DANBURY, Conn., Dec. 4, 2018 /PRNewswire/ -- Perosphere Pharmaceuticals Inc. today announced the presentation of clinical
The oral presentation focused on the safety and efficacy of ciraparantag (PER977) in reversing the factor Xa novel oral anticoagulants (NOACs) apixaban and rivaroxaban. The studies found that ciraparantag acetate doses of 100 mg and higher showed complete and sustained reversal of both steady-state apixaban and rivaroxaban in age-matched healthy volunteers as measured by whole blood clotting time (WBCT). In previous clinical trials, ciraparantag had shown complete and sustained reversal of the NOAC, edoxaban, and the LMWH, enoxaparin, following a single intravenous bolus dose, as measured by WBCT.i,ii,iii The safety profile of ciraparantag in these current studies is consistent with previous trials; the most common adverse events were transient mild facial flushing and dysgeusia. No pro-coagulant signals were observed in any clinical trials to date.
"There is a significant unmet need for improved broad spectrum anti-coagulant reversal agents for patients who present with life threatening uncontrolled bleeding," said Dr. Sol Steiner, Executive Chairman of Perosphere Pharmaceuticals. "These findings build on the already strong clinical research supporting ciraparantag and they further demonstrate that it offers rapid, complete and sustained reversal for patients on any Xa NOAC or LMWH, in a convenient ready-to-use vial presentation."
In the current studies, healthy subjects age-matched to the patient population, 50 to 75 years old, were administered either 10 mg apixaban p.o. BID for 3.5 days or 20 mg rivaroxaban p.o. QD for 3 days to steady-state. At maximal activity, either four hours after the third daily dose of rivaroxaban or three hours after the seventh twice daily dose of apixaban subjects were randomized 3:1::active:placebo in 16 subject dosing cohorts of 100 mg, 200 mg or 300 mg intravenous ciraparantag acetate, or placebo saline. Pharmacodynamic response was measured by WBCT, a modernized and standardized Lee White clotting time, in which the time for freshly drawn venous whole blood to clot after activation in glass test tubes maintained at physiologic temperature is measured by blinded observers. In these studies there were no ciraparantag treatment-related serious adverse events.
About the Need for Anticoagulation Reversal Anticoagulation is utilized for the treatment and prevention of thrombosis in upwards of seven million patients annually in the United States. Despite the volume of anticoagulants used, as many as half of the patients who are candidates for treatment do not receive appropriate therapy, often due to concerns by both physicians and patients regarding increased risk of hemorrhage and associate morbidity (intracranial hemorrhage, transfusion, hypovolemia, shock, compartment syndrome, cardiac arrest). An additional serious consideration among patients receiving anticoagulants is disruption of therapy in the event of emergency surgery or invasive procedures resulting in elevated risk of thrombosis in the interim. In the United States for the 12 months ending June 2013, among patients treated with anticoagulants enoxaparin, rivaroxaban, apixaban and dabigatran, it is estimated that approximately 299,000 patients experienced bleeding with approximately 106,000 emergency room and 68,000 hospital admissions. Current therapies for the management of bleeding secondary to anticoagulation are supportive. Therefore, a single broad-spectrum reversal agent for the novel oral anticoagulants (NOACs), low-molecular-weight heparin and unfractionated heparin would provide an improved therapeutic option for these serious conditions while addressing an unmet medical need.
About PER977 PER977 is a small synthetic water-soluble new molecular entity that directly combines with the NOACs (i.e., direct Xa- and IIa- inhibitors), fondaparinux, low molecular weight heparins and unfractionated heparins allowing rapid re-establishment of a normal blood coagulation state. This reversal effect is due to direct binding to the anticoagulant molecule with no binding to blood coagulation factors or to other proteins in the blood. PER977 is undergoing clinical development as a sterile, intravenous injection. Phase 2 studies are nearing completion.
About Perosphere Pharmaceuticals Perosphere Pharmaceuticals is a private specialty pharmaceutical company focused on developing rescue medications. For more information, please visit www.perospherepharma.com.
i Ansell JE, Bakhru SH, Laulicht BE, Steiner SS, Grosso MA, Brown K, Dishy V, Lanz HJ, Mercuri MF, Noveck RJ, Costin JC. "Single-dose ciraparantag safely and completely reverses anticoagulant effects of edoxaban." Thromb Haemost. 2017 Jan 26;117(2):238-245. ii Ansell JE, Laulicht BE, Bakhru SH, Hoffman M, Steiner SS, Costin JC. "Ciraparantag safely and completely reverses the anticoagulant effects of low molecular weight heparin." Thromb Res. 2016 Oct;146:113-118. iii Ansell JE, Bakhru SH, Laulicht BE, Steiner SS, Grosso M, Brown K, Dishy V, Noveck RJ, Costin JC. "Use of PER977 to reverse the anticoagulant effect of edoxaban." N Engl J Med. 2014 Nov 27;371(22):2141-2.
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SOURCE Perosphere Pharmaceuticals Inc.
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