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Chemistry

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Also known as: 20187-55-7, Bendazolic acid, Bindazac, 2-(1-benzyl-1h-indazol-3-yloxy)acetic acid, Zildasac, Versus
Molecular Formula
C16H14N2O3
Molecular Weight
282.29  g/mol
InChI Key
BYFMCKSPFYVMOU-UHFFFAOYSA-N
FDA UNII
G4AG71204O

Bendazac
Bendazac is an oxyacetic acid. Despite possessing anti-inflammatory, anti-necrotic, choleretic, and anti-lipidemic characteristics, most research has revolved around studying and demonstrating the agent's principal action in inhibiting the denaturation of proteins - an effect that has primarily proven useful in managing and delaying the progression of ocular cataracts [A39863. A39863]. Bendazac, however, has since been withdrawn or discontinued in various international regions due to its capability or risk for eliciting hepatotoxicity in patients although a small handful of regions may continue to have the medication available for purchase and use either as a topical anti-inflammatory/analgesic cream or eye drop formulation.
1 2D Structure

Bendazac

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-(1-benzylindazol-3-yl)oxyacetic acid
2.1.2 InChI
InChI=1S/C16H14N2O3/c19-15(20)11-21-16-13-8-4-5-9-14(13)18(17-16)10-12-6-2-1-3-7-12/h1-9H,10-11H2,(H,19,20)
2.1.3 InChI Key
BYFMCKSPFYVMOU-UHFFFAOYSA-N
2.1.4 Canonical SMILES
C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)OCC(=O)O
2.2 Other Identifiers
2.2.1 UNII
G4AG71204O
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Bendazolic Acid

2. Bendazolic Acid, Sodium Salt

3. Bindazac

2.3.2 Depositor-Supplied Synonyms

1. 20187-55-7

2. Bendazolic Acid

3. Bindazac

4. 2-(1-benzyl-1h-indazol-3-yloxy)acetic Acid

5. Zildasac

6. Versus

7. Bendazaco

8. Bendazacum

9. Iwazac

10. 1-benzylindazole-3-oxyacetic Acid

11. 2-((1-benzyl-1h-indazol-3-yl)oxy)acetic Acid

12. Af 983

13. ((1-(phenylmethyl)-1h-indazol-3-yl)oxy)acetic Acid

14. Einecs 243-569-2

15. ((1-benzyl-1h-indazol-3-yl)oxy)acetic Acid

16. Unii-g4ag71204o

17. Brn 0893958

18. [(1-benzyl-1h-indazol-3-yl)oxy]acetic Acid

19. Acetic Acid, [[1-(phenylmethyl)-1h-indazol-3-yl]oxy]-

20. Af 1934 [lysine]

21. Chebi:31257

22. G4ag71204o

23. Mfcd00866158

24. Acetic Acid, ((1-benzyl-1h-indazol-3-yl)oxy)-

25. Bindazac; Dogalina; Zildasac; Zildazac

26. Acetic Acid, ((1-(phenylmethyl)-1h-indazol-3-yl)oxy)-

27. 2-[(1-benzyl-1h-indazol-3-yl)oxy]acetic Acid

28. [[1-(phenylmethyl)-1h-indazol-3-yl]oxy]acetic Acid

29. Dogalina

30. Bendazacum [inn-latin]

31. Bendazaco [inn-spanish]

32. 2-(1-benzylindazol-3-yl)oxyacetic Acid

33. ((1-benzyl-1h-indazol-3-yl)oxy)essigsaeure

34. Bendazac [usan:inn:ban:jan]

35. Iwazac (tn)

36. Bendaline (salt/mix)

37. Bendazac [usan]

38. Bendazac [inn]

39. Bendazac [jan]

40. Bendazac [mi]

41. Bendazac [mart.]

42. Bendazac [who-dd]

43. Bendazac Lysine (salt/mix)

44. Schembl25979

45. Af-1934 Lysine

46. Bendazac (jan/usan/inn)

47. (1-benzyl-1h-indazol-3-yloxy)-aceticacid

48. 5-23-11-00246 (beilstein Handbook Reference)

49. Af 1934 (salt/mix)

50. Af 1934 Free Acid

51. Af-1934 Free Acid

52. Zinc1000

53. Bendazac, >=98% (hplc)

54. Chembl1089221

55. Dtxsid1048334

56. Bcp15554

57. Af-983

58. S5361

59. Akos000279916

60. Ab07517

61. Ac-6789

62. Ccg-267264

63. Db13501

64. Ks-1230

65. [(1-benzyl-3-indazolyl)oxy]acetic Acid

66. Bb166154

67. Hy-17480

68. Sy014542

69. 1-benzyl-3-[1-(carboxy)methoxy]indazole

70. B4223

71. Cs-0009216

72. Ft-0656910

73. D01594

74. [(1-benzyl-1h-indazol-3-yl)-oxy]acetic Acid

75. 187b557

76. A814317

77. Q862414

78. J-013103

79. Acetic Acid, 2-[[1-(phenylmethyl)-1h-indazol-3-yl]oxy]-

80. 2-(1-benzylindazol-3-yl)oxyacetic Acid;2-(1-benzyl-1h-indazol-3-yloxy)acetic Acid

81. Acetic Acid, ((1-(phenylmethyl)-1h-indazol-3-yl)oxy)- (2) ((1-benzyl-1h-indazol-3-yl)oxy)acetic Acid.

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 282.29 g/mol
Molecular Formula C16H14N2O3
XLogP33.1
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count5
Exact Mass282.10044231 g/mol
Monoisotopic Mass282.10044231 g/mol
Topological Polar Surface Area64.4 Ų
Heavy Atom Count21
Formal Charge0
Complexity357
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Prior to the withdrawal of bendazac from various international regions of use due to concerns for hepatotoxicity the chemical had demonstrated potential usefulness predominantly as the prescription medication bendazac lysine for the indication of managing the level of vision in patients with mild to moderate cataracts to facilitate delaying the need for surgical intervention. Elsewhere bendazac may still be available in a limited capacity as a non-prescription topical cream product for treating conditions like local pain, inflammation, dermatitis, eczema, pruritis, hives, insect bites, burns, erythema, and others - although such products may also be facing general discontinuation.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Bendazac principally demonstrates an antidenaturant action on proteins. This effect has been shown to inhibit the denaturation of various proteins like ocular lens proteins by heat, ultraviolet radiation, free radicals, and other chemicals. The medication may be administered to patients via a number of different formulations, including orally as the lysine salt, as eye drops, or even topical applications for the skin. Some preliminary studies have suggested that an apparent improvement of the blood-retinal barrier had been observed in diabetic patients using bendazac lysine 500 mg three times a day for three to six months. Moreover, the use of topical bendazac has also been shown to demonstrate anti-inflammatory effects in animal models and clinical studies to effectively treat varied dermatoses, especially those involving a necrotic component. Additionally, bendazac has also demonstrated choleretic and antilipidaemic activities that have resulted in substantial reductions in beta/alpha lipoprotein ratio, and total lipid, total cholesterol, and triglyceride levels in patients with dyslipidaemia using oral bendazac lysine 500 mg three times daily. The medication has also elicited the inhibition of phytohaemagglutinin induced lymphocyte transformation in vitro.


5.2 MeSH Pharmacological Classification

Anti-Inflammatory Agents, Non-Steroidal

Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. (See all compounds classified as Anti-Inflammatory Agents, Non-Steroidal.)


5.3 ATC Code

M - Musculo-skeletal system

M02 - Topical products for joint and muscular pain

M02A - Topical products for joint and muscular pain

M02AA - Antiinflammatory preparations, non-steroids for topical use

M02AA11 - Bendazac


S - Sensory organs

S01 - Ophthalmologicals

S01B - Antiinflammatory agents

S01BC - Antiinflammatory agents, non-steroids

S01BC07 - Bendazac


5.4 Absorption, Distribution and Excretion

Absorption

Administered as its lysine salt, a 500 mg oral tablet of bendazac is well absorbed into the human body with maximum plasma concentrations Cmax ranging from 35 to 55 mg/L being attained within 0.5 to 1 hour in healthy volunteers after oral administration of a single 500 mg dose.


Route of Elimination

About 60% of a dose of bendazac is eliminated via the urine as its primary metabolite, 5-hydroxybendazac. Approximately 15% of a dose is eliminated as unchanged drug and bendazac glucuronide in the urine as well.


Volume of Distribution

The volume of distribution documented for bendazac is 0.16 L/kg.


Clearance

The plasma clearance recorded for bendazac is given as 0.018 to 0.054 L/h/kg with a mean of 0.033 L/h/kg.


5.5 Metabolism/Metabolites

Bendazac is largely eliminated by metabolism, where more than 60% of an administered dose is excreted in the urine as the hydroxylated primary metabolite 5-hydroxybendazac and its glucuronide while up to approximately 15% of a bendazac dose is also excreted in the urine unchanged and as a glucuronide. Unfortunately, there is little data available regarding the specific enzymes responsible for bendazac's metabolism.


5.6 Biological Half-Life

The plasma elimination half-life recorded for bendazac is given as 1.7 to 5.2 hours, with a mean of 3.5 hours.


5.7 Mechanism of Action

Bendazac seems to elicit an anticataract action by inhibiting the denaturation of ocular lens proteins, although the precise mechanisms by which this action occurs has not yet been formally elucidated - despite there being many proposed mechanisms. In particular, the denaturation of lens proteins may in part be prevented by inhibiting the binding of certain chemicals like cyanates or sugars and 5-hydroxybendazac - the major metabolite of bendazac - has been shown to be capable of inhibiting the glycosylation of lens proteins by sugars like galactose or glucose-6-phosphate in a dose-dependent manner. Moreover, the apparent ability for administered bendazac to elicit free radical scavenger activities due to interactions with protein molecules suggests that the medication may also be able to prevent the oxidation of lens proteins by free radicals in the development of cataracts. Furthermore, bendazac may also be capable of reducing the sulfhydryl group oxidation of lens proteins by the saliva, serum, or urine from patients with cataracts following single dose administration and reduce biological liquid oxidant activity (BLOA) in doing so. Otherwise, it is believed that bendazac also possesses non-steroidal anti-inflammatory actions, as well as analgesic, antipyretic, and platelet-inhibitory effects These effects may be accounted for in part by the substance's capability to inhibit prostaglandin synthesis by inhibiting cyclooxygenase activity in converting arachidonic acid to cyclic endoperoxides - the precursors of prostaglandins.


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