Reversal of heparin-induced increases in aPTT in the rat by PM102, a novel heparin antagonist

European Journal of Pharmacology

Volumn 635, Issue 1-3, 2010, Pages 165-170

  Cushing, Daniel J ^a   Cooper, Warren D ^a   Cohen, Marlene L ^b   McVoy, Julie R S ^c   Sobel, Michael ^d   Harris, Robert B ^c  

^a Prism Pharmaceuticals Inc   (United States)

^b Creative Pharmacology Solutions LLC   (United States)

^c Commonwealth Biotechnologies Inc ^*  (United States)

^d UNIVERSITY OF WASHINGTON   (United States)

Author keywords

Anticoagulation; Heparin; PM102; Protamine

Indexed keywords

HEPARIN; HEPARIN ANTAGONIST; HEPARREST; PM 102; PROTAMINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BLOOD SAMPLING; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; ANTICOAGULANTS; BLOOD COAGULATION; DOSE-RESPONSE RELATIONSHIP, DRUG; HEPARIN; HEPARIN ANTAGONISTS; INJECTIONS, INTRAVENOUS; MALE; PARTIAL THROMBOPLASTIN TIME; PEPTIDES; PROTAMINES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 77952323138     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.03.016     Document Type: Article

References (19)

1. Protamine Sulfate Injection USP 2008, A.P.P. Pharmaceuticals, Package Insert, Schaumburg, IL.
2. Gibaldi M., Perrier D. Pharmacokinetics 1982, New York, Marcel Dekker. Second Ed.
3. Harris, R.B., Sobel, M., 1999. Heparin-binding peptides. US Patent No. 5,877,153.
4. Harris, R.B., Sobel, M., 2001. Heparin-binding peptides. US Patent No. 6,200,955.
5. Kikura M., Lee M.K., Levy J.H. Heparin neutralization with methylene blue, hexadimethrine, or vancomycin after cardiopulmonary bypass. Anesth. Analg. 1996, 83:223-227.
6. Kimmel S.E., Sekeres M.A., Berlin J.A., Goldberg L.R., Strom B.L. Adverse events after protamine administration in patients undergoing cardiopulmonary bypass: risks and predictors of under-reporting. J. Clin. Epidemiol. 1998, 51:1-10.
7. Kimmel S.E., Sekeres M., Berlin J.A., Ellison N. Mortality and adverse events after protamine administration in patients undergoing cardiopulmonary bypass. Anesth. Analg. 2002, 94:1402-1408.
8. Kishimoto T.K., Viswanathan K., Ganguly T., Elankumaran S., Smith S., Pelzer K., Lansing J.C., Sriranganathan N., Zhao G., Galcheva-Gargova Z., Al-Hakim A., Bailey G.S., Fraser B., Roy S., Rogers-Cotrone T., Buhse L., Whary M., Fox J., Nasr M., Dal Pan G.J., Shriver Z., Langer R.S., Venkataraman G., Austen K.F., Woodcock J., Sasisekharan R. Contaminated heparin associated with adverse clinical events and activation of the contact system. N. Engl. J. Med. 2008, 358:2457-2467.
9. Levy J.H., Cormack J.G., Morales A. Heparin neutralization by recombinant platelet factor 4 and protamine. Anesth. Analg. 1995, 81:35-37.
10. Guide for the Care and Use of Laboratory Animals 1996, NIH Publication, National Academy Press.
11. Panos A., Orrit X., Chevalley C., Kalangos A. Dramatic post-cardiotomy outcome, due to severe anaphylactic reaction to protamine. Eur. J. Cardiothorac. Surg. 2003, 24:325-327.
12. Racanelli A., Fareed J. Neutralization of the antithrombotic effects of heparin and Fraxiparin by protamine sulfate. Thromb. Res. 1992, 68:211-222.
13. Schick B.P., Maslow D., Moshinski A., San Antonio J.D. Novel concatameric heparin-binding peptides reverse heparin and low-molecular-weight heparin anticoagulant activities in patient plasma in vitro and in rats in vivo. Blood 2004, 103:1356-1363.
14. Shenoy S., Sobel M., Harris R.B. Development of heparin antagonists with focused biological activity. Curr. Pharm. Des. 1999, 5:965-986.
15. Stafford-Smith M., Lefrak E.A., Qazi A.G., Welsby I., Barber L., Hoeft A., Dorenbaum A., Mathias J., Rochon J.J., Newman M.F. Efficacy and safety of heparinase I versus protamine in patients undergoing coronary artery bypass grafting with and without cardiopulmonary bypass. Anesthesiology 2005, 103:229-240.
16. Wakefield, T.W., Stanley, J.C., Andrews, P.C., 1996. Peptides for heparin and low molecular weight heparin anticoagulation reversal. United States Patent No. 5,534,619.
17. Weiler J.M., Gellhaus M.A., Carter J.G., Meng R.L., Benson P.M., Hottel R.A., Schillig K.B., Vegh A.B., Clarke W.R. A prospective study of the risk of an immediate adverse reaction to protamine sulfate during cardiopulmonary bypass surgery. J. Clin. Immunol. 1990, 85:713-719.
18. Weiss M.E., Nyhan D., Peng Z.K., Horrow J.C., Lowenstein E., Hirshman C., Adkinson N.F. Association of protamine IgE and IgG antibodies with life-threatening reactions to intravenous protamine. N. Engl. J. Med. 1989, 320:886-892.
19. Welsby I., Newman M.F., Phillips-Bute B., Messier R.H., Kakkis E.D., Stafford-Smith M. Hemodynamic changes after protamine administration. Anesthesiology 2005, 103:229-240.