Lorlatinib

Lorlatinib Brand Name– Lorbrena

What is Lorlatinib

Lorlatinib is an oral kinase inhibitor approved for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) in patients whose disease has progressed on certain ALK kinase inhibitors.

It is also active against ROS1 and a variety of other chromosomal rearrangements, including mutant forms of ALK detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors.

It carries a risk of serious hepatotoxicity when administered with CYP3A inducers, and is contraindicated for use with strong CYP3A inducers. Hyperlipidemia is common while on therapy; a wide variety of central nervous system (CNS) effects have also been reported.

Indications

  • non-small cell lung cancer (NSCLC)

For the treatment of metastatic, ALK-positive non-small cell lung cancer (NSCLC) with disease progression on either alectinib or ceritinib as the first ALK inhibitor for metastatic disease, or disease progression on crizotinib and at least one other ALK inhibitor for metastatic disease

NOTE: Lorlatinib has been designated an orphan drug by the FDA for this indication.

Side Effects

  1. abnormal dreams
  2. acneiform rash
  3. agitation
  4. amnesia
  5. anemia
  6. anemia
  7. anxiety
  8. aphasia
  9. arthralgia
  10. arthralgia
  11. asthenia
  12. AV block
  13. back pain
  14. back pain
  15. blurred vision
  16. carpal tunnel syndrome
  17. confusion
  18. constipation
  19. cough
  20. dementia
  21. depression
  22. diarrhea
  23. diarrhea
  24. diplopia
  25. dizziness
  26. dizziness
  27. dysarthria
  28. dysesthesia
  29. dyspnea
  30. dyspnea
  31. edema
  32. edema
  33. elevated hepatic enzymes
  34. elevated hepatic enzymes
  35. emotional lability
  36. euphoria
  37. fatigue
  38. fatigue
  39. fever
  40. fever
  41. formication
  42. hallucinations
  43. hallucinations
  44. headache
  45. headache
  46. hepatotoxicity
  47. hyperactivity
  48. hyperamylasemia
  49. hyperamylasemia
  50. hypercholesterolemia
  51. hypercholesterolemia
  52. hyperglycemia
  53. hyperglycemia
  54. hyperkalemia
  55. hyperkalemia
  56. hypertension
  57. hypertriglyceridemia
  58. hypertriglyceridemia
  59. hypoalbuminemia
  60. hypoalbuminemia
  61. hypoesthesia
  62. hypomagnesemia
  63. hypophosphatemia
  64. hypophosphatemia
  65. impaired cognition
  66. impaired cognition
  67. infection
  68. insomnia
  69. irritability
  70. lymphopenia
  71. lymphopenia
  72. maculopapular rash
  73. mania
  74. memory impairment
  75. musculoskeletal pain
  76. myalgia
  77. myocardial infarction
  78. nausea
  79. nausea
  80. neurotoxicity
  81. nightmares
  82. paresthesias
  83. peripheral edema
  84. peripheral neuropathy
  85. peripheral neuropathy
  86. photophobia
  87. photopsia
  88. pneumonitis
  89. pneumonitis
  90. PR prolongation
  91. pulmonary edema
  92. rash
  93. rash
  94. seizures
  95. somnambulism
  96. suicidal ideation
  97. thrombocytopenia
  98. thrombocytopenia
  99. thromboembolism
  100. visual impairment
  101. visual impairment
  102. vomiting
  103. vomiting
  104. weakness
  105. weight gain
  106. weight gain

Monitoring Parameters

  • ECG
  • pregnancy testing
  • serum cholesterol
  • serum triglycerides

Contraindications

  • breast-feeding
  • cardiac arrhythmias
  • contraception requirements
  • hepatotoxicity
  • hypercholesterolemia
  • hypertriglyceridemia
  • infertility
  • male-mediated teratogenicity
  • neurological disease
  • neurotoxicity
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • reproductive risk
  • seizures

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Abemaciclib
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Afatinib
  • Alfentanil
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Apalutamide
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Avanafil
  • Avapritinib
  • Axitinib
  • Bedaquiline
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Benzhydrocodone; Acetaminophen
  • Betrixaban
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  • Bosentan
  • Brigatinib
  • Bromocriptine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Bupivacaine; Lidocaine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Buspirone
  • Butabarbital
  • Capmatinib
  • Carbamazepine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Cariprazine
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Clarithromycin
  • Clozapine
  • Cobicistat
  • Cobimetinib
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
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  • Deflazacort
  • Delavirdine
  • Dexamethasone
  • Diazepam
  • Dienogest; Estradiol valerate
  • Diethylstilbestrol, DES
  • Digoxin
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diltiazem
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Dolutegravir
  • Dolutegravir; Lamivudine
  • Dolutegravir; Rilpivirine
  • Doravirine
  • Doravirine; Lamivudine; Tenofovir disoproxil fumarate
  • Doxorubicin
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  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Edoxaban
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  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Elvitegravir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Encorafenib
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  • Eslicarbazepine
  • Esterified Estrogens
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  • Estrogens
  • Estropipate
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
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  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Etonogestrel
  • Etravirine
  • Fedratinib
  • Fentanyl
  • Flibanserin
  • Flurazepam
  • Fosamprenavir
  • Fosphenytoin
  • Glasdegib
  • Glecaprevir; Pibrentasvir
  • grapefruit juice
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guanfacine
  • Homatropine; Hydrocodone
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydroxyprogesterone
  • Ibuprofen; Oxycodone
  • Idelalisib
  • Ifosfamide
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  • Isradipine
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  • Lefamulin
  • Lemborexant
  • Letermovir
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  • Levonorgestrel
  • Lidocaine
  • Lidocaine; Prilocaine
  • Lopinavir; Ritonavir
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  • Lumacaftor; Ivacaftor
  • Lumateperone
  • Lurasidone
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  • Mitotane
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  • Nanoparticle Albumin-Bound Paclitaxel
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  • Norgestrel
  • Olaparib
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oxycodone
  • Paclitaxel
  • Pemigatinib
  • Pentobarbital
  • Perampanel
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  • Phenobarbital
  • Phenytoin
  • Pimavanserin
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  • Primidone
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  • Ranolazine
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  • Solifenacin
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  • Ubrogepant
  • Ulipristal
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  • Voriconazole
  • Voxelotor
  • Warfarin
  • Zanubrutinib
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