ceritinib

Contraindicated in:

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

Use Cautiously in:

HF, bradycardia, electrolyte abnormalities, or concurrent use of QT prolonging medications;
Severe renal impairment;
Moderate or severe hepatic impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: BRADYCARDIA, QT interval prolongation, TORSADES DE POINTES

Derm: rash, photosensitivity

Endo: hyperglycemia

F and E: hypophosphatemia

GI: ↑lipase, ↑liver enzymes, abdominal pain, constipation, diarrhea, dysphagia, gastroesophageal reflux, nausea, vomiting, HEPATOTOXICITY, PANCREATITIS

GU: ↑serum creatinine

Hemat: anemia

Metab: ↓appetite

Neuro: fatigue

Resp: INTERSTITIAL LUNG DISEASE (ILD)/PNEUMONITIS

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors, including ketoconazole, nefazodone, and ritonavir may ↑ levels and risk of toxicity; avoid concurrent use; if concurrent use necessary, ↓ 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 concurrent use necessary, ↓ CYP3A substrate dose.
May ↑ levels and risk of toxicity of CYP2C9 substrates, including warfarin; avoid concurrent use; if concurrent use necessary, ↓ CYP2C9 substrate dose.
Beta-blockers, diltiazem, verapamil, digoxin, ivabradine, and clonidine may ↑ risk of bradycardia; avoid concurrent use.
QT interval prolonging medications may ↑ risk of QT interval prolongation and torsades de pointes.

Drug-Natural Products:

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

Drug-Food:

Grapefruit/grapefruit juice may ↑ levels and risk of toxicity; avoid concurrent use.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 450 mg once daily; continue until disease progression or unacceptable toxicity; Concurrent use of strong CYP3A inhibitors:↓ dose by ⅓, rounded to the nearest 150-mg strength.

Hepatic Impairment

PO (Adults ): Severe hepatic impairment:↓ dose by ⅓, rounded to the nearest 150-mg strength.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Slowed progression of metastatic NSCLC.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Food significantly ↑ absorption and may ↑ risk of adverse reactions.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A isoenzymes. 68% eliminated unchanged in feces, 1.3% in urine.

Half-Life: 41 hr.

Time/Action Profile ⬆ ⬇

(clinical response)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4–6 hr‡	7.1–7.4 mo

‡Plasma concentrations

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Advise 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.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
Advise 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/symptoms of hepatotoxicity (feeling tired, itchy skin, skin or whites of eyes turn yellow, nausea and vomiting, ↓ 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 (↑ thirst, ↑ 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.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraceptives during and for 6 mo and to avoid breastfeeding during and for 2 wk following completion of therapy. Advise patient to notify health care provider if pregnancy is planned or suspected. Advise men with female partners of reproductive potential to use condoms during therapy and for 3 mo following completion of therapy.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

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)

54893- MSN Laboratories Private Limited
- 54893-0072-
  - 54893-0072-4- 20 kg in 1 DRUM (54893-0072-4)

66828- Novartis Pharma Produktions GmbH
- 66828-0254-
  - 66828-0254-1- 25000 TABLET, FILM COATED in 1 DRUM (66828-0254-1)

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Indications ⬇

Contraind./Precautions ⬆ ⬇