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Ganetespib

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Also known as STA 9090STA-9090GANETESPIB (STA-9090)

Summary

Ganetespib (CHEMBL2103879) is a phase-3 clinical-stage small molecule targeting HSP90AA1; indicated across 27 conditions including non-small cell lung carcinoma and lung adenocarcinoma; with CIViC clinical evidence for 2 variant-indication associations (e.g. MYC Overexpression in esophagus squamous cell carcinoma).

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (HSP90AA1)
  • Indications: 27 conditions
  • Clinical trials: 33
  • Precision-oncology evidence (CIViC): 2 variant–indication associations
  • Chemistry: 364.4 Da · C20H20N4O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2103879
NameGanetespib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID135564985
Molecular formulaC20H20N4O3
Molecular weight364.4
InChIKeyRVAQIUULWULRNW-UHFFFAOYSA-N

SMILES: CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)O)O

IUPAC name: 3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-(1-methylindol-5-yl)-1H-1,2,4-triazol-5-one

Also known as: Ganetespib, STA 9090, STA-9090, GANETESPIB, GANETESPIB (STA-9090), Ganetespib (STA-9090)

Patent coverage: 847 distinct patent families (2,075 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 1,674 (81%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
HSP90AA1heat shock protein 90 alpha family class A member 1Inhibition8.33.4%P07900

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Heat shock protein 75 kDa, mitochondrial, Endoplasmin, Heat shock protein HSP90, Heat shock protein HSP 90-alpha, Heat shock protein HSP 90-beta, Endoplasmin.

Bioactivity

ChEMBL activities: 11 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HSP90AB18.3IC505nMCHEMBL_ACT_13417804
HSP90AA18.3IC505nMCHEMBL_ACT_13417814
HSP90AA18.22IC506nMCHEMBL_ACT_25652302
P411488IC5010nMCHEMBL_ACT_13417794
HSP90AA17.9IC5012.71nMCHEMBL_ACT_29310825
TRAP17.42IC5037.7nMCHEMBL_ACT_20646450
HSP90B17.42IC5037.7nMCHEMBL_ACT_20646464
HSP90AA17.3IC5050.45nMCHEMBL_ACT_20646418
TRAP17.29IC5051nMCHEMBL_ACT_13417784
HSP90AA17.2IC5063nMCHEMBL_ACT_19400455
HSP90AA15.27IC505390nMCHEMBL_ACT_24836322

Target pathways

Aggregated over 1 target gene(s): HSP90AA1.

Top Reactome pathways

55 total, by targets touching each:

PathwayTargetsGenes
Signaling by ERBB21HSP90AA1
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants1HSP90AA1
Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation1HSP90AA1
DDX58/IFIH1-mediated induction of interferon-alpha/beta1HSP90AA1
vRNP Assembly1HSP90AA1
Regulation of actin dynamics for phagocytic cup formation1HSP90AA1
eNOS activation1HSP90AA1
Regulation of PLK1 Activity at G2/M Transition1HSP90AA1
Scavenging by Class F Receptors1HSP90AA1
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand1HSP90AA1
HSF1 activation1HSP90AA1
Attenuation phase1HSP90AA1
HSF1-dependent transactivation1HSP90AA1
Loss of Nlp from mitotic centrosomes1HSP90AA1
Recruitment of mitotic centrosome proteins and complexes1HSP90AA1
Loss of proteins required for interphase microtubule organization from the centrosome1HSP90AA1
Recruitment of NuMA to mitotic centrosomes1HSP90AA1
Sema3A PAK dependent Axon repulsion1HSP90AA1
VEGFA-VEGFR2 Pathway1HSP90AA1
VEGFR2 mediated vascular permeability1HSP90AA1
Uptake and function of diphtheria toxin1HSP90AA1
PIWI-interacting RNA (piRNA) biogenesis1HSP90AA1
Anchoring of the basal body to the plasma membrane1HSP90AA1
Constitutive Signaling by EGFRvIII1HSP90AA1
Regulation of necroptotic cell death1HSP90AA1
Interleukin-4 and Interleukin-13 signaling1HSP90AA1
Neutrophil degranulation1HSP90AA1
The role of GTSE1 in G2/M progression after G2 checkpoint1HSP90AA1
AURKA Activation by TPX21HSP90AA1
Downregulation of ERBB2 signaling1HSP90AA1

Dominant GO biological processes

GO termTargets
neuron migration1
activation of innate immune response1
positive regulation of defense response to virus by host1
skeletal muscle contraction1
protein folding1
mitochondrial transport1
response to unfolded protein1
telomere maintenance via telomerase1
response to heat1
response to cold1
response to xenobiotic stimulus1
response to salt stress1
positive regulation of lamellipodium assembly1
cardiac muscle cell apoptotic process1
protein import into mitochondrial matrix1

Indications & clinical

Indications

27 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
non-small cell lung carcinoma3MONDO:0005233EFO:0003060
lung adenocarcinoma3MONDO:0005061EFO:0000571
small cell lung carcinoma2MONDO:0008433EFO:0000702
melanoma2MONDO:0005105EFO:0000756
prostate adenocarcinoma2MONDO:0005082EFO:0000673
rectal cancer2MONDO:0006519EFO:1000657
angiosarcoma2MONDO:0016982EFO:0003968
gastric neoplasm2MONDO:0021085MONDO:0001056
breast neoplasm2MONDO:0021100MONDO:0007254
colonic neoplasm2MONDO:0005401MONDO:0021063
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
neoplasm1MONDO:0005070EFO:0000616
malignant pleural mesothelioma1MONDO:0005112EFO:0000770
hepatocellular carcinoma1MONDO:0007256EFO:0000182
myelodysplastic syndrome1MONDO:0018881EFO:0000198
acute myeloid leukemia1MONDO:0018874EFO:0000222
plasma cell myeloma1MONDO:0009693EFO:0001378
male breast carcinoma1MONDO:0005628EFO:0006861
malignant peripheral nerve sheath tumor1MONDO:0017827EFO:0000760
fallopian tube neoplasm1MONDO:0021092MONDO:0002158
ovarian cancer1MONDO:0008170MONDO:0008170
lung neoplasm1MONDO:0021117MONDO:0008903
carcinoma of esophagus1MONDO:0019086EFO:0002916
adenocarcinoma1MONDO:0004970MONDO:0003219

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

Clinical trials

Total trials: 33.

Phase distribution

PhaseTrials
PHASE214
PHASE111
PHASE1/PHASE26
PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01798485PHASE3TERMINATEDA Phase 3 Study of Ganetespib in Combination With Docetaxel Versus Docetaxel Alone in Patients With Advanced NSCLC
NCT01042379PHASE2RECRUITINGI-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT01031225PHASE2COMPLETEDA Study of the HSP90 Inhibitor, STA-9090 in Subjects With Stage IIIB or IV Non-Small Cell Lung Cancer (NSCLC)
NCT01039519PHASE2COMPLETEDA Study Evaluating STA-9090 in Patients With Metastatic and/or Unresectable Gastrointestinal Stromal Tumor (GIST)
NCT01111838PHASE2COMPLETEDClinical and Translational Study of STA-9090
NCT01167114PHASE2COMPLETEDSTA-9090 in Previously Treated Patients With Advanced Esophagogastric Cancer
NCT01173523PHASE2COMPLETEDStudy of Hsp90 Inhibitor, STA-9090 for Relapsed or Refractory Small Cell Lung Cancer
NCT01200238PHASE2COMPLETEDSTA-9090(Ganetespib) in Metastatic Ocular Melanoma
NCT01227018PHASE2TERMINATEDPhII Study STA-9090 as Second or Third-Line Therapy for Metastatic Pancreas Cancer
NCT01236144PHASE1/PHASE2COMPLETEDA Trial to Establish the Feasibility of Combining Either the Tyrosine Kinase Inhibitor AC220,CXCR4 Inhibitor Plerixafor or HSP90 Inhibitor Ganetespib With Chemotherapy in Older Patients With Acute Myeloid Leukaemia and High Risk Myelodysplastic Syndrome.
NCT01273896PHASE2COMPLETEDOpen-label Study of STA-9090 for Patients With Metastatic Breast Cancer
NCT01551693PHASE2TERMINATEDSTA-9090(Ganetespib) in Patients With Unresectable Stage III or Stage IV Melanoma
NCT01560416PHASE2COMPLETEDFulvestrant With or Without Ganetespib in HR+ Breast Cancer
NCT01562015PHASE2COMPLETEDA Study of Ganetespib in Subjects With ALK-Positive Non-Small-Cell Lung Cancer (NSCLC)
NCT01590160PHASE1/PHASE2COMPLETEDGanetespib With Platinum, in Patients With Malignant Pleural Mesothelioma
NCT01677455PHASE2COMPLETEDAn Open-Label Multicenter Phase 2 Window of Opportunity Study Evaluating Ganetespib in Women With Breast Cancer
NCT01962948PHASE1/PHASE2TERMINATEDPaclitaxel and Ganetespib in Treating Patients With Recurrent Ovarian, Fallopian Tube, or Primary Peritoneal Cancer
NCT02008877PHASE1/PHASE2COMPLETEDSARC023: Ganetespib and Sirolimus in Patients With MPNST (Malignant Peripheral Nerve Sheath Tumors)
NCT02012192PHASE1/PHASE2TERMINATEDGANNET53: Ganetespib in Metastatic, p53-mutant, Platinum-resistant Ovarian Cancer
NCT02261805PHASE1/PHASE2TERMINATEDA Phase I/II Study of Ganetespib in Combination With Doxorubicin
NCT03783949PHASE2COMPLETEDEuropean Trial on Enhanced DNA Repair Inhibition in Ovarian Cancer
NCT00687934PHASE1COMPLETEDStudy of STA-9090, Administered Once-Weekly in Patients With Solid Tumors
NCT00858572PHASE1COMPLETEDSTA-9090 for Treatment of AML, CML, MDS and Myeloproliferative Disorders
NCT00964873PHASE1COMPLETEDA Phase 1 Study of the HSP90 Inhibitor, STA-9090 in Subjects With Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia and Blast-phase Chronic Myelogenous Leukemia
NCT01485835PHASE1COMPLETEDA Phase I Study of Ganetespib +/- Bortezomib in Patients With Relapsed and/or Refractory Multiple Myeloma
NCT01554969PHASE1COMPLETEDPhase I Trial of Ganetespib, Capecitabine, and Radiation in Rectal Cancer
NCT01579994PHASE1COMPLETEDCrizotinib and Ganetespib (STA-9090) in ALK Positive Lung Cancers
NCT01665937PHASE1COMPLETEDSTA-9090 in Patients With Advanced Hepatocellular Cancer
NCT02060253PHASE1COMPLETEDGanetespib, Paclitaxel, Trastuzumab and Pertuzumab for Metastatic Human Epidermal Growth Factor Receptor 2 Positive Breast Cancer
NCT02192541PHASE1TERMINATEDGanetespib and Ziv-Aflibercept in Refractory Gastrointestinal Carcinomas, Non-Squamous Non-Small Cell Lung Carcinomas, Urothelial Carcinomas, and Sarcomas
NCT02334319PHASE1TERMINATEDGanetespib Window of Opportunity Study in Head and Neck Cancers
NCT02389751PHASE1COMPLETEDGanetespib in Combination With Paclitaxel, Carboplatin, and Radiation Therapy in Treating Patients With Stage II-III Esophageal Cancer
NCT02637375Not specifiedWITHDRAWNA Pilot Preoperative Trial of Ganetespib With Paclitaxel for Triple-Negative Breast Cancer

Clinical evidence (CIViC)

Variant × indication × effect (2 predictive associations from 2 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
MYC OverexpressionEsophagus Squamous Cell CarcinomaSensitivity/ResponseGanetespibCIViC DEID10151
UGT1A EXPRESSIONColorectal CancerResistanceGanetespibCIViC DEID866

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

47 molecules share ≥1 primary target. Top 47 by shared-target count:

MoleculeSourceStatusShared targets
BIFONAZOLEChEMBLPhase 4 (approved)HSP90AA1
BROXYQUINOLINEChEMBLPhase 4 (approved)HSP90AA1
CHLOROXINEChEMBLPhase 4 (approved)HSP90AA1
CLIOQUINOLChEMBLPhase 4 (approved)HSP90AA1
DAUNORUBICINChEMBLPhase 4 (approved)HSP90AA1
DIPYRIDAMOLEChEMBLPhase 4 (approved)HSP90AA1
DISULFIRAMChEMBLPhase 4 (approved)HSP90AA1
DOXORUBICINChEMBLPhase 4 (approved)HSP90AA1
ECONAZOLE NITRATEChEMBLPhase 4 (approved)HSP90AA1
FLUCONAZOLEChEMBLPhase 4 (approved)HSP90AA1
HALOFANTRINEChEMBLPhase 4 (approved)HSP90AA1
HEXACHLOROPHENEChEMBLPhase 4 (approved)HSP90AA1
KETOCONAZOLEChEMBLPhase 4 (approved)HSP90AA1
NITROXOLINEChEMBLPhase 4 (approved)HSP90AA1
NOVOBIOCINChEMBLPhase 4 (approved)HSP90AA1
PYRITHIONEChEMBLPhase 4 (approved)HSP90AA1
SERTACONAZOLE NITRATEChEMBLPhase 4 (approved)HSP90AA1
SULCONAZOLE NITRATEChEMBLPhase 4 (approved)HSP90AA1
TERCONAZOLEChEMBLPhase 4 (approved)HSP90AA1
TETRACYCLINEChEMBLPhase 4 (approved)HSP90AA1
THIAMINE IONChEMBLPhase 4 (approved)HSP90AA1
THONZONIUM BROMIDEChEMBLPhase 4 (approved)HSP90AA1
TRICLABENDAZOLEChEMBLPhase 4 (approved)HSP90AA1
TRICLOSANChEMBLPhase 4 (approved)HSP90AA1
DIACEREINChEMBLPhase 3HSP90AA1
ELESCLOMOLChEMBLPhase 3HSP90AA1
RETASPIMYCINChEMBLPhase 3HSP90AA1
TANESPIMYCINChEMBLPhase 3HSP90AA1
THIMEROSALChEMBLPhase 3HSP90AA1
ALVESPIMYCINChEMBLPhase 2HSP90AA1
BIIB021ChEMBLPhase 2HSP90AA1
CALCIMYCINChEMBLPhase 2HSP90AA1
CLOXYQUINChEMBLPhase 2HSP90AA1
DICHLOROPHENChEMBLPhase 2HSP90AA1
ETHAMIVANChEMBLPhase 2HSP90AA1
FENTICLORChEMBLPhase 2HSP90AA1
GELDANAMYCINChEMBLPhase 2HSP90AA1
IODOQUINOLChEMBLPhase 2HSP90AA1
LUMINESPIBChEMBLPhase 2HSP90AA1
MOLIBRESIBChEMBLPhase 2HSP90AA1
ONALESPIBChEMBLPhase 2HSP90AA1
PU-H71ChEMBLPhase 2HSP90AA1
SNX 5422ChEMBLPhase 2HSP90AA1
TAS-116ChEMBLPhase 2HSP90AA1
THIRAMChEMBLPhase 2HSP90AA1
ZERANOLChEMBLPhase 2HSP90AA1
PomalidomidePubChemApprovedHSP90AA1

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 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot