ELLIPTINIUM ACETATE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H17N2O.C2H3O2
Molecular Weight	336.3844
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC([O-])=O.CC1=C2C=C[N+](C)=CC2=C(C)C3=C1NC4=C3C=C(O)C=C4

InChI

InChIKey=BOMZMNZEXMAQQW-UHFFFAOYSA-N

InChI=1S/C18H16N2O.C2H4O2/c1-10-15-9-20(3)7-6-13(15)11(2)18-17(10)14-8-12(21)4-5-16(14)19-18;1-2(3)4/h4-9,21H,1-3H3;1H3,(H,3,4)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7003658

Elliptinium is an antineoplastic agent, which was used in the treatment of metastatic breast cancer in France under the name Celiptium. The drug is known to intercalate into DNA and inhibit topoisomerase II. Several studies have demonstrated that this molecule can be oxidized, yielding a reactive electrophilic form, which is able to bind covalently to a nucleophilic biological molecule.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
DNA 278 Target ID: CHEMBL2311221 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7003658	Binding Agent 1064
DNA topoisomerase II 66 Target ID: CHEMBL2094255 Sources: DOI 10.1007/978-1-4684-5242-6_17, Chandra P., 'New Experimental Modalities in the Control of Neoplasia' (2012), p. 236, Retrieved from https://books.google.com/books?id=5JPuBwAAQBAJ&dq	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Breast cancer 434 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8484977	Primary		Approved 8429	CELIPTIUM Approved Use Unknown

PubMed

Title	Date	PubMed
Virostatic in vivo effect of elliptinium on Friend's retrovirus (a model for HIV infection).	1990	1369686
Anti-cryptosporidial drug activity screened with an immunosuppressed rat model.	1991 Nov-Dec	1818183
Assessment of candidate anticryptosporidial agents in an immunosuppressed rat model.	1993 Mar	8440946
Inhibitors of human immunodeficiency virus integrase.	1993 Mar 15	8460151
Viral and immunologic follow up of 4 to 9 years of AIDS treatments by quadruple combinations of virostatics including integrase inhibitors applied in short sequences differing by drug rotation.	2002 Jan	11860730
Characterisation and internalisation of recombinant humanised HMFG-1 antibodies against MUC1.	2005 Nov 28	16265351
Anticancer drugs from marine flora: an overview.	2010	21461373
Immunotargeting of collagenase on thrombus.	2010 Nov 16	21187949

Sample Use Guides

In Vivo Use Guide

In a clinical study, elliptinium (acetate salt) was given at a dose of 80 mg/m2 daily for 3 consecutive days every 21 days.

Route of Administration: Intravenous

In Vitro Use Guide

Unknown

Name

Type

Language

ELLIPTINIUM ACETATE

Official Name

English

ELLIPTINIUM ACETATE [MI]

Common Name

English

HME

Common Name

English

elliptinium acetate [INN]

Common Name

English

9-HYDROXY-2,5,11-TRIMETHYL-6H-PYRIDO(4,3-B)CARBAZOLIUM ACETATE

Systematic Name

English

NSC-264137

Code

English

Elliptinium acetate [WHO-DD]

Common Name

English

CELIPTIUM

Brand Name

English

9-HYDROXY-2,5,11-TRIMETHYL-6H-PYRIDO(4,3-B)CARBAZOLIUM ACETATE (1:1)

Systematic Name

English

ELLIPTINIUM ACETATE [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1968