Compounds > gefitinib
Page last updated: 2024-09-03

gefitinib and ketoconazole

gefitinib has been researched along with ketoconazole in 12 studies

Compound Research Comparison

Studies
(gefitinib)		Trials
(gefitinib)		Recent Studies (post-2010)
(gefitinib)		Studies
(ketoconazole)		Trials
(ketoconazole)		Recent Studies (post-2010) (ketoconazole)
5,2315662,9196,2027061,269
5,2315662,9191490120

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)ketoconazole (IC50)
Solute carrier family 22 member 1 Homo sapiens (human)2.6
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrialHomo sapiens (human)0.34
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrialMus musculus (house mouse)0.36
Bile salt export pumpHomo sapiens (human)3.44
Steroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)1.5811
ATP-dependent translocase ABCB1Mus musculus (house mouse)6.7
ATP-dependent translocase ABCB1Homo sapiens (human)4.6771
Cytochrome P450 3A4Homo sapiens (human)0.2303
Steroid 21-hydroxylaseHomo sapiens (human)6.655
Cytochrome P450 2C8Homo sapiens (human)0.06
AromataseHomo sapiens (human)1.4111
Steroid 17-alpha-hydroxylase/17,20 lyase Rattus norvegicus (Norway rat)2.0802
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)5.425
Cholesterol side-chain cleavage enzyme, mitochondrial Rattus norvegicus (Norway rat)3.32
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)1.067
Cytochrome P450 2A2Rattus norvegicus (Norway rat)0.456
Cytochrome P450 11B1, mitochondrial Bos taurus (cattle)0.38
Cytochrome P450 11B1, mitochondrialHomo sapiens (human)0.4519
Translocator proteinRattus norvegicus (Norway rat)3.76
Cytochrome P450 7A1 Rattus norvegicus (Norway rat)1.2975
Cytochrome P450 11B2, mitochondrialHomo sapiens (human)0.5179
ATP-dependent translocase ABCB1Mus musculus (house mouse)3.8
Thromboxane-A synthase Homo sapiens (human)2.165
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)2
Sodium-dependent serotonin transporterHomo sapiens (human)0.531
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)0.0078
Cytochrome P450 4F2Homo sapiens (human)1.6
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)0.4144
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)1.9036
Lanosterol 14-alpha demethylaseHomo sapiens (human)0.19
Cytochrome P450 7A1Mus musculus (house mouse)1.2975
Lanosterol 14-alpha demethylase Rattus norvegicus (Norway rat)0.083
Epoxide hydrolase 1 Homo sapiens (human)0.04
Cytochrome P450 2D6Homo sapiens (human)2.774
Cytochrome P450 3A5Homo sapiens (human)0.2535
Bifunctional epoxide hydrolase 2Homo sapiens (human)0.04
Sterol 14-alpha demethylaseTrypanosoma cruzi strain CL Brener0.014

Research

Studies (12)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (16.67)29.6817
2010's9 (75.00)24.3611
2020's1 (8.33)2.80

Authors

AuthorsStudies
Artursson, P; Bergström, CA; Hoogstraate, J; Matsson, P; Norinder, U; Pedersen, JM1
Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A1
Ghosh, I; Manoharlal, R; Prakash, O; Prasad, R; Puri, N; Sharma, M1
Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ1
Ekins, S; Williams, AJ; Xu, JJ1
Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ1
Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Beijnen, JH; Rooswinkel, RW; Schinkel, AH; Sparidans, RW; van Herwaarden, AE; van Waterschoot, RA1
Hasegawa, T; Higashino, H; Kataoka, M; Masaoka, Y; Matsui, R; Sakuma, S; Yamamoto, M; Yamashita, S1
Jang, S; Jung, D; Lee, JW; Lee, S; Min, KH; Song, J1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1

Reviews

2 review(s) available for gefitinib and ketoconazole

ArticleYear
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
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

Other Studies

10 other study(ies) available for gefitinib and ketoconazole

ArticleYear
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
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
    European journal of medicinal chemistry, 2010, Volume: 45, Issue:11

    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.
    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
A predictive ligand-based Bayesian model for human drug-induced liver injury.
    Drug metabolism and disposition: the biological fate of chemicals, 2010, Volume: 38, Issue:12

    Topics: Bayes Theorem; Chemical and Drug Induced Liver Injury; Humans; Ligands

2010
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
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
Inhibition and stimulation of intestinal and hepatic CYP3A activity: studies in humanized CYP3A4 transgenic mice using triazolam.
    Drug metabolism and disposition: the biological fate of chemicals, 2009, Volume: 37, Issue:12

    Topics: Administration, Oral; Animals; Antineoplastic Agents; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Activators; Enzyme Inhibitors; Gefitinib; Humans; Hydroxylation; Intestines; Ketoconazole; Liver; Male; Mice; Mice, Knockout; Mice, Transgenic; Microsomes; Quinazolines; Species Specificity; Substrate Specificity; Triazolam

2009
In vitro-in vivo correlation of the effect of supersaturation on the intestinal absorption of BCS Class 2 drugs.
    Molecular pharmaceutics, 2014, Mar-03, Volume: 11, Issue:3

    Topics: Administration, Oral; Albendazole; Animals; Antineoplastic Agents; Calorimetry, Differential Scanning; Cytochrome P-450 CYP3A Inhibitors; Dipyridamole; Drug Stability; Gefitinib; In Vitro Techniques; Intestinal Absorption; Ketoconazole; Male; Quinazolines; Rats; Rats, Sprague-Dawley; Solubility; Solvents; Tubulin Modulators; Vasodilator Agents

2014
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.
    Bioorganic & medicinal chemistry letters, 2019, 02-01, Volume: 29, Issue:3

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cell Survival; Click Chemistry; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Structure; Mutation; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship

2019