# Gefitinib

Source: https://onco.cc/drugs/gefitinib/  
OnCo record `gefitinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

The lung-cancer pill whose dramatic responses in a few patients led to the discovery of EGFR mutations in 2004.

## Summary

Gefitinib is a reversible first-generation EGFR tyrosine kinase inhibitor selective for sensitising mutations. It received accelerated US approval in 2003 in unselected NSCLC after chemotherapy, but the ISEL trial (2005) failed to show a survival benefit in that population and US use was restricted. The dramatic responses seen in a minority of patients led Lynch and Paez in 2004 to discover activating EGFR mutations in responders, one of the founding discoveries of precision oncology. IPASS (NEJM 2009) then proved that mutation-selected first-line gefitinib was superior to chemotherapy, and the EU approved it for EGFR-mutant NSCLC in 2009; the US re-approved it in 2015 for first-line exon 19 deletion or L858R disease. Rash, diarrhoea and rare interstitial lung disease are the main toxicities. Gefitinib's story is the reason EGFR testing is now routine at diagnosis.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-08
- Tags: gap-fill; generic
- Brand: Iressa
- Modality: Small-molecule EGFR TKI (first generation, reversible)
- Mechanism: Reversible EGFR kinase inhibitor selective for sensitising mutations.
- Approvals: US 2003: NSCLC after chemotherapy (accelerated; restricted 2005); EU 2009: EGFR-mutant NSCLC; US 2015: First-line NSCLC with EGFR exon 19 del or L858R

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Gefitinib
- IPASS (NEJM 2009): https://doi.org/10.1056/NEJMoa0810699
- Label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=gefitinib

## Connected records

- biomarkers: [EGFR exon 19 deletion](https://onco.cc/biomarkers/egfr-exon-19-deletion/), [EGFR L858R](https://onco.cc/biomarkers/egfr-l858r/)
- cancers: [Adenosquamous carcinoma of the lung](https://onco.cc/cancers/lung-adenosquamous-carcinoma/), [EGFR-mutated non-small-cell lung cancer](https://onco.cc/cancers/egfr-mutant-nsclc/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [EGFR](https://onco.cc/targets/egfr/)
- companies: [AstraZeneca](https://onco.cc/companies/astrazeneca/)
- terms: [EGFR exon 19 deletion & L858R](https://onco.cc/terms/egfr-exon19-l858r/), [EGFR mutation subtypes (exon 19 deletion, L858R, exon 20 insertion, T790M)](https://onco.cc/terms/egfr-mutation-subtypes/), [Oncogene addiction](https://onco.cc/terms/oncogene-addiction/)
- trials: [A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RE](https://onco.cc/trials/nct02411448/), [AENEAS](https://onco.cc/trials/aeneas/), [ARCHER 1050](https://onco.cc/trials/nct01774721/), [FLAURA](https://onco.cc/trials/flaura/), [FURLONG](https://onco.cc/trials/furlong/), [Gefitinib vs gefitinib plus pemetrexed-carboplatin in EGFR-mutant lung cancer (Tata Memorial)](https://onco.cc/trials/gefitinib-chemo-tmh/), [Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD)](https://onco.cc/trials/nct03944772/), [Study to Allow Patients Previously Participating in a Novartis Sponsored Trial to Continue Receiving Capmatinib Treatment as Single Agent or in Combination With Other Treatments or the Combination Treatment Alone](https://onco.cc/trials/nct03040973/)
- key papers: [Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain](https://onco.cc/key-papers/paper-pao-egfr-t790m-acquired-resistance-plos-med-2005/), [Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib](https://onco.cc/key-papers/paper-lynch-egfr-activating-mutations-gefitinib-nejm-2004/), [Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers](https://onco.cc/key-papers/paper-yu-acquired-resistance-rebiopsy-egfr-ccr-2013/), [Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial](https://onco.cc/key-papers/paper-archer-1050-lancet-oncol-2017/), [EGFR mutation and resistance of non-small-cell lung cancer to gefitinib](https://onco.cc/key-papers/paper-kobayashi-egfr-t790m-gefitinib-resistance-nejm-2005/), [EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy](https://onco.cc/key-papers/paper-paez-egfr-mutations-gefitinib-science-2004/), [Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma](https://onco.cc/key-papers/paper-mok-ipass-gefitinib-pulmonary-adenocarcinoma-nejm-2009/), [Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors](https://onco.cc/key-papers/paper-sequist-genotypic-histological-evolution-egfr-resistance-sci-transl-med-2011/), [Improvement in overall survival in a randomized study that compared dacomitinib with gefitinib in patients with advanced non-small-cell lung cancer and EGFR-activating mutations](https://onco.cc/key-papers/paper-archer-1050-os-jco-2018/), [MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling](https://onco.cc/key-papers/paper-engelman-met-amplification-gefitinib-resistance-science-2007/)
- institutions: [Guangdong Provincial People's Hospital](https://onco.cc/institutions/guangdong-provincial-peoples-hospital/)
- roadmaps: [Targeted therapy roadmap: imatinib → designed for resistance → the undruggable drivers fall](https://onco.cc/roadmaps/targeted-therapy-roadmap/)

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