{"entity":{"id":"erlotinib","kind":"drug","name":"Erlotinib","aka":[],"tldr":"Erlotinib was one of the first EGFR pills for lung cancer; it was approved before anyone knew EGFR mutations predicted who would respond, then redefined by them.","summary":"Erlotinib is a reversible, ATP-competitive first-generation EGFR tyrosine kinase inhibitor that is most active against exon 19 deletions and the L858R mutation. It was first approved in the US in 2004 for advanced NSCLC after chemotherapy on the strength of BR.21 (2005), which showed a survival benefit in unselected pretreated patients before EGFR mutations were known to predict response. EURTAC (2012) and OPTIMAL then established first-line use in EGFR-mutant disease, leading to the 2013 US approval for exon 19 deletion or L858R tumours, and osimertinib later displaced it in the FLAURA trial. It is also approved with gemcitabine in pancreatic cancer since 2005, where the benefit is marginal. Rash and diarrhoea are the characteristic toxicities. Erlotinib is the drug that taught oncology to select patients by mutation rather than by histology alone.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Erlotinib","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=erlotinib"},{"label":"EMA Tarceva product page: pancreatic indication","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/tarceva"},{"label":"Sinn et al., CONKO-005 (JCO 2017)","url":"https://doi.org/10.1200/JCO.2017.72.6463"},{"label":"Abrams et al., RTOG 0848 step 1 (Am J Clin Oncol 2020)","url":"https://doi.org/10.1097/COC.0000000000000633"}],"tags":["gap-fill","generic"],"related":[],"cancers":["nsclc","pancreatic","egfr-mutant-nsclc"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["egfr"],"drugs":[],"companies":["roche-genentech","astellas"],"institutions":[],"pathways":[],"terms":["egfr-exon19-l858r","histology"],"trials":["nct02152631","nct02411448","nct05442060","conko-005","lap07"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["Pancreatic cancer: erlotinib with gemcitabine is licensed for metastatic disease in the United States (2005) and the EU on a trial whose survival gain was under two weeks, and it added nothing in the adjuvant CONKO-005 (disease-free survival 11.4 months in both arms), in RTOG 0848 step 1 (median survival 29.9 against 28.1 months) or in the first randomisation of LAP07 (13.6 months with gemcitabine against 11.9 with the combination). NICE NG85 does not recommend it and NCCN no longer lists it as a preferred option."],"brand":"Tarceva","modality":"Small-molecule EGFR TKI (first generation, reversible)","mechanism":"Reversible ATP-competitive inhibitor of EGFR kinase; most active against exon 19 deletion and L858R mutations.","approvals":[{"region":"US","year":2004,"indication":"Locally advanced/metastatic NSCLC after chemotherapy"},{"region":"US","year":2005,"indication":"Pancreatic cancer with gemcitabine"},{"region":"US","year":2013,"indication":"First-line NSCLC with EGFR exon 19 del or L858R"},{"region":"EU","year":2007,"indication":"Metastatic pancreatic cancer with gemcitabine (Tarceva product information: factors associated with prolonged survival should be taken into account when prescribing; 100 mg daily); marketing authorisation for the product 19 September 2005","note":"https://www.ema.europa.eu/en/medicines/human/EPAR/tarceva"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/erlotinib/","neighbours":{"cancer":[{"id":"lung-adenosquamous-carcinoma","kind":"cancer","name":"Adenosquamous carcinoma of the lung","route":"/cancers/lung-adenosquamous-carcinoma/"},{"id":"egfr-mutant-nsclc","kind":"cancer","name":"EGFR-mutated non-small-cell lung cancer","route":"/cancers/egfr-mutant-nsclc/"},{"id":"lung-cancer","kind":"cancer","name":"Lung cancer (all types)","route":"/cancers/lung-cancer/"},{"id":"nsclc","kind":"cancer","name":"Non-small-cell lung cancer","route":"/cancers/nsclc/"},{"id":"pancreatic","kind":"cancer","name":"Pancreatic ductal adenocarcinoma","route":"/cancers/pancreatic/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"egfr","kind":"target","name":"EGFR","route":"/targets/egfr/"}],"company":[{"id":"astellas","kind":"company","name":"Astellas","route":"/companies/astellas/"},{"id":"roche-genentech","kind":"company","name":"Roche / Genentech","route":"/companies/roche-genentech/"}],"term":[{"id":"egfr-exon19-l858r","kind":"term","name":"EGFR exon 19 deletion & L858R","route":"/terms/egfr-exon19-l858r/"},{"id":"egfr-mutation-subtypes","kind":"term","name":"EGFR mutation subtypes (exon 19 deletion, L858R, exon 20 insertion, T790M)","route":"/terms/egfr-mutation-subtypes/"},{"id":"hair-brows-and-lashes","kind":"term","name":"Eyebrow and eyelash loss (madarosis)","route":"/terms/hair-brows-and-lashes/"},{"id":"histology","kind":"term","name":"Histology","route":"/terms/histology/"},{"id":"pancreatic-failed-programmes","kind":"term","name":"Pancreatic cancer: the failed and stopped programmes and why","route":"/terms/pancreatic-failed-programmes/"}],"trial":[{"id":"nct02152631","kind":"trial","name":"A Study of Abemaciclib (LY2835219) in Participants With Previously Treated KRAS Mutated Lung Cancer","route":"/trials/nct02152631/"},{"id":"nct02411448","kind":"trial","name":"A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RE","route":"/trials/nct02411448/"},{"id":"alchemist","kind":"trial","name":"ALCHEMIST (Adjuvant Lung Cancer Enrichment Marker Identification and Sequencing Trials)","route":"/trials/alchemist/"},{"id":"nct01360554","kind":"trial","name":"ARCHER 1009: A Study Of Dacomitinib (PF-00299804) Vs. Erlotinib In The Treatment Of Advanced Non-Small Cell Lung Cancer","route":"/trials/nct01360554/"},{"id":"nct06483555","kind":"trial","name":"Basal-like PDAC Treated With Gemcitabine, Erlotinib, and Nab-paclitaxel","route":"/trials/nct06483555/"},{"id":"conko-005","kind":"trial","name":"CONKO-005","route":"/trials/conko-005/"},{"id":"cupisco","kind":"trial","name":"CUPISCO","route":"/trials/cupisco/"},{"id":"flaura","kind":"trial","name":"FLAURA","route":"/trials/flaura/"},{"id":"lap07","kind":"trial","name":"LAP07","route":"/trials/lap07/"},{"id":"lung-map","kind":"trial","name":"Lung-MAP (SWOG S1400 and S1900)","route":"/trials/lung-map/"},{"id":"mypathway","kind":"trial","name":"MyPathway","route":"/trials/mypathway/"},{"id":"tapur","kind":"trial","name":"TAPUR (Targeted Agent and Profiling Utilization Registry)","route":"/trials/tapur/"},{"id":"nct05442060","kind":"trial","name":"To Evaluate OBI-833/OBI-821 in Combination With First-Line Erlotinib in Patients With EGFR-Mutated, Globo H-Positive, Locally Advanced or Metastatic N","route":"/trials/nct05442060/"}],"paper":[{"id":"paper-pao-egfr-t790m-acquired-resistance-plos-med-2005","kind":"paper","name":"Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain","route":"/key-papers/paper-pao-egfr-t790m-acquired-resistance-plos-med-2005/"},{"id":"paper-lynch-egfr-activating-mutations-gefitinib-nejm-2004","kind":"paper","name":"Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib","route":"/key-papers/paper-lynch-egfr-activating-mutations-gefitinib-nejm-2004/"},{"id":"paper-yu-acquired-resistance-rebiopsy-egfr-ccr-2013","kind":"paper","name":"Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers","route":"/key-papers/paper-yu-acquired-resistance-rebiopsy-egfr-ccr-2013/"},{"id":"paper-sequist-genotypic-histological-evolution-egfr-resistance-sci-transl-med-2011","kind":"paper","name":"Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors","route":"/key-papers/paper-sequist-genotypic-histological-evolution-egfr-resistance-sci-transl-med-2011/"},{"id":"paper-lap07-chemoradiotherapy-locally-advanced-pancreatic-jama-2016","kind":"paper","name":"LAP07: chemoradiotherapy versus continued chemotherapy for locally advanced pancreatic cancer controlled after four months of gemcitabine","route":"/key-papers/paper-lap07-chemoradiotherapy-locally-advanced-pancreatic-jama-2016/"},{"id":"paper-engelman-met-amplification-gefitinib-resistance-science-2007","kind":"paper","name":"MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling","route":"/key-papers/paper-engelman-met-amplification-gefitinib-resistance-science-2007/"}],"institution":[{"id":"guangdong-provincial-peoples-hospital","kind":"institution","name":"Guangdong Provincial People's Hospital","route":"/institutions/guangdong-provincial-peoples-hospital/"}],"roadmap":[{"id":"ctdna-tests","kind":"roadmap","name":"ctDNA tests roadmap: from a curiosity in plasma to blood tests that decide treatment","route":"/roadmaps/ctdna-tests/"},{"id":"targeted-therapy-roadmap","kind":"roadmap","name":"Targeted therapy roadmap: imatinib → designed for resistance → the undruggable drivers fall","route":"/roadmaps/targeted-therapy-roadmap/"}],"drug":[{"id":"cobas-egfr-mutation-test","kind":"drug","name":"cobas EGFR Mutation Test v2","route":"/drugs/cobas-egfr-mutation-test/"}],"biomarker":[{"id":"egfr-exon-19-deletion","kind":"biomarker","name":"EGFR exon 19 deletion","route":"/biomarkers/egfr-exon-19-deletion/"},{"id":"egfr-l858r","kind":"biomarker","name":"EGFR L858R","route":"/biomarkers/egfr-l858r/"}],"pathway":[{"id":"pancreatic-cancer-signalling","kind":"pathway","name":"Pancreatic cancer (KEGG map)","route":"/pathways/pancreatic-cancer-signalling/"}]}}