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.
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.
Reversible ATP-competitive inhibitor of EGFR kinase; most active against exon 19 deletion and L858R mutations. Connects to EGFR.
1.Erlotinib slips into a pocket on EGFR.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026). Generic erlotinib is inexpensive.
Multi-source generic on low-cost tiers; usually no prior authorisation. Cash prices without insurance are modest. Some plans still require EGFR mutation documentation.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA258 · SMC advice: erlotinib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
| Region | Year | Indication |
|---|---|---|
| US | 2004 | Locally advanced/metastatic NSCLC after chemotherapy |
| US | 2005 | Pancreatic cancer with gemcitabine |
| US | 2013 | First-line NSCLC with EGFR exon 19 del or L858R |
| EU | 2007 | 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 · https://www.ema.europa.eu/en/medicines/human/EPAR/tarceva |
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Systemic chemotherapy is the backbone for locally advanced pancreatic cancer; consolidation chemoradiotherapy is an option to control local symptoms or as a bridge to surgery rather than a survival treatment.
It is the reference frequency table for resistance to first-generation EGFR inhibitors, and it made rebiopsy at progression standard rather than exceptional, because the mechanism decides the next treatment and cannot be guessed.
The case for re-biopsy at progression, for treating resistance as a diagnosis rather than an endpoint, and for the idea of a drug holiday. It is also the origin of resistance-directed sequencing: what you give next should depend on what the tumour became.
It defined bypass resistance as a category and set the treatment rule that follows from it: keep blocking the original target and add an inhibitor of the bypass, which is the logic of every EGFR plus MET combination since.
It generalised the single-patient finding and made the point that drug-resistant subclones are selected by treatment rather than created by it, which is the model the whole field now works with.
The template for every driver mutation since: find the responders, sequence them, and give the drug only to people whose tumour carries the lesion it was built for. Gefitinib had been close to abandonment on the strength of unselected trials.
Query for this drug: (TITLE:"Erlotinib" OR ABSTRACT:"Erlotinib" OR TITLE:"Tarceva" OR ABSTRACT:"Tarceva") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Erlotinib, not a curated reading list.
Shares Adenosquamous carcinoma of the lung, A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RE, Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain, EGFR exon 19 deletion & L858R and the tag generic.
Shares Lung cancer (all types), Non-small-cell lung cancer and the tag generic.
Shares LAP07: chemoradiotherapy versus continued chemotherapy for locally advanced pancreatic cancer controlled after four months of gemcitabine, LAP07, Roche / Genentech, Pancreatic ductal adenocarcinoma and the tag generic.
Shares Pancreatic ductal adenocarcinoma and the tag generic.
Shares CONKO-005, LAP07: chemoradiotherapy versus continued chemotherapy for locally advanced pancreatic cancer controlled after four months of gemcitabine, Basal-like PDAC Treated With Gemcitabine, Erlotinib, and Nab-paclitaxel, LAP07 and the tag generic.
Shares Lung cancer (all types), Non-small-cell lung cancer and the tag generic.
Shares Pancreatic ductal adenocarcinoma and the tag generic.
Shares Lung cancer (all types) and the tag generic.