NAV

SP1049C

Identification

Generic Name
SP1049C
DrugBank Accession Number
DB04978
Background

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.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Intended for the treatment of carcinoma of the oesophagus.

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Contraindications & Blackbox Warnings
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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 AvailableHumans
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

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
MargetuximabThe risk or severity of cardiotoxicity can be increased when Margetuximab is combined with SP1049C.
TrastuzumabThe risk or severity of cardiotoxicity can be increased when Trastuzumab is combined with SP1049C.
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Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
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. [Article]
  2. Link [Link]
PubChem Substance
347909870

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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

Targets

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Details1. DNA topoisomerase 2-alpha
Kind
Protein
Organism
Humans
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 at October 21, 2007 22:23 / Updated at June 12, 2020 16:52