Rezurock (belumosudil) 200 mg film-coated tablets

Rezurock (belumosudil) is an oral kinase inhibitor primarily used for the treatment of chronic graft-versus-host disease (cGVHD) in patients who have failed at least two prior lines of systemic therapy. cGVHD is a serious complication that can occur after a bone marrow or stem cell transplant, where the donated cells attack the recipient’s body. Rezurock works by inhibiting a specific enzyme that regulates immune and fibrotic responses, helping to reduce inflammation and fibrosis, thus improving symptoms of cGVHD. Each film-coated tablet contains 200 mg of belumosudil, and it is typically prescribed by specialists in hematology or oncology. Rezurock offers a novel approach to managing cGVHD, addressing both immune system dysregulation and fibrosis.

How It Works

Belumosudil, the active ingredient in Rezurock, is a ROCK2 inhibitor (Rho-associated coiled-coil kinase 2). ROCK2 plays a critical role in regulating the immune response, fibrosis, and tissue inflammation, which are hallmarks of chronic graft-versus-host disease.

Mechanism of Action:

1. Inhibition of ROCK2: Belumosudil specifically inhibits the ROCK2 pathway, which is involved in various immune and inflammatory processes. By blocking this pathway, it reduces the activation of immune cells and pro-inflammatory cytokines.
2. Reduction of Fibrosis: In cGVHD, fibrosis is a key component of disease progression, where tissues become scarred and thickened. Belumosudil helps to decrease fibrosis by preventing the deposition of extracellular matrix proteins in affected tissues.
3. Modulation of T-Cell Responses: Belumosudil suppresses the activity of pathogenic T-cells that are responsible for attacking the recipient’s organs, while promoting the activity of regulatory T-cells, which help restore immune tolerance.

By addressing both inflammation and fibrosis, Rezurock offers a dual approach in managing cGVHD, improving patients’ quality of life and reducing the severity of symptoms.

Side Effects

While Rezurock can offer significant benefits for patients with cGVHD, it may also cause side effects. The following list includes common and serious side effects reported by patients.

Common Side Effects:

• Fatigue: Many patients report feeling unusually tired or lethargic.
• Nausea: Gastrointestinal discomfort, including nausea, is a common complaint.
• Diarrhea: Frequent bowel movements or loose stools are frequently observed.
• Upper Respiratory Tract Infection: Some patients may develop mild respiratory infections.
• Cough: A persistent cough can occur in some individuals.
• Headache: Mild to moderate headaches may be experienced.

Serious Side Effects:

• Hepatotoxicity: Liver function abnormalities, including increased liver enzymes, can occur, necessitating monitoring of liver function.
• Severe Infections: Patients may be at increased risk for serious infections due to immune suppression.
• Pulmonary Complications: Some patients may experience worsening of lung-related symptoms, such as shortness of breath.
• Hypersensitivity Reactions: Although rare, serious allergic reactions may occur, such as rash, swelling, or difficulty breathing.

Indications

Rezurock is specifically indicated for the treatment of patients with chronic graft-versus-host disease (cGVHD) who have failed at least two prior lines of systemic therapy. This is a condition in which the transplanted donor immune cells attack the recipient’s organs and tissues, leading to inflammation, fibrosis, and potentially life-threatening complications.

Approved Indications:

1. Chronic Graft-Versus-Host Disease (cGVHD): Rezurock is used in patients whose cGVHD has not responded to other treatments, helping to manage symptoms such as skin tightening, organ damage, and immune system dysregulation.

Contraindications

There are certain situations in which Rezurock should not be used or should be used with caution.

Contraindications:

1. Severe Hypersensitivity to Belumosudil: Patients with known severe allergic reactions to belumosudil or any component of Rezurock should avoid the medication.
2. Severe Liver Impairment: Patients with severe hepatic dysfunction may experience worsened liver problems with Rezurock, and should be closely monitored.
3. Active Severe Infections: Because Rezurock can suppress the immune system, it is contraindicated in patients with active severe infections.
4. Pregnancy and Breastfeeding: Rezurock may pose risks to a developing fetus or nursing infant, and it should be avoided during pregnancy and lactation.

Price in Different Countries

Rezurock’s price can vary greatly depending on the country, availability, and whether patients have insurance coverage for rare disease medications. Below is a table showing estimated prices for Rezurock in different regions.

Country	Price (Per Tablet)	Reference
United States	$500 – $600	GoodRx
United Kingdom	£450 – £550	NHS
Canada	CAD $650 – $750	Canada Pharmacy
Australia	AUD $700	PBS Australia
India	INR ₹35,000 – ₹40,000	1mg

Top 5 Global Brands

Rezurock is produced by Kadmon Pharmaceuticals, a key player in the field of hematology and oncology. However, there are other major companies known for their contributions to treatments for chronic graft-versus-host disease and immune-related conditions.

1. Kadmon Pharmaceuticals

• Kadmon Pharmaceuticals is the manufacturer of Rezurock and specializes in treatments for autoimmune diseases, immune system disorders, and cancer.

2. Novartis

• Novartis is a global pharmaceutical leader involved in the development of therapies for immune-related conditions, including drugs for graft-versus-host disease.

3. Bristol-Myers Squibb

• Bristol-Myers Squibb develops treatments for immune modulation and cancer, including drugs used in transplant medicine and related complications.

4. Pfizer

• Pfizer has a broad portfolio of drugs that address immune system disorders and inflammation, and is involved in developing innovative treatments for cGVHD.

5. Gilead Sciences

• Gilead Sciences focuses on developing therapies for inflammatory conditions and immune modulation, making it a significant player in the treatment of graft-versus-host disease.