tacrine has been researched along with Acute Liver Injury, Drug-Induced in 60 studies
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.
| Excerpt | Relevance | Reference |
|---|---|---|
| "The safety of tacrine (Cognex), a centrally active, reversible acetylcholinesterase inhibitor approved in 1993 for the treatment of mild to moderate dementia of the Alzheimer type, was evaluated in 2,706 patients with Alzheimer disease (AD) in clinical trials and in 9861 patients with AD in a treatment investigational new drug (TIND) program." | 4.80 | Safety of tacrine: clinical trials, treatment IND, and postmarketing experience. ( Berghoff, WG; DeJong, R; Dombey, SL; Gracon, SI; Knapp, MJ; Kraemer, D; Lobbestael, SJ; Luscombe, FA; Pierce, M; Symons, J, 1998) |
| "Tacrine was the first acetylcholinesterase inhibitor approved for the treatment of Alzheimer disease." | 3.78 | Tacrine is implicated in oxidative stress in the laboratory guinea pig model. ( Bandouchova, H; Kracmarova, A; Pikula, J; Pohanka, M, 2012) |
| "Tacrine (THA) was the first clinically approved cholinesterase (ChE) inhibitor, which was withdrawn due to high hepatotoxicity." | 3.01 | Tacrine-Based Hybrids: Past, Present, and Future. ( Beloglazkina, E; Bubley, A; Erofeev, A; Gorelkin, P; Krasnovskaya, O; Majouga, A, 2023) |
| " Direct liver injury, possibly associated with the production of a toxic metabolite, would be consistent with reports of aberrant xenobiotic metabolism in Alzheimer's disease patients." | 2.67 | Clinical trials with velnacrine: (PROPP) the physician reference of predicted probabilities--a statistical model for the estimation of hepatotoxicity risk with velnacrine maleate. ( Hardiman, S; Miller, K; Murphy, M, 1993) |
| "Multicentre double blind, placebo controlled, random order crossover trial with individual determination of maximum tolerated dosage and four month follow up." | 2.67 | Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial. Groupe Français d'Etude de la Tetrahydroaminoacridine. ( Chatellier, G; Lacomblez, L, 1990) |
| " It has a mean bioavailability after oral administration of about 17 percent and an elimination half-life of approximately three hours." | 2.39 | Tacrine: first drug approved for Alzheimer's disease. ( Crismon, ML, 1994) |
| " The two drugs are special as the dosage of them is guided mainly by side effects and not by therapeutic effects in contrast to most drugs used for psychiatric disorders." | 2.38 | Side effects of long acting cholinesterase inhibitors. ( Beermann, B, 1993) |
| "Tacrine was the first drug used in the therapy of Alzheimer's disease (AD) and is one of the leading structures frequently pursued in the drug discovery of novel candidates for tackling AD." | 1.91 | UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes. ( Konecny, J; Korabecny, J; Kučera, R; Kuratkova, A; Lauschke, VM; Nevosadova, L; Novak, M; Prchal, L; Soukup, O; Svobodova, B, 2023) |
| "Rosmarinic acid (RA) is a natural compound of phenolic acids that has pharmacological activity for inhibiting Alzheimer's disease, as well as liver protection." | 1.91 | Rosmarinic acid potentiates and detoxifies tacrine in combination for Alzheimer's disease. ( Gao, W; Guo, L; Han, X; Huang, L; Ji, H; Li, X; Qiao, O; Wang, J; Wang, W; Yang, M; Zhang, X; Zhang, Y, 2023) |
| "Tacrine was withdrawn from clinical use as a drug against Alzheimer's disease in 2013, mainly due to drug-induced liver injury." | 1.91 | Tacrine First-Phase Biotransformation and Associated Hepatotoxicity: A Possible Way to Avoid Quinone Methide Formation. ( Kobrlova, T; Korabecny, J; Koutsilieri, S; Kučera, R; Lauschke, VM; Novak, M; Prchal, L; Raisova-Stuchlikova, L; Sismanoglou, DC; Skalova, L; Soukup, O; Svobodova, B; Vajrychova, M; Zarybnicky, T, 2023) |
| "Alzheimer's disease has become a public health priority, so an investigation of new therapies is required." | 1.56 | Combined Therapy for Alzheimer's Disease: Tacrine and PAMAM Dendrimers Co-Administration Reduces the Side Effects of the Drug without Modifying its Activity. ( Del V Alonso, S; Igartúa, DE; Martinez, CS; Prieto, MJ, 2020) |
| " However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2." | 1.46 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. ( Edginton, AN; McEneny-King, A; Osman, W; Rao, PPN, 2017) |
| " We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | 1.37 | FDA-approved drug labeling for the study of drug-induced liver injury. ( Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) |
| " An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems." | 1.36 | Developing structure-activity relationships for the prediction of hepatotoxicity. ( Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010) |
| "Ferulic acid is an antioxidant." | 1.36 | Tacrine-NO donor and tacrine-ferulic acid hybrid molecules as new anti-Alzheimer agents: hepatotoxicity and influence on the cytochrome P450 system in comparison to tacrine. ( Appenroth, D; Decker, M; Fang, L; Fleck, C; Lehmann, J; Lupp, A, 2010) |
| " The toxic effect of tacrine on hepatocytes was assayed by the reduction of methyl thiazolyl tetrazolium (MTT) and intracellular glutathione (GSH), as well as by albumin synthesis." | 1.34 | Re-evaluation of tacrine hepatotoxicity using gel entrapped hepatocytes. ( Bader, A; Meng, Q; Ru, J; Schmitmeier, S; Shen, C; Zhang, G, 2007) |
| " The role of acute dosing rodent models in identifying candidate genes associated with drug-induced liver injury in man deserves further study." | 1.34 | Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity. ( Alfirevic, A; Barratt, BJ; Carr, DF; Park, BK; Pirmohamed, M; Sherwood, J; Smith, J; Tugwood, JD, 2007) |
| "Fifty consecutive outpatients with Alzheimer's disease (AD) received treatment with the cholinesterase inhibitor tacrine in an open longitudinal study." | 1.32 | Five-year outcome of cholinergic treatment of Alzheimer's disease: early response predicts prolonged time until nursing home placement, but does not alter life expectancy. ( Gustafson, L; Minthon, L; Sjögren, M; Wallin, AK; Wattmo, C, 2004) |
| "The toxic effect of THA on mice liver was significantly reduced by DDB." | 1.31 | [Effect of dimethyl diphenyl bicarboxylate (DDB) on 9-amino-1,2,3,4-tetrahydroacridine-induced hepatotoxicity in mice]. ( Li, Y, 2001) |
| " A reliable caregiver is essential to ensure compliance with frequent dosing and weekly blood testing." | 1.29 | Alzheimer's disease: how to give and monitor tacrine therapy. ( Lantz, MS; Woo, JK, 1995) |
| "Seventy-nine patients with probable Alzheimer's disease were enrolled into a double-blind, placebo-controlled cross-over study to assess the therapeutic effect and safety of THA (tetrahydroaminoacridine; tacrine) without concomitant lecithin administration." | 1.29 | An evaluation of the efficacy and safety of tetrahydroaminoacridine (THA) without lecithin in the treatment of Alzheimer's disease. ( Boyle, M; Mulligan, K; Neubauer, KA; O'Neill, D; Royston, VH; Scott, M; Surmon, DJ; Wilcock, GK, 1993) |
| "Clinical trials with tacrine (THA) and its principal (1-OH) metabolite (velnacrine) for the treatment of Alzheimer's disease have been hampered by adverse hepatic events that were undetected in preclinical studies." | 1.29 | Cytotoxicity of tacrine and velnacrine metabolites in cultured rat, dog and human hepatocytes. ( Curren, RD; Viau, CJ; Wallace, K, 1993) |
| "Patients receiving THA for treatment of Alzheimer's disease need regular monitoring of liver function." | 1.28 | Heterogeneity of adverse hepatic reactions to tetrahydroaminoacridine. ( Ames, DJ; Bhathal, PS; Davies, BM; Fraser, JR; Gibson, PR; Roberts, S, 1990) |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 4 (6.67) | 18.7374 |
| 1990's | 19 (31.67) | 18.2507 |
| 2000's | 7 (11.67) | 29.6817 |
| 2010's | 22 (36.67) | 24.3611 |
| 2020's | 8 (13.33) | 2.80 |
| Authors | Studies |
|---|---|
| Shutske, GM | 1 |
| Pierrat, FA | 1 |
| Cornfeldt, ML | 1 |
| Szewczak, MR | 1 |
| Huger, FP | 1 |
| Bores, GM | 1 |
| Haroutunian, V | 1 |
| Davis, KL | 1 |
| Greene, N | 1 |
| Fisk, L | 1 |
| Naven, RT | 1 |
| Note, RR | 1 |
| Patel, ML | 1 |
| Pelletier, DJ | 1 |
| Morgan, RE | 2 |
| Trauner, M | 1 |
| van Staden, CJ | 2 |
| Lee, PH | 1 |
| Ramachandran, B | 1 |
| Eschenberg, M | 1 |
| Afshari, CA | 2 |
| Qualls, CW | 1 |
| Lightfoot-Dunn, R | 1 |
| Hamadeh, HK | 2 |
| Ekins, S | 1 |
| Williams, AJ | 1 |
| Xu, JJ | 1 |
| Chen, M | 1 |
| Vijay, V | 1 |
| Shi, Q | 2 |
| Liu, Z | 2 |
| Fang, H | 2 |
| Tong, W | 2 |
| Dawson, S | 1 |
| Stahl, S | 2 |
| Paul, N | 1 |
| Barber, J | 1 |
| Kenna, JG | 2 |
| Ding, D | 1 |
| Kelly, R | 1 |
| Sakatis, MZ | 1 |
| Reese, MJ | 1 |
| Harrell, AW | 1 |
| Taylor, MA | 1 |
| Baines, IA | 1 |
| Chen, L | 2 |
| Bloomer, JC | 1 |
| Yang, EY | 1 |
| Ellens, HM | 1 |
| Ambroso, JL | 1 |
| Lovatt, CA | 1 |
| Ayrton, AD | 1 |
| Clarke, SE | 1 |
| Warner, DJ | 1 |
| Chen, H | 1 |
| Cantin, LD | 1 |
| Walker, CL | 1 |
| Noeske, T | 1 |
| Chen, Y | 1 |
| Kalyanaraman, N | 1 |
| Kalanzi, J | 1 |
| Dunn, RT | 1 |
| Xie, SS | 1 |
| Lan, JS | 1 |
| Wang, XB | 1 |
| Jiang, N | 1 |
| Dong, G | 1 |
| Li, ZR | 1 |
| Wang, KD | 1 |
| Guo, PP | 1 |
| Kong, LY | 1 |
| Zha, X | 1 |
| Lamba, D | 1 |
| Zhang, L | 2 |
| Lou, Y | 1 |
| Xu, C | 1 |
| Kang, D | 1 |
| Xu, Y | 1 |
| De Simone, A | 1 |
| Samez, S | 1 |
| Pesaresi, A | 1 |
| Stojan, J | 1 |
| Lopez, MG | 1 |
| Egea, J | 1 |
| Andrisano, V | 1 |
| Bartolini, M | 1 |
| Dgachi, Y | 1 |
| Sokolov, O | 1 |
| Luzet, V | 1 |
| Godyń, J | 1 |
| Panek, D | 1 |
| Bonet, A | 1 |
| Martin, H | 1 |
| Iriepa, I | 1 |
| Moraleda, I | 1 |
| García-Iriepa, C | 1 |
| Janockova, J | 1 |
| Richert, L | 1 |
| Soukup, O | 5 |
| Malawska, B | 1 |
| Chabchoub, F | 1 |
| Marco-Contelles, J | 1 |
| Ismaili, L | 1 |
| McEneny-King, A | 1 |
| Osman, W | 1 |
| Edginton, AN | 1 |
| Rao, PPN | 1 |
| Cen, J | 1 |
| Guo, H | 1 |
| Hong, C | 1 |
| Lv, J | 1 |
| Yang, Y | 1 |
| Wang, T | 1 |
| Fang, D | 1 |
| Luo, W | 1 |
| Wang, C | 1 |
| Djafarou, S | 1 |
| Amine Khodja, I | 1 |
| Boulebd, H | 1 |
| Novak, M | 4 |
| Svobodova, B | 4 |
| Konecny, J | 3 |
| Kuratkova, A | 3 |
| Nevosadova, L | 3 |
| Prchal, L | 4 |
| Korabecny, J | 4 |
| Lauschke, VM | 4 |
| Kučera, R | 4 |
| Yang, M | 1 |
| Zhang, X | 1 |
| Qiao, O | 1 |
| Ji, H | 1 |
| Zhang, Y | 1 |
| Han, X | 1 |
| Wang, W | 1 |
| Li, X | 1 |
| Wang, J | 1 |
| Guo, L | 1 |
| Huang, L | 1 |
| Gao, W | 1 |
| Bubley, A | 1 |
| Erofeev, A | 1 |
| Gorelkin, P | 1 |
| Beloglazkina, E | 1 |
| Majouga, A | 1 |
| Krasnovskaya, O | 1 |
| Yang, H | 1 |
| Jia, H | 1 |
| Deng, M | 1 |
| Zhang, K | 1 |
| Liu, Y | 2 |
| Cheng, M | 1 |
| Xiao, W | 1 |
| Vajrychova, M | 1 |
| Koutsilieri, S | 1 |
| Sismanoglou, DC | 1 |
| Kobrlova, T | 1 |
| Zarybnicky, T | 1 |
| Raisova-Stuchlikova, L | 1 |
| Skalova, L | 1 |
| Niu, MW | 1 |
| Chen, P | 1 |
| Igartúa, DE | 1 |
| Martinez, CS | 1 |
| Del V Alonso, S | 1 |
| Prieto, MJ | 1 |
| Yip, LY | 1 |
| Aw, CC | 1 |
| Lee, SH | 1 |
| Hong, YS | 1 |
| Ku, HC | 1 |
| Xu, WH | 1 |
| Chan, JMX | 1 |
| Cheong, EJY | 1 |
| Chng, KR | 1 |
| Ng, AHQ | 1 |
| Nagarajan, N | 1 |
| Mahendran, R | 1 |
| Lee, YK | 1 |
| Browne, ER | 1 |
| Chan, ECY | 1 |
| Jin, M | 1 |
| Zhang, C | 1 |
| Zheng, T | 1 |
| Yao, D | 1 |
| Shen, L | 1 |
| Luo, J | 1 |
| Jiang, Z | 1 |
| Ma, J | 1 |
| Jin, XJ | 1 |
| Cui, J | 1 |
| Lee, JJ | 1 |
| Li, G | 1 |
| Park, SM | 1 |
| Ki, SH | 1 |
| Han, NR | 1 |
| Cho, IJ | 1 |
| Ku, SK | 1 |
| Kim, SC | 1 |
| Zhao, RJ | 1 |
| Kim, YW | 1 |
| Choi, JS | 1 |
| Han, YR | 1 |
| Byeon, JS | 1 |
| Choung, SY | 1 |
| Sohn, HS | 1 |
| Jung, HA | 1 |
| Byun, E | 1 |
| Jeong, GS | 1 |
| An, RB | 3 |
| Min, TS | 1 |
| Kim, YC | 3 |
| Lupp, A | 1 |
| Appenroth, D | 1 |
| Fang, L | 1 |
| Decker, M | 1 |
| Lehmann, J | 1 |
| Fleck, C | 1 |
| Hunt, CM | 1 |
| Kracmarova, A | 1 |
| Bandouchova, H | 1 |
| Pikula, J | 1 |
| Pohanka, M | 1 |
| Li, Y | 2 |
| Wallin, AK | 1 |
| Gustafson, L | 1 |
| Sjögren, M | 1 |
| Wattmo, C | 1 |
| Minthon, L | 1 |
| Oh, H | 1 |
| Sohn, DH | 1 |
| Meng, Q | 1 |
| Ru, J | 1 |
| Zhang, G | 1 |
| Shen, C | 1 |
| Schmitmeier, S | 1 |
| Bader, A | 1 |
| Carr, DF | 1 |
| Alfirevic, A | 1 |
| Tugwood, JD | 1 |
| Barratt, BJ | 1 |
| Sherwood, J | 1 |
| Smith, J | 1 |
| Pirmohamed, M | 3 |
| Park, BK | 3 |
| Ku, KL | 1 |
| Tsai, CT | 1 |
| Chang, WM | 1 |
| Shen, ML | 1 |
| Wu, CT | 1 |
| Liao, HF | 1 |
| Woo, JK | 1 |
| Lantz, MS | 1 |
| Crismon, ML | 1 |
| Hardiman, S | 1 |
| Miller, K | 1 |
| Murphy, M | 1 |
| Beermann, B | 1 |
| Watkins, PB | 1 |
| Zimmerman, HJ | 1 |
| Knapp, MJ | 2 |
| Gracon, SI | 2 |
| Lewis, KW | 1 |
| Wilcock, GK | 1 |
| Surmon, DJ | 1 |
| Scott, M | 1 |
| Boyle, M | 1 |
| Mulligan, K | 1 |
| Neubauer, KA | 1 |
| O'Neill, D | 1 |
| Royston, VH | 1 |
| Gauthier, S | 1 |
| Gauthier, L | 1 |
| Viau, CJ | 1 |
| Curren, RD | 1 |
| Wallace, K | 1 |
| Becquemont, L | 2 |
| Le Bot, MA | 2 |
| Riche, C | 2 |
| Beaune, P | 2 |
| Kitteringham, NR | 2 |
| Berson, A | 1 |
| Renault, S | 1 |
| Lettéron, P | 1 |
| Robin, MA | 1 |
| Fromenty, B | 1 |
| Fau, D | 1 |
| Durand-Schneider, AM | 1 |
| Feldmann, G | 2 |
| Pessayre, D | 2 |
| Lecoeur, S | 1 |
| Simon, T | 1 |
| Funck-Brentano, C | 1 |
| Jaillon, P | 1 |
| Berghoff, WG | 1 |
| Pierce, M | 1 |
| DeJong, R | 1 |
| Lobbestael, SJ | 1 |
| Symons, J | 1 |
| Dombey, SL | 1 |
| Luscombe, FA | 1 |
| Kraemer, D | 1 |
| De Sousa, M | 1 |
| Woolf, T | 1 |
| Lemière, J | 1 |
| Van Gool, D | 1 |
| Dom, R | 1 |
| Molloy, DW | 1 |
| Guyatt, GH | 1 |
| Wilson, DB | 1 |
| Duke, R | 1 |
| Rees, L | 1 |
| Singer, J | 1 |
| Chatellier, G | 1 |
| Lacomblez, L | 1 |
| Ames, DJ | 2 |
| Bhathal, PS | 2 |
| Davies, BM | 2 |
| Fraser, JR | 2 |
| Gibson, PR | 1 |
| Roberts, S | 1 |
| Hammel, P | 1 |
| Larrey, D | 1 |
| Bernuau, J | 1 |
| Kalafat, M | 1 |
| Fréneaux, E | 1 |
| Babany, G | 1 |
| Degott, C | 1 |
| Benhamou, JP | 1 |
| Summers, WK | 1 |
| Koehler, AL | 1 |
| Marsh, GM | 1 |
| Tachiki, K | 1 |
| Kling, A | 1 |
| Marx, JL | 1 |
8 reviews available for tacrine and Acute Liver Injury, Drug-Induced
| Article | Year |
|---|---|
Tacrine-Based Hybrids: Past, Present, and Future.
Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Chemical and Drug Induced Liver Inju | 2023 |
Mitochondrial and immunoallergic injury increase risk of positive drug rechallenge after drug-induced liver injury: a systematic review.
Topics: Amoxicillin-Potassium Clavulanate Combination; Antitubercular Agents; Azathioprine; Chemical and Dru | 2010 |
Tacrine: first drug approved for Alzheimer's disease.
Topics: Alanine Transaminase; Alzheimer Disease; Aspartate Aminotransferases; Chemical and Drug Induced Live | 1994 |
Side effects of long acting cholinesterase inhibitors.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Clinical Trial | 1993 |
What have we learned from the THA trials to facilitate testing of new AChE inhibitors.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Clinical Trial | 1993 |
The role of cytochrome P450 enzymes in hepatic and extrahepatic human drug toxicity.
Topics: Abnormalities, Drug-Induced; Acetaminophen; Chemical and Drug Induced Liver Injury; Cytochrome P-450 | 1995 |
Safety of tacrine: clinical trials, treatment IND, and postmarketing experience.
Topics: Adult; Aged; Aged, 80 and over; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Chi-Squar | 1998 |
Treatment of Alzheimer's disease: an evaluation of the cholinergic approach.
Topics: Acetylcholine; Alzheimer Disease; Animals; Carbamates; Chemical and Drug Induced Liver Injury; Choli | 1999 |
6 trials available for tacrine and Acute Liver Injury, Drug-Induced
| Article | Year |
|---|---|
Clinical trials with velnacrine: (PROPP) the physician reference of predicted probabilities--a statistical model for the estimation of hepatotoxicity risk with velnacrine maleate.
Topics: Age Factors; Aged; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibit | 1993 |
Hepatotoxic effects of tacrine administration in patients with Alzheimer's disease.
Topics: Aged; Alanine Transaminase; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Drug Administ | 1994 |
Effect of tetrahydroaminoacridine on cognition, function and behaviour in Alzheimer's disease.
Topics: Activities of Daily Living; Aged; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cogniti | 1991 |
Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial. Groupe Français d'Etude de la Tetrahydroaminoacridine.
Topics: Aged; Aged, 80 and over; Alzheimer Disease; Aminoacridines; Behavior; Chemical and Drug Induced Live | 1990 |
Long-term hepatotoxicity of tacrine.
Topics: Aminoacridines; Chemical and Drug Induced Liver Injury; Clinical Trials as Topic; Double-Blind Metho | 1989 |
FDA queries Alzheimer's trial results.
Topics: Alzheimer Disease; Aminoacridines; Chemical and Drug Induced Liver Injury; Clinical Trials as Topic; | 1988 |
46 other studies available for tacrine and Acute Liver Injury, Drug-Induced
| Article | Year |
|---|---|
(+/-)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity.
Topics: Alzheimer Disease; Aminoacridines; Animals; Chemical and Drug Induced Liver Injury; Chemical Phenome | 1988 |
Developing structure-activity relationships for the prediction of hepatotoxicity.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Humans; Structure-Activity Relationship; | 2010 |
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters | 2010 |
A predictive ligand-based Bayesian model for human drug-induced liver injury.
Topics: Bayes Theorem; Chemical and Drug Induced Liver Injury; Humans; Ligands | 2010 |
FDA-approved drug labeling for the study of drug-induced liver injury.
Topics: Animals; Benchmarking; Biomarkers, Pharmacological; Chemical and Drug Induced Liver Injury; Drug Des | 2011 |
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters | 2012 |
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
Topics: Animals; Anti-Infective Agents; Anti-Inflammatory Agents; Chemical and Drug Induced Liver Injury; Da | 2011 |
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
Topics: Chemical and Drug Induced Liver Injury; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme | 2012 |
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters | 2012 |
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily | 2013 |
Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
Topics: Alzheimer Disease; Animals; Antioxidants; Biphenyl Compounds; Blood-Brain Barrier; Cell Survival; Ch | 2015 |
Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.
Topics: Alzheimer Disease; Amyloid Precursor Protein Secretases; Animals; Aspartic Acid Endopeptidases; Beha | 2016 |
Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy.
Topics: Acetylcholinesterase; Alzheimer Disease; Aminoquinolines; Antioxidants; Blood-Brain Barrier; Chemica | 2017 |
Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity.
Topics: Benzoflavones; Binding Sites; Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A2; Cytoc | 2017 |
Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity.
Topics: Acetylcholinesterase; Alzheimer Disease; Animals; Biphenyl Compounds; Cell Line; Chemical and Drug I | 2018 |
Computational design of new tacrine analogs: an
Topics: Acetylcholinesterase; Alzheimer Disease; Antioxidants; Chemical and Drug Induced Liver Injury; Choli | 2023 |
UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Chromatography | 2023 |
UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Chromatography | 2023 |
UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Chromatography | 2023 |
UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; Chromatography | 2023 |
Rosmarinic acid potentiates and detoxifies tacrine in combination for Alzheimer's disease.
Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Chemical and Drug Induced L | 2023 |
Design, synthesis and evaluation of OA-tacrine hybrids as cholinesterase inhibitors with low neurotoxicity and hepatotoxicity against Alzheimer's disease.
Topics: Acetylcholinesterase; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhi | 2023 |
Tacrine First-Phase Biotransformation and Associated Hepatotoxicity: A Possible Way to Avoid Quinone Methide Formation.
Topics: Animals; Biotransformation; Chemical and Drug Induced Liver Injury; Humans; Indolequinones; Methamph | 2023 |
Gut microbiota and drug-induced liver injury: an update.
Topics: Animals; Chemical and Drug Induced Liver Injury; Gastrointestinal Microbiome; Humans; Liver; Tacrine | 2020 |
Combined Therapy for Alzheimer's Disease: Tacrine and PAMAM Dendrimers Co-Administration Reduces the Side Effects of the Drug without Modifying its Activity.
Topics: Alzheimer Disease; Animals; Cell Line; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibi | 2020 |
The liver-gut microbiota axis modulates hepatotoxicity of tacrine in the rat.
Topics: Animals; Biopsy, Needle; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Dose-Respon | 2018 |
A new phenyl glycoside from the aerial parts of Equisetum hyemale.
Topics: Antineoplastic Agents, Phytogenic; Chemical and Drug Induced Liver Injury; Drug Screening Assays, An | 2014 |
Tacrine, an oral acetylcholinesterase inhibitor, induced hepatic oxidative damage, which was blocked by liquiritigenin through GSK3-beta inhibition.
Topics: Alanine Transaminase; Animals; Aspartate Aminotransferases; Cell Line; Cell Survival; Chemical and D | 2015 |
Protective effect of fucosterol isolated from the edible brown algae, Ecklonia stolonifera and Eisenia bicyclis, on tert-butyl hydroperoxide- and tacrine-induced HepG2 cell injury.
Topics: Animals; Cell Survival; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Dose-Respons | 2015 |
Tribuli fructus constituents protect against tacrine-induced cytotoxicity in HepG2 cells.
Topics: Carbohydrate Sequence; Cell Line; Chemical and Drug Induced Liver Injury; Fruit; Guaiacol; Imides; M | 2010 |
Tacrine-NO donor and tacrine-ferulic acid hybrid molecules as new anti-Alzheimer agents: hepatotoxicity and influence on the cytochrome P450 system in comparison to tacrine.
Topics: Alzheimer Disease; Animals; Chemical and Drug Induced Liver Injury; Coumaric Acids; Cytochrome P-450 | 2010 |
Tacrine is implicated in oxidative stress in the laboratory guinea pig model.
Topics: Alzheimer Disease; Animals; Antioxidants; Brain; Caspase 3; Chemical and Drug Induced Liver Injury; | 2012 |
[Effect of dimethyl diphenyl bicarboxylate (DDB) on 9-amino-1,2,3,4-tetrahydroacridine-induced hepatotoxicity in mice].
Topics: Animals; Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A1; Dioxoles; Disease Models, | 2001 |
Five-year outcome of cholinergic treatment of Alzheimer's disease: early response predicts prolonged time until nursing home placement, but does not alter life expectancy.
Topics: Aged; Aged, 80 and over; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase I | 2004 |
Phenolic constituents of galla Rhois with hepatoprotective effects on tacrine- and nitrofurantoin-induced cytotoxicity in Hep G2 cells.
Topics: Cell Line, Tumor; Cell Survival; Chemical and Drug Induced Liver Injury; Drugs, Chinese Herbal; Huma | 2005 |
Hepatoprotective compounds of the roots of Cudrania tricuspidata on tacrine-induced cytotoxicity in Hep G2 cells.
Topics: Cell Line, Tumor; Chemical and Drug Induced Liver Injury; Humans; Magnetic Resonance Spectroscopy; M | 2006 |
Re-evaluation of tacrine hepatotoxicity using gel entrapped hepatocytes.
Topics: Albumins; Animals; Antidepressive Agents, Second-Generation; Cell Survival; Cells, Cultured; Chemica | 2007 |
Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity.
Topics: Alanine Transaminase; Alzheimer Disease; Animals; Chemical and Drug Induced Liver Injury; Gene Expre | 2007 |
Hepatoprotective effect of Cirsium arisanense Kitamura in tacrine-treated hepatoma Hep 3B cells and C57BL mice.
Topics: Animals; Antioxidants; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Survival; Chemical and Drug | 2008 |
Alzheimer's disease: how to give and monitor tacrine therapy.
Topics: Activities of Daily Living; Aged; Aged, 80 and over; Alanine Transaminase; Alzheimer Disease; Chemic | 1995 |
An evaluation of the efficacy and safety of tetrahydroaminoacridine (THA) without lecithin in the treatment of Alzheimer's disease.
Topics: Activities of Daily Living; Aged; Aged, 80 and over; Alzheimer Disease; Chemical and Drug Induced Li | 1993 |
Cytotoxicity of tacrine and velnacrine metabolites in cultured rat, dog and human hepatocytes.
Topics: Alanine Transaminase; Animals; Aspartate Aminotransferases; Carcinoma, Hepatocellular; Cells, Cultur | 1993 |
Influence of fluvoxamine on tacrine metabolism in vitro: potential implication for the hepatotoxicity in vivo.
Topics: Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A1; Cytochrome P-450 CYP1A2 Inhibitors; | 1996 |
Uncoupling of rat and human mitochondria: a possible explanation for tacrine-induced liver dysfunction.
Topics: Animals; Cells, Cultured; Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A2 Inhibitors | 1996 |
Glutathione S-transferase theta genetic polymorphism might influence tacrine hepatotoxicity in Alzheimer's patients.
Topics: Aged; Alanine Transaminase; Alzheimer Disease; Chemical and Drug Induced Liver Injury; Genotype; Glu | 1997 |
No association between tacrine transaminitis and the glutathione transferase theta genotype in patients with Alzheimer's disease.
Topics: Alzheimer Disease; Chemical and Drug Induced Liver Injury; Cholinesterase Inhibitors; DNA Primers; G | 1998 |
Heterogeneity of adverse hepatic reactions to tetrahydroaminoacridine.
Topics: Aged; Alzheimer Disease; Aminoacridines; Chemical and Drug Induced Liver Injury; Female; Humans; Liv | 1990 |
Acute hepatitis after tetrahydroaminoacridine administration for Alzheimer's disease.
Topics: Acute Disease; Aged; Alzheimer Disease; Aminoacridines; Chemical and Drug Induced Liver Injury; Fema | 1990 |
Hepatotoxicity of tetrahydroaminoacridine.
Topics: Alzheimer Disease; Aminoacridines; Chemical and Drug Induced Liver Injury; Female; Humans; Middle Ag | 1988 |