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Brand Name
Erlotinib
View Brand InformationFDA approval date: January 05, 2018
Classification: Kinase Inhibitor
Form: Tablet
What is Erlotinib?
Erlotinib tablet is a kinase inhibitor indicated for: The treatment of patients with metastatic non-small cell lung cancer whose tumors have epidermal growth factor receptor exon 19 deletions or exon 21 substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen.
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Brand Information
Erlotinib (Erlotinib)
1DOSAGE FORMS AND STRENGTHS
25 mg tablets
100 mg tablets
150 mg tablets
2CONTRAINDICATIONS
None.
3ADVERSE REACTIONS
The following serious adverse reactions, which may include fatalities, are discussed in greater detail in other sections of the labeling:
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
3.1Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Safety evaluation of erlotinib is based on more than 1200 cancer patients who received erlotinib as monotherapy, more than 300 patients who received erlotinib 100 or 150 mg plus gemcitabine, and 1228 patients who received erlotinib concurrently with other chemotherapies. The most common adverse reactions with erlotinib are rash and diarrhea usually with onset during the first month of treatment. The incidences of rash and diarrhea from clinical studies of erlotinib for the treatment of NSCLC and pancreatic cancer were 70% for rash and 42% for diarrhea.
Non-Small Cell Lung Cancer
First-Line Treatment of Patients with EGFR Mutations
The most frequent (≥ 30%) adverse reactions in erlotinib-treated patients were diarrhea, asthenia, rash, cough, dyspnea, and decreased appetite. In erlotinib-treated patients the median time to onset of rash was 15 days and the median time to onset of diarrhea was 32 days.
The most frequent Grade 3 to 4 adverse reactions in erlotinib-treated patients were rash and diarrhea.
Dose interruptions or reductions due to adverse reactions occurred in 37% of erlotinib-treated patients, and 14.3% of erlotinib-treated patients discontinued therapy due to adverse reactions. In erlotinib-treated patients, the most frequently reported adverse reactions leading to dose modification were rash (13%), diarrhea (10%), and asthenia (3.6%).
Common adverse reactions in Study 1, occurring in at least 10% of patients who received erlotinib or chemotherapy and an increase in ≥ 5% in the erlotinib-treated group, are graded by National Cancer Institute Common Toxicity Criteria for Adverse Events version 3.0 (NCI-CTCAE v3.0) Grade in Table 1. The median duration of erlotinib treatment was 9.6 months in Study 1.
Table 1: Adverse Reactions with an Incidence Rate ≥ 10% and an Increase of ≥ 5% in the Erlotinib-Treated Group (Study 1)
- Platinum-based chemotherapy (cisplatin or carboplatin with gemcitabine or docetaxel).
- Rash as a composite term includes rash, acne, folliculitis, erythema, acneiform dermatitis, dermatitis, palmar-plantar erythrodysesthesia syndrome, exfoliative rash, erythematous rash, rash pruritic, skin toxicity, eczema, follicular rash, skin ulcer.
Hepatic Toxicity: One erlotinib-treated patient experienced fatal hepatic failure and four additional patients experienced grade 3 to 4 liver test abnormalities in Study 1
Maintenance Treatment
Adverse reactions, regardless of causality, that occurred in at least 3% of patients treated with single-agent erlotinib at 150 mg and at least 3% more often than in the placebo group in the randomized maintenance trial (Study 3) are summarized by NCI-CTCAE v3.0 Grade in Table 2.
The most common adverse reactions in patients receiving single-agent erlotinib 150 mg were rash and diarrhea. Grade 3 to 4 rash and diarrhea occurred in 9% and 2%, respectively, in erlotinib-treated patients. Rash and diarrhea resulted in study discontinuation in 1% and 0.5% of erlotinib-treated patients, respectively. Dose reduction or interruption for rash and diarrhea was needed in 5% and 3% of patients, respectively. In erlotinib-treated patients the median time to onset of rash was 10 days, and the median time to onset of diarrhea was 15 days.
Table 2: NSCLC Maintenance Study: Adverse Reactions Occurring with an Incidence Rate ≥ 10% and an Increase of ≥ 5% in the Single-Agent Erlotinib Group compared to the Placebo Group (Study 3)
- Rash as a composite term includes: rash, acne, acneiform dermatitis, skin fissures, erythema, papular rash, rash generalized, pruritic rash, skin exfoliation, urticaria, dermatitis, eczema, exfoliative rash, exfoliative dermatitis, furuncle, macular rash, pustular rash, skin hyperpigmentation, skin reaction, skin ulcer.
Liver test abnormalities including ALT elevations were observed at Grade 2 or greater severity in 3% of erlotinib-treated patients and 1% of placebo-treated patients. Grade 2 and above bilirubin elevations were observed in 5% of erlotinib-treated patients and in < 1% in the placebo group
Second/Third Line Treatment
Adverse reactions, regardless of causality, that occurred in at least 10% of patients treated with single-agent erlotinib at 150 mg and at least 5% more often than in the placebo group in the randomized trial of patients with NSCLC are summarized by NCI-CTC v2.0 Grade in Table 3.
The most common adverse reactions in this patient population were rash and diarrhea. Grade 3 to 4 rash and diarrhea occurred in 9% and 6%, respectively, in erlotinib-treated patients. Rash and diarrhea each resulted in study discontinuation in 1% of erlotinib-treated patients. Six percent and 1% of patients needed dose reduction for rash and diarrhea, respectively. The median time to onset of rash was 8 days, and the median time to onset of diarrhea was 12 days.
Table 3: NSCLC 2Erlotinib Group Compared to the Placebo Group (Study 4)
- Rash as a composite term includes: rash, palmar-plantar erythrodysesthesia syndrome, acne, skin disorder, pigmentation disorder, erythema, skin ulcer, exfoliative dermatitis, papular rash, skin desquamation.
Liver function test abnormalities [including elevated alanine aminotransferase (ALT), aspartate aminotransferase (AST) and bilirubin] were observed in patients receiving single-agent erlotinib 150 mg. These elevations were mainly transient or associated with liver metastases. Grade 2 [> 2.5 to 5.0 x upper limit of normal (ULN)] ALT elevations occurred in 4% and < 1% of erlotinib and placebo treated patients, respectively. Grade 3 (> 5.0 to 20.0 x ULN) elevations were not observed in erlotinib-treated patients. Erlotinib dosing should be interrupted or discontinued if changes in liver function are severe
Pancreatic Cancer – Erlotinib Administered Concurrently with Gemcitabine
This was a randomized, double-blind, placebo-controlled study of erlotinib (150 mg or 100 mg daily) or placebo plus gemcitabine (1000 mg/m
Adverse reactions that occurred in at least 10% of patients treated with erlotinib 100 mg plus gemcitabine in the randomized trial of patients with pancreatic cancer (Study 5) were graded according to NCI-CTC v2.0 in Table 4.
The most common adverse reactions in pancreatic cancer patients receiving erlotinib 100 mg plus gemcitabine were fatigue, rash, nausea, anorexia and diarrhea. In the erlotinib plus gemcitabine arm, Grade 3 to 4 rash and diarrhea were each reported in 5% of patients. The median time to onset of rash and diarrhea was 10 days and 15 days, respectively. Rash and diarrhea each resulted in dose reductions in 2% of patients, and resulted in study discontinuation in up to 1% of patients receiving erlotinib plus gemcitabine. Severe adverse reactions (≥ Grade 3 NCI-CTC) in the erlotinib plus gemcitabine group with incidences < 5% included syncope, arrhythmias, ileus, pancreatitis, hemolytic anemia including microangiopathic hemolytic anemia with thrombocytopenia, myocardial infarction/ischemia, cerebrovascular accidents including cerebral hemorrhage, and renal insufficiency
The 150 mg cohort was associated with a higher rate of certain class-specific adverse reactions including rash and required more frequent dose reduction or interruption.
Table 4: Adverse Reactions Occurring with an Incidence Rate ≥ 10% and an Increase of ≥ 5% in Erlotinib-Treated Pancreatic Cancer Patients: 100 mg Cohort (Study 5)
- Rash as a composite term includes: rash, palmar-plantar erythrodysesthesia syndrome, pigmentation disorder, acneiform dermatitis, folliculitis, photosensitivity reaction, Stevens-Johnson syndrome, urticaria, erythematous rash, skin disorder, skin ulcer.
- Infections as a composite term include infections with unspecified pathogens as well as bacterial (including chlamydial, rickettsial, mycobacterial and mycoplasmal), parasitic (including helminthic, ectoparasitic and protozoal), viral and fungal infectious disorders.
Ten patients (4%) in the erlotinib/gemcitabine group and three patients (1%) in the placebo/gemcitabine group developed deep venous thrombosis. The overall incidence of grade 3 or 4 thrombotic events, including deep venous thrombosis was 11% for erlotinib plus gemcitabine and 9% for placebo plus gemcitabine.
The incidences of liver test abnormalities (≥ Grade 2) in Study 5 are provided in Table 5
Table 5: Liver Test Abnormalities in Pancreatic Cancer Patients: 100 mg Cohort (Study 5)
NSCLC and Pancreatic Indications: Selected Low Frequency Adverse Reactions
Gastrointestinal Disorders
Cases of gastrointestinal bleeding (including fatalities) have been reported, some associated with concomitant warfarin or NSAID administration
3.2Post-Marketing Experience
The following adverse reactions have been identified during post approval use of erlotinib. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Musculoskeletal and Connective Tissue Disorders: myopathy, including rhabdomyolysis, in combination with statin therapy
Eye Disorders: ocular inflammation including uveitis
4DRUG INTERACTIONS
CYP3A4 Inhibitors
Co-administration of erlotinib with a strong CYP3A4 inhibitor or a combined CYP3A4 and CYP1A2 inhibitor increased erlotinib exposure. Erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2. Increased erlotinib exposure may increase the risk of exposure-related toxicity [see Clinical Pharmacology (
Co-administration of erlotinib with a strong CYP3A4 inhibitor or a combined CYP3A4 and CYP1A2 inhibitor increased erlotinib exposure. Erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2. Increased erlotinib exposure may increase the risk of exposure-related toxicity [see Clinical Pharmacology (
Avoid co-administering erlotinib with strong CYP3A4 inhibitors (e.g., boceprevir, clarithromycin, conivaptan,indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telithromycin, voriconazole, grapefruit or grapefruit juice) or a combined CYP3A4 and CYP1A2 inhibitor (e.g., ciprofloxacin). Reduce the erlotinib dosage when co-administering with a strong CYP3A4 inhibitor or a combined CYP3A4 and CYP1A2 inhibitor if co-administration is unavoidable
CYP3A4 Inducers
Pre-treatment with a CYP3A4 inducer prior to erlotinib decreased erlotinib exposure [see Clinical Pharmacology (. Increase the erlotinib dosage if co-administration with CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin, rifabutin, rifapentine, phenobarbital and St. John's wort) is unavoidable [see Dosage and Administration (.
Pre-treatment with a CYP3A4 inducer prior to erlotinib decreased erlotinib exposure [see Clinical Pharmacology (. Increase the erlotinib dosage if co-administration with CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin, rifabutin, rifapentine, phenobarbital and St. John's wort) is unavoidable [see Dosage and Administration (.
CYP1A2 Inducers and Cigarette Smoking
Cigarette smoking decreased erlotinib exposure. Avoid smoking tobacco (CYP1A2 inducer) and avoid concomitant use of erlotinib with moderate CYP1A2 inducers (e.g., teriflunomide, rifampin, or phenytoin). Increase the erlotinib dosage in patients that smoke tobacco or when co-administration with moderate CYP1A2 inducers is unavoidable [see Dosage and Administration (.
Cigarette smoking decreased erlotinib exposure. Avoid smoking tobacco (CYP1A2 inducer) and avoid concomitant use of erlotinib with moderate CYP1A2 inducers (e.g., teriflunomide, rifampin, or phenytoin). Increase the erlotinib dosage in patients that smoke tobacco or when co-administration with moderate CYP1A2 inducers is unavoidable [see Dosage and Administration (.
Drugs that Increase Gastric pH
Co-administration of erlotinib with proton pump inhibitors (e.g., omeprazole) and H-2 receptor antagonists (e.g., ranitidine) decreased erlotinib exposure [see Clinical Pharmacology (. For proton pump inhibitors, avoid concomitant use if possible. For H-2 receptor antagonists and antacids, modify the dosing schedule [see Dosage and Administration (2.4)]. Increasing the dose of erlotinib when co-administered with gastric pH elevating agents is not likely to compensate for the loss of exposure.
Co-administration of erlotinib with proton pump inhibitors (e.g., omeprazole) and H-2 receptor antagonists (e.g., ranitidine) decreased erlotinib exposure [see Clinical Pharmacology (. For proton pump inhibitors, avoid concomitant use if possible. For H-2 receptor antagonists and antacids, modify the dosing schedule [see Dosage and Administration (2.4)]. Increasing the dose of erlotinib when co-administered with gastric pH elevating agents is not likely to compensate for the loss of exposure.
Anticoagulants
Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions, which in some cases were fatal, have been reported in patients receiving erlotinib. Regularly monitor prothrombin time or INR in patients taking coumarin-derived anticoagulants. Dose modifications of erlotinib are not recommended [see Warnings and Precautions (
Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions, which in some cases were fatal, have been reported in patients receiving erlotinib. Regularly monitor prothrombin time or INR in patients taking coumarin-derived anticoagulants. Dose modifications of erlotinib are not recommended [see Warnings and Precautions (
5OVERDOSAGE
Withhold erlotinib in patients with an overdose or suspected overdose and institute symptomatic treatment.
6DESCRIPTION
Erlotinib Tablets, a kinase inhibitor, is a quinazolinamine with the chemical name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine. Erlotinib Tablets contain erlotinib as the hydrochloride salt that has the following structural formula:
C
The molecule has a pK
Aqueous solubility of erlotinib hydrochloride is dependent on pH with increased solubility at a pH of less than 5 due to protonation of the secondary amine. Over the pH range of 1.4 to 9.6, maximal solubility of approximately 0.4 mg/mL occurs at a pH of approximately 2.
Erlotinib Tablets for oral administration are available in three dosage strengths containing erlotinib hydrochloride (27.3 mg, 109.3 mg and 163.9 mg) equivalent to 25 mg, 100 mg and 150 mg erlotinib and the following inactive ingredients: colloidal silicon dioxide, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulfate, sodium starch glycolate, titanium dioxide, and triacetin.
7HOW SUPPLIED/STORAGE AND HANDLING
Erlotinib Tablets are available as follows:
25 mg: Round, biconvex, unscored, white film-coated tablets, debossed
100 mg: Round, biconvex, unscored, white film-coated tablets, debossed
150 mg: Round, biconvex, unscored, white film-coated tablets, debossed
Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].
Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).
KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.
8PATIENT COUNSELING INFORMATION
Skin rash, bullous and exfoliative skin disorders
- Advise patients that skin reactions can occur or worsen on sun-exposed areas while taking erlotinib tablets, and proactive intervention may include alcohol-free emollient cream and use of sunscreen or avoidance of sun exposure. Advise patients that hyperpigmentation or dry skin, with or without digital skin fissures, have been reported and in the majority of cases were associated with rash
- Advise patients that erlotinib tablets can increase the risk of bullous and exfoliative skin disorders and to seek immediately medical attention for severe skin reactions
Diarrhea Advise patients that diarrhea can usually be managed with loperamide and to contact their healthcare provider for severe or persistent diarrhea [see Adverse Reactions (6.1)].
Interstitial lung disease Advise patients of the risk of severe or fatal ILD, including pneumonitis. Advise patients to contact their healthcare provider immediately to report new of worsening unexplained shortness of breath or coughing [see Dosage and Administration (2.4) and Warnings and Precautions (5.1)].
Renal failure Advise patients of the risk of developing renal failure. Inform patients of the need for the healthcare provider to monitor kidney function and electrolytes [see Warnings and Precautions (5.2)].
Hepatotoxicity
Advise patients to immediately report signs or symptoms of hepatotoxicity
Gastrointestinal perforations Advise patients that erlotinib tablets can increase the risk of gastrointestinal perforation or fistula and to seek immediate medical attention for severe abdominal pain [see Dosage and Administration (2.4) and Warnings and Precautions (5.4)].
Cerebrovascular accident Advise patients of the risk of cerebrovascular accident and see immediate medical attention [see Dosage and Administration (2.4) and Warnings and Precautions (5.6)].
Ocular disorders Advise patients promptly to contact their healthcare provider if they develop eye signs or symptoms, lacrimation, light sensitivity, blurred vision, eye pain, red eye, or changes in vision [see Dosage and Administration (2.4) and Warnings and Precautions (5.8)].
Hemorrhage in patients taking warfarin Advise patients who are receiving warfarin of the need to monitor INR or other coumarin-derivative anticoagulants [see Warnings and Precautions (5.9) and Drug Interactions (7)].
Hair and nail disorders Advise patients that hair and nail disorders, including hirsutism and brittle and loose nails, have been reported [see Adverse Reactions (6.1)].
Embryo-fetal toxicity
- Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy
- Advise females of reproductive potential to use effective contraception during treatment with erlotinib tablets, and for 1 month after the last dose
- Advise women not to breastfeed during treatment with erlotinib tablets and for 2 weeks after the final dose
- Advise patients to contact their health care provider for any changes in smoking status and that the dose of erlotinib tablets may need to be adjusted if they smoke
- Advise patients to stop smoking
For further information please call 1-888-838-2872.
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Rev. B 7/2019
9PRINCIPAL DISPLAY PANEL
NDC 0093-7662-56
Erlotinib
Tablets
25 mg
Rx only
30 TABLETS
TEVA
10PRINCIPAL DISPLAY PANEL
NDC 0093-7663-56
Erlotinib
Tablets
100 mg
Rx only
30 TABLETS
TEVA
11PRINCIPAL DISPLAY PANEL
NDC 0093-7664-56
Erlotinib
Tablets
150 mg
Rx only
30 TABLETS
TEVA
