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Non-small cell lung cancer: First-line treatment of metastatic non-small cell lung cancer (NSCLC) in tumors with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an approved test; treatment of locally advanced or metastatic NSCLC after failure of at least 1 prior chemotherapy regimen; maintenance treatment of locally advanced or metastatic NSCLC which has not progressed after 4 cycles of first-line platinum-based chemotherapy
Limitations of use: Use in combination with platinum-based chemotherapy is not recommended. First-line treatment in patients with metastatic NSCLC with EGFR mutations other than exon 19 deletion or exon 21 (L858R) substitution has not been evaluated.
Pancreatic cancer (not an approved use in Canada): First-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer (in combination with gemcitabine)
There are no contraindications listed in the manufacturer 's US labeling.
Canadian labeling: Hypersensitivity to erlotinib or any component of the formulation
Non-small cell lung cancer (NSCLC), metastatic, first-line therapy in patients with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations: Oral: 150 mg once daily until disease progression or unacceptable toxicity (Rosell 2012; Zhou 2011).
NSCLC, refractory: Oral: 150 mg once daily until disease progression or unacceptable toxicity (Shepherd 2005)
NSCLC, maintenance therapy: Oral: 150 mg once daily until disease progression or unacceptable toxicity (Capuzzo 2010)
Pancreatic cancer: Oral: 100 mg once daily until disease progression or unacceptable toxicity (in combination with gemcitabine) (Moore 2007)
Dosage adjustment for concomitant CYP3A4 inhibitors/inducers:
CYP3A4 inhibitors: Avoid concurrent use if possible; consider dose reductions for severe adverse reactions if erlotinib is administered concomitantly with strong CYP3A4 inhibitors (eg, azole antifungals, clarithromycin, erythromycin, nefazodone, protease inhibitors, telithromycin, grapefruit, or grapefruit juice). Dose reduction (if required) should be done in decrements of 50 mg (after toxicity has resolved to baseline or ≤ grade 1).
Concomitant CYP3A4 and CYP1A2 inhibitor (eg, ciprofloxacin): Avoid concurrent use if possible; consider dose reductions in decrements of 50 mg if severe adverse reactions occur (after toxicity has resolved to baseline or ≤ grade 1).
CYP3A4 inducers: Avoid concurrent use if possible; concomitant administration with CYP3A4 inducers (eg, carbamazepine, phenobarbital, phenytoin, rifamycins, and St John 's wort) may require increased erlotinib doses (increase as tolerated at 2-week intervals in 50 mg increments to a maximum of 450 mg); reduce erlotinib dose to recommended starting dose when CYP3A4 inducer is discontinued.
Dosage adjustment for concomitant smoking: Increase dose at 2-week intervals in 50 mg increments to a maximum dose of 300 mg (with careful monitoring) in patients who continue to smoke; immediately reduce erlotinib dose to recommended starting dose (based on indication) upon smoking cessation.
Refer to adult dosing.
Renal impairment at treatment initiation: There are no dosage adjustments provided in the manufacturer 's labeling (has not been studied), although <9% of a single dose is excreted in the urine.
Renal toxicity during treatment: Withhold treatment for grades 3/4 renal toxicity (consider discontinuing) and for risk of renal failure due to dehydration; may resume after euvolemia re-established (at previous dose). If treatment withheld due to toxicity and therapy is resumed, reinitiate with a 50 mg dose reduction after toxicity has resolved to baseline or ≤ grade 1.
Hepatic impairment at treatment initiation:
US labeling:
Total bilirubin > ULN or Child-Pugh classes A, B, and C: There are no dosage adjustments provided in the manufacturer 's labeling; use with caution and monitor closely during treatment.
Total bilirubin >3 times ULN: Use extreme caution.
Canadian labeling:
Moderate impairment: There are no dosage adjustments provided in the manufacturer 's labeling; however, a reduced dose should be considered.
Severe impairment (including total bilirubin >3 times ULN and/or transaminases >5 times ULN): Use is not recommended.
The following adjustments have also been studied: A reduced starting dose (75 mg once daily) has been recommended in patients with hepatic dysfunction (AST ≥3 times ULN or direct bilirubin 1 to 7 mg/dL), with individualized dosage escalation if tolerated (Miller 2007); another study determined that pharmacokinetic and safety profiles were similar between patients with normal hepatic function and moderate hepatic impairment (O 'Bryant 2012).
Hepatotoxicity during treatment: US labeling:
Patients with normal hepatic function at baseline: If total bilirubin >3 times ULN and/or transaminases >5 times ULN: Interrupt therapy (consider discontinuing); if treatment is resumed, reinitiate with a 50 mg dose reduction after bilirubin and transaminases return to baseline; discontinue treatment if there is no significant improvement or resolution within 3 weeks.
Patients with baseline hepatic impairment or biliary obstruction: If bilirubin doubles or transaminases triple over baseline: Interrupt therapy (consider discontinuing); if treatment is resumed, reinitiate with a 50 mg dose reduction after bilirubin and transaminases return to baseline; discontinue treatment if there is no significant improvement or resolution of hepatotoxicity within 3 weeks.
The manufacturer recommends administration on an empty stomach (at least 1 hour before or 2 hours after the ingestion of food). Avoid concomitant use with proton pump inhibitors (if possible). If taken with an H2-receptor antagonist (eg, ranitidine), administer erlotinib 10 hours after the H2-receptor antagonist dose and at least 2 hours prior to the next H2- receptor dose. If an antacid is necessary, separate dosing by several hours.
For patients unable to swallow whole, tablets may be dissolved in 100 mL water and administered orally or via feeding tube (silicone-based); to ensure full dose is received, rinse container with 40 mL water, administer residue and repeat rinse; administer immediately after preparation (data on file, Genentech [contact product manufacturer to obtain current information]; Siu 2007; Soulieres 2004).
Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]). NIOSH recommends single gloving for administration of an intact tablet. If manipulating tablets (eg, to prepare an oral suspension), NIOSH recommends double gloving, a protective gown, and preparation in a controlled device; if not prepared in a controlled device, respiratory and eye protection as well as ventilated engineering controls are recommended (NIOSH 2014).
Avoid grapefruit juice.
Store at 25 ‚ °C (77 ‚ °F); excursions are permitted between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Tarceva: 25 mg [contains fd&c yellow #6 (sunset yellow)]
Tarceva: 100 mg, 150 mg
Antacids: May decrease the serum concentration of Erlotinib. Management: Separate the administration of erlotinib and any antacid by several hours in order to minimize the risk of a significant interaction. Consider therapy modification
Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Ciprofloxacin (Systemic): May increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50mg decrements). Consider therapy modification
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Erlotinib. Management: Avoid combination if possible. If combination must be used, increase erlotinib dose by 50 mg increments every 2 weeks as tolerated, to a maximum of 450 mg/day. Consider therapy modification
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements). Consider therapy modification
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification
FluvoxaMINE: May increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements). Consider therapy modification
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination
Grapefruit Juice: May increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements). Consider therapy modification
H2-Antagonists: May decrease the serum concentration of Erlotinib. Management: Avoid H2-antagonists in patients receiving erlotinib when possible. If concomitant treatment cannot be avoided, erlotinib should be dosed once daily, 10 hours after and at least 2 hours before H2-antagonist dosing. Consider therapy modification
Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
Irinotecan Products: UGT1A1 Inhibitors may increase serum concentrations of the active metabolite(s) of Irinotecan Products. Specifically, concentrations of SN-38 may be increased. UGT1A1 Inhibitors may increase the serum concentration of Irinotecan Products. Avoid combination
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification
Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification
Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Proton Pump Inhibitors: May decrease the serum concentration of Erlotinib. Avoid combination
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
St Johns Wort: May decrease the serum concentration of Erlotinib. Management: Avoid combination if possible. If combination must be used, increase erlotinib dose by 50 mg increments every 2 weeks as tolerated, to a maximum of 450 mg/day. Consider therapy modification
Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Warfarin: Erlotinib may increase the serum concentration of Warfarin. Monitor therapy
Liver function tests (transaminases, bilirubin, and alkaline phosphatase [periodic], monitor more frequently with worsening liver function); renal function tests (periodic) and serum electrolytes (in patients at risk for dehydration; periodic); prothrombin time and INR (in patients on concomitant warfarin therapy); EGFR mutation status in patients with NSCLC adenocarcinoma (Keedy 2011); the cobas EGFR mutation test has been approved to detect EGFR mutation for first-line NSCLC treatment.
Consider a baseline ophthalmologic exam and reassess for ocular toxicities at 4 to 8 weeks after treatment initiation (Renouf 2012). Monitor hydration status; monitor for signs/symptoms of pulmonary toxicity, dermatologic toxicity, and ocular toxicity.
Adverse reactions reported with monotherapy:
>10%:
Cardiovascular: Chest pain ( ≤18%)
Central nervous system: Fatigue (9% to 52%)
Dermatologic: Skin rash (49% to 85%; grade 3: 5% to 13%; grade 4: <1%; median onset: 8 days), xeroderma (4% to 21%), pruritus (7% to 16%), paronychia (4% to 16%), alopecia (14% to 15%), acne vulgaris (6% to 12%)
Gastrointestinal: Diarrhea (20% to 62%; grade 3: 2% to 6%; grade 4: <1%; median onset: 12 days), anorexia (9% to 52%), nausea (23% to 33%), decreased appetite ( ≤28%), vomiting (13% to 23%), mucositis ( ≤18%), stomatitis (11% to 17%), abdominal pain (3% to 11%), constipation ( ≤8%)
Genitourinary: Urinary tract infection ( ≤4%)
Hematologic & oncologic: Anemia ( ≤11%; grade 4: 1%)
Infection: Increased susceptibility to infection (4% to 24%)
Miscellaneous: Fever ( ≤11%)
Neuromuscular & skeletal: Weakness ( ≤53%), back pain (19%), arthralgia ( ≤13%), musculoskeletal pain (11%)
Ophthalmic: Conjunctivitis (12% to 18%), keratoconjunctivitis sicca (12%)
Respiratory: Cough (33% to 48%), dyspnea (41% to 45%; grades 3/4: 8% to 28%)
1% to 10%:
Cardiovascular: Peripheral edema ( ≤5%)
Central nervous system: Pain ( ≤9%), headache ( ≤7%), anxiety ( ≤5%), dizziness ( ≤4%), insomnia ( ≤4%), neurotoxicity ( ≤4%), paresthesia ( ≤4%), voice disorder ( ≤4%)
Dermatologic: Folliculitis ( ≤8%), nail disease ( ≤7%), exfoliative dermatitis (5%), hypertrichosis (5%), skin fissure (5%), acneiform eruption (4% to 5%), erythema ( ≤5%), dermatitis (4%), erythematous rash ( ≤4%), palmar-plantar erythrodysesthesia ( ≤4%), bullous dermatitis
Endocrine & metabolic: Weight loss (4% to 5%)
Gastrointestinal: Dyspepsia ( ≤5%), xerostomia ( ≤3%), taste disorder ( ≤1%)
Hematologic & oncologic: Lymphocytopenia ( ≤4%; grade 3: 1%), leukopenia ( ≤3%), thrombocytopenia ( ≤1%)
Hepatic: Hyperbilirubinemia (7%; grade 3: ≤1%), increased serum ALT (grade 2: 2% to 4%; grade 3: 1% to 3%), increased gamma-glutamyl transferase ( ≤4%), hepatic failure ( ≤1%)
Neuromuscular & skeletal: Muscle spasm ( ≤4%), musculoskeletal chest pain ( ≤4%), ostealgia ( ≤4%)
Otic: Tinnitus ( ≤1%)
Renal: Increased serum creatinine ( ≤1%), renal failure ( ≤1%),
Respiratory: Nasopharyngitis ( ≤7%), epistaxis ( ≤4%), pulmonary embolism ( ≤4%), respiratory tract infection ( ≤4%), pneumonitis (3%), pulmonary fibrosis (3%)
<1%: Interstitial pulmonary disease
Adverse reactions reported with combination (erlotinib plus gemcitabine) therapy:
>10%:
Cardiovascular: Edema (37%), thrombosis (grades 3/4: 11%)
Central nervous system: Fatigue (73% to 79%), depression (19%), dizziness (15%), headache (15%), anxiety (13%)
Dermatologic: Skin rash (70%), alopecia (14%)
Gastrointestinal: Nausea (60%), anorexia (52%), diarrhea (48%), abdominal pain (46%), vomiting (42%), weight loss (39%), stomatitis (22%), dyspepsia (17%), flatulence (13%)
Hepatic: Increased serum ALT (grade 2: 31%, grade 3: 13%, grade 4: <1%), increased serum AST (grade 2: 24%, grade 3: 10%, grade 4 <1%), hyperbilirubinemia (grade 2: 17%, grade 3: 10%, grade 4: <1%)
Infection: Increased susceptibility to infection (39%)
Miscellaneous: Fever (36%)
Neuromuscular & skeletal: Ostealgia (25%), myalgia (21%), neuropathy (13%), rigors (12%)
Respiratory: Dyspnea (24%), cough (16%)
1% to 10%:
Cardiovascular: Cardiac arrhythmia (<5%), syncope (<5%), deep vein thrombosis (4%), cerebrovascular accident (3%; including cerebral hemorrhage), myocardial infarction (2%)
Gastrointestinal: Intestinal obstruction (<5%), pancreatitis (<5%)
Hematologic & oncologic: Hemolytic anemia (<5%), microangiopathic hemolytic anemia with thrombocytopenia (1%)
Renal: Renal insufficiency (<5%), renal failure (1%)
Respiratory: Interstitial pulmonary disease (<3%)
<1%: Bullous dermatitis, exfoliative dermatitis, hepatic failure
Mono- or combination therapy: <1% (Limited to important or life-threatening): Acute peptic ulcer with hemorrhage, bronchiolitis, corneal perforation, corneal ulcer, episcleritis, gastritis, gastrointestinal hemorrhage, gastrointestinal perforation, hearing loss, hematemesis, hematochezia, hepatorenal syndrome, hepatotoxicity, hirsutism, hyperpigmentation, hypokalemia, keratitis, melena, myopathy (in combination with statin therapy), peptic ulcer, rhabdomyolysis (in combination with statin therapy), skin photosensitivity, skin rash (acneiform; sparing prior radiation field), Stevens-Johnson syndrome, toxic epidermal necrolysis, tympanic membrane perforation
Cigarette smoking: Smoking reduces erlotinib exposure; smokers had a 24% higher rate of erlotinib clearance.
Concerns related to adverse effects:
- Cardiovascular events: Cerebrovascular accidents, MI, and myocardial ischemia have been reported.
- Dermatologic toxicity: Bullous, blistering, and/or exfoliating skin conditions, some suggestive of Stevens-Johnson or toxic epidermal necrolysis (TEN), have been reported (some fatal). An acne-like rash commonly appears on the face, back, and upper chest. Generalized or severe acneiform, erythematous or maculopapular rash may occur. Skin rash may correlate with treatment response and prolonged survival (Saif 2008); management of skin rashes that are not serious should include alcohol-free lotions, topical antibiotics, or topical corticosteroids, or if necessary, oral antibiotics and systemic corticosteroids; avoid sunlight. Reduce dose or temporarily interrupt treatment for severe skin reactions; discontinue treatment for bullous, blistering, or exfoliative skin toxicity.
- Gastrointestinal (GI) perforation: GI perforation (including fatalities) has been reported; risk for perforation is increased with concurrent anti-angiogenic agents, corticosteroids, NSAIDs, and/or taxane based-chemotherapy, and patients with history of peptic ulcers or diverticular disease. Permanently discontinue in patients who develop perforation.
- Hematologic effects: Microangiopathic hemolytic anemia (MAHA) with thrombocytopenia has been reported (rarely) with erlotinib in combination with gemcitabine.
- Hemorrhage: Elevated INR and bleeding events (including fatal hemorrhage) have been reported when erlotinib was administered concomitantly with warfarin; monitor prothrombin time and INR closely.
- Hepatotoxicity: Hepatic failure and hepatorenal syndrome have been reported (some fatal), particularly in patients with baseline hepatic impairment (although have also been observed in patients with normal hepatic function). Monitor liver function (transaminases, bilirubin, and alkaline phosphatase); patients with any hepatic impairment (total bilirubin >ULN; Child-Pugh class A, B, or C) should be closely and more frequently monitored, including those with hepatic disease due to tumor burden. Increased monitoring of liver function is required in patients with preexisting hepatic impairment or biliary obstruction. Dosage reduction, interruption, or discontinuation may be necessary for changes in hepatic function. Use with extreme caution in patients with total bilirubin >3 times ULN. Interrupt therapy if total bilirubin is >3 times ULN or transaminases are >5 times ULN in patients without preexisting hepatic impairment. In patients with baseline hepatic dysfunction or biliary obstruction, interrupt therapy if bilirubin doubles or transaminases triple from baseline values.
- Ocular toxicity: Corneal perforation and ulceration have been reported; decreased tear production, abnormal eyelash growth, keratoconjunctivitis sicca, or keratitis have also been reported and are known risk factors for corneal ulceration/perforation. Interrupt or discontinue treatment in patients presenting with eye pain or other acute or worsening ocular symptoms. Consider a baseline ophthalmologic exam and reassess for ocular toxicities at 4 to 8 weeks after treatment initiation (Renouf 2012).
- Pulmonary toxicity: Rare, sometimes fatal, interstitial lung disease (ILD) has occurred; symptoms include acute respiratory distress syndrome, interstitial pneumonia, obliterative bronchiolitis, pneumonitis (including radiation and hypersensitivity), pulmonary fibrosis, and pulmonary infiltrates. The onset of symptoms has been within 5 days to more than 9 months after treatment initiation (median: 39 days). Interrupt treatment for unexplained new or worsening pulmonary symptoms (dyspnea, cough, and fever); permanently discontinue for confirmed ILD.
- Renal impairment: Acute renal failure (some fatal), renal insufficiency, and hepatorenal syndrome have been reported, either secondary to hepatic impairment at baseline or due to severe dehydration; use with caution in patients with or at risk for renal impairment. Monitor closely for dehydration; monitor renal function and electrolytes in patients at risk for dehydration. If severe renal impairment develops, interrupt therapy until toxicity resolves.
Disease-related concerns:
- NSCLC: Some factors which correlate positively with response to EGFR-tyrosine kinase inhibitor (TKI) therapy in NSCLC include patients who have never smoked, EGFR mutation, and patients of Asian origin. EGFR mutations, specifically exon 19 deletions and exon 21 mutation (L858R), are associated with better response to erlotinib in patients with NSCLC (Riely 2006). Erlotinib treatment is not recommended in patients with NSCLC with K-ras mutations; they are not likely to benefit from erlotinib treatment (Eberhard 2005; Miller 2008). K-ras mutations correlated with poorer outcome with EGFR-TKI therapy in patients with NSCLC (Cooley 2008; Jackman 2008; Masarelli 2007; Shepherd 2005). The cobas EGFR mutation test has been approved to detect EGFR mutation for first-line NSCLC treatment.
Concurrent drug therapy issues:
- Drugs affecting gastric pH: Avoid concomitant use with proton pump inhibitors. If taken with an H2-receptor antagonist (eg, ranitidine), administer erlotinib 10 hours after the H2-receptor antagonist dose and at least 2 hours prior to the next H2-receptor dose. If an antacid is necessary, separate dosing by several hours.
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- Smokers: Erlotinib levels may be lower in patients who smoke; advise patients to stop smoking. Smokers treated with 300 mg/day exhibited steady-state erlotinib levels comparable to former- and never-smokers receiving 150 mg/day (Hughes 2009).
Special handling:
- Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).
Other warnings/precautions:
- Appropriate use: Concurrent erlotinib plus platinum-based chemotherapy is not recommended for treatment of locally-advanced or metastatic NSCLC due to a lack of clinical benefit. First-line treatment in patients with metastatic NSCLC with EGFR mutations other than exon 19 deletion or exon 21 (L858R) substitution has not been evaluated. Select patients for first-line treatment of metastatic NSCLC based on EGFR exon 19 deletions and exon 21 mutation (L858R) in tumor or plasma specimens; if these mutations are not detected in plasma specimen, tumor tissue (if available) may be tested.
- Lactose intolerance: Product may contain lactose; avoid use in patients with Lapp lactase deficiency, glucose-galactose malabsorption, or glucose intolerance.
D
Adverse events were observed in animal reproduction studies. Based on the mechanism of action, may cause fetal harm if administered in pregnancy. Females of reproductive potential should be advised to avoid pregnancy; highly effective contraception is recommended during treatment and for at least 2 weeks after the last erlotinib dose.
Reversibly inhibits overall epidermal growth factor receptor (HER1/EGFR) - tyrosine kinase activity. Intracellular phosphorylation is inhibited which prevents further downstream signaling, resulting in cell death. Erlotinib has higher binding affinity for EGFR exon 19 deletion or exon 21 L858R mutations than for the wild type receptor.
Oral: ~60% on an empty stomach; almost 100% on a full stomach
232 L
Hepatic, via CYP3A4 (major), CYP1A1 (minor), CYP1A2 (minor), and CYP1C (minor)
Primarily as metabolites: Feces (83%; 1% as unchanged drug); urine (8%; <1% as unchanged drug)
Plasma: 4 hours
36 hours
~93% to albumin and alpha1-acid glycoprotein
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience itching, acne, lack of appetite, mouth sores, headache, back pain, joint pain, muscle pain, hair or nail changes, or dry skin. Have patient report immediately to prescriber signs of infection, signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), signs of a severe pulmonary disorder (lung or breathing problems like difficulty breathing, shortness of breath, or a cough that is new or worse), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), angina, severe nausea, severe vomiting, severe diarrhea, signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; hematuria; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe or persistent bleeding), severe loss of strength and energy, vision changes, eye irritation, depression, severe abdominal pain, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes) (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.