Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H34O3 |
Molecular Weight | 370.525 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC(=O)[C@@]1(C)[C@H](C)C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@H]3[C@@H](O)C[C@]12C
InChI
InChIKey=QTTRZHGPGKRAFB-OOKHYKNYSA-N
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
Molecular Formula | C24H34O3 |
Molecular Weight | 370.525 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/rimexolone-ophthalmic.html
http://www.rxlist.com/vexol-drug.htm
http://www.wikidoc.org/index.php/Rimexolone
Curator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/rimexolone-ophthalmic.html
http://www.rxlist.com/vexol-drug.htm
http://www.wikidoc.org/index.php/Rimexolone
Rimexolone is a glucocorticoid receptor agonist. Rimexolone ophthalmic (for the eyes) is used to treat eye inflammation caused by infections, injury, surgery, or other conditions. It is FDA approved for the treatment of post-operative inflammation and anterior uveitis. Common adverse reactions include hypotension, erythema, pruritus, taste sense altered, headache, blurred vision, discharge from eye, pain in eye, pharyngitis, and rhinitis.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2034 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2386110 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | VEXOL Approved UseVEXOL® 1% (rimexolone ophthalmic suspension) is indicated for the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis. Launch Date1994 |
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Primary | VEXOL Approved UseVEXOL® 1% (rimexolone ophthalmic suspension) is indicated for the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis. Launch Date1994 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
564 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2347958 |
40 mg single, intraarticular dose: 40 mg route of administration: Intraarticular experiment type: SINGLE co-administered: |
RIMEXOLONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1091 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2347958 |
80 mg single, intraarticular dose: 80 mg route of administration: Intraarticular experiment type: SINGLE co-administered: |
RIMEXOLONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1331 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2347958 |
120 mg single, intraarticular dose: 120 mg route of administration: Intraarticular experiment type: SINGLE co-administered: |
RIMEXOLONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1786 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2347958 |
160 mg single, intraarticular dose: 160 mg route of administration: Intraarticular experiment type: SINGLE co-administered: |
RIMEXOLONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1 % 4 times / day steady, ophthalmic Recommended Dose: 1 %, 4 times / day Route: ophthalmic Route: steady Dose: 1 %, 4 times / day Sources: |
unhealthy |
Disc. AE: Ocular pain... AEs leading to discontinuation/dose reduction: Ocular pain (2%) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Ocular pain | 2% Disc. AE |
1 % 4 times / day steady, ophthalmic Recommended Dose: 1 %, 4 times / day Route: ophthalmic Route: steady Dose: 1 %, 4 times / day Sources: |
unhealthy |
PubMed
Title | Date | PubMed |
---|---|---|
Intraocular pressure-raising potential of 1.0% rimexolone in patients responding to corticosteroids. | 1996 Aug |
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Pharmacological validation of a feline model of steroid-induced ocular hypertension. | 1999 Mar |
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Ocular-hypertensive and anti-inflammatory response to rimexolone therapy in children. | 2003 Dec |
|
Two cases of corneal ulcer due to methicillin-resistant Staphylococcus aureus in high risk groups. | 2010 Aug |
|
Rimexolone inhibits proliferation, cytokine expression and signal transduction of human CD4+ T-cells. | 2010 Jun 15 |
Patents
Sample Use Guides
Post-Operative Inflammation: Apply one - two drops of Rimexolone 1% Ophthalmic Suspension into the conjunctival sac of the affected eye four times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period.
Anterior Uveitis: Apply one - two drops of Rimexolone 1% Ophthalmic Suspension into the conjunctival sac of the affected eye every hour during waking hours for the first week, one drop every two hours during waking hours of the second week, and then taper until uveitis is resolved.
Route of Administration:
Topical
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20363256
Isolated CD4+ T-cells were pre-incubated with rimexolone at different concentrations for 10 min (10(-11)/10(-8)/10(-5)M) and stimulated with anti-CD3/anti-CD28 for 96 h. Proliferation was determined by flow cytometry. The percentage of dividing cells was significantly reduced by 10(-5)M rimexolone.
Substance Class |
Chemical
Created
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Record UNII |
O7M2E4264D
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Record Status |
Validated (UNII)
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NDF-RT |
N0000175450
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WHO-VATC |
QS01BA13
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WHO-ATC |
S01BA13
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NCI_THESAURUS |
C521
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WHO-ATC |
H02AB12
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N0000175576
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QH02AB12
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C47705
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CHEMBL1200617
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C013769
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100000092226
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Rimexolone
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DB00896
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RIMEXOLONE
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CC-77
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Related Record | Type | Details | ||
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TARGET -> AGONIST |
Related Record | Type | Details | ||
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ACTIVE MOIETY |