Gefitinib

Summary

Gefitinib (CHEMBL939) is an approved small-molecule antineoplastic agent (ATC L01EB01) targeting EGFR; indicated across 51 conditions including non-small cell lung carcinoma and neoplasm; with CIViC clinical evidence for 130 variant-indication associations (e.g. EGFR L858R OR EGFR Exon 19 Deletion in lung non-small cell carcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EB01
• Targets: 1 (EGFR)
• Indications: 51 conditions
• Clinical trials: 295
• Precision-oncology evidence (CIViC): 130 variant–indication associations
• Chemistry: 446.9 Da · C22H24ClFN4O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL939
Name	Gefitinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	123631
ChEBI	CHEBI:49668
ATC	L01EB01
Molecular formula	C22H24ClFN4O3
Molecular weight	446.9
InChIKey	XGALLCVXEZPNRQ-UHFFFAOYSA-N

SMILES: COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

IUPAC name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine

ChEBI definition: A member of the class of quinazolines that is quinazoline which is substituted by a (3-chloro-4-fluorophenyl)nitrilo group, 3-(morpholin-4-yl)propoxy group and a methoxy group at positions 4,6 and 7, respectively. An EGFR kinase inhibitor used for the treatment of non-small cell lung cancer.

Pharmacological roles (ChEBI): antineoplastic agent, epidermal growth factor receptor antagonist.

Also known as: Gefitinib, Gefitinib mylan, Iressa, NSC-759856, ZD-1839, ZD1839, gefitinib, gefitnib, gifitinib, SID29215403, GEFITINIB, SID103905343

Patent coverage: 31,132 distinct patent families (117,814 SureChEMBL compound mentions), from 6 matched compound structure(s). One matched structure accounts for 114,569 (97%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
EGFR	epidermal growth factor receptor	Inhibition	7.23	17.5%	P00533

Broader ChEMBL bioactivity targets: 107 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase SBK1, Nucleotide-binding oligomerization domain-containing protein 1, Microtubule-associated protein tau, Nucleotide-binding oligomerization domain-containing protein 2, ATP-binding cassette sub-family C member 4, Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor-interacting serine/threonine-protein kinase 3, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase ABL1.

Bioactivity

ChEMBL activities: 559 potent at pChembl ≥ 5 of 585 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_13297481
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_13380887
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_14574803
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_23250047
EGFR	9.82	IC50	0.15	nM	CHEMBL_ACT_17989470
EGFR	9.77	IC50	0.17	nM	CHEMBL_ACT_17989481
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_13297507
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_13380877
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_14574810
EGFR	9.6	IC50	0.25	nM	CHEMBL_ACT_26199037
EGFR	9.49	IC50	0.32	nM	CHEMBL_ACT_23250044
EGFR	9.4	Ki	0.4	nM	CHEMBL_ACT_26023189
EGFR	9.4	Ki	0.4	nM	CHEMBL_ACT_3447717
EGFR	9.35	IC50	0.45	nM	CHEMBL_ACT_14974602
EGFR	9.35	IC50	0.45	nM	CHEMBL_ACT_14983535
EGFR	9.34	IC50	0.46	nM	CHEMBL_ACT_27322262
EGFR	9.33	IC50	0.47	nM	CHEMBL_ACT_19168555
EGFR	9.3	IC50	0.5	nM	CHEMBL_ACT_22844317
EGFR	9.29	IC50	0.51	nM	CHEMBL_ACT_16612196
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_2898900
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_7588273
EGFR	9.27	Kd	0.54	nM	CHEMBL_ACT_2898710
EGFR	9.27	Kd	0.54	nM	CHEMBL_ACT_7588268
EGFR	9.24	Kd	0.57	nM	CHEMBL_ACT_2898824
EGFR	9.24	Kd	0.57	nM	CHEMBL_ACT_2898862
EGFR	9.24	Kd	0.57	nM	CHEMBL_ACT_7588271
EGFR	9.24	Kd	0.57	nM	CHEMBL_ACT_7588272
EGFR	9.23	IC50	0.58	nM	CHEMBL_ACT_16655518
EGFR	9.22	IC50	0.6	nM	CHEMBL_ACT_13453602
EGFR	9.2	IC50	0.64	nM	CHEMBL_ACT_16655524

Target pathways

Aggregated over 1 target gene(s): EGFR.

Top Reactome pathways

37 total, by targets touching each:

Pathway	Targets	Genes
Signaling by ERBB2	1	EGFR
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	1	EGFR
Signaling by ERBB4	1	EGFR
SHC1 events in ERBB2 signaling	1	EGFR
PLCG1 events in ERBB2 signaling	1	EGFR
PIP3 activates AKT signaling	1	EGFR
Signaling by EGFR	1	EGFR
GRB2 events in EGFR signaling	1	EGFR
GAB1 signalosome	1	EGFR
SHC1 events in EGFR signaling	1	EGFR
EGFR downregulation	1	EGFR
GRB2 events in ERBB2 signaling	1	EGFR
PI3K events in ERBB2 signaling	1	EGFR
EGFR interacts with phospholipase C-gamma	1	EGFR
EGFR Transactivation by Gastrin	1	EGFR
Constitutive Signaling by Aberrant PI3K in Cancer	1	EGFR
Signal transduction by L1	1	EGFR
Constitutive Signaling by EGFRvIII	1	EGFR
Inhibition of Signaling by Overexpressed EGFR	1	EGFR
RAF/MAP kinase cascade	1	EGFR
ERBB2 Regulates Cell Motility	1	EGFR
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	EGFR
ERBB2 Activates PTK6 Signaling	1	EGFR
Cargo recognition for clathrin-mediated endocytosis	1	EGFR
Clathrin-mediated endocytosis	1	EGFR
PTK6 promotes HIF1A stabilization	1	EGFR
Downregulation of ERBB2 signaling	1	EGFR
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors	1	EGFR
Extra-nuclear estrogen signaling	1	EGFR
NOTCH3 Activation and Transmission of Signal to the Nucleus	1	EGFR

Dominant GO biological processes

GO term	Targets
cell morphogenesis	1
ossification	1
embryonic placenta development	1
positive regulation of protein phosphorylation	1
hair follicle development	1
ubiquitin-dependent protein catabolic process	1
signal transduction	1
cell surface receptor signaling pathway	1
epidermal growth factor receptor signaling pathway	1
salivary gland morphogenesis	1
learning or memory	1
positive regulation of cell population proliferation	1
gene expression	1
protein ubiquitination	1
cerebral cortex cell migration	1

Indications & clinical

Indications

51 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
non-small cell lung carcinoma	4	MONDO:0005233	EFO:0003060
neoplasm	4	MONDO:0005070	EFO:0000616
upper aerodigestive tract neoplasm	3	MONDO:0005398	EFO:0004284
lung carcinoma	3	MONDO:0005138	EFO:0001071
squamous cell carcinoma	3	MONDO:0005096	EFO:0000707
head and neck squamous cell carcinoma	3	MONDO:0010150	EFO:0000181
squamous cell lung carcinoma	3	MONDO:0005097	EFO:0000708
breast neoplasm	3	MONDO:0021100	EFO:0003869
head and neck cancer	3	MONDO:0005627	EFO:0006859
lung adenocarcinoma	3	MONDO:0005061	EFO:0000571
minimally invasive lung adenocarcinoma	3	MONDO:0004991	EFO:0000308
lung neoplasm	3	MONDO:0021117	MONDO:0008903
acute myeloid leukemia	2	MONDO:0018874	EFO:0000222
mesothelioma	2	MONDO:0005065	EFO:0000588
gliosarcoma	2	MONDO:0016681	EFO:1001465
tumor of uterus	2	MONDO:0021353	EFO:0003859
gastric carcinoma	2	MONDO:0004950	EFO:0000178
germ cell tumor	2	MONDO:0005040	EFO:0000514
glioblastoma	2	MONDO:0018177	EFO:0000519
neuroblastoma	2	MONDO:0005072	EFO:0000621
sarcoma	2	MONDO:0005089	EFO:0000691
small cell lung carcinoma	2	MONDO:0008433	EFO:0000702
gastric neoplasm	2	MONDO:0021085	EFO:0003897
male breast carcinoma	2	MONDO:0005628	EFO:0006861
fallopian tube carcinoma	2	MONDO:0006206	EFO:1000251
peritoneal neoplasm	2	MONDO:0006901	EFO:1001100
central nervous system neoplasm	2	MONDO:0006130	EFO:1000158
fallopian tube neoplasm	2	MONDO:0021092	MONDO:0002158
kidney cancer	2	MONDO:0002367	MONDO:0002367
skin neoplasm	2	MONDO:0002531	MONDO:0002898
salivary gland cancer	2	MONDO:0004669	MONDO:0004669
ovarian cancer	2	MONDO:0008170	MONDO:0008170
bile duct carcinoma	2	MONDO:0005496	EFO:0005540
gallbladder neoplasm	2	MONDO:0021253	MONDO:0005411
colorectal neoplasm	2	MONDO:0005335	MONDO:0005575
metastatic prostate carcinoma	1	MONDO:0004956	EFO:0000196
renal cell carcinoma	1	MONDO:0005086	EFO:0000681
exocrine pancreatic carcinoma	1	MONDO:0005192	EFO:0002618
carcinoma	1	MONDO:0004993	EFO:0000313
nasopharyngeal carcinoma	1	MONDO:0015459	MONDO:0015459

11 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 295.

Phase distribution

Phase	Trials
PHASE2	156
PHASE3	48
PHASE1	31
PHASE1/PHASE2	30
Not specified	17
PHASE4	6
PHASE2/PHASE3	6
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00536107	PHASE4	TERMINATED	Study to Assess Safety/Tolerability/Efficacy of Gefitinib Versus Docetaxel in Locally Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC)
NCT00608868	PHASE4	COMPLETED	SELINE: Second-Line Iressa Phase IV Study in NSCLC Patients
NCT00770588	PHASE4	COMPLETED	Assess the Efficacy, Safety and Tolerability of Gefitinib (Iressa® 250mg) as Maintenance Therapy in Locally Advanced or Metastatic (Stage IIIB/IV) Non Small Cell Lung Cancer (NSCLC)
NCT01203917	PHASE4	COMPLETED	Efficacy, Safety, Tolerability of Gefitinib as 1st Line in Caucasian Patients With EGFR Mutation Positive Advanced NSCLC
NCT02031601	PHASE4	UNKNOWN	Intercalated Combination of Chemotherapy and Tyrosine Kinase Inhibitors as First-line Treatment for Patients With Non-Small-Cell Lung Cancer
NCT02299765	PHASE4	TERMINATED	Intercalating and Maintenance Gefitinib in Combination With Chemotherapy for Advanced EGFR-mutant NSCLC
NCT02411448	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RELAY)
NCT03787992	PHASE3	ACTIVE_NOT_RECRUITING	Alflutinib Mesylate Versus Gefitinib in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer （FLAG）
NCT03866499	PHASE3	ACTIVE_NOT_RECRUITING	A Study of BPI-7711 Capsule in Non-small Cell Lung Cancer Patients
NCT04143607	PHASE3	ACTIVE_NOT_RECRUITING	ASK120067 Versus Gefitinib as First-line Treatment for EGFRm Locally Advanced or Metastatic NSCLC
NCT00006048	PHASE3	UNKNOWN	ZD 1839 Plus Combination Chemotherapy in Treating Patients With Non-Small Cell Lung Cancer
NCT00006049	PHASE3	UNKNOWN	ZD 1839 Plus Chemotherapy in Treating Patients With Non-Small Cell Lung Cancer
NCT00020709	PHASE3	COMPLETED	Combination Chemotherapy and Radiation Therapy With or Without Gefitinib in Treating Patients With Stage III Non-Small Cell Lung Cancer That Cannot Be Removed By Surgery
NCT00034879	PHASE3	COMPLETED	Iressa Expanded Access Program (EAP)
NCT00049543	PHASE3	COMPLETED	Gefitinib in Treating Patients With Stage IB, II, or IIIA Non-small Cell Lung Cancer That Was Completely Removed by Surgery
NCT00076388	PHASE3	COMPLETED	Iressa Versus Docetaxel (Taxotere)
NCT00080340	PHASE3	COMPLETED	Study of TLK286 (Telcyta) vs. Gefitinib in Locally Advanced or Metastatic Non-Small Cell Lung Cancer
NCT00088907	PHASE3	TERMINATED	Phase III Trial Of Docetaxel Versus Docetaxel Plus ZD1839 In Head And Neck Cancer
NCT00090675	PHASE3	WITHDRAWN	Maintenance ZD1839 (IRESSA®) Following Completion of Front Line, Platinum-Based, Double Chemotherapy in Subjects With Advanced or Metastatic Non-Small Cell Lung Cancer
NCT00091156	PHASE3	TERMINATED	Gefitinib After Chemotherapy in Treating Patients With Stage IIIB or Stage IV Non-Small Cell Lung Cancer
NCT00206219	PHASE3	COMPLETED	Head and Neck Phase III Iressa Versus Methotrexate Refractory: Iressa Versus Methotrexate (IMEX)
NCT00234429	PHASE2/PHASE3	COMPLETED	A Phase 2 Study of Tomudex & Iressa as Second Line Chemotherapy in Subjects With Colorectal Carcinoma
NCT00234468	PHASE3	TERMINATED	Iressa vs Placebo as Maintenance Therapy in Locally Advanced NSCLC
NCT00242801	PHASE3	COMPLETED	Iressa vs Best Supportive Care - 2nd/3rd Line Survival Study
NCT00259064	PHASE2/PHASE3	COMPLETED	Iressa v BSC (Best Supportive Care) in First Line NSCLC
NCT00322452	PHASE3	COMPLETED	First Line IRESSA™ Versus Carboplatin/Paclitaxel in Asia
NCT00352079	PHASE3	TERMINATED	BCG With or Without Gefitinib in Treating Patients With High-Risk Bladder Cancer
NCT00357734	PHASE3	COMPLETED	Iressa Follow-up Trial
NCT00455936	PHASE3	COMPLETED	First-line Gefitinib Versus Chemotherapy for Lung Adenocarcinoma in Never Smoker
NCT00478049	PHASE3	COMPLETED	Iressa as Second Line Therapy in Advanced NSCLC-Asia
NCT00635973	PHASE3	COMPLETED	Open-Label Extension of Other SZ1839 (Iressa) Trials
NCT00807066	PHASE3	COMPLETED	Randomized Gefitinib Trial
NCT00955695	PHASE3	UNKNOWN	Radiation Therapy to the Brain or Observation in Preventing Brain Metastases in Patients With Advanced Non-Small Cell Lung Cancer
NCT01017874	PHASE3	COMPLETED	A Study of Alimta/Cisplatin/Gefitinib for Asian Non-smoking Participants With Non Small Cell Lung Cancer
NCT01024413	PHASE3	COMPLETED	Phase III Trial to Evaluate the Elortinib vs Gefitinib in Advanced NSCLC With EGFR Exon 19 or 21 Mutations
NCT01040780	PHASE3	COMPLETED	Safety and Efficacy Study of Icotinb in Non-small Cell Lung Cancer (NSCLC) Patients
NCT01066195	PHASE3	UNKNOWN	Pemetrexed (ALIMTA) and Gefitinib (IRESSA®) in Never-Smoker and Adenocarcinoma Patients With Non-Small Cell Lung Cancer Previously Treated With Platinum-Based Chemotherapy
NCT01158170	PHASE3	UNKNOWN	Prophylactic Cranial Irradiation in Erlotinib/Gefitinib-responders With Non-small Cell Lung Cancer (NSCLC) (RT1001)
NCT01404260	PHASE3	COMPLETED	Intercalating and Maintenance Use of Iressa Versus Chemotherapy in Selected Advanced Non Small Cell Lung Cancer
NCT01405079	PHASE3	UNKNOWN	Gefitinib Versus Vinorelbine/Platinum as Adjuvant Treatment in Stage II-IIIA(N1-N2) NSCLC With EGFR Mutation

Clinical evidence (CIViC)

Variant × indication × effect (130 predictive associations from 183 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR L858R OR EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC A	EID11241 +1
SEC61G::EGFR Fusion	Childhood Ependymoma	Sensitivity/Response	Gefitinib	CIViC A	EID10933
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID1665 +3
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID1937 +3
EGFR Amplification	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID5924 +2
EGFR E746_T751delinsA	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID2531 +2
EGFR L858R	Lung Adenocarcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID2634 +2
EGFR R831H	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID2618 +2
EGFR S768I	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID2614 +2
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID1666 +1
EGFR Exon 19 Deletion	Lung Adenocarcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID2519 +1
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID229 +1
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Afatinib + Erlotinib	CIViC B	EID12202
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID413
EGFR Expression	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID4877
EGFR G719	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID4189
EGFR G719S	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID1736
EGFR Gain-of-function	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID4931
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib + Afatinib	CIViC B	EID12203
EGFR L858R OR EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4759
EGFR L861	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4298
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID2053
EGFR Mutation	Lung Cancer	Sensitivity/Response	Gefitinib	CIViC B	EID2939
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Pemetrexed + Gefitinib	CIViC B	EID7650
EGFR Mutation AND ( MET Amplification OR MET Overexpression )	Lung Non-small Cell Carcinoma	Sensitivity/Response	Tepotinib + Gefitinib	CIViC B	EID11456
EGFR Overexpression	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib	CIViC B	EID954
EGFR Rare Exon 18-21 Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4755
EGFR Rare Exon 18-21 Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID4762
EGFR VIII	Glioblastoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID1128
EGFR Y1092 PHOSPHORYLATION	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID923

+100 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for gefitinib and CYP2D6	DPWG	CYP2D6

PharmGKB also curates 22 clinical and 180 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

157 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR
ABEMACICLIB	ChEMBL	Phase 4 (approved)	EGFR
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	EGFR
AFATINIB DIMALEATE	ChEMBL	Phase 4 (approved)	EGFR
ALECTINIB	ChEMBL	Phase 4 (approved)	EGFR
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	EGFR
AXITINIB	ChEMBL	Phase 4 (approved)	EGFR
BACITRACIN	ChEMBL	Phase 4 (approved)	EGFR
BITHIONOL	ChEMBL	Phase 4 (approved)	EGFR
BOSUTINIB	ChEMBL	Phase 4 (approved)	EGFR
BRIGATINIB	ChEMBL	Phase 4 (approved)	EGFR
CABOZANTINIB	ChEMBL	Phase 4 (approved)	EGFR
CERITINIB	ChEMBL	Phase 4 (approved)	EGFR
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	EGFR
CHROMIC CHLORIDE	ChEMBL	Phase 4 (approved)	EGFR
CISPLATIN	ChEMBL	Phase 4 (approved)	EGFR
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	EGFR
COLISTIN	ChEMBL	Phase 4 (approved)	EGFR
CRIZOTINIB	ChEMBL	Phase 4 (approved)	EGFR
DACOMITINIB	ChEMBL	Phase 4 (approved)	EGFR
DASATINIB	ChEMBL	Phase 4 (approved)	EGFR
DOBUTAMINE	ChEMBL	Phase 4 (approved)	EGFR
DOCETAXEL	ChEMBL	Phase 4 (approved)	EGFR
EBASTINE	ChEMBL	Phase 4 (approved)	EGFR
ECONAZOLE	ChEMBL	Phase 4 (approved)	EGFR
ERLOTINIB	ChEMBL	Phase 4 (approved)	EGFR
FEDRATINIB	ChEMBL	Phase 4 (approved)	EGFR
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	EGFR
GENTIAN VIOLET	ChEMBL	Phase 4 (approved)	EGFR
GILTERITINIB	ChEMBL	Phase 4 (approved)	EGFR
HEXACHLOROPHENE	ChEMBL	Phase 4 (approved)	EGFR
IBRUTINIB	ChEMBL	Phase 4 (approved)	EGFR
IMATINIB	ChEMBL	Phase 4 (approved)	EGFR
LAPATINIB	ChEMBL	Phase 4 (approved)	EGFR
LAPATINIB DITOSYLATE	ChEMBL	Phase 4 (approved)	EGFR
LAZERTINIB	ChEMBL	Phase 4 (approved)	EGFR
LEVODOPA	ChEMBL	Phase 4 (approved)	EGFR
LORLATINIB	ChEMBL	Phase 4 (approved)	EGFR
METHYLDOPA	ChEMBL	Phase 4 (approved)	EGFR
MICONAZOLE	ChEMBL	Phase 4 (approved)	EGFR
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	EGFR
MITOXANTRONE	ChEMBL	Phase 4 (approved)	EGFR
MOBOCERTINIB	ChEMBL	Phase 4 (approved)	EGFR
MONTELUKAST	ChEMBL	Phase 4 (approved)	EGFR
NELFINAVIR	ChEMBL	Phase 4 (approved)	EGFR
NERATINIB	ChEMBL	Phase 4 (approved)	EGFR
NICLOSAMIDE	ChEMBL	Phase 4 (approved)	EGFR
OLMUTINIB	ChEMBL	Phase 4 (approved)	EGFR
OSIMERTINIB	ChEMBL	Phase 4 (approved)	EGFR
PERHEXILINE	ChEMBL	Phase 4 (approved)	EGFR
PONATINIB	ChEMBL	Phase 4 (approved)	EGFR
SORAFENIB	ChEMBL	Phase 4 (approved)	EGFR
SULOCTIDIL	ChEMBL	Phase 4 (approved)	EGFR
SUNITINIB	ChEMBL	Phase 4 (approved)	EGFR
TAMOXIFEN	ChEMBL	Phase 4 (approved)	EGFR
TERFENADINE	ChEMBL	Phase 4 (approved)	EGFR
THIORIDAZINE	ChEMBL	Phase 4 (approved)	EGFR
TRIBROMSALAN	ChEMBL	Phase 4 (approved)	EGFR
TUCATINIB	ChEMBL	Phase 4 (approved)	EGFR