ANISPERIMUS

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H39N7O3
Molecular Weight	401.5474
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C[C@@H](N)CCNCCCCNC(=O)OCC(=O)NCCCCCCNC(N)=N

InChI

InChIKey=PZDPVSFZTKORSP-OAHLLOKOSA-N

InChI=1S/C18H39N7O3/c1-15(19)8-13-22-9-6-7-12-25-18(27)28-14-16(26)23-10-4-2-3-5-11-24-17(20)21/h15,22H,2-14,19H2,1H3,(H,23,26)(H,25,27)(H4,20,21,24)/t15-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C18H39N7O3
Molecular Weight	401.5474
Charge	0
Count

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

Description
Sources: https://adisinsight.springer.com/drugs/800009259 | https://www.ncbi.nlm.nih.gov/pubmed/12393594

Anisperimus [LF 150195] is a deoxyspergualin analogue under development by Fournier Pharma (formerly Groupe Fournier) for the potential treatment of autoimmune disorders and transplant rejection. Anisperimus is a more potent, and less toxic analogue of 15-deoxyspergualin, an antibiotic used as an immunosuppressive agent to prevent rejection of organ transplants. Anisperimus enhances activation-induced T-cell death by facilitating caspase-8 and caspase-10 activation at the DISC level. Phase I clinical studies were being conducted by Fournier in France for Transplant rejection and Phase II clinical studies for Autoimmune disorders in Europe. However development of anisperimus has been discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
LF 15-0195 immunosuppressive agent enhances activation-induced T-cell death by facilitating caspase-8 and caspase-10 activation at the DISC level.	2003 Jan 1	12393594

Patents

Sample Use Guides

In Vivo Use Guide

Monkeys: Recipients received Anisperimus monotherapy at doses of 0.065 mg/kg per day (group 2, n=4), 0.13 mg/kg per day (group 3, n=4), or 0.2 mg/kg per day (group 4, n=4), administered subcutaneously, on postoperative days 0 to 14.

Route of Administration: Other

In Vitro Use Guide

Hoechst 33342 staining of the nuclear chromatin indicated thatexposure of Jurkat cells to Anisperimus [LF 150195] sensitized these cells to apoptosis triggered by various concentrations of CH-11 mAb and at various time points. Analysis of the dose-dependent effects of LF 15-0195 indicated that 0.1 uM was an optimal concentration for further studies. Higher concentra-tions such as 1uM and 10uM did not demonstrate significantly higher sensitization to 5 ng/mL CH11 anti-CD95 mAb. The 0.1uM concentration is about 10-fold lower than plasma levels measured in rats and monkeys receiving anintravenous injection of the studied compound.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:28:23 GMT 2023` Edited by `admin` on `Fri Dec 15 15:28:23 GMT 2023`
Record UNII	D0514P112G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ANISPERIMUS

Official Name

English

LF150195

Code

English

LF-150195

Code

English

LF 15-0195

Code

English

anisperimus [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C574