LOBENZARIT

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H10ClNO4
Molecular Weight	291.687
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)C1=C(NC2=C(C=CC(Cl)=C2)C(O)=O)C=CC=C1

InChI

InChIKey=UGDPYGKWIHHBMB-UHFFFAOYSA-N

InChI=1S/C14H10ClNO4/c15-8-5-6-10(14(19)20)12(7-8)16-11-4-2-1-3-9(11)13(17)18/h1-7,16H,(H,17,18)(H,19,20)

HIDE SMILES / InChI

Description
Sources: https://chugai-pharm.jp/hc/ss/pr/drug/car_fil0080/shiori/PDF/en/car_s_en.pdf
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/9161931 | http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=750

Lobenzarit is an immunomodulator and antioxidative agent, which has been used successfully in Japan for the treatment of rheumatoid arthritis. Lobenzarit is a scavenger of oxygen-free radicals such as hydroxyl radicals, superoxide, peroxyl and singlet oxygen. Side effects of this medicine are: decreased/considerably increased urinary volume, bloody urine, frequent urination.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glutathione reductase, mitochondrial 4 Target ID: P00390 Gene ID: 2936.0 Gene Symbol: GSR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8748682 \| https://www.ncbi.nlm.nih.gov/pubmed/8285143	Activator 1430
Glutathione S-transferases (rat) 2 Target ID: Glutathione S-transferases (rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8748682	Inhibitor 8297
response to oxidative stress 20 Target ID: GO:0006979 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9161931	Modulator 828

Conditions

Condition	Modality	Targets	Highest Phase	Product
Chronic rheumatoid arthritis 4 Sources: https://chugai-pharm.jp/hc/ss/pr/drug/car_fil0080/shiori/PDF/en/car_s_en.pdf https://chugai-pharm.jp/hc/ss/pr/drug/car_fil0040/if/PDF/car_if.pdf	Primary		Approved 8429	CARFENIL Approved Use This medicine improves immune abnormality and reduces inflammation and swelling of joints and so on. It is usually used to treat chronic rheumatoid arthritis. Launch Date 1986

PubMed

Title	Date	PubMed
Alpha-methyldopa-type autoimmune hemolytic anemia caused by lobenzarit disodium of a mefenamic acid derivative and immunomodulator.	1994 May 15	8180406
Study of the critical points in lobenzarit disodium hydrophilic matrices for controlled drug delivery.	2006 May	16651752
Estimation of the percolation thresholds in ternary lobenzarit disodium-dextran-HPMC hydrophilic matrices tablets: effects of initial porosity.	2009 Nov 5	19666114

Patents

Sample Use Guides

In Vivo Use Guide

2 tablets (80 mg of the active ingredient) at a time, 3 times a day, in combination with other antiphlogistic analgesic

Route of Administration: Oral

In Vitro Use Guide

The Iobenzarit at concentrations of 1, 30, 100 and 1000 uM Iobenzarit had no inhibitory effect on various rat liver microsomal P-450 activities: on the ethoxyresorufin O-dealkylation activity, on the pentoxyresorufin O-deaikylation activity or on the p-nitrophenol hydroxylation activity, when measured in liver microsomes isolated from rats induced with beta-naphthoflavone, phenobarbital and pyrazol.

Name

Type

Language

LOBENZARIT

Official Name

English

LOBENZARIT [MI]

Common Name

English

Lobenzarit [WHO-DD]

Common Name

English

4-CHLORO-2,2'-IMINODIBENZOATE

Systematic Name

English

lobenzarit [INN]

Common Name

English

BENZOIC ACID, 2-((2-CARBOXYPHENYL)AMINO)-4-CHLORO-

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C275