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Belumosudil

Belumosudil trade name Rezurock

Pregnancy category AU: D

Routes of administration By mouth

Belumosudil, is a medication used for the treatment of chronic graft versus host disease (cGvHD).

It is in the class of drugs known as serine/threonine kinase inhibitors.

It is an inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II).

Belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. 

This inhibits ROCK2-mediated signaling pathways which play major roles in pro- and anti-inflammatory immune cell responses. 

The  drug also has effects on oxidative phosphorylation, WNT signaling, angiogenesis, and KRAS signaling.

The most common side effects include infections, asthenia, nausea, diarrhea, dyspnea, cough, edema, hemorrhage, abdominal pain, musculoskeletal pain, headache, phosphate decreased, gamma glutamyl transferase increased, lymphocytes decreased, and hypertension.

It is considers it to be a first-in-class medication.

It is indicated for the treatment of people aged 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

Chronic GVHD causes inflammation and fibrosis in multiple tissues. 

Two cytokines controlled by the ROCK2 signaling pathway, IL-17 and IL-21, have a major role in the cGvHD response. 

ROCK2 inhibition with belumosudil targets both the immunologic and fibrotic components of cGvHD and reverses the symptoms of the disease.

It is approved belumosudil for people 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

Belumosudil dose is 200 mg taken orally once daily.

Increased ROCK activity has been found in the lungs of humans and animals with interstitial fibrosis

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