Erlotinib interactions

Food & lifestyle

• grapefruit juice

  Moderate

  Metabolism

  Grapefruit and grapefruit juice may increase the plasma concentrations of erlotinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

  What to do: Consumption of grapefruit and grapefruit juice should be avoided or limited during treatment with erlotinib. Patients who currently smoke cigarettes are advised to stop smoking as soon as possible. If cigarette smoking is continued while taking erlotinib, the manufacturer recommends increasing the dosage of erlotinib by 50 mg increments at 2-week intervals up to a maximum of 300 mg as tolerated. However, the efficacy and long-term safety of dosages higher than 150 mg daily have not been established. Data from a double-blind, randomized phase 3 study (MO22162, CURRENTS) demonstrated no benefit in progression free survival or overall survival with an erlotinib dosage of 300 mg daily relative to the recommended dosage of 150 mg daily in active smokers (average of 38 pack years) with locally advanced or metastatic NSCLC who have failed chemotherapy, although patients in the study were not selected based on epidermal growth factor receptor (EGFR) mutation status. Safety data were comparable between the two dosages, but a numerical increase in the incidence of rash, interstitial lung disease and diarrhea was observed with the higher dosage. Patients who have received a dosage increase should immediately revert to the recommended dosage of 150 mg or 100 mg once daily (depending on indication) upon cessation of smoking. Erlotinib should be administered on an empty stomach at least one hour before or two hours after the ingestion of food.

  4 sources

  1. "Product Information. Tarceva (erlotinib)." Genentech (2018):
  2. "Product Information. Tarceva (erlotinib)." Hoffmann-La Roche Limited (2018):
  3. "Product Information. Tarceva (erlotinib)." Roche Products Ltd (2022):
  4. "Product Information. Tarceva (erlotinib)." Roche Products Pty Ltd (2022):

Conditions

Conditions in which Erlotinib needs care, as documented in this source.

• Eye Diseases

  Major

  Some epidermal growth factor receptor (EGFR) inhibitors should be administered cautiously in patients with ocular disorders such as primary keratitis, ulcerative keratitis, or conjunctivitis. It is recommended to interrupt or discontinue treatment with these agents if patients present with acute or worsening ocular disorders.

  6 sources

  1. "Product Information. Iressa (gefitinib)." Astra-Zeneca Pharmaceuticals (2003):
  2. "Product Information. Erbitux (cetuximab)." Bristol-Myers Squibb (2004):
  3. "Product Information. Tarceva (erlotinib)." Genentech (2004):
  4. "Product Information. Vectibix (panitumumab)." Amgen USA (2006):
  5. "Product Information. Tykerb (lapatinib)." Novartis Pharmaceuticals (2007):
  6. "Product Information. Tagrisso (osimertinib)." Astra-Zeneca Pharmaceuticals (2015):

• Gastrointestinal Diseases

  Major

  The use of some EGFR inhibitors may be associated with gastrointestinal perforation and fatal cases have been reported. Patients receiving concomitant anti-angiogenic agents, corticosteroids, NSAIDs, or taxane-based chemotherapy, or who have prior history of peptic ulceration or diverticular disease may be at increased risk of perforation. Permanently discontinue these agents in patients who develop gastrointestinal perforation.

  2 sources

  1. "Product Information. Iressa (gefitinib)." Astra-Zeneca Pharmaceuticals (2003):
  2. "Product Information. Tarceva (erlotinib)." Genentech (2004):

• Heart Failure

  Major

  The use of erlotinib has been associated with hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome, in some cases with fatal outcomes. Patients with hepatic impairment (total bilirubin > upper limit of normal (ULN) or Child-Pugh A, B and C) should be closely monitored during therapy with erlotinib. Treatment with erlotinib should be used with extra caution in patients with total bilirubin > 3 x ULN. Clinical monitoring of hepatic function (transaminases, bilirubin, and alkaline phosphatase) is recommended during treatment and increase frequency of monitoring is required for patients with preexisting-existing hepatic impairment or biliary obstruction. In patients with preexisting-existing hepatic impairment or biliary obstruction with doubling of bilirubin or tripling of transaminases values over baseline, erlotinib therapy should be withhold and therapy should be discontinued in patients whose abnormal liver tests meeting the above criteria do not improve significantly or resolve within three weeks. Withhold erlotinib in patients developing severe renal impairment until renal toxicity is resolved. Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold erlotinib for severe renal toxicity.

  1 source

  1. "Product Information. Tarceva (erlotinib)." Genentech (2004):

• Lung Diseases

  Major

  The use of certain EGFR inhibitors has been associated with pulmonary toxicity. Serious cases of interstitial lung disease (ILD), including fatal cases and interstitial pneumonitis or pulmonary fibrosis have been reported. Caution is recommended when using these agents in patients with a history of interstitial pneumonitis or pulmonary fibrosis or those patients presenting with acute onset of new or progressive unexplained pulmonary symptoms such as dyspnea, cough, and fever pending diagnostic evaluation. If ILD is confirmed, permanently discontinue these agents and institute appropriate measures.

  6 sources

  1. "Product Information. Iressa (gefitinib)." Astra-Zeneca Pharmaceuticals (2003):
  2. "Product Information. Erbitux (cetuximab)." Bristol-Myers Squibb (2004):
  3. "Product Information. Tarceva (erlotinib)." Genentech (2004):
  4. "Product Information. Vectibix (panitumumab)." Amgen USA (2006):
  5. "Product Information. Tykerb (lapatinib)." Novartis Pharmaceuticals (2007):
  6. "Product Information. Tagrisso (osimertinib)." Astra-Zeneca Pharmaceuticals (2015):

• Stevens-Johnson Syndrome

  Major

  Cutaneous reactions, in some cases severe, have been reported with the use of EGFR inhibitors. Monitor patients who develop dermatologic or soft tissue toxicities while receiving these agents for the development of inflammatory or infectious sequelae. It is recommended to withhold treatment, and appropriate measures should be instituted as appropriate or discontinue the use of these agents for dermatologic or soft tissue toxicity associated with severe or life-threatening inflammatory or infectious complications. Advise patients to wear sunscreen and hats and limit sun exposure while receiving therapy with these agents as exposure to sunlight can exacerbate dermatologic toxicities.

  7 sources

  1. "Product Information. Iressa (gefitinib)." Astra-Zeneca Pharmaceuticals (2003):
  2. "Product Information. Erbitux (cetuximab)." Bristol-Myers Squibb (2004):
  3. "Product Information. Tarceva (erlotinib)." Genentech (2004):
  4. "Product Information. Vectibix (panitumumab)." Amgen USA (2006):
  5. "Product Information. Tykerb (lapatinib)." Novartis Pharmaceuticals (2007):
  6. "Product Information. Tagrisso (osimertinib)." Astra-Zeneca Pharmaceuticals (2015):
  7. "Product Information. Portrazza (necitumumab)." Eli Lilly and Company (2015):