Satraplatin

Identification

Name
Satraplatin
Accession Number
DB04996
Type
Small Molecule
Groups
Investigational
Description

Satraplatin is a platinum compound that is currently under investigation as one treatment of patients with advanced prostate cancer who have failed previous chemotherapy. As an investigation drug, it has not yet received U.S. Food and Drug Administration (FDA) approval and is not available in retail pharmacies.

Structure
Thumb
Synonyms
Not Available
External IDs
BMS-182751 / BMY-45594 / JM-216
Categories
UNII
8D7B37T28G
CAS number
129580-63-8
Weight
Average: 500.283
Monoisotopic: 499.060437065
Chemical Formula
C10H22Cl2N2O4Pt
InChI Key
CKNPWBAXEKSCRG-UHFFFAOYSA-J
InChI
InChI=1S/C6H13N.2C2H4O2.2ClH.H3N.Pt/c7-6-4-2-1-3-5-6;2*1-2(3)4;;;;/h6H,1-5,7H2;2*1H3,(H,3,4);2*1H;1H3;/q;;;;;;+4/p-4
IUPAC Name
platinum(4+) ion cyclohexanamine diacetate amine dichloride
SMILES
N.[Cl-].[Cl-].[Pt+4].CC([O-])=O.CC([O-])=O.NC1CCCCC1

Pharmacology

Indication

Investigated for use/treatment in lung cancer, prostate cancer, and solid tumors.

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

The drug has also been used in the treatment of lung and ovarian cancers. The mode of action is that the compound binds to the DNA of cancer cells rendering them incapable of dividing.

TargetActionsOrganism
UDNANot 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
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Satraplatin.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Satraplatin.Experimental
BevacizumabBevacizumab may increase the cardiotoxic activities of Satraplatin.Approved, Investigational
CabazitaxelSatraplatin may increase the myelosuppressive activities of Cabazitaxel.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Satraplatin.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Satraplatin.Experimental
DeslanosideDeslanoside may decrease the cardiotoxic activities of Satraplatin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Satraplatin.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Satraplatin.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Satraplatin.Approved
DocetaxelSatraplatin may increase the myelosuppressive activities of Docetaxel.Approved, Investigational
FosphenytoinThe serum concentration of Fosphenytoin can be decreased when it is combined with Satraplatin.Approved
GitoformateGitoformate may decrease the cardiotoxic activities of Satraplatin.Experimental
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Satraplatin.Experimental
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Satraplatin.Experimental
OleandrinOleandrin may decrease the cardiotoxic activities of Satraplatin.Experimental, Investigational
OuabainOuabain may decrease the cardiotoxic activities of Satraplatin.Approved
PaclitaxelSatraplatin may increase the myelosuppressive activities of Paclitaxel.Approved, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Satraplatin.Experimental
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Satraplatin.Approved, Vet Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Satraplatin.Experimental
TopotecanThe risk or severity of adverse effects can be increased when Satraplatin is combined with Topotecan.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Satraplatin.Approved, Investigational
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Compound
123974
PubChem Substance
175426927
ChemSpider
110493
ChEBI
85609
ChEMBL
CHEMBL3833367
Wikipedia
Satraplatin
ATC Codes
L01XA04 — Satraplatin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentAdvanced Cancers1
1CompletedTreatmentMetastatic Brain Tumors / Neoplasms, Brain / Tumors, Solid1
1TerminatedTreatmentMalignancies1
1TerminatedTreatmentProstate Cancer / Tumors1
1TerminatedTreatmentTumors1
1, 2TerminatedTreatmentLung Cancers / Non-Small Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentLung Cancers1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentPolymorphism, Genetic / Prostate Cancer1
2CompletedTreatmentProstate Cancer1
3CompletedTreatmentHormone Refractory Prostate Cancer / Prostate Cancer1
3TerminatedTreatmentProstate Cancer1
Not AvailableCompletedTreatmentProstate Cancer1

Pharmacoeconomics

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

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.4 mg/ml at pH 1-7.5Not Available
Predicted Properties
PropertyValueSource
logP1.17ChemAxon
pKa (Strongest Basic)10.45ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area26.02 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity30.93 m3·mol-1ChemAxon
Polarizability12.44 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.6502
Blood Brain Barrier+0.7841
Caco-2 permeable-0.6468
P-glycoprotein substrateNon-substrate0.6858
P-glycoprotein inhibitor INon-inhibitor0.9881
P-glycoprotein inhibitor IINon-inhibitor0.9863
Renal organic cation transporterNon-inhibitor0.9154
CYP450 2C9 substrateNon-substrate0.8261
CYP450 2D6 substrateNon-substrate0.8462
CYP450 3A4 substrateNon-substrate0.6351
CYP450 1A2 substrateNon-inhibitor0.8764
CYP450 2C9 inhibitorNon-inhibitor0.905
CYP450 2D6 inhibitorNon-inhibitor0.9427
CYP450 2C19 inhibitorNon-inhibitor0.866
CYP450 3A4 inhibitorNon-inhibitor0.8794
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9813
Ames testNon AMES toxic0.6304
CarcinogenicityNon-carcinogens0.811
BiodegradationReady biodegradable0.6692
Rat acute toxicity2.4085 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9732
hERG inhibition (predictor II)Non-inhibitor0.9639
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as cyclohexylamines. These are organic compounds containing a cyclohexylamine moiety, which consist of a cyclohexane ring attached to an amine group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Cyclohexylamines
Direct Parent
Cyclohexylamines
Alternative Parents
Acetate salts / Organic transition metal salts / Organic metal halides / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organic oxides / Organic chloride salts / Monoalkylamines / Hydrocarbon derivatives
show 1 more
Substituents
Cyclohexylamine / Acetate salt / Carboxylic acid salt / Carboxylic acid derivative / Organic metal halide / Carboxylic acid / Organic transition metal salt / Monocarboxylic acid or derivatives / Amine / Organic salt
show 10 more
Molecular Framework
Not Available
External Descriptors
platinum coordination entity (CHEBI:85609)

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
Unknown
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da

Drug created on October 21, 2007 16:23 / Updated on November 09, 2017 03:49