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Tanespimycin

drug
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Also known as 17aagBMS-722782CNF-1010CNF1010KOS-953NSC-330507TanespimicinaTanespimycineSID26756800SID26756801SID574817SID144205607

Summary

Tanespimycin (CHEMBL109480) is a phase-3 clinical-stage small-molecule antineoplastic agent; indicated across 39 conditions including plasma cell myeloma and prostate adenocarcinoma; with CIViC clinical evidence for 6 variant-indication associations (e.g. NRAS G13D in melanoma).

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Indications: 39 conditions
  • Clinical trials: 36
  • Precision-oncology evidence (CIViC): 6 variant–indication associations
  • Chemistry: C31H43N3O8

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL109480
NameTanespimycin
TypeSmall molecule
Max phase3
ChEBICHEBI:64153
Molecular formulaC31H43N3O8
InChIKeyAYUNIORJHRXIBJ-TXHRRWQRSA-N

SMILES: C=CCNC1=C2C[C@@H](C)C[C@H](OC)[C@H](O)[C@@H](C)/C=C(\C)[C@H](OC(N)=O)[C@@H](OC)/C=C\C=C(/C)C(=O)NC(=CC1=O)C2=O

ChEBI definition: A 19-membered macrocyle that is geldanamycin in which the methoxy substituent attached to the benzoquinone moiety has been replaced by an allylamino group. It is a potent inhibitor of heat shock protein 90 (Hsp90). A less toxic analogue than geldanamycin, it induces apoptosis and displays antitumour effects.

Pharmacological roles (ChEBI): antineoplastic agent, Hsp90 inhibitor, apoptosis inducer.

Also known as: 17aag, BMS-722782, CNF-1010, CNF1010, KOS-953, NSC-330507, Tanespimicina, Tanespimycin, Tanespimycine, SID26756800, SID26756801, SID574817

Patent coverage: 1,533 distinct patent families (3,645 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 16 (assay-derived). Sample: Heat shock protein 75 kDa, mitochondrial, Microtubule-associated protein tau, Survival motor neuron protein, Prelamin-A/C, Receptor tyrosine-protein kinase erbB-2, Lysine-specific demethylase 6B, Heat shock protein HSP90, Bcr/Abl fusion protein, Lysine-specific demethylase 5A, Lysine-specific demethylase 4B.

Bioactivity

ChEMBL activities: 83 potent at pChembl ≥ 5 of 92 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HSP90AA18.52IC503nMCHEMBL_ACT_2651405
HSP90AA18.4IC504nMCHEMBL_ACT_2651454
HSP90AA18.34Ki4.6nMCHEMBL_ACT_3201558
HSP90AA18.3IC505nMCHEMBL_ACT_25872475
HSP90AA18.15IC507nMCHEMBL_ACT_1882167
HSP90AB18.15IC507nMCHEMBL_ACT_3201598
HSP90AB18.14Kd7.3nMCHEMBL_ACT_7934872
HSP90AA18.1IC508nMCHEMBL_ACT_2651456
HSP90AB18.05Ki9nMCHEMBL_ACT_3201603
HSP90AA17.92EC5012nMCHEMBL_ACT_12178114
HSP90AB17.92IC5012nMCHEMBL_ACT_3201605
HSP90AB17.82IC5015nMCHEMBL_ACT_2617272
HSP90AA17.72EC5019nMCHEMBL_ACT_1733979
HSP90AA17.7IC5020nMCHEMBL_ACT_1882183
HSP90AA17.7IC5020nMCHEMBL_ACT_6277575
HSP90AA17.69IC5020.21nMCHEMBL_ACT_23171498
HSP90AA17.66EC5022nMCHEMBL_ACT_1733977
HSP90AA17.54Ki29nMCHEMBL_ACT_15168931
P411487.51IC5031nMCHEMBL_ACT_13417800
ERBB27.51IC5031nMCHEMBL_ACT_2617203
HSP90AA17.5IC5032nMCHEMBL_ACT_2651455
HSP90AA17.48IC5033nMCHEMBL_ACT_19400458
HSP90AB17.48IC5033nMCHEMBL_ACT_2617270
HSP90AA17.46EC5035nMCHEMBL_ACT_1733981
HSP90AB17.35IC5045nMCHEMBL_ACT_13417810
HSP90AA17.35EC5045nMCHEMBL_ACT_1746994
HSP90AA17.34IC5046nMCHEMBL_ACT_13417820
HSP90AA17.25IC5056nMCHEMBL_ACT_16826811
HSP90AA17.22EC5060nMCHEMBL_ACT_6277609
HSP90AA17.19EC5064.9nMCHEMBL_ACT_1763691

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

39 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).

IndicationTrial phaseMONDOEFO
plasma cell myeloma3MONDO:0009693EFO:0001378
prostate adenocarcinoma2MONDO:0005082EFO:0000673
melanoma2MONDO:0005105EFO:0000756
Hodgkins lymphoma2MONDO:0004952EFO:0000183
cutaneous melanoma2MONDO:0005012EFO:0000389
leukemia2MONDO:0005059EFO:0000565
lymphoma2MONDO:0005062EFO:0000574
neoplasm2MONDO:0005070EFO:0000616
anaplastic large cell lymphoma2MONDO:0020325EFO:0003032
mantle cell lymphoma2MONDO:0018876EFO:1001469
thyroid gland papillary carcinoma2MONDO:0005075EFO:0000641
myeloproliferative neoplasm2MONDO:0020076EFO:0002428
kidney cancer2MONDO:0002367MONDO:0002367
breast neoplasm2MONDO:0021100MONDO:0007254
thyroid gland follicular carcinoma2MONDO:0005034EFO:0000501
B-cell chronic lymphocytic leukemia1MONDO:0004948EFO:0000095
angioimmunoblastic T-cell lymphoma1MONDO:0004977EFO:0000255
Burkitt lymphoma1MONDO:0007243EFO:0000309
chondrosarcoma1MONDO:0008977EFO:0000333
diffuse large B-cell lymphoma1MONDO:0018905EFO:0000403
osteosarcoma1MONDO:0009807EFO:0000637
head and neck cancer1MONDO:0005627EFO:0006859
Sezary syndrome1MONDO:0017844EFO:1000785
mycosis fungoides1MONDO:0009691EFO:1001051
MALT lymphoma1MONDO:0007650EFO:0000191
Waldenstrom macroglobulinemia1MONDO:0100280EFO:0009441
prolymphocytic leukemia1MONDO:0001023MONDO:0001023
gastric neoplasm1MONDO:0021085MONDO:0001056
ovarian cancer1MONDO:0008170MONDO:0008170
lung neoplasm1MONDO:0021117MONDO:0008903
follicular lymphoma1MONDO:0018906MONDO:0018906
colorectal neoplasm1MONDO:0005335MONDO:0005575

7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 36.

Phase distribution

PhaseTrials
PHASE121
PHASE212
PHASE2/PHASE31
PHASE31
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00514371PHASE2/PHASE3COMPLETEDA Study of Tanespimycin (KOS-953) in Patients With Relapsed-refractory Multiple Myeloma
NCT00546780PHASE3COMPLETEDA Study of Tanespimycin (KOS-953) in Patients With Multiple Myeloma in First Relapse
NCT00082966PHASE2COMPLETEDBortezomib in Treating Patients With Relapsed or Refractory Hodgkin’s Lymphoma
NCT00087386PHASE2TERMINATEDTanespimycin in Treating Patients With Stage III-IV Melanoma
NCT00093405PHASE2COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Metastatic Kidney Cancer
NCT00093496PHASE2COMPLETEDGemcitabine Hydrochloride and Tanespimycin in Treating Patients With Recurrent Advanced Ovarian Epithelial or Peritoneal Cavity Cancer
NCT00096109PHASE2TERMINATEDTanespimycin in Treating Women With Refractory Locally Advanced or Metastatic Breast Cancer
NCT00104897PHASE2COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Metastatic Malignant Melanoma
NCT00117988PHASE2COMPLETED17-AAG in Treating Patients With Relapsed or Refractory Anaplastic Large Cell Lymphoma, Mantle Cell Lymphoma, or Hodgkin’s Lymphoma
NCT00118092PHASE2COMPLETED17-AAG in Treating Patients With Metastatic Prostate Cancer That Did Not Respond to Previous Hormone Therapy
NCT00118248PHASE2COMPLETEDTanespimycin in Treating Patients With Inoperable Locoregionally Advanced or Metastatic Thyroid Cancer
NCT00132015PHASE2COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Systemic Mastocytosis
NCT00577889PHASE2COMPLETEDGemcitabine Hydrochloride and Tanespimycin in Treating Patients With Stage IV Pancreatic Cancer
NCT00773344PHASE1/PHASE2COMPLETEDClinical Trial of the Combination of Trastuzumab (Herceptin) and Tanespimycin in Patients With Solid Tumors and Her2 Positive Metastatic Breast Cancer That Have Previously Failed Herceptin
NCT00779428PHASE2COMPLETEDClinical Trial of Continuing Treatment for Patients Who Have Participated on a Prior Protocol Investigating Tanespimycin
NCT00003969PHASE1COMPLETEDGeldanamycin Analogue in Treating Patients With Advanced Cancer
NCT00004065PHASE1COMPLETEDChemotherapy in Treating Patients With Refractory Advanced Solid Tumors or Hematologic Cancer
NCT00004075PHASE1COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Solid Tumors That Cannot Be Removed By Surgery
NCT00004241PHASE1COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Advanced Epithelial Cancer, Malignant Lymphoma, or Sarcoma
NCT00019708PHASE1TERMINATEDGeldanamycin Analogue in Treating Patients With Advanced Solid Tumors or Non-Hodgkin’s Lymphoma
NCT00047047PHASE1COMPLETEDTanespimycin, Gemcitabine Hydrochloride, and Cisplatin in Treating Patients With Advanced Solid Tumors
NCT00058253PHASE1COMPLETEDCombination Chemotherapy in Treating Patients With Metastatic or Unresectable Solid Tumors
NCT00066326PHASE1COMPLETEDImatinib Mesylate and 17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Chronic Myelogenous Leukemia
NCT00079404PHASE1COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Young Patients With Relapsed or Refractory Solid Tumors or Leukemia
NCT00087217PHASE1COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin and Paclitaxel in Treating Patients With Metastatic or Unresectable Solid Tumor
NCT00093821PHASE1COMPLETEDTanespimycin in Treating Young Patients With Recurrent or Refractory Leukemia or Solid Tumors
NCT00096005PHASE1TERMINATEDTanespimycin and Bortezomib in Treating Patients With Advanced Solid Tumors or Lymphomas
NCT00098423PHASE1COMPLETEDTanespimycin and Cytarabine in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia, Chronic Myelogenous Leukemia, Chronic Myelomonocytic Leukemia, or Myelodysplastic Syndromes
NCT00098488PHASE1TERMINATED17-N-Allylamino-17-Demethoxygeldanamycin With or Without Rituximab in Treating Patients With Relapsed B-Cell Chronic Lymphocytic Leukemia or Prolymphocytic Leukemia
NCT00100997PHASE1COMPLETED17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Chronic Phase Chronic Myelogenous Leukemia That Did Not Respond to Imatinib Mesylate
NCT00103272PHASE1TERMINATED17-N-Allylamino-17-Demethoxygeldanamycin and Bortezomib in Treating Patients With Relapsed or Refractory Hematologic Cancer
NCT00119236PHASE1COMPLETED17-AAG and Irinotecan in Treating Patients With Locally Advanced or Metastatic Solid Tumors
NCT00121264PHASE1COMPLETED17-AAG and Sorafenib in Treating Patients With Unresectable or Metastatic Solid Tumors
NCT00303797PHASE1COMPLETEDSorafenib and Bortezomib in Treating Patients With Advanced Cancer
NCT00319930PHASE1TERMINATEDPhase 1, Dose-Escalation, Pharmacodynamic Study of IV CNF1010 in ZAP-70 Positive CLL
NCT00354185PHASE1TERMINATEDPXD101 and 17-N-Allylamino-17-Demethoxygeldanamycin in Treating Patients With Metastatic or Unresectable Solid Tumors or Lymphoma

Clinical evidence (CIViC)

Variant × indication × effect (6 predictive associations from 6 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
NRAS G13DMelanomaSensitivity/ResponseTanespimycinCIViC CEID21
EML4::ALK Fusion AND ALK G1202RLung Non-small Cell CarcinomaSensitivity/ResponseTanespimycinCIViC DEID1352
EML4::ALK Fusion AND ALK T1151dupLung Non-small Cell CarcinomaSensitivity/ResponseTanespimycinCIViC DEID1349
PIK3CA MutationCancerSensitivity/ResponseTanespimycin + PictilisibCIViC DEID1358
PIK3CA MutationHead And Neck CancerSensitivity/ResponseTrametinib + Pictilisib + TanespimycinCIViC DEID1364
PTEN MutationHead And Neck CancerSensitivity/ResponseTanespimycin + PictilisibCIViC DEID1359

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 17

This page pulls from 17 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclinical_trialsefogtopdb_interactiongtopdb_ligandhgncmeshmondopatent_compoundpharmgkbpharmgkb_guidelinepubchemuniprot