What kind of medicine is Besudil/Yilaike and what are its main ingredients?

Belumosudil mesylate tablets (Belumosudil), trade name REZUROCK, is an innovative small molecule targeted drug, mainly used to treat patients with chronic graft-versus-host disease (cGVHD) who have poor response to glucocorticoids or other systemic treatments. The drug was developed by Kadmon Pharmaceuticals and was approved by the U.S. Food and Drug Administration (FDA) in 2021. It is one of the few new targeted drugs specifically used for chronic graft-versus-host disease. Its main component is Belumosudil mesylate, which is a Rho-related coiled-coil kinase 2 (ROCK2) inhibitor and plays a therapeutic role by regulating immune signaling and inflammatory response.

In terms of pathological mechanism, chronic graft-versus-host disease is one of the common complications after allogeneic hematopoietic stem cell transplantation. It is characterized by donor immune cells attacking the recipient's normal tissues, resulting in chronic damage to the skin, liver, lungs and mucous membranes. Traditional treatment methods are mainly glucocorticoids, but some patients do not respond well to hormones or immunosuppressants, and new treatment options are urgently needed. The emergence of besudil brings hope to these patients.

Different from previous immunosuppressive treatments, Besudil can downregulate pro-inflammatory cytokines such as IL-17, IL-21, etc. by targeting the ROCK2 pathway, while promoting the recovery of regulatory T cells (Treg), thereby rebalancing the immune system. This mechanism helps reduce tissue inflammation and fibrosis processes and improve patients' clinical symptoms.

The molecular structure of Besudil has been specially designed to have high oral bioavailability. It is often administered in the form of tablets, which is easy to use and has good safety. At present, besudil has been included in the guideline recommendations of many countries and is one of the important second-line treatment options for chronic GVHD.

Reference: https://www.drugs.com/pro/rezurock.html