Lapatinib
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Also known as GSK-572016GW-2016GW-572016GW-572016XGW572016TyverbTYKERBGW572016FLAPATINIB DITOSYLATE MONOHYDRATEFMMLAPATINIB (FREE BASE)GSK 572016LAPATINIB DITOSYLATELAPATANIBGSK572016GW2016LAPATINIB (GW-572016)SID50112760SID103905567
Summary
Lapatinib (CHEMBL554) is an approved small-molecule antineoplastic agent (ATC L01EH01) targeting EGFR and ERBB2; indicated across 36 conditions including neoplasm and breast carcinoma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EH01
- Targets: 2 (EGFR, ERBB2)
- Indications: 36 conditions
- Clinical trials: 262
- Chemistry: 581.1 Da · C29H26ClFN4O4S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL554 |
| Name | Lapatinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 208908 |
| ChEBI | CHEBI:49603 |
| ATC | L01EH01 |
| Molecular formula | C29H26ClFN4O4S |
| Molecular weight | 581.1 |
| InChIKey | BCFGMOOMADDAQU-UHFFFAOYSA-N |
SMILES: CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
IUPAC name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor.
Also known as: GSK-572016, GW-2016, GW-572016, GW-572016X, GW572016, Lapatinib, Tyverb, TYKERB, TYVERB, GW572016F, LAPATINIB DITOSYLATE MONOHYDRATE, FMM
Parent form; salt/anhydrous children: CHEMBL1076241, CHEMBL1201179, CHEMBL1201183, CHEMBL3526325
Patent coverage: 17,872 distinct patent families (69,326 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 68,757 (99%) 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 | 8 | 17.5% | P00533 |
| ERBB2 | erb-b2 receptor tyrosine kinase 2 | Inhibition | 7.89 | 17.7% | P04626 |
Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase ABL1, Platelet-derived growth factor receptor beta, Insulin receptor, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Menin/Histone-lysine N-methyltransferase MLL, Epidermal growth factor receptor and ErbB2 (HER1 and HER2), Aurora kinase B.
Bioactivity
ChEMBL activities: 243 potent at pChembl ≥ 5 of 263 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| EGFR | 10.22 | IC50 | 0.06 | nM | CHEMBL_ACT_22408240 |
| EGFR | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_22408232 |
| EGFR | 9.05 | Kd | 0.9 | nM | CHEMBL_ACT_25790342 |
| EGFR | 9.04 | Kd | 0.92 | nM | CHEMBL_ACT_25790322 |
| EGFR | 9.04 | Kd | 0.92 | nM | CHEMBL_ACT_2898753 |
| EGFR | 9.04 | Kd | 0.92 | nM | CHEMBL_ACT_7580142 |
| EGFR | 8.92 | Kd | 1.2 | nM | CHEMBL_ACT_25790328 |
| EGFR | 8.92 | Kd | 1.2 | nM | CHEMBL_ACT_25790343 |
| EGFR | 8.92 | Kd | 1.2 | nM | CHEMBL_ACT_2904727 |
| EGFR | 8.92 | Kd | 1.2 | nM | CHEMBL_ACT_7582068 |
| ERBB2 | 8.8 | Ki | 1.58 | nM | CHEMBL_ACT_9614678 |
| ERBB2 | 8.8 | Ki | 1.58 | nM | CHEMBL_ACT_9618393 |
| EGFR | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_19187589 |
| EGFR | 8.68 | Kd | 2.1 | nM | CHEMBL_ACT_25790323 |
| EGFR | 8.68 | Kd | 2.1 | nM | CHEMBL_ACT_25790344 |
| EGFR | 8.68 | Kd | 2.1 | nM | CHEMBL_ACT_2898791 |
| EGFR | 8.68 | Kd | 2.1 | nM | CHEMBL_ACT_7580143 |
| EGFR | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_25790324 |
| EGFR | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_25790345 |
| EGFR | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_2898829 |
| EGFR | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_7580144 |
| EGFR | 8.62 | Kd | 2.4 | nM | CHEMBL_ACT_25790320 |
| EGFR | 8.62 | Kd | 2.4 | nM | CHEMBL_ACT_25790346 |
| EGFR | 8.62 | Kd | 2.4 | nM | CHEMBL_ACT_2898677 |
| EGFR | 8.62 | Kd | 2.4 | nM | CHEMBL_ACT_7580140 |
| ERBB2 | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_15130273 |
| EGFR | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_20689378 |
| ERBB2 | 8.55 | IC50 | 2.8 | nM | CHEMBL_ACT_22408419 |
| EGFR | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_25790327 |
| EGFR | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_25790347 |
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
36 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 |
| breast carcinoma | 3 | MONDO:0004989 | EFO:0000305 |
| breast neoplasm | 3 | MONDO:0021100 | EFO:0003869 |
| brain disorder | 3 | MONDO:0005560 | EFO:0005774 |
| soft tissue sarcoma | 3 | MONDO:0018078 | EFO:1001968 |
| head and neck cancer | 3 | MONDO:0005627 | EFO:0006859 |
| head and neck neoplasm | 3 | MONDO:0005586 | EFO:0005950 |
| HER2 positive breast carcinoma | 3 | MONDO:0006244 | EFO:1000294 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| colorectal adenocarcinoma | 2 | MONDO:0005008 | EFO:0000365 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| pituitary gland adenoma | 2 | MONDO:0006373 | EFO:1000478 |
| esophageal squamous cell carcinoma | 2 | MONDO:0005580 | EFO:0005922 |
| breast ductal adenocarcinoma | 2 | MONDO:0005590 | EFO:0006318 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| brain cancer | 2 | MONDO:0001657 | MONDO:0001657 |
| peritoneal neoplasm | 2 | MONDO:0006901 | MONDO:0002087 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| bile duct carcinoma | 2 | MONDO:0005496 | EFO:0005540 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| gallbladder neoplasm | 2 | MONDO:0021253 | MONDO:0005411 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| chronic kidney disease | 1 | MONDO:0005300 | EFO:0003884 |
| renal cell carcinoma | 1 | MONDO:0005086 | EFO:0000681 |
| thyroid gland carcinoma | 1 | MONDO:0015075 | EFO:0002892 |
| endometrium neoplasm | 1 | MONDO:0021251 | MONDO:0011962 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 262.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 130 |
| PHASE1 | 62 |
| PHASE3 | 32 |
| PHASE1/PHASE2 | 19 |
| Not specified | 9 |
| EARLY_PHASE1 | 5 |
| PHASE2/PHASE3 | 4 |
| PHASE4 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01328054 | PHASE4 | COMPLETED | A Study in Cancer Patients to Evaluate the Effect of Lapatinib on the QTc Interval |
| NCT06313983 | PHASE3 | RECRUITING | A Phase Ⅲ Study of Hemay022 in Combination With AI In Advanced Breast Cancer |
| NCT00073528 | PHASE3 | COMPLETED | Study Comparing Lapatinib (GW572016) And Letrozole Versus Letrozole In Subjects With Advanced Or Metastatic Breast Cancer |
| NCT00075270 | PHASE3 | COMPLETED | Paclitaxel With / Without GW572016 (Lapatinib) As First Line Therapy For Women With Advanced Or Metastatic Breast Cancer |
| NCT00078572 | PHASE3 | COMPLETED | Capecitabine (XELODA) With Or Without Lapatinib (GW572016) For Women With Refractory Advanced or Metastatic Breast Cancer |
| NCT00272987 | PHASE3 | TERMINATED | ErbB2 Over-expressing Metastatic Breast Cancer Study Using Paclitaxel, Trastuzumab, and Lapatinib |
| NCT00281658 | PHASE3 | COMPLETED | Study In Women And Men With Metastatic Breast Cancer That Have Overexpression Of ErbB2 |
| NCT00320385 | PHASE3 | COMPLETED | Lapatinib In Combination With Trastuzumab Versus Lapatinib Monotherapy In Subjects With HER2-positive Metastatic Breast Cancer |
| NCT00374322 | PHASE3 | COMPLETED | Tykerb Evaluation After Chemotherapy (TEACH): Lapatinib Versus Placebo In Women With Early-Stage Breast Cancer |
| NCT00390455 | PHASE3 | COMPLETED | Fulvestrant With or Without Lapatinib in Treating Postmenopausal Women With Stage III or Stage IV Breast Cancer That is Hormone Receptor-Positive |
| NCT00424255 | PHASE3 | COMPLETED | Study Of Adjuvant Lapatinib In High-Risk Head And Neck Cancer Subjects After Surgery |
| NCT00450203 | PHASE2/PHASE3 | UNKNOWN | Chemotherapy With or Without Bevacizumab or Lapatinib to Treat Operable Oesophagogastric Cancer |
| NCT00486668 | PHASE3 | UNKNOWN | A Study of AC Followed by a Combination of Paclitaxel Plus Trastuzumab or Lapatinib or Both Given Before Surgery to Patients With Operable HER2 Positive Invasive Breast Cancer |
| NCT00486954 | PHASE3 | COMPLETED | Lapatinib in Combination With Weekly Paclitaxel in Patients With ErbB2 Amplified Advanced Gastric Cancer |
| NCT00490139 | PHASE3 | COMPLETED | ALTTO (Adjuvant Lapatinib And/Or Trastuzumab Treatment Optimisation) Study; BIG 2-06/N063D |
| NCT00508274 | PHASE3 | TERMINATED | Lapatinib +Capecitabine Treatment for Advanced Metastatic Breast Cancer in Women From China |
| NCT00553358 | PHASE3 | COMPLETED | Neo ALTTO (Neoadjuvant Lapatinib and/or Trastuzumab Treatment Optimisation) Study |
| NCT00667251 | PHASE3 | COMPLETED | Chemotherapy and Lapatinib or Trastuzumab in Treating Women With HER2/Neu-Positive Metastatic Breast Cancer |
| NCT00680901 | PHASE3 | COMPLETED | LOGiC - Lapatinib Optimization Study in ErbB2 (HER2) Positive Gastric Cancer: A Phase III Global, Blinded Study Designed to Evaluate Clinical Endpoints and Safety of Chemotherapy Plus Lapatinib |
| NCT00688194 | PHASE3 | UNKNOWN | Fulvestrant With or Without Lapatinib and/or Aromatase Inhibitor Therapy in Treating Postmenopausal Women With Metastatic Breast Cancer That Progressed After Previous Aromatase Inhibitor Therapy |
| NCT00770809 | PHASE3 | COMPLETED | Paclitaxel and Trastuzumab With or Without Lapatinib in Treating Patients With Stage II or Stage III Breast Cancer That Can Be Removed by Surgery |
| NCT00820222 | PHASE3 | COMPLETED | Lapatinib Plus Capecitabine Versus Trastuzumab Plus Capecitabine in ErbB2 (HER2) Positive Metastatic Breast Cancer |
| NCT00829166 | PHASE3 | COMPLETED | A Study of Trastuzumab Emtansine Versus Capecitabine + Lapatinib in Participants With HER2-positive Locally Advanced or Metastatic Breast Cancer |
| NCT00949455 | PHASE2/PHASE3 | UNKNOWN | A Double Blind Randomised Study of Lapatinib and Placebo in Metastatic TCC of the Urothelium |
| NCT00968968 | PHASE3 | TERMINATED | Continued HER2 Suppression With Lapatinib Plus Trastuzumab Versus Trastuzumab Alone |
| NCT01104571 | PHASE3 | UNKNOWN | Trastuzumab or Lapatinib Ditosylate in Treating Women With Early Breast Cancer |
| NCT01160211 | PHASE3 | COMPLETED | A Study to Compare the Safety and Efficacy of an Aromatase Inhibitor in Combination With Lapatinib, Trastuzumab or Both for the Treatment of Hormone Receptor Positive, HER2+ Metastatic Breast Cancer |
| NCT01526369 | PHASE3 | COMPLETED | A Randomized Study of TH Versus THL in First Line Treatment of HER2-positive Metastatic Breast Cancer |
| NCT01619111 | PHASE3 | COMPLETED | DETECT III - A Multicenter, Phase III Study to Compare Standard Therapy +/- Lapatinib in HER2-ve MBC-Patients With HER2+ve CTCs |
| 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 |
| NCT02394496 | PHASE3 | UNKNOWN | Overcoming Endocrine Resistance in Metastatic Breast Cancer |
| NCT03084939 | PHASE3 | COMPLETED | Efficacy and Safety of Trastuzumab Emtansine in Chinese Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Locally Advanced or Metastatic Breast Cancer |
| NCT03085368 | PHASE2/PHASE3 | UNKNOWN | A Randomized Controlled Trial of HER-2 Positive Breast Cancer Patients Treated With Lapatinib vs Herceptin |
| NCT03500380 | PHASE2/PHASE3 | UNKNOWN | A Study of RC48-ADC Administered Intravenously to Patients With HER2-Positive Metastatic Breast Cancer With or Without Liver Metastases |
| NCT03523585 | PHASE3 | COMPLETED | DS-8201a in Pre-treated HER2 Breast Cancer That Cannot be Surgically Removed or Has Spread [DESTINY-Breast02] |
| NCT03784014 | PHASE3 | COMPLETED | Molecular Profiling of Advanced Soft-tissue Sarcomas |
| NCT04185649 | PHASE3 | UNKNOWN | The Efficacy and Safety of BAT8001 Injection for the Treatment of HER2-positive Advanced Breast Cancer |
| NCT00999804 | PHASE2 | ACTIVE_NOT_RECRUITING | Extension Study of Lapatinib Plus Herceptin With or Without Endocrine Therapy |
| NCT01273610 | PHASE2 | ACTIVE_NOT_RECRUITING | Tolerability of the Combination of Lapatinib and Trastuzumab in Adults Age 60 or Older With HER2 Positive Locally Advanced or Metastatic Breast Cancer |
| NCT00044343 | PHASE2 | COMPLETED | GW572016, An Oral Drug For Colorectal Cancer Patients Having Prior Therapy With 5-FU Plus CPT-11 And/Or Oxaliplatin |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 14 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.
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 |
| 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 |
| 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 |
Related Atlas pages
- Genes: EGFR, ERBB2
- Diseases: neoplasm, breast carcinoma, breast neoplasm, brain disorder, soft tissue sarcoma, head and neck cancer, head and neck neoplasm, HER2 positive breast carcinoma
- Drugs: Afatinib, Crizotinib, Dacomitinib, Gefitinib, Lazertinib, Mobocertinib, Selumetinib, Acalabrutinib, Astemizole, Bithionol, Bosutinib, Brigatinib, Cabozantinib, Chlorpromazine, Clotrimazole, Colistin, Dasatinib, Ebastine, Econazole, Erlotinib, Fluphenazine, Hexachlorophene, Ibrutinib, Imatinib, Miconazole, Mitoxantrone, Neratinib, Osimertinib, Ponatinib, Sorafenib, Tamoxifen, Tribromsalan, Tucatinib, Vandetanib, Zanubrutinib, Alisertib, Alvocidib, Candesartan, Canertinib, Cediranib, Enclomiphene, Masitinib, Poziotinib, Pyrotinib, Remibrutinib, Zongertinib
- Biomarker genes: CDKN1B, ERBB3, ERBB4, NRG1