Is Besudil/Yilaike a targeted drug? What is its mechanism of action?

Belumosudil mesylate tablets (Belumosudil) is a targeted therapy drug, but its "targeting" concept is not a single tumor mutation target in the traditional sense, but precise regulation of the core pathogenesis of chronic graft-versus-host disease. This is also the key reason why it has received high attention in the field of immune-related diseases.

The core mechanism of action of Besudil is to selectively inhibitRho-related coiled-coil protein kinase 2 (ROCK2). The ROCK signaling pathway plays an important role in immune cell differentiation, inflammatory response, and fibrosis. Overseas studies believe that in patients with chronic GVHD, abnormal ROCK2 activity is closely related to increased expression of pro-inflammatory T cell factors, immune imbalance and tissue fibrosis, and Besudil plays a role by regulating this key node.

Different from traditional broad-spectrum immunosuppressants, Besudil does not simply "suppress immunity", but is more inclined to reshape immune balance. During its action, on the one hand, it can downregulate the activity of factors related to pro-inflammatory pathways and reduce the sustained damage of abnormal immune responses to target organs such as the skin, liver, and lungs; on the other hand, it can help restore part of the regulatory immune function, thereby reducing long-term hormone dependence and the risk of organ fibrosis. This "bidirectional regulation" property gives it unique advantages in the long-term management of chronic GVHD.

From the perspective of targeted drugs, besudil does not rely on specific gene mutation detection for use, but is based on targeted intervention at the disease pathway level, which is more in line with the pathological characteristics of chronic GVHD, an immune disorder disease. This also makes it highly applicable in clinical practice, especially for patients who have poor response to glucocorticoids or other systemic treatments.

Therefore, from the perspective of pharmacological mechanism, treatment concept and clinical positioning, besudil is undoubtedly a targeted therapy drug with clear targets and mechanism basis. Its emergence also marks the entry into a more refined era of chronicGVHD treatment.

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