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dapsone

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Dapsone, also known as diaminodiphenylsulfone, is a synthetic antibacterial drug used primarily for the treatment of leprosy and dermatitis herpetiformis. It is a sulfone derivative that inhibits bacterial growth by interfering with the synthesis of dihydrofolic acid, an essential precursor for bacterial DNA synthesis. Dapsone was first synthesized in 1908 and its therapeutic effects in leprosy were discovered in the 1940s. Dapsone is typically administered orally, and its effectiveness in treating leprosy has made it a vital tool in controlling the disease globally. However, dapsone can cause various side effects, including hemolytic anemia, methemoglobinemia, and liver damage. Research on dapsone is ongoing, with ongoing efforts to explore its potential in treating other conditions like inflammatory bowel disease, rheumatoid arthritis, and certain types of cancer. Additionally, researchers are investigating ways to improve the drug's efficacy and minimize its side effects. '

Cross-References

ID SourceID
PubMed CID2955
CHEMBL ID1043
CHEBI ID4325
SCHEMBL ID21428
MeSH IDM0005661

Synonyms (317)

Synonym
BIDD:GT0770
j04ba02
CHEMBL1043 ,
servidapson
nsc-6091d
MLS001076146
bdbm50029764
4,4''-sulfonylbisbenzenamine
4,4''-diaminodiphenyl sulfone
p,p''-diaminodiphenyl sulfone
1,1''-sulfonylbis(4-aminobenzene)
4,4''-dapsone
4,4''-sulfonyldianiline
4,4''-sulfonylbisaniline
BRD-K62363391-001-05-8
(4-sulfanilylphenyl)amine
DDS ,
p,p'-sulfonyldianiline
dapson
nsc6091
nsc 6091d
croysulfone
metabolite c
diaminodiphenylsulfone
avlosulfon
sulfona
4,4'-sulfonyldianiline
n,n'-diphenyl sulfondiamide
diphenasone
wln: zr dswr dz
diaphenylsulfon
dumitone
sulfona-mae
4,4'-sulfonylbisbenzamine
nci-c01718
bis(p-aminophenyl) sulfone
avlosulfone
1,1'-sulfonylbis[4-aminobenzene]
di(4-aminophenyl) sulfone
4,4'-diaminodiphenyl sulfone
novophone
dadps
eporal
dds, pharmaceutical
sulfadione
p-aminophenyl sulfone
nsc-6091
f 1358
1358f
diphone
p,p'-diaminodiphenyl sulfone
di(p-aminophenyl) sulfone
udolac
wr 448
benzenamine,4'-sulfonylbis-
bis(4-aminophenyl) sulfone
aniline,4'-sulfonyldi-
diaminodiphenyl sulfone
disulone
benzenamine, 4,4'-sulfonylbis-
KBIO1_000573
DIVK1C_000573
aczone
in-201
atrisone
SPECTRUM_000888
PRESTWICK_152
NCGC00016322-01
CBDIVE_013582
PRESTWICK3_000035
IDI1_000573
OPREA1_143052
4-aminophenylsulfone
sulfonyldianiline
bis(4-aminophenyl)sulfone
4-(4-aminophenyl)sulfonylaniline
sumicure s
BSPBIO_000129
SPECTRUM5_000825
PRESTWICK2_000035
BSPBIO_002129
4,4'-sulfonyldianiline (dapsone)
NCGC00023946-03
AB00051962
MLS001055349
sulfon-mere
sulfone ucb
hy 976
brn 0788055
hardener ht 976
dapsonum [inn-latin]
p,p-sulfonylbisbenzamine
di(4-aminophenyl)sulfone
4,4'-sulphonyldianiline
aniline, 4,4'-sulfonyldi-
di(p-aminophenyl)sulphone
1,1'-sulphonylbis(4-aminobenzene)
bis(4-aminophenyl)sulphone
4,4'-sulphonylbisbenzamine
bis(p-aminophenyl)sulphone
einecs 201-248-4
diaphenylsulphon
dapsona [inn-spanish]
4,4'-diaminodiphenyl suphone
diaminodifenilsulfona [spanish]
croysulphone
p,p-sulphonyldianiline
diamino-4,4'-diphenyl sulfone
diamino-4,4'-diphenyl sulphone
sulfone, diphenyl, 4,4'-diamino-
4,4'-diaminophenyl sulfone
araldite ht 976
dapsona
nsc 6091
dapsonum
4,4-diaminodifenylsulfon [czech]
hsdb 5073
dubronax
sulphadione
ht 976
di(4-aminophenyl)sulphone
diaphenylsulphone
avlosulphone
dds (pharmaceutical)
ccris 192
ai3-08087
dss (van)
tarimyl
p,p-diaminodiphenyl sulphone
4,4'-sulphonylbisbenzenamine
sulfanona-mae
p,p-sulfonylbisbenzenamine
sulphonyldianiline
C07666
4,4'-sulfonylbisbenzenamine
diaphenylsulfone
80-08-0
dapsone ,
4-aminophenyl sulfone, 97%
1,1'-sulfonylbis(4-aminobenzene)
4-(4-aminophenylsulfonyl)benzenamine
4-aminophenyl sulfone
4-(4-aminophenylsulfonyl)aniline
p,p-sulphonylbisbenzenamine
4,4'-dapsone
4,4'-diaminodiphenyl sulphone
4-(4-amino-benzenesulfonyl)-phenylamine
4,4'-sulfonylbisbenzeneamine
DB00250
4,4'-diaminodiphenylsulfone
p,p-sulphonylbisbenzamine
4,4'-sulfonyldianilin
4,4'-sulfonylbisaniline
dapsone (usp)
diaphenylsulfone (jan)
aczone (tn)
D00592
NCGC00023946-06
NCGC00023946-05
NCGC00023946-04
MLS000069409 ,
smr000059064
KBIO2_006504
KBIOGR_000900
KBIOSS_001368
KBIO2_001368
KBIO3_001349
KBIO2_003936
PRESTWICK0_000035
SPECTRUM2_001133
SPECTRUM4_000310
SPECTRUM3_000375
PRESTWICK1_000035
NINDS_000573
SPBIO_001025
SPBIO_002050
SPECTRUM1500222
BPBIO1_000143
azt + dapsone cominbation
NCGC00016322-02
4,4' diaminophenyl sulfone
sulfone, 4,4'-diaminophenyl
STK387118
HMS2091K04
AC-10922
D0089
CHEBI:4325 ,
HMS501M15
FT-0665473
HMS1568G11
HMS1920C14
NCGC00016322-08
AKOS000119322
4-(4-aminophenyl)sulfonylaniline;4,4'-diaminodiphenyl sulfone
A839828
BBL002412
HMS2095G11
HMS3259C13
NCGC00258899-01
tox21_300558
tox21_201347
NCGC00254533-01
4-[(4-aminobenzene)sulfonyl]aniline
nsc-756716
pharmakon1600-01500222
nsc756716
tox21_110371
dtxcid00371
dtxsid4020371 ,
cas-80-08-0
4-(4-aminobenzenesulfonyl)aniline
dds, diaphenylsulfone
sulphon-mere
HMS2231G09
S4612
CCG-40260
NCGC00016322-03
NCGC00016322-05
NCGC00016322-06
NCGC00016322-09
NCGC00016322-10
NCGC00016322-07
NCGC00016322-04
unii-8w5c518302
8w5c518302 ,
ec 201-248-4
dapsone [usan:usp:inn:ban]
4,4-diaminodifenylsulfon
diaminodifenilsulfona
FT-0624447
dapsone [hsdb]
dapsone [usp monograph]
dapsone [who-ip]
dapsone [mi]
dapsonum [who-ip latin]
dapsone [vandf]
diaphenylsulfone [jan]
dapsone [orange book]
dapsone [inn]
dapsone [iarc]
dapsone [mart.]
dapsone [ep monograph]
dapsone [who-dd]
dapsone [usan]
dapsone [usp-rs]
dapsone [ep impurity]
sulfacetamide sodium impurity d [ep impurity]
HMS3369B11
4,4'-dds
HY-B0688
4-[(4-aminophenyl)sulfonyl]aniline
NC00488
SCHEMBL21428
NCGC00016322-13
tox21_110371_1
4,4'-diamino diphenyl sulphone
Q-200435
bis sulfone
4,4'-sulfonylbis[benzamine]
4-[(4-aminophenyl)sulfonyl]phenylamine #
dianiline, 4,4'-sulfonyl-
ht 9664
4,4'-sulfonyldiphenylamine
diaphenyl sulfone
OPERA_ID_1950
AB00051962_19
mfcd00007887
F0266-3067
4,4 inverted exclamation mark(r)-sulfonyldianiline
sr-01000002976
SR-01000002976-2
dapsone, united states pharmacopeia (usp) reference standard
dapsone, vetranal(tm), analytical standard
dapsone, european pharmacopoeia (ep) reference standard
KS-1450
dapsone, pharmaceutical secondary standard; certified reference material
SR-01000002976-4
SBI-0051331.P003
HMS3712G11
4 4-diamino diphenyl sulfone 99.5%min cas:80-08-8
dapsone, british pharmacopoeia (bp) reference standard
1632119-29-9
Q422226
4 inverted exclamation marka-diaminodiphenyl sulfone
4 inverted exclamation marka-sulfonyldianiline
dapsone,(s)
2-(piperazin-1-yl)-aceticacidn-(2-phenylethyl)-amide
BRD-K62363391-001-15-7
AMY40781
gtpl10934
4,4'-diamino diphenyl sulfone
dapson 100 microg/ml in methanol
dapsone-d8(major)
EN300-19042
4,4'-diamino-15n2-diphenyl sulfone
4,4'-diaminodiphenyl-13c12-sulfone
Z104472374
p,p'-sulfonylbisbenzamine
p,p'-sulphonylbisbenzamine
dapsone (iarc)
sulfacetamide sodium impurity d (ep impurity)
dapsone (ep impurity)
p,p'-sulphonylbisbenzenamine
undolac
dapsone (ep monograph)
dapsonum (latin)
dapsone (mart.)
dapsone (usp-rs)
p,p'-diaminodiphenyl sulphone
d10ax05
4,4'-sulfonylbis(benzenamine)
p,p'-sulphonyldianiline
seikacure s
aczone7.5
dapsone (usp monograph)
4,4-diaminodifenylsulfon list acronyms
daspone

Research Excerpts

Overview

Dapsone is a sulfone chemical with reported anti-inflammatory and antibacterial properties. Dapsone (DAP)is a dual-function drug substance; however, its limited water solubility may impair its bioavailability.

ExcerptReferenceRelevance
"Dapsone is a "4,4'-diamino diphenyl sulfone" compound and an aniline derivative from synthetic sulphones. "( Dapsone for the treatment of acne vulgaris: do the risks outweigh the benefits?
Daye, M; Temiz, SA, 2022
)
3.61
"Dapsone is a sulfone chemical with reported anti-inflammatory and antibacterial properties."( The anti-inflammatory effect of dapsone on ovalbumin-induced allergic rhinitis in balb/c mice.
Alaeddini, M; Dabiri, S; Dehpour, AR; Etemad-Moghadam, S; Fatehi-Zardalou, M; Hemmati, S; Madanipour, MR; Rahimi, N; Shayan, M, 2022
)
1.73
"Dapsone is a topical drug approved by the U.S."( Efficacy and safety of dapsone gel for acne: a systematic review and meta-analysis.
Liu, H; Sun, L; Wang, X; Wang, Z; Zhang, F, 2022
)
1.75
"Dapsone (DAP)is a dual-function drug substance; however, its limited water solubility may impair its bioavailability. "( Highly water-soluble dapsone nanocrystals: Towards innovative preparations for an undermined drug.
Araci Bou-Chacra, N; de O Macedo, L; de Souza, A; Ishida, K; Lima Barros de Araújo, G; Löbenberg, R; Lopes Barreto, T; Nishitani Yukuyama, M; Paredes da Rocha, N, 2023
)
2.67
"Dapsone is a first line treatment option, however, there are limited options if this fails, or if contraindicated."( A Case of Successful Management of Adult-Onset Linear IgA Bullous Disease With Sulfasalazine During the COVID-19 Pandemic.
Ashraf, S; Elamin, S; Tolland, J, 2022
)
1.44
"Dapsone is an effective treatment for cutaneous Leishmaniasis."( Comparison Of Oral Dapsone With Intramuscular Meglumine Antimoniate In Cutaneous Leishmaniasis.
Ahmed, N; Fayyaz, I; Iftikhar, N; Malik, S; Rahman, A; Raza, N; Tahir, M,
)
1.9
"Dapsone (DAP) is an antibacterial used as anti-acne agent, but challenged by low water solubility and poor skin permeability."( Dapsone-Loaded Mixed Micellar Gel for Treatment OF Acne Vulgaris.
Deshpande, P; Deshpande, S; Rao, MR, 2023
)
3.07
"Dapsone is a highly useful drug for treating a variety of pathologies but oral dapsone is contraindicated in patients with G6PDd due to oxidative stress-induced anemia."( Hemolysis and Metabolic Lesion of G6PD Deficient RBCs in Response to Dapsone Hydroxylamine in a Humanized Mouse Model.
D'Alessandro, A; Dziewulska, KH; Hay, AM; Reisz, JA; Zimring, JC, 2023
)
1.87
"Dapsone is an expensive antibacterial drug with many side effects."( Multiple docking analysis and
Dhorajiwala, TM; Halder, ST; Samant, LR,
)
0.85
"Dapsone gel is a topical treatment for facial acne in adolescents and adults, and while systemic dapsone therapy is known to be associated with methemoglobinemia, once-daily topical dapsone has been well tolerated with few side effects in large randomized controlled trials. "( Severe methemoglobinemia due to topical dapsone misuse in a teenage girl.
McCarthy, J; McCarthy, P; McFadden, V; Stefanko, N; Yale, S, 2020
)
2.27
"Dapsone (DAP) is a long-established molecule that remains a promising therapeutic agent for various diseases mainly because it combines antimicrobial and anti-inflammatory activities. "( Emerging Technologies to Target Drug Delivery to the Skin - the Role of Crystals and Carrier-Based Systems in the Case Study of Dapsone.
Argenta, DF; Caon, T; Schneider-Rauber, G, 2020
)
2.21
"Dapsone is a rapid and extremely effective first-line treatment option and often used while transitioning to a gluten-free diet."( Significant improvement of dermatitis herpetiformis with tofacitinib.
Kahn, JS; Moody, K; Rosmarin, D, 2021
)
1.34
"Dapsone is a sulfone drug used to treat infectious conditions and also numerous dermatologic diseases. "( Dapsone-associated fixed drug eruption.
Cohen, PR; Garcia, D, 2017
)
3.34
"Dapsone is an extensively Used drug for the treatment of leprosy as well as'some other clinical problems worldwide: Its use has been predicted to increase further, especially in non leprosy conditions. "( Dapsone: An Update.
Aruna, B; Kallappa, H; Karjigi, S; Kusuma, MR; Murthy, SC; Reddy, YN, 2016
)
3.32
"Dapsone gel, 7.5% is a topical medication approved for acne in patients aged 12 years and older. "( Clinical Experience With Once-Daily Dapsone Gel, 7.5% Monotherapy in Patients With Acne Vulgaris.
Alvandi, N; Lain, E; Stockton, TC; Tanghetti, EA; Zeichner, JA, 2018
)
2.2
"Dapsone is a sulfone derived drug used in the treatment of leprosy and several chronic inflammatory dermatological diseases. "( Dapsone Hypersensitivity Syndrome (DHS): A Detrimental Effect of Dapsone? A Case Report.
George, NE; Priya, S; Shukkoor, AA; Thangavelu, S, 2019
)
3.4
"Dapsone is a sulfone drug mainly used as anti-microbial and anti-inflammatory agent for the treatment of various diseases including leprosy. "( DNA minor groove binding of a well known anti-mycobacterial drug dapsone: A spectroscopic, viscometric and molecular docking study.
Biswas, A; Chakraborty, A; Ghosh, R; Panda, AK, 2019
)
2.19
"Dapsone (DAP) is a bactericidal agent used in the treatment of leprosy, caused by Mycobacterium leprae. "( pH-responsive chitosan based hydrogels affect the release of dapsone: Design, set-up, and physicochemical characterization.
Celia, C; Chaves, LL; Cristiano, MC; Di Marzio, L; Ferreira, D; Lima, SC; Paolino, D; Reis, S; Sarmento, B; Silveri, A; Vieira, ACC, 2019
)
2.2
"• Dapsone is a bacteriostatic antibacterial sulfonamide drug found to be effective in the treatment of some inflammatory dermatological diseases like IgA vasculitis."( Indications and efficiency of dapsone in IgA vasculitis (Henoch-Schonlein purpura): case series and a review of the literature.
Dima, B; Gilliaux, O; Muyshont, L; Roman, C; Schurmans, T, 2019
)
1.36
"Dapsone is an inexpensive drug with a well-established safety profile."( Dapsone for primary immune thrombocytopenia in adults and children: an evidence-based review.
Gooneratne, L; Rodrigo, C, 2013
)
2.55
"Dapsone is a safe and cheap second-line therapy for ITP with a response rate of about 50% (majority being CR)."( Dapsone for immune thrombocytopenic purpura in children and adults.
Patel, AP; Patil, AS, 2015
)
2.58
"Dapsone is a drug commonly used in the treatment of various dermatological diseases. "( Livedo reticularis associated with dapsone therapy in a patient with chronic urticaria.
Sameem, F; Wafai, ZA; Zulfkar, Q,
)
1.85
"Dapsone is a sulfone-type drug used widely for different infectious, immune, and hypersensitivity disorders as an antibacterial treatment alone or in combination for leprosy and sometimes for infected skin lesions. "( Fulminant hepatitis linked to dapsone hypersensitivity syndrome requiring urgent living donor liver transplantation: a case report.
Choi, YR; Garcia, A; Hong, G; Kang, EK; Kang, HJ; Kim, JG; Lee, JM; Lee, KB; Lee, KW; Park, JD; Suh, KS; Suh, SW; Yi, NJ; You, T, 2014
)
2.13
"Dapsone is a drug commonly used in the treatment of leprosy. "( Acute Poisoning with Dapsone and Olanzapine: Severe Methemoglobinemia and Coma with a Favourable Outcome.
Grudeva-Popova, JG; Iliev, YT; Zagorov, MY,
)
1.89
"Dapsone resistance is a serious impediment to the implementation of the present leprosy control strategies. "( Discovery of a potential lead compound for treating leprosy with dapsone resistance mutation in M. leprae folP1.
Dhanasekaran, D; Nawaz Khan, F; Nisha, J; Ramanathan, K; Shanthi, V, 2016
)
2.11
"Dapsone is an effective and safe treatment option."( Successful treatment of eosinophilic cellulitis with dapsone.
Cardoso, J; Coelho de Sousa, V; Laureano Oliveira, A, 2016
)
1.41
"Dapsone is a chemotherapeutic agent with anti-inflammatory properties that is used as a steroid-sparing agent in PV."( Efficacy of Dapsone in the Treatment of Pemphigus Vulgaris: A Single-Center Case Study.
Barzilai, A; Baum, S; Debby, A; Gilboa, S; Trau, H, 2016
)
1.53
"Dapsone is an efficient anti-inflammatory and antimycobacterial agent. "( Dapsone-induced photosensitivity: a rare clinical presentation.
Kar, BR, 2008
)
3.23
"Dapsone is a chemotherapeutic agent primarily used in treating leprosy, Pneumocystis jiroveci (previously carinii) pneumonia, and malaria. "( Efficacy of dapsone in the treatment of pemphigus and pemphigoid: analysis of current data.
Ahmed, AR; Gürcan, HM, 2009
)
2.17
"Dapsone is a leprostatic agent commonly prescribed for the treatment of patients with leprosy, malaria, and a variety of blistering skin diseases, including dermatitis herpetiformis. "( Pathophysiologic mechanisms, diagnosis, and management of dapsone-induced methemoglobinemia.
Ashurst, JV; Fritz, WT; Hauger, W; Wasson, MN, 2010
)
2.05
"Dapsone is an antibacterial sulfonamide with anti-inflammatory property, which showed therapeutic activity in patients with immune thrombocytopenia (ITP); the activity in patients who showed refractoriness to rituximab is unknown. "( Dapsone salvage therapy for adult patients with immune thrombocytopenia relapsed or refractory to steroid and rituximab.
Chiozzotto, M; Fanin, R; Marin, L; Puglisi, S; Volpetti, S; Zaja, F, 2012
)
3.26
"Dapsone is a commonly prescribed medication in dermatological practice. "( Improving adherence to safe prescription guidelines for Dapsone: harnessing an enhanced electronic medical records system and a team approach.
Chan, RK; Choi, C; Leong, HH; Neoh, CY; Tan, AW; Tian, EA, 2012
)
2.07
"Dapsone syndrome is a potentially fatal hypersensitivity reaction to sulphone. "( Dapsone syndrome--first Malaysian paediatric case report.
Elizawaty, O; Norlijah, O; Thevarajah, S; Zurina, Z, 2012
)
3.26
"Dapsone is a sulfone with anti-inflammatory properties, therefore it may have a beneficial effect in the treatment of asthma and act as a corticosteroid-sparing agent."( Dapsone as an oral corticosteroid sparing agent for asthma.
Bara, A; Dean, T; Dewey, A; Walters, H, 2002
)
2.48
"Dapsone syndrome is a manifestation of the DRESS (drug rash with eosinophilia and systemic symptoms) syndrome which is a serious condition that has been reported in association with various drugs."( Dapsone induced cholangitis as a part of dapsone syndrome: a case report.
Choudhuri, G; Dhingra, S; Itha, S; Kumar, A, 2003
)
2.48
"Dapsone syndrome is a rare hypersensitivity reaction to dapsone and is characterized by high fever, papular or exfoliative dermatitis, progressing to liver toxicity and generalized lymphadenopathy, resembling a mononucleosis infection. "( Dapsone syndrome with acute renal failure during leprosy treatment: case report.
Alves-Rodrigues, EN; Fontes, CJ; Ribeiro, LC; Silva, MD; Takiuchi, A, 2005
)
3.21
"Dapsone appears to be an effective and safe alternative therapeutic option for hidradenitis suppurativa and may be particularly useful for women in the reproductive age group."( Hidradenitis suppurativa treated with dapsone: A case series of five patients.
Kaur, MR; Lewis, HM, 2006
)
2.05
"Dapsone is a component of multi-drug therapy (MDT) for the treatment of all types of leprosy. "( Mortality due to dapsone hypersensitivity syndrome complicating multi-drug therapy for leprosy in Nepal.
Hawksworth, RA; Lewis, J; Pandey, B; Shrestha, K; Walker, SL, 2007
)
2.12
"Dapsone is a leprostatic agent commonly prescribed for the management of leprosy, malaria, and the immunosuppression-induced infections of Pneumocystis carinii and Toxoplasma gondii. "( The recognition, physiology, and treatment of medication-induced methemoglobinemia: a case report.
Glickman, RS; Karlis, V; Turner, MD, 2007
)
1.78
"Dapsone is a potent cause for introgenic methemoglobinemia that is frequently unrecognized. "( Dapsone-induced methemoglobinemia: case report and literature review.
Leikin, JB; Rychter, K; Zosel, A,
)
3.02
"Dapsone is a sulfone essentially used to treat leprae. "( [Dapsone: an opportunity to spare corticoid use for Henoch-Schönlein treatment? A case report].
Bovy, C; Krzesinski, JM; Parotte, MC, 2007
)
2.69
"Dapsone is a helpful adjuvant to therapy."( Juvenile pemphigus.
Ahmed, AR; Salm, M, 1983
)
0.99
"Dapsone hydroxylamine is a direct-acting hemolytic agent responsible for dapsone-induced hemolytic anemia in the rat. "( Dapsone-induced hemolytic anemia: effect of dapsone hydroxylamine on sulfhydryl status, membrane skeletal proteins and morphology of human and rat erythrocytes.
Budinsky, RA; Jollow, DJ; McMillan, DC; Simson, JV, 1995
)
3.18
"1. Dapsone is a potent anti-inflammatory and anti-parasitic compound, which is metabolised by cytochrome P-450 to hydroxylamines, which in turn cause methaemoglobinaemia and haemolysis. "( Dapsone toxicity: some current perspectives.
Coleman, MD, 1995
)
2.36
"Dapsone is a drug widely prescribed in dermatology. "( [Agranulocytosis induced by dapsone prescribed for dermatitis herpetiformis].
Callens, A; Gargot, S; Lorette, G; Machet, L; Mercier, E; Vaillant, L, 1996
)
2.03
"Dapsone is a drug that is being used for a wide variety of clinical conditions. "( Acute dapsone intoxication: a pediatric case report.
MacDonald, RD; McGuigan, MA, 1997
)
2.22
"Dapsone is a drug of choice in the treatment of leprosy. "( Dapsone induced pulmonary eosinophilia without cutaneous allergic manifestations--an unusual encounter--a case report.
Arunthathi, S; Raju, S, 1998
)
3.19
"Dapsone is a drug which is administered orally, on a daily basis, for four to five years as a cure for leprosy. "( In vitro and in vivo dapsone release from hydroxyapatite reservoirs.
Bajpai, PK; Berty, S; Lasserre, A, 1997
)
2.06
"Dapsone is a cheap and effective prophylactic agent against P carinii in patients who cannot tolerate trimethoprim-sulfamethoxazole."( Bilateral upper-lobe cavitary Pneumocystis carinii pneumonia in a patient on dapsone prophylaxis.
Anandarao, N; Dama, S; Jawahar, DA; Miarrostami, R; Sadagdhar, H, 1999
)
1.25
"Dapsone is an alternative drug for Pneumocystis carinii pneumonia (PCP) prophylaxis in individuals intolerant to trimethoprim-sulfamethoxazole (T/S). "( Toxicity and efficacy of daily vs. weekly dapsone for prevention of Pneumocystis carinii pneumonia in children infected with human immunodeficiency virus. ACTG 179 Study Team. AIDS Clinical Trials Group.
Bonagura, V; Cooper, E; Jacobus, D; Kovacs, A; Lindsey, J; McIntosh, K; McNamara, J; Mirochnick, M; Mofenson, L; Nachman, S; Sacks, H; Sleasman, J; Spector, SA; Sullivan, JL; Xu, J; Yogev, R, 1999
)
2.01
"Dapsone is a potent anti-inflammatory and antibacterial agent that has been used extensively in the oral treatment of leprosy and dermatitis herpetiformis. "( Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone.
Bethem, RA; Buonarati, MH; Helton, DR; Osborne, DW; Pierson, SK, 2000
)
1.97
"Dapsone is a bacteriostatic agent that proved to be efficient in treating leprosy and malaria, but today it is used in treating dermatologic noninfectious inflammatory diseases."( [What do we know today about diaminodiphenylsulfone?].
Golusin, Z; Poljacki, M; Preveden, R; Rajić, N; Stojanović, S,
)
0.85
"Dapsone is a synthetic sulfone increasingly used in the treatment of a wide variety of dermatologic disorders. "( Recurrent methemoglobinemia after acute dapsone intoxication in a child.
Linakis, JG; Sax, C; Shannon, M; Woolf, A,
)
1.84
"Dapsone is an effective anti-inflammatory agent in conditions in which inflammation is mediated by neutrophils. "( Metabolism of dapsone to a hydroxylamine by human neutrophils and mononuclear cells.
Biggar, WD; Shear, NH; Uetrecht, J; Zahid, N, 1988
)
2.08
"Dapsone (DDS) is a drug of choice in the treatment of leprosy. "( Plasma dapsone and its metabolite monoacetyldapsone levels in leprotic patients.
Bakaya, V; Garg, SK; Kaur, S; Kumar, B; Lal, R; Shukla, VK, 1988
)
2.17

Effects

Dapsone may target the pathophysiology of pustular psoriasis more directly than many other systemic agents. Dapsone has a pharmacological double function as both an antibiotic and an antiphlogistic drug.

Dapsone has antimicrobial effects stemming from its sulfonamide-like ability to inhibit the synthesis of dihydrofolic acid. Dapsone utilized for the prevention of Pneumocystis jirovecii pneumonia in immunosuppressed patients.

ExcerptReferenceRelevance
"Dapsone has a much safer side effect profile and may target the pathophysiology of pustular psoriasis more directly than many other systemic agents. "( Dapsone Therapy for Pustular Psoriasis: Case Series and Review of the Literature.
Divito, SJ; Enamandram, M; Merola, JF; Sheu, JS, 2016
)
3.32
"Dapsone has a pharmacological double function as both an antibiotic and an antiphlogistic drug."( [Dapsone in granulomatous rosacea].
Hafner, J; Krause, MH; Kündig, T; Torricelli, R; Trüeb, RM, 1997
)
1.93
"Dapsone has been the mainstay for the treatment of leprosy since its discovery in the 1940s. "( Hematological alterations in lepromatous leprosy: A cross-sectional observational study.
Awan, KH; Chaudhary, M; Gupta, B; Gupta, S; Patil, S; Raj, AT, 2020
)
2
"Dapsone has antimicrobial effects stemming from its sulfonamide-like ability to inhibit the synthesis of dihydrofolic acid."( Update on the use of dapsone in dermatology.
Abbas, O; Ghaoui, N; Hanna, E; Kibbi, AG; Kurban, M, 2020
)
1.6
"Dapsone has been utilized for the prevention of Pneumocystis jirovecii pneumonia in immunosuppressed patients including pediatric kidney transplant recipients, in whom trimethoprim-sulfamethoxazole (TMP-SMX) is contraindicated. "( Dapsone-induced methemoglobinemia in pediatrics post-renal transplant.
Hindka, A; Huynh, D; Verghese, PS, 2021
)
3.51
"Dapsone has been part of the World Health Organization multidrug therapy for the treatment of leprosy. "( Fatal dapsone hypersensitivity syndrome with hypothyroidism and steroid-induced diabetes mellitus.
Munshi, R; Nayak, C; Pai, S,
)
2.05
"Dapsone has been the main active principle in the multidrug regimen recommended by the World Health Organization for the treatment of leprosy."( Metabolic, pharmacokinetic, and toxicological issues surrounding dapsone.
Brisigotti, V; Campanati, A; Molinelli, E; Offidani, A; Paolinelli, M, 2019
)
1.47
"Dapsone has been successfully used for the treatment of granulomatous rosacea and rosacea fulminans."( [Systemic therapy of rosacea].
Belge, K; Schaller, M, 2013
)
1.11
"Dapsone has been frequently used in treating disseminated disease in immunocompetent individuals."( Novel multidrug therapy for disseminated rhinosporidiosis, refractory to dapsone – case report.
Agarwala, M; Chopra, M; Deodhar, D; Dincy, P; George, L; Maheswaran, S; Pulimood, S; Rupali, P; Thomas, M, 2013
)
1.34
"Dapsone has been investigated predominantly by in vitro methods aiming to get more insights into the effect of dapsone to inflammatory effector cells, cytokines, and/or mediators, such as cellular toxic oxygen metabolism, myoloperoxidase-/halogenid system, adhesion molecules, chemotaxis, membrane-associated phospholipids, prostaglandins, leukotrienes, interleukin-8, tumor necrosis factor α, lymphocyte functions, and tumor growth."( Dapsone in dermatology and beyond.
Blasum, C; Wozel, G, 2014
)
2.57
"Dapsone is cheap and has response rates comparable to other second line treatment options like azathioprine, danazol, cyclophosphamide, cyclosporine, and vincristine."( Dapsone for immune thrombocytopenic purpura in children and adults.
Patel, AP; Patil, AS, 2015
)
2.58
"Dapsone has a much safer side effect profile and may target the pathophysiology of pustular psoriasis more directly than many other systemic agents. "( Dapsone Therapy for Pustular Psoriasis: Case Series and Review of the Literature.
Divito, SJ; Enamandram, M; Merola, JF; Sheu, JS, 2016
)
3.32
"Oral dapsone has demonstrated efficacy in acne, but was associated with severe side effects such as anemia, which was particularly serious in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency."( Aczone, a topical gel formulation of the antibacterial, anti-inflammatory dapsone for the treatment of acne.
Scheinfeld, N, 2009
)
1.04
"Oral dapsone has been available for over 60 years. "( An evaluation of dapsone gel 5% in the treatment of acne vulgaris.
Pickert, A; Raimer, S, 2009
)
1.21
"Dapsone has potent anti-inflammatory effects, and is used in the treatment of leprosy, cutaneous vasculitis, neutrophilic dermatoses, and dermatitis herpetiformis and other blistering disorders. "( Dapsone hypersensitivity syndrome with circulating 190-kDa and 230-kDa autoantibodies.
Chun, JS; Kim, SJ; Lee, JB; Lee, SC; Won, YH; Yun, SJ, 2009
)
3.24
"Dapsone has been associated with decreased lifespan of erythrocytes, with consequences such as anaemia and morbidity in patients treated with dapsone for malaria."( Dapsone hydroxylamine induces premature removal of human erythrocytes by membrane reorganization and antibody binding.
Bordin, L; Clari, G; Coleman, MD; Fiore, C; Ragazzi, E; Zen, F, 2010
)
2.52
"Dapsone has shown anti-convulsive properties in animal models of epilepsy. "( Safety and tolerability of dapsone for the treatment of patients with drug-resistant, partial-onset seizures: an open-label trial.
Corona, T; Diaz-Ruiz, A; López-Gómez, M; Ríos, C, 2011
)
2.11
"Dapsone has potent anti-inflammatory effects and remains an effective therapy in a variety of skin disorders: cutaneous vasculitis, neutrophilic dermatoses and blistering disorders. "( Alternative procedure to allow continuation of dapsone therapy despite serious adverse reaction in a case of dapsone-sensitive erythema elevatum diutinum.
Ezzedine, K; Guillet, S; Milpied, B; Seneschal, J; Taïeb, A, 2012
)
2.08
"Dapsone has been shown to be effective in treating immune thrombocytopenic purpura (ITP) in adults. "( Dapsone treatment in a girl with severe chronic thrombocytopenic purpura. Does it work? Do not touch it!
Nocerino, A; Passone, E; Pusiol, A; Tenore, A, 2012
)
3.26
"Dapsone has been shown to be effective in treating adults with immune thrombocytopenic purpura (ITP). "( Dapsone therapy for children with immune thrombocytopenic purpura.
Delaney, KS; Goldsby, R; Meeker, ND; Slayton, WB; Terrill, KR, 2003
)
3.2
"Dapsone has been used successfully as adjuvant therapy for bullous pemphigoid (BP). "( Treatment of bullous pemphigoid with dapsone, methylprednisolone, and topical clobetasol propionate: a retrospective study of 62 cases.
Bröcker, EB; Goebeler, M; Kraensel, R; Rzany, B; Schmidt, E; Sinkgraven, R; Zillikens, D, 2005
)
2.04
"Dapsone has several adverse effects in its profile that make it a potentially dangerous second-line agent."( Adverse reactions associated with dapsone therapy in HIV-positive patients: a case presentation and review.
Miller, JA; Reust, R; Stephens, JR; Stroup, JS, 2006
)
1.33
"Oral dapsone has been available for over 60 years and has been used to treat severe acne vulgaris; however, the oral formulation is known to cause dose-dependent haematological reactions and is currently indicated only for diseases such as dermatitis herpetiformis and Hansen's disease. "( Pharmacokinetics of dapsone gel, 5% for the treatment of acne vulgaris.
Garrett, S; Halder, R; Sharata, H; Thiboutot, DM; Willmer, J, 2007
)
1.18
"Dapsone has been used since 1976 in the treatment of relapsing polychondritis. "( [Chronic atrophic polychondritis. Critical analysis of the therapeutic efficacy of dapsone. 2 cases].
Abadie, JC; Gouet, D; Marechaud, R; Neau, JP; Rossi, F; Sudre, Y, 1984
)
1.94
"Dapsone has been used in various dermatological disorders and in leprosy. "( Dapsone induced hypohaptoglobinemia in lepromatous leprosy patients.
Bharadwaj, VP; Girdhar, BK; Sritharan, V; Venkatesan, K, 1981
)
3.15
"Dapsone has no therapeutic effect, but it does have a slight prophylactic effect, and in combination with clarithromycin it does not abrogate the effect of clarithromycin."( Clarithromycin, dapsone, and a combination of both used to treat or prevent disseminated Mycobacterium avium infection in beige mice.
Bermudez, LE; Inderlied, CB; Kolonoski, P; Petrofsky, M; Young, LS, 1994
)
1.36
"Dapsone has been proposed as a prophylactic agent for both Pneumocystis carinii pneumonia (PCP) and reactivation cerebral toxoplasmosis. "( Dapsone penetrates cerebrospinal fluid during Pneumocystis carinii pneumonia prophylaxis.
Mirochnick, M; Rich, JD, 1996
)
3.18
"Dapsone has a pharmacological double function as both an antibiotic and an antiphlogistic drug."( [Dapsone in granulomatous rosacea].
Hafner, J; Krause, MH; Kündig, T; Torricelli, R; Trüeb, RM, 1997
)
1.93
"Dapsone has clinical utility as an anti-inflammatory agent but the mechanism of this action remains unknown. "( Anti-inflammatory action of dapsone: inhibition of neutrophil adherence is associated with inhibition of chemoattractant-induced signal transduction.
Debol, SM; Herron, MJ; Nelson, RD, 1997
)
2.03
"Dapsone has been shown to activate flurbiprofen 4'-hydroxylation by expressed CYP2C9 enzyme and in human liver microsomes. "( Minimal in vivo activation of CYP2C9-mediated flurbiprofen metabolism by dapsone.
Branch, RA; Frye, RF; Huang, SM; Hutzler, JM; Korzekwa, KR; Tracy, TS, 2001
)
1.98
"Dapsone has been used successfully to treat a range of dermatologic disorders, most successfully those characterized by abnormal neutrophil and eosinophil accumulation."( Dapsone and sulfones in dermatology: overview and update.
Stiller, MJ; Zhu, YI, 2001
)
2.47
"Dapsone has been examined by two established animal anti-inflammatory models and found to possess anti-inflammatory activity comparable with established non-steroidal anti-inflammatory drugs. "( Anti-inflammatory actions of dapsone and its related biochemistry.
Best, R; Capstick, RB; Lewis, DA; Williams, K, 1976
)
1.99
"Dapsone has been shown to possess anti-inflammatory activity in a variety of animal models. "( The anti-inflammatory profile of dapsone in animal models of inflammation.
Gemmell, DK; Lewis, AJ; Stimson, WH, 1978
)
1.98
"Dapsone prophylaxis has been shown to prevent secondary cases in contacts up to 25 years old and should be used in these and possibly in older persons."( Management of household contacts of leprosy patients.
Filice, GA; Fraser, DW, 1978
)
0.98
"Dapsone has been shown to possibly inhibit lysosomal enzyme activity."( Relapsing polychondritis treated with dapsone.
Lynch, W; Martin, J; Roenigk, HH; Tingwald, FR, 1976
)
1.25
"Oral dapsone has certain advantages over other current forms of treatment: it is economical and widely available in countries where cutaneous leishmaniasis is common, and it is effective by mouth and well tolerated."( A double-blind study on the efficacy of oral dapsone in cutaneous leishmaniasis.
Dogra, J,
)
0.85
"Dapsone, which has been reported to be effective in the treatment of relapsing polychondritis, did not control the destructive scleral inflammation in six (75%) of eight patients; two (50%) of four patients with diffuse anterior scleritis were controlled with this drug."( Scleritis in relapsing polychondritis. Response to therapy.
Foster, CS; Hoang-Xaun, T; Rice, BA, 1990
)
1
"Dapsone has been suggested as a useful drug in the treatment of granuloma annulare; however, adverse reactions include a potentially life-threatening agranulocytosis. "( Agranulocytosis caused by dapsone therapy for granuloma annulare.
Kennedy, CT; Potter, MN; Slade, R; Yates, P, 1989
)
2.02
"Dapsone also has been associated with agranulocytosis."( Metabolism of dapsone to a hydroxylamine by human neutrophils and mononuclear cells.
Biggar, WD; Shear, NH; Uetrecht, J; Zahid, N, 1988
)
1.36
"Dapsone (DDS) has for about 4 decades been the most important antileprosy drug. "( Clinical pharmacokinetics of dapsone.
Hilbers-Modderman, ES; Merkus, FW; Zuidema, J,
)
1.87

Actions

Dapsone is a potent cause for introgenic methemoglobinemia that is frequently unrecognized. Dapsone can rarely cause a hypersensitivity reaction called dapsone syndrome, consisting of fever, hepatitis, exfoliative dermatitis, lymphadenopathy and hemolytic anemia.

ExcerptReferenceRelevance
"Dapsone treatment can cause a variety of side effects that can be categorized as pharmacological, dose-related, allergic, or idiosyncratic reactions."( Dapsone for the treatment of acne vulgaris: do the risks outweigh the benefits?
Daye, M; Temiz, SA, 2022
)
2.89
"Dapsone is known to cause hemolytic anemia (HA) and this adverse event during MDT seems to be more frequent than reported."( Hemolytic anemia in patients receiving daily dapsone for the treatment of leprosy.
Deps, P; Guerra, P; Nasser, S; Simon, M, 2012
)
1.36
"Dapsone can rarely cause a hypersensitivity reaction called dapsone syndrome, consisting of fever, hepatitis, exfoliative dermatitis, lymphadenopathy and hemolytic anemia. "( Dapsone induced cholangitis as a part of dapsone syndrome: a case report.
Choudhuri, G; Dhingra, S; Itha, S; Kumar, A, 2003
)
3.2
"Dapsone is a potent cause for introgenic methemoglobinemia that is frequently unrecognized. "( Dapsone-induced methemoglobinemia: case report and literature review.
Leikin, JB; Rychter, K; Zosel, A,
)
3.02
"Dapsone might not inhibit peroxidase-mediated antimicrobial activity, which occurs at high enzyme concentrations in the acid environment of phagolysosomes."( Inhibition of the human leukocyte enzymes myeloperoxidase and eosinophil peroxidase by dapsone.
Bozeman, PM; Learn, DB; Thomas, EL, 1992
)
1.23
"Dapsone was chosen because it inhibits neutrophil function and possesses anti-inflammatory effects in a variety of disorders."( The effect of dapsone in steroid-dependent asthma.
Berlow, BA; Dyer, Z; Liebhaber, MI; Spiegel, TM, 1991
)
1.36
"Dapsone alone did not produce any significant alteration in rifampicin pharmacokinetics parameters, while dapsone with clofazimine reduced rifampicin 1h serum levels (P less than 0.05) and Auc (P less than 0.05) significantly."( Effect of clofazimine and dapsone on rifampicin (Lositril) pharmacokinetics in multibacillary and paucibacillary leprosy cases.
Gandhi, IS; Mehta, J; Sane, SB; Wamburkar, MN,
)
1.15

Treatment

Dapsone gel-treated patients achieved superior results in terms of the investigator's global acne assessment. Oral dapsone treatment (34 microg/g/day, for 5 weeks) reduced the BrdU incorporation in the skin and the epithelial thickness in the esophagus.

ExcerptReferenceRelevance
"Dapsone treatment can cause a variety of side effects that can be categorized as pharmacological, dose-related, allergic, or idiosyncratic reactions."( Dapsone for the treatment of acne vulgaris: do the risks outweigh the benefits?
Daye, M; Temiz, SA, 2022
)
2.89
"Dapsone treated both bronchitis and COPD."( Bronchitis, COPD, and pneumonia after viral endemic of patients with leprosy on Sorok Island in South Korea.
Altschuler, E; Bourbeau, J; Choi, SH; Coleman, M; Kanwar, B; Khattak, A; Lee, JH; Lee, SJ; Park, J; Sergi, C, 2023
)
1.63
"Dapsone is the treatment of choice, which is started at a dosage of 0.5mg/kg/day."( Linear IgA bullous dermatosis of childhood.
Blickenstorfer, M; Jungo, P; Juratli, HA; Lapides, R; Mühleisen, B; Nasri, J; Navarini, AA; Roider, E, 2022
)
1.44
"Dapsone remains the treatment of choice but other valid therapeutic alternatives i.e., retinoids, phototherapy, or anti-TNF inhibitors also need to be explored because of the side effects associated with dapsone."( When Rings Are Not Ringworms: Case Reports and Review of Literature.
Baig, BU; Bhatti, H; Khalid, N; Rao, BK, 2015
)
1.14
"Dapsone is the treatment of choice to control the skin manifestations."( [Sneddon and Wilkinson's subcorneal pustulosis].
Martalo, O; Paquet, P; Piérard, GE, 2003
)
1.04
"Dapsone-treated animals showed a reduction of 93% (9.375 mg/kg dose) and 92% (12.5 mg/kg dose) in the infarction volume as compared to control values."( Neuroprotective effect of dapsone in an occlusive model of focal ischemia in rats.
Nader-Kawachi, J; Nava-Ruiz, C; Ríos, C; Rodriguez-Payán, AJ, 2004
)
1.34
"Dapsone gel-treated patients achieved superior results in terms of the investigator's global acne assessment (P < .001) and the mean percentage reduction in inflammatory, noninflammatory, and total lesion counts (all, P < .001) at week 12. "( Two randomized studies demonstrate the efficacy and safety of dapsone gel, 5% for the treatment of acne vulgaris.
Carter, E; Draelos, ZD; Elewski, B; Garrett, S; Lynde, C; Maloney, JM; Poulin, Y, 2007
)
2.02
"Dapsone treatment cleared her skin lesion, but did not remove the paraesthesia in the right ulnar nerve."( Leprosy in Vietnamese refugees: a case report.
Christiansen, JV; Jensen, JR; Søgård, H; Thestrup-Pedersen, K, 1983
)
0.99
"Dapsone treatment of 100 mg daily for 14 days brought down the haptoglobin level significantly as compared to the untreated cases and the controls (p less than 0.05)."( Dapsone induced hypohaptoglobinemia in lepromatous leprosy patients.
Bharadwaj, VP; Girdhar, BK; Sritharan, V; Venkatesan, K, 1981
)
2.43
"Oral dapsone treatment was 0.7 mg/kg twice daily for 3 days."( Dapsone or electric shock therapy of brown recluse spider envenomation?
Barrett, SM; Fisher, DE; Romine-Jenkins, M, 1994
)
2.19
"Oral dapsone treatment was begun in the emergency room."( Management of the brown recluse spider bite to the glans penis.
Broughton, G, 1996
)
0.75
"Oral dapsone treatment (34 microg/g/day, for 5 weeks) reduced the BrdU incorporation in the skin and the epithelial thickness in the esophagus."( Therapeutic interventions in mice with chronic proliferative dermatitis (cpdm/cpdm).
Bruijnzeel, PL; Elliott, GR; Gijbels, MJ; HogenEsch, H; van den Hoven, A; Zurcher, C, 2000
)
0.76
"Dapsone, a treatment used for pneumocystis carinii pneumonia (PCP), is ineffective when taken in conjunction with ddI. "( Dapsone not affected by chewable ddI.
,
)
3.02
"Dapsone treatment achieved complete healing in 5 weeks."( Dapsone in rosacea fulminans.
Bormann, G; Fischer, M; Gaber, G; Marsch, WC, 2001
)
2.47
"In dapsone-treated patients, there were significant reductions in the oral and genital ulcer parameters as well as the incidence of other cutanous and systemic manifestations."( Dapsone in Behçet's disease: a double-blind, placebo-controlled, cross-over study.
Abu-Raghif, AR; Najim, RA; Sharquie, KE, 2002
)
2.27
"Dapsone remains the treatment of choice, but several newer drugs show great promise, especially in those cases whose bacilli have become sulfone resistant."( The diagnosis and treatment of leprosy.
Jacobson, RR; Trautman, JR, 1976
)
0.98
"Dapsone treated group showed a disability rate of 63.8% as compared to 30.0% in untreated group."( Pattern of leprosy disabilities in Gorakhpur (Uttar Pradesh).
Arora, SK; Girdhar, M; Mohan, L; Mukhija, RD, 1989
)
1
"The dapsone treatment resulted in bringing these levels to normal."( Serum angiotensin-converting enzyme in leprosy.
Dhople, AM; Howell, PC; Storrs, EE; Williams, SL; Zeigler, JA,
)
0.61
"The dapsone treatment gave excellent results in 8 patients (24%), some effect in 8 patients (24%), while no response was seen in 17 patients (52%)."( Dapsone in the treatment of cutaneous lupus erythematosus.
Lindskov, R; Reymann, F, 1986
)
2.19
"A treatment with dapsone was prescribed and yielded rapid improvement."( Scarring alopecia in chronic cutaneous lupus erythematosus with neutrophils: A new scenario with therapeutic connotations.
Bello, JA; Cabo, F; Fernandez-Flores, A; Hermosa-Gelbard, A; Pérez, A, 2020
)
0.89
"Treatment with dapsone and metformin reversed the effects of testosterone in the DAP and MET groups."( The effect of dapsone in testosterone enanthate-induced polycystic ovary syndrome in rat.
Dehpour, AR; Khaledi, E; Khazaei, M; Noori, T; Sadeghi, F; Shirooie, S; Sobarzo-Sánchez, E, 2021
)
1.32
"Treatment with Dapsone is sometimes known'to be associated with side-effects, which include gastrointestinal intolerance, haemolysis, methaemoglobinaemia, agranulocytosis, psychosis, peripheral neuritis and varied dermatological conditions, varying from simple rash to severe life threatening epidermolytic reactions and Dapsone hypersensitivity syndrome (DHS)."( Dapsone: An Update.
Aruna, B; Kallappa, H; Karjigi, S; Kusuma, MR; Murthy, SC; Reddy, YN, 2016
)
2.22
"Treatment with dapsone was initiated at a dose of 50 mg per day."( Successful treatment of eosinophilic cellulitis with dapsone.
Cardoso, J; Coelho de Sousa, V; Laureano Oliveira, A, 2016
)
1.02
"Treatment with dapsone resulted in complete resolution of the skin lesions."( Erythema elevatum diutinum in systemic lupus erythematosus.
Chan, Y; Mok, CC; Tang, WY, 2011
)
0.71
"Treatment with dapsone was started and resulted in considerable improvement."( [Hypocomplementemic vasculitis treated with dapsone].
Barbaud, A; Beurey, P; Bursztejn, AC; Cuny, JF; Hérault, M; Mazet, J; Schmutz, JL,
)
0.73
"Treatment with dapsone and prednisolone resulted in gradual clinical improvement."( Atypical response to treatment in linear IgA bullous dermatosis of childhood: Revision of literature.
Calha, M; Moleiro, S; Pessoa, G; Santos, V, 2011
)
0.71
"Treatment with dapsone leads to amelioration within few weeks."( Erythema elevatum diutinum: an "idiopathic" case.
Belgith, I; El Fekih, N; Fazaa, B; Kamoun, MR; Remmah, S; Zéglaoui, F; Zermani, R, 2011
)
0.71
"Treatment with dapsone led to the disappearance of cutaneous lesions and pruritus within 48 hours."( Dermatitis herpetiformis: should direct immunofluorescence be the only diagnostic criterion?
Bajanca, R; Cabral, J; Fiadeiro, T; Sousa, L,
)
0.47
"Treatment with dapsone gel in adolescents also resulted in clinically meaningful improvements in acne lesion counts by week 12 in the pivotal studies and for up to 12 months in the long-term safety study."( Efficacy and safety of dapsone gel 5% for the treatment of acne vulgaris in adolescents.
Bourcier, M; Garrett, S; Maloney, JM; Papp, K; Raimer, S; Siegfried, E; Wilson, D, 2008
)
1
"Treatment with dapsone resulted in clearing of the skin in both cases."( [Dimorphous leprosy].
Esca, SA; Zelger, J, 1984
)
0.61
"Treatment with dapsone had no effect on the mycobacterial counts in blood, liver, or spleen, and the combination of dapsone with clarithromycin was no better than clarithromycin as a single agent."( Clarithromycin, dapsone, and a combination of both used to treat or prevent disseminated Mycobacterium avium infection in beige mice.
Bermudez, LE; Inderlied, CB; Kolonoski, P; Petrofsky, M; Young, LS, 1994
)
0.97
"The treatment of dapsone intoxication is intravenous methylene blue for symptomatic methemoglobinemia, gastric decontamination, and early administration of serial oral activated charcoal."( Dapsone intoxication: two case reports.
Challoner, KR; Hansen, DG; Smith, DE,
)
1.9
"Treatment with dapsone resulted in an improvement in the eruption after 2 weeks."( Ofuji's disease with unusual histological features.
Basarab, T; Jones, RR, 1996
)
0.63
"Treatment with dapsone may be beneficial."( Pterygium with granuloma faciale-like histologic picture.
Havelius, U; Rausing, A, 1998
)
0.64
"Treatment with dapsone, 1 mg/kg/24 h, and/or paracetamol and dicloxacillin was successful; one case required surgical treatment."( [Local dermonecrotic loxoscelism in children bitten by the spider Loxosceles reclusa (the "violin" spider)].
Escalante-Flores, I; Escalante-Galindo, P; Montoya-Cabrera, MA; Nava-Juárez, AR; Terroba-Larios, VM,
)
0.47
"Treatment with dapsone was effective for his skin and nails until he developed generalized lymphadenopathy which turned out to be malignant lymphoma."( A case of erythema elevatum diutinum associated with B-cell lymphoma: a rare distribution involving palms, soles and nails.
Futei, Y; Konohana, I, 2000
)
0.65
"Treatment with dapsone cleared the eruption but induced a progressive yet reversible neutropenia."( Linear IgA disease with haemorrhagic pompholyx and dapsone-induced neutropenia.
Charles-Holmes, R; Duhra, P, 1991
)
0.87
"Treatment with dapsone and etretinate was reasonably effective, but etretinate had to be discontinued due to the development of diffuse idiopathic skeletal hyperostosis."( Subcorneal pustular dermatosis and IgA paraproteinaemia: response to both etretinate and PUVA.
Bingham, EA; Burrows, D; Todd, DJ; Walsh, M, 1991
)
0.62
"Treatment with Dapsone resulted in no changes in xenobiotic biotransformation except for the induction of aniline hydroxylation."( [Comparative ability of three aniline derivatives to alter biotransformation enzymes in rat liver].
Wu, K, 1990
)
0.62
"Treatment with dapsone was dramatically successful in our patient whose lesions disappeared in 6 months.(ABSTRACT TRUNCATED AT 250 WORDS)"( [Cicatricial pemphigoid disclosed by superficial desquamative gingivitis. Clinical and immuno-electron microscopic study of a case].
Arbeille, B; de Muret, A; Goga, D; Lorette, G; Prime, A; Vaillant, L, 1990
)
0.62
"4. Treatment with Dapsone resulted in no changes in xenobiotic biotransformation except for the induction of aniline hydroxylation."( Effects of mutagenic and non-mutagenic aniline derivatives on rat liver drug-metabolizing enzymes.
Leslie, CL; Stacey, NH; Wu, K, 1989
)
0.6
"Treatment with dapsone, 50 mg daily, is recommended."( Chronic bullous dermatosis of childhood in Singapore.
Lee, CT; Ratnam, KV; Tan, T,
)
0.47
"Pretreatment with dapsone not only reduced surgical complications but also improved the outcome of patients bitten by the brown recluse spider."( Brown recluse spider bites. A comparison of early surgical excision versus dapsone and delayed surgical excision.
Altenbern, DP; King, LE; Lynch, JB; Rees, RS, 1985
)
0.82

Toxicity

Monotherapy with dapsone gel, 5% administered twice daily was safe and effective for treatment of facial acne in women with SOC. Dapsone-related adverse events were mild and promptly reversed by treatment withdrawal.

ExcerptReferenceRelevance
" The common side effect in all cases consisted of red and dark skin pigmentation of varying intensity occuring within 10 weeks of the commencement of therapy."( Side effects of clofazimine therapy.
Iyer, GG; Ramu, G, 1976
)
0.26
"The development of PCP, transfusion requirements, monthly complete blood cell counts, serious adverse reactions and death were recorded."( Oral dapsone versus nebulized pentamidine for Pneumocystis carinii pneumonia prophylaxis: an open randomized prospective trial to assess efficacy and haematological toxicity.
Hoy, JF; Kent, SJ; Lucas, CR; Pettinger, MB; Slavin, MA; Stewart, K, 1992
)
0.8
" There was no significant difference in the occurrence of serious adverse reactions (six in the dapsone and eight in the pentamidine arm)."( Oral dapsone versus nebulized pentamidine for Pneumocystis carinii pneumonia prophylaxis: an open randomized prospective trial to assess efficacy and haematological toxicity.
Hoy, JF; Kent, SJ; Lucas, CR; Pettinger, MB; Slavin, MA; Stewart, K, 1992
)
1.02
" The 3,3'DDS and MADDT derivatives were both significantly less toxic compared with DDS."( An investigation into the haematological toxicity of structural analogues of dapsone in-vivo and in-vitro.
Coleman, MD; Hussain, F; Park, BK; Storr, RC; Tingle, MD, 1991
)
0.51
" One adverse reaction of chloroquine that has an important bearing on its use is pruritus."( Toxicity and side-effects of antimalarials in Africa: a critical review.
Salako, LA, 1984
)
0.27
" Safe and effective drugs, capable of being administered as a single-dose or short-course treatment, are urgently needed to control the adaptable malaria parasite."( Falciparum malaria: the urgent need for safe and effective drugs.
Rieckmann, KH, 1983
)
0.27
" It is concluded that the combination RMP + ETH is the toxic component."( Hepatotoxicity of the combination of rifampin-ethionamide in the treatment of multibacillary leprosy.
Bourland, J; Davies, EM; Feracci, C; Grillone, S; Janssens, L; Pattyn, SR; Saylan, T, 1984
)
0.27
" Although these could have been engendered by dapsone toxicity, it was thought that a concommitant adverse reaction to rifampicin, which is known to be hepatotoxic, nephrotoxic and possibly capable of predisposing to the dapsone syndrome, could not be excluded."( A fatal case of drug-induced multi-organ damage in a patient with Hansen's disease: dapsone syndrome or rifampicin toxicity?
Lau, G, 1995
)
0.77
" Three of the 20 patients had an adverse reaction to dapsone."( Efficacy and safety of dapsone prophylaxis against Pneumocystis carinii pneumonia in human immunodeficiency virus-infected children.
Noel, GJ; Stavola, JJ, 1993
)
0.85
" For dapsone, among 100 patients given 100 mg daily instead of twice a week for 1 year (primary prophylaxis), seven fewer patients would develop P carinii pneumonia, but 17 more would have significant toxic reactions."( A meta-analysis of the relative efficacy and toxicity of Pneumocystis carinii prophylactic regimens.
Cappelleri, JC; Ioannidis, JP; Lau, J; Sacks, HS; Skolnik, PR, 1996
)
0.81
" Low doses of dapsone reduce toxic effects, but at the expense of some loss of efficacy."( A meta-analysis of the relative efficacy and toxicity of Pneumocystis carinii prophylactic regimens.
Cappelleri, JC; Ioannidis, JP; Lau, J; Sacks, HS; Skolnik, PR, 1996
)
0.65
"The overall incidence of adverse events (AE) in our study cohort was 39%."( Safety of dapsone as Pneumocystis carinii pneumonia prophylaxis in human immunodeficiency virus-infected patients with allergy to trimethoprim/sulfamethoxazole.
Beumont, MG; Graziani, A; MacGregor, RR; Ubel, PA, 1996
)
0.7
"Drug therapies for patients with human immunodeficiency virus (HIV) infection are associated with adverse events that can potentially limit their effectiveness."( Adverse events from drug therapy for human immunodeficiency virus disease.
Chaisson, RE; Fortgang, I; Keruly, J; Moore, RD, 1996
)
0.29
"We calculated specific and overall adverse event rates from use of zidovudine, didanosine, zalcitabine, cotrimoxazole, and dapsone in an observational urban cohort of 1,450 HIV-infected patients with a CD4+ count of 500 cells/mm3 or less."( Adverse events from drug therapy for human immunodeficiency virus disease.
Chaisson, RE; Fortgang, I; Keruly, J; Moore, RD, 1996
)
0.5
"Overall adverse event rates in order of incidence were dapsone, 16."( Adverse events from drug therapy for human immunodeficiency virus disease.
Chaisson, RE; Fortgang, I; Keruly, J; Moore, RD, 1996
)
0.54
" Adverse event rates increase progressively with decline in CD4+ count."( Adverse events from drug therapy for human immunodeficiency virus disease.
Chaisson, RE; Fortgang, I; Keruly, J; Moore, RD, 1996
)
0.29
" Paradoxically, other aspects of the glutathione-dependent cycling of the hydroxylamine metabolite may contribute to the major adverse reaction of the drug, agranulocytosis."( Dapsone toxicity: some current perspectives.
Coleman, MD, 1995
)
1.73
" The adverse reactions associated with the administration of dapsone are believed to be caused by metabolism to its hydroxylamine."( N-Hydroxylation of dapsone by multiple enzymes of cytochrome P450: implications for inhibition of haemotoxicity.
Gill, HJ; Park, BK; Tingle, MD, 1995
)
0.86
" Metabolism was assessed by high-pressure liquid chromatography-mass spectrometry and methemoglobin formation has been used as a toxic endpoint."( Comparison of the metabolism and toxicity of dapsone in rat, mouse and man.
Maggs, JL; Mahmud, R; Park, BK; Pirmohamed, M; Tingle, MD, 1997
)
0.56
"The differential incidence of adverse drug reactions (ADR) between trimethoprim-sulfamethoxazole and dapsone might be explained, in part, by differences in the inherent toxicity of the hydroxylamine metabolites of sulfamethoxazole and dapsone."( Comparison of the in vitro cytotoxicity of hydroxylamine metabolites of sulfamethoxazole and dapsone.
Bellevue, FH; Reilly, TP; Svensson, CK; Woster, PM, 1998
)
0.74
"Alternative independent routes of dapsone metabolism include N-hydroxylation to the hydroxylamine, a potentially toxic metabolite, by cytochrome P450 enzymes and acetylation to a nontoxic metabolite by N-acetyltransferase."( Development of dapsone toxicity in patients with inflammatory dermatoses: activity of acetylation and hydroxylation of dapsone as risk factors.
Adedoyin, A; Bluhm, RE; Branch, RA; McCarver, DG, 1999
)
0.94
" All four were slow acetylators and three were rapid hydroxylators, consistent with the toxic nature of dapsone hydroxylamine."( Development of dapsone toxicity in patients with inflammatory dermatoses: activity of acetylation and hydroxylation of dapsone as risk factors.
Adedoyin, A; Bluhm, RE; Branch, RA; McCarver, DG, 1999
)
0.87
"These observations are consistent with what is known about the toxicity profile of dapsone metabolites and suggest that assessing N-acetylation and N-hydroxylation capacities can help to identify subjects at increased risk of a toxic response."( Development of dapsone toxicity in patients with inflammatory dermatoses: activity of acetylation and hydroxylation of dapsone as risk factors.
Adedoyin, A; Bluhm, RE; Branch, RA; McCarver, DG, 1999
)
0.88
" We conclude that CFZ is a generally well tolerated and safe drug when given as a daily dose of 50mg, which is currently used in leprosy patients."( Biochemical and hematological side effects of clofazimine in leprosy patients.
Costa Queiroz, RH; de Souza, AM; Melchior, E; Sampaio, SV, 2002
)
0.31
"The introduction of multidrug therapy (WHO/MDT)-composed by the drugs dapsone, clofazimine and rifampicin has enabled the cure of Hansen's disease, however, the adverse effects of these drugs were not given priority by the health team."( [Adverse effects of multidrug therapy in leprosy patients: a five-year survey at a Health Center of the Federal University of Uberlândia].
Arbex, GL; Carneiro, MH; Gadia, R; Goulart, IM; Rodrigues, MS,
)
0.37
" The no or low adverse effect levels were in the range of 5 to 7 mg/kg/day artesunate."( Developmental toxicity of artesunate and an artesunate combination in the rat and rabbit.
A Clode, S; Clark, RL; Gaunt, I; Ward, SA; White, TE; Winstanley, P, 2004
)
0.32
"Many adverse drug reactions are caused by the cytochrome P450 (CYP) dependent activation of drugs into reactive metabolites."( An in vitro approach to detect metabolite toxicity due to CYP3A4-dependent bioactivation of xenobiotics.
Grossi, P; Kanter, Rd; Monaci, S; Monshouwer, M; Turlizzi, E; Vignati, L, 2005
)
0.33
" Adverse events were comparable between the treatment groups and rarely led to discontinuation."( Two randomized studies demonstrate the efficacy and safety of dapsone gel, 5% for the treatment of acne vulgaris.
Carter, E; Draelos, ZD; Elewski, B; Garrett, S; Lynde, C; Maloney, JM; Poulin, Y, 2007
)
0.58
" Panniculitis is a rare adverse reaction to mesotherapy that may result from injection pressure, local trauma, or the type of injected substances."( Mesotherapy-induced panniculitis treated with dapsone: case report and review of reported adverse effects of mesotherapy.
Rao, B; Tan, J,
)
0.39
"This case illustrates one of the potential adverse effects of mesotherapy and suggests that dapsone may be effective in the treatment of panniculitis resulting from such injections."( Mesotherapy-induced panniculitis treated with dapsone: case report and review of reported adverse effects of mesotherapy.
Rao, B; Tan, J,
)
0.61
" Common nonapplication site adverse events included headache (20%) and nasopharyngitis (15%)."( Dapsone gel 5% for the treatment of acne vulgaris: safety and efficacy of long-term (1 year) treatment.
Garrett, S; Jones, T; Ling, M; Lucky, AW; Maloney, JM; Roberts, J; Taylor, S, 2007
)
1.78
" The incidence of adverse events, including application-site events, was low and similar between treatment groups in the pivotal studies and was similarly low in the long-term safety study."( Efficacy and safety of dapsone gel 5% for the treatment of acne vulgaris in adolescents.
Bourcier, M; Garrett, S; Maloney, JM; Papp, K; Raimer, S; Siegfried, E; Wilson, D, 2008
)
0.66
" Dapsone-related adverse events were mild and promptly reversed by treatment withdrawal."( Efficacy and safety of dapsone as a second-line treatment in non-splenectomized adults with immune thrombocytopenic purpura.
Annichino-Bizzacchi, JM; De Paula, EV; Fabri, DR; Orsi, FL; Ozelo, MC; Vancine-Califani, SM, 2008
)
1.57
"Results of clinical chemical analysis and hematology values; plasma dapsone and N-acetyl dapsone concentrations; spontaneous reports of adverse events."( Hematologic safety of dapsone gel, 5%, for topical treatment of acne vulgaris.
Jarratt, M; Pariser, D; Piette, WW; Sheth, P; Taylor, S; Wilson, D, 2008
)
0.9
" DHS and other adverse effects of dapsone lead to withdrawal of the drug."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
0.83
"We reviewed the notes of patients who had dapsone withdrawn from their multi-drug therapy (MDT) following an adverse reaction to the drug between 1990 and 2007."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
0.81
"Rifampicin and clofazimine appear to be satisfactory treatment for both paucibacillary and multibacillary patients who have to have dapsone stopped because of severe adverse effects."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
0.75
" For many years scientists explored the possibility of developing a topical formulation of dapsone for the treatment of acne in the hope of minimizing the adverse hematologic effects of oral dapsone."( Dapsone 5% gel: a review of its efficacy and safety in the treatment of acne vulgaris.
Kissling, RF; Shalita, AR; Stotland, M, 2009
)
2.02
" Adverse effects, clinical response (treatment failure) and parasitological response were compared."( A randomized clinical trial comparing safety, clinical and parasitological response to artemether-lumefantrine and chlorproguanil-dapsone in treatment of uncomplicated malaria in pregnancy in Mulago hospital, Uganda.
Kaye, DK; Mutyaba, TS; Ndeezi, G; Nshemerirwe, R, 2008
)
0.55
" The adverse effects were comparable between the two groups."( A randomized clinical trial comparing safety, clinical and parasitological response to artemether-lumefantrine and chlorproguanil-dapsone in treatment of uncomplicated malaria in pregnancy in Mulago hospital, Uganda.
Kaye, DK; Mutyaba, TS; Ndeezi, G; Nshemerirwe, R, 2008
)
0.55
"The most prominent adverse effects seen during treatment with dapsone, an antibacterial and antiprotozoal agent, are hemolysis and methemoglobinemia."( Cytochrome P450-dependent toxicity of dapsone in human erythrocytes.
Ganesan, S; Sahu, R; Tekwani, BL; Walker, LA, 2010
)
0.87
"Dapsone-induced agranulocytosis is a rare but potentially fatal adverse effect of treatment for tuberculoid leprosy."( Total agranulocytosis caused by dapsone therapy for tuberculoid leprosy--an unappreciated serious side effect of anti-leprosy treatment with clinical implications.
De Silva, GV; Jayawardana, MA; Murugathas, S; Riyaaz, AA; Satarasinghe, RL; Wickrmasingha, UD; Wijesinghe, R, 2009
)
2.08
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" The reported adverse events were: mild methemoglobinemia (50%), headache (31."( Safety and tolerability of dapsone for the treatment of patients with drug-resistant, partial-onset seizures: an open-label trial.
Corona, T; Diaz-Ruiz, A; López-Gómez, M; Ríos, C, 2011
)
0.67
"To assess the adverse effects of multi drug therapy (MDT) in leprosy patients."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
0.37
" The adverse effects were recorded on the personal record of every individual patient, filled during the course of treatment."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
0.37
"176 patient's records were analysed, looking for adverse effects."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
0.37
" Its use is associated with a broad spectrum of adverse effects."( Improving adherence to safe prescription guidelines for Dapsone: harnessing an enhanced electronic medical records system and a team approach.
Chan, RK; Choi, C; Leong, HH; Neoh, CY; Tan, AW; Tian, EA, 2012
)
0.63
" This includes the performance of key laboratory tests before and after starting dapsone, ensuring adequate counseling before starting dapsone and screening for adverse effects using a questionnaire every visit."( Improving adherence to safe prescription guidelines for Dapsone: harnessing an enhanced electronic medical records system and a team approach.
Chan, RK; Choi, C; Leong, HH; Neoh, CY; Tan, AW; Tian, EA, 2012
)
0.85
"This system of dapsone prescription efficiently improved the adherence to safe prescription and monitoring guidelines."( Improving adherence to safe prescription guidelines for Dapsone: harnessing an enhanced electronic medical records system and a team approach.
Chan, RK; Choi, C; Leong, HH; Neoh, CY; Tan, AW; Tian, EA, 2012
)
0.98
"This study sought to verify the correlation between leprosy types and the adverse effects of treatment drugs."( Brazilian clinical trial of uniform multidrug therapy for leprosy patients: the correlation between clinical disease types and adverse effects.
Almeida, PC; Bührer-Sékula, S; Cruz, R; Gonçalves, Hde S; Moraes, ME; Penna, GO; Pontes, MA, 2012
)
0.38
" In this context, microencapsulation for pulmonary administration can offer an alternative to increase the bioavailability of dapsone, reducing its adverse effects."( Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation.
Guterres, SS; Jornada, DS; Ortiz, M; Pohlmann, AR, 2015
)
0.86
" Dapsone gel, 5% used twice daily was well tolerated, with no treatment-related adverse events."( The Efficacy and Safety of Topical Dapsone Gel, 5% for the Treatment of Acne Vulgaris in Adult Females With Skin of Color.
Alexis, AF; Burgess, C; Callender, VD; Gallagher, CJ; Herzog, JL; Roberts, WE; Schweiger, ES; Stockton, TC, 2016
)
1.62
"Monotherapy with dapsone gel, 5% administered twice daily was safe and effective for treatment of facial acne in women with SOC."( The Efficacy and Safety of Topical Dapsone Gel, 5% for the Treatment of Acne Vulgaris in Adult Females With Skin of Color.
Alexis, AF; Burgess, C; Callender, VD; Gallagher, CJ; Herzog, JL; Roberts, WE; Schweiger, ES; Stockton, TC, 2016
)
1.05
" Safety profile assessments included adverse events (AEs), physical examinations, laboratory tests, and local tolerability assessments."( Safety and Pharmacokinetics of Once-Daily Dapsone Gel, 7.5% in Patients With Moderate Acne Vulgaris.
Berk, DR; Chang-Lin, JE; Jarratt, MT; Jones, TM; Kaoukhov, A; Lin, V; Tong, W, 2016
)
0.7
" Most of these adverse effects were mild, did not require discontinuation of the medication, and resolved after stopping the medication or decreasing the dose."( The Comparative Safety of Multiple Alternative Agents in Refractory Chronic Urticaria Patients.
Khan, DA; Seth, S,
)
0.13
"The use of alternative agents for the treatment of chronic urticaria angioedema is generally safe when proper laboratory and clinical monitoring is observed."( The Comparative Safety of Multiple Alternative Agents in Refractory Chronic Urticaria Patients.
Khan, DA; Seth, S,
)
0.13
" Efficacy was evaluated using the Global Acne Assessment Score (GAAS), lesion counts, and Acne Symptom and Impact Scale (ASIS); adverse events (AEs) and tolerability were also assessed."( Efficacy, Safety, and Tolerability of Topical Dapsone Gel, 7.5% for Treatment of Acne Vulgaris by Fitzpatrick Skin Phototype.
Alexis, AF; Alvandi, N; Callender, VD; Cook-Bolden, FE; Downie, JB; McMichael, A; Rodriguez, DA; Taylor, SC, 2018
)
0.74
"The Clinical Trial for Uniform Multidrug Therapy for Leprosy Patients in Brazil (U-MDT/CT-BR), designed to evaluate the effectiveness of a six-months regimen, assessed the adverse effects caused by the drugs."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
0.48
"Describe adverse effects due to MDT in U-MDT/CT-BR, comparing the uniform regimen (U-MDT) to the current WHO regimen (R-MDT)."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
0.48
"2%) stopped dapsone intake due to adverse effects, of whom 16."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
0.86
"There was no statistical difference regarding adverse effects in the R-MDT and U-MDT groups but anemia was greater in patients from R-MDT/MB group, therefore adverse effects do not represent a constraint to recommend the six-month uniform regimen of treatment for all leprosy patients."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
0.48
"Dapsone may be used for Pneumocystis jirovecii pneumonia (PJP) prophylaxis in hematology patients receiving immunosuppressive therapy or after hematopoietic stem cell transplant (HSCT) in the setting of trimethoprim-sulfamethoxazole (TMP-SMX) adverse drug reaction (ADR) history."( Dapsone safety in hematology patients: Pathways to optimizing Pneumocystis jirovecii pneumonia prophylaxis in hematology malignancy and transplant recipients.
Pisasale, D; Trubiano, JA; Urbancic, KF; Wight, J, 2018
)
3.37
" Though these drugs are generally well tolerated, they can result in potentially severe adverse effects."( Murphy's law in force: sequential adverse events encountered during the treatment of Pneumocystis pneumonia (cotrimoxazole-induced acute peripheral neuropathy and primaquine-induced methemoglobinemia).
Agarwal, R; Dhooria, S; Muthu, V; Prasad, KT; Saxena, P; Sehgal, IS, 2020
)
0.56
" The aim was to describe the adverse effects of polychemotherapy, as well the most prevalent and most vulnerable populations."( Adverse effects of polychemotherapy for leprosy in 13 years of follow-up at a university hospital.
Brotas, AM; Carneiro, S; Daxbacher, EL; Tortelly, VD,
)
0.13
" A meta-analysis of randomized controlled trials was then conducted to analyze the efficacy and adverse events of dapsone gel treatment compared with excipient and other drug therapies."( Efficacy and safety of dapsone gel for acne: a systematic review and meta-analysis.
Liu, H; Sun, L; Wang, X; Wang, Z; Zhang, F, 2022
)
1.24
" There was no significant difference in the incidence of adverse events between the dapsone group and the control group (OR =0."( Efficacy and safety of dapsone gel for acne: a systematic review and meta-analysis.
Liu, H; Sun, L; Wang, X; Wang, Z; Zhang, F, 2022
)
1.26
"Dapsone gel is effective in treating acne, and there is no significant difference in adverse events compared with other drugs."( Efficacy and safety of dapsone gel for acne: a systematic review and meta-analysis.
Liu, H; Sun, L; Wang, X; Wang, Z; Zhang, F, 2022
)
2.47
" By early 2021, MADDS detected shifts in cocaine purity, alerted communities of a new toxic fentanyl analogue and a synthetic cannabinoid contaminant, and confirmed the increase of xylazine (a veterinary sedative) in Massachusetts."( Implementation and Uptake of the Massachusetts Drug Supply Data Stream: A Statewide Public Health-Public Safety Partnership Drug Checking Program.
Consigli, A; Del Pozo, B; Erowid, E; Erowid, F; Green, TC; Jarczyk, C; Michelson, L; Olson, R; Reilly, B; Ruiz, S; Thyssen, S; Wightman, R,
)
0.13

Pharmacokinetics

100 mg dapsone was administered orally to seven normal adult volunteers. No significant difference was observed in any of the pharmacokinetic parameters with aspirin. Three days after rifampicin the elimination half-life of daps one was reduced from 40.

ExcerptReferenceRelevance
" The elimination half-life of the first order kinetics was, on average, at 20--21 hr for both DDS and MADDS."( The pharmacokinetics of dapsone and acetylated dapsone in serum and saliva.
Kangas, L; Lammintausta, K; Lammintausta, R, 1979
)
0.57
" After the last maintenance dose of Maloprim, the following kinetic parameters (mean values) were determined for DDS and PYR, respectively: maximum plasma concentration (Cmax) = 1,134 and 116 ng ml-1; elimination half-life (t1/2) = 23 and 105 h; plasma clearance (CL) = 37."( Multiple-dose pharmacokinetics and in vitro antimalarial activity of dapsone plus pyrimethamine (Maloprim) in man.
Edstein, MD; Rieckmann, KH; Veenendaal, JR, 1990
)
0.51
" Three days after rifampicin the elimination half-life of dapsone was reduced from 40."( Influence of once-monthly rifampicin and daily clofazimine on the pharmacokinetics of dapsone in leprosy patients in Nigeria.
Pieters, FA; Woonink, F; Zuidema, J, 1988
)
0.74
"05) in the elimination half-life of chloramphenicol was observed before and after dapsone treatment in leprotic patients as compared with the normal volunteers, while no significant difference was observed in any of the pharmacokinetic parameters with aspirin."( Pharmacokinetics of aspirin and chloramphenicol in normal and leprotic patients before and after dapsone therapy.
Bakaya, V; Garg, SK; Kaur, S; Kumar, B; Lal, R; Shukla, VK, 1988
)
0.72
"A comparative pharmacokinetic study of Lositril (rifampicin) was carried out in six multibacillary and twelve paucibacillary leprosy cases."( Effect of clofazimine and dapsone on rifampicin (Lositril) pharmacokinetics in multibacillary and paucibacillary leprosy cases.
Gandhi, IS; Mehta, J; Sane, SB; Wamburkar, MN,
)
0.43
" This may relate to pharmacodynamic differences, but alternatively the concentration of oxidative metabolites rather than DDS or MADDS could be responsible for the therapeutic activity in dermatitis herpetiformis."( Pharmacokinetic observations on dapsone in dermatitis herpetiformis.
Ahmad, RA; Fry, L; Leonard, JN; Rogers, HJ; Swain, AF, 1983
)
0.55
" Plasma dapsone concentrations declined mono-exponentially with time, and the half-life (29."( Acute dapsone poisoning: clinical features and pharmacokinetic studies.
Charlton, B; Henderson, DB; Peaston, RT; Rawlins, MD; Woodhouse, KW, 1983
)
1.18
" This assay was shown to be satisfactory for pharmacokinetic studies."( Pharmacokinetics and protein binding interactions of dapsone and pyrimethamine.
Ahmad, RA; Rogers, HJ, 1980
)
0.51
" However, the suggested dosage regimen is based upon clinical experience with children with leprosy and dermatitis herpetiformis rather than pharmacokinetic and pharmacodynamic data obtained from the target patient population."( Pharmacokinetics of dapsone in human immunodeficiency virus-infected children.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Loy, A; Miletich, F, 1995
)
0.61
" In each study, pharmacokinetic variables were determined using noncompartmental methods and compared by analysis of variance."( Effects of the antacids in didanosine tablets on dapsone pharmacokinetics.
Cameron, DW; Gallicano, K; Garber, G; Oliveras, L; Sahai, J, 1995
)
0.55
" The pharmacokinetics of dapsone and pyrimethamine were examined by using a population pharmacokinetic model."( Pharmacokinetics and safety of weekly dapsone and dapsone plus pyrimethamine for prevention of pneumocystis pneumonia.
Amantea, MA; Byrne, A; Davey, RT; Falloon, J; Graziani, A; Lavelle, J; Morgan, A; Ogata-Arakaki, D; Ownby, K; Polis, M, 1994
)
0.86
" Elimination followed first-order kinetics; the mean elimination half-life was 15."( Pharmacokinetics of dapsone in children.
Breña, A; Clarke, D; Michaels, M; Mirochnick, M; Pelton, S; Regan, AM, 1993
)
0.61
" To examine the pharmacokinetic interactions among these drugs, eight HIV-infected patients (26 to 43 years old) with a mean CD4 count of 524."( Zidovudine, trimethoprim, and dapsone pharmacokinetic interactions in patients with human immunodeficiency virus infection.
Gambertoglio, JG; Lee, BL; Makrides, V; Safrin, S, 1996
)
0.58
" A one-compartment open model with first-order absorption and elimination was used as the structural pharmacokinetic model."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
0.58
" Serial blood samples were obtained over 24 hours after dosing and analyzed for trimetrexate, dapsone, and monoacetyldapsone, and pharmacokinetic parameters were determined."( Pharmacokinetics of trimetrexate and dapsone in AIDS patients with Pneumocystis carinii pneumonia.
Chatterjee, DJ; Dubé, MP; Koda, RT; Li, WY; Sattler, FR; Stansell, JD, 1999
)
0.8
" For the entire population, the median half-life was 22."( Pharmacokinetics of dapsone administered daily and weekly in human immunodeficiency virus-infected children.
Bonagura, VR; Cooper, E; Cunningham, CK; Dankner, W; Frenkel, LM; Jacobus, D; Johnson, D; Lindsey, J; McIntosh, K; McNamara, J; Mirochnick, M; Mofenson, L; Nachman, S; Rathore, MH; Sullivan, JL; Wara, DW; Xu, J, 1999
)
0.63
"Previous studies of dapsone pharmacokinetics in children have been too small to allow assessment of the relationships between dapsone pharmacokinetic parameters and patient characteristics or markers of efficacy and toxicity."( Population pharmacokinetics of dapsone in children with human immunodeficiency virus infection.
Bonagura, VR; Capparelli, E; Cooper, E; Jacobus, D; Lindsey, J; McIntosh, K; Mirochnick, M; Mofenson, L; Nachman, S; Spector, SA; Sullivan, JL; Xu, J; Yogev, R, 2001
)
0.92
"We used population analysis to estimate dapsone pharmacokinetic parameters in children participating in a phase I/II study of daily and weekly dapsone in children with human immunodeficiency virus (HIV) infection."( Population pharmacokinetics of dapsone in children with human immunodeficiency virus infection.
Bonagura, VR; Capparelli, E; Cooper, E; Jacobus, D; Lindsey, J; McIntosh, K; Mirochnick, M; Mofenson, L; Nachman, S; Spector, SA; Sullivan, JL; Xu, J; Yogev, R, 2001
)
0.86
" Dapsone pharmacokinetic parameters were not associated with toxicity, but higher dapsone AUC was associated with decreased risk of PCP."( Population pharmacokinetics of dapsone in children with human immunodeficiency virus infection.
Bonagura, VR; Capparelli, E; Cooper, E; Jacobus, D; Lindsey, J; McIntosh, K; Mirochnick, M; Mofenson, L; Nachman, S; Spector, SA; Sullivan, JL; Xu, J; Yogev, R, 2001
)
1.51
"The population pharmacokinetic parameter estimates for chlorproguanil were ka=00."( Population pharmacokinetic and pharmacodynamic modelling of the antimalarial chemotherapy chlorproguanil/dapsone.
Aarons, L; Bojang, K; Edwards, G; Hughes, D; Manyando, C; Simpson, JA; Ward, S; Watkins, WA; Winstanley, P, 2006
)
0.55
"Plasmodium falciparum malaria has no effect on the pharmacokinetic parameters for chlorproguanil, dapsone or chlorcycloguanil."( Population pharmacokinetic and pharmacodynamic modelling of the antimalarial chemotherapy chlorproguanil/dapsone.
Aarons, L; Bojang, K; Edwards, G; Hughes, D; Manyando, C; Simpson, JA; Ward, S; Watkins, WA; Winstanley, P, 2006
)
0.76
"To report the pharmacokinetic profile of topically applied dapsone gel, 5% in the treatment of acne vulgaris."( Pharmacokinetics of dapsone gel, 5% for the treatment of acne vulgaris.
Garrett, S; Halder, R; Sharata, H; Thiboutot, DM; Willmer, J, 2007
)
0.91
"Three prospective, open-label studies enrolled a total of 548 subjects with acne vulgaris: two phase I pharmacokinetic studies (crossover and drug interaction) and one phase III long-term safety study."( Pharmacokinetics of dapsone gel, 5% for the treatment of acne vulgaris.
Garrett, S; Halder, R; Sharata, H; Thiboutot, DM; Willmer, J, 2007
)
0.66
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Blood samples for pharmacokinetic analysis were collected up to 24 h post-first dose."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.63
"The pharmacokinetic analysis included 115 patients."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.63
"5% formulations, the highest daily exposure of dapsone (per the AUC) was observed with DAP-11080, with respective Cmax and AUC0-24 being approximately 28."( Safety and Pharmacokinetics of Once-Daily Dapsone Gel, 7.5% in Patients With Moderate Acne Vulgaris.
Berk, DR; Chang-Lin, JE; Jarratt, MT; Jones, TM; Kaoukhov, A; Lin, V; Tong, W, 2016
)
0.96
" On theoretical grounds we provide computed evidence why dapsone is not a pharmacodynamic lead for drug profiling because enthalpic terms do not change significantly at the moment of ligand binding to target."( Dapsone is not a Pharmacodynamic Lead Compound for its Aryl Derivatives.
Abdallah, HH; Laufer, S; Salvador-Atonal, K; Scior, T, 2020
)
2.25

Compound-Compound Interactions

Pyrimethamine in combination with a fixed concentration of dapsone at 0.5% reduced the mean number of inflammatory lesions. The anti-Mycobacterium leprae activity of the newly developed benzoxazinorifamycin was superior to that of the TMP combination with sulfamethoxazole (SMZ)

ExcerptReferenceRelevance
"The efficacy of dapsone alone or combined with pyrimethamine against Toxoplasma gondii was investigated experimentally."( Anti-Toxoplasma effects of dapsone alone and combined with pyrimethamine.
Chastang, C; Chau, F; Derouin, F; Piketty, C; Pocidalo, JJ; Rouveix, B, 1991
)
0.92
"The antibacterial effect of brodimoprim alone and in combination with dapsone has been studied in vitro in cell-free systems and in whole mycobacterial cells as well as in vivo in mice and humans."( In vitro and in vivo experiments with the new inhibitor of mycobacterium leprae brodimoprim alone and in combination with dapsone.
Dhople, AM; Jagannathan, R; Mahadevan, PR; Rosenfeld, M; Seydel, JK; Wempe, EG, 1990
)
0.72
"Blood induced Plasmodium berghei infection in Swiss mice was exposed during successive passages to melfloquine alone or melfoquine in combination with dapsone or primaquine or erythromycin, and the level of resistance to melfoquine in four sub-lines was compared at ED90 level."( Delay in emergence of mefloquine resistance in Plasmodium berghei by use of drug combinations.
Dutta, GP; Puri, SK, 1989
)
0.48
"Bacterial growth kinetics and checkerboard titration experiments have been performed to determine the inhibitory power of metioprim (I) and brodimoprim (II) alone and in combination with diaminodiphenylsulfone (DDS) using Escherichia coli and mycobacteria as test organisms."( Bacterial growth kinetics of Escherichia coli and mycobacteria in the presence of brodimoprim and metioprim alone and in combination with sulfamerazine and dapsone (VI).
Rosenfeld, M; Seydel, JK; Wempe, EG, 1983
)
0.46
"The prophylactic efficacies of atovaquone (ATQ) alone and in combination with azithromycin, clarithromycin, rifabutin, proguanil, PS-15, trimethoprim, co-trimoxazole, or dapsone were investigated in a SCID mouse model of Pneumocystis carinii pneumonia (PCP)."( Effect of atovaquone and atovaquone drug combinations on prophylaxis of Pneumocystis carinii pneumonia in SCID mice.
Comley, JC; Sterling, AM, 1995
)
0.49
"The potency of antimalarial dihydrofolate reductase inhibitors, alone and in synergistic combination with dihydropteroate synthetase inhibitors, against the Kenyan K39 strain of Plasmodium falciparum (pyrimethamine resistant) and against normal replicating human bone marrow cells in in vitro culture has been studied."( In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs.
Breckenridge, AM; Mberu, EK; Szwandt, IS; Watkins, WM; Winstanley, PA, 1995
)
0.29
"We examined the effect of epiroprim (Ro 11-8958), a dihydrofolate reductase inhibitor, alone and in combination with dapsone, against Toxoplasma gondii."( Activity of epiroprim (Ro 11-8958), a dihydrofolate reductase inhibitor, alone and in combination with dapsone against Toxoplasma gondii.
Arsenijevic, D; Chang, HR; Comte, R; Pechère, JC; Polak, A; Then, RL, 1994
)
0.71
" Its optimal dosage appears to be 400 mg daily, and combination with dapsone and clofazimine does not enhance its activity."( Clinical trial of ofloxacin alone and in combination with dapsone plus clofazimine for treatment of lepromatous leprosy.
Grosset, JH; Ji, B; N'Deli, L; Perani, EG; Petinom, C, 1994
)
0.77
"5 micrograms/ml dapsone significantly inhibited growth of MAC bacteria when used in combination with other drugs specifically acting at the mycobacterial cell-wall level."( Activity of subinhibitory concentrations of dapsone alone and in combination with cell-wall inhibitors against Mycobacterium avium complex organisms.
Goh, KS; Labrousse, V; Rastogi, N, 1993
)
0.89
"In this study, the in vitro and in vivo anti-Mycobacterium leprae activity of the newly developed benzoxazinorifamycin, KRM-1648, in combination with clofazimine (CFZ) or dapsone (DDS) was evaluated."( Therapeutic efficacy of benzoxazinorifamycin, KRM-1648, in combination with other antimicrobials against Mycobacterium leprae infection induced in nude mice.
Dekio, S; Saito, H; Sato, K; Tomioka, H, 1994
)
0.48
"In The Gambia, insecticide impregnation of bed nets, used alone or combined with Maloprim, reduced morbidity and mortality from malaria amongst children between one and 4 years of age."( A malaria control trial using insecticide-treated bed nets and targeted chemoprophylaxis in a rural area of The Gambia, west Africa. 8. Cost-effectiveness of bed net impregnation alone or combined with chemoprophylaxis in preventing mortality and morbidit
Aikins, M; Alonso, PL; Armstrong Schellenberg, JR; Greenwood, BM; Mills, A; Picard, J, 1993
)
0.29
"In MRC-5 cell cultures, the efficacy of the acyclic nucleoside ganciclovir (GCV) against human cytomegalovirus (CMV) was unaffected when combined with either amphotericin B (AMP B), ketoconazole (KCZ), dapsone (DAP), or trimethoprim/sulfamethoxazole (TMP/SMX)."( Efficacy of ganciclovir in combination with other antimicrobial agents against cytomegalovirus in vitro and in vivo.
Fraser-Smith, EB; Freitas, VR; Matthews, TR, 1993
)
0.47
" Its combination with dapsone (DDS) was synergistic and showed as in vitro activity superior to that of the TMP combination with sulfamethoxazole (SMZ)."( Antibacterial activities of epiroprim, a new dihydrofolate reductase inhibitor, alone and in combination with dapsone.
Angehrn, P; Hartman, PG; Locher, HH; Schlunegger, H; Then, RL, 1996
)
0.82
"The anticryptosporidial activity of four macrolides alone and in combination with other antimicrobial agents was investigated against ten clinical isolates of Cryptosporidium parvum recovered from stools of AIDS patients."( In-vitro activity of macrolides alone and in combination with artemisin, atovaquone, dapsone, minocycline or pyrimethamine against Cryptosporidium parvum.
Cirioni, O; Giacometti, A; Scalise, G, 1996
)
0.52
" The in vitro activities of WR99210 alone and in combination with a fixed concentration of dapsone (0."( Enhanced in vitro activity of WR99210 in combination with dapsone against Mycobacterium avium complex.
Cynamon, MH; DeStefano, MS; Shah, LM, 1996
)
0.76
"In the present study, we evaluated the in vivo anti-Mycobacterium leprae activities of KRM-1648 (KRM) given at long intervals in combination with ofloxacin (OFLX), clofazimine (CFZ), and dapsone (DDS)."( Studies on therapeutic activity of benzoxazinorifamycin KRM-1648 in combination with other antimicrobial agents and biological response modifiers interferon-gamma and granulocyte-macrophage colony-stimulating factor against M. leprae infection in athymic
Maw, WW; Saito, H; Sato, K; Tomioka, H, 1997
)
0.49
"The antimicrobial effects of a new dihydrofolate reductase inhibitor, epiroprim, alone and in combination with dapsone and brodimoprim against Mycobacterium leprae were evaluated in vitro in cell-free culture system."( In vitro activity of epiroprim, a dihydrofolate reductase inhibitor, singly and in combination with brodimoprim and dapsone, against Mycobacterium leprae.
Dhople, AM, 1999
)
0.72
"The antimicrobial effects of a new dihydrofolate reductase inhibitor, epiroprim, either singly or in combination with dapsone against Mycobacterium leprae, were evaluated in vivo using a mouse footpad model."( In vivo activity of epiroprim, a dihydrofolate reductase inhibitor, singly and in combination with dapsone, against Mycobacterium leprae.
Dhople, AM, 2002
)
0.74
" Further studies are now required to determine whether DDS, CPG or an as-yet unidentified metabolite of CPG interact with ASN, and whether a simple double combination of ASN with one or other of these would be as protective, against the selection of resistance, as CDA."( The chemotherapy of rodent malaria. LXIII. Drug combinations to impede the selection of drug resistance, part 6: the potential value of chlorproguanil and dapsone in combination, and with the addition of artesunate.
Peters, W; Robinson, BL; Stewart, LB, 2005
)
0.53
"By week 12, dapsone gel combined with any of the three additional treatments reduced the mean number of inflammatory lesions."( Dapsone gel 5% in combination with adapalene gel 0.1%, benzoyl peroxide gel 4% or moisturizer for the treatment of acne vulgaris: a 12-week, randomized, double-blind study.
Abramovits, W; Eichenfield, LF; Fleischer, AB; Garrett, S; Lucky, A; Shalita, A, 2010
)
2.18
"Dapsone gel in combination with adapalene gel or benzoyl peroxide gel is safe and well tolerated for the treatment of acne vulgaris."( Dapsone gel 5% in combination with adapalene gel 0.1%, benzoyl peroxide gel 4% or moisturizer for the treatment of acne vulgaris: a 12-week, randomized, double-blind study.
Abramovits, W; Eichenfield, LF; Fleischer, AB; Garrett, S; Lucky, A; Shalita, A, 2010
)
3.25
" The results suggest that anti-inflammatory agents such as dapsone can effectively treat early stages of acne (both comedonal and noncomedonal) when used in combination with a retinoid."( Clinical evidence for the role of a topical anti-inflammatory agent in comedonal acne: findings from a randomized study of dapsone gel 5% in combination with tazarotene cream 0.1% in patients with acne vulgaris.
Dhawan, S; Downie, J; Draelos, Z; Germain, MA; Green, L; Kasteler, JS; Kircik, L; Ling, M; Oefelein, MG; Tanghetti, E, 2011
)
0.82
" This study is aimed to evaluate the ability of DDS, alone or in combination with DZP starting their administration once the SE is onset to evaluate the control of seizures in rats."( Efficacy of dapsone administered alone or in combination with diazepam to inhibit status epilepticus in rats.
Baron-Flores, V; Caballero-Chacón, S; Díaz-Ruiz, A; Farfán-Briseño, AC; Franco-Pérez, J; Manjarrez-Marmolejo, J; Méndez-Armenta, M; Nava-Ruiz, C; Ríos, C; Ruiz-Diaz, A, 2019
)
0.89
" In this in vitro study, we evaluated the effectiveness of dapsone individually and in combination with cefuroxime and/or other antibiotics with intracellular activity including doxycycline, rifampin, and azithromycin against Borrelia biofilm forms utilizing crystal violet biofilm mass, and dimethyl methylene blue glycosaminoglycan assays combined with Live/Dead fluorescent microscopy analyses."( Effect of dapsone alone and in combination with intracellular antibiotics against the biofilm form of B. burgdorferi.
Freeman, PR; Gaur, G; Horowitz, RI; Murali, K; Sapi, E, 2020
)
1.2

Bioavailability

The low solubility of dapsone in water results in low bioavailability and high microbial resistance. Microencapsulation for pulmonary administration can offer an alternative to increase the bioavailability, reducing its adverse effects.

ExcerptReferenceRelevance
"001) serum concentrations of PYR were found in Papua New Guineans than in Caucasians at both sampling times, an observation which may reflect differences in the bioavailability of PYR between the two racial groups."( Race-linked differences in serum concentrations of dapsone, monoacetyldapsone and pyrimethamine during malaria prophylaxis.
Cochrane, JP; Cook, IF; Edstein, MD, 1986
)
0.52
"The absolute oral bioavailability of dapsone (DDS) was established in dogs and healthy volunteers by comparing AUC's after oral and intravenous administration."( The absolute oral bioavailability of dapsone in dogs and humans.
Pieters, FA; Zuidema, J, 1987
)
0.82
" Chronic treatment with dapsone does not appear to reduce the bioavailability of NET or EE."( Norethisterone and ethinyl estradiol kinetics during dapsone therapy.
Bhatki, S; Joshi, JV; Joshi, UM; Maitra, A; Sankolli, G, 1984
)
0.82
" dapsone, nimesulide and sulphapyridine, have the potential to reduce the bioavailability of neutrophil-derived HOCl and, in turn, to favour the alpha 1-antitrypsin-dependent control of neutrophil elastolytic activity."( Sulphonamides as anti-inflammatory agents: old drugs for new therapeutic strategies in neutrophilic inflammation?
Balbi, A; Bevilacqua, M; Dallegri, F; Dapino, P; Ottonello, L; Scirocco, MC, 1995
)
1.2
" Rifampin was found to increase the values of clearance/bioavailability (CL/F) and volume of distribution/ bioavailability (V/F) by approximately 70%."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
0.58
" Bioavailability was calculated at 78% after oral dosing and <1% after dermal application."( Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone.
Bethem, RA; Buonarati, MH; Helton, DR; Osborne, DW; Pierson, SK, 2000
)
0.53
"66 for the absorption rate constant."( Population pharmacokinetics of dapsone in children with human immunodeficiency virus infection.
Bonagura, VR; Capparelli, E; Cooper, E; Jacobus, D; Lindsey, J; McIntosh, K; Mirochnick, M; Mofenson, L; Nachman, S; Spector, SA; Sullivan, JL; Xu, J; Yogev, R, 2001
)
0.6
"To investigate the effect of histamine2 (H2)-receptor antagonist-induced elevation of gastric pH on oral bioavailability of a single dose of dapsone 100 mg."( Lack of effect of nizatidine-induced elevation of gastric pH on the oral bioavailability of dapsone in healthy volunteers.
Danziger, LH; Fischer, JH; Hariharan, R; Itokazu, GS; Manitpisitkul, P, 2002
)
0.74
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance."( Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies.
Cabral, LM; Castro, HC; da Silva, JH; de Sousa, VP; do Amaral, LH; do Carmo, FA; Lione, VF; Monteiro, LM; Nasciutti, LE; Rodrigues, CR, 2012
)
0.88
" There are several potential mechanisms by which histone deacetylase inhibition may alter dapsone metabolism including changes in hepatic acetylation or N-glucuronidation leading to an increase in the bioavailability of dapsone's hematotoxic metabolites."( Hemolytic anemia in two patients with glioblastoma multiforme: A possible interaction between vorinostat and dapsone.
Harmon, M; Lesser, GJ; Lewis, JA; Owen, J; Peacock, JE; Petty, WJ; Pirmohamed, M; Valente, K, 2015
)
0.85
" In this context, microencapsulation for pulmonary administration can offer an alternative to increase the bioavailability of dapsone, reducing its adverse effects."( Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation.
Guterres, SS; Jornada, DS; Ortiz, M; Pohlmann, AR, 2015
)
0.86
" However, its low bioavailability and non-specific distribution in the body leads to absorption throughout organs including skin, liver, and kidneys that can cause serious side effects."( Designing dapsone polymer conjugates for controlled drug delivery.
Deb, S; Fernandez-Gutierrez, M; Rojo, L; San Roman, J; Stevens, MM, 2015
)
0.82
"The low bioavailability and nonspecific distribution of dapsone and clofazimine, commonly applied in combination for the treatment of leprosy, can produce toxic effects."( Chromatographic method for the simultaneous quantification of dapsone and clofazimine in nanoformulations.
Barreiros, L; Chaves, LL; Fernandes, SR; Lima, SAC; Machado, S; Reis, S; Segundo, MA; Silva, EMP, 2018
)
0.97
"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
"Poor solubility and low dissolution rate of pharmaceuticals in many cases largely limit their bioavailability and efficacy."( Eutectics and Salt of Dapsone With Hydroxybenzoic Acids: Binary Phase Diagrams, Characterization and Evaluation.
Gong, J; Jia, L; Li, W; Shi, P; Sun, B; Tang, W; Zhang, M; Zhao, Y, 2020
)
0.87

Dosage Studied

Dapsone prophylaxis at this dosage is associated with significantly higher rates of PCP than is TMP-SMZ after allogeneic marrow transplantation. Dapsone was, however, too toxic for humans (because of the excess dosage which was administered at that time) and was considered to be of no value in the treatment of common bacterial infections.

ExcerptRelevanceReference
" Low dosage favoured the appearance of resistance; therefore regular treatment of lepromatous leprosy with dapsone in full dosage is recommended."( Sulphone resistance in leprosy. A review of one hundred proven clinical cases.
Pearson, JM; Rees, RJ; Waters, MF, 1975
)
0.47
" The statistically significant difference between the two treatment groups indicates that, contrary to previous teaching, dapsone given in higher dosage does not predispose patients to reversal reactions and indeed may prevent them."( Evidence for prevention of borderline leprosy reactions by dapsone.
Barnetson, RS; Pearson, JM; Rees, RJ, 1976
)
0.71
" The dosage of Dapsone needed to control the sin lesions could be reduced by more than 50% in 4 patients and the Dapsone could be stopped in 5 other patients on GFD."( The immunoglobulin-bearing cells in the lamina propria and the clinical response to a gluten-free diet in dermatitis herpetiformis.
Lindeman, J; Peña, AS; van der Harst-Oostveen, CJ; van Vloten, WA; Vermeer, BJ, 1977
)
0.61
" A permanent trachestomy was placed, azathioprine, 150 mg daily, was given and prednisone dosage was tapered to 25 mg daily when the patient subsequently was hospitalized for colapsed airway and Cushing's syndrome."( Relapsing polychondritis in a Latin American man.
Raebel, MA; Waller, ES, 1979
)
0.26
" The initial dosage of either of the drugs was 300 mg daily administered in divided doses of 100 mg three times a day."( Treatment of steroid dependant cases of recurrent lepra reaction with a combination of thalidomide and clofazimine.
Girdhar, A; Ramu, G, 1979
)
0.26
"A high-performance liquid chromatographic method was developed to enable dapsone, monoacetyl dapsone and pyrimethamine to be measured simultaneously in plasma samples from volunteers in England and Malaysia who had been dosed with Maloprim."( Determination of plasma concentrations of dapsone, monoacetyl dapsone and pyrimethamine in human subjects dosed with maloprim.
Jones, CR; Ovenell, SM, 1979
)
0.76
" The subjects of this study were receiving dapsone at the daily dosage of 25, 50 and 100 mg or bi-weekly dosage of 25, 50, 75, 100 and 200 mgs."( Monitoring self administration of dapsone by patients.
Balakrishnan, S, 1977
)
0.8
" It was found that Dapsone administered orally as a single dose once a week was therapeutically effective in most of the patients, and improvement, clinical or bacteriological, was directly related to the duration of treatment, irrespective of the dosage of Dapsone."( A comparison of low and conventional dosages of dapsone in the treatment of lepromatous leprosy.
Balakrishnan, S; Iyer, CG; Ramu, G, 1977
)
0.84
" After 24 weeks of treatment, the patients were randomly allocated to treatment either with 200 mg B663 daily 6 days per week (regimen 6) or with dapsone, beginning with a small dosage and increasing over a period of 8 weeks to 100 mg daily 6 days per week (regimen 7)."( Spaced clofazimine therapy of lepromatous leprosy.
, 1976
)
0.46
"A description of the clinical and biochemical course is given for a patient who developed haemolysis and methaemoglobinaemia following dapsone therapy in high dosage for 2 weeks."( High dose dapsone toxicity.
Goldwein, MI; Shelley, WB, 1976
)
0.86
" The Urine D/C ratio was estimated in 35 patients who were receiving a supervised daily dosage of either 50 or 100 mgs of DDS."( An evaluation of the self administration of DDS in Gudiyatham Taluk.
Chacko, CJ; George, B; Jesudasan, K; Job, CK; Kurian, PV; Taylor, PM, 1976
)
0.26
"84 patients of leprosy including 15 female patients were treated with Clofzimine on a predetermined dosage regimen."( Side effects of clofazimine therapy.
Iyer, GG; Ramu, G, 1976
)
0.26
" We conclude that cirrhosis is associated with minor changes in dapsone disposition and that dosage modification is not required."( The disposition of dapsone in cirrhosis.
Arns, PA; Branch, RA; Fleming, CM; May, DG; Porter, J; Richards, WO; Ryder, D; Wilkinson, GR, 1992
)
0.85
"The ratio of metabolite to parent dapsone concentrations at 3 hours after dosing has been used as a marker of acetylator phenotypes."( Reassessment of dapsone as a marker of acetylator phenotypes.
Dennis, S; Luke, DR; Reele, SB; Wiggan, EB, 1991
)
0.91
" carinii in vitro, a clinical trial of reduced dosage of dapsone given prophylactically to human beings is suggested."( Dapsone in low doses prevents Pneumocystis carinii pneumonia in the rat model.
González-Ruiz, A; Haworth, SJ; O'Neil, AB; Warhurst, DC, 1991
)
1.97
" Dosage data indicated that fatalities had taken higher doses and continued prophylaxis after onset of symptoms."( Serious adverse drug reactions to pyrimethamine-sulphadoxine, pyrimethamine-dapsone and to amodiaquine in Britain.
Phillips-Howard, PA; West, LJ, 1990
)
0.51
" These preliminary results indicate that MDT is effective in treatment of paucibacillary leprosy, and also that clinical cure can be achieved in much shorter duration, particularly with higher dosage of rifampicin."( Multidrug therapy for treatment of paucibacillary leprosy in western Kenya--preliminary communications.
Makokha, S; Nyawalo, J; Obura, M; Okelo, C; Okuku, P; Orege, PA, 1990
)
0.28
"A controlled-release dosage form was manufactured by dispersing ethyl cellulose sol in acetone into a medium of mineral oil."( Design and in vitro evaluation of dapsone-loaded micropellets of ethyl cellulose.
Das, SK; Gupta, BK; Pal, M; Roy, S, 1989
)
0.56
"The currently recommended dosage regimen for methylene blue (intermittent bolus dose) in the treatment of methaemoglobinaemia caused by dapsone is often inadequate."( Management of dapsone poisoning complicated by methaemoglobinaemia.
Dawson, AH; Whyte, IM,
)
0.69
" Nineteen patients had ocular manifestations of giant cell arteritis always from the onset, except for a fall in visual acuity; 26 relapses were observed in 18 patients, either during reduction of steroid dosage (21 cases) or after withdrawal (5 cases)."( [Prognosis of treated temporal arteritis. Retrospective study of 87 cases].
Alcalay, M; Becq-Giraudon, B; Boissonnot, L; Bontoux, D; Gil, R; Gouet, D; Le Berre, D; Lefevre, JP; Maréchaud, R; Risse, JF, 1986
)
0.27
" Intravenous TMP-SMX was begun at a dosage of 18 mg/kg/day of trimethoprim."( Treatment of Pneumocystis carinii pneumonia in patients with AIDS.
Hauptman, SP; Wordell, CJ, 1988
)
0.27
" A dose-response (20 mg, 40 mg, or 80 mg/kg/day for 2 weeks) analysis was done with a separate set of mice using a micronucleus test (MNT)."( Cytogenetic effect of dapsone, an antileprotic drug, in the mouse in vivo system.
Das, RK; Roy, B, 1988
)
0.59
" Seventy percent to 100% of patients who begin a strict gluten-free diet have been shown to be able to decrease the dosage of medication needed to control their DH after a mean of eight to 18 months on the diet."( Dietary management of dermatitis herpetiformis.
Hall, RP, 1987
)
0.27
" ENL was also more frequent in regimens C and D and was not prevented by CLO in the dosage used."( Prospective study on the relationship between intensive bactericidal therapy and leprosy reactions.
Coussens, L; Groenen, G; Janssens, L; Kayembe, T; Nollet, E; Pattyn, SR, 1986
)
0.27
"Twenty-one cases of agranulocytosis following dosage with one tablet of Maloprim given once or twice weekly are reviewed."( Agranulocytosis associated with maloprim: review of cases.
Farquhar, JA; Hutchinson, DB; Whiteman, PD, 1986
)
0.27
" A daily dosage of 75 to 100 mg would seem to provide a good compromise between the anti-inflammatory and haemolytic effects."( [Disulon in the treatment of Horton's disease. Experience with 20 patients].
Bonnetblanc, JM; Bordessoule, D; Liozon, F; Loustaud, V; Michel, JP; Vidal, E; Weinbreck, P, 1986
)
0.27
"20 patients with dermatitis herpetiformis maintained on once daily dosing of dapsone were studied to investigate the pharmacodynamics of dapsone in suppressing clinical disease."( The relationship between dapsone dose, serum concentration and disease severity in dermatitis herpetiformis.
Sanders, SW; Zone, JJ, 1986
)
0.8
" We studied the dose-response effect of DDS (10-1 mM) on the generation of oxygen intermediates (OI:O2-, H2O2, OH."( Dissociation of the inhibitory effect of dapsone on the generation of oxygen intermediates--in comparison with that of colchicine and various scavengers.
Miyachi, Y; Niwa, Y; Sakane, T, 1984
)
0.53
" Clinical characteristics of dapsone-induced neuropathy include a motor neuropathy affecting the extremities, usual onset within five years after the initiation of dapsone therapy, dapsone dosage usually equal to or greater than 300 mg/day, and, almost always, complete recovery from the neuropathy after dapsone-dose reduction or withdrawal."( Dapsone-induced peripheral neuropathy. Case report and review.
Siegle, RJ; Voorhees, JJ; Waldinger, TP; Weber, W, 1984
)
2
"The purpose of this study was to identify new drugs for the prevention and treatment of Pneumocystis carinii pneumonitis (PCP) induced in rats by continuous daily dosage with dexamethasone."( Efficacy of diaminodiphenylsulfone and other drugs in murine Pneumocystis carinii pneumonitis.
Hughes, WT; Smith, BL, 1984
)
0.27
" He did not improve until the prednisone dosage was increased to 4 mg per kg per day."( Cicatricial pemphigoid in a 6-year-old child: report of a case and review of the literature.
Esterly, NB; Gerson, CR; Greenwald, MJ; Rosenbaum, MM, 1984
)
0.27
"Exfoliative dermatitis associated with hepatitis has been reported in leprosy patients taking dapsone in daily dosage of 200 mg daily or more previously."( Sulphone induced exfoliative dermatitis and hepatitis.
Garg, BR; Lal, S, 1980
)
0.48
" To control ENL, they required high dosage of clofazimine and steroids for prolonged periods."( Oral zinc in recurrent Erythema Nodosum Leprosum reaction.
Bumb, RA; Mangal, HN; Mathur, NK, 1983
)
0.27
" No association was found between the incidence of DDS-resistant infection on the one hand and either the regularity or the initial dosage of DDS treatment on the other."( DDS-resistant infection among leprosy patients in the population of Gudiyatham Taluk, South India. Part 3. Prevalence, incidence, risk factors, and interpretation of mouse foot pad test results.
Almeida, JG; Chacko, CJ; Christian, M; Fritschi, EP; Taylor, PM, 1983
)
0.27
" However, the disease progressed despite relatively high dose steroid therapy, complications of which contraindicated increasing the dosage and even necessitated rapid withdrawal of steroids."( [Role of dapsone in the treatment of Horton's disease and polymyalgia rheumatica].
Celton, H; Doury, P; Eulry, F; Fabresse, FX; Larroque, P; Pattin, S, 1984
)
0.68
" Due to these encouraging results, the dosage and formulation will be further optimized."( Intramuscular injection of dapsone in therapy for leprosy: a new approach.
Huikeshoven, H; Leiker, DL; Merkus, FW; Modderman, ES; Zuidema, J, 1982
)
0.56
"To determine whether or not low dosage prothionamide (PTH), with or without diamino diphenyl sulphone (DDS), can replace PAS or thiacetazone as the companion drug to isoniazid (INH) in the treatment of tuberculosis, two experiments have been performed in mice."( The role of low dosage prothionamide with and without 4,4'-diamino diphenyl sulphone for use with isoniazid in the treatment of experimental mouse tuberculosis.
Boval, C; Grosset, J; Truffot, C, 1982
)
0.26
"A case of Dapsone poisoning, treated by repetitive dosing with activated charcoal, is reported."( Repetitive doses of activated charcoal in Dapsone poisoning in a child.
Lindsey, JM; Reigart, JR; Trammel, HL, 1982
)
0.93
" Although the sera varied in potency, they showed similar dose-response curves when tested against lymphocytes from a single donor."( Serum inhibitory factor in lepromatous leprosy: its effect on the pre-S-phase cell-cycle kinetics of mitogen-stimulated normal human lymphocytes.
Beck, JS; Brown, RA; Gibbs, JH; Potts, RC; Robertson, AJ; Sherif, MM, 1981
)
0.26
" However, the suggested dosage regimen is based upon clinical experience with children with leprosy and dermatitis herpetiformis rather than pharmacokinetic and pharmacodynamic data obtained from the target patient population."( Pharmacokinetics of dapsone in human immunodeficiency virus-infected children.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Loy, A; Miletich, F, 1995
)
0.61
" ATQ drug combinations affected the prophylactic efficacy of a subcurative dosage of ATQ (50 mg/kg/day given orally) in the following ways: dapsone (25 mg/kg/day) or co-trimoxazole (25 mg of sulfamethoxazole plus 5 mg of trimethoprim per kg/day) had no significant effect on ATQ, azithromycin (200 mg/kg/day) or clarithromycin (200 mg/kg/day) had a slight additive effect with ATQ, trimethoprim (100 mg/kg/day) or PS-15 (5 mg/kg/day) had an additive effect with ATQ, and proguanil (25 mg/kg/day) or rifabutin (200 mg/kg/day) had a marked synergistic effect on ATQ."( Effect of atovaquone and atovaquone drug combinations on prophylaxis of Pneumocystis carinii pneumonia in SCID mice.
Comley, JC; Sterling, AM, 1995
)
0.49
" Its optimal dosage appears to be 400 mg daily, and combination with dapsone and clofazimine does not enhance its activity."( Clinical trial of ofloxacin alone and in combination with dapsone plus clofazimine for treatment of lepromatous leprosy.
Grosset, JH; Ji, B; N'Deli, L; Perani, EG; Petinom, C, 1994
)
0.77
" We describe 3 such patients, and our experience in tapering their steroid dosage with the use of dapsone or methotrexate."( Steroid-sparing medications in temporal arteritis--report of three cases and review of 174 reported patients.
Nesher, G; Sonnenblick, M, 1994
)
0.51
" Ro 11-8958, TMP, and diaveridine used at a dosage of 20 mg/kg/day with SMX were only slightly more effective than SMX used alone."( Synergistic combinations of Ro 11-8958 and other dihydrofolate reductase inhibitors with sulfamethoxazole and dapsone for therapy of experimental pneumocystosis.
Foy, J; Steele, P; Walzer, PD; White, M, 1993
)
0.5
" Once the patient's liver function normalized, prednisone dosage was reduced by 5 mg weekly."( Dapsone hypersensitivity syndrome.
Prussick, R; Shear, NH, 1996
)
1.74
"The population pharmacokinetics of dapsone were examined in human immunodeficiency virus-infected patients receiving dapsone at a dosage of 100 mg twice weekly for the prevention of Pneumocystis carinii pneumonia."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
0.86
" Six patients had received oral dapsone for at least 1 month at the dosage regimen of 100 mg twice of three times weekly and four patients had received a single oral 100 mg dose."( Penetration of dapsone into cerebrospinal fluid of patients with AIDS.
Bassetti, M; Cruciani, M; Gatti, G; Hossein, J; Malena, M, 1997
)
0.93
" Routinely determining human acetylate phenotype status might be helpful in adjusting and modifying dapsone dosage regimen."( Relationship between high incidence of adverse dapsone reactions and slow acetylate phenotype or low plasma/lymphocyte glutathione level.
Guo, R; Lauterberg, B; Thormann, W, 1996
)
0.77
" Dosing or frequency of TMP-SMX did not seem to influence risk of chemoprophylaxis failure."( Pneumocystis carinii pneumonia incidence and chemoprophylaxis failure in ambulatory HIV-infected patients. HIV Outpatient Study (HOPS) Investigators.
Holmberg, SD; Moorman, AC; Palella, FJ; Von Bargen, JC, 1998
)
0.3
" Serial blood samples were obtained over 24 hours after dosing and analyzed for trimetrexate, dapsone, and monoacetyldapsone, and pharmacokinetic parameters were determined."( Pharmacokinetics of trimetrexate and dapsone in AIDS patients with Pneumocystis carinii pneumonia.
Chatterjee, DJ; Dubé, MP; Koda, RT; Li, WY; Sattler, FR; Stansell, JD, 1999
)
0.8
" 3 to 12 years) receiving a new proprietary liquid preparation by three dosing regimens (1 mg/kg of body weight daily, 2 mg/kg daily, or 4 mg/kg weekly)."( Pharmacokinetics of dapsone administered daily and weekly in human immunodeficiency virus-infected children.
Bonagura, VR; Cooper, E; Cunningham, CK; Dankner, W; Frenkel, LM; Jacobus, D; Johnson, D; Lindsey, J; McIntosh, K; McNamara, J; Mirochnick, M; Mofenson, L; Nachman, S; Rathore, MH; Sullivan, JL; Wara, DW; Xu, J, 1999
)
0.63
" Further studies are required to establish its role and the optimal dosage regimen of charcoal to be administered."( Position statement and practice guidelines on the use of multi-dose activated charcoal in the treatment of acute poisoning. American Academy of Clinical Toxicology; European Association of Poisons Centres and Clinical Toxicologists.
, 1999
)
0.3
" Dapsone prophylaxis at this dosage is associated with significantly higher rates of PCP than is TMP-SMZ after allogeneic marrow transplantation."( High rates of Pneumocystis carinii pneumonia in allogeneic blood and marrow transplant recipients receiving dapsone prophylaxis.
Boeckh, M; Crawford, SW; Flowers, ME; Gooley, TA; Souza, JP, 1999
)
1.43
" Therefore dapsone therapy was initiated at a dosage of 100 mg daily after checking the glucose-6-phosphate-dehydrogenase and with regular control of the blood methemoglobin level."( [Henoch-Schönlein purpura: successful treatment with Dapsone].
Abeck, D; Albrecht, J; Hein, R; Mempel, M; Ring, J, 1999
)
0.94
"Dapsone use in pediatric patients is increasing; however, the currently available tablet dosage form cannot be used in young children."( Stability of dapsone in two oral liquid dosage forms.
Morosco, RS; Nahata, MC; Trowbridge, JM,
)
1.94
" The dosage forms were stored in 10 amber plastic prescription bottles."( Stability of dapsone in two oral liquid dosage forms.
Morosco, RS; Nahata, MC; Trowbridge, JM,
)
0.5
" Dapsone was, however, too toxic for humans (because of the excess dosage which was administered at that time) and was thus considered to be of no value in the treatment of common bacterial infections."( A century of the synthesis of dapsone: its anti-infective capacity now and then.
Orni-Wasserlauf, R; Wolf, R, 2000
)
1.51
" Overall results from these studies indicate patients who are eligible for PCP prophylaxis should be advised to take double-strength trimethoprim/sulfamethoxazole (TMP/SMX) on a daily basis, a dosage found more effective than thrice-weekly."( Optimizing PCP therapy.
Cadman, J; Torres, G, 1997
)
0.3
"A rapid, sensitive and selective spectrophotometric method has been developed for the quantitative determination of metoclopramide hydrochloride (MCP) and dapsone (DAP) in both pure and dosage forms."( A spectrophotometric method for the determination of metoclopramide HCl and dapsone.
Manju, B; Revanasiddappa, HD, 2001
)
0.74
" In conclusion, CTX at the dosage employed for primary PCP/TE prophylaxis does not seem to protect against bacterial infections more than second-line DP."( Incidence and determinants of bacterial infections in HIV-positive patients receiving anti-Pneumocystis carinii/Toxoplasma gondii primary prophylaxis within a randomized clinical trial.
Ammassari, A; Antinori, A; Cingolani, A; De Luca, A; Grillo, R; Murri, R; Pallavicini, F; Pezzotti, P, 2001
)
0.31
"Acetyl acetone is introduced as a new coupling agent for the spectrophotometric determination of some chemotherapeutic agents, such as metoclopramide, dapsone, p-aminobenzoic acid, and cisapride in both pure and dosage forms."( Spectrophotometric determination of some chemotherapeutic agents using acetyl acetone.
Manju, B; Revanasiddappa, HD, 2002
)
0.51
"Leprosy patients on a dosage of 100 mg dapsone, are prone to haemolytic anaemia."( Haematological alterations in leprosy patients treated with dapsone.
Halim, NK; Ogbeide, E, 2002
)
0.83
" Within a short time of dosing such animals, there is little or none of the uncombined drug in the blood."( The treatment of experimental toxoplasmosis in rabbits.
BEVERLEY, JK; FRY, BA, 1957
)
0.24
" When maintaining a dapsone dosage at 25 mg/day no relapse occurred during 3 years and 1 year, respectively."( [Dapsone treatment of folliculitis decalvans].
Paquet, P; Piérard, GE, 2004
)
1.56
"Dapsone at moderate dosage was well tolerated and rapidly effective in treating the two cases of folliculitis decalvans."( [Dapsone treatment of folliculitis decalvans].
Paquet, P; Piérard, GE, 2004
)
2.68
" Relapses did not occur with the tapering of PSL dosage when the ELISA values decreased to 40% of initial values, although they were still not within the normal range."( Monitoring of ELISA for anti-BP180 antibodies: clinical and therapeutic analysis of steroid-treated patients with bullous pemphigoid.
Esaki, C; Ichiki, Y; Izumi, T; Kitajima, Y, 2004
)
0.32
" The results of the study therefore reveal that patients undergoing therapy had significantly greater DNA damage than untreated patients, indicating bacterial infection and drug therapy as the causal factors, since lepromatous-type disease is the more severe form with the patients having lower resistance to Mycobacterium leprae and requiring heavier and prolonged dosage of antibiotics."( DNA damage studies in untreated and treated leprosy patients.
Gandhi, G; Singh, B, 2004
)
0.32
" When dapsone is given in combination with rifabutin, dapsone dosage adjustment may be necessary in light of the increase in dapsone clearance."( The effect of clarithromycin, fluconazole, and rifabutin on dapsone hydroxylamine formation in individuals with human immunodeficiency virus infection (AACTG 283).
Greenspan, DL; Hooton, TM; Jacobson, M; Slattery, JT; Trapnell, CB; Unadkat, JD; Winter, HR, 2004
)
1.05
" Using the '4-day test', a low level of synergism or a simple additional action between CPG and DDS was observed with multiple dosing of these two compounds in a combination."( The chemotherapy of rodent malaria. LXIII. Drug combinations to impede the selection of drug resistance, part 6: the potential value of chlorproguanil and dapsone in combination, and with the addition of artesunate.
Peters, W; Robinson, BL; Stewart, LB, 2005
)
0.53
"A rapid, sensitive and selective spectrophotometric method has been developed for the quantitative determination of dapsone (DAP) and metoclopramide hydrochloride (MCP) in both pure and dosage forms."( Individual and simultaneous spectrophotometric determination of dapsone and metoclopramide HCl in pharmaceutical dosage forms and synthetic binary mixtures.
Omran, AA, 2005
)
0.78
"5 mg/d or less within 1 year of reaching the maximum dosage of the study drug."( Multicenter randomized, double-blind, placebo-controlled, clinical trial of dapsone as a glucocorticoid-sparing agent in maintenance-phase pemphigus vulgaris.
Albrecht, J; Chen, D; Fivenson, D; Jacobus, D; Pandya, AG; Rico, MJ; Werth, VP, 2008
)
0.58
" Rats were dosed either with dapsone (12."( Antioxidant, antiinflammatory and antiapoptotic effects of dapsone in a model of brain ischemia/reperfusion in rats.
Diaz-Ruiz, A; Montes, S; Nava-Ruiz, C; Orozco-Suarez, S; Ortiz-Plata, A; Pérez-Neri, I; Perez-Severiano, F; Ríos, C; Salgado-Ceballos, H; Zavala, C, 2008
)
0.88
" Although current CDC guidelines do not recommend adjusting dose by IBW or renal function, we suggest that consideration should be given to these dosing strategies."( Dapsone-induced hemolytic anemia in lung allograft recipients.
Force, S; Lawrence, EC; Lyon, GM; Naik, PM; Neujahr, DC; Pelaez, A; Ramirez, A, 2008
)
1.79
" It is well tolerated, with pharmacokinetic evidence indicating topical dosing in comparison to oral administration significantly reduces systemic concentrations of the drug, and therefore risk of serious side effects."( An evaluation of dapsone gel 5% in the treatment of acne vulgaris.
Pickert, A; Raimer, S, 2009
)
0.69
" For CCG and MADDS, small to moderate increases in exposure with artesunate dosing were observed."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.63
"Rats were dosed orally with chlorproguanil/dapsone/artesunate (including 11."( Localization of artesunate and its derivatives in the pregnant rat and fetus following oral administration and relationship to developmental toxicity.
Clark, RL; Gristwood, WE; Harrell, AW; Lewsley, R; Wilson, R, 2010
)
0.62
" Our results demonstrated that the dosage of dapsone in leprosy treatment does not promote a significant methemoglobinemia."( Methemoglobinemia and dapsone levels in patients with leprosy.
Martins, Ade N; Riveira, JG; Salgado, CG; Silva, JP; Vieira, JL,
)
0.71
" Monensin, salinomycin and maduramycin at the dosage of 120, 60, and 5 mg/kg were administered in feed for 14 days."( Effects of ionophores on liver CYP1A and 3A in male broilers.
Jiang, SX; Mo, F; Yu, ZG; Zhang, JR; Zhang, LL; Zhao, J, 2010
)
0.36
" Higher dapsone dosing is associated with increased risk."( Dapsone-induced methemoglobinemia: a dose-related occurrence?
Esbenshade, AJ; Friedman, DL; Ho, RH; Shintani, A; Smith, LA; Zhao, Z, 2011
)
2.25
" Drug-induced acute hemolytic anemia in G6PD A- subjects can be life-threatening, depending on the nature and dosage of the drug trigger."( Clinical spectrum and severity of hemolytic anemia in glucose 6-phosphate dehydrogenase-deficient children receiving dapsone.
Carter, N; Duparc, S; Luzzatto, L; Pamba, A; Premji, Z; Richardson, ND; Tiono, AB, 2012
)
0.59
" Studies included were trials in which: (1) the participants were classified as having GCA by the 1990 ACR criteria or biopsy proven disease; (2) parallel-group randomised control of at least 16 weeks duration had been conducted with at least 20 participants; (3) the design included either alternative adjunct immunosuppressant regimens, alternative GCs dosing or routes of administration; and (4) outcome data was included on either relapse rates or rates of infection."( Prednisolone combined with adjunctive immunosuppression is not superior to prednisolone alone in terms of efficacy and safety in giant cell arteritis: meta-analysis.
Loke, YK; MacGregor, AJ; Watts, RA; Yates, M, 2014
)
0.4
" In 2005, the University of Kentucky (UK) Transplant Center implemented a novel dosing regimen of weekly dapsone as an alternative for patients with contraindications or intolerability to trimethoprim-sulfamethoxazole (TMP-SMZ), which remains the drug of choice."( Efficacy of once-weekly dapsone dosing for Pneumocystis jirovecii pneumonia prophylaxis post transplantation.
Au, T; Clifford, TM; Evans, RA; Fugit, AM; Tang, S, 2015
)
0.94
" Future studies are warranted to show the efficacy of weekly dapsone dosing compared to other PCP prophylaxis regimens."( Efficacy of once-weekly dapsone dosing for Pneumocystis jirovecii pneumonia prophylaxis post transplantation.
Au, T; Clifford, TM; Evans, RA; Fugit, AM; Tang, S, 2015
)
0.97
" After a 2-month course of treatment with hydroxychloroquine dosage of 200 mg per day and a break of 3 months between courses, we observed a complete remission."( Unilateral unique Lupus tumidus: pathogenetic mystery and diagnostic problem.
Bakardzhiev, I; Chokoeva, AA; Krasnaliev, I; Lotti, T; Tana, C; Tchernev, G; Wollina, U, 2016
)
0.43
"Reducing the dosing frequency of topical acne treatments to once daily may improve adherence."( Safety and Pharmacokinetics of Once-Daily Dapsone Gel, 7.5% in Patients With Moderate Acne Vulgaris.
Berk, DR; Chang-Lin, JE; Jarratt, MT; Jones, TM; Kaoukhov, A; Lin, V; Tong, W, 2016
)
0.7
" She started dapsone at the dosage of 1 mg/kg/day, maintaining low dose prednisone; this treatment was successfully followed by the dramatic disappearance of skin lesions and limb pain."( Systemic Lupus Erythematosus and Bullous Pemphigoid with Dramatic Response to Dapsone.
Cimaz, R; Corsello, G; Maggio, MC; Prinzi, E, 2017
)
1.05
" Side effects occurred in 31% (n = 13) of patients, and required dapsone withdrawal in 22% (n = 9) or dosage reduction in 10% (n = 4) of the cases."( Efficacy and safety of dapsone as second line therapy for adult immune thrombocytopenia: A retrospective study of 42 patients.
Audia, S; Berthier, S; Bonnotte, B; Estève, C; Guilhem, A; Leguy-Seguin, V; Nicolas, B; Samson, M, 2017
)
1
" Cocrystallization via fluidized bed granulation represents a useful tool and a feasible alternative technique for the large scale manufacture of pharmaceutical cocrystals for solid dosage forms."( In Situ Cocrystallization of Dapsone and Caffeine during Fluidized Bed Granulation Processing.
Cabral, LM; Healy, AM; Todaro, V; Worku, ZA, 2019
)
0.81
" However, no clear evaluation of its indications, its effectiveness, or its usage guidelines (optimal dosage or duration of treatment) is available."( Indications and efficiency of dapsone in IgA vasculitis (Henoch-Schonlein purpura): case series and a review of the literature.
Dima, B; Gilliaux, O; Muyshont, L; Roman, C; Schurmans, T, 2019
)
0.8
" The pharmacology and pharmacokinetics of the preceding drugs include specific recommendations, generic names, availability, mode of administration, dosage schedule, and the essentials of drug management."( Pharmacology and Therapeutics of Corticosteroids Sparing Maintenance Immunosuppressive/Adjunct Therapy Drugs.
Malhotra, R; Sehgal, VN, 2019
)
0.51
" This case illustrates the potential for significant systemic dapsone absorption even with daily topical dosing and demonstrates the need for clear anticipatory guidance to prevent the potential morbidity and mortality associated with methemoglobinemia from improper topical dapsone use."( Severe methemoglobinemia due to topical dapsone misuse in a teenage girl.
McCarthy, J; McCarthy, P; McFadden, V; Stefanko, N; Yale, S, 2020
)
1.07
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antimalarialA drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human.
leprostatic drugA substance that suppresses Mycobacterium leprae, ameliorates the clinical manifestations of leprosy, and/or reduces the incidence and severity of leprous reactions.
antiinfective agentA substance used in the prophylaxis or therapy of infectious diseases.
anti-inflammatory drugA substance that reduces or suppresses inflammation.
[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 (2)

ClassDescription
sulfoneAn organosulfur compound having the structure RS(=O)2R (R =/= H).
substituted aniline
[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 (54)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.77830.003245.467312,589.2998AID2517
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
TDP1 proteinHomo sapiens (human)Potency22.14270.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency61.64480.000221.22318,912.5098AID743035
Smad3Homo sapiens (human)Potency3.54810.00527.809829.0929AID588855
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926; AID938
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency43.64860.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.39140.000214.376460.0339AID720691
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.57190.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.91250.001530.607315,848.9004AID1224841; AID1259401
estrogen nuclear receptor alphaHomo sapiens (human)Potency34.55490.000229.305416,493.5996AID743069; AID743075; AID743079
GVesicular stomatitis virusPotency2.75400.01238.964839.8107AID1645842
67.9K proteinVaccinia virusPotency12.58930.00018.4406100.0000AID720580
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency48.96620.001024.504861.6448AID743212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency38.89520.001019.414170.9645AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.03010.023723.228263.5986AID743223
cytochrome P450 2C9 precursorHomo sapiens (human)Potency0.79430.00636.904339.8107AID883
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency20.35110.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency25.92900.004611.374133.4983AID624296
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.94330.031610.279239.8107AID884; AID885
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency19.95260.00419.962528.1838AID2675
lamin isoform A-delta10Homo sapiens (human)Potency4.24600.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency2.75400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.75400.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency0.79430.00638.235039.8107AID883
Nuclear receptor ROR-gammaHomo sapiens (human)Potency33.49150.026622.448266.8242AID651802
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.75400.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.75400.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)567.00000.11007.190310.0000AID1209455; AID1443980; AID1449628; AID1473738
MyeloperoxidaseHomo sapiens (human)IC50 (µMol)0.42000.02001.88117.6800AID1514846
Dihydrofolate reductasePneumocystis cariniiIC50 (µMol)1.50000.00060.54766.2000AID55834
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.18300.00020.522910.0000AID763552
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (117)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
response to yeastMyeloperoxidaseHomo sapiens (human)
hypochlorous acid biosynthetic processMyeloperoxidaseHomo sapiens (human)
respiratory burst involved in defense responseMyeloperoxidaseHomo sapiens (human)
defense responseMyeloperoxidaseHomo sapiens (human)
response to oxidative stressMyeloperoxidaseHomo sapiens (human)
response to mechanical stimulusMyeloperoxidaseHomo sapiens (human)
removal of superoxide radicalsMyeloperoxidaseHomo sapiens (human)
response to foodMyeloperoxidaseHomo sapiens (human)
response to lipopolysaccharideMyeloperoxidaseHomo sapiens (human)
low-density lipoprotein particle remodelingMyeloperoxidaseHomo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
negative regulation of apoptotic processMyeloperoxidaseHomo sapiens (human)
defense response to fungusMyeloperoxidaseHomo sapiens (human)
response to gold nanoparticleMyeloperoxidaseHomo sapiens (human)
defense response to bacteriumMyeloperoxidaseHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (57)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
chromatin bindingMyeloperoxidaseHomo sapiens (human)
peroxidase activityMyeloperoxidaseHomo sapiens (human)
protein bindingMyeloperoxidaseHomo sapiens (human)
heparin bindingMyeloperoxidaseHomo sapiens (human)
heme bindingMyeloperoxidaseHomo sapiens (human)
metal ion bindingMyeloperoxidaseHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (43)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
nucleusMyeloperoxidaseHomo sapiens (human)
nucleoplasmMyeloperoxidaseHomo sapiens (human)
lysosomeMyeloperoxidaseHomo sapiens (human)
secretory granuleMyeloperoxidaseHomo sapiens (human)
azurophil granule lumenMyeloperoxidaseHomo sapiens (human)
azurophil granuleMyeloperoxidaseHomo sapiens (human)
intracellular membrane-bounded organelleMyeloperoxidaseHomo sapiens (human)
extracellular exosomeMyeloperoxidaseHomo sapiens (human)
phagocytic vesicle lumenMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (229)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID55882Inhibition of Dihydropteroate synthase of Mycobacterium 607 and log (1/MIC) was reported1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quantitative structure-activity analysis in dihydropteroate synthase inhibition by sulfones. Comparison with sulfanilamides.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1223481Elimination half life iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1653404Effect of metallo-protein haemoglobin in rat assessed as peak methemoglobin level at 400 mg/kg, sc administered as single dose2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653387Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.005 mg/L measured by bioluminescence assay (Rvb = 314 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID571304Antibacterial activity against Mycobacterium avium2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro and in vivo properties of dihydrophthalazine antifolates, a novel family of antibacterial drugs.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID322132In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1223478Total clearance in chimeric mouse with humanized liver at 3 mg/kg, iv by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1653402Half life in rat at 400 mg/kg, sc administered as single dose2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1223483Unbound fraction in iv dosed human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1653455Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.005 mg/L measured by bioluminescence assay (Rvb = 462 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653465Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.01 mg/L (Rvb = 1.28 +/- 0.14 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1514846Inhibition of MPO (unknown origin)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
The development of myeloperoxidase inhibitors.
AID624606Specific activity of expressed human recombinant UGT1A12000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
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.
AID1223477Total clearance in iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1653467Antimicrobial activity against Mycobacterium leprae2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID322129In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1653403Drug concentration in rat blood at 400 mg/kg, sc administered as single dose2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653399Antimycobacterial activity against DDS resistant Mycobacterium smegmatis ATCC 607 infected in mouse2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID55884Inhibitory activity against dihydropteroic acid synthase (SYN) from candida albicans2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID322131In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1145677Antibacterial activity against sensitive Pediococcus cerevisiae ATCC 808 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID763552Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.
AID624647Inhibition of AZT glucuronidation by human UGT enzymes from liver microsomes2005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1223482Ratio of drug level in blood to plasma in iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID55885Inhibitory activity against dihydropteroic acid synthase (SYN) from Escherichia coli2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
AID1145687Antibacterial activity against sensitive Escherichia coli ATCC 10536 assessed as reduction in growth in presence of p-aminobenzoic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145689Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as dose required to survivors for period of 60 days1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID294542Antimicrobial activity against Staphylococcus aureus ATCC 6538 by broth microdilution method2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Rapid synthesis of sulfone derivatives as potential anti-infectious agents.
AID115842Compound was tested for the number of control mice with decreased RBC to that of number of tested mice at 100 mg/kg p.o.; 3/151998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Discovery of FR115092: a novel antinephritic agent.
AID322127In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID119793Percentage of the number of platelets for the treated versus mitomycin C(MMC) control group in the MMC-induced thrombocytopenic mice at a dose of 100 mg/kg following peroral administration1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Synthesis and effects of novel thiazole derivatives against thrombocytopenia.
AID55834Inhibitory activity was determined against dihydrofolate reductase in Pneumocystis carinii. 1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii.
AID1653447Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.01 mg/L (Rvb = 0.95 +/- 0.01 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID119794Percentage of the number of platelets for the treated versus mitomycin C(MMC) control group in the MMC-induced thrombocytopenic mice at a dose of 32 mg/kg following peroral administration1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Synthesis and effects of novel thiazole derivatives against thrombocytopenia.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1653430Anti-leprotic activity against Mycobacterium leprae infected in CBA mouse assessed as number of Mycobacterium leprae in paw pads at 30 mg/kg administrated 5 times a week and measured 7.5 months post infection (Rvb = 3.91 +/- 0.33 10'5 No_unit)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID55887Inhibitory activity against dihydropteroic acid synthase (SYN) from Mycobacterium lufu (DDS resistant)2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID43581Inhibition of beta-lactamase at 100 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID280385Activation of human CYP2C9 assessed as (S)-Flurbiprofen hydroxylation2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Use of simple docking methods to screen a virtual library for heteroactivators of cytochrome P450 2C9.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1145676Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 to IC50 for sensitive Lactobacillus casei ATCC 74691977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1653466Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L (Rvb = 1.28 +/- 0.14 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653456Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.01 mg/L measured by bioluminescence assay (Rvb = 462 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653398Antimycobacterial activity against DDS sensitive Mycobacterium smegmatis ATCC 607 infected in mouse2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID52790Inhibition of chymotrypsin at 250 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1145678Antibacterial activity against chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1653439Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 314 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID55866Inhibitory activity (Enzyme inhibition index) against dihydropteroate synthase from Escherichia coli.1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Quantitative structure-activity relationships in dihydropteroate synthase inhibition by multisubstituted sulfones. Design and synthesis of some new derivatives with improved potency.
AID1653400Anti-leprotic activity against Mycobacterium leprae infected in albino mouse assessed survival against infection at 400 mg/kg, sc administered 58 days post-infection and subsequent compound dosing at 200 mg/kg at 0.5, 1 or 2 months interval2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID322130In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1653438Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.01 mg/L measured by bioluminescence assay (Rvb = 314 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1145672Antibacterial activity against chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1223486Intrinsic clearance in human hepatocytes from chimeric mouse with humanized liver assessed per 10'6 cells at 10 uM after 0.25 to 2 hrs by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1653472Anti-leprotic activity against Mycobacterium leprae infected in 538 CBA mouse assessed as number of Mycobacterium leprae in paw pads at 2 mg/kg administrated via gastric tube 5 times a week and measured 7 months post infection2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1223475Elimination half life in chimeric mouse with humanized liver at 3 mg/kg, iv by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1145688Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as active dose required to increase of 100% in mean survival time1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID55880In vitro inhibition of Mycobacterium lufu dihydopterate synthase.1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
A quantitative structure-activity relationship analysis of some 4-aminodiphenyl sulfone antibacterial agents using linear free energy and molecular modeling methods.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1145683Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction in growth in presence of 0.001 ug/ml folic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1145685Antibacterial activity against sensitive Pediococcus cerevisiae ATCC 808 assessed as reduction in growth in presence of 0.001 ug/ml folinic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID322133In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID116680Antinephritic activity on chronic graft-versus-host disease (GVHD) in mice at 10 mg/kg p.o.1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Discovery of FR115092: a novel antinephritic agent.
AID1145675Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID322126In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID322135Antimalarial activity against Plasmodium falciparum W2 as reduced [3H]hypoxanthine uptake after 72 hrs2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1653417Inhibition of PGL1 synthesis in Mycobacterium leprae infected Swiss Webster mouse macrophages assessed as decrease in [U-14C]PA incorporation at 2 uM preincubated for 4 days post infection followed by [U-14C]PA addition and measured after 7 days by liquid2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1653429Anti-leprotic activity against Mycobacterium leprae infected in CBA mouse assessed as number of Mycobacterium leprae in paw pads at 10 mg/kg administrated 5 times a week and measured 7.5 months post infection (Rvb = 3.91 +/- 0.33 10'5 No_unit)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID55877Inhibitory activity (apE=log(1/EII50)) against dihydropteroate synthase from Escherichia coli1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Quantitative structure-activity relationships in dihydropteroate synthase inhibition by multisubstituted sulfones. Design and synthesis of some new derivatives with improved potency.
AID55889Inhibitory activity against dihydropteroic acid synthase (SYN) from Plasmodium berghei2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1145674Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1653401Drug excretion in rat urine at 400 mg/kg, sc administered as single dose measured after 30 days2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID678720Metabolic stability in human liver microsomes assessed as low signal/noise ratio (S/N of 1 to 10) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID624612Specific activity of expressed human recombinant UGT1A92000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1145679Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 to IC50 for sensitive Pediococcus cerevisiae ATCC 8081977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID119792Percentage of the number of platelets for the treated versus mitomycin C(MMC) control group in the MMC-induced thrombocytopenic mice at a dose of 10 mg/kg following peroral administration1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Synthesis and effects of novel thiazole derivatives against thrombocytopenia.
AID1653464Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.005 mg/L (Rvb = 1.28 +/- 0.14 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1653446Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.005 mg/L (Rvb = 0.95 +/- 0.01 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1145680Antibacterial activity against sensitive Escherichia coli ATCC 10536 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1653448Anti-leprotic activity against Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L (Rvb = 0.95 +/- 0.01 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID294543Antimicrobial activity against Candida tropicalis IP 2031 by broth microdilution method2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Rapid synthesis of sulfone derivatives as potential anti-infectious agents.
AID116681Antinephritic activity on chronic graft-versus-host disease (GVHD) in mice at 32 mg/kg p.o.1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Discovery of FR115092: a novel antinephritic agent.
AID55888Inhibitory activity against dihydropteroic acid synthase (SYN) from Mycobacterium lufu (DDS sensitive)2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
AID55865Inhibition of dihydropteroate synthase of Escherichia coli1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quantitative structure-activity analysis in dihydropteroate synthase inhibition by sulfones. Comparison with sulfanilamides.
AID1145671Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1653418Inhibition of PGL1 synthesis in Mycobacterium leprae infected Swiss Webster mouse macrophages assessed as decrease in [U-14C]PA incorporation at 20 uM preincubated for 4 days post infection followed by [U-14C]PA addition and measured after 7 days by liqui2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1688332Antimalarial activity against Plasmodium vivax infected in human blood incubated for 24 to 36 hrs2020European journal of medicinal chemistry, Feb-15, Volume: 188Current progress in antimalarial pharmacotherapy and multi-target drug discovery.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1653388Antimalarial activity against Plasmodium berghei infected in albino mouse assessed survival against infection at 400 mg/kg, sc administered as single dose2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID117036Inhibition of proteinuria in the graft-versus-host disease mice following 100 mg/kg p.o. administration.1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Discovery of FR115092: a novel antinephritic agent.
AID322134Antimalarial activity against Plasmodium falciparum D6 as reduced [3H]hypoxanthine uptake after 72 hrs2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID322128In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs by SYBR green fluorescence assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening.
AID1653405Anti-leprotic activity against Mycobacterium leprae infected in BALB/c mouse assessed as time delay in bacterial multiplication in footpad at 0.0001 g/100g of diet administered via feed starting 60 or 75 day post infection up to 90 days by Shepard's kinet2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID106806Inhibition of malate dehydrogenase (MDH) at 400 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1653457Anti-leprotic activity against Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 462 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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.
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.
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.
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,416)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901952 (44.20)18.7374
1990's844 (19.11)18.2507
2000's670 (15.17)29.6817
2010's725 (16.42)24.3611
2020's225 (5.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 86.37

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 Index86.37 (24.57)
Research Supply Index8.61 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index169.47 (26.88)
Search Engine Supply Index2.12 (0.95)

This Compound (86.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials379 (7.41%)5.53%
Reviews501 (9.79%)6.00%
Case Studies1,529 (29.89%)4.05%
Observational13 (0.25%)0.25%
Other2,694 (52.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (72)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Trial Randomized, Placebo-controlled, Using Dapsone as a Neuroprotector During Acute Ischemia Stroke [NCT01144650]Phase 2/Phase 3300 participants (Anticipated)Interventional2009-07-31Recruiting
An Open-label Study to Investigate the Efficacy and Tolerability of Aczone Gel, 7.5% in the Treatment of Acne Vulgaris in Men and Women With Skin of Color [NCT03681470]Phase 420 participants (Actual)Interventional2019-04-09Completed
An Open-Label Phase 4 Safety and Efficacy Trial of ACZONE (Dapsone) Gel, 7.5% in 9 to 11 Year-Old Patients With Acne Vulgaris [NCT02959970]Phase 4100 participants (Actual)Interventional2016-10-31Completed
[NCT02117752]Phase 1237 participants (Actual)Interventional2014-04-30Completed
A Randomized, Placebo-Controlled, Multicenter Study to Assess the Safety and Efficacy of Dapsone for the Treatment of COVID-19 Positive Patients. [NCT04935476]Phase 33,000 participants (Anticipated)Interventional2021-11-22Recruiting
A Single-center, Double-blind, Randomized, Parallel-group Study, Comparing DPSG to a Placebo Control in the Treatment of Acne Vulgaris [NCT03132194]Phase 11,125 participants (Actual)Interventional2016-08-08Completed
[NCT02117739]Phase 158 participants (Actual)Interventional2014-04-30Completed
Oral Corticosteroids Therapy and Interstitial Fibrosis in Patients With Pneumocystis Jirovecii Pneumonia (PCP) and pO2 of >70 at Presentation. [NCT00636935]Phase 40 participants (Actual)Interventional2008-02-29Withdrawn(stopped due to No patient completed protocol)
Dapsone Induced Methemoglobinemia in Pediatric Hematologic Malignancy and Aplastic Anemia [NCT00993694]41 participants (Actual)Observational2009-01-31Completed
A Multi-center, Double-blind, Randomized, Placebo-controlled, Parallel-group Study Comparing Dapsone 5% Gel (SEEGPharm SA) to Aczone® and Both Active Treatments Compared to Placebo (Vehicle) in the Treatment of Acne Vulgaris [NCT02865005]Phase 32,361 participants (Actual)Interventional2016-02-29Completed
[NCT02108483]Phase 133 participants (Actual)Interventional2014-04-30Completed
A Multi-center,Double-blind,Randomized,Three-arm,Placebo-controlled,Parallel-group Study, Comparing Dapsone Gel,7.5% (Torrent Pharma) to Aczone® Gel,7.5% and Both Active Treatments to a Placebo Control in the Treatment of Acne Vulgaris [NCT04015375]Phase 31,150 participants (Actual)Interventional2019-07-11Completed
Prospective Multicenter Randomized Open-label Controlled Trial Assessing Efficacy and Safety of DAPSone as a Second-line Option in Adult Immune Thrombocytopenia [NCT02627417]Phase 3216 participants (Anticipated)Interventional2015-12-31Recruiting
A Randomized Multicenter Study for Isolated Skin Vasculitis [NCT02939573]Phase 290 participants (Anticipated)Interventional2017-01-01Recruiting
Independent Study to Establish the Efficacy of the Six Doses Uniform MDT Regimen (U-MDT) for Leprosy Patients [NCT00669643]Phase 4859 participants (Actual)Interventional2007-02-28Completed
Dapsone Gel, 5% for Topical Treatment of Dermatitis Herpetiformis [NCT01115244]Phase 41 participants (Actual)Interventional2010-07-31Terminated(stopped due to poor enrollment and lack of funding)
Pharmacokinetics of Chlorproguanil-Dapsone in Pregnant Women With Plasmodium Falciparum Infection, and Reinfection With P. Falciparum During Pregnancy Following Treatment [NCT00126971]Phase 1132 participants Interventional2005-07-31Suspended
A Phase III Comparative Study of Dapsone / Trimethoprim and Clindamycin / Primaquine Versus Trimethoprim / Sulfamethoxazole in the Treatment of Mild-to-Moderate PCP in Patients With AIDS [NCT00000640]Phase 3290 participants InterventionalCompleted
Comparison of Two Dosage Regimens of Oral Dapsone for Prophylaxis of Pneumocystis Carinii Pneumonia in Pediatric HIV Infection [NCT00000739]Phase 196 participants InterventionalCompleted
A Phase 3, Randomized, Double-blind, Multi-dose Study to Evaluate the Safety and Efficacy of 5% Dapsone Topical Gel, (DTG 5%) When Co-administered With Vehicle Control, Adapalene Gel 0.1% or Benzoyl Peroxide Gel 4% in the Treatment of Acne Vulgaris. [NCT00151541]Phase 3301 participants (Actual)Interventional2005-02-28Completed
An Open-label Three Arm Trial of the Efficacy and Safety of Chlorproguanil / Dapsone (Lapdap) Compared With Chloroquine and Sulfadoxine / Pyrimethamine for the Treatment of Vivax Malaria in Pakistan and Afghanistan [NCT00158561]Phase 3750 participants Interventional2004-02-29Completed
Efficacy and Safety of add-on Dapsone Versus add-on Methotrexate in Patients With Bullous Pemphigoid: A Randomized Controlled Trial [NCT05984381]Phase 462 participants (Anticipated)Interventional2023-08-01Recruiting
A Phase IV, Randomised, Multicentre, Double-blind, Study to Evaluate the Clinical Utility of Prospective Genetic Screening (HLA-B*1301) for Susceptibility to Dapsone Hypersensitivity Syndrome [NCT02550080]Phase 43,130 participants (Anticipated)Interventional2015-07-31Recruiting
Two-week Study to Determine and Compare the Tolerance and Irritation Potential of Clindamycin and Benzoyl Peroxide to Dapsone Gel Topical Acne Medications [NCT00964366]Phase 453 participants (Actual)Interventional2009-07-31Completed
Discontinuation of Primary and Secondary Prophylaxis for Opportunistic Infections in HIV-infected Patients Who Had CD4+ Cell Count <200 Cells/mm3 But Undetectable Plasma HIV-1 RNA [NCT01392430]74 participants (Actual)Interventional2009-06-30Completed
Phenotypic and Genotypic Evaluation of Cytochrome P450 Isoforms in Populations of Different Ethnic Composition [NCT00162383]1,200 participants (Anticipated)Interventional1995-07-31Recruiting
[NCT01425320]Phase 10 participants (Actual)Interventional2013-01-31Withdrawn(stopped due to Study was never initiated due to company decision. No study subjects were ever enrolled or dosed.)
Evaluation of 4 Artemisinin-based Combinations for Treating Uncomplicated Malaria in African Children [NCT00393679]Phase 34,112 participants (Actual)Interventional2007-07-31Completed
Drug Options for Intermittent Preventive Treatment for Malaria in Infants in an Area With High Resistance to Sulfadoxine/Pyrimethamine: an Evaluation of Short and Long-acting Antimalarial Drugs [NCT00158574]Phase 2/Phase 32,419 participants (Actual)Interventional2005-01-31Completed
A Double-blind, Randomized, Parallel-group, Side-by-side Single-center Study Comparing a Topical Steroid / Vehicle Combination to a Topical Steroid / Topical Dapsone Combination in Patients With Lichen Simplex Chronicus and/or Prurigo Nodularis [NCT01870050]20 participants (Anticipated)Interventional2013-09-30Not yet recruiting
A Multi-Center, Double-Blind, Randomized, Placebo Controlled, Parallel-Group Study, Comparing Test Gel, 5% to ACZONE Gel, 5% and Both Active Treatment to a Placebo Control in the Treatment of Acne Vulgaris [NCT02929719]Phase 11,134 participants (Actual)Interventional2014-04-30Completed
A Phase II, Randomized, Double-Blind, Parallel Design Study to Evaluate ACZONE™ (Dapsone) Gel, 5% As a Treatment For Rash Related to the Human Epidermal Growth Factor Receptor 1 (HER1)/Epidermal-Growth-Factor-Receptor (EGFR) Inhibitor Tarceva® (Erlotinib) [NCT00343187]Phase 22 participants (Actual)Interventional2006-06-30Terminated(stopped due to Lack of enrollment)
A Multi-centre, Randomised, Double-blind, Double Dummy Study Comparing the Efficacy and Safety of Chlorproguanil-dapsone-artesunate Versus Artemether-lumefantrine in the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria in Children and Adoles [NCT00344006]Phase 31,395 participants (Actual)Interventional2006-06-30Completed
A Prospective Randomized Placebo-Controlled Clinical Trial of Dapsone as a Glucocorticoid-Sparing Agent in Maintenance Phase Pemphigus Vulgaris [NCT00429533]Phase 248 participants Interventional1996-11-30Terminated
An Investigator-Blind, Phase 4 Study Assessing Mitigation of Facial Irritation When Comparing the Use of Two Acne Treatment Products (Retin-A Micro® 0.1 % Pump and Aczone®) With One Treatment Product (Retin-A Micro® 0.1 % Pump) Using a Split-Face Model [NCT01313728]Phase 426 participants (Actual)Interventional2010-12-31Completed
The Prevention of Anaemia and Malaria in Infants in an Area of Intense and Perennial Malaria Transmission [NCT00497471]832 participants (Actual)Interventional1995-02-28Terminated(stopped due to Follow-up end in 1999)
An Open, Randomised, Multi-centre Dose Ranging Phase II Study to Evaluate LAPDAP in Combination With Three Different Doses of Artesunate [NCT00519467]Phase 2120 participants (Actual)Interventional2003-06-30Completed
Open Study on the Tolerability and Efficacy of the Combination Chlorproguanil-Dapsone+Artesunate Compared to Amodiaquine+Sulfadoxine-Pyrimethamine for the Treatment of Uncomplicated Falciparum Malaria in Rwandan Children [NCT00461578]800 participants Interventional2005-04-30Completed
Randomized Trial of the Safety and Effectiveness of Lapdap and Coartemether for Uncomplicated Malaria in Operational Settings [NCT00118794]Phase 31,200 participants Interventional2004-09-30Completed
[NCT00834210]Phase 4171 participants (Actual)Interventional2008-12-31Completed
Comparison of the Efficacy of Clindamycin Phosphate 1% Gel Versus Once-daily Dapsone 5% Gel in the Treatment of Moderate Acne Vulgaris [NCT05926869]Phase 2100 participants (Actual)Interventional2022-08-01Completed
Effect of Fluconazole, Clarithromycin, and Rifabutin on the Pharmacokinetics of Sulfamethoxazole and Dapsone and Their Hydroxylamine Metabolites [NCT00000826]Phase 148 participants InterventionalCompleted
Efficacy and Safety of Pediatric Immunization-linked Preventive Intermittent Treatment With Antimalarials in Decreasing Anemia and Malaria Morbidity in Rural Western Kenya [NCT00111163]1,516 participants Interventional2004-03-31Completed
[NCT00000596]Phase 20 participants Interventional1978-06-30Completed
A Multi-centre, Randomised, Double-blind Study to Compare the Efficacy and Safety of Chlorproguanil-dapsone-artesunate Versus Chlorproguanil-dapsone in the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria in Children, Adolescents and Adults [NCT00371735]Phase 3900 participants (Actual)Interventional2006-04-30Completed
Treating Malaria During Pregnancy: A Randomized Trial of Potential Options for Treatment in an Area of High Drug Resistance in Tanzania [NCT00146731]Phase 3310 participants (Actual)Interventional2004-01-31Completed
A Double-blind Randomised Trial to Assess the Tolerability of Amodiaquine Plus Artesunate (AQ-Art) Versus Chlorproguanil Plus Dapsone Plus Artesunate (CDA) in the Treatment of Uncomplicated P. Falciparum Malaria in Malawi [NCT00164359]Phase 4212 participants Interventional2005-04-30Completed
An Open Randomised Trial of the Efficacy of Sulfadoxine-Pyrimethamine (SP), Amodiaquine + SP (AQ-SP), AQ + Artesunate (AQ-Art), Chlorproguanil-Dapsone + Art (CD-Art), and Lumefantrine-Artemether (LA) for Uncomplicated Malaria in Malawi [NCT00164710]Phase 4365 participants Interventional2005-04-30Completed
A Phase II, Randomized, Partial-Blind, Parallel-Group, Active- and Vehicle-Controlled, Multicenter Study of the Safety and Efficacy of ACZONE™ (Dapsone) Gel, 5% in Subjects With Papulopustular Rosacea [NCT00249782]Phase 2400 participants (Actual)Interventional2005-11-30Completed
[NCT01785836]Phase 10 participants (Actual)Interventional2013-03-31Withdrawn(stopped due to Study was never initiated due to company decision. No study subjects were ever enrolled or dosed.)
Pharmacokinetics and Distribution of Dapsone (DDS) in Leucocytes After Single-dose and Multiple-dose Administration in Healthy Subjects Genotyped for CYP2C9 and NAT2 and in Patients With Autoimmune Bullous Dermatoses [NCT02493283]Phase 123 participants (Actual)Interventional2011-09-30Completed
Efficacy of Dapsone Gel 7.5%in Comparison to Trichloroacetic Acid 20% for Treatment of Acne Vulgaris :Split Face Study [NCT05296460]Phase 430 participants (Anticipated)Interventional2022-09-01Not yet recruiting
[NCT01231334]Phase 4286 participants (Actual)Interventional2010-08-31Completed
Efficacy and Safety of Aczone 7.5% Gel in the Treatment of Truncal Acne Vulgaris [NCT02944461]Phase 420 participants (Actual)Interventional2016-10-31Completed
Use of Aczone 5% Gel as Maintenance Treatment of Acne Vulgaris Following Completion of Oral Doxycycline and Aczone 5% Gel Treatment [NCT01885910]Phase 432 participants (Actual)Interventional2013-07-31Completed
Dapsone 100 Mg Versus 50 as Primary Prophylaxis for Pneumocystis Carinii Pneumonia (PCP) in Patients With AIDS-Related Complex (ARC) [NCT00002043]0 participants InterventionalCompleted
Randomized Prospective Study of Dapsone Versus Trimethoprim-Sulfamethoxazole in the Treatment of First Episode Pneumocystis Carinii Pneumonia in AIDS Patients [NCT00002283]0 participants InterventionalCompleted
A Safety and Efficacy Study to Compare Dapsone Dermal Gel With Vehicle Control in Patients With Acne Vulgaris [NCT01974323]Phase 32,238 participants (Actual)Interventional2013-11-30Completed
Clinical Evaluation of New Treatment Strategy of Mucous Membrane Pemphigoid Using Large Dose of Prednisolone Plus Intra-lesional of Triamcinolone Acetonide Followed by Combination of Mycophenolate Mofetil, Dapsone and Low Dose Prednisolone [NCT04744623]Phase 2/Phase 310 participants (Actual)Interventional2020-09-30Active, not recruiting
A Randomized, Comparative Study of Daily Dapsone and Daily Atovaquone for Prophylaxis Against PCP in HIV-Infected Patients Who Are Intolerant of Trimethoprim and/or Sulfonamides [NCT00000802]Phase 3700 participants InterventionalCompleted
Off Label Use of Dapsone in SARS-CoV-2 Hospitalized Patients [NCT04918914]Early Phase 1100 participants (Anticipated)Interventional2020-10-18Recruiting
Population Pharmacokinetic Analysis of Dapsone in Normal, Overweight and Obese Volunteers [NCT01165840]Phase 437 participants (Actual)Interventional2010-07-31Completed
A Randomized, Comparative, Prospective Study of Monthly Aerosolized Pentamidine and Thrice Weekly Dapsone for Prophylaxis Against PCP in HIV-Infected Patients Who Are Intolerant to Trimethoprim and/or Sulfonamides [NCT00001028]Phase 3400 participants InterventionalCompleted
Randomized Phase I Study of Trimetrexate Glucuronate (TMTX) With Leucovorin (LCV) Protection Plus Dapsone Versus Trimethoprim / Sulfamethoxazole (TMP/SMX) for Treatment of Moderately Severe Episodes of Pneumocystis Carinii Pneumonia [NCT00002120]Phase 120 participants InterventionalCompleted
A Randomized Trial of Three Anti-Pneumocystis Agents Plus Zidovudine for the Primary Prevention of Serious Infections in Patients With Advanced HIV Infection [NCT00000991]Phase 3600 participants InterventionalCompleted
A Safety and Efficacy Study to Compare Dapsone Dermal Gel With Vehicle Control in Patients With Acne Vulgaris [NCT01974141]Phase 32,102 participants (Actual)Interventional2013-11-30Completed
Neuroprotective Effect of Dapsone in Patients With Aneurysmal Subarachnoid Hemorrhage: Prospective, Randomized, Double-Blinded, Placebo-Controlled, Clinical Trial [NCT05131295]Phase 349 participants (Actual)Interventional2007-09-05Completed
[NCT01773122]Phase 177 participants (Actual)Interventional2013-01-21Completed
[NCT00835198]Phase 4163 participants (Actual)Interventional2008-12-31Completed
A Phase III Randomized Double-blind Study of Prophylactic Topical Dapsone 5% Gel Versus Moisturizer for Cetuximab-induced Papulopustular (Acneiform) Rash in Patients With mCRC or HNSCC Without Previous or Concurrent RT [NCT01931150]Phase 311 participants (Actual)Interventional2013-08-31Completed
Efficacy of Sulphadoxine/Pyrimethamine and Chlorproguanil/Dapsone in 6-59 Month Old Children With Uncomplicated Malaria and in 2-10 Month Old Asymptomatic Infants. [NCT00361114]Phase 3112 participants (Actual)Interventional2006-07-31Terminated(stopped due to SP arms were stopped due to high levels of treatment failure.CD not available.)
[NCT02032407]Phase 468 participants (Actual)Interventional2013-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00834210 (4) [back to overview]Change From Baseline in Inflammatory Lesion Counts (Papules,Pustules, and Nodules) at Week 12
NCT00834210 (4) [back to overview]Change From Baseline in Investigator Global Assessment at Week 12
NCT00834210 (4) [back to overview]Change From Baseline in Non-Inflammatory Lesion Counts (Open and Closed Comedones) at Week 12
NCT00834210 (4) [back to overview]Change From Baseline in Overall Disease Severity at Week 12
NCT00835198 (4) [back to overview]Change From Baseline in Overall Disease Severity at Week 12
NCT00835198 (4) [back to overview]Change From Baseline in Non-Inflammatory Lesion Counts (Open and Closed Comedones) at Week 12
NCT00835198 (4) [back to overview]Change From Baseline in Investigator Global Assessment at Week 12
NCT00835198 (4) [back to overview]Change From Baseline in Inflammatory Lesion Counts (Papules, Pustules and Nodules) at Week 12
NCT00964366 (5) [back to overview]Skin Hydration
NCT00964366 (5) [back to overview]Transepidermal Water Loss (TEWL)
NCT00964366 (5) [back to overview]Sebum Measurements
NCT00964366 (5) [back to overview]Skin Dryness
NCT00964366 (5) [back to overview]Skin Erythema (Redness)
NCT01165840 (1) [back to overview]Serum Clearance
NCT01231334 (7) [back to overview]Percent Change From Baseline in Inflammatory Lesion Counts at Week 12
NCT01231334 (7) [back to overview]Percent Change From Baseline in Non-inflammatory Lesion Counts at Week 12
NCT01231334 (7) [back to overview]Percent Change From Baseline in Total Lesion Count at Week 12
NCT01231334 (7) [back to overview]Percentage of Participants at Week 12 Having at Least a One Point Decrease in Overall Disease Severity
NCT01231334 (7) [back to overview]Percentage of Participants With at Least a One Point Decrease in the Global Acne Assessment Score (GAAS) at Week 12
NCT01231334 (7) [back to overview]Change From Baseline in Global Acne Assessment Score (GAAS) at Week 12
NCT01231334 (7) [back to overview]Percentage of Participants Demonstrating a ≥ 1 Category Increase in Tolerability From Baseline at Week 12
NCT01313728 (6) [back to overview]Expert Grader Assessment - Dryness
NCT01313728 (6) [back to overview]Expert Grader Assessment - Erythema
NCT01313728 (6) [back to overview]Facial Tolerance
NCT01313728 (6) [back to overview]Subject Assessment - Burning/Stinging
NCT01313728 (6) [back to overview]Subject Assessment - Itching
NCT01313728 (6) [back to overview]Subject Assessment - Tightness
NCT01773122 (2) [back to overview]Maximum Plasma Level (Cmax) of Dapsone Metabolites
NCT01773122 (2) [back to overview]Maximum Plasma Level (Cmax) of Dapsone
NCT01885910 (10) [back to overview]Percentage of Participants Who Remained Responders at Week 24
NCT01885910 (10) [back to overview]Burning
NCT01885910 (10) [back to overview]Dryness
NCT01885910 (10) [back to overview]Erythema
NCT01885910 (10) [back to overview]Inflammatory and Non-inflammatory Lesion Counts
NCT01885910 (10) [back to overview]Nodule Counts
NCT01885910 (10) [back to overview]Oiliness
NCT01885910 (10) [back to overview]Peeling
NCT01885910 (10) [back to overview]Pruritis
NCT01885910 (10) [back to overview]Percentage of Participants Who Are Responders at Week 16 and 20
NCT01931150 (1) [back to overview]Number of Patients in Which the PI Observed a Notable Difference in the Number of Lesions
NCT01974141 (9) [back to overview]Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Oiliness on a the 5-Point ASIS Scale
NCT01974141 (9) [back to overview]Change From Baseline in Total Lesion Counts
NCT01974141 (9) [back to overview]Change From Baseline in the 9-Item ASIS Sign Domain Score
NCT01974141 (9) [back to overview]Change From Baseline in Noninflammatory Facial Lesion Counts
NCT01974141 (9) [back to overview]Change From Baseline in Inflammatory Facial Lesion Counts
NCT01974141 (9) [back to overview]Percentage of Patients With a Score of 0 (None) or 1 (Minimal) on the 5-point Global Acne Assessment Score (GAAS)
NCT01974141 (9) [back to overview]Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Redness on a the 5-Point ASIS Scale
NCT01974141 (9) [back to overview]Percentage Change From Baseline in Total Lesion Counts
NCT01974141 (9) [back to overview]"Percentage of Patients Reporting Very Good or Excellent on Item 10 of the 5-Point Acne Symptom Impact Scale (ASIS)"
NCT01974323 (9) [back to overview]Change From Baseline in Total Lesion Counts
NCT01974323 (9) [back to overview]Change From Baseline in the 9-Item ASIS Sign Domain Score
NCT01974323 (9) [back to overview]Change From Baseline in Noninflammatory Facial Lesion Counts
NCT01974323 (9) [back to overview]"Percentage of Patients Reporting Very Good or Excellent on Item 10 of the 5-Point Acne Symptom Impact Scale (ASIS)"
NCT01974323 (9) [back to overview]Percentage Change From Baseline in Total Lesion Counts
NCT01974323 (9) [back to overview]Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Oiliness on a the 5-Point ASIS Scale
NCT01974323 (9) [back to overview]Change From Baseline in Inflammatory Facial Lesion Counts
NCT01974323 (9) [back to overview]Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Redness on a the 5-Point ASIS Scale
NCT01974323 (9) [back to overview]Percentage of Patients With a Score of 0 (None) or 1 (Minimal) on the 5-point Global Acne Assessment Score (GAAS)
NCT02032407 (8) [back to overview]Percent Change From Baseline in Total Lesion Counts
NCT02032407 (8) [back to overview]Percentage of Participants With 0 (None) or 1 (Minimal) on the GAAS
NCT02032407 (8) [back to overview]Acne Symptom and Impact Scale (ASIS) Sign Domain Score
NCT02032407 (8) [back to overview]ASIS Impact Domain Score
NCT02032407 (8) [back to overview]Change From Baseline in the GAAS
NCT02032407 (8) [back to overview]Change From Baseline in the Global Assessment of Acne Severity (GAAS) Score by Physician
NCT02032407 (8) [back to overview]Percent Change From Baseline in Inflammatory Lesion Counts
NCT02032407 (8) [back to overview]Percent Change From Baseline in Non-Inflammatory Lesion Counts
NCT02944461 (4) [back to overview]Percent of Subjects Who Achieve at Least a Two Grade Improvement and a Rating of Clear or Almost Clear on the Investigator Global Assessment (IGA) Scale
NCT02944461 (4) [back to overview]The Percent Change in Total Lesion Count at Week 16 Compared to Baseline
NCT02944461 (4) [back to overview]The Percent Change in Non-inflammatory Lesion Count at Week 16 Compared to Baseline
NCT02944461 (4) [back to overview]The Percent Change in Inflammatory Lesion Count at Week 16 Compared to Baseline
NCT02959970 (19) [back to overview]Change From Baseline in Height
NCT02959970 (19) [back to overview]Absolute Change From Baseline in Non-inflammatory Lesion Counts
NCT02959970 (19) [back to overview]Absolute Change From Baseline in Total Lesion Counts on Face
NCT02959970 (19) [back to overview]Percent Change From Baseline in Non-inflammatory Lesion Counts
NCT02959970 (19) [back to overview]Percent Change From Baseline in Inflammatory Lesion Counts
NCT02959970 (19) [back to overview]Number of Participants With Adverse Events (AE)
NCT02959970 (19) [back to overview]Change From Baseline in Weight
NCT02959970 (19) [back to overview]Change From Baseline in Respiratory Rate
NCT02959970 (19) [back to overview]Change From Baseline in Heart Rate
NCT02959970 (19) [back to overview]Local Dermal Tolerability: Number of Participants With Stinging/Burning Symptoms as Assessed by Participants
NCT02959970 (19) [back to overview]Peak Plasma Concentration of Dapsone,Dapsone Hydroxylamine and N-acetyl Dapsone at Week 1
NCT02959970 (19) [back to overview]Local Dermal Tolerability: Number of Participants With Dryness, Scaling and Erythema as Assessed by Investigator
NCT02959970 (19) [back to overview]Change From Baseline in Systolic and Diastolic Blood Pressure
NCT02959970 (19) [back to overview]Percentage of Participants With None (0) or Minimal (1) Score Plus at Least a 2-Grade Improvement on the Investigator's Global Assessment (IGA) for Face
NCT02959970 (19) [back to overview]Change From Baseline in Body Temperature
NCT02959970 (19) [back to overview]Absolute Change From Baseline in Inflammatory Lesion Counts
NCT02959970 (19) [back to overview]Trough Plasma Concentration of Dapsone, Dapsone Hydroxylamine and N-acetyl Dapsone at Week 1
NCT02959970 (19) [back to overview]Percentage of Participants With None (0) or Minimal (1) Score on the Investigator's Global Assessment (IGA) for Face
NCT02959970 (19) [back to overview]Percent Change From Baseline in Total Lesion Counts on Face
NCT03681470 (7) [back to overview]"Number of Subjects With Score of 0 or 1 on ASIS Dark Spot Score at Weeks 4, 12, 18 and 24"
NCT03681470 (7) [back to overview]Change From Baseline in Global Acne Assessment Score (GAAS) at Week 4, 18 and 24
NCT03681470 (7) [back to overview]Change From Baseline in Melanin Index (MI) of Target Lesion at Weeks 12, 18 and 24
NCT03681470 (7) [back to overview]Change From Baseline in Post Acne Hyperpigmentation Index (PAHPI) at Weeks 12, 18 and 24
NCT03681470 (7) [back to overview]Number of Subjects With GAAS of 0 (None) or 1 (Minimal) at Weeks 4, 12, 18, 24
NCT03681470 (7) [back to overview]Percent Change From Baseline in All Lesion Counts (Inflammatory, Noninflammatory, and Total) at Weeks 4, 12, 18, and 24
NCT03681470 (7) [back to overview]Mean Change From Baseline to Week 12 in Global Acne Assessment Score (GAAS)

Change From Baseline in Inflammatory Lesion Counts (Papules,Pustules, and Nodules) at Week 12

Change from baseline in inflammatory lesion count (papules, pustules and nodules) at week 12. Papules and nodules are round, solid elevations of the skin with no visible fluid; papules are smaller (less than 5 or 10 millimeters in width and depth) and nodules are larger (greater than 5 or 10 millimeters in width and depth). Pustules are small elevations of the skin containing cloudy material. A negative number change from baseline indicates a reduction in lesion counts (improvement). (NCT00834210)
Timeframe: Baseline, Week 12

,
InterventionNumber of Lesions (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tazarotene Cream 0.1%38.94-25.77
Tazarotene Cream 0.1%40.78-24.82

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Change From Baseline in Investigator Global Assessment at Week 12

Change from baseline in the Investigator Global Assessment (IGA) at week 12. The IGA is a 5-point scale used by the investigator to assess overall acne severity, where 0 equals clear skin (no evidence of acne) and 4 equals severe acne. A negative number change from baseline indicates a reduction in acne severity (improvement). (NCT00834210)
Timeframe: Baseline, Week 12

,
InterventionScores on a scale (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tazarotene Cream 0.1%2.93-1.07
Tazarotene Cream 0.1%3.04-0.96

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Change From Baseline in Non-Inflammatory Lesion Counts (Open and Closed Comedones) at Week 12

"Change from baseline in non-inflammatory lesion counts(open/closed comedones) at week 12. Comedones are small bumps on the skin (lesions) caused by acne and found at the opening of a skin pore. Open comedones (also known as blackheads) have a microscopic opening to the skin surface, while closed comedones (also known as whiteheads or pimples) lack the opening to the skin. A negative number change from baseline indicates a reduction in lesion counts (improvement)." (NCT00834210)
Timeframe: Baseline, Week 12

,
InterventionNumber of lesions (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tazarotene Cream 0.1%46.42-26.73
Tazarotene Cream 0.1%46.48-21.74

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Change From Baseline in Overall Disease Severity at Week 12

Change from baseline in overall disease severity at week 12. The overall disease severity was evaluated by the investigator using a 7-point scale to rate the overall acne severity (lesions, inflammation, facial redness and skin condition), where 0=no acne lesions and 6=most severe acne. A negative number change from baseline indicates a reduction in overall acne disease severity (improvement). (NCT00834210)
Timeframe: Baseline, Week 12

,
InterventionScores on a scale (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tazarotene Cream 0.1%4.03-1.93
Tazarotene Cream 0.1%4.08-1.63

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Change From Baseline in Overall Disease Severity at Week 12

Change from baseline in overall disease severity at week 12. The overall disease severity was evaluated by the investigator using a 7-point scale to rate the overall acne severity (lesions, inflammation, facial redness and skin condition), where 0=no acne lesions and 6=most severe acne. A negative number change from baseline indicates a reduction in overall acne disease severity (improvement). (NCT00835198)
Timeframe: Baseline, Week 12

,
InterventionScores on a scale (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tretinoin Gel 0.025%4.05-1.76
Tretinoin Gel 0.025%4.14-1.79

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Change From Baseline in Non-Inflammatory Lesion Counts (Open and Closed Comedones) at Week 12

"Change from baseline in non-inflammatory lesion counts (open/closed comedones) at week 12. Comedones are small bumps on the skin (lesions) caused by acne and found at the opening of a skin pore. Open comedones (also known as a blackheads) have a microscopic opening to the skin surface, while closed comedones (also known as whiteheads or pimples) lack the opening to the skin. A negative number change from baseline indicates a reduction in lesion counts (improvement)." (NCT00835198)
Timeframe: Baseline, Week 12

,
InterventionNumber of lesions (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tretinoin Gel 0.025%40.69-15.81
Tretinoin Gel 0.025%40.94-19.91

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Change From Baseline in Investigator Global Assessment at Week 12

Change from baseline in the Investigator Global Assessment (IGA) at week 12. The IGA is a 5-point scale used by the investigator to assess overall acne severity, where 0 equals clear skin (no evidence of acne) and 4 equals severe acne. A negative number change from baseline indicates a reduction in acne severity (improvement). (NCT00835198)
Timeframe: Baseline, Week 12

,
InterventionScores on a scale (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tretinoin Gel 0.025%2.99-1.08
Tretinoin Gel 0.025%3.02-1.07

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Change From Baseline in Inflammatory Lesion Counts (Papules, Pustules and Nodules) at Week 12

Change from baseline in inflammatory lesion counts (papules, pustules and nodules) at week 12. Papules and nodules are round, solid elevations of the skin with no visible fluid; papules are smaller (less than 5 or 10 millimeters in width and depth) and nodules are larger (greater than 5 or 10 millimeters in width and depth). Pustules are small elevations of the skin containing cloudy material. A negative number change from baseline indicates a reduction in lesion counts (improvement). (NCT00835198)
Timeframe: Baseline, Week 12

,
InterventionNumber of Lesions (Mean)
BaselineWeek 12
Dapsone Gel 5% and Tretinoin Gel 0.025%40.06-25.82
Tretinoin Gel 0.025%38.96-24.05

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Skin Hydration

Evaluation of Skin Hydration using electrical conductance measurements,on weekdays during 14 days of treatment. The value recorded which is expressed in units of microsiemens represents the AC conductance 2-3 seconds after placing the spring-loaded probe tip to the sample site. (NCT00964366)
Timeframe: 2 weeks

,
InterventionMicrosiemens (Mean)
Baseline4 hours post 1st treatmentDay 3Day 7Day 14
Clindamycin and BPO Gel499.51430.38614.73460.65477.80
Dapsone Gel448.31404.68511.63456.73471.13

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Transepidermal Water Loss (TEWL)

To assess skin moisture and hydration using transepidermal water loss (TEWL). These tables record the data obtained for each panelist at Baseline, and on Days 3, 7 and 14 or upon early termination of site(s), if applicable. Results are measured on a continuous scale. (NCT00964366)
Timeframe: 2 Weeks

,
InterventionTEWL rates (gm/m2/hr) (Mean)
BaselineDay 3Day 7Day 14
Clindamycin and BPO Gel10.2912.3414.3913.88
Dapsone Gel10.411.2111.5311.26

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Sebum Measurements

To sample the skin surface, the sebum collector strips are applied to the skin sites for 10 seconds. Once removed, these samples will be immediately measured for the amount of sebum on the strip using the tape analyzer. The amount of sebum production was measured as the amount of sebum collected on a tape applied to the skin for 10 seconds and then converted to 1 of 10 incremental levels. Sebum production was measured in increments of 0 (minimum value) to 10 (maximum value). The higher the number, the greater amount of sebum produced. (NCT00964366)
Timeframe: 2 weeks

,
Interventionunits on a scale (Mean)
BaselineDay 3Day 7Day 14
Clindamycin and BPO Gel1.721.522.652.35
Dapsone Gel2.181.723.332.38

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Skin Dryness

"The amount of dryness on the left and right cheek of each panelist.~The scale used to evaluate skin dryness is:~Grade Description 0 None 2 Slight flaking 4 Moderate flaking/scaling 6 Marked scaling / slight fissuring 8 Severe scaling, fissuring~Expert Grader assessments of dryness were taken prior to product application on Days 0, 1, 2, 3, 6, 7, 8, 9, 10, 13 and 14." (NCT00964366)
Timeframe: Baseline, Day 1through Day 14

,
InterventionUnits on a scale (Mean)
BaselineDay 1Day 2Day 3Day 6Day 7Day 8Day 9Day 10Day 13Day 14
Clindamycin and BPO Gel0.110.040.100.160.270.210.540.50.570.570.55
Dapsone Gel0.120.280.230.480.370.230.170.100.150.170.12

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Skin Erythema (Redness)

"Assessment of erythema as part of an evaluation of tolerance of two treatments: clindamycin and benzoyl peroxide or dapsone gel. This was done by visual assessment by an independent blinded grader using the grading scale shown below.~Grade Description 0 None 2 Mild erythema 4 Moderate confluent erythema 6 Marked erythema with some edema 8 Marked erythema, edema, possible erosion" (NCT00964366)
Timeframe: 2 Weeks

,
InterventionUnits on a scale (Mean)
BaselineDay 1Day 2Day 3Day 6Day 7Day 8Day 9Day 10Day 13Day 14
Clindamycin and BPO Gel1.061.261.551.321.301.641.801.671.811.522.10
Dapsone Gel1.181.341.331.501.651.531.601.451.851.651.90

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Serum Clearance

Serum clearance of dapsone (NCT01165840)
Timeframe: 72 hours

InterventionL/h (Mean)
Dapsone2.55

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Percent Change From Baseline in Inflammatory Lesion Counts at Week 12

Percent Change from baseline in inflammatory lesion counts (papules, pustules and nodules) at week 12. Papules and nodules are round, solid elevations of the skin with no visible fluid; papules are smaller (less than 5 or 10 millimeters in width and depth) and nodules are larger (greater than 5 or 10 millimeters in width and depth). Pustules are small elevations of the skin containing cloudy material. A negative number change from baseline indicates a reduction in lesion counts (improvement). (NCT01231334)
Timeframe: Baseline, Week 12

InterventionPercent change (Median)
Aczone® Gel 5% Plus Differin® 0.3% Gel-70.7
Duac® Topical Gel Plus Differin® 0.3% Gel-75.9

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Percent Change From Baseline in Non-inflammatory Lesion Counts at Week 12

"Percent Change from baseline in non-inflammatory lesion counts (open/closed comedones) at week 12. Comedones are small bumps on the skin (lesions) caused by acne and found at the opening of a skin pore. Open comedones (also known as a blackheads) have a microscopic opening to the skin surface, while closed comedones (also known as whiteheads or pimples) lack the opening to the skin. A negative number change from baseline indicates a reduction in lesion counts (improvement)." (NCT01231334)
Timeframe: Baseline, Week 12

InterventionPercent change (Median)
Aczone® Gel 5% Plus Differin® 0.3% Gel-55.3
Duac® Topical Gel Plus Differin® 0.3% Gel-60.7

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Percent Change From Baseline in Total Lesion Count at Week 12

Percent change in total lesion counts: inflammatory (papules, pustules and nodules) and non-inflammatory (comedones) lesion counts from baseline. Papules and nodules are round, solid elevations of the skin with no visible fluid; papules are smaller (less than 5 or 10 millimeters ) and nodules are larger (greater than 5 or 10 millimeters). Pustules are small elevations of the skin containing cloudy material. Comedones are small bumps on the skin caused by acne and found at the opening of a skin pore. A negative change from baseline indicates a reduction in lesion counts (improvement). (NCT01231334)
Timeframe: Baseline, Week 12

InterventionPercent change (Median)
Aczone® Gel 5% Plus Differin® 0.3% Gel-62.7
Duac® Topical Gel Plus Differin® 0.3% Gel-65.0

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Percentage of Participants at Week 12 Having at Least a One Point Decrease in Overall Disease Severity

The overall disease severity was evaluated by the investigator at Baseline and Week 12 using a 7-point scale to rate the overall acne severity (lesions, inflammation, facial redness and skin condition), where 0=no acne lesions and 6=most severe acne. The percentage of participants with at least a one point decrease (improvement) from baseline is calculated. (NCT01231334)
Timeframe: Baseline, Week 12

InterventionPercentage of participants (Number)
Aczone® Gel 5% Plus Differin® 0.3% Gel83.5
Duac® Topical Gel Plus Differin® 0.3% Gel92.4

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Percentage of Participants With at Least a One Point Decrease in the Global Acne Assessment Score (GAAS) at Week 12

GAAS was conducted by the investigator at Baseline and Week 12. The patient's facial acne was evaluated on a 5 point scale 0=None (no evidence of acne), 1=Minimal (few lesions), 2=Mild (several to many non-inflammatory lesions; few inflammatory lesions), 3=Moderate (many lesions) to 4=Severe (Significant degree of inflammatory disease; papules/pustules present, few nodulo-cystic lesions; comedones may be present). Papules/nodules are round, solid elevations of the skin with no visible fluid. The percentage of participants with at least a one point decrease (improvement) in GAAS was calculated. (NCT01231334)
Timeframe: Baseline, Week 12

InterventionPercentage of participants (Number)
Aczone® Gel 5% Plus Differin® 0.3% Gel69.7
Duac® Topical Gel Plus Differin® 0.3% Gel81.4

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Change From Baseline in Global Acne Assessment Score (GAAS) at Week 12

GAAS was conducted by the investigator. The patient's facial acne was evaluated on a 5 point scale 0=None (no evidence of acne), 1=Minimal (few lesions), 2=Mild (several to many non-inflammatory lesions; few inflammatory lesions), 3=Moderate (many lesions) to 4=Severe (Significant degree of inflammatory disease; papules/pustules present, few nodulo-cystic lesions; comedones may be present). Papules and nodules are round, solid elevations of the skin with no visible fluid. A negative change from baseline indicates improvement. (NCT01231334)
Timeframe: Baseline, Week 12

,
InterventionScore on a scale (Mean)
BaselineChange from baseline at Week 12
Aczone® Gel 5% Plus Differin® 0.3% Gel2.80-0.87
Duac® Topical Gel Plus Differin® 0.3% Gel2.84-1.27

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Percentage of Participants Demonstrating a ≥ 1 Category Increase in Tolerability From Baseline at Week 12

The investigator rated the patient's current symptoms of erythema, dryness, peeling, and oiliness on a 5 point scale from 0 (Absent) to 4 (Severe). The investigator rated the symptoms of pruritus and burning since last visit on a 6 point scale of 0 (Absent) to 5 (Severe)-interfering with daily activities. Percentage of participants demonstrating a ≥1 category increase (improvement) in tolerability from baseline is calculated. (NCT01231334)
Timeframe: Baseline, Week 12

,
InterventionPercentage of participants (Number)
DrynessPeelingOilinessErythemaPruritusBurning
Aczone® Gel 5% Plus Differin® 0.3% Gel21.311.56.78.212.413.2
Duac® Topical Gel Plus Differin® 0.3% Gel11.99.36.06.88.512.7

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Expert Grader Assessment - Dryness

Ordinal dryness scores (on a scale of 0=none to 8=deep) were collected on weekdays for two weeks and the total daily score (for all subjects) was treated as a single interval measurement for comparative assessment between treatment regimens. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 2000 (highest possible score of 8, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel0.00.61.73.512.614.818.513.620.417.323.5
Tretinoin Gel Alone0.01.82.58.114.219.925.623.037.637.628.3

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Expert Grader Assessment - Erythema

Ordinal erythema scores (on a scale of 0=none to 8=severe scaling and fissuring) were collected on weekdays for two weeks and the total daily score (for all subjects) was treated as a single interval measurement for comparative assessment between treatment regimens. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 2000 (highest possible score of 8, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel0.00.40.41.66.89.710.810.611.611.616.6
Tretinoin Gel Alone0.02.02.06.47.617.120.920.120.423.019.5

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Facial Tolerance

All interval measurements were combined for comparative assessment between treatment regimens. Facial tolerance is the sum of scores from Erythema, Dryness, Burning/Stinging, Itching, and Tightness assessments, reported in Outcome Measures 1-5. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 6250 (highest possible combined score of 25, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel1.06.75.914.936.444.261.951.063.757.772.8
Tretinoin Gel Alone0.010.011.926.545.366.695.193.9124.6115.294.8

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Subject Assessment - Burning/Stinging

Ordinal burning/stinging scores (on a scale of 0=none to 3=severe) were collected on weekdays for two weeks and the total daily score (for all subjects) was treated as a single interval measurement for comparative assessment between treatment regimens. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 750 (highest possible score of 3, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel1.02.61.86.68.77.514.59.611.610.614.6
Tretinoin Gel Alone0.01.62.65.512.29.517.220.225.925.923.2

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Subject Assessment - Itching

Ordinal itching scores (on a scale of 0=none to 3=severe) were collected on weekdays for two weeks and the total daily score (for all subjects) was treated as a single interval measurement for comparative assessment between treatment regimens. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 750 (highest possible score of 3, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel0.01.60.50.62.63.65.65.67.68.67.6
Tretinoin Gel Alone0.02.81.91.82.87.612.412.417.113.49.4

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Subject Assessment - Tightness

Ordinal tightness scores (on a scale of 0=none to 3=severe) were collected on weekdays for two weeks and the total daily score (for all subjects) was treated as a single interval measurement for comparative assessment between treatment regimens. Thus, for the total for the 25 Participants measured, minimum possible score reported below is 0 and maximum is 750 (highest possible score of 3, times 10 days, times 25 subjects). (NCT01313728)
Timeframe: Baseline to 2 Weeks

,
InterventionScores on a Scale (Number)
Day 0 = BaselineDay 1Day 2Day 3Day 4Day 7Day 8Day 9Day 10Day 11Day 14
Dapsone Gel + Tretinoin Gel0.01.51.52.65.78.612.511.612.59.610.5
Tretinoin Gel Alone0.01.82.94.78.512.519.017.220.015.314.4

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Maximum Plasma Level (Cmax) of Dapsone Metabolites

Cmax is the maximum plasma level following multiple doses of dapsone. Plasma is the liquid component of the blood in which the blood cells are suspended. The dapsone metabolites are N-acetyl dapsone and dapsone hydroxylamine. (NCT01773122)
Timeframe: Day 28

,,,
InterventionNanograms/Milliliter (ng/mL) (Mean)
N-Acetyl DapsoneDapsone Hydroxylamine
Dapsone 5% Gel11.71.47
Dapsone Formulation A5.440.908
Dapsone Formulation B6.001.11
Dapsone Formulation C6.471.19

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Maximum Plasma Level (Cmax) of Dapsone

Cmax is the maximum plasma level following multiple doses of dapsone. Plasma is the liquid component of the blood in which the blood cells are suspended. (NCT01773122)
Timeframe: Day 28

InterventionNanograms/Milliliter (ng/mL) (Mean)
Dapsone Formulation A11.7
Dapsone Formulation B14.1
Dapsone Formulation C13.0
Dapsone 5% Gel17.6

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Percentage of Participants Who Remained Responders at Week 24

At week 12 responder had an IGA <3 on a 6-point scale ranging from 0 (clear) to 5 (very severe) and at Week 24 this response was maintained (NCT01885910)
Timeframe: Assessed every 4 weeks, reported at Week 24

Interventionpercentage of particpants (Number)
Aczone/Doxy82

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Burning

the burning severity scale ranges from 0 to 10 with 0 being no burning and 10 being most extreme burning (NCT01885910)
Timeframe: every 4 weeks

Interventionunits on a scale (Mean)
baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy0.10.100

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Dryness

the dryness severity scale ranges from 0 to 4 with 0 being no dryness and 4 being most extreme dryness (NCT01885910)
Timeframe: every 4 weeks

Interventionunits on a scale (Mean)
baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy0.60.30.10.1

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Erythema

the erythema severity scale ranges from 0 to 4 with 0 being no erythema and 4 being most extreme erythema (NCT01885910)
Timeframe: every 4 weeks

Interventionunits on a scale (Mean)
Baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy1.30.70.91.1

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Inflammatory and Non-inflammatory Lesion Counts

(NCT01885910)
Timeframe: Every 4 weeks

,
Interventionlesions (Mean)
baselineweek 16 (n=23,23)week 20 (n=23,23)week 24 (n=22,22)
Aczone/Doxy - Inflammatory27.35.87.37.0
Aczone/Doxy - Non Inflammatory38.310.08.36.6

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Nodule Counts

number of nodules counted (NCT01885910)
Timeframe: every four weeks

Interventionnodules (Mean)
BaselineWeek 16 (N=23)Week 20 (N=23)Week 24 (N=22)
Aczone/Doxy0.40.10.10.3

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Oiliness

the oiliness severity scale ranges from 0 to 10 with 0 being no oiliness and 10 being most extreme oiliness (NCT01885910)
Timeframe: every 4 weeks

Interventionunits on a scale (Mean)
baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy1.60.80.60.3

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Peeling

the peeling severity scale ranges from 0 to 4 with 0 being no peeling and 4 being most extreme peeling (NCT01885910)
Timeframe: every four weeks

Interventionunits on a scale (Mean)
baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy0.40.10.10.1

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Pruritis

the pruritis severity scale ranges from 0 to 5 with 0 being no pruritis and 5 being the most extreme pruritis (NCT01885910)
Timeframe: every 4 weeks

Interventionunits on a scale (Mean)
baselineweek 16 (N=23)week 20 (N=23)week 24 (N=22)
Aczone/Doxy0.40.20.10

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Percentage of Participants Who Are Responders at Week 16 and 20

Responders is the percentage of participants who have an IGA <3 at Week 16 and 20 (NCT01885910)
Timeframe: Assessed every 4 weeks, reported at weeks 16 and 20

Interventionpercentage of participants (Number)
responders at week 16responders at week 20
Aczone/Doxy7887

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Number of Patients in Which the PI Observed a Notable Difference in the Number of Lesions

Change from Baseline in the Number of Lesions at 28 days (NCT01931150)
Timeframe: 28 days

Interventionparticipants (Number)
Dapsone LEFT, Moisturizer RIGHT4
Dapsone RIGHT, Moisturizer LEFT4

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Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Oiliness on a the 5-Point ASIS Scale

The patient assessed their facial oiliness using item 1 on the 5-point ASIS. Item 1 scores ranged from 0 (Not at all oily) to 4 (Very oily). The percentage of patients who reported at least a 1-grade improvement from baseline in their facial oiliness are reported. (NCT01974141)
Timeframe: Baseline, Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel45.7
Dapsone Gel Vehicle51.8

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Change From Baseline in Total Lesion Counts

The Investigator evaluated the patient's inflammatory (papule, pustule and nodule/cyst) and non-inflammatory (blackhead and whitehead) lesions. A papule is a small, red, solid elevation less than 1.0 cm in diameter, a pustule is a small, circumscribed elevation of the skin that contains yellow-white exudate and a nodule/cyst is a circumscribed, elevated, solid lesion generally more than 0.5 cm in diameter with palpable depth. The total lesion count was the sum of the inflammatory and non-inflammatory lesion counts. A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974141)
Timeframe: Baseline, Week 12

,
InterventionTotal Lesion Counts (Least Squares Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel75.9-36.9
Dapsone Gel Vehicle78.1-31.7

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Change From Baseline in the 9-Item ASIS Sign Domain Score

The patient assessed signs of acne vulgaris using the ASIS. The sign domain is a composite of 9 items of the 17 items on the overall scale. Each of the items is assessed on a 5-point scale: 0 (best) to 4 (worst). The sign domain score is calculated as the average of the 9 items for a total possible score of 0 to 4. A negative number change from baseline indicates an improvement and a positive number change from baseline indicates a worsening. (NCT01974141)
Timeframe: Baseline, Week 12

,
InterventionScores on a Scale (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel4.2-0.73
Dapsone Gel Vehicle4.2-0.69

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Change From Baseline in Noninflammatory Facial Lesion Counts

The Investigator evaluated the patient's noninflammatory lesions (papule, pustule and nodule/cyst). A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974141)
Timeframe: Baseline, Week 12

,
InterventionNumber of Noninflammatory Lesions (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel47.0-20.8
Dapsone Gel Vehicle48.7-17.6

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Change From Baseline in Inflammatory Facial Lesion Counts

The Investigator evaluated the patient's inflammatory lesions (papule, pustule and nodule/cyst). A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974141)
Timeframe: Baseline, Week 12

,
InterventionNumber of Inflammatory Lesions (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel29.0-16.1
Dapsone Gel Vehicle29.4-14.1

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Percentage of Patients With a Score of 0 (None) or 1 (Minimal) on the 5-point Global Acne Assessment Score (GAAS)

The Investigator evaluated the patient's acne severity using the 5-point GAAS scale with 0 being none and 4 being severe. The complete scale is as follow: Grade 0 (none) = No evidence of facila acne vulgaris; Grade 1 (minimal) = Few noninflammatory lesions (comedones) are present, a few inflammatory lesions (papules/pustules) may be present, no nodulo-cyctic lesions are allowed; Grade 2 (mild) = Several to many noninflammatory lesions (comedones) are present, a few inflammatory lesions (papules/pustules) are present, no nodulo-cystic lesions are allowed; Grade 3 (moderate) = Many noninflammatory (comedones) and inflammatory lesions (papules/pustules) are present, no nodulo-cystic lesions are allowed; Grade 4 (severe) = Significant degree of inflammatory disease, papules/pustules are a predominant feature, a few nodulo-cystic lesions may be present, comedones may be present. (NCT01974141)
Timeframe: Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel29.9
Dapsone Gel Vehicle21.2

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Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Redness on a the 5-Point ASIS Scale

The patient assessed their facial redness using item 8 on the 5-point ASIS. Item 8 scores ranged from 0 (Not at all red) to 4 (Very red). The percentage of patients who reported at least a 1-grade improvement from baseline in their facial redness are reported. (NCT01974141)
Timeframe: Baseline, Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel55.6
Dapsone Gel Vehicle53.0

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Percentage Change From Baseline in Total Lesion Counts

The Investigator evaluated the patient's Inflammatory (papule, pustule and nodule/cyst) and Non-inflammatory (blackhead and whitehead) lesions. A papule is a small, red, solid elevation less than 1.0 cm in diameter, a pustule is a small, circumscribed elevation of the skin that contains yellow-white exudate and a nodule/cyst is a circumscribed, elevated, solid lesion generally more than 0.5 cm in diameter with palpable depth. The total lesion count was the sum of the inflammatory and non-inflammatory lesion counts. A negative percent change from baseline indicates a reduction in lesion counts (improvement) and a positive percent change from baseline indicates an increase in lesion counts (worsening). (NCT01974141)
Timeframe: Baseline, Week 12

InterventionPercent Change in Lesion Count (Least Squares Mean)
Dapsone Gel-48.7
Dapsone Gel Vehicle-42.4

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"Percentage of Patients Reporting Very Good or Excellent on Item 10 of the 5-Point Acne Symptom Impact Scale (ASIS)"

"The patient assessed the impact of their acne vulgaris on the look of their face using item 10 on the 5-point ASIS. Item 10 scores range from 1 (Excellent) to 5 (Bad). The percentage of patients who had an ASIS score of 4 (Fair) or 5 (Bad) at baseline and who reported Very good or Excellent at Week 12 are reported." (NCT01974141)
Timeframe: Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel23.8
Dapsone Gel Vehicle19.2

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Change From Baseline in Total Lesion Counts

The Investigator evaluated the patient's inflammatory (papule, pustule and nodule/cyst) and non-inflammatory (blackhead and whitehead) lesions. A papule is a small, red, solid elevation less than 1.0 cm in diameter, a pustule is a small, circumscribed elevation of the skin that contains yellow-white exudate and a nodule/cyst is a circumscribed, elevated, solid lesion generally more than 0.5 cm in diameter with palpable depth. The total lesion count was the sum of the inflammatory and non-inflammatory lesion counts. A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974323)
Timeframe: Baseline, Week 12

,
InterventionTotal Lesion Counts (Least Squares Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel76.4-36.2
Dapsone Gel Vehicle76.9-32.3

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Change From Baseline in the 9-Item ASIS Sign Domain Score

The patient assessed signs of acne vulgaris using the ASIS. The sign domain is a composite of 9 items of the 17 items on the overall scale. Each of the items is assessed on a 5-point scale: 0 (best) to 4 (worst). The sign domain score is calculated as the average of the 9 items for a total possible score of 0 to 4. A negative number change from baseline indicates an improvement and a positive number change from baseline indicates a worsening. (NCT01974323)
Timeframe: Baseline, Week 12

,
InterventionScores on a Scale (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel2.04-0.74
Dapsone Gel Vehicle2.07-0.68

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Change From Baseline in Noninflammatory Facial Lesion Counts

The Investigator evaluated the patient's noninflammatory lesions (papule, pustule and nodule/cyst). A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974323)
Timeframe: Baseline, Week 12

,
InterventionNumber of Noninflammatory Lesions (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel46.7-20.8
Dapsone Gel Vehicle46.7-18.7

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"Percentage of Patients Reporting Very Good or Excellent on Item 10 of the 5-Point Acne Symptom Impact Scale (ASIS)"

"The patient assessed the impact of their acne vulgaris on the look of their face using item 10 on the 5-point ASIS. Item 10 scores range from 1 (Excellent) to 5 (Bad). The percentage of patients who had an ASIS score of 4 (Fair) or 5 (Bad) at baseline and who reported Very good or Excellent at Week 12 are reported." (NCT01974323)
Timeframe: Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel24.2
Dapsone Gel Vehicle22.0

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Percentage Change From Baseline in Total Lesion Counts

The Investigator evaluated the patient's Inflammatory (papule, pustule and nodule/cyst) and Non-inflammatory (blackhead and whitehead) lesions. A papule is a small, red, solid elevation less than 1.0 cm in diameter, a pustule is a small, circumscribed elevation of the skin that contains yellow-white exudate and a nodule/cyst is a circumscribed, elevated, solid lesion generally more than 0.5 cm in diameter with palpable depth. The total lesion count was the sum of the inflammatory and non-inflammatory lesion counts. A negative percent change from baseline indicates a reduction in lesion counts (improvement) and a positive percent change from baseline indicates an increase in lesion counts (worsening). (NCT01974323)
Timeframe: Baseline, Week 12

InterventionPercent Change in Lesion Count (Least Squares Mean)
Dapsone Gel-48.9
Dapsone Gel Vehicle-43.2

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Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Oiliness on a the 5-Point ASIS Scale

The patient assessed their facial oiliness using item 1 on the 5-point ASIS. Item 1 scores ranged from 0 (Not at all oily) to 4 (Very oily). The percentage of patients who reported at least a 1-grade improvement from baseline in their facial oiliness are reported. (NCT01974323)
Timeframe: Baseline, Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel48.5
Dapsone Gel Vehicle49.3

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Change From Baseline in Inflammatory Facial Lesion Counts

The Investigator evaluated the patient's inflammatory lesions (papule, pustule and nodule/cyst). A negative change from baseline indicates a reduction in lesion counts (improvement) and a positive change from baseline indicates an increase in lesion counts (worsening). (NCT01974323)
Timeframe: Baseline, Week 12

,
InterventionNumber of Inflammatory Lesions (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel29.6-15.6
Dapsone Gel Vehicle30.0-14.0

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Percentage of Patients Reporting at Least a 1-Grade Improvement From Baseline in Facial Redness on a the 5-Point ASIS Scale

The patient assessed their facial redness using item 8 on the 5-point ASIS. Item 8 scores ranged from 0 (Not at all red) to 4 (Very red). The percentage of patients who reported at least a 1-grade improvement from baseline in their facial redness are reported. (NCT01974323)
Timeframe: Baseline, Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel53.8
Dapsone Gel Vehicle52.9

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Percentage of Patients With a Score of 0 (None) or 1 (Minimal) on the 5-point Global Acne Assessment Score (GAAS)

The Investigator evaluated the patient's acne severity using the 5-point GAAS scale with 0 being none and 4 being severe. The complete scale is as follow: Grade 0 (none) = No evidence of facila acne vulgaris; Grade 1 (minimal) = Few noninflammatory lesions (comedones) are present, a few inflammatory lesions (papules/pustules) may be present, no nodulo-cyctic lesions are allowed; Grade 2 (mild) = Several to many noninflammatory lesions (comedones) are present, a few inflammatory lesions (papules/pustules) are present, no nodulo-cystic lesions are allowed; Grade 3 (moderate) = Many noninflammatory (comedones) and inflammatory lesions (papules/pustules) are present, no nodulo-cystic lesions are allowed; Grade 4 (severe) = Significant degree of inflammatory disease, papules/pustules are a predominant feature, a few nodulo-cystic lesions may be present, comedones may be present. (NCT01974323)
Timeframe: Week 12

InterventionPercentage of Patients (Number)
Dapsone Gel29.8
Dapsone Gel Vehicle20.9

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Percent Change From Baseline in Total Lesion Counts

The investigator evaluated Inflammatory (papule, pustule and nodule/cyst) and Non-inflammatory (blackhead and whitehead) lesions. A papule is a small, red, solid elevation less than 1.0 cm in diameter, a pustule is a small, circumscribed elevation of the skin that contains yellow-white exudate and a nodule/cyst is a circumscribed, elevated, solid lesion generally more than 0.5 cm in diameter with palpable depth. The total lesion count was the sum of the inflammatory and non-inflammatory lesion counts. A negative percent change from baseline indicates a reduction in lesion counts (improvement). (NCT02032407)
Timeframe: Baseline, Weeks 2, 6 and 12

Interventionpercent change (Mean)
Change from Baseline at Week 2Change from Baseline at Week 6 (n=61)Change from Baseline at Week 12 (n=63)
Dapsone Gel-16.0-30.0-52.0

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Percentage of Participants With 0 (None) or 1 (Minimal) on the GAAS

The investigator evaluated the participant's acne severity using the 5-point GAAS grading scale: 0= No evidence of facial acne vulgaris to 4= Significant degree of inflammatory disease; papules/pustules were a predominant feature; a few nodulo-cystic lesions could have been present; comedones (small pumps on the skin caused by acne) could have been present. The percentage of participants with a score of 0=none or 1=minimal is reported. (NCT02032407)
Timeframe: Weeks 2, 6 and 12

Interventionpercentage of participants (Number)
Week 2Week 6 (n=61)Week 12 (n=63)
Dapsone Gel6.013.142.9

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Acne Symptom and Impact Scale (ASIS) Sign Domain Score

The participant assessed signs of acne vulgaris using the ASIS. The sign domain is a composite of 9 items of the 17 items on the overall scale. Each of the items is answered on a 5-point scale: 0 (best) to 4 (worst). The sign domain score is calculated as the average of the 9 items for a total possible score of 0 to 4. Higher scores indicate the presence of more severe signs of acne. (NCT02032407)
Timeframe: Weeks 2, 6 and 12

Interventionscore on a scale (Mean)
Week 2Week 6 (n=60)Week 12 (n=63)
Dapsone Gel1.71.31.1

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ASIS Impact Domain Score

The participant assessed the impact of acne vulgaris using the ASIS. The impact domain is a composite of 8 items assessing the psychosocial impacts (6 items emotional and 2 items social) of the 17 items on the overall scale. Each of the items is answered on a 5-point scale: 0 (best) to 4 (worst). The impact domain score is calculated as the average of the 8 items for a total possible score of 0 to 4. Higher scores on the ASIS Impact Domain indicate greater negative impact of acne on health-related quality of life and appearance. (NCT02032407)
Timeframe: Weeks 2, 6 and 12

Interventionscore on a scale (Mean)
Week 2Week 6 (n=60)Week 12 (n=63)
Dapsone Gel1.61.31.1

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Change From Baseline in the GAAS

The investigator evaluated the participant's acne severity using the 5-point GAAS grading scale: 0= No evidence of facial acne vulgaris to 4= Significant degree of inflammatory disease; papules/pustules were a predominant feature; a few nodulo-cystic lesions could have been present; comedones (small pumps on the skin caused by acne) could have been present. A negative change from Baseline indicated improvement. (NCT02032407)
Timeframe: Baseline, Weeks 2 and 6

Interventionscore on a scale (Mean)
BaselineChange from Baseline at Week 2Change from Baseline at Week 6
Dapsone Gel2.8-0.3-0.6

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Change From Baseline in the Global Assessment of Acne Severity (GAAS) Score by Physician

The investigator evaluated the participant's acne severity using the 5-point GAAS grading scale: 0= No evidence of facial acne vulgaris to 4= Significant degree of inflammatory disease; papules/pustules were a predominant feature; a few nodulo-cystic lesions could have been present; comedones (small pumps on the skin caused by acne) could have been present. A negative change from Baseline indicated improvement. (NCT02032407)
Timeframe: Baseline, Week 12

Interventionscore on a scale (Mean)
BaselineChange from Baseline at Week 12
Dapsone Gel2.8-1.2

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Percent Change From Baseline in Inflammatory Lesion Counts

The investigator evaluated Inflammatory lesions (papule, pustule and nodule/cyst). A negative percent change from baseline indicates a reduction in lesion counts (improvement). (NCT02032407)
Timeframe: Baseline, Weeks 2, 6 and 12

Interventionpercent change (Mean)
Change from Baseline at Week 2Change from Baseline at Week 6 (n=61)Change from Baseline at Week 12 (n=63)
Dapsone Gel-25.0-48.0-65.0

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Percent Change From Baseline in Non-Inflammatory Lesion Counts

The investigator evaluated Non-inflammatory (blackhead and whitehead) lesions. A negative percent change from baseline indicates a reduction in lesion counts (improvement). (NCT02032407)
Timeframe: Baseline, Weeks 2, 6 and 12

Interventionpercent change (Mean)
Change from Baseline at Week 2Change from Baseline at Week 6 (n=61)Change from Baseline at Week 12 (n=63)
Dapsone Gel-9.8-16.0-41.0

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Percent of Subjects Who Achieve at Least a Two Grade Improvement and a Rating of Clear or Almost Clear on the Investigator Global Assessment (IGA) Scale

Investigator will evaluate global acne severity using the IGA scale as follows: 1= Clear Skin, 2 = Almost Clear, 3 = Mild Severity, 4 = Severe, 5 = Very Severe (NCT02944461)
Timeframe: 16 weeks

InterventionParticipants (Count of Participants)
week 4week 10week 16
Dapsone Gel 7.5%037

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The Percent Change in Total Lesion Count at Week 16 Compared to Baseline

(NCT02944461)
Timeframe: 16 Weeks

Interventionpercent change in lesion count (Mean)
Dapsone Gel 7.5%-73

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The Percent Change in Non-inflammatory Lesion Count at Week 16 Compared to Baseline

(NCT02944461)
Timeframe: 16 Weeks

Interventionpercent change in lesion count (Mean)
Dapsone Gel 7.5%-72

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The Percent Change in Inflammatory Lesion Count at Week 16 Compared to Baseline

(NCT02944461)
Timeframe: 16 Weeks

Interventionpercent change in lesion count (Mean)
Dapsone Gel 7.5%-74

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Change From Baseline in Height

Change from baseline in height was assessed. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventioncentimeter (cm) (Mean)
PK Cohort: ACZONE 7.5%0.21
Non-PK Cohort: ACZONE 7.5%1.01

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Absolute Change From Baseline in Non-inflammatory Lesion Counts

Non-inflammatory lesion counts were defined as the sum of counts of the following lesion type (face only): open comedone - a pigmented dilated pilosebaceous orifice (blackhead); closed comedone - a tiny white papule (whitehead). Change from baseline was be calculated by subtracting post-dose value from the baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionlesions (Mean)
ACZONE 7.5%-17.8

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Absolute Change From Baseline in Total Lesion Counts on Face

Total lesion counts were defined as the sum of inflammatory lesion counts and noninflammatory lesion counts (face only). Change from baseline was be calculated by subtracting post-dose value from the baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionlesions (Mean)
ACZONE 7.5%-24.0

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Percent Change From Baseline in Non-inflammatory Lesion Counts

Noninflammatory lesion counts were defined as the sum of counts of the following lesion type (face only): open comedone - a pigmented dilated pilosebaceous orifice (blackhead); closed comedone - a tiny white papule (whitehead). (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionpercent change (Mean)
ACZONE 7.5%-46.45

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Percent Change From Baseline in Inflammatory Lesion Counts

Inflammatory lesion counts were the sum of counts of the following lesion types (face only): Papule - a small, red, solid elevation less than 1.0 cm in diameter; Pustule - a small, circumscribed elevation of the skin that contains yellow-white exudate; Nodule - a circumscribed, elevated, solid lesion generally more than 1.0 cm in diameter with palpable depth; Cyst - a smooth, dome-shaped, elevated, freely moveable, skin colored, round to ovoid lesion greater than 0.7 cm in diameter. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionpercent change (Mean)
ACZONE 7.5%-56.38

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Number of Participants With Adverse Events (AE)

"An AE was defined as any untoward medical occurrence in a clinical trial participant (regardless of the administration of the study drug and its causal relationship to it). An AE could therefore, be any unfavorable and unintended medical occurrence during the participant's participation in the trial, including deterioration of a pre-existing medical condition, an abnormal clinically significant finding in a laboratory assessment, or an abnormal clinically significant finding in the physical examination or vital sign." (NCT02959970)
Timeframe: From Baseline (Day 1) until Week 12

InterventionParticipants (Count of Participants)
PK Cohort: ACZONE 7.5%5
Non-PK Cohort: ACZONE 7.5%16

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Change From Baseline in Weight

Change from baseline in weight was assessed. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionkilogram (kg) (Mean)
PK Cohort: ACZONE 7.5%0.70
Non-PK Cohort: ACZONE 7.5%1.48

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Change From Baseline in Respiratory Rate

Change from baseline in respiratory rate was assessed. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionbreaths per minute (breaths/min) (Mean)
PK Cohort: ACZONE 7.5%0.5
Non-PK Cohort: ACZONE 7.5%-0.1

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Change From Baseline in Heart Rate

Change from baseline in heart rate was evaluated. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionbeats per minute (beats/min) (Mean)
PK Cohort: ACZONE 7.5%-0.8
Non-PK Cohort: ACZONE 7.5%0.6

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Local Dermal Tolerability: Number of Participants With Stinging/Burning Symptoms as Assessed by Participants

Local dermal tolerability was evaluated by participants in terms of presence and absence of prickling pain sensation immediately after (within 5 minutes of dosing) and its severity in the areas of body where medication was applied (face). Stinging/burning symptoms were graded on a 4-point scale of 0 - 3 where 0 = none (no stinging/burning), 1 = mild (slight warm, tingling/stinging sensation; not really bothersome), 2 = moderate (definite warm, tingling/stinging sensation that is somewhat bothersome), 3 = severe (hot, tingling/stinging sensation that has caused definite discomfort). The higher score indicated severe symptoms. (NCT02959970)
Timeframe: Week 12

,
Interventionparticipants (Number)
None (0)Mild (1)Moderate (2)Severe (3)
Non-PK Cohort: ACZONE 7.5%75200
PK Cohort: ACZONE 7.5%15000

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Peak Plasma Concentration of Dapsone,Dapsone Hydroxylamine and N-acetyl Dapsone at Week 1

The mean plasma peak (10 hours postdose) concentrations of dapsone, dapsone hydroxylamine and N-acetyl dapsone were reported. (NCT02959970)
Timeframe: Week 1 (Pre-dose and 10 hours post-dose)

Interventionnanogram per milliter (ng/mL) (Mean)
DapsoneDapsone hydroxylamineN-acetyl dapsone
PK Cohort: ACZONE 7.5%20.01.409.01

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Local Dermal Tolerability: Number of Participants With Dryness, Scaling and Erythema as Assessed by Investigator

Local dermal tolerability was evaluated by investigator in terms of presence and absence of dryness, scaling and erythema symptoms and its severity in the areas of body where medication was applied. These symptoms were assessed by using a 4 - point scale of 0 - 3, where 0 = none (no dryness, scaling and erythema) and 3 = severe (marked roughness, heavy scale production and intense redness). The higher score indicated severe symptoms. (NCT02959970)
Timeframe: Week 12

,
Interventionparticipants (Number)
Dryness: None (0)Dryness: Mild (1)Dryness: Moderate (2)Dryness: Severe (3)Scaling: None (0)Scaling: Mild (1)Scaling: Moderate (2)Scaling: Severe (3)Erythema: None (0)Erythema: Mild (1)Erythema: Moderate (2)Erythema: Severe (3)
Non-PK Cohort: ACZONE 7.5%7160070610651200
PK Cohort: ACZONE 7.5%150001500013200

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Change From Baseline in Systolic and Diastolic Blood Pressure

Change from baseline in systolic and diastolic blood pressure was evaluated. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

,
Interventionmillimeter of mercury (mmHg) (Mean)
Systolic Blood PressureDiastolic Blood Pressure
Non-PK Cohort: ACZONE 7.5%0.10.4
PK Cohort: ACZONE 7.5%3.92.3

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Percentage of Participants With None (0) or Minimal (1) Score Plus at Least a 2-Grade Improvement on the Investigator's Global Assessment (IGA) for Face

Overall severity of acne vulgaris was evaluated by using a 5-point IGA scale: Clear (0) - (no comedones; papules or pustules, residual hyperpigmentation and erythema may be present); Almost clear (1) - (rare comedones; no more than a few small papules and pustules); Mild (2) - (easily recognizable comedones in limited numbers; +/- presence of small papules and pustules); Moderate (3) - (many comedones; +/- easily recognizable small and medium-sized papules; no nodules or cysts; Severe (4) - (widespread and numerous comedones; many small, medium-sized and large papules and pustules; nodules or cysts may or may not be present). (NCT02959970)
Timeframe: Week 12

Interventionpercentage of participants (Number)
ACZONE 7.5%19.6

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Change From Baseline in Body Temperature

Change from baseline in body temperature was assessed. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventiondegree celsius (°C) (Mean)
PK Cohort: ACZONE 7.5%0.08
Non-PK Cohort: ACZONE 7.5%0.10

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Absolute Change From Baseline in Inflammatory Lesion Counts

Inflammatory lesion counts were the sum of counts of the following lesion types (face only): Papule - a small, red, solid elevation less than (<) 1.0 centimeter (cm) in diameter; Pustule - a small, circumscribed elevation of the skin that contains yellow-white exudate; Nodule - a circumscribed, elevated, solid lesion generally more than 1.0 cm in diameter with palpable depth; Cyst - a smooth, dome-shaped, elevated, freely moveable, skin-colored, round to ovoid lesion greater than 0.7 cm in diameter. Change from baseline was calculated by subtracting post-dose value from baseline value. (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionlesions (Mean)
ACZONE 7.5%-6.2

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Trough Plasma Concentration of Dapsone, Dapsone Hydroxylamine and N-acetyl Dapsone at Week 1

The trough plasma concentrations of Dapsone, Dapsone hydroxylamine and N-acetyl dapsone were reported. (NCT02959970)
Timeframe: Week 1 (Pre-dose)

Interventionng/mL (Mean)
DapsoneDapsone hydroxylamineN-acetyl dapsone
PK Cohort: ACZONE 7.5%17.21.057.02

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Percentage of Participants With None (0) or Minimal (1) Score on the Investigator's Global Assessment (IGA) for Face

Overall severity of acne vulgaris was evaluated by using a 5-point IGA scale: Clear (0) - (no comedones; papules or pustules, residual hyperpigmentation and erythema may be present); Almost clear (1) - (rare comedones; no more than a few small papules and pustules); Mild (2) - (easily recognizable comedones in limited numbers; +/- presence of small papules and pustules); Moderate (3) - (many comedones; +/- easily recognizable small and medium-sized papules; no nodules or cysts; Severe (4) - (widespread and numerous comedones; many small, medium-sized and large papules and pustules; nodules or cysts may or may not be present). (NCT02959970)
Timeframe: Week 12

Interventionpercentage of participants (Number)
ACZONE 7.5%46.7

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Percent Change From Baseline in Total Lesion Counts on Face

Total lesion counts were defined as the sum of inflammatory lesion counts and noninflammatory lesion counts (face only). (NCT02959970)
Timeframe: Baseline (Day 1), Week 12

Interventionpercent change (Mean)
ACZONE 7.5%-51.91

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"Number of Subjects With Score of 0 or 1 on ASIS Dark Spot Score at Weeks 4, 12, 18 and 24"

The participant assesses signs of acne vulgaris using the Acne Symptom and Impact Scale (ASIS). The sign domain is a composite of 9 items of the 17 items on the overall scale. Each of the items is answered on a 5-point scale: 0 (best) to 4 (worst). Total possible score of 0 to 68. Higher scores indicate the presence of more severe symptoms and poorer outcomes on acne health-related quality of life. (NCT03681470)
Timeframe: week 4, 12, 18, and 24

InterventionParticipants (Count of Participants)
week 4week 12week 18week 24
Patients With Acne Vulgaris2247

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Change From Baseline in Global Acne Assessment Score (GAAS) at Week 4, 18 and 24

"Change from baseline at week 4, week 18 and week 24.~GAAS assesses acne severity on a 5-point score:~0 - None: No evidence of facial acne vulgaris.~- Minimal: Few noninflammatory lesions are present; a few inflammatory lesions (papules/pustules) may be present; no nodulo-cystic lesions present.~- Mild: Several to many noninflammatory lesions are present; a few inflammatory lesions are present; no nodulo-cystic lesions present.~- Moderate: Many noninflammatory and inflammatory lesions are present; no nodulo-cystic lesions are present.~- Severe: Significant degree of inflammatory disease; papules and pustules are a predominant feature; a few nodulo-cystic lesions are present (no more than 2)" (NCT03681470)
Timeframe: baseline and week 4, week 18, and week 24

Interventionscore on a scale (Mean)
Baseline and Week 4Baseline and Week 18Baseline and Week 24
Patients With Acne Vulgaris-0.35-1.0-1.2

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Change From Baseline in Melanin Index (MI) of Target Lesion at Weeks 12, 18 and 24

"A narrowband reflectance spectrophotometer (mexameter MX-16) will be used to measure the degree of pigmentation of involved and adjacent uninvolved skin of one representation facial PIH lesion.~The mexameter contains 16 light emitting diodes arranged circularly that emit light at wavelengths of 568nm (green), 660nm (red), and 880nm (near infrared). The machine then measures the amount of light absorbed and reflected by the skin to measure the melanin content (melanin index or M - red and near infrared light).~There is no minimum or maximum to this index. Higher melanin index indicates more melanin content in the skin. Higher or increase MI indicates poorer health outcomes." (NCT03681470)
Timeframe: baseline and week 12, 18 and 24

InterventionMelanin Index (M) (Mean)
baseline and week12baseline and week 18baseline and week 24
Patients With Acne Vulgaris0.22-2.33-48.5

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Change From Baseline in Post Acne Hyperpigmentation Index (PAHPI) at Weeks 12, 18 and 24

"Change from baseline at weeks 12, 18, and 24.~PAHPI will be scored using the following formula:~Weighted Total PAHPI = S (lesion size) + I (lesion intensity) + N (lesion number). Total PAHPI Score can range from 6-22, with higher number indicating more pigmentation." (NCT03681470)
Timeframe: baseline and week 12, 18, and 24

Interventionscore on a scale (Mean)
baseline and week 12baseline and week 18baseline and week 24
Patients With Acne Vulgaris-1.7-2.22-3

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Number of Subjects With GAAS of 0 (None) or 1 (Minimal) at Weeks 4, 12, 18, 24

"The change in the proportion of subjects with GAAS scores equal to 0 (or 1) from baseline.~GAAS assesses acne severity:~0 - None: No evidence of facial acne vulgaris.~1 - Minimal: Few noninflammatory lesions are present; a few inflammatory lesions (papules/pustules) may be present; no nodulo-cystic lesions present." (NCT03681470)
Timeframe: Week 4, 12, 18 and 24

InterventionParticipants (Count of Participants)
Week 4Week12Week 18Week 24
Patients With Acne Vulgaris0234

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Percent Change From Baseline in All Lesion Counts (Inflammatory, Noninflammatory, and Total) at Weeks 4, 12, 18, and 24

(NCT03681470)
Timeframe: Baseline, Week 4, 12, 18, and 24

Interventionpercent change (Mean)
Baseline and week 4Baseline and week 12Baseline and week 18Baseline and week 24
Patients With Acne Vulgaris-29-46-55-53

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Mean Change From Baseline to Week 12 in Global Acne Assessment Score (GAAS)

"GAAS assesses acne severity on a 5-point score:~0 - None: No evidence of facial acne vulgaris.~- Minimal: Few noninflammatory lesions are present; a few inflammatory lesions (papules/pustules) may be present; no nodulo-cystic lesions present.~- Mild: Several to many noninflammatory lesions are present; a few inflammatory lesions are present; no nodulo-cystic lesions present.~- Moderate: Many noninflammatory and inflammatory lesions are present; no nodulo-cystic lesions are present.~- Severe: Significant degree of inflammatory disease; papules and pustules are a predominant feature; a few nodulo-cystic lesions are present (no more than 2)" (NCT03681470)
Timeframe: baseline and week 12

Interventionscore on a scale (Mean)
Patients With Acne Vulgaris-0.86

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