Axitinib
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Also known as AG-013736AG-13736InlytaNSC-757441SID124950168SID144207146SID170466656AxitinibÊAxitinibÂ
Summary
Axitinib (CHEMBL1289926) is an approved small-molecule antineoplastic agent (ATC L01EK01) targeting KDR and PLK4; indicated across 51 conditions including neoplasm and renal cell carcinoma; with CIViC clinical evidence for 47 variant-indication associations (e.g. BCR::ABL1 Fusion AND ABL1 T315I in chronic myeloid leukemia).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EK01
- Targets: 2 (KDR, PLK4)
- Indications: 51 conditions
- Clinical trials: 175
- Precision-oncology evidence (CIViC): 47 variant–indication associations
- Chemistry: 386.5 Da · C22H18N4OS
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1289926 |
| Name | Axitinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 6450551 |
| ChEBI | CHEBI:66910 |
| ATC | L01EK01 |
| Molecular formula | C22H18N4OS |
| Molecular weight | 386.5 |
| InChIKey | RITAVMQDGBJQJZ-FMIVXFBMSA-N |
SMILES: CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4
IUPAC name: N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
ChEBI definition: An indazole substituted at position 3 by a 2-(pyridin-2-yl)vinyl group and at position 6 by a 2-(N-methylaminocarboxy)phenylsulfanyl group. Used for the treatment of advanced renal cell carcinoma after failure of a first line systemic treatment.
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, vascular endothelial growth factor receptor antagonist.
Also known as: AG-013736, AG-13736, Axitinib, Inlyta, NSC-757441, AXITINIB, SID124950168, SID144207146, SID170466656, AxitinibÊ, axitinib, AxitinibÂ
Patent coverage: 6,544 distinct patent families (15,732 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 14,887 (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 | 8.23 | 1.1% | P35968 |
| PLK4 | polo like kinase 4 | Inhibition | 7.34 | 95.4% (common-essential) | O00444 |
Broader ChEMBL bioactivity targets: 109 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Hormonally up-regulated neu tumor-associated kinase, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Protein deacetylase HDAC6, Vascular endothelial growth factor receptor 1, Mitogen-activated protein kinase kinase kinase 12, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Vascular endothelial growth factor receptor 3.
Bioactivity
ChEMBL activities: 202 potent at pChembl ≥ 5 of 202 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| KDR | 10.7 | IC50 | 0.02 | nM | CHEMBL_ACT_26137497 |
| FLT4 | 10 | IC50 | 0.1 | nM | CHEMBL_ACT_18784844 |
| KDR | 10 | IC50 | 0.1 | nM | CHEMBL_ACT_18784845 |
| FLT1 | 10 | IC50 | 0.1 | nM | CHEMBL_ACT_18784846 |
| FLT1 | 10 | IC50 | 0.1 | nM | CHEMBL_ACT_18854174 |
| FLT4 | 10 | IC50 | 0.1 | nM | CHEMBL_ACT_18854179 |
| KDR | 9.74 | IC50 | 0.18 | nM | CHEMBL_ACT_18854169 |
| KDR | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_18149410 |
| ABL1 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_19161702 |
| KDR | 9.7 | Ki | 0.2 | nM | CHEMBL_ACT_27790658 |
| KDR | 9.6 | IC50 | 0.25 | nM | CHEMBL_ACT_3595752 |
| ABL1 | 9.38 | IC50 | 0.42 | nM | CHEMBL_ACT_17723420 |
| KIT | 9.31 | Kd | 0.49 | nM | CHEMBL_ACT_7587628 |
| PDGFRA | 9.29 | Kd | 0.51 | nM | CHEMBL_ACT_7589398 |
| ABL1 | 9.26 | IC50 | 0.55 | nM | CHEMBL_ACT_17723418 |
| PDGFRB | 9.24 | Kd | 0.57 | nM | CHEMBL_ACT_7587713 |
| KDR | 9.15 | AC50 | 0.7 | nM | CHEMBL_ACT_25167969 |
| KDR | 9.04 | IC50 | 0.91 | nM | CHEMBL_ACT_27142115 |
| ABL1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_19161698 |
| AURKC | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_7587606 |
| KIT | 8.85 | Kd | 1.4 | nM | CHEMBL_ACT_7587629 |
| ABL1 | 8.82 | Kd | 1.5 | nM | CHEMBL_ACT_7589353 |
| PDGFRB | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_26137498 |
| PDGFRB | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_29065593 |
| KIT | 8.77 | IC50 | 1.7 | nM | CHEMBL_ACT_26137499 |
| KIT | 8.77 | IC50 | 1.7 | nM | CHEMBL_ACT_29065594 |
| KIT | 8.77 | Kd | 1.7 | nM | CHEMBL_ACT_7587627 |
| ABL1 | 8.59 | IC50 | 2.6 | nM | CHEMBL_ACT_17723419 |
| KIT | 8.49 | Kd | 3.2 | nM | CHEMBL_ACT_7587623 |
| KIT | 8.46 | Kd | 3.5 | nM | CHEMBL_ACT_7587630 |
Target pathways
Aggregated over 2 target gene(s): KDR, PLK4.
Top Reactome pathways
14 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Neuropilin interactions with VEGF and VEGFR | 1 | KDR |
| VEGF binds to VEGFR leading to receptor dimerization | 1 | KDR |
| Integrin cell surface interactions | 1 | KDR |
| Regulation of PLK1 Activity at G2/M Transition | 1 | PLK4 |
| Loss of Nlp from mitotic centrosomes | 1 | PLK4 |
| Recruitment of mitotic centrosome proteins and complexes | 1 | PLK4 |
| Loss of proteins required for interphase microtubule organization from the centrosome | 1 | PLK4 |
| Recruitment of NuMA to mitotic centrosomes | 1 | PLK4 |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| Anchoring of the basal body to the plasma membrane | 1 | PLK4 |
| AURKA Activation by TPX2 | 1 | PLK4 |
| Signaling by membrane-tethered fusions of PDGFRA or PDGFRB | 1 | KDR |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 1 | KDR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 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 |
| endocardium development | 1 |
| endothelium development | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| positive regulation of cell population proliferation | 1 |
| regulation of cell shape | 1 |
Indications & clinical
Indications
51 indications (8 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 | 4 | MONDO:0005070 | EFO:0000616 |
| renal cell carcinoma | 4 | MONDO:0005086 | EFO:0000681 |
| clear cell renal carcinoma | 4 | MONDO:0005005 | EFO:0000349 |
| papillary renal cell carcinoma | 4 | MONDO:0017884 | EFO:0000640 |
| renal carcinoma | 4 | MONDO:0005206 | EFO:0002890 |
| collecting duct carcinoma | 4 | MONDO:0005220 | EFO:0003016 |
| renal cell adenocarcinoma | 4 | MONDO:0005549 | EFO:0005708 |
| kidney neoplasm | 3 | MONDO:0021163 | EFO:0003865 |
| kidney cancer | 3 | MONDO:0002367 | MONDO:0002367 |
| pancreatic ductal adenocarcinoma | 3 | MONDO:0005184 | MONDO:0005184 |
| adenoid cystic carcinoma | 2 | MONDO:0004971 | EFO:0000231 |
| carcinoid tumor | 2 | MONDO:0005369 | EFO:0004243 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| thyroid tumor | 2 | MONDO:0015074 | EFO:0003841 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| myelodysplastic syndrome | 2 | MONDO:0018881 | EFO:0000198 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| pancreatic neoplasm | 2 | MONDO:0021040 | EFO:0003860 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| nasopharyngeal neoplasm | 2 | MONDO:0005375 | EFO:0004252 |
| alveolar soft part sarcoma | 2 | MONDO:0011655 | EFO:0007143 |
| adrenal cortex carcinoma | 2 | MONDO:0006639 | EFO:1000796 |
| colorectal carcinoma | 2 | MONDO:0024331 | EFO:1001951 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| biliary tract neoplasm | 2 | MONDO:0005304 | EFO:0003891 |
| salivary gland cancer | 2 | MONDO:0004669 | MONDO:0004669 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| solitary fibrous tumor | 2 | MONDO:0016238 | MONDO:0016238 |
| skin neoplasm | 2 | MONDO:0002531 | EFO:0004198 |
| gastrointestinal stromal tumor | 2 | MONDO:0011719 | MONDO:0011719 |
| adrenal gland pheochromocytoma | 2 | MONDO:0004974 | EFO:0000239 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0021117 |
| carcinoma | 1 | MONDO:0004993 | EFO:0000313 |
| malignant pleural mesothelioma | 1 | MONDO:0005112 | EFO:0000770 |
| breast neoplasm | 1 | MONDO:0021100 | EFO:0003869 |
| gliosarcoma | 1 | MONDO:0016681 | EFO:1001465 |
| endometriosis | 1 | MONDO:0005133 | EFO:0001065 |
| blast phase chronic myelogenous leukemia, BCR-ABL1 positive | 1 | MONDO:0006115 | EFO:1000131 |
| gastric neoplasm | 1 | MONDO:0021085 | MONDO:0001056 |
7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 175.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 98 |
| PHASE1 | 33 |
| Not specified | 17 |
| PHASE1/PHASE2 | 16 |
| PHASE3 | 9 |
| PHASE2/PHASE3 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05059522 | PHASE3 | ACTIVE_NOT_RECRUITING | Continued Access Study for Participants Deriving Benefit in Pfizer-Sponsored Avelumab Parent Studies That Are Closing |
| NCT05522231 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Fruquintinib in Combination With Sintilimab in Advanced Renal Cell Carcinoma (FRUSICA-2) |
| NCT06364631 | PHASE3 | RECRUITING | CARE1 Pragmatic Clinical Trial |
| NCT07383441 | PHASE3 | NOT_YET_RECRUITING | Adding Biotherapy or Placebo to Standard Treatment for Advanced Kidney Cancer |
| NCT00471146 | PHASE3 | COMPLETED | Study Of Gemcitabine Plus AG-013736 Versus Gemcitabine For Advanced Pancreatic Cancer. |
| NCT00678392 | PHASE3 | COMPLETED | Axitinib (AG 013736) As Second Line Therapy For Metastatic Renal Cell Cancer |
| NCT00920816 | PHASE3 | COMPLETED | Axitinib (AG-013736) For the Treatment of Metastatic Renal Cell Cancer |
| NCT01599754 | PHASE3 | TERMINATED | Adjuvant Axitinib Therapy of Renal Cell Cancer in High Risk Patients |
| NCT01744249 | PHASE2/PHASE3 | COMPLETED | Sandostatin LAR and Axitinib vs Pbo in Pnts With Advanced Well-differentiated Non-pancreatic Neuroendocrine Carcinomas |
| NCT02684006 | PHASE3 | COMPLETED | A Study of Avelumab With Axitinib Versus Sunitinib In Advanced Renal Cell Cancer (JAVELIN Renal 101) |
| NCT02853331 | PHASE3 | COMPLETED | Study to Evaluate the Efficacy and Safety of Pembrolizumab (MK-3475) in Combination With Axitinib Versus Sunitinib Monotherapy in Participants With Renal Cell Carcinoma (MK-3475-426/KEYNOTE-426) |
| NCT02912572 | PHASE2 | ACTIVE_NOT_RECRUITING | Avelumab in Patients With MSS, MSI-H and POLE-mutated Recurrent or Persistent Endometrial Cancer and of Avelumab/Talazoparib and Avelumab/Axitinib in Patients With MSS Recurrent or Persistent Endometrial Cancer |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT03092856 | PHASE2 | ACTIVE_NOT_RECRUITING | Axitinib With or Without Anti-OX40 Antibody PF-04518600 in Treating Patients With Metastatic Kidney Cancer |
| NCT03172754 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Study of Nivolumab and Axitinib in Patients With Advanced Renal Cell Carcinoma |
| NCT03297606 | PHASE2 | RECRUITING | Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) |
| NCT03595124 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study to Compare Treatments for a Type of Kidney Cancer Called TFE/Translocation Renal Cell Carcinoma (tRCC) |
| NCT03839498 | PHASE2 | ACTIVE_NOT_RECRUITING | Study of Axitinib (AG-013736) With Evaluation of the VEGF-pathway in Pheochromocytoma/Paraganglioma |
| NCT04341181 | PHASE2 | RECRUITING | ProTarget - A Danish Nationwide Clinical Trial on Targeted Cancer Treatment Based on Genomic Profiling |
| NCT04996823 | PHASE2 | RECRUITING | Axitinib + Ipilimumab in Advanced Melanoma |
| NCT05256472 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of AK104 Monotherapy or AK104 Plus Axitinib in Advanced/Metastatic Renal Cell Carcinoma |
| NCT05327686 | PHASE2 | RECRUITING | Testing the Addition of Stereotactic Radiation Therapy With Immune Therapy for the Treatment of Patients With Unresectable or Metastatic Renal Cell Cancer, SAMURAI Trial |
| NCT05363631 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Seleno-L Methionine (SLM)-Axitinib-Pembrolizumab |
| NCT05384496 | PHASE2 | RECRUITING | Axitinib and Nivolumab for the Treatment of Mucosal Melanoma |
| NCT05768464 | PHASE2 | RECRUITING | Postoperative Adjuvant Therapy for Non-clear Renal Cell Carcinoma With High-risk Recurrence Factors |
| NCT05805501 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Immune Checkpoint Inhibitor Combinations With Axitinib in Participants With Untreated Locally Advanced Unresectable or Metastatic Renal Cell Carcinoma |
| NCT05808608 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Study of AK104 Plus Axitinib in Advanced/Metastatic Special Pathological Subtypes of Renal Cell Carcinoma |
| NCT05817903 | PHASE2 | RECRUITING | Axitinib Intensification Plus Nivolumab or Nivolumab Alone After Nivolumab Plus Ipilimumab in mRCC Patients |
| NCT05969496 | PHASE2 | RECRUITING | Neoadjuvant Pembrolizumab and Axitinib in Renal Cell Carcinoma With Inferior Vena Cava Tumor Thrombus |
| NCT06211114 | PHASE2 | RECRUITING | Study to Evaluate the Efficacy and Safety of Immunotherapy With Axitinib in Advanced Collecting Duct Carcinoma |
| NCT06279403 | PHASE2 | NOT_YET_RECRUITING | Upfront Immune Checkpoint Inhibitors With Deferred Cytoreductive Nephrectomy for Metastatic Renal Cell Carcinoma |
| NCT06690697 | PHASE2 | RECRUITING | Combination of Toripalimab and JS004 Therapy for ccRCC |
| NCT06889649 | PHASE2 | RECRUITING | SABR Combined with Axitinib and Toripalimab in Recurrent or Metastatic RCC |
| NCT06962787 | PHASE2 | RECRUITING | A Study of BL-B01D1+TKI±Pembrolizumab in Patients With Locally Advanced or Metastatic Renal Cancer |
| NCT07123090 | PHASE2 | RECRUITING | A Study of Sasanlimab, Palbociclib and Axitinib in Metastatic Renal Cell Carcinoma |
| NCT07159191 | PHASE2 | NOT_YET_RECRUITING | Envafolimab Combined With Axitinib as First-Line Treatment for Patients With Advanced Renal Cell Carcinoma |
| NCT07172386 | PHASE2 | RECRUITING | Preoperative Therapy of Super-selective Tumor Artery Embolization Combined With Toripalimab and Axitinib in Advanced RCC |
| NCT07227415 | PHASE1/PHASE2 | RECRUITING | Symbiotic-GU-08: A Study to Learn About the Medicine Called PF-08634404 Dosed Alone and in Combination With Other Anticancer Therapies in Adults With Locally Advanced or Metastatic Renal Cell Cancer |
| NCT07469683 | PHASE2 | RECRUITING | An Open-label, Randomized Phase 2 Clinical Trial to Evaluate the Efficacy and Safety of the Combination Therapy of SLC-3010 and Axitinib Compared to Axitinib Monotherapy as a Second-line Treatment for Locally Advanced or Metastatic Clear Cell Renal Cell Carcinoma |
| NCT00071006 | PHASE2 | COMPLETED | AG-013736 (Axitinib) In Patients With Poor Prognosis Acute Myeloid Leukemia (AML) Or Myelodysplastic Syndrome (MDS) |
Clinical evidence (CIViC)
Variant × indication × effect (47 predictive associations from 57 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| BCR::ABL1 Fusion AND ABL1 T315I | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC C | EID4369 +3 |
| BCR::ABL1 Fusion AND ABL1 V299L | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID4537 +1 |
| BCR::ABL1 Fusion AND ABL1 E279K | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID7772 |
| BCR::ABL1 Fusion AND ABL1 F359V AND ABL1 V299L | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12319 |
| BCR::ABL1 Fusion AND ABL1 M351T AND ABL1 V299L | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12318 |
| BCR::ABL1 Fusion AND ABL1 T315A | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID7768 |
| BCR::ABL1 Fusion AND ABL1 T315I AND ABL1 F359V | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12316 |
| BCR::ABL1 Fusion AND ABL1 T315I AND ABL1 H396R | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12317 |
| BCR::ABL1 Fusion AND ABL1 T315I AND ABL1 M244V | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12315 |
| BCR::ABL1 Fusion AND ABL1 T315L | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID12310 |
| BCR::ABL1 Fusion AND ABL1 T315V | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID7766 |
| KDR R1032Q | Colorectal Cancer | Sensitivity/Response | Lenvatinib + Axitinib + Cabozantinib + Dovitinib | CIViC D | EID9339 |
| LYN Y508F | Chronic Myeloid Leukemia | Sensitivity/Response | Axitinib | CIViC D | EID4804 |
| BCR::ABL1 Fusion AND ABL1 E255V | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4441 +1 |
| BCR::ABL1 Fusion AND ABL1 F317L | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4390 +1 |
| BCR::ABL1 Fusion AND ABL1 G250E | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4320 +1 |
| BCR::ABL1 Fusion AND ABL1 M351T | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4399 +1 |
| BCR::ABL1 Fusion AND ABL1 Q252H | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4323 +1 |
| BCR::ABL1 Fusion AND ABL1 Y253H | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4329 +1 |
| BCR::ABL1 Fusion AND ABL1 D276G | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4360 |
| BCR::ABL1 Fusion AND ABL1 E255K | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4355 |
| BCR::ABL1 Fusion AND ABL1 E255V AND ABL1 V299L | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID12314 |
| BCR::ABL1 Fusion AND ABL1 E292L | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID7773 |
| BCR::ABL1 Fusion AND ABL1 F311I | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4477 |
| BCR::ABL1 Fusion AND ABL1 F317L AND ABL1 F359V | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID12320 |
| BCR::ABL1 Fusion AND ABL1 F317R | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID7774 |
| BCR::ABL1 Fusion AND ABL1 F317V | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4535 |
| BCR::ABL1 Fusion AND ABL1 F359I | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4529 |
| BCR::ABL1 Fusion AND ABL1 F359V | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID3822 |
| BCR::ABL1 Fusion AND ABL1 F486S | Chronic Myeloid Leukemia | Resistance | Axitinib | CIViC D | EID4438 |
+17 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 19 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.
178 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| ERLOTINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | KDR, PLK4 |
| CERITINIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| DASATINIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| VANDETANIB | ChEMBL | Phase 4 (approved) | KDR, PLK4 |
| ALISERTIB | ChEMBL | Phase 3 | KDR, PLK4 |
| CEDIRANIB | ChEMBL | Phase 3 | KDR, PLK4 |
| DOVITINIB | ChEMBL | Phase 3 | KDR, PLK4 |
| LESTAURTINIB | ChEMBL | Phase 3 | KDR, PLK4 |
| LINIFANIB | ChEMBL | Phase 3 | KDR, PLK4 |
| AT-9283 | ChEMBL | Phase 2 | KDR, PLK4 |
| BMS-777607 | ChEMBL | Phase 2 | KDR, PLK4 |
| CENISERTIB | ChEMBL | Phase 2 | KDR, PLK4 |
| DANUSERTIB | ChEMBL | Phase 2 | KDR, PLK4 |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | KDR, PLK4 |
| ELLAGIC ACID | ChEMBL | Phase 2 | KDR, PLK4 |
| ENMD-2076 | ChEMBL | Phase 2 | KDR, PLK4 |
| FORETINIB | ChEMBL | Phase 2 | KDR, PLK4 |
| GLESATINIB | ChEMBL | Phase 2 | KDR, PLK4 |
| ILORASERTIB | ChEMBL | Phase 2 | KDR, PLK4 |
| MERESTINIB | ChEMBL | Phase 2 | KDR, PLK4 |
| OSI-632 | ChEMBL | Phase 2 | KDR, PLK4 |
| R-406 | ChEMBL | Phase 2 | KDR, PLK4 |
| REBASTINIB | ChEMBL | Phase 2 | KDR, PLK4 |
| SU-014813 | ChEMBL | Phase 2 | KDR, PLK4 |
| TANDUTINIB | ChEMBL | Phase 2 | KDR, PLK4 |
| TOZASERTIB | ChEMBL | Phase 2 | KDR, PLK4 |
| Afatinib | PubChem | Approved | KDR, PLK4 |
| Binimetinib | PubChem | Approved | KDR, PLK4 |
| Selumetinib | PubChem | Approved | KDR, PLK4 |
| FOSTAMATINIB | ChEMBL + PubChem | Phase 4 (approved) | PLK4 |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | KDR |
| ABEMACICLIB | ChEMBL | 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 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | KDR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | KDR |
| CABOZANTINIB S-MALATE | ChEMBL | Phase 4 (approved) | KDR |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | PLK4 |
| ENASIDENIB | 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 |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | PLK4 |
| GLAFENINE | ChEMBL | Phase 4 (approved) | KDR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | KDR |
Related Atlas pages
- Genes: KDR, PLK4
- Diseases: neoplasm, renal cell carcinoma, clear cell renal carcinoma, papillary renal cell carcinoma, renal carcinoma, collecting duct carcinoma, renal cell adenocarcinoma, kidney neoplasm, kidney cancer, pancreatic ductal adenocarcinoma, chronic myeloid leukemia, colorectal carcinoma
- Drugs: Crizotinib, Erlotinib, Fedratinib, Gefitinib, Imatinib, Pazopanib, Regorafenib, Ceritinib, Dasatinib, Entrectinib, Midostaurin, Nintedanib, Sorafenib, Sunitinib, Vandetanib, Alisertib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Afatinib, Binimetinib, Selumetinib, Fostamatinib, Abemaciclib, Abrocitinib, Acalabrutinib, Alectinib, Aurothioglucose, Brigatinib, Cabozantinib, Dabrafenib, Enasidenib, Erdafitinib, Estramustine, Fruquintinib, Futibatinib, Gilteritinib, Glafenine, Hexachlorophene
- Biomarker genes: ABL1, RET