Page last updated: 2024-11-05

hydrocortisone-17-butyrate

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

Description

Hydrocortisone-17-butyrate is a synthetic corticosteroid, specifically a derivative of hydrocortisone. It is created by attaching a butyrate ester group to the 17-position of the hydrocortisone molecule. This modification significantly enhances the compound's lipophilicity, increasing its ability to penetrate the skin. As a result, hydrocortisone-17-butyrate is primarily used as a topical anti-inflammatory agent for dermatological conditions like eczema, psoriasis, and dermatitis. It works by suppressing the immune response and reducing inflammation at the site of application. The butyrate ester group also contributes to the drug's prolonged action, allowing for fewer applications per day. The compound is extensively studied due to its effectiveness in treating various skin conditions, particularly those involving inflammation. Researchers continue to investigate its potential applications, including the development of new drug delivery systems and formulations to optimize its efficacy and minimize side effects.'

cortisol 17-butyrate : Cortisol esterified with butyric acid at the 17-hydroxy group. [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]

Cross-References

ID SourceID
PubMed CID26133
CHEMBL ID1683
CHEBI ID31674
SCHEMBL ID4695
MeSH IDM0051478

Synonyms (91)

Synonym
MLS002207122
AC-492
MLS001076086
MLS000028716 ,
smr000058859
11beta,17,21-trihydroxypregn-4-ene-3,20-dione 17-butyrate
cortisol 17-butyrate
einecs 237-093-4
hb(sub 17)
lacoid
pregn-4-ene-3,20-dione, 11,21-dihydroxy-17-(1-oxobutoxy)-, (11-beta)-
laticort
lacoidon
h.17b
alfason
hycortate
locoid lipocream
hydrocortisone-17-butyrate
hydrocortisone-17alpha-butyrate
cortisol, 17-butyrate
locoid
11-beta,17-alpha,21-trihydroxy-4-pregnene-3,20-dione 17-alpha-butyrate
pregn-4-ene-3,20-dione, 11,21-dihydroxy-17-(1-oxobutoxy)-, (11beta)-
bucort
hydrocortisone butyrate
h-17-b
11beta,21-dihydroxy-17alpha-butyryloxy-4-pregnene-3,20-dione
11beta,21-dihydroxy-3,20-dioxopregn-4-en-17-yl butanoate
CHEBI:31674 ,
17-o-butyrylcortisol
hydrocortisone 17-butyrate
locoid (tn)
D01619
hydrocortisone butyrate (jp17/usp)
nsc-758433
CHEMBL1683
butanoic acid [(8s,9s,10r,11s,13s,14s,17r)-11-hydroxy-17-(2-hydroxy-1-oxoethyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl] ester
[(8s,9s,10r,11s,13s,14s,17r)-10,13-dimethyl-11-oxidanyl-17-(2-oxidanylethanoyl)-3-oxidanylidene-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl] butanoate
A807026
nsc 758433
hydrocortisone butyrate [usan:usp:ban:jan]
unii-05rmf7ypwn
05rmf7ypwn ,
(1s,10s,11s,15s,17s,2r,14r)-17-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyl-5-ox otetracyclo[8.7.0.0<2,7>.0<11,15>]heptadec-6-en-14-yl butanoate
cas-13609-67-1
dtxcid2025896
dtxsid4045896 ,
tox21_111397
HMS2231B16
hydrocortisone butyrate [usp monograph]
hydrocortisone butyrate [usan]
11.beta.,17,21-trihydroxypregn-4-ene-3,20-dione 17-butyrate
hydrocortisone butyrate [usp-rs]
hydrocortisone butyrate [orange book]
hydrocortisone butyrate [vandf]
hydrocortisone butyrate [mart.]
hydrocortisone 17-butyrate [mi]
hydrocortisone butyrate [who-dd]
hydrocortisone butyrate [jan]
pregn-4-ene-3,20-dione, 11,21-dihydroxy-17-(1-oxobutoxy)-, (11.beta.)-
EPITOPE ID:119710
AKOS015895443
S6590
SCHEMBL4695
tox21_111397_1
NCGC00274077-01
CS-4474
H1506
W-108252
HY-B0983
OPERA_ID_188
hydrocortisone butyrate, united states pharmacopeia (usp) reference standard
hydrocortisone butyrate (hydrocortisone 17-butyrate)
mls001076086-01!11beta,17,21-trihydroxypregn-4-ene-3,20-dione 17-butyrate
Q5954743
(8s,9s,10r,11s,13s,14s,17r)-11-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl butanoate
DB14540
cortisol 17-butyrate;hydrocortisone butyrate
BCP11925
hydrocortisone-butyrate
bdbm323672
us10188667, example 00024
us10188667, example 00013
(1r,3as,3bs,9ar,9bs,10s,11as)-10-hydroxy-1-(2-hydroxyacetyl)-9a,11a-dimethyl-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl butanoate
EN300-7403907
hydrocortisone butyrate (usp-rs)
aquax-h
11beta,17,21-trihydroxypregn-4-ene-3,20-dione 17-butanoate
hydrocortisone butyrate (usan:usp:ban:jan)
hydrocortisone butyrate (usp monograph)
hydrocortisone butyrate (mart.)

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In the case of HBP, LD50 by oral administration was the highest, and followed by subcutaneous and intraperitoneal administration in mice and rats."( [Studies on toxicity of hydrocortisone 17-butyrate 21-propionate -1. Acute toxicity of hydrocortisone 17-butyrate 21-propionate and its analogues in mice, rats and dogs (author's transl)].
Abe, S; Nakane, S; Ohzeki, M; Sasajima, M; Tarumoto, Y; Tsutsui, Y, 1981
)
0.26
" These changes are considered to be common phenomena to other corticosteroids, and less toxic in female than male rats."( [Studies on toxicity of hydrocortisone 17-butyrate 21-propionate -2. Subacute toxicity in rats by subcutaneous administration (author's transl)].
Abe, S; Kasai, A; Kimura, M; Nakane, S; Noda, K; Ohzeki, M; Sasajima, M; Tarumoto, Y, 1981
)
0.26
" Rats receiving HBP showed the dose-dependent changes such as the suppression of body weight gain and food intake, emaciation, decrease in the number of white blood cells and lymphocytes, total protein, increase in the number of red cells, hematocrit, hemoglobin, blood sugar and total cholesterol, regressive changes in adrenal cortex, lymphatic and hematopoietic tissues and skin, and gastric erosion, which have been well known as toxic effects of synthetic corticosteroids."( [Studies of toxicity of hydrocortisone 17-butyrate 21-propionate -5. Chronic toxicity in rats by percutaneous administration (author's transl)].
Kimura, M; Nakane, S; Noda, K; Ohzeki, M; Sasajima, M; Shinozawa, R; Tarumoto, Y; Tokado, H; Tsuchida, T, 1981
)
0.26
"1% tacrolimus ointment was considered to be safe in the majority of patients."( Comparison of the efficacy and safety of 0.1% tacrolimus ointment with topical corticosteroids in adult patients with atopic dermatitis: review of randomised, double-blind clinical studies conducted in Japan.
Nakagawa, H, 2006
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
"We designed a parallel-group randomized controlled trial to compare the effectiveness of 308-nm excimer laser alone or in combination with topical hydrocortisone 17-butyrate cream in patients with vitiligo unresponsive to previous treatment with topical steroids or narrow-band ultraviolet (UV) B phototherapy."( Randomized controlled trial comparing the effectiveness of 308-nm excimer laser alone or in combination with topical hydrocortisone 17-butyrate cream in the treatment of vitiligo of the face and neck.
Cazzaniga, S; Chatenoud, L; Girolomoni, G; Marchesi, L; Naldi, L; Reseghetti, A; Sassi, F; Tessari, G, 2008
)
0.35
" In total, 84 patients (44 women and 40 men, mean age 44 years) were randomized to 308-nm excimer laser phototherapy twice weekly alone or in combination with topical hydrocortisone 17-butyrate cream twice daily for three periods of 3 weeks followed by a 1-week steroid-free interval."( Randomized controlled trial comparing the effectiveness of 308-nm excimer laser alone or in combination with topical hydrocortisone 17-butyrate cream in the treatment of vitiligo of the face and neck.
Cazzaniga, S; Chatenoud, L; Girolomoni, G; Marchesi, L; Naldi, L; Reseghetti, A; Sassi, F; Tessari, G, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
"This study was conducted to develop formulations of hydrocortisone butyrate (HB)-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles (PLGA NP) suspended in thermosensitive gel to improve ocular bioavailability of HB for the treatment of bacterial corneal keratitis."( Nanoparticle-Based Topical Ophthalmic Gel Formulation for Sustained Release of Hydrocortisone Butyrate.
Agrahari, V; Mitra, AK; Pal, D; Sheng, Y; Trinh, HM; Yang, X, 2016
)
0.43
"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

Dosage Studied

ExcerptRelevanceReference
" The regimen consisted of dosing patients with two applications of the two drugs every day for 4 weeks."( [Alclometasone dipropionate (Legederm) for the treatment of steroid-sensitive dermatoses in the elderly].
Criante, P; Giacchetti, A; Mambelli, V; Marchesi, E; Morresi, A; Mozzicafreddo, G; Simonacci, M; Sisti, S, 1990
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
dermatologic drugA drug used to treat or prevent skin disorders or for the routine care of skin.
drug allergenAny drug which causes the onset of an allergic reaction.
[role 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]

Drug Classes (3)

ClassDescription
cortisol ester
butyrate esterAny carboxylic ester where the carboxylic acid component is butyric acid.
primary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a -CH2 (methylene) group.
[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 (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
AR proteinHomo sapiens (human)Potency0.07890.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743036; AID743040; AID743042; AID743053; AID743054
progesterone receptorHomo sapiens (human)Potency0.87480.000417.946075.1148AID1346784; AID1347036
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.21720.000214.376460.0339AID720691; AID720692; AID720719
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency1.34220.001530.607315,848.9004AID1224841; AID1259401
pregnane X nuclear receptorHomo sapiens (human)Potency0.37580.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency5.13220.000229.305416,493.5996AID743069; AID743075; AID743079; AID743080; AID743091
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.18830.001723.839378.1014AID743083
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.01890.00419.984825.9290AID504444; AID720524
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency50.11870.425612.059128.1838AID504891
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency0.89130.004611.374133.4983AID624297
Interferon betaHomo sapiens (human)Potency0.02100.00339.158239.8107AID1347407
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.03760.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency0.03760.011912.222168.7989AID651632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (48)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID188016Anti-inflammatory effect in rat granuloma assay, activity relative to hydrocortisone and hydrocortisone 21-acetate1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Structure-activity relationships in the antiinflammatory steroids: a pattern-recognition approach.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID346025Binding affinity to beta cyclodextrin2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Convenient QSAR model for predicting the complexation of structurally diverse compounds with beta-cyclodextrins.
AID74385Relative binding affinity for glucocorticoid receptor of rat thymus cytosol by displacement of [3H]dexamethasone compared to cortisol1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Relative affinity of 17 alpha- and/or 21-esters and 17 alpha, 21-diesters of cortisol for a glucocorticoid receptor from rat thymocytes.
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.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (124)

TimeframeStudies, This Drug (%)All Drugs %
pre-199048 (38.71)18.7374
1990's25 (20.16)18.2507
2000's23 (18.55)29.6817
2010's20 (16.13)24.3611
2020's8 (6.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.43

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index27.43 (24.57)
Research Supply Index5.16 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index50.82 (26.88)
Search Engine Supply Index2.98 (0.95)

This Compound (27.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials42 (31.82%)5.53%
Reviews6 (4.55%)6.00%
Case Studies19 (14.39%)4.05%
Observational0 (0.00%)0.25%
Other65 (49.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A PHASE 3B/4, MULTICENTER, RANDOMIZED, ASSESSOR BLINDED, VEHICLE AND ACTIVE (TOPICAL CORTICOSTEROID AND CALCINEURIN INHIBITOR) CONTROLLED, PARALLEL GROUP STUDY OF THE EFFICACY, SAFETY, AND LOCAL TOLERABILITY OF CRISABOROLE OINTMENT, 2% IN PEDIATRIC AND AD [NCT03539601]Phase 4237 participants (Actual)Interventional2018-04-27Terminated(stopped due to This decision was made for business reasons only and is not related to any safety concerns regarding crisaborole.)
A Prospective, Randomised, Vehicle-Controlled, Double-Blind, Exploratory Clinical Trial To Assess The Efficacy And Steroid Sparing Potential Of DGLA Cream Topically Applied To Early Childhood Patients With Moderate To Severe Atopic Dermatitis [NCT03676933]Phase 25 participants (Actual)Interventional2015-10-31Completed
A Randomized Controlled Study on the Effectiveness of Local Injection Combined With Topical Steroids vs. Topical Steroids Mono-therapy in the Treatment of Idiopathic Granulomatous Mastitis [NCT03766997]Phase 4100 participants (Anticipated)Interventional2019-02-19Recruiting
A Double Blind, Multicentre, Randomised, Parallel Group Study to Demonstrate the Equivalence of the Response to Vaccination of a Tacrolimus Ointment Regimen to a Steroid Ointment Regimen in Children With Moderate to Severe Atopic Dermatitis [NCT00801957]Phase 2260 participants (Actual)Interventional2003-03-31Completed
Randomized, Placebo-Controlled Trial of Treatment of Atopic Dermatitis With Concurrent Altabax® and Topical Low-Potency Corticosteroids vs. Low-Potency Corticosteroid Mono-therapy [NCT00871208]Phase 40 participants (Actual)Interventional2009-05-31Withdrawn(stopped due to Funding withdrawn)
Adherence to Topical Hydrocortisone 17-butyrate 0.1% (Locoid®) Using Different Vehicles in Adults With Atopic Dermatitis [NCT00693693]Phase 426 participants (Actual)Interventional2006-11-30Completed
A Randomized, Evaluator Blinded, Within Subject, Single-Centre Evaluation of the Vasoconstriction Properties of MC2-01 Cream, Compared to 5 Other Corticosteroids in Healthy Subjects [NCT03758365]Phase 136 participants (Actual)Interventional2018-11-05Completed
Evaluation of Topical Steroids and Surgical Treatment for Idiopathic Granulomatous Mastitis [NCT02959580]Phase 4100 participants (Anticipated)Interventional2017-01-01Recruiting
Treatment of Tracheostomy Granulomas [NCT02116608]Phase 426 participants (Actual)Interventional2014-09-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00693693 (1) [back to overview]Adherence to Locoid
NCT02116608 (2) [back to overview]Categorical Improvement (Degree of Improvement)
NCT02116608 (2) [back to overview]Success and Failure Rates for Each Treatment Method
NCT03539601 (17) [back to overview]Number of Participants With Clinically Significant Abnormal Laboratory Parameters
NCT03539601 (17) [back to overview]Number of Participants With Clinically Significant Changes in Vital Signs
NCT03539601 (17) [back to overview]Number of Participants With Local Tolerability Adverse Events (AEs)
NCT03539601 (17) [back to overview]Percent Change From Baseline in the Eczema Area and Severity Index (EASI) Total Score at Day 29
NCT03539601 (17) [back to overview]Time to First Improvement From Baseline in Eczema Area and Severity Index (EASI) Total Score of Greater Than or Equal to (>=) 75%
NCT03539601 (17) [back to overview]Change From Baseline in Children's Dermatology Life Quality Index (CDLQI) in Participants Aged 4-15 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Change From Baseline in Dermatitis Family Impact Questionnaire (DFI) in Participants Aged 2-17 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Change From Baseline in Dermatology Life Quality Index (DLQI) in Participants Greater Than or Equal to (>=) 16 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Change From Baseline in Peak Pruritus Numerical Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Change From Baseline in Percent Body Surface Area (%BSA) at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants Who Achieved >=2 Point Improvement From Baseline in Peak Pruritus Numeric Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants Who Achieved >=3 Point Improvement From Baseline in Peak Pruritus Numeric Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants Who Achieved Greater Than or Equal to (>=) 75 Percent (%) Improvement From Baseline in Eczema Area and Severity Index (EASI) Total Score at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants Who Achieved Investigator's Static Global Assessment (ISGA) Score of Clear (0) or Almost Clear (1) at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants Who Achieved Success in the Investigator's Static Global Assessment (ISGA) (ISGA Score of Clear [0] or Almost Clear [1] With At-least a 2-Grade Improvement From Baseline) at Day 8, 15, 22 and 29
NCT03539601 (17) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs) and Treatment Discontinuations Due to AEs and SAEs
NCT03539601 (17) [back to overview]Percent Change From Baseline in Eczema Area and Severity Index (EASI) Total Score at Day 8, 15 and 22
NCT03758365 (2) [back to overview]Comparison of the Vasoconstriction Potential (Skin Blanching Effect) of the MC2-01 Cream With Active Comparators and Vehicle
NCT03758365 (2) [back to overview]Compare Local Tolerability of the MC2-01 Cream With Active Comparators and Vehicle

Adherence to Locoid

Adherence measured by MEMS cap as the % of days that the two total prescribed doses were applied (NCT00693693)
Timeframe: 2 weeks

Interventionpercentage of days (Mean)
Cream.55
Ointment.60
Lipocream.50

[back to top]

Categorical Improvement (Degree of Improvement)

"Categorical success/failure data. the size of the granuloma will be measured and recorded. The percent circumference will also be measured. The approximate percent decrease in the granuloma size will be determined to determine the category subject's change in granuloma:~i. Complete resolution: >90% improvement (Score = 4) ii. Improvement: 50 - 90% improvement (Score = 3) iii. Minimal improvement: < 50% improvement (Score = 2) iv. No improvement (Score = 1) v. Worsening (Score = 0)" (NCT02116608)
Timeframe: Over 6 Weeks

,,
InterventionParticipants (Count of Participants)
WorseningNo improvementMinimal improvement: < 50% improvementImprovement: 50-90% improvementComplete resolution: >90% improvement
Group 1: Betadine01224
Group 2: Hydrocortisone Butyrate Cream, 1.0%21103
Group 3: Silver Nitrate20005

[back to top]

Success and Failure Rates for Each Treatment Method

"Definition of success: The investigators are defining successful treatment of tracheostomy granulomas as a decrease in the frequency of granulomas over a six week observation period using the assigned treatment or partial or complete resolution of the granuloma. Partial resolution is defined as 25-75% resolution and complete resolution is defined as greater than 75% resolution.~Definition of failure: The investigators are defining a treatment as a failure if during the six week observation period of using the assigned treatment, there is either no improvement in the resolution or there has been an increase in size or frequency of tracheostomy granulomas." (NCT02116608)
Timeframe: Over 6 weeks

,,
InterventionParticipants (Count of Participants)
SuccessFailure
Group 1: Betadine63
Group 2: Hydrocortisone Butyrate Cream, 1.0%34
Group 3: Silver Nitrate52

[back to top]

Number of Participants With Clinically Significant Abnormal Laboratory Parameters

Hematology parameters included with criteria greater than (>) 1.2*upper limit of normal (ULN): leukocytes (10^3 per cubic millimeter [10^3/mm^3]), lymphocytes (10^3/mm^3), lymphocytes/leukocytes (%), neutrophils (10^3/mm^3), neutrophils/leukocytes (%), basophils/leukocytes (%), eosinophils (10^3/mm^3), eosinophils/leukocytes (%), monocytes (10^3/mm^3), monocytes/leukocytes (%). Clinical chemistry included parameters: aspartate aminotransferase (units per liter [U/L]) (>3.0* ULN), alanine aminotransferase (U/L) (>3.0* ULN), alkaline phosphatase (U/L) (>3.0* ULN), creatinine (milligram per deciliter [mg/dL]) (>1.3* ULN), potassium (milliequivalent per liter [mEq/L]) (>1.1* ULN), bicarbonate (mEq/L) (>1.1* ULN). (NCT03539601)
Timeframe: Screening up to Day 29

InterventionParticipants (Count of Participants)
Vehicle0
Crisaborole Ointment 2% BID0
Hydrocortisone Butyrate Cream 0.1% BID1
Pimecrolimus Cream 1% BID0

[back to top]

Number of Participants With Clinically Significant Changes in Vital Signs

Vital sign measurements included temperature, respiratory rate, pulse rate, and blood pressure. Temperature, respiratory rate, pulse rate, and blood pressure were taken in the seated or supine position, after the participant has been sitting or lying calmly for a minimum of 5 minutes (when possible for younger children). Position of recording was consistent within participant through-out the study. (NCT03539601)
Timeframe: Screening up to Day 29

InterventionParticipants (Count of Participants)
Vehicle0
Crisaborole Ointment 2% BID0
Hydrocortisone Butyrate Cream 0.1% BID1
Pimecrolimus Cream 1% BID0

[back to top]

Number of Participants With Local Tolerability Adverse Events (AEs)

Local tolerability AEs included application and instillation site reactions, application site discharge, application site erythema, application site exfoliation, application site pain, application site pruritus, application site swelling, dermatitis and eczema, dermatitis atopic, dermatitis contact, eczema, skin irritation, telangiectasia and related conditions, and urticarias. (NCT03539601)
Timeframe: From Baseline up to 28 days after last dose of study treatment (maximum up to 60 Days)

InterventionParticipants (Count of Participants)
Vehicle12
Crisaborole Ointment 2% BID13
Hydrocortisone Butyrate Cream 0.1% BID2
Pimecrolimus Cream 1% BID8

[back to top]

Percent Change From Baseline in the Eczema Area and Severity Index (EASI) Total Score at Day 29

EASI quantifies severity of participant's AD (excluded scalp) based on lesion severity and percent (%) body surface area (%BSA) affected. Lesion severity included erythema (E), induration/papulation (I), excoriation (Ex), lichenification (L) scored for 4 regions (head and neck [h], upper limbs [u], trunk [t] [including axillae, groin], lower limbs [l] [including buttocks]) on 4-point scale: 0= absent; 1= mild; 2= moderate; 3= severe. EASI area score (A) based upon %BSA with AD in body region: 0 (0%), 1 (>0 to <10%), 2 (10 to <30%), 3 (30 to <50%), 4 (50 to <70%), 5 (70 to <90%), 6 (90 to 100%). Total EASI score (aged >=8 years) =0.1*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et + It +Ext + Lt) + 0.4*Al*(El + Il + Exl + Ll); for aged 2 to <8 years =0.2*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et +It + Ext + Lt) + 0.3*Al*(El + Il + Exl + Ll). Total score ranges from 0.0 to 72.0, higher scores indicated greater AD severity. (NCT03539601)
Timeframe: Baseline, Day 29

InterventionPercent change (Mean)
Vehicle: Participants 2-17 Years-26.62
Crisaborole Ointment 2% BID: Participants 2-17 Years-49.47
Hydrocortisone Butyrate Cream 0.1% BID: Participants 2-17 Years-75.50
Pimecrolimus Cream 1% BID: Participants 2-17 Years-60.08
Vehicle: Participants >=18 Years-44.67
Crisaborole Ointment 2% BID: Participants >=18 Years-57.14
Hydrocortisone Butyrate Cream 0.1% BID: Participants >=18 Years-70.29
Pimecrolimus Cream 1% BID: Participants >=18 Years-62.59

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Time to First Improvement From Baseline in Eczema Area and Severity Index (EASI) Total Score of Greater Than or Equal to (>=) 75%

EASI quantifies severity of participant's AD (excluded scalp) based on lesion severity and %BSA affected. Lesion severity included erythema (E), induration/papulation (I), excoriation (Ex), lichenification (L) scored for 4 regions (head and neck [h], upper limbs [u], trunk [t] [including axillae, groin], lower limbs [l] [including buttocks]) on 4-point scale: 0= absent; 1= mild; 2= moderate; 3= severe. EASI area score(A) based upon %BSA with AD in body region: 0 (0%), 1 (>0 to <10%), 2 (10 to <30%), 3 (30 to <50%), 4 (50 to <70%), 5 (70 to <90%), 6 (90 to 100%). Total EASI score (aged >=8 years) =0.1*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et + It +Ext + Lt) + 0.4*Al*(El + Il + Exl + Ll); for aged 2 to <8 years =0.2*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et +It + Ext + Lt) + 0.3*Al*(El + Il + Exl + Ll). Total score ranges from 0.0 to 72.0, higher scores indicated greater AD severity. (NCT03539601)
Timeframe: Baseline up to Day 43

InterventionDays (Median)
VehicleNA
Crisaborole Ointment 2% BID43.0
Hydrocortisone Butyrate Cream 0.1% BID23.0
Pimecrolimus Cream 1% BID32.0

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Change From Baseline in Children's Dermatology Life Quality Index (CDLQI) in Participants Aged 4-15 Years at Day 8, 15, 22 and 29

The CDLQI was a 10-item questionnaire that measures the impact of skin disease on children's (aged 4 to 15 years) quality of life. Each question was evaluated on a 4-point scale ranging from 0 (not at all) to 3 (very much); where higher scores indicate more impact on quality of life. The CDLQI total score was the sum of individual scores of question 1-10 and ranged from 0 (not at all) to 30 (very much): 0-1 = no effect on the child's life; 2-6 = small effect; 7-12 = moderate effect; 13-18 = very large effect; 19-30 = extremely large effect. Higher scores indicated more impact on quality of life of children. (NCT03539601)
Timeframe: Baseline, Day 8, 15, 22 and 29

,,,
InterventionUnits on a scale (Mean)
Change at Day 8Change at Day 15Change at Day 22Change at Day 29
Crisaborole Ointment 2% BID-2.1-3.1-2.6-3.4
Hydrocortisone Butyrate Cream 0.1% BID-5.4-5.5-4.9-6.4
Pimecrolimus Cream 1% BID-1.7-1.6-2.5-3.4
Vehicle-0.2-2.0-2.7-3.1

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Change From Baseline in Dermatitis Family Impact Questionnaire (DFI) in Participants Aged 2-17 Years at Day 8, 15, 22 and 29

The DFI was a 10-item disease questionnaire that measures the impact of having a child (aged 2-17 years) with AD on family quality of life. It was completed by parent/legal guardian of the child (affected by AD), based on recall over the past week. Each question was scored on a 4-point scale ranging from 0 (not at all) to 30 (very much): where higher scores indicated worst quality of life of family. The DFI total score was the sum of individual scores of the 10 questions and ranged from 0 (no impact on life of family) to 30 (maximum effect on life of family), where higher DFI scores indicated maximum effect on life of family. (NCT03539601)
Timeframe: Baseline, Day 8, 15, 22 and 29

,,,
InterventionUnits on a scale (Mean)
Change at Day 8Change at Day 15Change at Day 22Change at Day 29
Crisaborole Ointment 2% BID-2.3-2.3-3.1-3.6
Hydrocortisone Butyrate Cream 0.1% BID-5.6-5.5-5.3-6.4
Pimecrolimus Cream 1% BID-2.8-3.2-4.5-4.8
Vehicle-1.2-1.1-2.5-1.8

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Change From Baseline in Dermatology Life Quality Index (DLQI) in Participants Greater Than or Equal to (>=) 16 Years at Day 8, 15, 22 and 29

DLQI is a 10-item questionnaire that measures the impact of skin disease on participants aged >=16 years. Each question was evaluated on a 4-point scale ranging from 0 (not at all) to 3 (very much); where higher scores indicated more impact on quality of life. Scores from all 10 questions were added up to give DLQI total score range from 0 (not at all) to 30 (very much). Higher scores indicated more impact on quality of life of participant. (NCT03539601)
Timeframe: Baseline, Day 8, 15, 22 and 29

,,,
InterventionUnits on a scale (Mean)
Change at Day 8Change at Day 15Change at Day 22Change at Day 29
Crisaborole Ointment 2% BID-3.8-3.5-3.4-3.9
Hydrocortisone Butyrate Cream 0.1% BID-5.1-6.8-6.9-7.0
Pimecrolimus Cream 1% BID-1.4-2.9-3.4-4.1
Vehicle-1.9-3.4-2.8-4.9

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Change From Baseline in Peak Pruritus Numerical Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29

"The severity of itch (pruritus) due to AD was assessed using the peak pruritus NRS for participants aged >=12 years. Participants at specified time points were asked the following question: how would you rate your itch at the worst moment during the previous 24 hours? The scale ranged from 0 to 10, where 0= no itch and 10= worst itch imaginable. Higher scores indicated worse itch." (NCT03539601)
Timeframe: Baseline, Day 8, 15, 22 and 29

,,,
InterventionUnits on a scale (Mean)
Change at Day 8Change at Day 15Change at Day 22Change at Day 29
Crisaborole Ointment 2% BID-1.01-1.08-1.28-1.65
Hydrocortisone Butyrate Cream 0.1% BID-2.24-3.21-3.83-4.02
Pimecrolimus Cream 1% BID-0.29-1.35-1.66-1.67
Vehicle-0.67-0.97-0.98-1.30

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Change From Baseline in Percent Body Surface Area (%BSA) at Day 8, 15, 22 and 29

Four body regions were evaluated: head and neck, upper limbs, trunk (including axillae) and lower limbs (including buttocks) excluding scalp. BSA was calculated using handprint method. Number of handprints (size of participant's full palmer hand in a closed position) fitting in affected area of a body region was estimated. Maximum number of handprints were: 10 for head, neck (20 for <8 years age), 20 for upper limbs, 30 for trunk, 40 for lower limbs (30 for <8 years age). Surface area (SA) of body region equivalent to 1 handprint: 10% for head, neck (5% for <8 years age), 5% for upper limbs, 3.33% for trunk, 2.5% for lower limbs (3.33% for <8 years age). Overall %BSA for a body region = total number of handprints in a body region * % SA equivalent to 1 handprint. % BSA for an individual: mean of % BSA of all 4 body regions, range =0-100%, higher values = greater AD severity. (NCT03539601)
Timeframe: Baseline, Day 8, 15, 22 and 29

,,,,,,,
InterventionPercent BSA (Mean)
Change at Day 8Change at Day 15Change at Day 22Change at Day 29
Crisaborole Ointment 2% BID: Participants >=18 Years-4.09-4.63-5.98-7.18
Crisaborole Ointment 2% BID: Participants 2-17 Years-2.63-4.32-7.14-9.95
Hydrocortisone Butyrate Cream 0.1% BID: Participants >=18 Years-2.74-5.00-4.91-7.18
Hydrocortisone Butyrate Cream 0.1% BID: Participants 2-17 Years-5.25-7.40-8.54-9.63
Pimecrolimus Cream 1% BID: Participants >=18 Years-1.44-3.56-4.17-6.86
Pimecrolimus Cream 1% BID: Participants 2-17 Years-2.84-3.72-6.52-7.30
Vehicle: Participants >=18 Years-1.39-3.73-4.19-6.76
Vehicle: Participants 2-17 Years-2.04-2.38-2.23-3.38

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Number of Participants Who Achieved >=2 Point Improvement From Baseline in Peak Pruritus Numeric Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29

"The severity of itch (pruritus) due to AD was assessed using the peak pruritus NRS for participants aged >=12 years. Participants at specified time points were asked the following question: how would you rate your itch at the worst moment during the previous 24 hours? The scale ranged from 0 to 10, where 0= no itch and 10= worst itch imaginable. Higher scores indicated worse itch." (NCT03539601)
Timeframe: Day 8, 15, 22 and 29

,,,
InterventionParticipants (Count of Participants)
Day 8Day 15Day 22Day 29
Crisaborole Ointment 2% BID7879
Hydrocortisone Butyrate Cream 0.1% BID21313232
Pimecrolimus Cream 1% BID1799
Vehicle39910

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Number of Participants Who Achieved >=3 Point Improvement From Baseline in Peak Pruritus Numeric Rating Scale (NRS) in Participants Aged Greater Than or Equal to (>=) 12 Years at Day 8, 15, 22 and 29

"The severity of itch (pruritus) due to AD was assessed using the Peak Pruritus NRS for participants aged >=12 years. Participants at specified time points were asked the following question: how would you rate your itch at the worst moment during the previous 24 hours? The scale ranged from 0 to 10, where 0= no itch and 10= worst itch imaginable. Higher scores indicated worse itch." (NCT03539601)
Timeframe: Day 8, 15, 22 and 29

,,,
InterventionParticipants (Count of Participants)
Day 8Day 15Day 22Day 29
Crisaborole Ointment 2% BID1546
Hydrocortisone Butyrate Cream 0.1% BID11212524
Pimecrolimus Cream 1% BID0346
Vehicle2546

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Number of Participants Who Achieved Greater Than or Equal to (>=) 75 Percent (%) Improvement From Baseline in Eczema Area and Severity Index (EASI) Total Score at Day 8, 15, 22 and 29

EASI quantifies severity of participant's AD (excluded scalp) based on lesion severity and %BSA affected. Lesion severity included erythema (E), induration/papulation (I), excoriation (Ex), lichenification (L) scored for 4 regions (head and neck [h], upper limbs [u], trunk [t] [including axillae, groin], lower limbs [l] [including buttocks]) on 4-point scale: 0= absent; 1= mild; 2= moderate; 3= severe. EASI area score(A) based upon %BSA with AD in body region: 0 (0%), 1 (>0 to <10%), 2 (10 to <30%), 3 (30 to <50%), 4 (50 to <70%), 5 (70 to <90%), 6 (90 to 100%). Total EASI score (aged >=8 years) =0.1*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et + It +Ext + Lt) + 0.4*Al*(El + Il + Exl + Ll); for aged 2 to <8 years =0.2*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et +It + Ext + Lt) + 0.3*Al*(El + Il + Exl + Ll). Total score ranges from 0.0 to 72.0, higher scores indicated greater AD severity. (NCT03539601)
Timeframe: Day 8, 15, 22 and 29

,,,
InterventionParticipants (Count of Participants)
Day 8Day 15Day 22Day 29
Crisaborole Ointment 2% BID7101317
Hydrocortisone Butyrate Cream 0.1% BID9252940
Pimecrolimus Cream 1% BID281117
Vehicle2489

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Number of Participants Who Achieved Investigator's Static Global Assessment (ISGA) Score of Clear (0) or Almost Clear (1) at Day 8, 15, 22 and 29

ISGA is a five point global assessment scale of AD severity, used to characterize participants' overall disease severity across all treatable AD lesions (excluding the scalp). ISGA score ranged from 0 to 4: where 0 = clear (minor residual hypo/hyperpigmentation; no erythema or induration/papulation; no oozing/crusting), 1= almost clear (trace faint pink erythema, with barely perceptible induration/papulation and no oozing/crusting), 2= mild (faint pink erythema with mild induration/papulation and no oozing/crusting), 3= moderate (pink-red erythema with moderate induration/papulation with or without oozing/crusting), 4= severe (deep or bright red erythema with severe induration/papulation and with oozing/crusting). Higher scores indicated greater severity of AD. (NCT03539601)
Timeframe: Day 8, 15, 22 and 29

,,,,,,,
InterventionParticipants (Count of Participants)
Day 8Day 15Day 22Day 29
Crisaborole Ointment 2% BID: Participants >=18 Years4389
Crisaborole Ointment 2% BID: Participants 2-17 Years37810
Hydrocortisone Butyrate Cream 0.1% BID: Participants >=18 Years4111320
Hydrocortisone Butyrate Cream 0.1% BID: Participants 2-17 Years12191927
Pimecrolimus Cream 1% BID: Participants >=18 Years2557
Pimecrolimus Cream 1% BID: Participants 2-17 Years59913
Vehicle: Participants >=18 Years0114
Vehicle: Participants 2-17 Years6666

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Number of Participants Who Achieved Success in the Investigator's Static Global Assessment (ISGA) (ISGA Score of Clear [0] or Almost Clear [1] With At-least a 2-Grade Improvement From Baseline) at Day 8, 15, 22 and 29

ISGA is a five point global assessment scale of AD severity, used to characterize participants' overall disease severity across all treatable AD lesions (excluding the scalp). ISGA score ranged from 0 to 4: where 0= clear (minor residual hypo/hyperpigmentation; no erythema or induration/papulation; no oozing/crusting), 1= almost clear (trace faint pink erythema, with barely perceptible induration/papulation and no oozing/crusting), 2= mild (faint pink erythema with mild induration/papulation and no oozing/crusting), 3= moderate (pink-red erythema with moderate induration/papulation with or without oozing/crusting), 4= severe (deep or bright red erythema with severe induration/papulation and with oozing/crusting). Higher scores indicated greater severity of AD. (NCT03539601)
Timeframe: Day 8, 15, 22 and 29

,,,,,,,
InterventionParticipants (Count of Participants)
Day 8Day 15Day 22Day 29
Crisaborole Ointment 2% BID: Participants >=18 Years0036
Crisaborole Ointment 2% BID: Participants 2-17 Years0325
Hydrocortisone Butyrate Cream 0.1% BID: Participants >=18 Years06913
Hydrocortisone Butyrate Cream 0.1% BID: Participants 2-17 Years281120
Pimecrolimus Cream 1% BID: Participants >=18 Years0112
Pimecrolimus Cream 1% BID: Participants 2-17 Years0257
Vehicle: Participants >=18 Years0013
Vehicle: Participants 2-17 Years2122

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Number of Participants With Treatment Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs) and Treatment Discontinuations Due to AEs and SAEs

An AE is any untoward medical occurrence in a study participant administered a product or medical device; the event need not necessarily have a causal relationship with the treatment or usage. TEAEs are events between the first dose of study drug up to 28 days after last dose that were absent before treatment or that worsened relative to pretreatment state. A SAE is any untoward medical occurrence at any dose that: results in death; is life-threatening (immediate risk of death); requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity (substantial disruption of the ability to conduct normal life functions); results in congenital anomaly/birth defect; or that is considered to be an important medical event. (NCT03539601)
Timeframe: From Baseline up to 28 days after last dose of study treatment (maximum up to 60 Days)

,,,
InterventionParticipants (Count of Participants)
TEAEsSAEsDiscontinuation due to AEsDiscontinuation due to SAEs
Crisaborole Ointment 2% BID25030
Hydrocortisone Butyrate Cream 0.1% BID12000
Pimecrolimus Cream 1% BID24000
Vehicle18000

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Percent Change From Baseline in Eczema Area and Severity Index (EASI) Total Score at Day 8, 15 and 22

EASI quantifies severity of participant's AD (excluded scalp) based on lesion severity and %BSA affected. Lesion severity included erythema (E), induration/papulation (I), excoriation (Ex), lichenification (L) scored for 4 regions (head and neck [h], upper limbs [u], trunk [t] [including axillae, groin], lower limbs [l] [including buttocks]) on 4-point scale: 0= absent; 1= mild; 2= moderate; 3= severe. EASI area score(A) based upon %BSA with AD in body region: 0 (0%), 1 (>0 to <10%), 2 (10 to <30%), 3 (30 to <50%), 4 (50 to <70%), 5 (70 to <90%), 6 (90 to 100%). Total EASI score (aged >=8 years) =0.1*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et + It +Ext + Lt) + 0.4*Al*(El + Il + Exl + Ll); for aged 2 to <8 years =0.2*Ah*(Eh + Ih + Exh + Lh) + 0.2*Au*(Eu + Iu + Exu + Lu) + 0.3*At*(Et +It + Ext + Lt) + 0.3*Al*(El + Il + Exl + Ll). Total score ranges from 0.0 to 72.0, higher scores indicated greater AD severity. (NCT03539601)
Timeframe: Baseline, Day 8, 15 and 22

,,,,,,,
InterventionPercent change (Mean)
Percent Change at Day 8Percent Change at Day 15Percent Change at Day 22
Crisaborole Ointment 2% BID: Participants >=18 Years-29.83-48.42-56.05
Crisaborole Ointment 2% BID: Participants 2-17 Years-26.79-36.72-38.87
Hydrocortisone Butyrate Cream 0.1% BID: Participants >=18 Years-42.48-56.29-61.82
Hydrocortisone Butyrate Cream 0.1% BID: Participants 2-17 Years-45.59-58.96-69.09
Pimecrolimus Cream 1% BID: Participants >=18 Years-18.75-37.18-42.25
Pimecrolimus Cream 1% BID: Participants 2-17 Years-34.20-42.75-59.86
Vehicle: Participants >=18 Years-14.77-25.93-34.43
Vehicle: Participants 2-17 Years-17.88-25.77-25.07

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Comparison of the Vasoconstriction Potential (Skin Blanching Effect) of the MC2-01 Cream With Active Comparators and Vehicle

Blanching of the skin will be assessed individually by two trained observers blinded to treatment. The observers will score the blanching of the skin from 0-4 (0 = No change in color skin; 1 = Slight (barely visible) blanching; 3 = Obvious blanching; 4 = Blanching judged to be maximal). The results is presented as Mean ± SD. (NCT03758365)
Timeframe: Day 2

Interventionscore on a scale (Mean)
MC2-01 CreamClobetasol Propionate 0.05% LotionBetamethasone Dipropionate 0.05% CreamTriamcinolone Acetonide 0.1% CreamHydrocortisone Butyrate 0.1% CreamDesonide 0.05% CreamVehicle Cream
MC2-01 Cream + Comparators1.663.052.451.922.062.110.14

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Compare Local Tolerability of the MC2-01 Cream With Active Comparators and Vehicle

The local tolerability of the creams will be assesed using a predefined scale: 0 = No reaction; 0.5 = Only slight erythema; 1 = Only erythema; 2 = Erythema with papules or oedema; 3 = Erythema, oedema with papules, oedema with vesicle; 4 = Blisters (NCT03758365)
Timeframe: Day 2

InterventionParticipants (Count of Participants)
MC2-01 Cream72211385Clobetasol Propionate 0.05% Lotion72211385Betamethasone Dipropionate 0.05% Cream72211385Triamcinolone Acetonide 0.1% Cream72211385Hydrocortisone Butyrate 0.1% Cream72211385Desonide 0.05% Cream72211385Vehicle Cream72211385
Erythema with papules or oedemaNo reactionOnly Slight reactionOnly erythemaErythema, oedema with papules, oedema with vesicleBlisters
MC2-01 Cream + Comparators0
MC2-01 Cream + Comparators36

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