Page last updated: 2024-09-04

abiraterone and ketoconazole

abiraterone has been researched along with ketoconazole in 26 studies

Compound Research Comparison

Studies
(abiraterone)
Trials
(abiraterone)
Recent Studies (post-2010)
(abiraterone)
Studies
(ketoconazole)
Trials
(ketoconazole)
Recent Studies (post-2010) (ketoconazole)
942978546,2027061,269
942978541490120

Protein Interaction Comparison

ProteinTaxonomyabiraterone (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 (26)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's2 (7.69)18.2507
2000's9 (34.62)29.6817
2010's14 (53.85)24.3611
2020's1 (3.85)2.80

Authors

AuthorsStudies
Barrie, SE; Jarman, M; Potter, GA; Rowlands, MG1
Brodie, AM; Chopra, P; Farquhar, R; Gediya, LK; Guo, Z; Handratta, VD; Kataria, R; Newman, D; Njar, VC; Qiu, Y; Vasaitis, TS1
Hansen, K; Hartmann, RW; Hille, UE; Jagusch, C; Müller-Vieira, U; Negri, M; Pinto-Bazurco Mendieta, MA; Schmidt, D1
Bartels, M; Cavalli, A; Hartmann, RW; Hille, UE; Hu, Q; Jagusch, C; Jahn-Hoffmann, K; Lauterbach, T; Müller-Vieira, U; Negri, M; Pinto-Bazurco Mendieta, MA; Recanatini, M; Rodenwaldt, B; Schmidt, D1
Hartmann, RW; Jagusch, C; Lauterbach, T; Müller-Vieira, U; Negri, M; Pinto-Bazurco Mendieta, MA1
Bartels, M; Hartmann, RW; Hu, Q; Jahn-Hoffmann, K; Lauterbach, T; Müller-Vieira, U; Negri, M; Olgen, S; Zhuang, Y1
Bartels, M; Hartmann, RW; Hille, UE; Hu, Q; Lauterbach, T; Müller-Vieira, U; Negri, M; Vock, C1
Hartmann, RW; Hille, UE; Hu, Q; Jagusch, C; Yin, L1
Hartmann, RW; Haupenthal, J; Hille, UE; Hu, Q; Jagusch, C1
Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ1
Frank, E; Kovács, D; Kovács, I; Szabó, N; Szécsi, M; Wölfling, J; Zupkó, I1
Brodie, AM; Njar, VC1
Frank, É; Kovács, D; Schelz, Z; Szabó, N; Szécsi, M; Wölfling, J; Zupkó, I1
Barrie, SE; Dowsett, M; Goddard, PM; Haynes, BP; Jarman, M; Potter, GA1
Hosaka, M; Takeda, M1
Ehmer, PB; Haidar, S; Hartmann, RW1
Ryan, CJ; Van Allen, EM1
Fong, L; Kantoff, P; Kheoh, T; Kim, J; Lee, G; Martins, V; Molina, A; Raynaud, F; Rosenberg, JE; Ryan, CJ; Small, EJ; Smith, MR1
Miller, K1
Kim, W; Ryan, CJ1
Alimohamed, N; Atenafu, EG; Joshua, AM; Knox, JJ; Leibowitz-Amit, R; Seah, JA; Sridhar, SS; Tannock, IF; Templeton, AJ; Vera-Badillo, FE1
Balk, SP; Bubley, GJ; Cai, C; Chen, EJ; Gao, S; Kantoff, PW; Lis, RL; Loda, M; Montgomery, RB; Nelson, PS; Schaefer, R; Sowalsky, AG; Taplin, ME; Troncoso, P; True, LD; Voznesensky, O; Ye, H1
Antonarakis, ES; Denmeade, SR; Luber, B; Teply, BA1
Abbott, DH; Bird, IM1
Chapman, JG; Guengerich, FP; McCarty, KD; Tateishi, Y1

Reviews

5 review(s) available for abiraterone and ketoconazole

ArticleYear
[Inhibitors of the key enzymes of androgen synthesis: potential agents as targets for prostate cancer].
    Nihon rinsho. Japanese journal of clinical medicine, 2000, Volume: 58 Suppl

    Topics: 17-Hydroxysteroid Dehydrogenases; Androgen Antagonists; Androstenes; Androstenols; Animals; Antineoplastic Agents, Hormonal; Carbazoles; Enzyme Inhibitors; Humans; Imidazoles; Ketoconazole; Male; Prostatic Neoplasms; Steroid 17-alpha-Hydroxylase; Testosterone

2000
Novel secondary hormonal therapy in advanced prostate cancer: an update.
    Current opinion in urology, 2009, Volume: 19, Issue:3

    Topics: Androgen Antagonists; Androstenes; Androstenols; Disease Progression; Humans; Ketoconazole; Male; Prostatic Neoplasms; Receptors, Androgen

2009
[Castration resistant prostate cancer 2011].
    Aktuelle Urologie, 2011, Volume: 42, Issue:2

    Topics: Androgen Antagonists; Androstenes; Androstenols; Antineoplastic Agents; Antineoplastic Agents, Hormonal; Biomarkers, Tumor; Bone Neoplasms; Cancer Vaccines; Clinical Trials as Topic; Docetaxel; Drug Resistance, Neoplasm; Humans; Ketoconazole; Male; Neoplasms, Hormone-Dependent; Orchiectomy; Prostate-Specific Antigen; Prostatic Neoplasms; Receptors, Androgen; Steroid 17-alpha-Hydroxylase; Taxoids; Tissue Extracts

2011
Androgen receptor directed therapies in castration-resistant metastatic prostate cancer.
    Current treatment options in oncology, 2012, Volume: 13, Issue:2

    Topics: Androgen Receptor Antagonists; Androstenes; Androstenols; Antineoplastic Agents; Antineoplastic Agents, Hormonal; Benzamides; Docetaxel; Drug Resistance, Neoplasm; Humans; Ketoconazole; Male; Nitriles; Orchiectomy; Phenylthiohydantoin; Prostatic Neoplasms; Receptors, Androgen; Steroid 17-alpha-Hydroxylase; Taxoids; Thiohydantoins

2012
The hunt for a selective 17,20 lyase inhibitor; learning lessons from nature.
    The Journal of steroid biochemistry and molecular biology, 2016, Volume: 163

    Topics: Adrenal Hyperplasia, Congenital; Androstadienes; Androstenes; Antineoplastic Agents; Benzimidazoles; Cytochrome P-450 CYP3A Inhibitors; Drug Therapy, Combination; Humans; Hydrocortisone; Imidazoles; Ketoconazole; Male; Naphthalenes; Prednisone; Prostate; Prostatic Neoplasms; Protective Factors; Steroid 17-alpha-Hydroxylase; Triazoles

2016

Trials

1 trial(s) available for abiraterone and ketoconazole

ArticleYear
Phase I clinical trial of the CYP17 inhibitor abiraterone acetate demonstrating clinical activity in patients with castration-resistant prostate cancer who received prior ketoconazole therapy.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2010, Mar-20, Volume: 28, Issue:9

    Topics: Aged; Aged, 80 and over; Androgen Antagonists; Androgens; Androstenes; Androstenols; Antineoplastic Agents; Dose-Response Relationship, Drug; Humans; Ketoconazole; Male; Middle Aged; Orchiectomy; Prostate-Specific Antigen; Prostatic Neoplasms; Steroid 17-alpha-Hydroxylase; Treatment Outcome

2010

Other Studies

20 other study(ies) available for abiraterone and ketoconazole

ArticleYear
Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.
    Journal of medicinal chemistry, 1995, Jun-23, Volume: 38, Issue:13

    Topics: Cytochrome P-450 Enzyme Inhibitors; Humans; Magnetic Resonance Spectroscopy; Male; Prostatic Neoplasms; Steroid 17-alpha-Hydroxylase; Steroids; Structure-Activity Relationship; Testis

1995
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
    Journal of medicinal chemistry, 2005, Apr-21, Volume: 48, Issue:8

    Topics: 5-alpha Reductase Inhibitors; Androgen Antagonists; Androstadienes; Animals; Antineoplastic Agents; Azoles; Benzimidazoles; Cell Line, Tumor; Cell Proliferation; Humans; Isoenzymes; Male; Mice; Mice, SCID; Mutation; Prostatic Neoplasms; Pyrazines; Radioligand Assay; Receptors, Androgen; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship; Tissue Distribution; Transcription, Genetic; Transcriptional Activation; Xenograft Model Antitumor Assays

2005
Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17.
    Bioorganic & medicinal chemistry letters, 2008, Jan-01, Volume: 18, Issue:1

    Topics: Biomimetic Materials; Enzyme Inhibitors; Heterocyclic Compounds; Humans; Liver; Models, Molecular; Naphthalenes; Progesterone; Steroid 17-alpha-Hydroxylase

2008
Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure.
    Bioorganic & medicinal chemistry, 2008, Feb-15, Volume: 16, Issue:4

    Topics: Binding Sites; Biological Availability; Enzyme Inhibitors; Heterocyclic Compounds; Humans; Imidazoles; Inhibitory Concentration 50; Liver; Models, Molecular; Polycyclic Aromatic Hydrocarbons; Steroid 17-alpha-Hydroxylase; Testosterone

2008
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.
    Journal of medicinal chemistry, 2008, Aug-28, Volume: 51, Issue:16

    Topics: Androstenes; Androstenols; Biphenyl Compounds; Enzyme Inhibitors; Humans; Male; Models, Molecular; Prostatic Neoplasms; Recombinant Proteins; Steroid 17-alpha-Hydroxylase

2008
Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge.
    Bioorganic & medicinal chemistry, 2008, Aug-15, Volume: 16, Issue:16

    Topics: Animals; Binding Sites; Biphenyl Compounds; Enzyme Inhibitors; Humans; Imidazoles; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Male; Models, Molecular; Protein Structure, Secondary; Rats; Spectrometry, Mass, Electrospray Ionization; Spectrophotometry, Infrared; Steroid 17-alpha-Hydroxylase; Testosterone

2008
Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls.
    European journal of medicinal chemistry, 2009, Volume: 44, Issue:7

    Topics: Biphenyl Compounds; Catalytic Domain; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Design; Enzyme Inhibitors; Humans; Models, Molecular; Steroid 11-beta-Hydroxylase; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship; Substrate Specificity

2009
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
    Journal of medicinal chemistry, 2010, Jul-08, Volume: 53, Issue:13

    Topics: Antineoplastic Agents, Hormonal; Biphenyl Compounds; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Male; Neoplasms, Hormone-Dependent; Prostatic Neoplasms; Pyridines; Spectrometry, Mass, Electrospray Ionization; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship; Substrate Specificity

2010
Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
    Journal of medicinal chemistry, 2010, Aug-12, Volume: 53, Issue:15

    Topics: Androgen Antagonists; Animals; Biphenyl Compounds; Cell Line; Cricetinae; Cricetulus; Humans; Imidazoles; In Vitro Techniques; Male; Microsomes; Prostatic Neoplasms; Pyridines; Steroid 11-beta-Hydroxylase; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship; Testis

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
An efficient approach to novel 17-5'-(1',2',4')-oxadiazolyl androstenes via the cyclodehydration of cytotoxic O-steroidacylamidoximes, and an evaluation of their inhibitory action on 17α-hydroxylase/C₁₇,₂₀-lyase.
    European journal of medicinal chemistry, 2013, Volume: 70

    Topics: Androstenes; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cyclization; Dehydration; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Inhibitors; HeLa Cells; Humans; Male; MCF-7 Cells; Molecular Conformation; Oximes; Rats; Rats, Wistar; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship; Testis

2013
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
    Journal of medicinal chemistry, 2015, Mar-12, Volume: 58, Issue:5

    Topics: Androgen Receptor Antagonists; Androstadienes; Benzimidazoles; Clinical Trials as Topic; Drug Discovery; Humans; Male; Molecular Structure; Molecular Targeted Therapy; Prostatic Neoplasms; Receptors, Androgen; Signal Transduction; Steroid 17-alpha-Hydroxylase; Tissue Distribution

2015
Synthesis of novel 17-(4'-formyl)pyrazolylandrosta-5,16-dienes and their derivatives as potent 17α-hydroxylase/C17,20-lyase inhibitors or antiproliferative agents depending on the substitution pattern of the heteroring.
    European journal of medicinal chemistry, 2016, Sep-14, Volume: 120

    Topics: Androstadienes; Animals; Antineoplastic Agents; Cell Proliferation; Enzyme Inhibitors; Female; Humans; Hydrazines; Lyases; Male; Pyrazoles; Rats; Steroid 17-alpha-Hydroxylase; Steroids; Structure-Activity Relationship

2016
Pharmacology of novel steroidal inhibitors of cytochrome P450(17) alpha (17 alpha-hydroxylase/C17-20 lyase).
    The Journal of steroid biochemistry and molecular biology, 1994, Volume: 50, Issue:5-6

    Topics: Abiraterone Acetate; Adrenal Glands; Aldehyde-Lyases; Androgens; Androstadienes; Androstenes; Androstenols; Animals; Cytochrome P-450 Enzyme Inhibitors; Flutamide; Guinea Pigs; Ketoconazole; Kidney; Luteinizing Hormone; Male; Mice; Orchiectomy; Organ Size; Prostate; Seminal Vesicles; Steroid 17-alpha-Hydroxylase; Testis; Testosterone

1994
Novel steroidal pyrimidyl inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase).
    Archiv der Pharmazie, 2001, Volume: 334, Issue:12

    Topics: Androstenes; Androstenols; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Ketoconazole; Male; Steroid 17-alpha-Hydroxylase; Structure-Activity Relationship

2001
Abiraterone acetate in metastatic castration-resistant prostate cancer: a retrospective review of the Princess Margaret experience of (I) low dose abiraterone and (II) prior ketoconazole.
    European journal of cancer (Oxford, England : 1990), 2014, Volume: 50, Issue:14

    Topics: Aged; Aged, 80 and over; Androstenes; Androstenols; Antineoplastic Combined Chemotherapy Protocols; Disease-Free Survival; Dose-Response Relationship, Drug; Humans; Ketoconazole; Male; Middle Aged; Neoplasm Metastasis; Prostatic Neoplasms, Castration-Resistant; Retrospective Studies; Treatment Outcome

2014
Abiraterone treatment in castration-resistant prostate cancer selects for progesterone responsive mutant androgen receptors.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2015, Mar-15, Volume: 21, Issue:6

    Topics: Aged; Aged, 80 and over; Androstenes; Antineoplastic Combined Chemotherapy Protocols; Cell Line, Tumor; DNA Helicases; DNA-Binding Proteins; Drug Resistance, Neoplasm; Dutasteride; Humans; Ketoconazole; Leuprolide; Male; Middle Aged; Mutation; Progesterone; Prostatic Neoplasms, Castration-Resistant; PTEN Phosphohydrolase; Receptors, Androgen; Steroid 17-alpha-Hydroxylase

2015
Singapore Cancer Network (SCAN) Guidelines for the Management of Advanced Castrate-Resistant Prostate Cancer.
    Annals of the Academy of Medicine, Singapore, 2015, Volume: 44, Issue:10

    Topics: Adenocarcinoma; Androgen Antagonists; Androstenes; Antineoplastic Agents; Benzamides; Cancer Vaccines; Docetaxel; Gonadotropin-Releasing Hormone; Humans; Ketoconazole; Male; Nitriles; Orchiectomy; Phenylthiohydantoin; Prostatic Neoplasms, Castration-Resistant; Radioisotopes; Radium; Singapore; Taxoids; Tissue Extracts

2015
The influence of prednisone on the efficacy of docetaxel in men with metastatic castration-resistant prostate cancer.
    Prostate cancer and prostatic diseases, 2016, Volume: 19, Issue:1

    Topics: Aged; Aged, 80 and over; Androstenes; Antineoplastic Combined Chemotherapy Protocols; Disease-Free Survival; Docetaxel; Humans; Ketoconazole; Male; Middle Aged; Neoplasm Metastasis; Prednisone; Proportional Hazards Models; Prostate-Specific Antigen; Prostatic Neoplasms, Castration-Resistant; Retrospective Studies; Taxoids; Treatment Outcome

2016
Stepwise binding of inhibitors to human cytochrome P450 17A1 and rapid kinetics of inhibition of androgen biosynthesis.
    The Journal of biological chemistry, 2021, Volume: 297, Issue:2

    Topics: Androgens; Androstenes; Antineoplastic Agents, Hormonal; Catalytic Domain; Cytochrome P-450 CYP3A; Enzyme Inhibitors; Humans; Imidazoles; Ketoconazole; Kinetics; Male; Naphthalenes; Pregnenolone; Progesterone; Prostatic Neoplasms; Steroid 17-alpha-Hydroxylase

2021