cangrelor profile

cangrelor: platelet P(2T) receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cangrelor : A nucleoside triphosphate analogue that is 5'-O-[({[dichloro(phosphono)methyl](hydroxy)phosphoryl}oxy)(hydroxy)phosphoryl]adenosine carrying additional 2-(methylsulfanyl)ethyl and (3,3,3-trifluoropropyl)sulfanyl substituents at positions N6 and C2 respectively. Used (in the form of its tetrasodium salt) as an intravenous antiplatelet drug that prevents formation of harmful blood clots in the coronary arteries. [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]

ID Source	ID
PubMed CID	9854012
CHEMBL ID	334966
CHEBI ID	90841
SCHEMBL ID	6113860
MeSH ID	M0421877

Synonym
n(6)-(2-methylthioethyl)-2-(3,3,3-trifluoropropylthio)-5'-adenylic acid monoanhydride with dichloromethylenebis(phosphonic acid)
kengreal
arl69931
[dichloro-[[[(2r,3s,4r,5r)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid
gtpl1776
D03359
163706-06-7
cangrelor (usan/inn)
cangrelor
ar-c69931xx
CHEMBL334966 ,
arl 69931mx
bdbm50118225
6aq1y404u7 ,
hsdb 8489
unii-6aq1y404u7
(dichloromethylene)diphosphonic n-(2-(methylsulfanyl)ethyl)-2-((3,3,3-trifluoropropyl)sulfanyl-5'-adenylic monoanhydride
cangrelor [usan:inn:ban]
5'-adenylic acid, n-(2-(methylthio)ethyl)-2-((3,3,3-trifluoropropyl)thio)-, monoanhydride with (dichloromethylene)bis(phosphonic acid)
cangrelor [who-dd]
5'-adenylicacid, n-(2-(methylthio)ethyl)-2-((3,3,3-trifluoropropyl)thio)-, monoanhydride with (dichloromethylene)bis(phosphonic acid)
cangrelor [usan]
cangrelor [mi]
cangrelor [orange book]
cangrelor [inn]
CHEBI:90841 ,
SCHEMBL6113860
5'-o-[({[dichloro(phosphono)methyl](hydroxy)phosphoryl}oxy)(hydroxy)phosphoryl]-n-[2-(methylsulfanyl)ethyl]-2-[(3,3,3-trifluoropropyl)sulfanyl]adenosine
AM85616
5'-adenylicacid,n-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]-,anhydridewithp,p'-(dichloromethylene)bis[phosphonicacid](1:1)
AC-28809
DTXSID90167651 ,
DB06441
cangrelor free acid
(dichloro((((((2r,3s,4r,5r)-3,4-dihydroxy-5-(6-((2-(methylthio)ethyl)amino)-2-((3,3,3-trifluoropropyl)thio)-9h-purin-9-yl)tetrahydrofuran-2-yl)methoxy)(hydroxy)phosphoryl)oxy)(hydroxy)phosphoryl)methyl)phosphonic acid
Q3655338
ar-c 69931
cangrelor; kengreal
NCGC00480787-02
163706-06-7 (free acid)
[dichloro({[({[(2r,3s,4r,5r)-3,4-dihydroxy-5-(6-{[2-(methylsulfanyl)ethyl]amino}-2-[(3,3,3-trifluoropropyl)sulfanyl]-9h-purin-9-yl)oxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy](hydroxy)phosphoryl})methyl]phosphonic acid
EN300-19634462
paebivwumlrpsk-idtavkcvsa-n
HY-19638
CS-0016143
b01ac25
cangrelorum
5'-o-((((dichloro(phosphono)methyl)(hydroxy)phosphoryl)oxy)(hydroxy)phosphoryl)-n-(2-(methylsulfanyl)ethyl)-2-((3,3,3-trifluoropropyl)sulfanyl)adenosine
(dichloro-((((2r,3s,4r,5r)-3,4-dihydroxy-5-(6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl)oxolan-2-yl)methoxy-hydroxyphosphoryl)oxy-hydroxyphosphoryl)methyl)phosphonic acid
dtxcid8090142

Excerpt	Reference	Relevance
"Cangrelor is an intravenous P2Y12 inhibitor that is an attractive option due its favorable pharmacokinetic profile and ease of measurability but optimal dosing remains unclear."	( Characterization of antiplatelet response to low-dose cangrelor utilizing platelet function testing in neuroendovascular patients. Boulos, AS; Bush, MC; Dalfino, JC; Entezami, P; Field, NC; Holden, DN; Paul, AR; Yamamoto, J, 2021)	1.59
"Cangrelor is a P2Y12 inhibitor antiplatelet agent, with a rapid onset and offset. "	( Long-Term Cangrelor Administration in Neurology Intensive Care: A Case Series. Abdennour, L; Clarencon, F; Degos, V; Drir, M; Duranteau, O; Frère, C; Jacquens, A, 2023)	2.76
"Cangrelor is an intravenous direct-acting P2Y12 platelet receptor antagonist that achieves therapeutic effect and eliminates rapidly."	( Novel Use of Cangrelor With Heparin During Cardiopulmonary Bypass in Patients With Heparin-Induced Thrombocytopenia Who Require Cardiovascular Surgery: A Case Series. Banks, DA; Gernhofer, YK; Golts, E; Pretorius, V, )	1.22
"Cangrelor is a P2Y12 inhibitor that does not require liver CYP activation."	( Evaluation of the Newly Developed Adenosine Diphosphate-Induced Platelet Aggregation Level System in Aggregometer on Automated Coagulation Analyzer. Arai, N; Enomoto, Y; Ishida, H; Kitano, K; Komiyama, Y; Omori, Y; Sakayori, T; Uematsu, K; Watanabe, Y, 2019)	1.24
"Cangrelor is a rapid onset and potent intravenous P2Y12 inhibitor that has been shown in large randomized controlled trials to reduce periprocedural complications for PCI compared with clopidogrel, the most commonly used P2Y12 inhibitor."	( Cangrelor in clinical use. Feng, KY; Mahaffey, KW, 2020)	2.72
"Cangrelor is an intravenously administered P2Y"	( Cangrelor use in a 6-year-old patient undergoing complex percutaneous coronary intervention after post-surgical myocardial infarction. Leonardi, S; Marianeschi, SM; Morici, N; Pedrazzini, G; Sirico, D; Soriano, F; Vignati, G, 2020)	3.44
"Cangrelor is an intravenous P2Y12 receptor inhibitor with a rapid onset/offset of action and a short half-life (3-6 min). "	( Cangrelor and Stenting in Acute Ischemic Stroke : Monocentric Case Series. Alamowitch, S; Clarençon, F; Degos, V; Drir, M; Elhorany, M; Frasca Polara, G; Godier, A; Lenck, S; Mahtout, J; Premat, K; Samson, Y; Shotar, E; Sourour, NA, 2021)	3.51
"Cangrelor is an intravenous P2Y12 inhibitor with a favorable pharmacokinetic profile for use during neuroendovascular stenting."	( Cangrelor dose titration using platelet function testing during cerebrovascular stent placement. Boulos, AS; Dalfino, JC; Entezami, P; Field, NC; Holden, DN; Nourollahzadeh, E; Paul, AR; Yamamoto, J, 2021)	2.79
"Cangrelor is a promising alternative to currently available therapies, especially in patients with a high hemorrhagic risk."	( Cangrelor dose titration using platelet function testing during cerebrovascular stent placement. Boulos, AS; Dalfino, JC; Entezami, P; Field, NC; Holden, DN; Nourollahzadeh, E; Paul, AR; Yamamoto, J, 2021)	3.51
"Cangrelor is a potent, intravenous (IV), P2Y12-receptor antagonist with a rapid onset and offset presented as an alternative antiplatelet agent."	( The use of cangrelor in neurovascular interventions: a multicenter experience. Aghaebrahim, A; Aguilar-Salinas, P; Clarençon, F; Cortez, GM; Dabus, G; Elhorany, M; Grigoryan, M; Hanel, RA; Linfante, I; Mirza, S; Monteiro, A; Murtaza, Y; Sauvageau, E; Sourour, N, 2021)	1.73
"IV cangrelor is a relatively new antiplatelet that was initially approved for coronary interventions."	( Use of intravenous cangrelor and stenting in acute ischemic stroke interventions: a new single center analysis and pooled-analysis of current studies. Boulos, A; Dalfino, J; Entezami, P; Field, N; Holden, D; Paul, AR, 2021)	1.46
"Cangrelor is a promising agent in this setting, and additional studies are warranted to confirm our findings."	( A Multicenter Preliminary Study of Cangrelor following Thrombectomy Failure for Refractory Proximal Intracranial Occlusions. Bourcier, R; Chalumeau, V; Clarençon, F; Consoli, A; Darcourt, J; Dargazanli, C; Delvoye, F; Desilles, JP; Elhorany, M; Finitsis, S; Gariel, F; Gory, B; Lapergue, B; Marnat, G; Mazighi, M; Richard, S; Sibon, I, 2021)	1.62
"Cangrelor is a reversible P2Y12 inhibitor that is administered as an intravenous infusion, and its quick onset and offset make it an appealing option for antiplatelet therapy, particularly for patients who are unable to take oral medications."	( Cangrelor: A New Route for P2Y12 Inhibition. Nawarskas, JJ; Sible, AM, )	2.3
"Cangrelor is an intravenous adenosine diphosphate (ADP) P2Y12 receptor antagonist, which has to be administered as a bolus followed by immediate infusion. "	( Pharmacosimulation of interruptions and its solution in intravenous administration of cangrelor. Heramvand, N; Jung, C; Kelm, M; Kollmann, M; Masyuk, M; Muessig, JM; Nia, AM; Polzin, A, 2018)	2.15
"Cangrelor is a novel P2Y12-receptor inhibitor which is administrated intravenously and thus allows immediate antiplatelet inhibition during PCI."	( What is the Role of Cangrelor in Patients Undergoing PCI? Droppa, M; Geisler, T, 2018)	1.53
"Cangrelor is an intravenous P2Y"	( Antiplatelet Therapy Bridging With Cangrelor in Patients With Coronary Stents: A Case Series. Bowman, S; Gass, J; Weeks, P, 2019)	2.23
"Cangrelor is an intravenous adenosine triphosphate analog P2Y12 receptor antagonist with a short plasma half-life that has been used off label in patients with recent coronary stents as a bridge to invasive procedures with excessive bleeding risk."	( Use of Cangrelor as a Bridge to Left Ventricular Assist Device Implantation in a Patient with a Recent Drug-Eluting Stent Who Developed Acute Tirofiban-Related Thrombocytopenia. Boyle, AJ; Danelich, IM; Entwistle, JW; Kabadi, RA; Marhefka, GD; Qureshi, AM; Reeves, G, 2019)	1.69
"Cangrelor is a potent intravenous adenosine diphosphate (ADP)-receptor antagonist that acts rapidly and has quickly reversible effects."	( Effect of platelet inhibition with cangrelor during PCI on ischemic events. Angiolillo, DJ; Bhatt, DL; Bramucci, E; Gallup, D; Généreux, P; Gibson, CM; Hamm, CW; Harrington, RA; Leonardi, S; Liu, T; Mahaffey, KW; McLaurin, BT; Prats, J; Price, MJ; Radke, PW; Skerjanec, S; Spriggs, D; Steg, PG; Stone, GW; Tauth, J; Todd, M; Tousek, F; White, HD; Widimský, P, 2013)	1.39
"Cangrelor is an intravenous P2Y12 inhibitor under investigation as an antiplatelet drug in the setting of acute coronary syndromes. "	( Electrocardiographic safety of cangrelor, a new intravenous antiplatelet agent: a randomized, double-blind, placebo- and moxifloxacin-controlled thorough QT study. Bellibas, SE; Green, CL; Krucoff, MW; Lambe, L; Prats, J; Whellan, DJ; Wijngaard, P, 2013)	2.12
"Cangrelor is a potent, rapid-acting, reversible intravenous platelet inhibitor that was tested for percutaneous coronary intervention (PCI) in three large, double-blind, randomised trials. "	( Effect of cangrelor on periprocedural outcomes in percutaneous coronary interventions: a pooled analysis of patient-level data. Bhatt, DL; Day, JR; French, WJ; Gibson, CM; Gogia, HS; Gruberg, L; Hamm, CW; Harrington, RA; Iwaoka, RS; Leonardi, S; Liu, T; Mahaffey, KW; Skerjanec, S; Steg, PG; Stone, GW; Stuckey, TD; White, HD, 2013)	2.23
"Cangrelor is a new parenteral adenosine diphosphate P2Y12 receptor inhibitor with rapid, profound and reversible inhibition of platelet activity. "	( Cangrelor for patients undergoing percutaneous coronary intervention: evidence from a meta-analysis of randomized trials. Chatterjee, S; Mushiyev, S; Nairooz, R; Pekler, G; Sardar, P; Visco, F, 2014)	3.29
"Cangrelor is a new antiplatelet agent that has been used in percutaneous coronary intervention (PCI) with mixed results. "	( Cangrelor versus clopidogrel in percutaneous coronary intervention: a systematic review and meta-analysis. Aryal Pandit, A; Aryal, MR; Hakim, FA; Jalota, L; Lee, HR; Mookadam, F; Pandit, A; Tleyjeh, IM, 2014)	3.29
"Cangrelor is a reversible, potent, intravenous, competitive inhibitor of the ADP P2Y12 receptor that rapidly achieves near complete and predictable platelet inhibition."	( Cangrelor: a review on pharmacology and clinical trial development. Angiolillo, DJ; Cho, JR; Franchi, F; Muñiz-Lozano, A; Rollini, F, 2013)	2.55
"Cangrelor is a potent, intravenous, direct-acting P2Y12 antagonist with rapid onset and quickly reversible action. "	( Cangrelor: an emerging therapeutic option for patients with coronary artery disease. Andruszkiewicz, A; Fabiszak, T; Gurbel, PA; Jeong, YH; Kozinski, M; Kubica, A; Kubica, J; Navarese, EP; Siller-Matula, JM; Tantry, U, 2014)	3.29
"Cangrelor is an intravenous agent that provides rapid and intensive inhibition of the P2Y12 receptor that quickly dissipates after discontinuation."	( Cangrelor for treatment of arterial thrombosis. Price, MJ; Walsh, JA, 2014)	2.57
"Cangrelor is an important addition to the current armamentarium of platelet inhibitors as it significantly reduces periprocedural myocardial infarction and stent thrombosis in a broad spectrum of patients, without increasing major bleeding or the need for transfusion. "	( Cangrelor for treatment of arterial thrombosis. Price, MJ; Walsh, JA, 2014)	3.29
"Cangrelor is a potent intravenous P2Y12 receptor inhibitor."	( Pharmacodynamic effects of cangrelor on platelet P2Y12 receptor-mediated signaling in prasugrel-treated patients. Angiolillo, DJ; Bass, TA; Cho, JR; Darlington, A; Desai, B; Ferreiro, JL; Franchi, F; Guzman, LA; Muñiz-Lozano, A; Patel, R; Rollini, F; Tello-Montoliu, A; Zenni, MM, 2014)	1.42
"Cangrelor is an intravenous antagonist of P2Y12 and its use will require transition to and from oral agents."	( Pharmacodynamic effects during the transition between cangrelor and ticagrelor. Agarwal, Z; Gogo, P; Keating, FK; Schneider, DJ; Seecheran, N, 2014)	2.09
"Cangrelor is an intravenous ATP analog that directly, selectively and reversibly inhibits P2Y12 receptors on platelets."	( Cangrelor for treatment during percutaneous coronary intervention. Dobesh, PP; Oestreich, JH, 2014)	2.57
"Cangrelor is an intravenous, non-thienopyridine antagonist of the P2Y12 receptor with a rapid, potent, predictable, and quickly reversible effect."	( Cangrelor: review of the drug and the CHAMPION programme (including PHOENIX). Leonardi, S; Marino, M; Rizzotti, D, 2014)	2.57
"Cangrelor is a potent intravenous P2Y12 inhibitor with rapid onset and offset. "	( Outcomes with cangrelor versus clopidogrel on a background of bivalirudin: insights from the CHAMPION PHOENIX (A Clinical Trial Comparing Cangrelor to Clopidogrel Standard Therapy in Subjects Who Require Percutaneous Coronary Intervention [PCI]). Bhatt, DL; Cortese, B; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Liu, T; Mahaffey, KW; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD; Wilensky, M, 2015)	2.22
"Cangrelor is a novel, intravenous, short-acting, reversible platelet P2Y12 inhibitor, which has been evaluated for the treatment of arterial thrombosis."	( Cangrelor for the treatment of arterial thrombosis: pharmacokinetics/pharmacodynamics and clinical data. Guasti, L; Riva, N; Squizzato, A; Tamborini Permunian, E, 2015)	2.58
"Cangrelor is a potent intravenous platelet P2Y12 receptor antagonist with rapid onset and offset of action."	( Impact of cangrelor overdosing on bleeding complications in patients undergoing percutaneous coronary intervention: insights from the CHAMPION trials. Angiolillo, DJ; Bhatt, DL; Gibson, CM; Hamm, CW; Harrington, RA; Liu, T; Mahaffey, KW; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD, 2015)	1.54
"Cangrelor is a rapid-acting, direct-binding, and reversible P2Y12 antagonist which has been studied for use during percutaneous coronary intervention (PCI) in patients with or without pretreatment with an oral P2Y12 antagonist. "	( Cangrelor inhibits the binding of the active metabolites of clopidogrel and prasugrel to P2Y12 receptors in vitro. Buckland, RJ; Jakubowski, JA; Judge, HM; Storey, RF, 2016)	3.32
"Cangrelor is an intravenous, direct-acting, reversible, potent P2Y12 receptor antagonist. "	( A Safety Evaluation of Cangrelor in Patients Undergoing PCI. Angiolillo, DJ; Franchi, F; Park, Y; Rollini, F, 2016)	2.19
"Cangrelor is an intravenous ADP receptor antagonist that leads to potent and reversible inhibition of platelet aggregation. "	( Efficacy and Safety of Cangrelor in Women Versus Men During Percutaneous Coronary Intervention: Insights From the Cangrelor versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition (CHAMPION PHOENIX) Trial. Bhatt, DL; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Liu, T; Mahaffey, KW; O'Donoghue, ML; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD, 2016)	2.19
"Cangrelor is an intravenous, reversibly-binding platelet P2Y12 receptor antagonist with ultra-rapid onset and offset of action that is approved in Europe and United States for use in patients undergoing PCI."	( Cangrelor for the management and prevention of arterial thrombosis. Sinha, A; Storey, RF, 2016)	2.6
"Cangrelor is an intravenous P2Y12 inhibitor approved to reduce periprocedural ischemic events in patients undergoing percutaneous coronary intervention not pretreated with a P2Y12 inhibitor."	( Consistent Reduction in Periprocedural Myocardial Infarction With Cangrelor as Assessed by Multiple Definitions: Findings From CHAMPION PHOENIX (Cangrelor Versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition). Bhatt, DL; Cavender, MA; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Leonardi, S; Mahaffey, KW; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD, 2016)	2.11
"Cangrelor is an intravenous P2Y12 receptor antagonist that provides a rapid onset and maximal platelet inhibition, which is quickly reversible."	( Optimizing the Use of Cangrelor in the Real World. Bhatt, DL; Qamar, A, 2017)	1.49
"Cangrelor is a potent intravenous adenosine diphosphate-receptor antagonist that in the CHAMPION trials reduced the 48-hour and 30-day rates of ischemic events during percutaneous coronary intervention without an increase in severe bleeding."	( Impact of Cerebrovascular Events Older Than One Year on Ischemic and Bleeding Outcomes With Cangrelor in Percutaneous Coronary Intervention. Bhatt, DL; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Mahaffey, KW; Prats, J; Price, MJ; Sawlani, NN; Steg, PG; Stone, GW; White, HD, 2017)	2.12
"Cangrelor is a recently developed P2Y(12) inhibitor that has the advantage of being an active drug not requiring metabolic conversion, although it is not orally available."	( Cangrelor attenuates coated-platelet formation. Dale, GL; Hann, CL; Norgard, NB, )	2.3
"Cangrelor is a potent, competitive inhibitor of the P2Y12 receptor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation."	( Cangrelor: a novel P2Y12 receptor antagonist. Norgard, NB, 2009)	2.52
"Cangrelor (AR-C69931MX) is an intravenous, direct-acting and reversible P2Y(12) receptor antagonist."	( Cangrelor: a review on its mechanism of action and clinical development. Angiolillo, DJ; Ferreiro, JL; Ueno, M, 2009)	2.52
"Cangrelor is an intravenously administered P2Y12 inhibitor that does not need metabolic conversion to an active metabolite for its antiplatelet action, and as a consequence exhibits a more potent and consistent antiplatelet profile as compared to clopidogrel."	( The influence of variation in the P2Y12 receptor gene on in vitro platelet inhibition with the direct P2Y12 antagonist cangrelor. Bouman, HJ; de Maat, MP; Hackeng, CM; Kruit, A; Leebeek, FW; Rudez, G; Ruven, HJ; Ten Berg, JM; van Werkum, JW, 2010)	1.29
"Cangrelor is a reversible, potent, competitive inhibitor of the ADP P2Y(12) receptor that is administered intravenously and rapidly achieves near complete inhibition of ADP-induced platelet aggregation."	( Update on the clinical development of cangrelor. Angiolillo, DJ; Ferreiro, JL; Ueno, M, 2010)	1.35
"Cangrelor is an intravenous direct and reversible inhibitor of the P2Y(12) receptor providing the highest level of inhibition and elinogrel is an intravenous and oral P2Y(12) antagonist with a direct and reversible action."	( [Myocardial infarction: Role of new antiplatelet agents]. Bellemain, A; Collet, JP; Ecollan, P; Montalescot, G; Silvain, J, 2011)	1.09
"Cangrelor is an intravenous antagonist of the P2Y(12) receptor characterized by rapid, potent, predictable, and reversible platelet inhibition. "	( Pharmacodynamic effects of cangrelor and clopidogrel: the platelet function substudy from the cangrelor versus standard therapy to achieve optimal management of platelet inhibition (CHAMPION) trials. Angiolillo, DJ; Becker, RC; Bhatt, DL; French, WJ; Harrington, RA; Huber, K; Liu, T; Prats, J; Price, MJ; Saucedo, JF; Schneider, DJ; Shaburishvili, T, 2012)	2.12
"Cangrelor is an intravenous, potent, and reversible P2Y(12) inhibitor with fast onset and offset of action."	( Rationale and design of the Cangrelor versus standard therapy to acHieve optimal Management of Platelet InhibitiON PHOENIX trial. Bhatt, DL; Dietrich, M; Gallup, D; Gibson, CM; Hamm, CW; Harrington, RA; Leonardi, S; Liu, T; Mahaffey, KW; Price, MJ; Skerjanec, S; Steg, GW; Stone, GW; Todd, M; White, HD, 2012)	1.39
"Cangrelor is a P2Y12 antagonist under development for treatment of acute coronary syndrome. "	( Cangrelor for treatment of coronary thrombosis. Cudd, LA; Fugate, SE, 2006)	3.22
"Cangrelor is a promising investigational medication for inhibition of platelet aggregation in acute arterial coronary events. "	( Cangrelor for treatment of coronary thrombosis. Cudd, LA; Fugate, SE, 2006)	3.22
"Cangrelor is a direct, parenteral, and reversible inhibitor of the platelet P2Y12 receptor currently undergoing Phase III testing. "	( Transitioning patients from cangrelor to clopidogrel: pharmacodynamic evidence of a competitive effect. Akers, WS; Charnigo, R; Ferraris, S; Oestreich, JH; Oh, JJ; Steinhubl, SR, 2008)	2.08
"Cangrelor is a direct-acting reversible antagonist being developed for short-term infusion; clopidogrel and prasugrel are oral prodrugs that provide irreversible inhibition via transient formation of active metabolites."	( The reversible P2Y antagonist cangrelor influences the ability of the active metabolites of clopidogrel and prasugrel to produce irreversible inhibition of platelet function. Dovlatova, NL; Heptinstall, S; Jakubowski, JA; Sugidachi, A, 2008)	1.36

Excerpt	Reference	Relevance
"Cangrelor has a potentially favorable pharmacodynamic profile in cardiogenic shock (CS). "	( Cangrelor in cardiogenic shock and after cardiopulmonary resuscitation: A global, multicenter, matched pair analysis with oral P2Y Bhatt, DL; de Waha-Thiele, S; Desch, S; Droppa, M; Fuernau, G; Gawaz, M; Geisler, T; Hack, L; Jaffer, FA; Ouarrak, T; Qamar, A; Rath, D; Roberts, RJ; Schneider, S; Singh, A; Szumita, PM; Thiele, H; Vaduganathan, M; Venkateswaran, RV; Zeymer, U, 2019)	3.4
"Cangrelor has a rapid onset and offset of action and achieves significantly greater degrees of platelet inhibition compared with clopidogrel."	( Cangrelor: a review on its mechanism of action and clinical development. Angiolillo, DJ; Ferreiro, JL; Ueno, M, 2009)	2.52
"Cangrelor has been used for antiplatelet bridging in perioperative settings or for patients unable to take oral medications. "	( Safety of Intravenous Cangrelor Administration for Antiplatelet Bridging in Hospitalized Patients: A Retrospective Study. Acker, MA; Domenico, C; Fanaroff, AC; Horton, ER; Johnson, BV; Kolansky, DM; Nathan, AS, 2021)	2.38
"Cangrelor has been studied in a broad population intended to receive PCI in the CHAMPION program, where it was compared with different clopidogrel regimens."	( Cangrelor: review of the drug and the CHAMPION programme (including PHOENIX). Leonardi, S; Marino, M; Rizzotti, D, 2014)	2.57
"Cangrelor has been tested in patients with coronary artery diseases undergoing percutaneous coronary intervention and as bridging therapy for patients undergoing coronary artery bypass graft. "	( Cangrelor for the treatment of arterial thrombosis: pharmacokinetics/pharmacodynamics and clinical data. Guasti, L; Riva, N; Squizzato, A; Tamborini Permunian, E, 2015)	3.3
"Cangrelor has been studied as an intravenous infusion in doses of 2 or 4 microg/kg/min."	( Cangrelor for treatment of coronary thrombosis. Cudd, LA; Fugate, SE, 2006)	2.5

Excerpt	Reference	Relevance
"Cangrelor treatment was associated with similar bleeding risk and significantly better TIMI flow improvement compared with oral P2Y"	( Cangrelor in cardiogenic shock and after cardiopulmonary resuscitation: A global, multicenter, matched pair analysis with oral P2Y Bhatt, DL; de Waha-Thiele, S; Desch, S; Droppa, M; Fuernau, G; Gawaz, M; Geisler, T; Hack, L; Jaffer, FA; Ouarrak, T; Qamar, A; Rath, D; Roberts, RJ; Schneider, S; Singh, A; Szumita, PM; Thiele, H; Vaduganathan, M; Venkateswaran, RV; Zeymer, U, 2019)	3.4
"Treatment with cangrelor reduced the incidence of MI at 48 hours (3.8% versus 4.7%; odds ratio [OR], 0.80; 95% confidence interval [CI], 0.67-0.97; P=0.02)."	( Consistent Reduction in Periprocedural Myocardial Infarction With Cangrelor as Assessed by Multiple Definitions: Findings From CHAMPION PHOENIX (Cangrelor Versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition). Bhatt, DL; Cavender, MA; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Leonardi, S; Mahaffey, KW; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD, 2016)	1.01

Excerpt	Reference	Relevance
" There were no deaths at 30 days and no serious adverse events attributed to AR-C69931MX."	( Open multicentre study of the P2T receptor antagonist AR-C69931MX assessing safety, tolerability and activity in patients with acute coronary syndromes. Oldroyd, KG; Storey, RF; Wilcox, RG, 2001)	0.31
" Four patients receiving AR-C69931MX discontinued treatment due to minor bleeding events, and 5 patients receiving placebo discontinued treatment due to other adverse events or deterioration in their condition."	( Safety profile and tolerability of intravenous AR-C69931MX, a new antiplatelet drug, in unstable angina pectoris and non-Q-wave myocardial infarction. Ellborg, M; Jacobsson, F; Swahn, E; Wallentin, L, 2002)	0.31
"As adjunctive therapy to aspirin and low-molecular-weight heparin in patients with unstable angina or non-Q-wave MI, intravenous AR-C69931MX was well tolerated, with no difference in the incidence of serious adverse events compared with placebo."	( Safety profile and tolerability of intravenous AR-C69931MX, a new antiplatelet drug, in unstable angina pectoris and non-Q-wave myocardial infarction. Ellborg, M; Jacobsson, F; Swahn, E; Wallentin, L, 2002)	0.31
" Bleeding and adverse clinical events were comparable among the groups."	( Preliminary experience with intravenous P2Y12 platelet receptor inhibition as an adjunct to reduced-dose alteplase during acute myocardial infarction: results of the Safety, Tolerability and Effect on Patency in Acute Myocardial Infarction (STEP-AMI) angi Borzak, S; Emanuelsson, H; Gibson, CM; Greenbaum, AB; Le May, MR; Lu, M; Ohman, EM; Stankowski, JE; Stebbins, AL; Weaver, WD, 2007)	0.34
" QTcI was not affected by plasma concentrations of cangrelor metabolites, and cangrelor had no other adverse effects on electrocardiographic parameters."	( Electrocardiographic safety of cangrelor, a new intravenous antiplatelet agent: a randomized, double-blind, placebo- and moxifloxacin-controlled thorough QT study. Bellibas, SE; Green, CL; Krucoff, MW; Lambe, L; Prats, J; Whellan, DJ; Wijngaard, P, 2013)	0.93
"In CHAMPION PHOENIX, cangrelor reduced the odds of major adverse cardiovascular events and stent thrombosis in women and men and appeared to offer greater net clinical benefit than clopidogrel."	( Efficacy and Safety of Cangrelor in Women Versus Men During Percutaneous Coronary Intervention: Insights From the Cangrelor versus Standard Therapy to Achieve Optimal Management of Platelet Inhibition (CHAMPION PHOENIX) Trial. Bhatt, DL; Deliargyris, EN; Gibson, CM; Hamm, CW; Harrington, RA; Liu, T; Mahaffey, KW; O'Donoghue, ML; Prats, J; Price, MJ; Steg, PG; Stone, GW; White, HD, 2016)	1.06
" The primary outcome of this retrospective cohort study was the incidence of bleeding events defined by the global use of strategies to open occluded coronary arteries criteria, and the secondary outcomes include the transfusion requirements, inpatient major cardiac adverse events, and cost savings per patient."	( Safety and Efficacy of Periprocedural Bridging With Cangrelor Versus Eptifibatide. Ji, CS; Roberts, RJ; Solomon, EJ; Toyoda, AY; Yun, AN, 2022)	0.97

Excerpt	Reference	Relevance
"In pharmacodynamic studies with antiplatelet agents, platelets are usually activated in vitro with single agonists (e."	( Pharmacodynamic profile of antiplatelet agents: marked differences between single versus costimulation with platelet activators. Graff, J; Harder, S; Klinkhardt, U, 2004)	0.32
"Because a variety of different agonists influence platelet activation and its distinct functions at a time, investigations which regard the concert of these agonists might be closer to the in vivo situation and better reflect the pharmacodynamic profile of an antiplatelet agent than using one single inducing agent."	( Pharmacodynamic profile of antiplatelet agents: marked differences between single versus costimulation with platelet activators. Graff, J; Harder, S; Klinkhardt, U, 2004)	0.32
" The infusion is continued for 60 minutes, and serial blood samples are obtained for evaluation of pharmacokinetic and pharmacodynamic parameters."	( Pharmacokinetics and pharmacodynamics of a bolus and infusion of cangrelor: a direct, parenteral P2Y12 receptor antagonist. Akers, WS; Ferraris, S; Oestreich, JH; Oh, JJ; Steinhubl, SR; Wethington, M, 2010)	0.6
" A prospectively designed platelet function substudy was performed in a selected cohort of patients to provide insight into the pharmacodynamic effects of cangrelor, particularly in regard to whether cangrelor therapy may interfere with the inhibitory effects of clopidogrel."	( Pharmacodynamic effects of cangrelor and clopidogrel: the platelet function substudy from the cangrelor versus standard therapy to achieve optimal management of platelet inhibition (CHAMPION) trials. Angiolillo, DJ; Becker, RC; Bhatt, DL; French, WJ; Harrington, RA; Huber, K; Liu, T; Prats, J; Price, MJ; Saucedo, JF; Schneider, DJ; Shaburishvili, T, 2012)	0.87
"As ticagrelor, clopidogrel and cangrelor therapies may be used in the same clinical setting, their potential pharmacodynamic interactions are of interest."	( Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model. Emanuelsson, BM; Ravnefjord, A; van Giezen, JJ; Weilitz, J, 2012)	0.66
" No pharmacodynamic interaction occurred between ticagrelor and cangrelor."	( Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model. Emanuelsson, BM; Ravnefjord, A; van Giezen, JJ; Weilitz, J, 2012)	0.62
"The extent of the pharmacodynamic drug-drug interactions observed between clopidogrel and cangrelor or ticagrelor apparently depends on the level of receptor occupancy when clopidogrel is administered."	( Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model. Emanuelsson, BM; Ravnefjord, A; van Giezen, JJ; Weilitz, J, 2012)	0.6
"Platelets from patients with diabetes mellitus (DM) are hyper-reactive and whether cangrelor, a potent intravenous P2Y(12) receptor blocker, has differential pharmacodynamic (PD) effects according DM status is unknown."	( Effects of cangrelor in coronary artery disease patients with and without diabetes mellitus: an in vitro pharmacodynamic investigation. Angiolillo, DJ; Bass, TA; Capodanno, D; Capranzano, P; Darlington, A; Desai, B; Dharmashankar, K; Ferreiro, JL; Guzman, LA; Rollini, F; Tello-Montoliu, A; Tomasello, SD; Ueno, M, 2013)	1
"This study sought to determine pharmacodynamic effects during transition from intravenous cangrelor to oral ticagrelor and from oral ticagrelor to intravenous cangrelor."	( Pharmacodynamic effects during the transition between cangrelor and ticagrelor. Agarwal, Z; Gogo, P; Keating, FK; Schneider, DJ; Seecheran, N, 2014)	0.87
" Pharmacodynamic effects (light transmission platelet aggregation in response to 20 and 5 μmol/l adenosine diphosphate, VerifyNow, P2Y12 assay (Accumetrics, San Diego, California), vasodilator-stimulated phosphoprotein index, and flow cytometry) were assessed during and after the cangrelor infusion."	( Pharmacodynamic effects during the transition between cangrelor and ticagrelor. Agarwal, Z; Gogo, P; Keating, FK; Schneider, DJ; Seecheran, N, 2014)	0.83
"Ticagrelor given before or during infusion of cangrelor did not attenuate the pharmacodynamic effects of cangrelor."	( Pharmacodynamic effects during the transition between cangrelor and ticagrelor. Agarwal, Z; Gogo, P; Keating, FK; Schneider, DJ; Seecheran, N, 2014)	0.91
"The aim of this study was to determine the impact of cangrelor and prasugrel on the pharmacodynamic effects of each agent."	( Pharmacodynamic effects during the transition between cangrelor and prasugrel. Gogo, P; Keating, FK; Raza, SS; Schneider, DJ; Seecheran, N, 2015)	0.92
" Pharmacodynamic effects (light transmission platelet aggregation in response to 20 μmol/l ADP, VerifyNow, and flow cytometry) were assessed during and after the cangrelor infusion."	( Pharmacodynamic effects during the transition between cangrelor and prasugrel. Gogo, P; Keating, FK; Raza, SS; Schneider, DJ; Seecheran, N, 2015)	0.86
" Pharmacodynamic studies have shown that this interaction is avoided when clopidogrel is given at the end of the cangrelor infusion."	( Pharmacodynamic Effects When Clopidogrel is Given Before Cangrelor Discontinuation. Agarwal, Z; Gogo, P; Schneider, DJ; Seecheran, N, 2015)	0.87

Excerpt	Reference	Relevance
" In conclusion, cangrelor in combination with ticagrelor results in consistent and strong P2Y12 inhibition during and after infusion and cangrelor may bridge the gap until oral P2Y12 inhibitors achieve effect in real-world STEMI patients undergoing primary PCI."	( Cangrelor in combination with ticagrelor provides consistent and potent P2Y12-inhibition during and after primary percutaneous coronary intervention in real-world patients with ST-segment-elevation myocardial infarction. Andell, P; Erlinge, D; Götberg, M; James, S; Koul, S; Mohammad, MA; Scherstén, F, 2017)	2.24

Excerpt	Reference	Relevance
" We highlighted a mechanism triggered mainly by the increased extracellular bioavailability of adenosine, which activates A2B and A3 receptors on the endothelium."	( Ticagrelor Prevents Endothelial Cell Apoptosis through the Adenosine Signalling Pathway in the Early Stages of Hypoxia. Brassart-Pasco, S; Djerada, Z; Feliu, C; Millart, H; Nguyen, P; Oszust, F; Peyret, H; Poitevin, G, 2020)	0.56

Excerpt	Relevance	Reference
" In addition, AYPGKF- and thrombin-induced TXA2 generation was significantly reduced in platelets from mice dosed with clopidogrel, confirming the results obtained with the human platelets."	( P2Y12 receptor-mediated potentiation of thrombin-induced thromboxane A2 generation in platelets occurs through regulation of Erk1/2 activation. Garcia, A; Kim, S; Kunapuli, SP; Prabhakar, J; Shankar, H, 2006)	0.33
"Two hundred patients (3 dosage groups and placebo) were studied in part 1, and 199 additional patients were then randomized in the second part, comparing 1 dose of cangrelor and abciximab."	( Initial experience with an intravenous P2Y12 platelet receptor antagonist in patients undergoing percutaneous coronary intervention: results from a 2-part, phase II, multicenter, randomized, placebo- and active-controlled trial. Becker, RC; Bittl, JA; Clegg, J; Emanuelsson, H; Gilchrist, IC; Greenbaum, AB; Grines, CL; Grogan, DR; Harrington, RA; Kereiakes, DJ; Stankowski, JE; Weaver, WD, 2006)	0.53
"To review and assess available literature on the chemistry, pharmacology, pharmacodynamics, pharmacokinetics, clinical studies, adverse events, drug interactions, special populations, and dosing and administration for cangrelor, a product in late stage Phase II clinical trials."	( Cangrelor for treatment of coronary thrombosis. Cudd, LA; Fugate, SE, 2006)	1.96
" Despite the unambiguous clinical benefit associated with clopidogrel, accumulating experience with this drug has also led to identification of some of its drawbacks, which are related to inadequate platelet inhibition with standard dosage regimens as well as to its irreversible antiplatelet effects."	( ADP receptor antagonism: what's in the pipeline? Angiolillo, DJ, 2007)	0.34
" Twenty-two healthy volunteers are randomized to receive 1 of 2 intravenous cangrelor dosing regimens: a 15-microg/kg bolus followed by a 2-microg/kg/min infusion or a 30-microg/kg bolus followed by a 4-microg/kg/min infusion."	( Pharmacokinetics and pharmacodynamics of a bolus and infusion of cangrelor: a direct, parenteral P2Y12 receptor antagonist. Akers, WS; Ferraris, S; Oestreich, JH; Oh, JJ; Steinhubl, SR; Wethington, M, 2010)	0.83
"Six male dogs all received 7 different dosing regimens separated by 1-5week washout periods: cangrelor (1μg/kg/min, intravenous infusion); ticagrelor (0."	( Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model. Emanuelsson, BM; Ravnefjord, A; van Giezen, JJ; Weilitz, J, 2012)	0.6
" With clopidogrel dosed 3hours after ticagrelor, IPA was reduced after washout of ticagrelor to 38% at 24hrs vs."	( Evaluation of ticagrelor pharmacodynamic interactions with reversibly binding or non-reversibly binding P2Y(12) antagonists in an ex-vivo canine model. Emanuelsson, BM; Ravnefjord, A; van Giezen, JJ; Weilitz, J, 2012)	0.38
" Additionally, we calculated the optimal dosage of a second bolus."	( Pharmacosimulation of interruptions and its solution in intravenous administration of cangrelor. Heramvand, N; Jung, C; Kelm, M; Kollmann, M; Masyuk, M; Muessig, JM; Nia, AM; Polzin, A, 2018)	0.7
" Additionally, we estimate the dosage of a possible second bolus which highly depends on the duration of the delay."	( Pharmacosimulation of interruptions and its solution in intravenous administration of cangrelor. Heramvand, N; Jung, C; Kelm, M; Kollmann, M; Masyuk, M; Muessig, JM; Nia, AM; Polzin, A, 2018)	0.7
" We report two cases of patients with AMI complicating ischemic stroke, successfully treated with cangrelor infusion, which was started during PCI and maintained up to 48 h at bridge therapy dosage (0."	( Acute myocardial infarction complicating ischemic stroke: is there room for cangrelor? Leonardi, S; Meani, P; Morici, N; Nava, S; Oliva, F; Oreglia, J; Ranucci, M; Rossini, R; Sacco, A; Viola, G, 2020)	1
" Larger studies should evaluate alternative dosing regimens."	( Clinical Use of Cangrelor After Percutaneous Coronary Intervention in Patients Requiring Mechanical Circulatory Support. Altshuler, D; Arnouk, S; Katz, A; Lewis, TC; Merchan, C; Papadopoulos, J; Smith, DE; Toy, B, 2021)	0.97
" More research is needed to determine the ideal dosing regimen."	( Use of intravenous cangrelor and stenting in acute ischemic stroke interventions: a new single center analysis and pooled-analysis of current studies. Boulos, A; Dalfino, J; Entezami, P; Field, N; Holden, D; Paul, AR, 2021)	0.95
" Cangrelor is an intravenous P2Y12 inhibitor that is an attractive option due its favorable pharmacokinetic profile and ease of measurability but optimal dosing remains unclear."	( Characterization of antiplatelet response to low-dose cangrelor utilizing platelet function testing in neuroendovascular patients. Boulos, AS; Bush, MC; Dalfino, JC; Entezami, P; Field, NC; Holden, DN; Paul, AR; Yamamoto, J, 2021)	1.78
" More research is needed to determine the ideal dosing regimen."	( Use of intravenous cangrelor in the treatment of ruptured and unruptured cerebral aneurysms: an updated single-center analysis and pooled analysis of current studies. Boulos, AS; Dalfino, JC; Entezami, P; Field, NC; Holden, DN; Najera, E; Paul, AR; Rock, AK; Yamamoto, J, 2023)	1.24

Role	Description
platelet aggregation inhibitor	A drug or agent which antagonizes or impairs any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system.
P2Y12 receptor antagonist	An antagonist at the P2Y12 receptor
[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]

Class	Description
nucleoside triphosphate analogue
organofluorine compound	An organofluorine compound is a compound containing at least one carbon-fluorine bond.
aryl sulfide	Any organic sulfide in which the sulfur is attached to at least one aromatic group.
organochlorine compound	An organochlorine compound is a compound containing at least one carbon-chlorine bond.
secondary amino compound	A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
adenosine 5'-phosphate
[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]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.1100	7.1903	10.0000	AID1449628
Ornithine decarboxylase	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0004	0.0004	0.0177	0.0350	AID150496
P2Y purinoceptor 12	Homo sapiens (human)	IC50 (µMol)	0.0043	0.0004	1.0489	10.0000	AID1232263; AID1267340; AID1298771; AID150496; AID1850679
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	P2Y purinoceptor 12	Homo sapiens (human)
monoatomic ion transport	P2Y purinoceptor 12	Homo sapiens (human)
substrate-dependent cell migration, cell extension	P2Y purinoceptor 12	Homo sapiens (human)
G protein-coupled receptor signaling pathway	P2Y purinoceptor 12	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	P2Y purinoceptor 12	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	P2Y purinoceptor 12	Homo sapiens (human)
hemostasis	P2Y purinoceptor 12	Homo sapiens (human)
calcium-mediated signaling	P2Y purinoceptor 12	Homo sapiens (human)
cerebral cortex radial glia-guided migration	P2Y purinoceptor 12	Homo sapiens (human)
cell projection organization	P2Y purinoceptor 12	Homo sapiens (human)
lamellipodium assembly	P2Y purinoceptor 12	Homo sapiens (human)
platelet activation	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of integrin activation by cell surface receptor linked signal transduction	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of cell adhesion mediated by integrin	P2Y purinoceptor 12	Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathway	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of monoatomic ion transport	P2Y purinoceptor 12	Homo sapiens (human)
response to axon injury	P2Y purinoceptor 12	Homo sapiens (human)
regulation of chemotaxis	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of chemotaxis	P2Y purinoceptor 12	Homo sapiens (human)
establishment of localization in cell	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	P2Y purinoceptor 12	Homo sapiens (human)
platelet aggregation	P2Y purinoceptor 12	Homo sapiens (human)
cellular response to ATP	P2Y purinoceptor 12	Homo sapiens (human)
visual system development	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of ruffle assembly	P2Y purinoceptor 12	Homo sapiens (human)
regulation of microglial cell migration	P2Y purinoceptor 12	Homo sapiens (human)
positive regulation of microglial cell migration	P2Y purinoceptor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
G protein-coupled adenosine receptor activity	P2Y purinoceptor 12	Homo sapiens (human)
G protein-coupled ADP receptor activity	P2Y purinoceptor 12	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	P2Y purinoceptor 12	Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activity	P2Y purinoceptor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
plasma membrane	P2Y purinoceptor 12	Homo sapiens (human)
cell surface	P2Y purinoceptor 12	Homo sapiens (human)
membrane	P2Y purinoceptor 12	Homo sapiens (human)
cell projection membrane	P2Y purinoceptor 12	Homo sapiens (human)
cell body membrane	P2Y purinoceptor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID157724	Platelet P2T receptor antagonist activity in human platelet assay	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy.
AID1267341	Agonist activity at human platelet P2X1 receptor assessed as increase in cytosolic calcium level at 1 uM by FLURO-4 staining based flow cytometric analysis relative to beta,gamma-CH2-ATP	2016	European journal of medicinal chemistry, Jan-01, Volume: 107	New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.
AID1232263	Antagonist activity at P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced aggregation preincubated for 5 mins followed by ADP addition by turbidimetric analysis	2015	Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14	GPCR crystal structures: Medicinal chemistry in the pocket.
AID1267340	Antagonist activity at human platelet P2Y12 receptor assessed as inhibition of ADP-mediated decrease in intra-platelet phosphorylated VASP by FLUO-4 staining based flow cytometric analysis	2016	European journal of medicinal chemistry, Jan-01, Volume: 107	New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.
AID1449628	Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID196346	Recovery of ADP-induced platelet aggregation 20 minutes post dose. mean of four determinations and spread of results	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy.
AID1298771	Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by turbidimetric method	2016	Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12	State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.
AID150496	The compound was evaluated for antagonist activity against platelet P2Y purinoceptor 12 (P2Y12)	2002	Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19	Purine and pyrimidine (P2) receptors as drug targets.
AID1850679	Inhibition of P2Y12 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Strategies for targeting the P2Y
AID1346320	Human P2Y12 receptor (P2Y receptors)	2002	Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19	Purine and pyrimidine (P2) receptors as drug targets.
AID1346305	Human P2Y13 receptor (P2Y receptors)	2003	Molecular pharmacology, Jul, Volume: 64, Issue:1	Pharmacological characterization of the human P2Y13 receptor.
AID1346320	Human P2Y12 receptor (P2Y receptors)	2001	Molecular pharmacology, Sep, Volume: 60, Issue:3	Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
AID1346857	Mouse GPR17 (Class A Orphans)	2008	PloS one, , Volume: 3, Issue:10	The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	1 (0.24)	18.2507
2000's	103 (25.12)	29.6817
2010's	224 (54.63)	24.3611
2020's	82 (20.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	54 (12.92%)	5.53%
Reviews	99 (23.68%)	6.00%
Case Studies	27 (6.46%)	4.05%
Observational	5 (1.20%)	0.25%
Other	233 (55.74%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (32)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
PharmacOdynaMic Effects of Cangrelor in PatiEnts wIth Acute or chronIc Coronary Syndrome Undergoing Percutaneous Coronary Intervention (POMPEII Registry) [NCT04790032]		100 participants (Anticipated)	Observational [Patient Registry]	2021-03-16	Recruiting
Platelet Inhibition With Cangrelor in Comatose Survivors of Out-of-hospital Cardiac Arrest Undergoing Primary Percutaneous Coronary Intervention [NCT04005729]	Phase 4	30 participants (Actual)	Interventional	2019-07-01	Completed
Proximal Internal Carotid Artery Acute Stroke Secondary to Tandem or Local Occlusion Thrombectomy Trial [NCT05611242]	Phase 3	404 participants (Anticipated)	Interventional	2023-11-01	Recruiting
MONET BRIDGE(Maintenance Of aNtiplatElet Therapy in Patients With Coronary Stenting Undergoing Surgery) - (Mantenimento Della Terapia Antiaggregante Nei Pazienti Portatori di Stent Coronarico Candidati a Chirurgia) [NCT03862651]	Phase 2	140 participants (Anticipated)	Interventional	2019-06-01	Not yet recruiting
Dutch Cangrelor Registry [NCT04138641]		250 participants (Actual)	Observational [Patient Registry]	2019-12-17	Completed
Effects of Cangrelor on MIcRovAscular Disfunction During Elective Percutaneous CORonary Intervention [NCT06089577]	Phase 4	80 participants (Anticipated)	Interventional	2023-10-31	Not yet recruiting
A Prospective, Open-Label, Single-Arm, Multi-Center Study To Assess The Pharmacokinetics/Pharmacodynamics (PK/PD) And Safety Of Different Cangrelor Doses In Neonatal Subjects At Risk Of Thrombosis [NCT02765633]	Phase 1	22 participants (Actual)	Interventional	2017-01-03	Completed
A Study of the Transition From IV Cangrelor to Oral Prasugrel, and Prasugrel to Cangrelor, in Patients With Coronary Artery Disease. [NCT01852019]	Phase 2	12 participants (Actual)	Interventional	2013-06-30	Completed
Cangrelor Versus Ticagrelor In Patients With Acute Myocardial Infarction Complicated With Initial Cardiogenic Shock [NCT03551964]	Phase 4	550 participants (Anticipated)	Interventional	2018-08-01	Recruiting
The Effect of Intravenous Cangrelor and Oral Ticagrelor on Platelets, the Microcirculation and Myocardial Damage in Patients Admitted With STEMI Treated by Primary Percutaneous Coronary Intervention: A Randomized Controlled Pilot Trial [NCT02733341]	Phase 4	100 participants (Actual)	Interventional	2016-07-21	Completed
A Double Blind, Placebo Controlled, Positive Controlled, Randomized, Crossover Study to Assess the Effect of Cangrelor at the Therapeutic Dose and a Supratherapeutic Dose Level on the QT/QTc Interval in Healthy Volunteers [NCT00699504]	Phase 1	67 participants (Actual)	Interventional	2008-06-30	Completed
Pharmacodynamic and Pharmacokinetic Profiles of Switching Between Cangrelor and Ticagrelor Following Ticagrelor Pre-treatment: The Switching Antiplatelet -5 (SWAP-5) Study [NCT04634162]	Phase 4	22 participants (Actual)	Interventional	2021-02-09	Completed
Pharmacokinetic/Pharmacodynamic Effects of add-on Antiplatelet Therapy With Parenteral Cangrelor as Compared to Standard Dual Antiplatelet Treatment in Patients With ST-elevation Myocardial Infarction Complicated by Out-of-hospital Cardiac Arrest and Trea [NCT03273075]	Phase 4	60 participants (Anticipated)	Interventional	2017-09-30	Recruiting
Cangrelor Administration Following Ticagrelor Loading vs Ticagrelor Loading Alone in ST Segment Elevation Myocardial Infarction Patients: A Randomized, Pharmacodynamic Study [NCT02943369]	Phase 4	30 participants (Actual)	Interventional	2017-07-28	Completed
A Clinical Trial Comparing Cangrelor to Clopidogrel in Subjects Who Require Percutaneous Coronary Intervention (PCI). [NCT00305162]	Phase 3	8,882 participants (Actual)	Interventional	2006-04-30	Terminated(stopped due to Insufficient evidence of the clinical effectiveness of cangrelor)
The Pharmacokinetics and Pharmacodynamics of a Cangrelor Bolus Plus Infusion in Healthy Volunteers [NCT00102674]	Phase 1	40 participants	Interventional	2005-03-31	Completed
Facilitation Through Aggrastat or Cangrelor Bolus and Infusion Over prasugreL: a mUlticenter Randomized Open-label Trial in patientS With ST-elevation Myocardial inFarction Referred for primAry percutaneouS inTERvention.FABOLUS FASTER Trial [NCT02978040]	Phase 4	122 participants (Actual)	Interventional	2017-07-04	Completed
A Study of the Transition From Cangrelor to Clopidogrel or Prasugrel in Patients With Coronary Artery Disease. [NCT01979445]	Phase 2	15 participants (Actual)	Interventional	2013-12-02	Completed
BRIDGE: Maintenance of Platelet inihiBition With cangRelor After dIscontinuation of ThienopyriDines in Patients Undergoing surGEry [NCT00767507]	Phase 2	221 participants (Actual)	Interventional	2008-10-31	Completed
A Study of the Transition From Cangrelor to Ticagrelor, and Ticagrelor to Cangrelor in Patients With Coronary Artery Disease [NCT01766466]	Phase 2	12 participants (Actual)	Interventional	2013-01-31	Completed
Platelet Inhibition With CANgrelor and Crushed TICagrelor in STEMI Patients Undergoing Primary Percutaneous Coronary Intervention: The CANTIC Study [NCT03247738]	Phase 4	50 participants (Actual)	Interventional	2017-11-20	Completed
Multicenter, Observational, Retrospective Cohort Study of Patients at High Risk of Bleeding Undergoing Percutaneous Coronary Intervention and Treated With Intravenous Cangrelor Infusion (ICARUS) [NCT05505591]		900 participants (Anticipated)	Observational	2022-06-06	Recruiting
A Randomized, Pilot, Single-center Study, Investigator-Initiated Study to Look at an Aggressive Therapeutic Approach in Aspirin Resistant Patients Comparing to Standard for Patient Undergoing Percutaneous Coronary Intervention [NCT01103440]	Phase 2	36 participants (Actual)	Interventional	2007-04-30	Completed
Comparison of Pharmacodynamic Effects of Tirofiban vs. Cangrelor in N-STEMI Patients Undergoing Percutaneous Coronary Intervention [NCT03048019]		10 participants (Actual)	Observational	2017-08-23	Terminated(stopped due to study terminated per PI)
Periprocedural Cangrelor in Patients With ST-Elevation Myocardial Infarction to Reduce Development of Myocardial Necrosis [NCT03043274]	Phase 4	23 participants (Actual)	Interventional	2017-01-31	Terminated
Cangrelor vs. Ticagrelor for Early Platelet Inhibition in ST-elevation Myocardial Infarction [NCT03182855]	Phase 4	80 participants (Anticipated)	Interventional	2018-09-01	Not yet recruiting
A Clinical Trial Comparing Cangrelor to Clopidogrel Standard of Care Therapy in Subjects Who Require Percutaneous Coronary Intervention (CHAMPION PHOENIX) [NCT01156571]	Phase 3	11,145 participants (Actual)	Interventional	2010-09-30	Completed
REperfusion With P2Y12 Inhibitors in Addition to mEchanical thRombectomy for perFUsion Imaging Selected Acute Stroke patiEnts (REPERFUSE) [NCT04667078]	Phase 3	368 participants (Anticipated)	Interventional	2022-03-02	Recruiting
A Clinical Trial Comparing Treatment With Cangrelor (in Combination With Usual Care) to Usual Care, in Subjects Who Require Percutaneous Coronary Intervention (PCI). [NCT00385138]	Phase 3	5,364 participants (Actual)	Interventional	2006-09-30	Terminated(stopped due to Insufficient evidence of the clinical effectiveness of cangrelor)
Pharmacodynamic and Pharmacokinetic Profiles on Switching From Cangrelor to Prasugrel in Patients With Acute Coronary Syndrome Undergoing Percutaneous Coronary Intervention: The Switching Antiplatelet -6 (SWAP-6) Study [NCT04668144]	Phase 4	77 participants (Actual)	Interventional	2021-02-09	Completed
Evaluation of Myocardial Reperfusion and Residual Thrombotic Burden After Primary PCI for STEMI in Patients With High on Ticagrelor Platelet Reactivity Treated by IV Cangrelor Versus Ticagrelor Alone [NCT04927949]	Phase 4	128 participants (Actual)	Interventional	2021-06-08	Completed
Platelet Inhibition to Target Reperfusion Injury: The PITRI Trial [NCT03102723]	Phase 2	228 participants (Actual)	Interventional	2017-10-01	Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00305162 (17) [back to overview]	Incidence of All Cause Mortality
NCT00305162 (17) [back to overview]	Incidence of MI
NCT00305162 (17) [back to overview]	Incidence of Stroke
NCT00305162 (17) [back to overview]	Incidence of Thrombolysis in Myocardial Infarction (TIMI) Major Bleeding
NCT00305162 (17) [back to overview]	Individual Incidence of All-cause Mortality
NCT00305162 (17) [back to overview]	Individual Incidence of IDR
NCT00305162 (17) [back to overview]	Incidence of Abrupt Closure, Threatened Abrupt Closure, Need for Urgent Coronary Artery Bypass Graft (CABG) Surgery, or Unsuccessful Procedure During the Index PCI
NCT00305162 (17) [back to overview]	Incidence of ACUITY Major Bleeding
NCT00305162 (17) [back to overview]	Incidence of ACUITY Major Bleeding (Without Hematoma >/= 5 cm)
NCT00305162 (17) [back to overview]	Incidence of Stroke
NCT00305162 (17) [back to overview]	Incidence of All-cause Mortality
NCT00305162 (17) [back to overview]	Incidence of All-cause Mortality and MI
NCT00305162 (17) [back to overview]	Incidence of All-cause Mortality or MI
NCT00305162 (17) [back to overview]	Incidence of All-cause Mortality, MI or IDR
NCT00305162 (17) [back to overview]	Incidence of All-cause Mortality, Myocardial Infarction (MI), and Ischemia-driven Revascularization (IDR)
NCT00305162 (17) [back to overview]	Incidence of GUSTO Severe / Life-threatening Bleeding
NCT00305162 (17) [back to overview]	Incidence of IDR
NCT00385138 (20) [back to overview]	Incidence of IDR
NCT00385138 (20) [back to overview]	Incidence of ACUITY Major Bleeding
NCT00385138 (20) [back to overview]	Incidence of ACUITY Major Bleeding Without Hematoma >/= 5 cm
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality or MI
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality or MI
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality, MI, or IDR
NCT00385138 (20) [back to overview]	Incidence of All-cause Mortality, Myocardial Infarction (MI), and Ischemia-driven Revascularization (IDR)
NCT00385138 (20) [back to overview]	Incidence of GUSTO Severe / Life-threatening
NCT00385138 (20) [back to overview]	Incidence of IDR
NCT00385138 (20) [back to overview]	Incidence of MI
NCT00385138 (20) [back to overview]	Incidence of MI
NCT00385138 (20) [back to overview]	Incidence of Procedure Events [Abrupt Closure, Threatened Abrupt Closure, Need for Urgent Coronary Artery Bypass Graft (CABG) Surgery, Unsuccessful Procedure, New Thrombus or Suspected Thrombus, and/or Acute Stent Thrombosis]
NCT00385138 (20) [back to overview]	Incidence of Stent Thrombosis
NCT00385138 (20) [back to overview]	Incidence of Stent Thrombosis
NCT00385138 (20) [back to overview]	Incidence of Stroke
NCT00385138 (20) [back to overview]	Incidence of Stroke
NCT00385138 (20) [back to overview]	Incidence of Thrombolysis in Myocardial Infarction (TIMI) Major
NCT00767507 (6) [back to overview]	Incidence of Excessive Coronary Artery Bypass Graft (CABG)-Related Bleeding
NCT00767507 (6) [back to overview]	Patients With Blood Product Transfusions up to 7 Days After Surgery or Discharge, Whichever Was Sooner
NCT00767507 (6) [back to overview]	Stage I: Percentage of Patient Samples That Maintained Platelet Inhibition Levels of Greater Than or Equal to 60% as Reported by the VerifyNow P2Y12 Point of Care Assay.
NCT00767507 (6) [back to overview]	Stage II: The Percentage of Patients That Maintained Platelet Reaction Units (PRU) < 240, as Determined by the VerifyNow P2Y12 Point of Care Assay, Measured During Study Drug Infusion Pre-surgery.
NCT00767507 (6) [back to overview]	Non-CABG (Preoperative) Bleeding - Protocol-defined GUSTO Severe/Life-threatening, Moderate and Mild
NCT00767507 (6) [back to overview]	Stage II: Analysis of Platelet Reactivity (ITT Population) / Patients With Platelet Reactivity < 240 PRU
NCT01103440 (2) [back to overview]	Number of Participants With Major Adverse Cardiac Event (MACE)
NCT01103440 (2) [back to overview]	Number of Participants With Elevation of Cardiac Enzyme
NCT01156571 (3) [back to overview]	Individual Incidence of Stent Thrombosis (ST), Death, Myocardial Infarction (MI) and Ischemia-driven Revascularization (IDR)
NCT01156571 (3) [back to overview]	Incidence of Major/Minor Non-coronary Artery Bypass Graft (CABG)-Related Hemorrhage by Clinical Relevant Criteria - GUSTO Severe/Life-threatening, Moderate and Mild
NCT01156571 (3) [back to overview]	The Composite Incidence of All-cause Mortality, Myocardial Infarction (MI), Ischemia-driven Revascularization (IDR) and Stent Thrombosis (ST)
NCT01766466 (3) [back to overview]	Extent of Aggregation Response During Ticagrelor Treatment
NCT01766466 (3) [back to overview]	Extent of Preservation of Inhibitory Effect Compared With Effect Observed During Cangrelor Treatment After Ticagrelor
NCT01766466 (3) [back to overview]	Extent of Preservation of Inhibitory Effect Compared With Effect Observed With Cangrelor Alone (at Timepoint 1, Either at 0.5 Hours or 1.25 Hours) or Ticagrelor Alone (Measured 5.25 Hours After Initiation of Cangrelor on Day 1)
NCT01852019 (5) [back to overview]	Extent of Preservation of Inhibitory Effect After Transition From Cangrelor to Prasugrel Compared With Effect Observed With Prasugrel Alone (Reference Timepoint)
NCT01852019 (5) [back to overview]	Extent of Preservation of Inhibitory Effect of Cangrelor Treatment After Prasugrel, Compared to Treatment With Cangrelor Alone
NCT01852019 (5) [back to overview]	Extent of Preservation of Inhibitory Effect of Cangrelor Treatment After Prasugrel, Compared to Treatment With Cangrelor Alone
NCT01852019 (5) [back to overview]	Bleeding Events in Accordance With the GUSTO Scale
NCT01852019 (5) [back to overview]	Extent of Preservation of Inhibitory Effect After Transition From Cangrelor to Prasugrel Compared With Effect Observed With Prasugrel Alone (Reference Timepoint)
NCT01979445 (5) [back to overview]	Bleeding Events In Accordance With GUSTO Scale
NCT01979445 (5) [back to overview]	Extent of Preservation of Platelet Inhibitory Effect of Cangrelor Treatment After Prasugrel or Clopidogrel Compared to Treatment With Cangrelor Alone Determined By VerifyNow P2Y12 Assay
NCT01979445 (5) [back to overview]	Extent Of Preservation Of Platelet Inhibitory Effect Of Cangrelor Treatment After Prasugrel Or Clopidogrel Compared To Treatment With Cangrelor Alone
NCT01979445 (5) [back to overview]	Extent of Preservation Of Platelet Inhibitory Effect After Transition From Cangrelor to Prasugrel Or Clopidogrel Compared With Effect Observed With Prasugrel Or Clopidogrel Alone Determined By VerifyNow P2Y12 Assay
NCT01979445 (5) [back to overview]	Extent of Preservation Of Platelet Inhibitory Effect After Transition From Cangrelor To Prasugrel Or Clopidogrel Compared With Effect Observed With Prasugrel Or Clopidogrel Alone
NCT03043274 (6) [back to overview]	IFN-γ
NCT03043274 (6) [back to overview]	Macrophage-derived Chemokine
NCT03043274 (6) [back to overview]	Interferon (IFN)-α2
NCT03043274 (6) [back to overview]	Change in Myocardial Infarction Size
NCT03043274 (6) [back to overview]	Peripheral Blood Count Quantification
NCT03043274 (6) [back to overview]	Platelet Reactivity
NCT03048019 (4) [back to overview]	Adenosine Diphosphate (ADP) Induced Platelet Aggregation (%)
NCT03048019 (4) [back to overview]	Shear-induced Thrombus Formation (AUC)
NCT03048019 (4) [back to overview]	Thrombin Induced Platelet-fibrin Clot Strength (mm)
NCT03048019 (4) [back to overview]	Thrombin Receptor Activator Peptide (TRAP) Induced Platelet Aggregation (%)
NCT03247738 (2) [back to overview]	Platelet Reactivity Measured by Vasodilator-stimulated Phosphoprotein (VASP)
NCT03247738 (2) [back to overview]	Platelet Reactivity Measured by VerifyNow PRU
NCT04634162 (1) [back to overview]	Platelet Reactivity Measured by VerifyNow

Incidence of All Cause Mortality

(excluding STEMI) (NCT00305162)
Timeframe: randomization through 1 year after randomization

Intervention	participants (Number)
Cangrelor Arm	116
Clopidogrel Arm	120

Intervention	participants (Number)
	primary hemorrhagic	infarction with hemorrhagic conversion	cerebral infarction	uncertain type
Cangrelor Arm	1	0	5	0
Clopidogrel Arm	0	0	7	0

Intervention	Patients (Number)
Stage II - Cangrelor Arm (0.75 mcg/kg/Min)	12
Stage II - Placebo Arm	10
Stage I, Cohort I - Cangrelor 0.5 mcg/kg/Min	0
Stage I, Cohort II - Cangrelor 0.75 mcg/kg/Min	1

Intervention	patients (Number)
Stage II - Cangrelor Arm (0.75 mcg/kg/Min)	34
Stage II - Placebo Arm	35
Stage I, Cohort 1 - Cangrelor (0.5 mcg/kg/Min)	1
Stage I - Cohort II - Cangrelor 0.75 mcg/kg/Min	4

Intervention	percentage of samples (Number)
Stage I, Cohort I - Cangrelor 0.5 mcg/kg/Min	76.5
Stage I, Cohort II - Cangrelor 0.75 mcg/kg/Min	94.4

Intervention	Percent of patients (Number)
Stage II - Cangrelor Arm (0.75 mcg/kg/Min)	98.8
Stage II - Placebo Arm	19.0

Intervention	participants (Number)
	GUSTO severe/life threatening	GUSTO moderate	GUSTO mild
Stage I, Cohort 1 - Cangrelor 0.5 mcg/kg/Min	0	0	1
Stage I, Cohort II - Cangrelor 0.75 mcg/kg/Min	0	2	1
Stage II - Cangrelor (0.75 mcg/kg/Min)	2	10	8
Stage II - Placebo Arm	1	4	5

Intervention	percent of patients (Number)
	Prior to study drug infusion (washout period)	Last sample during infusion	Following discontinuation of study drug infusion
Stage II - Cangrelor Arm (0.75 mcg/kg/Min)	62.4	98.8	26.9
Stage II - Placebo Arm	52.3	31.0	20.0

Intervention	participants (Number)
	Stent Thrombosis	Death	MI (myocardial infarction)	IDR (ischemia-driven revascularization)
Cangrelor Treatment Arm	46	18	207	28
Clopidogrel Treatment Arm	74	18	255	38

Intervention	participants (Number)
	GUSTO severe/life threatening	GUSTO moderate	GUSTO severe or moderate	TIMI major	TIMI minor	TIMI major or minor	Any blood transfusion
Cangrelor Treatment Arm	9	22	31	5	9	14	25
Clopidogrel Treatment Arm	6	13	19	5	3	8	16

Intervention	percentage of platelet reactivity (PR) (Mean)
	Reference 5.25 hours - PR	2.25 hours - PR	2.5 hours - PR	2.75 hours - PR	3 hours - PR	4 hours - PR
All Patients	4	12	19	10	7.1	4.6
Cangrelor + Ticagrelor 180mg at 0.5 h of Cangrelor Infusion	5.8	13	16	12	10	6.7
Cangrelor + Ticagrelor 180mg at 1.25 h of Cangrelor Infusion	2.2	11	21	7.8	4.5	2.5

Intervention	percentage of platelet reactivity (PR) (Mean)
	1.0 hours - PR	2.0 hours - PR
All Patients	1.5	1.3
Ticagrelor Discontinued 12 h Prior to Cangrelor Infusion	1.5	1.5
Ticagrelor Discontinued 24 h Prior to Cangrelor Infusion	1.5	1.2

Intervention	percentage of platelet reactivity (PR) (Mean)
	Reference 0.5/1.25 hours - PR	1.75 hours - PR	2.0 hours - PR
All Patients	1.7	2.2	2.3
Cangrelor + Ticagrelor 180mg at 0.5 h of Cangrelor Infusion	2	2.3	3.5
Cangrelor + Ticagrelor 180mg at 1.25 h of Cangrelor Infusion	1.3	2	1.2

Intervention	% aggregation (Mean)
	Prasugrel Reference (6.0h or 5.5 h)	2.25 h	2.5 h	2.75 h	3.0 h	4.0 h
Day 1 - Cangrelor + Prasugrel (60mg) a 1.0h	5.0	45	62	69	51	15
Day 1 - Cangrelor + Prasugrel (60mg) at 1.5h	2.8	25	42	31	24	10
Day 1 - Cangrelor + Prasugrel (60mg) Post Infusion (2.0h)	1.0	27	56	64	58	1.0

Intervention	platelet reaction units (PRU) (Mean)
	1.0 h - PRU	2.0 h - PRU
Day 8 - Prasugrel (10mg) Dosing (5 Doses)	8.3	13
Day 8 - Prasugrel (10mg) Dosing (6 Doses)	6.3	4.7

Intervention	% aggregation (Mean)
	1.0 h	2.0 h
Day 8 - Prasugrel (10mg) Dosing (5 Doses)	1.3	1.0
Day 8 - Prasugrel (10mg) Dosing (6 Doses)	0.5	0.0

Intervention	participants (Number)
	Mild	Moderate	Life-threatening/Severe
Day 8 - Prasugrel (10mg) Dosing (5 Doses)	0	0	0
Day 8 - Prasugrel (10mg) Dosing (6 Doses)	1	0	0

Intervention	platelet reaction units (PRU) (Mean)
	Prasugrel Reference (6.0h or 5.5h) - PRU	2.25h - PRU	2.5h - PRU	2.75h - PRU	3.0h - PRU	4.0h - PRU
Day 1 - Cangrelor + Prasugrel (60mg) a 1.0h	74	151	269	285	242	117
Day 1 - Cangrelor + Prasugrel (60mg) at 1.5h	41	82	181	134	127	56
Day 1 - Cangrelor + Prasugrel (60mg) Post Infusion (2.0h)	7.7	91	242	267	239	20

Intervention	PRU (Mean)
	Cangrelor Reference (2.5, 2, 1.5, or 1 hrs)	1.75 hrs	2 hrs
Clopidogrel 1 Hr During Cangrelor	7.0	6.3	5.7
Clopidogrel 1.5 Hrs During Cangrelor	17.7	25.0	28.8
Clopidogrel Within 5 Min After Cangrelor	7.3	3.7	NA
Prasugrel 30 Min After Cangrelor	208.0	3.3	5.3

Intervention	PRU (Mean)
	Prasugrel/Clopidogrel Reference (6 or 5.5 hrs)	2.25 hrs	2.5 hrs	2.75 hrs	3 hrs	4 hrs	5.5 hrs
Clopidogrel 1 Hr During Cangrelor	197.3	98.7	206.3	214.3	212.7	203.7	NA
Clopidogrel 1.5 Hrs During Cangrelor	211.3	90.3	229.8	255.8	234.5	215.5	NA
Clopidogrel Within 5 Min Post Cangrelor	159.0	99.0	220.7	233.0	215.7	182.0	155.0
Prasugrel 30 Min After Cangrelor	8.0	76.7	208.0	225.7	226.0	77.0	24.5

Intervention	cells per microliter (Mean)
	granulocyte platelet aggregates	Monocyte-platelet aggregate
Cangrelor	1166.7	139.8
No Cangrelor	2550.4	333.9

cangrelor

Description

Cross-References

Synonyms (50)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (6)

Protein Targets (3)

Inhibition Measurements

Biological Processes (49)

Molecular Functions (12)

Ceullar Components (14)

Bioassays (13)

Research

Studies (410)

Market Indicators

Research Demand Index: 66.20

Study Types

Clinical Trials (32)

Trial Overview

Trial Outcomes

Incidence of All Cause Mortality

Incidence of MI

Incidence of Stroke

Incidence of Thrombolysis in Myocardial Infarction (TIMI) Major Bleeding

Individual Incidence of All-cause Mortality

Individual Incidence of IDR

Incidence of Abrupt Closure, Threatened Abrupt Closure, Need for Urgent Coronary Artery Bypass Graft (CABG) Surgery, or Unsuccessful Procedure During the Index PCI

Incidence of ACUITY Major Bleeding

Incidence of ACUITY Major Bleeding (Without Hematoma >/= 5 cm)

Incidence of Stroke

Incidence of All-cause Mortality

Incidence of All-cause Mortality and MI

Incidence of All-cause Mortality or MI

Incidence of All-cause Mortality, MI or IDR

Incidence of All-cause Mortality, Myocardial Infarction (MI), and Ischemia-driven Revascularization (IDR)

Incidence of GUSTO Severe / Life-threatening Bleeding

Incidence of IDR

Incidence of IDR

Incidence of ACUITY Major Bleeding

Incidence of ACUITY Major Bleeding Without Hematoma >/= 5 cm

Incidence of All-cause Mortality

Incidence of All-cause Mortality

Incidence of All-cause Mortality

Incidence of All-cause Mortality or MI

Incidence of All-cause Mortality or MI

Incidence of All-cause Mortality, MI, or IDR

Incidence of All-cause Mortality, Myocardial Infarction (MI), and Ischemia-driven Revascularization (IDR)

Incidence of GUSTO Severe / Life-threatening

Incidence of IDR

Incidence of MI

Incidence of MI

Incidence of Procedure Events [Abrupt Closure, Threatened Abrupt Closure, Need for Urgent Coronary Artery Bypass Graft (CABG) Surgery, Unsuccessful Procedure, New Thrombus or Suspected Thrombus, and/or Acute Stent Thrombosis]

Incidence of Stent Thrombosis

Incidence of Stent Thrombosis

Incidence of Stroke

Incidence of Stroke

Incidence of Thrombolysis in Myocardial Infarction (TIMI) Major

Incidence of Excessive Coronary Artery Bypass Graft (CABG)-Related Bleeding

Patients With Blood Product Transfusions up to 7 Days After Surgery or Discharge, Whichever Was Sooner

Stage I: Percentage of Patient Samples That Maintained Platelet Inhibition Levels of Greater Than or Equal to 60% as Reported by the VerifyNow P2Y12 Point of Care Assay.

Stage II: The Percentage of Patients That Maintained Platelet Reaction Units (PRU) < 240, as Determined by the VerifyNow P2Y12 Point of Care Assay, Measured During Study Drug Infusion Pre-surgery.

Non-CABG (Preoperative) Bleeding - Protocol-defined GUSTO Severe/Life-threatening, Moderate and Mild

Stage II: Analysis of Platelet Reactivity (ITT Population) / Patients With Platelet Reactivity < 240 PRU

Number of Participants With Major Adverse Cardiac Event (MACE)

Number of Participants With Elevation of Cardiac Enzyme

Individual Incidence of Stent Thrombosis (ST), Death, Myocardial Infarction (MI) and Ischemia-driven Revascularization (IDR)

Incidence of Major/Minor Non-coronary Artery Bypass Graft (CABG)-Related Hemorrhage by Clinical Relevant Criteria - GUSTO Severe/Life-threatening, Moderate and Mild

The Composite Incidence of All-cause Mortality, Myocardial Infarction (MI), Ischemia-driven Revascularization (IDR) and Stent Thrombosis (ST)

Extent of Aggregation Response During Ticagrelor Treatment

Extent of Preservation of Inhibitory Effect Compared With Effect Observed During Cangrelor Treatment After Ticagrelor

Extent of Preservation of Inhibitory Effect Compared With Effect Observed With Cangrelor Alone (at Timepoint 1, Either at 0.5 Hours or 1.25 Hours) or Ticagrelor Alone (Measured 5.25 Hours After Initiation of Cangrelor on Day 1)

Intervention	seconds (Mean)
	ADP-induced aggregation	TRAP-induced aggregation
Cangrelor	102.2	285.8
No Cangrelor	333.4	624.8