Generic Name: ceritinib
Date of Approval: April 29, 2014
Company: Novartis

Treatment for: Non-Small Cell Lung Cancer

FDA Approves Zykadia

The U.S. FDA has granted accelerated approval of Zykadia (ceritinib), an oral anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor for the treatment of patients with metastatic ALK-positive non-small cell lung cancer (NSCLC) who have been previously treated with Xalkori (crizotinib), the only other approved ALK tyrosine kinase inhibitor.

The accelerated approval is based on a pivotal trial that included 163 patients with metastatic ALK+ non-small cell lung cancer who progressed on or were intolerant to treatment with crizotinib. Among the previously-treated patients, just over half had their tumors shrink and this effect lasted on average just over seven months.

Zykadia capsules are taken once daily on an empty stomach, and patients must not consume grapefruit and grapefruit juice during treatment.

Common side effects include diarrhea, nausea, elevated transaminases, vomiting, abdominal pain, fatigue, decreased appetite and constipation. Patients receiveing Zykadia should also be monitored for hepatotoxicity, interstitial lung disease (ILD)/pneumonitis, QTc interval prolongation, hyperglycemia and bradycardia.

Patient Information

Read this Patient Information before you receive this medicine and each time you receive treatment. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.

Slideshow: Flashback: FDA Drug Approvals 2013

What is Zykadia?

Zykadia is a cancer medication that interferes with the growth and spread of cancer cells in the body.

It is used to treat patients with a certain type of advanced non-small cell lung cancer (NSCLC).

Important Information

Zykadia may cause serious side effects, including:
  • Stomach and gastrointestinal problems including diarrhea, nausea, vomiting, and stomach-area pain. These problems can sometimes be severe.
  • Liver problems. You will need to have blood tests every month while you are taking this medicine to monitor your liver function. Tell your healthcare provider right away if you have any of the following symptoms:
    • tiredness
    • itchy skin
    • yellowing of your skin or the whites of your eyes
    • nausea or vomiting
    • decreased appetite
    • abdominal pain
    • dark urine
    • unusual bleeding or bruising
  • Lung problems (pneumonitis). Severe swelling of the lungs during treatment may be life threatening. Tell your healthcare provider right away if you have any of the following new or worsening symptoms:
    • trouble breathing or shortness of breath
    • cough with or without mucous
    • fever
    • chest pain
  • Heart problems including very slow, very fast, or abnormal heartbeats. You will need to have your heart monitored while you are taking this medicine. Tell your healthcare provider right away if you feel new chest pain or discomfort, dizziness or lightheadedness, if you faint, or have abnormal heartbeats. Tell your healthcare provider if you start to take or have any changes in heart or blood pressure medicines.

What should I tell my healthcare provider before taking Zykadia?

Tell your healthcare provider about all of your medical conditions, including if you have:

  • liver problems
  • diabetes
  • heart problems, including a condition called long QT syndrome

FDA pregnancy category D. Zykadia may harm your unborn baby. Tell your healthcare provider if you are pregnant or plan to become pregnant. Women who are able to become pregnant should use an effective method of birth control during treatment, and for at least two weeks after stopping.

See also: Pregnancy and breastfeeding warnings (in more detail)

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if ceritinib passes into your breastmilk. You should not breastfeed while you are taking Zykadia.

Tell your healthcare provider about all the medicines you take, including prescription medicines, over-the-counter medicines, vitamins, and herbal supplements.

How should I take Zykadia?

  • Take this medicine exactly as your healthcare provider tells you. Do not change your dose or stop taking unless your healthcare provider tells you to.
  • Take your prescribed dose once a day on an empty stomach. Do not eat for two hours before and after your dose.
  • If you miss a dose, take it as soon as you remember. If your next dose is due within 12 hours, then skip the missed dose. Just take the next dose at your regular time.

What should I avoid?

  • You should not drink grapefruit juice or eat grapefruit during your treatment. It may increase the levels of the drug in your blood to a harmful level.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Zykadia dosing information

Usual Adult Dose for Non-Small Cell Lung Cancer:

  • 750 mg orally once daily on an empty stomach (two hours before or after a meal).

Zykadia side effects

See Important Information for a list of serious side effects.

Other serious side effects include:

  • High blood sugar (hyperglycemia). People who have diabetes or glucose intolerance or who take a corticosteroid medicine have an increased risk of high blood sugar. Follow your healthcare provider’s instructions about monitoring your blood sugar. Call your healthcare provider right away if you have any symptoms of high blood sugar, including:
    • increased thirst
    • increased hunger
    • headaches
    • trouble thinking or concentrating
    • increased urination
    • blurred vision
    • tiredness
    • breath that smells like fruit

The most common side effects include:

  • stomach and intestinal (gastrointestinal) problems including diarrhea, nausea, vomiting, abdominal pain, decreased appetite and constipation.
  • tiredness and fatigue

These are not all of the possible side effects. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

What other drugs will affect Zykadia?

Other drugs may interact with ceritinib, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

The following drugs are known to interact with ceritinib:

  • some azole antifungals including ketoconazole
  • some antivirals including ritonavir
  • some macrolide antibiotics including telithromycin
  • rifampin
  • carbamazepine
  • phenytoin
  • St. John’s Wort
  • alfentanil
  • cyclosporine
  • dihydroergotamine
  • ergotamine
  • fentanyl
  • pimozide
  • quinidine
  • sirolimus
  • tacrolimus
  • warfarin

Doses may need to be adjusted or treatments changed if you take any of these drugs.

How should I store Zykadia?

Store capsules at room temperature between 68°F to 77°F (20°C to 25°C).Keep all medicines out of the reach of children.

General information

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use this medicine for a condition for which it was not prescribed. Do not give it to other people, even if they have the same symptoms you have. It may harm them. You can ask your healthcare provider or pharmacist for more information.

What are the ingredients in Zykadia?

Active ingredient: ceritinib

Inactive ingredients: colloidal anhydrous silica, L-hydroxypropylcellulose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate

Capsule shell contains: gelatin, indiogotine, and titanium dioxide