Page last updated: 2024-11-12

rpl 554

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

Description

ensifentrine: a phosphodiesterase 3/4 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9934746
CHEMBL ID4594287
SCHEMBL ID625876
SCHEMBL ID20720900
MeSH IDM0501302

Synonyms (48)

Synonym
LS-193855 ,
rpl554
298680-25-8
9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimidino(6,1-a)isoquinolin-4-one
rpl-554
SCHEMBL625876
9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6,1-a]isoquinolin-4-one
9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6,1-a]isoquinolin-4-one
CSOBIBXVIYAXFM-UHFFFAOYSA-N
9,10-dimethoxy-2-(2.4.6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6.1-a]isoquinolin-4-one
ls-193,855
ensifentrine [usan]
ensifentrine [who-dd]
n-(2-((2e)-9,10-dimetoxi-4-oxo-2-((2,4,6-trimetilfenil)imino)-6,7-dihidro-2h-pirimido(6,1-a)isoquinolein-3(4h)-il)etil)urea
urea, n-(2-(6,7-dihydro-9,10-dimethoxy-4-oxo-2-((2,4,6-trimethylphenyl)imino)-2h-pyrimido(6,1-a)isoquinolin-3(4h)-yl)ethyl)-
3E3D8T1GIX ,
ensifentrine
1884461-72-6
2-(9,10-dimethoxy-4-oxo-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido(6,1-a)isoquinolin-3-yl)ethylurea
ensifentrine [inn]
DTXSID00183983
unii-3e3d8t1gix
(2-{9,10-dimethoxy-4-oxo-2-[(2,4,6-trimethylphenyl)imino]-2h,3h,4h,6h,7h-pyrimido[4,3-a]isoquinolin-3-yl}ethyl)urea
ensifentrine [usan:inn]
who 10726
(e)-1-(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2h-pyrimido[6,1-a]isoquinolin-3(4h)-yl)ethyl)urea
SCHEMBL20720900
vmx-554
Q7277486
SB19810
2-[9,10-dimethoxy-4-oxo-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido[6,1-a]isoquinolin-3-yl]ethylurea
BCP31840
ensifentrina; ensifentrinum;rpl-554;rpl554;rpl 554
ensifentrine (usan/inn)
D11743
a]isoquinolin-3(4h)-yl}ethyl)urea
n-(2-{(2e)-9,10-dimethoxy-4-oxo-2-[(2,4,6-
trimethylphenyl)imino]-6,7-dihydro-2h-pyrimido[6,1-
MS-28860
rpl-554;ensifentrinum
CHEMBL4594287
A937318
gtpl11865
EX-A6633
HY-111477
(e/z)-ensifentrine
CS-0041580
AKOS040746804

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Overall, RPL554 was well tolerated, and adverse events were generally mild and of equal frequency between placebo and active treatment groups."( Efficacy and safety of RPL554, a dual PDE3 and PDE4 inhibitor, in healthy volunteers and in patients with asthma or chronic obstructive pulmonary disease: findings from four clinical trials.
Banner, KH; Burggraaf, J; Calzetta, L; Cazzola, M; Cohen, AF; de Kam, ML; Diamant, Z; Franciosi, LG; Kamerling, IM; Morelli, N; Page, CP; Singh, D; Spina, D; Walker, MJ; Zuiker, R, 2013
)
0.39

Dosage Studied

ExcerptRelevanceReference
" The primary endpoint of study 2 was maximum FEV1 reached during 6 h after dosing with RPL554 in patients with asthma."( Efficacy and safety of RPL554, a dual PDE3 and PDE4 inhibitor, in healthy volunteers and in patients with asthma or chronic obstructive pulmonary disease: findings from four clinical trials.
Banner, KH; Burggraaf, J; Calzetta, L; Cazzola, M; Cohen, AF; de Kam, ML; Diamant, Z; Franciosi, LG; Kamerling, IM; Morelli, N; Page, CP; Singh, D; Spina, D; Walker, MJ; Zuiker, R, 2013
)
0.39
"This study aimed to investigate the dose-response and pharmacology of a range of single doses of nebulised ensifentrine (RPL554), an inhaled dual phosphodiesterase (PDE) 3/4 inhibitor in patients with asthma."( Efficacy and safety of a first-in-class inhaled PDE3/4 inhibitor (ensifentrine) vs salbutamol in asthma.
Abbott-Banner, K; Bjermer, L; Newman, K, 2019
)
0.51
" For the two co-primary endpoints there was a clear ensifentrine dose-response relationship, with all treatments superior to placebo (p < 0."( Efficacy and safety of a first-in-class inhaled PDE3/4 inhibitor (ensifentrine) vs salbutamol in asthma.
Abbott-Banner, K; Bjermer, L; Newman, K, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1720050Induction of FEV1 in COPD patient at 18 ug/kg administered as single dose2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Advances in the Development of Phosphodiesterase-4 Inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (4.35)29.6817
2010's12 (52.17)24.3611
2020's10 (43.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.37

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

MetricThis Compound (vs All)
Research Demand Index29.37 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index6.15 (4.65)
Search Engine Demand Index28.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (29.17%)5.53%
Reviews4 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (54.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]