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Rezurock Dosage

Belumosudil is the first and best-in-class ROCK2 inhibitor, specifically designed as an immunomodulator to target both the inflammatory and fibrotic/sclerotic manifestations of cGVHD.1

Belumosudil decreases activation of STAT3, triggering the significant downregulation of both Th17 and Tfh cells, leading to the downregulation of pro-inflammatory cytokines (IL-21, IL-17).1,4

↓ Inflammation

Belumosudil increases phosphorylation of STAT5, causing the upregulation of Treg cells.3 Overall, this has an immunomodulatory effect on STAT3 and STAT5 phosphorylation, reducing inflammation.1,4

200 mg once daily administered orally6

REZUROCK® (belumosudil) is indicated for the treatment of adult and pediatric patients 12 years and older with cGVHD after failure of at least two prior lines of systemic therapy.6

Belumosudil prevents the polymerization of G-actin to F-actin, including the downregulation of MRTF-related profibrotic gene expression.5

↓ Fibrosis

Belumosudil downregulates fibrosis, as demonstrated by decreased collagen deposition around the bronchioles and the delayed progression of scleroderma in animal cGVHD models.2

Abbreviations

ROCK2: Rho associated coiled-coil containing protein kinase 2; STAT3: Signal transducer and activator of transcription 3; Th:  helper cells; Tfh: T follicular helper cells; IL-21 : Interleukin-21; IL-17: Interleukin-17; Treg: Regulatory  ; STAT5: Signal transducer and activator of transcription 5; G-actin: Globular protein; F-actin: Filamentous protein; MRTF: Myocardin-related transcription factor; cGVHD: Chronic graft-versus-host disease.

  1. Zanin-Zhorov et al. Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism. Proc Natl Acad Sci USA. 2014;111(47):16814-16819. doi:10.1073/pnas.1414189111
  2. Flynn et al. Targeted rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism. Blood. 2016;127(17):2144-2154. doi:10.1182/blood-2015-10-678706
  3. Chen et al. ROCK2, but not ROCK1 interacts with phosphorylated STAT3 and co-occupies TH17/TFH gene promoters in TH17-activated human T cells. Sci Rep. 2018;8(1):16636. doi:10.1038/s41598-018-35109-9
  4. Weiss et al. ROCK2 signaling is required to induce a subset of T follicular helper cells through opposing effects on STATs in autoimmune settings. Sci Signal. 2016;9(437):ra73. doi:10.1126/scisignal.aad8953
  5. Riches et al. ROCK and Rho: promising therapeutic targets to ameliorate pulmonary fibrosis. Am J Pathol. 2015;185(4):909-912. doi:10.1016/j.ajpath.2015.01.005
  6. Rezurock USPI. https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214783s000lbl.pdf
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