Valuable Targets

What are factor Xa inhibitors and how do you quickly get the latest development progress?

8 December 2023
4 min read

Factor Xa inhibitors are a class of anticoagulant drugs that work by inhibiting Factor Xa, a key enzyme in the coagulation cascade. The development of Factor Xa inhibitors began in the early 1980s, with the first inhibitor, antistasin, being isolated from the salivary glands of the Mexican leech Haementeria officinalis in 1987. 

Four drugs from this class are currently marketed worldwide. Rivaroxaban (Xarelto) was the first approved Factor Xa inhibitor, becoming commercially available in Europe and Canada in 2008. This was followed by the approval of apixaban (Eliquis) in Europe in 2011 and in the United States in 2012. Edoxaban (Lixiana, Savaysa) was approved in Japan in 2011 and in Europe and the US in 2015. The most recent addition to this class is betrixaban (Bevyxxa), which was approved in the US in 2017¹

Looking ahead, Factor Xa inhibitors are expected to continue to play a significant role in anticoagulant therapy. They are just as efficacious as low molecular weight heparin (LMWH) and warfarin but are given orally and don't need as strict monitoring. However, the emergence of resistance and the lack of an effective reversal drug when bleeding occurs are challenges that need to be addressed. Ongoing research and development efforts are focused on addressing these issues and expanding the clinical applications of Factor Xa inhibitors

The analysis of target factor Xa in the pharmaceutical industry reveals a competitive landscape with multiple companies focusing on its development. Pfizer Inc., Bristol Myers Squibb Co., AstraZeneca PLC, Daiichi Sankyo Co., Ltd., and Bayer AG are among the companies growing the fastest under this target. The indications for drugs targeting factor Xa cover a wide range of cardiovascular and thrombotic conditions, indicating their potential in treating these diseases. Small molecule drugs, chemical drugs, and recombinant coagulation factors are progressing rapidly under this target. The European Union, the United States, and Japan are leading in terms of drug development, but China has also shown progress. Further analysis is required to understand the specific progress in China and its impact on the future development of target factor Xa. Overall, target factor Xa presents a promising opportunity in the pharmaceutical industry with a diverse range of companies, indications, drug types, and countries/locations involved in its development.

The mechanism of action of factor Xa inhibitors

Factor Xa inhibitors are a type of medication that specifically target and inhibit the activity of factor Xa, which is a key enzyme involved in the blood clotting process. From a biomedical perspective, factor Xa is a crucial component of the coagulation cascade, a series of reactions that leads to the formation of blood clots. By inhibiting factor Xa, these medications prevent the formation of blood clots and reduce the risk of conditions such as deep vein thrombosis, pulmonary embolism, and stroke.

Factor Xa inhibitors work by binding to factor Xa and blocking its ability to activate other clotting factors, ultimately preventing the formation of a stable blood clot. This mechanism of action makes them anticoagulant drugs, meaning they help to prevent the excessive formation of blood clots.

These inhibitors are commonly used in the treatment and prevention of thromboembolic disorders, such as atrial fibrillation, venous thromboembolism, and post-operative prophylaxis. Examples of factor Xa inhibitors include rivaroxaban, apixaban, and edoxaban.

It's important to note that factor Xa inhibitors carry a risk of bleeding, as they interfere with the normal clotting process. Therefore, their use should be carefully monitored, and patients may require regular blood tests to assess their coagulation status. Additionally, factor Xa inhibitors should be used with caution in individuals with certain medical conditions or those taking other medications that increase the risk of bleeding.

Catalog of factor Xa Inhibitors

The currently marketed factor Xa inhibitors include:

For more information, please click on the image below.

What is the purpose of using factor Xa inhibitors?

Factor Xa inhibitors that are used to prevent and treat thromboembolic disorders. For more information, please click on the image below to log in and search.

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How can I get the most recent advancements in factor Xa inhibitors?

In the Synapse database, you can keep abreast of the latest research and development advances of factor Xa inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

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