Seritinib’s complete Chinese instruction manual download guide

1. Generic names: Ceritinib, Ceritinib

Product name: Zykadia, Zykadia

Other names: ceritinib, ceritinib

2. Indications:

Ceritinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK) positive on an FDA-approved test.

3. Usage and dosage:

1. Patient selection: Based on the presence of ALK positivity in tumor specimensSelect patients with metastatic non-small cell lung cancer treated with ZYKADIA.

2. Recommended dose: The recommended dose of ceritinib is450 mg, taken orally once a day with food until disease progression or unacceptable toxicity occurs. If a dose of ceritinib is missed, make up the dose unless the next dose is due within 12 hours. If vomiting occurs during treatment, do not administer additional doses and continue with the next scheduled dose of ceritinib.

3. Dose adjustment of adverse reactions: Adverse reactions may occur when using ceritinib. The dose of the drug can be adjusted under the guidance of a doctor. The first dose of ceritinib can be reduced300mg;< span>The second dose is reduced150 mg; it is taken orally once daily with food. Patients who cannot tolerate150 mg should discontinue ceritinib.

(1) StrongCYP3A inhibitors: During treatment, avoid concurrent use of strongCYP3A inhibitors. If concurrent use of a strong CYP3A inhibitor is unavoidable, reduce the ZYKADIA dose by approximately one-third, rounding to the nearest multiple of the 150 mg dose strength. After discontinuing a strong CYP3A inhibitor, resume the dose of ceritinib that was taken before taking the strong CYP3A inhibitor.

(2) Patients with severe hepatic impairment: For patients with severe hepatic impairment (Child-Pugh C), reduce the ceritinib dose by approximately one-third, rounding to the nearest multiple of the 150 mg dose strength.

4. Adverse reactions:

In clinical studies of ceritinib, the most common adverse reactions (incidence≥25%) were diarrhea, nausea, vomiting, fatigue, abdominal pain, decreased appetite, and weight loss.

5. Supply and storage:

Seritinib capsules are stored at a temperature of 20°C to 25°C (68°F to 77°F); excursions are allowed between 15°C and 30°C (59°F to 86°F).

6. Mechanism of action:

Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among them, cilitinib is the most effective against ALK. Ceritinib inhibited ALK autophosphorylation, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and ALK-dependent cancer cell proliferation in in vitro and in vivo assays.

Ceritinib inhibited the in vitro proliferation of cell lines expressingEML4-ALK and NPM-ALK fusion proteins and showed dose-dependent inhibition of the growth of EML4-ALK-positive NSCLC xenografts in mice and rats. Ceritinib demonstrated dose-dependent antitumor activity in mice bearing EML4 ALK-positive NSCLC xenografts, exhibiting resistance to crizotinib at concentrations within the clinically relevant range.

Reference materials:https://go.drugbank.com/drugs/DB09063