Page last updated: 2024-11-13

praliciguat

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

Description

praliciguat: soluble guanylate cyclase stimulator [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

praliciguat : A member of the class of pyrazoles that is 5-fluoro-2-(1H-pyrazol-3-yl)pyrimidine which is substituted by a 2-fluorobenzyl group at position 1, 1,2-oxazol-3-yl group at position 5, and by a [3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]nitrilo group at position 4. It is a soluble guanylate cyclase stimulator under clinical development for the treatment of heart failure with preserved ejection fraction. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID86269973
CHEMBL ID4297214
CHEBI ID142431
SCHEMBL ID16082414

Synonyms (36)

Synonym
praliciguat
1628730-49-3
CHEBI:142431
iw-1973
1,1,1,3,3,3-hexafluoro-2-[({5-fluoro-2-[1-(2-fluorobenzyl)-5-(1,2-oxazol-3-yl)-1h-pyrazol-3-yl]pyrimidin-4-yl}amino)methyl]propan-2-ol
praliciguatum
SCHEMBL16082414
1,1,1,3,3,3-hexafluoro-2-{[(5-fluoro-2-{1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)-1h-pyrazol-3-yl}pyrimidin-4-yl)amino]methyl}propan-2-ol
praliciguat [inn]
praliciguat [usan]
2-propanol, 1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-((2-fluorophenyl)methyl)-5-(3-isoxazolyl)-1h-pyrazol-3-yl)-4-pyrimidinyl)amino)methyl)-
praliciguat [who-dd]
R1S0H458SA ,
1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1h-pyrazol-3-yl) pyrimidin-4-yl)amino)methyl)propan-2-ol
unii-r1s0h458sa
gtpl9900
1,1,1-trifluoro-3-[(5-fluoro-2-{1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)-1h-pyrazol-3-yl}pyrimidin-4-yl)amino]-2-(trifluoromethyl)propan-2-ol
iw1973
1,1,1,3,3,3-hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)pyrazol-3-yl]pyrimidin-4-yl]amino]methyl]propan-2-ol
praliciguat (usan/inn)
D11274
bdbm321618
us10183021, compound i-324
CS-0031480
D87220
MS-29869
HY-109039
CHEMBL4297214
2-propanol, 1,1,1,3,3,3-hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1h-pyrazol-3-yl]-4-pyrimidinyl]amino]methyl]-
EX-A5960
BP177758
cysjntqnmdwajv-uhfffaoysa-n
DTXSID901101232
1,1,1,3,3,3-hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1h-pyrazol-3-yl]-4-pyrimidinyl]amino]methyl]-2-propanol
AC-37104
AKOS040742441

Research Excerpts

Overview

Praliciguat is an orally available sGC (soluble guanylate cyclase) stimulator. It has been reported both preclinically and in early stage clinical trials to have favorable effects in metabolic and hemodynamic outcomes.

ExcerptReferenceRelevance
"Praliciguat is an orally available sGC (soluble guanylate cyclase) stimulator that has been reported both preclinically and in early stage clinical trials to have favorable effects in metabolic and hemodynamic outcomes, suggesting that it may have a potential beneficial effect in peripheral artery disease."( Praliciguat Promotes Ischemic Leg Reperfusion in Leptin Receptor-Deficient Mice.
Buys, ES; Chapouly, C; Cornuault, L; Couffinhal, T; Foussard, N; Gadeau, AP; Mohammedi, K; Renault, MA; Reynaud, A; Rouault, P, 2023
)
3.07

Effects

ExcerptReferenceRelevance
"Praliciguat has been shown to be renoprotective in rodent models of hypertensive nephropathy and renal fibrosis."( Praliciguat inhibits progression of diabetic nephropathy in ZSF1 rats and suppresses inflammation and apoptosis in human renal proximal tubular cells.
Currie, MG; Jones, JE; Liu, G; Lonie, E; Masferrer, JL; Price, GM; Profy, AT; Shea, CM; Warren, W; Yan, S; Zimmer, DP, 2020
)
2.72

Treatment

Praliciguat treatment reduced blood pressure, improved cardiorenal damage, and attenuated the increase in circulating markers of inflammation and fibrosis. The drug did not significantly reduce albuminuria compared with placebo in the primary efficacy analysis.

ExcerptReferenceRelevance
"Praliciguat treatment reduced blood pressure, improved cardiorenal damage, and attenuated the increase in circulating markers of inflammation and fibrosis."( Soluble guanylate cyclase stimulator praliciguat attenuates inflammation, fibrosis, and end-organ damage in the Dahl model of cardiorenal failure.
Buys, ES; Currie, MG; Liu, G; Masferrer, JL; Price, GM; Sarno, R; Shea, CM, 2020
)
1.55
"Praliciguat treatment also attenuated transforming growth factor-β-mediated apoptosis, changes to a mesenchyme-like cellular phenotype, and phosphorylation of SMAD3 in RPTCs."( Praliciguat inhibits progression of diabetic nephropathy in ZSF1 rats and suppresses inflammation and apoptosis in human renal proximal tubular cells.
Currie, MG; Jones, JE; Liu, G; Lonie, E; Masferrer, JL; Price, GM; Profy, AT; Shea, CM; Warren, W; Yan, S; Zimmer, DP, 2020
)
2.72
"Praliciguat treatment for 12 weeks did not significantly reduce albuminuria compared with placebo in the primary efficacy analysis. "( Effects of the Soluble Guanylate Cyclase Stimulator Praliciguat in Diabetic Kidney Disease: A Randomized Placebo-Controlled Clinical Trial.
Bakris, GL; Carlson, K; Chickering, JG; Chien, YT; Cressman, MD; Currie, MG; de Boer, IH; Hanrahan, JP; Milne, GT; Profy, AT; Seferovic, JP; Wakefield, JD; Wilson, PJ, 2020
)
2.25
"Praliciguat treatment lowered hepatic steatosis and plasma cholesterol levels."( sGC stimulator praliciguat suppresses stellate cell fibrotic transformation and inhibits fibrosis and inflammation in models of NASH.
Bernier, SG; Catanzano, V; Currie, MG; Hall, KC; Jacobson, S; Liu, G; Masferrer, JL; Sarno, R; Zhang, PY, 2019
)
1.59

Toxicity

ExcerptReferenceRelevance
" No serious or severe adverse events (AEs) were reported."( A Randomized, Placebo-Controlled, Multiple-Ascending-Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Soluble Guanylate Cyclase Stimulator Praliciguat in Healthy Subjects.
Chickering, JG; Currie, MG; Hall, M; Hanrahan, JP; Mihova, M; Milne, GT; Profy, AT; Ruff, D; Wakefield, JD; Wilson, PJ, 2019
)
0.71

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetics were dose proportional, with an effective half-life of 24-37 hours, supporting once-daily dosing."( A Randomized, Placebo-Controlled, Multiple-Ascending-Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Soluble Guanylate Cyclase Stimulator Praliciguat in Healthy Subjects.
Chickering, JG; Currie, MG; Hall, M; Hanrahan, JP; Mihova, M; Milne, GT; Profy, AT; Ruff, D; Wakefield, JD; Wilson, PJ, 2019
)
0.71

Dosage Studied

ExcerptRelevanceReference
" Repeated once-daily dosing showed sustained decreases in BP."( A Randomized, Placebo-Controlled, Multiple-Ascending-Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Soluble Guanylate Cyclase Stimulator Praliciguat in Healthy Subjects.
Chickering, JG; Currie, MG; Hall, M; Hanrahan, JP; Mihova, M; Milne, GT; Profy, AT; Ruff, D; Wakefield, JD; Wilson, PJ, 2019
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
soluble guanylate cyclase activatorAny compound that binds to and activates soluble guanylate cyclase (EC 4.6.1.2).
anti-inflammatory agentAny compound that has anti-inflammatory effects.
vasodilator agentA drug used to cause dilation of the blood vessels.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[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 (7)

ClassDescription
isoxazolesOxazoles in which the N and O atoms are adjacent.
pyrazoles
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
aminopyrimidineA member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
tertiary alcoholA tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
monofluorobenzenesAny member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent.
[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]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (8.33)29.6817
2010's3 (25.00)24.3611
2020's8 (66.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.70

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 Index29.70 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index5.64 (4.65)
Search Engine Demand Index31.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (50.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (8.33%)4.05%
Observational0 (0.00%)0.25%
Other5 (41.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]