What important information is contained in the detailed instructions for Besudil/Elaco

1. Drug name

Common name: Besudil mesylate tablets,Belumosudil

Applicable age:12 years old and above

2. Indications

Belumosudil mesylate tablets (Belumosudil) is an oral small molecule kinase inhibitor, mainly suitable for patients with chronic graft-versus-host disease (cGVHD), especially those who have insufficient response to glucocorticoids or other systemic treatments. cGVHD is a common immune-related complication after hematopoietic stem cell transplantation. Patients may suffer from skin, liver, oral cavity and other organ involvement. By regulating immune signals and inhibiting inflammatory responses, this product can improve disease activity, delay disease progression, and provide new treatment options for refractory patients.

3. Usage and dosage

The recommended dose is oral administration, 200 mg once daily. It should be continued under the guidance of a physician until the patient's chronic graft-versus-host disease progresses and new systemic therapy is required. The medicine can be taken with food and does not need to be taken on an empty stomach. If you miss a dose, take it as soon as possible after discovering it. Do not take a double dose at one time. During treatment, it is recommended to regularly monitor blood routine, liver function, kidney function, blood pressure and other indicators in order to adjust the dose in a timely manner to ensure efficacy and safety.

4. Pharmacological effects

This product is an inhibitor of Rho-related coiled-coil forming protein kinase (ROCK). It can inhibit the activities of ROCK2 and ROCK1 at the same time. Its half inhibitory concentration (IC50) is about 100 nM and 3 μM respectively. By inhibiting ROCK2, this product can regulate T cell signaling pathways, including STAT3/STAT5 phosphorylation levels, change Th17/Treg immune balance, and thereby downregulate pro-inflammatory responses. In in vitro studies, this product has also shown activity in inhibiting aberrant pro-fibrotic signaling. In the in vivo cGVHD animal model, this product showed good anti-inflammatory and anti-fibrotic effects, providing a theoretical basis for clinical treatment.

5. Adverse reactions

In clinical studies, common adverse reactions of this product include infection, fatigue, nausea, diarrhea, dyspnea, cough, edema, bleeding, abdominal pain, musculoskeletal pain and headache, incidence rate≥20%. In addition, laboratory abnormalities are also common, including decreased serum phosphorus, increased gamma-glutamyl transferase, decreased lymphocyte count, and hypertension. Some adverse reactions may be relieved with dose adjustment or supportive treatment. Patients should closely observe their symptoms during medication. If serious infection, significant increase in blood pressure, or difficulty breathing occurs, they should seek medical treatment immediately and communicate with the doctor about the treatment plan.

6. Medication monitoring

To ensure safety and efficacy, it is recommended to regularly monitor the following indicators during treatment:

Routine blood count, including platelet, white blood cell and lymphocyte counts;

Liver function indicators, such asALT, AST and bilirubin levels;

Changes in kidney function and blood pressure;

Observe clinical symptoms, such as signs of infection, bleeding, and changes in organ function.

7. Dosage adjustment

If adverse reactions occur, the dose can be adjusted according to the doctor's advice, including temporarily stopping the drug, reducing the dose, or extending the dosing interval. Dose adjustment should be based on patient tolerance and laboratory test results to ensure that the therapeutic effect is maintained while controlling adverse reactions.

8. Storage and precautions

This product should be sealed and stored no more than25℃. It should be placed in the original packaging to prevent moisture. Please close the cap tightly after each use and do not discard the desiccant. Please keep this product out of the reach of children to avoid accidental ingestion. Avoid high temperature, humidity or direct light to maintain drug stability.

9. Precautions

This product is a prescription drug and a doctor should evaluate the patient's condition and indications before use.

Pregnant and lactating patients should consult a doctor before use.

Be aware of drug interactions when using other medications simultaneously, especially immunosuppressants and blood pressure medications.

If serious adverse reactions occur or the condition worsens during treatment, the drug should be discontinued immediately and medical guidance should be sought.

Reference: https://www.drugs.com/pro/rezurock.html