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letermovir

Brand: 老挝大熊
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Letermovir is a cell proliferation virus terminal transferase inhibitor that blocks the DNA replication process of CMV and inhibits virus proliferation by inhibiting the activity of the CMV DNA terminase complex (including pUL51, pUL56 and pUL89).

1. Drug name

1. Common name: Letermovir

2. English name: Letermovir

3. Trade name: PR EVYMIS®

II. Indications

1. For the prevention of CMV infection and disease in cytomegalovirus (CMV) seropositive (R+) allogeneic hematopoietic stem cell transplantation (HSCT) recipients 6 months and older and weighing at least 6kg.

2. For the prevention of CMV disease in high-risk (donor CMV positive/recipient CMV negative, D+/R-) kidney transplant recipients aged 12 years and above, weighing at least 40kg.

3. Specifications and properties

Tablet: 240mg

4. Main ingredients

1. Active ingredient: Letermovir (Letermovir)

2. Excipients include: colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, povidone, etc. The injection also contains hydroxypropyl betacyclodextrin.

V. Usage and Dosage

1. Adults and patients over 12 years old, weighing ≥30kg (HSCT) or ≥40kg (kidney transplant): The recommended dose is 480mg, taken orally or intravenously infused once a day (infusion time is 1 hour).

2. Children with HSCT from 6 months to under 12 years old or weighing <30kg: Adjust the dose according to body weight.

3. Treatment cycle: HSCT recipients usually need to wait until 100 days after transplantation, and the treatment period for high-risk patients can be extended to 200 days; for kidney transplant recipients, the treatment period lasts until 200 days after transplantation.

4. Oral tablets can be taken with food or alone, and need to be swallowed whole

VI. Dose adjustment

1. When combined with cyclosporine, the dose of letermovir in patients 12 years old and above should be reduced to 240 mg once a day; children under 12 years old need to adjust the dose according to body weight.

2. Patients with moderate to severe liver damage (Child-PughB or C) should use it with caution, and use with severe liver damage (Child-PughC) is not recommended.

3. Patients with renal insufficiency generally do not need to adjust the dose, but serum creatinine needs to be monitored when using injections (because hydroxypropyl betacyclodextrin may accumulate).

7. Medication Precautions

1. It can be taken before or after meals.

2. If you miss a dose, you should take it as soon as possible; if it is close to the next dose time, skip the missed dose and do not take double dose.

3. If vomiting occurs after taking the medicine, it is not recommended to take a supplementary dose. The next dose should be taken as originally planned.

4. Injections are only used for patients who cannot take oral medications and should be converted to oral preparations as soon as possible.

5. Injections must use infusion bags and infusion sets that do not contain diethylhexyl phthalate (DEHP).

8. Medication for special groups

1. Pregnant women: There is no sufficient human data, and the pros and cons need to be weighed.

2. Lactation period: It is unknown whether it will enter breast milk, so use with caution.

3. Children: It can be used in HSCT recipients over 6 months old and kidney transplant recipients over 12 years old. The safety has not been established for those at younger age or lower body weight.

4. Elderly people: No dose adjustment is required.

9. Adverse reactions

1. Common symptoms in HSCT recipients: Nausea, diarrhea, vomiting, peripheral edema, cough, headache, fatigue, and abdominal pain.

2. Common symptoms in kidney transplant recipients: Diarrhea.

3. Adverse reactions in children are similar to those in adults.

4. Injections may cause nephrotoxicity or ototoxicity due to accumulation of hydroxypropyl betacycline (based on animal data).

10. Contraindications

1. It is forbidden to use it in combination with pimozide and ergot alkaloids.

2. When used in combination with cyclosporine, it is prohibited to use pitavastatin or simvastatin together.

11. Drug interactions

1. Letermovir is a CYP3A and moderate inhibitor and OATP1B1/3 inhibitor. When used together, it may increase the concentration of drugs metabolized through these pathways.

2. Combined use with cyclosporine will significantly increase the concentration of letermovir, and the dose needs to be adjusted.

3. Avoid using it in combination with strong inducers such as rifampicin, carbamazepine, and St. John's wort, which may cause letermovir to be ineffective.

12. Storage method

1. Tablets: Store in original packaging, moisture-proof, 20°C–25°C (15°C–30°C allowed).

2. All dosage forms should be kept out of the reach of children.