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Article Abstract
Sepsis-induced coagulopathy (SIC) is a severe and frequent complication of sepsis, which is associated with high mortality in patients. So far, attempts have failed to establish a global standard of care in this difficult-to-treat indication. Anticoagulation with a dual inhibitor of the coagulation factors IIa (FIIa, thrombin) and Xa (FXa) has the potential to improve the treatment of life-threatening acute coagulation disorders, such as SIC. Herein, we describe the discovery of BAY 3389934 hydrochloride (), a potent and highly selective, direct dual FIIa/Xa inhibitor, with high solubility suited for application. This small molecule acts as a metabolically soft active pharmaceutical ingredient (API) due to a labile carboxylic ester group, which is responsible for the desired short pharmacokinetic and pharmacological half-life (), resulting in a high controllability of the pharmacological action.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC12207585 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.5c00538 | DOI Listing |
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