Desirudin

Desirudin is a recombinant hirudin — a 65-amino-acid direct thrombin inhibitor identical to natural hirudin except for desulfation of Tyr-63. It was approved for DVT prophylaxis after elective hip replacement surgery based on phase 3 trials showing superiority to unfractionated heparin and non-inferiority to enoxaparin. Subcutaneous administration twice daily. All marketing authorizations have been withdrawn; it is no longer commercially available (US discontinuation; EU Revasc withdrawal 2014).

Desirudin is a highly specific, irreversible (stoichiometric 1:1) direct inhibitor of human thrombin. It binds to both the active (catalytic) site and the fibrinogen-binding exosite (exosite 1) of free and clot-bound thrombin. Unlike heparin, desirudin does not require antithrombin III and is not inhibited by platelet factor 4, making it effective against clot-bound thrombin.

Pharmacokinetics: SC absorption; bioavailability ~100%; Tmax 1-2 h; half-life ~2 h; primarily renal excretion (>90% unchanged); accumulates in renal impairment.

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

Elective hip replacement: 15 mg SC every 12 h. First dose given 5-15 min prior to surgery (but after induction of regional block anesthesia). Continue for 9-12 days. In moderate renal impairment (CrCl 31–60 mL/min): reduce dose by factor of 3 (5 mg SC q12h). In severe renal impairment (CrCl <31 mL/min): reduce dose by factor of 9 (1.7 mg SC q12h). Monitor aPTT and serum creatinine daily in patients with renal impairment.

Studied regimens (not recommendations)

Various dose-ranging studies used 10-20 mg SC BID; the 15 mg BID dose was selected as the optimal balance of efficacy and safety.

What is not established

• DVT prophylaxis for knee replacement (not established; phase 3 data limited to hip replacement).

• Treatment of established VTE (not labeled).

• Use in ACS or PCI (not labeled; bivalirudin used instead for these indications).

• Pediatric use.

Established label risks

• Bleeding (most common). Desirudin carries an FDA boxed warning for spinal/epidural hematoma with neuraxial anesthesia — this is appropriate for a subcutaneously administered anticoagulant with prolonged half-life in renal impairment.

• Hypersensitivity to hirudins (contraindicated).

• Injection-site hematoma.

• Renal impairment increases bleeding risk; accumulation in renal impairment extends the half-life substantially.

Human-study signals

• Anti-hirudin antibodies: developed in ~44% of treated patients in long-term follow-up; did not appear to affect efficacy or safety in the short DVT-prophylaxis duration, but potential for anaphylaxis with re-exposure.

• No HIT (heparin-induced thrombocytopenia) because desirudin is not heparin-like.

Unknowns and product-quality risks

• Product has a boxed warning for spinal/epidural hematoma (same class warning as all anticoagulants used with neuraxial procedures).

• Reconstituted solution is stable for 24 h at room temperature; store lyophilized powder at 2-25°C.

Increased bleeding with antiplatelet agents, other anticoagulants, NSAIDs. Significant renal accumulation in CrCl <30 mL/min (contraindicated in some labels). No CYP-mediated interactions.

WADA status: desirudin was not identified by exact name in the 2026 Prohibited List. Marketing discontinuation is not itself a classification: S0 depends on whether a current governmental approval for human therapeutic use remains in any jurisdiction. This page does not resolve that global question, so athletes need a current, case-specific determination. No US federal CSA scheduling was identified as of 2026-08-06; state law and other jurisdictions were not assessed. Iprivask US marketing was discontinued; EU authorisation of Revasc was withdrawn on 18 July 2014 at the MAH's request for commercial reasons and was never marketed in any EU country. Desirudin is not commercially available in the US or EU as of 2026. Desirudin preceded bivalirudin as the first available recombinant hirudin analogue.

• No contemporary comparative data vs DOACs (rivaroxaban, apixaban, dabigatran, edoxaban) for hip replacement.

• Very limited data in renal impairment; no long-term safety database.

• Antibody formation risk with repeated intermittent exposure (e.g., bilateral staged hip replacements).

• Databases and registries: FDA label (accessdata.fda.gov), DailyMed, PubMed, ClinicalTrials.gov

• Search terms: desirudin, Iprivask, Revasc, recombinant hirudin, DVT prophylaxis, hip replacement

• Last searched: 2026-08-06

• Inclusion emphasis: FDA label, phase 3 RCTs, systematic reviews

1. FDA prescribing information: IPRIVASK (desirudin for injection). Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021271s006lbl.pdf (accessed 2026-08-06).

2. Eriksson BI, et al. A comparison of recombinant hirudin with a low-molecular-weight heparin to prevent thromboembolic complications after total hip replacement. N Engl J Med. 1997;337(19):1329-35. DOI: 10.1056/NEJM199711063371901. https://doi.org/10.1056/NEJM199711063371901

3. Eriksson BI, et al. Prevention of deep-vein thrombosis after total hip replacement: direct thrombin inhibition with recombinant hirudin, CGP 39393. Lancet. 1996;347(9001):635-9. DOI: 10.1016/S0140-6736(96)91200-3. https://doi.org/10.1016/S0140-6736(96)91200-3

4. PubChem. Desirudin, CID 16129703. https://pubchem.ncbi.nlm.nih.gov/compound/16129703 (accessed 2026-08-06).

5. World Anti-Doping Agency. 2026 Prohibited List. https://www.wada-ama.org/sites/default/files/2025-09/2026list_en_final_clean_september_2025.pdf

6. DrugBank. Desirudin (DB11095). https://go.drugbank.com/drugs/DB11095 (accessed 2026-08-06).