Erlotinib

Epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells. In some tumor cells signaling through this receptor plays a role in tumor cell survival and proliferation irrespective of EGFR mutation status.

• Erlotinib tablet is a kinase inhibitor indicated for: The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) 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 ( 1.1 ) First-line treatment of patients with locally advanced, unrespectable or metastatic pancreatic cancer, in combination with gemcitabine. ( 1.2 ) Limitations of Use: Safety and efficacy of erlotinib tablets have not been established in patients with NSCLC whose tumors have other EGFR mutations.ICD-10: C34.90

• None None ( 4 )contraindicated

NSCLC: 150mg orally, on an empty stomach, once daily ( 2.2 ) Pancreatic cancer: 100 mg orally, on an empty stomach, once daily. ( 2.3 ) 2.1 Selection of Patients with Metastatic NSCLC Select patients for the treatment of metastatic NSCLC with erlotinib tablets based on the presence of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations in tumor or plasma specimens [see Clinical Studies (14.1 , 14.2) ] . If these mutations are not detected in a plasma specimen, test tumor tissue if available. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics . 2.2 Recommended Dose – NSCLC The recommended daily dose of erlotinib tablets for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs. 2.3 Recommended Dose – Pancreatic Cancer The recommended daily dose of erlotinib tablets for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take erlotinib tablet on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs [see Clinical Studies (14.5) ] .

Interstitial lung disease (ILD) : Occurs in 1.1% of patients. Withhold erlotinib tablets for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue erlotinib if ILD is diagnosed. ( 5.1 ) Renal failure : Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold erlotinib tablets for severe renal toxicity. ( 5.2 ) Hepatotoxicity : Occurs with or without hepatic impairment, including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue erlotinib tablets for severe or worsening liver tests. ( 5.3 ) Gastrointestinal perforations : Discontinue erlotinib tablets. ( 5.4 ) Bullous and exfoliative skin disorders : Discontinue erlotinib tablets. ( 5.5 ) Cerebrovascular accident (CVA) : The risk of CVA is increased in patients with pancreatic cancer. ( 5.6 ) Microangiopathic hemolytic anemia (MAHA) : The risk of MAHA is increased in patients with pancreatic cancer. ( 5.7 ) Ocular disorders : Discontinue erlotinib tablets for corneal perforation, ulceration or persistent severe keratitis. ( 5.8 ) Hemorrhage in patients taking warfarin : Regularly monitor INR in patients taking warfarin or other coumarin-derivative anticoagulants. ( 5.9 ) Embryo-fetal toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to the fetus and to use effective contraception.( 5.10 , 8.1 , 8.3 ) 5.1 Interstitial Lung Disease (ILD) Cases of serious ILD, including fatal cases, can occur with erlotinib tablets treatment.

The following serious adverse reactions, which may include fatalities, are discussed in greater detail in other sections of the labeling: Interstitial Lung Disease (ILD) [see Warnings and Precautions (5.1) ] Renal Failure [see Warnings and Precautions (5.2) ] Hepatotoxicity with or without Hepatic Impairment [see Warnings and Precautions (5.3) ] Gastrointestinal Perforation [see Warnings and Precautions (5.4) ] Bullous and Exfoliative Skin Disorders [see Warnings and Precautions (5.5) ] Cerebrovascular Accident [see Warnings and Precautions (5.6) ] Microangiopathic Hemolytic Anemia with Thrombocytopenia [see Warnings and Precautions (5.7) ] Ocular Disorders [see Warnings and Precautions (5.8) ] Hemorrhage in Patients Taking Warfarin [see Warnings and Precautions (5.9) ] The most common adverse reactions (≥20%) with erlotinib tablets from a pooled analysis in patients with NSCLC across all approved lines of therapy, with and without EGFR mutations, and in patients with pancreatic cancer were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact 1-888-557-1212 or FDA at 1-800-FDA-1088 or http://www.fda.gov/medwatch 6.1 Clinical Trials Safety 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.

Lactation: Do not breastfeed ( 8.2 ) 8.1 Pregnancy Risk Summary Based on animal data and its mechanism of action, erlotinib tablets can cause fetal harm when administered to a pregnant woman. Limited available data on use of erlotinib tablets in pregnant women are not sufficient to inform a risk of major birth defects or miscarriage. When given during organogenesis, erlotinib administration resulted in embryo-fetal lethality and abortion in rabbits at exposures approximately 3 times the exposure at the recommended human daily dose of 150 mg. Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data Erlotinib has been shown to cause maternal toxicity resulting in embryo-fetal lethality and abortion in rabbits when given during the period of organogenesis at doses that result in plasma drug concentrations approximately 3 times those achieved at the recommended dose in humans (AUCs at 150 mg daily dose). During the same period, there was no increase in the incidence of embryo-fetal lethality or abortion in rabbits or rats at doses resulting in exposures approximately equal to those in humans at the recommended daily dose.

Metabolism

Absorption Erlotinib is about 60% absorbed after oral administration. Peak plasma levels occur 4 hours after dosing.

Withhold erlotinib tablets in patients with an overdose or suspected overdose and institute symptomatic treatment.

• Aug 28, 2015ANDAANDA091059Teva Pharms Usa Inc
• Nov 5, 2019ANDAANDA211960Shilpa
• Nov 5, 2019ANDAANDA210300Sun Pharm
• Apr 16, 2020ANDAANDA213065Zydus Pharms
• May 10, 2021ANDAANDA214366Msn
• Jul 8, 2021ANDAANDA214719Alembic
• Jun 22, 2022ANDAANDA216342Eugia Pharma
• May 24, 2024ANDAANDA209267Hetero Labs Ltd V

1. 1Death3,65730%
2. 2Diarrhoea1,33211%
3. 3Rash1,31111%
4. 4Off Label Use8987.2%
5. 5Malignant Neoplasm Progression8897.2%
6. 6Fatigue7185.8%
7. 7Nausea6955.6%
8. 8Vomiting5764.6%
9. 9Disease Progression5664.6%
10. 10Decreased Appetite5094.1%
11. 11Anaemia4974.0%
12. 12Dyspnoea4853.9%
13. 13Drug Resistance4733.8%
14. 14Asthenia4623.7%
15. 15Pneumonia4183.4%

Recent PubMed references pinned to Erlotinib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Erlotinib and Leflunomide Disrupt 6-Formylindolo[3,2-b]Carbazole Metabolism and Sensitize Keratinocytes to UVA Radiation-Induced Apoptosis.
  Photodermatology, photoimmunology & photomedicine · 2026 · Hartung F, Dairou J, Ramamoorthy S, et al.
  PMID 42218641DOI 10.1111/phpp.70099
• Liv-52 Attenuates Erlotinib-Induced Liver Injury via Modulation of Oxidative Stress, Inflammation, and Apoptosis in Rats.
  International journal of molecular sciences · 2026 · Bulut S, Altuner D, Suleyman B, et al.
  PMID 42123402DOI 10.3390/ijms27093817
• An In silico model-based feasibility assessment of erlotinib long-acting injectable formulation for the management of metastatic non-small cell lung cancer.
  Xenobiotica; the fate of foreign compounds in biological systems · 2026 · Joseph A, Akbar S, Malgave A, et al.
  PMID 42018335DOI 10.1080/00498254.2026.2661623
• Carcinoembryonic Antigen-Related Cell Adhesion Molecule 5 as a Biomarker for Predicting Response to Erlotinib and Gefitinib in Lung Adenocarcinoma: An Integrative Analysis of Transcriptomic Data of PC-9 and Drug-Resistant PC-9 Cell Lines.
  International journal of molecular sciences · 2026 · Raungrut P, Tanyapattrapong S, Maungchanburi S, et al.
  PMID 41977278DOI 10.3390/ijms27073092
• HIF-1α siRNA Enhances the Efficacy of Erlotinib in Non-small Cell Lung Cancer: A Novel Strategy to Reverse Hypoxia-Induced Drug Resistance.
  Drugs in R&D · 2026 · Jiang H, Cai S, Zhang X, et al.
  PMID 41931244DOI 10.1007/s40268-025-00534-5
• Ocular Surface Ulceration Associated With an Epidermal Growth Factor Receptor Inhibitor.
  Cornea · 2026 · Ziari M, Chen JL, Gonzalez C, et al.
  PMID 41919994DOI 10.1097/ICO.0000000000004143
• Erlotinib Induces Cell Death by Blocking NIX-mediated Mitophagy Through Lysosomal Swelling in IDH1-mutant Cholangiocarcinoma.
  Anticancer research · 2026 · Kang Y, Kim C, Jeong CY, et al.
  PMID 41760233DOI 10.21873/anticanres.18034
• Exploring synergistic therapeutic potential of Erlotinib and artemisinin in non-small cell lung Cancer (NSCLC) using pharmacological networking and mathematical modeling.
  Clinica chimica acta; international journal of clinical chemistry · 2026 · Suleman F, Khan T, Alshehade SA, et al.
  PMID 41672289DOI 10.1016/j.cca.2026.120890

The 10 most recently updated of 873 ClinicalTrials.gov registrations naming Erlotinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Review of Post-Study Clinical Endoscopy Reports in Follow Up to MAY2016-07-01
  Terminated · Observational · 42 enrolled · National Cancer Institute (NCI)
  NCT04674228updated 2026-06-11
• Study of the CHK1 Inhibitor BBI-355, an ecDNA-directed Therapy (ecDTx), and the RNR Inhibitor BBI-825, in Subjects With Tumors With Oncogene Amplifications
  Terminated · Phase 1 · Interventional · 85 enrolled · Boundless Bio, Inc.
  NCT05827614updated 2026-06-08
• Study of RADPLAT and Tarceva in Locally Advanced Head and Neck Squamous Cell Carcinoma (SCCA)
  Completed · Phase 2 · Interventional · 21 enrolled · Southern Illinois University
  NCT00304278updated 2026-06-08
• Maintenance Chemotherapy With or Without Local Consolidative Therapy in Treating Patients With Stage IV Non-small Cell Lung Cancer
  Active not recruiting · Phase 2 · Interventional · 218 enrolled · NRG Oncology
  NCT03137771updated 2026-06-08
• Testing of Bevacizumab, Erlotinib, and Atezolizumab in Combination for Advanced-Stage Kidney Cancer
  Recruiting · Phase 2 · Interventional · 65 enrolled · National Cancer Institute (NCI)
  NCT04981509updated 2026-06-03
• A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-6036 Alone or in Combination in Participants With Advanced or Metastatic Solid Tumors With a KRAS G12C Mutation
  Active not recruiting · Phase 1 · Interventional · 498 enrolled · Genentech, Inc.
  NCT04449874updated 2026-06-02
• Erlotinib Hydrochloride in Treating Patients With Stage IB-IIIA Non-small Cell Lung Cancer That Has Been Completely Removed by Surgery (An ALCHEMIST Treatment Trial)
  Active not recruiting · Phase 3 · Interventional · 390 enrolled · National Cancer Institute (NCI)
  NCT02193282updated 2026-05-29
• Genetic Testing in Screening Patients With Stage IB-IIIA Non-small Cell Lung Cancer That Has Been or Will Be Removed by Surgery (The ALCHEMIST Screening Trial)
  Active not recruiting · Interventional · 8,300 enrolled · National Cancer Institute (NCI)
  NCT02194738updated 2026-05-29
• Erlotinib Hydrochloride and Cabozantinib-s-Malate Alone or in Combination as Second or Third Line Therapy in Treating Patients With Stage IV Non-small Cell Lung Cancer
  Active not recruiting · Phase 2 · Interventional · 125 enrolled · National Cancer Institute (NCI)
  NCT01708954updated 2026-05-29
• A Phase I, Open-Label, Multi-center Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD6244 (ARRY-142886)
  Completed · Phase 1 · Interventional · 140 enrolled · AstraZeneca
  NCT00600496updated 2026-05-27

Frequently asked questions

How does Erlotinib work?

Epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells. In some tumor cells signaling through this receptor plays a role in tumor cell survival and proliferation irrespective of EGFR mutation status.

What is Erlotinib used for?

According to FDA labeling, Erlotinib carries indications including: Erlotinib tablet is a kinase inhibitor indicated for: The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) 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 ( 1.1 ) First-line treatment of patients with locally advanced, unrespectable or metastatic pancreatic cancer, in combination with gemcitabine. ( 1.2 ) Limitations of Use: Safety and efficacy of erlotinib tablets have not been established in patients with NSCLC whose tumors have other EGFR mutations.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Erlotinib?

Erlotinib is classified as Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, Kinase Inhibitor, HER1 Antagonists, Protein Kinase Inhibitors, Cellular Division Phase Alteration, Cellular Growth Phase Reduction, Increased Cellular Death, Vascular Growth Decrease.

What are the brand names for Erlotinib?

Erlotinib is marketed under brand names including Tarceva.

What are the contraindications for Erlotinib?

Erlotinib labeling lists contraindications including: None None ( 4 ). Always consult the full prescribing information and a clinician.