Page last updated: 2024-12-04

cytosine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID597
CHEMBL ID15913
CHEBI ID16040
SCHEMBL ID4059
MeSH IDM0005618

Synonyms (114)

Synonym
AC-2489
nsc 27787
einecs 200-749-5
AKOS005443393
4-amino-1,2-dihydropyrimidin-2-one
4-aminopyrimidin-2(1h)-one
zytosin
CHEBI:16040 ,
cytosin
4-amino-2-hydroxypyrimidine
nsc27787
cytosinimine
CYT ,
2(1h)-pyrimidinone, 4-amino-
4-amino-2(1h)-pyrimidinone
nsc-27787
NCI60_012445
4-amino-1h-pyrimidin-2-one
smr000857094
MLS001332636
MLS001332635
2(1h)-pyrimidinone, 6-amino-
2(1h)-pyrimidinone, 4-amino- (9ci)
cytosine (8ci)
ai3-52281
4-amino-2-pyrimidinol
STK366767
4-amino-2-oxo-1,2-dihydropyrimidine
C00380
71-30-7
CYTOSINE ,
cytosine, >=99%
6-aminopyrimidin-2(1h)-one
CBA1D098-C5AB-46CE-AAC6-754572886EB2
4-amino-2(1h)-pyrimidone
BMSE000180
CHEMBL15913
lamivudine impurity c rs
lamivudine impurity c
6-amino-1h-pyrimidin-2-one
AKOS000120336
6-amino-1h-pyrimidin-2-one;cytosine
A837149
NCGC00247019-01
4-amino-pyrimidin-2-ol
cas-71-30-7
NCGC00255926-01
tox21_302139
dtxsid4044456 ,
dtxcid2024456
BCP9000005
HMS2233N21
unii-8j337d1hzy
ec 200-749-5
8j337d1hzy ,
BP-20183
FT-0617471
EPITOPE ID:167475
SRI-2354-05
AKOS015896942
S4893
HMS3369N05
STL455080
4-aminopyrimidin-2-ol
cytosine [inci]
cytosine [usp-rs]
cytosine [who-dd]
lamivudine impurity c [usp impurity]
cytosine [mi]
lamivudine impurity e [ep impurity]
AM83918
SCHEMBL4059
SY001643
mfcd00006034
4-aminopyrimidin-2-(1h)-one
3h-cytosine
iminopyrimidinone
134434-40-5
STR01426
CS-W020703
4-amino-2(1h)pyrimidone
4-amino-2-oxypyrimidine
gtpl8490
4-amino-3h-pyrimidin-2-one
2-pyrimidinol, 1,4-dihydro-4-imino-, (z)- (9ci)
134434-39-2
107646-83-3
2(1h)-pyrimidinone, 3,4-dihydro-4-imino-, (e)- (9ci)
6-amino-1,2-dihydropyrimidin-2-one
cytosine, >=99.0% (hplc)
cytosine, united states pharmacopeia (usp) reference standard
cytosine, vetec(tm) reagent grade, 99%
cytosine, pharmaceutical secondary standard; certified reference material
gemcitabine impurity a, european pharmacopoeia (ep) reference standard
2-hydroxy-6-amino-pyrimidin
4-imino-3,4-dihydropyrimidin-2(1h)-one
2-pyrimidinol, 1,6-dihydro-6-imino-, (e)- (9ci)
4-aminopyrimidin-2(1h)-one (cytosine)
HY-I0626
2(1h)-pyrimidinone, 3,4-dihydro-4-imino-, (z)- (9ci)
107646-84-4
BCP22793
Q178425
EN300-21504
CCG-266052
aminopyrimidone
cid 5274263
2-pyrimidinol,1,6-dihydro-6-imino-,(e)-(9ci)
gemcitabine impurity a
2(1h)-pyrimidinone,3,4-dihydro-4-imino-,(e)-(9ci)
lamivudine impurity e (ep impurity)
cytosine (usp-rs)
lamivudine impurity c (usp impurity)
Z203045338

Research Excerpts

Overview

DNA cytosine methylation is an epigenetic mechanism involved in regulation of plant responses to biotic and abiotic stress. Its ability to change can vary with the sequence context in which a Cytosine appears. It is an important defense against invasive DNAs.

ExcerptReferenceRelevance
"DNA cytosine methylation is an epigenetic mechanism involved in regulation of plant responses to biotic and abiotic stress and its ability to change can vary with the sequence context in which a cytosine appears (CpG, CHG, CHH, where H = Adenine, Thymine, Cytosine). "( Herbivory induced methylation changes in the Lombardy poplar: A comparison of results obtained by epiGBS and WGBS.
Alonso, C; Medrano, M; Peña-Ponton, C; Troyee, AN; Verhoeven, KJF, 2023
)
1.47
"Cytosine methylation is an important defense against invasive DNAs. "( The genome of the Cauliflower mosaic virus, a plant pararetrovirus, is highly methylated in the nucleus.
Omae, N; Suzuki, M; Ugaki, M, 2020
)
2
"DNA cytosine modification is an important epigenetic mechanism that serves critical functions in a variety of biological processes in development and disease. "( High-Resolution Analysis of 5-Hydroxymethylcytosine by TET-Assisted Bisulfite Sequencing.
Huang, Z; Kohli, RM; Meng, Y; Pfeifer, GP; Szabó, PE, 2021
)
1.44
"Cytosine methylation is an epigenetic mark that promotes gene silencing and plays an important role in genome defence against transposons and invading DNA viruses. "( Geminivirus Rep protein interferes with the plant DNA methylation machinery and suppresses transcriptional gene silencing.
Bejarano, ER; Castillo, AG; Cruzado, L; Lozano-Durán, R; Piedra-Aguilera, A; Rodríguez-Negrete, E, 2013
)
1.83
"Cytosine methylation is a frequent epigenetic modification restricting the activity of gene regulatory elements. "( 5-Hydroxymethylcytosine is an essential intermediate of active DNA demethylation processes in primary human monocytes.
Andreesen, R; Gebhard, C; Klug, M; Rehli, M; Schmidhofer, S, 2013
)
2.19
"As cytosine conversion is a key element of successful methylation analysis using pyrosequencing, a support protocol for bisulfite treatment is also included."( Pyrosequencing: powerful and quantitative sequencing technology.
Hochstein, N; Kaiser, J; Kreutz, M; Narz, F; Peist, R, 2013
)
0.9
"Cytosine methylation is a DNA modification generally associated with transcriptional silencing. "( Function and information content of DNA methylation.
Schübeler, D, 2015
)
1.86
"DNA cytosine methylation is a key epigenetic mark that is required for normal mammalian development. "( Charting oxidized methylcytosines at base resolution.
Wu, H; Zhang, Y, 2015
)
1.28
"Cytosine is a nucleobase found in both DNA and RNA, while uracil is found only in RNA. "( pH-dependent UV resonance Raman spectra of cytosine and uracil.
Billinghurst, BE; Loppnow, GR; Oladepo, SA, 2009
)
2.06
"Cytosine methylation is a major epigenetic modification in most eukaryotes, and the primary function of which is to serve as a genome defense system including taming activity of transposable elements (TEs)."( Tissue culture-induced transpositional activity of mPing is correlated with cytosine methylation in rice.
Jiang, L; Liu, B; Ngezahayo, F; Pang, J; Wang, H; Xu, C, 2009
)
1.3
"DNA cytosine methylation is a conserved epigenetic modification frequently correlating with transcriptional silencing in a wide variety of eukaryotic organisms. "( Accurate sodium bisulfite sequencing in plants.
Cao, X; Chan, SR; Henderson, IR; Jacobsen, SE; Johnson, L, 2010
)
0.92
"DNA cytosine-5 methylation is a well-studied epigenetic pathway implicated in gene expression control and disease pathogenesis. "( Examination of the specificity of DNA methylation profiling techniques towards 5-methylcytosine and 5-hydroxymethylcytosine.
Jin, SG; Kadam, S; Pfeifer, GP, 2010
)
1.14
"Cytosine methylation is a post-replicative DNA modification associated with transcriptional repression. "( [Mechanism of DNA methylation and demethylation--its role in control of genes expression].
Foksiński, M; Guz, J; Oliński, R, 2010
)
1.8
"Cytosine deaminase is a non-mammalian enzyme of widespread interest for prodrug enzyme therapy due to its ability to convert prodrug 5-fluorocytosine into anticancer drug 5-fluorouracil. "( Synthesis and characterization of a novel chitosan based E. coli cytosine deaminase nanocomposite for potential application in prodrug enzyme therapy.
Ghosh, SS; Yata, VK, 2011
)
2.05
"DNA cytosine methylation is an epigenetic modification that has been implicated in many biological processes. "( Dynamic DNA cytosine methylation in the Populus trichocarpa genome: tissue-level variation and relationship to gene expression.
Freitag, M; Mockler, TC; Pellegrini, M; Pomraning, KR; Priest, HD; Strauss, SH; Vining, KJ; Wilhelm, LJ, 2012
)
1.32
"Cytosine deamination is a major promutagenic process, generating G:U mismatches that can cause transition mutations if not repaired. "( Structure and specificity of the vertebrate anti-mutator uracil-DNA glycosylase SMUG1.
Haushalter, K; Pearl, LH; Verdine, GL; Waters, TR; Wibley, JE, 2003
)
1.76
"Cytosine is a particularly good ligand at facilitating the formation of [B(x) + L](+) ions."( Using non-covalent complexes to direct the fragmentation of glycosidic bonds in the gas phase.
O'Hair, RA; Vrkic, AK, 2004
)
1.04
"Cytosine methylation is an epigenetic mechanism in eukaryotes that is often associated with stable transcriptional silencing, such as in X-chromosome inactivation and genomic imprinting. "( A population-epigenetic model to infer site-specific methylation rates from double-stranded DNA methylation patterns.
Bergstrom, CT; Genereux, DP; Laird, CD; Miner, BE, 2005
)
1.77
"Cytosine methylation is a common form of post-replicative DNA modification seen in both bacteria and eukaryotes. "( Cytosine methylation and DNA repair.
Walsh, CP; Xu, GL, 2006
)
3.22
"Cytosine methylation is an epigenetic mark that promotes gene silencing and plays important roles in development and genome defense against transposons. "( DEMETER and REPRESSOR OF SILENCING 1 encode 5-methylcytosine DNA glycosylases.
Ariza, RR; Martínez-Macías, MI; Morales-Ruiz, T; Ortega-Galisteo, AP; Ponferrada-Marín, MI; Roldán-Arjona, T, 2006
)
2.03
"Cytosine methylation is an important mechanism of gene regulation in mammals. "( Experimental manipulation of genomic methylation.
Jackson-Grusby, L; Jaenisch, R, 1996
)
1.74
"Flucytosine is an antifungal drug which can also be given by mouth and carries relatively low toxicity."( Candida osteomyelitis as a complication of parenteral nutrition in an infant. Successful treatment with flucytosine.
Berant, M; Kristal, C; Wagner, Y, 1979
)
0.99
"Flucytosine is a systemic antifungal drug that is readily absorbed from the gastrointestinal tract. "( Flucytosine.
Bennet, JE, 1977
)
1.5

Effects

A cytosine-based module has been prepared for supramolecular applications using a straightforward synthetic approach. Cytosine methylation has been shown to regulate essential cellular processes and impact biological adaptation.

ExcerptReferenceRelevance
"Cytosine methylation has been shown to regulate essential cellular processes and impact biological adaptation. "( Biogeographic conservation of the cytosine epigenome in the globally important marine, nitrogen-fixing cyanobacterium Trichodesmium.
Dolzhenko, E; Fu, F; Hutchins, DA; Lee, MD; Smith, AD; Walworth, NG; Webb, EA, 2017
)
2.18
"Cytosine methylation has been found to play a crucial role in various biological processes, including a number of human diseases. "( The role of cytosine methylation on charge transport through a DNA strand.
Anantram, MP; Govind, N; Qi, J, 2015
)
2.24
"Cytosine has only one abstractable proton at N1 but can also accept a proton at N3."( pH-dependent UV resonance Raman spectra of cytosine and uracil.
Billinghurst, BE; Loppnow, GR; Oladepo, SA, 2009
)
1.34
"Cytosine methylation has been implicated in the silencing of both transposable elements (TEs) and endogenous genes, and loss of methylation may have severe functional consequences."( DNA cytosine methylation in plant development.
Kimatu, JN; Liu, B; Xu, K; Zhang, M, 2010
)
1.64
"The cytosine richness has no known parallel in other eukaryotes, prokaryotes or archaebacteria."( A cytosine-rich region upstream of start codons serving as a signal for initiation of translation in Encephalitozoon cuniculi?
Fuglsang, A, 2005
)
1.53
"A cytosine-based module has been prepared for supramolecular applications using a straightforward synthetic approach."( Quadruply hydrogen bonded cytosine modules for supramolecular applications.
Aliev, AE; Bala, K; Golding, P; Hailes, HC; Horton, PN; Hursthouse, MB; Lafitte, VG, 2006
)
1.19
"Cytosine methylation has been implicated in epigenetic control of gene expression in animals, plants, and fungi. "( Dense nonsymmetrical DNA methylation resulting from repeat-induced point mutation in Neurospora.
Fritz, DY; Selker, EU; Singer, MJ, 1993
)
1.73
"The cytosine residue has swung completely out of the DNA helix and is positioned in the active site, which itself has undergone a large conformational change."( HhaI methyltransferase flips its target base out of the DNA helix.
Cheng, X; Klimasauskas, S; Kumar, S; Roberts, RJ, 1994
)
0.77
"Cytosine, however, has not been reported in analyses of meteorites nor is it among the products of electric spark discharge experiments."( Prebiotic cytosine synthesis: a critical analysis and implications for the origin of life.
Shapiro, R, 1999
)
1.43
"Cytosine methylation has been studied in wheat rRNA genes at nucleolar organizers displaying different activities. "( Regulation of cytosine methylation in ribosomal DNA and nucleolus organizer expression in wheat.
Flavell, RB; O'Dell, M; Thompson, WF, 1988
)
2.08
"Cytosine methylation has energetic and structural influences on left-handed Z-DNA formation in supercoiled plasmids. "( Cytosine methylation as an effector of right-handed to left-handed DNA structural transitions.
Caserta, M; Larson, JE; O'Connor, TR; Wells, RD; Zacharias, W, 1988
)
3.16

Actions

Cytosine methylation plays a major role in the regulation of sequential and tissue-specific expression of genes. Cytosine TNA promotes nonenzymatic, template-directed oligomerization of complementary activated rGMP.

ExcerptReferenceRelevance
"Cytosine methylation plays a major role in the regulation of sequential and tissue-specific expression of genes. "( Morphology-oriented epigenetic research.
Haraguchi, R; Kitazawa, R; Kitazawa, S, 2018
)
1.92
"Cytosine TNA promotes nonenzymatic, template-directed oligomerization of complementary activated rGMP, leading to selective and efficient formation of RNA products. "( Nonenzymatic oligomerization of RNA by TNA templates.
Heuberger, BD; Switzer, C, 2006
)
1.78

Toxicity

ExcerptReferenceRelevance
" In three patients, accumulation of toxic levels of 5-FC was related to diminished renal function."( Bone marrow toxicity associated with 5-fluorocytosine therapy.
Frame, PT; Kauffman, CA, 1977
)
0.52
" These results indicate that HPMPC is not toxic to the rabbit retina at 500-1000-fold the dose that is effective in suppressing CMV infections."( Lack of retinal toxicity of the anticytomegalovirus drug (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine.
Armani, R; Bergeron-Lynn, GL; Boscher, C; Capparelli, E; Connor, JD; De Clercq, E; Dolnak, DR; Munguia, D; Sherwood, C; Wiley, CA, 1992
)
0.5
" This effect and the fact that all three doses were toxic to the dams dictated that a second experiment be carried out at lower doses."( Developmental toxicity of bropirimine in rats after oral administration.
Marks, TA; Poppe, SM, 1988
)
0.27
" Nephrotoxicity in one subject was the only serious adverse event observed."( Pharmacokinetics, safety and bioavailability of HPMPC (cidofovir) in human immunodeficiency virus-infected subjects.
Cundy, KC; Fisher, PE; Jaffe, HS; Lietman, PS; Pastelak, A; Petty, BG; Wachsman, M, 1996
)
0.29
" Adverse drug reactions frequently observed were influenza-like symptoms such as fever (60."( [Bropirimine (U-54461S) early phase II clinical studies--to investigate the efficacy and safety of bropirimine treatment on various malignant tumors (urological, hematologic, and dermal cancers)].
Furue, H; Ikeda, S; Machida, T; Masaoka, T, 1997
)
0.3
"Intravitreal cidofovir has been shown to be a long acting and highly efficacious treatment for CMV retinitis; however decrease in IOP is an adverse effect."( An animal model for cidofovir (HPMPC) toxicity: intraocular pressure and histopathologic effects.
Banker, AS; Bergeron-Lynn, G; De Clercq, E; Flores-Aguilar, M; Freeman, WR; Keefe, K; Munguia, D; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
"The purpose of the study is to evaluate the adverse events and autopsy findings in a series of consecutive 20-microg intravitreous cidofovir injections at a single institution."( Adverse events and autopsy findings after intravitreous cidofovir (HPMPC) therapy in patients with acquired immune deficiency syndrome (AIDS).
Arevalo, JF; Banker, AS; De Clercq, E; Freeman, WR; Mueller, AJ; Rahhal, FM; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
" Sixty-three patients who had 246 injections in 93 eyes had 1 month's follow-up or longer for the evaluation of adverse events."( Adverse events and autopsy findings after intravitreous cidofovir (HPMPC) therapy in patients with acquired immune deficiency syndrome (AIDS).
Arevalo, JF; Banker, AS; De Clercq, E; Freeman, WR; Mueller, AJ; Rahhal, FM; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
"The most severe adverse event was postinjection chronic hypotony."( Adverse events and autopsy findings after intravitreous cidofovir (HPMPC) therapy in patients with acquired immune deficiency syndrome (AIDS).
Arevalo, JF; Banker, AS; De Clercq, E; Freeman, WR; Mueller, AJ; Rahhal, FM; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
"The most serious adverse event was postinjection chronic hypotony, which occurred in 3% of eyes."( Adverse events and autopsy findings after intravitreous cidofovir (HPMPC) therapy in patients with acquired immune deficiency syndrome (AIDS).
Arevalo, JF; Banker, AS; De Clercq, E; Freeman, WR; Mueller, AJ; Rahhal, FM; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
" Dose-dependent asymptomatic proteinuria (39%) and serum creatinine elevation (24%) were the most common adverse events thought to be related to cidofovir."( Randomized, controlled study of the safety and efficacy of intravenous cidofovir for the treatment of relapsing cytomegalovirus retinitis in patients with AIDS.
Hardy, WD; Holland, GN; Ives, DV; Jaffe, HS; Johnson, M; Kemper, CA; Kramer, F; Kuppermann, BD; Lalezari, JP; Lewis, RA; McKinley, GF; Nelson, R; Northfelt, DW; Ruby, AE; Simon, GL; Stagg, RJ; Weinberg, DV; Wolitz, RA; Youle, M, 1998
)
0.3
" Further, blood chemistry analysis showed no adverse effects of CHPMPC treatment on kidney or liver function."( Cyclic HPMPC is safe and effective against systemic guinea pig cytomegalovirus infection in immune compromised animals.
Bernstein, DI; Bourne, N; Bravo, FJ, 2000
)
0.31
" In cell culture (-)3TC is less toxic than its d(+)isomer (+)3TC, containing the natural nucleoside configuration, and both are considerably less toxic than ddC."( The molecular basis of inhibition and toxicity of modified cytosine analogues targetting HIV-1 reverse transcriptase.
Anderson, KS, 2001
)
0.55
" 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
" Our goal was to see if the assessment of DNA methylation might be a useful tool, when used in conjunction with initial, basic in vitro tests, to provide a more informative preliminary appraisal of the toxic potential of chemicals to prioritize them for further evaluation."( The value of DNA methylation analysis in basic, initial toxicity assessments.
Cockerell, GL; Goodman, JI; McKim, JM; Watson, RE, 2004
)
0.32
" Three patients suffered adverse events, two related to the hydration regimen associated with cidofovir administration."( Safety and tolerability of cidofovir in high-risk pediatric patients.
Bhadri, VA; Lee-Horn, L; Shaw, PJ, 2009
)
0.35
"Nephrotoxicity is a common and often clinically relevant adverse drug reaction."( [Drug-drug interactions and nephrotoxicity].
Czock, D; Keller, F, 2011
)
0.37
" No serious adverse events were attributed to CMX001 during therapy."( Safety and efficacy of CMX001 as salvage therapy for severe adenovirus infections in immunocompromised patients.
Anderson, M; Florescu, DF; Graham, ML; Guzman-Cottrill, JA; Johnston, C; Kurtzberg, J; Lanier, R; Lewinsohn, DA; Mommeja-Marin, H; Neely, MN; Painter, W; Papanicolaou, G; Pergam, SA; Qiu, F; Rigdon, J; Sande, J; van der Horst, C; Way, S, 2012
)
0.38
" No adverse events occurred that prevented dose escalation."( First pharmacokinetic and safety study in humans of the novel lipid antiviral conjugate CMX001, a broad-spectrum oral drug active against double-stranded DNA viruses.
Godkin, S; Lampert, B; Painter, G; Painter, W; Robertson, A; Trost, LC, 2012
)
0.38
" Treatment was well tolerated with most common adverse events being mild to moderate affecting lesional skin: pain/burning/irritation (25 patients) and ulceration (13 patients)."( Safety and efficacy of topical cidofovir to treat high-grade perianal and vulvar intraepithelial neoplasia in HIV-positive men and women.
Aboulafia, D; Berry, JM; Da Costa, M; Darragh, TM; Einstein, MH; Goldstone, SE; Jay, N; Lee, JY; Palefsky, JM; Panther, L; Stier, EA; Wilkin, T, 2013
)
0.39
" To date, a safe and effective therapy for CMV-induced hearing loss does not exist."( Safety of cidofovir by intratympanic delivery technique.
Choo, DI; Nassar, M; Reece, AL; Sidell, DR; Ward, JA, 2014
)
0.4
" Secondary outcomes were toxic effects (to assess safety) and adherence to treatment (to assess feasibility)."( Activity, safety, and feasibility of cidofovir and imiquimod for treatment of vulval intraepithelial neoplasia (RT³VIN): a multicentre, open-label, randomised, phase 2 trial.
Dutton, P; Fiander, A; Griffiths, G; Hibbitts, S; Hurt, CN; Jones, S; Madden, T; Man, S; Naik, R; Nordin, AJ; Powell, N; Tristram, A, 2014
)
0.4
" Adverse events of grade 3 or higher were reported in 31 (37%) of 84 patients allocated cidofovir and 39 (46%) of 84 patients assigned imiquimod; the most frequent grade 3 and 4 events were pain in the vulva, pruritus, fatigue, and headache."( Activity, safety, and feasibility of cidofovir and imiquimod for treatment of vulval intraepithelial neoplasia (RT³VIN): a multicentre, open-label, randomised, phase 2 trial.
Dutton, P; Fiander, A; Griffiths, G; Hibbitts, S; Hurt, CN; Jones, S; Madden, T; Man, S; Naik, R; Nordin, AJ; Powell, N; Tristram, A, 2014
)
0.4
"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
" The frequency and severity of adverse effects, particularly nephrotoxicity, in pediatric HSCT recipients are unclear, and pharmacokinetics (PK) of cidofovir in children have not previously been reported."( Pharmacokinetics and safety of intravenous cidofovir for life-threatening viral infections in pediatric hematopoietic stem cell transplant recipients.
Braverman, RS; Caruso Brown, AE; Cohen, MN; Giller, R; Levin, MJ; Rooney, JF; Tong, 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
" 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
"Results of this study support the safe intratympanic use of higher concentrations of antivirals when combined with DXA, both in solution and when applied via PPP hydrogel."( Combination therapies using an intratympanic polymer gel delivery system in the guinea pig animal model: A safety study.
Choo, DI; Nassar, M; Pordal, A; Quimby, C; Sidell, D; Ward, JA, 2016
)
0.43
" Analysis of renal function and adverse events from 3 BCV clinical studies in immunocompromised adult and pediatric subjects indicated little to no evidence of associated nephrotoxicity."( Brincidofovir Is Not a Substrate for the Human Organic Anion Transporter 1: A Mechanistic Explanation for the Lack of Nephrotoxicity Observed in Clinical Studies.
Brundage, TM; Momméja-Marin, H; Morrison, ME; Tippin, TK, 2016
)
0.43
" The most common adverse events were mild gastrointestinal events and asymptomatic, transient, and reversible elevations in serum transaminases."( Short-term clinical safety profile of brincidofovir: A favorable benefit-risk proposition in the treatment of smallpox.
Brundage, T; Chittick, G; Morrison, M; Nichols, WG, 2017
)
0.46
" The purpose of this study is to study potential biomarkers used for monitoring the toxic effects after chronic exposure to ATR by studying urine metabolites."( Potential biomarkers for monitoring the toxicity of long-term exposure to atrazine in rat by metabonomic analysis.
Geng, TQ; Li, LX; Zhang, CH; Zhang, XF; Zhang, Y; Zheng, J, 2018
)
0.48
"No clinically significant hematological/biochemical abnormalities or serious adverse events (SAE) were reported, although 6 mild to moderate adverse events (AE) occurred in relation to the study drug: 1 flu-like syndrome and 5 local AEs."( Safety and tolerance of cidofovir as a 2% gel for local application in high-grade cervical intraepithelial neoplasia: A phase 1 investigation.
Bossens, M; De Maertelaer, V; Evrard, B; Frankenne, F; Hubert, P; Jost, M; Simon, P; Snoeck, R; Van Pachterbeke, C, 2018
)
0.48
"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

Pharmacokinetics

ExcerptReferenceRelevance
" Concentrations of cidofovir in kidney declined with a half-life of 23 hr and were > 1,000-fold higher than plasma levels by 120 hr."( Pharmacokinetics of cidofovir in monkeys. Evidence for a prolonged elimination phase representing phosphorylated drug.
Cundy, KC; Hitchcock, MJ; Lee, WA; Li, ZH, 1996
)
0.29
" Pharmacokinetic parameters were generated by area-moment analysis."( Preclinical pharmacokinetics of beta-L-dioxolane-cytidine, a novel anticancer agent, in rats.
Boudinot, FD; Chu, CK; Moore, LE, 1997
)
0.3
" Because cidofovir is primarily eliminated by the kidneys and because its main adverse effect is nephrotoxicity, an understanding of the pharmacokinetic disposition of cidofovir in patients with renal insufficiency is necessary."( Pharmacokinetics of cidofovir in renal insufficiency and in continuous ambulatory peritoneal dialysis or high-flux hemodialysis.
Aweeka, FT; Brody, SR; Cundy, KC; Gambertoglio, JG; Humphreys, MH; Schoenfeld, P, 1999
)
0.3
" Serial serum and urine samples were collected to determine pharmacokinetic parameters with use of noncompartmental methods."( Pharmacokinetics of cidofovir in renal insufficiency and in continuous ambulatory peritoneal dialysis or high-flux hemodialysis.
Aweeka, FT; Brody, SR; Cundy, KC; Gambertoglio, JG; Humphreys, MH; Schoenfeld, P, 1999
)
0.3
" Mean volume of distribution at steady state did not change significantly in subjects with kidney disease and cidofovir serum elimination half-life was significantly increased in subjects with severe renal impairment."( Pharmacokinetics of cidofovir in renal insufficiency and in continuous ambulatory peritoneal dialysis or high-flux hemodialysis.
Aweeka, FT; Brody, SR; Cundy, KC; Gambertoglio, JG; Humphreys, MH; Schoenfeld, P, 1999
)
0.3
" 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
" After treatment on the fifth day, terminal half-life values averaged 39 (63) hours, and Cl(s) was reduced by approximately 20%, averaging 127 (27) mL/min."( Troxacitabine, an L-stereoisomeric nucleoside analog, on a five-times-daily schedule: a phase I and pharmacokinetic study in patients with advanced solid malignancies.
Baker, SD; de Bono, JS; Goetz, A; Hammond, LA; Hidalgo, M; Jolivet, J; Patnaik, A; Rowinsky, EK; Simmons, C; Siu, L; Stephenson, J; Weiss, G, 2002
)
0.31
" Average key pharmacokinetic parameters (Cmax, tmax, lambda z, AUC0-infinity, Vss, CL, CLR, fe, ER) for RDP differed by less than 17% from SDP and were consistent with previously reported SDP data."( Pharmacokinetics and renal effects of cidofovir with a reduced dose of probenecid in HIV-infected patients with cytomegalovirus retinitis.
Duncan, BA; Ingrosso, A; Mucci, M; Nickens, DJ; Rodríguez, CA; Wolf, DL, 2003
)
0.32
" First, the pharmacokinetic properties of the bropirimine analogues were examined in normal mice following oral dosing."( Pharmacokinetic properties, induction of interferon, and efficacy of selected 5-halo-6-phenyl pyrimidinones, bropirimine analogues, in a model of severe experimental autoimmune encephalomyelitis.
Brideau, RJ; Buxser, SE; Chapman, DL; Decker, DE; Dunn, CJ; Galinet, LA; Ready, KA; Vroegop, SM, 1999
)
0.3
" In paediatric patients this may be difficult to achieve due to lack of pharmacokinetic studies, administration of small doses, changes in body composition, continuous growth, and development and maturation of organs and systems."( The pharmacokinetics of antiviral therapy in paediatric patients.
Eksborg, S, 2003
)
0.32
"To develop and validate a population pharmacokinetic model for troxacitabine, a novel l-nucleoside analogue, administered by short infusion; to characterize clinical covariates that influence pharmacokinetic variability; and to design a dosage rate for continuous infusion administration to achieve low micromolar concentrations, which may be more efficacious than shorter infusions."( Population pharmacokinetics of troxacitabine, a novel dioxolane nucleoside analogue.
Baker, SD; Capparelli, E; Giles, F; Hidalgo, M; Jolivet, J; Lee, CK; Li, J; Moore, MJ; Rowinsky, EK, 2006
)
0.33
"Renal function and body surface area were identified as sources of troxacitabine pharmacokinetic variability."( Population pharmacokinetics of troxacitabine, a novel dioxolane nucleoside analogue.
Baker, SD; Capparelli, E; Giles, F; Hidalgo, M; Jolivet, J; Lee, CK; Li, J; Moore, MJ; Rowinsky, EK, 2006
)
0.33
"To assess the feasibility of administering troxacitabine, an L-nucleoside analog that is not a substrate for deoxycytidine deaminase, in combination with cisplatin, to identify pharmacokinetic interactions, and to seek preliminary evidence of antitumor activity."( Phase I and pharmacokinetic study of cisplatin and troxacitabine administered intravenously every 28 days in patients with advanced solid malignancies.
Beeram, M; De Bono, JS; Denis, LJ; Geyer, CE; Hao, D; Jolivet, J; Lin, CC; Ng, CM; Patnaik, A; Rha, SY; Rowinsky, EK; Takimoto, CH; Tolcher, AW, 2009
)
0.35
" Plasma and urine sampling were performed to characterize the pharmacokinetic parameters of troxacitabine in combination with cisplatin."( Phase I and pharmacokinetic study of cisplatin and troxacitabine administered intravenously every 28 days in patients with advanced solid malignancies.
Beeram, M; De Bono, JS; Denis, LJ; Geyer, CE; Hao, D; Jolivet, J; Lin, CC; Ng, CM; Patnaik, A; Rha, SY; Rowinsky, EK; Takimoto, CH; Tolcher, AW, 2009
)
0.35
" The addition of cisplatin did not substantially alter the pharmacokinetic behavior of troxacitabine."( Phase I and pharmacokinetic study of cisplatin and troxacitabine administered intravenously every 28 days in patients with advanced solid malignancies.
Beeram, M; De Bono, JS; Denis, LJ; Geyer, CE; Hao, D; Jolivet, J; Lin, CC; Ng, CM; Patnaik, A; Rha, SY; Rowinsky, EK; Takimoto, CH; Tolcher, AW, 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
" Levels of ODE-cCDV were measured by counting in a liquid scintillation counter, and pharmacokinetic (PK) parameters were determined."( Intraocular pharmacokinetics of a crystalline lipid prodrug, octadecyloxyethyl-cyclic-cidofovir, for cytomegalovirus retinitis.
Beadle, JR; Cheng, L; Freeman, WR; Hoh, C; Hostetler, KY; Tammewar, A, 2011
)
0.37
"ODE-cCDV in vitreous as a whole followed a 2-phase first-order elimination, whereas ODE-cCDV in retina and choroid manifested a nearly steady state during the first 3 weeks and then followed a first-order elimination with the apparent elimination half-life of 10."( Intraocular pharmacokinetics of a crystalline lipid prodrug, octadecyloxyethyl-cyclic-cidofovir, for cytomegalovirus retinitis.
Beadle, JR; Cheng, L; Freeman, WR; Hoh, C; Hostetler, KY; Tammewar, A, 2011
)
0.37
"A crystalline lipid prodrug, ODE-cCDV, has longer vitreous half-life than that in other ocular tissues due to its solid drug depot formation in vitreous."( Intraocular pharmacokinetics of a crystalline lipid prodrug, octadecyloxyethyl-cyclic-cidofovir, for cytomegalovirus retinitis.
Beadle, JR; Cheng, L; Freeman, WR; Hoh, C; Hostetler, KY; Tammewar, A, 2011
)
0.37
" The objectives of the study were to evaluate the safety and pharmacokinetic parameters of CMX001 after single and multiple doses."( First pharmacokinetic and safety study in humans of the novel lipid antiviral conjugate CMX001, a broad-spectrum oral drug active against double-stranded DNA viruses.
Godkin, S; Lampert, B; Painter, G; Painter, W; Robertson, A; Trost, LC, 2012
)
0.38
"46 ml/h/kg, and the elimination half-life time was 53."( Single-dose pharmacokinetics of cidofovir in continuous venovenous hemofiltration.
Gattringer, KB; Jäger, W; Kraff, S; Thalhammer, F; Vossen, MG, 2014
)
0.4
"Patients with gross haematuria and confirmed BK or adenovirus viruria following allo-HSCT were prospectively enrolled in an open-label pharmacokinetic study (ClinicalTrials."( Pharmacokinetics and safety of intravesicular cidofovir in allogeneic HSCT recipients.
Aitken, SL; Chemaly, RF; Ghantoji, SS; Jones, RB; Kontoyiannis, DP; Tam, VH; Zhou, J, 2016
)
0.43
" Mean values for volume of distribution, clearance and elimination half-life were 19."( Pharmacokinetics and safety of intravesicular cidofovir in allogeneic HSCT recipients.
Aitken, SL; Chemaly, RF; Ghantoji, SS; Jones, RB; Kontoyiannis, DP; Tam, VH; Zhou, J, 2016
)
0.43

Compound-Compound Interactions

The effects of monoclonal antibody used in combination with ganciclovir (GCV) or (S)-1-[3-hydroxy-(2-phosphonylmethoxy)propyl]cytosine (HPMPC) against murine cytomegalovirus (MCMV) were determined in vitro and in vivo, in mice. Under the influence of phosphemide in  combination with dexamethasone some characteristics of tumour DNA approximate the corresponding characteristics of DNA of healthy animals' liver.

ExcerptReferenceRelevance
"Suboptimal doses of amphotericin B in combination with either rifampin or 5-fluorocytosine were better than single-drug therapy in the treatment of disseminated Aspergillus fumigatus infection in mice."( Therapy of murine aspergillosis with amphotericin B in combination with rifampin of 5-fluorocytosine.
Arroyo, J; Kobayashi, GS; Medoff, G, 1977
)
0.7
" Weak inhibitory concentrations of CTM were tested in combination with levels of 5-FC or AMB that alone produced transient antifungal effects followed by rapid recovery of proliferative capacity."( Inhibition of potentially pathogenic yeastlike fungi by clotrimazole in combination with 5-fluorocytosine or amphotericin B.
Beggs, WH; Sarosi, GA; Steele, NM, 1976
)
0.47
" However, it produced statistically significant synergistic activity against P388 leukemia when used in combination with cyclophosphamide (CY)."( Relationship between modulation of natural killer cell activity and antitumor activity of bropirimine when used in combination with various types of chemotherapeutic drugs.
DeKoning, TF; Li, LH; Wallace, TL, 1987
)
0.27
" In vitro studies showed that 5-FC combined with CDase induced significant growth-inhibitory effects on the cultured glioma cells."( Antineoplastic effects in rats of 5-fluorocytosine in combination with cytosine deaminase capsules.
Ito, T; Katsuragi, T; Kawamoto, K; Kawamura, Y; Matsumura, H; Nishiyama, T; Ohyama, A; Sakai, T; Yamamoto, N, 1985
)
0.53
"It is shown that under the influence of phosphemide in combination with dexamethasone some characteristics of tumour DNA (content of 5 methyl cytosine, temperature, interval and enthalpy of melting) approximate the corresponding characteristics of DNA of healthy animals' liver better than under the influence of phosphemide only."( [Effect of phosphemide in combination with dexamethasone on DNA structure in sarcoma 45].
Ananian, GV; Aslanian, LL; Babaian, IuS; Garibian, DV,
)
0.33
"The effects of monoclonal antibody used in combination with ganciclovir (GCV) or (S)-1-[3-hydroxy-(2-phosphonylmethoxy)propyl]cytosine (HPMPC) against murine cytomegalovirus (MCMV) were determined in vitro and in vivo, in mice."( Effects of monoclonal antibody combined with ganciclovir or (S)-1-[3-hydroxy-(2-phosphonylmethoxy)-propyl]cytosine against murine cytomegalovirus infections in cell culture and in severe combined immunodeficient mice.
Barnett, BB; Sidwell, RW; Smee, DF; Sugiyama, ST,
)
0.55
" This study was conducted to define the dose-limiting toxicities (DLTs) of its combination with cytarabine (ara-C), idarubicin, or topotecan."( Randomized phase I/II study of troxacitabine combined with cytarabine, idarubicin, or topotecan in patients with refractory myeloid leukemias.
Cortes, JE; Douer, D; Estey, EH; Faderl, S; Garcia-Manero, G; Giles, FJ; Jeha, SS; Kantarjian, HM; Koller, CA; Levine, AM; O'Brien, SM; Thomas, DA, 2003
)
0.32
"To estimate the probability of response when intravesical bacille Calmette-Guérin (BCG) is given in combination with oral bropirimine for bladder carcinoma in situ, and to evaluate toxicity when the 2 agents are combined."( A phase II clinical trial of oral bropirimine in combination with intravesical bacillus Calmette-Guérin for carcinoma in situ of the bladder: a Southwest Oncology Group Study.
Benson, MC; Crawford, ED; Nestok, BR; Sagalowsky, AI; Sarosdy, MF; Schellhammer, PF; Tangen, CM; Weiss, GR; Wood, DP,
)
0.13
" To investigate the benefit of HAART combined with cidofovir, we retrospectively analysed the survival of 33 patients with AIDS-associated PML proven by PCR in CSF, biopsy or at autopsy."( Cidofovir in combination with HAART and survival in AIDS-associated progressive multifocal leukoencephalopathy.
Arendt, G; Evers, S; Husstedt, IW; Kraemer, C; Nolting, T, 2008
)
0.35
" Here we report on the use of RNA interference, either alone or in combination with cidofovir, as an approach to inhibit orthopoxvirus replication."( Inhibition of vaccinia virus replication by two small interfering RNAs targeting B1R and G7L genes and their synergistic combination with cidofovir.
Andrei, G; Crance, JM; Duraffour, S; Garin, D; Snoeck, R; Vigne, S, 2009
)
0.35
" Drug-drug interactions may occur at a pharmacokinetic or pharmacodynamic level."( [Drug-drug interactions and nephrotoxicity].
Czock, D; Keller, F, 2011
)
0.37
"The treatment of progressive vaccinia in individuals has involved antiviral drugs, such as cidofovir (CDV), brincidofovir, and/or tecovirimat, combined with vaccinia immune globulin (VIG)."( Enhanced efficacy of cidofovir combined with vaccinia immune globulin in treating progressive cutaneous vaccinia virus infections in immunosuppressed hairless mice.
Dagley, A; Downs, B; Hagloch, J; Smee, DF; Tarbet, EB, 2015
)
0.42
"This phase I trial aimed to assess the safety and determine the recommended Phase II dose (RP2D) of Cidofovir combined with chemoradiotherapy in patients with stage IB2-IVA cervical cancer."( Phase I trial evaluating the antiviral agent Cidofovir in combination with chemoradiation in cervical cancer patients.
Adam, J; Bayar, MA; Chargari, C; Deutsch, E; Haie-Meder, C; Lanoy, E; Laporte, M; Levy, A; Magné, N; Mazeron, R; Mondini, M; Pautier, P; Soria, JC; Varga, A; Vassal, G, 2016
)
0.43
"Cidofovir at a dose of 5mg/kg combined with chemoradiotherapy appeared tolerable and yielded tumor regressions."( Phase I trial evaluating the antiviral agent Cidofovir in combination with chemoradiation in cervical cancer patients.
Adam, J; Bayar, MA; Chargari, C; Deutsch, E; Haie-Meder, C; Lanoy, E; Laporte, M; Levy, A; Magné, N; Mazeron, R; Mondini, M; Pautier, P; Soria, JC; Varga, A; Vassal, G, 2016
)
0.43
" NV not only showed good tumor preventive effect, but also could successfully inhibited tumor development and metastasis when combined with anti-PD-L1, and induced long-term immune memory effect."( A generally minimalist strategy of constructing biomineralized high-efficiency personalized nanovaccine combined with immune checkpoint blockade for cancer immunotherapy.
Chen, J; Chen, X; Feng, Y; Hao, K; Li, H; Li, Z; Lin, L; Meng, M; Tang, Z; Tian, H; Xu, C; Zhang, S, 2022
)
0.72

Bioavailability

Sapacitabine is an orally bioavailable prodrug of the nucleoside analog 2'-C-cyano-2'-deoxy-1-β-D-arabino-pentofuranosylcytosine (CNDAC)

ExcerptReferenceRelevance
" Pharmacologic studies demonstrated a significant decrease in the bioavailability of the drug as it was administered in this study."( Phase I study of 2-amino-5-bromo-6-phenyl-4(3H)-pyrimidinone (ABPP), an oral interferon inducer, in cancer patients.
Fitzpatrick, FA; Gutknecht, GD; Hersh, EM; Reele, SB; Rios, A; Stringfellow, DA, 1986
)
0.27
" Bropirimine in solution was well absorbed in the overall small intestine, following first-order kinetics."( Small intestinal absorption of bropirimine in rats and effect of bile salt on the absorption.
Emori, H; Nishihata, T; Yokohama, S, 1995
)
0.29
"The postprandial effect on the bioavailability of bropirimine in dogs after oral administration of bropirimine tablets (Bropirimine 250 mg Tablet) was investigated."( Bioavailability of bropirimine 250 mg tablet in dogs: effect of food.
Emori, H; Nishihata, T; Yamamoto, K; Yokohama, S, 1995
)
0.29
" Subcutaneous bioavailability was essentially equivalent to that of the intravenous route, but the development of transient local fibrosis ad the volumes needed for subcutaneous dosing precluded higher subcutaneous dosing than 3 mg/kg."( Pharmacokinetics, safety and bioavailability of HPMPC (cidofovir) in human immunodeficiency virus-infected subjects.
Cundy, KC; Fisher, PE; Jaffe, HS; Lietman, PS; Pastelak, A; Petty, BG; Wachsman, M, 1996
)
0.29
" The subcutaneous bioavailability of cidofovir was 91."( Pharmacokinetics, bioavailability, metabolism, and tissue distribution of cidofovir (HPMPC) and cyclic HPMPC in rats.
Bidgood, AM; Cundy, KC; Griffin, L; Lee, WA; Lynch, G; Shaw, JP, 1996
)
0.29
" Much of the current antiviral research focuses on providing drugs with (i) improved oral bioavailability and pharmacokinetics which permit less frequent oral or topical dosing for suppressive treatment of herpes simplex virus (HSV) infections, (ii) different mechanisms of action for synergic effects in treating resistant HSV infections in the immunocompromised host and (iii) improved efficacy."( New therapeutic approaches to the alphaherpesvirus infections.
Cassady, KA; Whitley, RJ, 1997
)
0.3
" The nucleoside analog was slowly absorbed after oral administration and bioavailability varied greatly between individual rats, averaging 41 +/- 27% when calculated from urinary excretion data and 37 +/- 25% when calculated from plasma OddC concentration data."( Preclinical pharmacokinetics of beta-L-dioxolane-cytidine, a novel anticancer agent, in rats.
Boudinot, FD; Chu, CK; Moore, LE, 1997
)
0.3
"The bioavailability and metabolism of the antiviral nucleotide analog cidofovir (HPMPC) were examined in New Zealand white rabbits following topical administration to normal and abraded skin."( Bioavailability and metabolism of cidofovir following topical administration to rabbits.
Cundy, KC; Lee, WA; Lynch, G, 1997
)
0.3
"The pharmacokinetics and bioavailability of 1-[((S)-2-hydroxy-2-oxo-1,4,2-dioxaphosphorinan-5-yl)methyl]cytosi ne (cyclic HPMPC) were examined at four doses in 22 patients with human immunodeficiency virus infection."( Clinical pharmacokinetics of 1-[((S)-2-hydroxy-2-oxo-1,4,2-dioxaphosphorinan-5-yl)methyl]cytosine in human immunodeficiency virus-infected patients.
Barditch-Crovo, P; Cundy, KC; Jaffe, HS; Lietman, PS; Petty, BG; Redpath, M; Ruby, A, 1999
)
0.53
" 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
" 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
" The oral bioavailability of cyclic HPMPC from the aryl ester prodrugs ranged from 11."( Pharmacokinetics of salicylate ester prodrugs of cyclic HPMPC in dogs.
Arimilli, MN; Jones, RJ; Lee, WA; Oliyai, R,
)
0.13
"The nucleotide phosphonates cidofovir (CDV) and cyclic cidofovir (cCDV) are potent antiviral compounds when administered parenterally but are not well absorbed orally."( Enhanced inhibition of orthopoxvirus replication in vitro by alkoxyalkyl esters of cidofovir and cyclic cidofovir.
Beadle, JR; Harden, E; Hartline, C; Hostetler, KY; Keith, K; Kern, ER; Rodriguez, N, 2002
)
0.31
" In contrast to CDV, HDP-CDV is orally bioavailable and has been reported to be orally active in lethal cowpox virus infection in mice."( Increased antiviral activity of 1-O-hexadecyloxypropyl-[2-(14)C]cidofovir in MRC-5 human lung fibroblasts is explained by unique cellular uptake and metabolism.
Aldern, KA; Ciesla, SL; Hostetler, KY; Winegarden, KL, 2003
)
0.32
" The oral bioavailability was approximately 44%."( Antiviral activity and pharmacokinetics of 1-(2,3-dideoxy-2-fluoro-beta-L-glyceropent-2-enofuranosyl)cytosine.
Chen, H; Chu, CK; Feitelson, M; Glazkova, Y; Hurwitz, SJ; McClure, HM; Pai, SB; Schinazi, RF, 2003
)
0.53
" In this paper, the oral pharmacokinetics of 14C-labeled hexadecyloxypropyl-cidofir (HDP-CDV), octadecyloxyethyl-cidofir (ODP-CDV), and oleyloxypropyl-cidofir (OLP-CDV) are examined and oral bioavailability and tissue distribution assessed and compared with parenteral CDV."( Esterification of cidofovir with alkoxyalkanols increases oral bioavailability and diminishes drug accumulation in kidney.
Aldern, KA; Beadle, JR; Ciesla, SL; Hostetler, KY; Painter, GR; Trahan, J; Wan, WB, 2003
)
0.32
" To improve the bioavailability of CDV, others synthesized alkoxyalkanol esters of CDV and observed >100-fold more activity than unmodified CDV against cowpox, vaccinia, and variola virus (VARV) replication."( Efficacy of oral active ether lipid analogs of cidofovir in a lethal mousepox model.
Beadle, JR; Buller, RM; Hostetler, KY; Melman, L; Owens, G; Schriewer, J, 2004
)
0.32
"To improve the oral bioavailability of cidofovir (CDV), a series of ether lipid ester prodrugs were synthesized and evaluated for activity against murine cytomegalovirus (MCMV) infection."( Oral treatment of murine cytomegalovirus infections with ether lipid esters of cidofovir.
Beadle, JR; Collins, DJ; Hostetler, KY; Kern, ER; Quenelle, DC; Wan, WB, 2004
)
0.32
" CDV has raised recent interest because of its promising activity against smallpox, but its use is limited by its poor bioavailability and nephrotoxicity."( Encapsulation of antiviral nucleotide analogues azidothymidine-triphosphate and cidofovir in poly(iso-butylcyanoacrylate) nanocapsules.
Besnard, M; Chacun, H; Couvreur, P; Hillaireau, H; Janin, J; Le Doan, T, 2006
)
0.33
" Two prodrugs (3 and 4) created by conjugating ethylene glycol-linked amino acids (L-Val, L-Phe) with the cyclic form of cidofovir (cHPMPC) via a P-O ester bond were synthesized and their pH-dependent stability (3 and 4), potential for in vivo reconversion to drug (3), and oral bioavailability (3) were evaluated."( Synthesis and biological activation of an ethylene glycol-linked amino acid conjugate of cyclic cidofovir.
Borysko, KZ; Breitenbach, JM; Drach, JC; Eriksson, U; Hilfinger, JM; Kashemirov, BA; Kijek, P; Kim, JS; McKenna, CE; Mitchell, S, 2007
)
0.34
" 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
" treatment regimens with (N)-MCT were directly compared during a vaccinia virus (IHD strain) infection, indicating that the nucleoside has good oral bioavailability in mice."( Efficacy of N-methanocarbathymidine in treating mice infected intranasally with the IHD and WR strains of vaccinia virus.
Glazer, RI; Hurst, BL; Rahman, A; Sidwell, RW; Smee, DF; Wong, MH, 2007
)
0.34
" An ether-lipid analogue of CDV, CMX001 (HDP-CDV), has potent antiviral activity against a range of DNA viruses including poxviruses, excellent oral bioavailability and minimal nephrotoxicity."( Efficacy of therapeutic intervention with an oral ether-lipid analogue of cidofovir (CMX001) in a lethal mousepox model.
Almond, M; Buller, RM; Lampert, B; Oberle, C; Painter, G; Parker, S; Robertson, A; Touchette, E; Trost, LC, 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
)
0.59
" Perfusion studies in the rat establish that the mesenteric permeability to 4 is more than 20-fold greater than to 1, and the bioavailability of 4 is increased 6-fold relative to 1 in an in vivo murine model."( Serine peptide phosphoester prodrugs of cyclic cidofovir: synthesis, transport, and antiviral activity.
Borysko, KZ; Breitenbach, JM; Drach, JC; Eriksson, U; Hilfinger, JM; Kashemirov, BA; Kijek, P; Kim, JS; McKenna, CE; Mitchell, S; Peterson, LW,
)
0.13
" New antiviral agents are urgently needed with less adverse effects, good oral bioavailability and possibly novel targets or mechanisms of action to avoid cross-resistance and to improve the ability to suppress the selection of resistant virus strains by combination therapy."( Antiviral treatment of cytomegalovirus infection and resistant strains.
Bunjes, D; Härter, G; Mertens, T; Michel, D; Schreiber, A; Schubert, A, 2009
)
0.35
" Val-Ser-cyclic HPMPC (Val-Ser-cHPMPC) is a promising peptide prodrug which has previously been shown by us to improve the permeability and bioavailability of the parent compound in rodent models (Eriksson et al."( Puromycin-sensitive aminopeptidase: an antiviral prodrug activating enzyme.
Amidon, GL; Hilfinger, JM; Lee, KD; McKenna, CE; Nelson, CH; Peterson, LW; Provoda, CJ; Tehler, U, 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
" We evaluated the in vivo efficacy of an orally bioavailable analog of cidofovir, hexadecyloxypropyl-cidofovir (HDP-CDV), against guinea pig CMV (GPCMV) in a guinea pig model of congenital CMV infection."( Oral hexadecyloxypropyl-cidofovir therapy in pregnant guinea pigs improves outcome in the congenital model of cytomegalovirus infection.
Beadle, JR; Bernstein, DI; Bravo, FJ; Cardin, RD; Hostetler, KY, 2011
)
0.37
" CMX001 is an orally bioavailable lipid conjugate of cidofovir that is substantially less nephrotoxic than the parent drug and has excellent antiviral activity against all the human herpesviruses."( CMX001 potentiates the efficacy of acyclovir in herpes simplex virus infections.
Hartline, CB; Kern, ER; Lanier, ER; Prichard, MN; Quenelle, DC, 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
)
0.61
" We describe the clinical experience of 13 immunocompromised patients who received CMX001 (hexadecyloxypropyl cidofovir), an orally bioavailable lipid conjugate of cidofovir, for adenovirus disease."( Safety and efficacy of CMX001 as salvage therapy for severe adenovirus infections in immunocompromised patients.
Anderson, M; Florescu, DF; Graham, ML; Guzman-Cottrill, JA; Johnston, C; Kurtzberg, J; Lanier, R; Lewinsohn, DA; Mommeja-Marin, H; Neely, MN; Painter, W; Papanicolaou, G; Pergam, SA; Qiu, F; Rigdon, J; Sande, J; van der Horst, C; Way, S, 2012
)
0.38
"Sapacitabine is an orally bioavailable nucleoside analog prodrug that is in clinical trials for hematologic malignancies and solid tumors."( Sapacitabine for cancer.
Kantarjian, H; Liu, X; Plunkett, W, 2012
)
0.38
" We conclude that CMX001 is orally bioavailable and well tolerated in healthy volunteers at doses up to 2 mg/kg, approximately 140 mg in a typical adult."( First pharmacokinetic and safety study in humans of the novel lipid antiviral conjugate CMX001, a broad-spectrum oral drug active against double-stranded DNA viruses.
Godkin, S; Lampert, B; Painter, G; Painter, W; Robertson, A; Trost, LC, 2012
)
0.38
"Sapacitabine is an orally bioavailable prodrug of the nucleoside analog 2'-C-cyano-2'-deoxy-1-β-D-arabino-pentofuranosylcytosine (CNDAC)."( Sapacitabine, the prodrug of CNDAC, is a nucleoside analog with a unique action mechanism of inducing DNA strand breaks.
Liu, XJ; Nowak, B; Plunkett, W; Wang, YQ, 2012
)
0.59
" Nucleoside phosphonates are poorly absorbed primarily due to the presence of the phosphonic acid group, which ionizes at physiological pH."( Evolution of an amino acid based prodrug approach: stay tuned.
Hilfinger, JM; Kashemirov, BA; Krylov, IS; McKenna, CE, 2013
)
0.39
" Novel therapeutic approaches including CMX001, a new orally bioavailable lipid conjugate of cidofovir and the transfer of adenovirus-specific donor T cells in the context of allogeneic stem cell transplantation are discussed."( Diagnosis and treatment of adenovirus infection in immunocompromised patients.
Boztug, H; Lion, T; Matthes-Martin, S, 2013
)
0.39
" Furthermore, redox status has a profound impact on the bioavailability of ascorbate in the nucleus."( Regulation of the Epigenome by Vitamin C.
Wang, G; Young, JI; Züchner, S, 2015
)
0.42
"Brincidofovir (BCV) is an orally bioavailable lipid conjugate of cidofovir (CDV) with increased in vitro potency relative to CDV against all 5 families of double-stranded DNA viruses that cause human disease."( Brincidofovir Is Not a Substrate for the Human Organic Anion Transporter 1: A Mechanistic Explanation for the Lack of Nephrotoxicity Observed in Clinical Studies.
Brundage, TM; Momméja-Marin, H; Morrison, ME; Tippin, TK, 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
" Brincidofovir (BCV) is a lipid formulation of CDV, which has an improved oral bioavailability and favorable toxicity profile compared with CDV."( Adenovirus infection in pediatric transplant recipients: are effective antiviral agents coming our way?
Green, M; Lopez, SMC; Michaels, MG, 2018
)
0.48
" Its oral bioavailability and tolerable toxicity profile allow the drug to be used in an outpatient setting, especially in elderly unfit patients."( The efficacy of sapacitabine in treating patients with acute myeloid leukemia.
Czemerska, M; Robak, T; Wierzbowska, A, 2018
)
0.48
" Brincidofovir (BCV) is an orally bioavailable lipid conjugate of cidofovir, which has activity against adenoviruses."( Brincidofovir as a Salvage Therapy in Controlling Adenoviremia in Pediatric Recipients of Hematopoietic Stem Cell Transplant.
Kinsey, S; Meena, JP; Phillips, RS, 2019
)
0.51

Dosage Studied

The use of the antifungal agent flucytosine has been associated with dose-related hepatotoxicity and bone marrow depression. A reduction in the dosage of the 5-fluorocytosines resulted in a marked decrease in the excretion of urinary gravel. We show that this steep relationship can be explained by differences in the dose-response functions of 5-FC and cytosine.

ExcerptRelevanceReference
" High-dose T-cin controls survived despite having received a cumulative dosage of more than twice the reported (LD(50)) mean lethal dose value."( Comparative study of trichothecin, amphotericin B, and 5-fluorocytosine against Cryptococcus neoformans in vitro and in vivo.
Hariri, A; Larsh, HW; Sneller, MR; Sorenson, WG, 1977
)
0.5
" Therefore, amphotericin B dosage does not have to be adapted to kidney function, which is the case for flucytosine."( Pharmacokinetics of amphotericin B and flucytosine.
Polak, A, 1979
)
0.74
"The use of the antifungal agent flucytosine has been associated with dose-related hepatotoxicity and bone marrow depression, and measurement of plasma concentrations is useful in determining dosage schedules."( Assay of flucytosine (5-fluorocytosine) in human plasma by high-pressure liquid chromatography.
Bury, RW; Mashford, ML; Miles, HM, 1979
)
0.92
" A reduction in the dosage of the 5-fluorocytosine resulted in a marked decrease in the excretion of urinary gravel which was shown to be a coprecipitate of 5-fluorocytosine and uric acid."( Crystalluria during flucytosine therapy.
Chinwah, PM; Cobcroft, R; Williams, KM, 1979
)
0.83
" Three patients experienced leukopenia, which was readily reversed when the dosage of 5-FC was decreased and the serum concentration was lowered."( Bone marrow toxicity associated with 5-fluorocytosine therapy.
Frame, PT; Kauffman, CA, 1977
)
0.52
" Intravitreal injections of HPMPC may be efficacious in inhibiting CMV retinitis for longer dosing intervals than can be used with other anti-CMV compounds."( Lack of retinal toxicity of the anticytomegalovirus drug (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine.
Armani, R; Bergeron-Lynn, GL; Boscher, C; Capparelli, E; Connor, JD; De Clercq, E; Dolnak, DR; Munguia, D; Sherwood, C; Wiley, CA, 1992
)
0.5
" The minimal effective dosage required to prevent mortality from RCMV infection was a single dose of HPMPC at 2 mg/kg of body weight compared with DHPG therapy twice daily at 20 mg/kg/day for 5 days."( Comparative activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine and 9-(1,3-dihydroxy-2-propoxymethyl)guanine against rat cytomegalovirus infection in vitro and in vivo.
Bruggeman, CA; de Clercq, E; Stals, FS, 1991
)
0.52
" The binding of AFB1-Cl2 to polydC is substantiated by the dose-response template inhibition and by the dose-response template binding studies."( Evidence for the covalent binding of aflatoxin B1-dichloride to cytosine in DNA.
Bender, W; Chang, JC; Huang, JX; Wu, ZR; Yu, FL, 1991
)
0.52
" 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
" The dams were killed 24 hours after dosing and their uterine contents examined."( Variability in the developmental toxicity of bropirimine with the day of administration.
Black, DL; Branstetter, DG; Kirton, KT; Marks, TA; Terry, RD, 1990
)
0.28
"Oral bropirimine (an immunomodulator shown to induce interferon) was administered to timed-pregnant Sprague-Dawley rats in five experiments utilizing several different dosing schedules."( Bropirimine-induced embryolethality after oral administration to the pregnant rat.
Marks, TA; Poppe, SM; Renis, HE, 1989
)
0.28
"Timed-pregnant Upj:TUC(SD)spf (Sprague-Dawley) rats were orally (gastric intubation) dosed with bropirimine (an immunomodulator and inducer of interferon with antiviral and antitumor activities against experimental models) at 100, 200 or 400 mg/kg/day (first experiment), or at 25, 50, or 100 mg/kg/day (second experiment), on days 7-15 of gestation."( Developmental toxicity of bropirimine in rats after oral administration.
Marks, TA; Poppe, SM, 1988
)
0.27
" In the dosage used, TNF toxicity was mild, transient, and not influenced by ABPP."( Combined treatment of colon adenocarcinoma in rats with tumor necrosis factor and the interferon inducer ABPP.
de Bruin, RW; Eggermont, AM; Fiers, W; Jeekel, J; Marquet, RL, 1988
)
0.27
" Using an experimental protocol identical to that of CY and bropirimine combination therapy, and using a more or less equally effective dosage of the drug for the initial reduction of tumor burden (i."( Relationship between modulation of natural killer cell activity and antitumor activity of bropirimine when used in combination with various types of chemotherapeutic drugs.
DeKoning, TF; Li, LH; Wallace, TL, 1987
)
0.27
" The system was dosed initially and after 2 weeks of chronic exposure to 5-fluorocytosine with radiolabeled 5-fluorocytosine."( Conversion of 5-fluorocytosine to 5-fluorouracil by human intestinal microflora.
Diasio, RB; Federle, TW; Harris, BE; Manning, BW, 1986
)
0.81
" On the basis of our findings we have determined the optimal dosage that achieves desired concentrations."( [Monitoring of treatment involving 5-fluorocytosine].
Bernard, E; Chichmanian, RM; Dellamonica, P; Fournier, JP; Garraffo, R; Lapalus, P; Le Fichoux, Y; Marty, P, 1985
)
0.53
" Mild to moderate renal impairment produced marked increases in peak 5-FC concentrations in the serum of a group of eight patients on three different dosage schedules."( Pharmacological studies with 5-fluorocytosine.
Bennett, JE; Block, ER, 1972
)
0.52
" Renal clearance of 5-FC was about 75% of the creatinine clearance and a corresponding modification of drug dosage should be made in patients with renal insufficiency."( Use of 5-fluorocytosine in patients with impaired renal function.
Dawborn, JK; Page, MD; Schiavone, DJ, 1973
)
0.6
" Bioassays of specimens from patients treated with 5-fluorocytosine indicated that serum and cerebrospinal fluid concentrations of 10 to 30 mug/ml and 8 to 20 mug/ml, respectively were readily achieved with a dosage of 100 mg per kg per day."( In vitro studies with 5-fluorocytosine.
Shadomy, S, 1969
)
0.78
" Administration of ABPP or AIPP to mice by a dosage regimen similar to that resulting in interferon induction by these chemicals resulted in a significant depression in liver cytochrome P-450 levels."( Effects of 5-halopyrimidinones with antiviral and antineoplastic activity on murine cytochrome P-450.
Crowe, D; Nerland, DE; Sonnenfeld, G; Stringfellow, DA, 1984
)
0.27
" The best therapeutic response was observed when pyrimidinone was given every 4 days for a total of 7 injections; however, other schedules and dosing frequencies also gave significant responses."( Chemoimmunotherapy of B 16 melanoma and P388 leukemia with cyclophosphamide and pyrimidinones.
Johnson, MA; Li, LH; Moeller, RB; Wallace, TL, 1984
)
0.27
" Daily dosing of imiquimod for five consecutive days led to diminished production of IFN in mice as measured after the final dose."( Cytokine induction in mice by the immunomodulator imiquimod.
Miller, RL; Reiter, MJ; Testerman, TL; Tomai, MA; Weeks, CE, 1994
)
0.29
" The rate determining step for the disappearance of bropirimine from the small intestinal loop after dosing in the suspension was the dissolution process from suspension."( Small intestinal absorption of bropirimine in rats and effect of bile salt on the absorption.
Emori, H; Nishihata, T; Yokohama, S, 1995
)
0.29
"5 mg/kg with concomitant oral probenecid, saline prehydration, extended dosing intervals, and drug interruption for proteinuria (19 patients)."( (S)-1-[3-hydroxy-2-(phosphonylmethoxy)propyl]cytosine (cidofovir): results of a phase I/II study of a novel antiviral nucleotide analogue.
Cundy, K; Drew, WL; Fisher, PE; Flaherty, J; Glutzer, E; Hannigan, J; James, C; Lalezari, JP; Martin, JC; Miner, D, 1995
)
0.55
" Efficacy trials with CMV disease will define the therapeutic utility and optimal dosing interval for cidofovir."( Anticytomegaloviral activity and safety of cidofovir in patients with human immunodeficiency virus infection and cytomegalovirus viruria.
Baird, BF; Davey, RT; Falloon, J; Fisher, PE; Jaffe, HS; Kovacs, JA; Manischewitz, JF; Polis, MA; Spooner, KM; Walker, RE, 1995
)
0.29
" Similar comparisons of AUC-versus-effect curves for continuous and bolus dosing suggest that the AUC is an important determinant of antiviral activity for AUCs greater than 100 micrograms ."( Activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine against human cytomegalovirus when administered as single-bolus dose and continuous infusion in in vitro cell culture perfusion system.
Hamzeh, FM; Lee, FE; Lietman, PS; Moore, MR, 1994
)
0.53
" Only the virus recovered from the brains of mice treated with HPMPC at a dosage of 50 mg/kg/week had a slightly decreased susceptibility to HPMPC."( Efficacy of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)-cytosine and 9-(1,3-dihydroxy-2-propoxymethyl)-guanine in the treatment of intracerebral murine cytomegalovirus infections in immunocompetent and immunodeficient mice.
De Clercq, E; Neyts, J; Snoeck, R; Sobis, H; Vandeputte, M, 1993
)
0.53
" It is considered that the longer gastric residence time and larger volume of the gastric fluid induced by food-intake caused the increase in dissolution of bropirimine which increased the bioavailability after oral dosing of bropirimine 250-mg tablets."( Bioavailability of bropirimine 250 mg tablet in dogs: effect of food.
Emori, H; Nishihata, T; Yamamoto, K; Yokohama, S, 1995
)
0.29
" Radioactivity in vitreous at 240 h after intravitreal dosing with either drug contained cidofovir, cyclic HPMPC and cidofovir-phosphocholine."( Distribution and metabolism of intravitreal cidofovir and cyclic HPMPC in rabbits.
Cundy, KC; Hitchcock, MJ; Lee, WA; Lynch, G; Shaw, JP, 1996
)
0.29
" HPMPC confers a prolonged antiviral action, which lasts for several days or weeks, thus allowing infrequent dosing (i."( Therapeutic potential of Cidofovir (HPMPC, Vistide) for the treatment of DNA virus (i.e. herpes-, papova-, pox- and adenovirus) infections.
De Clercq, E, 1996
)
0.29
" Five subjects were randomized to receive drug and two to receive placebo at each of three dosage tier (1, 3, and 10 mg/kg) with a 2-week washout period doses."( Pharmacokinetics, safety and bioavailability of HPMPC (cidofovir) in human immunodeficiency virus-infected subjects.
Cundy, KC; Fisher, PE; Jaffe, HS; Lietman, PS; Pastelak, A; Petty, BG; Wachsman, M, 1996
)
0.29
" This may lead to modification of dosing regimens."( Effect of partial retinal destruction and gliosis on the intravitreal pharmacokinetics of HPMPC.
Besen, G; Capparelli, EV; Connor, JD; el-Haig, W; Freeman, WR; Kim, JW, 1995
)
0.29
" The prolonged elimination phase observed in monkeys is consistent with the long intracellular half-life of phosphorylated cidofovir in vitro and supports infrequent dosing of the drug for antiviral therapy."( Pharmacokinetics of cidofovir in monkeys. Evidence for a prolonged elimination phase representing phosphorylated drug.
Cundy, KC; Hitchcock, MJ; Lee, WA; Li, ZH, 1996
)
0.29
"25 to 3g) and multiple-dose study with one-day dosing (1 or 2g, every one or two hours, three times a day), bropirimine treatment was well tolerated by the patients with cancer."( [Bropirimine (U-54461S) phase I clinical studies].
Furue, H, 1996
)
0.29
" In addition, four treatment modifications were indicated to reduce the incidence of cidofovir-related nephrotoxicity: (a) dose reduction or interruption for changes in renal function; (b) concomitant administration of probenecid; (c) administration of 1 L of normal saline 1 h before infusion of cidofovir; and (d) extension of the dosing interval."( Cidofovir: a new therapy for cytomegalovirus retinitis.
Lalezari, JP, 1997
)
0.3
" Cidofovir's prolonged intracellular half-life permits dosing once every 2 weeks for maintenance treatment."( Clinical experience with cidofovir in the treatment of cytomegalovirus retinitis.
Kuppermann, BD; Lalezari, JP, 1997
)
0.3
" Much of the current antiviral research focuses on providing drugs with (i) improved oral bioavailability and pharmacokinetics which permit less frequent oral or topical dosing for suppressive treatment of herpes simplex virus (HSV) infections, (ii) different mechanisms of action for synergic effects in treating resistant HSV infections in the immunocompromised host and (iii) improved efficacy."( New therapeutic approaches to the alphaherpesvirus infections.
Cassady, KA; Whitley, RJ, 1997
)
0.3
" Each rat received one dosage level of OddC and the route of administration was assessed by a randomized crossover design."( Preclinical pharmacokinetics of beta-L-dioxolane-cytidine, a novel anticancer agent, in rats.
Boudinot, FD; Chu, CK; Moore, LE, 1997
)
0.3
" Treatment with one dosage of HPMPC at 20 mg/kg effectively reduced virus titers."( Effective treatment of experimental cytomegalovirus-induced encephalo-meningitis in immunocompromised rats with HPMPC.
Bruggeman, CA; Kloover, JS; Stals, FS; Vanagt, WY, 1997
)
0.3
" The guinea pig eye shows similar reduction in IOP and ciliary body changes as are seen in the human eye after intravitreal cidofovir and also appears to have a similar dose-response curve."( An animal model for cidofovir (HPMPC) toxicity: intraocular pressure and histopathologic effects.
Banker, AS; Bergeron-Lynn, G; De Clercq, E; Flores-Aguilar, M; Freeman, WR; Keefe, K; Munguia, D; Rao, NA; Taskintuna, I; Wiley, CA, 1997
)
0.3
" Advantages of the intravenous formulation include weekly dosing and efficacy."( Cidofovir use in acyclovir-resistant herpes infection.
Luks-Golger, DB; Martinez, CM, 1997
)
0.3
" A pretreatment regimen consisting of prednisone, H1 and H2 blockers was administered before the dosing of probenecid in order for the patient to continue with the antiviral therapy."( Probenecid hypersensitivity in AIDS: a case report.
Engler, RJ; Katial, RK; Myers, KW, 1998
)
0.3
" An unidentified metabolite has been observed previously in rat tissues and in urine of rabbits, rats and monkeys dosed with cidofovir."( Isolation and identification of a metabolite of cidofovir from rat kidney.
Bidgood, AM; Cundy, KC; Eisenberg, EJ; Krishnamurty, K; Lynch, GR, 1998
)
0.3
" Since cidofovir is cleared almost entirely by the kidneys, dosage adjustments must be made in patients with impaired renal function."( Cidofovir in the treatment of cytomegaloviral disease.
Fan-Havard, P; Kendle, JB, 1998
)
0.3
" Another advantage of cidofovir is its infrequent dosage schedule, which may prove beneficial in patients who are not compliant with daily intravenous dosing regimens."( Cidofovir in the treatment of cytomegaloviral disease.
Fan-Havard, P; Kendle, JB, 1998
)
0.3
"001) correlation observed between CLCR and CL in subjects with varying degrees of renal insufficiency indicates that aggressive dosage reduction of cidofovir would be necessary in subjects with kidney disease to ensure comparable drug exposure based on serum levels."( Pharmacokinetics of cidofovir in renal insufficiency and in continuous ambulatory peritoneal dialysis or high-flux hemodialysis.
Aweeka, FT; Brody, SR; Cundy, KC; Gambertoglio, JG; Humphreys, MH; Schoenfeld, P, 1999
)
0.3
" Furthermore, bropirimine was most efficacious when dosing was begun 5-10 days after injection of myelin basic protein, the protein isolated from the central nervous system and used for inducing EAE in our model."( Pharmacology of the biological response modifier bropirimine (PNU-54461) on experimental autoimmune encephalomyelitis (EAE) in mice.
Brideau, RJ; Buxser, SE; Chapman, DL; Decker, DE; Dunn, CJ; Galinet, LA; Ready, KA; Vroegop, SM, 1999
)
0.3
" Nevertheless, intravenous cidofovir offers a less intrusive administration regimen than intravenous ganciclovir or foscarnet because of its prolonged dosage interval."( Cidofovir: a review of its use in cytomegalovirus retinitis in patients with AIDS.
Noble, S; Plosker, GL, 1999
)
0.3
" Silencing arose de novo in individual R1, R2 and R3 plants despite the stability of the transgenic locus, although the basic structure of the locus, transgene dosage and position effects remained constant within the line."( Alternative silencing effects involve distinct types of non-spreading cytosine methylation at a three-gene, single-copy transgenic locus in rice.
Christou, P; Fu, X; Kohli, A; Twyman, RM, 2000
)
0.54
" Complete cures were obtained using 1% (w/v) topical cidofovir at dosing schedules of twice daily for 8 weeks beginning at 4 weeks after CRPV infection, which represents a time when papillomas were clearly visible."( In vivo anti-papillomavirus activity of nucleoside analogues including cidofovir on CRPV-induced rabbit papillomas.
Budgeon, LR; Christensen, ND; Kreider, JW; Pickel, MD, 2000
)
0.31
" The dosage of CDV was 1 to 5 mg/kg per week followed by maintenance every other week in some patients."( Cidofovir for cytomegalovirus infection and disease in allogeneic stem cell transplant recipients. The Infectious Diseases Working Party of the European Group for Blood and Marrow Transplantation.
Bacigalupo, A; Bornhäuser, M; Cesaro, S; Cordonnier, C; Crooks, B; Dekker, A; Deliliers, GL; Einsele, H; Gratecos, N; Klingebiel, T; Ljungman, P; Matthes-Martin, S; Musso, M; Platzbecker, U; Ribaud, P; Tagliaferri, E; Trenschel, R; Ullmann, AJ; Ullmann, J; Wacker, P, 2001
)
0.31
" In case of response with a decreasing number of pp65-positive leukocytes, CDV was scheduled in a dosage of 5 mg/kg body weight once a week for 2 weeks followed by maintenance therapy every 2 weeks in an outpatient setting."( Successful preemptive cidofovir treatment for CMV antigenemia after dose-reduced conditioning and allogeneic blood stem cell transplantation.
Bandt, D; Bornhäuser, M; Ehninger, G; Freiberg-Richter, J; Geissler, G; Helwig, A; Platzbecker, U; Plettig, R; Rethwilm, A; Schuler, U; Thiede, C, 2001
)
0.31
" Eight patients were enrolled on a dosage schedule of 1 mg/kg 3 times weekly."( Adenoviral infections and a prospective trial of cidofovir in pediatric hematopoietic stem cell transplantation.
Hoffman, JA; Kapoor, N; Ross, LA; Shah, AJ, 2001
)
0.31
" Cy and 3-Br-cy produced dual dose-response curves (DRC) at both halpha4beta2- and halpha4beta4-nACh receptors, but ACh produced dual DRC only at halpha4beta2-nACh receptors."( Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors.
Bermudez, I; Cassels, BK; Guerra, DL; Houlihan, LM; Kuo, YP; Lukas, RJ; Peng, JH; Slater, Y, 2001
)
0.31
" The emergence of drug resistance may be reduced by optimization of host immunity, use of potent antiviral drug regimens, and adherence to dosing regimens that adequately suppress viral replication."( Cytomegalovirus drug resistance and clinical implications.
Chou, SW, 2001
)
0.31
" Further clinical studies to find an efficacious yet tolerable dosage regimen of cidofovir, possibly using an improved pharmaceutical preparation, are required."( The effects of cidofovir 1% with and without cyclosporin a 1% as a topical treatment of acute adenoviral keratoconjunctivitis: a controlled clinical pilot study.
Böhringer, D; Cartsburg, O; De Clercq, E; Godehardt, E; Hillenkamp, J; Reinhard, T; Roggendorf, M; Ross, RS; Sundmacher, R, 2002
)
0.31
" Body surface area-based dosing was statistically significantly associated with a reduction in interpatient variability in drug clearance for only five of the 33 agents: docosahexaenoic acid (DHA)-paclitaxel, 5-fluorouracil/eniluracil, paclitaxel, temozolomide, and troxacitabine."( Role of body surface area in dosing of investigational anticancer agents in adults, 1991-2001.
Baker, SD; Donehower, RC; Grochow, LB; Rowinsky, EK; Schellens, JH; Sparreboom, A; Verweij, J, 2002
)
0.31
" The dosage of foscarnet should be 40 milligrams per kilogram three times per day or 60 milligrams per kilogram twice daily."( Management of acyclovir-resistant herpes simplex virus.
Chilukuri, S; Rosen, T, 2003
)
0.32
" The objectives of this study were to expand on the results of others that cidofovir (CDV) is effective in mice inoculated with cowpox virus (CV) or vaccinia virus (VV) and to document the efficacy of single and interval dosing beginning prior to or after infection, particularly including evaluations using suboptimal doses of CDV."( Efficacy of multiple- or single-dose cidofovir against vaccinia and cowpox virus infections in mice.
Collins, DJ; Kern, ER; Quenelle, DC, 2003
)
0.32
" These changes appear to be stepwise, implying an allele dosage effect."( The -514 C->T hepatic lipase promoter region polymorphism and plasma lipids: a meta-analysis.
Isaacs, A; Njajou, OT; Sayed-Tabatabaei, FA; van Duijn, CM; Witteman, JC, 2004
)
0.32
" These data may have important therapeutic and prognostic implication for P-gp-related drug dosage recommendation in Jewish populations."( Genotype and allele frequencies of C3435T polymorphism of the MDR1 gene in various Jewish populations of Israel.
Galski, H; Gazit, E; Korostishevsky, M; Nagler, A; Ostrovsky, O, 2004
)
0.32
" Eighteen healthy volunteers received two 1-g doses of dicloxacillin, one on the 1st study day and the other on the 11th day of rifampin dosing (600 mg daily)."( Effect of the MDR1 C3435T variant and P-glycoprotein induction on dicloxacillin pharmacokinetics.
Benet, LZ; Huang, Y; Putnam, WS; Woo, JM, 2005
)
0.33
"A positive dose-response relationship existed for gross skin changes; however, there was no dose-response relationship for severity of change in the epithelium."( Histopathologic effects of cidofovir on cartilage.
Andrus, JG; Heeren, T; Spiegel, JH; Stefanato, CM, 2005
)
0.33
"To develop and validate a population pharmacokinetic model for troxacitabine, a novel l-nucleoside analogue, administered by short infusion; to characterize clinical covariates that influence pharmacokinetic variability; and to design a dosage rate for continuous infusion administration to achieve low micromolar concentrations, which may be more efficacious than shorter infusions."( Population pharmacokinetics of troxacitabine, a novel dioxolane nucleoside analogue.
Baker, SD; Capparelli, E; Giles, F; Hidalgo, M; Jolivet, J; Lee, CK; Li, J; Moore, MJ; Rowinsky, EK, 2006
)
0.33
" The population pharmacokinetic model model-derived dosage rates for continuous infusion administration successfully achieved predetermined target plasma concentrations."( Population pharmacokinetics of troxacitabine, a novel dioxolane nucleoside analogue.
Baker, SD; Capparelli, E; Giles, F; Hidalgo, M; Jolivet, J; Lee, CK; Li, J; Moore, MJ; Rowinsky, EK, 2006
)
0.33
" However, questions remain regarding the optimal dosing schedule and side-effect profile."( 3.5-Year follow-up of intralesional cidofovir protocol for pediatric recurrent respiratory papillomatosis.
Akst, LM; Chung, BJ; Koltai, PJ, 2006
)
0.33
" Future studies will be needed to address modified dosing according to emerging pharmacokinetic and pharmacodynamic data and combination therapy which may lead to improved clinical benefit for troxacitabine in hematologic malignancies."( A phase II multicenter study of troxacitabine in relapsed or refractory lymphoproliferative neoplasms or multiple myeloma.
Baccarani, M; Belanger, R; Ben-Yehuda, D; Caballero, D; Coiffier, B; Facon, T; Fanin, R; Giles, F; Gregory, SA; Panwalkar, A; Vose, JM, 2007
)
0.34
" Cidofovir, when used in the modified dosing regimen and in combination with IVIg and renal protection measures, is a safe and potentially effective treatment option for adenovirus pneumonia in lung transplant recipients."( Treatment of adenovirus pneumonia with cidofovir in pediatric lung transplant recipients.
Dishop, MK; Doan, ML; Elidemir, O; Heinle, JS; Kaplan, SL; Mallory, GB; McKenzie, ED; Schecter, MG, 2007
)
0.34
" The main drawback in the use of most nucleoside anticancer agents originates from their hydrophilic nature, which property requires a high and frequent dosage for an intravenous administration."( Troxacitabine prodrugs for pancreatic cancer.
Adema, AD; Alexander, LE; Chu, CK; Daft, J; Hoebe, EK; Narayanasamy, J; Peters, GJ; Radi, M, 2007
)
0.34
" Treatment with a modified dosing regimen of cidofovir was well-tolerated and high-risk ADV infections resolved in all patients."( High-risk adenovirus-infected pediatric allogeneic hematopoietic progenitor cell transplant recipients and preemptive cidofovir therapy.
Anderson, EJ; Guzman-Cottrill, JA; Katz, BZ; Kletzel, M; Sullivan, C; Thormann, K; Zheng, X, 2008
)
0.35
"We have used these biomarkers to establish the optimal dosing regimen for treatment and reveal that a single dose of 25 mg/kg of CMX001 can be efficacious at treating lethal mousepox when administered on days 4 or 5 post-infection."( Using biomarkers to stage disease progression in a lethal mousepox model treated with CMX001.
Buller, RM; Lanier, R; Oberle, C; Painter, G; Parker, S; Robertson, A; Schriewer, J, 2008
)
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
" It demonstrated enhanced body weight normalized clearance of cidofovir and cidofovir dosage was augmented to 12 mg/kg per wk to reach adequate drug exposure."( Primary HHV 6 infection after liver transplantation with acute graft rejection and multi-organ failure: successful treatment with a 2.5-fold dose of cidofovir and reduction of immunosuppression.
Baba, HA; Ballauf, A; Breddemann, A; Dohna-Schwake, C; Fiedler, M; Gerner, P; Gierenz, N; Hoyer, PF; Läer, S, 2011
)
0.37
" We propose that spurious Pol II transcription throughout the intergenic spacers in hda6 mutants, combined with losses of histone deacetylase activity and/or maintenance DNA methylation, eliminates repressive chromatin modifications needed for developmental rRNA gene dosage control."( Mechanisms of HDA6-mediated rRNA gene silencing: suppression of intergenic Pol II transcription and differential effects on maintenance versus siRNA-directed cytosine methylation.
Blevins, T; Costa-Nunes, P; Earley, KW; Pikaard, CS; Pontes, O; Pontvianne, F; Tucker, S; Wierzbicki, AT, 2010
)
0.56
" The simulation results suggested that the less frequent dosing schedule of troxacitabine used currently in clinical studies was associated with less incidence of neutropenia compared to more frequent dosing schedule."( Mechanism-based pharmacokinetic/pharmacodynamic model for troxacitabine-induced neutropenia in cancer patients.
Beeram, M; Lin, CC; Ng, CM; Patnaik, A; Takimoto, CH, 2011
)
0.37
" 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
" This report describes a case of AdV hepatitis in a pediatric liver transplant recipient successfully treated with a modified, renal sparing dosing of CDV."( Treatment of adenovirus hepatitis with cidofovir in a pediatric liver transplant recipient.
Cimsit, B; Emre, S; Patel, SB; Rosencrantz, R; Tichy, EM, 2012
)
0.38
" Here we extend these studies by exploring different dosing regimens and performing randomized, blinded, placebo-controlled studies."( Efficacy of CMX001 as a post exposure antiviral in New Zealand White rabbits infected with rabbitpox virus, a model for orthopoxvirus infections of humans.
Adams, MM; Burrage, AM; Foster, S; Gray, SA; Lampert, B; Lanier, R; Lindsey, SF; Manning, BR; Moyer, RW; Painter, G; Rice, AD; Robertson, A; Smith, AJ; Swetnam, D; Wallace, G, 2011
)
0.37
" More studies are needed to better characterize the efficacy, safety, and dosing of topical cidofovir for the treatment of refractory warts."( Topical cidofovir for refractory verrucae in children.
Bayliss, SJ; Berk, DR; Gupta, M,
)
0.13
" This relationship allows for the prediction of systemic cidofovir exposure in individual patients and may be utilized to evaluate exposure-response relationships to optimize the cidofovir dosing regimen for BKV infection."( Pharmacokinetics of low-dose cidofovir in kidney transplant recipients with BK virus infection.
Gao, Y; Momper, JD; Randhawa, PS; Schonder, KS; Shapiro, R; Venkataramanan, R; Zhao, Y, 2013
)
0.39
" Administration should remain below established safe limits of dosing (3 mg/kg) and volume."( Current use of intralesional cidofovir for recurrent respiratory papillomatosis.
Chadha, NK; Derkay, CS; Froehlich, P; McMurray, JS; Pransky, SM; Rosen, CA; Volsky, PG, 2013
)
0.39
" To confirm the safety and tolerability of dosing schedules, after 20 patients had been treated in a group we enrolled an expanded cohort of 20-25 patients to that group if at least four patients had achieved complete remission or complete remission with incomplete blood count recovery, and if the 30 day death rate was 20% or less."( Oral sapacitabine for the treatment of acute myeloid leukaemia in elderly patients: a randomised phase 2 study.
Arellano, M; Chiao, J; Claxton, D; Coutre, S; Faderl, S; Garcia-Manero, G; Goldberg, SL; Jabbour, E; Kantarjian, H; Luger, S; Maness, L; Plunkett, W; Schiller, G; Seiter, K; Stock, W; Strickland, SA; Venugopal, P; Wetzler, M, 2012
)
0.38
"Cidofovir cream could be a useful therapeutic alternative, although further studies are required to establish the best dosage and its cost-effectiveness."( [Treatment of anogenital warts with topical cidofovir].
de Troya-Martín, M; Del Boz, J; Fernández-Morano, T; Frieyro-Elichegui, M; Padilla-España, L; Repiso, JB, 2013
)
0.39
" When dosed intravenously they display dose-limiting nephrotoxicity due to their accumulation in the kidney."( Evolution of an amino acid based prodrug approach: stay tuned.
Hilfinger, JM; Kashemirov, BA; Krylov, IS; McKenna, CE, 2013
)
0.39
" This study reviews the published dosing regimens of intralesional cidofovir in the treatment of RRP in order to provide a precedent for those that wish to prescribe it."( Systematic review of intralesional cidofovir dosing regimens in the treatment of recurrent respiratory papillomatosis.
Clamp, PJ; Saunders, MW, 2013
)
0.39
" There was wide variation in dosing regimens with different intervals between endoscopies, number of injections and total doses delivered."( Systematic review of intralesional cidofovir dosing regimens in the treatment of recurrent respiratory papillomatosis.
Clamp, PJ; Saunders, MW, 2013
)
0.39
" Further trials have to be done to determine the right dosage of cidofovir in patients undergoing CVVH to avoid toxic accumulation of the drug."( Single-dose pharmacokinetics of cidofovir in continuous venovenous hemofiltration.
Gattringer, KB; Jäger, W; Kraff, S; Thalhammer, F; Vossen, MG, 2014
)
0.4
" Subsequent dosing and frequency were determined by clinical response and side effects, as assessed by the treating physician."( Pharmacokinetics and safety of intravenous cidofovir for life-threatening viral infections in pediatric hematopoietic stem cell transplant recipients.
Braverman, RS; Caruso Brown, AE; Cohen, MN; Giller, R; Levin, MJ; Rooney, JF; Tong, S, 2015
)
0.42
" Bodyweight-adjusted dosing was used for patients weighing <50 kg at enrolment."( Experimental Treatment of Ebola Virus Disease with Brincidofovir.
Antierens, A; Carson, G; Castle, L; Ciglenecki, I; Dunning, J; Grove, J; Horby, PW; Howell-Jones, R; Kanapathipillai, R; Kennedy, SB; Lang, T; Olliaro, P; Pardinaz-Solis, R; Scott, J; Whitehead, J, 2016
)
0.43
" Cidofovir dosing in children needs to be optimized, and other therapeutic alternatives should be developed."( Renal Toxicity in Pediatric Patients Receiving Cidofovir for the Treatment of Adenovirus Infection.
Brothers, AW; Englund, JA; Vora, SB, 2017
)
0.46
" Our study suggests that inkjet printing technology can be utilized in the development of antiviral/anticancer combination dosage forms for mucosal application."( Inkjet printing of antiviral PCL nanoparticles and anticancer cyclodextrin inclusion complexes on bioadhesive film for cervical administration.
Aktaş, Y; Bilensoy, E; Sandler, N; Varan, C; Wickström, H, 2017
)
0.46
" 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
" Optimal dosing strategies in recipients with impaired kidney function remain undefined, with limited pharmacokinetic data to date."( Ganciclovir Dosing Strategies and Development of Cytomegalovirus Resistance in a Kidney Transplant Recipient: A Case Report.
Agrawal, N; Beltran, D; Echenique, IA; Najafian, N; Ramirez-Ruiz, L, 2017
)
0.46
" Results from phase 1 clinical studies supported once-daily oral dosing with ABT-072 in HCV infected patients."( Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability.
Beno, DWA; Beyer, JM; Colletti, L; Donner, PL; Dumas, EO; Hernandez, LE; Kati, WM; Koev, G; Krueger, AC; Lim, HB; Liu, D; Liu, Y; Longenecker, KL; Maring, CJ; Molla, A; Mondal, R; Motter, CE; Panchal, NS; Pratt, JK; Randolph, JT; Rockway, TW; Stewart, KD; Tufano, MD; Wagner, R, 2018
)
0.48
" Because activated natural killer T (NKT) cells can cooperate with pattern-recognition via TLRs to improve adaptive immune responses, we assessed the impact of combining a repeated dosing regimen of intratumoural CpG with a single intratumoural dose of the NKT cell agonist α-galactosylceramide (α-GalCer)."( Intratumoural administration of an NKT cell agonist with CpG promotes NKT cell infiltration associated with an enhanced antitumour response and abscopal effect.
Anderson, RJ; Burn, OK; Chen, CJ; Compton, BJ; Dasyam, N; Dundar, PR; Ferrer-Font, L; Godfrey, DI; Hermans, IF; Mattarollo, SR; Mayer, JU; Painter, GF; Prasit, KK; Ritchie, DS; Schmidt, AJ, 2022
)
0.72
" We show that this steep relationship can be explained by differences in the dose-response functions of 5-FC and cytosine."( Asymmetrical dose responses shape the evolutionary trade-off between antifungal resistance and nutrient use.
Alexander, EMM; Cisneros, AF; Després, PC; Dubé, AK; Gagné-Thivierge, C; Landry, CR; Sonigara, R, 2022
)
0.93
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
Escherichia coli metaboliteAny bacterial metabolite produced during a metabolic reaction in Escherichia coli.
Saccharomyces cerevisiae metaboliteAny fungal metabolite produced during a metabolic reaction in Baker's yeast (Saccharomyces cerevisiae).
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 (3)

ClassDescription
pyrimidine nucleobaseA nucleobase whose skeleton is derived from pyrimidine.
pyrimidoneA pyrimidine carrying one or more oxo substituents.
aminopyrimidineA member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
[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 (10)

PathwayProteinsCompounds
purine uptake14
Biomarkers for pyrimidine metabolism disorders1432
Renz2020 - GEM of Human alveolar macrophage with SARS-CoV-20490
pyrimidine nucleobases salvage II08
nucleoside and nucleotide degradation (archaea)722
pyrimidine ribonucleosides salvage III613
pyrimidine nucleobases salvage II418
blasticidin S biosynthesis925
arginomycin biosynthesis722
salvage pathways of pyrimidine ribonucleotides936
Biochemical pathways: part I0466

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.19210.006038.004119,952.5996AID1159523
GLI family zinc finger 3Homo sapiens (human)Potency76.48950.000714.592883.7951AID1259369
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
gemininHomo sapiens (human)Potency1.77830.004611.374133.4983AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID97848The concentration required (hypoxanthine+uridine) to inhibit the growth of L-1210 leukemic cells was evaluated1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
Synthesis and biological activity of a novel adenosine analogue, 3-beta-D-ribofuranosylthieno[2,3-d]pyrimidin-4-one.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID1145970Irreversible inhibition of Walker 256 rat tumor deoxycytidine kinase by [3H]deoxycytidine binding assay1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Irreversible enzyme inhibitors. 200. Active-site-directed inhibitors of deoxycytidine kinase.
AID1145972Irreversible inhibition of Walker 256 rat tumor deoxycytidine kinase assessed as ratio of V0/V1 by [3H]deoxycytidine binding assay1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Irreversible enzyme inhibitors. 200. Active-site-directed inhibitors of deoxycytidine kinase.
AID97843The concentration required to inhibit the growth of L-1210 leukemic cells was evaluated1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
Synthesis and biological activity of a novel adenosine analogue, 3-beta-D-ribofuranosylthieno[2,3-d]pyrimidin-4-one.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10,767)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903108 (28.87)18.7374
1990's1571 (14.59)18.2507
2000's2620 (24.33)29.6817
2010's2691 (24.99)24.3611
2020's777 (7.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 77.27

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 Index77.27 (24.57)
Research Supply Index9.33 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index142.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (77.27)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials142 (1.27%)5.53%
Reviews729 (6.53%)6.00%
Case Studies552 (4.94%)4.05%
Observational5 (0.04%)0.25%
Other9,740 (87.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]