Ceritinib (Zykadia) is a targeted therapy indicated for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC). As a second-generation ALK inhibitor, it has demonstrated significant efficacy in clinical practice.

Dosage and Administration of Ceritinib (Zykadia)

Recommended Standard Dosage

The recommended standard dosage of ceritinib is 450 mg orally once daily, taken with food.

Treatment should be continued until disease progression or the occurrence of unacceptable toxicities.

Administration Precautions

If a dose is missed, it should be taken as soon as remembered, unless it is less than 12 hours before the next scheduled dose.

If vomiting occurs after administration, do not take an additional dose; resume the next scheduled dose as planned.

Dietary Effects

Clinical studies have shown that administration with food significantly increases the bioavailability of ceritinib compared to fasting.

Notably, dose optimization studies have demonstrated that 450 mg of ceritinib taken with food achieves similar steady-state plasma concentrations to 750 mg taken on an empty stomach.

Dose Adjustments for Ceritinib (Zykadia)

Gastrointestinal Adverse Reactions

If severe or intolerable nausea, vomiting, or diarrhea occurs and is unresponsive to antiemetic or antidiarrheal therapy, discontinue ceritinib temporarily.

Resume treatment at the next lower dose after symptom improvement.

Hepatotoxicity

Discontinue ceritinib temporarily if alanine aminotransferase (ALT) or aspartate aminotransferase (AST) elevations exceed 5 times the upper limit of normal (ULN) with total bilirubin ≤ 2 times ULN.

Resume treatment at the next lower dose when liver function tests recover to baseline or ≤ 3 times ULN.

QT Interval Prolongation

Discontinue ceritinib temporarily if the QTc interval exceeds 500 milliseconds, confirmed by two independent electrocardiograms (ECGs).

Resume treatment at the next lower dose when the QTc interval decreases to < 481 milliseconds or returns to baseline.

Hyperglycemia

Discontinue ceritinib temporarily if persistent hyperglycemia > 250 mg/dL occurs and is unresponsive to optimized antidiabetic therapy.

Resume treatment at the next lower dose after adequate glycemic control is achieved.

Use in Special Populations

Patients with Hepatic Impairment

For patients with severe hepatic impairment (Child-Pugh Class C), it is recommended to reduce the ceritinib dose by approximately one-third, rounded to the nearest multiple of 150 mg.

Pregnant and Lactating Women

Based on its mechanism of action and animal study results, ceritinib may cause fetal harm.

Females of reproductive potential should use effective contraception during treatment and for 6 months after the completion of therapy.

Male patients with female partners of reproductive potential should use condoms during treatment and for 3 months after the completion of therapy.