Page last updated: 2024-09-05

lapatinib and ketoconazole

lapatinib has been researched along with ketoconazole in 13 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(ketoconazole)
Trials
(ketoconazole)
Recent Studies (post-2010) (ketoconazole)
1,9193051,4426,2027061,269
1,9193051,4421490120

Protein Interaction Comparison

ProteinTaxonomylapatinib (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 (13)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (7.69)29.6817
2010's9 (69.23)24.3611
2020's3 (23.08)2.80

Authors

AuthorsStudies
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
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V1
Cantin, LD; Chen, H; Kenna, JG; Noeske, T; Stahl, S; Walker, CL; Warner, DJ1
Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Arya, N; Beelen, A; Bowen, CJ; Herendeen, JM; Koch, KM; Smith, DA1
Biller, BM; Tritos, NA1
Badolo, L; Jede, C; Koziolek, M; Kubas, H; Lecomte, M; Wagner, C; Weber, C; Weigandt, M; Weitschies, W1
Jones, LH; Nadanaciva, S; Rana, P; Will, Y1
Norman, BH1
Abdel-Maksoud, MS; Alach, NN; Anbar, HS; El-Gamal, MI; El-Gamal, R; Oh, CH; Sbenati, RM; Shehata, MK; Tarazi, H; Zaraei, SO1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1

Reviews

4 review(s) available for lapatinib 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
Advances in medical therapies for Cushing's syndrome.
    Discovery medicine, 2012, Volume: 13, Issue:69

    Topics: Animals; Bexarotene; Cushing Syndrome; Etomidate; Humans; Ketoconazole; Lapatinib; Metyrapone; Mifepristone; Mitotane; Quinazolines; Somatostatin; Tetrahydronaphthalenes

2012
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

Trials

1 trial(s) available for lapatinib and ketoconazole

ArticleYear
Effects of ketoconazole and carbamazepine on lapatinib pharmacokinetics in healthy subjects.
    British journal of clinical pharmacology, 2009, Volume: 67, Issue:4

    Topics: Adolescent; Adult; Analgesics, Non-Narcotic; Antifungal Agents; Antineoplastic Agents; Area Under Curve; Carbamazepine; Cross-Over Studies; Drug Interactions; Female; Half-Life; Humans; Ketoconazole; Lapatinib; Male; Middle Aged; Protein Kinase Inhibitors; Quinazolines; Treatment Outcome; Young Adult

2009

Other Studies

8 other study(ies) available for lapatinib and ketoconazole

ArticleYear
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
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
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:12

    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
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
Improved Prediction of in Vivo Supersaturation and Precipitation of Poorly Soluble Weakly Basic Drugs Using a Biorelevant Bicarbonate Buffer in a Gastrointestinal Transfer Model.
    Molecular pharmaceutics, 2019, 09-03, Volume: 16, Issue:9

    Topics: Administration, Oral; Animals; Bicarbonates; Buffers; Chemical Precipitation; Drug Delivery Systems; Drug Liberation; Female; Gastrointestinal Absorption; Gastrointestinal Tract; Hydrogen-Ion Concentration; Indazoles; Ketoconazole; Lapatinib; Methylcellulose; Models, Biological; Phosphates; Pyrimidines; Rats; Rats, Wistar; Solubility; Sulfonamides

2019
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
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
    European journal of medicinal chemistry, 2021, Nov-15, Volume: 224

    Topics: Binding Sites; Catalytic Domain; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Humans; Imidazoles; Molecular Docking Simulation; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Receptor, ErbB-4; Structure-Activity Relationship; Thiazoles

2021