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.

emaRegulatory2 approval records · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
EU EMA	Lung Non-Small Cell Carcinoma	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.	withdrawnsince Sep 27, 2024	Sep 27, 2018	ema
EU EMA	Lung Non-Small Cell Carcinoma	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.	approved	Jun 24, 2009	ema

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 18 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 151–186 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
PBK OVEREXPRESSION1
Gefitinib	Lung Non-Small Cell Carcinoma

Clinical trials

Trials with this intervention (265)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 201–250 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
NCT01502202	Intercalated Administration of PamCis With Gefitinib or Placebo as First Line Lung Adenocarcinoma in Never Smokers	unknown	Phase 2	162	National Cancer Center, KoreaOTHER_GOV	1	Jun 20, 2012	clinicaltrials
NCT00478049	Iressa as Second Line Therapy in Advanced NSCLC-Asia(ISTANA)	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 21 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

SMO Amplification2
Gefitinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Resistance	3	submitted	EID2945 Activation of the Hh pathway was found in both models of EGFR-mutated and EGFR-WT NSCLC cell line resistant to EGFR-TKIs. In EGFR-WT NSCLC cell lines resistant to EGFR inhibitors, the combined inhibit… (full text at CIViC) PMID 26124204 · Della Corte et al., 2015 · Open in CIViC	civic
Gefitinib + SonidegibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID2946 Activation of the Hh pathway was found in both models of EGFR-mutated and EGFR-WT NSCLC cell line resistant to EGFR-TKIs. In EGFR-WT NSCLC cell lines resistant to EGFR inhibitors, the combined inhibit… (full text at CIViC) PMID 26124204 · Della Corte et al., 2015 · Open in CIViC	civic

BRAF V600E2
Gefitinib + VemurafenibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID10328 Five colorectal cancer (CRC) cell lines with BRAF V600E mutation were resistant to treatment with the BRAF inhibitor vemurafenib. An RNAi screen in the WiDr cell line (a V600E CRC line) identified EGF… (full text at CIViC) PMID 22281684 · Prahallad et al., 2012 · Open in CIViC	civic
Cetuximab + Gefitinib + VemurafenibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID1408 5 of 7 colorectal cancer (CRC) cell lines with BRAF V600E mutation were resistant to treatment with the BRAF inhibitor vemurafenib. An RNAi screen in the WiDr cell line (a V600E CRC line) identified E… (full text at CIViC) PMID 22281684 · Prahallad et al., 2012 · Open in CIViC	civic

KRAS G12C2
Erlotinib + GefitinibSubstitutes	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	B	Supports Resistance	3	accepted	EID1216 In a study of 448 metastatic colorectal cancer patients treated with EGFR-TKIs and tested for EGFR and KRAS mutations, 69 tested positive for KRAS mutations. In 38 EGFR wildtype patients treated with … (full text at CIViC) PMID 23313110 · Fiala et al., 2013 · Open in CIViC	civic
Gefitinib	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	2	accepted	EID2257 In recurrent lung cancer patients treated with the epidermal growth factor receptor tyrosine kinase inhibitor gefitinib, patients with KRAS mutations had a lower frequency of partial response (PR) and… (full text at CIViC) PMID 17409929 · Endoh et al., 2006 · Open in CIViC	civic

EGFR T790M2
Gefitinib + Multikinase Inhibitor AEE788Sequential	Malignant Lung Neoplasm	Predictive	D	Supports Resistance	5	accepted	EID642 Lung cancers can accumulate activating mutations in oncogenes such as EGFR. The common L858R EGFR mutation has been shown previously to be sensitive to small molecular tyrosine kinase inhibitors (ie. … (full text at CIViC) PMID 18227510 · Yun et al., 2008 · Open in CIViC	civic
Erlotinib + Gefitinib + Multikinase Inhibitor AEE788Substitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID3810 Experimental - EGFR T790M mutation has been associated with resistance to first generation EGFR tyrosine kinase inhibitors, including erlotinib and gefitinib. In an in vitro study, Ba/F3 cells stably … (full text at CIViC) PMID 19147750 · Kancha et al., 2009 · Open in CIViC	civic

KRAS G12D6
Gefitinib	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	2	accepted	EID2240 In recurrent lung cancer patients treated with the epidermal growth factor receptor tyrosine kinase inhibitor gefitinib, patients with KRAS mutations had a lower frequency of partial response (PR) and… (full text at CIViC) PMID 17409929 · Endoh et al., 2006 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	—	submitted	EID2241 In locally advanced or metastic (stage IIIB or IV) non-small cell lung cancer patients with KRAS mutations, those treated with the epidermal growth factor receptor tyrosine kinase inhibitor erlotinib … (full text at CIViC) PMID 16043828 · Eberhard et al., 2005 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	—	submitted	EID2243 In lung cancer patients, KRAS mutations were associated with reduced overall survival compared to patients with wildtype KRAS status (n=195, P=0.009, univariate analysis; risk ratio:1.8, 95% CI:1.1-3.… (full text at CIViC) PMID 10580029 · Nelson et al., 1999 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	—	submitted	EID2244 In stage II non-small cell lung cancer patients, KRAS mutations were associated with reduced overall survival compared to wildtype KRAS (13mo vs. 38mo, P=0.03). In patients with surgically resected st… (full text at CIViC) PMID 10080613 · Graziano et al., 1999 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	B	Supports Resistance	—	submitted	EID2245 Lung adenocarcinoma patients with KRAS mutations experienced reduced disease-free survival (63% vs. 44% , P=0.038) and overall survival (63% vs. n=32% , P=0.002) compared to wildtype KRAS patients. … (full text at CIViC) PMID 2199829 · Slebos et al., 1990 · Open in CIViC	civic
〃	Malignant Lung Neoplasm	Predictive	C	Supports Resistance	—	rejected	EID2246 KRAS mutations have also been observed in biliary tract, bladder, breast, cervix, colon, endometrial, kidney, liver, melanoma, myeloid leukemia, ovarian, pancreatic, and thyroid cancer. PMID 17384584 · Schubbert et al., 2007 · Open in CIViC	civic