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elesclomol

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EntityQ5359460· pop 7· linked from 271 articles

elesclomol

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Also known as STA-4783, 1-N'-Benzenecarbothioyl-3-(2-benzenecarbothioyl-2-methylhydrazinyl)-N'-methyl-oxopropanehydrazidide

Elesclomol (INN, codenamed STA-4783) is a drug that triggers apoptosis (programmed cell death) in cancer cells. It is being developed by Synta Pharmaceuticals and GlaxoSmithKline as a chemotherapy adjuvant, and has received both fast track and orphan drug status from the U.S. Food and Drug Administration for the treatment of metastatic melanoma. Synta Pharmaceuticals announced on February 26, 2009, the suspension of all clinical trials involving Elesclomol due to safety concerns. In March 2010, Synta announced that the FDA had approved resuming clinical development of elesclomol, and that they

Chemical data

Formula
C19H20N4O2S2
Molecular weight
400.5 g/mol
IUPAC name
1-N',3-N'-bis(benzenecarbonothioyl)-1-N',3-N'-dimethylpropanedihydrazide
SMILES
CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2
InChIKey
BKJIXTWSNXCKJH-UHFFFAOYSA-N
XLogP
2.9
Polar surface area
129 Ų
H-bond donors
2
H-bond acceptors
4
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 3
Molecule type
Small molecule
Indications
neoplasm, acute myeloid leukemia, melanoma, soft tissue sarcoma

via ChEMBL · EBI

Wikidata facts

Mass
400.102768
Show 4 more facts
chemical formula
C₁₉H₂₀N₄O₂S₂
canonical SMILES
CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2
World Health Organisation international non-proprietary name
elesclomol
Commons category
Elesclomol
Sources (2)

via Wikidata · CC0

~2 min read

Encyclopedic overview

3 sections
Contents
  • Mechanism of action
  • Discovery
  • References

Elesclomol (INN, codenamed STA-4783) is a drug that triggers apoptosis (programmed cell death) in cancer cells. It is being developed by Synta Pharmaceuticals and GlaxoSmithKline as a chemotherapy adjuvant, and has received both fast track and orphan drug status from the U.S. Food and Drug Administration for the treatment of metastatic melanoma. Synta Pharmaceuticals announced on February 26, 2009, the suspension of all clinical trials involving Elesclomol due to safety concerns. In March 2010, Synta announced that the FDA had approved resuming clinical development of elesclomol, and that they expected to initiate one or more clinical trials for elesclomol in the second half of the year.

In a small, randomized phase II study, elesclomol was shown to significantly increase progression-free survival in people with metastatic melanoma when given in addition to paclitaxel (Taxol).

Excerpted from Wikipedia’s “elesclomol” article, available under the CC BY-SA 4.0 licence.

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