Pharmacological effects of a novel recombinant hirudin, CX-397, in vivo and in vitro: comparison with recombinant hirudin variant-1, heparin, and argatroban.

Abstract	The novel recombinant hirudin analog CX-397 was investigated with respect to its pharmacological activity and antithrombin profiles in vivo and in vitro. In three different types of thrombosis models in rats, including stasis and thrombin-induced venous, glass surface-activated arterio-venous shunt, and ferric chloride-induced arterial thrombosis models, CX-397 and rHV-1 elicited potent antithrombotic effects, where the minimum effective doses of rHV-1 tended to be higher than those of CX-397 in the arterio-venous shunt and arterial thrombosis models. The hemorrhagic risk of CX-397 in template bleeding in rats was not higher than that of rHV-1, indicating that CX-397 is superior to rHV-1 for treating the platelet-dominant type of thrombosis. However, no differences were detected between CX-397 and rHV-1 in their effects on in vitro coagulation times and thrombin-induced platelet aggregation, suggesting the possibility that some unknown mechanisms other than simple thrombin inhibition are also involved in their antithrombotic actions.
Authors	Y Komatsu, Y Inoue, Y Goto, T Fukazawa, H Hayashi
Journal	Thrombosis and haemostasis (Thromb Haemost) Vol. 81 Issue 2 Pg. 250-5 (Feb 1999) ISSN: 0340-6245 [Print] Germany
PMID	10064001 (Publication Type: Comparative Study, Journal Article)
Chemical References	CX 397 Chlorides Ferric Compounds Fibrinolytic Agents Hirudins Pipecolic Acids Platelet Aggregation Inhibitors Recombinant Proteins Serine Proteinase Inhibitors Sulfonamides Heparin Arginine Thrombin argatroban desirudin ferric chloride
Topics	Amino Acid Sequence Animals Arginine (analogs & derivatives) Arterial Occlusive Diseases (chemically induced, drug therapy, prevention & control) Arteriovenous Shunt, Surgical Chlorides Drug Evaluation, Preclinical Ferric Compounds (toxicity) Fibrinolytic Agents (pharmacology, therapeutic use, toxicity) Glass Hemorrhage (chemically induced) Heparin (pharmacology, therapeutic use, toxicity) Hirudin Therapy Hirudins (analogs & derivatives, chemistry, pharmacology, toxicity) Molecular Sequence Data Pipecolic Acids (pharmacology, therapeutic use, toxicity) Platelet Aggregation (drug effects) Platelet Aggregation Inhibitors (pharmacology, therapeutic use, toxicity) Rats Recombinant Proteins (chemistry, pharmacology, therapeutic use, toxicity) Sequence Alignment Sequence Homology, Amino Acid Serine Proteinase Inhibitors (pharmacology, therapeutic use, toxicity) Sulfonamides Thrombin (antagonists & inhibitors, pharmacology) Thrombosis (chemically induced, drug therapy, prevention & control) Vena Cava, Inferior Venous Thrombosis (drug therapy, prevention & control)

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