来法莫林(Xenleta)的注意事项和药物相互作用

While using Xenleta, treatment progress needs to be checked regularly and any adverse reactions should be monitored.

Precautions for Xenleta

1. QT interval prolongation

It may prolong the QT interval of the electrocardiogram.

Avoid use in patients with known QT prolongation, ventricular arrhythmias (such as torsade de pointes), and current use of Class IA or Class III antiarrhythmic drugs or other drugs that can prolong the QT interval (such as antipsychotics, macrolide antibiotics, fluoroquinolones, tricyclic antidepressants).

If it must be used, it is recommended to conduct electrocardiogram monitoring and strictly follow the recommended dose and infusion rate.

2. Embryo-fetal toxicity

Animal studies have shown that lefamoren may cause damage to the fetus, leading to post-implantation loss, stillbirth and developmental delay.

Before taking the drug, it is necessary to confirm whether women of childbearing potential are pregnant, and it is recommended that they take effective contraceptive measures during treatment and within 2 days after the last dose.

3. Clostridium difficile-associated diarrhea (CDAD)

Almost all antibacterial drugs may cause Clostridium difficile-associated diarrhea, which may develop into fatal colitis in severe cases.

If the patient develops diarrhea during medication or within 2 months after discontinuing medication, it should be evaluated whether it is Clostridium difficile-related diarrhea. If necessary, antibacterial drugs that are not specific to Clostridium difficile should be discontinued and corresponding treatment measures should be taken.

4. Development of drug-resistant bacteria

To avoid the development of drug resistance, lefamorelin should only be used for confirmed or highly suspected bacterial infections.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Precautions for drug interactions with lefamoren (Xenleta)

1. Strong or moderate CYP3A inducers/P-gp inducers (such as rifampicin)

will reduce the blood concentration of lefamorelin, which may lead to a decrease in efficacy. Unless the benefits outweigh the risks, combined use should be avoided; if combined use is necessary, close monitoring of efficacy is required.

2. Strong CYP3A inhibitors/P-gp inhibitors (such as ketoconazole)

will significantly increase the exposure to lefamoren and increase the risk of adverse reactions. Concomitant use with lefamoren tablets is prohibited.

3. Moderate CYP3A inhibitors/P-gp inhibitors

Adverse reactions need to be monitored when combined with lefamoren tablets.

4. CYP3A substrates

Lefamoren tablets can significantly increase the plasma concentration of sensitive CYP3A substrates (such as midazolam, diltiazem, verapamil), and it is prohibited to be combined with CYP3A substrates that can prolong the QT interval. Toxic reactions need to be closely monitored when combined with other sensitive substrates.

Lefamoren injection does not affect the pharmacokinetics of CYP3A substrates.

5. Drugs that prolong the QT interval

Avoid combination with Class IA/III antiarrhythmic drugs, antipsychotics, macrolides, fluoroquinolones, etc.

Storage conditions of Xenleta

Xenleta tablets are blue oval film-coated tablets with black “LEF600” printed on one side. Tablets contain 600 mg of lefamorelin and should be stored at 20°C to 25°C (68°F to 77°F). Short-term storage is permitted within the range of 15°C to 30°C (59°F to 86°F).