Disease relevance of Rivaroxaban

• No other clinically relevant differences were observed, suggesting that rivaroxaban is unlikely to require dose adjustment for body weight or gender [1].
• Rivaroxaban has undergone extensive Phase II studies for venous thromboembolism prevention after orthopaedic surgery, and Phase III studies have begun [2].
• The primary end point (composite of any deep vein thrombosis, objectively confirmed pulmonary embolism, and all-cause mortality) was observed in 14.9%, 10.6%, 8.5%, 13.5%, 6.4%, and 25.2% of patients receiving 5, 10, 20, 30, and 40 mg rivaroxaban, and 40 mg enoxaparin, respectively (n=618, per-protocol population) [3].

High impact information on Rivaroxaban

• This randomized, two-way crossover study, with a naproxen run-in period, was performed to determine whether naproxen influences the tolerability, pharmacodynamics and pharmacokinetics of rivaroxaban [4].
• Least squares-means ratios for the AUC and C(max) of rivaroxaban after administration alone and with naproxen were 1.125 [90% confidence interval (CI) 0.995, 1.271] and 1.095 (90% CI 0.905, 1.325), respectively [4].
• Rivaroxaban inhibited Factor Xa activity by 35% and prolonged prothrombin time [by 1.4 times baseline (tb)], activated partial thromboplastin time (1.3 tb) and the HepTest (1.9 tb) [4].
• Rivaroxaban and naproxen given together significantly increased bleeding time compared with rivaroxaban alone (P = 0.017) [4].
• Naproxen had no influence on these measures and the combination of rivaroxaban and naproxen did not affect platelet aggregation [4].

Chemical compound and disease context of Rivaroxaban

• METHODS AND RESULTS: This randomized, double-blind, double-dummy, active-comparator-controlled, multinational, dose-ranging study assessed the efficacy and safety of once-daily rivaroxaban relative to enoxaparin for prevention of venous thromboembolism in patients undergoing elective total hip replacement [3].

Biological context of Rivaroxaban

• Aspirin did not affect the pharmacokinetics of rivaroxaban, including the fraction unbound [5].
• C(max) of rivaroxaban was unaffected in subjects >120 kg but was increased by 24% in subjects weighing </=50 kg, resulting in a small (15%) increase in prolongation of prothrombin time, which was not considered clinically relevant [1].

Associations of Rivaroxaban with other chemical compounds

• CONCLUSIONS: Rivaroxaban showed efficacy and safety similar to enoxaparin for thromboprophylaxis after total hip replacement, with the convenience of once-daily oral dosing and without the need for coagulation monitoring [3].

Analytical, diagnostic and therapeutic context of Rivaroxaban

• This was a randomized, 2-way crossover study in healthy male subjects, with an aspirin run-in period, to examine whether aspirin influences the safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban [5].
• A once-daily, oral, direct Factor Xa inhibitor, rivaroxaban (BAY 59-7939), for thromboprophylaxis after total hip replacement [3].

References