Sorafenib
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Also known as SID50112741SID124893321baxSID103904444SID124893323SorafinibNexavarSorafenibSorafenibÊSorafenibÂSorafenib Tosylate
Summary
Sorafenib (CHEMBL1336) is an approved small-molecule antineoplastic agent (ATC L01EX02) targeting PDGFRB, KIT, and FLT3; indicated across 84 conditions including neoplasm and hepatocellular carcinoma; with CIViC clinical evidence for 73 variant-indication associations (e.g. FLT3 ITD in acute myeloid leukemia).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX02
- Targets: 13 (PDGFRB, KIT, FLT3…)
- Indications: 84 conditions
- Clinical trials: 568
- Precision-oncology evidence (CIViC): 73 variant–indication associations
- Chemistry: 464.8 Da · C21H16ClF3N4O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1336 |
| Name | Sorafenib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 216239 |
| ChEBI | CHEBI:50924 |
| ATC | L01EX02 |
| Molecular formula | C21H16ClF3N4O3 |
| Molecular weight | 464.8 |
| InChIKey | MLDQJTXFUGDVEO-UHFFFAOYSA-N |
SMILES: CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
IUPAC name: 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
ChEBI definition: A member of the class of phenylureas that is urea in which one of the nitrogens is substituted by a 4-chloro-3-trifluorophenyl group while the other is substituted by a phenyl group which, in turn, is substituted at the para position by a [2-(methylcarbamoyl)pyridin-4-yl]oxy group.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor, tyrosine kinase inhibitor, angiogenesis inhibitor, anticoronaviral agent, ferroptosis inducer.
Also known as: Sorafenib, sorafenib, SID50112741, SID124893321, bax, SID103904444, SORAFENIB, SID124893323, Sorafinib, Nexavar; Sorafenib, SorafenibÊ, SorafenibÂ
Parent form; salt/anhydrous children: CHEMBL1200485, CHEMBL1760433, CHEMBL4297490
Patent coverage: 22,883 distinct patent families (86,060 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 83,779 (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 |
|---|---|---|---|---|---|
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 7.24 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 7.17 | 0.5% | P10721 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 7.24 | 0.9% | P36888 |
| FGFR1 | fibroblast growth factor receptor 1 | Inhibition | 6.24 | 11.5% | P11362 |
| KDR | kinase insert domain receptor | Inhibition | 7.05 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 7.7 | 0.2% | P35916 |
| DDR2 | discoidin domain receptor tyrosine kinase 2 | Inhibition | 8 | 0% | Q16832 |
| BRAF | B-Raf proto-oncogene, serine/threonine kinase | Inhibition | 7.66 | 8.6% | P15056 |
| CDK19 | cyclin dependent kinase 19 | Inhibition | 6.99 | 0.1% | Q9BWU1 |
| CDK8 | cyclin dependent kinase 8 | Inhibition | 7 | 6.5% | P49336 |
| RAF1 | Raf-1 proto-oncogene, serine/threonine kinase | Inhibition | 8.22 | P04049 | |
| RET | ret proto-oncogene | Inhibition | 7.9 | 0.4% | P07949 |
| TNNI3K | TNNI3 interacting kinase | Binding | 6.55 | 0% | Q59H18 |
Broader ChEMBL bioactivity targets: 161 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase TAO2, Cyclin-dependent kinase-like 3, Serine/threonine-protein kinase A-Raf, Nuclear receptor ROR-gamma, Receptor-interacting serine/threonine-protein kinase 3, Receptor tyrosine-protein kinase erbB-2, 5-hydroxytryptamine receptor 2B, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor.
Bioactivity
ChEMBL activities: 902 potent at pChembl ≥ 5 of 915 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| KDR | 10.68 | Ki | 0.02 | nM | CHEMBL_ACT_6324306 |
| KDR | 10.22 | IC50 | 0.06 | nM | CHEMBL_ACT_24687339 |
| KDR | 9.92 | Ki | 0.12 | nM | CHEMBL_ACT_6324310 |
| KDR | 9.8 | IC50 | 0.16 | nM | CHEMBL_ACT_6324286 |
| EPHB4 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_17955698 |
| EPHB4 | 9.66 | IC50 | 0.22 | nM | CHEMBL_ACT_18947881 |
| EPHB4 | 9.66 | IC50 | 0.22 | nM | CHEMBL_ACT_19364908 |
| PDGFRB | 9.59 | IC50 | 0.26 | nM | CHEMBL_ACT_28855802 |
| KDR | 9.47 | IC50 | 0.34 | nM | CHEMBL_ACT_28855805 |
| TEK | 9.41 | IC50 | 0.39 | nM | CHEMBL_ACT_18947864 |
| TEK | 9.41 | IC50 | 0.39 | nM | CHEMBL_ACT_19364887 |
| KDR | 9.35 | IC50 | 0.45 | nM | CHEMBL_ACT_17955648 |
| KDR | 9.32 | IC50 | 0.48 | nM | CHEMBL_ACT_15625880 |
| KDR | 9.32 | IC50 | 0.48 | nM | CHEMBL_ACT_15765248 |
| KDR | 9.26 | IC50 | 0.55 | nM | CHEMBL_ACT_26150949 |
| ERBB2 | 9.25 | IC50 | 0.56 | nM | CHEMBL_ACT_28855799 |
| TEK | 9.08 | IC50 | 0.83 | nM | CHEMBL_ACT_17955673 |
| KDR | 9.07 | IC50 | 0.85 | nM | CHEMBL_ACT_15154943 |
| KDR | 9.07 | IC50 | 0.85 | nM | CHEMBL_ACT_18328417 |
| BRAF | 9 | IC50 | 1 | nM | CHEMBL_ACT_2397024 |
| RAF1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_2397034 |
| BRAF | 9 | IC50 | 1 | nM | CHEMBL_ACT_5199776 |
| KDR | 8.97 | IC50 | 1.06 | nM | CHEMBL_ACT_13868196 |
| KDR | 8.97 | IC50 | 1.06 | nM | CHEMBL_ACT_14544388 |
| KDR | 8.92 | IC50 | 1.2 | nM | CHEMBL_ACT_16395735 |
| KDR | 8.9 | IC50 | 1.27 | nM | CHEMBL_ACT_18355977 |
| FLT3 | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_19043595 |
| KDR | 8.85 | IC50 | 1.42 | nM | CHEMBL_ACT_16435131 |
| DDR1 | 8.82 | Kd | 1.5 | nM | CHEMBL_ACT_15240090 |
| DDR1 | 8.82 | Kd | 1.5 | nM | CHEMBL_ACT_2897532 |
Target pathways
Aggregated over 13 target gene(s): PDGFRB, KIT, FLT3, FGFR1, KDR, FLT4, DDR2, BRAF, CDK19, CDK8, RAF1, RET, TNNI3K.
Top Reactome pathways
157 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| RAF/MAP kinase cascade | 6 | BRAF, FGFR1, FLT3, KIT, PDGFRB, RET |
| PIP3 activates AKT signaling | 4 | FGFR1, FLT3, KIT, PDGFRB |
| Disease | 4 | BRAF, CDK19, CDK8, KIT |
| Constitutive Signaling by Aberrant PI3K in Cancer | 4 | FGFR1, FLT3, KIT, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | FGFR1, FLT3, KIT, PDGFRB |
| Developmental Biology | 3 | CDK19, CDK8, KIT |
| Signal Transduction | 3 | BRAF, CDK8, KIT |
| Diseases of signal transduction by growth factor receptors and second messengers | 3 | BRAF, CDK8, KIT |
| PI3K Cascade | 2 | FGFR1, FLT3 |
| Metabolism | 2 | CDK19, CDK8 |
| VEGF binds to VEGFR leading to receptor dimerization | 2 | FLT4, KDR |
| PPARA activates gene expression | 2 | CDK19, CDK8 |
| Generic Transcription Pathway | 2 | CDK8, KIT |
| Transcriptional regulation of white adipocyte differentiation | 2 | CDK19, CDK8 |
| Regulation of lipid metabolism by PPARalpha | 2 | CDK19, CDK8 |
| Metabolism of lipids | 2 | CDK19, CDK8 |
| Negative regulation of FGFR1 signaling | 2 | BRAF, FGFR1 |
| Infectious disease | 2 | CDK19, CDK8 |
| RAF activation | 2 | BRAF, RAF1 |
| MAP2K and MAPK activation | 2 | BRAF, RAF1 |
| Negative feedback regulation of MAPK pathway | 2 | BRAF, RAF1 |
| Negative regulation of MAPK pathway | 2 | BRAF, RAF1 |
| MAPK family signaling cascades | 2 | BRAF, KIT |
| MAPK1/MAPK3 signaling | 2 | BRAF, KIT |
| Signaling by moderate kinase activity BRAF mutants | 2 | BRAF, RAF1 |
| Signaling by high-kinase activity BRAF mutants | 2 | BRAF, RAF1 |
| Signaling by BRAF and RAF1 fusions | 2 | BRAF, RAF1 |
| Paradoxical activation of RAF signaling by kinase inactive BRAF | 2 | BRAF, RAF1 |
| RNA Polymerase II Transcription | 2 | CDK8, KIT |
| Gene expression (Transcription) | 2 | CDK8, KIT |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 13 |
| cell surface receptor protein tyrosine kinase signaling pathway | 7 |
| positive regulation of cell population proliferation | 7 |
| protein autophosphorylation | 7 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 7 |
| positive regulation of MAPK cascade | 7 |
| signal transduction | 6 |
| peptidyl-tyrosine phosphorylation | 6 |
| cell migration | 6 |
| positive regulation of cell migration | 5 |
| positive regulation of ERK1 and ERK2 cascade | 5 |
| negative regulation of apoptotic process | 5 |
| angiogenesis | 4 |
| MAPK cascade | 4 |
| positive regulation of MAP kinase activity | 3 |
Indications & clinical
Indications
84 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 |
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| renal cell carcinoma | 3 | MONDO:0005086 | EFO:0000681 |
| kidney neoplasm | 3 | MONDO:0021163 | EFO:0003865 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| thyroid gland carcinoma | 3 | MONDO:0015075 | EFO:0002892 |
| melanoma | 3 | MONDO:0005105 | EFO:0000756 |
| carcinoma | 3 | MONDO:0004993 | EFO:0000313 |
| thyroid tumor | 3 | MONDO:0015074 | EFO:0003841 |
| thyroid gland papillary carcinoma | 3 | MONDO:0005075 | EFO:0000641 |
| hepatoblastoma | 3 | MONDO:0018666 | EFO:1000292 |
| kidney cancer | 3 | MONDO:0002367 | MONDO:0002367 |
| breast neoplasm | 3 | MONDO:0021100 | MONDO:0007254 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| leukemia | 2 | MONDO:0005059 | EFO:0000565 |
| portal hypertension | 2 | MONDO:0005080 | EFO:0000666 |
| keloid | 2 | MONDO:0005348 | EFO:0004212 |
| osteosarcoma | 2 | MONDO:0009807 | EFO:0000637 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| testicular cancer | 2 | MONDO:0005447 | EFO:0005088 |
| metastatic prostate carcinoma | 2 | MONDO:0004956 | EFO:0000196 |
| myelodysplastic syndrome | 2 | MONDO:0018881 | EFO:0000198 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| chronic myeloid leukemia | 2 | MONDO:0011996 | EFO:0000339 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| mesothelioma | 2 | MONDO:0005065 | EFO:0000588 |
| neuroblastoma | 2 | MONDO:0005072 | EFO:0000621 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| rhabdomyosarcoma | 2 | MONDO:0005212 | EFO:0002918 |
| kidney disorder | 2 | MONDO:0005240 | EFO:0003086 |
| pancreatic neoplasm | 2 | MONDO:0021040 | EFO:0003860 |
| ovarian neoplasm | 2 | MONDO:0021068 | EFO:0003893 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| nasopharyngeal neoplasm | 2 | MONDO:0005375 | EFO:0004252 |
| upper aerodigestive tract neoplasm | 2 | MONDO:0005398 | EFO:0004284 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| thyroid gland follicular carcinoma | 2 | MONDO:0005034 | EFO:0000501 |
| adrenal cortex carcinoma | 2 | MONDO:0006639 | EFO:1000796 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| gastrointestinal stromal tumor | 2 | MONDO:0011719 | MONDO:0011719 |
| malignant pancreatic neoplasm | 2 | MONDO:0009831 | EFO:1000359 |
| bile duct carcinoma | 2 | MONDO:0005496 | EFO:0005540 |
| uveal melanoma | 2 | MONDO:0006486 | EFO:1000616 |
| salivary gland cancer | 2 | MONDO:0004669 | MONDO:0004669 |
| type 1 diabetes mellitus | 2 | MONDO:0005147 | MONDO:0005147 |
| gallbladder neoplasm | 2 | MONDO:0021253 | MONDO:0005411 |
| Hermansky-Pudlak syndrome | 2 | MONDO:0019312 | MONDO:0019312 |
| acute biphenotypic leukemia | 2 | MONDO:0020322 | MONDO:0019460 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| squamous cell carcinoma | 1 | MONDO:0005096 | EFO:0000707 |
| pulmonary arterial hypertension | 1 | MONDO:0015924 | EFO:0001361 |
| acute promyelocytic leukemia | 1 | MONDO:0012883 | EFO:0000224 |
| cervical carcinoma | 1 | MONDO:0005131 | EFO:0001061 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| anaplastic astrocytoma | 1 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 1 | MONDO:0016696 | EFO:0002501 |
| rectal cancer | 1 | MONDO:0006519 | EFO:1000657 |
| acute lymphoblastic leukemia | 1 | MONDO:0004967 | EFO:0000220 |
| small cell carcinoma | 1 | MONDO:0000402 | EFO:0008524 |
| thrombotic disease | 1 | MONDO:0000831 | MONDO:0000831 |
| Kaposi’s sarcoma | 1 | MONDO:0005055 | EFO:0000558 |
| brain neoplasm | 1 | MONDO:0021211 | EFO:0003833 |
| plasma cell neoplasm | 1 | MONDO:0004959 | EFO:0000200 |
| cholangiocarcinoma | 1 | MONDO:0019087 | EFO:0005221 |
| myeloid leukemia | 1 | MONDO:0004643 | MONDO:0004643 |
11 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 568.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 247 |
| PHASE1 | 130 |
| PHASE3 | 66 |
| PHASE1/PHASE2 | 65 |
| Not specified | 37 |
| PHASE2/PHASE3 | 13 |
| PHASE4 | 9 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01409499 | PHASE4 | COMPLETED | Palliative Treatments for Patients With Advanced Hepatocellular Carcinoma (HCC) |
| NCT01849588 | PHASE4 | TERMINATED | HCV-RNA Kinetics During Sorafenib for Hepatocellular Carcinoma (HCC) |
| NCT02504983 | PHASE4 | UNKNOWN | Clinical Trial for GALNT14 Genotype - Guided, Sorafenib in Combination With TACE in Hepatocellular Carcinoma |
| NCT02733809 | PHASE4 | UNKNOWN | Mechanism of Sorafenib Resistance in Patients With Advanced Hepatocellular Carcinoma |
| NCT02961998 | PHASE4 | COMPLETED | Preventive Effect of Celecoxib on Sorafenib-related Hand Foot Syndrome, a Single Center, Randomized Controlled Clinical Trail |
| NCT03178656 | PHASE4 | UNKNOWN | A Trial to Compare Surgery With Sorafenib for Hepatic Celluler Cancer With Portal Vein Tumor Thrombosis |
| NCT03518502 | PHASE4 | UNKNOWN | Sorafenib Monotherapy vs. TACE-sorafenib Sequential Therapy for HCC With Metastasis |
| NCT04127396 | PHASE4 | UNKNOWN | Lenvatinib Plus TACE Versus Sorafenib Plus TACE for HCC With PVTT |
| NCT05113290 | PHASE4 | UNKNOWN | Effect and Safety of Recombinant Human Adenovirus Type 5 in Advanced HCC With Stable Disease After Sorafenib Treatment |
| NCT03017326 | PHASE3 | ACTIVE_NOT_RECRUITING | Paediatric Hepatic International Tumour Trial |
| NCT03298451 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Durvalumab and Tremelimumab as First-line Treatment in Patients With Advanced Hepatocellular Carcinoma |
| NCT03533582 | PHASE3 | ACTIVE_NOT_RECRUITING | Cisplatin and Combination Chemotherapy in Treating Children and Young Adults With Hepatoblastoma or Liver Cancer After Surgery |
| NCT03755791 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Cabozantinib in Combination With Atezolizumab Versus Sorafenib in Participants With Advanced Hepatocellular Carcinoma (HCC) Who Have Not Received Previous Systemic Anticancer Therapy |
| NCT04039607 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Nivolumab in Combination With Ipilimumab in Participants With Advanced Hepatocellular Carcinoma |
| NCT04344158 | PHASE3 | ACTIVE_NOT_RECRUITING | A Phase III Clinical Trial of AK105 Injection Combined With Anlotinib Hydrochloride Capsules Versus Sorafenib in Subjects With Advanced Hepatocellular Carcinoma (HCC) |
| NCT04770896 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Atezolizumab With Lenvatinib or Sorafenib Versus Lenvatinib or Sorafenib Alone in Hepatocellular Carcinoma Previously Treated With Atezolizumab and Bevacizumab |
| NCT06972641 | PHASE2/PHASE3 | RECRUITING | Molecular Genetics Guide the Maintenance Therapy After Allogeneic Hematopoietic Stem Cell Transplantation |
| NCT07264010 | PHASE2/PHASE3 | NOT_YET_RECRUITING | Sorafenib Combined With Venetoclax as Pre-emptive Therapy Strategy for MRD+ AML: a Prospective, Single-arm, Multicenter Clinical Study |
| NCT07463651 | PHASE3 | RECRUITING | MRD-guided Maintenance Post-HCT: Gilteritini vs Sorafenib |
| NCT00110019 | PHASE3 | COMPLETED | Carboplatin and Paclitaxel With or Without Sorafenib Tosylate in Treating Patients With Stage III or Stage IV Melanoma That Cannot Be Removed by Surgery |
| NCT00326898 | PHASE3 | COMPLETED | Sunitinib Malate or Sorafenib Tosylate in Treating Patients With Kidney Cancer That Was Removed By Surgery |
| NCT00474786 | PHASE3 | COMPLETED | Temsirolimus Versus Sorafenib As Second-Line Therapy In Patients With Advanced RCC Who Have Failed First-Line Sunitinib |
| NCT00478114 | PHASE3 | COMPLETED | Efficacy and Safety of Sorafenib in Advanced Renal Cell Carcinoma (RCC) |
| NCT00492258 | PHASE3 | COMPLETED | Sorafenib in Treating Patients at Risk of Relapse After Undergoing Surgery to Remove Kidney Cancer |
| NCT00541021 | PHASE3 | UNKNOWN | Gemcitabine With or Without Sorafenib in Treating Patients With Locally Advanced or Metastatic Pancreatic Cancer |
| NCT00558636 | PHASE3 | TERMINATED | A Trial Comparing Safety and Efficacy of Carboplatin and Paclitaxel Plus or Minus Sorafenib (BAY43-9006) in Chemonaive Patients With Stage IIIB-IV Non-Small Cell Lung Cancer (NSCLC) |
| NCT00606866 | PHASE3 | COMPLETED | MRI Study of BAY 43-9006 in Metastatic Renal Cell Carcinoma |
| NCT00678392 | PHASE3 | COMPLETED | Axitinib (AG 013736) As Second Line Therapy For Metastatic Renal Cell Cancer |
| NCT00699374 | PHASE3 | TERMINATED | Study Of Sunitinib Malate Versus Sorafenib In Patients With Inoperable Liver Cancer |
| NCT00732914 | PHASE3 | COMPLETED | Sequential Study to Treat Renal Cell Carcinoma |
| NCT00858871 | PHASE3 | COMPLETED | First Line Hepato Cellular Carcinoma (HCC) |
| NCT00920816 | PHASE3 | COMPLETED | Axitinib (AG-013736) For the Treatment of Metastatic Renal Cell Cancer |
| NCT01004978 | PHASE3 | COMPLETED | Chemoembolization With or Without Sorafenib Tosylate in Treating Patients With Liver Cancer That Cannot Be Removed by Surgery |
| NCT01009593 | PHASE3 | TERMINATED | Efficacy and Tolerability of ABT-869 Versus Sorafenib in Advanced Hepatocellular Carcinoma (HCC) |
| NCT01015833 | PHASE3 | COMPLETED | Sorafenib Tosylate With or Without Doxorubicin Hydrochloride in Treating Patients With Locally Advanced or Metastatic Liver Cancer |
| NCT01030783 | PHASE3 | COMPLETED | A Study to Compare Tivozanib (AV-951) to Sorafenib in Subjects With Advanced Renal Cell Carcinoma |
| NCT01075555 | PHASE3 | COMPLETED | Sorafenib Tosylate With or Without Pravastatin in Treating Patients With Liver Cancer and Cirrhosis |
| NCT01076010 | PHASE3 | COMPLETED | An Extension Treatment Protocol for Subjects Who Have Participated in a Study of Tivozanib Versus Sorafenib in Kidney Carcinoma (Protocol AV-951-09-301). |
| NCT01135056 | PHASE3 | UNKNOWN | Study to Compare Selective Internal Radiation Therapy (SIRT) Versus Sorafenib in Locally Advanced Hepatocellular Carcinoma (HCC) |
| NCT01214343 | PHASE3 | UNKNOWN | Comparing Efficacy of Sorafenib Versus Sorafenib in Combination With Low-dose FP in Patients With Advanced HCC |
Clinical evidence (CIViC)
Variant × indication × effect (73 predictive associations from 80 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| FLT3 ITD | Acute Myeloid Leukemia | Sensitivity/Response | Sorafenib | CIViC B | EID1040 +2 |
| FLT3 ITD | Acute Myeloid Leukemia | Sensitivity/Response | Sorafenib + Hematopoietic Cell Transplantation | CIViC B | EID9069 +1 |
| CCND1 Amplification | Skin Melanoma | Sensitivity/Response | Sorafenib + Carboplatin + Paclitaxel | CIViC B | EID1495 |
| FLT3 D835 & I836 | Acute Myeloid Leukemia | Sensitivity/Response | Lestaurtinib + Quizartinib + Sorafenib + FLT3/ABL/Aurora Kinase Inhibitor KW-2449 | CIViC B | EID8925 |
| KIT Exon 11 Mutation OR KIT Exon 9 Mutation OR PDGFRA Exon 18 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sorafenib | CIViC B | EID11327 |
| KRAS Amplification | Skin Melanoma | Sensitivity/Response | Sorafenib + Docetaxel + Carboplatin | CIViC B | EID1497 |
| KRAS G12C OR KRAS G12D OR KRAS G13D OR RET M918T OR KRAS G12A OR KRAS G12V OR KRAS G12R OR KRAS Amplification OR KRAS G12S OR KRAS G13R OR KRAS G12P | Solid Tumors, Advanced | Sensitivity/Response | Sorafenib | CIViC B | EID12700 |
| KRAS Mutation | Hepatocellular Carcinoma | Sensitivity/Response | Sorafenib + Refametinib | CIViC B | EID1642 |
| RAF1 Amplification | Skin Melanoma | Sensitivity/Response | Paclitaxel + Sorafenib + Carboplatin | CIViC B | EID1496 |
| RET M918T | Medullary Thyroid Carcinoma | Sensitivity/Response | Sorafenib | CIViC B | EID1365 |
| FLT3 D835 | Acute Myeloid Leukemia | Resistance | Quizartinib + Sorafenib | CIViC B | EID1038 |
| FLT3 D835 | Acute Myeloid Leukemia | Resistance | Sorafenib | CIViC B | EID1039 |
| FLT3 TKD MUTATION | Acute Myeloid Leukemia | Resistance | Sorafenib | CIViC B | EID248 |
| HMOX1 EXPRESSION | Renal Cell Carcinoma | Resistance | Sorafenib + Sunitinib | CIViC B | EID829 |
| PROM1 EXPRESSION | Hepatocellular Carcinoma | Resistance | Sorafenib | CIViC B | EID926 |
| ARAF S214C | Lung Non-small Cell Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID17 +1 |
| FLT3 D835Y | Acute Myeloid Leukemia | Sensitivity/Response | Sorafenib | CIViC C | EID12625 +1 |
| KIAA1549::BRAF Fusion | Spindle Cell Sarcoma | Sensitivity/Response | Sorafenib + Bevacizumab + Temsirolimus | CIViC C | EID1664 +1 |
| AGK::BRAF Fusion | Melanoma | Sensitivity/Response | Sorafenib | CIViC C | EID723 |
| BRAF G469R | Lung Non-small Cell Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID1938 |
| BRAF G469V | Lung Non-small Cell Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID1939 |
| FGF3 Amplification | Hepatocellular Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID1966 |
| FLT3 Amplification | Colorectal Cancer | Sensitivity/Response | Sorafenib | CIViC C | EID7103 |
| KIT D820E | Thymic Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID7356 |
| KIT P577_D579DEL | Thymic Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID7360 |
| ZHX2 Overexpression | Papillary Renal Cell Carcinoma | Sensitivity/Response | Sorafenib | CIViC C | EID9114 |
| FLT3 D835H | Acute Myeloid Leukemia | Resistance | Sorafenib | CIViC C | EID1556 |
| FLT3 ITD AND FLT3 D835Y | Acute Myeloid Leukemia | Resistance | Sorafenib | CIViC C | EID247 |
| BRAF V600E | Melanoma | Sensitivity/Response | Sorafenib | CIViC D | EID2122 +1 |
| ARID1A Loss | Liver Cancer | Sensitivity/Response | Sorafenib | CIViC D | EID7328 |
+43 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 40 clinical and 80 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.
284 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Afatinib | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| FORETINIB | ChEMBL | Phase 2 | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| Selumetinib | PubChem | Approved | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, RAF1, RET, TNNI3K |
| DORAMAPIMOD | ChEMBL | Phase 2 | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET |
| RAF-265 | ChEMBL | Phase 2 | BRAF, CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| ERLOTINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, DDR2, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| R-406 | ChEMBL | Phase 2 | BRAF, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| AXITINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| PONATINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, CDK8, DDR2, FGFR1, FLT3, KDR, KIT, PDGFRB, RET |
| QUIZARTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, DDR2, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| VANDETANIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| DASATINIB | ChEMBL | Phase 4 (approved) | BRAF, DDR2, FGFR1, FLT3, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| LESTAURTINIB | ChEMBL | Phase 3 | CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| LINIFANIB | ChEMBL | Phase 3 | CDK19, CDK8, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| MOTESANIB | ChEMBL | Phase 3 | BRAF, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RAF1, RET, TNNI3K |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, DDR2, FLT3, KDR, KIT, PDGFRB, RAF1, TNNI3K |
| MIDOSTAURIN | ChEMBL + PubChem | Phase 4 (approved) | CDK19, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TNNI3K |
| NILOTINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, DDR2, FLT3, KIT, PDGFRB, RAF1, RET, TNNI3K |
| REBASTINIB | ChEMBL | Phase 2 | BRAF, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, RAF1, RET |
| TOZASERTIB | ChEMBL | Phase 2 | CDK19, DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| Idelalisib | PubChem | Approved | BRAF, DDR2, FGFR1, FLT3, FLT4, KIT, PDGFRB, RAF1, RET |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| CEDIRANIB | ChEMBL | Phase 3 | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| DOVITINIB | ChEMBL | Phase 3 | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| CEP-32496 | ChEMBL | Phase 2 | BRAF, DDR2, FLT3, KDR, KIT, PDGFRB, RAF1, RET |
| ILORASERTIB | ChEMBL | Phase 2 | CDK8, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| SU-014813 | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| BOSUTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, DDR2, FLT3, KIT, PDGFRB, RET, TNNI3K |
| CABOZANTINIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, RET |
| ENTRECTINIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, RET |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | BRAF, FGFR1, FLT3, FLT4, KDR, KIT, RET |
| LENVATINIB | ChEMBL | Phase 4 (approved) | DDR2, FGFR1, FLT4, KDR, KIT, PDGFRB, RET |
| SEMAXANIB | ChEMBL | Phase 3 | FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| VATALANIB | ChEMBL | Phase 3 | CDK19, CDK8, FLT4, KDR, KIT, PDGFRB, RET |
| CENISERTIB | ChEMBL | Phase 2 | FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| DANUSERTIB | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, RET |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | DDR2, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| MILCICLIB | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, FLT4, KIT, PDGFRB, RET |
| OSI-632 | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, FLT4, KDR, PDGFRB, RET |
| TANDUTINIB | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, FLT4, KDR, KIT, PDGFRB |
| Binimetinib | PubChem | Approved | BRAF, DDR2, FGFR1, FLT3, KDR, PDGFRB, RET |
| Fostamatinib | ChEMBL + PubChem | Phase 4 (approved) | BRAF, DDR2, FGFR1, FLT3, PDGFRB, RET |
| PEXIDARTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, DDR2, FLT3, KDR, KIT, PDGFRB |
| RUXOLITINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, CDK19, DDR2, KIT, RET, TNNI3K |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT3, FLT4, KDR, KIT, RET |
| BRIVANIB | ChEMBL | Phase 3 | FGFR1, FLT4, KDR, KIT, PDGFRB, RET |
| CANERTINIB | ChEMBL | Phase 3 | FLT3, KDR, KIT, PDGFRB, RET, TNNI3K |
| SARACATINIB | ChEMBL | Phase 3 | DDR2, FLT3, KDR, KIT, PDGFRB, RET |
| ENMD-2076 | ChEMBL | Phase 2 | DDR2, FGFR1, FLT3, KDR, KIT, RET |
| LUCITANIB | ChEMBL | Phase 2 | DDR2, FGFR1, FLT4, KDR, PDGFRB, RET |
| MK-2461 | ChEMBL | Phase 2 | FGFR1, FLT3, FLT4, KDR, PDGFRB, RET |
| dacomitinib | PubChem | Approved | BRAF, DDR2, FGFR1, FLT3, PDGFRB, RET |
| Trametinib | PubChem | Approved | BRAF, DDR2, FGFR1, FLT3, PDGFRB, RET |
Related Atlas pages
- Genes: PDGFRB, KIT, FLT3, FGFR1, KDR, FLT4, DDR2, BRAF, CDK19, CDK8, RAF1, RET, TNNI3K
- Diseases: neoplasm, hepatocellular carcinoma, renal cell carcinoma, kidney neoplasm, non-small cell lung carcinoma, thyroid gland carcinoma, melanoma, carcinoma, thyroid tumor, thyroid gland papillary carcinoma, hepatoblastoma, kidney cancer, breast neoplasm, acute myeloid leukemia by FAB classification, cutaneous melanoma, gastrointestinal stromal tumor, medullary thyroid gland carcinoma, spindle cell sarcoma, colorectal carcinoma, thymic carcinoma, papillary renal cell carcinoma, liver cancer
- Drugs: Afatinib, Crizotinib, Pazopanib, Selumetinib, Gefitinib, Erlotinib, Fedratinib, Axitinib, Ponatinib, Quizartinib, Regorafenib, Sunitinib, Vandetanib, Dasatinib, Lestaurtinib, Linifanib, Motesanib, Imatinib, Midostaurin, Nilotinib, Idelalisib, Nintedanib, Tivozanib, Cediranib, Dovitinib, Bosutinib, Cabozantinib, Entrectinib, Infigratinib, Lenvatinib, Semaxanib, Vatalanib, Binimetinib, Fostamatinib, Pexidartinib, Ruxolitinib, Brigatinib, Brivanib, Canertinib, Saracatinib, dacomitinib, Trametinib
- Biomarker genes: ARAF, ARID1A, FGF19, FGF3, PROM1, RNASE3