verapamil has been researched along with ketoconazole in 96 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 2 (2.08) | 18.7374 |
| 1990's | 12 (12.50) | 18.2507 |
| 2000's | 28 (29.17) | 29.6817 |
| 2010's | 46 (47.92) | 24.3611 |
| 2020's | 8 (8.33) | 2.80 |
| Authors | Studies |
|---|---|
| Cvetkovic, M; Fromm, MF; Kim, RB; Leake, B; Wilkinson, GR | 1 |
| Choo, EF; Imamura, H; Kim, RB; Leake, B; Wandel, C; Wilkinson, GR; Wood, AJ | 1 |
| Desir, GV; Lang, R; Lee, G; Liu, W; Orias, M; Rafi, H; Segal, AS; Tian, S | 1 |
| Huang, L; Humphreys, JE; Morgan, JB; Polli, JW; Serabjit-Singh, CS; Webster, LO; Wring, SA | 1 |
| Casciano, CN; Clement, RP; Johnson, WW; Wang, EJ | 2 |
| Alvarez-Pedraglio, A; Colmenarejo, G; Lavandera, JL | 1 |
| Pajeva, IK; Wiese, M | 1 |
| Fischer, H; Huwyler, J; Poli, S; Schwab, D; Tabatabaei, A | 1 |
| Keserü, GM | 1 |
| Bacsó, Z; Cianfriglia, M; Fenyvesi, F; Goda, K; Kappelmayer, J; Lustyik, G; Nagy, H; Szabó, G; Szilasi, M | 1 |
| Nagashima, R; Nishikawa, T; Tobita, M | 1 |
| Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL | 1 |
| Jia, L; Sun, H | 1 |
| Artursson, P; Bergström, CA; Hoogstraate, J; Matsson, P; Norinder, U; Pedersen, JM | 1 |
| Ahlin, G; Artursson, P; Bergström, CA; Gustavsson, L; Karlsson, J; Larsson, R; Matsson, P; Norinder, U; Pedersen, JM | 1 |
| Pratim Roy, P; Roy, K | 1 |
| Choi, Y; Jin, Y; Jung, HY; Kaur, N; Kim, DK; Kim, EK; Kim, ES; Lee, K; Min, KH; Min, YK; Park, MK; Xia, Y | 1 |
| Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A | 1 |
| García-Mera, X; González-Díaz, H; Prado-Prado, FJ | 1 |
| Ghosh, I; Manoharlal, R; Prakash, O; Prasad, R; Puri, N; Sharma, M | 1 |
| Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ | 1 |
| Chen, X; Lin, X; Skolnik, S; Wang, J | 1 |
| Sen, S; Sinha, N | 1 |
| Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V | 1 |
| Freiwald, S; Jiang, Y; Jones, JP; Kaspera, R; Katayama, J; Lee, CA; Smith, E; Totah, RA; Walker, GS | 1 |
| Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR | 1 |
| Cantin, LD; Chen, H; Kenna, JG; Noeske, T; Stahl, S; Walker, CL; Warner, DJ | 1 |
| Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ | 1 |
| Artursson, P; Mateus, A; Matsson, P | 1 |
| Andréola, ML; Bailly, F; Calmels, C; Christ, F; Cotelle, P; Debyser, Z; Lion, C; Suchaud, V | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Budriesi, R; Carosati, E; Chiarini, A; Chiu, FC; Cosimelli, B; Frosini, M; Fusi, F; Ioan, P; Katneni, K; Matucci, R; Micucci, M; Saponara, S; Severi, E; Spinelli, D | 1 |
| Andréola, ML; Bailly, F; Billamboz, M; Christ, F; Cotelle, P; Debyser, Z; Lion, C; Suchaud, V | 1 |
| Antonov, L; Gastreich, M; Hristova, S; Neumann, B; Stammler, HG; Tzvetkov, NT | 1 |
| Cui, J; Dai, Y; Huang, W; Li, Z; Pan, M; Qian, H; Qiu, Q; Shi, W; Zhang, B | 1 |
| Cui, J; Deng, X; Huang, W; Li, J; Li, Z; Liao, C; Liu, B; Pan, M; Qian, H; Qiang, H; Qiu, Q; Shi, W; Zhang, B | 1 |
| Abel, B; Ambudkar, SV; Barbuti, AM; Chen, ZS; Patel, BA; Talele, TT; Velagapudi, UK | 1 |
| Akaike, M; Hirai, M; Kumai, T; Masubuchi, Y; Tanaka, M; Watanabe, M | 1 |
| Agarwal, KC; Tzanakakis, GN; Veronikis, DK; Vezeridis, MP | 1 |
| Baciewicz, AM; Bekemeyer, WB; Self, TH | 1 |
| Kolts, BE; Langfitt, M | 1 |
| Gustafsson, JA; Hamberg, M; Mode, A; Tollet, P | 1 |
| Bader, A; Christians, U; Gonschior, AK; Hackbarth, I; Lampen, A; Sewing, KF; von Engelhardt, W | 1 |
| Iga, T; Ishizuka, H; Kawahara, Y; Matsuo, H; Miyama, T; Naito, M; Sawada, Y; Takanaga, H; Tsuruo, T; Yamamoto, K; Yamano, K | 1 |
| Fukuda, T; Hasegawa, R; Murakami, T; Nagai, J; Takano, M; Yumoto, R | 1 |
| Artursson, P; Hidalgo, IJ; Raeissi, SD; Segura-Aguilar, J | 1 |
| Jansson, B; Knutson, L; Knutson, TW; Lennernäs, H; Sandström, R | 1 |
| Aguilar, AJ; Grace, JM; Skanchy, DJ | 1 |
| Back, DJ; Eagling, VA; Profit, L | 1 |
| Crego, AL; Gómez, J; Lavandera, JL; Marina, ML | 1 |
| Achira, M; Ito, K; Sugiyama, Y; Suzuki, H | 1 |
| Auchère, D; Bonhomme-Faivre, L; Farinotti, R; Forestier, F; Orbach-Arbouys, S; Soursac, M | 1 |
| Charman, WN; Johnson, BM; Porter, CJ | 1 |
| Kohno, Y; Suzuki, A; Yamamoto, T | 1 |
| Al-Shurbaji, A; Annas, A; Artursson, P; Lazorova, L; Svensson, JO; Yasar, U | 1 |
| Chang, JH; Kochansky, CJ; Shou, M | 1 |
| Obruśnik, A; Pekala, E; Szymura-Oleksiak, J; Wyska, E | 1 |
| Griffin, BT; O'Driscoll, CM | 1 |
| Boulenc, X; Hachad, H; Levy, RH; Ragueneau-Majlessi, I; Rauch, C | 1 |
| Hellum, BH; Nilsen, OG | 1 |
| Bondesson, U; Dickinson, P; Hedeland, M; Knutson, L; Lennernäs, H; Thörn, HA; Yasin, M | 1 |
| Georg Nilsen, O; Hellum, BH; Hoybakk, K; Rohloff, J; Thomsen, M; Tosse, A | 1 |
| Borchardt, RT; Jin, JY; Mudra, DR | 1 |
| Blasco, H; Bouzom, F; Cazade, F; Chenel, M; Perdaems, N; Vinson, C; Whalley, S | 1 |
| Annaert, P; Augustijns, P; Brouwers, J; Mols, R | 1 |
| Al-Bataineh, MM; Gehring, R; Schultz, BD; van der Merwe, D | 1 |
| Dickinson, PA; Lennernäs, H; Lundahl, A; Schrickx, JA; Thörn, HA | 1 |
| Cao, LH; Guo, M; Jiang, SX; Liu, N; Mo, F; Sun, YH; Yuan, Z | 1 |
| Dong, X; Meng, Q; Yin, J | 1 |
| Basu, A; Brito, JP; Singh, E | 1 |
| He, L; Ke, X; Tian, JL; Zhang, XY | 1 |
| Dickinson, PA; Lennernäs, H; Sjögren, E; Thörn, HA | 1 |
| Bellavance, E; Bourg, S; Duan, J; Garneau, M; Ribadeneira, MD; Rioux, N | 1 |
| Huang, J; Li, G; Si, L; Xue, K; Zhao, G | 1 |
| Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M | 1 |
| Abay, E; Calitz, C; Gouws, C; Hamman, J; Steenekamp, J; Viljoen, J; Wiesner, L | 1 |
| Baluom, M; Brealey, C; Craven, K; Gillen, M; Grossbard, EB; Lau, D; Mant, T; Martin, P; Millson, D; Oliver, S; Sweeny, D | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; Siissalo, S; van Dam, A | 1 |
| Aunes, M; Cullberg, M; Edvardsson, N; Frison, L; Johansson, S; Löfberg, B; Lunde, H | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; van de Steeg, E | 1 |
| Marathe, P; Rodrigues, AD; Shen, H; Sinz, M; Yao, M; Zhu, M | 1 |
| Chan, ECY; Cheong, EJY; Chua, DXY; Teo, DWX | 1 |
| Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK | 1 |
| Bloomer, WD; Papadopoulou, MV; Rosenzweig, HS | 1 |
| Chen, ZS; Gupta, P; Lei, ZN; Li, YN; Li, ZH; Liu, HM; Liu, Y; Ma, LY; Wang, B; Wang, JQ; Zhang, XH; Zhao, B; Zhao, YD | 1 |
| Cini, E; De Santis, R; Giannini, G; Manera, F; Manetti, F; Milazzo, FM; Pace, S; Petricci, E; Stasi, MA; Tallarico, C; Vesci, L | 1 |
| Hagenow, S; Karcz, T; Kieć-Kononowicz, K; Kotańska, M; Kuder, KJ; Latacz, G; Lubelska, A; Mogilski, S; Siwek, A; Sobolewski, M; Stark, H; Szczepańska, K | 1 |
| Dubrovskyi, O; Dye, K; Gutgesell, LM; Huang, F; Li, Y; Ratia, K; Shen, Z; Thatcher, GRJ; Tonetti, DA; Xiong, R; Zhao, H; Zhao, J | 1 |
| Guo, HF; Jin, J; Li, ZR; Liu, ZY; Xie, ZS; Xue, ST; Yi, H; Zhang, L | 1 |
| Balliano, TL; Barbosa, G; Carvalho, VF; da Silva, BA; de Souza, ET; Lima, LM; Martins, IRR; Martins, MA; Medeiros, MM; Moraes Junior, MO; Nunes, IKDC; Silva, PMR; Silva, SWD | 1 |
| Cho, HY; Jeon, YH; Jung, K; Kim, HS; Kim, K; Kim, S; Kwon, NH; Lee, JY; Lee, S; Seo, B; Suh, YG | 1 |
| Chen, SH; Duan, YC; Guan, YY; He, ZH; Jin, LF; Liu, YJ; Ren, HM; Song, Y; Xu, YT; Yuan, H; Zhang, SJ | 1 |
| Cho, Y; Choo, H; Jeon, B; Keum, G; Kim, D; Kim, HJ; Kim, J; Kwag, R; Lee, H; Lee, J; Woo, J; Yeom, M | 1 |
| Bandopadhyay, P; Das, N; Dastidar, UG; Ganguly, D; Pal, S; Rahaman, O; Roy, S; Sinha, BP; Talukdar, A | 1 |
1 review(s) available for verapamil and ketoconazole
| Article | Year |
|---|---|
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
4 trial(s) available for verapamil and ketoconazole
| Article | Year |
|---|---|
Involvement of P-glycoprotein and cytochrome P450 3A in the metabolism of florfenicol of rabbits.
Topics: Animals; Anti-Bacterial Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Fluvoxamine; Ketoconazole; Rabbits; Thiamphenicol; Verapamil | 2012 |
Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin.
Topics: Adolescent; Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1; Calcineurin Inhibitors; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Digoxin; Drug Interactions; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Verapamil | 2014 |
Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies.
Topics: Adult; Aminopyridines; Cross-Over Studies; Cytochrome P-450 CYP3A Inducers; Cytochrome P-450 CYP3A Inhibitors; Double-Blind Method; Drug Interactions; Humans; Ketoconazole; Male; Microsomes, Liver; Morpholines; Oxazines; Pyridines; Pyrimidines; Rifampin; Verapamil; Young Adult | 2016 |
In Silico Predictions and In Vivo Results of Drug-Drug Interactions by Ketoconazole and Verapamil on AZD1305, a Combined Ion Channel Blocker and a Sensitive CYP3A4 Substrate.
Topics: Adult; Anti-Arrhythmia Agents; Area Under Curve; Azabicyclo Compounds; Carbamates; Computer Simulation; Cross-Over Studies; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Male; Middle Aged; Verapamil; Young Adult | 2016 |
91 other study(ies) available for verapamil and ketoconazole
| Article | Year |
|---|---|
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
Topics: Animals; Anion Transport Proteins; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport, Active; Caco-2 Cells; Carrier Proteins; Genes, MDR; HeLa Cells; Histamine H1 Antagonists; Humans; LLC-PK1 Cells; Mice; Rats; Swine; Terfenadine; Tissue Distribution; Transfection; Vaccinia virus | 1999 |
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Brain; Caco-2 Cells; Dibenzocycloheptenes; HIV Protease Inhibitors; Humans; Inhibitory Concentration 50; Male; Mice; Quinolines; Testis | 2000 |
KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Topics: Animals; Base Sequence; Cyclic Nucleotide-Gated Cation Channels; DNA Primers; Female; Humans; In Vitro Techniques; Ion Channel Gating; Ion Channels; Membrane Potentials; Oocytes; Patch-Clamp Techniques; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Rabbits; Recombinant Proteins; Second Messenger Systems; Shaker Superfamily of Potassium Channels; Xenopus laevis | 2000 |
Rational use of in vitro P-glycoprotein assays in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cells, Cultured; Chromatography, Liquid; Enzyme Inhibitors; Fluoresceins; Fluorescent Dyes; Humans; Mass Spectrometry; Pharmacology; Spodoptera | 2001 |
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Topics: 3T3 Cells; Adrenergic Uptake Inhibitors; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding Sites; Biological Transport, Active; Cell Line; Cell Separation; Cell Survival; Flow Cytometry; Fluorescent Dyes; Humans; Inhibitory Concentration 50; Mice; Protein Binding; Reserpine; Spectrometry, Fluorescence; Substrate Specificity; Time Factors | 2001 |
Cheminformatic models to predict binding affinities to human serum albumin.
Topics: Adrenergic beta-Antagonists; Antidepressive Agents, Tricyclic; Chromatography, Affinity; Cyclooxygenase Inhibitors; Databases, Factual; Humans; Hydrophobic and Hydrophilic Interactions; Penicillins; Pharmaceutical Preparations; Protein Binding; Quantitative Structure-Activity Relationship; Reproducibility of Results; Serum Albumin; Steroids | 2001 |
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
Topics: Adenosine Triphosphatases; Algorithms; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding Sites; Binding, Competitive; Caco-2 Cells; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Fluoresceins; Humans; Ligands; Models, Molecular; Molecular Structure; Quantitative Structure-Activity Relationship; Radioligand Assay; Rhodamine 123; Stereoisomerism; Verapamil; Vinblastine | 2002 |
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Cells, Cultured; Drug Evaluation, Preclinical; Fluoresceins; Fluorescent Dyes; Humans; Indicators and Reagents; Mice; Models, Molecular; Rhodamines; Species Specificity; Swine | 2003 |
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Binding Sites; Biological Transport, Active; Biomarkers; Cells, Cultured; Drug Interactions; Fluorescent Dyes; Humans | 2003 |
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
Topics: Cation Transport Proteins; Databases, Factual; Discriminant Analysis; Ether-A-Go-Go Potassium Channels; Holography; Linear Models; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Quantitative Structure-Activity Relationship | 2003 |
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
Topics: Adenosine Triphosphatases; Animals; Anti-Bacterial Agents; Antibodies, Monoclonal; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding, Competitive; Calcium Channel Blockers; Cyclosporine; Detergents; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Flow Cytometry; Fluoresceins; Humans; Ivermectin; Mice; NIH 3T3 Cells; Substrate Specificity | 2004 |
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
Topics: Animals; CHO Cells; Cricetinae; Discriminant Analysis; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Potassium Channel Blockers; Potassium Channels, Voltage-Gated | 2005 |
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Topics: Adverse Drug Reaction Reporting Systems; Artificial Intelligence; Computers; Databases, Factual; Drug Prescriptions; Drug-Related Side Effects and Adverse Reactions; Endpoint Determination; Models, Molecular; Quantitative Structure-Activity Relationship; Software; United States; United States Food and Drug Administration | 2004 |
Support vector machines classification of hERG liabilities based on atom types.
Topics: Animals; Arrhythmias, Cardiac; CHO Cells; Computer Simulation; Cricetinae; Cricetulus; Discriminant Analysis; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Models, Chemical; Patch-Clamp Techniques; Potassium Channel Blockers; Potassium Channels, Voltage-Gated; Predictive Value of Tests; ROC Curve | 2008 |
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
Topics: Administration, Oral; Animals; Antineoplastic Agents; Antipsychotic Agents; Antiviral Agents; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Cell Line; Computer Simulation; Cytochrome P-450 Enzyme System; Drug-Related Side Effects and Adverse Reactions; Estradiol; Humans; Insecta; Liver; Models, Molecular; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Neoplasm Proteins; Pharmaceutical Preparations; Pharmacology; Structure-Activity Relationship | 2008 |
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
Topics: Cell Line; Computer Simulation; Drug Design; Gene Expression Profiling; Humans; Hydrogen Bonding; Liver; Molecular Weight; Organic Cation Transporter 1; Pharmaceutical Preparations; Predictive Value of Tests; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Structure-Activity Relationship | 2008 |
Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
Topics: Algorithms; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Enzyme Inhibitors; Factor Analysis, Statistical; Least-Squares Analysis; Linear Models; Models, Molecular; Neural Networks, Computer; Quantitative Structure-Activity Relationship; Reproducibility of Results | 2009 |
A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.
Topics: Adamantane; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cell Line, Tumor; Cytochrome P-450 CYP3A; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; Sarcoma; Structure-Activity Relationship | 2009 |
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship | 2010 |
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
Topics: Antiparasitic Agents; Molecular Structure; Neural Networks, Computer; Parasitic Diseases; Quantitative Structure-Activity Relationship; Species Specificity; Thermodynamics | 2010 |
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
Topics: Candida albicans; Membrane Transport Proteins; Saccharomyces cerevisiae; Structure-Activity Relationship; Substrate Specificity | 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; Biological Assay; Biological Transport; Cell Line; Cell Membrane; Chemical and Drug Induced Liver Injury; Cytoplasmic Vesicles; Drug Evaluation, Preclinical; Humans; Liver; Rats; Reproducibility of Results; Spodoptera; Transfection; Xenobiotics | 2010 |
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
Topics: Adenosine; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Sub-Family B Member 4; ATP-Binding Cassette Transporters; Biological Transport; Caco-2 Cells; Chromatography, Liquid; Dibenzocycloheptenes; Diketopiperazines; Drug Discovery; Heterocyclic Compounds, 4 or More Rings; Humans; Intestinal Absorption; Mass Spectrometry; Models, Biological; Neoplasm Proteins; Pharmaceutical Preparations; Predictive Value of Tests; Propionates; Quinolines; Substrate Specificity | 2011 |
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
Topics: Computer Simulation; Ether-A-Go-Go Potassium Channels; Humans; Molecular Structure; Organic Chemicals; Quantitative Structure-Activity Relationship | 2011 |
FDA-approved drug labeling for the study of drug-induced liver injury.
Topics: Animals; Benchmarking; Biomarkers, Pharmacological; Chemical and Drug Induced Liver Injury; Drug Design; Drug Labeling; Drug-Related Side Effects and Adverse Reactions; Humans; Pharmaceutical Preparations; Reproducibility of Results; United States; United States Food and Drug Administration | 2011 |
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
Topics: Amiodarone; Astemizole; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP2J2; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Danazol; Drug Discovery; Drug Interactions; Enzyme Inhibitors; Humans; Hydroxylation; In Vitro Techniques; Methylation; Microsomes, Liver; Models, Biological; Molecular Structure; Substrate Specificity; Tandem Mass Spectrometry; Terfenadine | 2012 |
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Topics: Atorvastatin; Biological Transport; Drug Interactions; Estradiol; Estrone; HEK293 Cells; Heptanoic Acids; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; In Vitro Techniques; Least-Squares Analysis; Liver; Liver-Specific Organic Anion Transporter 1; Models, Molecular; Multivariate Analysis; Organic Anion Transporters; Organic Anion Transporters, Sodium-Independent; Protein Isoforms; Pyrroles; Solute Carrier Organic Anion Transporter Family Member 1B3; Structure-Activity Relationship; Transfection | 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; Bile Acids and Salts; Cell Line; Chemical and Drug Induced Liver Injury; Humans; Quantitative Structure-Activity Relationship | 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 B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests | 2013 |
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
Topics: Animals; Brain; Dialysis; HEK293 Cells; High-Throughput Screening Assays; Humans; Pharmaceutical Preparations; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization | 2014 |
Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.
Topics: Aryl Hydrocarbon Hydroxylases; Cell Line, Tumor; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Resistance, Viral; HIV Integrase Inhibitors; HIV-1; Humans; Isoquinolines; Molecular Docking Simulation; Mutation; Structure-Activity Relationship | 2014 |
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
Topics: Animals; Cells, Cultured; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Guinea Pigs; Heart Atria; Humans; Male; Microsomes, Liver; Myocytes, Cardiac; Oxadiazoles; Oxidation-Reduction; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiazines; Vasodilator Agents | 2016 |
2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
Topics: Alkylation; Anti-HIV Agents; Cell Line; Drug Resistance, Viral; HIV Integrase Inhibitors; Humans; Isoquinolines; Structure-Activity Relationship | 2016 |
Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors.
Topics: Animals; Blood-Brain Barrier; Brain; Crystallography, X-Ray; Gastrointestinal Tract; Humans; Indazoles; Kinetics; Molecular Docking Simulation; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Permeability; Protein Binding; Protein Conformation; Rats; Solubility; Species Specificity; Structure-Activity Relationship; Water | 2017 |
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
Topics: Antibiotics, Antineoplastic; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cytochrome P-450 CYP3A; Doxorubicin; Drug Discovery; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; K562 Cells; Neoplasms; Niacinamide | 2017 |
Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance.
Topics: Adenosine Triphosphatases; Animals; Antibiotics, Antineoplastic; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Doxorubicin; Drug Resistance, Multiple; Humans; K562 Cells; Male; Quinazolines; Rats; Rats, Sprague-Dawley; Rhodamine 123; Spectrum Analysis | 2017 |
Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.
Topics: Adenosine Triphosphatases; Amino Acids; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding Sites; Chemistry Techniques, Synthetic; Humans; Molecular Docking Simulation; Peptidomimetics; Protein Conformation; Structure-Activity Relationship; Thiazoles | 2018 |
Disturbance or relatively important actions of antihypertensives, antifungal agent and opiate antagonist to the testicular steroidogenesis in rat.
Topics: Androstenedione; Animals; Antifungal Agents; Antihypertensive Agents; Clonidine; Estradiol; Ketoconazole; Male; Naloxone; Narcotic Antagonists; Prazosin; Rats; Testis; Testosterone; Verapamil | 1992 |
Effects of antiplatelet agents alone or in combinations on platelet aggregation and on liver metastases from a human pancreatic adenocarcinoma in the nude mouse.
Topics: Adenocarcinoma; Animals; Colforsin; Drug Interactions; Humans; Indomethacin; Ketoconazole; Liver Neoplasms; Mice; Mice, Nude; Neoplasm Transplantation; Pancreatic Neoplasms; Platelet Aggregation; Platelet Aggregation Inhibitors; Tumor Cells, Cultured; Verapamil | 1991 |
Update on rifampin drug interactions.
Topics: Adrenergic beta-Antagonists; Cyclosporins; Digoxin; Drug Interactions; Humans; Ketoconazole; Phenytoin; Rifampin; Theophylline; Verapamil | 1987 |
Drugs and the liver.
Topics: Acetaminophen; Adult; Aspirin; Chemical and Drug Induced Liver Injury; Chemical and Drug Induced Liver Injury, Chronic; Cholestasis; Cimetidine; Fatty Liver; Female; Hepatic Artery; Hepatic Veins; Humans; Ketoconazole; Liver; Liver Diseases; Liver Neoplasms; Methyldopa; Necrosis; Nitrofurantoin; Peliosis Hepatis; Portal Vein; Valproic Acid; Verapamil | 1984 |
Growth hormone signaling leading to CYP2C12 gene expression in rat hepatocytes involves phospholipase A2.
Topics: 5,8,11,14-Eicosatetraynoic Acid; Animals; Arachidonic Acid; Aryl Hydrocarbon Hydroxylases; Benzoquinones; Calcimycin; Calcium-Calmodulin-Dependent Protein Kinases; Cytochrome P-450 Enzyme System; Diglycerides; Enzyme Activation; Gene Expression Regulation; Growth Hormone; Insulin-Like Growth Factor I; Ketoconazole; Lactams, Macrocyclic; Liver; Phospholipases A; Phospholipases A2; Phospholipids; Phosphorylation; Proadifen; Protein-Tyrosine Kinases; Quinacrine; Quinones; Rats; Rats, Sprague-Dawley; Rifabutin; RNA, Messenger; Signal Transduction; Steroid Hydroxylases; Verapamil | 1995 |
Metabolism of the macrolide immunosuppressant, tacrolimus, by the pig gut mucosa in the Ussing chamber.
Topics: Animals; Anti-Bacterial Agents; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Gastric Mucosa; Immunosuppressive Agents; Ketoconazole; Oxidoreductases, N-Demethylating; Swine; Tacrolimus; Troleandomycin; Vasodilator Agents; Verapamil | 1996 |
P-glycoprotein-mediated transport of itraconazole across the blood-brain barrier.
Topics: Animals; Antifungal Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Behavior, Animal; Biological Transport; Blood-Brain Barrier; Brain; Drug Interactions; Injections, Intravenous; Itraconazole; Ketoconazole; Male; Mice; Mice, Knockout; Rats; Rats, Sprague-Dawley; Tissue Distribution; Verapamil; Vinblastine; Vincristine | 1998 |
Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells.
Topics: Anti-Bacterial Agents; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B; Biological Transport; Caco-2 Cells; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Erythromycin; GABA Modulators; Humans; Ketoconazole; Midazolam; Oxidoreductases, N-Demethylating; Rhodamine 123; Substrate Specificity; Vasodilator Agents; Verapamil | 1998 |
Interplay between CYP3A-mediated metabolism and polarized efflux of terfenadine and its metabolites in intestinal epithelial Caco-2 (TC7) cell monolayers.
Topics: Anti-Anxiety Agents; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Caco-2 Cells; Calcium Channel Blockers; Catalytic Domain; Cell Polarity; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Digoxin; Enzyme Inhibitors; Epithelial Cells; Gene Expression; Histamine H1 Antagonists; Humans; Hydroxylation; Intestinal Mucosa; Intestines; Ketoconazole; Kinetics; Oligonucleotide Probes; Oxidoreductases, N-Demethylating; Piperidines; RNA, Messenger; Terfenadine; Tritium; Verapamil | 1999 |
The effect of ketoconazole on the jejunal permeability and CYP3A metabolism of (R/S)-verapamil in humans.
Topics: Adult; Algorithms; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Calcium Channel Blockers; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Female; Humans; Infusions, Intravenous; Intestinal Absorption; Jejunum; Ketoconazole; Male; Oxidoreductases, N-Demethylating; Perfusion; Stereoisomerism; Verapamil | 1999 |
Metabolism of artelinic acid to dihydroqinqhaosu by human liver cytochrome P4503A.
Topics: Adult; Aged; Antifungal Agents; Antimalarials; Artemisinins; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Combinations; Drug Interactions; Drugs, Chinese Herbal; Enzyme Inhibitors; Female; Glycyrrhiza; Humans; Inactivation, Metabolic; Inhibitory Concentration 50; Isoenzymes; Ketoconazole; Liver; Male; Miconazole; Microsomes, Liver; Middle Aged; Oxidoreductases, N-Demethylating; Paeonia; Quinidine; Recombinant Proteins; Sesquiterpenes; Sulfaphenazole; Troleandomycin; Vasodilator Agents; Verapamil | 1999 |
Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Beverages; Caco-2 Cells; Citrus; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Gas Chromatography-Mass Spectrometry; HIV Protease Inhibitors; Humans; In Vitro Techniques; Ketoconazole; Liver; Mixed Function Oxygenases; Plant Extracts; Saquinavir; Time Factors; Verapamil | 1999 |
Application of capillary zone electrophoresis with off-line solid-phase extraction to in vitro metabolism studies of antifungals.
Topics: Acetic Acid; Acetonitriles; Antifungal Agents; Clotrimazole; Drug Stability; Electrophoresis, Capillary; Fluconazole; Humans; Itraconazole; Ketoconazole; Methanol; Microsomes, Liver; Molecular Structure; Molecular Weight; Pyrimidines; Reproducibility of Results; Sensitivity and Specificity; Solvents; Triazoles; Verapamil; Voriconazole | 2001 |
Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Cyclosporins; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Humans; Indans; Intestine, Small; Ketoconazole; Liver; Microsomes; Midazolam; Mixed Function Oxygenases; Piperazines; Verapamil; Vinblastine | 1999 |
Chronic administration of verapamil, ketoconazole and carbamazepine: impact on immunological parameters.
Topics: Animals; Anticonvulsants; Antifungal Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood Cell Count; Body Weight; Calcium Channel Blockers; Carbamazepine; Cytochrome P-450 Enzyme System; Immunity; Immunity, Cellular; Ketoconazole; Male; Mice; Monocytes; Verapamil | 2002 |
Application of compartmental modeling to an examination of in vitro intestinal permeability data: assessing the impact of tissue uptake, P-glycoprotein, and CYP3A.
Topics: Animals; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Cyclosporins; Cytochrome P-450 CYP3A; In Vitro Techniques; Intestinal Absorption; Jejunum; Ketoconazole; Male; Midazolam; Models, Biological; Oxidoreductases, N-Demethylating; Permeability; Rats; Rats, Sprague-Dawley; Time Factors; Verapamil | 2003 |
High-throughput screening for the assessment of time-dependent inhibitions of new drug candidates on recombinant CYP2D6 and CYP3A4 using a single concentration method.
Topics: Amiodarone; Animals; Baculoviridae; Binding, Competitive; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Diltiazem; Enzyme Inhibitors; Fluorescence; Humans; Inhibitory Concentration 50; Ketoconazole; Miconazole; Midazolam; Propafenone; Quinolines; Recombinant Proteins; Troleandomycin; Verapamil | 2004 |
Ketobemidone is a substrate for cytochrome P4502C9 and 3A4, but not for P-glycoprotein.
Topics: ATP Binding Cassette Transporter, Subfamily B; Biological Transport; Caco-2 Cells; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Humans; Isonipecotic Acids; Ketoconazole; Kinetics; Meperidine; Microsomes, Liver; Mutagenesis, Site-Directed; Phenols; Substrate Specificity; Sulfaphenazole; Troleandomycin; Verapamil | 2005 |
The role of P-glycoprotein in the bioactivation of raloxifene.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Biotransformation; Cells, Cultured; Cytochrome P-450 CYP3A Inhibitors; Enzyme Inhibitors; Fomepizole; Glutathione; Hepatocytes; Humans; Ketoconazole; Microsomes, Liver; Naphthalenes; Pyrazoles; Raloxifene Hydrochloride; Verapamil | 2006 |
Pharmacokinetic modelling of pentoxifylline and lisofylline after oral and intravenous administration in mice.
Topics: Adjuvants, Immunologic; Administration, Oral; Animals; Area Under Curve; Biological Transport; Hematologic Agents; Injections, Intravenous; Intestinal Absorption; Ketoconazole; Male; Mice; Models, Biological; Pentoxifylline; Verapamil | 2007 |
An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
Topics: Animals; Anti-HIV Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Availability; Biological Transport, Active; Cyclosporine; Cytochrome P-450 Enzyme System; Data Interpretation, Statistical; Intestinal Absorption; Ketoconazole; Lymphatic System; Male; Micelles; Rats; Rats, Wistar; Saquinavir; Triglycerides; Triolein; Verapamil | 2008 |
Quantitative correlations among CYP3A sensitive substrates and inhibitors: literature analysis.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Databases, Factual; Drug Interactions; Enzyme Inhibitors; Erythromycin; Fluconazole; Ketoconazole; Midazolam; Substrate Specificity; Verapamil | 2007 |
In vitro inhibition of CYP3A4 metabolism and P-glycoprotein-mediated transport by trade herbal products.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Digoxin; Herb-Drug Interactions; Humans; Ketoconazole; Plant Extracts; Plant Preparations; Testosterone; Verapamil | 2008 |
Different effects of ketoconazole on the stereoselective first-pass metabolism of R/S-verapamil in the intestine and the liver: important for the mechanistic understanding of first-pass drug-drug interactions.
Topics: Animals; Drug Interactions; Female; Intestinal Mucosa; Intestines; Jejunum; Ketoconazole; Liver; Male; Stereoisomerism; Swine; Verapamil | 2009 |
Potent in vitro inhibition of CYP3A4 and P-glycoprotein by Rhodiola rosea.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Baculoviridae; Caco-2 Cells; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Digoxin; DNA, Complementary; Herb-Drug Interactions; Humans; Inhibitory Concentration 50; Ketoconazole; Plant Extracts; Rhodiola; Structure-Activity Relationship; Testosterone; Verapamil | 2010 |
Absorption barriers in the rat intestinal mucosa: 2. Application of physiologically based mathematical models to quantify mechanisms of drug permeation and metabolism.
Topics: Acridines; Adrenergic beta-Antagonists; Algorithms; Animals; Atenolol; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biotransformation; Computer Simulation; Cyclosporins; Cytochrome P-450 CYP3A Inhibitors; Enzyme Inhibitors; Intestinal Absorption; Intestinal Mucosa; Ketoconazole; Models, Statistical; Pharmaceutical Preparations; Rats; Tetrahydroisoquinolines; Verapamil | 2010 |
Predictions of metabolic drug-drug interactions using physiologically based modelling: Two cytochrome P450 3A4 substrates coadministered with ketoconazole or verapamil.
Topics: Algorithms; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Metabolic Clearance Rate; Midazolam; Models, Biological; Monte Carlo Method; Verapamil | 2010 |
Validation of a differential in situ perfusion method with mesenteric blood sampling in rats for intestinal drug interaction profiling.
Topics: Adrenergic beta-Antagonists; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Carbamates; Drug Interactions; Furans; Intestinal Absorption; Ketoconazole; Male; Perfusion; Polyethylene Glycols; Rats; Rats, Wistar; Splanchnic Circulation; Sulfonamides; Verapamil; Vitamin E | 2010 |
Tumor necrosis factor alpha increases P-glycoprotein expression in a BME-UV in vitro model of mammary epithelial cells.
Topics: 14-alpha Demethylase Inhibitors; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP-Binding Cassette Transporters; Biological Transport; Calcium Channel Blockers; Cattle; Cell Line, Transformed; Cell Membrane Permeability; Cytokines; Digoxin; Enzyme Inhibitors; Epithelial Cells; Female; Inflammation; Ketoconazole; Mammary Glands, Animal; RNA, Messenger; Tumor Necrosis Factor-alpha; Verapamil | 2010 |
Drug metabolism of CYP3A4, CYP2C9 and CYP2D6 substrates in pigs and humans.
Topics: Animals; Aryl Hydrocarbon Hydroxylases; ATP-Binding Cassette Transporters; Biotransformation; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dextromethorphan; Diclofenac; Gene Expression; Glucuronosyltransferase; Humans; Jejunum; Ketoconazole; Liver; Male; Microsomes, Liver; RNA, Messenger; Species Specificity; Swine; Testosterone; Verapamil | 2011 |
Auto-inhibition of verapamil metabolism in rat hepatocytes of gel entrapment culture.
Topics: Animals; Cell Culture Techniques; Cells, Cultured; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Gels; Hepatocytes; Inactivation, Metabolic; Ketoconazole; Male; Rats; Rats, Sprague-Dawley; Verapamil | 2011 |
Iatrogenic heart block during treatment of a patient with Cushing's syndrome: report of a case.
Topics: Aged, 80 and over; Alkalosis; Antihypertensive Agents; Cushing Syndrome; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Enzyme Inhibitors; Female; Heart Block; Humans; Hypertension; Hypokalemia; Iatrogenic Disease; Ketoconazole; Treatment Outcome; Verapamil | 2012 |
[Transport of limonin in rat intestine in situ and Caco-2 cells in vitro].
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Availability; Biological Transport; Caco-2 Cells; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Humans; Intestinal Absorption; Ketoconazole; Limonins; Male; Perfusion; Probenecid; Rats; Verapamil | 2012 |
Binding processes determine the stereoselective intestinal and hepatic extraction of verapamil in vivo.
Topics: Administration, Oral; Animals; Antifungal Agents; Drug Combinations; Drug Interactions; Intestinal Mucosa; Intestines; Ketoconazole; Liver; Models, Biological; Protein Binding; Stereoisomerism; Swine; Tissue Distribution; Vasodilator Agents; Verapamil | 2012 |
Assessment of CYP3A-mediated drug-drug interaction potential for victim drugs using an in vivo rat model.
Topics: Animals; Buspirone; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Male; Microsomes, Liver; Rats; Rats, Wistar; Ritonavir; Verapamil | 2013 |
Enhanced intestinal absorption of etoposide by self-microemulsifying drug delivery systems: roles of P-glycoprotein and cytochrome P450 3A inhibition.
Topics: Animals; Antineoplastic Agents, Phytogenic; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Availability; Caco-2 Cells; Cell Survival; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Delivery Systems; Etoposide; Humans; Intestinal Absorption; Ketoconazole; Male; Rats; Rats, Sprague-Dawley; Verapamil | 2013 |
Rat precision-cut intestinal slices to study P-gp activity and the potency of its inhibitors ex vivo.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cyclosporine; Cyclosporins; In Vitro Techniques; Intestinal Mucosa; Isoquinolines; Ketoconazole; Male; Quinazolines; Quinidine; Rats, Wistar; Rhodamine 123; Verapamil | 2015 |
Herb-Drug Pharmacokinetic Interactions: Transport and Metabolism of Indinavir in the Presence of Selected Herbal Products.
Topics: Anti-HIV Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Caco-2 Cells; Cell Line, Tumor; Crotalid Venoms; Cytochrome P-450 CYP3A; Herb-Drug Interactions; Humans; Indinavir; Ketoconazole; Plant Extracts; Verapamil | 2015 |
The Consequence of Drug-Drug Interactions Influencing the Interplay between P-Glycoprotein and Cytochrome P450 3a: An Ex Vivo Study with Rat Precision-Cut Intestinal Slices.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cyclosporins; Cytochrome P-450 CYP3A; Drug Interactions; Ileum; Intestinal Absorption; Jejunum; Ketoconazole; Male; Pharmaceutical Preparations; Quinidine; Rats; Rats, Wistar; Valine; Verapamil | 2016 |
The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo.
Topics: Adult; Aged; Aged, 80 and over; ATP Binding Cassette Transporter, Subfamily B, Member 1; Colon; Cyclosporins; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Humans; Ileum; In Vitro Techniques; Isoquinolines; Jejunum; Ketoconazole; Male; Middle Aged; Quinazolines; Quinidine; Verapamil | 2017 |
Renal Excretion of Dabigatran: The Potential Role of Multidrug and Toxin Extrusion (MATE) Proteins.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport, Active; Dabigatran; Dogs; Drug Interactions; HEK293 Cells; Humans; Inhibitory Concentration 50; Ketoconazole; Madin Darby Canine Kidney Cells; Octamer Transcription Factor-1; Organic Anion Transporters, Sodium-Independent; Organic Cation Transport Proteins; Organic Cation Transporter 2; Quinidine; Renal Elimination; Transfection; Verapamil | 2019 |
Systematic Development and Verification of a Physiologically Based Pharmacokinetic Model of Rivaroxaban.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Atrial Fibrillation; Computer Simulation; Drug Interactions; Humans; Ketoconazole; Kidney; Models, Biological; Organic Anion Transporters, Sodium-Independent; Rivaroxaban; Verapamil | 2019 |
Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Topics: Administration, Oral; Adult; Aged; Alkynes; Aminopyridines; Area Under Curve; Benzimidazoles; Benzoxazines; Bosentan; Clarithromycin; Computer Simulation; Cyclin-Dependent Kinases; Cyclopropanes; Cytochrome P-450 CYP3A Inducers; Cytochrome P-450 CYP3A Inhibitors; Diltiazem; Drug Interactions; Female; Healthy Volunteers; Humans; Itraconazole; Ketoconazole; Male; Middle Aged; Modafinil; Models, Biological; Rifampin; Verapamil | 2020 |
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
Topics: Animals; Antitubercular Agents; Cell Line; Chlorocebus aethiops; Dose-Response Relationship, Drug; Humans; Imidazoles; Macrophages; Mice; Microbial Sensitivity Tests; Molecular Structure; Mycobacterium tuberculosis; Nitro Compounds; Structure-Activity Relationship; Triazoles | 2017 |
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance.
Topics: Administration, Oral; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Availability; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Design; Drug Resistance, Multiple; Gene Expression Regulation, Neoplastic; Humans; Intracellular Space; Models, Molecular; Molecular Docking Simulation; Protein Conformation; Protein Transport; Pyrimidines; Urea | 2018 |
Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.
Topics: Animals; Antineoplastic Agents; Cell Line; Cell Proliferation; Cell Survival; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Guanidine; Hedgehog Proteins; Humans; Mice; Mice, Nude; Molecular Structure; Neoplasms, Experimental; NIH 3T3 Cells; Structure-Activity Relationship; Thiourea | 2018 |
Optimization and preclinical evaluation of novel histamine H
Topics: Animals; Antineoplastic Agents; Body Weight; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Hep G2 Cells; Histamine H3 Antagonists; Humans; Ligands; Male; Mice; Models, Molecular; Molecular Structure; Piperazine; Rats; Receptors, Histamine H3; Structure-Activity Relationship | 2018 |
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Topics: Animals; Breast Neoplasms; Drug Resistance, Neoplasm; Fulvestrant; Humans; MCF-7 Cells; Mice; Models, Molecular; Piperazines; Protein Domains; Pyridines; Pyridones; Receptors, Estrogen; Tissue Distribution; Transcription Factors; Xenograft Model Antitumor Assays | 2020 |
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
Topics: Animals; Benzofurans; Bone Morphogenetic Protein 2; Caco-2 Cells; Disease Models, Animal; Dose-Response Relationship, Drug; Humans; Mice; Mice, Inbred BALB C; Molecular Structure; Osteoporosis; Ovariectomy; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiophenes; Zebrafish | 2020 |
Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
Topics: Animals; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Enzyme Inhibitors; Humans; Hydrazones; Hypersensitivity; Lung; Male; Mice | 2020 |
Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.
Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Movement; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Female; Humans; Lysine-tRNA Ligase; Mammary Neoplasms, Experimental; Mice; Mice, Inbred BALB C; Molecular Structure; Pyridines; Structure-Activity Relationship | 2021 |
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Histone Deacetylases; Histone Demethylases; Humans; Microsomes, Liver; Molecular Docking Simulation; Molecular Structure; Rats; Stomach Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured | 2021 |
Discovery of G Protein-Biased Antagonists against 5-HT
Topics: Animals; Autistic Disorder; Drug Design; Grooming; Male; Mice, Transgenic; Microfilament Proteins; Molecular Docking Simulation; Nerve Tissue Proteins; Pyrazoles; Receptors, Serotonin; Serotonin Antagonists | 2021 |
Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits.
Topics: Imidazoles; Ligands; Pyridines; Toll-Like Receptor 7; Toll-Like Receptor 9 | 2022 |