Belumosudil mesylate (KD025 mesylate) is a selective ROCK2 inhibitor with IC50 values of 105 nM for ROCK2 and 24 μM for ROCK1, demonstrating anti-fibrotic properties.

ROCK2:105 nM (IC50), ROCK1:24 μM (IC50)

Belumosudil (SLx-2119; 40 μM) significantly reduces Tsp-1 and CTGF mRNA levels in PASMC. Additionally, microarray analysis reveals that aRNA from HMVEC treated with Belumosudil exhibits a background five times higher than that of other arrays[1].

Belumosudil (KD-025), administered intraperitoneally at doses of 100, 200, or 300 mg/kg, has been shown to reduce infarct volume in a dose-dependent manner following transient middle cerebral artery occlusion. Its efficacy is consistent across different demographics, including aged, diabetic, or female mice, matching or exceeding that observed in normal adult male subjects[2].