Elesclomol

Summary

Elesclomol (CHEMBL1972860) is a phase-3 clinical-stage small-molecule antineoplastic agent; indicated across 5 conditions including melanoma and soft tissue sarcoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 5 conditions
• Clinical trials: 8
• Chemistry: 400.5 Da · C19H20N4O2S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1972860
Name	Elesclomol
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	300471
ChEBI	CHEBI:79369
Molecular formula	C19H20N4O2S2
Molecular weight	400.5
InChIKey	BKJIXTWSNXCKJH-UHFFFAOYSA-N

SMILES: CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2

IUPAC name: 1-N’,3-N’-bis(benzenecarbonothioyl)-1-N’,3-N’-dimethylpropanedihydrazide

ChEBI definition: A carbohydrazide obtained by formal condensation of the carboxy groups of malonic acid with the hydrino groups of two molar equivalents of N-methylbenzenecarbothiohydrazide

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

Also known as: Elesclomol, GSK-842879, GSK-842879A, STA-4783, STA4783, SID445356, ELESCLOMOL, SID137275831, ELESCLOMOL (STA-4783), ElesclomolÊ, Elesclomol (STA-4783), ElesclomolÂ

Patent coverage: 349 distinct patent families (774 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: 1 (assay-derived). Sample: Heat shock protein HSP90.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 6 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HSP90AA1	8.14	IC50	7.2	nM	CHEMBL_ACT_26329624
HSP90AA1	8.12	IC50	7.6	nM	CHEMBL_ACT_26329940
HSP90AA1	7.78	IC50	16.7	nM	CHEMBL_ACT_26329338
HSP90AA1	7.64	IC50	22.9	nM	CHEMBL_ACT_26329470
HSP90AA1	7.31	IC50	48.9	nM	CHEMBL_ACT_26329783
HSP90AA1	7.27	IC50	53.5	nM	CHEMBL_ACT_26330097

Target pathways

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

Indications & clinical

Indications

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
melanoma	3	MONDO:0005105	EFO:0000756
soft tissue sarcoma	2	MONDO:0018078	EFO:1001968
neoplasm	1	MONDO:0005070	EFO:0000616
acute myeloid leukemia	1	MONDO:0018874	EFO:0000222

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

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
PHASE1	4
PHASE2	2
PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00522834	PHASE3	TERMINATED	Elesclomol (STA-4783) With Paclitaxel Versus Paclitaxel Alone in Melanoma
NCT00084214	PHASE1/PHASE2	COMPLETED	STA-4783/Paclitaxel or Paclitaxel Alone in Melanoma
NCT00087997	PHASE2	COMPLETED	A Study of STA-4783 in Combination With Weekly Paclitaxel for Treatment of Patients With Soft Tissue Sarcomas
NCT00888615	PHASE2	COMPLETED	Elesclomol Sodium and Paclitaxel in Treating Patients With Recurrent or Persistent Ovarian Epithelial Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer
NCT00088114	PHASE1	COMPLETED	STA-4783 and Paclitaxel for Treatment of Solid Tumors
NCT00808418	PHASE1	COMPLETED	A Study to Determine the Maximum Tolerated Dose of Elesclomol Sodium Given With a Fixed Dose of Docetaxel and Prednisone in Patients With Metastatic Prostate Cancer
NCT00827203	PHASE1	SUSPENDED	A Safety Study to Determine the Maximum Tolerated Dose of Elesclomol Sodium in Patients With Solid Tumors
NCT01280786	PHASE1	UNKNOWN	Study Elesclomol Sodium in Patients With Relapsed or Refractory Acute Myeloid Leukemia

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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