Page last updated: 2024-12-08

difluprednate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

difluprednate: RN given refers to (6alpha,11beta)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID443936
CHEMBL ID1201749
CHEBI ID31485
SCHEMBL ID4580
MeSH IDM0065341

Synonyms (83)

Synonym
MLS001333701
MLS001148580
dfba
MLS000028663 ,
6alpha,9alpha-difluoroprednisolone 21-acetate 17-butyrate
smr000058924
difluprednate
23674-86-4
6-alpha,9-alpha-difluoroprednisolone 17-butyrate 21-acetate
myser
6alpha-9-difluoroprednisolone 21-acetate 17-butyrate
w 6309
cm 9155
difluprednato [inn-spanish]
6alpha,9-difluoro-11beta,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate 17-butyrate
21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)pregna-1,4-diene-3,20-dione (6alpha,11beta)-
difluprednate [usan:inn:jan]
epitopic
difluprednatum [inn-latin]
pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)-, (6alpha,11beta)-
einecs 245-815-4
pregna-1,4-diene-3,20-dione, 6-alpha,9-difluoro-11-beta,17,21-trihydroxy-, 21-acetate, 17-butyrate
6alpha,9alpha-difluoroprednisolone 21-acetate 17-butyrate, >=98%
D01266
durezol (tn)
difluprednate (jan/usan/inn)
difluoroprednisolone butyrate acetate
DB06781
chebi:31485 ,
w-6309 ,
CHEMBL1201749
[(6s,8s,9r,10s,11s,13s,14s,17r)-17-(2-acetyloxyacetyl)-6,9-difluoro-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] butanoate
cas-23674-86-4
tox21_112628
dtxsid0046773 ,
dtxcid8026773
HMS2231D18
S4095
s8a06qg2qe ,
durezol
unii-s8a06qg2qe
difluprednato
difluprednatum
difluprednate [inn]
difluprednate [vandf]
difluprednate [usan]
pregna-1,4-diene-3,20-dione, 21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)-, (6.alpha.,11.beta.)-
difluprednate [orange book]
difluprednate [who-dd]
difluprednate [mi]
difluprednate [mart.]
difluprednate [jan]
HY-17569
SCHEMBL4580
gtpl7474
Q-101389
OPERA_ID_1287
AB00383058_10
mfcd00214273
(1r,2s,8s,10s,11s,14r,15s,17s)-14-[2-(acetyloxy)acetyl]-1,8-difluoro-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl butanoate
AKOS027326853
sr-01000000265
SR-01000000265-4
mls001148580-01!6alpha,9alpha-difluoroprednisolone 21-acetate 17-butyrate
st60-1
WYQPLTPSGFELIB-JTQPXKBDSA-N
AS-15800
Q736113
CCG-269762
pregna-1,4-diene-3,20-dione,21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)-, (6a,11b)-
A932746
(6alpha,11beta)-21-(acetyloxy)-6,9-difluoro-11-hydroxy-17-(1-oxobutoxy)pregna-1,4-diene-3,20-dion
d07ac19
difluprednate (mart.)
6 alpha-9-difluoroprednisolone 21-acetate 17-butyrate
difluprednato (inn-spanish)
difluprednatum (inn-latin)
difluprednate ophthalmic
difluprednate ophthalmic emulsion
D5579
6 alpha ,9 alpha -difluoroprednisolone 21-acetate 17-butyrate
(1r,3as,3bs,5s,9as,9br,10s,11as)-1-[2-(acetyloxy)acetyl]-5,9b-difluoro-10-hydroxy-9a,11a-dimethyl-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl butanoate
EN300-7378069

Research Excerpts

Overview

Difluprednate 0.05% is a new topical therapeutic option indicated for the treatment of inflammation and pain management associated with ocular surgery. The drug has an off-label potential for treatment of other anterior segment inflammatory conditions.

ExcerptReferenceRelevance
"Difluprednate is a potent and strong steroid which causes a rapid decrease in persistent diabetic macular edema."( Efficacy and safety of topical difluprednate in persistent diabetic macular edema.
Kaur, S; Sachdev, N; Singh, S; Yangzes, S, 2016
)
1.44
"Difluprednate 0.05% is a new topical therapeutic option indicated for the treatment of inflammation and pain management associated with ocular surgery with an off-label potential for treatment of other anterior segment inflammatory conditions. "( Intraocular pressure elevation from topical difluprednate use.
Meehan, K; Sowka, J; Vollmer, L, 2010
)
2.06
"Difluprednate is an effective agent for both control of anterior segment inflammation and reduction of CME in pediatric patients with uveitis when used as an adjuvant to systemic immunomodulatory therapy. "( Efficacy and potential complications of difluprednate use for pediatric uveitis.
Herlihy, E; Ongchin, S; Slabaugh, MA; van Gelder, RN, 2012
)
2.09

Effects

ExcerptReferenceRelevance
"Difluprednate 0.05% has a reported associated increase in intraocular pressure (IOP) in 3% of patients."( Intraocular pressure elevation from topical difluprednate use.
Meehan, K; Sowka, J; Vollmer, L, 2010
)
1.34
"Difluprednate 0.05% has a reported associated increase in intraocular pressure (IOP) in 3% of patients."( Intraocular pressure elevation from topical difluprednate use.
Meehan, K; Sowka, J; Vollmer, L, 2010
)
1.34

Treatment

Some dogs developed mild to severe alopecia of the periocular region, face, and distal pinna. Difluprednate-treated and loteprednol-treated eyes achieved a mean best-corrected visual acuity of at least 20/25 by 1 week postoperatively.

ExcerptReferenceRelevance
"Some difluprednate treated dogs developed mild to severe alopecia of the periocular region, face, and distal pinna (5/9)."( Localized alopecia and suppression of hypothalamic-pituitary-adrenal (HPA) axis in dogs following treatment with difluprednate 0.05% ophthalmic emulsion (Durezol®).
Anderson, AL; Burn, JB; Del Valle, JM; Harman, CD; Komáromy, AM; Langlois, DK; Noland, EL; Occelli, LM; Petersen, AD; Petersen-Jones, SM; Pirie, CG; Quantz, K, 2021
)
1.29
"Difluprednate-treated and loteprednol-treated eyes achieved a mean best-corrected visual acuity of at least 20/25 by 1 week postoperatively (0.055 and 0.061 logarithm of the minimum angle of resolution, respectively; P=0.82)."( Comparison of Efficacy of Difluprednate 0.05% and Loteprednol Gel 0.5% After Cataract Surgery.
Abessi, B; Brooksby, L; Schultze, RL, 2018
)
1.5

Toxicity

ExcerptReferenceRelevance
" However, the potential side effect of raised intraocular pressure limits its use as an adjuvant therapy in non-steroid responders."( Efficacy and safety of topical difluprednate in persistent diabetic macular edema.
Kaur, S; Sachdev, N; Singh, S; Yangzes, S, 2016
)
0.72
" Safety included evaluation of adverse events."( Difluprednate versus prednisolone acetate for inflammation following cataract surgery in pediatric patients: a randomized safety and efficacy study.
Gedif, K; Lambert, SR; Markwardt, K; O'Halloran, H; Plager, DA; Roarty, J; VanderVeen, D; Wilson, ME, 2016
)
1.88

Pharmacokinetics

ExcerptReferenceRelevance
" The main objectives of the current study were to evaluate the pharmacokinetic and pharmacodynamic features of DFBA when used as an ophthalmic agent, and to compare these features with those of other common ophthalmic agents, to determine which has the highest activity."( Pharmacokinetic features of difluprednate ophthalmic emulsion in rabbits as determined by glucocorticoid receptor-binding bioassay.
Kida, T; Sakaki, H; Tajika, T; Tsuzuki, M; Waki, M, 2011
)
0.66

Compound-Compound Interactions

ExcerptReferenceRelevance
" In this regard, the present study was conducted with the aim of studying the efficacy of using fixed drug combination (Difluprednate and Moxifloxacin) in reducing ocular inflammation and pain in post-operative patients undergoing cataract surgery."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.66
"Our study clearly shows that fixed drug combination of antibiotic and steroid does not cause raised IOP in about 97% of cases of SICS in the post-operative period and also improves the compliance of the patients."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.46

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Increased permeation and retention in the layer of the eye are required to improve the bioavailability of ocular drugs."( Investigating the effectiveness of Difluprednate-Loaded core-shell lipid-polymeric hybrid nanoparticles for ocular delivery.
Kaviarasi, B; Mehra, NK; Pooja, YS; Rajalakshmi, AN; Rajana, N; Singh, SB, 2023
)
1.19

Dosage Studied

Difluprednate provides effective treatment for anterior uveitis and requires less frequent dosing than prednisolone acetate. Both dosage regimens reduced postoperative ocular inflammation and pain safely and effectively.

ExcerptRelevanceReference
"5 micrograms/kg dosage is similar to a non-effect dose."( [Chronic toxicity study on difluprednate in dogs].
Higuchi, M; Higuchi, T; Kurashima, Y; Miida, H, 1985
)
0.57
" Both difluprednate dosage regimens reduced postoperative ocular inflammation and pain safely and effectively compared with the placebo."( Difluprednate ophthalmic emulsion 0.05% for postoperative inflammation and pain.
Cooke, DL; Crockett, RS; Korenfeld, MS; Silverstein, SM; Vogel, R, 2009
)
2.28
" Difluprednate provides effective treatment for anterior uveitis and requires less frequent dosing than prednisolone acetate."( Durezol (Difluprednate Ophthalmic Emulsion 0.05%) compared with Pred Forte 1% ophthalmic suspension in the treatment of endogenous anterior uveitis.
Crockett, RS; Davanzo, R; Flynn, TE; Foster, CS; McLeod, K; Vogel, R, 2010
)
1.69
" Using this information, we calculated dose-response curves, IC(50) values, and K(d) values to evaluate each drug's K(i) value."( Pharmacokinetic features of difluprednate ophthalmic emulsion in rabbits as determined by glucocorticoid receptor-binding bioassay.
Kida, T; Sakaki, H; Tajika, T; Tsuzuki, M; Waki, M, 2011
)
0.66
" This was likely the result of low-frequency dosing and short duration of steroid use."( Comparison of prednisolone acetate 1.0% and difluprednate ophthalmic emulsion 0.05% after cataract surgery: Incidence of postoperative steroid-induced ocular hypertension.
Ernest, P; McBain, M; Mian, SI; Musch, DC; Niziol, LM; Person, E; Tijunelis, MA, 2017
)
0.72
"Topical corticosteroids are widely used in the treatment of inflammation and pain after ocular surgery, but they possess several shortcomings, including frequent dosing and low patient adherence."( Nonclinical Development of ENV905 (Difluprednate) Ophthalmic Implant for the Treatment of Inflammation and Pain Associated with Ocular Surgery.
Culp, D; Garcia, A; Gilger, BC; Hamm, L; Navratil, T; Robeson, R; Struble, C; Verhoeven, RS; Yerxa, B,
)
0.41
" Fixed drug combinations not only cut the cost but also the dosage and improve the compliance of patients in the immediate post operative period."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.46
"Randomised-controlled trials (RCTs) comparing difluprednate and prednisolone acetate regardless of the dosing regimen used."( Difluprednate versus Prednisolone Acetate after Cataract Surgery: a Systematic Review and Meta-Analysis.
Basiony, A; KhalafAllah, MT; Salama, A, 2019
)
2.21
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
corticosteroid hormoneAny of a class of steroid hormones that are produced in the adrenal cortex.
butyrate esterAny carboxylic ester where the carboxylic acid component is butyric acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.44670.003245.467312,589.2998AID2517
Chain A, Beta-lactamaseEscherichia coli K-12Potency14.12540.044717.8581100.0000AID485341
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID485281
Chain A, CruzipainTrypanosoma cruziPotency25.11890.002014.677939.8107AID1476
GLS proteinHomo sapiens (human)Potency31.62280.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency26.78520.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency0.01690.000221.22318,912.5098AID743036; AID743040; AID743042; AID743053; AID743054
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency0.00400.00137.762544.6684AID914; AID915
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.00390.000214.376460.0339AID720691; AID720692; AID720719
estrogen nuclear receptor alphaHomo sapiens (human)Potency6.33970.000229.305416,493.5996AID743075; AID743080; AID743091
IDH1Homo sapiens (human)Potency0.18360.005210.865235.4813AID686970
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.00600.001723.839378.1014AID743083
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency2.51190.10009.191631.6228AID1346983
importin subunit beta-1 isoform 1Homo sapiens (human)Potency29.09295.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency29.09295.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency29.09295.804816.996225.9290AID540253
gemininHomo sapiens (human)Potency0.72080.004611.374133.4983AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency0.56230.891312.067628.1838AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency2.51190.015812.3113615.5000AID1461
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID91225Antiinflammatory activity measured by using McKenzie-Stoughton human vasoconstrictor assay; Potent1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Computer-aided studies of the structure-activity relationships between the structure of some steroids and their antiinflammatory activity.
AID90104Potency relative to fluocinolone 16,17-acetonide in the human vasoconstictor test1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Structure-activity relationships in the antiinflammatory steroids: a pattern-recognition approach.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1346849Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)2011Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics, Feb, Volume: 27, Issue:1
Pharmacokinetic features of difluprednate ophthalmic emulsion in rabbits as determined by glucocorticoid receptor-binding bioassay.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (93)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (8.60)18.7374
1990's1 (1.08)18.2507
2000's7 (7.53)29.6817
2010's52 (55.91)24.3611
2020's25 (26.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 68.67

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index68.67 (24.57)
Research Supply Index4.69 (2.92)
Research Growth Index5.86 (4.65)
Search Engine Demand Index113.51 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (68.67)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (6.93%)5.53%
Reviews4 (3.96%)6.00%
Case Studies25 (24.75%)4.05%
Observational0 (0.00%)0.25%
Other65 (64.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (21)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Study of the Efficacy of the Ophthalmic Emulsion PRO-145 for the Management of Inflammation and Pain After Phacoemulsification Compared to Prednisolone Acetate 1%. [NCT03693989]Phase 3178 participants (Actual)Interventional2018-10-04Completed
A Phase 3 Multicenter, Randomized, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Difluprednate in the Treatment of Inflammation Following Ocular Surgery [NCT00430092]Phase 3219 participants (Actual)InterventionalCompleted
Macular Edema Nepafenac vs. Difluprednate Uveitis Trial [NCT01939691]Phase 49 participants (Actual)Interventional2018-09-12Terminated(stopped due to Difficulty enrolling)
Steroids and Cross-linking for Ulcer Treatment [NCT04097730]Phase 3279 participants (Actual)Interventional2020-09-24Active, not recruiting
[NCT00616070]Phase 3120 participants (Anticipated)Interventional2007-12-31Completed
A Phase IIIB, Multicenter, Randomized, Double-Masked, Parallel-Group, Active-Controlled Study of the Safety and Efficacy of Difluprednate Ophthalmic Emulsion, 0.05% (Durezol™) 4 Times Daily (QID) and Prednisolone Acetate Ophthalmic Suspension, 1.0% (Pred [NCT01124045]Phase 380 participants (Actual)Interventional2010-08-31Completed
Efficacy and Safety of Difluprednate Ophthalmic Emulsion vs. a Fixed-Combination of Prednisolone Acetate - Phenylephrine Ophthalmic Suspension on Post-operative Inflammation Following Cataract Surgery. [NCT04631315]Phase 4255 participants (Actual)Interventional2019-03-24Completed
A Phase 3 Multicenter, Randomized, Double-Masked Study of the Safety and Efficacy of Difluprednate 0.05% Ophthalmic Emulsion Compared to Prednisolone Acetate 1% Ophthalmic Suspension in the Treatment of Endogenous Anterior Uveitis [NCT01201798]Phase 3111 participants (Actual)Interventional2010-10-31Completed
[NCT00616993]Phase 3120 participants (Anticipated)Interventional2008-01-31Completed
Phase 2a Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treatment of Postoperative Inflammation After Cataract Surgery [NCT00407225]Phase 224 participants Interventional1999-12-31Completed
A Multi-Center, Randomized, Double-Masked Evaluation of Anti-Inflammatory Treatment in Patients With Dry Eye [NCT01276223]Phase 2722 participants (Actual)Interventional2011-02-28Completed
[NCT00501579]Phase 30 participants InterventionalCompleted
A Randomized, Masked Multi-center Safety & Efficacy Study of the Effects of Preoperative & Postoperative Cataract Surgery Use of Difluprednate Ophthalmic Emulsion, 0.05% Compared to Prednisolone Acetate Ophthalmic Suspension 1% on Visual Acuity & Corneal [NCT01244334]Phase 452 participants (Actual)Interventional2009-03-31Completed
Phase 3 Confimatory Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treament of Postoperative Inflammation [NCT00406341]Phase 3200 participants Interventional2004-04-30Completed
Phase 2a Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treatment of Postoperative Inflammation [NCT00406497]Phase 224 participants Interventional2003-04-30Completed
Phase 3 Confirmatory Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treatment of Anterior Uveitis (Including Panuveitis). [NCT00406887]Phase 3140 participants Interventional2002-08-31Completed
Phase 2a Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treatment of Anterior Uveitis (Inluding Iritis, Cyclitis, Iridocyclitis, and Panuveitis). [NCT00405496]Phase 224 participants Interventional2000-03-31Completed
Phase 3 Open-Labeled Study of 0.05% Difluprednate Ophthalmic Emulsion in the Treatment of Severe Anterior Uveitis (Including Panuveitis). [NCT00407056]Phase 320 participants Interventional2002-08-31Completed
A Randomized, Clinical Investigation of the Dextenza 0.4mg Intracanalicular Insert Delivery System Used in Conjunction With Cataract Surgery Performed in Combination With Minimally Invasive Glaucoma Surgery [NCT04687800]Phase 41 participants (Actual)Interventional2020-12-01Terminated(stopped due to Inability to enroll due to lack of access to the Ambulatory Surgery Center.)
A Phase 3 Multicenter, Randomized, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Difluprednate in the Treatment of Inflammation Following Ocular Surgery [NCT00429923]Phase 3219 participants (Actual)InterventionalCompleted
A Study of the Effect of Different Doses of Difluprednate Eye Drops on the Intraocular Pressure After Phacoemulsification [NCT05649111]Phase 420 participants (Anticipated)Interventional2022-11-01Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00429923 (1) [back to overview]"Anterior Chamber Cell Grade of 0 on Day 8 (Difluprednate QID vs Placebo)."
NCT00430092 (1) [back to overview]"Anterior Chamber Cell Grade of 0 on Day 8 (Difluprednate QID vs Placebo)."
NCT01124045 (13) [back to overview]Percentage of Patients With an Anterior Cell Grade of 0 (no Cells) at Day 15 ± 2 Days
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Anterior Chamber Cell Grade
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Anterior Chamber Flare Grade
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Chemosis
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Ciliary/Limbal Injection
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Conjunctival Injection
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Corneal Clarity
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Hypopyon
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Lacrimation
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Photophobia
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Vitritis
NCT01124045 (13) [back to overview]Global Assessment of Inflammation - Individual Component Scoring by Visit: Wound Integrity
NCT01124045 (13) [back to overview]Global Assessment Score of Postoperative Inflammation by Visit
NCT01201798 (10) [back to overview]Proportion of Subjects Who Discontinued Due to Lack of Efficacy
NCT01201798 (10) [back to overview]Change From Baseline (Day 0) in Anterior Chamber Cell Grade at All Time Points Other Than Day 14
NCT01201798 (10) [back to overview]Change From Baseline (Day 0) in Anterior Chamber Cell Grade at Day 14
NCT01201798 (10) [back to overview]Change From Baseline (Day 0) in Anterior Chamber Flare Grade at All Time Points
NCT01201798 (10) [back to overview]Change From Baseline (Day 0) in Slit-Lamp Total Sign Score at All Visits
NCT01201798 (10) [back to overview]Change From Baseline (Day 0) in Visual Analog Scale (VAS) Total Symptom Score at All Time Points
NCT01201798 (10) [back to overview]Proportion of Subjects With Anterior Chamber Cell Count ≤5 and Flare Grade of 0
NCT01201798 (10) [back to overview]Proportion of Subjects With Anterior Chamber Cell Count of 0
NCT01201798 (10) [back to overview]Proportion of Subjects With Anterior Chamber Cell Grade ≤1
NCT01201798 (10) [back to overview]Proportion of Subjects With Anterior Chamber Cell Grade of 0
NCT01276223 (1) [back to overview]Mean Change From Baseline (Week 0) in Visual Analog Scale (VAS) Global Ocular Discomfort Score Over 4 Weeks
NCT03693989 (5) [back to overview]Adverse Events
NCT03693989 (5) [back to overview]Central Thickness of the Retina
NCT03693989 (5) [back to overview]Intraocular Pressure
NCT03693989 (5) [back to overview]Visual Ability (VA)
NCT03693989 (5) [back to overview]Symptomatology Post Instillation

"Anterior Chamber Cell Grade of 0 on Day 8 (Difluprednate QID vs Placebo)."

"Measured on a 0 to 4 scale: 0 is ≤ 1 cell; 1 is 2-10 cells; 2 is 11-20 cells; 3 is 21-50 cells; 4 is > 50 cells." (NCT00429923)
Timeframe: Day 8 (QID)

,,
Interventionparticipants (Number)
Proportion of subjects w/AC cell grade=0 on Day 8
Difluprednate 0.05% BID0
Difluprednate 0.05% QID19
Placebo13

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"Anterior Chamber Cell Grade of 0 on Day 8 (Difluprednate QID vs Placebo)."

"Measured on a 0 to 4 scale: 0 is ≤ 1 cell; 1 is 2-10 cells; 2 is 11-20 cells; 3 is 21-50 cells; 4 is > 50 cells." (NCT00430092)
Timeframe: Day 8 (QID)

,,
Interventionparticipants (Number)
Proportion of Subjects w/AC cell grade=0 on Day 8
Difluprednate 0.05% BID0
Difluprednate 0.05% QID18
Placebo7

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Percentage of Patients With an Anterior Cell Grade of 0 (no Cells) at Day 15 ± 2 Days

Anterior cell grade was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 5-point scale: Grade 0=0 cells; Grade 1=1 to 10 cells; Grade 2=11 to 20 cells; Grade 3=21 to 50 cells; Grade 4=>50 cells. The presence of blood cells (red and white) in the anterior chamber of the eye (the fluid-filled space inside the eye between the iris and the cornea's innermost surface) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. (NCT01124045)
Timeframe: Day 15 ± 2 days

InterventionPercentage of patients (Number)
DUREZOL78.9
PRED FORTE77.5

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Anterior Chamber Cell Grade

Anterior chamber cell grade was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 5-point scale: Grade 0=0 cells; Grade 1=1 to 10 cells; Grade 2=11 to 20 cells; Grade 3=21 to 50 cells; Grade 4=>50 cells. The presence of blood cells (red and white) in the anterior chamber of the eye (the fluid-filled space inside the eye between the iris and the cornea's innermost surface) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 1: Grade 4Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 8: Grade 4Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 15: Grade 4Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 3Day 29: Grade 41 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 31 Week After Last Dose: Grade 4Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3Month 3: Grade 4
DUREZOL23.757.915.82.60.055.336.85.32.60.078.918.40.02.60.089.510.50.00.00.097.42.60.00.00.094.75.30.00.00.0
PRED FORTE40.030.027.50.02.557.532.510.00.00.077.517.55.00.00.095.02.52.50.00.095.02.52.50.00.097.50.02.50.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Anterior Chamber Flare Grade

Anterior chamber flare was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. The presence of flare (increased protein levels) in the anterior chamber of the eye (the fluid-filled space inside the eye between the iris and the cornea's innermost surface) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL41.051.37.70.061.535.92.60.074.417.97.70.087.212.80.00.094.92.62.60.092.35.12.60.0
PRED FORTE45.037.512.55.052.540.05.02.570.027.52.50.092.57.50.00.092.57.50.00.095.05.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Chemosis

Chemosis was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Chemosis (swelling of the conjunctiva) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL82.115.40.02.697.42.60.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE85.015.00.00.0100.00.00.00.097.52.50.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Ciliary/Limbal Injection

Ciliary/limbal injection was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Ciliary/limbal injection (redness of the white sclera of the eye near the limbal ring) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL69.228.20.02.689.710.30.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE57.540.02.50.090.010.00.00.0100.00.00.00.097.52.50.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Conjunctival Injection

Conjunctival injection was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Conjunctival injection (redness of the white sclera of the eye) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL46.248.72.62.679.520.50.00.089.710.30.00.097.42.60.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE25.065.010.00.077.522.50.00.092.57.50.00.095.05.00.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Corneal Clarity

Corneal clarity was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Lack of corneal clarity (1-3) is a sign of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL92.37.70.00.094.95.10.00.094.95.10.00.097.42.60.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE87.512.50.00.090.07.52.50.090.010.00.00.097.52.50.00.097.52.50.00.097.52.50.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Hypopyon

Hypopyon was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Hypopyon (pus in the anterior chamber of the eye) is a sign of ocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Lacrimation

Lacrimation was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Excessive lacrimation (tear production and secretion, 1-3) is a symptom of ocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL64.130.85.10.094.95.10.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE72.522.55.00.097.52.50.00.095.05.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Photophobia

Photophobia was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Photophobia (abnormal intolerance to visual perception of light) is a symptom of intraocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL71.820.57.70.089.710.30.00.097.42.60.00.097.42.60.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE60.035.05.00.087.510.02.50.095.05.00.00.092.55.00.02.597.52.50.00.0100.00.00.00.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Vitritis

Vitritis was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Vitritis (accumulation of inflammatory cells or exudates in the vitreous humor, the fluid that fills the middle chamber of the eye) is a sign of ocular inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2Month 3: Grade 3
DUREZOL100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE97.52.50.00.097.50.02.50.097.50.02.50.097.50.02.50.097.50.02.50.097.50.02.50.0

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Global Assessment of Inflammation - Individual Component Scoring by Visit: Wound Integrity

Wound integrity was assessed by the Investigator during slit lamp or ophthalmoscopy/light examination and graded on a 4-point scale: 0=absent; 1=mild; 2=moderate; 3=severe. Lack of wound integrity (healing, 1-3) is a sign of inflammation. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 1: Grade 3Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 8: Grade 3Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 15: Grade 3Day 29: Grade 0Day 29: Grade 1Day 29: Grade 2Day 29: Grade 31 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 21 Week after Last Dose: Grade 3Month 1: Grade 0Month 1: Grade 1Month 1: Grade 2Month 1: Grade 3
DUREZOL100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0
PRED FORTE100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0100.00.00.00.0

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Global Assessment Score of Postoperative Inflammation by Visit

A Global Assessment Score (GAS) was assigned by the Investigator based on the clinical evidence of postoperative inflammation: 0=clear, 1=improving satisfactorily; 2=not improving or worsening, withdrawal from study indicated to allow appropriate alternative therapy to be instituted. A score of 0 indicates an absence of inflammation. For this outcome measure, percentage of patients by grade and visit is reported. (NCT01124045)
Timeframe: Day 1, Day 8 ± 1 day, Day 15 ± 2 days, Day 29 ± 2 days, 1 Week after Last Dose + 2 days, 3 Months + 1 week

,
InterventionPercentage of patients (Number)
Day 1: Grade 0Day 1: Grade 1Day 1: Grade 2Day 8: Grade 0Day 8: Grade 1Day 8: Grade 2Day 15: Grade 0Day 15: Grade 1Day 15: Grade 2Day 29: Grade 0Day 29: Grade 1Day 29: Grade 21 Week after Last Dose: Grade 01 Week after Last Dose: Grade 11 Week after Last Dose: Grade 2Month 3: Grade 0Month 3: Grade 1Month 3: Grade 2
DUREZOL30.869.20.048.748.72.656.443.60.079.520.50.089.77.72.692.35.12.6
PRED FORTE17.582.50.025.070.05.050.050.00.072.525.02.590.07.52.592.57.50.0

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Proportion of Subjects Who Discontinued Due to Lack of Efficacy

Lack of efficacy was defined as those subjects who discontinued study participation either due to treatment failure or an adverse event with a preferred term of iridocyclitis, iritis, uveitis, or vitritis. Proportion is reported as percentage of subjects. (NCT01201798)
Timeframe: Time to Event

InterventionPercentage of subjects (Number)
Durezol0
Pred Forte14.9

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Change From Baseline (Day 0) in Anterior Chamber Cell Grade at All Time Points Other Than Day 14

Inflammatory cells in the anterior chamber were assessed by the investigator during slit lamp examination and graded on a 5-point scale, with 0 = ≤ 1 cell count; 1 = 2 to 10 cell count; 2 = 11 to 20 cell count; 3 = 21 to 50 cell count; and 4 = > 50 cell count. (NCT01201798)
Timeframe: Baseline (Day 0), Day 3, Day 7, Day 21, Day 28, Day 35, Day 42

,
InterventionUnits on a scale (Mean)
Baseline (Day 0)Day 3Day 7Day 21Day 28Day 35Day 42
Durezol2.6-1.1-1.8-2.4-2.3-2.3-2.3
Pred Forte2.6-1.0-1.6-2.1-2.1-2.1-2.1

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Change From Baseline (Day 0) in Anterior Chamber Cell Grade at Day 14

Inflammatory cells in the anterior chamber were assessed by the investigator during slit lamp examination and graded on a 5-point scale, with 0 = ≤ 1 cell count; 1 = 2 to 10 cell count; 2 = 11 to 20 cell count; 3 = 21 to 50 cell count; and 4 = > 50 cell count. (NCT01201798)
Timeframe: Baseline (Day 0), Day 14

,
InterventionUnits on a scale (Mean)
Baseline (Day 0)Day 14
Durezol2.6-2.2
Pred Forte2.6-2.0

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Change From Baseline (Day 0) in Anterior Chamber Flare Grade at All Time Points

Anterior chamber flare (protein escaping from dialated vessels) was assessed by the investigator during slit lamp examination and graded on a 5-point scale, with 0 = none; 1 = mild (trace to clearly noticeable, visible); 2 = moderate; 3 = marked; and 4 = severe. (NCT01201798)
Timeframe: Baseline (Day 0), Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionUnits on a scale (Mean)
Baseline (Day 0)Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol2.2-1.1-1.6-2.0-2.0-2.0-2.0-2.0
Pred Forte2.3-1.2-1.6-1.9-2.0-2.0-2.0-2.0

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Change From Baseline (Day 0) in Slit-Lamp Total Sign Score at All Visits

The following signs were each graded on a 0 - 3 scale (0 = absent; 1 = mild; 2 = moderate; 3 = severe): posterior synechia, hypopyon, limbal injection, and keratic precipitates. Peripheral synechia was graded by the combined number of clock hours affected (0 = absent; 1 = < 3 hrs; 2 = 3-6 hours; 3 = > 6 hours). The total sign score was calculated as the sum of the 5 individual sign scores, the anterior chamber cell grade and the anterior chamber flare grade. The minimum/best total sign score was 0, and the maximum/worst total sign score was 23. (NCT01201798)
Timeframe: Baseline (Day 0), Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionUnits on a scale (Mean)
Baseline (Day 0)Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol7.1-3.5-5.2-6.1-6.5-6.4-6.3-6.2
Pred Forte7.3-3.6-5.0-5.8-6.2-6.2-6.2-6.3

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Change From Baseline (Day 0) in Visual Analog Scale (VAS) Total Symptom Score at All Time Points

The following symptoms were each graded by the subject according to a 0-100 visual analog scale (VAS) using a mark on a 100 mm line (0 = absent, 100 = maximal): eye pain, photophobia, blurred vision, and lacrimation. The total symptom score was calculated as the sum of the 4 individual symptom scores. (NCT01201798)
Timeframe: Baseline (Day 0), Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionUnits on a scale (Mean)
Baseline (Day 0)Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol186.7-88.4-108.2-133.3-138.8-140.1-143.9-146.2
Pred Forte203.2-88.4-123.8-137.4-149.5-152.4-147.3-155.5

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Proportion of Subjects With Anterior Chamber Cell Count ≤5 and Flare Grade of 0

Inflammatory cells in the anterior chamber were assessed by the investigator during slit lamp examination and recorded based on actual cell count. Anterior chamber flare (protein escaping from dialated vessels) was assessed by the investigator during slit lamp examination and graded on a 5-point scale, with 0 = none; 1 = mild (trace to clearly noticeable, visible); 2 = moderate; 3 = marked; and 4 = severe. Proportion is reported as percentage of subjects. (NCT01201798)
Timeframe: Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionPercentage of subjects (Number)
Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol13.041.378.382.680.482.680.4
Pred Forte14.940.461.776.676.676.678.7

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Proportion of Subjects With Anterior Chamber Cell Count of 0

Inflammatory cells in the anterior chamber were assessed by the investigator during slit lamp examination and recorded based on actual cell count. Proportion is reported as a percentage of subjects. (NCT01201798)
Timeframe: Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionPercentage of subjects (Number)
Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol13.021.752.273.973.969.669.6
Pred Forte2.121.338.348.963.863.868.1

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Proportion of Subjects With Anterior Chamber Cell Grade ≤1

As assessed by the investigator during slit lamp examination. Anterior chamber cell grade was graded on a 5-point scale, with 0 = no cells; 1 = 1 to 10 cells; 2 = 11 to 20 cells; 3 = 21 to 50 cells; and 4 = more than 50 cells. Proportion is reported as percentage of subjects. (NCT01201798)
Timeframe: Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionPercentage of subjects (Number)
Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol50.087.093.593.593.593.591.3
Pred Forte57.480.985.189.487.285.185.1

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Proportion of Subjects With Anterior Chamber Cell Grade of 0

Inflammatory cells in the anterior chamber were assessed by the investigator during slit lamp examination and graded on a 5-point scale, with 0 = ≤ 1 cell count; 1 = 2 to 10 cell count; 2 = 11 to 20 cell count; 3 = 21 to 50 cell count; and 4 = > 50 cell count. Proportion is reported as percentage of subjects. (NCT01201798)
Timeframe: Day 3, Day 7, Day 14, Day 21, Day 28, Day 35, Day 42

,
InterventionPercentage of subjects (Number)
Day 3Day 7Day 14Day 21Day 28Day 35Day 42
Durezol15.234.865.284.880.478.376.1
Pred Forte6.425.555.363.870.270.274.5

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Mean Change From Baseline (Week 0) in Visual Analog Scale (VAS) Global Ocular Discomfort Score Over 4 Weeks

A Visual Analog Scale (VAS) was used by the subject to assess ocular discomfort, both frequency and severity, at baseline (pre-treatment) and weekly thereafter for 4 additional weeks. Each scale was 100 millimeters (mm) in length. The VAS score was calculated by measuring the length in mm from the start of the line to the intersection point of the vertical mark made by the subject. The Global Ocular Discomfort Score is a composite of the two VAS scores, ranging from 0 (very mildly) to 100 (very severely uncomfortable). (NCT01276223)
Timeframe: Baseline, up to 4 weeks

,
Interventionunits on a scale (Mean)
Baseline (Week 0)Change from Baseline to Week 1Change from Baseline to Week 2Change from Baseline to Week 3Change from Baseline to Week 4
Durezol78.3-1.1-4.4-4.5-6.2
Vehicle76.8-1.7-4.2-4.8-4.7

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Adverse Events

"The evaluation of adverse events requires a questioning conducted by the principal investigator and the appropriate exploratory techniques for its detection.~the number of cases with adverse events will be reported per study arm" (NCT03693989)
Timeframe: day 28 at the final visit

Interventioncases (Number)
PRO-145.93
Prednefrin89

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Central Thickness of the Retina

By means of optical coherence tomography (OCT) the Retinal central thickness (GCR) will be measured. OCT is a noninvasive imaging test that uses light waves to take photographs of the cross section of the retina (the light-sensitive tissue that lines the back of the eye).With a OCT, each of the characteristic layers of the retina can be observed, allowing mapping and measuring its thickness a micrometer result will be obtained and the analysis will be carried out between groups. (NCT03693989)
Timeframe: day 28 at the final visit

Interventionmicrons (Mean)
PRO-145.253.59
Prednefrin263.38

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Intraocular Pressure

Tonometry is the objective measure of Intraocular pressure, based primarily on the force required to flatten the cornea, or the degree of corneal indentation produced by a fixed force. Goldman's tonometry is based on the Imbert-Fick principle. the result will be expressed in millimeters of mercury and the comparison between groups will be carried out (NCT03693989)
Timeframe: day 28 at the final visit

InterventionmmHg (Mean)
PRO-145.13.88
Prednefrin13.04

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Visual Ability (VA)

The VA will be evaluated basally, without refractive correction with the Snellen chart. Which will be located in a place with adequate lighting, natural or artificial and at a distance of 3 meters from the subject to be evaluated. The result of the Snellen fraction will be transformed to its decimal equivalent in LogMAR, ex. 20/20= 1.0, 20/25=0.8, 20/40= 0.5, 20/200= 1.0, etc. The subjects will be averaged by group. (NCT03693989)
Timeframe: day 28 at the final visit

Interventionunits on a scale (LogMAR) (Mean)
PRO-145.0.91
Prednefrin0.87

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Symptomatology Post Instillation

"The subject will be questioned if after applying the medication he felt burning, pruritus, a foreign body sensation and blurred vision.~Presence or absence: it will be marked as present (1) or absent (0) for each of the symptoms questioned" (NCT03693989)
Timeframe: day 28 at the final visit

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InterventionParticipants (Count of Participants)
burning eyesitching eyesforeign body sensation eyesblurred vision
Prednefrin8023
PRO-145.12102

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