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Drug intelligence / Profile preview
A selective ROCK2 inhibitor is a class of small molecule therapeutics designed to selectively target and inhibit Rho-associated coiled-coil-containing protein kinase 2 (ROCK2) while sparing ROCK1. ROCK2 is a key regulator of cellular pathways involved in inflammation, fibrosis, metabolism, and gene expression. By selectively inhibiting ROCK2, these agents can downregulate pro-inflammatory Th17 cells, upregulate regulatory T cells (Tregs), and reduce pro-fibrotic signaling. Selective ROCK2 inhibitors, such as belumosudil and GV101, are being developed and utilized for various indications, including chronic graft-versus-host disease (cGvHD), multiple sclerosis, cerebral cavernous malformations, and fibrotic diseases.
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