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Details

Stereochemistry ACHIRAL
Molecular Formula C6H7N.2Cl.Pt.H3N
Molecular Weight 376.147
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PICOPLATIN

SMILES

N.[Cl-].[Cl-].[Pt++].CC1=NC=CC=C1

InChI

InChIKey=IIMIOEBMYPRQGU-UHFFFAOYSA-L
InChI=1S/C6H7N.2ClH.H3N.Pt/c1-6-4-2-3-5-7-6;;;;/h2-5H,1H3;2*1H;1H3;/q;;;;+2/p-2

HIDE SMILES / InChI

Description

Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
7530 μg/mL
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens
3250 μg/L
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
12000 μg × h/L
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens
13078 μg × h/L
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
0.83 h
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens
85.7 h
120 mg/m² 1 times / 3 weeks steady-state, intravenous
PICOPLATIN plasma
Homo sapiens

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
In a clinical trial, picoplatin was administered intravenously at a dose of 150 mg/m2 every 3 weeks.
Route of Administration: Intravenous
In Vitro Use Guide
In a growth inhibition assay, ovarian carcinoma cell lines were treated serial dilutions of picoplatin for 96 h. Among the cell lines, the drug demonstrated a mean IC50 value of 8.1 uM.