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
SMILES
N.[Cl-].[Cl-].[Pt++].CC1=CC=CC=N1
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
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.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00465491
Curator's Comment: Dosing from failed Phase III clinical trial.
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9472630
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.
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NCI_THESAURUS |
C1450
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FDA ORPHAN DRUG |
212305
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EU-Orphan Drug |
EU/3/07/502
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SS-50
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100000090660
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8205
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PICOPLATIN
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m8787
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DB04874
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B5TAN0L720
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181630-15-9
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CHEMBL3544907
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SUB29605
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C48416
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177358
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)