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ceritinib (Zykadia)
Tyrosine Kinase Inhibitors

How it is administered

Ceritinib is taken by mouth, usually as a tablet or capsule. The recommended dose for adults is 450 mg once daily with food. If a dose is missed and the next dose is not due within 12 hours, take the missed dose as soon as possible. If vomiting occurs after taking a dose, do not take an extra dose; continue with the next scheduled dose.

How it works

Ceritinib is a type of targeted therapy known as a kinase inhibitor. It works by blocking specific proteins called kinases, particularly the anaplastic lymphoma kinase (ALK). In some cancers, including certain types of non-small cell lung cancer (NSCLC), the ALK gene is abnormally activated, leading to uncontrolled cell growth. Ceritinib inhibits ALK and other related proteins, which helps to slow or stop the growth of cancer cells.

By targeting the ALK protein, ceritinib can be effective in treating cancers that have this specific genetic change. It is especially useful for patients whose cancer has become resistant to other ALK inhibitors.

Common side effects

  • Diarrhea
  • Nausea
  • Vomiting
  • Abdominal pain
  • Fatigue
  • Decreased appetite
  • Weight loss
  • Increased liver enzymes (ALT, AST)
  • Hyperglycemia (high blood sugar)
  • Rash
  • Constipation
  • Headache

Serious side effects can include liver problems, lung inflammation (pneumonitis), heart rhythm changes (QT prolongation, bradycardia), pancreatitis, and high blood sugar.

Who Should take it

Ceritinib is indicated for adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are ALK-positive, as detected by an FDA-approved test. This means it is used when the cancer has spread and tests show the presence of the ALK gene rearrangement.

It is generally prescribed for patients who have not received prior systemic therapy for metastatic disease or for those who have progressed on or are intolerant to other ALK inhibitors. Your doctor will determine if ceritinib is appropriate for you based on specific genetic testing of your tumor.

Who should not take it

Ceritinib does not have any absolute contraindications listed in its FDA label. However, it should be used with caution in certain situations:

  • If you have severe liver impairment, the dose may need to be adjusted.
  • Pregnant women should not take ceritinib, as it can harm an unborn baby.
  • It should not be used in combination with certain other medications that interact with its metabolism or cause similar side effects, such as drugs that prolong the QT interval or cause bradycardia.

Always inform your healthcare provider about all your medical conditions and medications before starting ceritinib.

Commonly used with

Ceritinib is typically used alone for the treatment of ALK-positive NSCLC. It is not commonly combined with other cancer medications, but supportive medications such as antiemetics (for nausea) or antidiarrheals may be used to manage side effects.

It is important to avoid taking ceritinib with medications that strongly affect liver enzymes (CYP3A inhibitors or inducers), as well as drugs that can prolong the QT interval or cause bradycardia.

Commonly tested with

Ceritinib has been compared in clinical trials to standard chemotherapy regimens, such as pemetrexed with cisplatin or carboplatin, followed by maintenance pemetrexed. It has also been tested in patients who previously received other ALK inhibitors, such as crizotinib.

Routine monitoring with blood tests (for liver function, blood sugar, and pancreatic enzymes) and electrocardiograms (ECGs) is recommended during treatment.

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