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Chemistry

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Also known as: Vexol, 49697-38-3, Rimexolon, Org-6216, Org 6216, Mls002154105
Molecular Formula
C24H34O3
Molecular Weight
370.5  g/mol
InChI Key
QTTRZHGPGKRAFB-OOKHYKNYSA-N
FDA UNII
O7M2E4264D

Rimexolone
Rimexolone is a derivative of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive property. Upon binding to the cytosolic glucocorticoid receptor and cell entry, rimexolone activates specific glucocorticoid response elements, resulting in altered gene expression. These include induction of synthesis of anti-inflammatory protein IkappaB-alpha and inhibition of synthesis of nuclear factor kappaB (NFkappa B). As a result, pro-inflammatory cytokine production such as interleukin-1 (IL-1), IL-2 and IL-6 is down-regulated and cytotoxic T-lymphocyte activation inhibited. Therefore, an overall reduction in chronic inflammation and autoimmune reactions may be achieved.
Rimexolone is a Corticosteroid. The mechanism of action of rimexolone is as a Corticosteroid Hormone Receptor Agonist.
1 2D Structure

Rimexolone

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
2.1.2 InChI
InChI=1S/C24H34O3/c1-6-20(27)24(5)14(2)11-18-17-8-7-15-12-16(25)9-10-22(15,3)21(17)19(26)13-23(18,24)4/h9-10,12,14,17-19,21,26H,6-8,11,13H2,1-5H3/t14-,17+,18+,19+,21-,22+,23+,24-/m1/s1
2.1.3 InChI Key
QTTRZHGPGKRAFB-OOKHYKNYSA-N
2.1.4 Canonical SMILES
CCC(=O)C1(C(CC2C1(CC(C3C2CCC4=CC(=O)C=CC34C)O)C)C)C
2.1.5 Isomeric SMILES
CCC(=O)[C@]1([C@@H](C[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)O)C)C)C
2.2 Other Identifiers
2.2.1 UNII
O7M2E4264D
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 11 Beta-hydroxy-16 Alpha,17 Alpha,21-trimethylpregna-1,4-diene-3,20-dione

2. Org 6216

3. Org-6216

4. Rimexel

5. Vexol

2.3.2 Depositor-Supplied Synonyms

1. Vexol

2. 49697-38-3

3. Rimexolon

4. Org-6216

5. Org 6216

6. Mls002154105

7. Rimexel

8. O7m2e4264d

9. Trimexolone

10. Rimexolona

11. Rimexolonum

12. Rimexolonum [inn-latin]

13. Rimexolona [inn-spanish]

14. Unii-o7m2e4264d

15. Rimexolone [usan:usp:inn:ban]

16. Vexol (tn)

17. Al 02178

18. Rimexolone [mi]

19. Rimexolone (usp/inn)

20. Rimexolone [inn]

21. Prestwick0_001020

22. Prestwick1_001020

23. Prestwick2_001020

24. Prestwick3_001020

25. Rimexolone [usan]

26. Rimexolone [vandf]

27. Rimexolone [mart.]

28. Rimexolone [usp-rs]

29. Rimexolone [who-dd]

30. Bspbio_001179

31. Schembl445300

32. Spbio_003050

33. Bpbio1_001297

34. Gtpl7099

35. Chembl1200617

36. Rimexolone [orange Book]

37. Rimexolone [usp Impurity]

38. Chebi:135566

39. Hms1571k21

40. Hms2098k21

41. Hms2235b18

42. Hms3715k21

43. Rimexolone [usp Monograph]

44. Hy-b1754

45. Zinc3945984

46. 11beta-hydroxy-16alpha,17,21-trimethyl-1,4-pregnadien-3,20-dion

47. Bdbm50103606

48. 11beta-hydroxy-16alpha,17alpha-dimethyl-17-propionylandrosta-1,4-dien-3-one

49. Al-2178

50. Ccg-221020

51. Db00896

52. Ncgc00179273-01

53. (8s,9s,10r,11s,13s,14s,16r,17s)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-3-one

54. Smr001233413

55. Ab00514006

56. Cs-0013781

57. D05729

58. 697r383

59. Sr-01000841221

60. Q7334443

61. Sr-01000841221-2

62. Brd-k31627533-001-03-8

63. 11.beta.-hydroxy-16.alpha.,17.alpha.-dimethyl-17-propionylandrosta-1,4-dien-3-one

64. (11beta, 16alpha, 17beta)-11-hydroxy-16,17-dimethyl-17-(1-oxopropyl)androstra-1,4-dien-3-one

65. (11beta,16alpha,17beta)-11-hydroxy-16,17-dimethyl-17-(1-oxopropyl)androsta-1,4-dien-3-one

66. Androsta-1,4-dien-3-one, 11-hydroxy-16,17-dimethyl-17-(1-oxopropyl)-, (11.beta.,16,alpha.,17.beta.)-

67. Androsta-1,4-dien-3-one, 11-hydroxy-16,17-dimethyl-17-(1-oxopropyl)-, (11beta,16alpha,17beta)-

2.4 Create Date
2005-12-16
3 Chemical and Physical Properties
Molecular Weight 370.5 g/mol
Molecular Formula C24H34O3
XLogP33.5
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count3
Rotatable Bond Count2
Exact Mass370.25079494 g/mol
Monoisotopic Mass370.25079494 g/mol
Topological Polar Surface Area54.4 Ų
Heavy Atom Count27
Formal Charge0
Complexity749
Isotope Atom Count0
Defined Atom Stereocenter Count8
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameVexol
PubMed HealthRimexolone (Into the eye)
Drug ClassesOphthalmologic Agent
Drug LabelVEXOL 1% Ophthalmic Suspension is a sterile, multi-dose topical ophthalmic suspension containing the corticosteroid, rimexolone. Rimexolone is a white, water-insoluble powder with an empirical formula of C24H34O3 and a molecular weight of 370.53. I...
Active IngredientRimexolone
Dosage FormSuspension/drops
RouteOphthalmic
Strength1%
Market StatusPrescription
CompanyAlcon

2 of 2  
Drug NameVexol
PubMed HealthRimexolone (Into the eye)
Drug ClassesOphthalmologic Agent
Drug LabelVEXOL 1% Ophthalmic Suspension is a sterile, multi-dose topical ophthalmic suspension containing the corticosteroid, rimexolone. Rimexolone is a white, water-insoluble powder with an empirical formula of C24H34O3 and a molecular weight of 370.53. I...
Active IngredientRimexolone
Dosage FormSuspension/drops
RouteOphthalmic
Strength1%
Market StatusPrescription
CompanyAlcon

4.2 Drug Indication

For the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Rimexolone is a glucocorticoid corticosteroid for systemic use. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation.


5.2 MeSH Pharmacological Classification

Glucocorticoids

A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system. (See all compounds classified as Glucocorticoids.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
RIMEXOLONE
5.3.2 FDA UNII
O7M2E4264D
5.3.3 Pharmacological Classes
Mechanisms of Action [MoA] - Corticosteroid Hormone Receptor Agonists
5.4 ATC Code

H - Systemic hormonal preparations, excl. sex hormones and insulins

H02 - Corticosteroids for systemic use

H02A - Corticosteroids for systemic use, plain

H02AB - Glucocorticoids

H02AB12 - Rimexolone


S - Sensory organs

S01 - Ophthalmologicals

S01B - Antiinflammatory agents

S01BA - Corticosteroids, plain

S01BA13 - Rimexolone


5.5 Absorption, Distribution and Excretion

Absorption

Systemically absorbed.


Route of Elimination

Following IV administration of radio-labelled rimexolone to rats, greater than 80% of the dose is excreted via the feces as rimexolone and metabolites.


5.6 Metabolism/Metabolites

Undergoes extensive metabolism. Following intravenous administration of radiolabeled rimexolone in rats, more than 80% of the dose was excreted in the feces as rimexolone and metabolites. Metabolites have been shown to be either less active than rimexolone or inactive in human glucocorticoid receptor binding assays.


5.7 Biological Half-Life

The serum half-life of rimexolone could not be reliably estimated due to the large number of samples below the quantitation limit of the assay (80 pg/mL). However, based on the time required to reach steady-state, the half-life appears to be short (1-2 hours).


5.8 Mechanism of Action

Rimexolone is a glucocorticoid receptor agonist. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. By binding to the glucocorticoid receptor, this drug ultimately leads to changes in genetic transcription involving the lipocortins and prostaglandins.


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