatment-naive patients."( Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naive adults with HIV-1 infection (SPRING-2 study): 96 week results from a randomised, double-blind, non-inferiority trial.
Albrecht, H; Almond, S; Baril, JG; Belonosova, E; Brennan, C; Domingo, P; Gatell, JM; Jaeger, H; Min, S; Quiros-Roldan, E; Raffi, F, 2013
)
0.39
" Median MEMS adherence rates were 98% (IQR: 93-100) for daily PrEP regimen, 91% (IQR: 73-97) for fixed intermittent dosing and 45% (IQR: 20-63) for post-coital dosing."( Safety, adherence and acceptability of intermittent tenofovir/emtricitabine as HIV pre-exposure prophylaxis (PrEP) among HIV-uninfected Ugandan volunteers living in HIV-serodiscordant relationships: a randomized, clinical trial.
Bahemuka, U; Bangsberg, DR; Barin, B; Bwanika, AN; Chetty, P; Fast, P; Haberer, JE; Kamali, A; Katende, D; Kibengo, FM; Mark, D; Priddy, FH; Rooney, JF; Ruzagira, E, 2013
)
0.39
"Both daily and intermittent oral PrEP dosing regimens were safe."( Safety, adherence and acceptability of intermittent tenofovir/emtricitabine as HIV pre-exposure prophylaxis (PrEP) among HIV-uninfected Ugandan volunteers living in HIV-serodiscordant relationships: a randomized, clinical trial.
Bahemuka, U; Bangsberg, DR; Barin, B; Bwanika, AN; Chetty, P; Fast, P; Haberer, JE; Kamali, A; Katende, D; Kibengo, FM; Mark, D; Priddy, FH; Rooney, JF; Ruzagira, E, 2013
)
0.39
"The MTD was 700 mg twice weekly when BIIB021 was dosed for 3 weeks out of each 4-week course."( A phase 1, dose-escalation, pharmacokinetic and pharmacodynamic study of BIIB021 administered orally in patients with advanced solid tumors.
Banerji, U; Castro, J; Lamanna, N; Mita, M; O'Brien, S; Saif, MW; Stogard, C; Takimoto, C; Von Hoff, D, 2014
)
0.4
" The 90% confidence interval (CI) of the geometric mean ratio for rilpivirine, emtricitabine, tenofovir exposure was estimated for fed versus fasted dosing and light versus standard meal, with equivalence boundaries of 80 - 125%."( Effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate, an antiretroviral single-tablet regimen for the treatment of HIV infection.
Cheng, A; Custodio, JM; Hepner, M; Kearney, BP; Ling, KH; Ramanathan, S; Yin, X, 2014
)
0.4
"At weeks 12 and 24, all 49 dosed subjects remained suppressed on RPV/FTC/TDF."( Efficacy and safety 48 weeks after switching from efavirenz to rilpivirine using emtricitabine/tenofovir disoproxil fumarate-based single-tablet regimens.
Brinson, C; Cheng, AK; Chuck, SK; Cohen, C; Dejesus, E; Mills, AM; Ramanathan, S; Wang, MH; White, K; Williams, S; Yale, KL,
)
0.13
"The objectives of this analysis were to develop a population pharmacokinetic model (PPK) for tenofovir without using potentially unreliable patient reported dosing records and to retrace patient dosing history using pharmacokinetic simulations conditioned on protocol design constraints to assess patient adherence."( Estimation of tenofovir's population pharmacokinetic parameters without reliable dosing histories and application to tracing dosing history using simulation strategies.
Chaturvedula, A; Fossler, MJ; Hendrix, CW, 2014
)
0.4
" A multiple dosing regimen may significantly increase the body clearance and volume distribution of the peripheral compartment compared to a single dosing regimen."( Population pharmacokinetics of adefovir dipivoxil tablets in healthy Chinese volunteers.
He, Y; Huang, J; Huang, X; Li, L; Li, Y; Lv, Y; Wang, K; Yang, J; Zhang, Y; Zheng, Q, 2014
)
0.4
"NAs are cleared by kidneys and their dosage should be adjusted in patients with creatinine clearance <50 mL/min."( Review article: nucleos(t)ide analogues in patients with chronic hepatitis B virus infection and chronic kidney disease.
Cholongitas, E; Papatheodoridis, G; Pipili, C, 2014
)
0.4
" Geometric-mean-ratios compared levels between each pair of dosing conditions."( Strong relationship between oral dose and tenofovir hair levels in a randomized trial: hair as a potential adherence measure for pre-exposure prophylaxis (PrEP).
Anderson, PL; Bacchetti, P; Buchbinder, SP; Gandhi, M; Goggin, K; Grant, R; Greenblatt, RM; Huang, Y; Jin, C; Liu, AY; Stojanovski, K; Yang, Q, 2014
)
0.4
"This study found a strong linear relationship between frequency of dosing and tenofovir levels in scalp hair."( Strong relationship between oral dose and tenofovir hair levels in a randomized trial: hair as a potential adherence measure for pre-exposure prophylaxis (PrEP).
Anderson, PL; Bacchetti, P; Buchbinder, SP; Gandhi, M; Goggin, K; Grant, R; Greenblatt, RM; Huang, Y; Jin, C; Liu, AY; Stojanovski, K; Yang, Q, 2014
)
0.4
" Antiviral treatments were withdrawn in patients who met all of the following 7 criteria: (i) no clinical and histologic evidence of cirrhosis, (ii) normal liver biochemistry, (iii) negative for both HBV DNA and hepatitis B envelope antigen (HBeAg), (iv) no resistance to antiviral agent, (v) antiviral therapy > 9 months, (vi) maintenance dosage of immunosuppressant for > 3 months, and (vii) no history of acute rejection during recent 6 months."( Successful withdrawal of antiviral treatment in kidney transplant recipients with chronic hepatitis B viral infection.
Cho, JH; Choi, JY; Huh, S; Kang, YJ; Kim, CD; Kim, HK; Kim, JS; Kim, YL; Kwon, O; Lim, JH; Park, GY; Park, SH, 2014
)
0.4
"Despite improvements in access to antiretroviral therapy and the use of simplified dosing regimens, HIV infection is still an important global public health problem."( An overview of antiretroviral pre-exposure prophylaxis of HIV infection.
McGowan, I, 2014
)
0.4
" Adherence support for the before-and-after dosing strategy (BAT 24) was provided at enrolment and at each monthly study visit."( Adherence in the CAPRISA 004 tenofovir gel microbicide trial.
Abdool Karim, Q; Abdool Karim, SS; Baxter, C; Grobler, A; MacQueen, KM; Madlala, BT; Mansoor, LE; Yende-Zuma, N, 2014
)
0.4
" A dosage form containing DPV must be able to deliver the drug to the tissue site of action."( Increased Dapivirine tissue accumulation through vaginal film codelivery of dapivirine and Tenofovir.
Akil, A; Cost, M; Devlin, B; Rohan, LC, 2014
)
0.4
"Pill burden, dosing frequency, and concerns about safety and tolerability are important obstacles to maintaining adequate medication adherence."( Switching from twice-daily raltegravir plus tenofovir disoproxil fumarate/emtricitabine to once-daily elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate in virologically suppressed, HIV-1-infected subjects: 48 weeks data.
Brinson, C; Cao, H; Cheng, A; Crofoot, G; Ebrahimi, R; Garner, W; Kulkarni, R; Mills, A; Ortiz, R; Rashbaum, B; Szwarcberg, J; Towner, W; Ward, D,
)
0.13
"Plasma concentrations of tenofovir consistent with daily dosing were highly predictive of protection from HIV acquisition."( HIV protective efficacy and correlates of tenofovir blood concentrations in a clinical trial of PrEP for HIV prevention.
Baeten, JM; Bangsberg, DR; Brantley, J; Bumpus, NN; Celum, C; Donnell, D; Haberer, JE; Hendrix, C; Mugo, N; Mujugira, A; Ndase, P, 2014
)
0.4
" A control group (n=34) received no drug, a second group (n=6) received oral tenofovir disoproxil fumarate/emtricitabine 3 days before each virus challenge and a third group (n=6) received the same dosing plus another dose 2 h after virus challenge."( Tenofovir diphosphate concentrations and prophylactic effect in a macaque model of rectal simian HIV transmission.
Anderson, PL; Bushman, LR; García-Lerma, JG; Glidden, DV; Heneine, W, 2014
)
0.4
"Patients with HIV on antiretroviral therapy might benefit from regimen simplification to reduce pill burden and dosing frequency."( Simplification to coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus continuation of ritonavir-boosted protease inhibitor with emtricitabine and tenofovir in adults with virologically suppressed HIV (STRATEGY-PI): 48 week results o
Arribas, JR; Di Perri, G; Ebrahimi, R; Gathe, J; Nguyen, T; Pialoux, G; Piontkowsky, D; Reynes, J; Tebas, P; White, K, 2014
)
0.4
" The granule form carries a risk of dosing errors and has a particularly strong, unpleasant taste."( Tenofovir in HIV-infected children. Antiretroviral efficacy, but beware of adverse effects on bone and the kidneys.
, 2014
)
0.4
" Adefovir dipivoxil (ADV) liquid suspension (GS-02-526), as a new form of oral ADV, not only has competent antiviral efficacy, but is also more convenient for patients with swallowing difficulties or patients with impaired renal function requiring dosage adjustment."( Liquid oral suspension adefovir dipivoxil (GS-02-526): an update on treatments for hepatitis B infection.
Chen, EQ; Shi, Y; Tang, H; Wu, DB, 2014
)
0.4
"Atazanavir/ritonavir 200/100 mg dosing provided adequate ATV AUC 0-24 when used with TDF in HIV-infected Thai children weighing between 25 and 50 kg."( Pharmacokinetics of atazanavir/ritonavir among HIV-infected Thai children concomitantly taking tenofovir disoproxil fumarate.
Ananworanich, J; Bunupuradah, T; Keadpudsa, S; Prasitsuebsai, W; Puthanakit, T; Sahakijpicharn, T; Srimuan, A; Techasaensiri, C; Thammajaruk, N, 2014
)
0.4
"In total, 128 patients with a decompensated state and lamivudine-resistant HBV were treated with ADV at a dosage of 10 mg/day for a median of 33 months in this multicenter cohort study."( Rescue therapy with adefovir in decompensated liver cirrhosis patients with lamivudine-resistant hepatitis B virus.
Cho, M; Choi, JY; Han, KH; Hwang, JS; Kim, BI; Kim, DJ; Lee, CK; Lee, HJ; Paik, SW; Suh, DJ; Um, SH; Woo, HY; Yoon, SK, 2014
)
0.4
" We report here the sequential modification of UNC1062 to address DMPK properties and yield a new potent and highly orally bioavailable Mer inhibitor, 11, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow."( UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
Cummings, CT; DeRyckere, D; Earp, HS; Frye, SV; Glaros, TG; Graham, DK; Hunter, D; Janzen, WP; Kireev, D; Lee, M; Liu, J; Minson, KA; Newton, DL; Sather, S; Stashko, MA; Wang, X; Zhang, D; Zhang, W, 2014
)
0.4
"Polymeric films can be used as a stable dosage form for the delivery of antiretroviral combinations as microbicides."( Formulation and characterization of polymeric films containing combinations of antiretrovirals (ARVs) for HIV prevention.
Agashe, H; Akil, A; Devlin, B; Dezzutti, CS; Hillier, SL; Moncla, BJ; Rohan, LC; Shi, Y; Uranker, K, 2015
)
0.42
" Significant improvement in survival was observed after treatment with BCX4430 at 4 mg/kg of body weight per day dosed intraperitoneally (i."( BCX4430, a novel nucleoside analog, effectively treats yellow fever in a Hamster model.
Babu, YS; Bantia, S; Julander, JG; Kotian, P; Minning, DM; Morrey, JD; Sheridan, WP; Smee, DF; Taubenheim, BR, 2014
)
0.4
"Electrospun fibers containing antiretroviral drugs have recently been investigated as a new dosage form for topical microbicides against HIV-1."( Manufacturing scale-up of electrospun poly(vinyl alcohol) fibers containing tenofovir for vaginal drug delivery.
Krogstad, EA; Woodrow, KA, 2014
)
0.4
"The difference in binding affinity of tenofovir (more than two orders of magnitude in terms of local concentration), a 30x higher dosage of the (R)-tenofovir enantiomer as compared to conformational isomeric or rotameric adefovir, and the constrained mutational space due to gene overlap in HBV may explain the absence of resistance mutations after 6 years of tenofovir monotherapy."( Differential binding of tenofovir and adefovir to reverse transcriptase of hepatitis B virus.
Berkhout, B; van Hemert, FJ; Zaaijer, HL, 2014
)
0.4
" A dosing regimen according to body-weight-band has been established for pediatric use."( Review of tenofovir use in HIV-infected children.
Aurpibul, L; Puthanakit, T, 2015
)
0.42
" Analysis of anti-CD20 mediated activation of natural killer cells isolated from patients on continued oral ibrutinib treatment suggested that repeated drug dosing inhibits these cells in vivo."( Ibrutinib interferes with the cell-mediated anti-tumor activities of therapeutic CD20 antibodies: implications for combination therapy.
Beurskens, FJ; Breij, EC; Da Roit, F; Engelberts, PJ; Golay, J; Gritti, G; Introna, M; Parren, PW; Rambaldi, A; Taylor, RP, 2015
)
0.42
" Blood, colonic biopsies and rectal and vaginal mucosal fluids were collected after the single oral TDF, the single topical TFV gel dose, and after 7 days of topical TFV gel dosing for extracellular analysis of TFV and intracellular analysis of the active metabolite tenofovir diphosphate (TFVdp) in peripheral blood mononuclear cells (PBMCs) and isolated mucosal mononuclear cells (MMC), including CD4+ and CD4- cell subsets."( A multi-compartment single and multiple dose pharmacokinetic comparison of rectally applied tenofovir 1% gel and oral tenofovir disoproxil fumarate.
Anton, PA; Bumpus, N; Cranston, R; Elliott, J; Hendrix, C; Kashuba, AD; Mauck, C; McGowan, I; Richardson-Harman, N; Tanner, K; Yang, KH, 2014
)
0.4
" As these anti-HIV lipid nanoparticles also prolonged plasma drug exposure, they hold promise as a long-acting dosage form for HIV patients in addressing residual virus in cells and tissue."( Anti-HIV drug-combination nanoparticles enhance plasma drug exposure duration as well as triple-drug combination levels in cells within lymph nodes and blood in primates.
Freeling, JP; Ho, RJ; Koehn, J; Shu, C; Sun, J, 2015
)
0.42
" In a recently published phase 3 trial (RESONATE) that compared ibrutinib and ofatumumab for the treatment of relapsed and refractory chronic lymphocytic leukemia or small lymphocytic lymphoma, ibrutinib at the daily dosage of 420 mg demonstrated a significantly higher overall response rate (43% in ibrutinib vs."( A review of a novel, Bruton's tyrosine kinase inhibitor, ibrutinib.
Kim, SS; Lee, CS; Rattu, MA, 2016
)
0.43
" These results provide a framework for future early investigations of antiretroviral efficacy in HIV prevention to optimize dosing strategies in clinical investigations."( Models for predicting effective HIV chemoprevention in women.
Cohen, MS; Emerson, CW; Fedoriw, Y; Geller, EJ; Kashuba, AD; Nelson, JA; Nicol, MR; Patterson, KB; Prince, HM; Sykes, C, 2015
)
0.42
"This case indicates that Fanconi's syndrome with osteomalacia can be acquired by a chronic hepatitis B patient taking ADV at a conventional dosage of 10 mg/day."( Osteomalacia and Fanconi's syndrome caused by long-term low-dose adefovir dipivoxil.
Chen, YS; Sun, FR; Wang, BF; Wang, BY; Wang, Y; Zhang, D, 2015
)
0.42
"Ibrutinib administered in fasted condition reduces exposure to approximately 60 % as compared with dosing in proximity to food-intake, regardless of timing/type of meal."( The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia.
Byrd, JC; Chauhan, V; de Jong, J; Hellemans, P; James, D; Jiao, J; Loury, DJ; Mannaert, E; Murphy, J; O'Brien, S; Skee, D; Sukbuntherng, J, 2015
)
0.42
" For each drug, its loaded concentration, gel properties and applied volume, and frequency of dosing can be designed to optimize PK and, thence, PD."( Vaginal deployment and tenofovir delivery by microbicide gels.
Chuchuen, O; Gao, Y; Ham, A; Katz, DF; Yang, KH; Yuan, A, 2015
)
0.42
" Adherence to the dosing regimen has emerged as a critical factor determining efficacy outcomes of clinical trials."( Pharmacokinetics of long-acting tenofovir alafenamide (GS-7340) subdermal implant for HIV prophylaxis.
Baum, MM; Beliveau, M; Fanter, R; Gunawardana, M; Hendrix, CW; Marzinke, MA; Miller, CS; Moss, JA; Remedios-Chan, M; Smith, TJ; Yang, F, 2015
)
0.42
" In a preclinical model of renal cell cancer, systemic administration of DSR-6434 dosed once weekly resulted in a significant anti-tumor response."( TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice.
Dovedi, SJ; Harada, H; Hirose, Y; Jewsbury, PJ; Koga-Yamakawa, E; Li, CJ; Murata, M; Ota, Y; Robinson, DT; Sugaru, E; Umehara, H; Wilkinson, RW; Yamamoto, S, 2015
)
0.42
"The CAPRISA 004 trial showed that coitally dosed tenofovir 1% gel reduced HIV acquisition by 39% overall and 54% when used consistently."( Genital Tenofovir Concentrations Correlate With Protection Against HIV Infection in the CAPRISA 004 Trial: Importance of Adherence for Microbicide Effectiveness.
Abdool Karim, SS; Gengiah, TN; Karim, QA; Kashuba, AD; Werner, L; White, NR; Yang, KH, 2015
)
0.42
" Finally, the in vivo mice bearing a SiHa xenograft, LicA dosed at 10 or 20 mg/kg significantly inhibited tumor growth."( Licochalcone A induces autophagy through PI3K/Akt/mTOR inactivation and autophagy suppression enhances Licochalcone A-induced apoptosis of human cervical cancer cells.
Hsieh, YH; Hsueh, JT; Lee, CH; Lin, CL; Tsai, JP; Ying, TH, 2015
)
0.42
" Both CQ and 3-MA were synergistic with VCR to inhibit the growth of retinoblastoma cells and the combinational use significantly reduced the dosage of each drug."( Low concentrations of chloroquine and 3-methyladenine suppress the viability of retinoblastoma cells synergistically with vincristine independent of autophagy inhibition.
Chen, X; Chen, YH; Jiang, PF; Li, LJ; Li, W; Shen, HQ; Zheng, XY, 2015
)
0.68
" Cohort 1 (n = 3) consisted of two phases, a single-dose (140 and 280 mg) phase and a multiple-dose (420 mg) phase of ibrutinib; cohort 2 (n = 6) included multiple doses of ibrutinib 560 mg; and cohort 3 (n = 6) included only patients with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) dosed at ibrutinib 420 mg."( Safety and tolerability of ibrutinib monotherapy in Japanese patients with relapsed/refractory B cell malignancies.
Aoki, T; Ishizawa, K; Morishita, T; Munakata, W; Ogura, M; Suzuki, T; Takahara, S; Tobinai, K; Uchida, T; Ushijima, Y, 2016
)
0.43
" Target engagement was confirmed in humans following single intranasal doses of 32 of ≥20 ng, and reproducible pharmacological response was demonstrated following repeat intranasal dosing at weekly intervals."( Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma.
Ahmed, M; Ball, DI; Biggadike, K; Coe, DM; Dalmas Wilk, DA; Edwards, CD; Gibbon, BH; Hardy, CJ; Hermitage, SA; Hessey, JO; Hillegas, AE; Hughes, SC; Lazarides, L; Lewell, XQ; Lucas, A; Mallett, DN; Price, MA; Priest, FM; Quint, DJ; Shah, P; Sitaram, A; Smith, SA; Stocker, R; Trivedi, NA; Tsitoura, DC; Weller, V, 2016
)
0.43
"Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of NAs, and combination therapy of NA and MRP inhibitors could reduce the dosage for long-term NA use."( Multidrug resistance protein 4 is a critical protein associated with the antiviral efficacy of nucleos(t)ide analogues.
Chen, Q; Liu, W; Liu, Y; Lu, M; Song, H; Wang, B; Xu, C; Xu, D; Yang, D; Zhang, W; Zheng, X, 2016
)
0.43
" Chronic dosing may exacerbate the emergence of drug resistance, with resistant mutations already observed in ibrutinib-treated patients."( Investigational Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis.
Norman, P, 2016
)
0.43
" Monitoring of renal function showed no case of the Fanconi syndrome, no significant alterations of median serum creatinine, eGFR and phosphate levels, although a reduction of TDF dosage was required in five patients (8."( Long-term efficacy and safety of switching from lamivudine+adefovir to tenofovir disoproxil fumarate in virologically suppressed patients.
Angarano, G; Fasano, M; Fiore, JR; Leone, A; Maggi, P; Santantonio, TA; Volpe, A, 2017
)
0.46
" When dosed once-daily, TAF results in approximately 90% lower levels of plasma TFV and a 4-fold increase in intracellular TFV-diphosphate (TFV-DP) in PBMCs compared with the TFV prodrug tenofovir disoproxil fumarate (TDF)."( Viability of primary osteoblasts after treatment with tenofovir alafenamide: Lack of cytotoxicity at clinically relevant drug concentrations.
Babusis, D; Callebaut, C; Kitrinos, K; Liu, Y; Miller, M; Ray, A, 2017
)
0.46
"After tenofovir alafenamide dosing in vivo , tenofovir-dp was unquantifiable in most tissues (91%) although cervical and vaginal epithelial cells efficiently formed tenofovir-dp from tenofovir alafenamide in vitro ."( Single-dose pharmacokinetics of tenofovir alafenamide and its active metabolite in the mucosal tissues.
Cottrell, ML; Emerson, CW; Garrett, KL; Gay, C; Kashuba, ADM; McCallister, S; Peery, A; Prince, HMA; Rooney, JF; Schauer, A; Sykes, C, 2017
)
0.46
" After a genetic diagnosis, febuxostat treatment was started on postoperative day 7, with the dosage gradually increased to 80 mg/day until complete the disappearance of 2,8-DHA crystals."( Febuxostat for the Prevention of Recurrent 2,8-dihydroxyadenine Nephropathy due to Adenine Phosphoribosyltransferase Deficiency Following Kidney Transplantation.
Kimura, T; Kurosawa, A; Nanmoku, K; Shimizu, T; Shinzato, T; Yagisawa, T, 2017
)
0.7
" Indeed, achieving the desired therapeutic outcome in the absence of an effective means of targeted delivery must rely on dosage escalation, which frequently causes severe toxicity."( Overcoming the Hydrolytic Lability of a Reaction Intermediate in Production of Protein/Drug Conjugates: Conjugation of an Acyclic Nucleoside Phosphonate to a Model Carrier Protein.
Kaltashov, IA; Xu, S, 2017
)
0.46
" When CCP dosage reached 200mg/kg/day, the area of renal pathological damage was decreased by 59."( Renoprotective effect of Chinese chive polysaccharides in adenine-induced chronic renal failure.
Chena, HR; Li, QM; Lu, CQ; Luo, JP; Pan, LH; Zha, XQ, 2018
)
0.73
" We conducted a prospective, randomized, crossover pharmacokinetic study of TFV-DP in DBS during 33%, 67%, or 100% of daily dosing under directly observed therapy (DOT)."( Intracellular Tenofovir-Diphosphate and Emtricitabine-Triphosphate in Dried Blood Spots following Directly Observed Therapy.
Anderson, PL; Buchbinder, S; Bushman, LR; Campbell, K; Castillo-Mancilla, JR; Gardner, EM; Ibrahim, M; Kiser, JJ; Liu, AY; MaWhinney, S; McHugh, C; Morrow, M; Seifert, SM; Wagner, T, 2018
)
0.48
" Secondary outcomes included DBS TFV-DP concentrations of >1246 fmol/punch (ie, near-perfect adherence) and plasma FTC >350 ng/mL (consistent with dosing within the past 24 hours)."( Randomized Controlled Trial of Daily Text Messages to Support Adherence to Preexposure Prophylaxis in Individuals at Risk for Human Immunodeficiency Virus: The TAPIR Study.
Anderson, P; Best, BM; Blumenthal, J; Collins, D; Corado, K; Daar, ES; Dubé, MP; Ellorin, E; Haubrich, R; Jain, S; Milam, J; Moore, DJ; Morris, SR; Sun, X; Young, J, 2018
)
0.48
" At week 12, iTAB was superior to SoC for dosing in past 24 hours by plasma FTC (47."( Randomized Controlled Trial of Daily Text Messages to Support Adherence to Preexposure Prophylaxis in Individuals at Risk for Human Immunodeficiency Virus: The TAPIR Study.
Anderson, P; Best, BM; Blumenthal, J; Collins, D; Corado, K; Daar, ES; Dubé, MP; Ellorin, E; Haubrich, R; Jain, S; Milam, J; Moore, DJ; Morris, SR; Sun, X; Young, J, 2018
)
0.48
" Patients with rapidly progressing disease received an accelerated dosing schedule (to 400 mg per day by week 3)."( Venetoclax for chronic lymphocytic leukaemia progressing after ibrutinib: an interim analysis of a multicentre, open-label, phase 2 trial.
Barr, PM; Byrd, JC; Cheson, BD; Choi, M; Chyla, B; Coutre, S; Davids, MS; Furman, RR; Humerickhouse, RA; Jones, JA; Lamanna, N; Mato, AR; Potluri, J; Salem, AH; Verdugo, M; Wierda, WG; Woyach, J; Zhou, L, 2018
)
0.48
" Effective rabies antivirals for therapeutic use need to be molecules that can be dosed into the cerebrospinal fluid and that rapidly and potently block ongoing virus replication and as such stop the further spread of the virus."( The path towards effective antivirals against rabies.
Jochmans, D; Neyts, J, 2019
)
0.51
" Areas covered: The favourable pharmacological profile of TAF allows a marked reduction in dosage (25 mg/day) thus reducing systemic exposure to tenofovir and improving the bone and renal safety, keeping however the same virological efficacy, compared to TDF 300 mg/day."( Tenofovir alafenamide (TAF) treatment of HBV, what are the unanswered questions?
Grossi, G; Lampertico, P; Loglio, A; Viganò, M, 2018
)
0.48
" These results have demonstrated that oral dosing with adenine at 50 mg/kg for 28 days is suitable to induce a stable anemia associated with CKD in mice."( A novel approach to adenine-induced chronic kidney disease associated anemia in rodents.
Hitomi, H; Kitada, K; Nakano, D; Nishiyama, A; Rahman, A; Sufiun, A; Yamazaki, D, 2018
)
1.05
" There was no inducibility difference after chronic dosing with washout."( Increased Susceptibility for Atrial and Ventricular Cardiac Arrhythmias in Mice Treated With a Single High Dose of Ibrutinib.
Jones, DL; Tuomi, JM; Xenocostas, A, 2018
)
0.48
" The additive and synergistic inhibition of this combination additionally supports a therapeutic strategy involving lower dosing of each drug to reduce potential side effects."( Additive and synergistic inhibition of mantle cell lymphoma cell growth by combining olaparib with ibrutinib.
Curtis, A; Rajan, S; Rueter, J; Shopland, L; Zhang, R, 2018
)
0.48
" This model represents a methodical alternative to long-term dietary dosing of adenine."( Short-term oral gavage administration of adenine induces a model of fibrotic kidney disease in rats.
Donnelly-Roberts, DL; Doyle, KJ; Gopalakrishnan, MM; McGaraughty, S; Namovic, MT; Nikkel, AL; Olsen, L; Salte, K; Su, Z; Widomski, D; Zhu, CZ,
)
0.62
" To study a possible direct effect of metformin on the development of vascular calcification, independent of its effect on renal function, metformin (200 mg/kg/day) or vehicle was dosed for ten weeks to rats with warfarin-induced vascular calcification."( Metformin prevents the development of severe chronic kidney disease and its associated mineral and bone disorder.
Brand, K; D'Haese, PC; De Broe, ME; De Maré, A; Gottwald-Hostalek, U; Kamel, S; Lalau, JD; Neven, E; Opdebeeck, B; Verhulst, A; Vervaet, B, 2018
)
0.48
" phase I/II trials have been conducted to evaluate the dosing schedules and activity of this agent."( BIIB021, an Hsp90 inhibitor: A promising therapeutic strategy for blood malignancies (Review).
He, W; Hu, H, 2018
)
0.48
"MTN-014 was a phase 1, cross-over, randomized sequence trial comparing the cross-compartment pharmacokinetics and pharmacodynamics of daily TFV reduced-glycerin 1% gel after 14 days each of rectal and vaginal application, with directly observed dosing and a 6-week washout period between phases."( Pharmacokinetics and Pharmacodynamics of Tenofovir Reduced-Glycerin 1% Gel in the Rectal and Vaginal Compartments in Women: A Cross-Compartmental Study With Directly Observed Dosing.
Balar, B; Dai, JY; Dezzutti, CS; Galaska, B; Hendrix, CW; Justman, JE; Kunjara Na Ayudhya, RP; Levy, L; Marzinke, MA; McGowan, I; Mushamiri, I; Nair, GL; Pan, Z; Piper, JM; Schwartz, JL, 2018
)
0.48
" TFV and TFV diphosphate (TFV-DP) were detected in most samples collected from the dosing compartment."( Pharmacokinetics and Pharmacodynamics of Tenofovir Reduced-Glycerin 1% Gel in the Rectal and Vaginal Compartments in Women: A Cross-Compartmental Study With Directly Observed Dosing.
Balar, B; Dai, JY; Dezzutti, CS; Galaska, B; Hendrix, CW; Justman, JE; Kunjara Na Ayudhya, RP; Levy, L; Marzinke, MA; McGowan, I; Mushamiri, I; Nair, GL; Pan, Z; Piper, JM; Schwartz, JL, 2018
)
0.48
" Although high TFV concentrations in the dosing compartment may be protective, low cross-compartment tissue concentrations are not likely to be protective."( Pharmacokinetics and Pharmacodynamics of Tenofovir Reduced-Glycerin 1% Gel in the Rectal and Vaginal Compartments in Women: A Cross-Compartmental Study With Directly Observed Dosing.
Balar, B; Dai, JY; Dezzutti, CS; Galaska, B; Hendrix, CW; Justman, JE; Kunjara Na Ayudhya, RP; Levy, L; Marzinke, MA; McGowan, I; Mushamiri, I; Nair, GL; Pan, Z; Piper, JM; Schwartz, JL, 2018
)
0.48
" Using a murine model, we compared the plasma and tissue pharmacokinetics of TFV and various TFV prodrugs, including tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), and hexadecyloxypropyl tenofovir (CMX157), after dosing as enema formulations with varying osmolality and ion content."( Development of rectal enema as microbicide (DREAM): Preclinical progressive selection of a tenofovir prodrug enema.
Bensouda, S; Cone, RA; Date, AA; Ensign, LM; Fuchs, EJ; Gumber, S; Hanes, J; Hendrix, C; Hoang, T; Marzinke, M; Ortiz, JO; Rohan, L; Villinger, F; Xiao, P; Young, TW, 2019
)
0.51
"This was an open-label, multicenter, phase-1 study to evaluate the drug interaction between steady-state ibrutinib and moderate (erythromycin) and strong (voriconazole) CYP3A inhibitors in patients with B-cell malignancies and to confirm dosing recommendations."( A drug-drug interaction study of ibrutinib with moderate/strong CYP3A inhibitors in patients with B-cell malignancies.
Chauhan, V; Córdoba, R; de Jong, J; De Wilde, S; de Zwart, L; Hellemans, P; Jiao, J; Manikhas, G; Masterson, T; Myasnikov, A; Osmanov, D; Ouellet, D; Panizo, C; Patricia, D; Snoeys, J; Sukbuntherng, J, 2018
)
0.48
"The goal of this work was to evaluate dosing strategies for tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), and emtricitabine (FTC) for pre-exposure prophylaxis (PrEP) with injection drug use with a pharmacokinetic/pharmacodynamics analysis of concentration data generated from two single-dose clinical studies conducted in healthy women."( A Pharmacokinetic/Pharmacodynamic Model to Predict Effective HIV Prophylaxis Dosing Strategies for People Who Inject Drugs.
Chen, J; Cottrell, ML; Dumond, JB; Garrett, KL; Maas, BM; Prince, HA; Schauer, AP; Sykes, C; White, N, 2018
)
0.48
" These findings suggest deterioration of the humoral immune system is associated with progressive CLL and altering the dosing of IgRT to achieve higher than conventional IgG target levels may have therapeutic activity."( Association of blood IgG with tumor necrosis factor-alpha and clinical course of chronic lymphocytic leukemia.
Huang, J; Lazarus, A; Norris, P; Shi, Y; Spaner, DE; Venema, R; Wang, G, 2018
)
0.48
" To test this postulate, a pilot study (NCT02801578) was designed to systematically reduce ibrutinib dosing within the same patient with CLL over the course of three 28-day cycles."( A pilot study of lower doses of ibrutinib in patients with chronic lymphocytic leukemia.
Bose, P; Chen, LS; Cruz, ND; Feng, S; Gandhi, V; Huang, X; Jain, N; Jiang, Y; Keating, MJ; Kroll, MH; Qiao, W; Thompson, PA; Wierda, WG; Wu, Q, 2018
)
0.48
" IM SMC concentrations were low relative to PBMC, as were EN concentrations, suggesting differences in cell phenotype and lineage in the MGT; these differences in phenotype and pharmacology may have an impact on selecting and dosing ARVs used in cure strategies."( Differential extracellular, but similar intracellular, disposition of two tenofovir formulations in the male genital tract.
Blake, KH; Chen, J; Cohen, MS; Dumond, JB; Gay, CL; Greene, SA; Kashuba, ADM; Maas, BM; Nelson, JAE; Prince, HMA; Schauer, AP; Sykes, C, 2019
)
0.51
"As oral targeted agents, such as ibrutinib, become more widely used, understanding the impact of suboptimal dosing on overall survival (OS) and progression-free survival (PFS) outside of clinical trials is imperative."( Ibrutinib Dose Adherence and Therapeutic Efficacy in Non-Hodgkin Lymphoma: A Single-Center Experience.
Baloga, E; Baran, AM; Barr, PM; Casulo, C; Friedberg, JW; Helber, M; Moore, J; Reagan, P; Williams, AM; Zent, CS, 2019
)
0.51
" Lack of adherence and insufficient dosing contributed to stone recurrence and AKI during pharmacotherapy."( Long-term renal outcomes of APRT deficiency presenting in childhood.
Agustsdottir, IM; Edvardsson, VO; Indridason, OS; Palsson, R; Runolfsdottir, HL, 2019
)
0.51
" At baseline (pre-switch) and at 12 weeks post-switch, we measured HIV-1 RNA in seminal plasma (SP) and blood plasma (BP), tenofovir (TFV) in SP and BP, and TFV-diphosphate (dp) in peripheral blood mononuclear cells (PBMCs) and seminal mononuclear cells (SMCs) at the end of the dosing interval (C24h)."( Seminal Tenofovir Concentrations, Viral Suppression, and Semen Quality With Tenofovir Alafenamide, Compared With Tenofovir Disoproxil Fumarate (Spanish HIV/AIDS Research Network, PreEC/RIS 40).
Cottrell, ML; Garcia, B; Imaz, A; Kashuba, ADM; Morenilla, S; Niubó, J; Perez, E; Podzamczer, D; Tiraboschi, JM, 2019
)
0.51
" Additionally, debate exists regarding the recommended dosing strategy for ibrutinib for this indication with disease remission demonstrated at 560 mg and 420 mg."( Ibrutinib for the treatment of Bing-Neel syndrome, a complication of Waldenström macroglobulinemia: Patient case report.
Arnall, JR; Hartsell, L; Janes, A; Larck, C; Park, S, 2019
)
0.51
"HPTN 067 assessed the feasibility of daily and non-daily dosing of open-label emtricitabine/tenofovir disoproxil fumarate (FTC/TDF)-based pre-exposure prophylaxis (PrEP)."( Factors Associated With Sex-Related Pre-exposure Prophylaxis Adherence Among Men Who Have Sex With Men in New York City in HPTN 067.
Amico, KR; Franks, J; Grant, RM; Hirsch-Moverman, Y; Hughes, JP; Li, M; Loquere, A; Mannheimer, S, 2019
)
0.51
"Factors associated with sex-related PrEP adherence were assessed among men who have sex with men (MSM) randomized to one of 3 PrEP dosing arms in HPTN 067 in New York City."( Factors Associated With Sex-Related Pre-exposure Prophylaxis Adherence Among Men Who Have Sex With Men in New York City in HPTN 067.
Amico, KR; Franks, J; Grant, RM; Hirsch-Moverman, Y; Hughes, JP; Li, M; Loquere, A; Mannheimer, S, 2019
)
0.51
" In the multivariable analyses, higher sex-related PrEP adherence was significantly associated with daily dosing arm, older age, employment, and higher PrEP adherence behavioral skills."( Factors Associated With Sex-Related Pre-exposure Prophylaxis Adherence Among Men Who Have Sex With Men in New York City in HPTN 067.
Amico, KR; Franks, J; Grant, RM; Hirsch-Moverman, Y; Hughes, JP; Li, M; Loquere, A; Mannheimer, S, 2019
)
0.51
"High urine FTC and TFV concentrations could provide an indication of adherence to daily oral dosing with TDF or TAF-based regimens used for treatment and prevention."( Brief Report: Urine Emtricitabine and Tenofovir Concentrations Provide Markers of Recent Antiretroviral Drug Exposure Among HIV-Negative Men Who Have Sex With Men.
Conway-Washington, C; Dinh, C; Fountain, J; Haaland, RE; Hall, L; Holder, A; Kelley, CF; Livermont, T; Lupo, LD; Martin, A, 2019
)
0.51
" Submaximal ibrutinib dosing will have to be further systematically evaluated."( Descriptive analysis of dosing and outcomes for patients with ibrutinib-treated relapsed or refractory chronic lymphocytic leukemia in a Canadian centre.
Banerji, V; Brown, K; Bucher, O; Dawe, DE; Dhaliwal, DH; Geirnaert, M; Hibbert, I; Johnston, JB; Uminski, K, 2019
)
0.51
" With the assistance of therapeutic drug monitoring, dolutegravir dosing was increased to 150 mg daily."( Successful use of once-daily high-dose darunavir and dolutegravir in multidrug-resistant HIV.
Fulco, PP; Gomes, D; Leibrand Kaczmar, CR; Smith, T, 2020
)
0.56
" It has been proven that HIV infection can be prevented by daily dosing of emtricitabine and tenofovir disoproxil fumarate."( Direct quantitation of tenofovir diphosphate in human blood with mass spectrometry for adherence monitoring.
Anderson, PL; Bushman, LR; Cooks, RG; Ouyang, Z; Pandey, S; Pu, F, 2020
)
0.56
" A link between the dosing compartment and the dihydrodiol-ibrutinib central compartment was added to assess for high first-pass hepatic metabolism."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" Recent dosing measures include antiretroviral levels in plasma or urine, as well as emtricitabine-triphosphate in dried blood spots (DBS) for those on tenofovir-emtricitabine-based therapy."( Approaches to Objectively Measure Antiretroviral Medication Adherence and Drive Adherence Interventions.
Anderson, PL; Castillo-Mancilla, J; Chai, PR; Gandhi, M; Haberer, JE; Spinelli, MA, 2020
)
0.56
"\ Conclusions: The patients were generally satisfied with the change in medication and well nformed about the dosage and advantages of TAF over TDF, but less well informed about the possible adverse effects of TAF."( Satisfaction and knowledge among patients with HIV after switching from tenofovir to tenofovir alafenamide in regimens containing emtricitabine and rilpivirine
Bermejo-Vicedo, T; Gramage-Caro, T; Montero-Llorente, B; Rodríguez-Sagrado, MÁ; Vélez-Díaz-Pallarés, M, 2020
)
0.56
"Fanconi syndrome with osteomalacia can develop in patients with chronic hepatitis B infection being treated with adefovir at a conventional low dosage of 10 mg/day."( Osteomalacia and renal failure due to Fanconi syndrome caused by long-term low-dose Adefovir Dipivoxil: a case report.
Cen, X; Cui, Y; Liu, Z; Mu, G; Xiang, Q; Xie, Q; Yu, Y; Zhang, H; Zhang, J, 2020
)
0.56
"TAF-DBS was a randomized, crossover clinical study of TFV-DP in DBS, following directly observed dosing of 33%, 67%, or 100% of daily TAF (25 mg)/FTC (200 mg)."( Intracellular Tenofovir-Diphosphate and Emtricitabine-Triphosphate in Dried Blood Spots Following Tenofovir Alafenamide: The TAF-DBS Study.
Anderson, PL; Brooks, KM; Bushman, LR; Castillo-Mancilla, J; Ibrahim, ME; Kiser, JJ; MaWhinney, S; McCallister, S; McHugh, C; Morrow, M; Yager, J, 2020
)
0.56
" Together, these moieties provide complementary measures of cumulative adherence and recent dosing for TAF/FTC."( Intracellular Tenofovir-Diphosphate and Emtricitabine-Triphosphate in Dried Blood Spots Following Tenofovir Alafenamide: The TAF-DBS Study.
Anderson, PL; Brooks, KM; Bushman, LR; Castillo-Mancilla, J; Ibrahim, ME; Kiser, JJ; MaWhinney, S; McCallister, S; McHugh, C; Morrow, M; Yager, J, 2020
)
0.56
"TGM and TGW on at least 6 months of stable sex hormone therapy containing testosterone or estradiol (respectively) were enrolled in a 4-week study of directly observed dosing of daily oral coformulated emtricitabine and tenofovir disoproxil fumarate (FTC/TDF)."( Sex Hormone Therapy and Tenofovir Diphosphate Concentration in Dried Blood Spots: Primary Results of the Interactions Between Antiretrovirals And Transgender Hormones Study.
Anderson, PL; Bhasin, S; Defechereux, PA; Deutsch, MB; Glidden, DV; Grant, RM; O'Neal, J; Pellegrini, M; Sevelius, J; Yager, J; Yu, M, 2021
)
0.62
" Ibrutinib is currently not available in a liquid oral dosage form."( Ibrutinib treatment via alternative administration in a patient with chronic lymphocytic leukemia and dysphagia.
Arnall, JR; DiSogra, KY; Janes, A; Moore, DC; Park, SI; Tran, T, 2021
)
0.62
" Potentially, lower IFN-α and IP-10 levels as well as once-weekly intranasal dosing vs daily subcutaneous or intramuscular dosing with recombinant type I IFNs could explain the lack of pregnancy effects; however, there was an undesired impact on offspring immune function."( GSK2245035, a TLR7 agonist, Does Not Increase Pregnancy Loss in Cynomolgus Monkeys.
Baker, A; Bray, M; Hillegas, AE; Maier, CC; Phadnis-Moghe, AS; Posobiec, LM; Price, MA; Stanislaus, DJ, 2021
)
0.62
" Here, CKD was developed by an oral dosage of adenine (AD) in the mice model."( Morin hydrate attenuates adenine-induced renal fibrosis via targeting cathepsin D signaling.
Kang, SC; Sharma, C; Singh, MP, 2021
)
1.18
"In this study, a green stability indicating chromatographic methods were developed and validated for the quantitative determination of tenofovir alafenamide in the presence of its degradation products in bulk powder as well as in dosage forms."( Assessment of the greenness of new stability indicating micellar UPLC and HPTLC methods for determination of tenofovir alafenamide in dosage forms.
Abdel-Razeq, SA; Nasr, ZA; Said, NS, 2021
)
0.62
"The model can be used to simulate clinical trials or various dosing scenarios."( Population Pharmacokinetics of Ibrutinib in Healthy Adults.
Al-Ghazawi, M; Najib, N; Najib, O; Saleh, MI; Salem, I, 2021
)
0.62
" TAF was well tolerated and only 4 patients discontinued therapy due to adverse event during a median duration of TAF dosing of 74 weeks."( Safety and Effectiveness of Tenofovir Alafenamide in Usual Clinical Practice Confirms Results of Clinical Trials: TARGET-HBV.
Bernstein, DE; Fried, MW; Lok, AS; Mospan, AR; Schiff, ER; Smith, CI; Trinh, HN; Zink, RC, 2022
)
0.72
" We sought to identify the optimal dosing combination, based on efficacy and toxicity, utilizing a continual reassessment method of 6 combinations of IBR (280 mg, 420 mg, and 560 mg by mouth daily) and VEN (max dose of 200 mg and 400 mg by mouth daily)."( Dose-finding study of ibrutinib and venetoclax in relapsed or refractory mantle cell lymphoma.
Budde, LE; Chen, RW; Cohen, JB; Kahl, BS; Petroni, GR; Portell, CA; Varhegyi, NE; Wages, NA; Williams, ME, 2022
)
0.72
" Ruxolitinib dosing was based on a previous phase I trial."( Janus kinases restrain chronic lymphocytic leukemia cells in patients on ibrutinib: Results of a phase II trial.
Gallagher, J; Luo, Y; Shi, Y; Spaner, DE; Tsui, H; Wang, G, 2021
)
0.62
" Study 1 evaluated the safety and tolerability of IM galidesivir over single day dosing, single day dosing ± lidocaine, and 7-day dosing with lidocaine."( Pharmacokinetics and Safety of the Nucleoside Analog Antiviral Drug Galidesivir Administered to Healthy Adult Subjects.
Collins, D; Dobo, S; Mathis, A; Sheridan, WP; Taylor, R; Walling, DM, 2022
)
0.72
" Chronic adenine dosing resulted in severe CKD in vehicle-treated rats as indicated by a marked rise in serum creatinine levels, a marked decrease in creatinine clearance, and a disturbed mineral metabolism."( Progression of established non-diabetic chronic kidney disease is halted by metformin treatment in rats.
Corremans, R; D'Haese, PC; De Broe, ME; Leysen, H; Maudsley, S; Neven, E; Verhulst, A; Vervaet, BA, 2022
)
1.14
" Ibrutinib dosing was held (≥7 days) for 79 patients and reduced for 31 patients because of AEs; these AEs resolved or improved in 85% (67 of 79) and 90% (28 of 31) of patients, respectively."( Up to 8-year follow-up from RESONATE-2: first-line ibrutinib treatment for patients with chronic lymphocytic leukemia.
Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dearden, C; Ghia, P; Grosicki, S; Hillmen, P; Hsu, E; Kipps, TJ; Li, JY; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Szoke, A; Tedeschi, A; Zhou, C, 2022
)
0.72
" Systemic drug disposition during TAF implant dosing was explained by a multi-compartment pharmacokinetic (PK) model."( Fundamental aspects of long-acting tenofovir alafenamide delivery from subdermal implants for HIV prophylaxis.
Baum, MM; Beliveau, M; Buser, C; Caprioli, RM; Castonguay, AE; Gallay, PA; Gunawardana, M; Hendrix, CW; Kuo, J; Marzinke, MA; Moss, JA; Remedios-Chan, M; Reyzer, ML; Sanchez, D; Trinh, M; Tuck, M; Webster, P; Webster, S, 2022
)
0.72
" The collective results support the utility of AOPPs as a potential target for drug and/or dosage adjustment in CKD patients."( Advanced oxidation protein products upregulate ABCB1 expression and activity via HDAC2-Foxo3α-mediated signaling in vitro and in vivo.
Chen, Y; Feng, H; Lin, Z; Mo, L; Wang, X; Xun, T; Yang, X; Ye, C; Zhang, M; Zhao, J, 2022
)
0.72
" A traditional 3 + 3 dose escalation design with 5 dosing cohorts was used."( Phase I dose escalation study of dual PI3K/mTOR inhibition by Sapanisertib and Serabelisib in combination with paclitaxel in patients with advanced solid tumors.
Meissner, T; Rojas-Espaillat, L; Starks, DC; Williams, CB, 2022
)
0.72
" We observed significant dose-response relationships between number of HIV risk factors and PrEP drug concentrations."( Alignment of PrEP adherence with periods of HIV risk among adolescent girls and young women in South Africa and Zimbabwe: a secondary analysis of the HPTN 082 randomised controlled trial.
Anderson, PL; Bekker, LG; Celum, C; Chirenje, ZM; Delany-Moretlwe, S; Donnell, D; Hosek, S; Marzinke, MA; Mgodi, N; Velloza, J, 2022
)
0.72
" Due to binding interactions between polyvalent cations and bictegravir and the potential impact on antiretroviral efficacy, construction of a daily medication schedule to avoid interactions between the antiretroviral regimen and the supplements while promoting optimal dosing of each supplement was necessary; however there is currently no guidance on twice-daily cation dosing with coadministered bictegravir and limited guidance on multivitamin coadministration in this context."( Achievement of virologic suppression with HIV antiretroviral therapy in a patient also taking multiple daily cation supplement doses: A case report and review of the literature.
Buscemi, L; Mossholder, B, 2023
)
0.91
" Our existing PK model, supported by an intravenous (IV) dosing dog study, was adapted to analyze mechanistic aspects underlying implant TAF delivery."( Preclinical Considerations for Long-acting Delivery of Tenofovir Alafenamide from Subdermal Implants for HIV Pre-exposure Prophylaxis.
Baum, MM; Beliveau, M; Fanter, R; Gallay, PA; Gunawardana, M; Kuo, J; Marzinke, MA; Moss, JA; Ramirez, CM; Remedios-Chan, M; Sanchez, D; Trinh, M; Webster, P; Webster, S, 2023
)
0.91
"Antiretroviral agents with novel mechanisms and dosing intervals could expand treatment options for people with HIV."( Lenacapavir administered every 26 weeks or daily in combination with oral daily antiretroviral therapy for initial treatment of HIV: a randomised, open-label, active-controlled, phase 2 trial.
Baeten, JM; Benson, P; Berhe, M; Crofoot, G; Dvory-Sobol, H; Gupta, SK; Koenig, E; Liu, SY; McDonald, C; Ramgopal, M; Rhee, MS; Ruane, P; Sanchez, WE; Scribner, A; Sims, J; VanderVeen, LA, 2023
)
0.91
" This semimechanistic model describes the population pharmacokinetics of tenofovir when dosed as either TDF or TAF in an African population living with HIV and can be used as a tool for exposure prediction in patients, and to simulate alternative regimes to inform further clinical trials."( Population pharmacokinetics of tenofovir given as either tenofovir disoproxil fumarate or tenofovir alafenamide in an African population.
Chandiwana, N; Denti, P; Kawuma, AN; Maartens, G; Sinxadi, P; Sokhela, SM; Venter, WDF; Wasmann, RE; Wiesner, L, 2023
)
0.91
" However, considering its rapid uptake into target cells, we suggest only a cautious increase of tenofovir alafenamide dosage intervals to 2 or 3 days only in case of moderate or severe CKD, respectively."( Population pharmacokinetic modelling to characterize the effect of chronic kidney disease on tenofovir exposure after tenofovir alafenamide administration.
Alves Saldanha, S; Andre, P; Buclin, T; Cavassini, M; Courlet, P; Decosterd, LA; Desfontaine, V; Guidi, M; Kusejko, K; Thoueille, P, 2023
)
0.91
"Icariin at the dosage of 100 mg/kg/d and 200 mg/kg/d markedly ameliorated rat renal function in a dose-dependent manner."( Icariin, the main prenylflavonoid of Epimedii Folium, ameliorated chronic kidney disease by modulating energy metabolism via AMPK activation.
Lu, J; Lv, C; Yang, W; Zhang, X; Zhao, Y, 2023
)
0.91
" Although no dosage adjustment is needed for Oral Nirmatrelvir/Ritonavir in patients with mild renal impairment and coronavirus disease 2019, the dosage is reduced to twice daily in those with moderate renal impairment."( Medication safety in chronic kidney disease.
Singh, S, 2023
)
0.91
"Cabotegravir plus rilpivirine is the only approved complete long-acting regimen for the maintenance of HIV-1 virological suppression dosed every 2 months."( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random
Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023
)
0.91
" Participants with HIV-1 RNA less than 50 copies per mL were randomly assigned (2:1), stratified by sex at birth and BMI, to either long-acting cabotegravir (600 mg) plus rilpivirine (900 mg) dosed intramuscularly every 2 months or to continue daily oral bictegravir (50 mg), emtricitabine (200 mg), and tenofovir alafenamide (25 mg)."( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random
Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023
)
0.91
"These data support the use of long-acting cabotegravir plus rilpivirine dosed every 2 months as a complete antiretroviral regimen that has similar efficacy to a commonly used integrase strand transfer inhibitor-based first-line regimen, while addressing unmet psychosocial issues associated with daily oral treatment."( Efficacy, safety, and tolerability of switching to long-acting cabotegravir plus rilpivirine versus continuing fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV, 12-month results (SOLAR): a random
Berni, A; Castagna, A; Cazanave, C; Chounta, V; D'Amico, R; Di Perri, G; Diaz-Brito, V; Dretler, R; Garges, HP; Latham, CL; Oka, S; Osiyemi, O; Pascual Bernáldez, M; Patel, P; Ramgopal, MN; Sims, J; Smith, K; Spreen, WR; Sutherland-Phillips, D; Sutton, K; Van Eygen, V; Van Solingen-Ristea, R; van Wyk, J; Walmsley, S; Zhang, F, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
Daphnia magna metaboliteA Daphnia metabolite produced by the species Daphnia magna.
Saccharomyces cerevisiae metaboliteAny fungal metabolite produced during a metabolic reaction in Baker's yeast (Saccharomyces cerevisiae).
Escherichia coli metaboliteAny bacterial metabolite produced during a metabolic reaction in Escherichia coli.
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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
6-aminopurinesAny compound having 6-aminopurine (adenine) as part of its structure.
purine nucleobaseA nucleobase whose skeleton is derived from purine.
[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 (112)

PathwayProteinsCompounds
Metabolism14961108
Nucleotide metabolism89125
Nucleotide salvage2128
Purine salvage1322
Amino acid and derivative metabolism250260
Methionine salvage pathway616
Sulfur amino acid metabolism2763
DNA Repair25547
Base Excision Repair3523
Base-Excision Repair, AP Site Formation1716
Depurination107
Cleavage of the damaged purine47
Purine Metabolism3766
Adenosine Deaminase Deficiency3766
Adenylosuccinate Lyase Deficiency3766
Gout or Kelley-Seegmiller Syndrome3766
Lesch-Nyhan Syndrome (LNS)3766
Molybdenum Cofactor Deficiency3766
Xanthine Dehydrogenase Deficiency (Xanthinuria)3766
Purine Nucleoside Phosphorylase Deficiency3766
AICA-Ribosiduria3766
Azathioprine Action Pathway4782
Mercaptopurine Action Pathway4780
Thioguanine Action Pathway4781
Xanthinuria Type I3766
Xanthinuria Type II3766
Adenine Phosphoribosyltransferase Deficiency (APRT)3766
Mitochondrial DNA Depletion Syndrome-33766
Myoadenylate Deaminase Deficiency3766
Quorum Sensing1020
S-Adenosyl-L-Methionine Biosynthesis817
PreQ0 Metabolism623
Methylphosphonate Degradation I711
Adenine and Adenosine Salvage I412
Adenine and Adenosine Salvage II411
Adenine and Adenosine Salvage III58
Citrate Lyase Activation311
Purine Ribonucleosides Degradation717
Purine Deoxyribonucleosides Degradation414
S-Adenosyl-L-Methionine Cycle414
Spermidine Biosynthesis and Metabolism39
Methionine Metabolism and Salvage1534
Cytokinins Degradation113
Disease1278231
Diseases of metabolism69121
Mitochondrial DNA Depletion Syndrome3566
S-methyl-5'-thioadenosine degradation II04
adenine salvage09
L-methionine salvage cycle II (plants)829
adenine and adenosine salvage II08
L-methionine salvage cycle I (bacteria and plants)232
purine nucleosides salvage II (plant)419
S-methyl-5'-thioadenosine degradation I214
cytokinins degradation114
purine uptake14
Purine nucleotides and Nucleosides metabolism ( Purine nucleotides and Nucleosides metabolism )10577
Adenosine + Orthophosphate = Adenine + D-Ribose 1-phosphate ( Purine nucleotides and Nucleosides metabolism )13
AMP + Pyrophosphate = Adenine + D-5-Phospho-ribosyl 1-diphosphate ( Purine nucleotides and Nucleosides metabolism )14
Deoxy-adenosine + Orthophosphate = 2-Deoxy-D-ribose 1-phosphate + Adenine ( Purine nucleotides and Nucleosides metabolism )14
Purine metabolism1336
Organic Nitrogen Assimilation436
fluoroacetate and fluorothreonine biosynthesis016
Renz2020 - GEM of Human alveolar macrophage with SARS-CoV-20490
The impact of Nsp14 on metabolism (COVID-19 Disease Map)084
Diseases of nucleotide metabolism35
Nucleotide salvage defects24
Defective APRT disrupts adenine salvage12
T cell modulation in pancreatic cancer459
adenine and adenosine salvage III012
Gravitropism under normal or artificial gravity environments5811
Regulation of lemma joints development and leaf angle by cytokinin111
methionine salvage cycle III1028
purine ribonucleosides degradation to ribose-1-phosphate316
S-methyl-5'-thioadenosine degradation16
1,4-dihydroxy-6-naphthoate biosynthesis II714
fluoroacetate and fluorothreonine biosynthesis422
(aminomethyl)phosphonate degradation1231
superpathway of demethylmenaquinol-6 biosynthesis II619
autoinducer AI-2 biosynthesis I319
autoinducer AI-2 biosynthesis II (Vibrio)213
S-methyl-5'-thioadenosine degradation IV17
S-methyl-5'-thioadenosine degradation I417
S-methyl-5'-thioadenosine degradation II26
cytokinins degradation519
superpathway of microbial D-galacturonate and D-glucuronate degradation3592
adenosine nucleotides degradation III27
adeninyl adenosylcobamide biosynthesis from adenosylcobinamide-GDP310
purine ribonucleosides degradation822
purine deoxyribonucleosides degradation I212
superpathway of purine deoxyribonucleosides degradation637
nucleoside and nucleotide degradation (archaea)722
drosopterin and aurodrosopterin biosynthesis422
malonate decarboxylase activation26
citrate lyase activation412
superpathway of purine nucleotide salvage1334
L-methionine salvage cycle I (bacteria and plants)1938
adenine and adenosine salvage III925
adenine salvage311
L-methionine salvage cycle III1029
adenine and adenosine salvage I07
adenine and adenosine salvage V417
L-methionine salvage cycle II (plants)832
adenine and adenosine salvage II415
L-cysteine biosynthesis VI (from L-methionine)518
glyphosate degradation III718
salinosporamide A biosynthesis1129
queuosine biosynthesis521
guanosine nucleotides degradation III1425
superpathway of menaquinol-8 biosynthesis III722
methylphosphonate degradation I717
methylphosphonate degradation II116
D-galacturonate degradation II426
hopanoid biosynthesis (bacteria)830
S-adenosyl-L-methionine cycle I417
adenine and adenosine salvage IV510
salvage pathways of adenine, hypoxanthine and their nucleosides816
superpathway of purine nucleosides salvage920
methionine salvage pathway513
purine nucleosides salvage II (plant)613
salvage pathways of purine nucleosides021
salvage pathways of adenine, hypoxanthine, and their nucleosides023
purine and pyrimidine metabolism032
salvage pathways of purine nucleosides I027
salvage pathways of purine and pyrimidine nucleotides030
2'-(5'-phosphoribosyl)-3'-dephospho-CoA biosynthesis I (citrate lyase)06
aminomethylphosphonate degradation419
Methionine de novo and salvage pathway148
Biochemical pathways: part I0466
Purine metabolism and related disorders2353
Responses to stimuli: abiotic stimuli and stresses9526
Yang cycle217

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.00890.003245.467312,589.2998AID2517
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.49150.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency32.64270.000811.382244.6684AID686979
AR proteinHomo sapiens (human)Potency14.91060.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743042; AID743054
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency24.25810.001022.650876.6163AID1224838; AID1224893
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency24.54540.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency13.80060.000214.376460.0339AID720692
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency44.38190.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency27.30600.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency28.92730.000229.305416,493.5996AID1259244; AID743075; AID743080; AID743091
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency6.42560.001723.839378.1014AID743083
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.09290.00419.984825.9290AID504444
heat shock protein beta-1Homo sapiens (human)Potency33.48890.042027.378961.6448AID743210; AID743228
importin subunit beta-1 isoform 1Homo sapiens (human)Potency56.23415.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency56.23415.804836.130665.1308AID540253
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency89.12510.129810.833132.6090AID493005
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency56.23415.804816.996225.9290AID540253
lamin isoform A-delta10Homo sapiens (human)Potency2.51190.891312.067628.1838AID1487
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.84930.001557.789015,848.9004AID1259244
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.84930.001551.739315,848.9004AID1259244
TAR DNA-binding protein 43Homo sapiens (human)Potency14.12541.778316.208135.4813AID652104
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency18.83360.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency18.83360.011912.222168.7989AID651632
[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)
Chain A, MTA/SAH nucleosidaseEscherichia coliKi300.0000300.0000300.0000300.0000AID977610
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Cyclin-dependent kinase 1Homo sapiens (human)IC50 (µMol)200.00000.00041.345210.0000AID51554
Heat shock protein HSP 90-betaHomo sapiens (human)IC50 (µMol)4,000.00000.00100.683610.0000AID1799223; AID419781
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC50 (µMol)43.25000.00132.81389.8200AID1799677; AID287937
Protein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)IC50 (µMol)15.00002.40006.40979.0000AID1734010
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)IC50 (µMol)15.80900.00040.39438.3000AID1817494
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)Ki6.71500.00061.13536.7150AID1817495
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ribosome-inactivating protein alpha-trichosanthinTrichosanthes kirilowiiKd260.0000260.0000260.0000260.0000AID977611
Chain A, Ricin A chainRicinus communis (castor bean)Kd700.0000700.0000700.0000700.0000AID977611
Chain A, Ribosome-inactivating protein 3Zea maysKd0.00630.00630.00630.0063AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
Chain A, Phenylethanolamine N-methyltransferaseHomo sapiens (human)Kd180.00004.6000234.7667690.0000AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (242)

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)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organizationCyclin-dependent kinase 1Homo sapiens (human)
DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
DNA repairCyclin-dependent kinase 1Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-dependent kinase 1Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
DNA damage responseCyclin-dependent kinase 1Homo sapiens (human)
mitotic nuclear membrane disassemblyCyclin-dependent kinase 1Homo sapiens (human)
centrosome cycleCyclin-dependent kinase 1Homo sapiens (human)
pronuclear fusionCyclin-dependent kinase 1Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 1Homo sapiens (human)
response to toxic substanceCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
regulation of Schwann cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
response to amineCyclin-dependent kinase 1Homo sapiens (human)
response to activityCyclin-dependent kinase 1Homo sapiens (human)
cell migrationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
chromosome condensationCyclin-dependent kinase 1Homo sapiens (human)
epithelial cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
animal organ regenerationCyclin-dependent kinase 1Homo sapiens (human)
protein localization to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein import into nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of circadian rhythmCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
response to ethanolCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
regulation of embryonic developmentCyclin-dependent kinase 1Homo sapiens (human)
response to cadmium ionCyclin-dependent kinase 1Homo sapiens (human)
response to copper ionCyclin-dependent kinase 1Homo sapiens (human)
symbiont entry into host cellCyclin-dependent kinase 1Homo sapiens (human)
fibroblast proliferationCyclin-dependent kinase 1Homo sapiens (human)
rhythmic processCyclin-dependent kinase 1Homo sapiens (human)
response to axon injuryCyclin-dependent kinase 1Homo sapiens (human)
cell divisionCyclin-dependent kinase 1Homo sapiens (human)
ventricular cardiac muscle cell developmentCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitotic sister chromatid segregationCyclin-dependent kinase 1Homo sapiens (human)
protein-containing complex assemblyCyclin-dependent kinase 1Homo sapiens (human)
cellular response to hydrogen peroxideCyclin-dependent kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeCyclin-dependent kinase 1Homo sapiens (human)
cellular response to organic cyclic compoundCyclin-dependent kinase 1Homo sapiens (human)
Golgi disassemblyCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein localization to nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of attachment of mitotic spindle microtubules to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organization involved in mitosisCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitochondrial ATP synthesis coupled electron transportCyclin-dependent kinase 1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingCyclin-dependent kinase 1Homo sapiens (human)
protein deubiquitinationCyclin-dependent kinase 1Homo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-betaHomo sapiens (human)
placenta developmentHeat shock protein HSP 90-betaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-betaHomo sapiens (human)
virion attachment to host cellHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathwayHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal ubiquitin-dependent protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of apoptotic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of cell differentiationHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of cell cycleHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to interleukin-4Heat shock protein HSP 90-betaHomo sapiens (human)
supramolecular fiber organizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of protein localization to cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-betaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-betaHomo sapiens (human)
allantoin metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of protein phosphorylationXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell proliferationXanthine dehydrogenase/oxidaseHomo sapiens (human)
guanine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
inosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyinosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
adenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyadenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyguanosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
AMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
IMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
lactationXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of gene expressionXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron-sulfur cluster assemblyXanthine dehydrogenase/oxidaseHomo sapiens (human)
amide catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell differentiationXanthine dehydrogenase/oxidaseHomo sapiens (human)
GMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dGMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dAMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of p38MAPK cascadeXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vascular endothelial growth factor signaling pathwayXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vasculogenesisXanthine dehydrogenase/oxidaseHomo 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)
negative regulation of transcription by RNA polymerase IIProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
protein poly-ADP-ribosylationProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
negative regulation of gene expressionProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
negative regulation of GTPase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
MAPK cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein import into nucleusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
response to oxidative stressLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrion organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
lysosome organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
JNK cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Rho protein signal transductionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
spermatogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuromuscular junction developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
determination of adult lifespanLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to starvationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of protein kinase A signalingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein processingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of neuron projection developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of neuron maturationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of macroautophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peptidyl-threonine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
calcium-mediated signalingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
striatum developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
olfactory bulb developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
tangential migration from the subventricular zone to the olfactory bulbLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein ubiquitinationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of protein stabilityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to oxidative stressLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to reactive oxygen speciesLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular signal transductionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of kidney sizeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
exploration behaviorLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
locomotory exploration behaviorLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of lysosomal lumen pHLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of locomotionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of membrane potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of programmed cell deathLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of MAP kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP metabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein autophosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular distribution of mitochondriaLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projection morphogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrion localizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of mitochondrial depolarizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
excitatory postsynaptic potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of dopamine receptor signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of dopamine receptor signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of ER to Golgi vesicle-mediated transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of dendritic spine morphogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localization to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localization to endoplasmic reticulum exit siteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to manganese ionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of mitochondrial fissionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of excitatory postsynaptic potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projection arborizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of synaptic vesicle endocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein autoubiquitinationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of neuroblast proliferationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic vesicle transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of late endosome to lysosome transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of autophagosome assemblyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of thioredoxin peroxidase activity by peptidyl-threonine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein targeting to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein processing involved in protein targeting to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to dopamineLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of microglial cell activationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Wnt signalosome assemblyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of retrograde transport, endosome to GolgiLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of CAMKK-AMPK signaling cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of branching morphogenesis of a nerveLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic vesicle exocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of reactive oxygen species metabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
signal transductionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (89)

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)
virus receptor activityCyclin-dependent kinase 1Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 1Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein bindingCyclin-dependent kinase 1Homo sapiens (human)
ATP bindingCyclin-dependent kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 1Homo sapiens (human)
kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 1Homo sapiens (human)
Hsp70 protein bindingCyclin-dependent kinase 1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
double-stranded RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-betaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-betaHomo sapiens (human)
heat shock protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
peptide bindingHeat shock protein HSP 90-betaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
cadherin bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein dimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
receptor ligand inhibitor activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone methyltransferase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
xanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron ion bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein homodimerization activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
molybdopterin cofactor bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
FAD bindingXanthine dehydrogenase/oxidaseHomo 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)
transcription corepressor activityProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
protein bindingProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
nucleotidyltransferase activityProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
NAD+ bindingProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
SNARE bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
magnesium ion bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
actin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTPase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein serine/threonine kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
JUN kinase kinase kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
MAP kinase kinase kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTPase activator activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
ATP bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
microtubule bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
tubulin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
syntaxin-1 bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
signaling receptor complex adaptor activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
clathrin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
small GTPase bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP-dependent protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peroxidase inhibitor activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
co-receptor bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
identical protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein homodimerization activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
transmembrane transporter bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein kinase A bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein serine kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
beta-catenin destruction complex bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (83)

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)
mitochondrial matrixCyclin-dependent kinase 1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 1Homo sapiens (human)
mitochondrionCyclin-dependent kinase 1Homo sapiens (human)
endoplasmic reticulum membraneCyclin-dependent kinase 1Homo sapiens (human)
centrosomeCyclin-dependent kinase 1Homo sapiens (human)
cytosolCyclin-dependent kinase 1Homo sapiens (human)
spindle microtubuleCyclin-dependent kinase 1Homo sapiens (human)
membraneCyclin-dependent kinase 1Homo sapiens (human)
midbodyCyclin-dependent kinase 1Homo sapiens (human)
extracellular exosomeCyclin-dependent kinase 1Homo sapiens (human)
mitotic spindleCyclin-dependent kinase 1Homo sapiens (human)
cyclin A1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin B1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 1Homo sapiens (human)
cytoplasmCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
COP9 signalosomeHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-betaHomo sapiens (human)
nucleusHeat shock protein HSP 90-betaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
membraneHeat shock protein HSP 90-betaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-betaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-betaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-betaHomo sapiens (human)
dynein axonemal particleHeat shock protein HSP 90-betaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-betaHomo sapiens (human)
aryl hydrocarbon receptor complexHeat shock protein HSP 90-betaHomo sapiens (human)
HSP90-CDC37 chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo sapiens (human)
peroxisomeXanthine dehydrogenase/oxidaseHomo sapiens (human)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
sarcoplasmic reticulumXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo 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)
nucleusProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
cytoplasmProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
nucleusProtein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)
Golgi membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
extracellular spaceLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial outer membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial inner membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial matrixLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
lysosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulumLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi apparatusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi-associated vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
trans-Golgi networkLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytosolLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoskeletonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
plasma membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
microvillusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
axonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
dendriteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
growth coneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
synaptic vesicle membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmic vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmic side of mitochondrial outer membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
dendrite cytoplasmLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projectionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuronal cell bodyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
terminal boutonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
perikaryonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular membrane-bounded organelleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
amphisomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
autolysosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
extracellular exosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum exit siteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
multivesicular body, internal vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
postsynapseLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
glutamatergic synapseLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
caveola neckLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
presynaptic cytosolLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
ribonucleoprotein complexLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Wnt signalosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (145)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID613171Inhibition of ROCK1 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613143Inhibition of IKK-beta expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613155Inhibition of ErbB2 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID566703Inhibition of human recombinant MMP2 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566699Inhibition of mushroom tyrosinase at 1 mM after 10 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566702Inhibition of human recombinant MMP1 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID613162Inhibition of MK2 expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID566705Inhibition of human recombinant MMP8 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID445467Displacement of [3H]adenine from adenine 1 receptor in rat brain cortical membrane by liquid scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID419781Binding affinity to ATP binding site of full length human Hsp90beta after 30 mins by fluorescence polarization assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.
AID287938Inhibition of human xanthine oxidase at 30 uM2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
AID338748Inhibition of phosphatidylinositol 4-kinase in human A431 cell membrane by liquid scintillation counting
AID613156Inhibition of ErbB4 expressed in Escherichia coli or baculovirus-infected insect cells at 400 to 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID243493Inhibition of human Protein kinase B alpha at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID453744Inhibition of Escherichia coli recombinant N-terminal hexahistidine-tagged CTP synthetase expressed in Escherichia coli BL21 (DE3) assessed as inhibition of CTP formation by continuous spectrophotometric assay in presence of 150 mM NH4Cl2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.
AID243583Inhibition of human Mitogen-activated protein kinase 1 at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID243566Inhibition of human c-Jun N-terminal kinase-2 alpha-2 at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID613151Inhibition of AurB expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID287937Inhibition of human xanthine oxidase2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID613158Inhibition of GSK3-beta expressed in Escherichia coli or baculovirus-infected insect cells using ATP as substrate at 667 uM by fluorescence polarization assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
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.
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.
AID613169Inhibition of PIM1 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
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.
AID243617Inhibition of human stress-activated protein kinase-2 alpha (p38 MAP-kinase) at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID243637Inhibition of human Mitogen activated protein kinase kinase 1 (MEK1) at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
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.
AID1817495Binding affinity to human GST tagged truncated LRRK2 G2019S mutant incubated for 2 hrs by TR-FRET based Lanthascreen kinase activity assay
AID243565Inhibition of human c-Jun N-terminal kinase-1 alpha-1 at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID243475Inhibition of human Protein kinase C alpha2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID566707Inhibition of mouse recombinant iNOS at 1 mM after 40 mins by colorimetric assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID243555Inhibition of human Rho-dependent protein kinase-II at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID613161Inhibition of JAK3 expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID1065710Displacement of [2,8-3H]-adenosine from Trypanosoma brucei AT1/P2 expressed in bloodstream stage of Trypanosoma brucei brucei B482013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Structure-activity relationships of synthetic cordycepin analogues as experimental therapeutics for African trypanosomiasis.
AID566700Inhibition of human recombinant 5-lipoxygenase at 1 mM after 10 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID717236Binding affinity to Streptomyces avidinii streptavidin at 4 mM using dye labeled Streptavidin binding aptamer by fluorescence spectral analysis method2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Specific interactions between adenosine and streptavidin/avidin.
AID243516Inhibition of rat c-Jun N-terminal kinase-3 at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID445484Inhibition of [3H]adenine uptake at rat adenine 1 receptor expressed in human 1321N1 cells at 1 mM after 1 min by liquid scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID445475Agonist activity at rat adenine 1 receptor expressed in human 1321N1 cells assessed as inhibition of isoproterenol-induced [3H]cAMP formation by scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID613147Inhibition of AKT1 expressed in Escherichia coli or baculovirus-infected insect cells using gamma-[33P]ATP at 400 uM by scintillation proximity assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID445473Selectivity ratio of Ki for adenine 1 receptor in HEK293 cells to Ki for adenine 1 receptor in rat brain cortical membrane2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID613167Inhibition of PI3Kalpha expressed in Escherichia coli or baculovirus-infected insect cells using gamma-[33P]ATP at 400 uM by scintillation proximity assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613152Inhibition of B-Raf expressed in Escherichia coli or baculovirus-infected insect cells using ATP as substrate at 400 uM by fluorescence polarization assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613160Inhibition of ITK expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID243481Inhibition of human cAMP-dependent protein kinase (PKA)2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID152454Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 10 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID613154Inhibition of FES expressed in Escherichia coli or baculovirus-infected insect cells using ATP as substrate at 400 uM by fluorescence polarization assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613150Inhibition of AurA expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
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.
AID1817494Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti-phospho-LRRKtide antibody addition and measured after 30 mins by TR-FRET
AID613165Inhibition of PAK2 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613163Inhibition of p38alpha expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID1452128Inhibition of ATPgammaS-BODIPY binding to Thermotoga maritima His-tagged HK853 expressed in Escherichia coli BL21(DE3)pLysS Rosetta preincubated for 30 mins prior to ATPgammaS-BODIPY addition measured after 1 hr by coomassie staining-based SDS-PAGE analys2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID613153Inhibition of EGFR expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID440574Binding affinity to Mycobacterium tuberculosis adenosine-5'-phosphosulfate reductase assessed as S-sulfocysteine formation at pH 5.5 by single turnover method in absence of thioredoxin2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Identification of critical ligand binding determinants in Mycobacterium tuberculosis adenosine-5'-phosphosulfate reductase.
AID51554Inhibitory activity against purified cdc2 p34/Cyclin B obtained from M phase oocytes of the starfish Marthasterias glacialis.1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds.
AID243699Inhibition of rat Calcium/calmodulin-dependent protein kinase type II at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID566701Inhibition of recombinant anthrax lethal factor at 1 mM after 30 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID613166Inhibition of PDK1 expressed in Escherichia coli or baculovirus-infected insect cells using gamma-[33P]ATP at 400 uM by scintillation proximity assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID445476Agonist activity at rat adenine 1 receptor expressed in human 1321N1 cells assessed as inhibition of isoproterenol-induced [3H]cAMP formation at 1 uM by scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID613148Inhibition of AKT2 expressed in Escherichia coli or baculovirus-infected insect cells using gamma-[33P]ATP at 400 uM by scintillation proximity assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID152455Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 1 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID1267460Inhibition of recombinant N-terminal truncated human cytosolic 5'-nucleotidase-2 assessed as inhibition of inosine 5'-monophosphate hydrolysis at 1 mM by rapid green malachite assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Identification of Noncompetitive Inhibitors of Cytosolic 5'-Nucleotidase II Using a Fragment-Based Approach.
AID613159Inhibition of IGF1R expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID243584Inhibition of human Mitogen-activated protein kinase 2 at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID613168Inhibition of PI3Kdelta expressed in Escherichia coli or baculovirus-infected insect cells using gamma-[33P]ATP at 400 uM by scintillation proximity assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613172Inhibition of SGK1 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613149Inhibition of ASK1 expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by IMAP assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID613144Inhibition of PI3Kgamma expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by fluorescence polarization assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID243585Inhibition of human lymphocyte protein tyrosine kinase Lck at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID566704Inhibition of human recombinant MMP3 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID453747Inhibition of Escherichia coli recombinant N-terminal hexahistidine-tagged CTP synthetase expressed in Escherichia coli BL21 (DE3) assessed as inhibition of CTP formation by continuous spectrophotometric assay in presence of 10 mM L-glutamine and 0.15 mM 2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.
AID613170Inhibition of RIP2 expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by fluorescence polarization assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
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.
AID613157Inhibition of FAK expressed in Escherichia coli or baculovirus-infected insect cells at 400 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID566706Inhibition of human recombinant MMP9 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID105205Potency against non nucleoside reverse transcriptor was determined in MT-4 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Threshold interaction energy of NRTI's (2'-deoxy 3'-substituted nucleosidic analogs of reverse transcriptase inhibitors) to undergo competitive inhibition.
AID445471Displacement of [3H]adenine from adenine 1 receptor in HEK293 cells by liquid scintillation counting2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Structure-activity relationships of adenine and deazaadenine derivatives as ligands for adenine receptors, a new purinergic receptor family.
AID613145Inhibition of JNK1 expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID1361355Inhibition of fungal FcyB expressed in Aspergillus nidulans assessed as reduction in FcyB-mediated [2,8-3H]-adenine accumulation2018European journal of medicinal chemistry, Aug-05, Volume: 156Structure-activity relationships in fungal nucleobases transporters as dissected by the inhibitory effects of novel purine analogues.
AID243690Inhibition of human RAF proto-oncogene serine/threonine-protein kinase at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID613173Inhibition of SYK expressed in Escherichia coli or baculovirus-infected insect cells at 667 uM by TR-FRET assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Selectivity of kinase inhibitor fragments.
AID243554Inhibition of human Glycogen synthase kinase-3 beta at 30 uM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
AID152453Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 100 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2010The Biochemical journal, Oct-01, Volume: 431, Issue:1
Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors.
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.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2007Nucleic acids research, , Volume: 35, Issue:18
Structure-function study of maize ribosome-inactivating protein: implications for the internal inactivation region and the sole glutamate in the active site.
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.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2003Toxicon : official journal of the International Society on Toxinology, Apr, Volume: 41, Issue:5
Structural basis for the interaction of [E160A-E189A]-trichosanthin with adenine.
AID1811Experimentally measured binding affinity data derived from PDB2003Toxicon : official journal of the International Society on Toxinology, Apr, Volume: 41, Issue:5
Structural basis for the interaction of [E160A-E189A]-trichosanthin with adenine.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2004The Journal of biological chemistry, Nov-05, Volume: 279, Issue:45
Reaction intermediates in the catalytic mechanism of Escherichia coli MutY DNA glycosylase.
AID1811Experimentally measured binding affinity data derived from PDB2004The Journal of biological chemistry, Nov-05, Volume: 279, Issue:45
Reaction intermediates in the catalytic mechanism of Escherichia coli MutY DNA glycosylase.
AID1811Experimentally measured binding affinity data derived from PDB2007BMC structural biology, Nov-06, Volume: 7Fragment-based identification of determinants of conformational and spectroscopic change at the ricin active site.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2007BMC structural biology, Nov-06, Volume: 7Fragment-based identification of determinants of conformational and spectroscopic change at the ricin active site.
AID1811Experimentally measured binding affinity data derived from PDB2001Structure (London, England : 1993), Oct, Volume: 9, Issue:10
Structure of E. coli 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidase reveals similarity to the purine nucleoside phosphorylases.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2001Structure (London, England : 1993), Oct, Volume: 9, Issue:10
Structure of E. coli 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidase reveals similarity to the purine nucleoside phosphorylases.
AID1799223Fluorescence Polarization (FP) Assay from Article 10.1021/jm900357y: \\Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.\\2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.
AID1799677Xanthine Oxidase Inhibition Assay from Article 10.1080/14756360500112326: \\6-(N-benzoylamino)purine as a novel and potent inhibitor of xanthine oxidase: inhibition mechanism and molecular modeling studies.\\2005Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 20, Issue:4
6-(N-benzoylamino)purine as a novel and potent inhibitor of xanthine oxidase: inhibition mechanism and molecular modeling studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20,995)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905873 (27.97)18.7374
1990's2360 (11.24)18.2507
2000's4514 (21.50)29.6817
2010's6394 (30.45)24.3611
2020's1854 (8.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.84

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 Index73.84 (24.57)
Research Supply Index10.05 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index157.51 (26.88)
Search Engine Supply Index2.30 (0.95)

This Compound (73.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,153 (5.26%)5.53%
Reviews1,275 (5.82%)6.00%
Case Studies912 (4.16%)4.05%
Observational68 (0.31%)0.25%
Other18,495 (84.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]