Ceritinib

Ceritinib, as one of the important drugs for the treatment of ALK-positive non-small cell lung cancer, has been widely used and recognized around the world.

1. Drug name

1. Generic name: Ceritinib (Ceritinib)

2. Trade name: ZYKADIA®

2. Indications

It is used to treat adult patients with metastatic non-small cell lung cancer (NSCLC) who are ALK-positive and confirmed to be ALK-positive by FDA-approved testing methods.

3. Specifications and properties

Capsule : 150mg

4. Main ingredients

Active ingredient: Ceritinib.

5. Usage and dosage

1. Recommended dosage of : 450mg orally, once a day, take with food.

2. Missed dose of : If it is >12 hours before the next dose, you can take it again, otherwise skip it.

3. Vomiting : No need to retake the dose, take the next dose as originally planned.

6. Dose adjustment of

1. The first reduction of : 300mg/day; the second reduction of : 150mg/day; if intolerable, discontinue the drug.

2. Situations that require adjustment :

Severe gastrointestinal reactions (such as diarrhea, vomiting);

Hepatotoxicity (ALT/AST elevation >5 times ULN);

QTc interval prolongation>500ms;

Hyperglycemia>250 mg/dL;

Pancreatitis (amylase/lipase>2 times ULN).

7. Medication precautions

1. Take with food:

Reduce gastrointestinal adverse reactions.

2. Drug interactions :

Avoid the combined use of strong CYP3A inhibitors/inducers (such as ketoconazole, Rifampin);

Avoid co-administration of -sensitive CYP3A substrate (such as midazolam) or CYP2C9 substrate (such as warfarin).

3. Monitoring requirements :

Liver function (monthly), electrocardiogram (QT interval), fasting blood glucose, pancreatic enzymes (amylase/lipase).

8. Medication for special groups

1. Pregnant women: may cause harm to the fetus and requires contraception (for women during treatment and 6 months after stopping the drug, for men 3 months after stopping the drug).

2. Lactation period : Breastfeeding is prohibited.

3. Liver injury : Patients with Child-Pugh C grade need to reduce the dose by 1/3.

9. Adverse reactions

1. Common (≥25%) :

Diarrhea, nausea, vomiting, abdominal pain, fatigue.

2. Serious adverse reactions :

Hepatotoxicity (28% ALT elevation), ILD/pneumonitis (2.4%), QT prolongation, hyperglycemia (13% grade 3-4), pancreatitis.

10. Contraindications

There are no absolute contraindications, but it should be used with caution in patients with QT prolongation, bradycardia, and severe liver damage.

11. Drug interactions

1. CYP3A inhibitor/inducer : Adjust the dose or avoid combined use.

2. QT prolonging drugs : Such as antiarrhythmic drugs, close monitoring is required.

3. Drugs that cause bradycardia : For example, β-blockers, avoid combined use.

12. Storage method

If it is not clearly stated, it is recommended to refer to the instructions and keep it in the original packaging, away from light and moisture.