Related Experiment Video

Updated: Oct 25, 2025

Tail Vein Transection Bleeding Model in Fully Anesthetized Hemophilia A Mice
08:13

Tail Vein Transection Bleeding Model in Fully Anesthetized Hemophilia A Mice

Published on: September 30, 2021

6.7K

From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa

Robert M Knabb1, Ruth R Wexler2

  • 1Research and Development (retired), Bristol Myers Squibb Company, P.O. Box 5400, Princeton, NJ, 08543, USA.

Journal of Thrombosis and Thrombolysis
|August 5, 2021
PubMed

Insights

The development of oral factor Xa inhibitors, like Eliquis (apixaban), represents a significant advance in treating and preventing thromboembolic diseases by balancing efficacy and safety.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Cardiovascular Medicine

Background:

  • Thromboembolic diseases require treatments balancing efficacy and safety.
  • Current standards of care present challenges in achieving this balance.
  • Oral factor Xa inhibitors have emerged as a key therapeutic advance.

Purpose of the Study:

  • To describe the drug discovery program for Eliquis (apixaban).
  • To highlight the commitment to developing a compound with an optimal safety and efficacy profile.
  • To discuss the impact of oral factor Xa inhibitors in anticoagulation therapy.

Main Methods:

  • Retrospective account of the Eliquis (apixaban) discovery program.
  • Focus on the medicinal chemistry and pharmacological optimization process.
  • Evaluation of target product profile for anticoagulants.

Main Results:

  • Successful identification and development of apixaban (Eliquis).
  • Apixaban demonstrates a favorable profile for treating thromboembolic disorders.
  • Oral factor Xa inhibitors offer an improved therapeutic option.

Conclusions:

  • The discovery of apixaban exemplifies successful drug development in anticoagulation.
  • Optimizing for both efficacy and safety is crucial for new antithrombotic agents.
  • Oral factor Xa inhibitors have significantly advanced the management of thromboembolic diseases.
Keywords:
ApixabanEliquisFactor Xa inhibitorProteaseThrombosis

More Related Videos

Author Spotlight: Advancing Thrombolytic Testing by Integrating Flow Dynamics in In Vitro Models06:16

Author Spotlight: Advancing Thrombolytic Testing by Integrating Flow Dynamics in In Vitro Models

Published on: April 19, 2024

1.3K
Facilitating Drug Discovery: An Automated High-content Inflammation Assay in Zebrafish07:50

Facilitating Drug Discovery: An Automated High-content Inflammation Assay in Zebrafish

Published on: July 16, 2012

14.4K

Related Concept Videos

Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants01:18

Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants

Oral anticoagulants are vital tools in preventing and treating blood clotting disorders. This diverse class of medications can be categorized as vitamin K antagonists, exemplified by warfarin, and direct thrombin inhibitors (DTIs), such as dabigatran, as well as factor Xa inhibitors, including rivaroxaban.
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
1.5K
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
774
Venous Thrombosis III: Interprofessional Care01:29

Venous Thrombosis III: Interprofessional Care

Venous thrombosis requires effective prevention and treatment strategies to improve patient outcomes and reduce potential complications.Prevention StrategiesHealthcare providers must prioritize preventing venous thromboembolism (VTE) for all adult patients upon admission. Interventions depend on bleeding and thrombosis risk, medical history, current medications, diagnoses, planned procedures, and patient preferences. Patients on bed rest should change positions every two hours and, if not...
66
Anticoagulant Drugs: Low-Molecular-Weight Heparins01:30

Anticoagulant Drugs: Low-Molecular-Weight Heparins

Hemostasis is a crucial process that prevents excessive blood loss from damaged blood vessels. It involves various mechanisms such as vasoconstriction, platelet adhesion and activation, and fibrin formation. The importance of each mechanism depends on the type of vessel injury. In contrast, thrombosis is the abnormal formation of a blood clot within the blood vessels, leading to potential complications if the clot obstructs blood flow. Thrombosis can be caused by increased coagulability of the...
1.1K
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
9.7K
Biopharmaceutical Factors Influencing Drug Product Design: Overview01:22

Biopharmaceutical Factors Influencing Drug Product Design: Overview

Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though...
55