EPTAPLATIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C8H18N2O2.C3H2O4.Pt
Molecular Weight	471.37
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[Pt++].[O-]C(=O)CC([O-])=O.[H][C@]1(CN)OC(O[C@]1([H])CN)C(C)C

InChI

InChIKey=XJXKGUZINMNEDK-GPJOBVNKSA-L

InChI=1S/C8H18N2O2.C3H4O4.Pt/c1-5(2)8-11-6(3-9)7(4-10)12-8;4-2(5)1-3(6)7;/h5-8H,3-4,9-10H2,1-2H3;1H2,(H,4,5)(H,6,7);/q;;+2/p-2/t6-,7-;;/m1../s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19688066 | https://adisinsight.springer.com/drugs/800004468 | http://www.skchemicals.com/page/ls/eng/product/info9_03.do

Eptaplatin (also known as Heptaplatin) is a third-generation platinum antitumor drug, which has been approved for the clinical treatment of advanced gastric cancer in Korea. Although the anticancer mechanism of eptaplatin has not been studied well, it is supposed to be similar to that of cisplatin and oxaliplatin. Eptaplatin may bind to DNA to form various types of adducts, thus leading to cell death.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
DNA 278 Target ID: CHEMBL2311221 Sources: http://aip.scitation.org/doi/full/10.1063/1.4893672	Crosslinking Agent 81

Conditions

Condition	Modality	Targets	Highest Phase	Product
Gastric cancer 53 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19688066	Primary		Approved 8429	SUNPLA Approved Use Treatment of progressive, metastatic or post-operative relapsing gastric cancer combined with 5-fluorouracil. Launch Date 1999

PubMed

Title	Date	PubMed
Combination chemotherapy of heptaplatin, paclitaxel and 5-fluorouracil in patients with advanced gastric cancer: a pilot study.	2004 Jun	20396542
Combination chemotherapy with 5-fluorouracil and heptaplatin as first-line treatment in patients with advanced gastric cancer.	2004 Jun	15201502
Molecular mechanisms of heptaplatin effective against cisplatin-resistant cancer cell lines: less involvement of metallothionein.	2004 Oct 19	15494073
Combined effect of heptaplatin and ionizing radiation on human squamous carcinoma cell lines.	2005 Feb 28	15750352
Randomized, multicenter, phase III trial of heptaplatin 1-hour infusion and 5-fluorouracil combination chemotherapy comparing with cisplatin and 5-fluorouracil combination chemotherapy in patients with advanced gastric cancer.	2009 Mar	19688066

Patents

Sample Use Guides

In Vivo Use Guide

Patients received eptaplatin (400 mg/m2) as a 1-hour continuous infusion on day 1, followed by 5-FU (1,000 mg/m2/day) as a 12-hour continuous infusion on days 1-5 every 4 weeks.

Route of Administration: Intravenous

In Vitro Use Guide

In a cytotoxicity assay, SNU-601 cells were treated with 1-10000 ng/ml eptaplatin for 24 hr.

Name

Type

Language

EPTAPLATIN

Official Name

English

EPTAPLATIN [MART.]

Common Name

English

CIS-((4R,5R)-2-ISOPROPYL-1,3-DIOXOLANE-4,5-BIS(METHYLAMINE)-N,N')(MALONATO(2-)-O,O')PLATINUM

Common Name

English

NSC-D-644591

Code

English

Eptaplatin [WHO-DD]

Common Name

English

eptaplatin [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1450