What are the side effects of Ceritinib (Zykadia)?

ceritinib lung cancer

Ceritinib is the second-line treatment for patients with non-small cell lung cancer with an ALK gene translocation. It is used when the tumor is at an advanced stage and is no longer sensitive to Crizotinib.

Very common side effects (may occur in more than 1 in 10 patients)

  • Diarrhea
  • Nausea and/or vomiting
  • Heart Burn

Common side effects (may occur in more than 1 in 100 patients)

  • Liver toxicity (hepatotoxicity)
  • Reduced heart rate (brachycardia)

Rare side effects (may occur in more than 1 in 10,000 patients)

  • Pneumonia. Your doctor should be contacted in the event of an acute and/or unexplained onset of or worsening dyspnea, cough, fever.
  • Hyperglycemia
  • Pancreatic toxicity, with an elevation of amylases and lipases.

Fertility, pregnancy and lactation

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. It is recommended that women do not become pregnant and men should refrain from generating children during treatment with ceritinib, as it may harm the baby.

If there is a possibility that the person taking this medicine may become pregnant or become a father, he will have to use a valid contraceptive method for the duration of the treatment and for at least 90 days after completion of the therapy, as oral contraceptives may not be effective if taken concomitantly with ceritinib.

How to take Ceritinib

The commercially available tablets are 150 mg. The recommended dose is 750 mg a day, equivalent to taking 5 tablets. The capsules should be taken once a day, every day at the same time. They must be swallowed whole with water and must not be chewed or crushed.

They should not be taken on an empty stomach and food should not be ingested in the two hours before and in the two subsequent doses.

Pharmacokinetic interactions

During treatment with Zykadia, concomitant use of potent CYP3A inhibitors should be avoided. Therefore, concomitant use of the following drugs is not recommended:

  • phenytoin, carbamazepine or phenobarbital – used for seizures or convulsions;
  • ketoconazole, ritonavir, saquinavir, telithromycin, itraconazole, voriconazole, posaconazole and nefazodone – used in the treatment of certain viral and fungal infections;
  • rifabutin or rifampicin – used for the treatment of tuberculosis (TB);
  • St. John’s wort (Hypericum perforatum) – a herbal medicine used for the treatment of depression;
  • warfarin – used for blood clots;
  • alfentanil, fentanyl and other painkillers – used for operations;
  • rosuvastatin – used to lower the cholesterol level.

Ceritinib demonstrates a pH-dependent solubility and becomes poorly soluble with increasing pH in vitro. Therefore, agents that reduce stomach acidity, such as proton pump inhibitors, H2 receptor antagonists or antacids, can alter the solubility of ceritinib and reduce its bioavailability, hence its efficacy and are not recommended. 

If they cannot be avoided, they must be taken at a distantly from ceritinib. H2 receptor antagonists are preferred over proton pump inhibitors.

Patients should avoid eating grapefruit or drinking grapefruit juice during treatment.

– Therapies for ALK positive patients