Erlotinib

Erlotinib Brand Name– Tarceva

What is Erlotinib

Erlotinib is an oral, selective epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) that is FDA-approved as monotherapy for the treatment of metastatic non-small cell lung cancer (NSCLC) in patients with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations and in combination with gemcitabine for the treatment of locally advanced, unresectable, or metastatic pancreatic cancer.

EGFR is expressed, overexpressed, or dysregulated in many cancers; clinically,

EGFR expression has been associated with poor prognosis, development of metastasis, and resistance to chemotherapy, hormonal therapy, and radiation therapy.

Indications

  1. head and neck cancer
  2. non-small cell lung cancer (NSCLC)
  3. pancreatic cancer

For the treatment of non-small cell lung cancer (NSCLC)

for the first-line treatment of metastatic NSCLC in patients whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations, in combination with ramucirumab

Side Effects

  1. acneiform rash
  2. anorexia
  3. anorexia
  4. arrhythmia exacerbation
  5. arthralgia
  6. arthralgia
  7. asthenia
  8. back pain
  9. back pain
  10. bullous rash
  11. chest pain (unspecified)
  12. chest pain (unspecified)
  13. colitis
  14. conjunctivitis
  15. conjunctivitis
  16. cough
  17. cough
  18. dehydration
  19. depression
  20. depression
  21. diarrhea
  22. diarrhea
  23. dyspnea
  24. dyspnea
  25. elevated hepatic enzymes
  26. elevated hepatic enzymes
  27. erythema
  28. exfoliative dermatitis
  29. fatigue
  30. fatigue
  31. fever
  32. fever
  33. folliculitis
  34. gastritis
  35. GI bleeding
  36. GI perforation
  37. headache
  38. headache
  39. hematemesis
  40. hemolytic anemia
  41. hepatic failure
  42. hepatotoxicity
  43. hyperbilirubinemia
  44. hyperbilirubinemia
  45. hypertrichosis
  46. ileus
  47. infection
  48. infection
  49. keratitis
  50. keratoconjunctivitis
  51. lacrimation
  52. maculopapular rash
  53. melena
  54. musculoskeletal pain
  55. musculoskeletal pain
  56. myocardial infarction
  57. myopathy
  58. nausea
  59. nausea
  60. ocular inflammation
  61. palmar-plantar erythrodysesthesia (hand and foot syndrome)
  62. peptic ulcer
  63. photosensitivity
  64. pneumonitis
  65. prolonged bleeding time
  66. pruritus
  67. pruritus
  68. rash
  69. rash
  70. renal failure (unspecified)
  71. rhabdomyolysis
  72. skin hyperpigmentation
  73. skin ulcer
  74. Stevens-Johnson syndrome
  75. stomatitis
  76. stomatitis
  77. stroke
  78. syncope
  79. thrombocytopenia
  80. thromboembolism
  81. thrombosis
  82. toxic epidermal necrolysis
  83. uveitis
  84. weight loss
  85. weight loss
  86. xerosis
  87. xerosis

Monitoring Parameters

  • LFTs
  • serum creatinine/BUN
  • serum electrolytes

Contraindications

  • biliary obstruction
  • breast-feeding
  • chronic lung disease (CLD)
  • contraception requirements
  • corticosteroid therapy
  • dehydration
  • diverticulitis
  • GI perforation
  • hepatic disease
  • hepatotoxicity
  • keratitis
  • ocular disease
  • peptic ulcer disease
  • pneumonitis
  • pregnancy
  • pulmonary disease
  • renal disease
  • renal failure
  • renal impairment
  • reproductive risk
  • tobacco smoking

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Aluminum Hydroxide
  • Aluminum Hydroxide; Magnesium Carbonate
  • Aluminum Hydroxide; Magnesium Hydroxide
  • Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
  • Aluminum Hydroxide; Magnesium Trisilicate
  • Amiodarone
  • Amlodipine; Celecoxib
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Antacids
  • Apalutamide
  • Armodafinil
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Omeprazole
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bexarotene
  • Bosentan
  • Budesonide
  • Budesonide; Formoterol
  • Butabarbital
  • Cabazitaxel
  • Calcium Carbonate
  • Calcium Carbonate; Magnesium Hydroxide
  • Calcium Carbonate; Risedronate
  • Calcium Carbonate; Simethicone
  • Carbamazepine
  • Celecoxib
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Cimetidine
  • Ciprofloxacin
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Cortisone
  • Dabrafenib
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deflazacort
  • Delavirdine
  • Dexamethasone
  • Dexlansoprazole
  • Diclofenac
  • Diclofenac; Misoprostol
  • Diflunisal
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Docetaxel
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enzalutamide
  • Eslicarbazepine
  • Esomeprazole
  • Esomeprazole; Naproxen
  • Etodolac
  • Etravirine
  • Famotidine
  • Famotidine; Ibuprofen
  • Fenoprofen
  • Fludrocortisone
  • Flurbiprofen
  • Fluvoxamine
  • Fosamprenavir
  • Fosphenytoin
  • grapefruit juice
  • Hydrocodone; Ibuprofen
  • Hydrocortisone
  • Ibuprofen
  • Ibuprofen; Oxycodone
  • Ibuprofen; Pseudoephedrine
  • Idelalisib
  • Indinavir
  • Indomethacin
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Ketoprofen
  • Ketorolac
  • Lansoprazole
  • Lansoprazole; Naproxen
  • Letermovir
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Lumateperone
  • Magnesium Hydroxide
  • Meclofenamate Sodium
  • Mefenamic Acid
  • Meloxicam
  • Mephobarbital
  • Methohexital
  • Methylprednisolone
  • Mifepristone
  • Mitotane
  • Modafinil
  • Nabumetone
  • Nafcillin
  • Nanoparticle Albumin-Bound Paclitaxel
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nefazodone
  • Nelfinavir
  • Nevirapine
  • Nilotinib
  • Nizatidine
  • Nonsteroidal antiinflammatory drugs
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole
  • Omeprazole; Amoxicillin; Rifabutin
  • Omeprazole; Sodium Bicarbonate
  • Osilodrostat
  • Oxaprozin
  • Oxcarbazepine
  • Paclitaxel
  • Pantoprazole
  • Pentobarbital
  • Pexidartinib
  • Phenobarbital
  • Phenytoin
  • Piroxicam
  • Posaconazole
  • Prednisolone
  • Prednisone
  • Primidone
  • Quinine
  • Rabeprazole
  • Ranitidine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rofecoxib
  • Saquinavir
  • Secobarbital
  • Simeprevir
  • Sodium Bicarbonate
  • St. John’s Wort, Hypericum perforatum
  • Sulindac
  • Taxanes
  • Telithromycin
  • Thiopental
  • Tipranavir
  • tobacco
  • Tolmetin
  • Trandolapril; Verapamil
  • Triamcinolone
  • Tucatinib
  • Valdecoxib
  • Verapamil
  • Voriconazole
  • Warfarin
  • Zafirlukast
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