Neratinib

Summary

Neratinib (CHEMBL180022) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EH02) targeting EGFR and ERBB2; indicated across 16 conditions including breast neoplasm and breast carcinoma; with CIViC clinical evidence for 38 variant-indication associations (e.g. ERBB2 Amplification in her2-receptor positive breast cancer).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EH02
• Targets: 2 (EGFR, ERBB2)
• Indications: 16 conditions
• Clinical trials: 82
• Precision-oncology evidence (CIViC): 38 variant–indication associations
• Chemistry: 557 Da · C30H29ClN6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL180022
Name	Neratinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9915743
ChEBI	CHEBI:61397
ATC	L01EH02
Molecular formula	C30H29ClN6O3
Molecular weight	557
InChIKey	JWNPDZNEKVCWMY-VQHVLOKHSA-N

SMILES: CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C

IUPAC name: (E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide

ChEBI definition: A quinoline compound having a cyano group at the 3-position, a 3-chloro-4-(2-pyridylmethoxy)anilino group at the 4-position, a 4-dimethylamino-trans-but-2-enoylamido group at the 6-position, and an ethoxy group at the 7-position.

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

Also known as: CDP-820, HKI-272, Neratinib, WAY-179272, neratinib, NERATINIB, SID124950160, NERATINIB (HKI-272), Napatanib, Neratinib (HKI-272), Neratinib; Neralynx

Parent form; salt/anhydrous children: CHEMBL3989921

Patent coverage: 3,777 distinct patent families (9,404 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 9,127 (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	7.04	17.5%	P00533
ERBB2	erb-b2 receptor tyrosine kinase 2	Inhibition	7.23	17.7%	P04626

Broader ChEMBL bioactivity targets: 118 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Mitogen-activated protein kinase kinase kinase 13, Microtubule-associated serine/threonine-protein kinase 1, ATP-binding cassette sub-family C member 4, Vasopressin V2 receptor, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Dual serine/threonine and tyrosine protein kinase.

Bioactivity

ChEMBL activities: 219 potent at pChembl ≥ 5 of 224 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	10.7	IC50	0.02	nM	CHEMBL_ACT_22408231
EGFR	10.7	IC50	0.02	nM	CHEMBL_ACT_22408239
EGFR	10.1	IC50	0.08	nM	CHEMBL_ACT_1943195
EGFR	9.74	IC50	0.18	nM	CHEMBL_ACT_1943214
EGFR	9.43	Kd	0.37	nM	CHEMBL_ACT_7567884
EGFR	9.43	Kd	0.37	nM	CHEMBL_ACT_7567891
EGFR	9.41	IC50	0.39	nM	CHEMBL_ACT_24907894
EGFR	9.24	IC50	0.58	nM	CHEMBL_ACT_24907641
EGFR	9.21	Kd	0.61	nM	CHEMBL_ACT_7567886
EGFR	9.2	Kd	0.63	nM	CHEMBL_ACT_7567892
MAP4K5	9.19	Kd	0.65	nM	CHEMBL_ACT_7567948
EGFR	9.17	Kd	0.67	nM	CHEMBL_ACT_7567889
EGFR	9.1	IC50	0.8	nM	CHEMBL_ACT_22408223
EGFR	9.04	Kd	0.91	nM	CHEMBL_ACT_7567885
EGFR	9.03	Kd	0.93	nM	CHEMBL_ACT_7567887
EGFR	9	IC50	1	nM	CHEMBL_ACT_2246121
ERBB2	9	IC50	1	nM	CHEMBL_ACT_2246144
EGFR	9	Kd	1	nM	CHEMBL_ACT_7567888
EGFR	8.96	Kd	1.1	nM	CHEMBL_ACT_19218711
EGFR	8.96	Kd	1.1	nM	CHEMBL_ACT_7567882
EGFR	8.85	IC50	1.4	nM	CHEMBL_ACT_19187588
EGFR	8.82	Kd	1.5	nM	CHEMBL_ACT_7567893
EGFR	8.76	IC50	1.73	nM	CHEMBL_ACT_28170578
ERBB2	8.75	IC50	1.76	nM	CHEMBL_ACT_24907865
ERBB2	8.71	IC50	1.96	nM	CHEMBL_ACT_28170575
ERBB2	8.7	EC50	2	nM	CHEMBL_ACT_2206795
ERBB2	8.7	EC50	2	nM	CHEMBL_ACT_2206796
EGFR	8.66	IC50	2.2	nM	CHEMBL_ACT_13322674
EGFR	8.64	Kd	2.3	nM	CHEMBL_ACT_7567883
ERBB4	8.62	Kd	2.4	nM	CHEMBL_ACT_7597981

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

16 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
breast neoplasm	3	MONDO:0021100	EFO:0003869
breast carcinoma	3	MONDO:0004989	EFO:0000305
neoplasm	3	MONDO:0005070	EFO:0000616
biliary tract neoplasm	3	MONDO:0005304	EFO:0003891
HER2 positive breast carcinoma	3	MONDO:0006244	EFO:1000294
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
glioblastoma	2	MONDO:0018177	EFO:0000519
angiosarcoma	2	MONDO:0016982	EFO:0003968
prostate adenocarcinoma	2	MONDO:0005082	EFO:0000673
carcinoma	1	MONDO:0004993	EFO:0000313
ovarian cancer	1	MONDO:0008170	MONDO:0008170
chronic myeloid leukemia	1	MONDO:0011996	EFO:0000339
hepatocellular carcinoma	1	MONDO:0007256	EFO:0000182
gastric neoplasm	1	MONDO:0021085	MONDO:0001056
colorectal neoplasm	1	MONDO:0005335	MONDO:0005575

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

Clinical trials

Total trials: 82.

Phase distribution

Phase	Trials
PHASE2	35
PHASE1	24
PHASE1/PHASE2	12
Not specified	6
PHASE3	4
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05615818	PHASE3	RECRUITING	Personalized Medicine for Advanced Biliary Cancer Patients
NCT05760612	PHASE3	RECRUITING	Adjuvant Trastuzumab Plus Neratinib in Hormone Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Positive Breast Cancer After Neoadjuvant Trastuzumab Plus Pertuzumab
NCT00878709	PHASE3	COMPLETED	Study Evaluating The Effects Of Neratinib After Adjuvant Trastuzumab In Women With Early Stage Breast Cancer
NCT01808573	PHASE3	COMPLETED	A Study of Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer Who Have Received Two or More Prior HER2 Directed Regimens in the Metastatic Setting
NCT01042379	PHASE2	RECRUITING	I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT02932280	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Safety and Dose Finding Study of Neratinib in Children and Young Adults With Cancer That Has Returned or Not Responded to Treatment
NCT02977780	PHASE2	RECRUITING	INdividualized Screening Trial of Innovative Glioblastoma Therapy (INSIGhT)
NCT03377387	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Capecitabine 7/7 Schedule With Neratinib in Patients With Metastatic HER2-Positive Breast Cancer
NCT03919292	PHASE1/PHASE2	RECRUITING	Neratinib + Valproate in Advanced Solid Tumors, w/Expansion Cohort in Ras-Mutated Ca
NCT04374305	PHASE2	RECRUITING	Innovative Trial for Understanding the Impact of Targeted Therapies in NF2-Related Schwannomatosis (INTUITT-NF2)
NCT04886531	PHASE2	RECRUITING	Trial of Pre-operative Neratinib and Endocrine Therapy With Trastuzumab in ER-Positive, HER-2 Positive Breast Cancers
NCT05252988	PHASE2	ACTIVE_NOT_RECRUITING	Three Antidiarrheal Strategies in HER2+/HR+ Early Breast Cancer Patients Treated With Extended Adjuvant Neratinib
NCT05388149	PHASE2	RECRUITING	Kadcyla And Neratinib for Interception of HER2+ Breast Cancer With Molecular Residual Disease
NCT05919108	PHASE2	RECRUITING	Neoadjuvant Neratinib in Stage I-III HER2-Mutated Lobular Breast Cancers
NCT05933395	PHASE2	RECRUITING	Genetically-informed Therapy for ER+ Breast Cancer Post-CDK4/6 Inhibitor
NCT06109467	PHASE2	RECRUITING	Neratinib In Combination With Chemotherapy/Trastuzumab/Pembrolizumab In HER2 Gastroesophageal Cancer
NCT06519110	PHASE2	NOT_YET_RECRUITING	Neratinib Tablets Monotherapy for Advanced Solid Tumors With HER2 Mutations
NCT06813079	PHASE2	NOT_YET_RECRUITING	Using Tumor Models to Determine Treatments
NCT07152782	PHASE2	NOT_YET_RECRUITING	T-DXd With or Without Neratinib for HER2 Positive Breast Cancer With Brain Metastasis
NCT00266877	PHASE2	COMPLETED	Study Evaluating the Safety Of HKI-272 (Neratinib) In Subjects With Advanced Non-Small Cell Lung Cancer
NCT00300781	PHASE2	COMPLETED	Study Evaluating HKI-272 (Neratinib) In Subjects With Advanced Breast Cancer
NCT00398567	PHASE1/PHASE2	COMPLETED	A Phase 1/2 Study Of HKI-272 (Neratinib) in Combination With Trastuzumab (Herceptin) In Subjects With Advanced Breast Cancer
NCT00445458	PHASE1/PHASE2	COMPLETED	A Phase 1/2 Study of HKI-272 (Neratinib) in Combination With Paclitaxel (Taxol) in Subjects With Solid Tumors and Breast Cancer
NCT00706030	PHASE1/PHASE2	COMPLETED	Study Evaluating Neratinib (HKI-272) In Combination With Vinorelbine In Subjects With Solid Tumors And Metastatic Breast Cancer
NCT00741260	PHASE1/PHASE2	COMPLETED	Study Evaluating The Combination Of Neratinib And Capecitabine In Solid Tumors And Breast Cancer
NCT00777101	PHASE2	COMPLETED	Study Evaluating Neratinib Versus Lapatinib Plus Capecitabine For ErbB2 Positive Advanced Breast Cancer
NCT00915018	PHASE2	COMPLETED	Study Evaluating Neratinib Plus Paclitaxel VS Trastuzumab Plus Paclitaxel In ErbB-2 Positive Advanced Breast Cancer
NCT01008150	PHASE2	COMPLETED	Phase II Randomized Trial Evaluating Neoadjuvant Therapy With Neratinib and/or Trastuzumab Followed by Postoperative Trastuzumab in Women With Locally Advanced HER2-positive Breast Cancer
NCT01111825	PHASE1/PHASE2	COMPLETED	Temsirolimus Plus Neratinib for Patients With Metastatic HER2-Amplified or Triple Negative Breast Cancer
NCT01494662	PHASE2	COMPLETED	HKI-272 for HER2-Positive Breast Cancer and Brain Metastases
NCT01670877	PHASE2	COMPLETED	Neratinib +/- Fulvestrant in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer
NCT01827267	PHASE2	COMPLETED	Neratinib With and Without Temsirolimus for Patients With HER2 Activating Mutations in Non-Small Cell Lung Cancer
NCT01953926	PHASE2	TERMINATED	Basket Study of Neratinib in Participants With Solid Tumors Harboring Somatic HER2 or EGFR Exon 18 Mutations
NCT01960023	PHASE1/PHASE2	WITHDRAWN	Safety and Efficacy Study of Neratinib and Cetuximab to Treat Patients With Quadruple Wild-Type Metastatic Colorectal Cancer
NCT02236000	PHASE1/PHASE2	COMPLETED	A Dose-Escalation Study Evaluating the Combination of Trastuzumab Emtansine (T-DM1) With Neratinib in Women With Metastatic HER2-Positive Breast Cancer
NCT02400476	PHASE2	COMPLETED	An Open-Label Study to Characterize the Incidence and Severity of Diarrhea in Patients With Early-Stage HER2+ Breast Cancer Treated With Neratinib and Loperamide
NCT02673398	PHASE2	COMPLETED	Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer
NCT03094052	PHASE2	COMPLETED	Incidence and Severity of Diarrhea in Patients With HER2 Positive Breast Cancer Treated With Trastuzumab and Neratinib
NCT03101748	PHASE1/PHASE2	TERMINATED	Neratinib and Paclitaxel With or Without Pertuzumab and Trastuzumab Before Combination Chemotherapy in Treating Patients With Metastatic or Locally Advanced Breast Cancer
NCT03182634	PHASE2	UNKNOWN	The UK Plasma Based Molecular Profiling of Advanced Breast Cancer to Inform Therapeutic CHoices (plasmaMATCH) Trial

Clinical evidence (CIViC)

Variant × indication × effect (38 predictive associations from 43 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab + Neratinib	CIViC A	EID1113 +2
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Capecitabine + Neratinib	CIViC A	EID8048 +1
ERBB2 Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Neratinib	CIViC B	EID761 +2
ERBB2 G292R	Urinary Bladder Cancer	Sensitivity/Response	Neratinib	CIViC B	EID12119
ERBB2 Mutation	Breast Cancer	Sensitivity/Response	Neratinib	CIViC B	EID5338
ERBB2 V777L	Cancer	Sensitivity/Response	Neratinib	CIViC B	EID12106
ERBB2 L755S	Triple-receptor Negative Breast Cancer	Sensitivity/Response	Capecitabine + Neratinib	CIViC C	EID8055
ERBB2 L869R	Breast Cancer	Sensitivity/Response	Neratinib	CIViC C	EID6173
ERBB2 T798I	Breast Cancer	Resistance	Neratinib	CIViC C	EID6175
EGFR EGFRVIII	Lung Non-small Cell Carcinoma	Sensitivity/Response	Neratinib	CIViC D	EID12821
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Neratinib	CIViC D	EID2628
EGFR M766Q	Lung Non-small Cell Carcinoma	Sensitivity/Response	Neratinib	CIViC D	EID7389
EGFR T790M	Lung Non-small Cell Carcinoma	Sensitivity/Response	Neratinib	CIViC D	EID2162
ERBB2 D769H	Breast Cancer	Sensitivity/Response	Neratinib + Lapatinib	CIViC D	EID279
ERBB2 D769Y	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID280
ERBB2 G292R	Cancer	Sensitivity/Response	Trastuzumab + Afatinib + Osimertinib + Lapatinib + Neratinib	CIViC D	EID12116
ERBB2 G309A	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID282
ERBB2 G778_P780dup	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID285
ERBB2 L755S	Colon Cancer	Sensitivity/Response	Lapatinib + Neratinib + Trastuzumab	CIViC D	EID1176
ERBB2 L755S	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID283
ERBB2 L755W	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID284
ERBB2 L755_T759del	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID281
ERBB2 L866M	Colon Cancer	Sensitivity/Response	Trastuzumab + Neratinib + Lapatinib	CIViC D	EID1178
ERBB2 R34Q	Cancer	Sensitivity/Response	Lapatinib + Osimertinib + Afatinib + Trastuzumab + Neratinib	CIViC D	EID11600
ERBB2 R678Q	Breast Cancer	Sensitivity/Response	Lapatinib + Neratinib	CIViC D	EID286
ERBB2 R896C	Breast Cancer	Sensitivity/Response	Neratinib	CIViC D	EID287
ERBB2 S310F/Y	Colon Cancer	Sensitivity/Response	Neratinib + Trastuzumab + Lapatinib	CIViC D	EID1179
ERBB2 V777L	Pancreatic Ductal Adenocarcinoma	Sensitivity/Response	Neratinib	CIViC D	EID11569
ERBB2 V777L	Colon Cancer	Sensitivity/Response	Lapatinib + Trastuzumab + Neratinib	CIViC D	EID1177
ERBB2 V777L	Cancer	Sensitivity/Response	Afatinib + Lapatinib + Osimertinib + Neratinib	CIViC D	EID12101

+8 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

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

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2
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
AFATINIB DIMALEATE	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
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