Elomotecan hydrochloride

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C29H32ClN3O4.ClH
Molecular Weight	558.496
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CC[C@@]1(O)CC(=O)OCC2=C1C=C3N(CC4=C(CN5CCC(C)CC5)C6=C(C=C(Cl)C(C)=C6)N=C34)C2=O

InChI

InChIKey=OLYFGLXPXPABOP-XXIQNXCHSA-N

InChI=1S/C29H32ClN3O4.ClH/c1-4-29(36)12-26(34)37-15-21-22(29)10-25-27-20(14-33(25)28(21)35)19(13-32-7-5-16(2)6-8-32)18-9-17(3)23(30)11-24(18)31-27;/h9-11,16,36H,4-8,12-15H2,1-3H3;1H/t29-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C29H32ClN3O4
Molecular Weight	522.035
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10498216 | https://www.ncbi.nlm.nih.gov/pubmed/15256467 | https://adisinsight.springer.com/drugs/800013582

Elomotecan (BN 80927), a homocamptothecin derivative, inhibits both topoisomerase I and topoisomerase II mediated DNA relaxation. It potently inhibits proliferation of human tumor cells in vitro and in vivo. Elomotecan was being developed for the treatment of solid tumors.

Originator

Approval Year

PubMed

Title	Date	PubMed
BN80927: a novel homocamptothecin that inhibits proliferation of human tumor cells in vitro and in vivo.	2004-07-15	15256467
The homocamptothecin, BN 80927, is a potent topoisomerase I poison and topoisomerase II catalytic inhibitor.	2000	11193906
The dual topoisomerase inhibitor, BN 80927, is highly potent against cell proliferation and tumor growth.	2000	11193907
BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II.	1999-09-06	10498216

Patents

Sample Use Guides

In Vivo Use Guide

Phase I study. Elomotecan was administered as a 30-min intravenous infusion at doses ranging from 1.5 to 75 mg once every 3 weeks to 56 patients with advanced solid tumors. Plasma concentration data and adverse effects were modeled using the population approach.

Route of Administration: Intravenous

In Vitro Use Guide

The antiproliferative activity of elomotecan (BN 80927) was determined on various human tumor cell lines from a diverse set of target organs, including leukemia and solid tumors (colon, prostate, ovary, lung, bladder, and breast cell lines). BN80927 was an antiproliferative agent on all of the cell lines tested. On this set of cell lines, BN80927 has IC50 values 2–81 nM.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:56:50 GMT 2025` Edited by `admin` on `Mon Mar 31 20:56:50 GMT 2025`
Record UNII	5WM1F45I4Y
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BN 80927

Preferred Name

English

Elomotecan hydrochloride

Common Name

English

BN-80927

Code

English

Code System Code Type Description

FDA UNII

5WM1F45I4Y