Identification

Name
S-8184
Accession Number
DB05281
Type
Small Molecule
Groups
Investigational
Description

S8184 is a cremophor free, vitamin E based paclitaxel emulsion incorporating a p glycoprotein inhibitor and particle size based tumor targeting designed to reduce toxicity, allow bolus dosing in 15 minutes, and potentially increase efficacy.

Synonyms
Not Available
International/Other Brands
TOCOSOL paclitaxel
Categories
Not Available
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

Ovarian cancer or primary peritoneal carcinoma

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

S-8184 binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). The vitamin-E based emulsion allows bolus infusion without steroid premedication and may diminish hypersensitivity reactions; tumor tissue may be passively targeted due to preferential deposition of emulsion particles while an emulsion formulation component inhibits the P-glycoprotein drug efflux pump.

TargetActionsOrganism
UTubulin alpha-4A chainNot AvailableHuman
UApoptosis regulator Bcl-2Not 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
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910056

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentNeoplasm, Bladder / Transitional Cell Carcinoma / Ureteral Neoplasms / Urethral Neoplasms1
3TerminatedTreatmentNeoplasms, Breast1

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
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBA4A
Uniprot ID
P68366
Uniprot Name
Tubulin alpha-4A chain
Molecular Weight
49923.995 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appea...
Gene Name
BCL2
Uniprot ID
P10415
Uniprot Name
Apoptosis regulator Bcl-2
Molecular Weight
26265.66 Da

Drug created on November 18, 2007 11:23 / Updated on November 06, 2017 06:45