ketoconazole and saquinavir

ketoconazole has been researched along with saquinavir in 34 studies

Research

Studies (34)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's5 (14.71)18.2507
2000's17 (50.00)29.6817
2010's10 (29.41)24.3611
2020's2 (5.88)2.80

Authors

AuthorsStudies
Jones, LH; Nadanaciva, S; Rana, P; Will, Y1
Norman, BH1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Cvetkovic, M; Fromm, MF; Kim, RB; Leake, B; Wilkinson, GR1
Choo, EF; Imamura, H; Kim, RB; Leake, B; Wandel, C; Wilkinson, GR; Wood, AJ1
Huang, L; Humphreys, JE; Morgan, JB; Polli, JW; Serabjit-Singh, CS; Webster, LO; Wring, SA1
Fischer, H; Huwyler, J; Poli, S; Schwab, D; Tabatabaei, A1
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL1
Artursson, P; Bergström, CA; Hoogstraate, J; Matsson, P; Norinder, U; Pedersen, JM1
Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A1
Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ1
Chen, X; Lin, X; Skolnik, S; Wang, J1
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V1
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR1
Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ1
Artursson, P; Mateus, A; Matsson, P1
Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Collins, JM; Fitzsimmons, ME1
Jordan, WC1
Back, DJ; Eagling, VA; Profit, L1
Granda, BW; Greenblatt, DJ; Harmatz, JS; Shader, RI; von Moltke, LL; Zalma, A1
Blanco, MS; Collazos, J; Martinez, E; Mayo, J1
Cameron, DW; Gallicano, K; Khaliq, Y; Kravcik, S; Venance, S1
Bryson, H; Goggin, T; Grub, S; Jorga, K; Lüdin, E1
Back, DJ; Eagling, VA; Whitcombe, IW; Wiltshire, H1
Autar, RS; Burger, DM; Cooper, DA; Hassink, E; Hill, A; Kimenai, E; Lange, JM; Phanuphak, P; Ruxrungtham, K; Sankote, J; Sutthichom, D; Wit, FW1
Griffin, BT; O'Driscoll, CM1
Abel, S; Muirhead, GJ; Ridgway, CE; Russell, D; Taylor-Worth, RJ1
Collins, C; Dickins, M; Hyland, R; Jones, B; Jones, H1
Cheung, C; Gonzalez, FJ; Idle, JR; Krausz, KW; Ma, X; Shah, YM; Wang, T1
Bour, F; Kaeser, B; Schmitt, C; Zandt, H; Zhang, X; Zwanziger, E1
de Greef-van der Sandt, IC; Freidig, AP; Nijmeijer, S; Treijtel, N; van Eijkeren, JC1

Reviews

3 review(s) available for ketoconazole and saquinavir

ArticleYear
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
    Journal of medicinal chemistry, 2020, 10-22, Volume: 63, Issue:20

    Topics: Animals; Cell Line; Cell Survival; Chemical and Drug Induced Liver Injury; Drug Discovery; Drug Evaluation, Preclinical; Hepatocytes; Humans; Liver; Mitochondria, Liver; Pharmaceutical Preparations; Risk Assessment; Tissue Distribution

2020
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells

2022
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
    Drug discovery today, 2016, Volume: 21, Issue:4

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk

2016

Trials

5 trial(s) available for ketoconazole and saquinavir

ArticleYear
Effect of ketoconazole on ritonavir and saquinavir concentrations in plasma and cerebrospinal fluid from patients infected with human immunodeficiency virus.
    Clinical pharmacology and therapeutics, 2000, Volume: 68, Issue:6

    Topics: Adult; Antifungal Agents; Dose-Response Relationship, Drug; Drug Interactions; Female; HIV Infections; HIV Protease Inhibitors; Humans; Ketoconazole; Longitudinal Studies; Male; Middle Aged; Ritonavir; Saquinavir

2000
The interaction of saquinavir (soft gelatin capsule) with ketoconazole, erythromycin and rifampicin: comparison of the effect in healthy volunteers and in HIV-infected patients.
    European journal of clinical pharmacology, 2001, Volume: 57, Issue:2

    Topics: Adult; Aged; Analysis of Variance; Anti-Bacterial Agents; Antifungal Agents; Area Under Curve; Biological Availability; Cross-Over Studies; Drug Administration Schedule; Drug Interactions; Erythromycin; Half-Life; HIV Infections; HIV Protease Inhibitors; Humans; Ketoconazole; Male; Middle Aged; Rifampin; Saquinavir

2001
Ketoconazole is inferior to ritonavir as an alternative booster for saquinavir in a once daily regimen in Thai HIV-1 infected patients.
    AIDS (London, England), 2007, Jul-31, Volume: 21, Issue:12

    Topics: Adult; Antiretroviral Therapy, Highly Active; CD4 Lymphocyte Count; Drug Administration Schedule; Female; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Ketoconazole; Male; Ritonavir; Saquinavir; Treatment Outcome; Viral Load

2007
Effects of CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers.
    British journal of clinical pharmacology, 2008, Volume: 65 Suppl 1

    Topics: Adolescent; Anti-HIV Agents; Antifungal Agents; Atazanavir Sulfate; CCR5 Receptor Antagonists; Cyclohexanes; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Drug Therapy, Combination; Female; HIV Infections; HIV Protease Inhibitors; Humans; Ketoconazole; Male; Maraviroc; Middle Aged; Oligopeptides; Pyridines; Saquinavir; Statistics as Topic; Triazoles

2008
Drug-drug interaction study of ketoconazole and ritonavir-boosted saquinavir.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:2

    Topics: Adult; Aged; Anti-HIV Agents; Antifungal Agents; Area Under Curve; Cross-Over Studies; Drug Interactions; Female; Half-Life; HIV Infections; HIV Protease Inhibitors; Humans; Ketoconazole; Male; Middle Aged; Ritonavir; Saquinavir; Young Adult

2009

Other Studies

26 other study(ies) available for ketoconazole and saquinavir

ArticleYear
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
    Bioorganic & medicinal chemistry letters, 2016, 08-15, Volume: 26, Issue:16

    Topics: Adenosine Triphosphate; Benzbromarone; Cell Line; Cell Survival; Chromans; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Humans; Pharmaceutical Preparations; Thiazolidinediones; Troglitazone

2016
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
    Drug metabolism and disposition: the biological fate of chemicals, 1999, Volume: 27, Issue:8

    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.
    Drug metabolism and disposition: the biological fate of chemicals, 2000, Volume: 28, Issue:6

    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
Rational use of in vitro P-glycoprotein assays in drug discovery.
    The Journal of pharmacology and experimental therapeutics, 2001, Volume: 299, Issue:2

    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
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
    Journal of medicinal chemistry, 2003, Apr-24, Volume: 46, Issue:9

    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
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
    Current drug discovery technologies, 2004, Volume: 1, Issue:4

    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
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
    Journal of medicinal chemistry, 2008, Jun-12, Volume: 51, Issue:11

    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
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
    Chemical research in toxicology, 2010, Volume: 23, Issue:1

    Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship

2010
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2010, Volume: 118, Issue:2

    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.
    Drug metabolism and disposition: the biological fate of chemicals, 2011, Volume: 39, Issue:2

    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
FDA-approved drug labeling for the study of drug-induced liver injury.
    Drug discovery today, 2011, Volume: 16, Issue:15-16

    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
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
    Journal of medicinal chemistry, 2012, May-24, Volume: 55, Issue:10

    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
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2013, Volume: 136, Issue:1

    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.
    Journal of medicinal chemistry, 2014, Apr-10, Volume: 57, Issue:7

    Topics: Animals; Brain; Dialysis; HEK293 Cells; High-Throughput Screening Assays; Humans; Pharmaceutical Preparations; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

2014
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
    Hepatology (Baltimore, Md.), 2014, Volume: 60, Issue:3

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Chemical and Drug Induced Liver Injury; Humans; Male; Mitochondria, Liver; Rats; Rats, Sprague-Dawley; Severity of Illness Index

2014
Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small-intestinal cytochrome P4503A4: potential contribution to high first-pass metabolism.
    Drug metabolism and disposition: the biological fate of chemicals, 1997, Volume: 25, Issue:2

    Topics: Anti-HIV Agents; Biotransformation; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Histamine H1 Antagonists; HIV Protease Inhibitors; Humans; Indinavir; Intestine, Small; Ketoconazole; Microsomes; Microsomes, Liver; Mixed Function Oxygenases; Oxidation-Reduction; Saquinavir; Terfenadine

1997
The effectiveness of combined saquinavir and ketoconazole treatment in reducing HIV viral load.
    Journal of the National Medical Association, 1998, Volume: 90, Issue:10

    Topics: Antifungal Agents; Drug Therapy, Combination; HIV Infections; HIV Protease Inhibitors; Humans; Ketoconazole; Saquinavir; Viral Load

1998
Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.
    British journal of clinical pharmacology, 1999, Volume: 48, Issue:4

    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
Ketoconazole may improve PI penetration.
    AIDS patient care and STDs, 1999, Volume: 13, Issue:12

    Topics: Blood-Brain Barrier; Drug Synergism; Drug Therapy, Combination; HIV Protease Inhibitors; Humans; Ketoconazole; Ritonavir; Saquinavir; Viral Load

1999
In vitro metabolism of trazodone by CYP3A: inhibition by ketoconazole and human immunodeficiency viral protease inhibitors.
    Biological psychiatry, 2000, Apr-01, Volume: 47, Issue:7

    Topics: Antidepressive Agents, Second-Generation; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; HIV Protease Inhibitors; Humans; In Vitro Techniques; Indinavir; Ketoconazole; Microsomes, Liver; Nelfinavir; Oxidoreductases, N-Demethylating; Piperazines; Ritonavir; Saquinavir; Selective Serotonin Reuptake Inhibitors; Serotonin Receptor Agonists; Trazodone

2000
Effect of ketoconazole on plasma concentrations of saquinavir.
    The Journal of antimicrobial chemotherapy, 2000, Volume: 46, Issue:1

    Topics: Adult; Drug Interactions; Humans; Ketoconazole; Male; Saquinavir

2000
CYP3A4-mediated hepatic metabolism of the HIV-1 protease inhibitor saquinavir in vitro.
    Xenobiotica; the fate of foreign compounds in biological systems, 2002, Volume: 32, Issue:1

    Topics: Adult; Biological Availability; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; DNA, Complementary; Enzyme Inhibitors; Female; Gene Expression; HIV Protease Inhibitors; Humans; In Vitro Techniques; Indinavir; Ketoconazole; Kinetics; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Microsomes, Liver; Mixed Function Oxygenases; Nelfinavir; Ritonavir; Saquinavir

2002
An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat.
    Pharmaceutical research, 2008, Volume: 25, Issue:5

    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
Maraviroc: in vitro assessment of drug-drug interaction potential.
    British journal of clinical pharmacology, 2008, Volume: 66, Issue:4

    Topics: Area Under Curve; Atazanavir Sulfate; Cyclohexanes; Cytochrome P-450 CYP3A; Drug Interactions; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Ketoconazole; Liver; Male; Maraviroc; Microsomes, Liver; Oligopeptides; Predictive Value of Tests; Pyridines; Ritonavir; Saquinavir; Triazoles

2008
A double transgenic mouse model expressing human pregnane X receptor and cytochrome P450 3A4.
    Drug metabolism and disposition: the biological fate of chemicals, 2008, Volume: 36, Issue:12

    Topics: Animals; Carbamates; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Female; Furans; Gene Expression; Gene Expression Regulation; HIV Protease Inhibitors; Humans; Intestine, Small; Ketoconazole; Liver; Male; Mice; Mice, Knockout; Mice, Transgenic; Microsomes, Liver; Models, Animal; Nelfinavir; Pregnane X Receptor; Pregnenolone Carbonitrile; Receptors, Steroid; Rifampin; Saquinavir; Sex Characteristics; Sulfonamides

2008
Clearance and clearance inhibition of the HIV-1 protease inhibitors ritonavir and saquinavir in sandwich-cultured rat hepatocytes and rat microsomes.
    Toxicology in vitro : an international journal published in association with BIBRA, 2009, Volume: 23, Issue:1

    Topics: Animals; Biological Transport, Active; Cell Culture Techniques; Cell Survival; Cells, Cultured; Cyclosporine; Cyclosporins; Dose-Response Relationship, Drug; Hepatocytes; HIV Protease Inhibitors; Ketoconazole; Male; Metabolic Clearance Rate; Microsomes, Liver; Rats; Rats, Wistar; Ritonavir; Saquinavir

2009