Recombinant hirudin · clot prevention
Desirudin is a recombinant form of hirudin, the anticoagulant protein of the medicinal leech, produced in yeast. It blocks thrombin, the final enzyme of blood clotting. It was approved to prevent deep vein thrombosis after joint replacement: hip surgery in the US, as Iprivask, and hip or knee surgery in Europe, as Revasc. Both products have since left the market.
Clotting ends with thrombin, an enzyme that turns fibrinogen into the fibrin mesh of a clot. Desirudin binds thrombin directly and very tightly, blocking both thrombin circulating freely in the blood and thrombin already bound inside a clot. Heparins work indirectly, through the helper protein antithrombin; desirudin does not need it. At the levels reached in use it has little effect on other clotting enzymes such as factor Xa or plasmin. Its effect shows up as a longer aPTT clotting time. It is a single-chain protein of 65 amino acids held in shape by three disulfide bridges. The kidneys clear and break down most of it, so reduced kidney function raises blood levels and the anticoagulant effect.
The evidence comes from human surgical trials. In a double-blind trial of 445 people having total hip replacement, desirudin started before surgery was compared with unfractionated heparin; confirmed deep vein thrombosis occurred in 7% versus 23% of evaluable patients, with no significant difference in bleeding1.
A larger trial of 2,079 patients at 31 European centers compared it with enoxaparin, a low-molecular-weight heparin: proximal clots fell from 7.5% to 4.5% and overall deep vein thrombosis from 25.5% to 18.4%, and the two groups' side-effect profiles were similar2.
A 2000 review judged it clearly more effective than heparin for this use, while results in heart attack and unstable angina were inconclusive3. A 2011 review describes it as one of few non-heparin injectable options with shown efficacy for clot prevention and notes that reduced kidney function calls for adjustment4.
In a dose-finding study, about 10% of patients formed antibodies to it, with no apparent effect on clots, bleeding or allergic reactions5.
The FDA approved desirudin as Iprivask in 2003 to prevent deep vein thrombosis in people undergoing elective hip replacement, and FDA records now list the product as discontinued. In the EU, Revasc was authorised in 1997 for hip or knee replacement and withdrawn in 2014 at the holder's request6.
Bleeding is the most common reaction, as with other anticoagulants; in the hip-replacement trials bleeding rates were similar to heparin and enoxaparin. The European label listed anemia, nausea, wound secretion, low blood pressure, deep thrombophlebitis, fever, injection-site masses, bruising and leg swelling as common. It warned of allergic reactions including anaphylaxis and shock, noting fatal anaphylaxis on re-exposure to other hirudin products. It was not to be used with active bleeding or severe kidney or liver impairment.
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