Vandetanib
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Also known as CaprelsaGNF-PF-2188NSC-744325NSC-760766ZactimaZD-64ZD-6474ZD6474SID50112766SID103905338SID124893338SID144206064SID170465617VANDETANIB (ZD6474)VandetinibVandetanibÊVandetanibÂ
Summary
Vandetanib (CHEMBL24828) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EX04) targeting EGFR, KDR, and RET; indicated across 53 conditions including thyroid gland carcinoma and thyroid tumor; with CIViC clinical evidence for 8 variant-indication associations (e.g. RET Fusion in lung non-small cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX04
- Targets: 3 (EGFR, KDR, RET)
- Indications: 53 conditions
- Clinical trials: 102
- Precision-oncology evidence (CIViC): 8 variant–indication associations
- Chemistry: 475.4 Da · C22H24BrFN4O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL24828 |
| Name | Vandetanib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 3081361 |
| ChEBI | CHEBI:49960 |
| ATC | L01EX04 |
| Molecular formula | C22H24BrFN4O2 |
| Molecular weight | 475.4 |
| InChIKey | UHTHHESEBZOYNR-UHFFFAOYSA-N |
SMILES: CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC
IUPAC name: N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
ChEBI definition: A quinazoline that is 7-[(1-methylpiperidin-4-yl)methoxy]quinazoline bearing additional methoxy and 4-bromo-2-fluorophenylamino substituents at positions 6 and 4 respectively. Used for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease.
Pharmacological roles (ChEBI): tyrosine kinase inhibitor, antineoplastic agent.
Also known as: Caprelsa, GNF-PF-2188, NSC-744325, NSC-760766, Vandetanib, Zactima, ZD-64, ZD-6474, ZD6474, GNF-Pf-2188, vandetanib, SID50112766
Parent form; salt/anhydrous children: CHEMBL533849
Patent coverage: 12,325 distinct patent families (42,230 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 35,115 (83%) 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 | 6.52 | 17.5% | P00533 |
| KDR | kinase insert domain receptor | Inhibition | 8 | 1.1% | P35968 |
| RET | ret proto-oncogene | Inhibition | 7 | 0.4% | P07949 |
Broader ChEMBL bioactivity targets: 137 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Nuclear receptor ROR-gamma, Hormonally up-regulated neu tumor-associated kinase, Receptor tyrosine-protein kinase erbB-2, 5-hydroxytryptamine receptor 2B, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Alpha-2A adrenergic receptor, Vascular endothelial growth factor receptor 1.
Bioactivity
ChEMBL activities: 499 potent at pChembl ≥ 5 of 512 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FLT4 | 9.96 | IC50 | 0.11 | nM | CHEMBL_ACT_24867122 |
| RET | 9.89 | IC50 | 0.13 | nM | CHEMBL_ACT_24867102 |
| SRC | 9.1 | IC50 | 0.79 | nM | CHEMBL_ACT_24789092 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_24867256 |
| RET | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_27908483 |
| KDR | 8.38 | AC50 | 4.2 | nM | CHEMBL_ACT_25167978 |
| RIPK2 | 8.34 | Kd | 4.6 | nM | CHEMBL_ACT_2907550 |
| RIPK2 | 8.34 | Kd | 4.6 | nM | CHEMBL_ACT_7578574 |
| EGFR | 8.32 | Kd | 4.8 | nM | CHEMBL_ACT_2898732 |
| EGFR | 8.32 | Kd | 4.8 | nM | CHEMBL_ACT_7580571 |
| EGFR | 8.23 | Kd | 5.9 | nM | CHEMBL_ACT_2898808 |
| EGFR | 8.23 | Kd | 5.9 | nM | CHEMBL_ACT_7580573 |
| KDR | 8.2 | Ki | 6.31 | nM | CHEMBL_ACT_9630093 |
| RET | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_24867251 |
| EGFR | 8.1 | Kd | 7.9 | nM | CHEMBL_ACT_2898884 |
| EGFR | 8.1 | Kd | 7.9 | nM | CHEMBL_ACT_7580575 |
| EGFR | 8.06 | Kd | 8.7 | nM | CHEMBL_ACT_2904706 |
| EGFR | 8.06 | Kd | 8.7 | nM | CHEMBL_ACT_7580577 |
| KDR | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_1516652 |
| RET | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_22952710 |
| EGFR | 8.05 | Kd | 8.9 | nM | CHEMBL_ACT_2898922 |
| ABL1 | 8.05 | Kd | 9 | nM | CHEMBL_ACT_7580564 |
| EGFR | 8.05 | Kd | 8.9 | nM | CHEMBL_ACT_7580576 |
| EGFR | 8.02 | Kd | 9.5 | nM | CHEMBL_ACT_19218710 |
| EGFR | 8.02 | Kd | 9.5 | nM | CHEMBL_ACT_2898694 |
| EGFR | 8.02 | Kd | 9.6 | nM | CHEMBL_ACT_2898770 |
| EGFR | 8.02 | Kd | 9.5 | nM | CHEMBL_ACT_7580570 |
| EGFR | 8.02 | Kd | 9.6 | nM | CHEMBL_ACT_7580572 |
| EGFR | 8.01 | AC50 | 9.8 | nM | CHEMBL_ACT_25168844 |
| ABL1 | 8.01 | Kd | 9.8 | nM | CHEMBL_ACT_7580557 |
Target pathways
Aggregated over 3 target gene(s): EGFR, KDR, RET.
Top Reactome pathways
48 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| RAF/MAP kinase cascade | 2 | EGFR, RET |
| 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 |
| Neuropilin interactions with VEGF and VEGFR | 1 | KDR |
| VEGF binds to VEGFR leading to receptor dimerization | 1 | KDR |
| GRB2 events in ERBB2 signaling | 1 | EGFR |
| PI3K events in ERBB2 signaling | 1 | EGFR |
| EGFR interacts with phospholipase C-gamma | 1 | EGFR |
| Integrin cell surface interactions | 1 | KDR |
| EGFR Transactivation by Gastrin | 1 | EGFR |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | EGFR |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| Signal transduction by L1 | 1 | EGFR |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| Constitutive Signaling by EGFRvIII | 1 | EGFR |
| Inhibition of Signaling by Overexpressed EGFR | 1 | EGFR |
| ERBB2 Regulates Cell Motility | 1 | EGFR |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | EGFR |
| ERBB2 Activates PTK6 Signaling | 1 | EGFR |
| RET signaling | 1 | RET |
| Cargo recognition for clathrin-mediated endocytosis | 1 | EGFR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of cell migration | 3 |
| positive regulation of MAPK cascade | 3 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 3 |
| protein phosphorylation | 3 |
| cell surface receptor protein tyrosine kinase signaling pathway | 3 |
| positive regulation of protein phosphorylation | 2 |
| signal transduction | 2 |
| positive regulation of cell population proliferation | 2 |
| neuron differentiation | 2 |
| negative regulation of apoptotic process | 2 |
| epithelial cell proliferation | 2 |
| positive regulation of epithelial cell proliferation | 2 |
| positive regulation of ERK1 and ERK2 cascade | 2 |
| MAPK cascade | 2 |
| cell morphogenesis | 1 |
Indications & clinical
Indications
53 indications (7 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 |
|---|---|---|---|
| thyroid gland carcinoma | 4 | MONDO:0015075 | EFO:0002892 |
| thyroid tumor | 4 | MONDO:0015074 | EFO:0003841 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| thyroid gland papillary carcinoma | 4 | MONDO:0005075 | EFO:0000641 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| lung neoplasm | 3 | MONDO:0021117 | MONDO:0008903 |
| mesothelioma | 2 | MONDO:0005065 | EFO:0000588 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| prostate carcinoma | 2 | MONDO:0005159 | EFO:0001663 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| clear cell renal carcinoma | 2 | MONDO:0005005 | EFO:0000349 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| colorectal adenocarcinoma | 2 | MONDO:0005008 | EFO:0000365 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| oligoastrocytoma | 2 | MONDO:0016702 | EFO:0000630 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| anaplastic astrocytoma | 2 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 2 | MONDO:0016696 | EFO:0002501 |
| breast neoplasm | 2 | MONDO:0021100 | EFO:0003869 |
| head and neck cancer | 2 | MONDO:0005627 | EFO:0006859 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| thyroid gland follicular carcinoma | 2 | MONDO:0005034 | EFO:0000501 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| peritoneal neoplasm | 2 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| ureter cancer | 2 | MONDO:0008627 | MONDO:0008627 |
| gastrointestinal stromal tumor | 2 | MONDO:0011719 | MONDO:0011719 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| neuroblastoma | 1 | MONDO:0005072 | EFO:0000621 |
| carcinoma of esophagus | 1 | MONDO:0019086 | EFO:0002916 |
| diffuse intrinsic pontine glioma | 1 | MONDO:0006033 | EFO:1000026 |
| central nervous system neoplasm | 1 | MONDO:0006130 | EFO:1000158 |
| rectal cancer | 1 | MONDO:0006519 | EFO:1000657 |
| glioma | 1 | MONDO:0021042 | MONDO:0100342 |
| adrenal gland pheochromocytoma | 1 | MONDO:0004974 | EFO:0000239 |
| carcinoma | 1 | MONDO:0004993 | EFO:0000313 |
| paraganglioma | 1 | MONDO:0000448 | EFO:1000453 |
| adenocarcinoma | 1 | MONDO:0004970 | MONDO:0003219 |
11 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 102.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 49 |
| PHASE1 | 33 |
| PHASE3 | 9 |
| PHASE1/PHASE2 | 6 |
| Not specified | 4 |
| PHASE4 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01496313 | PHASE4 | COMPLETED | To Compare The Effects Of Two Doses Of Vandetanib In Patients With Advanced Medullary Thyroid Cancer |
| NCT04211337 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer |
| NCT00312377 | PHASE3 | COMPLETED | ZACTIMA (an Anti-EGFR / Anti-VEGF Agent) Combined With Docetaxel Compared to Docetaxel in Non-small Cell Lung Cancer |
| NCT00364351 | PHASE3 | COMPLETED | Efficacy Trial Comparing ZD6474 With Erlotinib in NSCLC After Failure of at Least One Prior Chemotherapy |
| NCT00404924 | PHASE3 | COMPLETED | ZD6474 (ZACTIMA™) Phase III Study in EGFR Failures |
| NCT00410761 | PHASE3 | COMPLETED | An Efficacy Study Comparing ZD6474 to Placebo in Medullary Thyroid Cancer |
| NCT00418886 | PHASE3 | COMPLETED | Efficacy Study Comparing ZD6474 in Combination With Pemetrexed and Pemetrexed Alone in 2nd Line NSCLC Patients |
| NCT01298323 | PHASE3 | COMPLETED | Study to Determine if Contacting Patients With MTC More Frequently Results in Earlier Detection and Treatment of Signs and Symptoms of AEs and Thus a Decrease in the Percentage of Time Patients Experience AEs During First 12 Months on Vandetanib Treatment |
| NCT01876784 | PHASE3 | COMPLETED | Evaluation of Efficacy, Safety of Vandetanib in Patients With Differentiated Thyroid Cancer |
| NCT04760288 | PHASE3 | WITHDRAWN | A Study of Pralsetinib Versus Standard of Care (SOC) for Treatment of RET-Mutated Medullary Thyroid Cancer (MTC). |
| NCT02299999 | PHASE2 | ACTIVE_NOT_RECRUITING | SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer |
| NCT06482086 | PHASE2 | RECRUITING | Efficacy of Organoid-Based Drug Screening to Guide Treatment for Locally Advanced Thyroid Cancer |
| NCT00034918 | PHASE2 | COMPLETED | This Study is to Assess the Efficacy and Safety of ZD6474 in Subjects With Metastatic Breast Cancer |
| NCT00047788 | PHASE2 | COMPLETED | Efficacy Study of ZD6474 to Treat Multiple Myeloma Cancer |
| NCT00047840 | PHASE2 | COMPLETED | This Study is to Assess the Efficacy and Safety of ZD6474 in Subjects With Non-small Cell Lung Cancer. |
| NCT00059722 | PHASE2 | COMPLETED | This Study is to Compare the Efficacy of ZD6474 and ZD1839 in Subjects With NSCLC. |
| NCT00066313 | PHASE2 | COMPLETED | ZD6474 in Treating Patients With Small Cell Lung Cancer |
| NCT00071188 | PHASE2 | COMPLETED | ZD6474 Alone or in Combination With Paclitaxel and Carboplatin in Subjects With Previously Untreated Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) |
| NCT00098345 | PHASE2 | COMPLETED | Efficacy and Tolerability of ZD6474 in Patients With Thyroid Cancer |
| NCT00290537 | PHASE2 | TERMINATED | Phase II Study of ZD6474 in Advanced NSCLC |
| NCT00358956 | PHASE2 | COMPLETED | A Study To Assess ZD6474 (ZACTIMA™) Monotherapy In Locally Advanced or Metastatic Hereditary Medullary Thyroid Cancer |
| NCT00402896 | PHASE2 | TERMINATED | Malignant Pleural Effusion With ZD6474 |
| NCT00410189 | PHASE2 | COMPLETED | BATTLE Program: ZD6474 in Previously Treated Subjects With NSCLC |
| NCT00441142 | PHASE1/PHASE2 | COMPLETED | Zactima With Temodar During Radiation Treatment for Newly Diagnosed Stage IV Brain Tumors |
| NCT00445549 | PHASE2 | TERMINATED | Vandetanib to Treat Women With Ovarian, Fallopian Tube, or Primary Peritoneal Cancer |
| NCT00454116 | PHASE2 | COMPLETED | A Phase II, Double Blind Study of 2 Doses of ZACTIMA™(ZD6474) in Combination With FOLFIRI vs FOLFIRI Alone for the Treatment of Colorectal Cancer in Patients |
| NCT00459043 | PHASE2 | COMPLETED | Docetaxel in Combination With Zactima (ZD6474) in Patients With Locally Advanced Squamous Cell Carcinoma of the the Head and Neck |
| NCT00459121 | PHASE2 | TERMINATED | Vandetanib, Carboplatin, and Paclitaxel in Treating Patients With Stage I, Stage II, or Stage III Non-Small Cell Lung Cancer That Can Be Removed by Surgery |
| NCT00481845 | PHASE2 | TERMINATED | Phase 2 Anastrozole and Vandetanib (ZD6474) in Neoadjuvant Treatment of Postmenopausal Hormone Receptor-Positive Breast Cancer |
| NCT00494481 | PHASE2 | COMPLETED | E3 Breast Cancer Taxotere Combination |
| NCT00498797 | PHASE2 | COMPLETED | E3-Hormone Refractory Prostrate Cancer Taxotere Combination |
| NCT00500292 | PHASE2 | COMPLETED | A Phase II Study of 2 Doses of ZD6474 (Vandetanib) in Combination With FOLFOX vs FOLFOX Alone for the Treatment of Colorectal Cancer |
| NCT00508001 | PHASE2 | COMPLETED | Phase II Study of Best Support Care (BSC) Plus ZD6474(Vandetanib) in Patients With Inoperable Hepatocellular Carcinoma (HCC) |
| NCT00514046 | PHASE1/PHASE2 | COMPLETED | Vandetanib to Treat Children and Adolescents With Medullary Thyroid Cancer |
| NCT00537095 | PHASE2 | COMPLETED | Efficacy and Safety of Vandetanib (ZD6474) in Patients With Metastatic Papillary or Follicular Thyroid Cancer |
| NCT00597116 | PHASE2 | TERMINATED | An Efficacy and Safety Study With Vandetanib to Treat Inoperable or Relapsed Malignant Mesothelioma |
| NCT00613626 | PHASE2 | COMPLETED | Cisplatin + Etoposide +/- Concurrent ZD6474 in Previously Untreated Extensive Stage Small Cell Lung Cancer |
| NCT00659438 | PHASE2 | COMPLETED | Efficacy and Safety of Zactima™ in Patients With Castration-refractory Metastatic Prostate Cancer |
| NCT00683787 | PHASE2 | TERMINATED | Docetaxel With or Without Vandetanib in Treating Patients With Metastatic Stomach Cancer or Gastroesophageal Junction Cancer |
| NCT00686036 | PHASE2 | TERMINATED | Trial Assessing Zactima Against Placebo in Prostate Cancer Subjects Undergoing Intermittent Androgen Deprivation Hormonal Therapy |
Clinical evidence (CIViC)
Variant × indication × effect (8 predictive associations from 9 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| RET Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Vandetanib | CIViC B | EID4848 +1 |
| SDHB Mutation | Hereditary Renal Cell Carcinoma | Sensitivity/Response | Vandetanib + Metformin | CIViC B | EID7959 |
| AKT2 Amplification | Lung Adenocarcinoma | Sensitivity/Response | Vandetanib + Everolimus | CIViC C | EID1621 |
| KIF5B::RET Fusion | Lung Adenocarcinoma | Sensitivity/Response | Everolimus + Vandetanib | CIViC C | EID1622 |
| KIF5B::RET Fusion | Lung Adenocarcinoma | Sensitivity/Response | Vandetanib | CIViC C | EID698 |
| RET Overexpression | Estrogen-receptor Negative Breast Cancer | Sensitivity/Response | Vandetanib | CIViC D | EID2992 |
| RET Overexpression | Breast Cancer | Sensitivity/Response | Vandetanib | CIViC D | EID740 |
| KIF5B::RET Fusion AND RET G810A | Lung Non-small Cell Carcinoma | Resistance | Vandetanib | CIViC D | EID4852 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 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.
282 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR, RET |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR, RET |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR, RET |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR, RET |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR, RET |
| ALECTINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| AXITINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| CERITINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| DASATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| PONATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| SORAFENIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| SUNITINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| VEMURAFENIB | ChEMBL | Phase 4 (approved) | EGFR, KDR, RET |
| ALISERTIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| BARASERTIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| BRIVANIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| CANERTINIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| CEDIRANIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| DOVITINIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| LESTAURTINIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| LINIFANIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| MOTESANIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| QUERCETIN | ChEMBL | Phase 3 | EGFR, KDR, RET |
| SARACATINIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| VATALANIB | ChEMBL | Phase 3 | EGFR, KDR, RET |
| AEE-788 | ChEMBL | Phase 2 | EGFR, KDR, RET |
| BEMCENTINIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| CENISERTIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| CEP-32496 | ChEMBL | Phase 2 | EGFR, KDR, RET |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| DORAMAPIMOD | ChEMBL | Phase 2 | EGFR, KDR, RET |
| FORETINIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| ILORASERTIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| OSI-632 | ChEMBL | Phase 2 | EGFR, KDR, RET |
| R-406 | ChEMBL | Phase 2 | EGFR, KDR, RET |
| SU-014813 | ChEMBL | Phase 2 | EGFR, KDR, RET |
| TOZASERTIB | ChEMBL | Phase 2 | EGFR, KDR, RET |
| Binimetinib | PubChem | Approved | EGFR, KDR, RET |
| DACOMITINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, RET |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | EGFR, KDR |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, RET |
| SELPERCATINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, RET |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | EGFR, KDR |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | EGFR, RET |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | KDR, RET |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | EGFR, RET |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | EGFR, KDR |
| IMATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | KDR, RET |
| LAPATINIB | ChEMBL | Phase 4 (approved) | EGFR, RET |
| LENVATINIB | ChEMBL | Phase 4 (approved) | KDR, RET |
| NERATINIB | ChEMBL | Phase 4 (approved) | EGFR, KDR |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | EGFR, KDR |
Related Atlas pages
- Genes: EGFR, KDR, RET
- Diseases: thyroid gland carcinoma, thyroid tumor, neoplasm, thyroid gland papillary carcinoma, non-small cell lung carcinoma, lung neoplasm, hereditary renal cell carcinoma, lung adenocarcinoma, estrogen-receptor negative breast cancer, breast carcinoma
- Drugs: Afatinib, Crizotinib, Gefitinib, Pazopanib, Selumetinib, Alectinib, Axitinib, Brigatinib, Cabozantinib, Ceritinib, Dasatinib, Erlotinib, Fedratinib, Ibrutinib, Midostaurin, Ponatinib, Sorafenib, Sunitinib, Vemurafenib, Alisertib, Barasertib, Brivanib, Canertinib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Motesanib, Quercetin, Saracatinib, Vatalanib, Binimetinib, Dacomitinib, Regorafenib, Selpercatinib, Abemaciclib, Acalabrutinib, Bosutinib, Entrectinib, Gilteritinib, Hexachlorophene, Imatinib, Infigratinib, Lapatinib, Lenvatinib, Neratinib, Niclosamide