Drug · Small Molecule

Gefitinib

CI-DRUG-00000270Explore in graph →NCIt C1855 CHEMBL939 CIViC Approved

Regulatory

Approvals (10)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

openfdaRegulatory1 approval record · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
US FDA	Lung Non-Small Cell Carcinoma	IRESSA is indicated for the first-line 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 [see Clinical Studies (14) ] . Limitation of Use: Safety and efficacy of IRESSA have not been established in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations [see Clinical Studies (14) ] . IRESSA is a tyrosine kinase inhibitor indicated for the first-line 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. (1) Limitation of Use: Safety and efficacy of IRESSA have not been established in patients whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations. (1)	approved	Jul 13, 2015	openfda

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 13 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	9	1	49	259	10	CA, EU, US	Dec 17, 2003	1999-09
Malignant Lung Neoplasm	Approved	Phase 4	5	0	38	124	3	EU, US	Jun 24, 2009	1999-09
Malignant Bladder Neoplasm	Phase3	Phase 3	0	0	1	4	0	—	—	2001-02
Malignant Breast Neoplasm	Phase3	Phase 3	0	0	1	20	0

Curated evidence

Clinical evidence (186)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 186 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
EGFR Fusion2
Gefitinib	Childhood Ependymoma

Clinical trials

Trials with this intervention (265)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 151–200 of 265 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT00955695	Radiation Therapy to the Brain or Observation in Preventing Brain Metastases in Patients With Advanced Non-Small Cell Lung Cancer	unknown	Phase 3	242	National Cancer Center, KoreaOTHER_GOV	0	Aug 2, 2013	clinicaltrials
NCT00014170	Gefitinib in Treating Patients With Newly Diagnosed Glioblastoma Multiforme	completed

Molecule

Record

Kind: Small Molecule
Mechanism: Epidermal growth factor receptor erbB1 inhibitor
Targets: 1 gene
UNII: S65743JHBS
Aliases: 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline, APO-GEFITINIB, AURO-GEFITINIB, EUGIA-GEFITINIB, Gefitinib, Gefitinib mylan, Iressa, IRESSA, JAMP GEFITINIB, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholin) Propoxy]-4-quinazolinamine, NAT-GEFITINIB, NSC-759856, SANDOZ GEFITINIB, Tykessa, ZD 1839, ZD-1839, ZD1839

Data updated 16 hours agoSource updated unknown

Identifiers

Codes (18)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EB01	GEFITINIB
ATC (WHO)	L01XE02	Antineoplastic agents

EGFR E746_T751>I4
Gefitinib	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	2	accepted	EID4209 Mutational profiling was performed on EGFR exons 18-24 from a group of 10 retrospectively chosen lung cancer patients who had shown partial response or clinical imporvement in response to gefitinib. O… (full text at CIViC) PMID 15329413 · Pao et al., 2004 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	—	submitted	EID2522 In a phase 3 clinical trial of Japanese NSCLC patients with EGFR mutations (n=230), patients treated with gefitinib were associated with improved progression free survival (10.8 months vs 5.4 months, … (full text at CIViC) PMID 20573926 · Maemondo et al., 2010 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	—	submitted	EID2523 In a phase 3 clinical trial of Japanese NSCLC patients with EGFR mutations (n=177), patients treated with gefitinib were associated with improved progression free survival (9.2 months vs 6.3 months, H… (full text at CIViC) PMID 20022809 · Mitsudomi et al., 2010 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	—	rejected	EID2526 In an in vitro study using PC9 cells (EGFR exon 19 deletion), inhibition of cell viability was used as an assay to determine sensitivity to EGFR tyrosine kinase inhibitors. PC9 cells demonstrated an i… (full text at CIViC) PMID 24893891 · Cross et al., 2014 · Open in CIViC	civic

EGFR Exon 19 Deletion2
Gefitinib	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID2519 In a phase 3 clinical trial of Korean, never-smoker, lung adenocarcinoma patients, a subset of patients with EGFR mutations (n=42) treated with gefitinib were associated with improved overall response… (full text at CIViC) PMID 22370314 · Han et al., 2012 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID6184 A Japanese Phase III clinical study assessed the noninferiority of gefitinib in comparison to erlotinib in 561 patients with postoperative or recurrent stage IIIB/IV lung adenocarcinoma. Patients were… (full text at CIViC) PMID 27022112 · Urata et al., 2016 · Open in CIViC	civic

EGFR L858R3
Gefitinib	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID2634 In a phase 3 clinical trial of Korean, never-smoker, lung adenocarcinoma patients, a subset of patients with EGFR mutations (n=42) treated with gefitinib were associated with improved overall response… (full text at CIViC) PMID 22370314 · Han et al., 2012 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	2	accepted	EID6183 In a Japanese Phase III clinical trial, noninferiority of Gefitinib as compared to Erlotinib was assessed in 561 postoperative recurrent or stage IIIb/VI patients who had undergone prior chemotherapy … (full text at CIViC) PMID 27022112 · Urata et al., 2016 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	1	accepted	EID2624 Mutational profiling was performed on EGFR exons 18-24 from a group of 10 retrospectively chosen patients who had shown partial response or clinical improvement in response to gefitinib. Of 7 tumors w… (full text at CIViC) PMID 15329413 · Pao et al., 2004 · Open in CIViC	civic

PIK3CA E545K2
Gefitinib	Lung Adenocarcinoma	Predictive	D	Supports Resistance	2	accepted	EID1171 HCC827 cell lines harboring activated PI3K (HCC827 p110α E545K cells) were more resistant to gefitinib in vitro (IC50, 1 μM) compared with those harboring GFP alone (IC50, 0.01 μM). The presence of p1… (full text at CIViC) PMID 16906227 · Engelman et al., 2006 · Open in CIViC	civic
Erlotinib + GefitinibSubstitutes	Lung Adenocarcinoma	Predictive	C	Supports Resistance	2	accepted	EID1670 48 tumor samples from 41 patients with EGFR mutant lung adenocarcinoma that were resistant to tyrosine kinase inhibition underwent next generation sequencing (AmpliSeq Cancer Hotspot Panel (v2) failed… (full text at CIViC) PMID 27304188 · Belchis et al., 2016 · Open in CIViC	civic

EGFR Amplification3
Erlotinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID5924 The result of the analysis found that EGFR gene copy number was associated with increased OS and PFS, supporting the idea that EGFR gene copy number is a biomarker for response to EGFR-TKI therapy in … (full text at CIViC) PMID 20826716 · Dahabreh et al., 2011 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID5925 Among TKI-treated patients, increased EGFR gene copy number appears to be associated with improved survival outcomes. PMID 27664271 · Zhang et al., 2017 · Open in CIViC	civic
Erlotinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Does Not Support Sensitivity Response	2	accepted	EID977 In 290 patients with advanced NSCLC, 177 of which were treated with EGFR TKI (erlotinib or gefitinib). EGFR amplification (Multiplex ligation-dependent probe amplification; MLPA) and Mutation (PCR) we… (full text at CIViC) PMID 26722081 · Fiala et al., 2016 · Open in CIViC	civic