Ceritinib

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Ceritinib Brand Name– Zykadia

What is Ceritinib

Ceritinib is an oral kinase inhibitor, primarily targeting anaplastic lymphoma kinase (ALK) but also insulin-like growth factor 1 (IFG-1) and ROS1.

It has demonstrated efficacy in the first-line metastatic non-small cell lung cancer (NSCLC) setting as well as after failure of crizotinib; unlike some other kinase inhibitors, ceritinib has also demonstrated efficacy on intracranial lesions in a subgroup analysis.

It is indicated for the treatment of ALK-positive NSCLC; approximately 1/3 of patients with ALK-positive NSCLC relapse due to an acquired mutation in the ALK tyrosine kinase domain or amplification of the ALK fusion gene.

Ceritinib has been associated with concentration-dependent QT prolongation and should be avoided if possible in patients with congenital long QT syndrome.

Coadministration of certain drugs may need to be avoided or dosage adjustments may be necessary; review drug interactions.

Indications

  • non-small cell lung cancer (NSCLC)

For the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC)

Side Effects

  1. abdominal pain
  2. abdominal pain
  3. acneiform rash
  4. anemia
  5. anemia
  6. anorexia
  7. anorexia
  8. asthenia
  9. asthenia
  10. back pain
  11. back pain
  12. blurred vision
  13. bradycardia
  14. constipation
  15. cough
  16. dehydration
  17. diarrhea
  18. diarrhea
  19. dizziness
  20. dizziness
  21. dysesthesia
  22. dyspepsia
  23. dysphagia
  24. dyspnea
  25. elevated hepatic enzymes
  26. elevated hepatic enzymes
  27. fatigue
  28. fatigue
  29. fever
  30. gastroesophageal reflux
  31. GI bleeding
  32. headache
  33. headache
  34. hepatotoxicity
  35. hyperamylasemia
  36. hyperamylasemia
  37. hyperbilirubinemia
  38. hyperbilirubinemia
  39. hyperglycemia
  40. hyperglycemia
  41. hypoesthesia
  42. hypophosphatemia
  43. hypophosphatemia
  44. hypotonia
  45. infection
  46. maculopapular rash
  47. musculoskeletal pain
  48. musculoskeletal pain
  49. nausea
  50. nausea
  51. neutropenia
  52. neutropenia
  53. pancreatitis
  54. paresthesias
  55. pericardial effusion
  56. pericarditis
  57. pericarditis
  58. peripheral neuropathy
  59. photopsia
  60. pneumonitis
  61. pneumonitis
  62. pruritus
  63. pruritus
  64. QT prolongation
  65. QT prolongation
  66. rash
  67. rash
  68. renal failure (unspecified)
  69. seizures
  70. thrombocytopenia
  71. thrombocytopenia
  72. visual impairment
  73. vomiting
  74. vomiting
  75. weakness
  76. weight loss
  77. weight loss

Monitoring Parameters

  • blood glucose
  • blood pressure
  • ECG
  • heart rate
  • LFTs
  • pregnancy testing
  • serum amylase
  • serum lipase

Contraindications

  • alcoholism
  • bradycardia
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • contraception requirements
  • coronary artery disease
  • diabetes mellitus
  • electrolyte imbalance
  • females
  • geriatric
  • heart failure
  • hepatic disease
  • hepatotoxicity
  • hyperglycemia
  • hypertension
  • hypocalcemia
  • long QT syndrome
  • male-mediated teratogenicity
  • malnutrition
  • myocardial infarction
  • pancreatitis
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • QT prolongation
  • reproductive risk
  • thyroid disease
  • torsade de pointes
  • ventricular arrhythmias

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Abemaciclib
  • Acalabrutinib
  • Acebutolol
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Ado-Trastuzumab emtansine
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Almotriptan
  • Alosetron
  • Alprazolam
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Apalutamide
  • Apomorphine
  • Aprepitant, Fosaprepitant
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
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  • grapefruit juice
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