Page last updated: 2024-11-13

act-246475

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

Description

selatogrel: a P2Y12 receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID59534142
CHEMBL ID4297589
SCHEMBL ID2928412
MeSH IDM000609964

Synonyms (15)

Synonym
SCHEMBL2928412
4-((r)-2-((6-((s)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl)amino)-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester
selatogrel
1-piperazinecarboxylic acid, 4-((2r)-2-(((6-((3s)-3-methoxy-1-pyrrolidinyl)-2-phenyl-4-pyrimidinyl)carbonyl)amino)-1-oxo-3-phosphonopropyl)-, 1-butyl ester
unii-6dpk7o4pr7
selatogrel [inn]
6DPK7O4PR7 ,
((2r)-3-(4-butoxycarbonylpiperazin-1-yl)-2-((6-((3s)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl)amino)-3-oxopropyl)phosphonic acid
1159500-34-1
act-246475
1-piperazinecarboxylic acid, 4-[(2r)-2-[[[6-[(3s)-3-methoxy-1-pyrrolidinyl]-2-phenyl-4-pyrimidinyl]carbonyl]amino]-1-oxo-3-phosphonopropyl]-, 1-butyl ester
DB15163
CHEMBL4297589
7Y5 ,
((r)-3-(4-(butoxycarbonyl)piperazin-1-yl)-2-(6-((s)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carboxamido)-3-oxopropyl)phosphonic acid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Selatogrel was safe and well-tolerated with transient dyspnoea occurring overall in 7% (16/229) of patients (95% confidence interval: 4-11%)."( Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y12 receptor antagonist, in patients with chronic coronary syndromes.
Angiolillo, DJ; Bernaud, C; Dangas, GD; Frenoux, JM; Gorog, DA; Gurbel, PA; Hmissi, A; James, SK; Kunadian, V; Storey, RF; Tanguay, JF; Ten Berg, J; Tran, H; Trenk, D; Ufer, M; Van der Harst, P; Van't Hof, AWJ, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" Non-compartmental pharmacokinetic analysis was performed."( A new reversible and potent P2Y12 receptor antagonist (ACT-246475): tolerability, pharmacokinetics, and pharmacodynamics in a first-in-man trial.
Astruc, B; Baldoni, D; Bruderer, S; Dingemanse, J; Gueret, P; Gutierrez, M; Krause, A, 2014
)
0.65
"5 h post-dose, terminal half-life (t ½) was ~10 h."( A new reversible and potent P2Y12 receptor antagonist (ACT-246475): tolerability, pharmacokinetics, and pharmacodynamics in a first-in-man trial.
Astruc, B; Baldoni, D; Bruderer, S; Dingemanse, J; Gueret, P; Gutierrez, M; Krause, A, 2014
)
0.65
" Pharmacodynamic responders were defined as patients having P2Y12 reaction units (PRU) <100 at 30 min post-dose and lasting ≥3 h."( Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y12 receptor antagonist, in patients with chronic coronary syndromes.
Angiolillo, DJ; Bernaud, C; Dangas, GD; Frenoux, JM; Gorog, DA; Gurbel, PA; Hmissi, A; James, SK; Kunadian, V; Storey, RF; Tanguay, JF; Ten Berg, J; Tran, H; Trenk, D; Ufer, M; Van der Harst, P; Van't Hof, AWJ, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" Exploratory formulations enhanced the bioavailability and antiplatelet effect of ACT-246475."( A new reversible and potent P2Y12 receptor antagonist (ACT-246475): tolerability, pharmacokinetics, and pharmacodynamics in a first-in-man trial.
Astruc, B; Baldoni, D; Bruderer, S; Dingemanse, J; Gueret, P; Gutierrez, M; Krause, A, 2014
)
0.88

Dosage Studied

ExcerptRelevanceReference
" Moreover, equivalent antithrombotic dosing regimens of ticagrelor and clopidogrel reduced laser-induced calcium mobilization in the endothelium, restricted neutrophil adhesion and subsequent fibrin formation and thus reduced fibrin-mediated stabilization of the hemostatic seals."( Selatogrel, a reversible P2Y12 receptor antagonist, has reduced off-target interference with haemostatic factors in a mouse thrombosis model.
Caroff, E; Crescence, L; Darbousset, R; Dubois, C; Hubler, F; Panicot-Dubois, L; Riederer, MA, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's2 (12.50)24.3611
2020's14 (87.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.52

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 Index11.52 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (35.29%)5.53%
Reviews2 (11.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (52.94%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]