PICOPLATIN

Investigational

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 Search

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

Molecular Formula	H3N
Molecular Weight	17.0305
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C6H7N
Molecular Weight	93.1265
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	Pt
Molecular Weight	195.084
Charge	2
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11249584 | https://www.ncbi.nlm.nih.gov/pubmed/24163749

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 Target	Pharmacology	Condition	Potency
DNA 282 Target ID: CHEMBL2311221 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24212665 \| https://www.ncbi.nlm.nih.gov/pubmed/10626362	Crosslinking Agent 83
DNA topoisomerase I 60 Target ID: CHEMBL1781 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15292710	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Small-cell lung cancer 41 Sources: https://clinicaltrials.gov/show/NCT00465491	Primary	Phase III 665	Unknown Approved Use Unknown
Colorectal cancer 102 Sources: https://clinicaltrials.gov/ct2/show/NCT00478946	Primary	Phase II 1147	Unknown Approved Use Unknown
Hormone refractory prostate cancer 5 Sources: https://clinicaltrials.gov/ct2/show/NCT00448734	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
7530 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12645906	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3250 μg/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12671715	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
12000 μg × h/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12645906	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
13078 μg × h/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12671715	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
0.83 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12645906	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
85.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12671715	120 mg/m² 1 times / 3 weeks steady-state, intravenous dose: 120 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered:		PICOPLATIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	OCT1 393 OCT3 92 OCT2 434 MRP1 113

Drug as victim

Target	Modality	Activity
OCT3 92	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/20371711/	no [IC50 3.2 uM]
MRP1 113	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/9683290/	no
OCT2 434	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/20371711/	yes [IC50 0.277 uM]
OCT1 393	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/20371711/	yes [IC50 0.44 uM]

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA0022XE	https://www.aablocks.com/goods/Goods/detail?id=AA0022XE
Aaron Chemicals	AR0023P6	http://www.aaronchem.com/181630-15-9
ABI Chem	AC1L42P3
Adooq BioScience	A14108	https://www.adooq.com/picoplatin.html
AN PharmaTech	AN-30599
BioSynth	J-011604	https://www.biosynth.com/en/products/all-products/products/J-011604.html
ChemMol	49420136	http://www.chemmol.com/chemmol/49420136.html
eNovation Chemicals	Y1054892	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1054892
iChemical	EBD36764	http://www.ichemical.com/chemicals/cas-181630-15-9
MolPort	MolPort-006-170-014	https://www.molport.com/shop/molecule-link/MolPort-006-170-014
NovoSeek	177358

PubMed

Title	Date	PubMed
ZD-0473 AstraZeneca.	2000-10	11249584
In vitro circumvention of cisplatin resistance by the novel sterically hindered platinum complex AMD473.	1998	9472630

Patents

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.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 08:41:13 GMT 2025` Edited by `admin` on `Wed Apr 02 08:41:13 GMT 2025`
Record UNII	B5TAN0L720
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

PICOPLATIN

Official Name

English

AMD-473

Preferred Name

English

AMD473

Code

English

NX473

Code

English

PLATINUM, AMMINEDICHLORO(2-METHYLPYRIDINE)-, (SP-4-3)-

Common Name

English

Picoplatin [WHO-DD]

Common Name

English

(SP-4-3)-Amminedichloro(2-methylpyridine)platinium

Common Name

English

PICOPLATIN [MART.]

Common Name

English

PICOPLATIN [USAN]

Common Name

English

ZD-0473

Code

English

picoplatin [INN]

Common Name

English

ZD0473

Code

English

PICOPLATIN [MI]

Common Name

English

NX-473

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C1450