deferiprone profile

Deferiprone (DFP) is a chelating agent used to treat iron overload in patients with thalassemia and other blood disorders. It was originally synthesized in the 1970s and its use as an iron chelator was discovered shortly after. Deferiprone is a small molecule with a high affinity for iron and forms a stable complex with it. This allows the body to excrete excess iron through the urine. The compound has been shown to be effective in reducing iron overload and improving survival rates in patients with thalassemia. It is also being investigated for its potential use in treating other iron-related diseases, such as hemochromatosis. Deferiprone is typically administered orally. It is relatively well-tolerated, although it can cause side effects such as nausea, vomiting, and diarrhea. In rare cases, it can also cause more serious side effects, such as agranulocytosis (a low white blood cell count). Therefore, close monitoring of patients receiving deferiprone is necessary. Deferiprone is a promising treatment option for iron overload, but further research is needed to optimize its use and minimize its side effects.'

Deferiprone: A pyridone derivative and iron chelator that is used in the treatment of IRON OVERLOAD in patients with THALASSEMIA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

deferiprone : A member of the class of 4-pyridones that is pyridin-4(1H)-one substituted at positions 1 and 2 by methyl groups and at position 3 by a hydroxy group. A lipid-soluble iron-chelator used for treatment of thalassaemia. [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]

ID Source	ID
PubMed CID	2972
CHEMBL ID	70927
CHEBI ID	68554
SCHEMBL ID	94474
MeSH ID	M0130907

Synonym
HMS3393C05
NCGC00090548-02
3-hydroxy-1,2-dimethyl-4(1h)-pyridone
smr000059136
MLS000069481 ,
deferiprone (inn)
dn-180-01-af
cp020
ferriprox
l1
deferum
crmd-001
apo-066
cgp-37391
brn 1447108
4(1h)-pyridone, 3-hydroxy-1,2-dimethyl-
1,2-dimethyl-3-hydroxy-4(1h)-pyridinone
1,2-dimethyl-3-hydroxypyrid-4-one
cp20 (chelating agent)
D07416
ferriprox (tn)
deferiprone (usan/inn)
deferiprone
30652-11-0
4(1h)-pyridinone, 1,2-dimethyl-3-hydroxy-
3-hydroxy-1,2-dimethyl-pyridin-4-one
hk-1
cp20
PL1 ,
MLS000758227
3-hydroxy-1,2-dimethyl-4(1h)-pyridone, 98%
NCGC00090548-01
3-hydroxy-1,2-dimethyl-4-pyridinone
1,2-dimethyl-3-hydroxy-4-pyridinone
1,2-dimethyl-3-hydroxypyridin-4-one
dmohpo
3-hydroxy-1,2-dimethylpyridin-4(1h)-one
HMS2051C05
pl-1
dn-18001af
chebi:68554 ,
cp-20
l-1
apo-66
CHEMBL70927
nsc-758880
deferipron
inchi=1/c7h9no2/c1-5-7(10)6(9)3-4-8(5)2/h3-4,10h,1-2h3
tzxkocqbrnjulo-uhfffaoysa-
H0944
3-hydroxy-1,2-dimethylpyridin-4-one
HMS3264P17
cas-30652-11-0
dtxsid6040666 ,
tox21_112429
dtxcid4020666
A820470
nsc758880
MLS001424029
pharmakon1600-01504512
HMS2232E24
S4067
CCG-100760
nsc 758880
unii-2bty8kh53l
deferiprone [usan:inn:ban]
ccris 8318
2bty8kh53l ,
hsdb 8335
FT-0606424
deferiprone [orange book]
deferiprone [usan]
deferiprone [who-dd]
deferiprone [mi]
deferiprone [vandf]
deferiprone [inn]
4(1h)-pyridinone, 3-hydroxy-1,2-dimethyl-
deferiprone [ema epar]
deferiprone [ep monograph]
deferiprone [mart.]
AKOS015902286
BP-12415
DB08826
1,2-dimethyl-3-hydroxypyridine-4-one
SCHEMBL94474
MLS006011689
NC00010
gtpl7456
HY-B0568
CS-5240
3-hydroxy-1,2-dimethyl-4- pyridinone
TZXKOCQBRNJULO-UHFFFAOYSA-N
1,2-dimetyl-3-hydroxy-4-pyridinone
3-hydroxy-1,2-dimethylpyrid-4-one
3-hydroxy-1,2-dimethyl-4(1h)-pyridinone
AC-33026
1,2-dimethyl-3-hydroxy-4-pyridone
AB00572605_12
AB00572605_11
OPERA_ID_366
mfcd00134497
EX-A972
deferidone
sr-01000721891
SR-01000721891-4
SBI-0207041.P001
DS-5493
SY052576
BCP09606
Q749664
STL559018
BBL036482
HMS3873L13
NCGC00090548-04
1,2 dimethyl 3 hydroxypyrid 4 one
hdmpp
1,2 dimethyl 3 hydroxy 4 pyridinone
1,2 dimethyl 3 hydroxypyridin 4 one
3 hydroxy 1,2 dimethyl 4 pyridinone
NCGC00090548-05
deferiprone 1,2-dimethyl-3-hydroxy-4-pyridone
bdbm50525976
deferiprona
deferipronum
deferiprone (mart.)
v03ac02
deferiprone (ep monograph)
3-hydroxy-1,2-dimethyl-1,4-dihydropyridin-4-one
EN300-1718313
Z1255390865

Excerpt	Reference	Relevance
"Deferiprone (Ferriprox®) is an oral iron chelator indicated for the treatment of transfusional iron overload due to thalassemia syndromes and has been recently approved as a treatment for iron overload in adult and pediatric patients with SCD and other anemias."	( The pharmacokinetic and safety profile of single-dose deferiprone in subjects with sickle cell disease. Fradette, C; Mercier-Ross, J; Rozova, A; Soulières, D; Tricta, F; Tsang, YC, 2022)	1.69
"Deferiprone (L1) is an EMA- and FDA-approved drug used worldwide for the treatment of iron overload and also other conditions where there are no effective treatments."	( Deferiprone: A Forty-Year-Old Multi-Targeting Drug with Possible Activity against COVID-19 and Diseases of Similar Symptomatology. Kontoghiorghes, GJ, 2022)	2.89
"Deferiprone is an oral chelation option that could improve adherence and outcomes in children."	( Deferiprone versus deferoxamine for transfusional iron overload in sickle cell disease and other anemias: Pediatric subgroup analysis of the randomized, open-label FIRST study. Ebeid, FSE; El-Beshlawy, A; Elalfy, MS; Fradette, C; Hamdy, M; Inusa, B; Kanter, J; Kwiatkowski, JL; Lee, D; Temin, NT; Tricta, F; Veríssimo, MPA; Williams, S, 2024)	3.61
"Deferiprone is an iron chelator that has recently been used to treat patients with infratentorial superficial siderosis (iSS). "	( Risks associated with oral deferiprone in the treatment of infratentorial superficial siderosis. Banerjee, G; Cowley, P; Eleftheriou, P; Farmer, S; Hylton, B; Porter, J; Sammaraiee, Y; Werring, DJ, 2020)	2.3
"Deferiprone (DFP) is a clinically available iron chelator, which has demonstrated potential therapeutic advantages of chelating iron in neurodegenerative disorders, and is currently in clinical trials for AD."	( Deferiprone Treatment in Aged Transgenic Tau Mice Improves Y-Maze Performance and Alters Tau Pathology. Adlard, PA; Finkelstein, DI; Lago, L; McColl, G; Rao, SS; Shukla, JJ; Volitakis, I, 2021)	2.79
"Deferiprone (DFP) is a metal chelating agent generally used to treat patients with thalassaemia, due to iron overload in clinical settings.Studies have revealed that long-term use of DFP can induce hepatotoxicity, however, mechanisms of its toxic action remain unclear. "	( Metabolic activation of deferiprone mediated by CYP2A6. Ding, Z; Li, W; Peng, Y; Wang, X; Zheng, J; Zheng, X, 2021)	2.37
"Deferiprone is an oral iron chelator approved for use in the United States as a second line agent for the treatment of transfusional iron overload in patients with thalassemia."	( Deferiprone for the treatment of transfusional iron overload in thalassemia. Belmont, A; Kwiatkowski, JL, 2017)	2.62
"Deferiprone (DFP) is an oral iron chelator used for the treatment of systemic iron overload disorders, and has recently been tested for Parkinson's disease."	( Iron chelator deferiprone rescues memory deficits, hippocampal BDNF levels and antioxidant defenses in an experimental model of memory impairment. Alcalde, LA; Bogo, MR; de Freitas Crivelaro, PC; de Freitas, BS; Dornelles, VC; Gus, H; Kist, LW; Machado, GDB; Monteiro, RT; Schröder, N, 2018)	1.56
"Deferiprone is an effective oral iron chelator but is known to cause significant arthropathy."	( Distal ulnar changes in children with thalassemia and deferiprone related arthropathy. Anand, R; Chandra, J; Pemde, H; Seth, A; Sharma, R; Singh, V, 2013)	1.36
"Deferiprone (L1) is an effective iron-chelating drug that is widely used for the treatment of iron-overload diseases. "	( Inhibition of Fe(2+)- and Fe(3+)- induced hydroxyl radical production by the iron-chelating drug deferiprone. Kobzeva, TV; Kontoghiorghes, GJ; Polyakov, NE; Timoshnikov, VA, 2015)	2.08
"Deferiprone is a blood brain barrier permeable, low molecular weight iron chelator that has been used for many years to treat systemic iron disease."	( Characterization of the neuroprotective potential of derivatives of the iron chelating drug deferiprone. Kontoghiorghes, GJ; Maher, P, 2015)	1.36
"Deferiprone is a highly efficacious and safe chelation therapy for patients with thalassemia major who are non-compliant to Deferrioxamine. "	( Comparison of deferiprone and deferrioxamine for the treatment of transfusional iron overload in children with beta thalassemia major. Ali, S; Butt, MA; Waheed, N, )	1.93
"Deferiprone has proved to be a successful iron selective chelator in a range of pathologies. "	( Design and synthesis of novel pegylated iron chelators with decreased metabolic rate. Abbate, V; Bansal, SS; Hider, RC; Kong, X; Li, J; Lu, Z; Ma, Y; Zhang, X, 2015)	1.86
"Deferiprone is a hydroxypyridinone iron chelator used therapeutically to remove this excess iron and prevent tissue damage."	( Deferiprone glucuronidation by human tissues and recombinant UDP glucuronosyltransferase 1A6: an in vitro investigation of genetic and splice variants. Benoit-Biancamano, MO; Caron, P; Connelly, J; Guillemette, C; Villeneuve, L, 2009)	2.52
"Deferiprone (L1) seems to be a promising agent as an adjuvant in the treatment for severe P. "	( Deferiprone (L1) as an adjuvant therapy for Plasmodium falciparum malaria. Ghosh, K; Karnad, D; Mohanty, D; Pathare, AV, 2002)	3.2
"Deferiprone is an iron chelator that has the potential to be more effective than deferoxamine in removing intracellular iron from the heart."	( Comparative effects of deferiprone and deferoxamine on survival and cardiac disease in patients with thalassemia major: a retrospective analysis. Fogliacco, E; Gaglioti, C; Piga, A; Tricta, F, 2003)	1.35
"Deferiprone is an effective iron chelator, but arthropathy and neutropenia are very frequent side effects and need strict monitoring during therapy. "	( Deferiprone, efficacy and safety. Choudhry, VP; Malaviya, AN; Pati, HP; Saxena, A, 2004)	3.21
"Deferiprone is a promising, orally active Fe chelator for the treatment of Fe overload in birds, although its potential side effects need to be considered."	( Clinical evaluation of the oral iron chelator deferiprone for the potential treatment of iron overload in bird species. Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Whiteside, DP, 2004)	1.3
"Deferiprone (DFP,L1) is a bidentate oral iron chelator which binds to iron in a 3:1 ratio. "	( Efficacy and adverse effects of oral iron chelator deferiprone (l1, 1,2- dimethyl-3-hydroxypyrid-4-one) in patients with beta thalassaemia major in Pakistan. Ali, W; Anwar, M; Ayyub, M; Hussain, S; Hussain, T; Ijaz, A; Khan, MN; Waqar, A, )	1.83
"Deferiprone (L1) is an orally active iron-chelation agent that is being evaluated as a treatment for iron overload in thalassemia major. "	( Liver fibrosis and iron levels during long-term deferiprone treatment of thalassemia major patients. Peng, CT; Tsai, CH; Wu, KH; Wu, SF, 2006)	2.03
"Deferiprone is a three-times-daily oral iron chelator, but has limited availability in the United States."	( Consequences and costs of noncompliance with iron chelation therapy in patients with transfusion-dependent thalassemia: a literature review. Baladi, JF; Coates, TD; Delea, TE; Edelsberg, J; Phatak, PD; Sofrygin, O; Thomas, SK, 2007)	1.06
"Deferiprone is a bidentate oral iron chelator used for the treatment of transfusional iron overload in people. "	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the white leghorn chicken. Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	2.03
"Deferiprone is a bidentate oral iron chelator used for the treatment of iron overload in people. "	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the domestic pigeon (Columba livia). Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	2.03
"Deferiprone is a recently developed iron chelator that has been extensively evaluated for the treatment of patients requiring chronic blood transfusions."	( Systemic administration of the iron chelator deferiprone attenuates subarachnoid hemorrhage-induced cerebral vasospasm in the rabbit. Arthur, AS; Fergus, AH; Kassell, NF; Lanzino, G; Lee, KS; Mathys, J, 1997)	1.28
"Deferiprone (L1; CP20) is an orally absorbed bidentate hydroxypyridinone iron chelator that can induce urinary iron excretion, promote negative iron balance and reduce hepatic iron levels in some transfusion-dependent patients, particularly in those who are markedly iron overloaded and have not received regular deferoxamine therapy."	( A risk-benefit assessment of iron-chelation therapy. Porter, JB, 1997)	1.02
"Deferiprone (L1) is a largely studied oral chelator in clinical setting, however, no definite conclusions concerning efficacy and toxicity still could be drawn. "	( Oral iron chelating therapy. A single center interim report on deferiprone (L1) in thalassemia. Amurri, B; De Marco, S; Giua, R; Lazzari, G; Masi, C; Mazza, P; Moscogiuri, R; Palazzo, G; Sebastio, AM; Semeraro, F; Spartera, MA; Suma, V, 1998)	1.98
"Deferiprone is an orally active iron-chelating agent that is being evaluated as a treatment for iron overload in thalassemia major. "	( Long-term safety and effectiveness of iron-chelation therapy with deferiprone for thalassemia major. Brittenham, GM; Burt, AD; Cameron, RG; Fleming, KA; McClelland, RA; McLaren, CE; Olivieri, NF; Templeton, DM, 1998)	1.98
"Deferiprone is a safe and effective oral iron-chelating agent which can be used, under strict supervision, in transfusion-dependent iron overloaded children."	( A trial of deferiprone in transfusion-dependent iron overloaded children. De Silva, DD; Fernandopulle, M; Fonseka, EA; Lucas, GN; Perera, BJ, 2000)	2.14

Excerpt	Reference	Relevance
"Deferiprone has the potential to limit scar tissue formation and should be considered in future clinical applications."	( Deferiprone has anti-inflammatory properties and reduces fibroblast migration in vitro. Gouzos, M; Ooi, ML; Psaltis, AJ; Ramezanpour, M; Smith, JLP; Vreugde, S; Wormald, PJ, 2019)	2.68
"Deferiprone has high affinity for copper binding and can be considered for the potential treatment of copper toxicity and overloading conditions, such as Wilson's disease."	( Effective inhibition of copper-catalyzed production of hydroxyl radicals by deferiprone. Kobzeva, T; Kontoghiorghes, GJ; Polyakov, NE; Selyutina, OY; Timoshnikov, VA, 2019)	1.46
"Deferiprone has proved to be a successful iron selective chelator in a range of pathologies. "	( Design and synthesis of novel pegylated iron chelators with decreased metabolic rate. Abbate, V; Bansal, SS; Hider, RC; Kong, X; Li, J; Lu, Z; Ma, Y; Zhang, X, 2015)	1.86
"Deferiprone (L1) has been shown to be effective and safe in the reversal of accelerating oxidative stress related tissue damage in iron loading and non iron loading conditions such as cardiomyopathy in thalassaemia, acute kidney disease and Friedreich ataxia."	( Prospects for introducing deferiprone as potent pharmaceutical antioxidant. Kontoghiorghes, GJ, 2009)	1.37
"Deferiprone (L1) has been used in several countries for iron chelation therapy for over one decade. "	( Long-term response to deferiprone therapy in Asian Indians. Das, RR; Marwaha, RK; Panigrahi, I, 2010)	2.12
"Deferiprone has been reported to inhibit HIV-1 replication in tissue culture."	( Inhibition of HIV-1 gene expression by Ciclopirox and Deferiprone, drugs that prevent hypusination of eukaryotic initiation factor 5A. D'Alliessi Gandolfi, D; Hanauske-Abel, HM; Hoque, M; Mathews, MB; Palumbo, P; Park, MH; Pe'ery, T; Saxena, D, 2009)	1.32
"Deferiprone (L1) has been shown to abolish the stimulating effect of iron on lipid peroxidation and reduced glutathione (GSH) levels, and also to inhibit the influence of iron on the activity of TrxR and GPx."	( The effect of iron(III) on the activity of selenoenzymes and oxidative damage in the liver of rats. Interaction with natural antioxidants and deferiprone. Cerná, P; Eybl, V; Hodková, A; Kotyzová, D, 2010)	1.28
"Deferiprone (DFP) has been evaluated in a wide range of disorders, but most data come from transfusion-dependent thalassemia. "	( Deferiprone. Longo, F; Massano, D; Piga, A; Roggero, S; Salussolia, I; Serra, M, 2010)	3.25
"Deferiprone has been shown to be capable of reducing the iron burden in patients with β-thalassaemia."	( Pharmacokinetics of deferiprone in patients with β-thalassaemia: impact of splenectomy and iron status. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Jittangprasert, P; Limenta, LM; Morales, NP; Wilairat, P; Yamanont, P, 2011)	1.41
"Deferiprone has been reported to be superior to deferoxamine for the removal of cardiac iron and improvement in left ventricular (LV) function but little is known of their relative effects on the right ventricle (RV), which is being increasingly recognised as an important prognostic factor in cardiomyopathy."	( Effect of deferiprone or deferoxamine on right ventricular function in thalassemia major patients with myocardial iron overload. Aessopos, A; Alam, MH; Alpendurada, F; Berdoukas, V; Carpenter, JP; Galanello, R; Gotsis, ED; Karagiorga, M; Ladis, V; Pennell, DJ; Piga, A; Roughton, M; Smith, GC; Tanner, MA; Westwood, MA, 2011)	1.49
"Deferiprone has equivalent iron removal efficacy and comparable toxicity to deferoxamine."	( The design and development of deferiprone (L1) and other iron chelators for clinical use: targeting methods and application prospects. Kolnagou, A; Kontoghiorghes, GJ; Neocleous, K; Pattichis, K, 2004)	1.33
"Deferiprone (L1) has been recommended as an effective oral chelation therapy for patients with beta-thalassemia major (TM). "	( Deferiprone or deferoxamine vs. combination therapy in patients with beta-thalassemia major: a case study in Taiwan. Hsiao, CC; Jang, RC; Liang, DC; Peng, CT; Wang, LY; Wu, KH; Wu, SF; Yang, CP, 2006)	3.22
"Deferiprone (L1), has previously been reported to be associated with immunological abnormalities in iron loaded thalassemia patients. "	( Immune and neural status of thalassemic patients receiving deferiprone or combined deferiprone and deferoxamine chelation treatment. Athanassiou-Metaxa, M; Economou, M; Kanakoudi-Tsakalidou, F; Perifanis, V; Taparkou, A; Tourkantoni, N; Tzimouli, V; Zafiriou, D, 2008)	2.03
"Deferiprone has been shown to induce sustained decreases in body iron to concentrations associated with survival free from the complications of iron overload in deferoxamine (DFO)-treated patients."	( Long-term therapy with deferiprone. Olivieri, NF, 1996)	1.33
"Deferiprone has now been shown to induce sustained decreases in tissue iron to concentrations that are associated with survival free of the complications of iron overload in deferoxamine-treated patients."	( Orally active iron chelators in the treatment of iron overload. Olivieri, NF, 1996)	1.02
"Deferiprone has additive, or possibly synergistic, effects on iron excretion when combined with deferoxamine."	( Deferiprone: a review of its clinical potential in iron overload in beta-thalassaemia major and other transfusion-dependent diseases. Barman Balfour, JA; Foster, RH, 1999)	2.47
"Deferiprone has been suggested as an effective oral chelation therapy for thalassemia major. "	( Deferiprone versus deferoxamine in patients with thalassemia major: a randomized clinical trial. Capra, M; Ciaccio, C; Cianciulli, P; D'Amico, G; D'Ascola, DG; Di Gregorio, F; Garozzo, G; Maggio, A; Magnano, C; Malizia, R; Mangiagli, A; Midiri, M; Morabito, A; Quarta, G; Rizzo, A; Rizzo, M, )	3.02

Excerpt	Reference	Relevance
"Deferiprone reversed the increase in c-Fos expression induced by swim stress in 5-HTT KO mice in the lateral amygdala."	( Novel Antidepressant-Like Properties of the Iron Chelator Deferiprone in a Mouse Model of Depression. Aitken, C; Bush, AI; Hale, MW; Hannan, AJ; Li, S; Mawal, CH; Opazo, CM; Payet, JM; Renoir, T; Tran, H; Uzungil, V; Wilson, C, 2022)	1.69
"Deferiprone, because of its lower molecular weight, might cross into heart mitochondria more efficiently, improving their activity and, thereby, myocardial cell function."	( Long-term treatment with deferiprone enhances left ventricular ejection function when compared to deferoxamine in patients with thalassemia major. Barone, R; Calvaruso, G; Campisi, S; Capra, M; Caruso, V; Casale, M; Ciancio, A; Cianciulli, P; Cuccia, L; D'Ascola, G; Filosa, A; Gagliardotto, F; Gerardi, C; Maggio, A; Pitrolo, L; Prossomariti, L; Rigano, P; Rizzo, M; Vitrano, A, 2013)	1.41

Excerpt	Reference	Relevance
"Deferiprone treatment tended to decrease muscle iron levels in mdx mice (-30%, P < 0.1), which was associated with lower oxidative stress and fibrosis, but suppressed haem-containing proteins and mitochondrial content."	( Iron overload and impaired iron handling contribute to the dystrophic pathology in models of Duchenne muscular dystrophy. Alves, FM; Ayton, S; Bush, AI; Caldow, MK; Chung, JD; Crouch, PJ; Hardee, JP; Hare, DJ; Koopman, R; Kysenius, K; Lynch, GS; Trieu, J, 2022)	1.44
"Deferiprone treatment showed significant improvements in neurological severity scores, locomotor/gait performance and cognitive function, and attenuated anxiety-like symptoms post-TBI."	( Deferiprone attenuates neuropathology and improves outcome following traumatic brain injury. Adlard, PA; Daglas, M; Juan, SMA; Miles, LQ; Rao, SS; Truong, PH, 2023)	3.07
"Deferiprone treatment reduced iron deposition and IR in DC rats except for blood glucose."	( Deferiprone attenuates inflammation and myocardial fibrosis in diabetic cardiomyopathy rats. Bao, Y; Jia, X; Jin, Q; Li, L; Liu, R; Liu, X; Xie, R; Zou, C, 2017)	2.62
"Deferiprone-treated patients receiving 20 or 40mg/kg/day showed a decline in the left ventricular mass index, compared to an increase in the placebo-treated patients."	( Deferiprone in Friedreich ataxia: a 6-month randomized controlled trial. Arpa, J; Delatycki, MB; Le Quan Sang, KH; Mariotti, C; Munnich, A; Pandolfo, M; Sanz-Gallego, I; Spino, M; Tai, G; Tarnopolsky, MA; Taroni, F; Tricta, F, 2014)	2.57
"The deferiprone-treated group had significantly decreased skin thickness (p<0.05) and significantly decreased dermal fibrosis compared to the Omniscan-only group."	( Evidence Suggesting a Role of Iron in a Mouse Model of Nephrogenic Systemic Fibrosis. Bose, C; Hall, KA; Hiatt, KM; Karaduta, O; Megyesi, JK; Shah, SV; Swaminathan, S, 2015)	0.9
"Deferiprone-treated hearts had greater mass (16.5% increase) and increased myocyte hypertrophy."	( Deferasirox and deferiprone remove cardiac iron in the iron-overloaded gerbil. Aguilar, MI; Gonzalez, I; Moats, R; Nelson, M; Nick, H; Otto-Duessel, M; Shimada, H; Wood, JC, 2006)	1.4
"Five deferiprone-treated patients had progression of fibrosis, as compared with none of those given deferoxamine (P=0.04)."	( Long-term safety and effectiveness of iron-chelation therapy with deferiprone for thalassemia major. Brittenham, GM; Burt, AD; Cameron, RG; Fleming, KA; McClelland, RA; McLaren, CE; Olivieri, NF; Templeton, DM, 1998)	0.99
"Treatment with deferiprone, gut dysbiosis and disturbance of metabolites were attenuated in HFe-fed WT mice, but not in HFe-fed BKO mice."	( Deferiprone has less benefits on gut microbiota and metabolites in high iron-diet induced iron overload thalassemic mice than in iron overload wild-type mice: A preclinical study. Buddhasiri, S; Chattipakorn, N; Chattipakorn, SC; Fucharoen, S; Kittichotirat, W; Kumfu, S; Nawara, W; Sarichai, P; Sriwichaiin, S; Thiennimitr, P; Thonusin, C, 2022)	2.5
"Treatment with deferiprone of UROS-deficient erythroid cell lines and peripheral blood CD34+-derived erythroid cultures from a patient with CEP inhibited iron-dependent protein ALAS2 and iron-responsive element-binding protein 2 expression and reduced porphyrin production."	( Iron chelation rescues hemolytic anemia and skin photosensitivity in congenital erythropoietic porphyria. Bedel, A; Blouin, JM; Costet, P; Daher, R; Ged, C; Gouya, L; Karim, Z; Lalanne, M; Lamrissi-Garcia, I; Moreau-Gaudry, F; Morice-Picard, F; Puy, H; Richard, E, 2020)	0.9

Excerpt	Reference	Relevance
" During the course of the trial, several possible adverse effects have been encountered."	( Efficacy and possible adverse effects of the oral iron chelator 1,2-dimethyl-3-hydroxypyrid-4-one (L1) in thalassemia major. al-Refaie, FN; Hoffbrand, AV; Kontoghiorghes, GJ; Nortey, P; Wickens, DG; Wonke, B, 1992)	0.28
" Major emphasis was given in the use of these two and also of other chelators in conditions of iron overload, imbalance and toxicity, as well as the incidence and possible causes of toxic side effects in both animals and humans."	( Comparative efficacy and toxicity of desferrioxamine, deferiprone and other iron and aluminium chelating drugs. Kontoghiorghes, GJ, 1995)	0.54
" The bidentate chelators CP20 and CP94 (150 microM) appeared to be as effective as the hexadentate chelator desferrioxamine (50 microM) in the protection of rat and human hepatocytes against the toxic effect of iron load achieved by culturing the cells for 1 day in the presence of 50 microM iron citrate."	( Inhibition of iron toxicity in rat and human hepatocyte cultures by the hydroxypyridin-4-ones CP20 and CP94. Brissot, P; Chenoufi, N; Cillard, J; Hubert, N; Lescoat, G; Loréal, O; Morel, I; Pasdeloup, N, 1995)	0.29
" According to the results of this study, uremia did not increase the toxic effects of L1."	( Four-week oral toxicity study of 1,2-dimethyl-3-hydroxypyrid-4-one (L1) in uremic rats. Corbella, J; del Castillo, D; Domingo, JL; Gomez, M; Llobet, JM, 1995)	0.29
" Adverse effects of DFP were nausea and vomiting (30%), significant arthropathy requiring stopping of the drug (30%), and reversible neutropenia in one patient."	( Efficacy and safety of oral iron chelating agent deferiprone in beta-thalassemia and hemoglobin E-beta thalassemia. Adhikari, D; Basu, AK; Bhattacharya, B; Biswas, A; Chakraborty, ML; Chandra, S; Maitra, TK; Roy, TB, 1995)	0.55
"A single oral dose of Al nitrate nonahydrate (1,327 mg/kg) was given on gestation day 12, the most sensitive time for Al-induced maternal and developmental toxic effects in mice."	( Evaluation of the protective activity of deferiprone, an aluminum chelator, on aluminum-induced developmental toxicity in mice. Albina, ML; Bellés, M; Domingo, JL; Sanchez, DJ, 2000)	0.57
" No beneficial effects of deferiprone on these adverse effects could be observed."	( Evaluation of the protective activity of deferiprone, an aluminum chelator, on aluminum-induced developmental toxicity in mice. Albina, ML; Bellés, M; Domingo, JL; Sanchez, DJ, 2000)	0.87
" These data show that the drug was effective in reducing serum ferritin levels and the incidence of adverse events was not greater than the frequency reported in clinical trials."	( The safety and effectiveness of deferiprone in a large-scale, 3-year study in Italian patients. Baiardi, P; Cappellini, MD; Carnelli, V; Ceci, A; De Sanctis, V; Felisi, M; Galanello, R; Maggio, A; Masera, G; Piga, A; Schettini, F; Stefàno, I; Tricta, F, 2002)	0.6
"Deferiprone at a dose of 75 mg/kg/day is not sufficiently effective to maintain iron stores at a level which has been considered safe in all patients with iron overload."	( Safety and effectiveness of 100 mg/kg/day deferiprone in patients with thalassemia major: a two-year study. Dhillon, AP; Ellis, G; Hoffbrand, AV; Inati, A; Koussa, S; Sharara, A; Sheikh-Taha, M; Taher, A, 2005)	2.04
" We conducted a study in order to determine the efficacy and adverse effects of DFP in Pakistani thalassaemic patients."	( Efficacy and adverse effects of oral iron chelator deferiprone (l1, 1,2- dimethyl-3-hydroxypyrid-4-one) in patients with beta thalassaemia major in Pakistan. Ali, W; Anwar, M; Ayyub, M; Hussain, S; Hussain, T; Ijaz, A; Khan, MN; Waqar, A, )	0.38
" We conclude that the short-term use of L1, with or without DFO, was safe and efficacious in our Chinese patient cohort."	( A randomized controlled study evaluating the safety and efficacy of deferiprone treatment in thalassemia major patients from Hong Kong. Chan, GC; Chik, KW; Ha, SY; Lam, CW; Lee, AC; Ling, SC; Luk, CW; Ng, IO, 2006)	0.57
" There was no significant difference in the proportion of patients with adverse events in the two therapy groups although the nature of the adverse events differed according to the chelation regimen."	( A prospective randomized controlled trial on the safety and efficacy of alternating deferoxamine and deferiprone in the treatment of iron overload in patients with thalassemia. Fischer, R; Galanello, R; Kattamis, A; Ladis, V; Leoni, G; Lund, U; Piga, A; Tricta, F; Voi, V, 2006)	0.55
" However, despite these fatalities it would appear that there is no regular monitoring of such toxicities or of effects such as the accumulation of toxic metals."	( Update on toxicity and efficacy aspects of treatment with deferasirox and its implication on the morbidity and mortality of transfused iron loaded patients. Kontoghiorghes, GJ, 2008)	0.35
" Drug-related adverse events were mostly mild to moderate and resolved without discontinuing treatment."	( Efficacy and safety of deferasirox, an oral iron chelator, in heavily iron-overloaded patients with beta-thalassaemia: the ESCALATOR study. Al Jefri, A; Al Zir, K; Daar, S; El-Beshlawy, A; Elalfy, MS; Habr, D; Hmissi, A; Kriemler-Krahn, U; Taher, A, 2009)	0.35
" No unexpected adverse reactions were observed."	( The safety, tolerability, and efficacy of a liquid formulation of deferiprone in young children with transfusional iron overload. El Alfy, M; El-Beshlawy, A; ElAlfy, MS; Lee, CL; Sari, TT; Tricta, F, 2010)	0.6
" Incidence of adverse effects was comparable to that in thalassemic patients."	( Efficacy and safety of administration of oral iron chelator deferiprone in patients with early myelodysplastic syndrome. Cermak, J; Hochova, I; Jonasova, A; Neuwirtova, R; Siskova, M; Vondrakova, J; Walterova, L, 2011)	0.61
"Superficial siderosis is a neurodegenerative disease caused by toxic accumulation of hemosiderin on the surface of the brain and spinal cord for which there is no known effective treatment."	( Pilot safety trial of deferiprone in 10 subjects with superficial siderosis. Levy, M; Llinas, R, 2012)	0.69
"Over a 90-day period, deferiprone had no significant adverse effects on hematologic, liver, or neurological function."	( Pilot safety trial of deferiprone in 10 subjects with superficial siderosis. Levy, M; Llinas, R, 2012)	1.01
"Deferiprone proved safe in this small population of superficial siderosis subjects."	( Pilot safety trial of deferiprone in 10 subjects with superficial siderosis. Levy, M; Llinas, R, 2012)	2.14
"A record 4113 fatalities were reported in 2012 in a postmarketing surveillance of patients treated with deferasirox, despite warnings of life-threatening toxic side effects, and the need for regular monitoring and prophylactic measures."	( A record number of fatalities in many categories of patients treated with deferasirox: loopholes in regulatory and marketing procedures undermine patient safety and misguide public funds? Kontoghiorghes, GJ, 2013)	0.39
" Two independent authors assessed data from extracted randomized trials for efficacy and safety in the measurements of serum ferritin (SF), live iron concentration (LIC), myocardial iron content (MIC), left ventricular ejection fraction (LVEF) and adverse events (AEs)."	( Comparative efficacy and safety of deferoxamine, deferiprone and deferasirox on severe thalassemia: a meta-analysis of 16 randomized controlled trials. Huang, L; Jiang, H; Xia, S; Zhang, W, 2013)	0.64
"Findings indicated that the most effective and safe iron chelators remains to be proven, and further large-scale, long-term studies are needed."	( Comparative efficacy and safety of deferoxamine, deferiprone and deferasirox on severe thalassemia: a meta-analysis of 16 randomized controlled trials. Huang, L; Jiang, H; Xia, S; Zhang, W, 2013)	0.64
"DFP/DFX combination proved superior in improving cardiac T2*, treatment compliance, and patients satisfaction with no greater adverse events."	( Efficacy and safety of a novel combination of two oral chelators deferasirox/deferiprone over deferoxamine/deferiprone in severely iron overloaded young beta thalassemia major patients. Adly, AM; Elalfy, MS; Elhenawy, YI; Samir, A; Tony, S; Wali, Y, 2015)	0.65
"The liquid formulation of deferiprone is safe in young children with transfusion-induced iron overload."	( Safety profile of a liquid formulation of deferiprone in young children with transfusion-induced iron overload: a 1-year experience. Chuansumrit, A; Kadegasem, P; Sasanakul, W; Sirachainan, N; Songdej, D; Wongwerawattanakoon, P, 2016)	1
"There is a lack of knowledge regarding the incidence of serious adverse drug reactions (ADR) to the oral iron chelator deferiprone in Chinese children with transfusion-dependent thalassaemia."	( Safety Profile of Oral Iron Chelator Deferiprone in Chinese Children with Transfusion-Dependent Thalassaemia. Botzenhardt, S; Ceci, A; Chan, GC; Felisi, M; Neubert, A; Rascher, W; Sing, CW; Wong, IC; Wong, LY, 2016)	0.92
" Selected protocols using DFO, L1, and their combination can be designed for personalized chelation therapy in TI, which can effectively and safely remove all the excess toxic iron and prevent cardiac, liver, and other organ damage."	( Efficacy and safety of iron-chelation therapy with deferoxamine, deferiprone, and deferasirox for the treatment of iron-loaded patients with non-transfusion-dependent thalassemia syndromes. Kontoghiorghe, CN; Kontoghiorghes, GJ, 2016)	0.67
" At every visit for blood transfusion, all patients were clinically assessed for any adverse effects; liver and renal functions were monitored 6-monthly."	( Comparative Efficacy and Safety of Oral Iron Chelators and their Novel Combination in Children with Thalassemia. Gomber, S; Jain, P; Narang, M; Sharma, S, 2016)	0.43
" No significant adverse reactions were noticed in either the monotherapy or the combination group."	( Comparative Efficacy and Safety of Oral Iron Chelators and their Novel Combination in Children with Thalassemia. Gomber, S; Jain, P; Narang, M; Sharma, S, 2016)	0.43
"Oral combination therapy of deferiprone and deferasirox appears to be an efficacious and safe modality to reduce serum ferritin in multi-transfused children with thalassemia."	( Comparative Efficacy and Safety of Oral Iron Chelators and their Novel Combination in Children with Thalassemia. Gomber, S; Jain, P; Narang, M; Sharma, S, 2016)	0.73
" The combination of drugs was well tolerated and no new adverse effects were observed."	( Efficacy and Safety of Combined Oral Chelation With Deferiprone and Deferasirox in Children With β-Thalassemia Major: An Experience From North India. Chandra, J; Dhingra, B; Jain, R; Mahto, D; Parakh, N; Sharma, S, 2017)	0.71
"Premature ventricular contractions are a rare side effect of filgrastim, reported mainly in elderly men."	( Premature ventricular contractions as a side effect of filgrastim in a child with B-thalassaemia. Joshi, N; Nazir, HF; Wali, YA, 2018)	0.48
" No unexpected, serious, or severe adverse events were seen in the ES-DFP group."	( Safety and efficacy of early start of iron chelation therapy with deferiprone in young children newly diagnosed with transfusion-dependent thalassemia: A randomized controlled trial. Adly, A; Awad, H; Berdoukas, V; Elalfy, MS; Tarif Salam, M; Tricta, F, 2018)	0.72
" Random effects model was used to generate direct, indirect and mixed treatment comparison pooled estimates for the following outcomes: serum ferritin, liver iron concentration (LIC), changes in serum ferritin, mortality, urine iron excretion, adverse events, neutropenia, agranulocytosis and number of patients withdrawing the chelating therapy."	( Efficacy and safety of iron chelators in thalassemia and sickle cell disease: a multiple treatment comparison network meta-analysis and trial sequential analysis. Sivaramakrishnan, G; Sridharan, K, 2018)	0.48
" DFP/DFO was associated with higher LVEF, low risk of adverse events and reduced end of serum ferritin compared to DFO."	( Efficacy and safety of iron chelators in thalassemia and sickle cell disease: a multiple treatment comparison network meta-analysis and trial sequential analysis. Sivaramakrishnan, G; Sridharan, K, 2018)	0.48
" We compared changes in liver and heart iron, adverse effects and other outcomes, in patients treated with deferiprone or deferasirox."	( Single-center retrospective study of the effectiveness and toxicity of the oral iron chelating drugs deferiprone and deferasirox. Gallie, BL; Olivieri, NF; Sabouhanian, A, 2019)	0.94
"Treatment with DFP proved safe and well tolerated."	( Efficacy and safety of deferiprone for the treatment of superficial siderosis: results from a long-term observational study. Abbruzzese, G; Cossu, G; Forni, GL; Marchese, R; Matta, G; Oppo, V; Pinto, V; Ruffinengo, U, 2019)	0.82
" Deferiprone was well tolerated and adverse events were similar between the treatment groups, except for anaemia, which was seen in 12 (21%) of 58 patients in the deferiprone group, but was not seen in any patients in the placebo group."	( Safety and efficacy of deferiprone for pantothenate kinase-associated neurodegeneration: a randomised, double-blind, controlled trial and an open-label extension study. Aguilar, C; Basu, A; Blamire, AM; Büchner, B; Chinnery, PF; Dušek, P; Fradette, C; Hayflick, SJ; Hogarth, P; Horvath, R; Kálmán, B; Karin, I; Klopstock, T; Kmieć, T; Küpper, C; Nardocci, N; Neuhofer, C; Neumayr, L; Spino, M; Steele, HE; Tricta, F; Vichinsky, E; Wilson, I; Yapici, Z; Zhao, F; Zibordi, F; Zorzi, G, 2019)	1.73
"Chitogel in combination with Def 20 mM is safe and effective in decreasing the inflammatory process and may possibly reduce post-operative adhesions following laminectomy."	( Prevention of peridural adhesions in spinal surgery: Assessing safety and efficacy of Chitogel with Deferiprone in a sheep model. Anne Fong, S; Bassiouni, A; Chryssidis, S; James Psaltis, A; Jukes, A; Mascarenhas, A; Moratti, S; Nguyen-Hoang, A; Otto, S; Patel, S; Richter, K; Vediappan, RS; Vreugde, S; Wormald, PJ, 2020)	0.77
" No significant difference between the groups was shown in the occurrence of serious and drug-related adverse events."	( Evaluation of the efficacy and safety of deferiprone compared with deferasirox in paediatric patients with transfusion-dependent haemoglobinopathies (DEEP-2): a multicentre, randomised, open-label, non-inferiority, phase 3 trial. Bejaoui, M; Bonifazi, D; Ceci, A; Christou, S; Cosmi, C; Cuccia, L; Del Vecchio, GC; Della Pasqua, O; El-Beshlawy, A; Felisi, M; Filosa, A; Hassab, H; Kattamis, A; Kreka, M; Maggio, A; Origa, R; Putti, MC; Reggiardo, G; Sherief, L; Spino, M; Telfer, P; Tempesta, B; Tricta, F; Tsang, YC; Vitrano, A; Zaka, A, 2020)	0.82
"In paediatric patients with transfusion-dependent haemoglobinopathies, deferiprone was effective and safe in inducing control of iron overload during 12 months of treatment."	( Evaluation of the efficacy and safety of deferiprone compared with deferasirox in paediatric patients with transfusion-dependent haemoglobinopathies (DEEP-2): a multicentre, randomised, open-label, non-inferiority, phase 3 trial. Bejaoui, M; Bonifazi, D; Ceci, A; Christou, S; Cosmi, C; Cuccia, L; Del Vecchio, GC; Della Pasqua, O; El-Beshlawy, A; Felisi, M; Filosa, A; Hassab, H; Kattamis, A; Kreka, M; Maggio, A; Origa, R; Putti, MC; Reggiardo, G; Sherief, L; Spino, M; Telfer, P; Tempesta, B; Tricta, F; Tsang, YC; Vitrano, A; Zaka, A, 2020)	1.06
" They were also monitored monthly for any adverse effects."	( Efficacy and Safety of Combined Oral Chelation with Deferiprone and Deferasirox on Iron Overload in Transfusion Dependent Children with Thalassemia - A Prospective Observational Study. Delhikumar, CG; DivakarJose, RR; Ram Kumar, G, 2021)	0.87
" The drugs were tolerated well without any serious adverse effects."	( Efficacy and Safety of Combined Oral Chelation with Deferiprone and Deferasirox on Iron Overload in Transfusion Dependent Children with Thalassemia - A Prospective Observational Study. Delhikumar, CG; DivakarJose, RR; Ram Kumar, G, 2021)	0.87
" Sal significantly increased testicular P concentration compared with untreated controls and significantly elevated the testicular Ca and Fe concentrations compared with the toxic control group."	( Ameliorative effects of deferiprone and tetraethylammonium salt of salinomycinic acid on lead-induced toxicity in mouse testes. Dorkov, P; Gluhcheva, Y; Helbich, TH; Ivanova, J; Keppler, B; Koellensperger, G; Pashkunova-Martic, I; Pavlova, E; Petrova, E; Schaier, M, 2021)	0.93
" Moreover, this therapeutic combination of agents is safe and does not weaken the healing of the sutured enterotomy site."	( Prevention of adhesions post-abdominal surgery: Assessing the safety and efficacy of Chitogel with Deferiprone in a rat model. Bassiouni, A; Bennett, C; Cooksley, C; Finnie, J; Jones, CF; Maddern, G; Moratti, S; Psaltis, AJ; Quarrington, RD; Trochsler, M; Vediappan, RS; Vreugde, S; Wormald, PJ, 2021)	0.84
" In this context, the use of curcumin, a dietary phytochemical derived from turmeric, as a natural and safe antioxidant with iron-chelating activity may be a useful strategy for the management of iron overload."	( Protective Effects of Curcumin against Iron-induced Toxicity. Barati, M; Iranshahy, M; Moinipour, N; Sahebkar, A; Shakeri, A, 2022)	0.72
" Two subjects reported mild adverse events unrelated to the study drug, and no other safety concerns were reported."	( The pharmacokinetic and safety profile of single-dose deferiprone in subjects with sickle cell disease. Fradette, C; Mercier-Ross, J; Rozova, A; Soulières, D; Tricta, F; Tsang, YC, 2022)	0.97

Excerpt	Reference	Relevance
" The mean elimination half-life of the drug is 3 hours, suggesting that a divided dose every 8 hours may assure better chelation."	( Relationship between the pharmacokinetics and iron excretion pharmacodynamics of the new oral iron chelator 1,2-dimethyl-3-hydroxypyrid-4-one in patients with thalassemia. Chung, D; Grunau, V; Hermann, C; Klein, J; Koren, G; Matsui, D; McClelland, R; Olivieri, N; St-Louis, P, 1991)	0.28
" The elimination half-life (elt1/2) of the drug was 91."	( Pharmacokinetics of the oral iron chelator deferiprone (L1) in patients with iron overload. al-Refaie, FN; Hoffbrand, AV; Nortey, P; Sheppard, LN; Wonke, B, 1995)	0.55
" Pharmacokinetic values were calculated."	( Comparison of the pharmacokinetics of 1,2-dimethyl-3-hydroxypyrid-4-one (L1) in healthy volunteers, with and without co-administration of ferrous sulfate, to thalassemia patients. Bentur, Y; Fernandes, D; Klein, J; Koren, G; Matsui, D; Olivieri, N; Stobie, S; Tyberg, J, 1993)	0.29
" The purpose of this study was to determine the pharmacokinetic disposition of deferiprone in the white leghorn chicken as a potential model upon which to base therapeutic regimens for the treatment of iron storage disease (hemochromatosis) in affected avian species."	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the white leghorn chicken. Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	0.82
" The purpose of this study was to determine the pharmacokinetic disposition of deferiprone in the domestic pigeon (Columba livia) and to compare the results with a previous study in the white leghorn chicken."	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the domestic pigeon (Columba livia). Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	0.82
"No statistically significant differences in any pharmacokinetic parameters of either deferiprone or deferiprone-glucuronide among the genotype groups were noted."	( UGT1A6 genotype-related pharmacokinetics of deferiprone (L1) in healthy volunteers. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Limenta, LM; Morales, NP; Svasti, S; Tankanitlert, J; Wilairat, P, 2008)	0.83
" We hypothesized that splenectomy and iron status might influence the pharmacokinetic profiles of deferiprone in patients with β-thalassaemia/haemoglobin E, and the present study was aimed at examining this hypothesis."	( Pharmacokinetics of deferiprone in patients with β-thalassaemia: impact of splenectomy and iron status. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Jittangprasert, P; Limenta, LM; Morales, NP; Wilairat, P; Yamanont, P, 2011)	0.91
"No significant difference in the pharmacokinetic parameters of non-conjugated deferiprone was observed between splenectomized and non-splenectomized patients."	( Pharmacokinetics of deferiprone in patients with β-thalassaemia: impact of splenectomy and iron status. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Jittangprasert, P; Limenta, LM; Morales, NP; Wilairat, P; Yamanont, P, 2011)	0.92
" A greater degree of iron overload in splenectomized patients results in alterations in pharmacokinetic parameters (the C(max) and AUC) of deferiprone glucuronide and deferiprone-chelated iron, as well as a significant increase in UIE."	( Pharmacokinetics of deferiprone in patients with β-thalassaemia: impact of splenectomy and iron status. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Jittangprasert, P; Limenta, LM; Morales, NP; Wilairat, P; Yamanont, P, 2011)	0.89
" The method was successfully applied to a pharmacokinetic study of deferiprone in six thalassemia patients."	( Development of a fast LC-MS/MS assay for the determination of deferiprone in human plasma and application to pharmacokinetics. Chen, TL; Hour, MJ; Hsieh, YW; Liu, CH; Peng, CT; Song, TS, 2012)	0.86
" Pharmacokinetic studies of generic formulations are required in local condition before placed on the market."	( Quantitative determination of deferiprone in human plasma by reverse phase high performance liquid chromatography and its application to pharmacokinetic study. Abbas, M; Alim, M; Asi, MR; Iqbal, T; Nawaz, R, 2012)	0.67
" Pharmacokinetic parameters including C(max) and area under concentration time curve from time zero to infinity (AUC(0-∞)) as well as urinary excretion of non-conjugated and glucuronide-conjugated deferiprone (L1 and L1-G) increased proportionally with the dose of deferiprone."	( Comparison of pharmacokinetics and urinary iron excretion of two single doses of deferiprone in β-thalassemia/hemoglobin E patients. Chantraraksri, U; Fucharoen, S; Morales, NP; Rodrat, S; Tankanitlert, J; Yamanont, P, 2012)	0.79
"4 mg l(-1) h, whereas Cmax increased from 17."	( Population pharmacokinetics of deferiprone in healthy subjects. Bellanti, F; Danhof, M; Della Pasqua, O, 2014)	0.69
"2 mg · h/mL, and mean Cmax ± SD was found to be 10."	( Sampling Optimization in Pharmacokinetic Bridging Studies: Example of the Use of Deferiprone in Children With β-Thalassemia. Bellanti, F; Danhof, M; Della Pasqua, O; Di Iorio, VL, 2016)	0.66
" All subjects received a single oral dose of 33 mg kg(-1) DFP, provided serum and urine samples for pharmacokinetic assessment over 24 h and were monitored for safety."	( Effects of renal impairment on the pharmacokinetics of orally administered deferiprone. Fradette, C; Jayashankar, S; Pichette, V; Sicard, É; Spino, M; Stilman, A; Tricta, F; Tsang, YC, 2016)	0.66
" However, based on Cmax , AUC(0,t) and AUC(0,∞), there were no significant group differences in systemic exposure, because less than 4% of the drug was excreted unchanged in the urine."	( Effects of renal impairment on the pharmacokinetics of orally administered deferiprone. Fradette, C; Jayashankar, S; Pichette, V; Sicard, É; Spino, M; Stilman, A; Tricta, F; Tsang, YC, 2016)	0.66
" Based on pharmacokinetic bridging concepts, we also evaluate whether the recommended doses yield appropriate systemic exposure in this group of patients."	( Population pharmacokinetics and dosing recommendations for the use of deferiprone in children younger than 6 years. Bellanti, F; Ceci, A; Connelly, J; Cosmi, C; Del Vecchio, GC; Della Pasqua, O; Filosa, A; Maggio, A; Mangiarini, L; Putti, MC; Spino, M, 2017)	0.69
" The present study aims to characterize the pharmacokinetic (PK) profile of deferiprone (DFP) in adult subjects with SCD."	( The pharmacokinetic and safety profile of single-dose deferiprone in subjects with sickle cell disease. Fradette, C; Mercier-Ross, J; Rozova, A; Soulières, D; Tricta, F; Tsang, YC, 2022)	1.2

Excerpt	Reference	Relevance
"Antifungal effects of iron chelators (lactoferrin, deferoxamine, deferiprone, and ciclopirox) were tested alone and in combination with antifungal drugs against Aspergillus fumigatus B5233 conidia."	( Antifungal activities of natural and synthetic iron chelators alone and in combination with azole and polyene antibiotics against Aspergillus fumigatus. Cruz, AR; Gallin, JI; Huang, CY; Zarember, KA, 2009)	0.59
" Apart from hemin, zinc protoporphyrin-IX, and other iron providing agents such as ferrous sulfate and ferriammonium sulfate combined with mefloquine exhibited no toxic effect against schistosomes."	( Mefloquine in combination with hemin causes severe damage to adult Schistosoma japonicum in vitro. Qiao, C; Wang, L; Xiao, SH; Xue, J, 2014)	0.4
" Evidence from small randomized controlled trials (RCTs) published to date for deferiprone (DFP) monotherapy or in combination with deferoxamine (DFO) is unclear."	( A systematic review and meta-analysis of deferiprone monotherapy and in combination with deferoxamine for reduction of iron overload in chronically transfused patients with β-thalassemia. Kuo, KH; Mrkobrada, M, 2014)	0.9

Excerpt	Reference	Relevance
" Food prolongs the rate of absorption of L1, but it does not affect significantly the extent of absorption measured by the area under the plasma concentration-time curve."	( Relationship between the pharmacokinetics and iron excretion pharmacodynamics of the new oral iron chelator 1,2-dimethyl-3-hydroxypyrid-4-one in patients with thalassemia. Chung, D; Grunau, V; Hermann, C; Klein, J; Koren, G; Matsui, D; McClelland, R; Olivieri, N; St-Louis, P, 1991)	0.28
" Our results indicate that the poor oral bioavailability of DFO can be attributed to the low epithelial permeability of the molecule coupled with its size (mol wt 656)."	( The transport of two iron chelators, desferrioxamine B and L1, across Caco-2 monolayers. Halleux, C; Hamilton, KO; Hassan, I; Jin, Y; Mackay, M; Stallibrass, L, 1994)	0.29
" After a 30-day washout period, 5 birds from the NIL-DFP group were used for a bioavailability study of deferiprone administered intravenously at the same dose."	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the white leghorn chicken. Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	0.8
" Six NIL-DFP birds were also administered deferiprone intravenously to determine the bioavailability of the drug after a 30-day washout period."	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the domestic pigeon (Columba livia). Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	0.85
"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
" In this respect, gamma radiation-induced crosslinking was used to produce St/PEG/PAAc nanogel particles, and then, it was used as a nanocarrier for DFP as an attempt to overcome the poor bioavailability and short half-life of DFP."	( Effectiveness of deferiprone-loaded nanocarrier in experimentally induced rhabdomyolysis: A dose-comparison study. Deghiedy, NM; El-Ghazaly, MA; El-Hazek, RM; El-Sabbagh, WA; Rashed, ER; Rashed, RR, 2020)	0.9

Excerpt	Relevance	Reference
" Their pharmacokinetics were determined in rats to establish dosing parameters for microdialysis studies of BBB permeation."	( The pharmacokinetics and blood-brain barrier permeation of the chelators 1,2 dimethly-, 1,2 diethyl-, and 1-[ethan-1'ol]-2-methyl-3-hydroxypyridin-4-one in the rat. Allen, DD; Fredenburg, AM; Sethi, RK; Yokel, RA, 1996)	0.29
" One month later each patient received the other of the 2 dosing regimens for 72 hours immediately prior to transfusion."	( The pharmacokinetics and pharmacodynamics of the oral iron chelator deferiprone (L1) in relation to hemoglobin levels. Fassos, FF; Fernandes, D; Klein, J; Koren, G; Matsui, D; Olivieri, NF, 1996)	0.53
" These effects can be largely avoided if the dosage is adjusted to take account of the degree of iron overload (using the therapeutic index) and if the mean daily dose does not exceed 40 mg/kg."	( A risk-benefit assessment of iron-chelation therapy. Porter, JB, 1997)	0.3
" When studies with patients receiving lower dosage (< or = 50 mg x k(-1) x day(-1)) were included, the success rate was 45."	( Meta-analytic review of the clinical effectiveness of oral deferiprone (L1). Addis, A; Einarson, TR; Koren, G; Loebstein, R, 1999)	0.55
" This may reflect factors such as suboptimal dosage and/or severe degree of iron overload at baseline in some instances."	( Deferiprone: a review of its clinical potential in iron overload in beta-thalassaemia major and other transfusion-dependent diseases. Barman Balfour, JA; Foster, RH, 1999)	1.75
" Although it appears to be less effective than deferoxamine at the recommended dosage and there are concerns regarding its tolerability, it may nevertheless offer a therapeutic alternative in the management of patients unable or unwilling to receive the latter drug."	( Deferiprone: a review of its clinical potential in iron overload in beta-thalassaemia major and other transfusion-dependent diseases. Barman Balfour, JA; Foster, RH, 1999)	1.75
" The rats were given 20 mg elemental iron/kg as a ferrous sulfate solution + 1 mEq sodium bicarbonate/kg, and then dosed orally with 150 mg deferiprone/kg immediately or after 15 min."	( Acute iron intoxication: the efficacy of deferiprone and sodium biocarbonate in the prevention of iron absorption from the digestive tract. Barr, J; Berkovitch, M; Eshel, G; Kariv, N; Schejter, A; Tavori, I, 1999)	0.77
" A dose-response study suggested that basic pyridinones are relatively more effective at lower doses when compared with N-alkyl hydroxypyridinones."	( Design, synthesis and evaluation of N-basic substituted 3-hydroxypyridin-4-ones: orally active iron chelators with lysosomotrophic potential. Hider, RC; Khodr, HH; Liu, ZD; Lu, SL, 2000)	0.31
" Deferiprone, administered orally at a dosage of 50 mg/kg twice daily to birds that had been experimentally Fe loaded, significantly reduced hepatic Fe concentrations compared with levels in Fe-loaded and non-Fe-loaded controls."	( Clinical evaluation of the oral iron chelator deferiprone for the potential treatment of iron overload in bird species. Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Whiteside, DP, 2004)	1.49
"Combination chelation therapy with desferrioxamine and deferiprone has recently been suggested as a more effective tissue iron-chelating treatment for transfusion-dependent beta-thalassemia patients, although a standard dosage protocol has not yet been established."	( Intensive chelation therapy in beta-thalassemia and possible adverse cardiac effects of desferrioxamine. Aessopos, A; Deftereos, S; Farmakis, D; Kati, M; Polonifi, E; Tsironi, M, 2007)	0.59
" To evaluate if deferiprone induces its own metabolism, the pharmacokinetic disposition of the drug was also studied in the IL-DFP group after oral therapy with deferiprone at a dosage of 50 mg/kg q12h for 30 days."	( Pharmacokinetic disposition of the oral iron chelator deferiprone in the domestic pigeon (Columba livia). Barker, IK; Conlon, PD; Jacobs, RM; Mehren, KG; Spino, M; Tesoro, A; Thiessen, JJ; Whiteside, DP, 2007)	0.93
" Further advantages have been identified for the oral use of L1 and its combination with DFO, including synergistic efficacy and lower dosing with limited toxicity."	( Immune and neural status of thalassemic patients receiving deferiprone or combined deferiprone and deferoxamine chelation treatment. Athanassiou-Metaxa, M; Economou, M; Kanakoudi-Tsakalidou, F; Perifanis, V; Taparkou, A; Tourkantoni, N; Tzimouli, V; Zafiriou, D, 2008)	0.59
" Unfortunately, enhanced EPR signal intensities were observed at 300 min after dosing in patients with serum molar ratio of deferiprone to iron less than 3, suggesting the formation of incomplete iron-deferiprone complexes and consequently free radical formation."	( Pharmaco/ferrokinetic-related pro-oxidant activity of deferiprone in beta-thalassemia. Chantharaksri, U; Fucharoen, S; Jirasomprasert, T; Limenta, LM; Morales, NP; Sirijaroonwong, S; Wilairat, P; Yamanont, P, 2009)	0.81
" For DFP, the choice of dosage is crucial to optimize the effect on liver iron concentration, according to the iron load degree and transfusional iron input."	( Deferiprone. Longo, F; Massano, D; Piga, A; Roggero, S; Salussolia, I; Serra, M, 2010)	1.8
" In summary, deferiprone induced declines in proliferative responses at a dosage that is within peak serum pharmacological concentrations."	( Deferiprone modulates in vitro responses by peripheral blood T cells from control and relapsing-remitting multiple sclerosis subjects. Benedict, SH; Garcia, SL; LeVine, SM; Lynch, SG; Rues, L; Slusser, JG; Sweeney, ME, 2011)	2.18
" Dosing with DFP protected photoreceptors, decreasing the numbers of TUNEL-positive photoreceptors and increasing the number of surviving photoreceptors."	( Systemic administration of the iron chelator deferiprone protects against light-induced photoreceptor degeneration in the mouse retina. Dunaief, JL; Hadziahmetovic, M; Song, D; Song, Y; Zhong, Y, 2012)	0.64
" A constant ratio of AUC(0-∞) of L1-G to L1 and a percentage of urinary excretion of L1-G indicated that increasing the dosage does not influence deferiprone biotransformation."	( Comparison of pharmacokinetics and urinary iron excretion of two single doses of deferiprone in β-thalassemia/hemoglobin E patients. Chantraraksri, U; Fucharoen, S; Morales, NP; Rodrat, S; Tankanitlert, J; Yamanont, P, 2012)	0.81
"This study implements the design of an innovative dosage form using ultrasound-assisted compression of thermoplastic polymers and the development of controlled release tablets for the oral administration of deferiprone in two doses per day."	( A new deferiprone controlled release system obtained by ultrasound-assisted compression. Aguilar-De-Leyva, A; Caraballo, I; Daza, V; Gonçalves-Araujo, T, 2014)	1.07
" Moreover, it provides the basis for dosing recommendations in renal impairment."	( Population pharmacokinetics of deferiprone in healthy subjects. Bellanti, F; Danhof, M; Della Pasqua, O, 2014)	0.69
"Despite wide clinical experience with deferiprone, the optimum dosage in children younger than 6 years remains to be established."	( Sampling Optimization in Pharmacokinetic Bridging Studies: Example of the Use of Deferiprone in Children With β-Thalassemia. Bellanti, F; Danhof, M; Della Pasqua, O; Di Iorio, VL, 2016)	0.93
"These data suggest that no adjustment of the DFP dosage regimen in patients with renal impairment is necessary, as there were no significant changes in the systemic exposure to the drug."	( Effects of renal impairment on the pharmacokinetics of orally administered deferiprone. Fradette, C; Jayashankar, S; Pichette, V; Sicard, É; Spino, M; Stilman, A; Tricta, F; Tsang, YC, 2016)	0.66
" The pooled effects across the different dosing ratios are: serum ferritin, mean difference (MD) 454."	( Deferasirox for managing iron overload in people with thalassaemia. Allert, R; Bassler, D; Bollig, C; Meerpohl, JJ; Motschall, E; Niemeyer, CM; Rücker, G; Schell, LK, 2017)	0.46
" The PK profile of DFP in SCD subjects is consistent with previous reports in healthy adult volunteers, suggesting no special dosing adjustments are indicated for this population."	( The pharmacokinetic and safety profile of single-dose deferiprone in subjects with sickle cell disease. Fradette, C; Mercier-Ross, J; Rozova, A; Soulières, D; Tricta, F; Tsang, YC, 2022)	0.97
" In principle, iron chelators can be combined with an infinite number of dosing regimens; these involve simultaneous or sequential exposure to the chelators on the same day or alternating the drugs on different days."	( Combination chelation therapy. Aydinok, Y, 2023)	0.91

Role	Description
iron chelator	null
protective agent	Synthetic or natural substance which is given to prevent a disease or disorder or are used in the process of treating a disease or injury due to a poisonous agent.
[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]

Class	Description
4-pyridones	Any pyridone that is pyridin-4-one or its derivatives by substitution of one of more of the hydrogens.
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolase	Giardia intestinalis	Potency	6.1904	0.1409	11.1940	39.8107	AID2451
Chain A, JmjC domain-containing histone demethylation protein 3A	Homo sapiens (human)	Potency	15.8489	0.6310	35.7641	100.0000	AID504339
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	8.4279	0.1778	14.3909	39.8107	AID2147
phosphopantetheinyl transferase	Bacillus subtilis	Potency	34.1050	0.1413	37.9142	100.0000	AID1490
apical membrane antigen 1, AMA1	Plasmodium falciparum 3D7	Potency	19.9526	0.7079	12.1943	39.8107	AID720542
nonstructural protein 1	Influenza A virus (A/WSN/1933(H1N1))	Potency	0.3162	0.2818	9.7212	35.4813	AID2326
bromodomain adjacent to zinc finger domain 2B	Homo sapiens (human)	Potency	42.2395	0.7079	36.9043	89.1251	AID504333
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	1.5849	0.0355	20.9770	89.1251	AID504332
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	3.1623	0.0025	5.8400	31.6228	AID899
cytochrome P450 2C9 precursor	Homo sapiens (human)	Potency	2.5119	0.0063	6.9043	39.8107	AID883
chromobox protein homolog 1	Homo sapiens (human)	Potency	100.0000	0.0060	26.1688	89.1251	AID540317
geminin	Homo sapiens (human)	Potency	18.3564	0.0046	11.3741	33.4983	AID624296
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	2.5119	0.0063	8.2350	39.8107	AID883
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	35.4813	0.0096	10.5250	35.4813	AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Lysine-specific demethylase 6A	Homo sapiens (human)	IC50 (µMol)	4.2000	0.2000	3.9017	9.0000	AID1872468
Lysine-specific demethylase 4A	Homo sapiens (human)	IC50 (µMol)	3.2750	0.2000	2.8319	4.7600	AID1885301; AID1885302
Lysine-specific demethylase 5C	Homo sapiens (human)	IC50 (µMol)	5.6000	0.1600	2.6837	7.9433	AID1872467
Lysine-specific demethylase 2B	Homo sapiens (human)	IC50 (µMol)	8.1000	0.2100	3.8367	8.1000	AID1872466
Deoxyhypusine hydroxylase	Homo sapiens (human)	IC50 (µMol)	5.0000	5.0000	5.0000	5.0000	AID1601772
Lysine-specific demethylase 2A	Homo sapiens (human)	IC50 (µMol)	6.8000	0.1600	2.4596	6.9000	AID1872465
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
chromatin remodeling	Lysine-specific demethylase 6A	Homo sapiens (human)
regulation of gene expression	Lysine-specific demethylase 6A	Homo sapiens (human)
heart development	Lysine-specific demethylase 6A	Homo sapiens (human)
negative regulation of autophagy	Lysine-specific demethylase 4A	Homo sapiens (human)
positive regulation of gene expression	Lysine-specific demethylase 4A	Homo sapiens (human)
negative regulation of gene expression	Lysine-specific demethylase 4A	Homo sapiens (human)
cardiac muscle hypertrophy in response to stress	Lysine-specific demethylase 4A	Homo sapiens (human)
apoptotic chromosome condensation	Lysine-specific demethylase 4A	Homo sapiens (human)
response to nutrient levels	Lysine-specific demethylase 4A	Homo sapiens (human)
positive regulation of neuron differentiation	Lysine-specific demethylase 4A	Homo sapiens (human)
negative regulation of DNA-templated transcription	Lysine-specific demethylase 4A	Homo sapiens (human)
negative regulation of astrocyte differentiation	Lysine-specific demethylase 4A	Homo sapiens (human)
chromatin remodeling	Lysine-specific demethylase 4A	Homo sapiens (human)
regulation of gene expression	Lysine-specific demethylase 4A	Homo sapiens (human)
response to toxic substance	Lysine-specific demethylase 5C	Homo sapiens (human)
negative regulation of DNA-templated transcription	Lysine-specific demethylase 5C	Homo sapiens (human)
rhythmic process	Lysine-specific demethylase 5C	Homo sapiens (human)
chromatin remodeling	Lysine-specific demethylase 5C	Homo sapiens (human)
regulation of DNA-templated transcription	Lysine-specific demethylase 5C	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Lysine-specific demethylase 2B	Homo sapiens (human)
chromatin remodeling	Lysine-specific demethylase 2B	Homo sapiens (human)
spermatogenesis	Lysine-specific demethylase 2B	Homo sapiens (human)
midbrain-hindbrain boundary morphogenesis	Lysine-specific demethylase 2B	Homo sapiens (human)
fourth ventricle development	Lysine-specific demethylase 2B	Homo sapiens (human)
lateral ventricle development	Lysine-specific demethylase 2B	Homo sapiens (human)
third ventricle development	Lysine-specific demethylase 2B	Homo sapiens (human)
initiation of neural tube closure	Lysine-specific demethylase 2B	Homo sapiens (human)
positive regulation of cell growth	Lysine-specific demethylase 2B	Homo sapiens (human)
forebrain development	Lysine-specific demethylase 2B	Homo sapiens (human)
midbrain development	Lysine-specific demethylase 2B	Homo sapiens (human)
hindbrain development	Lysine-specific demethylase 2B	Homo sapiens (human)
negative regulation of neuron apoptotic process	Lysine-specific demethylase 2B	Homo sapiens (human)
embryonic camera-type eye morphogenesis	Lysine-specific demethylase 2B	Homo sapiens (human)
positive regulation of stem cell population maintenance	Lysine-specific demethylase 2B	Homo sapiens (human)
negative regulation of neural precursor cell proliferation	Lysine-specific demethylase 2B	Homo sapiens (human)
protein demethylation	Lysine-specific demethylase 2B	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Lysine-specific demethylase 2B	Homo sapiens (human)
peptidyl-lysine modification to peptidyl-hypusine	Deoxyhypusine hydroxylase	Homo sapiens (human)
double-strand break repair via nonhomologous end joining	Lysine-specific demethylase 2A	Homo sapiens (human)
chromatin remodeling	Lysine-specific demethylase 2A	Homo sapiens (human)
negative regulation of transcription by competitive promoter binding	Lysine-specific demethylase 2A	Homo sapiens (human)
circadian regulation of gene expression	Lysine-specific demethylase 2A	Homo sapiens (human)
regulation of circadian rhythm	Lysine-specific demethylase 2A	Homo sapiens (human)
protein demethylation	Lysine-specific demethylase 2A	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Lysine-specific demethylase 2A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein binding	Lysine-specific demethylase 6A	Homo sapiens (human)
histone demethylase activity	Lysine-specific demethylase 6A	Homo sapiens (human)
metal ion binding	Lysine-specific demethylase 6A	Homo sapiens (human)
histone H3K27me2/H3K27me3 demethylase activity	Lysine-specific demethylase 6A	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Lysine-specific demethylase 6A	Homo sapiens (human)
chromatin DNA binding	Lysine-specific demethylase 6A	Homo sapiens (human)
protein binding	Lysine-specific demethylase 4A	Homo sapiens (human)
zinc ion binding	Lysine-specific demethylase 4A	Homo sapiens (human)
ubiquitin protein ligase binding	Lysine-specific demethylase 4A	Homo sapiens (human)
histone demethylase activity	Lysine-specific demethylase 4A	Homo sapiens (human)
methylated histone binding	Lysine-specific demethylase 4A	Homo sapiens (human)
histone H3K36 demethylase activity	Lysine-specific demethylase 4A	Homo sapiens (human)
histone H3K36me2/H3K36me3 demethylase activity	Lysine-specific demethylase 4A	Homo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activity	Lysine-specific demethylase 4A	Homo sapiens (human)
histone H3K9 demethylase activity	Lysine-specific demethylase 4A	Homo sapiens (human)
DNA binding	Lysine-specific demethylase 5C	Homo sapiens (human)
protein binding	Lysine-specific demethylase 5C	Homo sapiens (human)
zinc ion binding	Lysine-specific demethylase 5C	Homo sapiens (human)
histone demethylase activity	Lysine-specific demethylase 5C	Homo sapiens (human)
histone H3K4 demethylase activity	Lysine-specific demethylase 5C	Homo sapiens (human)
histone H3K4me/H3K4me2/H3K4me3 demethylase activity	Lysine-specific demethylase 5C	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Lysine-specific demethylase 2B	Homo sapiens (human)
DNA binding	Lysine-specific demethylase 2B	Homo sapiens (human)
protein binding	Lysine-specific demethylase 2B	Homo sapiens (human)
zinc ion binding	Lysine-specific demethylase 2B	Homo sapiens (human)
rRNA binding	Lysine-specific demethylase 2B	Homo sapiens (human)
histone demethylase activity	Lysine-specific demethylase 2B	Homo sapiens (human)
unmethylated CpG binding	Lysine-specific demethylase 2B	Homo sapiens (human)
histone H3K36 demethylase activity	Lysine-specific demethylase 2B	Homo sapiens (human)
histone H3K36me/H3K36me2 demethylase activity	Lysine-specific demethylase 2B	Homo sapiens (human)
transcription coregulator activity	Lysine-specific demethylase 2B	Homo sapiens (human)
iron ion binding	Deoxyhypusine hydroxylase	Homo sapiens (human)
protein binding	Deoxyhypusine hydroxylase	Homo sapiens (human)
deoxyhypusine monooxygenase activity	Deoxyhypusine hydroxylase	Homo sapiens (human)
protein binding	Lysine-specific demethylase 2A	Homo sapiens (human)
zinc ion binding	Lysine-specific demethylase 2A	Homo sapiens (human)
histone demethylase activity	Lysine-specific demethylase 2A	Homo sapiens (human)
unmethylated CpG binding	Lysine-specific demethylase 2A	Homo sapiens (human)
histone H3K36 demethylase activity	Lysine-specific demethylase 2A	Homo sapiens (human)
histone H3K36me/H3K36me2 demethylase activity	Lysine-specific demethylase 2A	Homo sapiens (human)
transcription coregulator activity	Lysine-specific demethylase 2A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleus	Lysine-specific demethylase 6A	Homo sapiens (human)
nucleoplasm	Lysine-specific demethylase 6A	Homo sapiens (human)
MLL3/4 complex	Lysine-specific demethylase 6A	Homo sapiens (human)
histone methyltransferase complex	Lysine-specific demethylase 6A	Homo sapiens (human)
fibrillar center	Lysine-specific demethylase 4A	Homo sapiens (human)
nucleus	Lysine-specific demethylase 4A	Homo sapiens (human)
nucleoplasm	Lysine-specific demethylase 4A	Homo sapiens (human)
cytosol	Lysine-specific demethylase 4A	Homo sapiens (human)
pericentric heterochromatin	Lysine-specific demethylase 4A	Homo sapiens (human)
nucleus	Lysine-specific demethylase 4A	Homo sapiens (human)
chromatin	Lysine-specific demethylase 4A	Homo sapiens (human)
nucleus	Lysine-specific demethylase 5C	Homo sapiens (human)
nucleoplasm	Lysine-specific demethylase 5C	Homo sapiens (human)
cytosol	Lysine-specific demethylase 5C	Homo sapiens (human)
nucleus	Lysine-specific demethylase 5C	Homo sapiens (human)
chromatin	Lysine-specific demethylase 5C	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
nucleus	Lysine-specific demethylase 2B	Homo sapiens (human)
nucleoplasm	Lysine-specific demethylase 2B	Homo sapiens (human)
chromosome	Lysine-specific demethylase 2B	Homo sapiens (human)
nucleolus	Lysine-specific demethylase 2B	Homo sapiens (human)
PcG protein complex	Lysine-specific demethylase 2B	Homo sapiens (human)
cellular_component	Deoxyhypusine hydroxylase	Homo sapiens (human)
cytosol	Deoxyhypusine hydroxylase	Homo sapiens (human)
nucleoplasm	Lysine-specific demethylase 2A	Homo sapiens (human)
chromosome	Lysine-specific demethylase 2A	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1675815	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability at 1.25 to 100 uM after 16 hrs by MTT assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID736789	Selectivity index, ratio of GI50 for human HL60 cells to GI50 for Trypanosoma brucei TC211	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID1583811	Toxicity in Sprague-Dawley rat assessed as reduction in total white cell counts at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID1583813	Toxicity in Sprague-Dawley rat assessed as reduction in lymphocytes counts at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID363032	Iron-clearing efficiency in po dosed [59Fe]ferritin-loaded Wistar rat assessed as iron mobilization	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1675833	Induction of iron chelation in Pseudomonas aeruginosa PAO1 assessed as increase in intracellular pyoverdin level at 1.25 to 20 uM in presence of 10 uM FeCl3 by fluorescence microplate reader assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID1583753	Lipophilicity coefficient, logP of the compound in Tris buffer at pH 7.0 (100 mM/n-octanol)	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID1583814	Toxicity in Sprague-Dawley rat assessed as reduction in monocytes counts at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID15965	Partition coefficient (logD7.4)	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1663429	Metal chelating activity assessed as Fe3+ complex formation by measuring stability constant for Fe(I)2 in using pre Fe+3 complexed compound (FeCl3) in 0.1 M KCl :DMSO solution UV-pH titration based spectrophotometric analysis	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID24869	pFe3+ (negative logarithm of the concentration of the free Iron(III) in solution) of the compound.	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID363029	Dissociation constant, pKa corresponding to dissociation of the 3-hydroxyl group by potentiometric titration	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1570046	Dissociation constant, pKa1 of compound for protonation of the 4-oxo group in DMSO:KCl at 30 uM/L incubated for 1 min by UV-Vis spectrophotometry	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID191834	The treatment period of compound (microg of Fe/15h) for urinary excretion of Iron after peroral administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID1292132	Binding affinity to iron(3) assessed as pFe3+ values after 5 mins	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID1663430	Metal chelating activity assessed as Fe3+ complex formation by measuring stability constant for Fe(I)3 in using pre Fe+3 complexed compound (FeCl3) in 0.1 M KCl :DMSO solution UV-pH titration based spectrophotometric analysis	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID26628	Ligand pka1 value was investigated by spectrophotometric titration	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1675849	Antibiofilm activity against Pseudomonas aeruginosa PAO1 assessed as inhibition of biofilm formation after 18 hrs by crystal violet staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID193840	The amount iron excretion in the bile duct-cannulated rats when iron chelator administered orally at dose 100 mg/kg	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID193972	The amount iron excretion in the bile duct-cannulated rats when iron chelator administered subcutaneously at dose 100 mg/kg	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID135326	BBB penetration classification	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1583747	Distribution coefficient, logP (FeL3) of the compound	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID195539	Compound was tested for 50% Inhibition of lipid peroxidation in rat brain homogenate	2000	Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15	3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID363026	Dissociation constant, pKa corresponding to dissociation of the 3-hydroxyl group by spectrophotometric titration	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID775827	Binding affinity to human holo-transferrin assessed as pseudo-first-order rate constant measured as removal of ferric ion at 1 mM measured for 1 hr by UV-vis spectrophotometric analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Investigating the selectivity of metalloenzyme inhibitors.
AID26839	Ligand pka2 value was investigated by spectrophotometric titration	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1570049	Binding affinity to Fe3+ assessed as equilibrium binding constant logK2 in DMSO:KCl pH 2 to 10.5 at 30 uM incubated for 1 min by UV-Vis spectrophotometric method	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID577271	Inhibition of soybean lipoxygenase at 100 uM after 15 mins	2011	Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3	Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease.
AID363031	Partition coefficient, log P of the compound	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1872465	Inhibition of KDM2A (unknown origin)	2022	European journal of medicinal chemistry, Mar-05, Volume: 231	Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
AID248013	Inhibitory concentration against growth of murine L1210 cells at 48 hours	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID1292133	Octanol-water partition coefficient, log P of the compound by shake-flask method	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID1675841	Metal chelating activity assessed as negative logarithm of total free ferric ion concentration in a solution at 60 uM measured after 48 hrs in presence of CP645 probe and Fe-NTA by fluorescence spectrophotometry analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID191832	Biliary excretion of iron was measured after giving intravenous dose of 0.2 mmol/kg during treatment period in rat	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Mobilization of iron by chiral and achiral anionic 3-hydroxypyrid-4-ones.
AID1675836	Induction of iron chelation in Pseudomonas aeruginosa PAO1 assessed as increase in iron deficiency by measuring change in total ferric ion concentration at 20 uM by inductively coupled plasma mass spectrometry (Rvb = 1.91 +/- 0.8 uM)	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID174351	The control period of compound (microg of Fe/h) for biliary excretion of Iron after intravenous administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID1498400	Antibacterial activity against Pseudomonas aeruginosa CGMCC 1.2342 assessed as growth inhibition at 100 ug/ml after 24 hrs	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers.
AID1292130	Drug metabolism in human liver microsomes assessed as glucuronidation at 10 uM after 24 hrs by mass spectrophotometry in presence of NADPH and UDPGA	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID179682	The compound was tested in vivo for Iron Mobilization efficacy in Fe-Ferritin Loaded Rat model	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: structure-activity investigation of metalloenzyme inhibition by iron chelators.
AID26569	Compound was determined for their affinity constants(log K2) with Fe(III) complex	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID191835	The treatment period of compound (microg of Fe/h) for biliary excretion of Iron after intravenous administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID1583748	Iron scavenging activity in 59Fe-ferritin-loaded rat assessed as iron mobilization level at 450 umol/kg, po dosed 1 hr after 59Fe-ferritin injection and measured 24 hrs after 59Fe-ferritin injection by gamma counting method relative to control	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID460410	Toxicity in human SK-N-MC cells by MTT method	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID229913	Spectrophotometric selectivity ratio for pKa2 and pKa3	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1663427	Metal chelating activity assessed as iron chelation	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1498402	Antibacterial activity against Bacillus subtilis CGMCC 1.0108 assessed as growth inhibition at 100 ug/ml after 24 hrs	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers.
AID1675832	Induction of iron chelation in Pseudomonas aeruginosa PAO1 assessed as increase in intracellular pyochelin level at 1.25 to 20 uM in presence of 10 uM FeCl3 by fluorescence microplate reader assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1776746	Antifungal activity against Candida albicans ATCC 10231
AID191836	Urinary iron excretion was measured after giving oral dose of 1 mmol/kg during treatment period in rat	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Mobilization of iron by chiral and achiral anionic 3-hydroxypyrid-4-ones.
AID251614	Iron clearing efficiency in bile-duct-cannulated rodents following a subcutaneous dosage of 450 umol/kg	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID26754	log K3 value of the compound	1994	Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4	Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID251610	Iron clearing efficiency in bile of rodents following a subcutaneous dosage of 450 umol/kg	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID249436	Ratio of intracellular concentration to that of treatment concentration in L1210 cells	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID28954	Partition coefficient (logP)	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: structure-activity investigation of metalloenzyme inhibition by iron chelators.
AID26553	Compound was determined for their affinity constants(log K1) with Fe(III) complex.	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID251612	Iron clearing efficiency in urine of rodents following a subcutaneous dosage of 450 umol/kg	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID203884	Compound was tested for the inhibition of spermidine transporter by using [3H]SPD transport in L1210 cell	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID439757	Antiproliferative activity against mouse L1210 cells	2009	Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17	Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID363024	Dissociation constant, pKa corresponding to protonation of the 4-hydroxy group by spectrophotometric titration	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID96445	Compound was determined for spermine (SPM) level in L1210 cells after treatment at a concentration of 50 uM and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID252379	Intracellular concentration was determined in murine L1210 cells after treatment with 50 uM compound for 48 h	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID736793	Antitrypanosomal activity against Trypanosoma brucei TC211 after 24 hrs by alamar blue assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID28984	Partition coefficient (logD7.4)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID1776747	Antibiofilm activity against Candida albicans ATCC 10231 assessed as inhibition of biofilm formation
AID1079935	Cytolytic 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]
AID1706515	Octanol/water partition coefficient, log P of the compound shaken for 45 mins and measured after 15 mins	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
AID1570047	Binding affinity to Fe3+ assessed as equilibrium binding constant logK1 in pH 0.9 to 2.1 at 30 uM incubated for 20 mins by UV-Vis spectrophotometric method	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID29366	Acid dissociation constant (pKa1) was determined	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID1824819	Metal chelating activity assessed as compound-Fe(3) complex formation assessed as free ion concentration by fluorescence spectroscopy	2022	Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1	New
AID736787	Selectivity index, ratio of GI50 for human HL60 cells to GI50 for Leishmania infantum MHOM/BR/1972/LD promastigotes	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID1428595	Binding affinity to Zn2+ assessed as cumulative stability constant	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID1583825	Toxicity in Sprague-Dawley rat assessed as induction of histopathological changes in thymus at 25 to 116 mg/kg, po dosed daily for 4 weeks and measured after additional 4 weeks period in absence of drug	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID1885302	Inhibition of KDM4A (unknown origin) measured by LANCEUltra assay	2022	Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14	Recent Advances with KDM4 Inhibitors and Potential Applications.
AID499569	Biodistribution in Dunkin-Hartley guinea pig brain parenchyma at 800 uM, iv after 20 mins using [3H]mannitol vascular space marker by scintillation counting	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	Glucosylated deferiprone and its brain uptake: implications for developing glucosylated hydroxypyridinone analogues intended to cross the blood-brain barrier.
AID1428593	Binding affinity to Fe3+ assessed as cumulative stability constant	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID1292131	Drug metabolism in human liver microsomes assessed as hydroxylation at 10 uM after 24 hrs by mass spectrophotometry in presence of NADPH and UDPGA	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID26251	Partition coefficient (logD7.4) for iron(III) complexes	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID203887	Compound was tested for the enzyme activity against Spermidine/spermine N1-acetyl transferase (SSAT) in L1210 cells and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID19829	Partition coefficient (logP)	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1079936	Choleostatic 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]
AID199306	Compound was tested for the enzyme activity against S-Adenosyl-methionine decarboxylase in L1210 cells and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1583817	Toxicity in Sprague-Dawley rat assessed as increase in reticulocyte population at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID460408	Partition coefficient, log P in presence of Fe(3+) by RP-HPLC	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID26838	Ligand pka2 value was investigated by potentiometric titration	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID26574	Compound was determined for their affinity constants(log K3) with Fe(III) complex.	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1706513	Binding affinity to iron assessed as pFe3+	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
AID7188	Inhibitory activity against 5-lipoxygenase, by using soybean lipoxygenase spectrophotometric assay	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: structure-activity investigation of metalloenzyme inhibition by iron chelators.
AID1583824	Toxicity in Sprague-Dawley rat assessed as induction of histopathological changes in bone marrow at 25 to 116 mg/kg, po dosed daily for 4 weeks and measured after additional 4 weeks period in absence of drug	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID1675814	Cytotoxicity against human L02 cells assessed as reduction in cell viability at 1.25 to 100 uM after 16 hrs by MTT assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1
AID1570056	Binding affinity to Fe3+ assessed as equilibrium binding constant logK3 in KCl pH 2 to 10.5 at incubated for 1 mins 30 uM by UV-Vis spectrophotometric method	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID196215	Ability to protect cerebellar granule cells (CGC) from iodoacetate (IAA)-induced toxicity	2000	Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15	3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID29379	Acid dissociation constant (pKa2) was determined	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID1663428	Metal chelating activity assessed as Fe3+ complex formation by measuring stability constant for FeI in using pre Fe+3 complexed compound (FeCl3) in 0.1 M KCl :DMSO solution UV-pH titration based spectrophotometric analysis	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID174350	The control period of compound (microg of Fe/15h) for urinary excretion of Iron after peroral administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID174349	The control period of compound (microg of Fe/15h) for urinary excretion of Iron after intravenous administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID363030	Octanol-MOPS buffer distribution coefficient, DC at pH 7.4	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1583810	Toxicity in Sprague-Dawley rat assessed as induction of mortality at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID191833	The treatment period of compound (microg of Fe/15h) for urinary excretion of Iron after intravenous administration to the rats	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones.
AID1885301	Inhibition of KDM4A (unknown origin) measured by formaldehyde dehydrogenase (FDH)-coupled fluorescence assay	2022	Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14	Recent Advances with KDM4 Inhibitors and Potential Applications.
AID196221	Relative efficacy gives an indication of the percent of viable cells (Rat cerebellar granule cells) at the maximal efficacious concentration of 46.7 uM	2000	Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15	3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID1498399	Antibacterial activity against Escherichia coli CGMCC 1.0907 assessed as growth inhibition at 100 ug/ml after 24 hrs	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers.
AID244579	Ability to compete with [3H]SPD for the polyamine transport apparatus in L1210 cells	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID28931	Logarithm of cumulative stability constant was determined	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID193977	The amount of iron-binding when iron chelator administered in the bile duct-cannulated rats.	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1706522	Iron scavenging activity in 59Fe-ferritin-loaded Wistar rat assessed as iron mobilization efficacy at 450 umol/kg, po dosed 1 hr after 59Fe-ferritin injection and measured 24 hrs after 59Fe-ferritin injection by gamma counting method relative to control	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
AID96466	Compound was tested for the growth inhibition of L1210 cell at a duration of 96 h	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID1292134	Octanol-water partition coefficient, log P of the compound with iron complex by shake-flask method	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID210782	Percentage of removal of iron from iron-protein-transferrin	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID1824793	Antibiofilm activity against Pseudomonas aeruginosa PAO1 assessed as effect on pyochelin production fluorescence at 1.25 to 20 uM by fluorescence assay	2022	Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1	New
AID363034	Iron-clearing efficiency in po dosed [59Fe]ferritin-loaded Wistar rat assessed as iron removal	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID736784	Iron cheating activity assessed as pFe3+ value at pH 7.45 by spectrophotometry	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID26620	Compound was tested for equilibrium constants (pKa1) spectrophotometrically.	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1292135	Binding affinity to iron(3) assessed as pFe3+ values after 10 to 30 mins	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone.
AID1428594	Binding affinity to Cu2+ assessed as cumulative stability constant	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID150565	Compound was tested for the enzyme activity against ornithine decarboxylase (ODC) in L1210 cells and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID26572	log K2 value of the compound	1994	Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4	Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies.
AID23940	Affinity constant log beta-3 value for Fe(III) complex	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1570048	Dissociation constant, pKa2 of compound for 3-(or 5-) hydroxyl group in DMSO:KCl at 30 uM/L incubated for 1 min by UV-Vis spectrophotometry	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID96460	Compound was tested for the growth inhibition of L1210 cell at a duration of 48 h	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID96304	Compound was determined for putrescine (PUT) level in L1210 cells after treatment at a concentration of 50 uM and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID96442	Compound was determined for spermidine (SPD) level in L1210 cells after treatment at a concentration of 50 uM and expressed as percent compound found in untreated controls.	2003	Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25	Polyamine-iron chelator conjugate.
AID1498401	Antibacterial activity against Staphylococcus aureus CGMCC 1.0089 assessed as growth inhibition at 100 ug/ml after 24 hrs	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers.
AID26573	Affinity constant log K3 value for Fe(III) complex	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID26568	Affinity constant log K2 value for Fe(III) complex	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1583818	Toxicity in Sprague-Dawley rat assessed as reduction in erythrocyte population at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID499568	Biodistribution in Dunkin-Hartley guinea pig brain at 800 uM, iv after 20 mins using [3H]mannitol vascular space marker by scintillation counting	2010	Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15	Glucosylated deferiprone and its brain uptake: implications for developing glucosylated hydroxypyridinone analogues intended to cross the blood-brain barrier.
AID72978	Percentage of removal of iron from iron-protein-ferritin	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
AID577273	Inhibition of soybean lipoxygenase after 15 mins	2011	Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3	Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease.
AID736792	Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes after 24 hrs by MTT assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID26823	Acid dissociation constant was determined	1994	Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4	Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies.
AID1079938	Chronic 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]
AID363033	Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM267TR after 24 hrs by [3H]hypoxanthine	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1428596	Binding affinity to CP645 probe-labeled Fe3+ in DMSO/MOPS buffer assessed as concentration of free Fe3+ in solution at 60 uM after 48 hrs by spectrofluorophotometric method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID1893771	Inhibition of recombinant human QC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis	2022	ACS medicinal chemistry letters, Sep-08, Volume: 13, Issue:9	2-Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRPα Checkpoint.
AID1663414	Dissociation constant, pKa2 of compound for dissociation of the 3-hydroxyl group in 0.1 M KCl incubated for 1 min by UV-pH titration based spectrophotometric analysis	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1706563	Electrochemical behavior of the compound assessed as redox potential	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
AID736791	Antileishmanial activity against Leishmania infantum MHOM/BR/1972/LD promastigotes after 48 hrs by MTT assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID736796	Antimalarial activity against Plasmodium falciparum ITG2G1	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID26615	Acid dissociation constant was determined	1994	Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4	Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies.
AID370490	Induction of iron removal from 59Fe]transferrin assessed as iron release after 3 hrs relative to control	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID1583812	Toxicity in Sprague-Dawley rat assessed as reduction in neutrophils counts at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID1583815	Toxicity in Sprague-Dawley rat assessed as reduction in eosinophils counts at 200 mg/kg, po dosed once daily for 2 months as 5 days per week schedule	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID179655	Compound was tested in vivo for Iron mobilization efficacy against hepatocytes in normal fasted rats(loaded with [59Fe]-Ferritin).	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1776748	Antibiofilm activity against Candida albicans ATCC 10231 assessed as reduction in mature biofilm
AID248014	Inhibitory concentration against growth of murine L1210 cells at 96 hours	2005	Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12	Polyamine-vectored iron chelators: the role of charge.
AID1570050	Binding affinity to Fe3+ assessed as equilibrium binding constant logK3 in DMSO:KCl pH 2 to 10.5 at 30 uM incubated for 1 min by UV-Vis spectrophotometric method	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID460409	Toxicity in MDCK cells by MTT method	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID1663413	Dissociation constant, pKa1 of compound for protonation of the 4-oxo group in 0.1 M KCl incubated for 1 min by UV-pH titration based spectrophotometric analysis	2020	Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12	Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
AID1872466	Inhibition of KDM2B (unknown origin)	2022	European journal of medicinal chemistry, Mar-05, Volume: 231	Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
AID26567	log K1 value of the compound	1994	Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4	Copper complexation by 3-hydroxypyridin-4-one iron chelators: structural and iron competition studies.
AID1079933	Acute 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
AID1706557	Antiviral activity against HIV1 BaL infected in human peripheral blood lymphocytes assessed as reduction in p24 production incubated for 5 days by ELISA	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
AID26551	Affinity constant log K1 value for Fe(III) complex	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1601772	Inhibition of DOHH (unknown origin)	2019	European journal of medicinal chemistry, Mar-01, Volume: 165	Medicinal chemistry of metal chelating fragments in metalloenzyme active sites: A perspective.
AID26828	Compound was tested for equilibrium constants (pKa2) of the (carboxyalkyl) pyridinone corresponds to the carboxylic function spectrophotometrically..	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID26627	Ligand pka1 value was investigated by potentiometric titration	1999	Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23	Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: novel iron chelators with enhanced pFe(3+) values.
AID1570055	Binding affinity to Fe3+ assessed as equilibrium binding constant logK2 in KCl pH 2 to 10.5 at 30 uM incubated for 20 mins by UV-Vis spectrophotometric method	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.
AID1079931	Moderate 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]
AID1872468	Inhibition of KDM6A (unknown origin)	2022	European journal of medicinal chemistry, Mar-05, Volume: 231	Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
AID179221	Compound was tested for its inhibitory activity against lipid peroxidation in rat brain homogenates.	2002	Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22	Prodrug and covalent linker strategies for the solubilization of dual-action antioxidants/iron chelators.
AID736790	Cytotoxicity against human HL60 cells by alamar blue assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID460407	Partition coefficient, log P by shake flask method	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID736788	Selectivity index, ratio of GI50 for human HL60 cells to GI50 for Trypanosoma cruzi trypomastigotes	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID363027	Dissociation constant, pKa corresponding to protonation of the 4-hydroxy group by potentiometric titration	2008	European journal of medicinal chemistry, May, Volume: 43, Issue:5	Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
AID1872467	Inhibition of KDM5C (unknown origin)	2022	European journal of medicinal chemistry, Mar-05, Volume: 231	Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID26260	Partition coefficient (logD7.4)	1998	Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18	Synthesis, physicochemical properties, and evaluation of N-substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID184512	The compound was tested for % iron mobilization in Fe-Ferritin Loaded Rat model	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: structure-activity investigation of metalloenzyme inhibition by iron chelators.
AID1583823	Toxicity in Sprague-Dawley rat assessed as induction of histopathological changes in pancreas at 25 to 116 mg/kg, po dosed daily for 4 weeks and measured after additional 4 weeks period in absence of drug	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	CN128: A New Orally Active Hydroxypyridinone Iron Chelator.
AID460406	Partition coefficient, log P by RP-HPLC	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID558870	Antifungal activity against Aspergillus fumigatus B5233 conidia after 16 hrs by fluorescence-based microplate assay at pH 7.2	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antifungal activities of natural and synthetic iron chelators alone and in combination with azole and polyene antibiotics against Aspergillus fumigatus.
AID460411	Induction of [59Fe] mobilization in human SK-N-MC cells prelabeled with [59Fe]transferrin at 50 uM after 3 hrs relative to untreated control	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID588461	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set	2006	Cytometry. 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.
AID588461	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588460	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set	2006	Cytometry. 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.
AID588460	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. 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.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. 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.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. 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.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set	2006	Cytometry. 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.
AID588459	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal 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.
AID1745855	NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854	NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1224864	HCS microscopy assay (F508del-CFTR)	2016	PloS one, , Volume: 11, Issue:10	Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	20 (2.04)	18.7374
1990's	197 (20.10)	18.2507
2000's	313 (31.94)	29.6817
2010's	345 (35.20)	24.3611
2020's	105 (10.71)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	142 (13.98%)	5.53%
Reviews	136 (13.39%)	6.00%
Case Studies	62 (6.10%)	4.05%
Observational	10 (0.98%)	0.25%
Other	666 (65.55%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (57)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Increased Survival and Reversion of Iron-Induced Cardiac Disease in Patients With Thalassemia Major Receiving Intensive Combined Chelation Therapy [NCT00800761]	Phase 4	0 participants	Interventional	2001-12-31	Completed
Safety and Acceptability of Deferiprone Delayed Release Tablets in Patients With Systemic Iron Overload [NCT03802916]	Phase 2	30 participants (Actual)	Interventional	2019-03-06	Completed
A Phase Ib Randomized, Double-blind, Placebo-controlled, Ascending Sequential Dose, Adaptive Design Study to Evaluate the Safety, Antiretroviral Activity, and Pharmacokinetics of Intravenous Deferiprone in Treatment-Naïve HIV-Positive Subjects [NCT02456558]	Phase 1	30 participants (Actual)	Interventional	2015-06-30	Completed
The Shuttle Effect : Combination Therapy With Deferiprone and Deferasirox in Transfusion-dependent Thalassemia Patients. [NCT02198508]		13 participants (Actual)	Interventional	2007-07-31	Completed
A 24-Week, Open Label, Uncontrolled Study of the Safety and Efficacy of Ferriprox™ (Deferiprone) Oral Solution in Iron Overloaded Pediatric Patients With Transfusion-Dependent Anemia [NCT00529152]	Phase 3	100 participants (Actual)	Interventional	2007-08-31	Completed
Study of Safty and Efficacy of Adjuvant Vitamin c in Augmenting Iron Chelation [NCT02083575]	Phase 2/Phase 3	50 participants (Anticipated)	Interventional	2014-04-30	Not yet recruiting
A Phase II, Randomized, Double-Blind, Placebo-Controlled Trial to Assess the Efficacy and Safety of CRMD-001 in Contrast-Induced Acute Oxidative Kidney Injury [NCT01146925]	Phase 2	60 participants (Anticipated)	Interventional	2010-06-30	Completed
Feasibility and Safety Pilot Therapeutic Study of the Iron Chelator Deferiprone in Amyotrophic Lateral Sclerosis [NCT02164253]	Phase 2	23 participants (Actual)	Interventional	2013-09-30	Completed
The Effect of Treatment With the Oral Iron Chelator Deferiprone on the Oxidative Stress of Blood Cells and on Iron Overload Status in Transfusion Dependent, Iron-overloaded Patients With Low Risk Myelodysplastic Syndrome [NCT02477631]	Phase 2	19 participants (Actual)	Interventional	2016-02-29	Completed
Single Dose Crossover Comparative Bioavailability Study of Deferiprone 600 mg Delayed Release Tablets Versus Deferiprone Oral Solution in Healthy Male and Female Volunteers Following a 1200 mg Dose [NCT02442310]	Phase 1	20 participants (Actual)	Interventional	2015-05-31	Completed
Long-term Safety and Efficacy Study of Ferriprox® for the Treatment of Transfusional Iron Overload in Patients With Sickle Cell Disease or Other Anemias [NCT02443545]	Phase 4	300 participants (Anticipated)	Interventional	2015-05-31	Enrolling by invitation
A Decisional Algorithm to Start Iron Chelation in Minimally Transfused Young Beta-thalassemia Major Patients Naive to Iron Chelation Therapy. A Comparative Randomized Prospective Study [NCT02173951]	Phase 2/Phase 3	64 participants (Anticipated)	Interventional	2014-07-31	Not yet recruiting
A Double Blind, Placebo-controlled, Dose-escalating, Multiple Dose Study, Investigating the Safety, Antiretroviral Activity, Tolerability and Pharmacokinetic Profile of Deferiprone When Administered in Healthy Volunteers and Asymptomatic HIV Infected Subj [NCT02191657]	Phase 1	26 participants (Actual)	Interventional	2006-11-30	Completed
Phase IV Study of the Use of Sequential DFP-DFO Versus DFP in Thalassemia Major Patients [NCT00733811]	Phase 4	213 participants (Actual)	Interventional	2000-09-30	Completed
Efficacy and Safety of the Iron Chelator Deferiprone on Iron Overload in the Brain in Parkinson's Disease [NCT00943748]	Phase 2/Phase 3	40 participants (Actual)	Interventional	2009-10-31	Completed
An Open-label, Single Treatment, Safety and Efficacy, Long-term Study of Deferiprone in Subjects With Friedreich's Ataxia [NCT00897221]	Phase 2	36 participants (Actual)	Interventional	2009-06-30	Completed
Thalassemia Clinical Research Network - Cardiac L1/DFO Trial [NCT00115349]	Phase 2	20 participants (Actual)	Interventional	2005-06-30	Terminated(stopped due to due to low enrollment)
Treatment of Wolfram Syndrome Type 2 With the Chelator Deferiprone, and Incretin Based Therapy [NCT02882477]	Phase 2/Phase 3	20 participants (Anticipated)	Interventional	2016-12-31	Not yet recruiting
A Phase III, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Assess the Efficacy and Safety of Deferiprone in the Reduction of Morbidity and Mortality in Patients With Chronic Kidney Disease Undergoing Diagnostic or Interventional Cardi [NCT01391520]	Phase 3	0 participants (Actual)	Interventional	2012-01-31	Withdrawn(stopped due to Sponsor encountered funding issues for this study.)
An N of One Clinical Trial to Pilot the Feasibility of Using the Iron-Chelator Deferiprone on Mild Cognitive Impairment [NCT02878538]	Early Phase 1	0 participants (Actual)	Interventional	2018-01-31	Withdrawn(stopped due to Study was withdrawn before IRB approval)
Randomized Trial Comparing the Relative Efficacy of Deferiprone to That of Deferoxamine in Removing Excess Cardiac Iron in Thalassemia Major Patients [NCT00105495]	Phase 4	60 participants	Interventional	2002-12-31	Completed
Safety and Efficacy of Early-start Deferiprone Treatment in Infants and Young Children Newly Diagnosed With Transfusion-dependent Beta Thalassemia [NCT03591575]	Phase 4	64 participants (Actual)	Interventional	2018-11-09	Completed
Compassionate Use of Deferiprone in Patients With Thalassemia and Iron-Induced Heart Disease [NCT00293098]		0 participants	Expanded Access	2006-03-31	Approved for marketing
Long-term Iron Chelation in the Prevention of Secondary Remote Degeneration After Stroke [NCT05111821]	Phase 2	100 participants (Anticipated)	Interventional	2022-06-08	Recruiting
A Randomized Prospective Comparative Study of Efficacy and Safety of Continued Iron Chelation Therapy In Poly-transfused Thalassemia Patients With Low Serum Ferritin (< 500 ng/ml) [NCT01996683]		50 participants (Anticipated)	Interventional	2014-11-30	Not yet recruiting
A Dose-Ranging Study of the Efficacy, Safety, and Pharmacokinetics of Deferiprone Delayed Release Tablets in Patients With Parkinson's Disease [NCT02728843]	Phase 2	140 participants (Actual)	Interventional	2016-10-12	Completed
Modulation of Oxidative Stress and Apoptosis of Energy Metabolism by Deferiprone From the Circulating Lymphocytes of Patients With Parkinson's Disease or Amyotrophic Lateral Sclerosis [NCT02880033]		90 participants (Actual)	Interventional	2011-02-28	Completed
A Six-month Double-blind, Randomized, Placebo-controlled Study Investigating the Safety and Tolerability of Deferiprone in Patients With Friedreich's Ataxia [NCT00530127]	Phase 1/Phase 2	80 participants (Anticipated)	Interventional	2008-04-30	Completed
A Phase 1/2a Exploratory Clinical Trial to Evaluate the Safety of Oral Deferiprone (14 Days) Including Its Effect on Decreasing the Content of Iron in Subjects With Aneurysmal Subarachnoid Hemorrhage (aSAH) sIRB [NCT03754725]	Phase 1/Phase 2	66 participants (Anticipated)	Interventional	2020-10-01	Recruiting
Retrospective and Prospective Multicenter Study Using Deferiprone (L1) Alone or in Combination With Desferrioxamine for the Treatment of Iron Overload in Transfusion-dependent Patients [NCT00349453]	Phase 2	24 participants (Actual)	Interventional	2005-03-31	Completed
Randomized Open-label Phase III Study With Deferiprone and/or Desferrioxamine in Iron Overloaded Patients [NCT00350662]	Phase 3	95 participants (Actual)	Interventional	2002-01-31	Completed
Characterisation of Relative Bioavailability of a Generic Deferiprone Formulation in Comparison With a Marketed Reference Product in a Single Dose, 2-period-crossover Design Under Fasting Conditions; Controlled, Open, Randomised, no Blinded Study With Bio [NCT02980458]	Phase 1	25 participants (Actual)	Interventional	2016-08-31	Completed
A Prospective Randomized Comparative Study of Efficacy and Safety of Combined Deferiprone (DFP) and Deferasirox Versus DFP and Desferrioxamine (DFO) Therapy in Diseases With Severe Iron Overload [NCT01511848]	Phase 2/Phase 3	60 participants (Anticipated)	Interventional	2012-02-29	Not yet recruiting
A Randomized, Placebo Controlled, Double Blind Trial of the Effect of Combined Therapy With Deferoxamine and Deferiprone on Myocardial Iron in Thalassemia Major Using Cardiovascular Magnetic Resonance [NCT00103753]	Phase 4	65 participants	Interventional	2004-05-31	Active, not recruiting
Multicentre, Randomised, Open Label, Non-inferiority Trial to Evaluate the Efficacy and Safety of Deferiprone Compared to Deferasirox in Patients Aged From 1 Month to Less Than 18 Years Affected by Transfusion Dependent Haemoglobinopathies [NCT01825512]	Phase 3	435 participants (Actual)	Interventional	2014-03-17	Completed
The Pharmacokinetic Profile of a Single Dose of Ferriprox® in Patients With Sickle Cell Disease [NCT01835496]	Phase 1	8 participants (Actual)	Interventional	2013-05-31	Completed
Multi-centre, Oral Single Dose Experimental and Modelling Study to Evaluate the Pharmacokinetics of Deferiprone in Patients Aged From 1 Month to Less Than 6 Years of Age Affected by Transfusion-dependent Haemoglobinopathies. [NCT01740713]	Phase 2	23 participants (Actual)	Interventional	2012-12-31	Completed
A Randomized, Double-blind, Placebo-controlled Trial of Deferiprone in Patients With Pantothenate Kinase-associated Neurodegeneration (PKAN) [NCT01741532]	Phase 3	89 participants (Actual)	Interventional	2012-12-13	Completed
Deferiprone to Delay Dementia (The 3D Study): a Clinical Proof of Concept Study [NCT03234686]	Phase 2	171 participants (Anticipated)	Interventional	2018-01-19	Active, not recruiting
Conservative Iron Chelation as a Disease-modifying Strategy in Amyotrophic Lateral Sclerosis: Multicentre, Parallel-group, Placebo-controlled, Randomized Clinical Trial of Deferiprone [NCT03293069]	Phase 2/Phase 3	372 participants (Actual)	Interventional	2019-01-01	Active, not recruiting
"Conservative Iron Chelation as a Disease-modifying Strategy in Parkinson's Disease. European Multicentre, Parallel-group, Placebo-controlled, Randomized Clinical Trial of Deferiprone" [NCT02655315]	Phase 2	372 participants (Actual)	Interventional	2016-02-09	Completed
The Compassionate Use of Deferiprone in Patients With Pantothenate Kinase-Associated Neurodegeneration [NCT02635841]		0 participants	Expanded Access		No longer available
Effect of Antioxidant Cocktail in Beta-thalassemia/Hb E Patients [NCT01597765]		60 participants (Actual)	Interventional	2009-06-30	Completed
The Efficacy and Safety of Ferriprox® for the Treatment of Transfusional Iron Overload in Patients With Sickle Cell Disease or Other Anemias [NCT02041299]	Phase 4	230 participants (Actual)	Interventional	2014-04-17	Terminated(stopped due to Difficulties with additional recruitment as pool of potential patients was exhausted, and sufficient information for determination of study outcome measure was already obtained)
Thalassemia Clinical Research Network (TCRN) [NCT00000623]		1,000 participants (Anticipated)	Observational	2000-07-31	Completed
An Open-Label Study to Compare the Pharmacokinetic Profiles of a Single Dose of Ferriprox® in Subjects With Impaired Hepatic Function and Healthy Volunteers [NCT01767103]	Phase 4	21 participants (Actual)	Interventional	2013-01-31	Completed
"Ferrochelating Treatment in Patients Affected by Neurodegeneration With Brain Iron Accumulation (NBIA)" [NCT00907283]	Phase 2	20 participants (Anticipated)	Interventional	2008-11-30	Active, not recruiting
Long-term Safety and Efficacy Study of Deferiprone in Patients With Pantothenate Kinase-Associated Neurodegeneration (PKAN) [NCT02174848]	Phase 3	68 participants (Actual)	Interventional	2014-06-30	Completed
Clinical Curative Effect Evaluation Study of Treatment of Oral Deferiprone Tablets in Aceruloplasminaemia Patients [NCT04184453]	Early Phase 1	5 participants (Anticipated)	Interventional	2019-12-23	Recruiting
A Pilot Clinical Trial With the Iron Chelator Deferiprone in Parkinson's Disease [NCT01539837]	Phase 2	22 participants (Actual)	Interventional	2012-02-29	Completed
Single-dose Pharmacokinetic Study of Deferiprone Extended Release Tablets Versus Ferriprox Immediate Release Tablets Under Fasting and Fed Conditions in Healthy Volunteers [NCT02465489]	Phase 1	20 participants (Actual)	Interventional	2015-06-30	Completed
A Double-Blind, Randomized, Crossover, Thorough QT/QTc Trial to Evaluate the Potential of Deferiprone to Prolong the QT Interval in Healthy Subjects [NCT01860703]	Phase 4	50 participants (Actual)	Interventional	2012-11-30	Completed
An Open-label Study to Compare the Pharmacokinetic Profiles of a Single Dose of Ferriprox in Subjects With Impaired Renal Function and Healthy Volunteers [NCT01770652]	Phase 4	32 participants (Actual)	Interventional	2013-01-31	Completed
A Single Center, Phase I, Double-blind, Placebo-controlled Evaluation of the Safety, Tolerability, and Pharmacokinetics of Single Ascending Doses of Deferiprone Administered by Intravenous Infusion to Healthy Male and Female Volunteers [NCT01989455]	Phase 1	64 participants (Actual)	Interventional	2013-11-30	Completed
Pilot Study of Deferasirox and Deferiprone Combination Oral Chelation for Individuals With Transfusion Dependent Thalassemia and High Iron Burden [NCT01709032]	Phase 1/Phase 2	9 participants (Actual)	Interventional	2012-09-30	Completed
Cardiac MRI-guided Deferiprone Therapy for Acute Myocardial Infarction Patients [NCT05604131]	Phase 1	60 participants (Anticipated)	Interventional	2022-11-24	Recruiting
Pilot Study of the Pharmacokinetic Profile of a Single Dose of Deferiprone Sustained-Release Formulation in Healthy Volunteers [NCT02189941]	Phase 1	11 participants (Actual)	Interventional	2014-05-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00115349 (1) [back to overview]	Change in Left Ventricular Ejection Fraction (LVEF).
NCT00529152 (2) [back to overview]	Change in Serum Ferritin Concentration From Baseline.
NCT00529152 (2) [back to overview]	Occurrence of Adverse Events
NCT01539837 (2) [back to overview]	Number of Participants With Serious Adverse Events
NCT01539837 (2) [back to overview]	Iron Concentrations in the Dentate Nucleus
NCT01709032 (2) [back to overview]	Number of Participants With Improvement in Liver Iron Concentration
NCT01709032 (2) [back to overview]	Number of Participants With Improvement in Cardiac T2* MRI
NCT01740713 (9) [back to overview]	CL/F
NCT01740713 (9) [back to overview]	Adverse Events
NCT01740713 (9) [back to overview]	AUC (0-8h)
NCT01740713 (9) [back to overview]	Cmax
NCT01740713 (9) [back to overview]	Cmin
NCT01740713 (9) [back to overview]	Css
NCT01740713 (9) [back to overview]	Ka
NCT01740713 (9) [back to overview]	Tmax
NCT01740713 (9) [back to overview]	V/F
NCT01741532 (8) [back to overview]	Change in Level of Brain Iron
NCT01741532 (8) [back to overview]	Change in Score on Barry-Albright Dystonia Scale
NCT01741532 (8) [back to overview]	Change in Score on Functional Independence Measure
NCT01741532 (8) [back to overview]	Change in Score on Pittsburgh Sleep Quality Index
NCT01741532 (8) [back to overview]	Change in Score on WeeFIM
NCT01741532 (8) [back to overview]	Score on Patient Global Impression of Improvement at End of Study
NCT01741532 (8) [back to overview]	Change in Score on Pediatric Quality of Life
NCT01741532 (8) [back to overview]	Change in Score on Unified Parkinson's Disease Rating Scale
NCT01767103 (7) [back to overview]	Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01767103 (7) [back to overview]	Safety and Tolerability of Ferriprox in Subjects With or Without Hepatic Impairment.
NCT01767103 (7) [back to overview]	AUC0-∞ for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01767103 (7) [back to overview]	Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01767103 (7) [back to overview]	T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01767103 (7) [back to overview]	CumAe for Urine Deferiprone and Deferiprone 3-O-glucuronide
NCT01767103 (7) [back to overview]	Fe% for Urine Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	AUC Zero to Infinity (AUC0-∞) for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	Ae24 for Urine Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	Fe24 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01770652 (7) [back to overview]	Safety and Tolerability of Ferriprox® in Subjects With Renal Impairment.
NCT01825512 (4) [back to overview]	Ferritin Level
NCT01825512 (4) [back to overview]	Cardiac MRI T2*
NCT01825512 (4) [back to overview]	Liver MRI
NCT01825512 (4) [back to overview]	Percentage of Successfully Chelated Patients
NCT01835496 (6) [back to overview]	Frequency of Serious Adverse Events
NCT01835496 (6) [back to overview]	AUC0-∞ for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01835496 (6) [back to overview]	Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01835496 (6) [back to overview]	Tmax for Deferiprone and Deferiprone 3-O-glucuronide
NCT01835496 (6) [back to overview]	T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01835496 (6) [back to overview]	Frequency of Adverse Events
NCT01860703 (10) [back to overview]	Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 50 mg/kg Deferiprone
NCT01860703 (10) [back to overview]	Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of Moxifloxacin
NCT01860703 (10) [back to overview]	Number of Participants With Adverse Events
NCT01860703 (10) [back to overview]	AUC0-infinity for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]	Cmax of Deferiprone and Deferiprone 3-O Glucuronide
NCT01860703 (10) [back to overview]	Maximum Change From Baseline (dQT/dQTc)
NCT01860703 (10) [back to overview]	Maximum Postdose QT/QTc Interval
NCT01860703 (10) [back to overview]	Tmax of Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]	T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]	Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 33 mg/kg Deferiprone
NCT01989455 (8) [back to overview]	Absolute Bioavailability of Deferiprone
NCT01989455 (8) [back to overview]	Safety and Tolerability of a Single 1000 mg Oral Dose of Deferiprone
NCT01989455 (8) [back to overview]	Safety and Tolerability of Single Ascending Doses of Deferiprone When Administered by Intravenous Infusion in Healthy Volunteers.
NCT01989455 (8) [back to overview]	Area Under the Curve From Zero to Infinity (AUC0-∞) for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01989455 (8) [back to overview]	Comparison of Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide Between Deferiprone for Infusion and Oral Deferiprone
NCT01989455 (8) [back to overview]	Maximum Measured Serum Concentration (Cmax) for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01989455 (8) [back to overview]	The Terminal Elimination Half-life (T1/2el) for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01989455 (8) [back to overview]	Time to Maximum Observed Serum Concentration (Tmax) for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02041299 (4) [back to overview]	Change From Baseline in Serum Ferritin
NCT02041299 (4) [back to overview]	Change in Patient-reported Quality of Life, as Measured by the Short Form Health Survey (SF-36) or the Child Health Questionnaire (CHQ-PF50).
NCT02041299 (4) [back to overview]	Change From Baseline in Liver Iron Concentration (LIC)
NCT02041299 (4) [back to overview]	Change From Baseline in Cardiac Iron
NCT02174848 (6) [back to overview]	Change in Score on the BAD Scale -- Comparison of Treatment Groups Over Each Study
NCT02174848 (6) [back to overview]	Number of Participants With Adverse Events
NCT02174848 (6) [back to overview]	Proportion of Patients With Improved or Unchanged BAD Score
NCT02174848 (6) [back to overview]	Change in Score on the BAD Scale -- Comparison of DFP-DFP Patients Across Studies
NCT02174848 (6) [back to overview]	Change in Score on the BAD Scale -- Comparison of Placebo-DFP Patients Across Studies
NCT02174848 (6) [back to overview]	Patient Global Impression of Improvement (PGI-I) Comparison of Placebo-DFP Patients Across Studies
NCT02189941 (6) [back to overview]	Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02189941 (6) [back to overview]	Safety and Tolerability of Deferiprone Sustained Release Tablets
NCT02189941 (6) [back to overview]	AUCinf for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02189941 (6) [back to overview]	AUCt for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02189941 (6) [back to overview]	Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02189941 (6) [back to overview]	Thalf for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02442310 (4) [back to overview]	Number of Subjects With Adverse Events (AEs)
NCT02442310 (4) [back to overview]	Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02442310 (4) [back to overview]	AUC0-∞for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02442310 (4) [back to overview]	Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT02465489 (4) [back to overview]	Tmax for Serum Deferiprone
NCT02465489 (4) [back to overview]	Number of Subjects With Adverse Events (AEs)
NCT02465489 (4) [back to overview]	Cmax for Serum Deferiprone
NCT02465489 (4) [back to overview]	AUC0-∞for Serum Deferiprone
NCT03802916 (3) [back to overview]	The Percentage of Patients in Each Treatment Group Who Experience Post-dose Increases in Liver Enzyme Levels That Are Considered a Safety Concern.
NCT03802916 (3) [back to overview]	The Percentage of Patients in Each Group Who Indicate That They Prefer the Deferiprone DR Formulation Over the Immediate-release Formulation.
NCT03802916 (3) [back to overview]	The Percentage of Patients in Each Treatment Group Who Report Post-dose Occurrences of Gastrointestinal (GI) Distress.

Change in Left Ventricular Ejection Fraction (LVEF).

The primary outcome variable is change in left ventricular ejection fraction (blood ejected from the heart into the body) as measured by MRI from baseline to one year. The unit of primary outcome (left ventricular ejection fraction) is the percent of the blood in left ventricle. (NCT00115349)
Timeframe: Baseline to one year

Intervention	Percent of the blood in left ventricle (Least Squares Mean)
Deferoxamine (DFO) and Deferiprone (L1) Combination Therapy	7.2
Deferoxamine (DFO) + Monotherapy	6.3

Intervention	micromol*h/L (Median)
Deferiprone 25 mg/kg/Day	116.7
Deferiprone 50 mg/kg/Day	210.0
Deferiprone 100 mg/kg/Day	428.8

Intervention	microM (Median)
Deferiprone 25 mg/kg/Day	61.7
Deferiprone 50 mg/kg/Day	119.8
Deferiprone 100 mg/kg/Day	229.5

Intervention	hour (Median)
Deferiprone 25 mg/kg/Day	0.33
Deferiprone 50 mg/kg/Day	0.33
Deferiprone 100 mg/kg/Day	0.37

Intervention	score on a scale (Least Squares Mean)
	Patient self-report, total score	Parent proxy-report, total score
Deferiprone	1.21	-4.90
Placebo	1.34	-2.37

Intervention	score on a scale (Least Squares Mean)
	UPDRS Part I	UPDRS Part II	UPDRS Part III	UPDRS Part VI
Deferiprone	-0.25	1.09	5.38	-2.17
Placebo	-0.07	2.36	2.06	-7.66

Intervention	hour (Median)
	Tmax of deferiprone	Tmax of deferiprone 3-O-glucuronide
Mild Hepatic Failure	0.7500	3.000
Moderate Hepatic Failure	0.7500	3.000
Normal Hepatic Function (Healthy Volunteers)	0.7500	2.000

Intervention	ug*hr/mL (Mean)
	AUC0-∞ for serum deferiprone	AUC0-∞ for serum deferiprone 3-O-glucuronide
Mild Hepatic Failure	82.02	305.1
Moderate Hepatic Failure	105.5	305.9
Normal Hepatic Function (Healthy Volunteers)	92.64	337.3

Intervention	ug/mL (Mean)
	Cmax for serum deferiprone	Cmax for serum deferiprone 3-O-glucuronide
Mild Hepatic Failure	36.26	56.91
Moderate Hepatic Failure	35.94	55.33
Normal Hepatic Function (Healthy Volunteers)	49.00	69.03

Intervention	hour (Mean)
	T1/2 for serum deferiprone	T1/2 for deferiprone 3-O-glu
Mild Hepatic Failure	1.855	2.518
Moderate Hepatic Failure	2.180	2.479
Normal Hepatic Function (Healthy Volunteers)	1.994	2.621

Intervention	mg (Mean)
	CumAe of urine deferiprone	CumAe of urine deferiprone 3-O-glucuronide
Mild Hepatic Failure	59.5	6787
Moderate Hepatic Failure	62.9	5979
Normal Hepatic Function (Healthy Volunteers)	69.0	6670

Intervention	ms (Mean)
Placebo	30.74
Deferiprone 20mg	30.59
Deferiprone 30mg	29.86

Intervention	percentage of dose excreted in urine (Mean)
	Fe of urine deferiprone	Fe of urine 3-O-glucuronide
Mild Hepatic Failure	2.18	110
Moderate Hepatic Failure	2.36	97.7
Normal Hepatic Function (Healthy Volunteers)	2.56	109

Intervention	μg*h/mL (Mean)
	AUC0-∞ for serum deferiprone 3-O-Glucuronide	AUC0-∞ for serum deferiprone
Mild Renal Impairment	76.9	319.1
Moderate Renal Impairment	74.9	703.2
Normal Renal Function	78.1	252.6
Severe Renal Impairment	70.9	1438.5

Intervention	hour (Median)
	Tmax for Serum Deferiprone	Tmax for Serum Deferiprone 3-O-glucuronide
Mild Renal Impairment	0.75	2.50
Moderate Renal Impairment	1.00	3.00
Normal Renal Function	0.50	2.50
Severe Renal Impairment	0.75	4.00

Intervention	hour (Mean)
	T1/2 for Serum Deferiprone	T1/2 for Serum Deferiprone 3-O-Glucuronide
Mild Renal Impairment	1.77	2.58
Moderate Renal Impairment	2.03	2.58
Normal Renal Function	1.68	2.14
Severe Renal Impairment	2.20	3.35

Intervention	mg (Mean)
	Ae24 for urine deferiprone	e24 for urine deferiprone 3-O-Glucuronide
Mild Renal Impairment	69	6608
Moderate Renal Impairment	36	5812
Normal Renal Function	78	5987
Severe Renal Impairment	24	5318

Intervention	% of dose excreted in urine from 0-24 hr (Mean)
	Fe24 for urine deferiprone	Fe24 for urine deferiprone 3-O-glucuronide
Mild Renal Impairment	2.9	123.2
Moderate Renal Impairment	1.5	104.5
Normal Renal Function	3.5	115.0
Severe Renal Impairment	1.0	97.9

Intervention	μg/mL (Mean)
	Cmax for serum deferiprone	Cmax for serum deferiprone-3-o-glucuronide
Mild Renal Impairment	33.4	60.8
Moderate Renal Impairment	43.3	118.8
Normal Renal Function (Healthy Volunteers)	37.1	47.8
Severe Renal Impairment	30.6	150.8

Intervention	hr (Median)
	Tmax for serum seferiprone	Tmax for serum deferiprone 3-O-glucuronide
Ferriprox	1.000	2.750

Intervention	participants (Number)
Arm A - Maximum Therapeutic Dose	12
Treatment Arm B - Supratherapeutic Dose	35
Arm C - Placebo Control	10
Arm D - Positive Control	5

Intervention	μg *hr/mL (Mean)
	AUC0-infinity for serum deferiprone	AUC0-infinity for serum deferiprone -O-glucuronide
Arm A - Maximum Therapeutic Dose	95.4	205.5
Treatment Arm B - Supratherapeutic Dose	152.1	331.2

deferiprone

Description

Cross-References

Synonyms (130)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (1)

Protein Targets (20)

Potency Measurements

Inhibition Measurements

Biological Processes (37)

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Bioassays (214)

Research

Studies (980)

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Research Demand Index: 66.07

Study Types

Clinical Trials (57)

Trial Overview

Trial Outcomes

Change in Left Ventricular Ejection Fraction (LVEF).

Change in Serum Ferritin Concentration From Baseline.

Occurrence of Adverse Events

Number of Participants With Serious Adverse Events

Iron Concentrations in the Dentate Nucleus

Number of Participants With Improvement in Liver Iron Concentration

Number of Participants With Improvement in Cardiac T2* MRI

CL/F

Adverse Events

AUC (0-8h)

Cmax

Cmin

Css

Ka

Tmax

V/F

Change in Level of Brain Iron

Change in Score on Barry-Albright Dystonia Scale

Change in Score on Functional Independence Measure

Change in Score on Pittsburgh Sleep Quality Index

Change in Score on WeeFIM

Score on Patient Global Impression of Improvement at End of Study

Change in Score on Pediatric Quality of Life

Change in Score on Unified Parkinson's Disease Rating Scale

Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

Safety and Tolerability of Ferriprox in Subjects With or Without Hepatic Impairment.

AUC0-∞ for Serum Deferiprone and Deferiprone 3-O-glucuronide

Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide

CumAe for Urine Deferiprone and Deferiprone 3-O-glucuronide

Fe% for Urine Deferiprone and Deferiprone 3-O-glucuronide

AUC Zero to Infinity (AUC0-∞) for Serum Deferiprone and Deferiprone 3-O-glucuronide

Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide

Ae24 for Urine Deferiprone and Deferiprone 3-O-glucuronide

Fe24 for Serum Deferiprone and Deferiprone 3-O-glucuronide

Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

Safety and Tolerability of Ferriprox® in Subjects With Renal Impairment.

Ferritin Level

Cardiac MRI T2*

Liver MRI

Percentage of Successfully Chelated Patients

Frequency of Serious Adverse Events

AUC0-∞ for Serum Deferiprone and Deferiprone 3-O-glucuronide

Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

Tmax for Deferiprone and Deferiprone 3-O-glucuronide

T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide

Frequency of Adverse Events

Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 50 mg/kg Deferiprone

Intervention	μg/mL (Mean)
	Cmax of serum deferiprone	Cmax of serum deferiprone 3-O-glucuronide
Arm A - Maximum Therapeutic Dose	34.1	35.2
Treatment Arm B - Supratherapeutic Dose	54.4	51.4

Intervention	percentage of participants (Number)
	QTcF ≤ 30 msec	QTcF >30 but ≤ 60 msec	QTcF >60 msec
Arm A - Maximum Therapeutic Dose	100	0	0
Arm B - Supratherapeutic Dose	100	0	0
Arm C - Placebo Control	100	0	0
Arm D - Positive Control	96	4	0

Intervention	percentage of participants (Number)
	QTcF ≤ 450 msec	QTcF > 450 to ≤ 480 msec	QTcF > 480 to ≤ 500 msec	QTcF > 500 msec
Arm A - Maximum Therapeutic Dose	100	0	0	0
Arm B - Supratherapeutic Dose	96	4	0	0
Arm C - Placebo Control	98	2	0	0
Arm D - Positive Control	89	11	0	0

Intervention	hour (Median)
	Tmax of serum deferiprone	Tmax of serum deferiprone -O-glucuronide
Arm A - Maximum Therapeutic Dose	0.8185	3.066
Treatment Arm B - Supratherapeutic Dose	0.8175	3.071

Intervention	μg*h/mL (Mean)
1000 mg Deferiprone for Infusion	41.805
1000 mg Oral Deferiprone	30.796

Intervention	participants (Number)
500 mg Deferiprone for Infusion	10
1000 mg Deferiprone for Infusion	7
1500 mg Deferiprone for Infusion	8
2000 mg Deferiprone for Infusion	10
Placebo	3

Intervention	hour (Mean)
	T1/2el for serum deferiprone	T1/2el for serum deferiprone 3-O-glucuronide
1000 mg Deferiprone for Infusion	1.77	1.94
1500 mg Deferiprone for Infusion	1.83	2.01
2000 mg Deferiprone for Infusion	1.85	1.94
500 mg Deferiprone for Infusion	1.68	2.00

Intervention	score on a scale (Mean)
	SF-36 Physical Summary	SF-36 Mental Summary	CHQ-PF50 Physical Summary	CHQ-PF50 Psychosocial Summary
Deferiprone	43.1	44.7	29.3	42.5
Deferoxamine	43.0	40.9	30.5	41.3

Intervention	score on a scale (Mean)
	Change in BAD score over initial study	Change in BAD score over extension study
DFP-DFP	1.9	1.4
Placebo-DFP	4.4	1.4

Intervention	Participants (Count of Participants)
	Number of patients with at least one AE	Number of patients with at least one SAE	Number of patients who withdrew due to an AE
DFP-DFP	42	14	1
Placebo-DFP	22	12	2