Antisense inhibition of coagulation factor XI prolongs APTT without increased bleeding risk in cynomolgus monkeys

Blood

Volumn 119, Issue 10, 2012, Pages 2401-2408

  Younis, Husam S ^a   Crosby, Jeff ^a   Huh, Jung Im ^b   Lee, Hong Soo ^b   Rime, Soyub ^b   Monia, Brett ^a   Henry, Scott P ^a  

^a ISIS PHARMACEUTICALS   (United States)

^b Korea Institute of Toxicology   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; BLOOD CLOTTING FACTOR 11; BLOOD CLOTTING INHIBITOR; ENOXAPARIN; HEMATOXYLIN; ISIS 416858; MESSENGER RNA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BASOPHIL; DRUG ACTIVITY; DRUG SAFETY; DRUG UPTAKE; FEMALE; HAPLORHINI; LACERATION; LIVER; LOADING DRUG DOSE; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; PROTHROMBIN TIME;

EID: 84863229481     PISSN: 00064971     EISSN: 15280020     Source Type: Journal    
DOI: 10.1182/blood-2011-10-387134     Document Type: Article

References (35)

1. Stashenko GJ, Tapson VF. Prevention of venous thromboembolism in medical patients and outpatients. Nat Rev Cardiol. 2009;6(5):356-363.
2. Fisher WD. Impact of venous thromboembolism on clinical management and therapy after hip and knee arthroplasty. Can J Surg. 2011;54(4):7310.
3. Haas S. New anticoagulants-towards the development of an "ideal" anticoagulant. Vasa. 2009; 38(1):13-29.
4. Schulman S. Rivaroxaban in orthopedic surgery-a change of paradigm? Clin Appl Thromb Hemost. 2009;15(6):613-620.
5. Gailani D. Gene targeting in hemostasis. factor XI. Front Biosci. 2001;6:D201-D207.
6. Kravtsov DV, Matafonov A, Tucker EI, et al. Factor XI contributes to thrombin generation in the absence of factor XII. Blood. 2009;114(2):452- 458.
7. Meijers JC, Tekelenburg WL, Bouma BN, Bertina RM, Rosendaal FR. High levels of coagulation factor XI as a risk factor for venous thrombosis. N Engl J Med. 2000;342(10):696-701. (Pubitemid 30131422)
8. Siegerink B, Govers-Riemslag JW, Rosendaal FR, Ten Cate H, Algra A. Intrinsic coagulation activation and the risk of arterial thrombosis in young women: results from the risk of arterial thrombosis in relation to oral contraceptives (RATIO) case-control study. Circulation. 2010;122(18):1854-1861.
9. Schumacher WA, Luettgen JM, Quan ML, Seiffert DA. Inhibition of factor XIa as a new approach to anticoagulation. Arterioscler Thromb Vasc Biol. 2010;30(3):388-392.
10. Salomon O, Steinberg DM, Koren-Morag N, Tanne D, Seligsohn U. Reduced incidence of ischemic stroke in patients with severe factor XI deficiency. Blood. 2008;111(8):4113-4117.
11. Salomon O, Steinberg DM, Zucker M, Varon D, Zivelin A, Seligsohn U. Patients with severe factor XI deficiency have a reduced incidence of deep-vein thrombosis. Thromb Haemost. 2011;105(2): 269-273.
12. Salomon O, Steinberg DM, Dardik R, et al. Inherited factor XI deficiency confers no protection against acute myocardial infarction. J Thromb Haemost. 2003;1(4):658-661.
13. Rosen ED, Gailani D, Castellino FJ. FXI is essential for thrombus formation following FeCl3- induced injury of the carotid artery in the mouse. Thromb Haemost. 2002;87(4):774-776. (Pubitemid 34302972)
14. Wang X, Smith PL, Hsu MY, et al. Effects of factor XI deficiency on ferric chloride-induced vena cava thrombosis in mice. J Thromb Haemost. 2006; 4(9):1982-1988. (Pubitemid 44226778)
15. Zhang H, Löwenberg EC, Crosby JR, et al. Inhibition of the intrinsic coagulation pathway factor XI by antisense oligonucleotides: a novel antithrombotic strategy with lowered bleeding risk. Blood. 2010;116(22):4684- 4692.
16. Tucker EI, Marzec UM, White TC, et al. Prevention of vascular graft occlusion and thrombus-associated thrombin generation by inhibition of factor XI. Blood. 2009;113(4):936-944.
17. Seligsohn U. Factor XI deficiency in humans. J Thromb Haemost. 2009;1(7 suppl):84-87.
18. Gomez K, Bolton-Maggs P. Factor XI deficiency. Haemophilia. 2008;14(6):1183-1189.
19. Crooke ST. Progress in antisense technology: the end of the beginning. Methods Enzymol. 2000; 313:3-45. (Pubitemid 29506409)
20. Geary RS, Watanabe TA, Truong L, et al. Pharmacokinetic properties of 2′-O-(2-methoxyethyl)- modified oligonucleotide analogs in rats. J Pharmacol Exp Ther. 2001;296(3):890-897. (Pubitemid 32187362)
21. Crooke ST, Vickers T, Lima W, Wu H. Mechanisms of antisense drug action, and introduction. In: Crooke ST, ed. Antisense Drug Technology. New York, NY: CRC Press; 2006:3-47.
22. Geary RS. Antisense oligonucleotide pharmacokinetics and metabolism. Expert Opin Drug Metab Toxicol. 2009;5(4):381-391.
23. Hall RL, Everds NE. Principles of clinical pathology for toxicology studies. In: Hayes AW, ed. Principles and Methods of Toxicology. New York, NY: CRC Press; 2007:1328-1350.
24. Butler M, Stecker K, Bennett CF. Cellular distribution of phosphorothioate oligodeoxynucleotides in normal rodent tissues. Lab Invest. 1997;77(4): 379-388. (Pubitemid 27465599)
25. Yu RZ, Kim TW, Hong A, Watanabe TA, Gaus HJ, Geary RS. Cross-species pharmacokinetic comparison from mouse to man of a second-generation antisense oligonucleotide, ISIS 301012, targeting human apolipoprotein B-100. Drug Metab Dispos. 2007;35(3):460-468. (Pubitemid 46333910)
26. Geary RS, Yu RZ, Siwkowski A, Levin AA. Toxico-logic properties of 2-o-methoxyethyl chimeric antisense inhibitors in animals and man. Antisense Drug Technology, 2nd ed. New York, NY: CRC Press; 2007:305-326.
27. Akdim F, Visser ME, Tribble DL, et al. Effect of mipomersen, an apolipoprotein B synthesis inhibitor, on low-density lipoprotein cholesterol in patients with familial hypercholesterolemia. Am J Cardiol. 2010;105(10):1413- 1419.
28. Di Cresce C, Koropatnick J. Antisense treatment in human prostate cancer and melanoma. Curr Cancer Drug Targets. 2010;10(6):555-565.
29. Gruber A, Hanson SR. Factor XI-dependence of surface- and tissue factor-initiated thrombus propagation in primates. Blood. 2003;102(3):953- 955.
30. Henry SP, Kim TW, Kramer-Stickland K, Zanardi TA, Fey RA, Levin AA. Toxicologic properties of 2-O-methoxyethyl chimeric antisense inhibitors in animals and man. Antisense Drug Technology, 2nd ed. New York, NY: CRC Press; 2007:327-364.
31. Henry SP, Geary RS, Yu R, Levin AA. Drug properties of second-generation antisense oligonucleotides: how do they measure up to their predecessors? Curr Opin Investig Drugs. 2001;2(10): 1444-1449. (Pubitemid 32994399)
32. Kowe TJ. An overview of the clinical safety experience of first- and second-generation antisense oligonucleotides. Antisense Drug Technology, 2nd ed. New York, NY: CRC Press; 2007:365- 399.
33. Tucker EI, Gailani D, Hurst S, Cheng Q, Hanson SR, Gruber A. Survival advantage of coagulation factor XI-deficient mice during peritoneal sepsis. J Infect Dis. 2008;198(2):271-274. (Pubitemid 352019293)
34. Itakura A, Verbout NG, Phillips KG, et al. Activated factor XI inhibits chemotaxis of polymor-phonuclear leukocytes. J Leukoc Biol. 2011; 90(5):923-927.
35. Jankowski M, Undas A, Kaczmarek P, Butenas S. Activated factor XI and tissue factor in chronic obstructive pulmonary disease: links with inflammation and thrombin generation. Thromb Res. 2011;127(3):242-246.