Contemporary developments in the discovery of selective factor Xa inhibitors: A review

Area of Science:

• Cardiovascular Medicine
• Pharmacology
• Medicinal Chemistry

Background:

• Thrombosis, a significant cause of death in cardiovascular diseases like myocardial infarction (MI) and acute coronary syndrome (ACS), leads to substantial morbidity and mortality.
• Current antithrombotic therapies, including vitamin K antagonists and heparin analogs, present limitations such as bleeding risks, narrow therapeutic windows, and inconvenient administration.
• There is a critical unmet medical need for safe, orally active anticoagulants.

Purpose of the Study:

• To review and compile research on the development of novel oral anticoagulants targeting Factor Xa (FXa).
• To provide an overview of Factor Xa inhibitors reported since 2010.
• To highlight advancements in creating small, safe, and orally bioavailable FXa inhibitors.

Main Methods:

• Literature review of scientific publications and research work on Factor Xa inhibitors.
• Compilation of studies focusing on the development of orally active anticoagulants.
• Analysis of research efforts in medicinal chemistry aimed at modulating blood coagulation.

Main Results:

• Factor Xa has emerged as a key target for developing new oral anticoagulants.
• Significant research efforts have focused on identifying and synthesizing small molecule FXa inhibitors.
• The period since 2010 has seen considerable progress in the development of orally bioavailable FXa inhibitors.

Conclusions:

• Factor Xa inhibitors represent a promising therapeutic strategy for anticoagulation.
• Continued research is essential to optimize the safety and efficacy of oral FXa inhibitors.
• The development of these inhibitors addresses the demand for safer and more convenient antithrombotic treatments.