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.

health-canada-dpdRegulatory10 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as JAMP GEFITINIB (DIN 02500663) under ATC L01EB01 GEFITINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Dec 23, 2020	health-canada-dpd
CA Health Canada	—	Marketed in Canada as NAT-GEFITINIB (DIN 02491796) under ATC L01EB01 GEFITINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Dormantsince Mar 1, 2026	Nov 13, 2019	health-canada-dpd
CA Health Canada	—	Marketed in Canada as SANDOZ GEFITINIB (DIN 02487748) under ATC L01EB01 GEFITINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Market

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 19 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 101–150 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 L858R2
Erlotinib + Gefitinib

Clinical trials

Trials with this intervention (265)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 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
NCT07829926	Lenvatinib Plus Tislelizumab With or Without Gefitinib for Advanced Liver Cancer(LENTIG-HCC)	not yet recruiting	Phase 2	120	First Affiliated Hospital of Wenzhou Medical UniversityOTHER	0	Sep 21, 2026	clinicaltrials
NCT03040973	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

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 22 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 Exon 19 Deletion + EGFR L858R3
Erlotinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID4759 In a study of 1261 non-small cell lung cancer patients, 49.8% of the analyzed tumors had EGFR mutations including deletions in exon 19 (n=258), L858R (n=260), T790M (n=6) and insertions or duplication… (full text at CIViC) PMID 21531810 · Wu et al., 2011 · Open in CIViC	civic
Gefitinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	A	Supports Sensitivity Response	4	accepted	EID11241 In this phase-IV, open-label, single-arm study, 106 patients with NSCLC and EGFR mutations including exon 19 deletion and exon 21 L858R point mutations were administered 250 mg daily doses of gefitini… (full text at CIViC) PMID 24263064 · Douillard et al., 2014 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	4	accepted	EID2156 A phase 2 study of 120 stage IIIB-IV lung adenocarcinoma patients reported improved progression free survival in patients with EGFR mutation (defined as exon 19 deletion or exon 21 mutation) when trea… (full text at CIViC) PMID 24755888 · Yu et al., 2014 · Open in CIViC	civic

EGFR Mutation7
Gefitinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	5	accepted	EID1937 This open label Phase 3 Trial performed across 36 centers in Japan (WJTOG3405) assessed patients with postoperative recurrent or stage IIIB/IV NSCLC and activating EGFR mutations (Exon 19 deletion and… (full text at CIViC) PMID 20022809 · Mitsudomi et al., 2010 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	5	accepted	EID2148 In a phase 3 clinical trial of East Asian advanced pulmonary adenocarcinoma patients, a subset of patients with EGFR mutations (n=261) treated with gefitinib were associated with improved response (HR… (full text at CIViC) PMID 19692680 · Mok et al., 2009 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	accepted	EID2559 Mutational profiling was performed on EGFR exons 18-24 from a group of 10 retrospectively chosen patients who had shown partial response or clinical imporvement in response to gefitinib, and in 8 pati… (full text at CIViC) PMID 15329413 · Pao et al., 2004 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	accepted	EID3016 In a phase 3 clinical trial of non-small cell lung cancer (NSCLC) patients, a subset of patients with EGFR mutations (n=44) treated with gefitinib were associated with improved progression free surviv… (full text at CIViC) PMID 20038723 · Douillard et al., 2010 · Open in CIViC	civic
Afatinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Resistance	3	submitted	EID6465 Three major drug resistance mutations, namely L718Q, L844V, and C797S were identified in EGFR and caused resistance to both WZ4002 and CO-1686. In contrast, only EGFR C797S caused AZD9291 resistance.… (full text at CIViC) PMID 25948633 · Ercan et al., 2015 · Open in CIViC	civic
Erlotinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID2053 In a retrospective study, 166 non-small cell lung cancer (NSCLC) patients that tended to have selected characteristics known to be predictive for TKI sensitivity (i.e. women, never smokers, and patien… (full text at CIViC) PMID 21258250 · Ludovini et al., 2011 · Open in CIViC	civic
Gefitinib + PemetrexedCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	submitted	EID7650 A phase 2 study was conducted to compare treatment with pemetrexed and gefinitib (P+G) versus gefinitib monotherapy for a population of 195 East Asian non-squamous NSCLC patients with EGFR mutations (… (full text at CIViC) PMID 31605797 · Yang et al., 2020 · Open in CIViC	civic

EGFR R831H3
Gefitinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	—	submitted	EID2618 EGFR belongs to a family of receptor tyrosine kinases that includes EGFR/erbB-1, Her2/erbB-2, Her3/erbB-3, and Her4/erbB-4. Ligand binding causes receptor homo- or hetero-dimerization, leading to acti… (full text at CIViC) PMID 20966921 · Pao et al., 2010 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	—	submitted	EID2619 EGFR belongs to a family of receptor tyrosine kinases that includes EGFR/erbB-1, Her2/erbB-2, Her3/erbB-3, and Her4/erbB-4. PMID 15870435 · Cappuzzo et al., 2005 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	—	submitted	EID2620 Mutations in exon 19 or exon 21 of EGFR were found at higher frequencies in of tumors from patients who had a clinically significant response to gefitinib treatment compared with patients who had no c… (full text at CIViC) PMID 15118072 · Green, 2004 · Open in CIViC	civic

EGFR Rare Exon 18-21 Mutation2
Erlotinib + GefitinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID4755 In a cohort of NSCLC patients treated with tyrosine kinase inhibitors erlotinib or gefitinib, 61 patients with uncommon mutations of unknown clinical significance (UMUCS) in EGFR exons 18-21 responded… (full text at CIViC) PMID 21531810 · Wu et al., 2011 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Does Not Support Sensitivity Response	2	accepted	EID4762 In a cohort of NSCLC patients tested for mutation in EGFR exons 18-21 a subset had uncommon mutations of unknown clinical significance (UMUCS). The most commonly occurring UMUCS were G719 and L861 mut… (full text at CIViC) PMID 21531810 · Wu et al., 2011 · Open in CIViC	civic

EGFR S768I3
Gefitinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	—	submitted	EID2614 In response to gefitinib treatment, lung adenocarcinoma patients with somatic EGFR S768I mutation had longer median progression-free survival when there was a concomitant L858R mutation or in-frame de… (full text at CIViC) PMID 19060236 · Wu et al., 2008 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	—	submitted	EID2615 Partial response to gefitinib was achieved in two non-small cell lung cancer patients having a S768I mutation with concomitant G719C mutation. PMID 15998907 · Takano et al., 2005 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	—	submitted	EID2616 In vitro studies showed that cells with S768I mutation had moderate sensitivity (IC50=90-315nM) to gefitinib , in comparison to the del747-753insS (IC50= 7nM) or L858R (IC50=12-20nM) mutations that co… (full text at CIViC) PMID 16205628 · Chen et al., 2006 · Open in CIViC	civic