RADNOR, Pa.—(BUSINESS WIRE)— PolyMedix, Inc. (OTC BB: PYMX, http://polymedix.com), an emerging biotechnology company developing new therapeutic drug products to treat infectious diseases and acute cardiovascular disorders based on biomimetics, has initiated dosing and commenced a second clinical trial, a Phase 1B pilot proof of concept study, in the U.S. with its anticoagulant reversing agent PMX-60056 under an Investigational New Drug application (IND) filed with the U.S. Food and Drug Administration (FDA). PMX-60056 represents a new class of drug, which PolyMedix calls a heptagonist, and is believed to be the only reversing agent for heparin and the Low Molecular Weight Heparins (LMWH) in clinical development.
The second clinical trial is being conducted in healthy volunteers, and will involve first administering heparin to healthy subjects, and then afterwards administering a single dose of PMX-60056. This study is intended primarily to assess the safety of using PMX-60056 in heparinized subjects, and will also measure the ability of PMX-60056 to neutralize heparin and normalize blood clotting time. This study is utilizing a crossover double-blind design, and is planned to be conducted in a total of six subjects. Results are expected by the end of 2009. Following this clinical trial, significant additional clinical studies and regulatory submissions will be required to obtain regulatory approval from the FDA and other regulatory bodies before PMX-60056 could be commercially sold.
Heparin and LMWH are widely used anticoagulants, drugs to prevent blood clotting. However, they have the risk of potentially serious bleeding side effects. Protamine is currently the only approved drug used to reverse the action of heparin, and there is no approved reversing agent for LMWH. However, there are serious potential side effects associated with protamine. Based on preclinical studies conducted by PolyMedix and its collaborators, potential advantages of PMX-60056 over protamine may include reduced bleeding complications, reduced risk of immune-mediated side effects, and the ability to neutralize LMWH.
PMX-60056 was designed to bind to the pentasaccharide region found on heparin and LMWH. PMX-60056 is believed to form a stable electrostatic bond to heparin and LMWH, blocking its action. This molecular combination is believed to persist until removed from circulation by normal processes. In previous studies conducted by PolyMedix and other groups, PMX-60056 has been demonstrated to reverse the action of heparin in isolated human plasma, isolated human whole blood, and in animal studies in rats and dogs.
On March 11, 2009 PolyMedix announced the completion of the first Phase 1 clinical study with PMX-60056. That ascending single-dose intravenous pharmacokinetic and safety study was also conducted in healthy volunteers, and met the necessary Phase I goals of defining both a limiting single dose for ten-minute infusions and also the plasma distribution/elimination kinetics for the drug in the absence of heparin.