Sexual HealthEndotis Pharma Reports Successful Completion Of Phase I Program With EP42675, A First In Class Synthetic Parenteral Anticoagulant
Endotis Pharma, the biopharmaceutical company dedicated to the discovery and development of small-glyco drugs for applications in thrombosis and oncology, announced that EP42675 has successfully completed its Phase I program.
EP42675 is the first representative of a new class of synthetic, parenteral, antithrombotic drugs with a dual mechanism of action combining an indirect factor Xa inhibitor and a direct thrombin inhibitor in a single molecule. Thus, EP42675 inhibits both thrombin formation and activity.
EP42675 was well tolerated in 100 healthy subjects enrolled in five phase I, including single-dose and multiple ascending dose studies and a pharmacodynamic interaction study with a combination of oral aspirin and clopidogrel. The only drug-related adverse effects were minor episodes of bleedings (mostly at the injection or blood sampling site) explained by the anticoagulant activity of EP42675. Vital signs, physical examination, ECG (including the QTc interval) and safety laboratory parameters did not show any treatment-emergent clinically relevant abnormalities.
Treatment with EP42675 resulted in dose-dependent increases in standard and specific coagulation tests, and decrease in thrombin generation. The pharmacodynamic and pharmacokinetic time-profiles of EP42675 followed a parallel pattern, with a low intra and inter subjects variability. Further details will be provided at the International Society of Thrombosis and Hemostasis (ISTH) congress to be held this July in Boston, since two abstracts have been accepted.
Eric Neuhart, head of Endotis Pharma"s clinical Research and Development department commented: "EP42675 is the first representative of a new class of parenteral synthetic anticoagulants combining indirect Xa inhibition and direct free and clot-bound thrombin inhibition. EP42675 has a predictable pharmacokinetic and pharmacodynamic profile and therefore is expected to be used either intravenously or subcutaneously at a fixed dose regimen, without the need for routine anticoagulation monitoring."
Eric Neuhart added: "Endotis is also developing EP217609, the neutralizable form of EP42675, and in parallel its specific antidote avidin. Both drugs are expected to enter Phase I this summer. Avidin is able to neutralize the anticoagulant activity of EP217609, and should represent a clinically relevant advantage in the treatment of major bleeding and prevention of major bleeding risk over reference anticoagulants. Endotis" strategy is to pursue the clinical development of this new class of anticoagulant with EP217609 in the treatment of patients with acute coronary syndromes undergoing a percutaneous coronary intervention, the first target indication".
Charles Woler, Endotis Pharma"s Chief Executive Officer added: "The successful completion of a fully fledged Phase I program with EP42675 proves that Endotis" clinical team is able to organize and execute high-quality studies. The scientific value of the data generated has been acknowledged as the results of these studies will be presented at the ISTH congress. Looking beyond this first success, the development of other parenteral and oral anticoagulants is progressing well and should enable Endotis to benefit from a broad and unique anticoagulant franchise, including neutralizable drugs such as EP217609".
Endotis Pharma