Regorafenib
drugOn this page
Also known as BAY-734506BAY-734506 MONOHYDRATERegorafenib anhydrousRegorafenib hydrateRegorafenib monohydrateStivargaSID137275982
Summary
Regorafenib (CHEMBL1946170) is an approved small-molecule antineoplastic agent (ATC L01EX05) targeting KDR and BRAF; indicated across 41 conditions including colorectal adenocarcinoma and neoplasm; with CIViC clinical evidence for 50 variant-indication associations (e.g. KIT Exon 11 Mutation in gastrointestinal stromal tumor).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX05
- Targets: 2 (KDR, BRAF)
- Indications: 41 conditions
- Clinical trials: 241
- Precision-oncology evidence (CIViC): 50 variant–indication associations
- Chemistry: 482.8 Da · C21H15ClF4N4O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1946170 |
| Name | Regorafenib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 11167602 |
| ChEBI | CHEBI:68647 |
| ATC | L01EX05 |
| Molecular formula | C21H15ClF4N4O3 |
| Molecular weight | 482.8 |
| InChIKey | FNHKPVJBJVTLMP-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)F
IUPAC name: 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
ChEBI definition: A pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previously received chemotherapy, anti-EGFR or anti-VEGF therapy.
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, hepatotoxic agent.
Also known as: BAY-734506, BAY-734506 MONOHYDRATE, Regorafenib, Regorafenib anhydrous, Regorafenib hydrate, Regorafenib monohydrate, Stivarga, REGORAFENIB, SID137275982, regorafenib
Patent coverage: 5,357 distinct patent families (12,678 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 12,094 (95%) 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 |
|---|---|---|---|---|---|
| KDR | kinase insert domain receptor | Inhibition | 7.9 | 1.1% | P35968 |
| BRAF | B-Raf proto-oncogene, serine/threonine kinase | Inhibition | 7.55 | 8.6% | P15056 |
Broader ChEMBL bioactivity targets: 50 (assay-derived). Sample: Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, RAF proto-oncogene serine/threonine-protein kinase, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Amine oxidase [flavin-containing] A, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Retinoic acid receptor gamma.
Bioactivity
ChEMBL activities: 117 potent at pChembl ≥ 5 of 122 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| EPHX2 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_13349258 |
| BRAF | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239343 |
| TEK | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239344 |
| P35917 | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239345 |
| P35918 | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239346 |
| FLT1 | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239347 |
| PDGFRB | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239348 |
| RAF1 | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239349 |
| FGFR1 | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_19239350 |
| RET | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_24867135 |
| RET | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_24906930 |
| RET | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_25871811 |
| RET | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_26137494 |
| RAF1 | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_24867133 |
| RAF1 | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_25871810 |
| RAF1 | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_26137495 |
| RAF1 | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_29065624 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_24788770 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_18854163 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_19449716 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_24867138 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_25663322 |
| P35918 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_25871806 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_26001069 |
| P35918 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_26137490 |
| KDR | 8.38 | Ki | 4.2 | nM | CHEMBL_ACT_27790676 |
| KDR | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_29065620 |
| PDGFRA | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_29279127 |
| KDR | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_25484193 |
| KDR | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_19238842 |
Target pathways
Aggregated over 2 target gene(s): KDR, BRAF.
Top Reactome pathways
46 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Spry regulation of FGF signaling | 1 | BRAF |
| Signal Transduction | 1 | BRAF |
| Disease | 1 | BRAF |
| Signaling by NTRKs | 1 | BRAF |
| Prolonged ERK activation events | 1 | BRAF |
| Frs2-mediated activation | 1 | BRAF |
| ARMS-mediated activation | 1 | BRAF |
| Signaling by NTRK1 (TRKA) | 1 | BRAF |
| Signalling to ERKs | 1 | BRAF |
| Signalling to p38 via RIT and RIN | 1 | BRAF |
| Signaling by FGFR | 1 | BRAF |
| Neuropilin interactions with VEGF and VEGFR | 1 | KDR |
| VEGF binds to VEGFR leading to receptor dimerization | 1 | KDR |
| Integrin cell surface interactions | 1 | KDR |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| Negative regulation of FGFR1 signaling | 1 | BRAF |
| Negative regulation of FGFR2 signaling | 1 | BRAF |
| Negative regulation of FGFR3 signaling | 1 | BRAF |
| Negative regulation of FGFR4 signaling | 1 | BRAF |
| Signaling by FGFR1 | 1 | BRAF |
| Signaling by FGFR2 | 1 | BRAF |
| Signaling by FGFR3 | 1 | BRAF |
| Signaling by FGFR4 | 1 | BRAF |
| Diseases of signal transduction by growth factor receptors and second messengers | 1 | BRAF |
| RAF activation | 1 | BRAF |
| RAF/MAP kinase cascade | 1 | BRAF |
| MAP2K and MAPK activation | 1 | BRAF |
| Negative feedback regulation of MAPK pathway | 1 | BRAF |
| Negative regulation of MAPK pathway | 1 | BRAF |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| negative regulation of neuron apoptotic process | 2 |
| positive regulation of ERK1 and ERK2 cascade | 2 |
| negative regulation of endothelial cell apoptotic process | 2 |
| protein phosphorylation | 2 |
| cell differentiation | 2 |
| negative regulation of apoptotic process | 2 |
| angiogenesis | 1 |
| ovarian follicle development | 1 |
| branching involved in blood vessel morphogenesis | 1 |
| vasculogenesis | 1 |
| positive regulation of protein phosphorylation | 1 |
| positive regulation of endothelial cell proliferation | 1 |
| lymph vessel development | 1 |
| positive regulation of mesenchymal cell proliferation | 1 |
| epithelial cell maturation | 1 |
Indications & clinical
Indications
41 indications (6 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 |
|---|---|---|---|
| colorectal adenocarcinoma | 4 | MONDO:0005008 | EFO:0000365 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| colorectal neoplasm | 4 | MONDO:0005335 | EFO:0004142 |
| colorectal carcinoma | 4 | MONDO:0024331 | EFO:1001951 |
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| colonic neoplasm | 3 | MONDO:0005401 | MONDO:0021063 |
| gastrointestinal stromal tumor | 3 | MONDO:0011719 | MONDO:0011719 |
| adenoid cystic carcinoma | 2 | MONDO:0004971 | EFO:0000231 |
| bile duct carcinoma | 2 | MONDO:0005496 | EFO:0005540 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| cholangiocarcinoma | 2 | MONDO:0019087 | EFO:0005221 |
| ovarian neoplasm | 2 | MONDO:0021068 | EFO:0003893 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| ovarian carcinoma | 2 | MONDO:0005140 | EFO:0001075 |
| rectal cancer | 2 | MONDO:0006519 | EFO:1000657 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| liposarcoma | 2 | MONDO:0005060 | EFO:0000569 |
| osteosarcoma | 2 | MONDO:0009807 | EFO:0000637 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| angiosarcoma | 2 | MONDO:0016982 | EFO:0003968 |
| cutaneous melanoma | 2 | MONDO:0005012 | EFO:0000389 |
| macular degeneration | 2 | MONDO:0003004 | EFO:0009606 |
| colon adenocarcinoma | 2 | MONDO:0002271 | EFO:1001949 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| intrahepatic cholangiocarcinoma | 2 | MONDO:0003210 | EFO:1001961 |
| meningioma | 2 | MONDO:0016642 | MONDO:0020634 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| small cell lung carcinoma | 1 | MONDO:0008433 | EFO:0000702 |
| rhabdomyosarcoma | 1 | MONDO:0005212 | EFO:0002918 |
| bone cancer | 1 | MONDO:0002129 | EFO:1000350 |
| myelodysplastic syndrome | 1 | MONDO:0018881 | EFO:0000198 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 241.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 129 |
| PHASE1 | 32 |
| PHASE1/PHASE2 | 28 |
| Not specified | 23 |
| PHASE3 | 21 |
| PHASE2/PHASE3 | 7 |
| PHASE4 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04874207 | PHASE4 | COMPLETED | Evaluation of Treatment PERSOnalization Based on Its Therapeutic Monitoring in Patients With Metastatic Colorectal Cancer Treated With REgorafenib |
| NCT03829462 | PHASE3 | ACTIVE_NOT_RECRUITING | Assessing a Regorafenib-irinotecan Combination Versus Regorafenib Alone in Metastatic Colorectal Cancer Patients |
| NCT03970447 | PHASE2/PHASE3 | RECRUITING | A Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma |
| NCT04879368 | PHASE3 | ACTIVE_NOT_RECRUITING | RegoNivo vs Standard of Care Chemotherapy in AGOC |
| NCT05425940 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of XL092 + Atezolizumab vs Regorafenib in Participants With Metastatic Colorectal Cancer |
| NCT05462613 | PHASE2/PHASE3 | RECRUITING | Regorafenib With Low-dose Chemotherapies and Aspirin Followed by Standard Chemotherapies in Metastatic Colorectal Cancer |
| NCT05794971 | PHASE3 | RECRUITING | Regorafenib Combined With Irinotecan Drug-Eluting Beads for Colorectal Cancer Liver Metastases |
| NCT06199973 | PHASE3 | ACTIVE_NOT_RECRUITING | Injection of SHR-A1811 Versus Physician Choiced Treatment in Patients With Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-fu, and Irinotecan |
| NCT06820957 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Testing a New Combination of Anti-cancer Drugs in Patients Newly Diagnosed With Ewing Sarcoma Who Have Cancer That Has Spread to Other Parts of the Body |
| NCT07134205 | PHASE3 | NOT_YET_RECRUITING | The Study of JMT101 Combined With Irinotecan as a ≥3rd-Line Treatment in Metastatic Colorectal Cancer |
| NCT07300488 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Pracytarabine Versus Regorafenib in the Treatment of Patients With Hepatocellular Carcinoma |
| NCT07379047 | PHASE2/PHASE3 | NOT_YET_RECRUITING | Efficacy and Safety of NB003 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST) |
| NCT07384377 | PHASE3 | NOT_YET_RECRUITING | JSKN003 Versus Physician Choiced Treatment in Patients With HER2-positive and Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-Fu, and Irinotecan |
| NCT07392866 | PHASE2/PHASE3 | NOT_YET_RECRUITING | A Clinical Study of SH006 Injection in Combination Therapy Versus Regorafenib in the Treatment of Advanced Hepatocellular Carcinoma |
| NCT07483684 | PHASE3 | NOT_YET_RECRUITING | A Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs |
| NCT01189903 | PHASE2/PHASE3 | UNKNOWN | Clinical Evaluation - A Phase IIA Proof of Concept Study of Regorafenib (Bayer 73-4506) in Biopsy-amenable Asian Colorectal Cancer Patients |
| NCT01584830 | PHASE3 | COMPLETED | Asian Subjects With Metastatic Colorectal Cancer Treated With Regorafenib or Placebo After Failure of Standard Therapy |
| NCT01786538 | PHASE3 | WITHDRAWN | Second-line FOLFOX With or Without Regorafenib in mCRC Patients Failed to First-line Irinotecan Plus Fluoropyrimidines |
| NCT02664077 | PHASE3 | TERMINATED | A Study Evaluating Regorafenib Following Completion of Standard Chemotherapy for Patients With Colon Cancer |
| NCT02773524 | PHASE3 | UNKNOWN | A Study of Regorafenib in Refractory Advanced Gastro-Oesophageal Cancer |
| NCT02788279 | PHASE3 | COMPLETED | A Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma (COTEZO IMblaze370) |
| NCT02934529 | PHASE3 | COMPLETED | Metastatic Colorectal Cancer (RAS-wildtype) After Response to First-line Treatment With FOLFIR Plus Cetuximab |
| NCT03465722 | PHASE3 | COMPLETED | (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST |
| NCT04776148 | PHASE3 | COMPLETED | Study of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017) |
| NCT04985136 | PHASE3 | TERMINATED | A Study of Camrelizumab Combined With Rivoceranib Mesylate Versus Investigator’s Choice of Regimen in Treatment of Patients With Advanced Hepatocellular Carcinoma (HCC) |
| NCT05064059 | PHASE3 | COMPLETED | A Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007) |
| NCT05198934 | PHASE3 | COMPLETED | Sotorasib and Panitumumab Versus Investigator’s Choice for Participants With Kirsten Rat Sarcoma (KRAS) p.G12C Mutation |
| NCT05328908 | PHASE3 | TERMINATED | A Study of Nivolumab-relatlimab Fixed-dose Combination Versus Regorafenib or TAS-102 in Participants With Later-lines of Metastatic Colorectal Cancer |
| NCT05600309 | PHASE3 | COMPLETED | A Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)-China Extension Study |
| NCT02389244 | PHASE2 | ACTIVE_NOT_RECRUITING | A Phase II Study Evaluating Efficacy and Safety of Regorafenib in Patients With Metastatic Bone Sarcomas |
| NCT02657551 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study Using Regorafenib as Second or Third Line Therapy in Metastatic Medullary Thyroid Cancer |
| NCT02693535 | PHASE2 | RECRUITING | TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT02955940 | PHASE2 | ACTIVE_NOT_RECRUITING | An Open-Label Study to Enable Continued Treatment Access for Subjects Previously Enrolled in Studies of Ruxolitinib |
| NCT03657641 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Regorafenib and Pembrolizumab in Treating Participants With Advanced or Metastatic Colorectal Cancer |
| NCT03844620 | PHASE2 | ACTIVE_NOT_RECRUITING | Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer |
| NCT03899428 | PHASE2 | RECRUITING | Immune Checkpoint Therapy vs Target Therapy in Reducing Serum HBsAg Levels in Patients With HBsAg+ Advanced Stage HCC |
| NCT04116541 | PHASE2 | RECRUITING | A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors. |
| NCT04117945 | PHASE2 | ACTIVE_NOT_RECRUITING | Regorafenib, With Cetuximab or Panitumumab, for the Treatment of Unresectable, Locally Advanced, or Metastatic Colorectal Cancer |
| NCT04625907 | PHASE1/PHASE2 | RECRUITING | FaR-RMS: An Overarching Study for Children and Adults With Frontline and Relapsed RhabdoMyoSarcoma |
Clinical evidence (CIViC)
Variant × indication × effect (50 predictive associations from 54 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| KIT Exon 11 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC B | EID4599 +2 |
| KIT Exon 9 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC B | EID4628 |
| KIT Wildtype | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC B | EID4144 |
| KRAS Exon 2 Mutation | Colorectal Cancer | Sensitivity/Response | Regorafenib Anhydrous | CIViC B | EID87 |
| KIT Exon 9 Mutation | Gastrointestinal Stromal Tumor | Reduced Sensitivity | Regorafenib Anhydrous | CIViC B | EID4139 +1 |
| PIK3CA E542K | Colorectal Cancer | Resistance | Regorafenib Anhydrous | CIViC B | EID83 |
| BRAF Exon 15 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID4121 |
| BRAF Kinase Domain Duplication | Acinic Cell Carcinoma | Sensitivity/Response | Regorafenib | CIViC C | EID12470 |
| FLT3 Amplification | Colorectal Cancer | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID7102 |
| KDR R961W | Colorectal Adenocarcinoma | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID1191 |
| KIT D820Y | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID4589 |
| KIT N822K | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID4595 |
| KRAS G12A | Lung Non-small Cell Carcinoma | Sensitivity/Response | Regorafenib Anhydrous | CIViC C | EID3716 |
| KRAS G12D | Colorectal Cancer | Resistance | Regorafenib Anhydrous | CIViC C | EID3947 +1 |
| BRAF Exon 15 Mutation | Gastrointestinal Stromal Tumor | Resistance | Regorafenib Anhydrous | CIViC C | EID4605 |
| BRAF V600E | Colon Cancer | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID3776 |
| KIT A502_Y503dup | Cancer | Sensitivity/Response | Imatinib + Ponatinib + Regorafenib Anhydrous | CIViC D | EID4630 |
| KIT K550_W557del | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sunitinib + Imatinib + Regorafenib Anhydrous + Ponatinib | CIViC D | EID4583 |
| KIT K558delinsNP | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sunitinib + Ponatinib + Regorafenib Anhydrous + Imatinib | CIViC D | EID4594 |
| KIT K642E | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID4146 |
| KIT P551_E554delPMYE | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous + Sunitinib + Imatinib | CIViC D | EID4455 |
| KIT V559D | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous + Ponatinib + Imatinib | CIViC D | EID4459 |
| KIT V560D | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sunitinib + Ponatinib + Regorafenib Anhydrous + Imatinib | CIViC D | EID4127 |
| KIT V560G | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib + Ponatinib + Regorafenib Anhydrous | CIViC D | EID7395 |
| KIT V560_L576del | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID4061 |
| KIT W557_K558del | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sunitinib + Regorafenib Anhydrous | CIViC D | EID4087 |
| KRAS G12V | Colon Cancer | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID3932 |
| KRAS G13D | Colon Cancer | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID3897 |
| RET C634W | Gastrointestinal Stromal Tumor | Sensitivity/Response | Regorafenib Anhydrous | CIViC D | EID3695 |
| FBXW7 G579W | Colorectal Cancer | Resistance | Regorafenib Anhydrous | CIViC D | EID4822 |
+20 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
183 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, KDR |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, KDR |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | BRAF, KDR |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| DASATINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| IMATINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| PONATINIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| VEMURAFENIB | ChEMBL | Phase 4 (approved) | BRAF, KDR |
| MOTESANIB | ChEMBL | Phase 3 | BRAF, KDR |
| QUERCETIN | ChEMBL | Phase 3 | BRAF, KDR |
| CEP-32496 | ChEMBL | Phase 2 | BRAF, KDR |
| DORAMAPIMOD | ChEMBL | Phase 2 | BRAF, KDR |
| ELLAGIC ACID | ChEMBL | Phase 2 | BRAF, KDR |
| FORETINIB | ChEMBL | Phase 2 | BRAF, KDR |
| R-406 | ChEMBL | Phase 2 | BRAF, KDR |
| RAF-265 | ChEMBL | Phase 2 | BRAF, KDR |
| REBASTINIB | ChEMBL | Phase 2 | BRAF, KDR |
| Afatinib | PubChem | Approved | BRAF, KDR |
| Binimetinib | PubChem | Approved | BRAF, KDR |
| Selumetinib | PubChem | Approved | BRAF, KDR |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | KDR |
| ABROCITINIB | ChEMBL | Phase 4 (approved) | KDR |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | KDR |
| ALECTINIB | ChEMBL | Phase 4 (approved) | KDR |
| AUROTHIOGLUCOSE | ChEMBL | Phase 4 (approved) | KDR |
| AXITINIB | ChEMBL | Phase 4 (approved) | KDR |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | KDR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | KDR |
| CABOZANTINIB S-MALATE | ChEMBL | Phase 4 (approved) | KDR |
| CERITINIB | ChEMBL | Phase 4 (approved) | KDR |
| COBIMETINIB | ChEMBL | Phase 4 (approved) | BRAF |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | BRAF |
| ENASIDENIB | ChEMBL | Phase 4 (approved) | KDR |
| ENCORAFENIB | ChEMBL | Phase 4 (approved) | BRAF |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | KDR |
| ERDAFITINIB | ChEMBL | Phase 4 (approved) | KDR |
| ESTRAMUSTINE | ChEMBL | Phase 4 (approved) | KDR |
| FOSTAMATINIB DISODIUM | ChEMBL | Phase 4 (approved) | KDR |
| FRUQUINTINIB | ChEMBL | Phase 4 (approved) | KDR |
| FUTIBATINIB | ChEMBL | Phase 4 (approved) | KDR |
| GLAFENINE | ChEMBL | Phase 4 (approved) | KDR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | KDR |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | KDR |
| INDIGOTINDISULFONATE | ChEMBL | Phase 4 (approved) | KDR |
| ISOXICAM | ChEMBL | Phase 4 (approved) | KDR |
| LENVATINIB | ChEMBL | Phase 4 (approved) | KDR |
| MEBENDAZOLE | ChEMBL | Phase 4 (approved) | KDR |
| MESALAMINE | ChEMBL | Phase 4 (approved) | KDR |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | KDR |
| NERATINIB | ChEMBL | Phase 4 (approved) | KDR |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | KDR |
| NILOTINIB | ChEMBL | Phase 4 (approved) | BRAF |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | KDR |
| NINTEDANIB ESYLATE | ChEMBL | Phase 4 (approved) | KDR |
| NOVOBIOCIN | ChEMBL | Phase 4 (approved) | KDR |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | KDR |
Related Atlas pages
- Genes: KDR, BRAF
- Diseases: colorectal adenocarcinoma, neoplasm, colorectal neoplasm, colorectal carcinoma, hepatocellular carcinoma, colonic neoplasm, gastrointestinal stromal tumor, acinar cell carcinoma, malignant colon neoplasm, cancer
- Drugs: Crizotinib, Gefitinib, Pazopanib, Abemaciclib, Dasatinib, Erlotinib, Fedratinib, Imatinib, Infigratinib, Ponatinib, Sorafenib, Vemurafenib, Motesanib, Quercetin, Afatinib, Binimetinib, Selumetinib, Abrocitinib, Acalabrutinib, Alectinib, Aurothioglucose, Axitinib, Brigatinib, Cabozantinib, Ceritinib, Cobimetinib, Dabrafenib, Enasidenib, Encorafenib, Entrectinib, Erdafitinib, Estramustine, Fruquintinib, Futibatinib, Glafenine, Hexachlorophene, Ibrutinib, Isoxicam, Lenvatinib, Mebendazole, Mesalamine, Midostaurin, Neratinib, Niclosamide, Nilotinib, Nintedanib, Novobiocin, Olmutinib
- Biomarker genes: FLT3, KIT, KRAS, RET