Page last updated: 2024-10-25

clioquinol and Alzheimer Disease

clioquinol has been researched along with Alzheimer Disease in 105 studies

Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.
5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease.

Alzheimer Disease: A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)

Research Excerpts

ExcerptRelevanceReference
"Cholinesterase inhibitors and memantine are widely used for the treatment of Alzheimer disease (AD) and other non-AD dementia worldwide."4.86[Drug therapy for Alzheimer's disease]. ( Shoji, M, 2010)
"Alzheimer's disease is the most frequent neurodegenerative illness in the long run."3.01Understanding Alzheimer's Disease and its Metal Chelation Therapeutics: A Narrative Review. ( Karwasra, R; Thakur, R; Umar, T, 2023)
"PBT2 is a metal-protein attenuating compound (MPAC) that affects the Cu2(+)-mediated and Zn2(+)-mediated toxic oligomerisation of Abeta seen in Alzheimer's disease (AD)."2.73Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial. ( Ames, D; Batsman, S; Blennow, K; Bush, AI; Harrison, J; Lannfelt, L; Masters, CL; Murdoch, R; Ritchie, CW; Targum, S; Wilson, J; Zetterberg, H, 2008)
"Alzheimer's disease is the most common form of dementia in the elderly, and it is characterized by elevated brain iron levels and accumulation of copper and zinc in cerebral beta-amyloid deposits (e."2.44Therapeutics for Alzheimer's disease based on the metal hypothesis. ( Bush, AI; Tanzi, RE, 2008)
" We also describe how the development of therapeutic agents designed to modulate metal bioavailability has provided promising results in the treatment of Alzheimer's disease."2.43Therapeutic treatments for Alzheimer's disease based on metal bioavailability. ( Barnham, KJ; Bush, AI; Crouch, PJ; White, AR, 2006)
"The cause of Alzheimer's disease (AD) is closely related to the aggregation of a normal protein, beta-amyloid (Abeta), within the neocortex."2.42The metallobiology of Alzheimer's disease. ( Bush, AI, 2003)
"Clioquinol is an example from this class, which has recently shown encouraging efficacy from early clinical evaluation in the absence of any compelling evidence of subacute myelopathic optic neuritis, which has been associated with this drug's use in Japanese populations."2.42Metal-protein attenuating compounds and Alzheimer's disease. ( Bush, AI; Masters, CL; Ritchie, CW, 2004)
"Clioquinol is a drug that acts on amyloid by perturbing amyloid's metallo-chemistry, and Clioquinol treatment has been shown to be beneficial in a mouse model of AD."2.41'...and C is for Clioquinol' - the AbetaCs of Alzheimer's disease. ( Melov, S, 2002)
"Although Alzheimer's disease (AD) was first described over a century ago, it remains the leading cause of age-related dementia."1.72Alzheimer's Drug PBT2 Interacts with the Amyloid β 1-42 Peptide Differently than Other 8-Hydroxyquinoline Chelating Drugs. ( Dolgova, NV; George, GN; Harris, HH; Kroll, T; Millhauser, GL; Pickering, IJ; Pushie, MJ; Roseman, G; Schilling, KM; Sokaras, D; Summers, KL, 2022)
"To target the multi-facets of Alzheimer's disease (AD), a series of novel GSK-3β inhibitors containing the 2,3-diaminopyridine moiety were designed and synthesized."1.51Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease. ( Liu, P; Liu, ZP; Shi, XL; Wu, JD, 2019)
" Further drug-like property analysis demonstrated that the optimized compound, 8d (WI-1758), had liver microsomal metabolic stability, was well tolerated (>2000 mg/kg), and had a rational pharmacokinetic profile, as well as an oral bioavailability of 14."1.48Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. ( Chan, ASC; Feng, X; Hu, J; Huang, L; Li, X; Wang, Z; Yang, X, 2018)
" Here, a new series of orally bioavailable multifunctional antioxidants (MFAO-2s) possessing a 2-diacetylamino-5-hydroxypyrimidine moiety is described."1.42Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases. ( Kador, PF; Kawada, H, 2015)
"Patients of Alzheimer's disease (AD) frequently have lower bone mineral density and higher rate of hip fracture."1.42Iron Chelation Inhibits Osteoclastic Differentiation In Vitro and in Tg2576 Mouse Model of Alzheimer's Disease. ( Cui, S; Guo, JP; Pan, JX; Xia, WF; Xiong, L; Xiong, WC, 2015)
" The pathogenic Aβ 1-42 peptide forms more oligomers and is more toxic than Aβ 1-40 and genome-wide genetic screens identified genes that are known risk factors for AD."1.40Clioquinol promotes the degradation of metal-dependent amyloid-β (Aβ) oligomers to restore endocytosis and ameliorate Aβ toxicity. ( Caldwell, GA; Caldwell, KA; Hamamichi, S; Lindquist, S; Matlack, KE; Narayan, P; Tardiff, DF, 2014)
" elegans model of full length Aß₁₋₄₂ expression can now be adopted for use in screens to rapidly identify and assist in development of potential therapeutics and to study underlying toxic mechanism(s) of Aß."1.38Utility of an improved model of amyloid-beta (Aβ₁₋₄₂) toxicity in Caenorhabditis elegans for drug screening for Alzheimer's disease. ( Barnham, KJ; Bush, AI; Cherny, RA; Kenche, VB; Link, CD; Masters, CL; McColl, G; Pukala, TL; Roberts, BR; Roberts, CM; Ryan, TM, 2012)
" However, clinical trial studies have shown that long-term use of metal chelator can cause adverse side effect, subacute myelo-optic neuropathy."1.38Mesoporous silica nanoparticle-based H2O2 responsive controlled-release system used for Alzheimer's disease treatment. ( Chen, C; Geng, J; Li, M; Qu, X; Wu, L, 2012)
"As a disease-modifying approach for Alzheimer's disease (AD), clioquinol (CQ) targets beta-amyloid (Abeta) reactions with synaptic Zn and Cu yet promotes metal uptake."1.35Rapid restoration of cognition in Alzheimer's transgenic mice with 8-hydroxy quinoline analogs is associated with decreased interstitial Abeta. ( Adlard, PA; Barnham, KJ; Bush, AI; Cappai, R; Charman, SA; Cherny, RA; Cortes, M; Deleva, K; Finkelstein, DI; Gautier, E; Kok, G; Laughton, K; Li, QX; Liu, X; Lynch, T; Masters, CL; Nicolazzo, JA; Perez, K; Ritchie, CW; Robb, E; Smith, JP; Tanzi, RE; Volitakis, I; Wilkins, S, 2008)
"Clioquinol (CQ) is a "metal protein attenuating compound" that crosses the blood-brain barrier and binds, with high affinity, copper(II) and zinc(II), two metal ions critically involved in amyloid-beta aggregation and toxicity."1.35Clioquinol decreases amyloid-beta burden and reduces working memory impairment in a transgenic mouse model of Alzheimer's disease. ( Casamenti, F; Casini, A; Fiorentini, A; Francese, S; Gabbiani, C; Grossi, C; Luccarini, I; Messori, L; Moneti, G; Rosi, MC, 2009)
"Isoflurane also promotes Abeta aggregation."1.34The inhalation anesthetic isoflurane induces a vicious cycle of apoptosis and amyloid beta-protein accumulation. ( Crosby, G; Culley, DJ; Dong, Y; Maeda, U; Moir, RD; Tanzi, RE; Xia, W; Xie, Z, 2007)
"The key protein in Alzheimer's disease, the amyloid precursor protein (APP), is a ubiquitously expressed copper-binding glycoprotein that gives rise to the Abeta amyloid peptide."1.32Clioquinol mediates copper uptake and counteracts copper efflux activities of the amyloid precursor protein of Alzheimer's disease. ( Bayer, TA; Cappai, R; Hafner, M; Multhaup, G; Simons, A; Strauss, M; Treiber, C, 2004)

Research

Studies (105)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's47 (44.76)29.6817
2010's46 (43.81)24.3611
2020's12 (11.43)2.80

Authors

AuthorsStudies
Moret, V1
Laras, Y1
Pietrancosta, N1
Garino, C1
Quéléver, G1
Rolland, A1
Mallet, B1
Norreel, JC1
Kraus, JL1
Chen, SY1
Chen, Y1
Li, YP1
Chen, SH1
Tan, JH1
Ou, TM1
Gu, LQ1
Huang, ZS1
Bulic, B1
Pickhardt, M1
Mandelkow, E1
Lu, C1
Guo, Y1
Yan, J3
Luo, Z2
Luo, HB2
Yan, M1
Huang, L8
Li, X10
Li, SY1
Wang, XB3
Kong, LY3
Kawada, H1
Kador, PF1
Wang, Z6
Wang, Y3
Wang, B2
Li, W3
Martínez, A1
Alcendor, R1
Rahman, T1
Podgorny, M1
Sanogo, I1
McCurdy, R1
Wang, ZM1
Cai, P2
Liu, QH2
Xu, DQ1
Yang, XL2
Wu, JJ2
Wang, H2
Lu, Z1
Zheng, X2
Ni, W1
Zhu, J2
Fu, Y1
Lian, F1
Zhang, N1
Li, J3
Zhang, H1
Mao, F4
Chen, H1
Lu, CJ1
Li, F1
Wang, J1
Xu, YX1
Li, XK1
Dong, SN1
Liu, WW1
Gong, Q1
Wang, TD1
Tang, Y1
Zhang, HY1
Hu, J2
Yang, X2
Feng, X2
Chan, ASC1
D'Acunto, CW1
Kaplánek, R1
Gbelcová, H1
Kejík, Z1
Bříza, T1
Vasina, L1
Havlík, M1
Ruml, T1
Král, V1
Pan, T1
An, B1
Li, Z1
Shi, XL1
Wu, JD2
Liu, P1
Liu, ZP2
Yang, Z1
Song, Q1
Cao, Z1
Yu, G1
Liu, Z2
Tan, Z1
Deng, Y1
Nerella, A1
Jeripothula, M1
Bowroju, SK1
Penthala, NR1
Lakkaniga, NR1
Balasubramaniam, M1
Ayyadevara, S1
Shmookler Reis, RJ1
Crooks, PA1
Wang, XX1
Xie, F1
Jia, CC1
Yan, N1
Zeng, YL1
Cotrina, EY1
Santos, LM1
Rivas, J1
Blasi, D1
Leite, JP1
Liz, MA1
Busquets, MA1
Planas, A1
Prohens, R1
Gimeno, A1
Jiménez-Barbero, J1
Gales, L1
Llop, J1
Quintana, J1
Cardoso, I1
Arsequell, G1
Lin, G1
Zhu, F1
Kanaan, NM1
Asano, R1
Shirafuji, N1
Sasaki, H1
Yamaguchi, T1
Enomoto, S1
Endo, Y1
Ueno, A1
Ikawa, M1
Hayashi, K1
Yamamura, O1
Yen, SH1
Nakamoto, Y1
Hamano, T1
Summers, KL3
Roseman, G1
Schilling, KM1
Dolgova, NV1
Pushie, MJ2
Sokaras, D1
Kroll, T1
Harris, HH2
Millhauser, GL2
Pickering, IJ3
George, GN3
Thakur, R1
Karwasra, R1
Umar, T1
Cao, M1
Xiang, H1
Wang, W1
Pretsch, D1
Rollinger, JM1
Schmid, A1
Genov, M1
Wöhrer, T1
Krenn, L1
Moloney, M1
Kasture, A1
Hummel, T1
Pretsch, A1
Lu, L1
Wang, S1
Tang, C1
Zhang, Y1
Yao, G1
Zeng, J1
Ge, S1
Wen, H1
Xu, M1
Guyatt, G1
Xu, N1
Roseman, GP1
Sopasis, GJ1
Cilliers, K1
Rajasekhar, K1
Mehta, K1
Govindaraju, T1
Saini, RK1
Shuaib, S1
Goyal, D1
Goyal, B1
Zhang, YH1
Raymick, J1
Sarkar, S1
Lahiri, DK2
Ray, B1
Holtzman, D1
Dumas, M1
Schmued, LC1
Nienaber, KH1
Cotelesage, JJ1
Ponomarenko, O1
Nichol, HK1
Sampson, EL2
Jenagaratnam, L4
McShane, R4
Matlack, KE1
Tardiff, DF1
Narayan, P1
Hamamichi, S1
Caldwell, KA1
Caldwell, GA1
Lindquist, S1
Jia, X1
Miao, H1
Sun, Y3
Ryan, TM2
Roberts, BR2
McColl, G2
Hare, DJ1
Doble, PA1
Li, QX4
Lind, M1
Roberts, AM1
Mertens, HD1
Kirby, N1
Pham, CL1
Hinds, MG1
Adlard, PA4
Barnham, KJ11
Curtain, CC1
Masters, CL11
Seo, BR1
Lee, SJ1
Cho, KS1
Yoon, YH1
Koh, JY1
Wu, R1
Guo, JP1
Pan, JX1
Xiong, L1
Xia, WF1
Cui, S1
Xiong, WC1
Prati, F1
Bergamini, C1
Fato, R1
Soukup, O1
Korabecny, J1
Andrisano, V1
Bartolini, M1
Bolognesi, ML1
Su, T1
Zhang, T1
Xie, S1
Wu, Y1
Saito, Y1
Sakai, K1
Konagaya, M1
Cherny, RA7
Finkelstein, DI2
Gautier, E1
Robb, E1
Cortes, M1
Volitakis, I6
Liu, X1
Smith, JP1
Perez, K1
Laughton, K1
Charman, SA1
Nicolazzo, JA1
Wilkins, S1
Deleva, K1
Lynch, T1
Kok, G1
Ritchie, CW6
Tanzi, RE7
Cappai, R4
Bush, AI17
Relkin, NR1
Lannfelt, L2
Blennow, K2
Zetterberg, H2
Batsman, S1
Ames, D2
Harrison, J2
Targum, S1
Murdoch, R1
Wilson, J1
Bolognin, S2
Zatta, P3
Drago, D2
Tognon, G1
Parnigotto, PP1
Ricchelli, F1
Cahoon, L1
Grossi, C1
Francese, S1
Casini, A1
Rosi, MC1
Luccarini, I1
Fiorentini, A1
Gabbiani, C1
Messori, L2
Moneti, G1
Casamenti, F1
Rival, T1
Page, RM1
Chandraratna, DS1
Sendall, TJ1
Ryder, E1
Liu, B1
Lewis, H1
Rosahl, T1
Hider, R1
Camargo, LM1
Shearman, MS1
Crowther, DC1
Lomas, DA1
Sensi, SL1
Mancino, AM1
Hindo, SS1
Kochi, A1
Lim, MH1
Faux, NG1
Gunn, A1
Rembach, A1
Tsatsanis, A1
Bedo, J1
Ingelsson, M1
Cummings, JL1
Herd, CM1
Shoji, M1
Budimir, A1
Humbert, N1
Elhabiri, M1
Osinska, I1
Biruš, M1
Albrecht-Gary, AM1
Barcia, E1
Salama, A1
Fernández-Carballido, A1
Negro, S1
Kenche, VB2
Bica, L1
White, AR5
Nurjono, M1
Filiz, G2
Crouch, PJ4
Donnelly, PS2
Savva, MS1
Hung, LW2
Mot, AI1
Parker, SJ1
Greenough, MA1
Faller, P1
Wang, T1
Wang, CY1
Shan, ZY1
Teng, WP1
Wang, ZY1
Pukala, TL1
Roberts, CM1
Link, CD1
Geng, J1
Li, M1
Wu, L1
Chen, C1
Qu, X1
Helmuth, L2
Rogers, JT1
Randall, JD1
Cahill, CM1
Eder, PS1
Huang, X2
Gunshin, H1
Leiter, L1
McPhee, J1
Sarang, SS1
Utsuki, T1
Greig, NH1
Giordano, T1
Gullans, SR1
Cole, GM1
Abramov, AY1
Canevari, L1
Duchen, MR1
Finefrock, AE1
Doraiswamy, PM2
Mastwyk, M2
Macfarlane, S2
LoGiudice, D1
Sullivan, KA1
Rosenberg, RN2
Mackinnon, A1
MacGregor, L1
Kiers, L1
Cherny, R1
Tammer, A1
Carrington, D1
Mavros, C1
Xilinas, M1
Davis, S1
Beyreuther, K2
Di Vaira, M1
Bazzicalupi, C1
Orioli, P1
Bruni, B1
Treiber, C1
Simons, A1
Strauss, M1
Hafner, M1
Bayer, TA2
Multhaup, G2
McCarthy, AM1
Huckle, R1
Raman, B1
Ban, T1
Yamaguchi, K1
Sakai, M1
Kawai, T1
Naiki, H1
Goto, Y1
Ibach, B1
Haen, E1
Marienhagen, J1
Hajak, G1
Puglielli, L1
Friedlich, AL1
Setchell, KD1
Nagano, S1
Opazo, C2
Wade, JD1
Melov, S2
Kovacs, DM1
Xiong, GL1
Luza, S1
Villemagne, VL1
Rowe, C1
Strozyk, D1
Masters, C1
Du, T2
Laughton, KM1
Sharples, RA1
Xilinas, ME2
Hoke, DE1
Holsinger, RM1
Evin, G1
Hill, AF1
Domingo, JL1
Schäfer, S1
Pajonk, FG1
Xie, Z1
Dong, Y1
Maeda, U1
Moir, RD2
Xia, W1
Culley, DJ1
Crosby, G1
Ferrada, E1
Arancibia, V1
Loeb, B1
Norambuena, E1
Olea-Azar, C1
Huidobro-Toro, JP1
Sampson, E1
Price, KA1
Caragounis, A1
Iwata, N1
Tabira, T1
Gouras, GK1
Beal, MF1
Atwood, CS1
Gray, DN1
Jones, WD1
McLean, CA1
Fraser, FW1
Kim, Y1
Goldstein, LE1
Lim, JT1
Zheng, H1

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A 12-Week, Randomised, Double-Blind, Placebo-Controlled, Parallel Three-Group Study to Assess the Safety, Tolerability and Efficacy of Two Dose Levels of PBT2 to Slow Progression of Disease in Patients With Early Alzheimer's Disease[NCT00471211]Phase 280 participants (Anticipated)Interventional2006-12-31Completed
A Randomized, Double-blind, Placebo-controlled Study to Assess the Safety and Tolerability, and Efficacy of PBT2 in Patients With Early to Mid-stage Huntington Disease[NCT01590888]Phase 2109 participants (Actual)Interventional2012-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Change From Baseline in Behaviour

Total Behavioural score from the Unified Huntington Disease Rating Scale. The behavioural assessment measures the frequency and severity of symptoms related to affect, thought content and coping styles. The total behaviour score is the sum of all responses, with scale range of 0 to 8. Higher scores on the behaviour assessments indicate more severe disturbance than lower scores. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionunits on a scale (Mean)
PBT2 250mg-2.3
PBT2 100mg3.0
Sugar Pill0.7

Change From Baseline in Blood Biomarkers

Biomarkers assessed primarily with mutant huntingtin protein, normalised to lysate protein concentrations, as a change from baseline. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionratio (Mean)
PBT2 250mg1.97
PBT2 100mg0.14
Sugar Pill-1.72

Change From Baseline in Blood Biomarkers

Biomarkers assessed primarily with soluble huntingtin protein, normalised to lysate protein concentrations, as a change from baseline. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionmg/mL (Mean)
PBT2 250mg-3.18
PBT2 100mg-2.09
Sugar Pill-3.07

Change From Baseline in Blood Biomarkers - Selenium

Biomarkers assessed primarily with plasma selenium as a change from baseline. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionug/L (Mean)
PBT2 250mg1.3
PBT2 100mg-6.3
Sugar Pill2.0

Change From Baseline in Brain Function (MRI)

Measure of the structural brain volume as assessed by the left caudate volume. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionmm^3 (Mean)
PBT2 250mg50.0
PBT2 100mg27.5
Sugar Pill-170.5

Change From Baseline in Brain Function (MRI)

Measure of whole brain iron concentrations. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionmm^3 (Mean)
PBT2 250mg0.0029
PBT2 100mg0.0067
Sugar Pill0.0098

Change From Baseline in Cognitive Test Battery - TMT Part B

"Trail Making Test Part B was assessed by the number of seconds to complete the test (from 0 to 240 seconds).~The Trails Making Test Part B actual change from baseline at Week 26 was analysed." (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionseconds (Mean)
PBT2 250mg-6.3
PBT2 100mg12.8
Sugar Pill8.9

Change From Baseline in Functional Abilities

"Total Functional Capacity (TFC) assessment was based on an individual's ability to perform common daily tasks. TFC score range was 0 to 13.~Higher scores on the function scales indicate better functioning than lower scores." (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionunits on a scale (Mean)
PBT2 250mg1.1
PBT2 100mg1.3
Sugar Pill1.3

Change From Baseline in Investigator Global Assessments by Efficacy Index

Global function was assessed by the Investigator using the clinical global impression (CGI) scale which included assessing the severity of illness and global improvement and calculating the efficacy index for each participant. The efficacy index aims to relate therapeutic effects to reported side effects as assessed by the Investigator (range from 0 [marked improvement and no side effects] to 4 [unchanged or worse] and side effects outweigh therapeutic effects) and is calculated for each participant by dividing the therapeutic effect score by the side effects score. An improvement is reflected by CGI scale Efficacy Index values >1. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionratio (Mean)
PBT2 250mg1.313
PBT2 100mg1.276
Sugar Pill1.176

Change From Baseline in Motor Function

Total motor score calculated from the Unified Huntington Disease Rating Scale - Motor Function. The motor section of the UHDRS assesses motor features of HD with standardized ratings of oculomotor function, dysarthria, chorea, dystonia, gait, and postural stability. The total motor impairment scores is the sum of all the individual motor ratings, with higher scores indicating more severe motor impairment than lower scores. A maximum score of 60 is possible (range 0-60). (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionunits on a scale (Mean)
PBT2 250mg-0.7
PBT2 100mg1.3
Sugar Pill-1.3

Change From Baseline in Urine Biomarkers

Biomarkers assessed primarily with 8-hydroxy-2'-deoxyguanosine, normalised to creatinine concentrations, as a change from baseline. (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionng/mL (Mean)
PBT2 250mg-0.4258
PBT2 100mg0.0832
Sugar Pill35.5302

Safety and Tolerability of PBT2 in Patients With HD

As measured by the total number of participants in each dose group who reported at least one adverse events during the study, (NCT01590888)
Timeframe: Baseline to 26 weeks

Interventionparticipants (Number)
PBT2 250mg32
PBT2 100mg30
Sugar Pill28

Change From Baseline in Cognitive Test Battery - Composite z Scores

Cognition composite z-scores were calculated for each participant. The composite scores were defined as the mean of the individual z-scores for the various cognition assessments. The Main Composite z-score was calculated for Category Fluency Test, Trail Making Test Part B, Map Search, Symbol Digit Modalities Test and Stroop Word Reading Test. The Exploratory Composite z-score was calculated for Category Fluency Test, Trail Making Test Part B, Map Search, Symbol Digit Modalities Test, Stroop Word Reading Test and Speeded Tapping test. The Executive Function Composite z-score was calculated from Category Fluency Test and Trail Making Test Part B. There is no unit of measure for the z score as it is the pure number calculated from the SD from the mean. A higher z score indicates an improvement. (NCT01590888)
Timeframe: Baseline to 26 weeks

,,
Interventionz score (Mean)
Main Composite z-scoreExploratory Composite z-scoreExecutive Function z-score
PBT2 100mg-0.0413-0.0287-0.1026
PBT2 250mg0.05920.05300.2274
Sugar Pill-0.0194-0.01440.0553

Reviews

25 reviews available for clioquinol and Alzheimer Disease

ArticleYear
Progress and developments in tau aggregation inhibitors for Alzheimer disease.
    Journal of medicinal chemistry, 2013, Jun-13, Volume: 56, Issue:11

    Topics: Alzheimer Disease; Animals; Clinical Trials as Topic; Humans; Hydrogen Bonding; Models, Molecular; P

2013
Understanding Alzheimer's Disease and its Metal Chelation Therapeutics: A Narrative Review.
    Current pharmaceutical design, 2023, Volume: 29, Issue:30

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Chelating Agents; Clioquinol; Copper; Humans; Metals

2023
Anti-Aβ agents for mild to moderate Alzheimer's disease: systematic review and meta-analysis.
    Journal of neurology, neurosurgery, and psychiatry, 2020, Volume: 91, Issue:12

    Topics: Acitretin; Alanine; Alzheimer Disease; Amyloid beta-Peptides; Antibodies, Monoclonal, Humanized; Anx

2020
Trace element alterations in Alzheimer's disease: A review.
    Clinical anatomy (New York, N.Y.), 2021, Volume: 34, Issue:5

    Topics: Alzheimer Disease; Clioquinol; Copper; Deferoxamine; Humans; Metals; Penicillamine; Siderophores; Tr

2021
Metal protein attenuating compounds for the treatment of Alzheimer's dementia.
    The Cochrane database of systematic reviews, 2014, Feb-21, Issue:2

    Topics: Aged; Alzheimer Disease; Amyloid beta-Peptides; Chelating Agents; Clioquinol; Humans; Randomized Con

2014
Therapeutics for Alzheimer's disease based on the metal hypothesis.
    Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, 2008, Volume: 5, Issue:3

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Clioquinol; Humans; Metalloproteins; Metals; Mode

2008
Alzheimer's disease, metal ions and metal homeostatic therapy.
    Trends in pharmacological sciences, 2009, Volume: 30, Issue:7

    Topics: Alzheimer Disease; Animals; Clioquinol; Homeostasis; Humans; Metals; Plaque, Amyloid

2009
[Drug therapy for Alzheimer's disease].
    Brain and nerve = Shinkei kenkyu no shinpo, 2010, Volume: 62, Issue:7

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Anti-Inflammatory Agents, Non-Steroidal; Cholinesterase In

2010
Alzheimer's disease & metals: therapeutic opportunities.
    British journal of pharmacology, 2011, Volume: 163, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Binding Sites; Cations; Clinical Trials as Topic;

2011
Metal protein attenuating compounds for the treatment of Alzheimer's dementia.
    The Cochrane database of systematic reviews, 2012, May-16, Issue:5

    Topics: Aged; Alzheimer Disease; Chelating Agents; Clioquinol; Humans; Randomized Controlled Trials as Topic

2012
Modulating metals as a therapeutic strategy for Alzheimer's disease.
    Future medicinal chemistry, 2012, Volume: 4, Issue:8

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Clioquinol; Copper; Humans; Metals; Molecular Tar

2012
The metallobiology of Alzheimer's disease.
    Trends in neurosciences, 2003, Volume: 26, Issue:4

    Topics: Alzheimer Disease; Amebicides; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Clioq

2003
Current status of metals as therapeutic targets in Alzheimer's disease.
    Journal of the American Geriatrics Society, 2003, Volume: 51, Issue:8

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Chelating Agents; Clioquinol; Copper; Deferoxamin

2003
Metal-protein attenuating compounds and Alzheimer's disease.
    Expert opinion on investigational drugs, 2004, Volume: 13, Issue:12

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Clioquinol; Humans; Mice

2004
PBT-1 Prana Biotechnology.
    Current opinion in investigational drugs (London, England : 2000), 2005, Volume: 6, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Clinical Trials as Topic; Clioquinol; Humans

2005
Translational research on the way to effective therapy for Alzheimer disease.
    Archives of general psychiatry, 2005, Volume: 62, Issue:11

    Topics: Alzheimer Disease; Amyloid beta-Protein Precursor; Amyloid Precursor Protein Secretases; Apolipoprot

2005
Pharmacological strategies for the prevention of Alzheimer's disease.
    Expert opinion on pharmacotherapy, 2006, Volume: 7, Issue:1

    Topics: Alzheimer Disease; Clioquinol; Drug Delivery Systems; Humans; Pharmaceutical Preparations

2006
Clioquinol for the treatment of Alzheimer's Disease.
    The Cochrane database of systematic reviews, 2006, Jan-25, Issue:1

    Topics: Aged; Alzheimer Disease; Chelating Agents; Clioquinol; Humans; Randomized Controlled Trials as Topic

2006
Aluminum and other metals in Alzheimer's disease: a review of potential therapy with chelating agents.
    Journal of Alzheimer's disease : JAD, 2006, Volume: 10, Issue:2-3

    Topics: Aluminum; Alzheimer Disease; Chelating Agents; Clioquinol; Copper; Humans; Mercury; Zinc

2006
Therapeutic treatments for Alzheimer's disease based on metal bioavailability.
    Drug news & perspectives, 2006, Volume: 19, Issue:8

    Topics: Aging; Alzheimer Disease; Amyloid beta-Peptides; Animals; Biological Availability; Brain; Clioquinol

2006
Metal protein attenuating compounds for the treatment of Alzheimer's disease.
    The Cochrane database of systematic reviews, 2008, Jan-23, Issue:1

    Topics: Aged; Alzheimer Disease; Chelating Agents; Clioquinol; Humans; Randomized Controlled Trials as Topic

2008
The role of metals in modulating metalloprotease activity in the AD brain.
    European biophysics journal : EBJ, 2008, Volume: 37, Issue:3

    Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Animals; Brain; Cell Culture Techniques; Chelatin

2008
[Therapeutic effect of clioquinol for Alzheimer disease].
    Nihon yakurigaku zasshi. Folia pharmacologica Japonica, 2008, Volume: 131, Issue:3

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Anesthetics, Inhalation; Animals; Brain; Caspase 3; Choles

2008
Metal chelator decreases Alzheimer beta-amyloid plaques.
    Neuron, 2001, Volume: 30, Issue:3

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Chelating Agents; Clioquinol; Plaque, Amyloid

2001
'...and C is for Clioquinol' - the AbetaCs of Alzheimer's disease.
    Trends in neurosciences, 2002, Volume: 25, Issue:3

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Chelating Agents; Clioquinol; Disease Models, Ani

2002

Trials

4 trials available for clioquinol and Alzheimer Disease

ArticleYear
Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial.
    The Lancet. Neurology, 2008, Volume: 7, Issue:9

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Biomarkers; Brain; Clioquinol; Do

2008
Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial.
    The Lancet. Neurology, 2008, Volume: 7, Issue:9

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Biomarkers; Brain; Clioquinol; Do

2008
Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial.
    The Lancet. Neurology, 2008, Volume: 7, Issue:9

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Biomarkers; Brain; Clioquinol; Do

2008
Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial.
    The Lancet. Neurology, 2008, Volume: 7, Issue:9

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Biomarkers; Brain; Clioquinol; Do

2008
PBT2 rapidly improves cognition in Alzheimer's Disease: additional phase II analyses.
    Journal of Alzheimer's disease : JAD, 2010, Volume: 20, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Area Under Curve; Australia; Clioquinol; Cognition Disorde

2010
Why participate in an Alzheimer's disease clinical trial? Is it of benefit to carers and patients?
    International psychogeriatrics, 2003, Volume: 15, Issue:2

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Australia; Caregivers; Clioquinol; Consumer Behavior; Co

2003
Metal-protein attenuation with iodochlorhydroxyquin (clioquinol) targeting Abeta amyloid deposition and toxicity in Alzheimer disease: a pilot phase 2 clinical trial.
    Archives of neurology, 2003, Volume: 60, Issue:12

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Chelating Agents; Clioquinol; Cog

2003

Other Studies

76 other studies available for clioquinol and Alzheimer Disease

ArticleYear
1,1'-Xylyl bis-1,4,8,11-tetraaza cyclotetradecane: a new potential copper chelator agent for neuroprotection in Alzheimer's disease. Its comparative effects with clioquinol on rat brain copper distribution.
    Bioorganic & medicinal chemistry letters, 2006, Jun-15, Volume: 16, Issue:12

    Topics: Alzheimer Disease; Animals; Chelating Agents; Clioquinol; Copper; Heterocyclic Compounds, 1-Ring; Mo

2006
Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer's disease.
    Bioorganic & medicinal chemistry, 2011, Sep-15, Volume: 19, Issue:18

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Cell Line, Tumor; Chelating Agents; Curcumin

2011
Design, synthesis, and evaluation of multitarget-directed resveratrol derivatives for the treatment of Alzheimer's disease.
    Journal of medicinal chemistry, 2013, Jul-25, Volume: 56, Issue:14

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Blood-Brain Barrier; Cholinesterase

2013
Design, synthesis and biological evaluation of imine resveratrol derivatives as multi-targeted agents against Alzheimer's disease.
    European journal of medicinal chemistry, 2014, Volume: 71

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Cell Line, Tumor; Copper; Humans; Neuroprote

2014
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
    Journal of medicinal chemistry, 2015, Nov-25, Volume: 58, Issue:22

    Topics: Alzheimer Disease; Animals; Antioxidants; Biological Availability; Brain; Cell Line, Tumor; Cell Sur

2015
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
    Journal of medicinal chemistry, 2015, Nov-12, Volume: 58, Issue:21

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Benzofurans; Clioquinol; Cognition;

2015
Ionophoric polyphenols selectively bind Cu(2+), display potent antioxidant and anti-amyloidogenic properties, and are non-toxic toward Tetrahymena thermophila.
    Bioorganic & medicinal chemistry, 2016, 08-15, Volume: 24, Issue:16

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Blood-Brain Barrier; Carbon-13 Magnetic Reso

2016
Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2016, Nov-10, Volume: 123

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Blood-Brain Barrier; Cell S

2016
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
    Journal of medicinal chemistry, 2016, Sep-22, Volume: 59, Issue:18

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Cell Line; Ch

2016
Synthesis and evaluation of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) as effective inhibitor of metal-induced Aβ aggregation and antioxidant.
    Bioorganic & medicinal chemistry, 2016, 10-01, Volume: 24, Issue:19

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Blood-Brain Barrier; Copper; Drug Design; Hu

2016
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
    Bioorganic & medicinal chemistry, 2017, 07-15, Volume: 25, Issue:14

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Apoptosis; Binding Sites; Blood-Bra

2017
Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2018, Jan-01, Volume: 143

    Topics: Acetylcholinesterase; Alzheimer Disease; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors;

2018
Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease.
    Journal of medicinal chemistry, 2018, 03-08, Volume: 61, Issue:5

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Blood-Brain Barrier; Cell Proliferation; Drug Des

2018
Metallomics for Alzheimer's disease treatment: Use of new generation of chelators combining metal-cation binding and transport properties.
    European journal of medicinal chemistry, 2018, Apr-25, Volume: 150

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Cations; Cell Proliferation; Cell Survival; Chelating Agen

2018
Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2019, Feb-01, Volume: 163

    Topics: Alzheimer Disease; Aminopyridines; Animals; Benzamides; Clioquinol; Cyclic Nucleotide Phosphodiester

2019
Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease.
    European journal of medicinal chemistry, 2019, Apr-01, Volume: 167

    Topics: Alzheimer Disease; Amides; Amines; Animals; Antioxidants; Blood-Brain Barrier; Cell Line; Chelating

2019
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
    Bioorganic & medicinal chemistry, 2020, 04-01, Volume: 28, Issue:7

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Clioquinol; Drug Discovery; Flurbiprofen; Humans; Ligands;

2020
Design, synthesis and biological evaluation of novel deoxyvasicinone-indole as multi-target agents for Alzheimer's disease.
    Bioorganic & medicinal chemistry letters, 2021, 10-01, Volume: 49

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Butyrylcholinesterase; Cata

2021
Novel hydroxybenzylamine-deoxyvasicinone hybrids as anticholinesterase therapeutics for Alzheimer's disease.
    Bioorganic & medicinal chemistry, 2021, 09-01, Volume: 45

    Topics: Acetylcholinesterase; Alkaloids; Alzheimer Disease; Amyloid beta-Peptides; Animals; Benzylamines; Bu

2021
Synthesis and biological evaluation of selective histone deacetylase 6 inhibitors as multifunctional agents against Alzheimer's disease.
    European journal of medicinal chemistry, 2021, Dec-05, Volume: 225

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Cell Survival; Copper; Dose-Response Relationship, Drug; H

2021
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease.
    European journal of medicinal chemistry, 2021, Dec-15, Volume: 226

    Topics: Alzheimer Disease; Calorimetry; Dose-Response Relationship, Drug; Drug Discovery; Humans; Models, Mo

2021
Clioquinol Decreases Levels of Phosphorylated, Truncated, and Oligomerized Tau Protein.
    International journal of molecular sciences, 2021, Nov-08, Volume: 22, Issue:21

    Topics: Alzheimer Disease; Autophagy; Cell Line, Tumor; Clioquinol; Copper; Gene Expression Regulation; Huma

2021
Alzheimer's Drug PBT2 Interacts with the Amyloid β 1-42 Peptide Differently than Other 8-Hydroxyquinoline Chelating Drugs.
    Inorganic chemistry, 2022, Sep-19, Volume: 61, Issue:37

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Chelating Agents; Clioquinol; Copper; Humans; Ions; Metals

2022
WBQ5187, a Multitarget Directed Agent, Ameliorates Cognitive Impairment in a Transgenic Mouse Model of Alzheimer's Disease and Modulates Cerebral β-Amyloid, Gliosis, cAMP Levels, and Neurodegeneration.
    ACS chemical neuroscience, 2019, 12-18, Volume: 10, Issue:12

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Anesthetics, General; Animals; Benzofurans; Biological Ava

2019
Prolongation of metallothionein induction combats Aß and α-synuclein toxicity in aged transgenic Caenorhabditis elegans.
    Scientific reports, 2020, 07-16, Volume: 10, Issue:1

    Topics: Aging; alpha-Synuclein; Alzheimer Disease; Amyloid beta-Peptides; Animals; Animals, Genetically Modi

2020
Copper(II) Binding to PBT2 Differs from That of Other 8-Hydroxyquinoline Chelators: Implications for the Treatment of Neurodegenerative Protein Misfolding Diseases.
    Inorganic chemistry, 2020, Dec-07, Volume: 59, Issue:23

    Topics: Alzheimer Disease; Animals; Chelating Agents; Clioquinol; Coordination Complexes; Copper; Density Fu

2020
Hybrid Multifunctional Modulators Inhibit Multifaceted Aβ Toxicity and Prevent Mitochondrial Damage.
    ACS chemical neuroscience, 2018, 06-20, Volume: 9, Issue:6

    Topics: Alzheimer Disease; Animals; Antioxidants; Chelating Agents; Clioquinol; Mitochondria; Oxidative Stre

2018
Insights into the inhibitory mechanism of a resveratrol and clioquinol hybrid against Aβ
    Journal of biomolecular structure & dynamics, 2019, Volume: 37, Issue:12

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Clioquinol; Humans; Hydrogen Bonding; Hydrophobic and Hydr

2019
Can we reverse Alzheimer's? New approaches from Harvard offer hope.
    Harvard health letter, 2013, Volume: 38, Issue:3

    Topics: Alzheimer Disease; Clioquinol; Cognition; Health Behavior; Humans; Mental Processes; Risk Reduction

2013
Efficacy and toxicity of clioquinol treatment and A-beta42 inoculation in the APP/PSI mouse model of Alzheimer's disease.
    Current Alzheimer research, 2013, Volume: 10, Issue:5

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Antigens, CD; Ant

2013
The solution structure of the copper clioquinol complex.
    Journal of inorganic biochemistry, 2014, Volume: 133

    Topics: Alzheimer Disease; Chelating Agents; Clioquinol; Copper; Humans; Molecular Structure; Neoplasms; Sol

2014
Clioquinol promotes the degradation of metal-dependent amyloid-β (Aβ) oligomers to restore endocytosis and ameliorate Aβ toxicity.
    Proceedings of the National Academy of Sciences of the United States of America, 2014, Mar-18, Volume: 111, Issue:11

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Caenorhabditis elegans; Clioquinol; Drug Discover

2014
New multi-target-directed small molecules against Alzheimer's disease: a combination of resveratrol and clioquinol.
    Organic & biomolecular chemistry, 2014, Aug-21, Volume: 12, Issue:31

    Topics: Absorption, Physiological; Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Blood-Br

2014
Design, synthesis, and evaluation of multitarget-directed selenium-containing clioquinol derivatives for the treatment of Alzheimer's disease.
    ACS chemical neuroscience, 2014, Oct-15, Volume: 5, Issue:10

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Blood-Brain Barrier; Capillary Perm

2014
Stabilization of nontoxic Aβ-oligomers: insights into the mechanism of action of hydroxyquinolines in Alzheimer's disease.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2015, Feb-18, Volume: 35, Issue:7

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Benzothiazoles; Biophysics; Caenorhabditis elegan

2015
The zinc ionophore clioquinol reverses autophagy arrest in chloroquine-treated ARPE-19 cells and in APP/mutant presenilin-1-transfected Chinese hamster ovary cells.
    Neurobiology of aging, 2015, Volume: 36, Issue:12

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Autophagy; Chloro

2015
Computer-assisted designed "selenoxy-chinolin": a new catalytic mechanism of the GPx-like cycle and inhibition of metal-free and metal-associated Aβ aggregation.
    Dalton transactions (Cambridge, England : 2003), 2015, Dec-28, Volume: 44, Issue:48

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Antioxidants; Azoles; Biocompatible Materials; Bl

2015
Iron Chelation Inhibits Osteoclastic Differentiation In Vitro and in Tg2576 Mouse Model of Alzheimer's Disease.
    PloS one, 2015, Volume: 10, Issue:11

    Topics: Alzheimer Disease; Animals; Bone Resorption; Cation Transport Proteins; Cell Differentiation; Cells,

2015
Novel 8-Hydroxyquinoline Derivatives as Multitarget Compounds for the Treatment of Alzheimer's Disease.
    ChemMedChem, 2016, 06-20, Volume: 11, Issue:12

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Blood-Brain Barrier; Butyrylcholinesterase;

2016
Discovery of novel PDE9 inhibitors capable of inhibiting Aβ aggregation as potential candidates for the treatment of Alzheimer's disease.
    Scientific reports, 2016, Feb-25, Volume: 6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Alzheimer Disease; Amyloid beta-Peptides; Blood-Brain Barrier;

2016
The prevalence of dementia in subacute myelo-optico-neuropathy (SMON) patients who underwent medical checkups.
    Nihon Ronen Igakkai zasshi. Japanese journal of geriatrics, 2016, Volume: 53, Issue:2

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Anti-Infective Agents; Clioquinol; Dementia; Female; Hum

2016
Rapid restoration of cognition in Alzheimer's transgenic mice with 8-hydroxy quinoline analogs is associated with decreased interstitial Abeta.
    Neuron, 2008, Jul-10, Volume: 59, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Analysis of Variance; Anim

2008
Testing the mettle of PBT2 for Alzheimer's disease.
    The Lancet. Neurology, 2008, Volume: 7, Issue:9

    Topics: Aged; Alzheimer Disease; Amyloid beta-Peptides; Clinical Trials, Phase II as Topic; Clioquinol; Huma

2008
Mutual stimulation of beta-amyloid fibrillogenesis by clioquinol and divalent metals.
    Neuromolecular medicine, 2008, Volume: 10, Issue:4

    Topics: Alzheimer Disease; Amino Acid Substitution; Amyloid beta-Peptides; Animals; Cell Line, Tumor; Chelat

2008
The curious case of clioquinol.
    Nature medicine, 2009, Volume: 15, Issue:4

    Topics: Alzheimer Disease; Anti-Infective Agents, Local; Blindness; Clioquinol; Humans; Japan; Memory; Memor

2009
Clioquinol decreases amyloid-beta burden and reduces working memory impairment in a transgenic mouse model of Alzheimer's disease.
    Journal of Alzheimer's disease : JAD, 2009, Volume: 17, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Analysis of Variance; Anim

2009
Fenton chemistry and oxidative stress mediate the toxicity of the beta-amyloid peptide in a Drosophila model of Alzheimer's disease.
    The European journal of neuroscience, 2009, Volume: 29, Issue:7

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Animals, Genetically Modified; Apoferritins; Brai

2009
Effects of clioquinol on metal-triggered amyloid-beta aggregation revisited.
    Inorganic chemistry, 2009, Oct-19, Volume: 48, Issue:20

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Chelating Agents; Clioquinol; Copper; Humans; Metals; Solu

2009
Hydroxyquinoline based binders: promising ligands for chelatotherapy?
    Journal of inorganic biochemistry, 2011, Volume: 105, Issue:3

    Topics: Alzheimer Disease; Cations, Divalent; Chelating Agents; Clioquinol; Colorimetry; Drug Stability; Hum

2011
Protective effects of clioquinol on human neuronal-like cells: a new formulation of clioquinol-loaded PLGA microspheres for Alzheimer's disease.
    Journal of drug targeting, 2011, Volume: 19, Issue:8

    Topics: Alzheimer Disease; Biocompatible Materials; Cell Culture Techniques; Cell Death; Cell Line, Tumor; C

2011
Metal ionophore treatment restores dendritic spine density and synaptic protein levels in a mouse model of Alzheimer's disease.
    PloS one, 2011, Mar-11, Volume: 6, Issue:3

    Topics: Alzheimer Disease; Animals; Cells, Cultured; Clioquinol; Dendritic Spines; Disease Models, Animal; F

2011
The Alzheimer's therapeutic PBT2 promotes amyloid-β degradation and GSK3 phosphorylation via a metal chaperone activity.
    Journal of neurochemistry, 2011, Volume: 119, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Blotting, Western; Calcineurin; Calcineurin Inhibitors; Ca

2011
Copper in Alzheimer disease: too much, too little, or misplaced?
    Free radical biology & medicine, 2012, Feb-15, Volume: 52, Issue:4

    Topics: Alzheimer Disease; Animals; Brain; Clioquinol; Copper; Hepatolenticular Degeneration; Humans; Menkes

2012
Clioquinol reduces zinc accumulation in neuritic plaques and inhibits the amyloidogenic pathway in AβPP/PS1 transgenic mouse brain.
    Journal of Alzheimer's disease : JAD, 2012, Volume: 29, Issue:3

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Brain; Chelating

2012
Utility of an improved model of amyloid-beta (Aβ₁₋₄₂) toxicity in Caenorhabditis elegans for drug screening for Alzheimer's disease.
    Molecular neurodegeneration, 2012, Nov-21, Volume: 7

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Animals, Genetically Modified; Caenorhabditis ele

2012
Mesoporous silica nanoparticle-based H2O2 responsive controlled-release system used for Alzheimer's disease treatment.
    Advanced healthcare materials, 2012, Volume: 1, Issue:3

    Topics: Alzheimer Disease; Animals; Cell Survival; Clioquinol; Delayed-Action Preparations; Hydrogen Peroxid

2012
New therapies. New Alzheimer's treatments that may ease the mind.
    Science (New York, N.Y.), 2002, Aug-23, Volume: 297, Issue:5585

    Topics: Alzheimer Disease; Alzheimer Vaccines; Amyloid beta-Peptides; Amyloid Precursor Protein Secretases;

2002
An iron-responsive element type II in the 5'-untranslated region of the Alzheimer's amyloid precursor protein transcript.
    The Journal of biological chemistry, 2002, Nov-22, Volume: 277, Issue:47

    Topics: 5' Untranslated Regions; Alzheimer Disease; Amyloid beta-Protein Precursor; Animals; Base Sequence;

2002
Ironic fate: can a banned drug control metal heavies in neurodegenerative diseases?
    Neuron, 2003, Mar-27, Volume: 37, Issue:6

    Topics: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; Alzheimer Disease; Animals; Clioquinol; Ferritins; Gen

2003
Changes in intracellular calcium and glutathione in astrocytes as the primary mechanism of amyloid neurotoxicity.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2003, Jun-15, Volume: 23, Issue:12

    Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Animals; Astrocytes; Calcium; Calcium Signaling;

2003
Metal chelation therapy for Alzheimer disease.
    Archives of neurology, 2003, Volume: 60, Issue:12

    Topics: Alzheimer Disease; Chelating Agents; Chelation Therapy; Clioquinol; Humans; Zinc

2003
Clioquinol, a drug for Alzheimer's disease specifically interfering with brain metal metabolism: structural characterization of its zinc(II) and copper(II) complexes.
    Inorganic chemistry, 2004, Jun-28, Volume: 43, Issue:13

    Topics: Alzheimer Disease; Brain; Chelating Agents; Clioquinol; Copper; Crystallography, X-Ray; Molecular Co

2004
Clioquinol mediates copper uptake and counteracts copper efflux activities of the amyloid precursor protein of Alzheimer's disease.
    The Journal of biological chemistry, 2004, Dec-10, Volume: 279, Issue:50

    Topics: Alzheimer Disease; Amyloid beta-Protein Precursor; Animals; Biological Transport, Active; Chelating

2004
Prana Biotechnology, Limited: metal attenuation in the treatment of neurodegenerative disease.
    Chemistry & biology, 2004, Volume: 11, Issue:11

    Topics: Alzheimer Disease; Animals; Biotechnology; Clioquinol; Copper; Metalloproteins; Mice; Neurodegenerat

2004
Metal ion-dependent effects of clioquinol on the fibril growth of an amyloid {beta} peptide.
    The Journal of biological chemistry, 2005, Apr-22, Volume: 280, Issue:16

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Anti-Infective Agents, Local; Circular Dichroism; Clioquin

2005
Clioquinol treatment in familiar early onset of Alzheimer's disease: a case report.
    Pharmacopsychiatry, 2005, Volume: 38, Issue:4

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Brain; Chelating Agents; Clioquinol; Cognition; Female; Hu

2005
Alzheimer disease beta-amyloid activity mimics cholesterol oxidase.
    The Journal of clinical investigation, 2005, Volume: 115, Issue:9

    Topics: Adult; Aged; Aged, 80 and over; Alzheimer Disease; Amyloid beta-Peptides; Animals; Brain; Cells, Cul

2005
Radioiodinated clioquinol as a biomarker for beta-amyloid: Zn complexes in Alzheimer's disease.
    Aging cell, 2006, Volume: 5, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Biomarkers; Brain; Clioquinol; Humans; Iodine Rad

2006
Clioquinol treatment in familiar early onset of Alzheimer's disease: Ibach B et al., Pharmacopsychiatry 2005; 38: 178-179.
    Pharmacopsychiatry, 2006, Volume: 39, Issue:2

    Topics: Alzheimer Disease; Anti-Infective Agents, Local; Clioquinol; Humans

2006
Degradation of the Alzheimer disease amyloid beta-peptide by metal-dependent up-regulation of metalloprotease activity.
    The Journal of biological chemistry, 2006, Jun-30, Volume: 281, Issue:26

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Anti-Infective Agents, Local; Cell Line, Tumor; C

2006
Copper and clioquinol treatment in young APP transgenic and wild-type mice: effects on life expectancy, body weight, and metal-ion levels.
    Journal of molecular medicine (Berlin, Germany), 2007, Volume: 85, Issue:4

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Animals, Genetica

2007
The inhalation anesthetic isoflurane induces a vicious cycle of apoptosis and amyloid beta-protein accumulation.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2007, Feb-07, Volume: 27, Issue:6

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid Precursor Protein Secretases; Anesthetics, Inhalat

2007
Stoichiometry and conditional stability constants of Cu(II) or Zn(II) clioquinol complexes; implications for Alzheimer's and Huntington's disease therapy.
    Neurotoxicology, 2007, Volume: 28, Issue:3

    Topics: Adenosine Triphosphate; Algorithms; Alzheimer Disease; Animals; Chemical Phenomena; Chemistry, Physi

2007
Neuroscience. An antibiotic to treat Alzheimer's?
    Science (New York, N.Y.), 2000, Nov-17, Volume: 290, Issue:5495

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Brain; Clinical Trials, Phase II as Topic; Clioqu

2000
Clioquinol's return: cautions from Japan.
    Science (New York, N.Y.), 2001, Jun-22, Volume: 292, Issue:5525

    Topics: Alzheimer Disease; Animals; Clinical Trials, Phase II as Topic; Clioquinol; Humans; Japan; Mice; Mye

2001
Treatment with a copper-zinc chelator markedly and rapidly inhibits beta-amyloid accumulation in Alzheimer's disease transgenic mice.
    Neuron, 2001, Volume: 30, Issue:3

    Topics: Age Factors; Alzheimer Disease; Amyloid beta-Peptides; Animals; Chelating Agents; Clioquinol; Copper

2001