Compounds > per977
Page last updated: 2024-11-13

per977

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

Description

PER977: a factor Xa inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71576543
CHEMBL ID3544919
SCHEMBL ID14985871
MeSH IDM000600479

Synonyms (29)

Synonym
SCHEMBL14985871
unii-u2r67kv65q
per 977
n1,n1'-(piperazine-1,4-diylbis(propane-1,3-diyl))bis-l-argininamide
u2r67kv65q ,
ciraparantag
per977
pentanamide, n,n'-(1,4-piperazinediyldi-3,1-propanediyl)bis(2-amino-5-((aminoiminomethyl)amino)-, (2s,2's)-
per-977
1438492-26-2
aripazine
ciraparantag [usan]
ciraparantag [who-dd]
ciraparantag [inn]
CHEMBL3544919
HY-18660
AKOS030526536
CS-5640
ciraparantag (usan)
D10868
ciraparantag(per977)
DB15199
Q27290602
(2s,2's)-n,n'-(piperazine-1,4-diylbis(propane-3,1-diyl))bis(2-amino-5-guanidinopentanamide)
1438492-26-2 (free base)
(2s)-2-amino-n-[3-[4-[3-[[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]propyl]piperazin-1-yl]propyl]-5-(diaminomethylideneamino)pentanamide
pentanamide, n,n'-(1,4-piperazinediyldi-3,1-propanediyl)bis[2-amino-5-[(aminoiminomethyl)amino]-, (2s,2's)-
(2s)-2-amino-n-[3-(4-{3-[(2s)-2-amino-5-carbamimidamidopentanamido]propyl}piperazin-1-yl)propyl]-5-carbamimidamidopentanamide
DTXSID701045783

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The no observable adverse effect level (NOAEL) for 14-day intravenous exposure to both rats and dogs was 20 mg/kg/d."( Nonclinical Safety Assessment of PER977: A Small Molecule Reversal Agent for New Oral Anticoagulants and Heparins.
Bakhru, S; Gad, SC; Laulicht, B; Steiner, S; Sullivan, DW, )		0.41
"Ciraparantag reverses the whole blood clotting time induced by enoxaparin in a dose related manner and produces no procoagulant signal or deleterious adverse events in doses up to 300mg."( Ciraparantag safely and completely reverses the anticoagulant effects of low molecular weight heparin.
Ansell, JE; Bakhru, SH; Costin, JC; Hoffman, M; Laulicht, BE; Steiner, SS, 2016)		0.43
" Potentially related adverse events were periorbital and facial flushing and cool sensation following IV injection of ciraparantag."( Single-dose ciraparantag safely and completely reverses anticoagulant effects of edoxaban.
Ansell, JE; Bakhru, SH; Brown, K; Costin, JC; Dishy, V; Grosso, MA; Lanz, HJ; Laulicht, BE; Mercuri, MF; Noveck, RJ; Steiner, SS, 2017)		0.46

Pharmacokinetics

ExcerptReferenceRelevance
" Ciraparantag reaches maximum concentration within minutes after IV administration with a half-life of 12 to 19 minutes."( Ciraparantag, an anticoagulant reversal drug: mechanism of action, pharmacokinetics, and reversal of anticoagulants.
Ansell, J; Baker, C; Bakhru, SH; Burnett, A; Chen, L; Jiang, X; Laulicht, BE; Steiner, S; Villano, S, 2021)		0.62

Dosage Studied

ExcerptRelevanceReference
" Nonetheless, the absence of the ability for clinicians to assess compliance or washout with a simple laboratory test (or to adjust dosing with a similar assessment) and the absence of an antidote to rapidly stop major hemorrhage or to enhance safety in the setting of emergent or urgent surgery/procedures have been limitations to greater non-vitamin K antagonist oral anticoagulant usage and better thromboembolic prevention."( NOAC monitoring, reversal agents, and post-approval safety and effectiveness evaluation: A cardiac safety research consortium think tank.
Kaminskas, E; Reiffel, JA; Reilly, P; Sager, P; Sarich, T; Seltzer, J; Weitz, JI, 2016)		0.43
" In addition to familiarity with the dosing and monitoring of vitamin K antagonists, clinicians are accustomed to using vitamin K if there is a need to reverse the anticoagulant effect of vitamin K antagonists."( Management of Bleeding With Non-Vitamin K Antagonist Oral Anticoagulants in the Era of Specific Reversal Agents.
Antman, EM; Giugliano, RP; Ruff, CT, 2016)		0.43
"Ciraparantag provides a dose-related reversal of anticoagulation induced by steady-state dosing of apixaban or rivaroxaban."( Ciraparantag reverses the anticoagulant activity of apixaban and rivaroxaban in healthy elderly subjects.
Ansell, J; Bakhru, S; Freedman, D; Laulicht, BE; Tracey, G; Villano, S, 2022)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1823248Binding affinity to heparin (unknown origin) assessed as apparent dissociation constant by SPR assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Dynamic Combinatorial Optimization of
AID1823251Inhibition of heparin (unknown origin) assessed as reversal of heparin reduced FXa protease activity by measuring Z-D-LGR-N(Me)ANBA peptide substrate at 1 uM hydrolysis after 30 mins2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Dynamic Combinatorial Optimization of
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (45)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's37 (82.22)24.3611
2020's8 (17.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.28

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 Index18.28 (24.57)
Research Supply Index3.91 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (6.52%)5.53%
Reviews31 (67.39%)6.00%
Case Studies1 (2.17%)4.05%
Observational0 (0.00%)0.25%
Other11 (23.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
beta-alanine
[no description available]		3.1910amino acid zwitterion;
beta-amino acid		agonist;
fundamental metabolite;
human metabolite;
inhibitor;
neurotransmitter
dalteparin
Dalteparin: A low-molecular-weight fragment of heparin, prepared by nitrous acid depolymerization of porcine mucosal heparin. The mean molecular weight is 4000-6000 daltons. It is used therapeutically as an antithrombotic agent. (From Merck Index, 11th ed)		3.6320
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		13.1443arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
thiazoles
[no description available]		9.22911,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
dabigatran
Dabigatran: A THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.. dabigatran : An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism.		9.22181aromatic amide;
benzimidazoles;
beta-alanine derivative;
carboxamidine;
pyridines		anticoagulant;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
EC 3.4.21.5 (thrombin) inhibitor
vitamin k semiquinone radical
vitamin K semiquinone radical: found in active preparations of vitamin K-dependent carboxylase. vitamin K : Any member of a group of fat-soluble 2-methyl-1,4-napthoquinones that exhibit biological activity against vitamin K deficiency. Vitamin K is required for the synthesis of prothrombin and certain other blood coagulation factors.		4.4630
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		8.62131aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
apixaban
[no description available]		8.54121aromatic ether;
lactam;
piperidones;
pyrazolopyridine		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
betrixaban
betrixaban: a highly potent, selective, and orally efficacious factor Xa inhibitor; structure in first source. betrixaban : A secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade.		3.3110benzamides;
guanidines;
monochloropyridine;
monomethoxybenzene;
secondary carboxamide		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
edoxaban
edoxaban : A monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism.		14.2291chloropyridine;
monocarboxylic acid amide;
tertiary amino compound;
thiazolopyridine		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor;
platelet aggregation inhibitor
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		3.3110benzenes;
hydroxycoumarin;
methyl ketone
ConditionIndicatedRelationship StrengthStudiesTrials
Bleeding
[description not available]		09.66261
Hemorrhage
Bleeding or escape of blood from a vessel.		09.66261
Nasal Bleeding
[description not available]		02.2510
Epistaxis
Bleeding from the nose.		02.2510
Thromboembolism, Venous
[description not available]		05.0240
Venous Thromboembolism
Obstruction of a vein or VEINS (embolism) by a blood clot (THROMBUS) in the blood stream.		17.0240
Hypercoagulability
[description not available]		03.0610
Apoplexy
[description not available]		05.5460
Thrombophilia
A disorder of HEMOSTASIS in which there is a tendency for the occurrence of THROMBOSIS.		03.0610
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		05.5460
Blood Loss, Postoperative
[description not available]		03.9420
Blood Loss, Surgical
Loss of blood during a surgical procedure.		03.0910
Brain Hemorrhage
[description not available]		03.9520
Blood Pressure, High
[description not available]		03.0910
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		03.0910
Intracranial Hemorrhages
Bleeding within the SKULL, including hemorrhages in the brain and the three membranes of MENINGES. The escape of blood often leads to the formation of HEMATOMA in the cranial epidural, subdural, and subarachnoid spaces.		03.9520
Auricular Fibrillation
[description not available]		04.5530
Cardiac Diseases
[description not available]		03.1210
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		04.5530
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		03.1210
Thromboembolism
Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.		03.920
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		03.4520
Blood Clot
[description not available]		02.1510
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		02.1510
Coagulation Disorders, Blood
[description not available]		03.0410
Blood Coagulation Disorders
Hemorrhagic and thrombotic disorders that occur as a consequence of abnormalities in blood coagulation due to a variety of factors such as COAGULATION PROTEIN DISORDERS; BLOOD PLATELET DISORDERS; BLOOD PROTEIN DISORDERS or nutritional conditions.		03.0410
Injuries
Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.		03.0410
Wounds and Injuries
Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.		03.0410
Emergencies
Situations or conditions requiring immediate intervention to avoid serious adverse results.		03.0410