Drug

Gefitinib

Approved · EMA

ClassEpidermal growth factor receptor erbB1 inhibitorEmerging researchLate-stage developmentSteady momentum

Also known as 4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline, Iressa, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine.

RxNorm328134 ChEMBLCHEMBL939 ATCL01EB01UNIIS65743JHBS

Research papers

Active clinical trials

Epidermal growth factor receptor

Primary target

Regulatory events

Latest activity

beta

Recent clinical, regulatory, research and industry developments relating to this drug.

A Phase III, Randomized, Double-blind Study to Assess the Efficacy and Safety of Lazertinib Versus Gefitinib as the First-line Treatment in Patients With Epidermal Growth Factor Receptor Sensitizing Mutation Positive, Locally Advanced or Metastatic Non-Small Cell Lung Cancer

Clinical trial2026-06-29Results posted · ClinicalTrials.gov

APPLE Trial: Feasibility and Activity of AZD9291 (Osimertinib) Treatment on Positive PLasma T790M in EGFR Mutant NSCLC Patients

Clinical trial2026-06-02Results posted · ClinicalTrials.gov

A Phase 1/2 Study of Osimertinib in Combination With Gefitinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer

Clinical trial2026-04-29Results expected Q4 2026 · ClinicalTrials.gov

A Phase III, Double-blind, Randomised Study to Assess the Safety and Efficacy of AZD9291 Versus a Standard of Care Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor as First Line Treatment in Patients With Epidermal Growth Factor Receptor Mutation Positive, Locally Advanced or Metastatic Non Small Cell Lung Cancer.

Clinical trial2026-04-21Results posted · ClinicalTrials.gov

OstEvo - Osteosarcoma Evolves

Clinical trial2026-03-17Results expected Q1 2028 · ClinicalTrials.gov

A Multicenter, Randomized, Double-Blind Study of Erlotinib in Combination With Ramucirumab or Placebo in Previously Untreated Patients With EGFR Mutation-Positive Metastatic Non-Small Cell Lung Cancer

Clinical trial2026-01-16Results posted · ClinicalTrials.gov

Market withdrawal: Gefitinib Mylan (EMA)

Regulatory2024-09-27EMA

Overall Survival with Osimertinib in Untreated, <i>EGFR</i>-Mutated Advanced NSCLC.

Research2019-11-21The New England journal of medicine

Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer.

Research2017-11-18The New England journal of medicine

Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial.

Research2013-08-13The Lancet. Oncology

Phase II study of gefitinib adaptive dose escalation to skin toxicity in recurrent or metastatic squamous cell carcinoma of the head and neck.

Research2012-04-17Oral oncology

Approval: Iressa (EMA)

Regulatory2009-06-24EMA

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name

Gefitinib

Aliases & brands

4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazolineIressaN-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine

RxNorm CUI

328134

ChEMBL ID

CHEMBL939

ATC codes

L01EB01

UNII

S65743JHBS

Primary mechanism

Epidermal growth factor receptor erbB1 inhibitor

Regulatory jurisdictions

ema

Pharmacology & targets

1 target

Known molecular targets and mechanisms supported by curated pharmacology databases.

Epidermal growth factor receptor

EGFR · P00533

INHIBITOREpidermal growth factor receptor erbB1 inhibitor

Regulatory timeline

2 events

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval

2009-06-24

Latest approval

2009-06-24

Authorities

EMA

Total events

emaEuropean Medicines Agency· 2 events

2024-09-27Market withdrawalMarket

Market withdrawal: Gefitinib Mylan (EMA)

Indication: Gefitinib Mylan is indicated as monotherapy for the treatment of adult patients with locally advanced or metastatic non small cell lung cancer (NSCLC) with activating mutations of… Show full indication

Gefitinib Mylan is indicated as monotherapy for the treatment of adult patients with locally advanced or metastatic non small cell lung cancer (NSCLC) with activating mutations of EGFR TK.

Evidence ↗

2009-06-24Approval

Approval: Iressa (EMA)

Indication: Iressa is indicated for the treatment of adult patients with locally advanced or metastatic non-small-cell lung cancer with activating mutations of… Show full indication

Iressa is indicated for the treatment of adult patients with locally advanced or metastatic non-small-cell lung cancer with activating mutations of epidermal-growth-factor-receptor tyrosine kinase.

Evidence ↗

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

197 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme

CLINICALTRIALS.GOV · LIVE REGISTRY

197

registered trials across all phases

LATEST COMPLETION 2026

Active studies

Recruiting

Late-stage (III+)

128

Completed

Discontinued

PHASE DISTRIBUTIONn = 197

Phase 118Phase 1 / 219Phase 2107Phase 2 / 35Phase 336Phase 45Phase N / A7

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Randomised, Controlled Study Comparing Chemotherapy Plus Intercalated EGFR-Tyrosine Kinase Inhibitors Combination Therapy With EGFR-Tyrosine Kinase Inhibitors Alone Therapy as First-line Treatment for Patients With Non-Small-Cell Lung Cancer

Unknown statusPH IVQilu Hospital of Shandong Universityn=2502017

A Randomized, Open-label, Multiple-centre Study of Intercalating and Maintenance Gefitinib in Combination With Chemotherapy for Advanced NSCLC With EGFR Mutation Positive

TerminatedPH IVSichuan Universityn=612017

An Open Label, Multicentre, Single Arm Study to Characterise the Efficacy, Safety and Tolerability of Gefitinib 250 mg (IRESSA™) as First Line Treatment in Caucasian Patients, Who Have Epidermal Growth Factor Receptor (EGFR) Mutation Positive Locally Advanced or Metastatic Non-Small Cell Lung Cancer

CompletedPH IVKey trialAstraZenecan=1,0602016

A Placebo-Controlled, Multicentre, Randomised, Parallel Group, Trial to Assess the Efficacy, Safety and Tolerability of Gefitinib (Iressa® 250mg) as Maintenance Therapy in Locally Advanced or Metastatic (StageIIIB/IV) Non Small Cell Lung Cancer (NSCLC) Chinese Patients Who HaveNot Experienced Disease Progression or Unacceptable Toxicity During Front Line Standard Platinum-Based Chemotherapy

CompletedPH IVAstraZenecan=2962011

A Randomized/Open Label/Parallel Group/Multicenter/Phase IV Study to Assess Safety/Tolerability/Efficacy of Oral Gefitinib 250 mg Versus IV Docetaxel 60 mg/m2 in Patients With Locally Advanced or Metastatic NSCL Cancer of Adenocarcinoma Histology Previous Treated With One Platinum Base Chemotherapy

TerminatedPH IVAstraZenecan=142009

Recent completions

Trials that read out recently, adding to the completed evidence base.

CompletedPH IIIYuhan Corporationn=3932026

CompletedPH IIIAstraZenecan=6742025

APPLE Trial: Feasibility and Activity of AZD9291 (Osimertinib) Treatment on Positive PLasma T790M in EGFR Mutant NSCLC Patients

CompletedPH IIEuropean Organisation for Research and Treatment of Cancer - EORTCn=1562025

A Randomized, Open-label, Controlled, Multi-Center Phase II/III Study to Assess the Efficacy and Safety of AZD3759 vs. a Standard of Care EGFR TKI, as First Line Treatment to EGFR Mutation Positive Advanced NSCLC With CNS Metastases

CompletedPH II/IIIAlpha Biopharma (Jiangsu) Co., Ltd.n=4922022

Exploratory Study of Drug Sensitivity Prediction Software (IRCR-DReSS) With Patient-derived Tumor Cells of Metastatic Gastric Cancer

CompletedPH IISamsung Medical Centern=662021

A Phase Ib/II Multicenter, Randomized, Open Label Trial to Compare Tepotinib (MSC2156119J) Combined With Gefitinib Versus Chemotherapy as Second-Line Treatment in Subjects With MET Positive, Locally Advanced or Metastatic NSCLC Harboring EGFR Mutation and Having Acquired Resistance to Prior EGFR-TKI Therapy (INSIGHT)

CompletedPH I/IIMerck KGaA, Darmstadt, Germanyn=882021

Research activity

10 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Publications over time

20042020

Most influential

Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma.

The New England journal of medicine · 2009 · 6,372 cites

Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer.

The New England journal of medicine · 2018 · 4,173 cites

Overall Survival with Osimertinib in Untreated, <i>EGFR</i>-Mutated Advanced NSCLC.

The New England journal of medicine · 2020 · 2,267 cites

Clinical features and outcome of patients with non-small-cell lung cancer who harbor EML4-ALK.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2009 · 1,412 cites

Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2004 · 1,188 cites

Epidermal growth factor receptor gene and protein and gefitinib sensitivity in non-small-cell lung cancer.

Journal of the National Cancer Institute · 2005 · 1,173 cites

Related diseases

2 conditions

Regulator-approved indications and conditions co-mentioned with this drug across the research literature. Number shows shared papers.

Active research areas

Carcinoma, Non-Small-Cell Lung6 Lung Neoplasms6

Related drugs

7 matches

Drugs sharing diseases, protein targets and literature with this one. Ranked by graph evidence (shared targets + diseases weighted above co-mentions).

Erlotinib Hydrochloride

Acts on the same molecular target as Gefitinib, with 4 overlapping disease areas.

Shared target4 shared diseases4 shared papers

Osimertinib

Acts on the same molecular target as Gefitinib, with 2 overlapping disease areas.

Shared target2 shared diseases2 shared papers

Cisplatin

Studied across 4 of the same disease areas as Gefitinib in the shared literature.

4 shared diseases1 shared paper

Gemcitabine

Studied across 4 of the same disease areas as Gefitinib in the shared literature.

4 shared diseases1 shared paper

Carboplatin

Studied across 3 of the same disease areas as Gefitinib in the shared literature.

3 shared diseases1 shared paper

Deoxycytidine

Studied across 3 of the same disease areas as Gefitinib in the shared literature.

3 shared diseases1 shared paper

Paclitaxel

Studied across 3 of the same disease areas as Gefitinib in the shared literature.

3 shared diseases1 shared paper

References & data sources

RxNorm (U.S. National Library of Medicine) — drug identity
ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
Europe PMC — research literature
ClinicalTrials.gov — clinical trials
Regulatory event sources are credited in the Regulatory Timeline above.