Abstract
Objective: The present study compared the bioavailability of subcutaneous (s.c.) Chemi Enoxaparin with Clexane (80 mg/0.8 mL) under fasting conditions in healthy subjects. Materials and methods: This study was an open-label, randomized, single-dose, two-treatment period crossover study. We included healthy male and female subjects aged 18 – 55 years with a body mass index of 18 – 30 kg/m2. The primary pharmacodynamic endpoints were anti-FIIa and anti-FXa activity. Bioequivalence was achieved when the 95% confidence interval (CI) for the geometric means of Cmax and AUC0–t was between 80.00 and 125.00%. Results: 47 subjects were randomized for the treatment sequences. The 95% CI of the ratios of the geometric least squared means of anti-FXa activity was 96.28 – 102.65 IU/mL for Cmax and 100.67 – 105.15 h×IU/mL for the AUC0–t of Chemi Enoxaparin compared with those of Clexane, and for anti-FIIa activity, they were 86.65 – 96.73 IU/mL for the Cmax and 87.72 – 97.25 h×IU/mL AUC0–t, which met the criterion for bioequivalence. The number of subjects reporting at least 1 treatment-emergent adverse event (TEAE) was low, mostly of mild severity, and similar for both compounds. Conclusion: Chemi enoxaparin is bioequivalent to the reference enoxaparin, and both compounds show similar tolerability and safety profiles.
Highlights
Enoxaparin is a low-molecular-weight heparin (LMWH) that, like unfractionated heparin, acts at the final common pathway of the coagulation cascade
It was first approved and marketed in France in 1987, and thereafter became available in most countries worldwide, including the United States in 1993. It is currently indicated in the European Union (EU) for prophylaxis of venous thromboembolic disease in moderate- and high-risk surgical patients or medical patients with an acute illness, such as acute heart failure, respiratory insufficiency, severe infections or rheumatic diseases; in those with reduced mobility who are at increased risk of venous thromboembolism; for the treatment of deep vein thrombosis and pulmonary embolism; for the prevention of thrombus formation in extra-corporeal circulation during hemodialysis; and for the treatment of acute coronary syndrome, including treatment of unstable angina and non-ST-segment elevation myocardial infarction, in combination with oral acetylsalicylic acid, and the treatment of acute ST-segment elevation myocardial infarction [4]
Three of the randomized subjects were withdrawn; 2 subjects were withdrawn because of 2 serious adverse events that were unrelated to the study medications, and 1 subject was withdrawn at the request of the sponsor due to menstrual irregularities. 47 patients were included in the safety population, and 44 patients were in the pharmacokinetic population (Supplemental Figure 1)
Summary
Enoxaparin is a low-molecular-weight heparin (LMWH) that, like unfractionated heparin, acts at the final common pathway of the coagulation cascade. A large number of randomized clinical trials have demonstrated that enoxaparin was effective in several arterial thromboembolic disorders, such as unstable angina, acute coronary syndrome, and ST-elevation myocardial infarction, in patients who underwent elective percutaneous coronary intervention, and in the prophylaxis or treatment of venous thromboembolism [3]. It was first approved and marketed in France in 1987, and thereafter became available in most countries worldwide, including the United States in 1993. Compared with other parenteral anticoagulants, including unfractionated heparin, enoxaparin has several advantages: rapid and predictable absorption, higher bioavailability, and once- or twice-daily dosing, which favor home-based administration without the need of monitoring [3]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: International journal of clinical pharmacology and therapeutics
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
