Lepirudin is a recombinant hirudin analogue and a direct thrombin inhibitor. It binds directly and specifically to thrombin, inhibiting its enzymatic activity and preventing the conversion of fibrinogen to fibrin.
Lepirudin was developed from hirudin, a naturally occurring anticoagulant originally identified in medicinal leeches. It is a peptide-based biological pharmaceutical ingredient used as an anticoagulant in specific clinical settings.
Lepirudin is a specialized peptide/biological pharmaceutical API requiring controlled recombinant production, purification and extensive biological and physicochemical characterization.
Important quality attributes include identity, purity, peptide integrity, biological activity, aggregation, host-cell proteins, residual DNA, endotoxins, bioburden and sterility.
CAS Number: 138068-37-8
Molecular Formula: C287H440N80O110S6
Molecular Weight: Approximately 6963.3 Da
Drug Class: Anticoagulant
Pharmacological Class: Direct Thrombin Inhibitor
Therapeutic Class: Antithrombotic Agent
Therapeutic Area: Hematology / Cardiovascular
Lepirudin binds directly to thrombin, including both its catalytic site and fibrin-binding region.
Thrombin is a central enzyme in the coagulation cascade. By inhibiting thrombin, lepirudin reduces:
Lepirudin has been used as an anticoagulant in patients with heparin-induced thrombocytopenia (HIT) and associated thrombotic complications.
Its clinical use and availability depend on the applicable regulatory status and local treatment guidelines.
Lepirudin is structurally related to hirudin, a highly specific natural thrombin inhibitor. Unlike heparin, which enhances the activity of antithrombin, lepirudin acts by directly binding to thrombin.
This direct mechanism makes it pharmacologically distinct from indirect anticoagulants.
Typical recombinant production may involve:
Lepirudin quality evaluation may include:
Lepirudin should be stored according to validated stability data and approved product requirements. Temperature control and protection from inappropriate environmental conditions are important for maintaining peptide/protein stability.
Lepirudin is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |