Belumosudil is a prescription medication used to manage certain medical conditions. It works by influencing specific pathways within the body.
Treating Chronic Graft-versus-Host Disease
Chronic graft-versus-host disease (cGVHD) is a serious complication that can occur after an allogeneic hematopoietic stem cell transplant. This procedure involves transferring healthy blood-forming stem cells from a donor to a recipient, typically to treat certain cancers or blood disorders. In cGVHD, the donor’s immune cells recognize the recipient’s cells as foreign and begin to attack them, leading to inflammation and damage in various organs and tissues throughout the body.
The disease can manifest in almost any organ, including the skin, mouth, eyes, liver, and lungs, causing significant discomfort and impairing organ function. Belumosudil, marketed as Rezurock by Kadmon Pharmaceuticals, received approval from the U.S. Food and Drug Administration (FDA) on July 16, 2021, for treating adult and pediatric patients 12 years and older with cGVHD. It is specifically prescribed when patients have not responded adequately to at least two prior systemic therapies.
How Belumosudil Works
Belumosudil functions as a selective inhibitor of Rho-associated coiled-coil containing protein kinase 2, often referred to as ROCK2. This enzyme plays a role in various cellular processes, including immune cell function and inflammation. By inhibiting ROCK2, belumosudil helps to modulate the immune system’s response.
The inhibition of ROCK2 by belumosudil can lead to a reduction in certain pro-inflammatory cytokines, such as interleukin-17 and interleukin-21, which contribute to the inflammatory and fibrotic processes seen in cGVHD. It also promotes the development and function of regulatory T cells, which help to suppress excessive immune activity. This dual action helps to restore balance to the immune system and reduce the harmful inflammation and tissue damage associated with chronic graft-versus-host disease.
Taking Belumosudil
Belumosudil is available as an oral tablet and is taken once a day. The usual dosage for both adults and pediatric patients 12 years and older is 200 mg. Swallow the tablets whole; do not cut, crush, or chew them.
For optimal absorption, take belumosudil with a meal at approximately the same time each day. If a dose is missed, take it as soon as possible on the same day, but do not take extra doses to compensate. Follow your healthcare provider’s instructions regarding dosage and administration.
Potential Side Effects and Important Information
Belumosudil can cause side effects. Common side effects include:
Infections
Fatigue
Nausea
Diarrhea
Abdominal pain
Dyspnea
Cough
Swelling
Bleeding
Musculoskeletal pain
Headache
Decreased phosphate levels
Changes in liver enzyme levels (gamma glutamyl transferase)
Reduced lymphocyte counts
Seek medical attention if you experience severe nausea, vomiting, diarrhea, or signs of multi-organ failure. Liver function should be monitored during treatment; dose adjustments or discontinuation may be necessary if liver enzyme levels become significantly elevated. Belumosudil should be avoided in patients with moderate or severe liver dysfunction not related to cGVHD. Individuals who are pregnant or breastfeeding should discuss the potential risks and benefits with their healthcare provider before starting this medication.