Afatinib

Summary

Afatinib (CHEMBL1173655) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EB03) targeting EGFR and ERBB2; indicated across 30 conditions including neoplasm and head and neck squamous cell carcinoma; with CIViC clinical evidence for 98 variant-indication associations (e.g. EGFR L858R in lung non-small cell carcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EB03
• Targets: 2 (EGFR, ERBB2)
• Indications: 30 conditions
• Clinical trials: 186
• Precision-oncology evidence (CIViC): 98 variant–indication associations
• Chemistry: 485.9 Da · C24H25ClFN5O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1173655
Name	Afatinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	10184653
ChEBI	CHEBI:61390
ATC	L01EB03
Molecular formula	C24H25ClFN5O3
Molecular weight	485.9
InChIKey	ULXXDDBFHOBEHA-CWDCEQMOSA-N

SMILES: CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[C@H]4CCOC4

IUPAC name: (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide

ChEBI definition: A quinazoline compound having a 3-chloro-4-fluoroanilino group at the 4-position, a 4-dimethylamino-trans-but-2-enamido group at the 6-position, and an (S)-tetrahydrofuran-3-yloxy group at the 7-position. Used (as its dimaleate salt) for the first-line treatment of patients with metastatic non-small cell lung cancer.

Pharmacological roles (ChEBI): tyrosine kinase inhibitor, antineoplastic agent.

Also known as: Afatinib, Bibw 2992, BIBW-2992, BIBW2992, Gilotrif, Giotrif, NSC-750691, Tomtovok, Tovok, AFATINIB, TOVOK, AFATINIB DIMALEATE

Parent form; salt/anhydrous children: CHEMBL2105712

Patent coverage: 6,227 distinct patent families (15,144 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 14,879 (98%) 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	7.82	17.5%	P00533
ERBB2	erb-b2 receptor tyrosine kinase 2	Inhibition	7.85	17.7%	P04626

Broader ChEMBL bioactivity targets: 52 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase SBK1, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase ABL1, Cholecystokinin receptor type A, Alpha-2B adrenergic receptor, Receptor-type tyrosine-protein kinase FLT3, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Muscarinic acetylcholine receptor M2.

Bioactivity

ChEMBL activities: 235 potent at pChembl ≥ 5 of 242 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	10.21	IC50	0.06	nM	CHEMBL_ACT_29296692
EGFR	10.1	IC50	0.08	nM	CHEMBL_ACT_25094728
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_22844197
EGFR	10	Kd	0.1	nM	CHEMBL_ACT_7576836
EGFR	9.99	IC50	0.1	nM	CHEMBL_ACT_29296689
EGFR	9.96	Kd	0.11	nM	CHEMBL_ACT_7576835
EGFR	9.92	Kd	0.12	nM	CHEMBL_ACT_7576839
EGFR	9.92	Kd	0.12	nM	CHEMBL_ACT_7576840
EGFR	9.85	Kd	0.14	nM	CHEMBL_ACT_7576838
EGFR	9.85	Kd	0.14	nM	CHEMBL_ACT_7576844
EGFR	9.79	IC50	0.16	nM	CHEMBL_ACT_25078783
EGFR	9.78	IC50	0.17	nM	CHEMBL_ACT_25078707
EGFR	9.72	IC50	0.19	nM	CHEMBL_ACT_13852012
EGFR	9.72	Kd	0.19	nM	CHEMBL_ACT_7576837
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_22844221
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_26199035
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_26212556
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_29233545
EGFR	9.7	Kd	0.2	nM	CHEMBL_ACT_7576841
EGFR	9.64	Kd	0.23	nM	CHEMBL_ACT_7576843
EGFR	9.62	IC50	0.24	nM	CHEMBL_ACT_22968079
EGFR	9.6	Kd	0.25	nM	CHEMBL_ACT_19218671
EGFR	9.6	Kd	0.25	nM	CHEMBL_ACT_7576834
EGFR	9.59	IC50	0.26	nM	CHEMBL_ACT_25078767
EGFR	9.55	IC50	0.28	nM	CHEMBL_ACT_19319721
EGFR	9.52	IC50	0.3	nM	CHEMBL_ACT_22408225
EGFR	9.48	IC50	0.33	nM	CHEMBL_ACT_24848036
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_18456238
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_18997556
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_24862039

Target pathways

Aggregated over 2 target gene(s): EGFR, ERBB2.

Top Reactome pathways

53 total, by targets touching each:

Pathway	Targets	Genes
Signaling by ERBB2	2	EGFR, ERBB2
SHC1 events in ERBB2 signaling	2	EGFR, ERBB2
PLCG1 events in ERBB2 signaling	2	EGFR, ERBB2
PIP3 activates AKT signaling	2	EGFR, ERBB2
GRB2 events in ERBB2 signaling	2	EGFR, ERBB2
PI3K events in ERBB2 signaling	2	EGFR, ERBB2
Constitutive Signaling by Aberrant PI3K in Cancer	2	EGFR, ERBB2
RAF/MAP kinase cascade	2	EGFR, ERBB2
ERBB2 Regulates Cell Motility	2	EGFR, ERBB2
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	2	EGFR, ERBB2
ERBB2 Activates PTK6 Signaling	2	EGFR, ERBB2
Downregulation of ERBB2 signaling	2	EGFR, ERBB2
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors	2	EGFR, ERBB2
Signaling by ERBB2 KD Mutants	2	EGFR, ERBB2
Signaling by ERBB2 ECD mutants	2	EGFR, ERBB2
Signaling by ERBB2 TMD/JMD mutants	2	EGFR, ERBB2
Developmental Lineage of Mammary Gland Myoepithelial Cells	2	EGFR, ERBB2
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	1	EGFR
Signaling by ERBB4	1	EGFR
GRB7 events in ERBB2 signaling	1	ERBB2
Downregulation of ERBB2:ERBB3 signaling	1	ERBB2
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
EGFR interacts with phospholipase C-gamma	1	EGFR
EGFR Transactivation by Gastrin	1	EGFR
Sema4D induced cell migration and growth-cone collapse	1	ERBB2
Signal transduction by L1	1	EGFR

Dominant GO biological processes

GO term	Targets
signal transduction	2
cell surface receptor signaling pathway	2
epidermal growth factor receptor signaling pathway	2
neuron differentiation	2
positive regulation of cell growth	2
ERBB2-EGFR signaling pathway	2
negative regulation of apoptotic process	2
positive regulation of MAPK cascade	2
phosphatidylinositol 3-kinase/protein kinase B signal transduction	2
positive regulation of epithelial cell proliferation	2
cellular response to epidermal growth factor stimulus	2
protein phosphorylation	2
cell surface receptor protein tyrosine kinase signaling pathway	2
cell population proliferation	2
regulation of cell population proliferation	2

Indications & clinical

Indications

30 indications (0 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
neoplasm	3	MONDO:0005070	EFO:0000616
head and neck squamous cell carcinoma	3	MONDO:0010150	EFO:0000181
squamous cell carcinoma	3	MONDO:0005096	EFO:0000707
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
breast neoplasm	3	MONDO:0021100	EFO:0003869
upper aerodigestive tract neoplasm	3	MONDO:0005398	EFO:0004284
head and neck cancer	3	MONDO:0005627	EFO:0006859
prostate adenocarcinoma	2	MONDO:0005082	EFO:0000673
small cell lung carcinoma	2	MONDO:0008433	EFO:0000702
tumor of uterus	2	MONDO:0021353	EFO:0003859
colorectal neoplasm	2	MONDO:0005335	EFO:0004142
esophageal squamous cell carcinoma	2	MONDO:0005580	EFO:0005922
gallbladder carcinoma	2	MONDO:0003220	EFO:1001956
lung neoplasm	2	MONDO:0021117	MONDO:0008903
chordoma	2	MONDO:0008978	MONDO:0008978
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
paraganglioma	2	MONDO:0000448	EFO:1000453
liver disorder	1	MONDO:0005154	EFO:0001421
glioblastoma	1	MONDO:0018177	EFO:0000519
exocrine pancreatic carcinoma	1	MONDO:0005192	EFO:0002618
endometriosis	1	MONDO:0005133	EFO:0001065
metastatic neoplasm	1	MONDO:0024883	EFO:0009709
kidney failure	1	MONDO:0001106	HP:0000083
brain cancer	1	MONDO:0001657	MONDO:0001657
gastric neoplasm	1	MONDO:0021085	EFO:0003897
cholangiocarcinoma	1	MONDO:0019087	EFO:0005221

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

Clinical trials

Total trials: 186.

Phase distribution

Phase	Trials
PHASE2	84
PHASE1	44
Not specified	22
PHASE3	17
PHASE1/PHASE2	11
PHASE4	6
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04413201	PHASE4	ACTIVE_NOT_RECRUITING	AFAMOSI: Efficacy and Safety of Afatinib Followed by Osimertinib Compared to Osimertinib in Patients with EGFRmutated/T790M Mutation Negative Nonsquamous NSCLC
NCT02208843	PHASE4	COMPLETED	Afatinib as Second-line Therapy for Lung Cancer With Epidermal Growth Factor Receptor (EGFR) Mutation
NCT02514174	PHASE4	COMPLETED	Afatinib Treatment for Patients With EGFR Mutation Positive NSCLC Who Are Age 70 or Older
NCT02695290	PHASE4	TERMINATED	Afatinib in EGFR+NSCLC (Recurrent or Stage IV) - Patients With Poor Performance Status (ECOG 2 or 3)
NCT04132102	PHASE4	UNKNOWN	To Evaluate the Efficacy of Afatinib in Advanced Lung Squamous Cell Carcinoma With EGFR Sensitive Mutation
NCT04814056	PHASE4	UNKNOWN	To Evaluate the Efficacy of Afatinib in the Treatment of Locally Advanced/Metastatic Non-Small Cell Lung Cancer With NRG1 Fusion
NCT06486142	PHASE3	RECRUITING	EGFR-mutated Lung Cancer in Randomized Investigator-Initiated Study
NCT06759857	PHASE3	ENROLLING_BY_INVITATION	FHND9041 Versus Afatinib for Non-small Cell Lung Cancer
NCT00656136	PHASE3	COMPLETED	BIBW 2992 and BSC Versus Placebo and BSC in Non-small Cell Lung Cancer Patients Failing Erlotinib or Gefitinib (LUX-LUNG 1)
NCT00949650	PHASE3	COMPLETED	BIBW 2992 (Afatinib) Versus Chemotherapy as First Line Treatment in NSCLC With EGFR Mutation
NCT01085136	PHASE3	COMPLETED	LUX-Lung 5: Afatinib Plus Weekly Paclitaxel Versus Investigator’s Choice of Single Agent Chemotherapy Following Afatinib Monotherapy in Non-small Cell Lung Cancer Patients Failing Erlotinib or Gefitinib
NCT01121393	PHASE3	COMPLETED	BIBW 2992 (Afatinib) vs Gemcitabine-cisplatin in 1st Line Non-small Cell Lung Cancer (NSCLC)
NCT01125566	PHASE3	COMPLETED	LUX-Breast 1: BIBW 2992 (Afatinib) in HER2-positive Metastatic Breast Cancer Patients After One Prior Herceptin Treatment
NCT01345669	PHASE3	TERMINATED	LUX-Head&Neck 2: A Phase III Trial of Afatinib (BIBW 2992) Versus Placebo for the Treatment of Head and Neck Squamous Cell Cancer After Treatment With Chemo-radiotherapy
NCT01345682	PHASE3	COMPLETED	LUX-Head&Neck 1: A Phase III Trial of Afatinib (BIBW2992) Versus Methotrexate for the Treatment of Recurrent and/or Metastatic (R/M) Head and Neck Squamous Cell Cancer After Platinum Based Chemotherapy
NCT01427478	PHASE3	COMPLETED	Evaluation of Afatinib in Maintenance Therapy in Squamous Cell Carcinoma of the Head and Neck
NCT01523587	PHASE3	COMPLETED	LUX-Lung 8: A Phase III Trial of Afatinib (BIBW 2992) Versus Erlotinib for the Treatment of Squamous Cell Lung Cancer After at Least One Prior Platinum Based Chemotherapy
NCT01814553	PHASE3	COMPLETED	ADAM-Afatinib Diarrhea Assessment and Management
NCT01853826	PHASE3	COMPLETED	An Open Label Trial of Afatinib (Giotrif) in Treatment-naive (1st Line) or Chemotherapy Pre-treated Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) Harboring EGFR Mutation(s)
NCT01856478	PHASE3	COMPLETED	LUX-Head&Neck 3: Afatinib (BIBW2992) Versus Methotrexate for the Treatment of Recurrent and/or Metastatic Head and Neck Squamous Cell Cancer After Platinum Based Chemotherapy
NCT01953913	PHASE3	COMPLETED	Afatinib (BIBW 2992) in Advanced Non-Small Cell Lung Cancer Patients With EGFR Mutation
NCT02044380	PHASE3	COMPLETED	Afatinib in Patients With Non Small Cell Lung Cancer (NSCLC) With Epidermal Growth Factor Receptor (EGFR) Mutations
NCT02131155	PHASE3	TERMINATED	LUX-Head & Neck 4: Afatinib (BIBW 2992) Versus Placebo for the Treatment of Head and Neck Squamous Cell Cancer After Treatment With Chemo-radiotherapy
NCT02438722	PHASE2/PHASE3	COMPLETED	S1403, Afatinib Dimaleate With or Without Cetuximab in Treating Patients With Newly Diagnosed Stage IV or Recurrent, EGFR Mutation Positive Non-small Cell Lung Cancer
NCT01553942	PHASE2	ACTIVE_NOT_RECRUITING	Afatinib With CT and RT for EGFR-Mutant NSCLC
NCT02465060	PHASE2	ACTIVE_NOT_RECRUITING	Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02491099	PHASE2	RECRUITING	A Phase II Evaluation of Afatinib in Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma
NCT02925234	PHASE2	RECRUITING	The Drug Rediscovery Protocol (DRUP Trial)
NCT03785249	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1
NCT04183712	PHASE2	RECRUITING	Target Therapy With GEMOX in Recectable Gallbladder Carcinoma Patients Monitored by ctDNA
NCT04439136	PHASE2	ACTIVE_NOT_RECRUITING	Testing Afatinib as a Potential Targeted Treatment in Cancers With HER2 Genetic Changes (MATCH-Subprotocol B)
NCT04497584	PHASE2	ACTIVE_NOT_RECRUITING	Phase 2 Trial of Afatinib Plus Prednisone for Advanced Squamous NSCLC
NCT05070403	PHASE2	RECRUITING	Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma
NCT05215548	PHASE2	ACTIVE_NOT_RECRUITING	Primary Tumor Resection With EGFR TKI for Stage IV NSCLC
NCT06062823	PHASE2	RECRUITING	Study of EGFR TKI in Patients With Advanced NSCLC Harbouring EGFR Mutations
NCT06071013	PHASE1/PHASE2	RECRUITING	Nintedanib Plus EGFR TKI In EGFR-mutated Non-small Cell Lung Cancer Patients
NCT06085755	PHASE1/PHASE2	RECRUITING	Trastuzumab Deruxtecan(T-DXd) and Afatinib Combination in HER2-low Advanced Gastric Cancer
NCT06385483	PHASE2	ACTIVE_NOT_RECRUITING	Testing Afatinib as Potentially Targeted Treatment in Cancers With EGFR Genetic Changes (MATCH - Subprotocol A)
NCT06648096	PHASE1/PHASE2	RECRUITING	Afatinib in Patients With Fanconi Anemia (FA) and Advanced Head and Neck Squamous Cell Carcinoma (HNSCC)
NCT07010120	PHASE1/PHASE2	RECRUITING	A Clinical Trial of Neoadjuvant Targeted Therapy, Immunotherapy, and Lysogenic HSV-Based Virotherapy in Resectable Head and Neck Squamous Cell Carcinoma

Clinical evidence (CIViC)

Variant × indication × effect (98 predictive associations from 127 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC A	EID2997 +3
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC A	EID2996 +2
EGFR G719	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC A	EID11242
EGFR S768I OR EGFR G719A OR EGFR L861Q	Lung Adenocarcinoma	Sensitivity/Response	Afatinib	CIViC A	EID11229
EGFR Exon 19 Deletion	Lung Adenocarcinoma	Sensitivity/Response	Afatinib	CIViC B	EID880 +3
EGFR L858R	Lung Adenocarcinoma	Sensitivity/Response	Afatinib	CIViC B	EID879 +2
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID1728 +2
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Afatinib	CIViC B	EID1011 +2
ERBB2 A775_G776insYVMA	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID7202 +1
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Afatinib + Erlotinib	CIViC B	EID12202
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib + Afatinib	CIViC B	EID12203
ERBB2 Activating Mutation	Cancer	Sensitivity/Response	Afatinib	CIViC B	EID11676
ERBB2 Activating Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID7201
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab + Afatinib	CIViC B	EID1013
ERBB2 Amplification	Transitional Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID7810
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Afatinib + Lapatinib + Trastuzumab	CIViC B	EID887
ERBB3 G284R	Transitional Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID1748
ERBB3 R103G	Transitional Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID1747
ERBB3 V104M	Transitional Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC B	EID1746
CDKN2A p16 Expression	Head And Neck Squamous Cell Carcinoma	Resistance	Afatinib	CIViC B	EID1155
EGFR Exon 20 Insertion	Lung Adenocarcinoma	Resistance	Afatinib	CIViC B	EID1809
EGFR T790M	Lung Non-small Cell Carcinoma	Resistance	Afatinib	CIViC B	EID1863
EGFR E746_A750del	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2515 +2
CD74::NRG1 Fusion	Mucinous Adenocarcinoma	Sensitivity/Response	Afatinib	CIViC C	EID7490 +1
EGFR E746V	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2540 +1
EGFR E746_S752delinsD	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2571 +1
EGFR E746_T751>I	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2527 +1
EGFR L747_A750delinsP	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2550 +1
EGFR L747_P753>Q	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2599 +1
EGFR L747_P753delinsS	Lung Non-small Cell Carcinoma	Sensitivity/Response	Afatinib	CIViC C	EID2610 +1

+68 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 9 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.

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

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
LAPATINIB DITOSYLATE	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
LAZERTINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
MOBOCERTINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
BITHIONOL	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
BOSUTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
BRIGATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
CABOZANTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
COLISTIN	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
DASATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
EBASTINE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
ECONAZOLE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
ERLOTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
HEXACHLOROPHENE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
IBRUTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
IMATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
LAPATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
MICONAZOLE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
MITOXANTRONE	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
NERATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
OSIMERTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
PONATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
SORAFENIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
TAMOXIFEN	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
TRIBROMSALAN	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
TUCATINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
VANDETANIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
ZANUBRUTINIB	ChEMBL	Phase 4 (approved)	EGFR, ERBB2
ALISERTIB	ChEMBL	Phase 3	EGFR, ERBB2
ALVOCIDIB	ChEMBL	Phase 3	EGFR, ERBB2
CANDESARTAN	ChEMBL	Phase 3	EGFR, ERBB2
CANERTINIB	ChEMBL	Phase 3	EGFR, ERBB2
CEDIRANIB	ChEMBL	Phase 3	EGFR, ERBB2
ENCLOMIPHENE	ChEMBL	Phase 3	EGFR, ERBB2
MASITINIB	ChEMBL	Phase 3	EGFR, ERBB2
POZIOTINIB	ChEMBL	Phase 3	EGFR, ERBB2
PYROTINIB	ChEMBL	Phase 3	EGFR, ERBB2
REMIBRUTINIB	ChEMBL	Phase 3	EGFR, ERBB2
ZONGERTINIB	ChEMBL	Phase 3	EGFR, ERBB2
AEE-788	ChEMBL	Phase 2	EGFR, ERBB2
ALLITINIB	ChEMBL	Phase 2	EGFR, ERBB2
ATUZABRUTINIB	ChEMBL	Phase 2	EGFR, ERBB2
CENISERTIB	ChEMBL	Phase 2	EGFR, ERBB2
CLOSANTEL	ChEMBL	Phase 2	EGFR, ERBB2
CP-724714	ChEMBL	Phase 2	EGFR, ERBB2
DEFOSBARASERTIB	ChEMBL	Phase 2	EGFR, ERBB2
ELLAGIC ACID	ChEMBL	Phase 2	EGFR, ERBB2
FALNIDAMOL	ChEMBL	Phase 2	EGFR, ERBB2
FORETINIB	ChEMBL	Phase 2	EGFR, ERBB2
ILORASERTIB	ChEMBL	Phase 2	EGFR, ERBB2
IODOQUINOL	ChEMBL	Phase 2	EGFR, ERBB2
PELITINIB	ChEMBL	Phase 2	EGFR, ERBB2