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 Source	ID
PubMed CID	59534142
CHEMBL ID	4297589
SCHEMBL ID	2928412
MeSH ID	M000609964

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

Excerpt	Reference	Relevance
" 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

Excerpt	Reference	Relevance
" 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

Excerpt	Reference	Relevance
" 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

Excerpt	Relevance	Reference
" 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	2 (12.50)	24.3611
2020's	14 (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.

Metric	This Compound (vs All)
Research Demand Index	11.52 (24.57)
Research Supply Index	3.18 (2.92)
Research Growth Index	4.69 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.52)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	6 (35.29%)	5.53%
Reviews	2 (11.76%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	9 (52.94%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
adenosine monophosphate Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.	2.41	1	0	adenosine 5'-phosphate; purine ribonucleoside 5'-monophosphate	adenosine A1 receptor agonist; cofactor; EC 3.1.3.1 (alkaline phosphatase) inhibitor; EC 3.1.3.11 (fructose-bisphosphatase) inhibitor; fundamental metabolite; micronutrient; nutraceutical
clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.	6.02	2	2	methyl ester; monochlorobenzenes; thienopyridine	anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor
organophosphonates hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.	10.39	16	6	divalent inorganic anion; phosphite ion
ticagrelor Ticagrelor: An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION.. ticagrelor : A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.	6.02	2	2	aryl sulfide; hydroxyether; organofluorine compound; secondary amino compound; triazolopyrimidines	P2Y12 receptor antagonist; platelet aggregation inhibitor
prasugrel hydrochloride Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels.	4.62	1	1
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	4.55	1	1	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Liver Dysfunction [description not available]	0	2.41	1	0
Liver Diseases Pathological processes of the LIVER.	1	4.41	1	0
Symptom Cluster [description not available]	0	4.96	2	1
Syndrome A characteristic symptom complex.	0	4.96	2	1
Acute Coronary Syndrome An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.	0	3.9	3	0
Blood Clot [description not available]	0	3.6	2	0
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	0	3.6	2	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	4.55	1	1
Cardiovascular Stroke [description not available]	0	4.96	2	1
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	1	6.96	2	1

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