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Epitopic

Epitopic structure

CAS No:
23674-86-4
Formula:
C27H34F2O7
Chemical Name:
Epitopic
Synonyms:
Pregna-1,4-diene-3,20-dione,21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)-,(6α,11β)-;Pregna-1,4-diene-3,20-dione,6α,9-difluoro-11β,17,21-trihydroxy-,21-acetate 17-butyrate;Butyric acid,17-ester with 6α,9-difluoro-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate;(6α,11β)-21-(Acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)pregna-1,4-diene-3,20-dione;Difluprednate;6α,9α-Difluoroprednisolone 21-acetate 17-butyrate;6a,9-Difluoro-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate 17-butyrate;W 6309;6α,9-Difluoroprednisolone 21-acetate 17-butyrate;Myser;Epitopic;CM 9155;Durezol;6-Alpha,9α-difluoroprednisolone 21-acetate 17-butyrate
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.IC50 value:Target: Difluprednate ophthalmic emulsion 0.05% is also being studied in other ocular inflammatory diseases, including a U.S. Phase 3 study evaluating difluprednate for the treatment of anterior uveitis.

Solid

Difluprednate is a corticosteroid hormone and a butyrate ester.|Difluprednate is a topical corticosteroid indicated for the treatment of infammation and pain associated with ocular surgery. It is a butyrate ester of 6(α), 9(α)-difluoro prednisolone acetate. Difluprednate is abbreviated DFBA, or difluoroprednisolone butyrate acetate. It is indicated for treatment of endogenous anterior uveiti.|Difluprednate is a topical corticosteroid and prednisolone acetate derivative, with anti-inflammatory activity. Upon instillation into the eye, difluprednate binds to and activates the glucocorticoid receptor (GR). The receptor-ligand complex binds to promoter regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of phospholipase A2 inhibitory proteins, thereby inhibiting the synthesis of arachidonic acid and preventing the synthesis of certain inflammatory mediators, such as prostaglandins and leukotrienes. This reduces ocular inflammation and pain.

Epitopic Basic Attributes

Molecular Weight：

508.55

Exact Mass：

508.55

EC Number：

245-815-4

UNII：

S8A06QG2QE

DSSTox ID：

DTXSID0046773

NCI Thesaurus Code：

C80259

ATC Code：

D - Dermatologicals

Characteristics

PSA：

107

XLogP3：

3.67

Appearance：

Solid

Density：

1.3±0.1 g/cm3

Melting Point：

191-194 °C

Boiling Point：

600.3±55.0 °C at 760 mmHg

Flash Point：

316.9±31.5 °C

Refractive Index：

1.545

Storage Conditions：

2-8°C

Vapor Pressure：

6.46E-17mmHg at 25°C

Specific rotation：

D22 +31.7° (c = 0.5 in dioxane)

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

RTECS Number：

TU3831500

Stability/Shelf Life：

Stable at normal temperatures and pressures.

Precautionary statement(s)：

P201, P202, P260, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P308+P313, P312, P314, P321, P322, P330, P332+P313, P337+P313, P362, P363, P403+P233, P405, P501

Hazard Statements：

H302+H312+H332

GHS Classification：

|Danger|H302+H312+H332 (33.33%): Harmful if swallowed, in contact with skin or if inhaled [Warning Acute toxicity, oral; acute toxicity, dermal; acute toxicity, inhalation]|P201, P202, P260, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P308+P313, P312, P314, P322, P330, P363, P405, and P501|Aggregated GHS information provided by 4 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity Summary：

Preclinical pharmacokinetic and toxicity studies have established that difluprednate ophthalmic emulsion 0.05% given 4 times a day is not toxic to the eye.

Drug Information

Drug Indication：

For the treatment of inflammation and pain associated with ocular surgery.|FDA Label

Pharmacology：

Difluprednate is a corticosteroid used as an anti-inflammatory steroidal drug used primarily in ocular surgery.

MeSH：

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.)

Absorption：

Difluprednate penetrates the corneal epithelium rapidly and effectively. Low systemic absorption.|78.5% of radioactivity was excreted aftert 24 hours, and 99.5% by 7 days after a single dose of labeled difluprednate instilled in the right eyes of pigmented rabbits.

Metabolism/Metabolites：

Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the drug’s active metabolite. Endogenous tissue esterases then metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), which limits systemic exposure to the active compound.

Mechanism of Action：

Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). It is postulated that these proteins control the biosynthesis of potent mediators of infammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

MeSH Entry Terms：

C.M.9155

Epitopic Use and Manufacturing

Uses

A corticosteroid (derivative of prednisolone), approved for the treatment of post-operative ocular inflammation.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:508.5
XLogP3:3.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:8
Exact Mass:508.22725974
Monoisotopic Mass:508.22725974
Topological Polar Surface Area:107
Heavy Atom Count:36
Complexity:1050
Defined Atom Stereocenter Count:8
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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