메뉴 건너뛰기




Volumn 70, Issue 1, 2010, Pages 65-77

Pharmacokinetics, pharmacodynamics, safety and tolerability of multiple ascending doses of ticagrelor in healthy volunteers

Author keywords

Antiplatelet therapy; AZD6140; Inhibition of platelet aggregation; P2Y 12 antagonist; Pharmacokinetics; Ticagrelor

Indexed keywords

CLOPIDOGREL; DRUG METABOLITE; TICAGRELOR;

EID: 77953498801     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2010.03669.x     Document Type: Article
Times cited : (142)

References (37)
  • 1
    • 34547772153 scopus 로고    scopus 로고
    • Guidelines for the diagnosis and treatment of non-ST-segment elevation acute coronary syndromes. Task force for diagnosis and treatment of non-ST-segment elevation acute coronary syndromes of the European Society of Cardiology
    • Bassand JP, Hamm CW, Ardissino D, Boersma E, Budaj A, Fernández-Avilés F, Fox KA, Hasdai D, Ohman EM, Wallentin L, Wijns W. Guidelines for the diagnosis and treatment of non-ST-segment elevation acute coronary syndromes. Task force for diagnosis and treatment of non-ST-segment elevation acute coronary syndromes of the European Society of Cardiology. Eur Heart J 2007 28 : 1598 1660.
    • (2007) Eur Heart J , vol.28 , pp. 1598-1660
    • Bassand, J.P.1    Hamm, C.W.2    Ardissino, D.3    Boersma, E.4    Budaj, A.5    Fernández-Avilés, F.6    Fox, K.A.7    Hasdai, D.8    Ohman, E.M.9    Wallentin, L.10    Wijns, W.11
  • 3
    • 0037406216 scopus 로고    scopus 로고
    • Durability of platelet inhibition by clopidogrel
    • Gurbel PA, Bliden KP. Durability of platelet inhibition by clopidogrel. Am J Cardiol 2003 91 : 1123 1125.
    • (2003) Am J Cardiol , vol.91 , pp. 1123-1125
    • Gurbel, P.A.1    Bliden, K.P.2
  • 4
    • 0038291914 scopus 로고    scopus 로고
    • Prevalence of clopidogrel non-responders among patients with stable angina pectoris scheduled for elective coronary stent placement
    • Müller I, Besta F, Schulz C, Massberg S, Schönig A, Gawaz M. Prevalence of clopidogrel non-responders among patients with stable angina pectoris scheduled for elective coronary stent placement. Thromb Haemost 2003 89 : 783 787.
    • (2003) Thromb Haemost , vol.89 , pp. 783-787
    • Müller, I.1    Besta, F.2    Schulz, C.3    Massberg, S.4    Schönig, A.5    Gawaz, M.6
  • 9
    • 33645967456 scopus 로고    scopus 로고
    • Variable therapeutic effectiveness of clopidogrel in acute coronary syndromes
    • Heptinstall S. Variable therapeutic effectiveness of clopidogrel in acute coronary syndromes. J Thromb Haemost 2006 4 : 539 541.
    • (2006) J Thromb Haemost , vol.4 , pp. 539-541
    • Heptinstall, S.1
  • 10
    • 33846837282 scopus 로고    scopus 로고
    • Increased risk in patients with high platelet aggregation receiving chronic clopidogrel therapy undergoing percutaneous coronary intervention. Is the current antiplatelet therapy adequate?
    • Bliden KP, DiChiara J, Tantry US, Bassi AK, Chaganti SK, Gurbel PA. Increased risk in patients with high platelet aggregation receiving chronic clopidogrel therapy undergoing percutaneous coronary intervention. Is the current antiplatelet therapy adequate? J Am Coll Cardiol 2007 49 : 657 666.
    • (2007) J Am Coll Cardiol , vol.49 , pp. 657-666
    • Bliden, K.P.1    Dichiara, J.2    Tantry, U.S.3    Bassi, A.K.4    Chaganti, S.K.5    Gurbel, P.A.6
  • 13
    • 77953498911 scopus 로고    scopus 로고
    • Eli Lilly and Company. Available at. (last accessed 28 January 2010)
    • Eli Lilly and Company. Effient™ (prasugrel) Prescribing Information. Available at http://pi.lilly.com/us/effient.pdf (last accessed 28 January 2010).
    • Effient™ (Prasugrel) Prescribing Information
  • 16
    • 27744444421 scopus 로고    scopus 로고
    • Resistance to antiplatelet drugs: Current status and future research
    • Tantry US, Bliden KP, Gurbel PA. Resistance to antiplatelet drugs: current status and future research. Expert Opin Pharmacother 2005 6 : 2027 2045.
    • (2005) Expert Opin Pharmacother , vol.6 , pp. 2027-2045
    • Tantry, U.S.1    Bliden, K.P.2    Gurbel, P.A.3
  • 17
    • 67649492154 scopus 로고    scopus 로고
    • Optimizing platelet inhibition
    • van Giezen JJJ. Optimizing platelet inhibition. Eur Heart J Suppl 2008 10 Suppl. D D23 D29.
    • (2008) Eur Heart J Suppl , vol.10 , Issue.SUPPL. D
    • Van Giezen, J.J.J.1
  • 18
    • 18044388905 scopus 로고    scopus 로고
    • Preclinical and clinical studies with selective reversible direct P2Y12 antagonists
    • van Giezen JJJ, Humphries RG. Preclinical and clinical studies with selective reversible direct P2Y12 antagonists. Semin Thromb Hemost 2005 31 : 195 204.
    • (2005) Semin Thromb Hemost , vol.31 , pp. 195-204
    • Van Giezen, J.J.J.1    Humphries, R.G.2
  • 19
    • 33646261670 scopus 로고    scopus 로고
    • Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: A double-blind comparison to clopidogrel with aspirin
    • Husted S, Emanuelsson H, Heptinstall S, Sandset PM, Wickens M, Peters G. Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin. Eur Heart J 2006 27 : 1038 1047.
    • (2006) Eur Heart J , vol.27 , pp. 1038-1047
    • Husted, S.1    Emanuelsson, H.2    Heptinstall, S.3    Sandset, P.M.4    Wickens, M.5    Peters, G.6
  • 21
    • 67649356342 scopus 로고    scopus 로고
    • Direct oral P2Y12 receptor antagonist AZD6140 potently and reversibly binds to the rh-P2Y12 receptor expressed on CHO-K1 cells
    • Abstract P207
    • van Giezen JJJ, Berntsson P, Wissing B-M. Direct oral P2Y12 receptor antagonist AZD6140 potently and reversibly binds to the rh-P2Y12 receptor expressed on CHO-K1 cells. Arterioscler Thromb Vasc Biol 2008 28 : e-72. Abstract P207.
    • (2008) Arterioscler Thromb Vasc Biol , vol.28 , pp. 72
    • Van Giezen, J.J.J.1    Berntsson, P.2    Wissing, B.-M.3
  • 22
    • 70349877890 scopus 로고    scopus 로고
    • Evidence for distinct ligand binding sites on recombinant P2Y12 receptors
    • Abstract 1313
    • Nilsson L, van Giezen JJJ, Greasley PJ. Evidence for distinct ligand binding sites on recombinant P2Y12 receptors. Circulation 2006 114 (Suppl. II 248. Abstract 1313.
    • (2006) Circulation , vol.114 , Issue.SUPPL. II , pp. 248
    • Nilsson, L.1    Van Giezen, J.J.J.2    Greasley, P.J.3
  • 24
    • 62949141274 scopus 로고    scopus 로고
    • Comparison of ticagrelor, the first reversible oral P2Y12 receptor antagonist, with clopidogrel in patients with acute coronary syndromes: Rationale, design, and baseline characteristics of the PLATelet inhibition and patient Outcomes (PLATO) trial
    • James S, Åkerblom A, Cannon C, Emanuelsson H, Husted S, Katus H, Skene A, Steg PG, Storey RF, Harrington R, Becker R, Wallentin L. Comparison of ticagrelor, the first reversible oral P2Y12 receptor antagonist, with clopidogrel in patients with acute coronary syndromes: rationale, design, and baseline characteristics of the PLATelet inhibition and patient Outcomes (PLATO) trial. Am Heart J 2009 157 : 599 605.
    • (2009) Am Heart J , vol.157 , pp. 599-605
    • James, S.1    Åkerblom, A.2    Cannon, C.3    Emanuelsson, H.4    Husted, S.5    Katus, H.6    Skene, A.7    Steg, P.G.8    Storey, R.F.9    Harrington, R.10    Becker, R.11    Wallentin, L.12
  • 26
    • 77953517212 scopus 로고    scopus 로고
    • AZD6140, the first reversible oral platelet P2Y12 receptor antagonist, has linear pharmacokinetics and provides near complete inhibition of platelet aggregation, with reversibility of effect, in healthy subjects
    • Abstract 9
    • Teng R, Butler K. AZD6140, the first reversible oral platelet P2Y12 receptor antagonist, has linear pharmacokinetics and provides near complete inhibition of platelet aggregation, with reversibility of effect, in healthy subjects. Can J Clin Pharmacol 2008 15 : e426. Abstract 9.
    • (2008) Can J Clin Pharmacol , vol.15 , pp. 426
    • Teng, R.1    Butler, K.2
  • 27
    • 84881610688 scopus 로고    scopus 로고
    • Sanofi-Aventis. May 2009. Available at. (last accessed April 2010)
    • Sanofi-Aventis. PLAVIX® (clopidogrel) prescribing information. May 2009. Available at http://packageinserts.bms.com/pi/pi-plavix.pdf (last accessed April 2010).
    • PLAVIX® (Clopidogrel) Prescribing Information
  • 28
    • 35548995394 scopus 로고    scopus 로고
    • Safety, tolerability, and initial efficacy of AZD6140, the first reversible oral adenosine diphosphate receptor antagonist, compared with clopidogrel, in patients with non-ST-segment elevation acute coronary syndrome: Primary results of the DISPERSE-2 Trial
    • Cannon CP, Husted S, Harrington RA, Scirica BM, Emanuelsson H, Peters G, Storey RF DISPERSE-2 Investigators. Safety, tolerability, and initial efficacy of AZD6140, the first reversible oral adenosine diphosphate receptor antagonist, compared with clopidogrel, in patients with non-ST-segment elevation acute coronary syndrome: primary results of the DISPERSE-2 Trial. J Am Coll Cardiol 2007 50 : 1844 1851.
    • (2007) J Am Coll Cardiol , vol.50 , pp. 1844-1851
    • Cannon, C.P.1    Husted, S.2    Harrington, R.A.3    Scirica, B.M.4    Emanuelsson, H.5    Peters, G.6
  • 29
    • 0346367328 scopus 로고
    • Aggregation of blood platelets by adenosine diphosphate and its reversal
    • Born GV. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature 1962 194 : 927 929.
    • (1962) Nature , vol.194 , pp. 927-929
    • Born, G.V.1
  • 30
    • 23644437489 scopus 로고    scopus 로고
    • Matching the evaluation of the clinical efficacy of clopidogrel to platelet function tests relevant to the biological properties of the drug
    • Labarthe J, Théroux P, Angioï M, Ghitescu M. Matching the evaluation of the clinical efficacy of clopidogrel to platelet function tests relevant to the biological properties of the drug. J Am Coll Cardiol 2005 46 : 638 645.
    • (2005) J Am Coll Cardiol , vol.46 , pp. 638-645
    • Labarthe, J.1    Théroux, P.2    Angioï, M.3    Ghitescu, M.4
  • 31
    • 77954468084 scopus 로고    scopus 로고
    • Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y12 receptor antagonist, in healthy subjects
    • Teng R, Butler K. Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y12 receptor antagonist, in healthy subjects. Eur J Clin Pharmacol 2010 66 : 487 496.
    • (2010) Eur J Clin Pharmacol , vol.66 , pp. 487-496
    • Teng, R.1    Butler, K.2
  • 32
    • 23044461331 scopus 로고    scopus 로고
    • Single dose pharmacokinetics and pharmacodynamics of AZD6140 - An oral reversible ADP receptor antagonist
    • Peters G, Robbie G. Single dose pharmacokinetics and pharmacodynamics of AZD6140 - an oral reversible ADP receptor antagonist. Haematologica 2004 89 (Suppl. 7 14 15.
    • (2004) Haematologica , vol.89 , Issue.7 SUPPL. , pp. 14-15
    • Peters, G.1    Robbie, G.2
  • 34
    • 2942641718 scopus 로고    scopus 로고
    • Platelet ADP receptor antagonists: Ticlopidine and clopidogrel
    • Jacobson AK. Platelet ADP receptor antagonists: ticlopidine and clopidogrel. Best Pract Res Clin Haematol 2004 17 : 55 64.
    • (2004) Best Pract Res Clin Haematol , vol.17 , pp. 55-64
    • Jacobson, A.K.1
  • 35
    • 67649356342 scopus 로고    scopus 로고
    • Direct oral P2Y12 receptor antagonist AZD6140 potently and reversibly binds to the rh-P2Y12 receptor expressed on CHO-K1 cells
    • Abstract P207
    • van Giezen JJJ, Berntsson P, Wissing B-M. Direct oral P2Y12 receptor antagonist AZD6140 potently and reversibly binds to the rh-P2Y12 receptor expressed on CHO-K1 cells. Arterioscler Thromb Vasc Biol 2008 28 : e-72. Abstract P207.
    • (2008) Arterioscler Thromb Vasc Biol , vol.28 , pp. 72
    • Van Giezen, J.J.J.1    Berntsson, P.2    Wissing, B.-M.3
  • 37
    • 77953497812 scopus 로고    scopus 로고
    • No significant food effect on the pharmacokinetics of ticagrelor (AZD6140), the first reversibly binding oral P2Y12 receptor antagonist, in healthy subjects
    • March 18-21, 2009; Washington, DC
    • Butler K, Mitchell PD, Teng R. No significant food effect on the pharmacokinetics of ticagrelor (AZD6140), the first reversibly binding oral P2Y12 receptor antagonist, in healthy subjects. Presented at: 110th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; March 18-21, 2009; Washington, DC.
    • 110th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics
    • Butler, K.1    Mitchell, P.D.2    Teng, R.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.