Ceritinib

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
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• Anagrelide
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