Hirudin recombinant

The most potent thrombin inhibitor is hirudin, originally isolated from the salivary glands of the medicinal leech Hirudo medicinalis. Its inhibition constant is in the femtomolar (10-15 M) range (57). It is a 65-amino-acid tyrosine-sulfated single-chain polypeptide. Recombinant hirudin differs from native hirudin by the absence of the sulfate group on tyrosine 63 (Tyr-63) and is referred to as desulfato hirudin. The loss of this sulfate group reduces the thrombin inhibitory potency by 10-fold. [Pg.149]

Rydel T. J., Ravichandran K. G., Tulinsky A., et al. The structure of a complex of recombinant hirudin and human alpha-thrombin. Science 1990 249,277-80. [Pg.166]

Eriksson B. I., Ekmann S. T Kalebo P., et al. Prevention of deep-vein thrombosis after total hip replacement Direct thrombin inhibition with recombinant hirudin, CCG 39393. Lancet 1996 347,635-9. [Pg.166]

Figure 12.9 Overview of the production of Refludan (recombinant hirudin). The exact details of many steps remain confidential for obvious commercial reasons. A number of QC checks are carried out on the final product to confirm the product s structure. These include amino acid composition, HPLC analysis and peptide mapping...

Fischer, K. 2004. The role of recombinant hirudins in the management of thrombotic disorders. Biodrugs 18(4), 235-268. [Pg.367]

Zhang Y, Zhang Q, Sun Y, Sun J, Wang X, Chen M (2005) Nasal recombinant hirudin-2 delivery absorption and its mechanism in vivo and in vitro studies. Biol Pharm Bull 28 2263-2267. [Pg.132]

Pharmacology Lepirudin (rDNA), a recombinant hirudin derived from yeast cells, is a highly specific direct inhibitor of thrombin. [Pg.147]

Contraindications Hypersensitivity to natural or recombinant hirudins (anticoagulation factors), active bleeding, irreversible coagulation disorders... [Pg.337]

The oleosin fusion procedure was used for the purification of the commercially valuable plant-based blood anticoagulant hirudin in transgenic Brassica carinata and Brassica napus. Hirudin, a natural protein from the medicinal leech Hirudo medicinalis, is superior to other anticoagulants such as heparin. Recombinant hirudin was cleaved from oil-bodies using endoproteinase Factor Xa. Released hirudin was biologically active, as determined by a colorimetric thrombin inhibition assay. [Pg.43]

Gietz, U., R. Alder, P. Langguth, T. Arvinte, and H.P. Merkle, Chemical degradation kinetics of recombinant hirudin (HVI) in aqueous solution effect of pH. Pharm Res, 1998.15(9) 1456-62. [Pg.61]

A. General description Lepirudin is a recombinant hirudin, a highly specific direct inhibitor of thrombin, derived from yeast cells. The polypeptide is composed of 65 amino acids and has a molecular weight of 7 kD. Natural hirudin is produced in trace amounts as a family of highly homologous isopolypeptides by the medicinal leech. Lepirudin is identical to natural hirudin except for the substitution of leucine for isoleucine at the N-terminal end... [Pg.151]

A. General description Bivalirudin, a 20 amino-acid synthetic peptide, is a direct thrombin inhibitor. It is an analogue of recombinant hirudin (Refludan), a 65 amino-acid anticoagulant derived from the leech. The molecular weight of bivalirudin is about 2.2kDa (anhydrous free base peptide). [Pg.153]

F. Role in therapy The potential advantages of Angiomax—a direct thrombin inhibitor—over heparin include activity against clot-bound thrombin, more predictable anticoagulation, and no inhibition by components of the platelet release reaction. The place in therapy of Angiomax will be determined by further comparisons with heparin, low-molecular weight heparins, and recombinant hirudin. [Pg.154]

Bivalirudin, reversible thrombin inhibitor, recombinant hirudin... [Pg.454]

Latham P, et al. Use of recombinant hirudin in patients with heparin-induced thrombocytopenia with thrombosis requiring cardiopulmonary, bypass. Anesthesiology 2000 92 263-6. [Pg.264]

REFLUDAN (Lepirudin) [recombinant hirudin polypeptide expressed in yeast cells] Berlex Lyophilized 50 mg single-dose vial... [Pg.328]

Liu, Y., et al. 2005. Pharmacodynamics and pharmacokinetics of recombinant hirudin via four nonparenteral routes. Peptides 26 243. [Pg.146]

Characteristics Recombinant hirudins Bivalirudin Argatroban Ximelagatran and melagatran Dabigatran... [Pg.87]

I 5 van den Bos AA, Deckers JW, Heyndrickx GR, et al, Safety and efficacy of recombinant hirudin (CGP 39 393) versus heparin in patients with stable angina undergoing coronary angioplasty, Circulation 1993 88 2058-2066. [Pg.91]

I 6 Hafner G, Rupprecht HJ, Luz M, et al. Recombinant hirudin as a periprocedural antithrombotic in coronary angioplasty for unstable angina pectoris. Eur Heart J 1996 17 1207-1215,... [Pg.91]

Berry CN, Girardot C, Lecoffre C, et al. Effects of the synthetic thrombin inhibitor argatroban on fibrin- or clot-incorporated thrombin comparison with heparin and recombinant Hirudin. Thromb Haemost 1994 72 381-386. [Pg.105]

Greinacher A, Volpel H, Janssens U, et al. Recombinant hirudin (Lepirudin) provides safe and effective anticoagulation in patients with heparin-induced thrombocytopenia. A prospective study. Circulation 1999 99 73-80. [Pg.106]

Zeymer U, von Essen R, Tebbe U, et al, Frequency of optimal anticoagulation for acute myocardial infarction after thrombolysis with front-loaded recombinant tissue-type plasminogen activator and conjunctive therapy with recombinant hirudin (HBW 023). ALKK Study Group. Am J Cardiol 1995 76 997-1001. [Pg.106]

Potzsch B, Hund S, Madlener K, et al. Monitoring of recombinant hirudin assessment of a plasma-based ecarin clotting time assay. Thromb Res 1997 86 373-383. [Pg.106]

The Global Use of Strategies to Open Occluded Coronary Arteries (GUSTO I la) Investigators. Randomized trial of intravenous heparin versus recombinant hirudin for acute coronary syndromes. Circulation 1994 90 1631-1637. [Pg.107]

GUSTO II b Investigators. A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes. N Engl J Med 1996 335 775-782. [Pg.107]

Lubenow N, Greinacher A. Management of patients with heparin-induced thrombocytopenia focus on recombinant hirudin. J Thromb Thrombolysis 2000 10 S47-S57. [Pg.134]

Recently, several reports comparing the effects of heparin and hirudin on various parameters have become available. A study comparing heparin and recombinant hirudin for the prophylaxis of deep venous thrombosis (DVT) provided impressive data in favor of hirudin. In a second study, LMWHs also were compared with hirudin for postsurgical prophylaxis of DVT the results favored hirudin. Both studies emphasize an important point about the validity of well-designed clinical trials, It is important to understand that the efficacy and safety of a new drug may not be determined by trials for a single indication, Therefore, clinical trials are needed for various specific indications. [Pg.615]

Herrmann KS (1983) Platelet aggregation induced in the hamster cheek pouch by a photochemical process with excited fluorescein isothiocyanate-dextran. Micovasc Res 26 238-249 Just M, Tripier D, Seiffge D (1991b) Antithrombotic effects of recombinant hirudin in different animal models. Haemostasis 21 (Suppl l) 80-87 Matsuno H, Uematsu T, Nagashima S, Nakashima M (1991) Photochemically induced thrombosis model in rat femoral artery and evaluation of effects of heparin and tissue-type plasminogen activator with use of this model. J Pharmacol Methods 25 303-317... [Pg.289]

Agnelli G, Pascucci C, Cosmi B, Nenci GG (1990) The comparative effects of recombinant hirudin (CGP 39393) and standard heparin on thrombus growth in rabbits. Thromb Haemost 63 204-207... [Pg.316]

Paulus, A., and Gassmann, E. (1989). Purification control of recombinant hirudin by capillary electrophoresis. Beckman Appl. Data Sheet DS-752. [Pg.67]

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