Page last updated: 2024-12-11

denufosol tetrasodium

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

Description

denufosol tetrasodium: for treatment of cystic fibrosis [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10219163
CHEMBL ID1767407
MeSH IDM0438654
PubMed CID9875516
CHEMBL ID507282
SCHEMBL ID24414847
MeSH IDM0438654

Synonyms (45)

Synonym
uridine 5'-(pentahydrogen tetraphosphate), p'''-5'-ester with 2'-deoxycytidine, tetrasodium salt
denufosol tetrasodium salt
318250-11-2
denufosol tetrasodium (usan)
D03685
denufosol tetrasodium
ins-37217
ins37217
ins 37217
chembl1767407 ,
82m942wz4a ,
2'-deoxycytidine(5')tetraphospho(5')uridine tetrasodium salt
uridine 5'-(pentahydrogen tetraphosphate), p'''-5'-ester with ''-deoxycytidine, tetrasodium salt
denufosol tetrasodium [usan]
unii-82m942wz4a
uridine 5'-(pentahydrogen tetraphosphate), p'''->5'-ester with ''-deoxycytidine, tetrasodium salt
denufosol tetrasodium salt [mi]
denufosol tetrasodium [mart.]
HY-U00196
CS-7295
uridine 5'-(pentahydrogen tetraphosphate), 2'-deoxy-, p''' inverted exclamation marku5'-ester with cytidine, tetrasodium salt
tetrasodium;[[(2r,3s,5r)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate
Q27269345
318250-11-2 (sodium)
[[[[(2r,3s,5r)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] [(2r,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
gtpl1737
up4dc
dcp4u
bdbm50270553
denufosol
CHEMBL507282 ,
ins 3721
p(1)-(uridine 5')-p(4)-(2'-deoxycytidine 5')tetraphosphate, tetrasodium salt
unii-5pc250kssh
5pc250kssh ,
denufosol [inn]
211448-85-0
ins3721
denufosol [mi]
denufosol [who-dd]
DB04983
Q908026
uridine 5'-(pentahydrogen tetraphosphate), 2'-deoxy-, p''' inverted exclamation marku5'-ester with cytidine
DTXSID50870235
SCHEMBL24414847

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The percent of subjects experiencing adverse events was similar between the denufosol and placebo groups."( Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis.
Daines, C; Deterding, R; Engels, J; Gibson, R; Gorden, J; Lavange, L; Marshall, B; Mathews, D; Milgram, L; Milla, C; Ramsey, B; Retsch-Bogart, G; Schaberg, A; Williams, J; Zeitlin, PL, 2005
)
0.33
" The most common adverse event was cough (52% of placebo patients and 47% of denufosol patients)."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34
"Denufosol administered three times daily for 28 days appeared to be safe and well tolerated in this population with mild cystic fibrosis and provided preliminary evidence of potential benefit in lung function."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34

Dosage Studied

ExcerptRelevanceReference
" Forced expiratory volume in 1 sec (FEV(1)) profiles following dosing were similar across treatment groups, with some acute, reversible decline seen in both groups, most notably in subjects with lower lung function at baseline."( Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis.
Daines, C; Deterding, R; Engels, J; Gibson, R; Gorden, J; Lavange, L; Marshall, B; Mathews, D; Milgram, L; Milla, C; Ramsey, B; Retsch-Bogart, G; Schaberg, A; Williams, J; Zeitlin, PL, 2005
)
0.33
" All treatments were generally well tolerated, with no dose-response trends observed with respect to safety parameters."( Phase 2 randomized safety and efficacy trial of nebulized denufosol tetrasodium in cystic fibrosis.
Brody, AS; Coquillette, SJ; Deterding, RR; Engels, JM; Lavange, LM; Mathews, DW; Millard, SP; Ramsey, BW, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
P2Y purinoceptor 2Homo sapiens (human)EC50 (µMol)0.20000.00560.682810.0000AID593134
P2Y purinoceptor 4Homo sapiens (human)EC50 (µMol)0.80000.02301.362310.0000AID593135
P2Y purinoceptor 6Homo sapiens (human)EC50 (µMol)1.00000.01302.393020.0000AID593136
P2Y purinoceptor 2Homo sapiens (human)EC50 (µMol)0.21000.00560.682810.0000AID280297; AID404832; AID460573
P2Y purinoceptor 4Homo sapiens (human)EC50 (µMol)0.14000.02301.362310.0000AID404834
P2Y purinoceptor 6Homo sapiens (human)EC50 (µMol)0.95000.01302.393020.0000AID404830
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
intracellular monoatomic ion homeostasisP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
positive regulation of mucus secretionP2Y purinoceptor 2Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 2Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 4Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 4Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
phagocytosisP2Y purinoceptor 6Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
activation of phospholipase C activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of smooth muscle cell migrationP2Y purinoceptor 6Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol 1,4,5-trisphosphate-sensitive calcium-release channel activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeP2Y purinoceptor 6Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 6Homo sapiens (human)
cellular response to purine-containing compoundP2Y purinoceptor 6Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationP2Y purinoceptor 6Homo sapiens (human)
cellular response to pyrimidine ribonucleotideP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
intracellular monoatomic ion homeostasisP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
positive regulation of mucus secretionP2Y purinoceptor 2Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 2Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 4Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 4Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2Y purinoceptor 4Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 4Homo sapiens (human)
phagocytosisP2Y purinoceptor 6Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
activation of phospholipase C activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of smooth muscle cell migrationP2Y purinoceptor 6Homo sapiens (human)
transepithelial chloride transportP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol 1,4,5-trisphosphate-sensitive calcium-release channel activityP2Y purinoceptor 6Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeP2Y purinoceptor 6Homo sapiens (human)
cellular response to prostaglandin E stimulusP2Y purinoceptor 6Homo sapiens (human)
cellular response to purine-containing compoundP2Y purinoceptor 6Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationP2Y purinoceptor 6Homo sapiens (human)
cellular response to pyrimidine ribonucleotideP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
protein bindingP2Y purinoceptor 2Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 2Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 2Homo sapiens (human)
protein bindingP2Y purinoceptor 4Homo sapiens (human)
ATP bindingP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor activityP2Y purinoceptor 6Homo sapiens (human)
protein bindingP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UDP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 6Homo sapiens (human)
protein bindingP2Y purinoceptor 2Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 2Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 2Homo sapiens (human)
protein bindingP2Y purinoceptor 4Homo sapiens (human)
ATP bindingP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 4Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled receptor activityP2Y purinoceptor 6Homo sapiens (human)
protein bindingP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UDP receptor activityP2Y purinoceptor 6Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 4Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 4Homo sapiens (human)
presynaptic active zone membraneP2Y purinoceptor 4Homo sapiens (human)
glutamatergic synapseP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 6Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 6Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 4Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 4Homo sapiens (human)
presynaptic active zone membraneP2Y purinoceptor 4Homo sapiens (human)
glutamatergic synapseP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 4Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 6Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 6Homo sapiens (human)
plasma membraneP2Y purinoceptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID593136Agonist activity at P2Y6 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors.
AID593135Agonist activity at P2Y4 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors.
AID593134Agonist activity at P2Y2 receptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors.
AID404832Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID404834Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID404830Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
AID280297Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
AID460573Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.
AID1346348Human P2Y4 receptor (P2Y receptors)2002The Journal of pharmacology and experimental therapeutics, Sep, Volume: 302, Issue:3
Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis.
AID1347028Human P2Y2 receptor (P2Y receptors)1996British journal of pharmacology, Jan, Volume: 117, Issue:1
Enzymatic synthesis of UTP gamma S, a potent hydrolysis resistant agonist of P2U-purinoceptors.
AID1347028Human P2Y2 receptor (P2Y receptors)2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates.
AID1347028Human P2Y2 receptor (P2Y receptors)2002The Journal of pharmacology and experimental therapeutics, Sep, Volume: 302, Issue:3
Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (3.33)18.2507
2000's18 (60.00)29.6817
2010's11 (36.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.99

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.99 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (23.08%)5.53%
Trials0 (0.00%)5.53%
Reviews6 (23.08%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other14 (53.85%)84.16%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]