Etoposide
drugOn this page
Also known as Etoposide resolution mixtureEtoposidoEtoposidumNSC-141540SintopozidToposarVepesidVP-16EtopsideSID56463308Etoposide (VP-16)SID164339423EtoposidegC0164599
Summary
Etoposide (CHEMBL44657) is an approved small-molecule antineoplastic agent (ATC L01CB01) targeting TOP2A; indicated across 147 conditions including small cell lung carcinoma and neoplasm; with CIViC clinical evidence for 10 variant-indication associations (e.g. TP53 Overexpression in stomach cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01CB01
- Targets: 1 (TOP2A)
- Indications: 147 conditions
- Clinical trials: 1,300
- Precision-oncology evidence (CIViC): 10 variant–indication associations
- Chemistry: 588.6 Da · C29H32O13
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL44657 |
| Name | Etoposide |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 36462 |
| ChEBI | CHEBI:4911 |
| ATC | L01CB01 |
| Molecular formula | C29H32O13 |
| Molecular weight | 588.6 |
| InChIKey | VJJPUSNTGOMMGY-MRVIYFEKSA-N |
SMILES: C[C@@H]1OC[C@@H]2[C@@H](O1)[C@@H]([C@H]([C@@H](O2)O[C@H]3[C@H]4COC(=O)[C@@H]4[C@@H](C5=CC6=C(C=C35)OCO6)C7=CC(=C(C(=C7)OC)O)OC)O)O
IUPAC name: (5S,5aR,8aR,9R)-5-[[(2R,4aR,6R,7R,8R,8aS)-7,8-dihydroxy-2-methyl-4,4a,6,7,8,8a-hexahydropyrano[3,2-d][1,3]dioxin-6-yl]oxy]-9-(4-hydroxy-3,5-dimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[6,5-f][1,3]benzodioxol-8-one
Pharmacological roles (ChEBI): antineoplastic agent, DNA synthesis inhibitor.
Also known as: Etoposide, Etoposide resolution mixture, Etoposido, Etoposidum, NSC-141540, Sintopozid, Toposar, Vepesid, VP-16, etoposide, Etopside, ETOPOSIDE
Patent coverage: 57,548 distinct patent families (226,069 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 226,046 (100%) 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 |
|---|---|---|---|---|---|
| TOP2A | DNA topoisomerase II alpha | Inhibition | 7.3 | 99.6% (common-essential) | P11388 |
Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Nuclear receptor coactivator 3, Nuclear receptor coactivator 1, Solute carrier organic anion transporter family member 1B3, Latent membrane protein 1, DNA topoisomerase 2-alpha, DNA topoisomerase II, DNA topoisomerase 2-beta, Polyunsaturated fatty acid lipoxygenase ALOX15.
Bioactivity
ChEMBL activities: 14 potent at pChembl ≥ 5 of 38 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| TOP2B | 7.16 | IC50 | 69.8 | nM | CHEMBL_ACT_18438702 |
| NCOA3 | 6.43 | IC50 | 374.7 | nM | CHEMBL_ACT_8260754 |
| P03230 | 6.4 | AC50 | 400 | nM | CHEMBL_ACT_7471832 |
| P03230 | 6.28 | AC50 | 531 | nM | CHEMBL_ACT_7362764 |
| TOP2B | 6.1 | IC50 | 790 | nM | CHEMBL_ACT_18548571 |
| TOP2A | 6.09 | EC50 | 810 | nM | CHEMBL_ACT_1139762 |
| TOP2A | 6.09 | EC50 | 810 | nM | CHEMBL_ACT_1228466 |
| TOP2A | 6.09 | EC50 | 810 | nM | CHEMBL_ACT_171992 |
| TOP2A | 6.09 | EC50 | 810 | nM | CHEMBL_ACT_222775 |
| TOP2A | 6.09 | EC50 | 810 | nM | CHEMBL_ACT_363954 |
| NCOA1 | 5.94 | IC50 | 1153 | nM | CHEMBL_ACT_9632427 |
| P12530 | 5.5 | IC50 | 3187 | nM | CHEMBL_ACT_7675964 |
| SLCO1B3 | 5.38 | IC50 | 4180 | nM | CHEMBL_ACT_15188475 |
| TOP2A | 5.33 | IC50 | 4700 | nM | CHEMBL_ACT_25558596 |
Target pathways
Aggregated over 1 target gene(s): TOP2A.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Transcription of E2F targets under negative control by DREAM complex | 1 | TOP2A |
| SUMOylation of DNA replication proteins | 1 | TOP2A |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| resolution of meiotic recombination intermediates | 1 |
| sister chromatid segregation | 1 |
| hematopoietic progenitor cell differentiation | 1 |
| DNA topological change | 1 |
| chromatin organization | 1 |
| DNA damage response | 1 |
| chromosome segregation | 1 |
| female meiotic nuclear division | 1 |
| apoptotic chromosome condensation | 1 |
| embryonic cleavage | 1 |
| regulation of circadian rhythm | 1 |
| positive regulation of apoptotic process | 1 |
| positive regulation of single stranded viral RNA replication via double stranded DNA intermediate | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| rhythmic process | 1 |
Indications & clinical
Indications
147 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 |
|---|---|---|---|
| small cell lung carcinoma | 4 | MONDO:0008433 | EFO:0000702 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| lung neoplasm | 4 | MONDO:0021117 | MONDO:0008903 |
| small cell carcinoma | 4 | MONDO:0000402 | EFO:0008524 |
| acute lymphoblastic leukemia | 3 | MONDO:0004967 | EFO:0000220 |
| leukemia | 3 | MONDO:0005059 | EFO:0000565 |
| neuroblastoma | 3 | MONDO:0005072 | EFO:0000621 |
| ependymoma | 3 | MONDO:0016698 | EFO:1000028 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| medulloblastoma | 3 | MONDO:0007959 | EFO:0002939 |
| mantle cell lymphoma | 3 | MONDO:0018876 | EFO:1001469 |
| neoplasm of mature B-cells | 3 | MONDO:0004949 | EFO:0000096 |
| Ewing sarcoma | 3 | MONDO:0012817 | EFO:0000174 |
| Hodgkins lymphoma | 3 | MONDO:0004952 | EFO:0000183 |
| myelodysplastic syndrome | 3 | MONDO:0018881 | EFO:0000198 |
| T-cell acute lymphoblastic leukemia | 3 | MONDO:0004963 | EFO:0000209 |
| peripheral T-cell lymphoma, not otherwise specified | 3 | MONDO:0004964 | EFO:0000211 |
| acute monocytic leukemia | 3 | MONDO:0007896 | EFO:0000221 |
| acute myeloid leukemia | 3 | MONDO:0018874 | EFO:0000222 |
| acute myelomonocytic leukemia M4 | 3 | MONDO:0018871 | EFO:0000223 |
| Burkitt lymphoma | 3 | MONDO:0007243 | EFO:0000309 |
| carcinoma | 3 | MONDO:0004993 | EFO:0000313 |
| diffuse large B-cell lymphoma | 3 | MONDO:0018905 | EFO:0000403 |
| germ cell tumor | 3 | MONDO:0005040 | EFO:0000514 |
| lymphoma | 3 | MONDO:0005062 | EFO:0000574 |
| osteosarcoma | 3 | MONDO:0009807 | EFO:0000637 |
| sarcoma | 3 | MONDO:0005089 | EFO:0000691 |
| squamous cell lung carcinoma | 3 | MONDO:0005097 | EFO:0000708 |
| plasma cell myeloma | 3 | MONDO:0009693 | EFO:0001378 |
| thymus neoplasm | 3 | MONDO:0005197 | EFO:0002626 |
| rhabdomyosarcoma | 3 | MONDO:0005212 | EFO:0002918 |
| acute megakaryoblastic leukemia | 3 | MONDO:0018872 | EFO:0003025 |
| acute myeloblastic leukemia without maturation | 3 | MONDO:0005224 | EFO:0003027 |
| acute basophilic leukemia | 3 | MONDO:0019458 | EFO:0003029 |
| myelodysplastic syndrome with single lineage dysplasia | 3 | MONDO:0005272 | EFO:0003802 |
| brain neoplasm | 3 | MONDO:0021211 | EFO:0003833 |
| testicular cancer | 3 | MONDO:0005447 | EFO:0004281 |
| lymphoid leukemia | 3 | MONDO:0005402 | EFO:0004289 |
| primitive neuroectodermal tumor | 3 | MONDO:0005462 | EFO:0005235 |
| non-Hodgkin lymphoma | 3 | MONDO:0018908 | EFO:0005952 |
| myeloid sarcoma | 3 | MONDO:0006861 | EFO:1001052 |
| soft tissue sarcoma | 3 | MONDO:0018078 | EFO:1001968 |
| lung adenocarcinoma | 3 | MONDO:0005061 | EFO:0000571 |
| adrenal cortex carcinoma | 3 | MONDO:0006639 | EFO:1000796 |
| acute erythroid leukemia | 3 | MONDO:0017858 | EFO:0000218 |
| ganglioneuroblastoma | 3 | MONDO:0005035 | EFO:0000502 |
| myeloproliferative neoplasm | 3 | MONDO:0020076 | EFO:0002428 |
| acute myeloblastic leukemia with maturation | 3 | MONDO:0020320 | EFO:0003028 |
| myelodysplastic syndrome with excess blasts | 3 | MONDO:0019454 | EFO:0003811 |
| mediastinal cancer | 3 | MONDO:0005843 | EFO:0007362 |
| central nervous system neoplasm | 3 | MONDO:0006130 | EFO:1000158 |
| hepatoblastoma | 3 | MONDO:0018666 | EFO:1000292 |
| ovarian embryonal carcinoma | 3 | MONDO:0003581 | EFO:1000415 |
| ovarian yolk sac tumor | 3 | MONDO:0006344 | EFO:1000437 |
| choriocarcinoma of testis | 3 | MONDO:0003508 | EFO:1000564 |
| testicular yolk sac tumor | 3 | MONDO:0003402 | EFO:1000574 |
| chronic myelomonocytic leukemia | 3 | MONDO:0020311 | EFO:1001779 |
| gastric neoplasm | 3 | MONDO:0021085 | MONDO:0001056 |
| brain cancer | 3 | MONDO:0001657 | MONDO:0001657 |
| kidney cancer | 3 | MONDO:0002367 | MONDO:0002367 |
| teratoma | 3 | MONDO:0002601 | MONDO:0002601 |
| seminoma | 3 | MONDO:0003001 | MONDO:0003001 |
| breast neoplasm | 3 | MONDO:0021100 | MONDO:0007254 |
| ovarian cancer | 3 | MONDO:0008170 | MONDO:0008170 |
| follicular lymphoma | 3 | MONDO:0018906 | MONDO:0018906 |
| Wilms tumor | 3 | MONDO:0006058 | MONDO:0019004 |
| nasal cavity and paranasal sinus lethal midline granuloma | 3 | MONDO:0006828 | MONDO:0019472 |
| HIV infectious disease | 3 | MONDO:0005109 | EFO:0000180 |
| retinoblastoma | 3 | MONDO:0008380 | MONDO:0008380 |
| B-cell acute lymphoblastic leukemia | 3 | MONDO:0004947 | EFO:0000094 |
| colorectal neoplasm | 3 | MONDO:0005335 | MONDO:0005575 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| alveolar rhabdomyosarcoma | 2 | MONDO:0009994 | EFO:0000248 |
| embryonal rhabdomyosarcoma | 2 | MONDO:0009993 | EFO:0000437 |
| oligoastrocytoma | 2 | MONDO:0016702 | EFO:0000630 |
| oligodendroglioma | 2 | MONDO:0016695 | EFO:0000632 |
| anaplastic astrocytoma | 2 | MONDO:0016684 | EFO:0002499 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| anaplastic large cell lymphoma | 2 | MONDO:0020325 | EFO:0003032 |
| relapsing-remitting multiple sclerosis | 2 | MONDO:0005314 | EFO:0003929 |
| thymoma | 2 | MONDO:0006456 | EFO:1000581 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| cutaneous neuroendocrine carcinoma | 2 | MONDO:0019210 | EFO:1001471 |
| hematologic disorder | 2 | MONDO:0005570 | HP:0001871 |
| AIDS | 2 | MONDO:0012268 | EFO:0000765 |
| stiff-person syndrome | 2 | MONDO:0008491 | EFO:0007498 |
| optic nerve glioma | 2 | MONDO:0003235 | EFO:0009254 |
| Waldenstrom macroglobulinemia | 2 | MONDO:0100280 | EFO:0009441 |
| anaplastic oligodendroglioma | 2 | MONDO:0016696 | EFO:0002501 |
| neuromyelitis optica | 2 | MONDO:0019100 | EFO:0004256 |
| myasthenia gravis | 2 | MONDO:0009688 | EFO:0004991 |
| pancreatic endocrine carcinoma | 2 | MONDO:0005893 | EFO:0007416 |
| Guillain-Barre syndrome, familial | 2 | MONDO:0007691 | EFO:0009538 |
| opsoclonus-myoclonus syndrome | 2 | MONDO:0015247 | EFO:1001383 |
| neutropenia | 2 | MONDO:0001475 | MONDO:0001475 |
| neuroendocrine carcinoma | 2 | MONDO:0002120 | MONDO:0002120 |
| graft versus host disease | 2 | MONDO:0013730 | MONDO:0013730 |
| Castleman disease | 2 | MONDO:0015564 | MONDO:0015564 |
| T-cell non-Hodgkin lymphoma | 2 | MONDO:0015760 | MONDO:0015760 |
| astrocytoma (excluding glioblastoma) | 2 | MONDO:0019781 | MONDO:0016691 |
| oropharynx cancer | 2 | MONDO:0004608 | MONDO:0021364 |
| carcinoid tumor | 2 | MONDO:0005369 | MONDO:0024503 |
| hematopoietic and lymphoid system neoplasm | 2 | MONDO:0002334 | MONDO:0044881 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| MALT lymphoma | 2 | MONDO:0007650 | EFO:0000191 |
| plasma cell neoplasm | 2 | MONDO:0004959 | EFO:0000200 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| lung large cell carcinoma | 2 | MONDO:0003050 | EFO:0003050 |
| olfactory neuroblastoma | 2 | MONDO:0006329 | EFO:1000407 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| glioma | 2 | MONDO:0021042 | MONDO:0003268 |
| chronic myeloid leukemia | 1 | MONDO:0011996 | EFO:0000339 |
| Kaposi’s sarcoma | 1 | MONDO:0005055 | EFO:0000558 |
| plasma cell leukemia | 1 | MONDO:0018689 | EFO:0006475 |
| peritoneal neoplasm | 1 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 1 | MONDO:0021092 | MONDO:0002158 |
| myelodysplastic/myeloproliferative disease | 1 | MONDO:0020077 | MONDO:0020077 |
| primary effusion lymphoma | 1 | MONDO:0018842 | EFO:1000491 |
| neuroendocrine neoplasm | 1 | MONDO:0019496 | EFO:1001901 |
| neuroepithelial neoplasm | 0 | MONDO:0021193 | MONDO:0021193 |
24 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 1,300.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 615 |
| PHASE3 | 277 |
| PHASE1 | 175 |
| PHASE1/PHASE2 | 127 |
| Not specified | 48 |
| PHASE2/PHASE3 | 27 |
| PHASE4 | 18 |
| EARLY_PHASE1 | 13 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05518383 | PHASE4 | RECRUITING | B-cell Mature Non-Hodgkin’s Lymphoma Treatment Protocol in Children and Adolescents 2021 |
| NCT06931145 | PHASE4 | NOT_YET_RECRUITING | Benmelstobart, Anlotinib and Chemotherapy as First-line Treatment for Extensive-stage Small-cell Lung Cancer |
| NCT00198991 | PHASE4 | COMPLETED | German Multicenter Trial for Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Adults (07/2003) |
| NCT00199147 | PHASE4 | UNKNOWN | Efficacy of G-CSF-Priming in Elderly AML Patients |
| NCT00526175 | PHASE4 | COMPLETED | LAL-BR/2001: Study Treatment to Low Risk ALL |
| NCT01424839 | PHASE4 | UNKNOWN | Prospective Trial for the Diagnosis and Treatment of Intracranial Germ Cell Tumors |
| NCT01501136 | PHASE4 | UNKNOWN | Treatment of Natural Killer/T Cell Lymphoma-I/II |
| NCT01746992 | PHASE4 | UNKNOWN | CTOP/ITE/MTX Compared With CHOP as the First-line Therapy for Newly Diagnosed Young Patients With T Cell Lymphoma |
| NCT01873807 | PHASE4 | UNKNOWN | HD-Idarubicin/Etoposide Intensified Conditioning Regimen Allo-HSCT for Adult ALL |
| NCT02036489 | PHASE4 | COMPLETED | Pethema LAL-RI/2008: Treatment for Patients With Standard Risk Acute Lymphoblastic Leukemia |
| NCT02348450 | PHASE4 | UNKNOWN | Irinotecan Plus Cisplatin Compared With Etoposide Plus Cisplatin for Extensive Stage Small-cell Lung Cancer |
| NCT02858804 | PHASE4 | COMPLETED | EDOCH Alternating With DHAP for New Diagnosed Younger MCL |
| NCT03071822 | PHASE4 | UNKNOWN | Combination Chemotherapy Including Cisplatin, Ifosfamide, Gemcitabine, L-asparaginase, Etoposide and Dexamethasone as Treatment of Newly Diagnosed and Relapsed/Refractory Peripheral T Cell Lymphomas |
| NCT03707847 | PHASE4 | UNKNOWN | Crizotinib Combined With Etoposide Capsule Followed by Auto-HSCT for Relapsed and Refractory ALK+ ALCL |
| NCT04038411 | PHASE4 | UNKNOWN | PD-1 Antibody, Chidamide, Lenalidomide and Etoposide for Relapsed or Refractory NK/T Cell Lymphoma |
| NCT04490590 | PHASE4 | UNKNOWN | A Clinical Trial of Chidamide Combined With Etoposide in Relapsed or Refractory NK/T-cell Lymphoma |
| NCT04999878 | PHASE4 | UNKNOWN | A Prospective Clinical Study of Ruxolitinib and Etoposide Combined With DDGP Regimen (RUE-DDGP) in Induction Therapy of T/NK Cell Lymphoma-associated Hemophagocytic Syndrome. |
| NCT05491304 | PHASE4 | UNKNOWN | Cytokine Guided Risk Stratification and Treatment in Pediatric Hemophagocytic Lymphohistiocytosis |
| NCT00379340 | PHASE3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Radiation Therapy in Treating Young Patients With Newly Diagnosed Stage III or Stage IV Wilms’ Tumor |
| NCT00470223 | PHASE3 | ACTIVE_NOT_RECRUITING | Combined Chemotherapy With or Without Zoledronic Acid for Patients With Osteosarcoma |
| NCT00572169 | PHASE3 | ACTIVE_NOT_RECRUITING | UARK 2006-66, Total Therapy 3B: An Extension of UARK 2003-33 Total Therapy |
| NCT01704716 | PHASE3 | RECRUITING | High Risk Neuroblastoma Study 1.8 of SIOP-Europe (SIOPEN) |
| NCT02003222 | PHASE3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Blinatumomab in Treating Patients With Newly Diagnosed BCR-ABL-Negative B Lineage Acute Lymphoblastic Leukemia |
| NCT02101853 | PHASE3 | ACTIVE_NOT_RECRUITING | Blinatumomab in Treating Younger Patients With Relapsed B-cell Acute Lymphoblastic Leukemia |
| NCT02112916 | PHASE3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Bortezomib in Treating Younger Patients With Newly Diagnosed T-Cell Acute Lymphoblastic Leukemia or Stage II-IV T-Cell Lymphoblastic Lymphoma |
| NCT02166463 | PHASE3 | ACTIVE_NOT_RECRUITING | Brentuximab Vedotin and Combination Chemotherapy in Treating Children and Young Adults With Stage IIB, Stage IIIB, IVA, or IVB Hodgkin Lymphoma |
| NCT02176967 | PHASE3 | ACTIVE_NOT_RECRUITING | Response and Biology-Based Risk Factor-Guided Therapy in Treating Younger Patients With Non-high Risk Neuroblastoma |
| NCT02306161 | PHASE3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Ganitumab in Treating Patients With Newly Diagnosed Metastatic Ewing Sarcoma |
| NCT02405676 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | BNHL-2015 for Children or Adolescents in China |
| NCT02429687 | PHASE3 | RECRUITING | TC or BEP in Treating Patients With Malignant Ovarian Germ Cell Tumors |
| NCT02429700 | PHASE3 | RECRUITING | TC or BEP in Treating Patients With Ovarian Malignant Sex Cord-Stromal Tumors |
| NCT02443077 | PHASE3 | ACTIVE_NOT_RECRUITING | Ibrutinib Before and After Stem Cell Transplant in Treating Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma |
| NCT02521493 | PHASE3 | ACTIVE_NOT_RECRUITING | Response-Based Chemotherapy in Treating Newly Diagnosed Acute Myeloid Leukemia or Myelodysplastic Syndrome in Younger Patients With Down Syndrome |
| NCT02582697 | PHASE3 | RECRUITING | Accelerated v’s Standard BEP Chemotherapy for Patients With Intermediate and Poor-risk Metastatic Germ Cell Tumours |
| NCT02661503 | PHASE3 | ACTIVE_NOT_RECRUITING | HD21 for Advanced Stages |
| NCT02845882 | PHASE3 | ACTIVE_NOT_RECRUITING | LBL-2016 for Children or Adolescents in China |
| NCT03007147 | PHASE3 | ACTIVE_NOT_RECRUITING | Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia |
| NCT03017326 | PHASE3 | ACTIVE_NOT_RECRUITING | Paediatric Hepatic International Tumour Trial |
| NCT03020030 | PHASE3 | ACTIVE_NOT_RECRUITING | Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Children and Adolescents |
| NCT03043872 | PHASE3 | ACTIVE_NOT_RECRUITING | Durvalumab ± Tremelimumab in Combination With Platinum Based Chemotherapy in Untreated Extensive-Stage Small Cell Lung Cancer (CASPIAN) |
Clinical evidence (CIViC)
Variant × indication × effect (10 predictive associations from 10 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| TP53 Overexpression | Stomach Cancer | Sensitivity/Response | Cisplatin + Mitomycin + Etoposide | CIViC B | EID2799 |
| ETV6::NTRK3 Fusion | B-lymphoblastic Leukemia/lymphoma | Sensitivity/Response | Etoposide + Methotrexate + Larotrectinib | CIViC C | EID8917 |
| TP53 Mutation | Stomach Carcinoma | Sensitivity/Response | Cisplatin + Etoposide + Doxorubicin | CIViC C | EID2820 |
| TP53 R273C | Stomach Carcinoma | Sensitivity/Response | Etoposide + Mitomycin + Cisplatin | CIViC C | EID2292 |
| TP53 Y220C | Stomach Carcinoma | Sensitivity/Response | Mitomycin + Cisplatin + Etoposide | CIViC C | EID2306 |
| SF3B1 K700E | Leukemia | Sensitivity/Response | Etoposide + Olaparib | CIViC D | EID10139 |
| TOP2A TOP2A/90 | Leukemia | Resistance | Etoposide | CIViC D | EID9634 |
| TOP2A TOP2A/90 | Leukemia | Resistance | Etoposide + Pixantrone + DVP Regimen + 4’-(9-acridinylamino)methanesulfon-m-anisidide + MVT Regimen | CIViC D | EID9635 |
| TP53 R248Q | Ovarian Cancer | Resistance | Paclitaxel + Doxorubicin + Etoposide | CIViC D | EID7175 |
| NPM1 W288FS | Acute Myeloid Leukemia | Sensitivity/Response | Daunorubicin + Cytarabine + Etoposide | CIViC E | EID153 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 16 clinical and 38 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.
27 molecules share ≥1 primary target. Top 27 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AMSACRINE | ChEMBL | Phase 4 (approved) | TOP2A |
| CIPROFLOXACIN | ChEMBL | Phase 4 (approved) | TOP2A |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | TOP2A |
| DEXRAZOXANE | ChEMBL | Phase 4 (approved) | TOP2A |
| DOXORUBICIN | ChEMBL | Phase 4 (approved) | TOP2A |
| EPIRUBICIN | ChEMBL | Phase 4 (approved) | TOP2A |
| IDARUBICIN | ChEMBL | Phase 4 (approved) | TOP2A |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | TOP2A |
| TENIPOSIDE | ChEMBL | Phase 4 (approved) | TOP2A |
| TOPOTECAN | ChEMBL | Phase 4 (approved) | TOP2A |
| CURCUMIN | ChEMBL | Phase 3 | TOP2A |
| GEPOTIDACIN | ChEMBL | Phase 3 | TOP2A |
| AXL-1717 | ChEMBL | Phase 2 | TOP2A |
| DECERNOTINIB | ChEMBL | Phase 2 | TOP2A |
| LOSOXANTRONE | ChEMBL | Phase 2 | TOP2A |
| NEMORUBICIN | ChEMBL | Phase 2 | TOP2A |
| PIROXANTRONE | ChEMBL | Phase 2 | TOP2A |
| Afatinib | PubChem | Approved | TOP2A |
| Binimetinib | PubChem | Approved | TOP2A |
| Crizotinib | PubChem | Approved | TOP2A |
| Gefitinib | PubChem | Approved | TOP2A |
| Idelalisib | PubChem | Approved | TOP2A |
| Pazopanib | PubChem | Approved | TOP2A |
| podofilox | PubChem | Approved | TOP2A |
| regorafenib | PubChem | Approved | TOP2A |
| Selumetinib | PubChem | Approved | TOP2A |
| Trametinib | PubChem | Approved | TOP2A |
Related Atlas pages
- Genes: TOP2A
- Diseases: small cell lung carcinoma, neoplasm, lung neoplasm, small cell carcinoma, acute lymphoblastic leukemia, leukemia, neuroblastoma, ependymoma, non-small cell lung carcinoma, medulloblastoma, mantle cell lymphoma, neoplasm of mature B-cells, Ewing sarcoma, Hodgkins lymphoma, myelodysplastic syndrome, T-cell acute lymphoblastic leukemia, peripheral T-cell lymphoma, not otherwise specified, acute monocytic leukemia, acute myeloid leukemia, Burkitt lymphoma, carcinoma, diffuse large B-cell lymphoma, germ cell tumor, lymphoma, osteosarcoma, sarcoma, squamous cell lung carcinoma, plasma cell myeloma, thymus neoplasm, rhabdomyosarcoma, acute megakaryoblastic leukemia, acute myeloblastic leukemia without maturation, acute basophilic leukemia, myelodysplastic syndrome with single lineage dysplasia, brain neoplasm, testicular cancer, lymphoid leukemia, primitive neuroectodermal tumor, non-Hodgkin lymphoma, myeloid sarcoma, soft tissue sarcoma, lung adenocarcinoma, adrenal cortex carcinoma, ganglioneuroblastoma, myeloproliferative neoplasm, acute myeloblastic leukemia with maturation, myelodysplastic syndrome with excess blasts, mediastinal cancer, central nervous system neoplasm, hepatoblastoma, ovarian embryonal carcinoma, ovarian yolk sac tumor, choriocarcinoma of testis, testicular yolk sac tumor, chronic myelomonocytic leukemia, gastric neoplasm, brain cancer, kidney cancer, teratoma, seminoma, breast neoplasm, ovarian cancer, follicular lymphoma, Wilms tumor, nasal cavity and paranasal sinus lethal midline granuloma, HIV infectious disease, retinoblastoma, B-cell acute lymphoblastic leukemia, colorectal neoplasm, gastric carcinoma, ovarian carcinoma, acute myeloid leukemia by FAB classification
- Drugs: Amsacrine, Ciprofloxacin, Daunorubicin, Dexrazoxane, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Teniposide, Topotecan, Curcumin, Gepotidacin, Afatinib, Binimetinib, Crizotinib, Gefitinib, Idelalisib, Pazopanib, podofilox, regorafenib, Selumetinib, Trametinib