• Anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC).

Contraindicated in:

• Congenital long QT syndrome.
• OB: Pregnancy
• Lactation: Lactation

Use Cautiously in:

• Moderate to severe hepatic impairment/severe renal impairment (CCr <30 mL/min)
• HF, bradycardia, electrolyte abnormalities, or concurrent use of QT prolonging medications
• Concurrent use of strong CYP3A4 inhibitors
• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: QT interval prolongation, BRADYCARDIA, TORSADES DE POINTES.

Derm: rash, photosensitivity.

Endo: hyperglycemia.

F and E: hypophosphatemia.

GI: ↓ appetite, ↑ lipase, ↑ liver enzymes, abdominal pain, constipation, diarrhea, esophagitis/reflux/dysphagia, nausea, vomiting, HEPATOTOXICITY, PANCREATITIS.

GU: ↑ serum creatinine.

Hemat: anemia.

Neuro: fatigue.

Resp: INTERSTITIAL LUNG DISEASE/PNEUMONITIS.

Drug-Drug:

• Concurrent use of strong CYP3A inhibitors including ketoconazole, nefazodone, and ritonavir ↑ levels and risk of toxicity; avoid concurrent use; if unavoidable, ↓ ceritinib dose.
• Strong CYP3A inducers, including carbamazepine, phenytoin, and rifampin may ↓ levels and effectiveness; avoid concurrent use.
• May ↑ levels and risk of toxicity of CYP3A substrates, including midazolam; avoid concurrent use; if unavoidable, ↓ dose of CYP3A substrate.
• May ↑ levels and risk of toxicity of CYP2C9 substrates, including warfarin; avoid concurrent use; if unavoidable, ↓ dose of CYP2C9 substrate.
• Beta-blockers, diltiazem, verapamil, digoxin, and clonidine may ↑ risk of bradycardia; avoid concurrent use, if possible.
• Concurrent use of QT interval prolonging medications may ↑ risk of QT interval prolongation and torsades de pointes.

Drug-Natural Products:

• St. John's wort ↓ levels and effectiveness; avoid concurrent use.

Drug-Food:

• Grapefruit/grapefruit juice ↑ levels and the risk of toxicity; avoid concurrent ingestion.

• Tablets: 150 mg;

• PO (Adults): 450 mg once daily; continue until disease progression or unacceptable toxicity; Concurrent use of strong CYP3A inhibitors: ↓ dose by 1/3, rounded to the nearest 150-mg strength.

Zykadia

• Acts as a tyrosine kinase inhibitor, inhibiting anaplastic lymphoma kinase as well as other kinases, resulting in decreased growth of certain malignant cell lines.

• Slowed progression of metastatic NSCLC.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Absorption follows oral administration; food significantly ↑ absorption and may ↑ risk of adverse reactions.

Distribution: Slight preference to distribute from plasma into red blood cells.

Metabolism/Excretion: Metabolized in the liver (mostly by CYP3A) and is a substrate of P-glycoprotein (P-gp); 68% eliminated unchanged in feces, 1.3% in urine.

Half-life: 41 hr.

(clinical response)

• Instruct patient to take ceritinib as directed. Take missed doses as soon as remembered unless within 12 hr of next dose. If vomiting occurs, do not administer additional dose, continue with next scheduled dose. Instruct patient to read Patient Information prior to starting therapy and with each Rx refill in case of changes.
• Inform patient to avoid consuming grapefruit and grapefruit juice during therapy.
• Advise patient to notify health care professional if nausea, vomiting, and diarrhea is severe or persistent; if signs and symptoms of hepatotoxicity (feeling tired, itchy skin, skin or whites of eyes turn yellow, nausea and vomiting, decreased appetite, pain on right side of stomach, dark or brown, tea-colored urine, bleed or bruise easily); pneumonitis; QTc interval prolongation or bradycardia (new chest pain, changes in heartbeat, palpitations, dizziness, fainting, or changes in or use of a new heart or BP medication); hyperglycemia (increased thirst, increased hunger, headaches, trouble thinking or concentration, urinating often, blurred vision, tiredness, breath smells like fruit), or pancreatitis (upper abdominal pain that may spread to the back and get worse with eating) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other Rx, OTC, or herbal products, especially St. John's Wort.
• Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraceptives during and for 6 mo and to avoid breast feeding during and for 2 wk following completion of therapy. Advise patient to notify health care provider if pregnancy is planned or suspected. Advise males with female partners of reproductive potential to use condoms during therapy and for 3 mo following completion of therapy.

se-RI-ti-nib

NDC Code^*

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0640- ZYKADIA
    • 0078-0640-70- 70 CAPSULE in 1 BOTTLE (0078-0640-70)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0694- ZYKADIA
    • 0078-0694-48- 21 TABLET, FILM COATED in 1 BOTTLE (0078-0694-48)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0694- ZYKADIA
    • 0078-0694-84- 84 TABLET, FILM COATED in 1 BOTTLE (0078-0694-84)