Identification

Name
SP1049C
Accession Number
DB04978
Type
Small Molecule
Groups
Investigational
Description

SP1049C is a novel anthracycline chemotherapeutic agent designed to overcome drug resistance in a number of cancers. It has successfully completed Phase 1 trials. Phase 2 results are currently under final review. Preliminary data, in its first clinically tested indication, shows that SP1049C is active in Stage IV non-resectable adenocarcinoma of the oesophagus. Median survival is encouraging and correlates strongly with dose levels.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Intended for the treatment of carcinoma of the oesophagus.

Pharmacodynamics
Not Available
Mechanism of action

SP1049C is a novel anticancer agent containing doxorubicin and two nonionic pluronic block copolymers. Doxorubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Doxorubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.

TargetActionsOrganism
UDNA topoisomerase 2-alphaNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Danson S, Ferry D, Alakhov V, Margison J, Kerr D, Jowle D, Brampton M, Halbert G, Ranson M: Phase I dose escalation and pharmacokinetic study of pluronic polymer-bound doxorubicin (SP1049C) in patients with advanced cancer. Br J Cancer. 2004 Jun 1;90(11):2085-91. [PubMed:15150584]
  2. Link [Link]
External Links
PubChem Substance
347909870

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Ubiquitin binding
Specific Function
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segr...
Gene Name
TOP2A
Uniprot ID
P11388
Uniprot Name
DNA topoisomerase 2-alpha
Molecular Weight
174383.88 Da

Drug created on October 21, 2007 16:23 / Updated on October 01, 2018 13:58