Picoplatin

Identification

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Name
Picoplatin
Accession Number
DB04874
Type
Small Molecule
Groups
Investigational
Description

Picoplatin is a cytotoxic platinum compound in clinical development for the treatment of patients with solid tumors. It causes apoptosis (cell death) by binding to DNA and interfering with DNA replication and transcription.

Structure
Thumb
Synonyms
  • (SP-4-3)-Amminedichloro(2-methylpyridine)platinium
  • Picoplatin
External IDs
AMD-473 / AMD473 / NX 473 / NX-473 / ZD-0473 / ZD0473
Categories
UNII
B5TAN0L720
CAS number
181630-15-9
Weight
Average: 376.147
Monoisotopic: 374.986878193
Chemical Formula
C6H10Cl2N2Pt
InChI Key
IIMIOEBMYPRQGU-UHFFFAOYSA-L
InChI
InChI=1S/C6H7N.2ClH.H3N.Pt/c1-6-4-2-3-5-7-6;;;;/h2-5H,1H3;2*1H;1H3;/q;;;;+2/p-2
IUPAC Name
platinum(2+) ion 2-methylpyridine amine dichloride
SMILES
N.[Cl-].[Cl-].[Pt++].CC1=CC=CC=N1

Pharmacology

Indication

For the treatment of patients with solid tumors.

Pharmacodynamics

Picoplatin is a sterically hindered platinum (II) complex designed to deliver an extended spectrum of anti-cancer activity and overcome platinum resistance.

Mechanism of action

Picoplatin causes apoptosis (cell death) by binding to DNA and interfering with DNA replication and transcription.

TargetActionsOrganism
UDNANot 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
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. Kelland L: Broadening the clinical use of platinum drug-based chemotherapy with new analogues. Satraplatin and picoplatin. Expert Opin Investig Drugs. 2007 Jul;16(7):1009-21. [PubMed:17594186]
External Links
PubChem Compound
177358
PubChem Substance
175426881
ChemSpider
154428
Wikipedia
Picoplatin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentBladder Cancers / Cancer of the Ovary / Cancer, Breast / Colorectal Cancers / Head and Neck Carcinoma / Lung Cancers / Malignant Neoplasm of Pancreas / Neoplasms, Gastrointestinal / Prostate Cancer1
1CompletedTreatmentMalignant Lymphomas / Small Intestine Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1Unknown StatusTreatmentTumors, Solid1
1, 2Unknown StatusTreatmentHormone Refractory Prostate Cancer1
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2Unknown StatusTreatmentLung Cancers1
3Unknown StatusTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1

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
PropertyValueSource
logP0.89ChemAxon
pKa (Strongest Basic)5.81ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.89 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity28.49 m3·mol-1ChemAxon
Polarizability10.39 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9651
Blood Brain Barrier+0.9764
Caco-2 permeable+0.7284
P-glycoprotein substrateNon-substrate0.7948
P-glycoprotein inhibitor INon-inhibitor0.9923
P-glycoprotein inhibitor IINon-inhibitor0.994
Renal organic cation transporterNon-inhibitor0.8565
CYP450 2C9 substrateNon-substrate0.7671
CYP450 2D6 substrateNon-substrate0.8139
CYP450 3A4 substrateNon-substrate0.7494
CYP450 1A2 substrateNon-inhibitor0.7636
CYP450 2C9 inhibitorNon-inhibitor0.8311
CYP450 2D6 inhibitorNon-inhibitor0.7598
CYP450 2C19 inhibitorNon-inhibitor0.7224
CYP450 3A4 inhibitorNon-inhibitor0.7689
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8801
Ames testNon AMES toxic0.58
CarcinogenicityNon-carcinogens0.835
BiodegradationNot ready biodegradable0.8478
Rat acute toxicity2.1744 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9532
hERG inhibition (predictor II)Non-inhibitor0.9347
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

Classification
Not classified

Targets

1. DNA
Kind
Nucleotide
Organism
Humans
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 20, 2007 05:20 / Updated on June 04, 2019 06:12