Orally Available Inhibitors of Factor Xa

Morphochem AG, a leader in novel chemistries for small molecule drug discovery, has announced that one of its leading programmes, inhibitors of blood coagulation Factor Xa, led to the identification of novel, orally available anti-thrombotics in preclinical studies. Details of these preclinical studies will be presented at a meeting of investment analysts and pharmaceutical executives to be held in Basel on 21st November.
Commenting on the Factor Xa programme, Dr Lutz Weber, CEO of Morphochem said,

“Our strategy is to progress series of compounds into development as we apply the drug discovery engine that we built. The Factor Xa compounds are validating this approach. They have emerged from our protease target platform, are generated by applying our novel MCR chemistries and proprietary MolMind© technologies, and have moved from assay implementation to advanced preclinical compounds in less than three years, a significant achievement.”

A novel series of low molecular weight compounds which demonstrate direct inhibition of Factor Xa have been synthesized using Morphochem?s integrated evolutionary chemistry. Data from preclinical studies demonstrate that the lead compounds are highly effective and specific. Good oral availability and reduced side effects were reported. These parameters could lead to significant pharmaco-economic benefits through decreased patient hospitalisation and decreased monitoring of blood coagulation parameters respectively.

Dr Peter Seufer-Wasserthal, Vice President Business Development of Morphochem, commented,

“An orally available inhibitor for Factor Xa is actively sought in the pharmaceutical industry as a cost effective and safe anti-thrombotic. We are now in active discussions with several pharmaceutical companies to explore the optimum strategy for clinical development of our compounds.”

The anti-thrombotics market covers a multitude of venous or arterial thrombotic disorders, such as deep vein thrombosis (DVT), unstable angina, myocardial infarction, and stroke. Currently this market is worth over $ 8 billion, with approximately a fifth related to DVT prophylaxis, and therapy in hip and knee surgery. Orally available direct inhibitors of Factor Xa are believed to have a market potential of $ 1 billion in various indication areas.