BENDAZAC LYSINE DIHYDRATE

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C16H14N2O3.C6H14N2O2.2H2O
Molecular Weight	464.5121
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.O.NCCCC[C@H](N)C(O)=O.OC(=O)COC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3

InChI

InChIKey=PSIKNBYUZWDTBM-QEJHLSQBSA-N

InChI=1S/C16H14N2O3.C6H14N2O2.2H2O/c19-15(20)11-21-16-13-8-4-5-9-14(13)18(17-16)10-12-6-2-1-3-7-12;7-4-2-1-3-5(8)6(9)10;;/h1-9H,10-11H2,(H,19,20);5H,1-4,7-8H2,(H,9,10);2*1H2/t;5-;;/m.0../s1

HIDE SMILES / InChI

Molecular Formula	C6H14N2O2
Molecular Weight	146.1876
Charge	0
Count

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

Molecular Formula	C16H14N2O3
Molecular Weight	282.294
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/2190795
Curator's Comment: description was created based on several sources, including: http://database.japic.or.jp/pdf/newPINS/00056628.pdf http://www.kegg.jp/medicus-bin/japic_med?japic_code=00056628 http://www.ncbi.nlm.nih.gov/pubmed/5317253

Bendazac, (1-benzyl-1H-indazol-3-yl-oxy)-acetic acid, is structurally related to indomethacin. Its lysine salt has been reported to be absorbed better than the parent compound. It is applied topically as bendazac lysine 0.5% (wt/vol) aqueous solution for delaying the progression of cataract. Topical application of bendazac is associated with transient burning sensation. It reduces the secretion of the skin ulcer surface, promotes skin formation and accelerates tissue repair.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
reactive oxygen species 8 Target ID: reactive oxygen species Sources: http://www.ncbi.nlm.nih.gov/pubmed/8736488	Modulator 846
Xanthine dehydrogenase/oxidase 41 Target ID: CHEMBL1075246 Sources: http://www.ncbi.nlm.nih.gov/pubmed/21781693	Inhibitor 8504		0.33 mM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Burn ulcer and radiation ulcers 4 Sources: http://database.japic.or.jp/pdf/newPINS/00056628.pdf	Primary	Approved 8583	Zildasac Ointment Approved Use Indications: Pressure sores, burns ulcers, radiation ulcers; Contact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster
Contact dermatitis 20 Sources: http://database.japic.or.jp/pdf/newPINS/00056628.pdf	Primary	Approved 8583	Zildasac Ointment Approved Use Indications: Pressure sores, burns ulcers, radiation ulcers; Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster
Eczema 46 Sources: http://database.japic.or.jp/pdf/newPINS/00056628.pdf	Primary	Approved 8583	Zildasac Ointment Approved Use Indications: Pressure sores, burns ulcers, radiation ulcers; Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster
Psoriasis vulgaris 5 Sources: http://database.japic.or.jp/pdf/newPINS/00056628.pdf	Primary	Approved 8583	Zildasac Ointment Approved Use Indications: Pressure sores, burns ulcers, radiation ulcers; Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster
Herpes zoster infections 15 Sources: http://database.japic.or.jp/pdf/newPINS/00056628.pdf	Palliative	Approved 8583	Zildasac Ointment Approved Use Indications: Pressure sores, burns ulcers, radiation ulcers; Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster
Cataract 15 Sources: http://www.120ty.net/bencandy.php?fid=52&id=44224	Primary	Approved 8583	BENDAZAC LYSINE Approved Use Adjuvant in the treatment of cataracts (cataract degenerative presenile and senile, juvenile cataracts, diabetic cataract, opacification of the cortex or the crystalline core of different origin and nature)

C_max

Value	Dose	Analyte	Population
41.9 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
36.4 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
41.9 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
27.6 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
31.2 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
25.5 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
159 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
339 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
159 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
150 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
149 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
84 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
3.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Analyte	Population
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/		BENDAZAC plasma	Homo sapiens
0.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.8% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.7% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	BENDAZAC plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
500 mg 3 times / day multiple, oral Studied dose Dose: 500 mg, 3 times / day Route: oral Route: multiple Dose: 500 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2889942/	unhealthy Health Status: unhealthy Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2889942/	Disc. AE: Hepatotoxicity... AEs leading to discontinuation/dose reduction: Hepatotoxicity (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/2889942/

AEs

AE	Significance	Dose	Population
Hepatotoxicity	2 patients Disc. AE	500 mg 3 times / day multiple, oral Studied dose Dose: 500 mg, 3 times / day Route: oral Route: multiple Dose: 500 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2889942/	unhealthy Health Status: unhealthy Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2889942/

PubMed

Title	Date	PubMed
Antidenaturant drugs for cataract and other condensation diseases.	2001 Jan	11133267
Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents.	2010 Apr 1	20223660

Patents

Sample Use Guides

In Vivo Use Guide

Single Dose Eye drops: 2 drops in each eye or half the contents of a single-dose, three times a day Multi-dose eye drops: 2 drops in each eye, three times a day oral: single dosage benzadac lysine in tables (500 mg) Skin ulcers: An appropriate amount of this product is applied to the affected area several times a day. Incidentally, it performs patch therapy 1-2 times daily as needed. Inflammatory skin disease: An appropriate amount of this product is applied to the affected area several times a day.

Route of Administration: Other

In Vitro Use Guide

The inhibition of labelled cyanate binding to lens proteins increased with increasing concentration of bendazac (max at 40 mM).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:51:49 GMT 2025` Edited by `admin` on `Mon Mar 31 17:51:49 GMT 2025`
Record UNII	MOQ12WCD7V
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BENDAZAC LYSINE DIHYDRATE

Common Name

English

2-((1-(PHENYLMETHYL)-1H-INDAZOL-3-YL)OXY)ACETIC ACID, L-LYSINE SALT DIHYDRATE

Preferred Name

English

Code System Code Type Description

PUBCHEM

70401396

Created by admin on Mon Mar 31 17:51:49 GMT 2025 , Edited by admin on Mon Mar 31 17:51:49 GMT 2025

PRIMARY

SMS_ID

300000029337

Created by admin on Mon Mar 31 17:51:49 GMT 2025 , Edited by admin on Mon Mar 31 17:51:49 GMT 2025

PRIMARY

FDA UNII

MOQ12WCD7V

Created by admin on Mon Mar 31 17:51:49 GMT 2025 , Edited by admin on Mon Mar 31 17:51:49 GMT 2025

PRIMARY

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Details

SMILES

InChI

DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/2190795Curator's Comment: description was created based on several sources, including: http://database.japic.or.jp/pdf/newPINS/00056628.pdf http://www.kegg.jp/medicus-bin/japic_med?japic_code=00056628 http://www.ncbi.nlm.nih.gov/pubmed/5317253

Originator

Approval Year

Targets

Conditions

Approved Use

Approved Use

Approved Use

Approved Use

Approved Use

Approved Use

Cmax

AUC

T1/2

Funbound

Doses

AEs

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound